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    • 22. 发明申请
    • Five-membered heterocyclic compounds
    • 五元杂环化合物
    • US20060135578A1
    • 2006-06-22
    • US10527426
    • 2003-09-09
    • Yu MomoseNobuyuki TakakuraTsuyoshi MaekawaHiroyuki OdakaHiroyuki Kimura
    • Yu MomoseNobuyuki TakakuraTsuyoshi MaekawaHiroyuki OdakaHiroyuki Kimura
    • A61K31/422C07D413/14
    • C07D263/32C07F9/6558C07F9/65583
    • The present invention provides a compound represented by the formula: wherein R1 is an optionally substituted 5-membered heterocyclic group; X, Y and V are the same or different and each is a bond, an oxygen atom, a sulfur atom and the like; Q is a divalent hydrocarbon group having 1 to 20 carbon atoms; ring A is an aromatic ring optionally further having 1 to 3 substituents; Z is —(CH2)n-Z1- or -Z1-(CH2)n— (n is an integer of 0 to 8, Z1 is a bond, an oxygen atom, a sulfur atom and the like); ring B is a nitrogen-containing heterocycle optionally further having 1 to 3 substituents; W is a bond or a divalent hydrocarbon group having 1 to 20 carbon atoms; R2 is a hydrogen atom, a cyano group, —PO(OR9)(OR10) (R9 and R10 are the same or different and each is a hydrogen atom or an optionally substituted hydrocarbon group, and R9 and R10 are optionally bonded to form an optionally substituted ring) and the like, or a salt thereof, which has a superior adipose tissue weight decreasing action, a hypoglycemic action and a hypolipidemic action, and which is useful as an agent for the prophylaxis or treatment of obesity, diabetes mellitus, hyperlipidemia, impaired glucose tolerance, hypertension and the like.
    • 本发明提供由下式表示的化合物:其中R 1是任选取代的5元杂环基; X,Y和V相同或不同,各自为键,氧原子,硫原子等; Q为碳原子数为1〜20的二价烃基; 环A是任选进一步具有1至3个取代基的芳环; Z是 - (CH 2)n - - - - - - - - 1 - (CH 2) (n为0〜8的整数,Z 1为键,氧原子,硫原子等); n为0〜8的整数。 环B是任选进一步具有1至3个取代基的含氮杂环; W是碳原子数为1〜20的键或二价烃基; R 2是氢原子,氰基,-PO(OR 9)(OR 10)(R 10) SUP>和R 10相同或不同,各自为氢原子或任选取代的烃基,R 9和R 10为 任选地键合以形成任选取代的环)等,或其盐,其具有优异的脂肪组织重量减少作用,降血糖作用和降血脂作用,并且其可用作预防或治疗 肥胖症,糖尿病,高脂血症,葡萄糖耐量降低,高血压等。
    • 30. 发明授权
    • Hydroxypyridine derivatives their production and use
    • 羟基吡啶衍生物的生产和使用
    • US5891895A
    • 1999-04-06
    • US834123
    • 1997-04-14
    • Mitsuru ShiraishiTsuyoshi MaekawaToshifumi Watanabe
    • Mitsuru ShiraishiTsuyoshi MaekawaToshifumi Watanabe
    • C07D213/65C07D213/89A61K31/44C07D213/53
    • C07D213/89C07D213/65
    • Hydroxypyridine derivatives of the formula ##STR1## wherein R.sup.1 is a branched C.sub.3-8 alkyl group or a C.sub.3-8 cycloalkyl group, each of which may be substituted;R.sup.2 is a halogen atom, a C.sub.1-4 alkyl group or a C.sub.1-4 alkoxy group;X is an oxygen atom or NR.sup.3 in which R.sup.3 is a hydrogen atom or a C.sub.1-4 alkyl group;R.sup.4, R.sup.5 and R.sup.6 are independently (1) a hydrogen atom, (2) a halogen atom, (3) a cyano group, (4) a nitro group, (5) a C.sub.1-4 acyl group, (6) a C.sub.1-4 alkoxy group which may be substituted with halogen, (7) a C.sub.1-4 alkyl group which may be substituted with halogen or (8) a mercapto group which may be substituted with a C.sub.1-4 alkyl group;m is 0 to 3; andn is 0 or 1;provided that all of R.sup.4, R.sup.5 and R.sup.6 are not hydrogen atom, or a salt thereof, which have potassium channel opening activity and are useful as therapeutic agents of cardiovascular diseases such as angina pectoris, hypertension, etc.
    • 其中R 1是支链C 3-8烷基或C 3-8环烷基,其中每一个可以被取代; R2是卤素原子,C1-4烷基或C1-4烷氧基; X是氧原子或NR 3,其中R 3是氢原子或C 1-4烷基; R4,R5和R6独立地为(1)氢原子,(2)卤素原子,(3)氰基,(4)硝基,(5)C1-4酰基,(6)C1 -4-烷氧基,(7)可被卤素取代的C 1-4烷基或(8)可被C 1-4烷基取代的巯基; m为0〜3; 并且n为0或1; 条件是所有R4,R5和R6不是氢原子,或其盐,其具有钾通道开放活性,并且可用作心血管疾病如心绞痛,高血压等的治疗剂。