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1. 发明授权

US07189717B2 Medicinal compositions promoting bowel movement 失效
标题翻译：促进排便的药物成分
公开(公告)号：US07189717B2
公开(公告)日：2007-03-13
申请号：US10257091
申请日：2001-04-26
申请人： Masahiro Yasuda , Hitoshi Harada , Shuhei Miyazawa , Seiichi Kobayashi , Kokichi Harada , Takayuki Hida , Hisashi Shibata , Nobuyuki Yasuda , Osamu Asano , Yoshihiko Kotake
发明人： Masahiro Yasuda , Hitoshi Harada , Shuhei Miyazawa , Seiichi Kobayashi , Kokichi Harada , Takayuki Hida , Hisashi Shibata , Nobuyuki Yasuda , Osamu Asano , Yoshihiko Kotake
IPC分类号： A61K31/506
CPC分类号： A61K31/506 , A61K31/519 , A61K31/522 , A61K31/5377 , A61K31/7076 , H04B10/112
摘要： The present invention provides a medicament having a gentle but strong defecation-promoting action without causing diarrhea. That is, it provides a defecation-promoting agent comprising a compound having an adenosine A2 receptor antagonism, preferably an adenosine A2b receptor antagonism, or a salt thereof.
摘要翻译：本发明提供一种具有温和但强烈的排便促进作用而不引起腹泻的药物。也就是说，它提供了包含具有腺苷A 2受体拮抗作用的化合物，优选腺苷A 2b受体拮抗剂或其盐的排便促进剂。

2. 发明申请

US20060270674A1 Pharmaceutical composition promoting defecation 审中-公开
标题翻译：药物组成促进排便
公开(公告)号：US20060270674A1
公开(公告)日：2006-11-30
申请号：US11500903
申请日：2006-08-09
申请人： Masahiro Yasuda , Hitoshi Harada , Shuhei Miyazawa , Seiichi Kobayashi , Kokichi Harada , Takayuki Hida , Hisashi Shibata , Nobuyuki Yasuda , Osamu Asano , Yoshihiko Kotake
发明人： Masahiro Yasuda , Hitoshi Harada , Shuhei Miyazawa , Seiichi Kobayashi , Kokichi Harada , Takayuki Hida , Hisashi Shibata , Nobuyuki Yasuda , Osamu Asano , Yoshihiko Kotake
IPC分类号： A61K31/5377 , A61K31/506 , C07D413/14 , C07D403/14
CPC分类号： A61K31/506 , A61K31/519 , A61K31/522 , A61K31/5377 , A61K31/7076 , H04B10/112
摘要： The present invention provides a medicament having a gentle but strong defecation-promoting action without causing diarrhea. That is, it provides a defecation-promoting agent comprising a compound having an adenosine A2receptor antagonism, preferably an adenosine A2b receptor antagonism, or a salt thereof.
摘要翻译：本发明提供一种具有温和但强烈的排便促进作用而不引起腹泻的药物。也就是说，它提供了包含具有腺苷A 2受体拮抗作用的化合物，优选腺苷A 2b受体拮抗剂或其盐的排便促进剂。

3. 发明申请

US20070054876A1 Pharmaceutical composition promoting defecation 审中-公开
标题翻译：药物组成促进排便
公开(公告)号：US20070054876A1
公开(公告)日：2007-03-08
申请号：US11594132
申请日：2006-11-08
申请人： Masahiro Yasuda , Hitoshi Harada , Shuhei Miyazawa , Seiichi Kobayashi , Kokichi Harada , Takayuki Hida , Hisashi Shibata , Nobuyuki Yasuda , Osamu Asano , Yoshihiko Kotake
发明人： Masahiro Yasuda , Hitoshi Harada , Shuhei Miyazawa , Seiichi Kobayashi , Kokichi Harada , Takayuki Hida , Hisashi Shibata , Nobuyuki Yasuda , Osamu Asano , Yoshihiko Kotake
IPC分类号： A61K31/7076 , A61K31/522
CPC分类号： A61K31/506 , A61K31/519 , A61K31/522 , A61K31/5377 , A61K31/7076 , H04B10/112
摘要： The present invention provides a medicament having a gentle but strong defecation-promoting action without causing diarrhea. That is, it provides a defecation-promoting agent comprising a compound having an adenosine A2 receptor antagonism, preferably an adenosine A2b receptor antagonism, or a salt thereof.
摘要翻译：本发明提供一种具有温和但强烈的排便促进作用而不引起腹泻的药物。也就是说，它提供了包含具有腺苷A 2受体拮抗作用的化合物，优选腺苷A 2b受体拮抗剂或其盐的排便促进剂。

4. 发明申请

US20050004149A1 Pyrimidine compound and medicinal composition thereof 失效
公开(公告)号：US20050004149A1
公开(公告)日：2005-01-06
申请号：US10492905
申请日：2002-10-22
申请人： Hitoshi Harada , Osamu Asano , Masato Ueda , Shuhei Miyazawa , Yoshihiko Kotake , Yasuhiro Kabasawa , Masahiro Yasuda , Nobuyuki Yasuda , Daisuke Iida , Junichi Nagakawa , Kazuo Hirota , Makoto Nakagawa
发明人： Hitoshi Harada , Osamu Asano , Masato Ueda , Shuhei Miyazawa , Yoshihiko Kotake , Yasuhiro Kabasawa , Masahiro Yasuda , Nobuyuki Yasuda , Daisuke Iida , Junichi Nagakawa , Kazuo Hirota , Makoto Nakagawa
IPC分类号： A61K31/506 , A61P1/00 , A61P1/10 , A61P3/04 , A61P3/10 , A61P9/12 , A61P11/06 , A61P13/02 , A61P19/10 , A61P25/16 , A61P25/28 , A61P43/00 , C07D401/04 , C07D405/14 , C07D409/14 , C07
CPC分类号： C07D405/14 , A61K31/506 , C07D401/04 , C07D409/14
摘要： The present invention provides a novel pyrimidine compound having an excellent adenosine receptor (A1, A2A, A2B receptor) antagonistic action. More specifically, it provides a compound represented by the following formula, a salt thereof or a solvate of them. In the formula, R1 and R2 are the same as or different from each other and each represents a hydrogen atom, an alkyl group having one to six carbon atoms which may be substituted, an alkenyl group having two to six carbon atoms which may be substituted, an alkynyl group having two to six carbon atoms which may be substituted, a cycloalkyl group having three to eight carbon atoms which may be substituted, a cycloalkenyl group having three to eight carbon atoms which may be substituted, a 5 to 14-membered non-aromatic heterocyclic group which may be substituted, an aromatic hydrocarbon cyclic group having six to fourteen carbon atoms which may be substituted, a 5 to 14-membered aromatic heterocyclic group which may be substituted, an acyl group having one to six carbon atoms which may be substituted or an alkylsulfonyl group having one to six carbon atoms which may be substituted; R3 represents a hydrogen atom, a halogen atom, a cyano group, an alkyl group having one to six carbon atoms which may be substituted, an alkenyl group having two to six carbon atoms which may be substituted, an alkynyl group having two to six carbon atoms which may be substituted, an aromatic hydrocarbon cyclic group having six to fourteen carbon atoms which may be substituted, a 5 to 14-membered aromatic heterocyclic group which may be substituted, a nitrogen atom which may be substituted, an oxygen atom which may be substituted or a sulfur atom which may be substituted; R4 represents an aromatic hydrocarbon cyclic group having six to fourteen carbon atoms which may be substituted, a 5 to 14-membered aromatic heterocyclic group which may be substituted or a 5 to 14-membered non-aromatic heterocyclic group having at least one or more unsaturated bonds which may be substituted; and R5 represents an aromatic hydrocarbon cyclic group having six to fourteen carbon atoms which may be substituted or a 5 to 14-membered aromatic heterocyclic group which may be substituted.

5. 发明授权

US07160892B2 Pyrimidone compounds and pharmaceutical compositions containing the same 失效
标题翻译：嘧啶酮化合物和含有它们的药物组合物
公开(公告)号：US07160892B2
公开(公告)日：2007-01-09
申请号：US10492547
申请日：2002-10-22
申请人： Hitoshi Harada , Osamu Asano , Masato Ueda , Shuhei Miyazawa , Yoshihiko Kotake , Yasuhiro Kabasawa , Masahiro Yasuda , Nobuyuki Yasuda
发明人： Hitoshi Harada , Osamu Asano , Masato Ueda , Shuhei Miyazawa , Yoshihiko Kotake , Yasuhiro Kabasawa , Masahiro Yasuda , Nobuyuki Yasuda
IPC分类号： A61K31/5377 , A61K31/513 , C07D417/02 , C07D413/02 , C07D43/02
CPC分类号： C07D239/34 , A61K31/513
摘要： The invention provides novel pyrimidone compounds exhibiting excellent antagonism against adenosine receptors (A1, A2A, and A2B receptors), particularly, compounds represented by the general formula (1), salts thereof, or solvates of both: (1) wherein R1 and R2 are each independently hydrogen, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-8 cycloalkyl, C3-8 cycloalkenyl, a 5- to 14-membered nonaromatic heterocyclic group, a C6-14 aromatic hydrocarbon group, a 5- to 14-membered aromatic heterocyclic group, C1-6 acyl, or C1-6 alkylsulfonyl; R3 is hydrogen, C1-6 alkyl, C2-6 alkenyl, or C2-6 alkynyl; R4 is a C6-14 aromatic hydrocarbon group; a 5- to 14-membered aromatic heterocyclic group, or a 5- to 14-membered nonaromatic heterocyclic group having at least one unsaturated bond; and R5 is a C6-14 aromatic hydrocarbon group or a 5- to 14-membered aromatic heterocyclic group (with the proviso that every group except hydrogen may be substituted).
摘要翻译：本发明提供了对腺苷受体（A 1 SUB，A 2A和A 2B 2受体）表现出优异拮抗作用的新型嘧啶酮化合物，特别是表示的化合物通式（1）表示的盐，其盐或两者的溶剂合物：（1）其中R 1和R 2各自独立地为氢，C 1〜 C 1-6烷基，C 2-6链烯基，C 2-6炔基，C 3-8环烷基，C 1 -C 6 - 3-8环烯基，5至14元非芳族杂环基，C 6-14芳族烃基，5至14元芳族杂环基，C _{1-6酰基或C 1-6烷基磺酰基; R 3是氢，C 1-6烷基，C 2-6链烯基或C 2-6亚烷基，炔基; R 4是C 6-14芳族烃基; 5至14元芳族杂环基或具有至少一个不饱和键的5至14元非芳族杂环基; 和R 5是C 6-14芳族烃基或5至14元芳族杂环基（条件是除了氢以外的每个基团可以被取代）。}

6. 发明授权

US06750232B2 2-aminopyridine compounds and use thereof as drugs 失效
标题翻译： 2-氨基吡啶化合物及其作为药物的用途
公开(公告)号：US06750232B2
公开(公告)日：2004-06-15
申请号：US10333689
申请日：2003-01-23
申请人： Hitoshi Harada , Osamu Asano , Shuhei Miyazawa , Masato Ueda , Masahiro Yasuda , Nobuyuki Yasuda
发明人： Hitoshi Harada , Osamu Asano , Shuhei Miyazawa , Masato Ueda , Masahiro Yasuda , Nobuyuki Yasuda
IPC分类号： C07D40102
CPC分类号： C07D213/80 , A61K31/4409 , A61K31/443 , A61K31/4436 , A61K31/444 , A61K31/455 , C07D213/82 , C07D213/85 , C07D405/04 , C07D405/14 , C07D409/14
摘要： A class of substituted compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by formula (II), wherein R1 is selected from hydrido, halo, alkoxy, aryl, alkylthio, alkylamino, aralkoxy, azido and alkenyloxy; wherein R2 is selected from hydrido, cyano, hydroxyalkyl, haloalkyl, aminoalkyl, alkylaminoalkyl, alkylcarbonyloxyalkyl, aminocarbonyl and alkylcarbonylaminoalkyl; and wherein R5 and R6 are one more radicals independently selected from halo, alkylsulfonyl, aminosulfonyl, alkoxy and alkylthio; provided one of R5 and R6 is substituted with alkysulfonyl, aminosulfonyl, or haloalkylsulfonyl; or a pharmaceutically-acceptable salt thereof.
摘要翻译：描述了一类取代的化合物用于治疗炎症和炎症相关疾病。特别感兴趣的化合物由式（II）定义，其中R 1选自氢，卤素，烷氧基，芳基，烷硫基，烷基氨基，芳烷氧基，叠氮基和烯氧基; 氰基，羟基烷基，卤代烷基，氨基烷基，烷基氨基烷基，烷基羰氧基烷基，氨基羰基和烷基羰基氨基烷基;其中R 2选自氢，氰基，并且其中R 5和R 6分别独立地选自卤素，烷基磺酰基，氨基磺酰基，烷氧基和烷硫基; 其中R 5和R 6之一被烷基磺酰基，氨基磺酰基或卤代烷基磺酰基取代; 或其药学上可接受的盐。

7. 发明授权

US06841549B1 Condensed imidazole compounds and a therapeutic agent for diabetes mellitus 失效
标题翻译：缩合咪唑化合物和糖尿病治疗剂
公开(公告)号：US06841549B1
公开(公告)日：2005-01-11
申请号：US10018688
申请日：2000-06-30
申请人： Osamu Asano , Hitoshi Harada , Seiji Yoshikawa , Nobuhisa Watanabe , Takashi Inoue , Tatsuo Horizoe , Nobuyuki Yasuda , Kaya Ohashi , Hiroe Minami , Junsaku Nagaoka , Manabu Murakami , Seiichi Kobayashi , Isao Tanaka , Tsutomu Kawata , Naoyuki Shimomura , Hiroshi Akamatsu , Naoki Ozeki , Toshikazu Shimizu , Kenji Hayashi , Toyokazu Haga , Shigeto Negi , Toshihiko Naito
发明人： Osamu Asano , Hitoshi Harada , Seiji Yoshikawa , Nobuhisa Watanabe , Takashi Inoue , Tatsuo Horizoe , Nobuyuki Yasuda , Kaya Ohashi , Hiroe Minami , Junsaku Nagaoka , Manabu Murakami , Seiichi Kobayashi , Isao Tanaka , Tsutomu Kawata , Naoyuki Shimomura , Hiroshi Akamatsu , Naoki Ozeki , Toshikazu Shimizu , Kenji Hayashi , Toyokazu Haga , Shigeto Negi , Toshihiko Naito
IPC分类号： A61P3/10 , A61P43/00 , C07D471/04 , C07D473/00 , C07D473/34 , C07D473/40 , A16K31/33 , C07D239/70 , C07D471/00 , C07D487/00 , A16K31/52
CPC分类号： C07D471/04 , C07D473/00 , C07D473/34 , C07D473/40
摘要： The present invention provides a preventive or therapeutic agent for diabetes mellitus and diabetic complications, which is a new type based on an adenosine A2 receptor antagonist action.That is, it provides a novel condensed imidazole compound which has an adenosine A2 receptor antagonist action, is effective for preventing or treating diabetes mellitus and diabetic complications, and is represented by the formula (I); (wherein R1 represents e.g. an amino group which may be substituted with an alkyl group; R2 represents e.g. hydrogen atom, an alkyl group, a cycloalkyl group or an alkyl group, alkenyl group or alkynyl group which may be substituted with hydrox etc.; R3 represents e.g. an optionally substituted alkyl group, alkenyl group, alkynyl group, aryl group, heteroaryl group, pyridinone group, pyrimidinone group or piperadinone group; Ar represents e.g. an optionally substituted aryl or heteroaryl group; and Q and W are the same as or different from each other and each represents N or CH), a pharmacologically acceptable salt or hydrates thereof.
摘要翻译：本发明提供了一种基于腺苷A2受体拮抗剂作用的新型糖尿病和糖尿病并发症的预防或治疗剂。即提供了具有腺苷A2受体拮抗剂作用的新颖的缩合咪唑化合物，是有效预防或治疗糖尿病和糖尿病并发症，并由式（I）表示;（其中R 1表示例如可被烷基取代的氨基; R 2表示例如氢原子，可以被羟基取代的烷基，环烷基或烷基，烯基或炔基; R 3表示例如任选取代的烷基，烯基，炔基，芳基，杂芳基，吡啶酮基，嘧啶酮基或哌嗪酮基; Ar表示例如任选取代的芳基或杂芳基; Q和W彼此相同或不同，每个代表 N或CH），其药理学上可接受的盐或其水合物。

8. 再颁专利

USRE39112E1 Purine derivatives and adenosine A2 receptor antagonists serving as preventives/remedies for diabetes 失效
标题翻译：嘌呤衍生物和腺苷A2受体拮抗剂作为糖尿病的预防药物/治疗药物
公开(公告)号：USRE39112E1
公开(公告)日：2006-05-30
申请号：US11057854
申请日：1998-12-24
申请人： Osamu Asano , Hitoshi Harada , Yorihisa Hoshino , Seiji Yoshikawa , Takashi Inoue , Tatsuo Horizoe , Nobuyuki Yasuda , Kaya Ohashi , Junsaku Nagaoka , Manabu Murakami , Seiichi Kobayashi
发明人： Osamu Asano , Hitoshi Harada , Yorihisa Hoshino , Seiji Yoshikawa , Takashi Inoue , Tatsuo Horizoe , Nobuyuki Yasuda , Kaya Ohashi , Junsaku Nagaoka , Manabu Murakami , Seiichi Kobayashi
IPC分类号： C07D473/34 , C07D473/30 , C07D473/00 , A61K31/52 , A61K31/522
CPC分类号： C07D473/30 , A61K31/52 , C07D473/00 , C07D473/34
摘要： The present invention provides a preventive or therapeutic agent of a new type for diabetes mellitus and diabetic complications on the basis of an adenosine A2 receptor antagonist action.A purine compound represented by the formula (I), its pharmacologically acceptable salt or hydrates thereof has an adenosine A2 receptor antagonistic action and is useful for prevention or therapy of diabetes mellitus and diabetic complications. In addition, adenosine A2 receptor antagonists having different structures from those of the compounds described above, for example KW6002, are also effective for prevention or therapy of diabetes mellitus and diabetic complications. In the formula, W is —CH2CH2—, or —CH═CH— or —C≡C—; R1 is: (in the formula, X is hydrogen atom, hydroxyl group, a lower alkyl group, a lower alkoxy group, etc.; and R5 and R6 are the same as or different from each other and each represents hydrogen atom, a lower alkyl group, a cycloalkyl group, etc.) and the like; R2 is an amino group, etc. which maybe substituted with a lower alkyl group, etc.; R3 is a cycloalkyl group, an optionally substituted aryl group, etc.; and R4 is a lower alkyl group etc.
摘要翻译：本发明提供了基于腺苷A2受体拮抗剂作用的糖尿病新型糖尿病并发症的预防或治疗剂。由式（I）表示的嘌呤化合物，其药理学上可接受的盐或其水合物具有腺苷A2受体拮抗作用，可用于预防或治疗糖尿病和糖尿病并发症。此外，与上述化合物（例如KW6002）具有不同结构的腺苷A2受体拮抗剂对于糖尿病和糖尿病并发症的预防或治疗也是有效的。在该式中，W是-CH 2 CH 2 - ，或-CH-CH-或-C≡C-; R 1是：（在该式中，X是氢原子，羟基，低级烷基，低级烷氧基等; R 5和R 5， SUP> 6 <！ - SIPO - >相同或不同，各自表示氢原子，低级烷基，环烷基等）等; R 2是可以被低级烷基等取代的氨基等; R 3是环烷基，任选取代的芳基等; R 4是低级烷基等。

9. 发明授权

US06579868B1 Purine derivatives and adenosine A2 receptor antagonists serving as preventives/remedies for diabetes 有权
标题翻译：嘌呤衍生物和腺苷A2受体拮抗剂作为糖尿病的预防药物/治疗药物
公开(公告)号：US06579868B1
公开(公告)日：2003-06-17
申请号：US09582840
申请日：2000-07-05
申请人： Osamu Asano , Hitoshi Harada , Yorihisa Hoshino , Seiji Yoshikawa , Takashi Inoue , Tatsuo Horizoe , Nobuyuki Yasuda , Kaya Nagata , Junsaku Nagaoka , Manabu Murakami , Seiichi Kobayashi
发明人： Osamu Asano , Hitoshi Harada , Yorihisa Hoshino , Seiji Yoshikawa , Takashi Inoue , Tatsuo Horizoe , Nobuyuki Yasuda , Kaya Nagata , Junsaku Nagaoka , Manabu Murakami , Seiichi Kobayashi
IPC分类号： C07D47334
CPC分类号： C07D473/30 , A61K31/52 , C07D473/00 , C07D473/34
摘要： The present invention provides a preventive or therapeutic agent of a new type for diabetes mellitus and diabetic complications on the basis of an adenosine A2 receptor antagonistic action. A purine compound represented by the formula (I), its pharmacologically acceptable salt or hydrates thereof has an adenosine A2 receptor antagonistic action and is useful for prevention or therapy of diabetes mellitus and diabetic complications. In addition, adenosine A2 receptor antagonists having different structures from those of the compounds described above, for example KW6002, are also effective for prevention or therapy of diabetes mellitus and diabetic complications. In the formula, W is —CH2CH2—, —CH═CH— or —C≡C—; R1 is: (in the formula, X is hydrogen atom, hydroxyl group, a lower alkyl group, a lower alkoxy group, etc.; and R5 and R6 are the same as or different from each other and each represents hydrogen atom, a lower alkyl group, a cycloalkyl group, etc.) and the like; R2 is an amino group, etc. which maybe substituted with a lower alkyl group, etc.; R3 is a cycloalkyl group, an optionally substituted aryl group, etc.; and R4 is a lower alkyl group etc.
摘要翻译：本发明提供了基于腺苷A2受体拮抗作用的新型糖尿病和糖尿病并发症的预防或治疗剂。由式（I）表示的嘌呤化合物，其药理学上可接受的盐或其水合物具有腺苷A2受体拮抗作用，可用于预防或治疗糖尿病和糖尿病并发症。此外，与上述化合物例如KW6002具有不同结构的腺苷A2受体拮抗剂对于预防或治疗糖尿病和糖尿病并发症也是有效的。在该式中，W是-CH 2 CH 2 - ， - CH = CH - 或-C = C-; R1为（式中，X为氢原子，羟基，低级烷基，低级烷氧基等），R5和R6彼此相同或不同，分别表示氢原子，低级烷基，环烷基等）等; R2是可被低级烷基取代的氨基等; R3是环烷基，任选取代的芳基等; R4为低级烷基等。

10. 发明申请

US20050195929A1 Sampling frequency conversion apparatus 审中-公开
标题翻译：采样变频装置
公开(公告)号：US20050195929A1
公开(公告)日：2005-09-08
申请号：US11100128
申请日：2005-04-06
申请人： Nobuyuki Yasuda , Kazunobu Ohkuri
发明人： Nobuyuki Yasuda , Kazunobu Ohkuri
IPC分类号： G10L19/00 , H03H17/00 , H03H17/06 , H04B14/02 , H04B14/04 , H04H5/00 , H04H20/89 , H04L7/02 , H04L25/05 , H04B1/38
CPC分类号： H03H17/0628 , H03H17/0621 , H04B14/026 , H04H20/89 , H04L25/05
摘要： A sampling frequency conversion apparatus which easily controls the phase difference (time difference) between the input data and the output data in converting the sampling frequency, and comprises storage means 13 for continuously writing the input data or the data obtained by over-sampling the input data and for continuously reading out the data written maintaining a predetermined address difference relative to the write address, and interpolation processing means 14 for interpolating the data read out from the storage means 13 to obtain data of which the sampling frequency is converted. In converting the sampling frequency, an address difference between a write address and a read address in the storage means 13 is optimized, the address difference being optimized without limitation for a predetermined period of time from the start of supplying the input data and, then, being optimized by imposing a predetermined limitation after the passage of the predetermined period of time.
摘要翻译：一种采样频率转换装置，其在转换采样频率时容易地控制输入数据和输出数据之间的相位差（时间差），并且包括用于连续写入输入数据或通过对输入进行过采样而获得的数据的存储装置13 数据，并连续地读出相对于写入地址保持预定地址差的写入数据;以及内插处理装置14，用于内插从存储装置13读出的数据，以获得采样频率被转换的数据。在转换采样频率时，优化存储装置13中的写入地址和读取地址之间的地址差异，在从提供输入数据开始的预定时间段内对地址差进行优化，而不限于此，通过在经过预定时间段之后施加预定的限制来优化。

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