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    5-membered n-heterocyclic compounds with hypoglycemic and hypolipidemic activity
    2.
    发明授权
    5-membered n-heterocyclic compounds with hypoglycemic and hypolipidemic activity 有权
    具有低血糖和降血脂活性的5元正构杂环化合物

    公开(公告)号：US07179823B1

    公开(公告)日：2007-02-20

    申请号：US10129702

    申请日：2000-11-09

    申请人： Yu Momose ,  Tsuyoshi Maekawa ,  Hiroyuki Odaka ,  Hiroyuki Kimura

    发明人： Yu Momose ,  Tsuyoshi Maekawa ,  Hiroyuki Odaka ,  Hiroyuki Kimura

    IPC分类号： C07D263/32 ,  C07D277/24 ,  C07D401/04 ,  A61K31/422 ,  A61K31/4439

    CPC分类号： C07D231/12 ,  A61K31/501 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D417/14 ,  Y02P20/55

    摘要： A compound of formula (I) F wherein R1 represents a hydrocarbon group which may be substituted or a heterocyclic group which may be substituted; x represents a bond, an oxygen atom, a sulfur atom, or a group of the formula: —CO—, —CS—, —CR4(OR5)— or —NR6— wherein each of R4 and R6 represents a hydrogen atom or a hydrocarbon group which may be stubstituted, R5 represents a hydrogen atom or a protective group for a hydroxyl group; m represents an integer of 0 to 3; Y represents an oxygen atom, a sulfur atom, or a group of the formula: —SO—, —SO2—, —NR7—, —CONR7— or —NR7CO— wherein R7 represents a hydrogen atom or a hydrocarbon group which may be substituted; ring A represents an aromatic ring which may further have 1 to 3 substituents; n represents an integer of 1 to 8; ring B represents a nitrogen-containing 5-membered hetero ring which may further be substituted by an alkyl group.

    摘要翻译： 式（I）F化合物，其中R 1表示可被取代的烃基或可被取代的杂环基; X表示键，氧原子，硫原子或下式基团：-CO-，-CS-，-CR 4（OR 5） - 或-NR 6 - ，其中R 4和R 6各自表示氢原子或可以被取代的烃基，R SUP > 5表示氢原子或羟基的保护基; m表示0〜3的整数， Y表示氧原子，硫原子或下式的基团：-SO - ， - SO 2 - ， - NR 7 - ， - CONR 7 - 或-NR 7 CO-，其中R 7表示氢原子或可被取代的烃基; 环A表示可以进一步具有1至3个取代基的芳环; n表示1〜8的整数， 环B表示可以进一步被烷基取代的含氮5元杂环。

    Function regulator for retinoid relative receptor
    3.
    发明授权
    Function regulator for retinoid relative receptor 失效
    类视黄醇相对受体的功能调节剂

    公开(公告)号：US07223791B2

    公开(公告)日：2007-05-29

    申请号：US10481033

    申请日：2002-06-25

    申请人： Tsuyoshi Maekawa ,  Jun Kunitomo ,  Hiroyuki Odaka ,  Hiroyuki Kimura

    发明人： Tsuyoshi Maekawa ,  Jun Kunitomo ,  Hiroyuki Odaka ,  Hiroyuki Kimura

    IPC分类号： A61K31/341

    CPC分类号： C07D207/337 ,  A61K31/00 ,  A61K31/341 ,  A61K31/381 ,  A61K31/40 ,  A61K31/4196 ,  A61K31/42 ,  A61K31/4245 ,  A61K31/433 ,  A61K31/4418 ,  A61K31/625 ,  C07D213/61 ,  C07D249/08 ,  C07D261/08 ,  C07D271/107 ,  C07D307/54 ,  C07D333/24

    摘要： The present invention provides a retinoid-related receptor (except retinoic acid receptors) function regulating agent comprising a compound represented by the formula: wherein one of R1 and R2 is an optionally substituted monocyclic aromatic hydrocarbon group or an optionally substituted monocyclic aromatic heterocyclic group containing one heteroatom, and the other is a hydrogen atom and the like; B is a 5- or 6-membered heterocycle (except 1,3-azole); A is an optionally substituted aromatic hydrocarbon group or an optionally substituted aromatic heterocyclic group; and R3 is a hydrogen atom and the like, or a salt thereof, which is useful as an agent for the prophylaxis or treatment of diabetes mellitus, hyperlipidemia, impaired glucose tolerance or the like.

    摘要翻译： 本发明提供了一种类视黄醇相关受体（视黄酸受体除外）的功能调节剂，其包含由下式表示的化合物：其中R 1和R 2中的一个为 任选取代的单环芳族烃基或含有一个杂原子的任选取代的单环芳族杂环基，另一个是氢原子等; B是5-或6-元杂环（除了1,3-唑）; A是任选取代的芳族烃基或任选取代的芳族杂环基; R 3是氢原子等或其盐，其可用作预防或治疗糖尿病，高脂血症，葡萄糖耐量异常等的药剂。

    Five-membered heterocyclic compounds
    4.
    发明授权
    Five-membered heterocyclic compounds 失效
    五元杂环化合物

    公开(公告)号：US07368578B2

    公开(公告)日：2008-05-06

    申请号：US10527426

    申请日：2003-09-09

    申请人： Yu Momose ,  Nobuyuki Takakura ,  Tsuyoshi Maekawa ,  Hiroyuki Odaka ,  Hiroyuki Kimura

    发明人： Yu Momose ,  Nobuyuki Takakura ,  Tsuyoshi Maekawa ,  Hiroyuki Odaka ,  Hiroyuki Kimura

    IPC分类号： C07D263/02 ,  C07D263/00 ,  C07D263/30 ,  C07D261/00 ,  C07D261/04 ,  C07D261/06 ,  A01N43/76 ,  A01N43/80

    CPC分类号： C07D263/32 ,  C07F9/6558 ,  C07F9/65583

    摘要： 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.

    摘要翻译： 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＆gt;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。

    Five-membered heterocyclic compounds
    5.
    发明申请
    Five-membered heterocyclic compounds 失效
    五元杂环化合物

    公开(公告)号：US20060135578A1

    公开(公告)日：2006-06-22

    申请号：US10527426

    申请日：2003-09-09

    申请人： Yu Momose ,  Nobuyuki Takakura ,  Tsuyoshi Maekawa ,  Hiroyuki Odaka ,  Hiroyuki Kimura

    发明人： Yu Momose ,  Nobuyuki Takakura ,  Tsuyoshi Maekawa ,  Hiroyuki Odaka ,  Hiroyuki Kimura

    IPC分类号： A61K31/422 ,  C07D413/14

    CPC分类号： C07D263/32 ,  C07F9/6558 ,  C07F9/65583

    摘要： 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.

    摘要翻译： 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＆gt;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。

    Five-membered heterocyclic alkanoic acid derivative
    6.
    发明授权
    Five-membered heterocyclic alkanoic acid derivative 失效
    五元杂环烷酸衍生物

    公开(公告)号：US07241785B2

    公开(公告)日：2007-07-10

    申请号：US10472159

    申请日：2002-03-22

    申请人： Yu Momose ,  Tsuyoshi Maekawa ,  Hiroshi Imoto ,  Hiroyuki Odaka ,  Hiroyuki Kimura

    发明人： Yu Momose ,  Tsuyoshi Maekawa ,  Hiroshi Imoto ,  Hiroyuki Odaka ,  Hiroyuki Kimura

    IPC分类号： C07D413/10 ,  C07D413/12 ,  A61K31/422

    CPC分类号： C07D413/12 ,  C07D263/32 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14

    摘要： The present invention relates to a compound represented by the formula wherein R1 is an optionally substituted 5-membered heterocyclic group; X is a bond etc.; Q is a divalent hydrocarbon group having 1 to 20 carbon atoms; Y is a bond etc.; ring A is an aromatic ring optionally further having 1 to 3 substituents; Z is —(CH2)n—Z1— (n is an integer of 0 to 8 and Z1 is a bond etc.) and the like; ring B is a 5-membered heterocycle optionally further having 1 to 3 substituents; W is a divalent saturated hydrocarbon group having 1 to 20 carbon atoms; R2 is —OH etc., or a salt thereof. A pharmaceutical composition containing this compound is useful as a prophylactic or therapeutic agent of diseases such as diabetes mellitus and the like.

    摘要翻译： 本发明涉及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是债券等; Q为碳原子数为1〜20的二价烃基; Y是债券等; 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 - n 1 - （n是0至8的整数，Z <1） SUP>是债券等）等; 环B是任选进一步具有1至3个取代基的5元杂环; W是碳原子数为1〜20的二价饱和烃基; R 2是-OH等，或其盐。 含有该化合物的药物组合物可用作糖尿病等疾病的预防或治疗剂。

    Alkanoic acid derivatives process for their production and use thereof
    7.
    发明授权
    Alkanoic acid derivatives process for their production and use thereof 失效
    用于其生产和使用的烷酸衍生物方法

    公开(公告)号：US07238716B2

    公开(公告)日：2007-07-03

    申请号：US10465938

    申请日：2001-12-28

    申请人： Yu Momose ,  Tsuyoshi Maekawa ,  Nobuyuki Takakura ,  Hiroyuki Odaka ,  Hiroyuki Kimura ,  Tatsuya Ito

    发明人： Yu Momose ,  Tsuyoshi Maekawa ,  Nobuyuki Takakura ,  Hiroyuki Odaka ,  Hiroyuki Kimura ,  Tatsuya Ito

    IPC分类号： A61K31/4439 ,  C07D413/12

    CPC分类号： C07D403/04 ,  C07D263/32 ,  C07D277/24 ,  C07D277/42 ,  C07D413/04 ,  C07D413/06 ,  C07D413/12 ,  C07D413/14 ,  C07D417/06 ,  C07D417/12 ,  C07D417/14

    摘要： An alkanoic acid derivative useful as a prophylactic or therapeutic agent of diabetes mellitus, hyperlipidemia, impaired glucose tolerance and the like can be provided by a compound represented by the formula wherein R1 is an optionally substituted 5-membered aromatic heterocyclic group; X is a bond and the like; Q is a divalent hydrocarbon group having 1 to 20 carbon atoms; Y is a bond and the like; ring A is an aromatic ring optionally further having 1 to 3 substituents; Z is —(CH2)n-Z1-(n is an integer of 1 to 8 and Z1 is an oxygen atom and the like) and the like; ring B is a pyridine ring optionally further having 1 to 3 substituents, and the like; U is a bond and the like; W is a divalent hydrocarbon group having 1 to 20 carbon atoms; and R3 is —OH and the like, provided that, when ring B is a benzene ring optionally further having 1 to 3 substituents, U should be a bond, or a salt thereof.

    摘要翻译： 可用作糖尿病，高脂血症，葡萄糖耐量异常等的预防或治疗剂的链烷酸衍生物可由下式表示的化合物提供：其中R 1为任选取代的5元 芳香族杂环基; X是一个键等; Q为碳原子数为1〜20的二价烃基; Y是一个债券等; 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 - n 1 - （n是1至8的整数，Z <1） SUP>是氧原子等）等; 环B是任选还含有1至3个取代基的吡啶环等; U是一个债券等; W是碳原子数为1〜20的二价烃基; 且R 3为-OH等，条件是当环B为任选还含有1至3个取代基的苯环时，U应为键或其盐。

    Oxyiminoalkanoic acid derivatives
    9.
    发明授权
    Oxyiminoalkanoic acid derivatives 失效
    氧亚氨基链烷酸衍生物

    公开(公告)号：US06495581B1

    公开(公告)日：2002-12-17

    申请号：US09714699

    申请日：2000-11-16

    申请人： Yu Momose ,  Hiroyuki Odaka ,  Hiroshi Imoto ,  Hiroyuki Kimura ,  Junichi Sakamoto

    发明人： Yu Momose ,  Hiroyuki Odaka ,  Hiroshi Imoto ,  Hiroyuki Kimura ,  Junichi Sakamoto

    IPC分类号： A61K31425

    CPC分类号： C07D213/74 ,  A61K31/42 ,  A61K31/421 ,  A61K31/4245 ,  A61K31/426 ,  A61K31/427 ,  A61K31/44 ,  A61K31/4439 ,  A61K31/47 ,  A61K31/4745 ,  A61K31/505 ,  C07D215/14 ,  C07D239/42 ,  C07D261/08 ,  C07D263/32 ,  C07D271/06 ,  C07D277/24 ,  C07D413/12 ,  C07D471/04

    摘要： 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.

    摘要翻译： 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。