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1. 发明授权

US07683059B2 Triazole compounds and uses related thereto 失效
标题翻译：三唑化合物及其用途
公开(公告)号：US07683059B2
公开(公告)日：2010-03-23
申请号：US10587846
申请日：2006-09-05
申请人： Mario G. Cardozo , Jay P. Powers , Hiroyuki Goto , Kazuhito Harada , Katsuaki Imamura , Makoto Kakutani , Isamu Matsuda , Yasuhiro Ohe , Shinji Yata
发明人： Mario G. Cardozo , Jay P. Powers , Hiroyuki Goto , Kazuhito Harada , Katsuaki Imamura , Makoto Kakutani , Isamu Matsuda , Yasuhiro Ohe , Shinji Yata
IPC分类号： A61K31/4196 , A61K31/5377 , C07D413/12 , C07D249/08
CPC分类号： C07D401/12 , A61K31/18 , A61K31/4196 , A61K31/64 , A61K38/28 , A61K45/06 , C04B35/632 , C07D249/08 , C07D249/14 , C07D401/04 , C07D401/10 , C07D401/14 , C07D403/04 , C07D403/10 , C07D405/04 , C07D409/04 , C07D413/10 , C07D491/10
摘要： The present invention provides a triazole compound of the following formula: a prodrug thereof or a pharmaceutically acceptable salt thereof. The above-mentioned triazole compound is useful as a therapeutic drug for the treatment of diabetes, obesity or metabolic syndrome.
摘要翻译：本发明提供下式的三唑化合物：其前药或其药学上可接受的盐。上述三唑化合物可用作治疗糖尿病，肥胖或代谢综合征的治疗药物。

2. 发明申请

US20080249084A1 Triazole Compounds and Uses Related Thereto 失效
标题翻译：三唑化合物及其用途
公开(公告)号：US20080249084A1
公开(公告)日：2008-10-09
申请号：US10587846
申请日：2004-10-27
申请人： Jay P. Powers , Mario G. Cardozo , Hiroyuki Goto , Kazuhito Harada , Katsuaki Imamura , Makoto Kakutani , Isamu Matsuda , Yasuhiro Ohe , Shinji Yata
发明人： Jay P. Powers , Mario G. Cardozo , Hiroyuki Goto , Kazuhito Harada , Katsuaki Imamura , Makoto Kakutani , Isamu Matsuda , Yasuhiro Ohe , Shinji Yata
IPC分类号： A61K31/4196 , C07D401/14 , C07D401/04 , C07D249/08 , C07D403/10 , C07D413/12 , A61P3/04 , A61P3/10 , C07D417/04 , A61K31/554 , A61K31/5377 , A61K31/496 , A61K31/454
CPC分类号： C07D401/12 , A61K31/18 , A61K31/4196 , A61K31/64 , A61K38/28 , A61K45/06 , C04B35/632 , C07D249/08 , C07D249/14 , C07D401/04 , C07D401/10 , C07D401/14 , C07D403/04 , C07D403/10 , C07D405/04 , C07D409/04 , C07D413/10 , C07D491/10
摘要： The present invention provides a triazole compound of the following formula: a prodrug thereof or a pharmaceutically acceptable salt thereof. The above-mentioned triazole compound is useful as a therapeutic drug for the treatment of diabetes, obesity or metabolic syndrome.
摘要翻译：本发明提供下式的三唑化合物：其前药或其药学上可接受的盐。上述三唑化合物可用作治疗糖尿病，肥胖或代谢综合征的治疗药物。

3. 发明申请

US20070072908A1 Heterocyclic compounds 审中-公开
标题翻译：杂环化合物
公开(公告)号：US20070072908A1
公开(公告)日：2007-03-29
申请号：US11448980
申请日：2006-06-08
申请人： Hiroshi Yamamoto , Yasuhiro Ohe , Hiroyuki Goto , Kazuhito Harada , Shinji Yata , Takashi Ito , Jun Nishiu , Makoto Kakutani , Shunsuke Fujii , Kota Asahina
发明人： Hiroshi Yamamoto , Yasuhiro Ohe , Hiroyuki Goto , Kazuhito Harada , Shinji Yata , Takashi Ito , Jun Nishiu , Makoto Kakutani , Shunsuke Fujii , Kota Asahina
IPC分类号： A61K31/454 , C07D403/14
CPC分类号： C07D403/06 , C07D401/14 , C07D403/14 , C07D409/14 , C07D413/14 , C07D417/14
摘要： The present invention provides a compound represented by the following formula [1′] or a salt thereof: wherein ring A, R2, R3, R4 and X are as defined in the description, and an agent for the treatment or prophylaxis of a pathology involving glucocorticoid, or a 11βHSD1 inhibitor, containing the compound or a salt thereof.
摘要翻译：本发明提供由下式[1']表示的化合物或其盐：其中环A，R 2，R 3，R 4， / SUP＆gt;和X如说明书中所定义，以及用于治疗或预防包含该化合物或其盐的糖皮质激素或11betaHSD1抑制剂的病理的药剂。

4. 发明申请

US20110245223A1 HETEROCYCLIC COMPOUNDS 审中-公开
标题翻译：杂环化合物
公开(公告)号：US20110245223A1
公开(公告)日：2011-10-06
申请号：US12958071
申请日：2010-12-01
申请人： Hiroshi Yamamoto , Yasuhiro Ohe , Hiroyuki Goto , Kazuhito Harada , Shinji Yata , Takashi Ito , Jun Nishiu , Makoto Kakutani , Shunsuke Fujii , Kota Asahina
发明人： Hiroshi Yamamoto , Yasuhiro Ohe , Hiroyuki Goto , Kazuhito Harada , Shinji Yata , Takashi Ito , Jun Nishiu , Makoto Kakutani , Shunsuke Fujii , Kota Asahina
IPC分类号： A61K31/4545 , C07D401/14 , A61K31/454 , C07D417/14 , A61K31/541 , A61K31/496 , C07D409/14 , A61K31/506 , A61K31/55 , C07D413/14 , A61K31/538 , C07C205/56 , C07C201/12 , C07D207/277 , C07D207/26 , C07D207/04 , A61P3/10 , A61P3/04 , A61P1/16 , A61P9/12 , A61P27/06 , A61P19/10 , A61P25/18 , A61P37/04
CPC分类号： C07D403/06 , C07D401/14 , C07D403/14 , C07D409/14 , C07D413/14 , C07D417/14
摘要： The present invention provides a compound represented by the following formula [1′] or a salt thereof: wherein ring A, R2, R3, R4 and X are as defined in the description, and an agent for the treatment or prophylaxis of a pathology involving glucocorticoid, or a 11βHSD1 inhibitor, containing the compound or a salt thereof.
摘要翻译：本发明提供由下式[1']表示的化合物或其盐：其中环A，R 2，R 3，R 4和X如说明书中所定义，和用于治疗或预防涉及糖皮质激素或含有该化合物或其盐的11βBBHSD1抑制剂。

5. 发明授权

US08008292B2 Condensed benzamide compounds and inhibitors of vanilloid receptor subtype 1 (VR1) activity 有权
标题翻译：浓缩的苯甲酰胺化合物和香草素受体亚型1（VR1）活性的抑制剂
公开(公告)号：US08008292B2
公开(公告)日：2011-08-30
申请号：US11183265
申请日：2005-07-15
申请人： Yoshihisa Koga , Shinji Yata , Takashi Watanabe , Takuya Matsuo , Takayuki Yamasaki , Masahiro Sakata , Wataru Kondo , Hidekazu Ozeki , Yoshikazu Hori
发明人： Yoshihisa Koga , Shinji Yata , Takashi Watanabe , Takuya Matsuo , Takayuki Yamasaki , Masahiro Sakata , Wataru Kondo , Hidekazu Ozeki , Yoshikazu Hori
IPC分类号： A61K31/535 , C07D265/36 , C07D498/02
CPC分类号： A61K45/06 , C07D401/04 , C07D413/04 , C07D413/14 , C07D417/04 , C07D417/14
摘要： To provide a compound having an excellent inhibitory effect on vanilloid receptor subtype 1 (VR1) activity which is effective in treating diseases to which the vanilloid receptor subtype 1 (VR1) activity is involved, such as pain, acute pain, chronic pain, neuropathic pain, rheumatoid arthritis pain, neuralgia, etc. and a pharmaceutical composition containing the compound. The object has been attained by a condensed benzamide compound represented by the following formula (the symbols in the formula have the same meanings defined in the specification) or its salt:
摘要翻译：为了提供对于涉及涉及香草素受体亚型1（VR1）活性的疾病（例如疼痛，急性疼痛，慢性疼痛，神经性疼痛）有效治疗对香草素受体亚型1（VR1）活性具有优异抑制作用的化合物，类风湿性关节炎疼痛，神经痛等，以及含有该化合物的药物组合物。本发明的目的是通过下述式（式中的符号与说明书中所定义的相同含义）或其盐进行缩合的苯甲酰胺化合物来实现：

6. 发明申请

US20100062972A1 TRIAZOLE COMPOUNDS AND USES RELATED THERETO 失效
标题翻译：三唑化合物及其相关用途
公开(公告)号：US20100062972A1
公开(公告)日：2010-03-11
申请号：US12621922
申请日：2009-11-19
申请人： JAY P. POWERS , Mario G. CARDOZO , Hiroyuki GOTO , Kazuhito HARADA , Katsuaki IMAMURA , Makoto KAKUTANI , Isamu MATSUDA , Yasuhiro OHE , Shinji YATA
发明人： JAY P. POWERS , Mario G. CARDOZO , Hiroyuki GOTO , Kazuhito HARADA , Katsuaki IMAMURA , Makoto KAKUTANI , Isamu MATSUDA , Yasuhiro OHE , Shinji YATA
IPC分类号： A61K31/4196 , A61P3/10 , A61K31/4545 , A61K31/454 , A61K31/5377 , A61K31/422 , A61K31/438 , A61K31/496 , A61K38/28 , A61P3/04
CPC分类号： C07D401/12 , A61K31/18 , A61K31/4196 , A61K31/64 , A61K38/28 , A61K45/06 , C04B35/632 , C07D249/08 , C07D249/14 , C07D401/04 , C07D401/10 , C07D401/14 , C07D403/04 , C07D403/10 , C07D405/04 , C07D409/04 , C07D413/10 , C07D491/10
摘要： The present invention provides a triazole compound of the following formula: a prodrug thereof or a pharmaceutically acceptable salt thereof. The above-mentioned triazole compound has superior HSD1 inhibitory activity, and is useful as an HSD1 inhibitor, a therapeutic drug of diabetes or a therapeutic drug of obesity or a therapeutic drug of metabolic syndrome.
摘要翻译：本发明提供下式的三唑化合物：其前药或其药学上可接受的盐。上述三唑化合物具有优异的HSD1抑制活性，可用作HSD1抑制剂，糖尿病治疗药或肥胖症治疗药物或代谢综合征治疗药物。

7. 发明申请

US20060035882A1 CONDENSED BENZAMIDE COMPOUNDS AND INHIBITORS OF VANILLOID RECEPTOR SUBTYPE 1 (VR1) ACTIVITY 有权
标题翻译：甘氨酸受体亚型1（VR1）活性的简并的苄基化合物和抑制剂
公开(公告)号：US20060035882A1
公开(公告)日：2006-02-16
申请号：US11183265
申请日：2005-07-15
申请人： Yoshihisa Koga , Shinji Yata , Takashi Watanabe , Takuya Matsuo , Takayuki Yamasaki , Masahiro Sakata , Wataru Kondo , Hidekazu Ozeki , Yoshikazu Hori
发明人： Yoshihisa Koga , Shinji Yata , Takashi Watanabe , Takuya Matsuo , Takayuki Yamasaki , Masahiro Sakata , Wataru Kondo , Hidekazu Ozeki , Yoshikazu Hori
IPC分类号： A61K31/5513 , A61K31/553 , A61K31/554
CPC分类号： A61K45/06 , C07D401/04 , C07D413/04 , C07D413/14 , C07D417/04 , C07D417/14
摘要： To provide a compound having an excellent inhibitory effect on vanilloid receptor subtype 1 (VR1) activity which is effective in treating diseases to which the vanilloid receptor subtype 1 (VR1) activity is involved, such as pain, acute pain, chronic pain, neuropathic pain, rheumatoid arthritis pain, neuralgia, etc. and a pharmaceutical composition containing the compound. The object has been attained by a condensed benzamide compound represented by the following formula (the symbols in the formula have the same meanings defined in the specification) or its salt:
摘要翻译：为了提供对于涉及涉及香草素受体亚型1（VR1）活性的疾病（例如疼痛，急性疼痛，慢性疼痛，神经性疼痛）有效治疗对香草素受体亚型1（VR1）活性具有优异抑制作用的化合物，类风湿性关节炎疼痛，神经痛等，以及含有该化合物的药物组合物。本发明的目的是通过下述式（式中的符号与说明书中所定义的相同含义）或其盐进行缩合的苯甲酰胺化合物来实现：

8. 发明申请

US20050272793A1 Pyrazole compounds and uses related thereto 失效
标题翻译：吡唑化合物及其用途
公开(公告)号：US20050272793A1
公开(公告)日：2005-12-08
申请号：US11084734
申请日：2005-03-18
申请人： Hiroyuki Goto , Makoto Kakutani , Jun Nishiu , Yasuhiro Ohe , Jay Powers , Shinji Yata
发明人： Hiroyuki Goto , Makoto Kakutani , Jun Nishiu , Yasuhiro Ohe , Jay Powers , Shinji Yata
IPC分类号： A61K31/415 , C07D211/04 , C07D231/12 , C07D263/04 , C07D401/04 , C07D401/06 , C07D401/08 , C07D401/10 , C07D401/14 , C07D403/10 , C07D405/04 , C07D413/10
CPC分类号： C07D231/12 , C07D401/04 , C07D401/06 , C07D401/08 , C07D401/10 , C07D401/14 , C07D403/10 , C07D405/04 , C07D413/10
摘要： Substituted pyrazoles are provided that are useful for the treatment of, for example, diabetes, obesity and metabolic syndrome.
摘要翻译：提供了可用于治疗例如糖尿病，肥胖症和代谢综合征的取代的吡唑。

9. 发明授权

US5536737A Compound having prolyl endopeptidase inhibitory activity and pharmaceutical use thereof 失效
标题翻译：具有脯氨酰内肽酶抑制活性的化合物及其药物用途
公开(公告)号：US5536737A
公开(公告)日：1996-07-16
申请号：US446592
申请日：1995-05-24
申请人： Koji Kobayashi , Minoru Akamatsu , Shinji Yata , Hiroyuki Abe , Katsuo Toide , Motohiro Kogayu , Itsuo Uchida
发明人： Koji Kobayashi , Minoru Akamatsu , Shinji Yata , Hiroyuki Abe , Katsuo Toide , Motohiro Kogayu , Itsuo Uchida
IPC分类号： C07D207/16 , C07D277/06 , C07D417/06 , C07D403/06 , A61K31/40 , A61K31/425
CPC分类号： C07D417/06 , C07D207/16 , C07D277/06
摘要： Compounds of the formula ##STR1## wherein R is a hydrogen atom or an acyl; U is --O--, --CHR.sup.1 -- or --NR.sup.2 -- wherein R.sup.1 is a hydrogen atom or a hetero ring, and R.sup.2 is a hydrogen atom or a lower alkoxycarbonyl lower alkyl; V is --O--, --S--, --CHR.sup.3 -- or --NR.sup.4 -- wherein R.sup.3 is a hydrogen atom or a lower alkoxycarbonyl, and R.sup.4 is a hydrogen atom, a lower alkyl or an acyl; W is methyl, a hetero ring or optionally substituted phenyl; X and Y are the same or different and each is --CH.sub.2 -- or --S--; m is an integer of 0 to 6; and n is an integer of 1 to 4, and pharmaceutically acceptable salts thereof.The compounds of the present invention have specifically strong inhibitory activity against prolyl endopeptidase, and suppress decomposition and inactivation of TRH, substance P, neurotensin, vasopressin and the like. Accordingly, the compounds can be used for the prophylaxis and/or treatment of dementia and amnesia including Alzheimer's disease.
摘要翻译： PCT No.PCT / JP93 / 01687 Sec。 371日期：1995年5月24日 102（e）日期1995年5月24日PCT提交1993年11月17日PCT公布。公开号WO94 / 12474 日期：1997年11月17日。式（I）的化合物，其中R是氢原子或酰基; U是-O-，-CHR1-或-NR2-，其中R1是氢原子或杂环，R2是氢原子或低级烷氧基羰基低级烷基; V是-O - ， - S - ， - CH 3 - 或-NR 4 - ，其中R 3是氢原子或低级烷氧基羰基，R 4是氢原子，低级烷基或酰基。 W是甲基，杂环或任选取代的苯基; X和Y相同或不同，各自为-CH 2 - 或-S-; m为0〜6的整数。 n为1〜4的整数，及其药学上可接受的盐。本发明的化合物对脯氨酰内肽酶具有特异的强抑制活性，抑制TRH，物质P，神经降压素，加压素等的分解失活。因此，该化合物可用于预防和/或治疗包括阿尔茨海默病在内的痴呆和遗忘。

10. 发明申请

US20120115827A1 3-AMINOBENZAMIDE COMPOUNDS AND VANILLOID RECEPTOR SUBTYPE 1 (VR1) INHIBITORS 审中-公开
标题翻译： 3-氨基苯甲酸化合物和VANILLOID受体亚型1（VR1）抑制剂
公开(公告)号：US20120115827A1
公开(公告)日：2012-05-10
申请号：US13155143
申请日：2011-06-07
申请人： Yoshihisa Koga , Shinji Yata , Takashi Watanabe , Takuya Matsuo , Masahiro Sakata , Wataru Kondo
发明人： Yoshihisa Koga , Shinji Yata , Takashi Watanabe , Takuya Matsuo , Masahiro Sakata , Wataru Kondo
IPC分类号： A61K31/56 , A61K31/44 , A61K31/4402 , C07D498/04 , A61K31/5383 , C07C237/40 , A61K31/167 , C07D413/04 , A61K31/538 , C07D401/12 , A61K31/4709 , A61K31/444 , A61K31/4545 , C07D213/79 , C07D213/81 , A61P29/00 , A61P25/00 , A61P25/28 , A61P9/00 , A61P17/00 , A61P17/04 , A61P11/06 , A61P11/00 , A61P13/10 , A61P1/00 , A61P1/04 , A61P31/12 , A61P25/08 , A61P9/06 , A61P23/00 , A61P11/02 , A61P25/06 , A61P19/02 , A61M37/00 , C07D213/74
CPC分类号： C07C237/40 , C07D213/74 , C07D213/82 , C07D401/12 , C07D413/04
摘要： The present invention relates to a novel 3-aminobenzamide, compound represented by the following formula which effectively inhibits vanilloid receptor subtype 1 (VR1) activity (wherein, for example, R1 is a C1-6 alkyl group which may be substituted, R2 is a hydrogen atom, a C1-6 alkyl group or a C1-6 alkoxy group which may be substituted, R3 is a hydrogen atom or a C1-6 alkyl group, R4 is a C1-6 alkyl group, a C1-6 alkoxy group, or a halo C1-6 alkyl group, m is an integer of 1 to 5 and P is a carbon or hetero ring) or a pharmaceutically acceptable salt thereof. The pharmaceutical composition comprising as active ingredients the 3-aminobenzamide, compound or a pharmaceutically acceptable salt thereof is useful for treating diseases involved in VR1 activity such as pain, acute pain, chronic pain, neuropathicpain, rheumatoid arthritis pain, and neuralgia.
摘要翻译：本发明涉及一种新的3-氨基苯甲酰胺，其由下式表示，其有效抑制香草素受体亚型1（VR1）活性（其中，例如，R 1为可被取代的C 1-6烷基，R 2为氢原子，可以被取代的C 1-6烷基或C 1-6烷氧基，R 3是氢原子或C 1-6烷基，R 4是C 1-6烷基，C 1-6烷氧基，或卤代C 1-6烷基，m为1〜5的整数，P为碳或杂环）或其药学上可接受的盐。包含3-氨基苯甲酰胺，化合物或其药学上可接受的盐作为活性成分的药物组合物可用于治疗涉及VR1活性的疾病，例如疼痛，急性疼痛，慢性疼痛，神经性疼痛，类风湿性关节炎疼痛和神经痛。

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