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1. 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：

2. 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：

3. 发明申请

US20110212952A1 3,4-DIHYDROBENZOXAZINE COMPOUNDS AND INHIBITORS OF VANILLOID RECEPTOR SUBTYPE 1 (VRI) ACTIVITY 审中-公开
标题翻译：丹酚酸受体亚型1（VRI）活性的3,4-二氢苯并恶唑化合物和抑制剂
公开(公告)号：US20110212952A1
公开(公告)日：2011-09-01
申请号：US13019030
申请日：2011-02-01
申请人： Yoshihisa Koga , Shinji Yata , Takayuki Yamasaki , Tatsuya Matsumoto , Masahiro Sakata , Wataru Kondo , Yoshikazu Hori
发明人： Yoshihisa Koga , Shinji Yata , Takayuki Yamasaki , Tatsuya Matsumoto , Masahiro Sakata , Wataru Kondo , Yoshikazu Hori
IPC分类号： A61K31/538 , C07D413/04 , C07D413/14 , A61P25/24 , A61P25/04 , A61P31/12 , A61P29/00 , A61P17/00 , A61P11/06 , A61P1/04 , A61P13/00
CPC分类号： C07D413/04 , C07D413/14
摘要： A 3,4-dihydrobenzoxazine compound of the present invention is represented by the following formula [1] (wherein X is a nitrogen atom or CR3; R1 is a hydrogen atom or a halogen atom; R2 is a C1-6 alkoxy group which may be substituted with the same or different 1 to 5 substituents selected from a halogen atom and a hydroxyl group; and R3 is a halogen atom. However, R1 is a halogen atom when X is CR3). This compound is effective in treating diseases to which the vanilloid receptor subtype 1 (VR1) activity is involved, such as pain, etc.
摘要翻译：本发明的3,4-二氢苯并恶嗪化合物由下式[1]表示（其中X为氮原子或CR 3; R 1为氢原子或卤素原子; R 2为C 1-6烷氧基，被相同或不同的1至5个选自卤素原子和羟基的取代基取代; R3为卤素原子，但当X为CR 3时，R 1为卤素原子。该化合物可有效治疗涉及到香草素受体亚型1（VR1）活性的疾病，如疼痛等。

4. 发明授权

US07906508B2 3,4-dihydrobenzoxazine compounds and inhibitors of vanilloid receptor subtype 1 (VRI) activity 有权
标题翻译： 3,4-二氢苯并恶嗪化合物和香草素受体亚型1（VRI）活性的抑制剂
公开(公告)号：US07906508B2
公开(公告)日：2011-03-15
申请号：US11616962
申请日：2006-12-28
申请人： Yoshihisa Koga , Shinji Yata , Takayuki Yamasaki , Tatsuya Matsumoto , Masahiro Sakata , Wataru Kondo , Yoshikazu Hori
发明人： Yoshihisa Koga , Shinji Yata , Takayuki Yamasaki , Tatsuya Matsumoto , Masahiro Sakata , Wataru Kondo , Yoshikazu Hori
IPC分类号： C07D413/04 , C07D413/14 , A61K31/538
CPC分类号： C07D413/04 , C07D413/14
摘要： A 3,4-dihydrobenzoxazine compound of the present invention is represented by the following formula [1] (wherein X is a nitrogen atom or CR3; R1 is a hydrogen atom or a halogen atom; R2 is a C1-6 alkoxy group which may be substituted with the same or different 1 to 5 substituents selected from a halogen atom and a hydroxyl group; and R3 is a halogen atom. However, R1 is a halogen atom when X is CR3). This compound is effective in treating diseases to which the vanilloid receptor subtype 1 (VR1) activity is involved, such as pain, etc.
摘要翻译：本发明的3,4-二氢苯并恶嗪化合物由下式[1]表示（其中X为氮原子或CR 3; R 1为氢原子或卤素原子; R 2为C 1-6烷氧基，被相同或不同的1至5个选自卤素原子和羟基的取代基取代; R3为卤素原子，但当X为CR 3时，R 1为卤素原子。该化合物可有效治疗涉及到香草素受体亚型1（VR1）活性的疾病，如疼痛等。

5. 发明申请

US20070149517A1 3,4-DIHYDROBENZOXAZINE COMPOUNDS AND INHIBITORS OF VANILLOID RECEPTOR SUBTYPE 1 (VRI) ACTIVITY 有权
标题翻译：丹酚酸受体亚型1（VRI）活性的3,4-二氢苯并恶唑化合物和抑制剂
公开(公告)号：US20070149517A1
公开(公告)日：2007-06-28
申请号：US11616962
申请日：2006-12-28
申请人： Yoshihisa Koga , Shinji Yata , Takayuki Yamasaki , Tatsuya Matsumoto , Masahiro Sakata , Wataru Kondo , Yoshikazu Hori
发明人： Yoshihisa Koga , Shinji Yata , Takayuki Yamasaki , Tatsuya Matsumoto , Masahiro Sakata , Wataru Kondo , Yoshikazu Hori
IPC分类号： A61K31/538 , C07D265/36
CPC分类号： C07D413/04 , C07D413/14
摘要： A 3,4-dihydrobenzoxazine compound of the present invention is represented by the following formula [1] (wherein X is a nitrogen atom or CR3; R1 is a hydrogen atom or a halogen atom; R2 is a C1-6 alkoxy group which may be substituted with the same or different 1 to 5 substituents selected from a halogen atom and a hydroxyl group; and R3 is a halogen atom. However, R1 is a halogen atom when X is CR3). This compound is effective in treating diseases to which the vanilloid receptor subtype 1 (VR1) activity is involved, such as pain, etc.
摘要翻译：本发明的3,4-二氢苯并恶嗪化合物由下式[1]表示（其中X为氮原子或CR 3，R 1为氢原子或卤素原子; R 2是可被相同或不同的1至5个选自卤素原子和羟基的取代基取代的C 1-6烷氧基; 3是卤素原子，但当X是CR 3时，R 1是卤素原子。该化合物可有效治疗涉及到香草素受体亚型1（VR1）活性的疾病，如疼痛等。

6. 发明申请

US20060035939A1 3-Aminobenzamide compounds and inhibitors of vanilloid receptor subtype 1 (VR1) activity 审中-公开
标题翻译： 3-氨基苯甲酰胺化合物和香草素受体亚型1（VR1）活性抑制剂
公开(公告)号：US20060035939A1
公开(公告)日：2006-02-16
申请号：US11181235
申请日：2005-07-14
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： A61K31/455 , A61K31/165
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, neuropathic pain, rheumatoid arthritis pain, and neuralgia.
摘要翻译：本发明涉及有效抑制香草素受体亚型1（VR1）活性的下式所示的新型3-氨基苯甲酰胺化合物（其中，例如R 1是C 1-6烷基，可以被取代，R 2是氢原子，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是1〜5的整数，P 是碳或杂环）或其药学上可接受的盐。包含3-氨基苯甲酰胺化合物或其可药用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。

7. 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。

8. 发明授权

US5807850A Therapeutic agent for osteoporosis and triazepine compound 失效
标题翻译：骨质疏松症和三氮化合物治疗剂
公开(公告)号：US5807850A
公开(公告)日：1998-09-15
申请号：US836243
申请日：1997-05-05
申请人： Takeshi Nakamura , Yoshihisa Koga , Masanori Shindo
发明人： Takeshi Nakamura , Yoshihisa Koga , Masanori Shindo
IPC分类号： C07D255/04 , C07D401/06 , C07D487/04 , C07D495/04 , C07D495/14 , A61K31/55 , C07D409/12
CPC分类号： C07D401/06 , C07D255/04 , C07D487/04 , C07D495/04 , C07D495/14
摘要： Therapeutic agents for osteoporosis comprising, as an active ingredient, a triazepine compound of the formula �I! ##STR1## wherein R.sup.1 is aryl or heteroaryl; R.sup.2 is hydrogen atom, hydroxy, halogen atom or lower alkyl; R.sup.4 is hydrogen atom or halogen atom, or R.sup.2 and R.sup.4 form carbonyl combinedly together with the carbon atom to which they bond; R.sup.3 is hydrogen atom, lower alkyl, lower alkoxy, cycloalkyl, aryl, heteroaryl, --X--Y wherein X is --(CH.sub.2).sub.m --, --CO--, --COCH.sub.2 --, --NH--, --NHCH.sub.2 --, --CH.sub.2 NH--, --CH.sub.2 NHCO--, --OCH.sub.2 --, --(CH.sub.2).sub.n O-- or --CH.sub.2 S-- and Y is halogen atom, cycloallyl, aryl or heteroaryl; and A is benzene ring or thiophene ring, or a salt thereof, novel triazepine compounds, and intermediate triazepine compounds for producing these triazepine compounds. The triazepine compounds of the formula �I! have superior bone resorption-inhibitory action and are useful as therapeutic agents for osteoporosis.
摘要翻译： PCT No.PCT / JP95 / 02338 Sec。 371日期：1997年5月5日 102（e）日期1997年5月5日PCT提交1995年11月15日PCT公布。公开号WO96 / 16062 日期：1996年5月30日用于骨质疏松症的治疗剂包括作为活性成分的式[I]的三氮化合物其中R 1是芳基或杂芳基; R2是氢原子，羟基，卤素原子或低级烷基; R4是氢原子或卤原子，或R2和R4与它们键合的碳原子一起形成羰基; R3是氢原子，低级烷基，低级烷氧基，环烷基，芳基，杂芳基，-XY其中X是 - （CH2）m-，-CO-，-COCH2-，-NH-，-NHCH2-，-CH2NH-， - （CH 2）n O-或-CH 2 S-，Y是卤素原子，环烯基，芳基或杂芳基; A是苯环或噻吩环，或其盐，新的三氮化合物和用于制备这些三氮化合物的中间体三氮化合物。式[I]的三氮化合物具有优异的骨吸收抑制作用，可用作骨质疏松症的治疗剂。

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