摘要:
A compound selected from those of formula (I): wherein: X and Y represent a group selected from hydrogen, halogen, alkoxy, nitro, cyano, alkyl, alkenyl, polyhaloalkyl and —NRaRb wherein Ra and Rb are as defined in the description, Z represents oxygen or NRc wherein Rc is as defined in the description, Ar represents aryl or heteroaryl, R1 represents hydrogen or alkyl, R2 represents a group selected from hydrogen, alkyl, —ORa and —NRaRb wherein Ra and Rb are as defined in the description, R3 and R4 represent hydrogen or alkyl, R5 represents hydrogen, ORc, NRcRd, W1—C(W2)—U—V, W1—C(W2)—W3-T1 or Z-CO—CH═CHAr wherein Rc, Rd, W1, W2, W3, U, V, T, Z and Ar are as defined in the description, its isomers, 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,烷氧基,硝基,氰基,烷基,烯基,多卤代烷基和-NR a R 其中R a a和R b b如说明书中所定义,Z表示氧或NR C c,其中R - >如说明书中所定义,Ar表示芳基或杂芳基,R 1表示氢或烷基,R 2表示选自氢,烷基 其中R a a和R b都是 - , - - - - - - - - >如说明书中所定义,R 3和R 4代表氢或烷基,R 5表示氢,或C 1-4烷基, R 1,R 2,R 2,R 2,R 2,R 2, (W 2)-W 3 -T 1或Z-CO-CH-CHAr其中R R 1,R 2,W 3,W 2,W 3,U 3, ,V,T,Z和Ar定义如下 在其描述中,其异构体及其与药学上可接受的酸或碱的加成盐,以及含有该物质的药物可用于治疗癌症。
摘要:
A compound selected from those of formula (I): wherein: B1, B2 represent carbon or nitrogen, X, Y, X1 and Y1 represent a group selected from hydrogen, halogen, hydroxy, alkoxy, nitro, cyano, trihaloalkyl and NRaRb wherein Ra and Rb are as defined in the description, R1 represents hydrogen or alkyl, R2 represents a group selected from hydrogen, alkyl, —OR″a, —NR′aR′b, —O-Ta-OR″a, —NR″a-Ta-NR′aR′b, NR″a—C(O)-TaH, —O—C(O)-TaH, —O-Ta-NRa′Rb′, —NR″a-Ta-OR″a, —NR″a-Ta-CO2R″a and —NR″a—C(O)-Ta-NR′aR′b wherein R′a, R′b, R″a and Ta are as defined in the description, R3, R4 represent hydrogen or alkyl, A represents a group of formula —CH(R5)—CH(R6)—, —CH═C(R7)—, —C(R7)═CH—, —C(O)—CH(R8)— or —CH(R8)—C(O)— wherein R5, R6, R7 and R8 are as defined in the description, its isomers, 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:
A compound selected from those of formula (I): wherein: X and Y represent a group selected from hydrogen, halogen, hydroxy, alkoxy, nitro, cyano, alkyl, trihaloalkyl and NRaRb, wherein Ra and Rb are as defined in the description R1 represents hydrogen or alkyl R2 represents a group selected from hydrogen, alkyl, —OR″a, —NR′aR′b, —O-Ta-OR″a, —NR″a-Ta-NR′aR′b, —NR″a—C(O)-TaH, —O—C(O)-TaH, —O-Ta-NR′aR′b, —NR″a-Ta-OR″a, —NR″a-Ta-CO2R″a and —NR″a—C(O)-Ta-NR′aR′b, wherein R′a, R″a, R′b and Ta are as defined in the description R3 and R4 represent hydrogen or alkyl A represents a group of formula —CH(R5)—CH(R6)—, —CH═C(R7)—, —C(R7)═CH—, —C(O)—CH(R8) or —CH(R8)—C(O), wherein R5, R6, R7 and R8 are as defined in the description its isomers, 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:
A compound selected from those of formula (I): wherein: X and Y represent a group selected from hydrogen, halogen, alkoxy, nitro, cyano, alkyl, alkenyl, polyhaloalkyl and —NRaRb wherein Ra and Rb are as defined in the description, Z represents oxygen or NRc wherein Rc is as defined in the description, Ar represents aryl or heteroaryl, R1 represents hydrogen or alkyl, R2 represents a group selected from hydrogen, alkyl, —ORa and —NRaRb wherein Ra and Rb are as defined in the description, R3 and R4 represent hydrogen or alkyl, R5 represents hydrogen, ORc, NRcRd, W1—C(W2)—U—V, W1—C(W2)—W3-T1 or Z-CO—CH═CHAr wherein Rc, Rd, W1, W2, W3, U, V, T, Z and Ar are as defined in the description, its isomers, 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,烷氧基,硝基,氰基,烷基,烯基,多卤代烷基和-NR a R 其中R a a和R b b如说明书中所定义,Z表示氧或NR C c,其中R - >如说明书中所定义,Ar表示芳基或杂芳基,R 1表示氢或烷基,R 2表示选自氢,烷基 其中R a a和R b都是 - , - - - - - - - - >如说明书中所定义,R 3和R 4代表氢或烷基,R 5表示氢,或C 1-4烷基, R 1,R 2,R 2,R 2,R 2,R 2, (W 2)-W 3 -T 1或Z-CO-CH-CHAr其中R R 1,R 2,W 3,W 2,W 3,U 3, ,V,T,Z和Ar定义如下 在其描述中,其异构体及其与药学上可接受的酸或碱的加成盐,以及含有该物质的药物可用于治疗癌症。
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。
摘要:
A compound of formula (I): wherein: R represents hydrogen, optionally substituted alkyl or alkenyl, R1 to R8, which may be identical or different, each represents hydrogen, optionally substituted alkyl, hydroxy, acyloxy, optionally substituted amino, carboxy, optionally substituted alkoxy, or alkenyloxy, or one of R1 to R8 forms, with another of R1 to R8 that is adjacent, an alkylenedioxy group, X represents oxygen or NR16 wherein R16 represents hydrogen, alkyl, aryl or arylalkyl, R9 represents hydrogen, aryl, heteroaryl, or optionally substituted, saturated or unsaturated alkyl, an isomer thereof, or an addition salt thereof with a pharmaceutically acceptable acid or base. Medicinal products containing the same which are useful as anti-cancer agents.
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.
摘要:
A compound selected from those of formula (I): wherein: B1, B2 represent carbon or nitrogen, X, Y, X1 and Y1 represent a group selected from hydrogen, halogen, hydroxy, alkoxy, nitro, cyano, trihaloalkyl and NRaRb wherein Ra and Rb are as defined in the description, R1 represents hydrogen or alkyl, R2 represents a group selected from hydrogen, alkyl, —OR″a, —NR′aR′b, —O-Ta-OR″a, —NR″a-Ta-NR′aR′b, NR″a—C(O)-TaH, —O—C(O)-TaH, —O-Ta-NRa′Rb′, —NR″a-Ta-OR″a, —NR″a-Ta-CO2R″a and —NR″a—C(O)-Ta-NR′aR′b wherein R′a, R′b, R″a and Ta are as defined in the description, R3, R4 represent hydrogen or alkyl, A represents a group of formula —CH(R5)—CH(R6)—, —CH═C(R7)—, —C(R7)═CH—, —C(O)—CH(R8)— or —CH(R8)—C(O)— wherein R5, R6, R7 and R8 are as defined in the description, its isomers, 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:
The invention relates to compounds of formula (I), wherein R1 is a group selected from hydrogen, alkyl, aryl, aryalkil, heteroaryl, heteroarylalkyl, alkylcarbonyl, arylcarbonyl, arylalkylcarbonyl, alkoxycarbonyl, aryloxycarbonyl, arylalkoxycarbonyl, heterocycloalkoxycarbonyl, alkylsulfonyl, arylsulfonyl, arylalkylsulfonyl, phosphonic and Si(Ra)2Rb, Y is a group selected from HN—NH and N—R2, R3 is a hydrogen atom, an alkyl, cycloalkyl, aryl, arylalkyl group, R4 is hydrogen atom or an alkyl group, enantiomers, diastereoisomers and the salts thereof
摘要翻译:本发明涉及式(I)化合物,其中R 1是选自氢,烷基,芳基,芳亚烷基,杂芳基,杂芳基烷基,烷基羰基,芳基羰基,芳基烷基羰基,烷氧基羰基,芳氧基羰基,芳基烷氧基羰基, 杂环烷氧基羰基,烷基磺酰基,芳基磺酰基,芳基烷基磺酰基,膦酸和Si(R a)2 R b,Y是选自HN-NH和NR 2 R 3是氢原子,烷基,环烷基,芳基,芳基烷基,R 4是氢原子或烷基,对映异构体,非对映异构体及其盐
摘要:
The invention relates to compounds of formula (I), wherein R1 is a group selected from hydrogen, alkyl, aryl, aryalkil, heteroaryl, heteroarylalkyl, alkylcarbonyl, arylcarbonyl, arylalkylcarbonyl, alkoxycarbonyl, aryloxycarbonyl, arylalkoxycarbonyl, heterocycloalkoxycarbonyl, alkylsulfonyl, arylsulfonyl, arylalkylsulfonyl, phosphonic and Si(Ra)2Rb, Y is a group selected from HN—NH and N—R2, R3 is a hydrogen atom, an alkyl, cycloalkyl, aryl, arylalkyl group, R4 is hydrogen atom or an alkyl group, enantiomers, diastereoisomers and the salts thereof.
摘要翻译:本发明涉及式(I)化合物,其中R 1是选自氢,烷基,芳基,芳亚烷基,杂芳基,杂芳基烷基,烷基羰基,芳基羰基,芳基烷基羰基,烷氧基羰基,芳氧基羰基,芳基烷氧基羰基, 杂环烷氧基羰基,烷基磺酰基,芳基磺酰基,芳基烷基磺酰基,膦酸和Si(R a)2 R b,Y是选自HN-NH和NR 2 R 3是氢原子,烷基,环烷基,芳基,芳基烷基,R 4是氢原子或烷基,对映异构体,非对映异构体及其盐 。