摘要:
Novel pyrazolopyridylpyridazinone derivatives characterized by being represented by general formula (1) and pharmacologically acceptable salts thereof, which exhibit a phosphodiesterase inhibiting activity and have a selective potent bronchodilating effect on the respiratory tract: a process for the preparation of them: and bronchodilators containing the same as the activity ingredient: wherein R 1 is C 1 -C 4 lower alkyl or C 3 -C 6 cycloalkyl: and R 2 , R 3 , R 4 and R 5 are each independently hydrogen, C 1 -C 4 lower alkyl or phenyl, or alternatively R 3 and R 5 may be united to form a double bond.
摘要翻译:新型吡唑并吡啶酮衍生物,其特征在于由通式(1)表示的化合物及其药理学上可接受的盐,其具有磷酸二酯酶抑制活性并对呼吸道具有选择性有效的支气管扩张作用:其制备方法:和支气管扩张剂 含有与活性成分相同的化合物:其中R 1为C 1 -C 4低级烷基或C 3 -C 6环烷基; R 2,R 3,R 4和R 5各自独立地为氢, C 1 -C 4低级烷基或苯基,或者R 3和R 5可以结合形成双键。
摘要:
The present invention provides novel N-benzyldioxothiazolidylbenzamide derivatives that improve the insulin resistance and have potent hypoglycemic and lipid-lowering effects and processes for preparing the same, and relates to N-benzyldioxothiazolidylbenzamide derivatives characterized by being represented by a general formula (1) [wherein R 1 and R 2 denote identically or differently hydrogen atoms, lower alkyl groups with carbon atoms of 1 to 4, lower alkoxy groups with carbon atoms of 1 to 3, lower haloalkyl groups with carbon atoms of 1 to 3, lower haloalkoxy groups with carbon atoms of 1 to 3, halogen atoms, hydroxyl groups, nitro groups, amino groups which may be substituted with lower alkyl group(s) with carbon atoms of 1 to 3 or hetero rings, or R 1 and R 2 link to form a methylenedioxy group, R 3 denotes a lower alkoxy group with carbon atoms of 1 to 3, hydroxyl group or halogen atom, and dotted line indicates double bond or single bond in combination with solid line], and processes for preparing the same.
摘要:
o-Anisamide derivatives which serve as peroxisome proliferator-activated receptor (PPAR) agonists, in particular human PPAR agonists, and are efficacious in preventing and/or treating metabolic diseases in which they participate (hyperlipemia, diabetes, etc.), acid addition salts thereof and a process for producing the same. Namely, o-anisamide derivatives represented by general formula (1), pharmaceutically acceptable salts thereof and hydrates of the same, wherein R represents carboxy, carboxymethyl, CH2CHXCOY (wherein X represents mercapto or S(O)nMe wherein n is 0, 1 or 2; and Y represents amino or hydroxy).
摘要:
The invention provides o-anisamide derivatives and their addition salts effective for the prevention and/or therapy of metabolic diseases such as hyperlipidemia and diabetes, in which peroxisome proliferator-activated receptor (PPAR) being intranuclear receptor, in particular, human PPAR participates, as agonistic drugs thereon, and processes for preparing them. The invention relates to o-anisamide derivatives represented by a general formula (1) [wherein R denotes a carboxyl group, carboxymethyl group or CH 2 CHXCOY (here X denotes a mercapto group or S(O)nMe (n=0, 1 or 2) and Y denotes an amino group or hydroxyl group)], their medicinally acceptable salts, their hydrates, and processes for preparing them.
摘要:
Novel N-benzyldioxothiazolidylbenzamide derivatives represented by general formula (1) which improve insulin resistance and have potent hypoglycemic and lipid-lowering effects, wherein R?1 and R2¿ are the same or different and each represents hydrogen, lower (C¿1-4?) alkyl, lower (C1-3) alkoxy, lower (C1-3) haloalkyl, lower (C1-3) haloalkoxy, halogeno, hydroxy, nitro, amino optionally substituted by lower (C1-3) alkyl or a heterocycle, or R?1 and R2¿ may be bonded to each other to thereby form methylenedioxy; R3 represents lower (C¿1-3?) alkoxy, hydroxy or halogeno; and --- represents a double or single bond.
摘要:
The invention provides novel N-substituted dioxothiazolidylbenzamide derivatives that improve the insulin resistance and have potent hypoglycemic effect and lipid-lowering effect, and the process for preparing them, and relates to N-substituted dioxothiazolidylbenzamide derivatives characterized by being represented by a general formula (1) [wherein R 1 and R 2 denote identically or differently hydrogen atoms, lower alkyl groups with carbon atoms of 1 to 4, lower alkoxy groups with carbon atoms of 1 to 3, lower haloalkyl groups with carbon atoms of 1 to 3, lower haloalkoxy groups with carbon atoms of 1 to 3, halogen atoms or hydroxyl groups, or R 1 and R 2 combine to form a methylenedioxy group, R 3 denotes a hydrogen atom, lower alkoxys group with carbon atoms of 1 to 3, hydroxyl group or halogen atom, R 4 denotes a hydrogen or lower alkyl group with carbon atoms of 1 to 3, n denotes an integer of 0 to 2, and X denotes N or CH], and process for preparing the same.