摘要:
Compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, A, D, X, Y and Z have the meaning as defined in the claims exhibit protein tyrosine kinase and protein serin/threonine kinase inhibitory activity.
摘要:
Compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, A, D, X, Y and Z have the meaning as defined in the claims exhibit protein tyrosine kinase and protein serin/threonine kinase inhibitory activity.
摘要:
Compounds of general formula (I) wherein: R1 is H or optionally joined with R2 to form a fused ring selected from the group consisting of five to ten membered aryl, heteroaryl or heterocyclyl rings, R2 and R3 are independently H, HET, aryl, C1-12 aliphatic, CN, NO2, halogen, R10, —OR10, —SR10, —S(O)R10, —SO2R10, —NR10R11, —NR11R12, —NR12COR11, —NR12CO2R11, —NR12CONR11R12, —NO12SO2R11, —NR12C(NR 12)NHR11, —COR11, —CO2R11, —CONR12R11, —SO2NR12R11, —OCONR12R11, C(NR12)NR12R11, R6 and R7 are independently halogen, CN, NO2, —CONR10R11, —SO2NR10R11, —NR10R11, or —OR11, where R10 and R11 are as defined below; R8 is OH, NHSO2R12 or NHCOCF3; and their use in therapy, especially in the treatment of disorders mediated by cRaf1 kinase.
摘要翻译:通式(I)的化合物,其中:R 1为H或任选地与R 2连接形成选自5至10元芳基,杂芳基或杂环基环的稠环,R 2和R 3独立地为H,HET,芳基, C 12-12脂族基,CN,NO 2,卤素,R 10,-OR 10,-SR 10,-S(O)R 10,-SO 2 R 10,-NR 10 R 11,-NR 11 R 12,-NR 12 COR 11,-NR 12 CO 2 R 11,-NR 12 CONR 11 R 12,-NO 12 SO 2 R 11, NR 12)NHR 11,-COR 11,-CO 2 R 11,-CONR 12 R 11,-SO 2 NR 12 R 11,-OCONR 12 R 11,C(NR 12)NR 12 R 11,R 6和R 7独立地为卤素,CN,NO 2,-CONR 10 R 11,-SO 2 NR 10 R 11,-NR 10 R 11或-OR 11, 其中R 10和R 11如下所定义; R8是OH,NHSO2R12或NHCOCF3; 及其在治疗中的应用,特别是治疗由cRaf1激酶介导的疾病。
摘要:
Diarylmethylpiperazine compounds having utility as receptor-binding species, e.g., for mediating analgesia, and for combatting drug addiction, alcohol addiction, and drug overdose. The compounds may be administered orally, rectally, topically, nasally, ophthalmically, or parenterally (subcutaneously, intramuscularly, and intravenously), for veterinary and human use, and include delta receptor and mu receptor binding species.
摘要:
The present invention relates generally to novel amine substituted oxindole compounds and compositions. Such compounds and compositions have utility as pharmacological agents in treating diseases or conditions alleviated by the inhibition or antagonism of protein kinase activated signalling pathways in general, and in particular in the pathological processes which involve aberrant cellular proliferation, such as tumor growth. In particular, the present invention relates to a series of substituted oxindole compounds, which exhibit protein tyrosine kinase and protein serine/threonine kinase inhibition, and which are useful in inhibiting tumor growth via inhibition of tumor-related angiogenesis.
摘要:
The present invention is related to oxindole derivatives of structure (I), compositions containing the same, and methods of use and manufacture of the same. Such compounds generally are useful pharmacologically as agents in those disease states alleviated by the alteration of mitogen activated signaling pathways in general, and in particular in the inhibition or antagonism of protein kinases, which pathologically involve aberrant cellular proliferation. Such disease states include tumor growth, restenosis, atherosclerosis, pain and thrombosis. In particular, the present invention relates to a series of substituted oxindole compounds, which exhibit Trk family protein tyrosine kinase inhibition, and which are useful in cancer therapy and chronic pain indications.
摘要:
A method for the treatment or prophylaxis of one or more conditions or disorders selected from the group consisting of physiological pain, diarrhea, urinary incontinence, mental illness, drug and alcohol addiction/overdose, lung edema, depressioysema, apnea, cognitive disorders and gastrointestinal disorders, comprising administration to a subject in need of such treatment or prophylaxis, of a diarylmethylpiperazine or piperidine opioid compound.