摘要:
Compounds and their use as pharmaceuticals particularly as Raf kinase inhibitors for the treatment of neurotraumatic diseases, cancer, chronic neurodegeneration, pain, migraine and cardiac hypertrophy.
摘要:
Compounds of formula (I): wherein X is O, CH2, S or NH, or the moiety X—R1 is hydrogen; V is CH or N; R1 is hydrogen, C1-6alkyl, C3-7cycloalkyl, aryl, arylC1-6alkyl, heterocyclyl, heterocyclyl-C1-6alkyl, heteroaryl, or heteroarylC1-6alkyl any of which except hydrogen may be optionally substituted; R2 and R3 independently represent hydrogen, C1-6alkyl, C3-7cycloalkyl, aryl, arylC1-6alkyl, heteroaryl, heteroarylC1-6alkyl, heterocyclyl, or heterocyclylC1-6alkyl any one of which except hydrogen may be optionally substituted, or R2 and R3 together with the nitrogen atom to which they are attached form a 4- to 10-membered optionally substituted monocyclic or bicyclic ring; Ar is an aryl or heteroaryl ring either of which may be optionally substituted; one of X1 and X2 is N and the other is NR4, wherein R4 is hydrogen, C1-6alkyl, or arylC1-6alkyl; or pharmaceutically acceptable salts thereof; their use as inhibitors of Raf kinases and pharmaceutical compositions containing them.
摘要翻译:式(I)的化合物:其中X是O,CH 2,S或NH,或X-R 1部分是氢; V是CH或N; R 1是氢,C 1-6烷基,C 3-7环烷基,芳基,芳基C 1-6 烷基,杂环基,杂环基-C 1-6烷基,杂芳基或杂芳基C 1-6烷基,除氢以外的任何一个可以任选被取代; R 2和R 3独立地表示氢,C 1-6烷基,C 3-7环烷基,芳基 ,芳基C 1-6烷基,杂芳基,杂芳基C 1-6烷基,杂环基或杂环基C 1-6烷基,除氢以外的任何一个 可以任选地被取代,或者R 2和R 3与它们所连接的氮原子一起形成4-至10-元任选取代的单环或双环; Ar是任选被取代的芳基或杂芳基环; X 1和X 2之一是N,另一个是NR 4,其中R 4是氢, C 1-6烷基或芳基C 1-6烷基; 或其药学上可接受的盐; 它们用作Raf激酶的抑制剂和含有它们的药物组合物。
摘要:
The present invention relates to a compound of formula (I): or a salt thereof; which is an inhibitor of spleen tyrosine kinase (Syk) and therefore potentially of use in treating diseases resulting from inappropriate activation of mast and/or basophil cells, macrophages, and B-cells and related inflammatory responses and tissue damage, for instance inflammatory disease and/or allergic disorders, and in cancer therapy, specifically heme malignancies, chronic spontaneous urticaria and autoimmune conditions.
摘要:
The wave break has an elongated shape and three wave-breaking surfaces mounted thereon and forming an elongated triangular configuration. The wave break has a lazy side on its forward edge, such that the force of the wave tilts it about the forward edge to increase a projection of its wave-breaking surfaces against the incoming wave. Because of the lazy forward side of the wave break, the leading stringer dive into each wave without deviating substantially from a horizontal plane. The trailing side of the wave break is subject to the lifting forces of each wave and therefore, the trailing side tilts upward and downward in use. The trailing side tilts upward and downward about the leading stringer to rotate the wave-breaking barriers into a more or less perpendicular alignment relative to the wave movement, for breaking the wave more effectively.
摘要:
The present invention relates to novel piperazine and azepine derivatives having pharmacological activity, processes for their preparation, to compositions containing them and to their use in the treatment of neurodegenerative disorders including Alzheimer's disease.
摘要:
The present invention relates to novel benzazepine derivatives having pharmacological activity, processes for their preparation, to compositions containing them and to their use in the treatment of neurological and psychiatric disorders.
摘要:
Novel oxadiazole derivatives of formula (I) having pharmacological activity, processes for their preparation, compositions containing them and their use in the treatment of neurological, psychiatric disorders and gastrointestinal disorders through modulation of the nicotinic α7 receptor.
摘要:
The invention relates to compounds of formula (I) or salts and solvates thereof, processes for their preparation, to compositions containing them and to their use in the treatment of various disorders, such as allergic rhinitis: wherein R1 and R2 are as defined in the specification.
摘要:
A compound of the formula and physiologically acceptable salts and or N-oxides thereof wherein, X1 is N or CR3; X2 is N or CR4; X3 is N or CR5; X4 is N or CR6. with the proviso that at least one but not more than two of X1, X2, X3 and X4 represents N. R1 is a 5-, or 6-membered heterocyclic group selected from group a, b, c or d wherein X5 is a group selected from N or CR7 and X6 is a group selected from O, S or NR8; X7 and X8 which may be the same or different is a group selected from N or CR9; X9 is a group selected from O, S or NR8 and X10 is N or CR10; X11, X12 and X13 may be the same or different and selected from a group N or CR11; processes for their preparation, pharmaceutical compositions containing them and their use in medicine.
摘要翻译:下式的化合物及其生理上可接受的盐和/或其N-氧化物,其中X 1是N或CR 3; X 2是N或CR 4; X 3是N或CR 5; X 4是N或CR 6。 条件是X 1,X 2,X 3和X 4中的至少一个但不多于两个, SUB>表示N. R 1是选自a,b,c或d的5-或6-元杂环基,其中X 5是选自 N或CR 7和X 6是选自O,S或NR 8的基团; X 7和X 8可以相同或不同,是选自N或CR 9的基团。 X 9是选自O,S或NR 8和X 10的基团是N或CR 10; X 11,X 12和X 13可以相同或不同,并且选自N或C 11 SUB >; 其制备方法,含有它们的药物组合物及其在医药中的用途。
摘要:
Compounds of formula (I): wherein; R1 is hydrogen or C1-6alkyl; R2 is hydrogen, C1-6alkyl, perhalomethylC0-5alkyl-O—, or C1-6alkoxy; R3 is hydrogen, C1-6alkyl, or C1-6alkoxyC1-6alkyl; R4 is hydrogen, C1-6alkyl, perhalomethylC1-6alkyl; or unsubstituted C3-6cycloalkylC1-6 alkyl; A is C—R5 or N; B is C—R6 or N; D is C—R7 or N; with the proviso that at least one of A, B, and D, is N; R5 is hydrogen or C1-6alkyl; R6 is hydrogen or C1-6alkyl; R7 is hydrogen, C1-6alkyl, C1-6alkoxy, or hydroxy; R8 is hydrogen or C1-6alkyl, with the proviso that one of R4 and R8 is hydrogen; R9 is hydrogen or hydroxy; R10 is hydrogen or C1-6alkyl; and salts thereof are PAD4 inhibitors and may be useful in the treatment of various disorders, for example rheumatoid arthritis, vasculitis, systemic lupus erythematosus, ulcerative colitis, cancer, cystic fibrosis, asthma, cutaneous lupus erythematosis, and psoriasis.
摘要翻译:式(I)的化合物:其中; R1是氢或C1-6烷基; R 2是氢,C 1-6烷基,全卤代甲基C 0-5烷基-O-或C 1-6烷氧基; R3是氢,C1-6烷基或C1-6烷氧基C1-6烷基; R 4是氢,C 1-6烷基,全卤代甲基C 1-6烷基; 或未取代的C 3-6环烷基C 1-6烷基; A为C-R5或N; B为C-R6或N; D为C-R7或N; 条件是A,B和D中的至少一个为N; R5是氢或C1-6烷基; R6是氢或C1-6烷基; R7是氢,C1-6烷基,C1-6烷氧基或羟基; R8是氢或C1-6烷基,条件是R4和R8中的一个是氢; R9是氢或羟基; R 10是氢或C 1-6烷基; 其盐是PAD4抑制剂,并且可用于治疗各种疾病,例如类风湿性关节炎,血管炎,系统性红斑狼疮,溃疡性结肠炎,癌症,囊性纤维化,哮喘,皮肤红斑狼疮和牛皮癣。