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1. 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.

2. 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）。}

3. 发明授权

US07396836B2 Pyrimidine compound and medicinal composition thereof 失效
标题翻译：嘧啶化合物及其药用组合物
公开(公告)号：US07396836B2
公开(公告)日：2008-07-08
申请号：US10492905
申请日：2002-10-22
申请人： Hitoshi Harada , Masato Ueda , Yoshihiko Kotake , Masahiro Yasuda , Daisuke Iida , Junichi Nagakawa , Makoto Nakagawa
发明人： Hitoshi Harada , Masato Ueda , Yoshihiko Kotake , Masahiro Yasuda , Daisuke Iida , Junichi Nagakawa , Makoto Nakagawa
IPC分类号： A61K31/505 , C07D239/02
CPC分类号： C07D405/14 , A61K31/506 , C07D401/04 , C07D409/14
摘要： A compound having excellent adenosine receptor (A1, A2A, A2B receptor) antagonistic action, of the following formula, a salt thereof or a solvate of them: wherein, R1 and R2, same or different, each represents a hydrogen atom, an alkyl group, an alkenyl group, an alkynyl group, a cycloalkyl group, a cycloalkenyl group, an aromatic hydrocarbon cyclic group, an acyl group or an alkylsulfonyl group, which groups may be substituted (except the hydrogen atom); R3 represents a hydrogen atom, a halogen atom, a cyano group, an alkyl group, an alkenyl group, an alkynyl group, an aromatic hydrocarbon cyclic group, a nitrogen atom, an oxygen atom or a sulfur atom, which groups may be substituted (except the hydrogen atom, the halogen atom and the cyano group); R4 represents an aromatic hydrocarbon cyclic group which may be substituted, and R5 represents an aromatic hydrocarbon cyclic group which may be substituted.
摘要翻译：具有优异的腺苷受体（A 1 H 1，A 2 A 2，A 2B 2受体）的化合物，下式的拮抗作用，其盐或它们的溶剂化物：其中R 1，R 2和R 2相同或不同，各自表示氢原子，烷基，烯基，炔基，环烷基，环烯基，芳香族烃基，酰基或烷基磺酰基，该基团可被取代（氢原子除外）。 R 3表示氢原子，卤素原子，氰基，烷基，烯基，炔基，芳族烃环状基团，氮原子，氧原子或硫原子原子，该基团可被取代（氢原子，卤素原子和氰基除外）; R 4表示可以被取代的芳族烃环状基团，R 5表示可以被取代的芳族烃环状基团。

4. 发明申请

US20090030023A1 PYRIMIDINE COMPOUNDS AND MEDICINAL COMPOSITION THEREOF 审中-公开
标题翻译：吡嗪化合物及其药物组合物
公开(公告)号：US20090030023A1
公开(公告)日：2009-01-29
申请号：US12054337
申请日：2008-03-24
申请人： Hitoshi Harada , Masato Ueda , Yoshihiko Kotake , Masahiro Yasuda , Daisuke Iida , Junichi Nagakawa , Makoto Nakagawa
发明人： Hitoshi Harada , Masato Ueda , Yoshihiko Kotake , Masahiro Yasuda , Daisuke Iida , Junichi Nagakawa , Makoto Nakagawa
IPC分类号： C07D239/42 , A61K31/505 , C12N5/00 , A61P1/00
CPC分类号： C07D405/14 , A61K31/506 , C07D401/04 , C07D409/14
摘要： A compound represented by the following formula (I), a salt, or a solvate thereof: wherein, R1 and R2 are the same as or different from each other and each represents a hydrogen atom, an alkyl group, an alkenyl group, an alkynyl group, a cycloalkyl group, a cycloalkenyl group, a non-aromatic heterocyclic group, an aromatic hydrocarbon cyclic group, an aromatic heterocyclic group, an acyl group or an alkylsulfonyl group all of which may be substituted and wherein one, or both, of R1 or R2 is an aromatic, or non-aromatic, heterocyclic group which may be substituted; R3 represents a hydrogen atom, a halogen atom, a cyano group, an alkyl group, an alkenyl group, an alkynyl group, an aromatic hydrocarbon cyclic group, an aromatic heterocyclic group, a nitrogen atom, an oxygen atom or a sulfur atom all of which may be substituted if possible; and R4 is a pyridyl group which may be substituted.
摘要翻译：由下式（I）表示的化合物，其盐或溶剂化物：其中，R1和R2彼此相同或不同，各自表示氢原子，烷基，烯基，炔基基团，环烷基，环烯基，非芳族杂环基，芳香族烃环基，芳香族杂环基，酰基或烷基磺酰基，其全部可以被取代，并且其中R1或或R 2是可以被取代的芳族或非芳族杂环基; R3表示氢原子，卤原子，氰基，烷基，烯基，炔基，芳香族烃环基，芳香族杂环基，氮原子，氧原子或硫原子全部如果可能的话可以被替代; R4为可被取代的吡啶基。

5. 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。

6. 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。

7. 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。

8. 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。

9. 发明申请

US20140147801A1 GRAPHITE CRUCIBLE 审中-公开
标题翻译：石墨坩埚
公开(公告)号：US20140147801A1
公开(公告)日：2014-05-29
申请号：US14129547
申请日：2012-03-28
申请人： Masahiro Yasuda
发明人： Masahiro Yasuda
IPC分类号： F27B14/10
CPC分类号： F27B14/10 , F27D1/0006
摘要： There is provided a graphite crucible including a bottom part, a body part, a treatment part including an input port, and a gas discharge part that is closed at a lower end side and is opened at an upper end side of the body part. Since graphite is porous, at the time when graphite is eluted into an object to be treated or is consumed, a gas in the pores of a graphite crucible is released as air bubbles continuously into the molten object to be treated. Therefore, gasification of a gas dissolved inside the object to be treated can be enhanced, and bumping of the object to be treated can be prevented.
摘要翻译：提供了一种石墨坩埚，其包括底部，主体部分，包括输入端口的处理部分和在下端侧封闭并且在主体部分的上端侧开口的气体排出部分。由于石墨是多孔的，因此当石墨被洗脱到待处理物体或被消耗时，石墨坩埚的孔隙中的气体连续地被释放到待处理的熔融物体中。因此，可以提高溶解在待处理物体内的气体的气化，能够防止待处理物体的碰撞。

10. 发明申请

US20090045891A1 Micro Wave Chemical Reaction Device 有权
标题翻译：微波化学反应装置
公开(公告)号：US20090045891A1
公开(公告)日：2009-02-19
申请号：US11794233
申请日：2005-12-28
申请人： Tadashi Okamoto , Eiji Matsuo , Masahiro Yasuda
发明人： Tadashi Okamoto , Eiji Matsuo , Masahiro Yasuda
IPC分类号： H01P3/12
CPC分类号： B01J19/126 , B01J2219/1227 , B01J2219/1239 , B01J2219/1242 , B01J2219/1245 , B01J2219/1266 , B01J2219/1269 , B01J2219/1272 , B01J2219/1284 , H05B6/704 , H05B6/74 , H05B6/806
摘要： The invention performs uniform chemical reactions with high efficiency by action of microwave onto reaction targets placed within a flow path along a center axis of a waveguide for transmission of microwave. The microwave chemical reaction device includes a circular waveguide for transmission of TM or TE mode microwave or a square waveguide for transmission of TE mode microwave and a flow path shielded from a space within the waveguide by a bulkhead of low microwave loss and coaxially extending along the center axis of the waveguide. Reaction targets to be subjected to chemical reactions are accommodated in the flow path and the microwave acts on the reaction targets within the flow path.
摘要翻译：本发明通过微波对放置在沿着波导的中心轴的流路中的反应靶上的微波作用进行高效率的均匀化学反应。微波化学反应装置包括用于传输TM或TE模式微波的圆形波导或用于传输TE模式微波的方波导和通过低微波损耗的隔板与波导内的空间隔离的流路，并沿着波导的中心轴。在流路中容纳要进行化学反应的反应靶，微波作用在流路内的反应靶上。

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