Compounds for treatment of cancer
AssigneesGTx, Inc., University of Tennessee
InventorsYan Lu, Chien-Ming Li, Zhao Wang, Jianjun Chen, Wei Li, James T. Dalton, Duane D. Miller, Charles Duke, Sunjoo Ahn
Life of this patent
Estimating the term…
Abstract
The present invention relates to novel compounds having anti-cancer activity, methods of making these compounds, and their use for treating cancer and drug-resistant tumors, e.g. melanoma, metastatic melanoma, drug resistant melanoma, prostate cancer and drug resistant prostate cancer.
Claims63
A compound represented by the structure of formula (Ia):
- A is substituted or unsubstituted single-, fused- or multiple-ring, aryl or (hetero)cyclic ring systems;
- substituted or unsubstituted, saturated or unsaturated N-heterocycles;
- substituted or unsubstituted, saturated or unsaturated S-heterocycles;
- substituted or unsubstituted, saturated or unsaturated O-heterocycles;
- substituted or unsubstituted, saturated or unsaturated cyclic hydrocarbons;
- or substituted or unsubstituted, saturated or unsaturated mixed heterocycles;
- B is
- R1, R2 and R3 are independently hydrogen, O-alkyl, O-haloalkyl, F, Cl, Br, I, CF3, CN, —CH2CN, NH2, hydroxyl, —(CH2)iNHCH3, —(CH2)iNH2, —(CH2)iN(CH3)2, —OC(O)CF3, C1-C5 linear or branched alkyl, haloalkyl, alkylamino, aminoalkyl, —OCH2Ph, —NHCO-alkyl, COOH, —C(O)Ph, C(O)O-alkyl, C(O)H, —C(O)NH2 or NO2;
- R10 and R11 are independently hydrogen, O-alkyl, O-haloalkyl, F, Cl, Br, I, CF3, CN, —CH2CN, NH2, hydroxyl, —(CH2)iNHCH3, —(CH2)iNH2, —(CH2)iN(CH3)2, —OC(O)CF3, C1-C5 linear or branched alkyl, haloalkyl, alkylamino, aminoalkyl, —OCH2Ph, —NHCO-alkyl, COOH, —C(O)Ph, C(O)O-alkyl, C(O)H, —C(O)NH2 or NO2;
- X is a bond, NH, C1 to C5 hydrocarbon, O, or S;
- Y is a bond, —C═O, —C═S, —C═N—NH2, —C═N—OH, —CH—OH, —C═CH—CN,
- C═N—CN, —CH═CH—, —C═C(CH3)2, —C═N—OMe, —(C═O)—NH, —NH—(C═O), —(C═O)—O, —O—(C═O), —(CH2)1-5—(C═O), (C═O)—(CH2)1-5, —(SO2)—, SO2, SO or S;
- wherein said A and B rings are optionally substituted by 1-5 substituents which are independently O-alkyl, O-haloalkyl, F, Cl, Br, I, CF3, CN, —CH2CN, NH2, hydroxyl, —(CH2)iNHCH3, —(CH2)iNH2, —(CH2)iN(CH3)2, —OC(O)CF3, C1-C5 linear or branched alkyl, haloalkyl, alkylamino, aminoalkyl, —OCH2Ph, —NHCO-alkyl, COOH, —C(O)Ph, C(O)O-alkyl, C(O)H, —C(O)NH2 or NO2;
- i is an integer between 0-5;
- l is an integer between 1-2;
- m is an integer between 1-3;
- and
- wherein if B is a benzene ring, a thiophene ring, a furan ring or an indole ring then X is not a bond or CH2 and A is not indole;
- if B is indole then X is not O;
- and
- if B is a thiazole ring then X is not a bond.
(canceled)
(canceled)
(canceled)
(canceled)
(canceled)
(canceled)
(canceled)
(canceled)
(canceled)
(canceled)
(canceled)
(canceled)
The method according to 35, wherein said administering is carried out in combination with another cancer therapy.
(canceled)
A compound represented by the structure of formula IX:
- R4 and R5 are independently selected from hydrogen, O-alkyl, O-haloalkyl, F, Cl, Br, I, CF3, CN, —CH2CN, NH2, hydroxyl, —(CH2)iNHCH3, —(CH2)iNH2, —(CH2)iN(CH3)2, —OC(O)CF3, C1-C5 linear or branched alkyl, haloalkyl, alkylamino, aminoalkyl, —OCH2Ph, —NHCO-alkyl, COOH, —C(O)Ph, C(O)O-alkyl, C(O)H, —(O)NH2 or NO2;
- A′ is substituted or unsubstituted single-, fused- or multiple-ring, aryl or (hetero)cyclic ring systems, including saturated and unsaturated N-heterocycles, saturated and unsaturated S-heterocycles, and saturated and unsaturated O-heterocycles, saturated or unsaturated cyclic hydrocarbons, saturated or unsaturated mixed heterocycles or aliphatic straight- or branched-chain C1 to C30 hydrocarbons;
- wherein said A′ ring is optionally substituted by 1-5 substituents which are independently O-alkyl, O-haloalkyl, F, Cl, Br, CF3, CN, —CH2CN, NH2, hydroxyl, —(CH2)iNHCH3, —(CH2)iNH2, —(CH2)iN(CH3)2, —OC(O)CF3, C1-C5 linear or branched alkyl, haloalkyl, alkylamino, aminoalkyl, —OCH2Ph, —NHCO-alkyl, COOH, —C(O)Ph, C(O)O-alkyl, C(O)H, —C(O)NH2 or NO2;
- i is an integer from 0-5;
- and
- n is an integer between 1-3.
(canceled)
(canceled)
(canceled)
(canceled)
(canceled)
(canceled)
(canceled)
(canceled)
(canceled)
(canceled)
(canceled)
The method according to 57, wherein said administering is carried out in combination with another cancer therapy.
(canceled)
Dependencies are inferred from the claim text.