摘要:
Disclosed are: a novel compound which has both an antagonistic activity on an angiotensin II receptor and a PPARγ-activating activity and is therefore useful as a prophylactic and/or therapeutic agent for hypertension, heart diseases, arteriosclerosis, type-2 diabetes, diabetic complications, metabolic syndrome or the like; and a pharmaceutical composition containing the compound. Specifically disclosed are: a compound represented by general formula (I) (wherein the ring A represents a pyridine ring; the ring B represents a tetrazole ring or an oxadiazol-5(4H)-one ring; X represents C-R 5 or a nitrogen atom; R 1 represents a C 1-6 alkyl group; R 2 represents a C 1-6 alkyl group or a C 3-8 cycloalkyl group; and R 3 , R 4 , R 5 independently represent a hydrogen atom, a halogen atom, a C 1-6 alkyl group, a halo-C 1-6 alkyl group, or a C 1-6 alkoxy group which may have a substituent), a salt of the compound, or a solvate of the compound or the salt; and a pharmaceutical composition containing the compound, the salt or the solvate.
摘要翻译:公开了一种对血管紧张素II受体具有拮抗作用和PPAR 3活化活性的新型化合物,因此可用作高血压,心脏病,动脉硬化,2型糖尿病,糖尿病并发症的预防和/或治疗剂 ,代谢综合征等; 和含有该化合物的药物组合物。 具体公开的是:由通式(I)表示的化合物(其中环A表示吡啶环;环B表示四唑环或恶二唑-5(4H) - 酮环; X表示CR 5或氮原子 R 1表示C 1-6烷基; R 2表示C 1-6烷基或C 3-8环烷基; R 3,R 4,R 5独立地表示氢原子,卤素原子, 可以具有取代基的C 1-6烷基,卤代C 1-6烷基或C 1-6烷氧基,化合物的盐或化合物或其盐的溶剂合物; 和含有化合物,盐或溶剂合物的药物组合物。
摘要:
The present invention provides: a compound represented by general formula (I) below, that has both angiotensin II receptor antagonism and a PPARγ activation effect and that is useful as a preventative and/or therapeutic agent for high blood pressure, cardiac disease, arteriosclerosis, type-2 diabetes, and the like; and a drug composition containing the compound. General formula (I) (in the formula: ring A represents a pyridine ring; ring B represents a tetrazole ring or an oxadiazol-5 (4H) -one ring; X represents C-R 5 or a nitrogen atom; R 1 represents an alkyl group; R 2 represents an alkyl group or a cycloalkyl group; and R 3 , R 4 , and R 5 each independently represents a hydrogen atom, a halogen atom, an alkyl group, an alkoxy group or similar.
摘要翻译:本发明提供:下述通式(I)表示的化合物,其具有血管紧张素II受体拮抗作用和PPAR 3活化作用,并且可用作高血压,心脏病,动脉硬化等的预防和/或治疗剂, 2型糖尿病等; 和含有该化合物的药物组合物。 通式(I)(式中,环A表示吡啶环,环B表示四唑环或恶二唑-5-(4H) - 酮环,X表示CR 5或氮原子,R 1表示烷基 R 2表示烷基或环烷基; R 3,R 4和R 5各自独立地表示氢原子,卤素原子,烷基,烷氧基等。
摘要:
Diamine compounds represented by general formula (I) and acid addition salts thereof, and a brain protecting agent containing the same, wherein R1 to R6 may be the same or different from one another and each represents hydrogen, halogen, hydroxy, lower alkyl, lower alkoxy, lower acyloxy, lower alkoxycarbonyloxy, lower alkylsulfonyloxy or amino, among which the lower alkyl and lower alkoxy may be each substituted by halogen or phenyl; R7 and R8 may be the same or different from each other and each represents lower alkyl, or they may be combined together to form alkylene having 1 to 4 carbon atoms; A and A' may be the same or different from each other and each represents a single bond, -O-, -NH-, -NHCO←, -CONH←, -NHCOO←, -NHCONH-, -SONH2← or -COS←, wherein symbol '←' represents a bond to Y or Y'; and Y and Y' may be the same or different from each other and each represents lower alkylene or lower alkenylene. They have an excellent activity of protecting the brain, are highly safe, and can exhibit potent activities by oral administration. Medicines containing them are effecting in treating or preventing the progress of cerebral dysfunctions accompanying cerebral hemorrhage, cerebral infarction, subarachnoid hemorrhage, transient cerebral ischemic attack, or cerebrovascular diseases.
摘要:
The present invention provides a diamine compound of formula (I) or an acid addition salt thereof:
wherein R1, R2, R3, R4, R5 and R6 are the same or different from each other and represent individually a hydrogen atom, halogen atom, hydroxyl group, lower alkyl group, lower alkoxy group, lower acyloxy group, lower alkoxycarbonyloxy group, lower alkylsulfonyloxy group or am amino group, among which the lower alkyl group and lower alkoxy group may be substituted by a halogen atom or a phenyl group; R7 and R8 are the same or different from each other and represent individually a lower alkyl group or the two bind to each other to represent an alkylene group having 1 to 4 carbon atoms; A and A' are the same or different from each other and represent individually a single bond, -O-, -NH-, -NHCO→, -CONH→, -NHCOO→, NHCONH-, -SO₂NH→ or -COS→ (here, the symbol '→' denotes a bond to Y or Y'), Y and Y' are the same or different from each other and represent a lower alkylene group or lower alkenylene group; and cerebral protective drugs containing such compound. The diamine compounds (I) or its acid addition salts have an excellent cerebral protective action, are very safe, and exhibit a strong action when even orally administered, and therefore, medicines containing such compounds are effective for treating disorders caused by cerebral hemorrhage, cerebral infarction, subarachnoid hemorrhage, transient ischemic attack, cerebrovascular disorders and the like, or preventing progress of such disorders.
摘要:
Disclosed is a compound which has both an angiotensin-II receptor antagonistic activity and a PPARγ activation activity and is useful as a prophylactic and/or therapeutic agent for hypertension, heart diseases, angina pectoris, cerebrovascular disorders, cerebral circulatory disorders, ischemic peripheral circulatory disorders, renal diseases, arteriosclerosis, inflammatory diseases, type-2 diabetes, diabetic complications, insulin resistance syndrome, syndrome X, metabolic syndrome and hyperinsulinemia. [In the formula, A represents a 5- to 10-membered heteroaryl group; R 1 and R 2 independently represent a C 1-6 alkyl group; and each of R 3 to R 5 is absent or represents H, a halogen atom, OH, NO 2 , a halo-C 1-6 alkyl group, a (substituted) C 1-6 alkoxy group, a (substituted) C 3 - 6 cycloalkyloxy group, or a 5- to 10-membered heteroaryl group.]
摘要:
To provide a novel JAK3 inhibitor that is useful as a preventive and/or therapeutic agent for rejection and graft versus host disease (GvHD) in organ transplantation, rheumatoid arthritis, multiple sclerosis, systemic lupus erythematosus, Sjögren syndrome, Behcet's disease, type I diabetes mellitus, autoimmune thyroiditis, idiopathic thrombocytopenic purpura, ulcerative colitis, Crohn's disease, asthma, allergic rhinitis, atopic dermatitis, contact dermatitis, urticaria, eczema, psoriasis, allergic conjunctivitis, uveitis, cancer, leukemia and the like. The pyridine-3-carboxyamide derivative represented by the general formula (1):
摘要:
The present invention relates a specific tetrahydroisoquinoline compound which is useful as a chemokine receptor type 3 (CCR3) antagonist, and a pharmaceutical composition comprising the same as an active ingredient. The tetrahydroisoquinoline compound of the present invention is useful for the treatment or prevention of a disease in which CCR3 participates.