摘要:
The invention relates to compounds of formula (I): in which R1, R2, L1, X, R3, A, R4, R4′, R4″, R4″′, R5, Y and L2 are as herein defined, salts and prodrugs thereof, to their use as protein kinase inhibitors, and to methods of treating diseases comprising adminstration thereof.
摘要:
The invention relates to compounds of formula (I): in which R1, R2, L1, X, R3, A, R4, R4′, R4″, R4″′, R5, Y and L2 are as herein defined, salts and prodrugs thereof, to their use as protein kinase inhibitors, and to methods of treating diseases comprising adminstration thereof.
摘要:
The disclosure relates to a cyclic urea compound of formula I: as defined herein, to the process for its preparation, pharmaceutical composition comprising it and its pharmaceutical use as an inhibitor on a protein kinase. Thus, the compound of formula I is useful for preventing or treating a physiological disorder capable of being modulated by inhibiting the activity of a protein kinase, such as a solid tumor.
摘要:
The present invention relates to a cyclic urea compound of formula I: as defined herein. The invention is also directed to the process for its preparation, pharmaceutical composition comprising it and its pharmaceutical use, as an inhibitor on a protein kinase. Thus, it is useful for preventing or treating a physiological disorder capable of being modulated by inhibiting the activity of a protein kinase, such as a solid tumor.
摘要:
The disclosure relates to the novel compounds of formula (I): wherein R1, R2, R2′, R3, R3′, p, A, B, Y, Y1, and Y2 have the meanings given in the description, and to salts thereof, pharmaceutical compositions comprising said compounds and use thereof as protein kinase inhibitors.
摘要:
The disclosure relates to compounds of formula (I): wherein Y, Y1, Yo, R1, R2, R2′, p, R3, R3′, A, B and Y2 have the meanings given in the description, and to salts thereof, pharmaceutical compositions comprising said compounds and use thereof as protein kinase inhibitors.
摘要:
Compounds of formula (I): wherein R1, R2, R3, R4, and R5 have the meanings given in the description, and to salts thereof, pharmaceutical compositions comprising said compounds and the use thereof as protein kinase inhibitors.
摘要:
The present invention relates to novel derivatives of general formula (I) in which R3 is a (1–6C)alkyl, aryl, aryl(1–6C)alkyl, heteroaryl, heteroaryl(1–6C)alkyl, aryl or heteroaryl fused to a (1–10C)cycloalkyl, heterocycle, heterocycloalkyl, cycloalkyl, adamantyl, polycycloalkyl, alkenyl, alkynyl, CONR1R2, COOR1, SO2R1, C(═NH)R1 or C(═NH)NR1 radical; R5 and R6 are, independently of one another, chosen from the following radicals: halogen, CN, NO2, NH2, OH, COOH, C(O)OR8, —O—C(O)R8, NR8R9, NHC(O)R8, C(O)NR8R9, NHC(S)R8, C(S)NR8R9, SR8, S(O)R8, SO2R8, NHSO2R8, SO2NR8R9, —O—SO2R8, —SO2—O—R8, trifluoromethyl, trifluoromethoxy, (1–6C)alkyl, (1–6C)alkoxy, aryl, aryl(1–6C)alkyl, heteroaryl, heteroaryl(1–6C)alkyl, heterocycle, cycloalkyl, alkenyl, alkynyl, adamantyl or polycycloalkyl.
摘要翻译:本发明涉及通式(I)的新型衍生物,其中R3是(1-6C)烷基,芳基,芳基(1-6C)烷基,杂芳基,杂芳基(1-6C)烷基,芳基或杂芳基 (1-10C)环烷基,杂环,杂环烷基,环烷基,金刚烷基,多环烷基,烯基,炔基,CONR1R2,COOR1,SO2R1,C(-NH)R1或C(-NH)NR1 激进; R 5和R 6彼此独立地选自以下基团:卤素,CN,NO 2,NH 2,OH,COOH,C(O)OR 8, -OC(O)R8,NR8R9,NHC(O)R8,C(O)NR8R9,NHC(S)R8,C(S)NR8R9,SR8,S(O) R 8,NHSO 2 R 8,SO 2 NR 8 R 9,-O-SO 2 R 8,-SO 2 -O (1-6C)烷氧基,芳基,芳基(1-6C)烷基,杂芳基,杂芳基(1-6C)烷基,杂环,环烷基,链烯基,炔基,金刚烷基 或多环烷基。
摘要:
Novel compounds of the formula ##STR1## wherein the substituents are defined as in the application and their salts with non-toxic, pharmaceutically acceptable acids and bases having 5-.alpha.-reductase inhibiting activity and a process and intermediates for their preparation.
摘要:
The present invention relates to the use of novel derivatives of general formula (I) in which R3 is a (1-6C)alkyl, aryl, aryl(1-6C)alkyl, heteroaryl, heteroaryl(1-6C)alkyl, aryl or heteroaryl fused to a (1-10C) cycloalkyl, heterocycle, heterocycloalkyl, cycloalkyl, adamantyl, polycycloalkyl, alkenyl, alkynyl, CONR1R2, COOR1, SO2R1, C(═NH)R1 or C(═NH)NR1 radical; R5, R6 and R7 are, independently of one another, chosen from the following radicals: halogen, CN, NO2, NH2, OH, OR8, COOH, C(O)OR8, —O—C(O)R8, NR8R9, NHC(O)R8, C(O)NR8R9, NHC(S)R8, C(S)NR8R9, SR8, S(O)R8, SO2R8, NHSO2R8, SO2NR8R9, —O—SO2R8, —SO2—O—R8, trifluoromethyl, trifluoromethoxy, (1-6C)alkyl, (1-6C)alkoxy, aryl, aryl(1-6C)alkyl, heteroaryl, heteroaryl(1-6C)alkyl, heterocycle, cycloalkyl, alkenyl, alkynyl, adamantyl or polycycloalkyl, to treat a disease selected from the group consisting of: neurodegenerative diseases, strokes, cranial and spinal traumas and peripheral neuropathies, obesity, metabolic diseases, type II diabetes, essential hypertension, atherosclerotic cardiovascular diseases, polycystic ovaries syndrome, syndrome X, immunodeficiency and cancer.
摘要翻译:本发明涉及通式(I)的新型衍生物,其中R3是(1-6C)烷基,芳基,芳基(1-6C)烷基,杂芳基,杂芳基(1-6C)烷基,芳基或 与(1-10C)环烷基,杂环,杂环烷基,环烷基,金刚烷基,多环烷基,烯基,炔基,CONR1R2,COOR1,SO2R1,C(-NH)R1或C( - NH)NR1基; R 5,R 6和R 7彼此独立地选自以下基团:卤素,CN,NO 2,NH 2,OH,OR 8,COOH,C( O)OR 8,-OC(O)R 8,NR 8 R 9,NHC(O)R 8,C(O)NR 8 R 9,NHC(S)R 8,C(S)NR 8 R 9,SR 8,S(O)R 8,SO 2 R 8,NHSO 2 R 8,SO 2 NR 8 R 9,-O-SO 2 R 8,-SO 2, (1-6C)烷氧基,芳基,芳基(1-6C)烷基,杂芳基,杂芳基(1-6C)烷基,杂环,环烷基,烯基 ,炔基,金刚烷基或多环烷基,以治疗选自以下的疾病:神经变性疾病,中风,颅脑和脊髓创伤和周围神经病变,肥胖症,代谢疾病,II型糖尿病,原发性高血压,动脉粥样硬化心血管疾病,多囊卵巢综合征 ,综合征X,免疫缺陷和癌症。