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    • 2. 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。
    • 6. 发明授权
    • Five-membered heterocyclic compounds
    • 五元杂环化合物
    • US07368578B2
    • 2008-05-06
    • US10527426
    • 2003-09-09
    • Yu MomoseNobuyuki TakakuraTsuyoshi MaekawaHiroyuki OdakaHiroyuki Kimura
    • Yu MomoseNobuyuki TakakuraTsuyoshi MaekawaHiroyuki OdakaHiroyuki Kimura
    • C07D263/02C07D263/00C07D263/30C07D261/00C07D261/04C07D261/06A01N43/76A01N43/80
    • 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。
    • 8. 发明授权
    • Oxyiminoalkanoic acid derivatives
    • 氧亚氨基链烷酸衍生物
    • US06495581B1
    • 2002-12-17
    • US09714699
    • 2000-11-16
    • Yu MomoseHiroyuki OdakaHiroshi ImotoHiroyuki KimuraJunichi Sakamoto
    • Yu MomoseHiroyuki OdakaHiroshi ImotoHiroyuki KimuraJunichi Sakamoto
    • A61K31425
    • C07D213/74A61K31/42A61K31/421A61K31/4245A61K31/426A61K31/427A61K31/44A61K31/4439A61K31/47A61K31/4745A61K31/505C07D215/14C07D239/42C07D261/08C07D263/32C07D271/06C07D277/24C07D413/12C07D471/04
    • A compound represented by the formula: wherein R1 is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group; X is a bond, —CO—, —CH(OH)— or a group represented by —NR6— wherein R6 is a hydrogen atom or an optionally substituted alkyl group; n is an integer of 1 to 3; Y is an oxygen atom, a sulfur atom, —SO—, —SO2— or a group represented by —NR7— wherein R7 is a hydrogen atom or an optionally alkyl group; ring A is a benzene ring optionally having additional one to three substituents; p is an integer of 1 to 8; R2 is a hydrogen atom, an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group; q is an integer of 0 to 6; m is 0 or 1; R3 is a hydroxy group, OR8 (R8 is an optionally substituted hydrocarbon group.) or NR9R10 (R9 and R10 are the same or different groups which are selected from a hydrogen atom, an optionally substituted hydrocarbon group, an optionally substituted heterocyclic group or an optionally substituted acyl group or R9 and R10 combine together to form a ring); R4 and R5 are the same or different groups which are selected from a hydrogen atom or an optionally substituted hydrocarbon group wherein R4 may form a ring with R2; provided that when R1 is a ethoxymethyl, a C1-3 alkyl, phenyl or p-methoxyphenyl and q=m=0, R3 is NR9R10; and provided that O-[2-chloro-4-(2-quinolylmethoxy)phenylmethyl]oxime and a methyl pyruvate of [2-chloro-4-(2-quinolylmethoxy)phenylmethyl]-2-iminoxypropionic acid are excluded; or a salt thereof which has excellent hypoglycemic and hypolipidemic actions.
    • 由下式表示的化合物:其中R1是任选取代的烃基或任选取代的杂环基; X是键,-CO - , - CH(OH) - 或-NR 6 - 表示的基团,其中R 6是氢原子或任选取代的烷基; n为1〜3的整数。 Y是氧原子,硫原子,-SO-,-SO 2 - 或-NR 7 - 表示的基团,其中R 7是氢原子或任意烷基; 环A是任选具有另外一个至三个取代基的苯环; p为1〜8的整数, R2是氢原子,任选取代的烃基或任选取代的杂环基; q为0〜6的整数; m为0或1; R3是羟基,OR8(R8是任选取代的烃基)或NR9R10(R9和R10是相同或不同的基团,其选自氢原子,任选取代的烃基,任选取代的杂环基或 任选取代的酰基或R 9和R 10结合在一起形成环); R4和R5是选自氢原子或任选取代的烃基的相同或不同的基团,其中R 4可以与R 2形成环; 条件是当R1是乙氧基甲基,C1-3烷基,苯基或对甲氧基苯基且q = m = 0时,R3是NR9R10; 并且排除了[2-氯-4-(2-喹啉基甲氧基)苯基甲基] -2-亚氨基丙酸的O- [2-氯-4-(2-喹啉基甲氧基)苯甲基]肟和丙酮酸甲酯。 或其盐,其具有优异的降血糖和降血脂作用。