| Sonstiges: |
- Nachgewiesen in: USPTO Patent Applications
- Sprachen: English
- Document Number: 20120270881
- Publication Date: October 25, 2012
- Appl. No: 13/508531
- Application Filed: August 03, 2010
- Assignees: POLYPHOR AG (Allschwil, CH)
- Claim: 1. Compounds consisting of a cyclic arrangement of the building blocks A, B and C and represented by the general formulae Ia or Ib [chemical expression included] wherein building block A (“Template”) is represented by [chemical expression included] building block B (“Modulator”) is represented by [chemical expression included] building block C (“Bridge”) is represented by [chemical expression included] respectively [chemical expression included] and wherein M represents a divalent or trivalent radical selected from the group of [chemical expression included] forming an integral part of the M-L connectivity which in turn represents a divalent radical selected from the group of [chemical expression included] U represents a divalent radical selected from the group of [chemical expression included] X represents a divalent radical selected from the group of [chemical expression included] V and W are independently representing a divalent radical selected from the group of [chemical expression included] and wherein said building block A is a bivalent radical selected from the group of [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] building block B is a bivalent radical selected from the group of [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] building block C is a bivalent radical selected from the group of [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] and wherein further R1 is H; F; Cl; Br; I; CF3; OCF3; OCHF2; NO2; CN; alkyl; alkenyl; alkynyl; cycloalkyl; heterocycloalkyl; aryl; heteroaryl; aryl alkyl; heteroarylalkyl; —(CR18R19)qOR20; —(CR18R19)qSR20; —(CR18R19)qNR4R11; —(CR18R19)qOCONR4R11; —(CR18R19)qOCOOR21; —(CR18R19)qNR4COOR21; —(CR18R19)qNR4COR22; —(CR18R19)qNR4CONR4R11; —(CR18R19)qNR4SO2R23; —(CR18R19)qNR4SO2NR4R11; —(CR18R19)qCOOR21; —(CR18R19)qCONR4R11; —(CR18R19)qSO2NR4R11; —(CR18R19)qPO(OR21)2; —(CR18R19)qOPO(OR21)2; —(CR18R19)qCOR22; —(CR18R19)qSO2R23; —(CR18R19)qOSO3R21; —(CR18R19)qR24; —(CR18R19)qR25; or —(CR18R19)qR26; R2 is H; CF3; alkyl; alkenyl; cycloalkyl; heterocycloalkyl; aryl; heteroaryl; arylalkyl; heteroarylalkyl; —(CR18R19)qOR20; —(CR18R19)qSR20; —(CR18R19)qNR4R11; —(CR18R19)qOCONR4R11; —(CR18R19)qOCOOR21; —(CR18R19)qNR4COOR21; —(CR18R19)qNR4COR22; —(CR18R19)qNR4CONR4R11; —(CR18R19)qNR4SO2R23; —(CR18R19)qNR4SO2NR4R11; —(CR18R19)qCOOR21; —(CR18R19)qCONR4R11; —(CR18R19)qSO2NR4R11; —(CR18R19)qPO(OR21)2; —(CR18R19)qCOR22; —(CR18R19)qSO2R23; —(CR18R19)qR24; —(CR18R19)qR25; or —(CR18R19)qR26; R3 is H; CF3; alkyl; cycloalkyl; heterocycloalkyl; aryl; heteroaryl; arylalkyl; or heteroarylalkyl; R4 is H; alkyl; alkenyl; cycloalkyl; heterocycloalkyl; aryl; heteroaryl; arylalkyl; heteroarylalkyl; or a suitable N-protecting group; R5, R7 and R9 are independently defined as is H; F; CF3; alkyl; alkenyl; cycloalkyl; heterocycloalkyl; aryl; heteroaryl; arylalkyl; heteroarylalkyl; —(CR18R19)qOR20; —(CR18R19)qSR20; —(CR18R19)qNR4R11; —(CR18R19)qOCONR4R11; —(CR18R19)qOCOOR21; —(CR18R19)qNR4COOR21; —(CR18R19)qNR4COR22; —(CR18R19)qNR4CONR4R11; —(CR18R19)qNR4SO2R23; —(CR18R19)qNR4SO2NR4R11; —(CR18R19)qCOOR21; —(CR18R19)qCONR4R11; —(CR18R19)qSO2NR4R11; —(CR18R19)qPO(OR21)2; —(CR18R19)qCOR22; —(CR18R19)qSO2R23; —(CR18R19)qR24; —(CR18R19)qR25; or —(CR18R19)qR26; R6, R8 and R10 are independently defined as H; F; CF3; alkyl; alkenyl; cycloalkyl; heterocycloalkyl; aryl; heteroaryl; arylalkyl; or heteroarylalkyl; R11 is H; alkyl; alkenyl; cycloalkyl; heterocycloalkyl; aryl; heteroaryl; arylalkyl; heteroarylalkyl; a suitable protecting group; —(CR18R19)rOR20; —(CR18R19)rSR20; —(CR18R19)rNR4R27; —(CR18R19)rOCONR4R27; —(CR18R19)rOCOOR21; —(CR18R19)rNR4COOR21; —(CR18R19)rNR4CONR4R27; —(CR18R19)rNR4SO2R23; —(CR18R19)rNR4SO2NR4R27; —(CR18R19)qCOOR21; —(CR18R19)qCONR4R27; —(CR18R19)qCOR22; —(CR18R19)qSO2R23; —(CR18R19)qSO2NR4R27; —(CR18R19)qR24; —(CR18R19)sR25; —(CR18R19)qR26; or —(CR18R19)qR31; R12 and R13 are independently defined as H; or alkyl; R14 and R16 are independently defined as H; F; CF3; alkyl; alkenyl; cycloalkyl; heterocycloalkyl; aryl; heteroaryl; arylalkyl; heteroarylalkyl; —(CR18R19)qOR20; —(CR18R19)qNR4R11; —(CR18R19)qNR4COOR21; —(CR18R19)qNR4COR22; —(CR18R19)qNR4CONR4R11; —(CR18R19)qNR4SO2R23; —(CR18R19)qNR4SO2NR4R11; —(CR18R19)qCOOR21; —(CR18R19)qCONR4R11; —(CR18R19)qSO2NR4R11; or —(CR18R19)qCOR22; R15 and R17 are independently defined as H; F; CF3; alkyl; alkenyl; cycloalkyl; heterocycloalkyl; aryl; heteroaryl; arylalkyl; or heteroarylalkyl; R18 is H; F; CF3; alkyl; alkenyl; cycloalkyl; heterocycloalkyl; aryl; heteroaryl; arylalkyl; heteroarylalkyl; —(CR29R30)sOR31; —(CR29R30)sSR31; —(CR29R30)sNR28R31; —(CR29R30)sOCONR28R31; —(CR29R30)sOCOOR21; —(CR29R30)sNR28COOR21; —(CR29R30)sNR28SO2NR28R31; —(CR29R30)qCOOR21; —(CR29R30)qCONR28R31; —(CR29R30)qSO2NR28R31; —(CR29R30)qPO(OR21)2; —(CR29R30)qCOR31; —(CR29R30)qSO2R23; —(CR29R30)qR24; —(CR29R30)qR25; or —(CR29R30)qR26; R19 is H; CF3; alkyl; alkenyl; cycloalkyl; heterocycloalkyl; aryl; heteroaryl; arylalkyl; or heteroarylalkyl; R20 is H; alkyl; alkenyl; cycloalkyl; heterocycloalkyl; aryl; heteroaryl; arylalkyl; heteroarylalkyl; —(CR29R30)rOR31; —(CR29R30)rSR31; —(CR29R30)rNR28R31; —(CR29R30)rOCONR28R31; —(CR29R30)rNR28COOR21; —(CR29R30)rNR28COR31; —(CR29R30)rNR28CONR28R31; —(CR29R30)rNR28SO2R23; —(CR29R30)rNR28SO2NR28R31; —(CR29R30)qCOOR21; —(CR29R30)qCONR28R31; —(CR29R30)qSO2NR28R31; —(CR29R30)qCOR31; —(CR29R30)qSO2R23; —(CR29R30)qR24; —(CR29R30)qR25; —(CR29R30)qR26; or —(CR29R30)qR31; R21 is H; alkyl; alkenyl; cycloalkyl; heterocycloalkyl; aryl; heteroaryl; arylalkyl; heteroarylalkyl; or a suitable O-protecting group; R22 is alkyl; alkenyl; cycloalkyl; heterocycloalkyl; aryl; heteroaryl; arylalkyl; heteroarylalkyl; —(CR29R30)sOR31; —(CR29R30)sSR31; —(CR29R30)sNR28R31; —(CR29R30)sOCONR28R31; —(CR29R30)sNR28COOR21; —(CR29R30)sNR28COR31; —(CR29R30)sNR28CONR28R31; —(CR29R30)sNR28SO2R23; —(CR29R30)sNR28SO2NR28R31; —(CR29R30)sCOOR21; —(CR29R30)sCONR28R31; —(CR29R30)sSO2NR28R31; —(CR29R30)tCOR31; —(CR29R30)sSO2R23; —(CR29R30)tR24; —(CR29R30)tR25; —(CR29R30)tR26; or —(CR29R30)tR31; R23 is H; alkyl; alkenyl; cycloalkyl; heterocycloalkyl; aryl; heteroaryl; arylalkyl; heteroarylalkyl; or —(CR32R33)tR24; R24 is aryl; heteroaryl; —C6H2R34R35R31; or a group of one of the formulae [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] R25 is a group of one of the formulae [chemical expression included] R26 is a group of one of the formulae [chemical expression included] R27 is H; alkyl; lower alkenyl; cycloalkyl; heterocycloalkyl; aryl; heteroaryl; lower arylalkyl; lower heteroarylalkyl; a suitable protecting group; or —(CR29R30)qR24; R28 is H; alkyl; lower alkenyl; cycloalkyl; heterocycloalkyl; aryl; heteroaryl; lower arylalkyl; lower heteroarylalkyl; a suitable N-protecting group; —(CR32R33)sOR21; —(CR32R33)sNR43R42; —(CR32R33)sNR42CONR43R42; —(CR32R33)sNR42COR21; —(CR32R33)sNR42SO2NR21; —(CR32R33)qCOOR21; —(CR32R33)qCOR23; or —(CR32R33)qSO2R21; R29 is H; F; CF3; alkyl; alkenyl; cycloalkyl; heterocycloalkyl; aryl; heteroaryl; arylalkyl; heteroarylalkyl; —(CR32R33)sOR31; —(CR32R33)sSR31; —(CR32R33)sNR28R31; —(CR32R33)sOCONR28R31; —(CR32R33)sOCOOR21; —(CR32R33)sNR28COOR21; —(CR32R33)sNR28COR31; —(CR32R33)sNR28CONR28R31; —(CR32R33)sNR28SO2R23; —(CR32R33)sNR28SO2NR28R31; —(CR32R33)qCOOR21; —(CR32R33)qCONR28R31; —(CR32R33)qSO2NR28R31; —(CR32R33)qPO(OR21)2; —(CR32R33)qCOR31; —(CR32R33)qSO2R23; or —(CR32R33)qR31; R30 is H; F; CF3; alkyl; alkenyl; cycloalkyl; heterocycloalkyl; aryl; heteroaryl; arylalkyl; or heteroarylalkyl; R31 is H; alkyl; alkenyl; cycloalkyl; heterocycloalkyl; aryl; heteroaryl; arylalkyl; heteroarylalkyl; or a group of one of the formulae [chemical expression included] R32 and R33 are independently defined as H; F; CF3; alkyl; alkenyl; cycloalkyl; heterocycloalkyl; aryl; heteroaryl; arylalkyl; or heteroarylalkyl; R34 and R35 are independently defined as H; F; Cl; CF3; OCF3; OCHF2; NO2; CN; alkyl; alkenyl; alkynyl; cycloalkyl; heterocycloalkyl; aryl; heteroaryl; arylalkyl; heteroarylalkyl; —(CR29R30)qOR31; —(CR29R30)qSR31; —(CR29R30)qNR28R31; —(CR29R30)qOCONR28R31; —(CR29R30)qNR28COOR21; —(CR29R30)qNR28COR31; —(CR29R30)qNR28CONR28R31; —(CR29R30)qNR28SO2R23; —(CR29R30)qNR28SO2NR28R31; —(CR29R30)qCOOR21; —(CR29R30)qCONR28R31; —(CR29R30)qSO2NR28R31; —(CR29R30)qCOR31; —(CR29R30)qSO2R23; or —(CR29R30)qR31; R36 is H; alkyl; alkenyl; alkynyl; cycloalkyl; heterocycloalkyl; aryl; heteroaryl; arylalkyl; heteroarylalkyl; or —NR28R31; R37 is H; alkyl; alkenyl; cycloalkyl; heterocycloalkyl; aryl; heteroaryl; arylalkyl; heteroarylalkyl; a suitable N-protecting group; —(CR29R30)rOR31; —(CR29R30)rSR31; —(CR29R30)rNR28R31; —(CR29R30)rOCONR28R31; —(CR29R30)rNR28COOR21; —(CR29R30)rNR28COR31; —(CR29R30)rNR28CONR28R31; —(CR29R30)rNR28SO2R23; —(CR29R30)rNR28SO2NR28R31; —(CR29R30)qCOOR21; —(CR29R30)qCONR28R31; —(CR29R30)rSO2NR28R31; —(CR29R30)qCOR31; —(CR29R30)rSO2R23; or —(CR29R30)qR31; R38 is H; alkyl; alkenyl; cycloalkyl; heterocycloalkyl; aryl; heteroaryl; arylalkyl; heteroarylalkyl; —(CR29R30)qOR31; —(CR29R30)qSR31; —(CR29R30)qNR28R31; —(CR29R30)qNR28COOR21; —(CR29R30)qNR28COR31; —(CR29R30)qNR28CONR28R31; —(CR29R30)qCOOR21; —(CR29R30)qCONR28R31; —(CR29R30)qCOR31; or —(CR29R30)qR31; R39 is H; F; CF3; alkyl; alkenyl; cycloalkyl; heterocycloalkyl; aryl; heteroaryl; arylalkyl; heteroarylalkyl; —(CR32R33)uOR21; —(CR32R33)uNR28R43; —(CR32R33)tCOOR21; or —(CR32R33)tCONR28R43; R40 is H; F; CF3; alkyl; alkenyl; cycloalkyl; heterocycloalkyl; aryl; heteroaryl; arylalkyl; heteroarylalkyl; —(CR32R33)uOR21; —(CR32R33)uNR28R43; —(CR32R33)tCOOR21; or —(CR32R33)tCONR28R43; R41 is H; CF3; alkyl; alkenyl; cycloalkyl; heterocycloalkyl; aryl; heteroaryl; arylalkyl; heteroarylalkyl; —OR21; —NR28R43; —NR28COR23; —NR28COOR21; —NR28SO2R23; —NR28CONR28R43; —COOR21; —CONR28R43; —C(═NR43)NR28R43; —NR28C(═NR43)NR28R43; or a group of one of the formulae [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] [chemical expression included] R42 is H; alkyl; alkenyl; cycloalkyl; cycloheteroalkyl; aryl; heteroaryl; —(CR23R33)sOR21; —(CR23R33)sNR4R43; —(CR23R33)qCOOR21; or —(CR23R33)qCONR4R43; R43 is H; alkyl; alkenyl; cycloalkyl; heterocycloalkyl; aryl; heteroaryl; arylalkyl; heteroarylalkyl; or a suitable N-protecting group; R44, R45 and R46 are independently defined as H; F; CF3; OCF3; OCHF2; NO2; CN; alkyl; alkenyl; alkynyl; cycloalkyl; heterocycloalkyl; aryl; heteroaryl; arylalkyl; heteroarylalkyl; —OR23; —NR28R43; —NR28COR23; —NR28SO2R23; NR28SO2R23; —NR28CONR28R43; —COR23; or —SO2R23; R47 is H; CF3; alkyl; alkenyl; alkynyl; cycloalkyl; heterocycloalkyl; aryl; heteroaryl; arylalkyl; heteroarylalkyl; —COOR21; or —CONR28R43; R48 is H; F; CF3; alkyl; alkenyl; cycloalkyl; cycloheteroalkyl; aryl; heteroaryl; —(CR23R33)tOR21; —(CR23R33)tNR28R43; —(CR23R33)tCOOR21; or —(CR23R33)tCONR21R43; R49 and R50 are independently defined as H; F; CF3; alkyl; alkenyl; cycloalkyl; heterocycloalkyl; aryl; heteroaryl; arylalkyl; heteroarylalkyl; —(CR32R33)qOR21; —(CR32R33)qNR28R43; —(CR32R33)qCOOR21; or —(CR32R33)qCONR28R43; R51 is H; F; Cl; CF3; OCF3; or lower alkyl; R52 is H; F; Cl; CF3; OCF3; OCHF2; NO2; CN; lower alkyl; lower alkenyl; lower alkynyl; lower cycloalkyl; lower heterocycloalkyl; aryl; heteroaryl; lower arylalkyl; or lower heteroarylalkyl; R53 is CF3; OCF3; CN; lower alkyl; lower cycloalkyl; aryl; lower alkoxy; or aryloxy; taken together (R4 and R11); (R4 and R27); (R5 and R6); (R5 and R7); (R5 and R9); (R5 and R14); (R5 and R16); (R7 and R8); (R7 and R9); (R7 and R16); (R9 and R10); (R14 and R15); (R16 and R17); (R18 and R19); (R27 and R28); (R28 and R31); (R28 and R43); (R29 and R30); (R32 and R33); (R34 and R35); (R37 and R38); (R39 and R40); (R39 and R41); (R39 and R49); (R42 and R43); (R44 and R45); or (R44 and R46) can form optionally substituted cycloalkyl or heterocycloalkyl moieties; in addition, the structural elements —NR4R11; —NR11R27; —NR27R28; —NR28R31 or —NR28R43 can form one of the groups of the formulae [chemical expression included] Z is O; S; S(═O); S(═O)2; or NR28; Y is O; S; or NR4; Q is O; S; or NR28; T is CR46 or N; in case T occurs several times in the same ring structure each T is defined independently of the other; q is an integer of 0-4; r is an integer of 2-4; s is an integer of 1-4; t is an integer of 0-2; u is an integer of 1-2; and all possible stereoisomers of such compounds; or salts, solvates, clathrates, N-oxides, isotopically enriched or enantiomerically enriched versions thereof.
- Claim: 2. Compounds according to claim 1 wherein the building block of type A is selected from A1 to A626; the building block of type B is selected from B1 to B21; the building block of type C is selected from C1 to C101; and wherein M is —N(R4)—; and all possible stereoisomers of such compounds; or pharmaceutical acceptable salts thereof.
- Claim: 3. Compounds according to claim 1 or 2 wherein the building block of type A is selected from A1(a1); A2(a1); A3(a1); A4(a1); A5(a1); A6(a1); A7(a1); A9(a1); A10(a1); A73(a2); A80(a2); A170(a4); A171(a4); A209(a7); A210(a7); A240(a10); A241(a10); A242(a10); A243(a10); A272(a10); A530(a18); A531(a18); A532(a18); A533(a18); A609(a24); A610(a24); A611(a24); A612(a24); A613(a24); A614(a24); A615(a24); A631(a1); A632(a1); A633(a1); A641(a1); A642(a1); A643(a1); A651(a1); A652(a1); or A653(a1); the building block of type B is selected from B4(b3); B5(b3); B6(b3); B7(b3); B8(b3); B9(b3); B10(b3); B12(b4); B13(b4); B14(b4); B15(b4); B16(b4) or B17(b5); the building block of type C is selected from C1; C2; C3; C4; C5; C6; C7; C8; C9; C10; C11; C12; C13; C14; C15; C16; C17; C18; C19; C20; C21; C25; C26; C27; C28; C29; C30; C34; C35; C36; C37; C38; C39; C43; C44; C45; C46; C47; C48; C49; C50; C51; C52; C53; C54; C55; C56; C57; C58; C59; C60; C61; C62; C63; C64; C65; C66; C67; C68; C69; C70; C71; C72; C73; C74; C75; C76; C77; C78; C79; C80; C81; C86; C87; C88; C89; C90; C91; C92; or C93; and wherein R1 is H; F; Cl; Br; I; CF3; OCF3; OCHF2; NO2; CN; lower alkyl; lower alkenyl; lower alkynyl; lower cycloalkyl; lower heterocycloalkyl; aryl; heteroaryl; lower arylalkyl; lower heteroarylalkyl; —(CR18R19)qOR20; —(CR18R19)qNR4R11; —(CR18R19)qNR4COOR21; —(CR18R19)qNR4COR22; —(CR18R19)qNR4CONR4R11; —(CR18R19)qNR4SO2R23; —(CR18R19)qNR4SO2NR4R11; —(CR18R19)qCOOR21; —(CR18R19)qCONR4R11; —(CR18R19)qSO9NR4R11; —(CR18R19)qPO(OR21)2; —(CR18R19)qCOR22; —(CR18R19)qSO2R23; —(CR18R19)qOSO3R21; —(CR18R19)qR24; —(CR18R19)qR25; or —(CR18R19)qR26; R2 is H; CF3; lower alkyl; lower alkenyl; cycloalkyl; heterocycloalkyl; aryl; heteroaryl; lower arylalkyl; lower heteroarylalkyl; —(CR18R19)qOR20; —(CR18R19)qNR4R11; —(CR18R19)qNR4COOR21; —(CR18R19)qNR4COR22; —(CR18R19)qNR4CONR4R11; —(CR18R19)q(NR4SO2R23; —(CR18R19)qNR4SO2NR4R11; —(CR18R19)qCOOR21; —(CR18R19)qCONR4R11; —(CR18R19)qSO2NR4R11; —(CR18R19)qPO(OR21)2; —(CR18R19)qCOR22; —(CR18R19)qSO2R23; —(CR18R19)qR24; —(CR18R19)qR25; or —(CR18R19)qR26; R4 is H; lower alkyl; lower alkenyl; lower cycloalkyl; lower heterocycloalkyl; or a suitable N-protecting group; R5, R7 and R9 are independently defined as H; F; CF3; lower alkyl; lower alkenyl; lower cycloalkyl; lower heterocycloalkyl; aryl; heteroaryl; lower arylalkyl; lower heteroarylalkyl; —(CR18R19)qOR20; —(CR18R19)qNR4R11; —(CR18R19)qNR4COOR21; —(CR18R19)qNR4COR22; —(CR18R19)qNR4CONR4R11; —(CR18R19)qNR4SO2R23; —(CR18R19)qNR4SO2NR4R11; —(CR18R19)qCOOR21; —(CR18R19)qCONR4R11; —(CR18R19)qSO2NR4R11; —(CR18R19)qPO(OR21)2; —(CR18R19)qCOR22; —(CR18R19)qSO2R23; —(CR18R19)qR24; —(CR18R19)qR25; or —(CR18R19)qR26; R6, R8 and R10 are independently defined as H; CF3; or lower alkyl; R11 is H; alkyl; alkenyl; cycloalkyl; lower heterocycloalkyl; aryl; heteroaryl; lower arylalkyl; lower heteroarylalkyl; a suitable protecting group; —(CR18R19)rOR20; —(CR18R19)rNR4R27; —(CR18R19)rNR4COOR21; —(CR18R19)rNR4CONR4R27; —(CR18R19)rNR4SO2R23; —(CR18R19)rNR4SO2NR4R27; —(CR18R19)qCOOR21; —(CR18R19)qCONR4R27; —(CR18R19)qCOR22; —(CR18R19)qSO2R23; —(CR18R19)qSO2NR4R27; —(CR18R19)qR24; —(CR18R19)sR25; —(CR18R19)qR26; or —(CR18R19)qR31; R12 and R13 are independently defined as H; or lower alkyl; R14 and R16 are independently defined as H; F; CF3; lower alkyl; lower alkenyl; lower cycloalkyl; lower heterocycloalkyl; aryl; heteroaryl; lower arylalkyl; lower heteroarylalkyl; —(CR18R19)qOR20; —(CR18R19)qNR4R11; —(CR18R19)qNR4COOR21; —(CR18R19)qNR4COR22; —(CR18R19)qNR4CONR4R11; —(CR18R19)qNR4SO2R23; —(CR18R19)qCOOR21; —(CR18R19)qCONR4R11; or —(CR18R19)qCOR22; R15 and R17 are independently defined as H; CF3; or lower alkyl; R18 is H; F; CF3; lower alkyl; lower alkenyl; lower cycloalkyl; lower heterocycloalkyl; aryl; heteroaryl; lower arylalkyl; lower heteroarylalkyl; —(CR29R30)sOR31; —(CR29R30)sNR28R31; —(CR29R30)sNR28COOR21; —(CR29R30)sNR28COR31; —(CR29R30)sNR28CONR28R31; —(CR29R30)sNR28SO2R23; —(CR29R30)sNR28SO2NR28R31; —(CR29R30)qCOOR21; —(CR29R30)qCONR28R31; —(CR29R30)qSO2NR28R31; —(CR29R30)qPO(OR21)2; —(CR29R30)qCOR31; —(CR29R30)qSO2R23; —(CR29R30)qR24; —(CR29R30)qR25; or —(CR29R30)qR26; R19 is H; CF3; or lower alkyl; R20 is H; lower alkyl; lower alkenyl; lower cycloalkyl; lower heterocycloalkyl; aryl; heteroaryl; lower arylalkyl; lower heteroarylalkyl; —(CR29R30)rOR31; —(CR29R30)rNR28R31; —(CR29R30)rNR28COOR21; —(CR29R30)rNR28COR31; —(CR29R30)rNR28CONR28R31; —(CR29R30)rNR28SO2R23; —(CR29R30)qCOOR21; —(CR29R30)qCONR28R31; —(CR29R30)qSO2NR28R31; —(CR29R30)qCOR31; —(CR29R30)qSO2R23; —(CR29R30)qR24; —(CR29R30)qR25; —(CR29R30)qR26; or —(CR29R30)qR31; R22 is lower alkyl; lower alkenyl; lower cycloalkyl; lower heterocycloalkyl; aryl; heteroaryl; lower arylalkyl; lower heteroarylalkyl; —(CR29R30)sOR31; —(CR29R30)sNR28R31; —(CR29R30)sNR28COOR21; —(CR29R30)sNR28COR31; —(CR29R30)sNR28CONR28R31; —(CR29R30)sNR28SO2R23; —(CR29R30)sCOOR21; —(CR29R30)sCONR28R31; —(CR29R30)sSO2NR28R31; —(CR29R30)tCOR31; —(CR29R30)sSO2R23; —(CR29R30)tR24; —(CR29R30)tR25; —(CR29R30)tR26; or —(CR29R30)tR31; R29 is H; F; CF3; lower alkyl; lower alkenyl; lower cycloalkyl; lower heterocycloalkyl; aryl; heteroaryl; lower arylalkyl; lower heteroarylalkyl; —(CR32R33)sOR31; —(CR32R33)sNR28R31; —(CR32R33)sNR28COOR21; —(CR32R33)sNR28COR31; —(CR32R33)sNR28CONR28R31; —(CR32R33)sNR28SO2R23; —(CR32R33)qCOOR21; —(CR32R33)qCONR28R31; —(CR32R33)qSO2NR28R31; —(CR32R33)qPO(OR21)2; —(CR32R33)qCOR31; —(CR32R33)qSO2R23; or —(CR32R33)qR31; R30 and R33 are independently defined as H; CF3; or lower alkyl; R34 and R35 are independently defined as H; F; Cl; CF3; OCF3; OCHF2; NO2; CN; lower alkyl; lower alkenyl; lower alkynyl; lower cycloalkyl; lower heterocycloalkyl; aryl; heteroaryl; lower arylalkyl; lower heteroarylalkyl; —(CR29R30)qOR31; —(CR29R30)qNR28R31; (CR29R30)qNR28COOR21; —(CR29R30)qNR28COR31; (CR29R30)qNR28CONR28R31; —(CR29R30)qNR28SO2R23; —(CR29R30)qCOOR21; —(CR29R30)qCONR28R31; —(CR29R30)qSO2NR28R31; —(CR29R30)qCOR31; —(CR29R30)qSO2R23; or —(CR29R30)qR31; R37 is H; lower alkyl; lower alkenyl; lower cycloalkyl; lower heterocycloalkyl; aryl; heteroaryl; lower arylalkyl; lower heteroarylalkyl; a suitable N-protecting group; —(CR29R30)rOR31; —(CR29R30)rNR28R31; —(CR29R30)rNR28COOR21; —(CR29R30)rNR28COR31; —(CR29R30)rNR28CONR28R31; —(CR29R30)rNR28SO2R23; —(CR29R30)qCOOR21; —(CR29R30)qCONR28R31; —(CR29R30)rSO2NR28R31; —(CR29R30)qCOR31; —(CR29R30)qSO2R23; or —(CR29R30)qR31; R38 is H; lower alkyl; lower alkenyl; lower cycloalkyl; lower heterocycloalkyl; aryl; heteroaryl; lower arylalkyl; lower heteroarylalkyl; —(CR29R30)qOR31; —(CR29R30)qNR28R31; —(CR29R30)qNR28COOR21; —(CR29R30)qNR28COR31; —(CR29R30)qNR28CONR28R31; —(CR29R30)qCOOR21; —(CR29R30)qCONR28R31; —(CR29R30)qCOR31; or —(CR29R30)R31; Z is O; S; S(═O); or S(═O)2; U is —C(═O)—; —NR4—C(═O)—; —C(═O)—C(═O)—; or —C(—OR20)2—C(═O)—.
- Claim: 4. Compounds according to claim 1 or 2 wherein the building block of type A is selected from A1(a1); A2(a1); A3(a1); A4(a1); A5(a1); A6(a1); A7(a1); A9(a1); A10(a1); A73(a2); A170(a4); A209(a7); A240(a10); A272(a10); A532(a18); A614(a24); A631(a1); A632(a1); A633(a1); A641(a1); A642(a1); A643(a1); A651(a1); A652(a1); or A653(a1); the building block of type B is selected from B7(b3); B8(b3); B9(b3); B10(b3); or B17(b5); the building block of type C is selected from C1; C2; C4; C7; C8; C9; C10; C11; C12; C13; C14; C15; C16; C17; C18; C19; C20; C21; C25; C26; C27; C28; C29; C30; C34; C35; C36; C37; C38; C39; C43; C44; C45; C46; C47; C48; C49; C90; C91; C92; or C93; and wherein R1 is H; F; Cl; CF3; OCF3; OCHF2; NO2; CN; lower alkyl; lower alkenyl; lower alkynyl; lower cycloalkyl; lower heterocycloalkyl; aryl; heteroaryl; lower arylalkyl; lower heteroarylalkyl; —(CR18R19)qOR20; —(CR18R19)qNR4R11; —(CR18R19)qNR4COR22; —(CR18R19)qNR4CONR4R11; —(CR18R19)qNR4SO2R23; —(CR18R19)qNR4SO2NR4R11; —(CR18R19)qCOOR21; —(CR18R19)qCONR4R11; —(CR18R19)qSO2NR4R11; —(CR18R19)qCOR22; —(CR18R19)qSO2R23; —(CR18R19)qR24; —(CR18R19)qR25; or —(CR18R19)qR26; R2 is H; CF3; lower alkyl; lower alkenyl; cycloalkyl; heterocycloalkyl; aryl; heteroaryl; lower arylalkyl; lower heteroarylalkyl; —(CR18R19)qOR20; —(CR18R19)qNR4R11; —(CR18R19)qNR4COR22; —(CR18R19)qNR4CONR4R11; —(CR18R19)qNR4SO2R23; —(CR18R19)qNR4SO2NR4R11; —(CR18R19)qCOOR21; —(CR18R19)qCONR4R11; —(CR18R19)qSO2NR4R11; —(CR18R19)qCOR22; —(CR18R19)qSO2R23; —(CR18R19)qR24; —(CR18R19)qR25; or —(CR18R19)qR26; R4 is H; lower alkyl; lower alkenyl; or a suitable N-protecting group; R5, R7 and R9 are independently defined as H; CF3; lower alkyl; lower alkenyl; lower cycloalkyl; lower heterocycloalkyl; aryl; heteroaryl; lower arylalkyl; lower heteroarylalkyl; —(CR18R19)qOR20; —(CR18R19)qNR4R11; —(CR18R19)qNR4COR22; —(CR18R19)qNR4CONR4R11; —(CR18R19)qNR4SO2R23; —(CR18R19)qCOOR21; —(CR18R19)qCONR4R11; —(CR18R19)qSO2NR4R11; —(CR18R19)qCOR22; —(CR18R19)qSO2R23; —(CR18R19)qR24; —(CR18R19)qR25; or —(CR18R19)qR26; R6, R8 and R10 are independently defined as H; CF3; or CH3; R11 is H; alkyl; alkenyl; cycloalkyl; lower heterocycloalkyl; aryl; heteroaryl; lower arylalkyl; lower heteroarylalkyl; a suitable protecting group; —(CR18R19)rOR20; —(CR18R19)rNR4R27; —(CR18R19)rNR4CONR4R27; —(CR18R19)rNR4SO2R23; —(CR18R19)qCOOR21; —(CR18R19)qCONR4R27; —(CR18R19)qCOR22; —(CR18R19)qR24; —(CR18R19)R25; (CR18R19)qR26; or —(CR18R19)qR31; R12 and R13 are independently defined as H; or lower alkyl; R14 and R16 are independently defined as H; F; CF3; lower alkyl; lower alkenyl; lower cycloalkyl; lower heterocycloalkyl; aryl; heteroaryl; lower arylalkyl; lower heteroarylalkyl; —(CR18R19)qOR20; —(CR18R19)qNR4R11; —(CR18R19)qNR4COR22; —(CR18R19)qCOOR21; or —(CR18R19)qCONR4R11; R15 and R17 are independently defined as H; CF3; or CH3; R18 is H; F; CF3; lower alkyl; lower alkenyl; lower cycloalkyl; lower heterocycloalkyl; aryl; heteroaryl; lower arylalkyl; lower heteroarylalkyl; —(CR29R30)sOR31; —(CR29R30)sNR28R31; —(CR29R30)sNR28COR31; —(CR29R30)sNR28CONR28R31; —(CR29R30)sNR2SO2R23; —(CR29R30)qCOOR2; —(CR29R30)qCONR28R31; —(CR29R30)qSO2NR28R31; —(CR29R30)qCOR31; —(CR29R30)qSO2R23; —(CR29R30)qR24; —(CR29R30)qR25; or —(CR29R30)qR26; R19 is H; CF3; or CH3; R20 is H; lower alkyl; lower alkenyl; lower cycloalkyl; lower heterocycloalkyl; aryl; heteroaryl; lower arylalkyl; lower heteroarylalkyl; —(CR29R30)rOR31; —(CR29R30)rNR28R31; —(CR29R30)rNR28COR31; —(CR29R30)sNR28CR28CONR28R31; —(CR29R30)rNR28SO2R23; —(CR29R30)qCOOR21; —(CR29R30)qCONR28R31; —(CR29R30)qSO2NR28R31; —(CR29R30)qCOR31; —(CR29R30)qSO2R23; —(CR29R30)qR24; —(CR29R30)qR25; —(CR29R30)qR26; or —(CR29R30)qR31; R22 is lower alkyl; lower alkenyl; lower cycloalkyl; lower heterocycloalkyl; aryl; heteroaryl; lower arylalkyl; lower heteroarylalkyl; —(CR29R30)sOR31; —(CR29R30)sNR28R31; —(CR29R30)sNR28COR31; —(CR29R30)sNR28CONR28R31; —(CR29R30)sNR28SO2R23; —(CR29R30)sCOOR21; —(CR29R30)sCONR28R31; —(CR29R30)sSO2NR28R31; —(CR29R30)tCOR31; —(CR29R30)sSO2R23; —(CR29R30)tR24; —(CR29R30)tR25; —(CR29R30)tR26; or —(CR29R30)tR31; R29 is H; F; CF3; lower alkyl; lower alkenyl; lower cycloalkyl; lower heterocycloalkyl; aryl; heteroaryl; lower arylalkyl; lower heteroarylalkyl; —(CR32R33)sOR31; —(CR32R33)sNR28R31; —(CR32R33)sNR28COR31; —(CR32R33)sNR28CONR28R31; —(CR32R33)qCOOR21; —(CR32R33)qCONR28R31; —(CR32R33)qCOR31; or —(CR32R33)qR31; R30 and R33 are independently defined as H; CF3; or CH3; R34 and R35 are independently defined as H; F; Cl; CF3; OCF3; OCHF2; lower alkyl; lower alkenyl; lower alkynyl; lower cycloalkyl; lower heterocycloalkyl; aryl; heteroaryl; lower arylalkyl; lower heteroarylalkyl; —(CR29R30)qOR31; —(CR29R30)qNR28R31; —(CR29R30)qNR28COR31; —(CR29R30)qNR28CONR28R31; —(CR29R30)qNR28SO2R23; —(CR29R30)qCOOR21; —(CR29R30)qCONR28R31; —(CR29R30)qSO2NR28R31; —(CR29R30)qCOR31; —(CR29R30)qSO2R23; or —(CR29R30)qR31; R37 is H; lower alkyl; lower alkenyl; lower cycloalkyl; lower heterocycloalkyl; aryl; heteroaryl; lower arylalkyl; lower heteroarylalkyl; a suitable N-protecting group; —(CR29R30)rOR31; —(CR29R30)NR28R31; —(CR29R30)rNR28COOR21; —(CR29R30)rNR28COR31; —(CR29R30)rNR28CONR28R31; —(CR29R30)qCOOR21; —(CR29R30)qCONR28R31; —(CR29R30)qCOR31; or —(CR29R30)qR31; R38 is H; lower alkyl; lower alkenyl; lower cycloalkyl; lower heterocycloalkyl; aryl; heteroaryl; lower arylalkyl; lower heteroarylalkyl; —(CR29R30)qOR31; —(CR29R30)qNR28R31; —(CR29R30)qNR28COR31; —(CR29R30)qNR28CONR28R31; —(CR29R30)qCOOR21; —(CR29R30)qCONR28R31; —(CR29R30)qCOR31; or —(CR29R30)qR31; Z is O; S or S(═O)2; U is —C(═O)—; —NR4—C(═O)—; or —C(═O)—C(═O)—.
- Claim: 5. Compounds according to claim 1 or 2 wherein the building block of type A is selected from A1(a1); A2(a1); A3(a1); A4(a1); A5(a1); A6(a1); A7(a1); A9(a1); A10(a1); A73(a2); A170(a4); A209(a7); A240(a10); A272(a10); A532(a18); A614(a24); A631(a1); A632(a1); A633(a1); A641(a1); A642(a1); A643(a1); A651(a1); A652(a1); or A653(a1); the building block of type B is selected from B7(b3); B8(b3); B9(b3); B10(b3); or B17(b5); the building block of type C is selected from C1; C8; C9; C11; C12; C15; C17; C19; C20; C25; or C47; and wherein R1 is H; F; Cl; Br; CF3; OCF3; OCHF2; CN; lower alkyl; lower alkenyl; cycloalkyl; heterocycloalkyl; aryl; heteroaryl; lower arylalkyl; lower heteroarylalkyl; —(CR29R30)qOR20; —(CR29R30)qNR4R11; —(CR29R30)qNR4COR22; —(CR29R30)qNR4CONR4R11; —(CR29R30)qNR4SO2R23; —(CR29R30)qCOOR21; —(CR29R30)qCONR4R11; —(CR29R30)qSO2NR4R11; —(CR29R30)qCOR22; —(CR29R30)qSO2R23; —(CR29R30)qR24; —(CR29R30)qR25; or —(CR29R30)qR26; R2 is H; CF3; lower alkyl; lower alkenyl; lower cycloalkyl; lower heterocycloalkyl; aryl; heteroaryl; lower arylalkyl; lower heteroarylalkyl; —(CR29R30)qOR20; —(CR29R30)qNR4R11; —(CR29R30)qNR4COR22; —(CR29R30)qNR4CONR4R11; —(CR29R30)qNR4SO2R23; —(CR29R30)qCOOR21; —(CR29R30)qCONR4R11; —(CR29R30)qSO2NR4R11; —(CR29R30)qCOR22; —(CR29R30)qSO2R23; —(CR29R30)qR24; —(CR29R30)qR25; or —(CR29R30)qR26; R4 is H; acetyl; lower alkyl; lower alkenyl; or a suitable N-protecting group; R5, R7 and R9 are independently defined as H; CF3; lower alkyl; lower alkenyl; lower cycloalkyl; lower heterocycloalkyl; aryl; heteroaryl; lower arylalkyl; lower heteroarylalkyl; —(CR18R19)qOR20; —(CR18R19)qNR4R12; —(CR18R19)qNR4COR22; —(CR18R19)qNR4CONR4R11; —(CR18R19)qNR4SO2R23; —(CR18R19)qCOOR21; —(CR18R19)qCONR4R11; —(CR18R19)qSO2NR4R11; —(CR18R19)qCOR22; —(CR18R19)qSO2R23; —(CR18R19)qR24; —(CR18R19)qR25; or —(CR18R19)qR26; R6, R8 and R10 are independently defined as H; CF3; CH3; or benzyl; R11 is H; alkyl; alkenyl; cycloalkyl; lower heterocycloalkyl; aryl; heteroaryl; lower arylalkyl; lower heteroarylalkyl; a suitable protecting group; —(CR18R19)rOR20; —(CR18R19)rNR4R27; —(CR18R19)rNR4CONR4R27; —(CR18R19)rNR4SO2R23; —(CR18R11)qCOOR21; —(CR18R19)qCONR4R27; —(CR18R19)qCOR22; —(CR18R19)qR24; —(CR18R19)sR25; —(CR18R19)qR26; or —(CR18R19)qR31; R12 and R13 are independently defined as H; or lower alkyl; R14 and R16 are independently defined as H; F; CF3; lower alkyl; lower alkenyl; lower cycloalkyl; lower heterocycloalkyl; aryl; heteroaryl; lower arylalkyl; lower heteroarylalkyl; —(CR29R30)qOR20; —(CR29R30)qNR4R11; —(CR29R30)qNR4COR22; —(CR29R30)qCOOR21; or —(CR29R30)qCONR4R11; R15 and R17 are independently defined as H; CF3; or CH3; R18 is H; F; CF3; lower alkyl; lower alkenyl; lower cycloalkyl; lower heterocycloalkyl; aryl; heteroaryl; lower arylalkyl; lower heteroarylalkyl; —(CR29R30)sOR31; —(CR29R30)sNR28R31; —(CR29R30)sNR28COR31; —(CR29R30)sNR28CONR28R31; —(CR29R30)sNR28SO2R23; —(CR29R30)qCOOR21; —(CR29R30)qCONR28R31; —(CR29R30)qSO2NR28R31; —(CR29R30)qCOR31; —(CR29R30)qSO2R23; —(CR29R30)qR24; —(CR29R30)qR25; or —(CR29R30)qR26; R19 is H; CF3; or CH3; R20 is H; lower alkyl; lower alkenyl; lower cycloalkyl; lower heterocycloalkyl; aryl; heteroaryl; lower arylalkyl; lower heteroarylalkyl; —(CR29R30)rOR31; —(CR29R30)rNR28R31; —(CR29R30)rNR28COR31; —(CR29R30)rNR28CONR28CONR28R31; —(CR29R30)rNR28SO2R23; —(CR29R30)qCOOR21; —(CR29R30)qCONR28R31; —(CR29R30)qSO2NR28R31; —(CR29R30)qCOR31; —(CR29R30)qSO2R23; —(CR29R30)qR24; —(CR29R30)qR25; —(CR29R30)qR26; or —(CR29R30)qR31; R22 is lower alkyl; lower alkenyl; lower cycloalkyl; lower heterocycloalkyl; aryl; heteroaryl; lower arylalkyl; lower heteroarylalkyl; —(CR29R30)sOR31; —(CR29R30)sNR28R31; —(CR29R30)sNR28COR31; —(CR29R30)sNR28CONR28R31; —(CR29R30)sNR28SO2R23; —(CR29R30)sCOOR21; —(CR29R30)sCONR28R31; —(CR29R30)sSO2NR28R31; —(CR29R30)tCOR31; —(CR29R30)sSO2R23; —(CR29R30)tR24; —(CR29R30)tR25; —(CR29R30)tR26; or —(CR29R30)tR31; R24 is aryl; heteroaryl; or —C6H2R34R35R31; R25 and R26 are independently defined as heterocycloalkyl; R27 is H; lower alkyl; lower alkenyl; lower cycloalkyl; lower heterocycloalkyl; aryl; heteroaryl; lower arylalkyl; lower heteroarylalkyl; a suitable protecting group; or —(CR29R30)qR24; R28 is H; —(CR32R33)sOR21; or —(CR32R33)sNR43R42; R29 is H; F; CF3; lower alkyl; lower alkenyl; lower cycloalkyl; lower heterocycloalkyl; aryl; heteroaryl; lower arylalkyl; lower heteroarylalkyl; —(CR32R33)OR31; —(CR32R33)sNR28R31; —(CR32R33)sNR28COR31; —(CR32R33)sNR28CONR28R31; (CR32R33)qCOOR21; —(CR32R33)qCONR28R31; —(CR32R33)qCOR31; or —(CR32R33)qR31; R30 and R33 are independently defined as H; F; CF3; or CH3; R31 is H; alkyl; alkenyl; cycloalkyl; heterocycloalkyl; aryl; heteroaryl; arylalkyl; or heteroarylalkyl; R32 is H; F; CF3; lower alkyl; lower alkenyl; lower cycloalkyl; lower heterocycloalkyl; aryl; heteroaryl; lower arylalkyl; or lower heteroarylalkyl; R34 and R35 are independently defined as H; F; Cl; CF3; lower alkyl; lower alkenyl; lower cycloalkyl; lower heterocycloalkyl; aryl; heteroaryl; lower arylalkyl; lower heteroarylalkyl; —(CR29R30)qOR31; —(CR29R30)qNR28R31; —(CR29R30)qNR28COR31; —(CR29R30)qNR28CONR28R31; —(CR29R30)qNR28SO2R23; —(CR29R30)qCOOR21; —(CR29R30)qCONR28R31; —(CR29R30)qSO2NR28R31; —(CR29R30)qCOR31; —(CR29R30)qSO2R23; or —(CR29R30)qR31; R38 is H; lower alkyl; lower alkenyl; lower cycloalkyl; lower heterocycloalkyl; aryl; heteroaryl; lower arylalkyl; lower heteroarylalkyl; —(CR29R30)qOR31; —(CR29R30)qNR28R31; —(CR29R30)qNR28COR31; —(CR29R30)qNR28CONR28R31; —(CR29R30)qCOOR21; —(CR29R30)qCONR28R31; —(CR29R30)qCOR31; or —(CR29R30)qR31; R42 and R43 are independently defined as H; lower alkyl; lower alkenyl; lower cycloalkyl; lower heterocycloalkyl; aryl; heteroaryl; lower arylalkyl; lower heteroarylalkyl; or a suitable N-protecting group; X is O; S; S(═O); or S(═O)2; Y is O; S; or NR4; Z is O; S or S(═O)2; U is —C(═O)—; —NR4—C(═O)—; or —C(═O)—C(═O)—; or pharmaceutically acceptable salts, solvates, clathrates, isotopically enriched or enantiomerically enriched versions thereof.
- Claim: 6. Compounds according to claim 1 or 2 wherein the building block of type A is selected from A2(a1); A5(a1); A9(a1); A73(a2); A209(a7); A272(a10); A532(a18); A614(a24); A641(a1); or A651(a1); the building block of type B is selected from B7; B9; B10 or B17; the building block of type C is selected from C1; C8; C9; C11; C15; C17; C19; C20; C25; or C47; and wherein R1 is H; F; Cl; Br; CH3; OCH3; OH; or aryl; R2 is H; CH3; heterocycloalkyl; aryl; benzyl; heteroaryl; —OR20; —NR4R11; —NR4COOR21; —NR4COR22; —NR4CONR4R11; or —NR4SO2R23; R3 is H; R4 is H; acetyl; lower alkyl; lower alkenyl; or a suitable N-protecting group; R5, R7 and R9 are independently defined as H; CF3; lower alkyl; lower alkenyl; lower cycloalkyl; lower heterocycloalkyl; aryl; heteroaryl; lower arylalkyl; lower heteroarylalkyl; —OR20; —NR4R11; —NR4COR22; —NR4CONR4R11; NR4SO2R23; —COOR21; —CONR4R11; or —COR22; R6, R8 and R10 are defined as H; R11 is H; alkyl; aryl; heteroaryl; lower arylalkyl; lower heteroarylalkyl; —(CR18R19)rOR20; —(CR18R19)rNR4R27; —(CR18R19)qCOOR21; —COR22; —(CR18R19)qR24; or —(CR18R19)qR31; R12 and R13 are defined as H; R14 and R16 are independently defined as H; lower alkyl; or lower arylalkyl; R15 and R17 are defined as H; R18 and R19 are defined as H; R20 is H; aryl; heteroaryl; lower arylalkyl; lower heteroarylalkyl; or —(CR29R30)qR24; R21 is H; lower alkyl; lower arylalkyl; or a suitable O-protecting group; R22 is lower alkyl; lower alkenyl; aryl; heteroaryl; lower arylalkyl; lower heteroarylalkyl; —(CR29R30)sOR31; —(CR29R30)sNR28R31; —(CR29R31)sCOOR21; —(CR29R30)tR24; or —(CR29R30)tR31; R23 is H; lower alkyl; aryl; heteroaryl; or —R24; R24 is aryl; heteroaryl; or —C6H2R34R35R31; R27 is H; acetyl; CH3; or —(CH2)qR24; R28 is H; —(CR32R33)sOR21; or —(CR32R33)sNR43R42; R29 is H; lower alkyl; aryl; or heteroaryl; R30, R32 and R33 are independently defined as H; CF3; or CH3; R31 is H; alkyl; cycloalkyl; heterocycloalkyl; aryl; heteroaryl; arylalkyl; or heteroarylalkyl; R34 and R35 are independently defined as H; heterocycloalkyl; —OR31; or —NR28R31; R38 is II; —NR28R31; —NR28COR31; or —NR28COOR31; R42 and R43 are independently defined as H; CH3; or benzyl; X is O; S; S(═O); or S(═O)2; Y is O; S; or NR4; Z is O; S or S(═O)2; U is —C(═O)—; —NR4—C(═O)—; or —C(═O)—C(═O)—; or pharmaceutically acceptable salts, solvates, clathrates, isotopically enriched or enantiomerically enriched versions thereof.
- Claim: 7. Compounds according to claim 4 wherein the building block of type C is represented by [chemical expression included] and wherein CAA is an amino acid or its complementary enantiomer selected from the list of Ala L-Alanine; Arg L-Arginine; Asn L-Asparagine; Asp L-Aspartic acid; Cys L-Cysteine; Glu L-Glutamic acid; Gln L-Glutamine; Gly Glycine; Ile L-Isoleucine; Leu L-Leucine; Lys L-Lysine; Met L-Methionine; Phe L-Phenylalanine; Pro L-Proline; Ser L-Serine; Thr L-Threonine; Trp L-Tryptophan; Tyr L-Tyrosine; Val L-Valine; Apa 3-Amino-propanoic acid; H-β3-HAla-OH (3S)-3-Amino-butyric acid; H-β3-HVal-OH (3R)-3-Amino-4-methyl-valeric acid; H-β3-HIle-OH (3R,4S)-3-Amino-4-methyl-hexanoic acid; H-β3-HLeu-OH (3S)-3-Amino-5-methyl-hexanoic acid; H-β3-HMet-OH (3S)-3-Amino-5-methylthio pentanoic acid; H-β3-HTyr-OH (3S)-3-Amino-4-(4′-hydroxyphenyl)-butyric acid; H-β3-HHis-OH (3S)-3-Amino-4-(imidazole-4′-yl)-butyric acid; H-β3-HPhe-OH (3S)-3-Amino-4-phenyl butyric acid; H-β3-HTrp-OH (3S)-3-Amino-4-(indol-3′-yl)-butyric acid; H-β3-HSer-OH (3R)-3-Amino-4-hydroxy-butyric acid; H-β3-HAsp-OH 3-Amino-pentanedioic acid; H-β3-HGlu-OH (3S)-3-Amino-hexanedioic acid; H-β3-HLys-OH (3S)-3,7-Diamino-heptanoic acid; H-β3-HArg-OH (3S)-3-Amino-6-guanidino-hexanoic-acid; H-β3-HCys-OH (3R)-3-Amino-4-mercapto-butyric acid; H-β3-HAsn-OH (3S)-3-Amino-4-carbamoyl-butyric acid; H-β3-HGln-OH (3S)-3-Amino-5-carbamoyl-pentanoic acid; H-β3-HThr-OH (3R,4R)-3-Amino-4-hydroxy-pentanoic acid; Gaba 4-Amino-butyric acid; H-γ4-DiHAJa-OH (4S)-4-Amino-pentanoic acid; H-γ4-DiHVal-OH (4R)-4-Amino-5-methyl-hexanoic acid; H-γ4-DiHIle-OH (4R,5S)-4-Amino-5-methyl-heptanoic acid; H-γ4-DiHLeu-OH (4R)-4-Amino-6-methyl-heptanoic acid; H-γ4-DiHMet-OH (4R)-4-Amino-6-methylthio-hexanoic acid; H-γ4-DiHlTyr-OH (4R)-4-Amino-5-(4′-hydroxyphenyl)-pentanoic acid; H-γ4-DiHHis-OH (4R)-4-Amino-5-(imidazole-4′-yl)-pentanoic acid; H-γ4-DiHPhe-OH (4R)-4-Amino-5-phenyl-pentanoic acid; H-γ4-DiHTrp-OH (4R)-4-Amino-5-(indol-3′-yl)-pentanoic acid; H-γ4-DiHSer-OH (4R)-4-Amino-5-hydroxy-pentanoic acid; H-γ4-DiHAsp-OH (4R)-4-Amino-hexanedioic acid; H-γ4-DiHfGlu-OH 4-Amino-heptanedioic acid; H-γ4-DiHLys-OH (4S)-4,8-Diamino-octanoic acid; H-γ4-DiHArg-OH (4S)-4-Amino-7-guanidino-heptanoic-acid; H-γ4-DiHCys-OH (4R)-4-Amino-5-mercapto-pentanoic acid; H-γ4-DiHiAsn-OH (4R)-4-Amino-5-carbamoyl-pentanoic acid; H-γ4-DiHGln-OH (3S)-3-Amino-5-carbamoyl-hexanoic acid; H-γ4-DiHThr-OH (4R,5R)-4-Amino-5-hydroxy-hexanoic acid; Cit L-Citrulline; Orn L-Omnithine; tBuA L-t-Butylalanine; Sar Sarcosine; Pen L-Penicillamine; tBuG L-tert.-Butylglycine; 4AmPhe L-para-Aminophenylalanine; 3AmPhe L-meta-Aminophenylalanine; 2AmPhe L-ortho-Aminophenylalanine; Phe(mC(NH12)═NH) L-meta-Amidinophenylalanine; Phe(pC(NH12)═NH) L-para-Amidinophenylalanine; Phe(mNHC(NH2)═NH) L-meta-Guanidinophenylalanine; Phe(pNHC(NH2)═NH) L-para-Guanidinophenylalanine; 2Pal (2S)-2-Amino-3-(pyridine-2′-yl)-propionic acid; 4Pal (2S)-2-Amino-3-(pyridine-4′-yl)-propionic acid; Phg L-Phenylglycine; Cha L-Cyclohexylalanine; C4al L-3-Cyclobutylalanine; C5al L-3-Cyclopentylalanine; Nle L-Norleucine; 2-Nal L-2-Naphthylalanine; 1-Nal L-1-Naphthylalanine; 4ClPhe L-4-Chlorophenylalanine; 3 ClPhe L-3-Chlorophenylalanine; 2ClPhe L-2-Chlorophenylalanine; 3,4Cl2 Phe L-3,4-Dichlorophenylalanine; 4FPhe L-4-Fluorophenylalanine; 3FPhe L-3-Fluorophenylalanine; 2FPhe L-2-Fluorophenylalanine; Thi L-β-2-Thienylalanine; Tza L-2-Thiazolylalanine; Mso L-Methionine sulfoxide; AcLys N-Acetyllysine; Dap 2,3-Diaminopropionic acid; Dab 2,4-Diaminobutyric acid; Dbu (2S)-2,3-Diamino-butyric acid; Abu γ-Aminobutyric acid (GABA); Aha ε-Aminohexanoic acid; Aib α-Aminoisobutyric acid; ACC 1-Amino cyclopropane carboxylic acid; ACBC 1-Amino cyclobutane carboxylic acid; ACPC 1-Amino cyclopentane carboxylic acid; ACHC 1-Amino cyclohexane carboxylic acid; Y(Bzl) L-O-Benzyltyrosine; H(Bzl) (3S)-2-Amino-3-(1′-benzylimidazole-4′-yl)-propionic acid; Bip L-(4-phenyl)phenylalanine; S(Bzl) L-O-Benzylserine; T(Bzl) L-O-Benzylthreonine; alloT (2S,3S)-2-Amino-3-hydroxy-butyric acid; Leu3OH (2S,3R)-2-Amino-3-hydroxy-4-methyl-pentanoic acid; hAla L-Homo-alanine; hArg L-Homo-arginine; hiCys L-Homo-cysteine; hGlu L-Homo-glutamic acid; hGln L-Homo-glutamine; hHis L-Homo-histidine; hIle L-Homo-isoleucine; hLeu L-Homo-leucine; hNle L-Homo-norleucine; hLys L-Homo-lysine; hnMet L-Homo-methionine; hPhe L-Homo-phenylalanine; hSer L-Homo-serine; hThr L-Homo-threonine; hTrp L-Homo-tryptophan; hTyr L-Homo-tyrosine; hVal L-Homo-valine; hCha L-Homo-cyclohexylalanine; Bpa L-4-Benzoylphenylalanine; OctG L-Octylglycine; Tic (3S)-1,2,3,4-Tetrahydroisoquinoline-3-carboxylic acid; Tiq (1S)-1,2,3,4-Tetrahydroisoquinoline-1-carboxylic acid; Oic (2S,3aS,7aS)-1-Octahydro-1H-indole-2-carboxylic acid; 4AmPyrr1 (2S,4S)-4-Amino-pyrrolidine-2-carboxylic acid; 4AmPyrr2 (2S,4R)-4-Amino-pyrrolidine-2-carboxylic acid; 4PhePyrr1 (2S,4R)-4-Phenyl-pyrrolidine-2-carboxylic acid; 4PhePyrr2 (2S,4S)-4-Phenyl-pyrrolidine-2-carboxylic acid; 5PhePyrr1 (2S,5R)-5-Phenyl-pyrrolidine-2-carboxylic acid; 5PhePyrr2 (2S,5S)-5-Phenyl-pyrrolidine-2-carboxylic acid; 4Hyp1 (4S)-L-Hydroxyproline; 4Hyp2 (4R)-L-Hydroxyproline; 4 Mp1 (4S)-L-Mercaptoproline; 4 Mp2 (4R)-L-Mercaptoproline; Pip L-Pipecolic acid; H-β3-HCit-OH (3S)-3-Amino-6-carbamidyl-hexanoic acid; H-β3-HOrn-OH (3S)-3,6-Diamino-hexanoic acid; H-β3-HtBuA-OH (3S)-3-Amino-5,5-dimethyl-hexanoic acid; H-β3-HSar-OH N-Methyl-3-amino-propionic acid; H-β3-HPen-OH (3R)-3-Amino-4-methyl-4-mercapto-pentanoic acid; H-β3-HtBuG-OH (3R)-3-Amino-4,4-dimethyl-pentanoic acid; H-β3-H4AmPhe-OH (3S)-3-Amino-4-(4′-aminophenyl)-butyric acid; H-β3-H3AmPhe-OH (3S)-3-Amino-4-(3′-aminophenyl)-butyric acid; H-β3-H2AmPhe-OH (3S)-3-Amino-4-(2′-aminophenyl)-butyric acid; H-β3-HPhe(mC(NH2)═NH)—OH (3S)-3-Amino-4-(3′-amidinophenyl)-butyric acid; H-β3-HPhe(pC(NH2)═NH)—OH (3S)-3-Amino-4-(4′-amidinophenyl)-butyric acid; H-β3-HPhe(mNHC(NH2)═NH)—OH (3S)-3-Amino-4-(3′-guanidinophenyl)-butyric acid; H-β3-HPhe(pNHC(NH2)═NH)—OH (3S)-3-Amino-4-(4′-guanidino-phenyl)-butyric acid; H-β3-H2Pal-OH (3S)-3-Amino-4-(pyridine-2′-yl)-butyric acid; H-β3-H4Pal-OH (3S)-3-Amino-4-(pyridine-4′-yl)-butyric acid; H-β3-HPhg-OH (3R)-3-Amino-3-phenyl-propionic acid; H-β3-HCha-OH (3S)-3-Amino-4-cyclohexyl-butyric acid; H-β3-HC4al-OH (3S)-3-Amino-4-cyclobutyl-butyric acid; H-β3-HC5al-OH (3S)-3-Amino-4-cyclopentyl-butyric acid; H-β3-HNle-OH (3S)-3-Amino-heptanoic acid; H-β3-H2Na1-OH (3S)-3-Amino-4-(2′-naphthyl)-butyric acid; H-β3-H1Na1-OH (3S)-3-Amino-4-(1′-naphthyl)-butyric acid; H-β3-H4ClPhe-OH (3S)-3-Amino-4-(4′-chlorophenyl)-butyric acid; H-β3-H3ClPhe-OH (3S)-3-Amino-4-(3′-chlorophenyl)-butyric acid; H-β3-H2ClPhe-OH (3S)-3-Amino-4-(2′-chlorophenyl)-butyric acid; H-β3-H3,4Cl2Phe-OH (3S)-3-Amino-4-(3′,4′-dichlorophenyl)-butyric acid; H-β3-H4FPhe-OH (3S)-3-Amino-4-(4′-fluorophenyl)-butyric acid; H-β3-H3FPhe-OH (3S)-3-Amino-4-(3′-fluorophenyl)-butyric acid; H-β3-H2FPhe-OH (3S)-3-Amino-4-(2′-fluorophenyl)-butyric acid; H-β3-HThi-OH (3R)-3-Amino-4-(2′-thienyl)-butyric acid; H-β3-HTza-OH (3R)-3-Amino-4-(2′-thiazolyl)-butyric acid; H-β3-HMso-OH (3R)-3-Amino-4-methylsulfoxyl-butyric acid; H-β3-HAcLys-OH (3S)-7-Acetylamino-3-amino-heptanoic acid; H-β3-HDpr-OH (3R)-3,4-diamino-butyric acid; H-β3-HA2Bu-OH (3S)-3,5-Diamino-pentanoic acid; H-β3-HDbu-OH (3R)-3,4-Diamino-pentanoic acid; H-β3-HAib-OH Amino-dimethyl acetic acid; H-β3-HCyp-OH 1-Amino-cyclopentane-1-yl-acetic acid; H-β3-HY(Bzl)-OH (3S)-3-Amino-4-(4′-benzyloxyphenyl)-butyric acid; H-β3-HH(Bzl)-OH (3S)-3-Amino-4-(1′-benzylimidazole-4′-yl)-butyric acid; H-β3-HBip-OH (3S)-3-Amino-4-biphenylyl-butyric acid; H-β3-HS(Bzl)-OH (3S)-3-Amino-4-(benzyloxy)-butyric acid; H-β3-HT(Bzl)-OH (3R,4R)-3-Amino-4-benzyloxy-pentanoic acid; H-β3-HalloT-OH (3R,4S)-3-Amino-4-hydroxy-pentanoic acid; H-β3-HLeu3OH—OH (3R,4R)-3-Amino-4-hydroxy-5-methyl-hexanoic acid; H-β3-HhAla-OH (3S)-3-Amino-pentanoic acid; H-β3-HhArg-OH (3S)-3-Amino-7-guanidino-heptanoic acid; H-β3-HhCys-OH (3R)-Amino-5-mercapto-pentanoic acid; H-β3-HhGlu-OH (3S)-3-Amino-heptanedioic acid; H-β3-HhGln-OH (3S)-3-Amino-6-carbamoyl hexanoic acid; H-β3-HhHis-OH (3S)-3-Amino-5-(imidazole-4′-yl)-pentanoic acid; H-β3-HhIle-OH (3S,5S)-3-Amino-5-methyl-heptanoic acid; H-β3-HhLeu-OH (3S)-3-Amino-6-methyl-heptanoic acid; H-β3-HhNle-OH (3S)-3-Amino-octanoic acid; H-β3-DiAoc-OH (3S)-3,8-Diamino-octanoic acid; H-β3-HhMet-OH (3S)-3-Amino-6-methylthio-hexanoic acid; H-β3-HhPe-OH (3S)-3-Amino-5-phenyl-pentanoic acid; H-β3-HhSer-OH (3S)-3-Amino-5-hydroxy-pentanoic acid; H-β3-HhThr-OH (3S,5R)-3-Amino-5-hydroxy-hexanoic acid; H-β3-HhTrp-OH (3S)-3-Amino-5-(indol-3′-yl)-pentanoic acid; H-β3-HhThr-OH (3S)-3-Amino-5-(4′-hydroxyphenyl)-pentanoic acid; H-β3-HhCha-OH (3S)-3-Amino-5-cyclohexyl-pentanoic acid; H-β3-HBpa-OH (3S)-3-Amino-4-(4′-benzoylphenyl)-butyric acid; H-β3-HOctG-OH (3S)-3-Amino-undecanoic acid; H-β3-HNle-OH (3S)-3-Amino-heptanoic acid; H-β3-HTic-OH (3S)-1,2,3,4-Tetrahydroisoquinoline-3-yl-acetic acid; H-β3-HTiq-OH (1S)-1,2,3,4-Tetrahydroisoquinoline-1-acetic acid; H-β3-HOic-OH (2S,3aS,7aS)-1-Octahydro-1H-indole-2-yl-acetic acid; H-β3-H4AmPyrr1-OH (2S,4S)-4-Amino-pyrrolidine-2-acetic acid; H-β3-H4AmPyrr2-OH (2S,4R)-4-Amino-pyrrolidine-2-acetic acid; H-β3-H4PhePyrr1-OH (2S,4R)-4-Phenyl-pyrrolidine-2-acetic acid; H-β3-H4PhePyrr2-OH (2S,4S)-4-Phenyl-pyrrolidine-2-acetic acid; H-β3-H5PhePyrr1-OH (2S,5R)-5-Phenyl-pyrrolidine-2-acetic acid; H-β3-H5PhePyrr2-OH (2S,5S)-5-Phenyl-pyrrolidine-2-acetic acid; H-β3-H4Hyp1-OH (2S,4S)-4-Hydroxy-pyrrolidine-2-acetic acid; H-β3-H4Hyp2-OH (2S,4R)-4-Hydroxy-pyrrolidine-2-acetic acid; H-β3-H4Mp1-OH (2R,4S)-4-Mercapto-pyrrolidine-2-acetic acid; H-β3-H4Mp2-OH (2R,4R)-4-Mercapto-pyrrolidine-2-acetic acid; H-β3-HPip-OH (2S)-Piperidine-2-acetic acid; H-β3-HPro-OH (2S)-Pyrrolidine-2-acetic acid; Ahb 4-Amino-2-hydroxy butyric acid; H-γ4-DiHCit-OH (4S)-4-Amino-7-carbamidyl-heptanoic acid; H-γ4-DiHOrn-OH (4S)-4,7-Diamino-heptanoic acid; H-γ4-DiHtBuA-OH (4R)-4-Amino-6,6-dimethyl-heptanoic acid; H-γ4-DiHSar-OH N-Methyl-4-amino-butyric acid; H-γ4-DiHPen-OH (4R)-4-Amino-5-methyl-5-mercapto-hexanoic acid; H-γ4-DiHtBuG-OH (4R)-4-Amino-5,5-dimethyl-hexanoic acid; H-γ4-DiH4AmPhe-OH (4R)-4-Amino-5-(4′-aminophenyl)-pentanoic acid; H-γ4-DiH3AmPhe-OH (4R)-4-Amino-5-(3′-aminophenyl)-pentanoic acid; H-γ4-DiH2AmPhe-OH (4R)-4-Amino-5-(2′-aminophenyl)-pentanoic acid; H-γ4-DiHPhe(mC(NH2)═NH)—OH (4R)-4-Amino-5-(3′-amidinophenyl)-pentanoic acid; H-γ4-DiHPhe(pC(NH2)═NH)—OH (4R)-4-Amino-5-(4′-amidinophenyl)-pentanoic acid; H-γ4-DiHPhe(mNHC(NH2)═NH)—OH (4R)-4-Amino-5-(3′-guanidino-phenyl)-pentanoic acid; H-γ4-DiHPhe(pNHC(NH2)═NH)—OH (4R)-4-Amino-5-(4′-guanidino-phenyl)-pentanoic acid; H-γ4-DiH2Pal-OH (4R)-4-Amino-5-(pyridine-4′-yl)-pentanoic acid; H-γ4-DiH4Pal-OH (4R)-4-Amino-5-(pyridine-4′-yl)-pentanoic acid; H-γ4-DiHPhg-OH (4R)-4-Amino-4-phenyl-butyric acid; H-γ4-DiHCha-OH (4R)-4-Amino-5-cyclohexyl-pentanoic acid; H-γ4-DiHC4al-OH (4R)-4-Amino-5-cyclobutyl-pentanoic acid; H-γ4-DiHC5al-OH (4R)-4-Amino-5-cyclopentyl-pentanoic acid; H-γ4-DiH1Nle-OH (4S)-4-Amino-octanoic acid; H-γ4-DiH2Nal-OH (4S)-4-Amino-5-(2′-naphthyl)-pentanoic acid; H-γ4-DiH1Nal-OH (4S)-4-Amino-5-(1′-naphthyl)-pentanoic acid; H-γ4-DiH4ClPhe-OH (4R)-4-Amino-5-(4′-chlorophenyl)-pentanoic acid; H-γ4-DiH3ClPhe-OH (4R)-4-Amino-5-(3′-chlorophenyl)-pentanoic acid; H-γ4-DiH2ClPhe-OH (4R)-4-Amino-5-(2′-chlorophenyl)-pentanoic acid; H-γ4-DiH3,4Cl2Phe-OH (4R)-4-Amino-5-(3′,4′-dichloro-phenyl)-pentanoic acid H-γ4-DiH4FPhe-OH (4R)-4-Amino-5-(4′-fluorophenyl)-pentanoic acid; H-γ4-DiH3FPhe-OH (4R)-4-Amino-5-(3′-fluorophenyl)-pentanoic acid; H-γ4-DiH2FPhe-OH (4R)-4-Amino-5-(2′-fluorophenyl)-pentanoic acid; H-γ4-DiHThi-OH (4R)-4-Amino-5-(2′-thienyl)-pentanoic acid; H-γ4-DiHTza-OH (4R)-4-Amino-5-(2′-thiazolyl)-pentanoic acid; H-γ4-DiHMso-OH (4R)-4-Amino-5-methylsulfoxyl-pentanoic acid; H-γ4-DiHAcLys-OH (4S)-8-Acetylamino-4-amino-ocatanoic acid; H-γ4-DiHDpr-OH (4R)-4,5-diamino-pentanoic acid; H-γ4-DiHA2Bu-OH (4R)-4,5-Diamino-hexanoic acid; H-γ4-DiHDbu-OH (4R)-4,5-Diamion-hexanoic acid; H-γ4-DiHAib-OH 3-Amino-3,3-dimethyl propionic acid; H-γ4-DiHCyp-OH (1′-Amino-cyclopentane-1′-yl)-3-propionic acid; H-γ4-DiHY(Bzl)-OH (4R)-4-Amino-5-(4′-benzyloxyphenyl)-pentanoic acid; H-γ4-DiHH(Bzl)-OH (4R)-4-Amino-5-(1′-benzylimidazole-4′-yl)-pentanoic acid; H-γ4-DiHBip-OH (4R)-4-Amino-5-biphenylyl-pentanoic acid; H-γ4-DiHS(Bzl)-OH (4S)-4-Amino-5-(benzyloxy)-pentanoic acid; H-γ4-DiHT(Bzl)-OH (4R,5R)-4-Amino-5-benzyloxy-hexanoic acid; H-γ4-DiHalloT-OH (4R,5S)-4-Amino-5-hydroxy-hexanoic acid; H-γ4-DiHLeu3OH—OH (4R,5R)-4-Amino-5-hydroxy-6-methyl-heptanoic acid; H-γ4-DiHhAla-OH (4S)-4-Amino-hexanoic acid; H-γ4-DiHhArb-OH (4S)-4-Amino-8-guanidino-octanoic acid; H-γ4-DiHhCys-OH (4R)-Amino-6-mercapto-hexanoic acid; H-γ4-DiHhGlu-OH (4S)-4-Amino-ocatanedioic acid; H-γ4-DiHhGln-OH (4S)-4-Amino-7-carbamoyl-heptanoic acid; H-γ4-DiHhHis-OH (4S)-4-Amino-6-(imidazole-4′-yl)-hexanoic acid; H-γ4-DiHhIle-OH (4S,6S)-4-Amino-6-methyl-octanoic acid; H-γ4-DiHhLeu-OH (4S)-4-Amino-7-methyl-ocatanoic acid; H-γ4-DiHhNle-OH (4S)-4-Amino-nonanoic acid; H-γ4-DiHhLys-OH (4S)-4,9-Diamino-nonanoic acid; H-γ4-DiHhMet-OH (4R)-4-Amino-7-methylthioheptanoic acid; H-γ4-DiHhPhe-OH (4S)-4-Amino-6-phenyl-hexanoic acid; H-γ4-DiHhSer-OH (4R)-4-Amino-6-hydroxy-hexanoic acid; H-γ4-DiHhThr-OH (4R,6R)-4-Amino-6-hydroxy-heptanoic acid; H-γ4-DiHhTrp-OH (4S)-4-Amino-6-(indol-3′-yl)-hexanoic acid; H-γ4-DiHhTyr-OH (4S)-4-Amino-6-(4′-hydroxyphenyl)-hexanoic acid; H-γ4-DiHhCha-OH (4R)-4-Amino-5-cyclohexyl-pentanoic acid; H-γ4-DihBpa-OH (4R)-4-Amino-5-(4′-benzoylphenyl)-pentanoic acid; H-γ4-DiHOctG-OH (4S)-4-Amino-dodecanoic acid; H-γ4-DiHNle-OH (4S)-4-Amino-octanoic acid; H-γ4-DiHTic-OH (3R)-1′,2′,3′,4′-Tetrahydroisoquinoline-3′-yl-3-propionic acid; H-γ4-DiHTiq-OH (1′R)-1′,2′,3′,4′-Tetrahydroisoquinoline-1′-yl-3-propionic acid; H-γ4-DiHOic-OH (2′S,3′aS,7′aS)-1′-Octahydro-1H-indole-2′-yl-3-propionic acid; H-γ4-DiH4AmPyrr1-OH (2′R,4′S)-4′-Amino-pyrrolidine-2′-yl-3-propionic acid; H-γ4-DiH4AmPyrr2-OH (2′R,4′R)-4′-Amino-pyrrolidine-2′-yl-3-propionic acid; H-γ4-DiH4PhePyrr1-OH (2′R,4′R)-4′-Phenyl-pyrrolidine-2′-yl-3-propionic acid; H-γ4-DiH4PhePyrr2-OH (2′R,4′S)-4′-Phenyl-pyrrolidine-2′-yl-3-propionic acid H-γ4-DiH5PhePyrr1-OH (2′S,5′R)-5′-Phenyl-pyrrolidine-2′-yl-3-propionic acid; H-γ4-DiH5PhePyrr2-OH (2′S,5′S)-5′-Phenyl-pyrrolidine-2′-yl-3-propionic acid H-γ4-DiH4Hyp1-OH (2′R,4′S)-4′-Hydroxy-pyrrolidine-2′-yl-2-propionic acid; H-γ4-DiH4Hyp2-OH (2′R,4′R)-4′-Hydroxy-pyrrolidine-2′-yl-3-propionic acid; H-γ4-DiH4 Mp1-OH (2′R,4′S)-4′-Mercapto-pyrrolidine-2′-yl-3-propionic acid; H-γ4-DiH4 Mp2-OH (2′R,4′R)-4′-Mercapto-pyrrolidine-2′-yl-3-propionic acid; H-γ4-DiHPip-OH (2′S)-Piperidine-2′-yl-3-propionic acid; H-γ4-DiHPro-OH (2′S)-Pyrrolidine-2′-yl-3-propionic acid; (AEt)G N-(2-Aminoethyl)glycine; (APr)G N-(3-Amino-n-propyl)glycine; (ABu)G N-(4-Amino-n-butyl)glycine; (APe)G N-(5-Amino-n-pentyl)glycine; (GuEt)G N-(2-Guanidinoethyl)glycine; (GuPr)G N-(3-Guanidino-n-propyl)glycine; (GuBu)G N-(4-Guanidino-n-butyl)glycine; (GuPe)G N-(5-Guanidino-n-pentyl)glycine; (PEG3-NH2)G N—[H2N—(CH2)3—(OCH2—CH2)2—O(CH2)3]glycine; (Me)G N-Methylglycine; (Et)G N-ethylglycine; (Bu)G N-Butylglycine; (Pe)G N-Pentylglycine; (Tp)G N-Isopropylglycine; (2MePr)G N-(2-Methylpropyl)glycine; (3MeBu)G N-(3-Methylbutyl)glycine; (1MePr)G (1S)—N-(1-Methylpropyl)glycine; (2MeBu)G (2S)—N-(2-Methylbutyl)glycine; (MthEt)G N-(Methylthio ethyl)glycine; (MthPr)G N-(Methylthiopropyl)glycine; (Ben)G N-(Benzyl)glycine; (PhEt)G N-(2-Phenylethyl)glycine; (HphiMe)G N-([4′-hydroxyphenyl]methyl)glycine; (HphEt)G N-(2-[4′-hydroxyphenyl]ethyl)glycine (ImMe)G N-(Imidazol-5-yl-methyl)glycine; (ImEt)G N-(2-(Imidazol-5′-yl)ethyl)glycine; (InMe)G N-(Indol-2-yl-methyl)glycine; (InEt)G N-(2-(Indol-2′-yl)ethyl)glycine; (CboMe)G N-(Carboxymethyl)glycine; (CboEt)G N-(2-Carboxyethyl)glycine; (CboPr)G N-(3-Carboxypropyl)glycine; (CbaMe)G N-(Carbamoylmethyl)glycine; (CbaEt)G N-(2-Carbamoylethyl)glycine; (CbaPr)G N-(3-Carbamoylpropyl)glycine; (HyEt)G N-(2-Hydroxyethyl)glycine; (HyPr)G (2R)—N-(2-Hydroxypropyl)glycine; or (Mcet)G N-(2-Mercaptoethyl)glycine.
- Claim: 8. Compounds according to claim 1, selected from: (2S,11S,19aS)—N-[2-(dimethylamino)ethyl]-15-fluoro-7,12-dimethyl-2-{[(1-naphthylamino)carbonyl]amino}-5,8,13-trioxo-2,3,6,7,8,9,10,11,12,13,19,19a-dodecahydro-1H,5H-pyrrolo[2,1-c][1,4,7,12]benzoxatriazacyclopentadecine-11-carboxamide; (2S,11S,19aS)—N-(2-aminoethyl)-15-fluoro-7,12-dimethyl-2-{[2-(1-naphthyl)acetyl]amino}-5,8,13-trioxo-2,3,6,7,8,9,10,11,12,13,19,19a-dodecahydro-1H,5H-pyrrolo[2,1-c][1,4,7,12]benzoxatriazacyclopentadecine-11-carboxamide; (2S,11S,19aS)—N-(2-{[amino(imino)methyl]amino}ethyl)-15-fluoro-7,12-dimethyl-2-{[2-(1-naphthyl)acetyl]amino}-5,8,13-trioxo-2,3,6,7,8,9,10,11,12,13,19,19a-dodecahydro-1H,5H-pyrrolo[2,1-c][1,4,7,12]benzoxatriazacyclopentadecine-11-carboxamide; (2S,11S,19aS)-15-fluoro-7,12-dimethyl-2-{[2-(1-naphthyl)acetyl]amino}-5,8,13-trioxo-N-[2-(2-pyridinylamino)ethyl]-2,3,6,7,8,9,10,11,12,13,19,19a-dodecahydro-1H,5H-pyrrolo[2,1-c][1,4,7,12]benzoxatriazacyclopentadecine-11-carboxamide; (2S,11S,19aS)—N-[2-(dimethylamino)ethyl]-15-fluoro-7,12-dimethyl-2-{[2-(1-naphthyl)ethyl]amino}-5,8,13-trioxo-2,3,6,7,8,9,10,11,12,13,19,19a-dodecahydro-1H,5H-pyrrolo[2,1-c][1,4,7,12]benzoxatriazacyclopentadecine-11-carboxamide; (2S,11S,19aS)—N-[2-(acetylamino)ethyl]-15-fluoro-7,12-dimethyl-2-[2-(1-naphthyl)acetyl]amino-5,8,13-trioxo-2,3,6,7,8,9,10,11,12,13,19,19a-dodecahydro-1H,5H-pyrrolo[2,1-c][1,4,7,12]benzoxatriazacyclopentadecine-11-carboxamide; (2S,11S,19aS)—N-[2-(dimethylamino)ethyl]-15-fluoro-7,12-dimethyl-2-{[2-(2-naphthyl)acetyl]amino}-5,8,13-trioxo-2,3,6,7,8,9,10,11,12,13,19,19a-dodecahydro-1H,5H-pyrrolo[2,1-c][1,4,7,12]benzoxatriazacyclopentadecine-11-carboxamide; (2S,11S,19aS)—N-[2-(dimethylamino)ethyl]-15-fluoro-7,12-dimethyl-5,8,13-trioxo-2-(2-[3-(trifluoromethyl)phenyl]acetylamino)-2,3,6,7,8,9,10,11,12,13,19,19a-dodecahydro-1H,5H-pyrrolo[2,1-c][1,4,7,12]benzoxatriazacyclopentadecine-11-carboxamide; (2S,11S,19aS)—N-[2-(dimethylamino)ethyl]-15-fluoro-2-[2-(3-methoxyphenyl)acetyl]amino-7,12-dimethyl-5,8,13-trioxo-2,3,6,7,8,9,10,11,12,13,19,19a-dodecahydro-1H,5H-pyrrolo[2,1-c][1,4,7,12]benzoxatriazacyclopentadecine-11-carboxamide; (2S,1S,19aS)—N-[3-(dimethylamino)propyl]-15-fluoro-7,12-dimethyl-2-[2-(1-naphthyl)acetyl]amino-5,8,13-trioxo-2,3,6,7,8,9,10,11,12,13,19,19a-dodecahydro-1H,5H-pyrrolo[2,1-c][1,4,7,12]benzoxatriazacyclopentadecine-11-carboxamide; (2S,11S,19aS)-15-fluoro-7,12-dimethyl-2-[2-(1-naphthyl)acetyl]amino-5,8,13-trioxo-N-(3-pyridinylmethyl)-2,3,6,7,8,9,10,11,12,13,19,19a-dodecahydro-1H,5H-pyrrolo[2,1-c][1,4,7,12]-benzoxatriazacyclopentadecine-11-carboxamide; N-[(4S,6S,10S)-14-methyl-6-[2-(2-naphthyl)acetyl]amino-9,15-dioxo-2-oxa-8,14-diazatricyclo[14.3.1.04,8]icosa-1(20),16,18-trien-10-yl]decanamide; N-[(4S,6S,10)-14-methyl-10-{[2-(2-naphthyl)acetyl]amino}-9,15-dioxo-2-oxa-8,14-diazatricyclo[14.3.1.04,8]icosa-1(20),16,18-trien-6-yl]-2-(2-naphthyl)acetamide; N-[(4S,6S,10S)-14-methyl-6-[2-(2-naphthyl)acetyl]amino-9,15-dioxo-2-oxa-8,14-diazatricyclo[14.3.1.04,8]icosa-1(20),16,18-trien-10-yl]-2-(1-naphthyl)acetamide; N-[(4S,6S,10S)-14-methyl-9,15-dioxo-10-[(3-toluidinocarbonyl)amino]-2-oxa-8,14-diazatricyclo[14.3.1.04,8]icosa-1(20),16,18-trien-6-yl]-2-(2-naphthyl)acetamide; N-[(4S,6S,10S)-10-([3-(dimethylamino)anilino]carbonylamino)-14-methyl-9,15-dioxo-2-oxa-8,14-diazatricyclo[14.3.1.04,8]icosa-1(20),16,18-trien-6-yl]-2-(2-naphthyl)acetamide; N-[(4S,6S,10S)-6-({[3-(dimethylamino)anilino]carbonyl}amino)-14-methyl-9,15-dioxo-2-oxa-8,14-diazatricyclo[14.3.1.04,8]icosa-1(20),16,18-trien-10-yl]-2-(2-naphthyl)acetamide; N-[(4S,6S,10S)-14-methyl-9,15-dioxo-6-[(3-phenylpropanoyl)amino]-2-oxa-8,14-diazatricyclo[14.3.1.04,8]icosa-1(20),16,18-trien-10-yl]decanamide; N-[(4S,6S,10S)-14-methyl-6-[(3-morpholinobenzoyl)amino]-9,15-dioxo-2-oxa-8,14-diazatricyclo[14.3.1.04,8]icosa-1(20),16,18-trien-10-yl]decanamide; N-[(4S,6S,10S)-6-({[3-(dimethylamino)anilino]carbonyl}amino)-14-methyl-9,15-dioxo-2-oxa-8,14-diazatricyclo[14.3.1.04,8]icosa-1(20),16,18-trien-10-yl]decanamide; N-[(4S,6S,10S)-6-({[3-(dimethylamino)anilino]carbonyl}amino)-14-methyl-9,15-dioxo-2-oxa-8,14-diazatricyclo[14.3.1.04,8]icosa-1(20),16,18-trien-10-yl]-2-(1-naphthyl)acetamide; N-[(4S,6S,10S)-6-{[(3-methoxyanilino)carbonyl]amino}-14-methyl-9,15-dioxo-2-oxa-8,14-diazatricyclo[14.3.1.04,8]icosa-1(20),16,18-trien-10-yl]-2-(2-naphthyl)acetamide; N-[(4S,6S,10S)-14-methyl-9,15-dioxo-6-{[2-(3-phenoxyphenyl)acetyl]amino}-2-oxa-8,14-diazatricyclo[14.3.1.04,8]icosa-1(20),16,18-trien-10-yl]decanamide; N-[(4S,6S,10S)-14-methyl-6-{[2-(2-naphthyl)acetyl]amino}-9,15-dioxo-2-oxa-8,14-diazatricyclo[14.3.1.04,8]icosa-1(20),16,18-trien-O1-yl]-6-phenylhexanamide; N-[(4S,6S,10S)-14-methyl-6-{[2-(2-naphthyl)acetyl]amino}-9,15-dioxo-2-oxa-8,14-diazatricyclo[14.3.1.04,8]icosa-1(20),16,18-trien-10-yl]-5-phenoxypentanamide; (E)-N-[(4S,6S,10S)-14-methyl-6-[2-(2-naphthyl)acetyl]amino-9,15-dioxo-2-oxa-8,14-diazatricyclo[14.3.1.04,8]icosa-1(20),16,18-trien-10-yl]-3-decanamide; N-[(4S,6S,10S)-14-methyl-6-{[2-(1-naphthyl)acetyl]amino}-9,15-dioxo-2-oxa-8,14-diazatricyclo[14.3.1.04,8]icosa-1(20),16,18-trien-10-yl]decanamide; 6-(benzyloxy)-N-[(4S,6S6S,10S)-14-methyl-6-[2-(2-naphthyl)acetyl]amino-9,15-dioxo-2-oxa-8,14-diazatricyclo[14.3.1.04,8]icosa-1(20),16,18-trien-10-yl]hexanamide; 2-[1,1′-biphenyl]-4-yl-N-[(4S,6S,10S)-14-methyl-6-{[2-(2-naphthyl)acetyl]amino}-9,15-dioxo-2-oxa-8,14-diazatricyclo[14.3.1.04,8]icosa-1(20),16,18-trien-10-yl]acetamide; N-[(4S,6S,10S)-14-methyl-6-{[2-(2-naphthyl)acetyl]amino}-9,15-dioxo-2-oxa-8,14-diazatricyclo[14.3.1.04,8]icosa-1(20),16,18-trien-10-yl]-3,3-diphenylpropanamide; 6-(benzyloxy)-N-[(4S,6S,10S)-14-methyl-9,15-dioxo-10-[(6-phenylhexanoyl)amino]-2-oxa-8,14-diazatricyclo[14.3.1.04,8]icosa-1(20),16,18-trien-6-yl]hexanamide; 2-[1,1′-biphenyl]-3-yl-N-[(4S,6S,10S)-6-([3-(dimethylamino)anilino]carbonylamino)-14-methyl-9,15-dioxo-2-oxa-8,14-diazatricyclo[14.3.1.04,8]icosa-1(20),16,18-trien-10-yl]acetamide; 2-[1,1′-biphenyl]-4-yl-N-[(4S,6S,10S)-6-([3-(dimethylamino)anilino]carbonylamino)-14-methyl-9,15-dioxo-2-oxa-8,14-diazatricyclo[14.3.1.04,8]icosa-1(20),16,18-trien-10-yl]acetamide; N-[(4S,6S,10S)-10-[([1,1′-biphenyl]-4-ylsulfonyl)amino]-14-methyl-9,15-dioxo-2-oxa-8,14-diazatricyclo[14.3.1.04,8]icosa-1(20),16,18-trien-6-yl]-2-(2-naphthyl)acetamide; N-[(4S,6S,10S)-6-{[(3-fluoroanilino)carbonyl]amino}-14-methyl-9,15-dioxo-2-oxa-8,14-diazatricyclo[14.3.1.04,8]icosa-1(20),16,18-trien-10-yl]-2-(2-naphthyl)acetamide; N-[(4S,6S,10S)-6-({[4-(dimethylamino)anilino]carbonyl}amino)-14-methyl-9,15-dioxo-2-oxa-8,14-diazatricyclo[14.3.1.04,8]icosa-1(20),16,18-trien-10-yl]-2-(2-naphthyl)acetamide; phenyl N-[(4S,6S,10S)-14-methyl-10-{[2-(2-naphthyl)acetyl]amino}-9,15-dioxo-2-oxa-8,14-diazatricyclo[14.3.1.04,8]icosa-1(20),16,18-trien-6-yl]carbamate; N-[(4S,6S,10S)-14-methyl-9,15-dioxo-6-[2-(7-quinolinyl)acetyl]amino-2-oxa-8,14-diazatricyclo[14.3.1.04,8]icosa-1(20),16,18-trien-10-yl]-2-(2-naphthyl)acetamide; N-[(4S,6S,105)-14-methyl-9,15-dioxo-6-{[2-(3-phenoxyphenyl)acetyl]amino}-2-oxa-8,14-diazatricyclo[14.3.1.04,8]icosa-1(20),16,18-trien-10-yl]-2-(2-naphthyl)acetamide; N-[(4S,6S,10S)-14-methyl-10-{[2-(2-naphthyl)acetyl]amino}-9,15-dioxo-2-oxa-8,14-diazatricyclo[14.3.1.04,8]icosa-1(20),16,18-trien-6-yl]decanamide; N-[(4S,6S,10S)-14-methyl-10-{[2-(1-naphthyl)acetyl]amino}-9,15-dioxo-2-oxa-8,14-diazatricyclo[14.3.1.04,8]icosa-1(20),16,18-trien-6-yl]decanamide; N-[(4S,6S,10S)-14-methyl-10-{[2-(1-naphthyl)acetyl]amino}-9,15-dioxo-2-oxa-8,14-diazatricyclo[14.3.1.04,8]icosa-1(20),16,18-trien-6-yl]hexanamide; 2-[1,1′-biphenyl]-4-yl-N-[(4S,6S,10S)-14-methyl-10-{[2-(1-naphthyl)acetyl]amino}-9,15-dioxo-2-oxa-8,14-diazatricyclo[14.3.1.04,8]icosa-1(20),16,18-trien-6-yl]acetamide; N-[(4S,6S,10S)-10-[(2-[1,1′-biphenyl]-4-ylacetyl)amino]-14-methyl-9,15-dioxo-2-oxa-8,14-diazatricyclo[14.3.1.04,8]icosa-1(20),16,18-trien-6-yl]-2,2-diphenylacetamide; N-[(4S,6S,10S)-6-[(2-[1,1′-biphenyl]-4-ylacetyl)amino]-14-methyl-9,15-dioxo-2-oxa-8,14-diazatricyclo[14.3.1.04,8]icosa-1(20),16,18-trien-10-yl]-2,2-diphenylacetamide; N-[(4S,6S,10S)-6-[(2,2-diphenylacetyl)amino]-14-methyl-9,15-dioxo-2-oxa-8,14-diazatricyclo[14.3.1.04,8]icosa-1(20),16,18-trien-10-yl]decanamide; N-[(4S,6S,10S)-14-methyl-10-{[2-(1-naphthyl)acetyl]amino}-9,15-dioxo-2-oxa-8,14-diazatricyclo[14.3.1.04,8]icosa-1(20),16,18-trien-6-yl]-2,2-diphenylacetamide; N-[(4S,6S,100S)-6-[(3,3-diphenylpropanoyl)amino]-14-methyl-9,15-dioxo-2-oxa-8,14-diazatricyclo[14.3.1.04,8]icosa-1(20),16,18-trien-10-yl]decanamide; 2-[1,1′-biphenyl]-4-yl-N-[(4S,6S,10S)-10-[(2-[1,1′-biphenyl]-4-ylacetyl)amino]-14-methyl-9,15-dioxo-2-oxa-8,14-diazatricyclo[14.3.1.04,8]icosa-1(20),16,18-trien-6-yl]acetamide; N-[(4S,6S,10S)-6-({[3-(dimethylamino)anilino]carbonyl}amino)-14-methyl-9,15-dioxo-2-oxa-8,14-diazatricyclo[14.3.1.04,8]icosa-1(20),16,18-trien-10-yl]-3,3-dimethylbutanamide; N-[(4S,6S,10S)-6-({[3-(dimethylamino)anilino]carbonyl}amino)-9,15-dioxo-2-oxa-8,14-diazatricyclo[14.3.1.04,8]icosa-1(20),16,18-trien-10-yl]-2-(2-naphthyl)acetamide; benzyl N-[(4S,6S,10S)-6-{[2-(2-naphthyl)acetyl]amino}-9,15-dioxo-2-oxa-8,14-diazatricyclo[14.3.1.04,8]icosa-1(20),16,18-trien-10-yl]carbamate; N-[(4S,6S,10S)-6-{[2-(2-naphthyl)acetyl]amino}-9,15-dioxo-2-oxa-8,14-diazatricyclo[14.3.1.04,8]icosa-1(20),16,18-trien-10-yl]decanamide; (4S,6R,15S)-11,16-dimethyl-N-(2-naphthylmethyl)-9,12,17-trioxo-6-{[3-(4-pyridinyl)propanoyl]amino}-2-thia-8,11,16-triazatricyclo[16.3.1.04,8]docosa-1(22),18,20-triene-15-carboxamide; tert-butyl N-[(4S,6R,15S)-11,16-dimethyl-15-{[(2-naphthylmethyl)amino]carbonyl}-9,12,17-trioxo-2-thia-8,11,16-triazatricyclo[16.3.1.04,8]docosa-1(22),18,20-trien-6-yl]carbamate; (4S,6R,15S)-11,16-dimethyl-N-(2-naphthylmethyl)-9,12,17-trioxo-6-(pentanoylamino)-2-thia-8,11,16-triazatricyclo[16.3.1.04,8]docosa-1(22),18,20-triene-15-carboxamide; (4S,6R,15S)-6-(acetylamino)-11,16-dimethyl-N-(2-naphthylmethyl)-9,12,17-trioxo-2-thia-8,11,16-triazatricyclo[16.3.1.04,8]docosa-1(22),18,20-triene-15-carboxamide; (2S,11S,19aS)-15-fluoro-7,12-dimethyl-2-(1-naphthoylamino)-N-(2-naphthylmethyl)-5,8,13-trioxo-2,3,6,7,8,9,10,11,12,13,19,19a-dodecahydro-1H,5H-pyrrolo[2,1-c][1,4,7,12]benzoxatriazacyclopentadecine-11-carboxamide; (2S,11S,19aS)-15-fluoro-7,12-dimethyl-2-[2-(2-naphthyl)acetyl]amino-N-(1-naphthylmethyl)-5,8,13-trioxo-2,3,6,7,8,9,10,11,12,13,19,19a-dodecahydro-1H,5H-pyrrolo[2,1-c][1,4,7,12]benzoxatriazacyclopentadecine-11-carboxamide; (2S,11S,19aS)-2-[(3-chlorobenzoyl)amino]-15-fluoro-7,12-dimethyl-N-(1-naphthylmethyl)-5,8,13-trioxo-2,3,6,7,8,9,10,11,12,13,19,19a-dodecahydro-1H,5H-pyrrolo[2,1-c][1,4,7,12]benzoxatriazacyclopentadecine-11-carboxamide.
- Claim: 9. Compounds according to claim 2, selected from: (2S,11S,19aS)-2-(acetylamino)-15-fluoro-N-[2-(1H-indol-3-yl)ethyl]-7,12-dimethyl-5,8,13-trioxo-2,3,6,7,8,9,10,11,12,13,19,19a-dodecahydro-1H,5H-pyrrolo[2,1-c][1,4,7,12]benzoxatriazacyclopentadecine-11-carboxamide; (2S,11S,19aS)—N-[2-(dimethylamino)ethyl]-15-fluoro-2-{[2-(1H-indol-3-yl)acetyl]amino}-7,12-dimethyl-5,8,13-trioxo-2,3,6,7,8,9,10,11,12,13,19,19a-dodecahydro-1H,5H-pyrrolo[2,1-c]-[1,4,7,12]benzoxatriazacyclopentadecine-11-carboxamide; (2S,11S,19aS)-15-fluoro-2-{[2-(1H-indol-3-yl)acetyl]amino}-N-[2-(1H-indol-3-yl)ethyl]-7,12-dimethyl-5,8,13-trioxo-2,3,6,7,8,9,10,11,12,13,19,19a-dodecahydro-1H,5H-pyrrolo[2,1-c][1,4,7,12]-benzoxatriazacyclopentadecine-11-carboxamide; (2S,11S,19aS)-2-{[2-(dimethylamino)acetyl]amino}-15-fluoro-N-[2-(1H-indol-3-yl)ethyl]-7,12-dimethyl-5,8,13-trioxo-2,3,6,7,8,9,10,11,12,13,19,19a-dodecahydro-1H,5H-pyrrolo[2,1-c]-[1,4,7,12]benzoxatriazacyclopentadecine-11-carboxamide; tert-butyl N-[(2S,11S,19aS)-15-fluoro-11-({[2-(1H-indol-3-yl)ethyl]amino}carbonyl)-7,12-dimethyl-5,8,13-trioxo-2,3,6,7,8,9,10,11,12,13,19,19a-dodecahydro-1H,5H-pyrrolo[2,1-c]-[1,4,7,12]benzoxatriazacyclopentadecin-2-yl]carbamate; (2S,11S,19aS)—N-[2-(dimethylamino)ethyl]-15-fluoro-7,12-dimethyl-2-{[2-(1-naphthyl)acetyl]amino}-5,8,13-trioxo-2,3,6,7,8,9,10,11,12,13,19,19a-dodecahydro-1H,5H-pyrrolo[2,1-c]-[1,4,7,12]benzoxatriazacyclopentadecine-11-carboxamide; benzyl N-[(4S,6S,10S)-14-methyl-6-{[2-(2-naphthyl)acetyl]amino}-9,15-dioxo-2-oxa-8,14-diazatricyclo[14.3.1.04,8]icosa-1(20),16,18-trien-10-yl]carbamate; benzyl N-[(4S,6S,13S)-6-{[2-(1H-indol-3-yl)acetyl]amino}-11,15-dimethyl-9,12,16-trioxo-2-oxa-8,11,15-triazatricyclo[15.3.1.04,8]henicosa-1(21),17,19-trien-13-yl]carbamate; N-[(4S,6S,13S)-6-{[2-(1H-indol-3-yl)acetyl]amino}-11,15-dimethyl-9,12,16-trioxo-2-oxa-8,11,15-triazatricyclo[15.3.1.04,8]henicosa-1(21),17,19-trien-13-yl]decanamide.
- Claim: 10. Compounds according to claim 1 for use as therapeutically active substances.
- Claim: 11. Compounds according to claim 10 for use as therapeutically active substances having agonistic or antagonistic activity on the motilin receptor (MR receptor), on the serotonin receptor of subtype 5-HT2B (5-HT2B receptor), on the prostaglandin F2α receptor (FP receptor), on the purinoreceptor P2Y1, on the voltage-gated potassium channel Kv11.3; or on the canonical (β-catenin-dependent) Wnt pathway.
- Claim: 12. A pharmaceutical composition containing a compound or a mixture of compounds according to any claim 1 and at least one therapeutically inert excipient.
- Claim: 13. A composition according to claim 12 containing a compound or a mixture of compounds according to claim 1, having agonistic or antagonistic activity on the motilin receptor (MR receptor), on the serotonin receptor of subtype 5-HT2B (5-HT2B receptor), on the prostaglandin F2α receptor (FP receptor), on the purinoreceptor P2Y1, on the voltage-gated potassium channel Kv1.3; or on the canonical (β-catenin-dependent) Wnt pathway.
- Claim: 14. A composition according to claim 12 suitable for oral, topical, transdermal, injection, buccal, transmucosal, pulmonary or inhalation administration, particularly in form of tablets, dragees, capsules, solutions, liquids, gels, plaster, creams, ointments, syrup, slurries, suspensions, spray, nebulizer or suppositories.
- Claim: 15. The use of compounds according to claim 1, having agonistic or antagonistic activity on the motilin receptor (MR receptor), on the serotonin receptor of subtype 5-HT2B (5-HT2B receptor), on the prostaglandin F2α receptor (FP receptor), on the purinoreceptor P2Y1, on the voltage-gated potassium channel Kv1.3; or on the canonical (β-catenin-dependent) Wnt pathway, for the manufacture of a medicament.
- Claim: 16. The use of compounds according to claim 1 for the manufacture of a medicament, wherein said medicament is intended for the treatment of motility disorders of the gastrointestinal tract such as functional dyspepsia, diabetic gastroparesis or constipation type irritable bowl syndrome; of CNS related diseases like migraine, schizophrenia, psychosis, depression or Alzheimer disease; of ocular hypertension such as associated with glaucoma and of preterm labour; of CNS inflammatory disorders like multiple sclerosis; of thromboembolic disorders; of cell proliferation disorders, especially various cancer types; or of bone and cartilage-related disorders.
- Claim: 17. The use of compounds according to claim 1 for pharmaceutical lead finding.
- Current U.S. Class: 514/250
- Current International Class: 07; 07; 61; 61; 61; 61; 61; 61; 61; 61; 61; 61; 61; 61
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