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1. 发明授权

US06545009B1 Retinoid-related receptor function regulating agent 失效
标题翻译：类视黄醇相关受体功能调节剂
公开(公告)号：US06545009B1
公开(公告)日：2003-04-08
申请号：US09720644
申请日：2000-12-28
申请人： Yasuo Sugiyama , Yu Momose , Hiroyuki Kimura , Junichi Sakamoto , Hiroyuki Odaka
发明人： Yasuo Sugiyama , Yu Momose , Hiroyuki Kimura , Junichi Sakamoto , Hiroyuki Odaka
IPC分类号： A61K31435
CPC分类号： C07D413/04 , C07D263/32 , C07D277/30 , C07D417/04
摘要： 1,3-Azole derivatives, pharmaceutical compositions thereof and methods for regulating the function of retinoid-related receptors with 1,3-azole derivatives are disclosed. Such regulation may be useful for preventing or treating diabetes, preventing or treating hyperlipidemia, preventing or treating impaired glucose tolerance (IGT) or for preventing transition from impaired glucose tolerance to diabetes.
摘要翻译：公开了1,3-唑衍生物，其药物组合物和调节具有1,3-唑衍生物的类视黄醇相关受体功能的方法。这种调节可用于预防或治疗糖尿病，预防或治疗高脂血症，预防或治疗葡萄糖耐量异常（IGT）或预防糖耐量受损转变为糖尿病。

2. 发明申请

US20050239854A1 Body weight gain inhibitors 审中-公开
标题翻译：体重增加抑制剂
公开(公告)号：US20050239854A1
公开(公告)日：2005-10-27
申请号：US11168357
申请日：2005-06-29
申请人： Yasuo Sugiyama , Hiroyuki Odaka , Hiroyuki Kimura
发明人： Yasuo Sugiyama , Hiroyuki Odaka , Hiroyuki Kimura
IPC分类号： A61K31/00 , A61K31/195 , A61K31/235 , A61K31/421 , A61K45/06 , A61P3/04 , A61P3/10 , C07D263/32 , C07D263/02
CPC分类号： C07D263/32 , A61K31/00 , A61K31/195 , A61K31/235 , A61K31/421 , A61K45/06 , A61K2300/00
摘要： An agent for inhibiting body weight gain derived from a PPARγ agonist-like substance, which contains a PPARδ agonist-like substance, is useful for the treatment of diabetes and the like.
摘要翻译：用于抑制来自含有PPARδ激动剂样物质的PPARγ激动剂样物质的体重增加剂可用于治疗糖尿病等。

3. 发明申请

US20060135578A1 Five-membered heterocyclic compounds 失效
标题翻译：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。

4. 发明授权

US07179823B1 5-membered n-heterocyclic compounds with hypoglycemic and hypolipidemic activity 有权
标题翻译：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。

5. 发明授权

US06924300B2 Oxyiminoalkanoic acid derivatives 失效
公开(公告)号：US06924300B2
公开(公告)日：2005-08-02
申请号：US10331056
申请日：2002-12-27
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： A61K31/195 , A61K31/235 , A61K31/42 , A61K31/421 , A61K31/422 , A61K31/4245 , A61K31/426 , A61K31/427 , A61K31/437 , A61K31/44 , A61K31/4402 , A61K31/4439 , A61K31/47 , A61K31/4704 , A61K31/4745 , A61K31/496 , A61K31/505 , A61P3/06 , A61P3/10 , A61P9/10 , A61P29/00 , A61P43/00 , C07D213/74 , C07D215/14 , C07D239/42 , C07D261/08 , C07D263/32 , C07D271/06 , C07D277/24 , C07D413/04 , C07D413/12 , C07D471/04 , C07D263/30 , C07D277/20
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： To provide a novel oxyiminoalkanoic acid derivative which has excellent hypoglycemic and hypolipidemic actions and which is used for the prevention or treatment of diabetes mellitus, hyperlipemia, insulin insensitivity, insulin resistance and impaired glucose tolerance.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.

6. 发明授权

US06495581B1 Oxyiminoalkanoic acid derivatives 失效
标题翻译：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。

7. 发明授权

US07223791B2 Function regulator for retinoid relative receptor 失效
标题翻译：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。

8. 发明申请

US20060148858A1 1, 2-Azole derivatives with hypoglycemic and hypolipidemic activity 审中-公开
标题翻译： 1，具有低血糖和降血脂活性的2-唑衍生物
公开(公告)号：US20060148858A1
公开(公告)日：2006-07-06
申请号：US10517214
申请日：2003-05-22
申请人： Tsuyoshi Maekawa , Ryoma Hara , Hiroyuki Odaka , Hiroyuki Kimura , Hideya Mizufune , Kohji Fukatsu
发明人： Tsuyoshi Maekawa , Ryoma Hara , Hiroyuki Odaka , Hiroyuki Kimura , Hideya Mizufune , Kohji Fukatsu
IPC分类号： A61K31/4439 , A61K31/42 , C07D413/02 , C07D403/02
CPC分类号： C07D231/12 , C07D231/14 , C07D231/20 , C07D231/22 , C07D261/08 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/14 , C07D413/12 , C07D417/04
摘要： A compound represented by the formula (1) wherein ring A is a ring optionally having 1 to 3 substituents; ring B is a 1,2-azole ring which may further have 1 to 3 substituents; Xa, Xb and Xc are the same or different and each is a bond, —O—, —S— and the like; Ya is a divalent aliphatic hydrocarbon residue having 1 to 20 carbon atoms; Yb and Yc are the same or different and each is a bond or a divalent aliphatic hydrocarbon residue having 1 to 20 carbon atoms; ring C is a monocyclic aromatic ring which may further have 1 to 3 substituents; and R represents —OR4 (R4 is hydrogen atom or optionally substituted hydrocarbon group) and the like, or a salt thereof or a prodrug thereof is useful as an agent for the prophylaxis or treatment of diabetes and the like.
摘要翻译：由式（1）表示的化合物，其中环A是任选具有1至3个取代基的环; 环B是可以进一步具有1至3个取代基的1,2-吡咯环; Xa，Xb和Xc相同或不同，各自为键，-O - ， - S-等; Ya是具有1至20个碳原子的二价脂族烃残基; Yb和Yc相同或不同，各自为键或碳原子数1〜20的二价脂肪族烃残基; 环C是可以进一步具有1至3个取代基的单环芳环; 和R表示-OR 4（R 4是氢原子或任选取代的烃基）等，或其盐或其前药可用作预防或治疗糖尿病等。

9. 发明授权

US07368578B2 Five-membered heterocyclic compounds 失效
标题翻译：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。

10. 发明授权

US07241785B2 Five-membered heterocyclic alkanoic acid derivative 失效
标题翻译：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。

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