公开(公告)号：US07056929B2

公开(公告)日：2006-06-06

申请号：US10627463

申请日：2003-07-26

申请人： Michel Koch ,  Francois Tillequin ,  Sylvie Michel ,  Elisabeth Seguin ,  Abdelhakim El Omri ,  John Hickman ,  Alain Pierre ,  Bruno Pfeiffer ,  Pierre Renard

发明人： Michel Koch ,  Francois Tillequin ,  Sylvie Michel ,  Elisabeth Seguin ,  Abdelhakim El Omri ,  John Hickman ,  Alain Pierre ,  Bruno Pfeiffer ,  Pierre Renard

IPC分类号： A61K31/44

CPC分类号： C07D491/04

摘要： A method for treating a living body afflicted with a cancer selected from lung and ovarian carcinoma, comprising the step of administering to the living animal body an amount of a compound selected from those of formula (I): wherein: X and Y represent group selected from hydrogen, halogen, mercapto, cyano, nitro, alkyl, trihaloalkyl, trihaloalkylcarbonylamino, —ORa, —NRaRb, —NRa—C(O)-T1, —O—C(O)-T1, —O-T2-NRaRb, —O-T2-ORa, —NRa-T2-NRaRb, —NRa-T2-ORa and —NRa-T2-CO2Ra wherein Ra, Rb, T1, T2 are as defined in the description, or X and Y together form a methylenedioxy or ethylenedioxy, R1 represents hydrogen or alkyl, R2 represents a group selected from hydrogen, —ORa, —NRaRb, —NRa—C(O)-T1, —O—C(O)-T1, —O-T2-NRaRb, —O-T2-ORa, —NRa-T2-NRaRb, —NRa-T2-ORa and —NRa-T2-CO2Ra wherein Ra, Rb, T1 and T2 are as defined hereinbefore, R3 and R4 represent hydrogen or alkyl, W represents a group of formula —CH(R5)—CH(R6)—, —CH═C(R7)—, —C(R7)═CH— or —C(O)—CH(R8)— wherein R5, R6, R7 and R8 are as defined in the description, their isomers and N-oxides, and addition salts thereof with a pharmaceutically acceptable acid or base, and medicinal products containing the same are useful in the treatment of cancer.

公开(公告)号：US06642248B2

公开(公告)日：2003-11-04

申请号：US10205566

申请日：2002-07-25

申请人： Michel Koch ,  François Tillequin ,  Sylvie Michel ,  Elisabeth Seguin ,  Abdelhakim El Omri ,  John Hickman ,  Alain Pierre ,  Bruno Pfeiffer ,  Pierre Renard

发明人： Michel Koch ,  François Tillequin ,  Sylvie Michel ,  Elisabeth Seguin ,  Abdelhakim El Omri ,  John Hickman ,  Alain Pierre ,  Bruno Pfeiffer ,  Pierre Renard

IPC分类号： A61K314741

CPC分类号： C07D491/04

摘要： A compound selected from those of formula (I): wherein: X and Y represent group selected from hydrogen, halogen, mercapto, cyano, nitro, alkyl, trihaloalkyl, trihaloalkylcarbonylamino, —ORa, —NRaRb, —NRa—C(O)—T1, —O—C(O)—T1, —O—T2-NRaRb, —O—T2-ORa, —NRa—T2-NRaRb, —NRa—T2-ORa and —NRa—T2-CO2Ra wherein Ra, Rb, T1, T2 are as defined in the description, R1 represents hydrogen or alkyl, R2 represents a group selected from hydrogen, —ORa, —NRaRb, —NRa—C(O)—T1, —O—C(O)—T1, —O—T2-NRaRb, —O—T2-ORa, —NRa—T2-NRaRb, —NRa—T2-ORa and —NRa—T2-CO2Ra wherein Ra, Rb, T1 and T2 are as defined hereinbefore, R3 and R4 represent hydrogen or alkyl, W represents a group of formula —CH(R5)—CH(R6)—, —CH═C(R7)—, —C(R7)═CH— or —C(O)—CH(R8)— wherein R5, R6, R7 and R8 are as defined in the description, their isomers and N-oxides, and addition salts thereof with a pharmaceutically acceptable acid or base, and medicinal products containing the same which are useful in the treatment of cancer.

摘要翻译： 选自式（I）的化合物：其中：X和Y表示选自氢，卤素，巯基，氰基，硝基，烷基，三卤代烷基，三卤代烷基羰基氨基，-OR a，-NR a R b，-NR a -C（O） - T1，-OC（O）-T1，-O-T2-NRaRb，-O-T2-ORa，-NRa-T2-NRaRb，-NRa-T2-ORa和-NRa-T2-CO2Ra，其中Ra，Rb，T1 ，T 2如说明书中所定义，R 1表示氢或烷基，R 2表示选自氢，-OR a，-NR a R b，-NR a -C（O）-T1，-OC（O）-T1，-O- R2-NRaRb，-O-T2-ORa，-NRa-T2-NRaRb，-NRa-T2-ORa和-NRa-T2-CO2Ra，其中Ra，Rb，T1和T2如上所定义，R3和R4代表氢或 烷基，W表示式-CH（R 5）-CH（R 6） - ， - CH = C（R 7） - ， - C（R 7）= CH-或-C（O）-CH（R 8） R5，R6，R7和R8如说明书中所定义，它们的异构体和N-氧化物及其与药学上可接受的酸或碱的加成盐，以及含有它们的药物，可用于治疗癌症。