摘要:
The invention provides compositions, pharmaceutical preparations, and methods for modulating angiogenesis and/or cell migration in a subject having a cellular proliferative disease (e.g., cancer), or a disease or condition amenable to treatment by enhancing cellular proliferation and cell migration (e.g., angiogenesis), by modulating the activity of an aquaporin, such as aquaporin-1. The compositions and pharmaceutical preparations of the invention may comprise one or more of compounds that modulate the activity of aquaporin-1.
摘要:
A description is given of derivatives of benzoylpyrazoles of the formula (I) and of their use as herbicides. In this formula (I) R1a, R1b, R1c, R2, R3, R4 and R5 stand for various radicals, X for a bridging atom, L for a carbon chain and Y for a chalcogen atom.
摘要:
Compounds of formula (I), or a pharmaceutically acceptable derivative thereof, wherein R1 and R3 independently represent H, C1-6alkyl, C3-8cycloalkyl, or halogen; R2 represents C1-6alkyl, CF3 or aryl; a represents 1 or 2; R4, R5, R7 and R8 independently represent H, C1-6alkyl, C1-6alkyloxy, CN or halogen, or R4 and R5, or R7 and R8, together with the ring to which they are attached form an aryl or heterocyclic fused ring system; X represents C or N; Y represents CH2 or O; R6 represents H, CN or halo provided that, when X represents N, R6 is absent. The compounds are useful for treating endometriosis, uterine fibroids (leiomyomata), menorrhagia, adenomyosis, primary and secondary dysmenorrhoea (including symptoms of dyspareunia, dyschexia and chronic pelvic pain), or chronic pelvic pain syndrome.
摘要翻译:式(I)化合物或其药学上可接受的衍生物,其中R 1和R 3独立代表H,C 1-6烷基 C 3-8环烷基或卤素; R 2表示C 1-6烷基,CF 3或芳基; a代表1或2; R 4,R 5,R 7和R 8独立地表示H,C 1-6 C 1-6烷基,C 1-6烷氧基,CN或卤素,或R 4和R 5或R 7 和它们所连接的环连接形成芳基或杂环稠环体系; X表示C或N; Y表示CH 2或O; R 6表示H,CN或卤素,条件是当X表示N时,R 6不存在。 这些化合物可用于治疗子宫内膜异位症,子宫肌瘤(平滑肌瘤),月经过多,子宫腺肌症,原发性和继发性痛经(包括性交疼痛,dyschexia和慢性盆腔疼痛症状)或慢性盆腔疼痛综合征。
摘要:
The present invention provides a pharmaceutical composition comprising (a) a phosphodiesterase (PDE)-IV inhibitor or a pharmaceutically acceptable salt thereof and (b) an immunosuppressant, a therapeutic and/or preventive agent for chronic skin diseases comprising (a) a PDE-IV inhibitor or a pharmaceutically acceptable salt thereof and (b) an immunosuppressant, a therapeutic and/or preventive agent for chronic skin diseases to be administered simultaneously or separately with an interval comprising (a) a PDE-IV inhibitor or a pharmaceutically acceptable salt thereof and (b) an immunosuppressant, as active ingredients; and the like.
摘要:
An object of the present invention is to provide a medicament and method which is useful for prevention and/or therapy of arterial wall injury. According to the present invention, there is provided a method for prevention and/or therapy of arterial wall injury which comprises a step of administering the pyrazolone derivative represented by the following formula (I) or the physiologically acceptable salt thereof, or the hydrate or solvate thereof in a preventively or therapeutically effective amount to mammals including humans: wherein R1 represents a hydrogen atom, an aryl group, an alkyl group, or an alkoxycarbonylalkyl group; R2 represents a hydrogen atom, an aryloxy group, an arylmercapto group, an alkyl group or a hydroxyalkyl group; or R1 and R2 are combined with each other to represent an alkylene group; and R3 represents a hydrogen atom, an alkyl group, a cycloalkyl group, a hydroxyalkyl group, a benzyl group, a naphthyl group, a phenyl group, or a phenyl group substituted with 1 to 3 substituents selected from the group consisting of an alkyl group, an alkoxy group, a hydroxyalkyl group, an alkoxycarbonyl group, an alkylmercapto group, an alkylamino group, a dialkylamino group, a halogen atom, a trifluoromethyl group, a carboxyl group, a cyano group, a hydroxyl group, a nitro group, an amino group and an acetamide group.
摘要翻译:本发明的目的是提供一种可用于预防和/或治疗动脉壁损伤的药物和方法。 根据本发明,提供了一种预防和/或治疗动脉壁损伤的方法,包括给予由下式(I)表示的吡唑啉酮衍生物或其生理学上可接受的盐,或其水合物或溶剂化物 其具有预防或治疗有效量的哺乳动物包括人:其中R 1表示氢原子,芳基,烷基或烷氧基羰基烷基; R 2表示氢原子,芳氧基,芳基巯基,烷基或羟烷基; 或R 1和R 2彼此结合以表示亚烷基; R 3表示氢原子,烷基,环烷基,羟基烷基,苄基,萘基,苯基或被1〜3个取代基取代的苯基 由烷基,烷氧基,羟基烷基,烷氧基羰基,烷基巯基,烷基氨基,二烷基氨基,卤素原子,三氟甲基,羧基,氰基, 羟基,硝基,氨基和乙酰胺基。
摘要:
The invention features compounds that are inhibitors of COX-2 activity. Certain of the compounds are inhibitors of FAAH activity as well as COX-2 activity. The compounds include a 5-membered or 6-membered substituted or unsubstituted heteroaryl or heterocyclyl ring having one or two heteroatoms selected from the group consisting of O, S, and N that is linked to two substituted or unsubstituted 6-membered aryl or heteroaryl groups that can be the same or different.
摘要:
The invention relates to 5-aminoalkylaminopyrazole derivatives of formula (I) or salts thereof: wherein the various symbols are as defined in the description, to processes for their preparation, to compositions thereof, and to their use for the control of pests (including arthropods and helminths).
摘要:
Compounds useful for treating cellular proliferative diseases and disorders by modulating the activity of one or more mitotic kinesins are disclosed.
摘要:
The invention relates to the compounds of formula (I): in which R1, R2, R3, R4, Q and Z are as defined in the specification. The invention also relates to the pharmaceutical compositions containing these compounds.