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- Nachgewiesen in: USPTO Patent Applications
- Sprachen: English
- Document Number: 20110263653
- Publication Date: October 27, 2011
- Appl. No: 13/053161
- Application Filed: March 21, 2011
- Claim: 1-47. (canceled)
- Claim: 48. A method for treating breast tumor metastasis in a subject comprising: administering to a subject in need thereof a therapeutically effective amount of a composition comprising a compound having one of the following structures: [chemical expression included] or pharmaceutically acceptable salt thereof; wherein R1 and R2 are hydrogen or lower alkyl; R3, R5 and R6 are C1-6 alkyl; the bond is a single bond or a double bond; R4 is halogen, —OR4A, —OC(═O)R4A or —NR4AR4B; wherein R4A and R4B are independently hydrogen; a nitrogen protecting group selected from a carbamate, an amide, a cyclic imide derivative, an N-alkyl amine, an N-aryl amine, an imine derivative or an enamine derivative or an oxygen protecting group selected from a substituted methyl ether, a substituted ethyl ether, a substituted benzyl ether, a silyl ether, an ester, a carbonate, a cyclic acetal or a ketal; or R4A and R4B, taken together with the nitrogen atom to which they are attached, form a C3-20 heterocyclic or C3-14 heteroaryl moiety; or R4, taken together with the carbon atom to which it is attached forms a moiety having the structure: [chemical expression included] or R4A and R4B are independently a C1-16 alkyl group optionally substituted with one or more of C1-20 aliphatic; C3-14 aryl; C3-14 heteroaryl; C1-20 alkylC3-14aryl; C1-20 alkylC3-14heteroaryl, C3-14 aryloxy; C1-20 heteroalkoxy, C3-14 heteroaryloxy; C1-20 alkylthio; C3-14 arylthio; heteroC1-20alkylthio; heteroC3-14arylthio; F; Cl; Br; I; —OH; —NO2; —CN; —CF3; —CH2CF3; —CHCl2; —CH2OH; —CH2CH2OH; —CH2NH2; —CH2SO2CH3; —C(O)Rx; —CO2(Rx); —CON(Rx)2; —OC(O)Rx; —OCO2Rx; —OCON(Rx)2; —N(Rx)2; S(O)2Rx; —NRx(CO)Rx wherein each occurrence of Rx is independently C1-20 aliphatic, heteroC1-20 aliphatic, C3-14 aryl, C3-14 heteroaryl, C1-20 alkylC3-14aryl or C1-20 alkylC3-14heteroaryl; X1 is O, S, NRX1 or CRX1RX2; wherein RX1 and RX2 are independently hydrogen, halogen, or a substituted or unsubstituted C1-20 alkyl, heteroC1-20alkyl, cycloC3-10alkyl, heterocyclo C3-10alkyl, C3-14 aryl or C3-14 heteroaryl, or a nitrogen protecting group selected from a carbamate, an amide, a cyclic imide derivative, an N-alkyl amine, an N-aryl amine, an imine derivative or an enamine derivative; Q is hydrogen, halogen, —CN, —S(O)1-2RQ1, —NO2, —CORQ1, —CO2RQ1, —NRQ1C(═O)RQ2, —NRQ1C(═O)ORQ2, —CONRQ1RQ2, or a substituted or unsubstituted C1-20 aliphatic, heteroC1-20 aliphatic, C3-20 alicyclic, heteroC3-20 alicyclic, C3-14 aryl or C3-14 heteroaryl moiety, or —WRQ1; wherein W is independently O, S or NRQ3 and each occurrence of RQ1, RQ2 and RQ3 is independently hydrogen, or a substituted or unsubstituted C1-20 aliphatic, heteroC1-20 aliphatic, C3-20 alicyclic, heteroC3-20 alicyclic, C3-14aryl or C3-14 heteroaryl moiety; Y2 is hydrogen, or a substituted or unsubstituted C1-20 alkyl, heteroC1-20alkyl, cyclo C3-10alkyl, heterocycloC3-10alkyl, C3-14aryl, or C3-14 heteroaryl moiety; or —WRY1; W is O or NH; and RY1 and RY2 are independently hydrogen, or a substituted or unsubstituted C1-20 aliphatic, heteroC1-20 aliphatic, C3-20 alicyclic, heteroC3-20 alicyclic, C3-14 aryl or C3-14 heteroaryl moiety; wherein for the compound of formula (a), when X1 is O and the bond is a double bond, Q is hydrogen, halogen, —CN, —S(O)1-2RQ1, —NO2, —CORQ1, —CO2RQ1, —NRQ1C(═O)RQ2, —NRQ1C(═O)ORQ2, —CONRQ1RQ2, or —WRQ1; wherein W is independently O, S or NRQ3 and each occurrence of RQ1, RQ2 and RQ3 is independently hydrogen, or a substituted or unsubstituted C1-20 aliphatic, heteroC1-20 aliphatic, C3-20 alicyclic, heteroC3-20 alicyclic, C3-14aryl or C3-14 heteroaryl moiety; wherein the composition is administered at a dose corresponding to a dose in a mouse that is between about 10 mg/kg and about 20 mg/kg.
- Claim: 49-57. (canceled)
- Claim: 58. The method of claim 48 wherein in the composition, the compound has one of the following structures: [chemical expression included]
- Claim: 59. (canceled)
- Claim: 60. The method of claim 48, further comprising administering a cytotoxic agent.
- Claim: 61. The method of claim 60, wherein the cytotoxic agent is an anticancer agent.
- Claim: 62. The method of claim 48, further comprising administering a palliative agent.
- Claim: 63. The method of claim 48, wherein in the composition the compound has one of the following structures: [chemical expression included] or pharmaceutically acceptable salt thereof.
- Claim: 64. The method of claim 63, wherein in the compound of the composition R1 and R2 are each hydrogen.
- Claim: 65. The method of claim 63, wherein in the compound of the composition R5 and R6 are each methyl.
- Claim: 66. The method of claim 63, wherein in the compound of the composition R3 is lower alkyl.
- Claim: 67. The method of claim 66, wherein in the compound of the composition R3 is methyl.
- Claim: 68. The method of claim 63, wherein in the compound of the composition R4 is OH.
- Claim: 69. The method of claim 63, wherein in the compound of the composition Y2 is lower alkyl and RY1 is hydrogen or lower alkyl.
- Claim: 70. The method of claim 63, wherein in the compound of the composition RY1 is hydrogen and Y2 is CF3.
- Claim: 71. The method of claim 63, wherein in the composition the compound has the structure: [chemical expression included] or a pharmaceutically acceptable salt thereof, wherein n is 3; Y2 is lower alkyl substituted with one or more halogen atoms selected from F, Cl, Br and I, and RY1 is hydrogen or lower alkyl.
- Claim: 72. The method of claim 71, wherein RY1 is hydrogen and Y2 is CF3.
- Claim: 73. The method of claim 63, wherein in the composition the compound has one of the following structures: [chemical expression included] or a pharmaceutically acceptable salt thereof, wherein Y2 is lower alkyl substituted with one or more halogen atoms selected from F, Cl, Br and I, and RY1 is hydrogen or lower alkyl.
- Claim: 74. The method of claim 73, wherein RY1 is hydrogen and Y2 is CF3.
- Claim: 75. A method for treating breast tumor metastasis in a subject comprising: administering to a subject in need thereof a therapeutically effective amount of a composition comprising a compound having the following structure: [chemical expression included] or a pharmaceutically acceptable salt thereof; wherein X1 is CH2, NH or O; Y1 and Y2 are independently OH, C(RY)3 or Y1 and Y2 taken together with the carbon atom to which they are attached are —C═O, wherein RY is halo; the bond is a single bond or a double bond; R6 is H or lower alkyl; R5 is H or lower alkyl; R4 is OH; and R3 is lower alkyl; wherein the composition is administered at a dose corresponding to a dose in a mouse that is between about 10 mg/kg and about 20 mg/kg.
- Current U.S. Class: 514/337
- Current International Class: 61; 61; 61
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