Abstract:
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—R5 or a nitrogen atom; R1 represents a C1-6 alkyl group; R2 represents a C1-6 alkyl group or a C3-8 cycloalkyl group; and R3, R4, R5 independently represent a hydrogen atom, a halogen atom, a C1-6 alkyl group, a halo-C1-6 alkyl group, or a C1-6 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.
Abstract:
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; R1 and R2 independently represent a C1-6 alkyl group; and each of R3 to R5 is absent or represents H, a halogen atom, OH, NO2, a halo-C1-6 alkyl group, a (substituted) C1-6 alkoxy group, a (substituted) C3-6 cycloalkyloxy group, or a 5- to 10-membered heteroaryl group.]
Abstract:
Disclosed is a novel 1-(biphenyl-4-yl-methyl)-1H-imidazole derivative represented by general formula (I), which has both angiotensin II receptor antagonist activity and PPAR-γ activating activity and is useful as a prophylactic and/or therapeutic agent for cardiovascular diseases and metabolic diseases. Also disclosed is a pharmaceutical composition which contains the novel 1-(biphenyl-4-yl-methyl)-1H-imidazole derivative. In general formula (I), ring A represents a group represented by formula (II) or (III); R1 represents a C1-6 alkyl group; R2 represents a C1-6 alkyl group which may be substituted by a hydroxy group, or a group represented by formula —CO—R4 (wherein R4 represents a hydroxy group, a C1-6 alkoxy group, an amino group, a mono(C1-6 alkyl)amino group, a di(C1-6 alkyl)amino group, a morpholino group, a piperidino group or a pyrrolidino group); R3 represents a halogen atom or a C1-6 alkoxy group; and X and Y may be the same or different and each represents a nitrogen atom or CH.
Abstract:
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 R1 and R1′ independently represent a C1-6 alkyl group; R2 and R2′ independently represent a substituted or unsubstituted C1-6 alkyl group; R3 represents a hydrogen atom, a substituted or unsubstituted C1-6 alkyl group, or a group represented by formula (IV) [wherein X and Y independently represent CH or N; Z represents a C1-6 alkylene chain, or the like; R11 represents a hydrogen atom, a C6-10 aryl group, or the like; and m represents 0 or 1]; and R4 represents a substituted C1-6 alkyl group]; R5 and R6 independently represent a C1-6 alkyl group: R7 represents a carboxyl group, or the like; R8, R9 and R10 independently represent a hydrogen atom, a halogen atom, or the like; and n represents an integer of 1 to 3.]
Abstract:
Provided are novel compounds that have both angiotensin II receptor-antagonist effects and PPAR-activating effects that are useful as agents for preventing and/or treating hypertension, heart disease, angina, cerebral vascular accident, cerebrovascular disorder, ischemic peripheral circulatory disorder, kidney disease, atherosclerosis, inflammatory disease, type 2 diabetes mellitus, diabetic complication, insulin resistance syndrome, Syndrome X, metabolic syndrome, and hyperinsulinemia. Disclosed are 3-(5-alkoxypyrimidin-2-yl)pyrimidin-4(3H)-one derivatives represented by the General formula (I): [wherein R represents a C1-4 alkyl group], or salts or solvates thereof (I)
Abstract:
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—R5 or a nitrogen atom; R1 represents an alkyl group; R2 represents an alkyl group or a cycloalkyl group; and R3, R4, and R5 each independently represents a hydrogen atom, a halogen atom, an alkyl group, an alkoxy group or similar.
Abstract translation: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PPARγ活化作用,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C-R5或氮原子; R1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。
Abstract:
Disclosed is a novel 2-pyridone derivative represented by general formula (1), which has both angiotensin II receptor antagonist activity and PPAR-γ activating activity and is useful as a prophylactic and/or therapeutic agent for cardiovascular diseases and metabolic diseases. Also disclosed is a pharmaceutical composition which contains the novel 2-pyridone derivative. In general formula (1), R1 represents a C1-6 alkyl group or a C1-6 alkoxy group; R2 represents a C1-6 alkyl group or a C3-8 cycloalkyl group; R3 represents a C1-6 alkyl group, a C6-10 aryl-C1-6 alkyl group, a C1-6 alkoxy-C1-6 alkyl group or a group represented by formula (2) (wherein A represents a nitrogen atom or CH, and R5 represents a hydrogen atom or a C1-6 alkoxy group); and R4 represents a group represented by formula (3) or (4).
Abstract translation:公开了由通式(1)表示的新型2-吡啶酮衍生物,其具有血管紧张素II受体拮抗剂活性和PPAR-γ活化活性,并且可用作心血管疾病和代谢疾病的预防和/或治疗剂。 还公开了含有新的2-吡啶酮衍生物的药物组合物。 在通式(1)中,R 1表示C 1-6烷基或C 1-6烷氧基; R2表示C1-6烷基或C3-8环烷基; R 3表示C 1-6烷基,C 6-10芳基-C 1-6烷基,C 1-6烷氧基-C 1-6烷基或由式(2)表示的基团(其中A表示氮原子或CH R 5表示氢原子或C 1-6烷氧基)。 并且R 4表示由式(3)或(4)表示的基团。
Abstract:
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; R1 and R2 independently represent a C1-6 alkyl group; and each of R3 to R5 is absent or represents H, a halogen atom, OH, NO2, a halo-C1-6 alkyl group, a (substituted) C1-6 alkoxy group, a (substituted) C3-6 cycloalkyloxy group, or a 5- to 10-membered heteroaryl group.]
Abstract:
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—R5 or a nitrogen atom; R1 represents an alkyl group; R2 represents an alkyl group or a cycloalkyl group; and R3, R4, and R5 each independently represents a hydrogen atom, a halogen atom, an alkyl group, an alkoxy group or similar.
Abstract translation:本发明提供:下述通式(I)表示的化合物,既具有血管紧张素II受体拮抗作用又具有PPARγ活化作用,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C-R5或氮原子; R1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。
Abstract:
Disclosed is novel compound and medicinal formulation containing same, possessing both angiotensin II receptor blocking and PPARγ activation effect, of use as a medicine for prevention and/or treatment of hypertension, heart disease, angina pectoris, cerebrovascular disorder, cerebral circulatory disturbances, post-ischemic peripheral circulatory damage, renal disease, arteriosclerosis, inflammatory disorder, type 2 diabetes, diabetic complications, insulin resistance syndrome, syndrome X, metabolic syndrome and hyperinsulinaemia. Further disclosed is the general formula I (where one or both of R1 and R2 represent a C1-6 alkyl group, R3 represents a C1-6 alkyl group which may contain one or more substituent groups selected from group A, or a C3-8 cycloalkyl group which may contain one or more substituent groups selected from group B.) which represents the compound, and salts thereof, solvates thereof, and medicinal compositions containing any of these.