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1. 发明申请

US20090018331A1 CONDENSED IMIDAZOLE DERIVATIVES 失效
标题翻译：稠密咪唑衍生物
公开(公告)号：US20090018331A1
公开(公告)日：2009-01-15
申请号：US12199982
申请日：2008-08-28
申请人： Seiji Yoshikawa , Eita Emori , Fumiyoshi Matsuura , Richard Clark , Hironori Ikuta , Kazunobu Kira , Nobuyuki Yasuda , Tadashi Nagakura , Kazuto Yamazaki
发明人： Seiji Yoshikawa , Eita Emori , Fumiyoshi Matsuura , Richard Clark , Hironori Ikuta , Kazunobu Kira , Nobuyuki Yasuda , Tadashi Nagakura , Kazuto Yamazaki
IPC分类号： C07D498/14 , C07D473/04 , C07D487/04
CPC分类号： C07D473/30 , C07D471/04 , C07D473/04 , C07D473/06 , C07D473/18 , C07D473/36 , C07D473/40 , C07D487/04 , C07D491/14
摘要： The present invention is related to compounds represented by the following formula, or salts or hydrates thereof wherein, T1 represents a 4- to 12-membered heterocyclic group containing one or two nitrogen atoms in the ring, which is a monocyclic or bicyclic structure that may have one or more substituents; X represents a C1-6 alkyl group which may have one or more substituents, or such; Z1 and Z2 each independently represent a nitrogen atom or a group represented by the formula —CR2—; R1 and R2 independently represent a hydrogen atom, a C1-6 alkyl group which may have one or more substituents, or a C1-6 alkoxy group which may have one or more substituents, or such. These are novel compounds that exhibit an excellent DPPIV-inhibiting activity.
摘要翻译：本发明涉及由下式表示的化合物或其盐或水合物，其中，T1表示在环中含有一个或两个氮原子的4至12元杂环基，其为单环或双环结构，其可以是具有一个或多个取代基; X表示可以具有一个或多个取代基的C 1-6烷基; Z 1和Z 2各自独立地表示氮原子或由式-CR 2表示的基团; R1和R2独立地表示氢原子，可以具有一个或多个取代基的C 1-6烷基或可以具有一个或多个取代基的C 1-6烷氧基等。这些是表现出优异的DPPIV抑制活性的新型化合物。

2. 发明授权

US07238720B2 Pharmaceutical use of N-carbamoylazole derivatives 失效
标题翻译： N-氨基甲酰唑衍生物的药用
公开(公告)号：US07238720B2
公开(公告)日：2007-07-03
申请号：US10766388
申请日：2004-01-27
申请人： Nobuyuki Yasuda , Tadashi Nagakura , Kazuto Yamazaki , Seiji Yoshikawa , Toshimi Okada , Hironori Ikuta , Mika Koyanagi
发明人： Nobuyuki Yasuda , Tadashi Nagakura , Kazuto Yamazaki , Seiji Yoshikawa , Toshimi Okada , Hironori Ikuta , Mika Koyanagi
IPC分类号： A61K31/4196 , A61K31/416 , C07D43/02
CPC分类号： C07D451/02 , C07D249/12 , C07D401/12 , C07D403/12 , C07D405/12 , C07D413/12 , C07D471/04
摘要： The present invention relates to use of 1-carbamoylazole derivatives as medicaments and pharmaceutical compositions containing 1-carbamoylazole derivatives as the active ingredient, based on their DPPIV inhibiting effects. The present invention provides a dipeptidyl peptidase IV inhibiting agent comprising a compound represented by the general formula (I):
摘要翻译：本发明涉及1-氨基甲酰唑衍生物作为药物的用途，以及含有1-氨基甲酰唑衍生物作为活性成分的药物组合物，基于其DPPIV抑制作用。本发明提供了包含通式（I）表示的化合物的二肽基肽酶IV抑制剂：

3. 发明申请

US20050014833A1 Cyclic compound and ppar agonist 失效
标题翻译：循环化合物和ppar激动剂
公开(公告)号：US20050014833A1
公开(公告)日：2005-01-20
申请号：US10486396
申请日：2002-08-16
申请人： Richard Clark , Fumiyoshi Matsuura , Eita Emori , Masanobu Shinoda , Shunji Kasai , Hideki Yoshitomi , Kazuto Yamazaki , Takashi Inoue , Sadakazu Miyashita , Taro Hihara
发明人： Richard Clark , Fumiyoshi Matsuura , Eita Emori , Masanobu Shinoda , Shunji Kasai , Hideki Yoshitomi , Kazuto Yamazaki , Takashi Inoue , Sadakazu Miyashita , Taro Hihara
IPC分类号： A61P1/00 , A61P1/04 , A61P3/04 , A61P3/06 , A61P3/10 , A61P9/00 , A61P9/10 , A61P19/10 , A61P29/00 , A61P35/00 , A61P37/02 , C07C233/87 , C07C251/60 , C07D213/53 , C07D263/32 , C07D277/56 , C07D307/24 , C07D307/30 , C07D317/32 , C07D339/08 , C07D405/06 , C07D405/12 , C07D407/12 , C07D413/12 , C07D417/12 , C07D417/14 , C07C229/02 , A61K31/195
CPC分类号： C07D213/53 , C07C233/87 , C07C251/60 , C07C2601/02 , C07C2601/14 , C07D263/32 , C07D277/56 , C07D307/24 , C07D307/30 , C07D317/32 , C07D339/08 , C07D405/06 , C07D405/12 , C07D407/12 , C07D413/12 , C07D417/12 , C07D417/14
摘要： The present invention provides a novel compound having an excellent PPAR agonist action. More specifically, it provides a compound represented by the following formula, a salt thereof, an ester thereof or a hydrate of them. Wherein a, b and c are the same as or different from one another and each represents 0 to 4; R1 to R6 are the same as or different from one another and each represents a hydrogen atom, a hydroxyl group, a cyano group, a halogen atom, etc.; A1 and A2 are the same as or different from each other and each represents a single bond, an oxygen atom, etc.; L, M and T each represent a single bond, an alkylene group having one to six carbon atoms, etc.; W represents a carboxyl group; the partial structure represented by the formula: represents a single bond or a double bond; X represents a single bond, an oxygen atom, —NRX1CQ1O—, etc.; Y represents Y1—Y2— (wherein Y1 represents a 5 to 14-membered aromatic ring having one to four substituents, etc.; and Y2 represents a single bond or a 5 to 14-membered aromatic ring); and the ring Z represents a 5 to 14-membered aromatic ring which have one to four substituents selected form the above-mentioned Group A, may have one or more hetero atoms and may be partially saturated.
摘要翻译：本发明提供具有优异的PPAR激动剂作用的新化合物。更具体地，它提供由下式表示的化合物，其盐，其酯或它们的水合物。其中a，b和c彼此相同或不同，各自表示0〜4; R 1〜R 6彼此相同或不同，表示氢原子，羟基，氰基，卤素原子等; A 1和A 2彼此相同或不同，各自表示单键，氧原子等; L，M和T各自表示单键，具有1〜6个碳原子的亚烷基等; W表示羧基; 由式表示的部分结构表示单键或双键; X表示单键，氧原子，-NR X 1 C 10 O等; Y表示Y 1 -Y 2 - （其中Y 1表示具有1〜4个取代基的5〜14元芳环等，Y 2表示单键或5〜14个芳环）; 并且环Z表示具有一至四个选自上述A组的取代基的5至14元芳环，可具有一个或多个杂原子并且可部分饱和。

4. 发明申请

US20100333216A1 Non-human gene-disrupted animal with disrupted Adam11 gene 失效
标题翻译：非人基因破坏动物与Adam11基因被破坏
公开(公告)号：US20100333216A1
公开(公告)日：2010-12-30
申请号：US11988619
申请日：2006-07-12
申请人： Koji Sagane , Eiki Takahashi , Kazuto Yamazaki , Turo Oki
发明人： Koji Sagane , Eiki Takahashi , Kazuto Yamazaki , Turo Oki
IPC分类号： G01N33/00 , A01K67/00 , A01K67/027 , C12N5/16 , C12N5/18 , C12N15/873 , A61K38/48 , C12N9/50 , C12N15/85 , A61K31/7088 , A61P25/00
CPC分类号： A01K67/0276 , A01K2217/075 , A01K2227/105 , A01K2267/0356 , A61K38/00 , C12N9/6489 , C12N15/8509 , G01N33/5088
摘要： It is an object of the present invention to provide a non-human gene-disrupted animal with a disrupted ADAM11 gene. According to the present invention, a non-human gene-disrupted animal, wherein either one of or both alleles of an ADAM11 gene are disrupted, is provided.
摘要翻译：本发明的目的是提供具有破坏的ADAM11基因的非人基因破坏的动物。根据本发明，提供了非人基因破坏的动物，其中ADAM11基因的一个或两个等位基因被破坏。

5. 发明授权

US07687664B2 Carboxylic acid derivative, a salt thereof or an ester of them, and medicament comprising it 失效
标题翻译：羧酸衍生物，其盐或它们的酯，以及包含它们的药物
公开(公告)号：US07687664B2
公开(公告)日：2010-03-30
申请号：US10479427
申请日：2002-06-04
申请人： Fumiyoshi Matsuura , Eita Emori , Masanobu Shinoda , Richard Clark , Shunji Kasai , Hideki Yoshitomi , Kazuto Yamazaki , Takashi Inoue , Sadakazu Miyashita , Taro Hihara
发明人： Fumiyoshi Matsuura , Eita Emori , Masanobu Shinoda , Richard Clark , Shunji Kasai , Hideki Yoshitomi , Kazuto Yamazaki , Takashi Inoue , Sadakazu Miyashita , Taro Hihara
IPC分类号： C07C57/34 , A01N37/44 , A01N43/08 , A01N43/10
CPC分类号： C07D213/40 , C07C59/68 , C07C69/732 , C07C69/734 , C07C233/87 , C07C235/52 , C07C271/22 , C07C271/28 , C07C2601/08 , C07C2601/14 , C07D213/75 , C07D213/79 , C07D213/80 , C07D261/18 , C07D277/56 , C07D307/68 , C07D307/79 , C07D333/38 , C07D417/04 , C07D417/12
摘要： The present invention provides novel carboxylic acid derivatives useful as an insulin sensitizer, a salt thereof or a hydrate of them, and a medicament comprising the derivative as the active ingredient. Specifically, it provides a carboxylic acid derivative represented by the following formula (I): (wherein Y, L, X, T, Z, U, M and W are defined in the specification) and a salt thereof, and ester thereof or a hydrate of them.
摘要翻译：本发明提供可用作胰岛素敏化剂，其盐或其水合物的新型羧酸衍生物和包含该衍生物作为活性成分的药物。具体地说，它提供由下式（I）表示的羧酸衍生物：其中Y，L，X，T，Z，U，M和W在说明书中定义）及其盐及其酯或它们的水合物。

6. 发明授权

US07244861B2 Benzene compound and salt thereof 失效
标题翻译：苯化合物及其盐
公开(公告)号：US07244861B2
公开(公告)日：2007-07-17
申请号：US10471254
申请日：2002-03-27
申请人： Fumiyoshi Matsuura , Eita Emori , Masanobu Shinoda , Richard Clark , Shunji Kasai , Hideki Yoshitomi , Kazuto Yamazaki , Takashi Inoue , Sadakazu Miyashita , Taro Hihara
发明人： Fumiyoshi Matsuura , Eita Emori , Masanobu Shinoda , Richard Clark , Shunji Kasai , Hideki Yoshitomi , Kazuto Yamazaki , Takashi Inoue , Sadakazu Miyashita , Taro Hihara
IPC分类号： C07C229/00 , C07C227/00
CPC分类号： C07D307/79 , A61K31/00 , C07C233/87 , C07C235/12 , C07C235/52 , C07C255/60 , C07C2601/08 , C07C2601/14 , C07D261/18 , C07D277/56 , C07D417/12
摘要： The present invention provides a medicament comprising a benzene compound useful as an insulin sensitizer, a salt thereof or a hydrate of them and a derivative of them as the active ingredient. Specifically, it provides a benzene compound represented by the following formula, a salt thereof or a hydrate of them. In the formula, X represents 1) a C6-10 aryl group which may have one or more substituents or 2) a 5- to 10-membered heteroaryl group which may have one or more substituents; Y represents a group represented by the formula: (in the above formulae, Ry1, Ry2 and Ry3 are the same as or different from one another and each represents a hydrogen atom, a halogen atom, a C1-6 alkyl group, a C1-6 alkoxy group, or a C3-7 cycloalkyl group) etc.; Z represents a group represented by the formula: (in the formula, m represents an integer of 0 to 2; Rz1, Rz2, Rz3 and Rz4 are the same as or different from one another and each represents a hydrogen atom, a halogen atom, a C1-6 alkyl group, a C1-6 alkoxy group, a C3-7 cycloalkyl group, a halogenated C1-6 alkyl group, a halogenated C1-6 alkoxy group etc.); and R1, R2, R3 and R4 are the same as or different from one another and each represents a hydrogen atom, a halogen atom, a C1-6 alkyl group, a C1-6 alkoxy group, a C3-7 cycloalkyl group etc.
摘要翻译：本发明提供一种药物，其包含可用作胰岛素敏化剂的苯化合物，其盐或它们的水合物及其衍生物作为活性成分。具体地说，它提供由下式表示的苯化合物，其盐或它们的水合物。在该式中，X表示1）可具有一个或多个取代基的C 6-14芳基，或2）可具有一个或多个取代基的5至10元杂芳基; Y表示由下式表示的基团：（在上式中，R y1，R y2，R y2，R y3和Y 3都相同或不同）各自表示氢原子，卤素原子，C 1-6烷基，C 1-6烷氧基或C 1 -C 6烷氧基， 3-7环烷基）等; Z表示由下式表示的基团：（式中，m表示0〜2的整数，R 0，Z 1，R z，Z 2，R z， SUP＆gt;和R z4彼此相同或不同，并且各自表示氢原子，卤素原子，C 1-6烷基，C 1〜 C 1-6烷基，C 3-7环烷基，卤代C 1-6烷基，卤代C 1 -6个烷氧基等）; 且R 1，R 2，R 3和R 4彼此相同或不同，并且各自表示氢原子，卤素原子，C 1-6烷基，C 1-6烷氧基，C 3-7烷基， SUB>环烷基等

7. 发明申请

US20060100199A1 Novel condensed imidazole derivatives 审中-公开
标题翻译：新型稠合咪唑衍生物
公开(公告)号：US20060100199A1
公开(公告)日：2006-05-11
申请号：US10516971
申请日：2003-06-03
申请人： Seiji Yoshikawa , Eita Emori , Eumiyoshi Matsuura , Richard Clark , Hironori Ikuta , Kazunobu Kira , Nobuyuki Yasuda , Tadashi Nagakura , Kazuto Yamazaki
发明人： Seiji Yoshikawa , Eita Emori , Eumiyoshi Matsuura , Richard Clark , Hironori Ikuta , Kazunobu Kira , Nobuyuki Yasuda , Tadashi Nagakura , Kazuto Yamazaki
IPC分类号： A61K31/551 , A61K31/522 , A61K31/503 , A61K31/4745 , C07D473/02 , C07D487/02
CPC分类号： C07D473/30 , C07D471/04 , C07D473/04 , C07D473/06 , C07D473/18 , C07D473/36 , C07D473/40 , C07D487/04 , C07D491/14
摘要： The present invention is related to compounds represented by the following formula, or salts or hydrates thereof wherein, T1 represents a 4- to 12-membered heterocyclic group containing one or two nitrogen atoms in the ring, which is a monocyclic or bicyclic structure that may have one or more substituents; X represents a C1-6 alkyl group which may have one or more substituents, or such; Z1 and Z2 each independently represent a nitrogen atom or a group represented by the formula —CR2—; R1 and R2 independently represent a hydrogen atom, a C1-6 alkyl group which may have one or more substituents, or a C1-6 alkoxy group which may have one or more substituents, or such. These are novel compounds that exhibit an excellent
摘要翻译：本发明涉及由下式表示的化合物或其盐或水合物，其中T 1表示在环中含有一个或两个氮原子的4至12元杂环基，其中是可以具有一个或多个取代基的单环或双环结构; X表示可具有一个或多个取代基的C 1-6烷基; Z 1和Z 2各自独立地表示氮原子或由式-CR 2 -O 2 - 表示的基团。 R 1和R 2独立地表示氢原子，可以具有一个或多个取代基的C 1-6烷基或C 可以具有一个或多个取代基的烷基，等等。这些是显示出优异的新型化合物

8. 发明申请

US20060094722A1 Combination drug 审中-公开
标题翻译：联合用药
公开(公告)号：US20060094722A1
公开(公告)日：2006-05-04
申请号：US10528353
申请日：2003-09-22
申请人： Nobuyuki Yasuda , Kazuto Yamazaki
发明人： Nobuyuki Yasuda , Kazuto Yamazaki
IPC分类号： A61K31/522 , A61K31/503
CPC分类号： A61K31/496 , A61K31/155 , A61K31/5025 , A61K31/522 , A61K45/06 , A61K2300/00
摘要： The present invention provides pharmaceutical agents comprising a dipeptidyl peptidase IV (DPPIV) inhibitor and a biguanide agent in combination, which enhance the effects of active circulating glucagon-like peptide-1 (GLP-1) and/or active circulating glucagon-like peptide-2 (GLP-2).
摘要翻译：本发明提供组合包含二肽基肽酶IV（DPPIV）抑制剂和双胍类药物的药剂，其增强了活性循环胰高血糖素样肽-1（GLP-1）和/或活性循环胰高血糖素样肽 - 2（GLP-2）。

9. 发明申请

US20060063787A1 Condensed imidazole derivatives 审中-公开
标题翻译：缩合咪唑衍生物
公开(公告)号：US20060063787A1
公开(公告)日：2006-03-23
申请号：US11212407
申请日：2005-08-26
申请人： Seiji Yoshikawa , Eita Emori , Fumiyoshi Matsuura , Richard Clark , Hironori Ikuta , Kazunobu Kira , Nobuyuki Yasuda , Tadashi Nagakura , Kazuto Yamazaki
发明人： Seiji Yoshikawa , Eita Emori , Fumiyoshi Matsuura , Richard Clark , Hironori Ikuta , Kazunobu Kira , Nobuyuki Yasuda , Tadashi Nagakura , Kazuto Yamazaki
IPC分类号： A61K31/522 , C07D473/02 , A61K31/4745 , C07D471/02
CPC分类号： C07D473/30 , C07D471/04 , C07D473/04 , C07D473/06 , C07D473/18 , C07D473/36 , C07D473/40 , C07D487/04 , C07D491/14
摘要： The present invention is related to compounds represented by the following formula, or salts or hydrates thereof wherein, T1 represents a 4- to 12-membered heterocyclic group containing one or two nitrogen atoms in the ring, which is a monocyclic or bicyclic structure that may have one or more substituents; X represents a C1-6 alkyl group which may have one or more substituents, or such; Z1 and Z2 each independently represent a nitrogen atom or a group represented by the formula —CR2—; R1 and R2 independently represent a hydrogen atom, a C1-6 alkyl group which may have one or more substituents, or a C1-6 alkoxy group which may have one or more substituents, or such. These are novel compounds that exhibit an excellent DPPIV-inhibiting activity.
摘要翻译：本发明涉及由下式表示的化合物或其盐或水合物

10. 发明授权

US07253178B2 Carboxylic acids 失效
标题翻译：羧酸
公开(公告)号：US07253178B2
公开(公告)日：2007-08-07
申请号：US10469173
申请日：2002-03-27
申请人： Hitoshi Harada , Masanobu Shinoda , Richard Clark , Fumiyoshi Matsuura , Eita Emori , Shunji Kasai , Hideki Yoshitomi , Kazuto Yamazaki , Takashi Inoue , Sadakazu Miyashita , Taro Hihara
发明人： Hitoshi Harada , Masanobu Shinoda , Richard Clark , Fumiyoshi Matsuura , Eita Emori , Shunji Kasai , Hideki Yoshitomi , Kazuto Yamazaki , Takashi Inoue , Sadakazu Miyashita , Taro Hihara
IPC分类号： A61K31/435 , A61K31/44 , C07D211/72 , C07D211/70
CPC分类号： C07D213/64 , C07D213/79
摘要： The present invention provides a novel carboxylic acid derivative, a salt thereof or a hydrate of them which is useful as an insulin sensitizer, and a medicament comprising the derivative as the effective ingredient. More specifically, it provides a carboxylic acid compound represented by the formula (I), a salt thereof or a hydrate of them. In the formula, Ar represents a 6- to 14-membered aromatic ring group which may have at least one substituent; R1, R2, R3, R4, R5, R6, R7 and R8 are the same as or different from each other and each represents a hydrogen atom, a halogen atom, a hydroxyl group, a C1-6 alkyl group or a C1-6 alkoxy group; X represents an oxygen atom or a methylene group; Y represents a group represented by the formula (II) or (III): (wherein Z represents a group represented by the formula (IV): (wherein R9, R10, R11 and R12 are the same as or different from each other and each represents a hydrogen atom, a halogen atom, a hydroxyl group, a C1-6 alkyl group or a C1-6 alkoxy group)); m is 0 or 1; and n is 0 or 1.
摘要翻译：本发明提供了可用作胰岛素敏化剂的新型羧酸衍生物，其盐或其水合物，以及包含该衍生物作为有效成分的药物。更具体地，它提供由式（I）表示的羧酸化合物，其盐或它们的水合物。在该式中，Ar表示可以具有至少一个取代基的6至14元芳环基团; R 1，R 2，R 3，R 4，R 5， R 6，R 7和R 8彼此相同或不同，并且各自表示氢原子，卤素原子，羟基，C 1-6烷基或C 1-6烷氧基; X表示氧原子或亚甲基; Y表示由式（II）或（III）表示的基团：（其中Z表示由式（IV）表示的基团：（其中R 9，R 10， >，R 11和R 12彼此相同或不同，并且各自表示氢原子，卤素原子，羟基，C 1 -C 12烷基， 1-6烷基或C 1-6烷氧基））; m为0或1; n为0或1。

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