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:
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:
An α-phenoxybenzeneacetic acid derivative represented by general formula (I), 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, metabolic syndrome or the like, a salt of the derivative, or a solvate of the derivative or the salt; and a pharmaceutical composition containing the derivative, the salt or the solvate. [In the formula, Q represents a group represented by formula (II) or (III) [wherein R 1 and R 1' independently represent a C 1-6 alkyl group; R 2 and. R 2' independently represent a substituted or unsubstituted C 1-6 alkyl group; R 3 represents a hydrogen atom, a substituted or unsubstituted C 1-6 alkyl group, or a group represented by formula (IV) [wherein X and Y independently represent CH or N; Z represents a C 1-6 alkylene chain, or the like; R 11 represents a hydrogen atom, a C 6-10 aryl group, or the like; and m represents 0 or 1] ; and R 4 represents a substituted C 1-6 alkyl group]; R 5 and R 6 independently represent a C 1-6 alkyl group: R 7 represents a carboxyl group, or the like; R 8 , R 9 and R 10 independently represent a hydrogen atom, a halogen atom, or the like; and n represents an integer of 1 to 3.]
摘要翻译:由通式(I)表示的± - 苯氧基苯乙酸衍生物,其具有血管紧张素II受体拮抗作用和PPAR 3活化活性,可用作高血压,代谢综合征等的预防和/或治疗剂,盐 的衍生物,或衍生物或盐的溶剂合物; 和含有衍生物,盐或溶剂化物的药物组合物。 [式中,Q表示由式(II)或(III)表示的基团[其中R 1和R 1'独立地表示C 1-6烷基; R 2和。 R 2'独立地表示取代或未取代的C 1-6烷基; R 3表示氢原子,取代或未取代的C 1-6烷基或由式(IV)表示的基团[其中X和Y独立地表示CH或N; Z表示C 1-6亚烷基链等; R 11表示氢原子,C 6-10芳基等; m表示0或1]; R 4表示取代的C 1-6烷基]; R 5和R 6独立地表示C 1-6烷基:R 7表示羧基等; R 8,R 9和R 10独立地表示氢原子,卤素原子等; n表示1〜3的整数。
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:
Disclosed is a novel compound which has both angiotensin II receptor antagonist activity and PPARγ activating 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, kidney diseases, arteriosclerosis, inflammatory diseases, type 2 diabetes, diabetic complication, insulin resistant syndrome, syndrome X, metabolic syndrome and hyperinsulinemia. Also disclosed is a pharmaceutical composition which contains the novel compound. Specifically disclosed are: a sulfonamide derivative represented by general formula (I), a salt thereof, or a solvate of the derivative or salt; and a pharmaceutical composition which contains the sulfonamide derivative, a salt thereof, or a solvate of the derivative or salt. (In the formula, R 1 represents a C 1-6 alkyl group; R 2 and R 3 each represents a C 1-6 alkyl group or the like; and R 4 represents a hydrogen atom, a C 1-6 alkyl group, a C 1-6 alkanoyl group or a C 3-8 cycloalkylcarbonyl group.)