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1. 发明申请

US20070254881A1 Pyrazole Derivative 审中-公开
标题翻译：吡唑衍生物
公开(公告)号：US20070254881A1
公开(公告)日：2007-11-01
申请号：US11573098
申请日：2005-08-08
申请人： Naoaki Kanaya , Takashi Ishiyama , Ryo Muto , Toshiyuki Watanabe , Yuichi Ochiai
发明人： Naoaki Kanaya , Takashi Ishiyama , Ryo Muto , Toshiyuki Watanabe , Yuichi Ochiai
IPC分类号： A61K31/501 , A61K31/444 , A61K31/4545 , A61P7/02 , C07D401/14 , C07D413/14 , C07D403/14 , C07D211/32 , A61K31/5377 , A61K31/497
CPC分类号： C07D401/14 , C07D403/14 , C07D413/14 , C07D417/14
摘要： A compound represented by Formula (I): wherein Ar1 represents Formula (II): Ar2 represents a 5- or 6-membered aromatic heterocyclic group which may be substituted; and X represents Formula (III): a salt thereof, or a solvate of the compound or the salt. A potent platelet aggregation suppressant which does not inhibit COX-1 and COX-2 is provided.
摘要翻译：由式（I）表示的化合物：其中Ar 1代表式（II）：Ar 2表示可被取代的5或6元芳族杂环基; 并且X表示式（III）：其盐或化合物或其盐的溶剂合物。提供了不抑制COX-1和COX-2的有效的血小板聚集抑制剂。

2. 发明申请

US20080064682A1 Pyrazole Derivatives 审中-公开
标题翻译：吡唑衍生物
公开(公告)号：US20080064682A1
公开(公告)日：2008-03-13
申请号：US11571387
申请日：2005-07-01
申请人： Naoaki Kanaya , Takashi Ishiyama , Ryo Muto , Toshiyuki Watanabe , Yuichi Ochiai
发明人： Naoaki Kanaya , Takashi Ishiyama , Ryo Muto , Toshiyuki Watanabe , Yuichi Ochiai
IPC分类号： A61K31/55 , A61K31/415 , A61K31/44 , A61P9/00 , C07D231/02 , C07D401/00 , C07D413/00 , C07D243/08 , C07D211/68 , A61K31/445 , A61K31/5375
CPC分类号： C07D401/14 , C07D417/14
摘要： A compound represented by formula (I): (wherein Ar1 represents a phenyl group which may have 1 to 3 substituents, or a non-substituted 5- or 6-membered aromatic heterocyclic group; Ar2 represents (i) a non-substituted phenyl group, (ii) a phenyl group which has been substituted by a lower alkyl group having 1 to 3 groups or atoms selected from among a carbamoyl group, an amino group, a hydroxyl group, a lower alkoxy group, and a halogen atom, or (iii) a 5- or 6-membered nitrogen-containing aromatic heterocyclic group which has been substituted by 1 to 3 groups or atoms selected from among a lower alkyl group, a lower alkynyl group, a lower alkanoyl group, a carbamoyl group, a cyano group, an amino group, a hydroxyl group, a lower alkoxy group, and a halogen atom; and X represents a group represented by formula (II): (wherein the ring structure represents a 4- to 7-membered heterocyclic group which may have, in addition to the nitrogen atom shown in formula (II), one heteroatom selected from among nitrogen, oxygen, a sulfur, and which may be substituted by 1 to 4 groups or atoms selected from among a lower alkyl group, a carbamoyl group, an amino group, a hydroxyl group, a lower alkoxy group, an oxo group a lower alkanoyl group, a lower alkylsulfonyl group, and a halogen atom)), a salt thereof, a solvate of the compound or the salt, and a drug.
摘要翻译：由式（I）表示的化合物：其中Ar 1表示可具有1至3个取代基的苯基或未取代的5或6元芳族杂环基团; Ar _{2 表示（i）未取代的苯基，（ii）被具有1〜3个选自氨基甲酰基，氨基，羟基，低级烷氧基和卤素原子，或（iii）被1〜3个选自低级烷基，低级烷氧基，低级炔基，低级烷酰基，氨基甲酰基，氰基，氨基，羟基，低级烷氧基和卤素原子; X表示由式（II）表示的基团：（其中环结构表示除了式（II）所示的氮原子之外还可以具有o至4个的7-元杂环基选自氮，氧，硫的杂原子，可以被1〜4个选自低级烷基，氨基甲酰基，氨基，羟基，低级烷氧基，氧代基，低级烷酰基，低级烷基磺酰基和卤原子）），其盐，化合物或其盐的溶剂化物和药物。}

3. 发明申请

US20070219210A1 Amidopyrazole Derivative 审中-公开
标题翻译：吡唑衍生物
公开(公告)号：US20070219210A1
公开(公告)日：2007-09-20
申请号：US10584632
申请日：2004-12-27
申请人： Naoaki Kanaya , Takashi Ishiyama , Ryo Muto , Yuichi Ochiai , Toshiyuki Watanabe , Noriko Shima
发明人： Naoaki Kanaya , Takashi Ishiyama , Ryo Muto , Yuichi Ochiai , Toshiyuki Watanabe , Noriko Shima
IPC分类号： A61K31/415 , A61K31/4427 , A61K31/497 , A61K31/501 , C07D231/04 , C07D401/14
CPC分类号： C07D401/14 , C07D401/04 , C07D403/04 , C07D403/14 , C07D405/14 , C07D417/14
摘要： A platelet coagulation inhibitor which inhibits neither COX-1 nor COX-2 is provided. The inhibitor is a compound represented by general formula (I): wherein Ar1 and Ar2 independently represent a 5- or 6-membered aromatic heterocyclic group optionally substituted with 1 to 3 substituents, or a phenyl group optionally substituted with 1 to 3 substituents; R1 represents a lower acyl group, carboxyl group, a lower alkoxy carbonyl group, a lower alkoxy group, a lower alkyl group optionally substituted with 1 or 2 substituents, a carbamoyl group optionally substituted with 1 or 2 substituents, an oxamoyl group optionally substituted with 1 or 2 substituents, an amino group optionally substituted with 1 or 2 substituents, a 4- to 7-membered alicyclic heterocyclic group optionally substituted with 1 or 2 substituents, a phenyl group optionally substituted with 1 to 3 substituents, or a 5- or 6-membered aromatic heterocyclic group optionally substituted with 1 to 3 substituents; and R2 represents hydrogen atom, a halogeno group, or the like.
摘要翻译：提供了既不抑制COX-1也不抑制COX-2的血小板凝血抑制剂。抑制剂是由通式（I）表示的化合物：其中Ar 1和Ar 2独立地表示任选被1至 3个取代基或任选被1至3个取代基取代的苯基; R 1表示低级酰基，羧基，低级烷氧基羰基，低级烷氧基，任选被1或2个取代基取代的低级烷基，任选被1或2个取代基取代的氨基甲酰基，任选被 1或2个取代基，任选被1或2个取代基取代的氨基，任选被1或2个取代基取代的4-至7-元脂环族杂环基，任选被1至3个取代基取代的苯基，或5-或任选被1至3个取代基取代的6元芳族杂环基; R 2表示氢原子，卤代基等。

4. 发明申请

US20060128685A1 Pyrazole derivative 失效
标题翻译：吡唑衍生物
公开(公告)号：US20060128685A1
公开(公告)日：2006-06-15
申请号：US10543915
申请日：2004-02-06
申请人： Naoaki Kanaya , Hiroaki Ishihara , Youichi Kimura , Takashi Ishiyama , Yuichi Ochiai
发明人： Naoaki Kanaya , Hiroaki Ishihara , Youichi Kimura , Takashi Ishiyama , Yuichi Ochiai
IPC分类号： A61K31/55 , A61K31/541 , A61K31/5377 , A61K31/496 , A61K31/454 , A61K31/4178 , C07D417/02 , C07D413/02 , C07D403/02
CPC分类号： A61K31/551 , A61K31/4439 , A61K31/4545 , A61K31/496 , A61K31/501 , A61K31/5377 , A61K31/541 , C07D231/14 , C07D401/04 , C07D401/14 , C07D403/04 , C07D413/14 , C07D493/04
摘要： The present invention is directed to a strong platelet aggregation-inhibiting agent which does not inhibit COX-1 or COX-2. The present invention provides compounds represented by formula (I) or formula (II), salts of the compounds, and solvates of the compounds or the salts. Also provided are medicaments containing any of the compounds, salts, or solvates and preventive and/or therapeutic agents for ischemic diseases, containing any of the compounds, salts, or the solvates.
摘要翻译：本发明涉及不抑制COX-1或COX-2的强烈的血小板聚集抑制剂。本发明提供由式（I）或式（II）表示的化合物的盐，化合物的盐和化合物或其盐的溶剂合物。还提供了含有任何化合物，盐或溶剂合物的药物，以及含有任何化合物，盐或溶剂合物的缺血性疾病的预防和/或治疗剂。

5. 发明授权

US07622471B2 Pyrazole derivatives having a pyridazine and pyridine functionality 失效
标题翻译：具有哒嗪和吡啶官能团的吡唑衍生物
公开(公告)号：US07622471B2
公开(公告)日：2009-11-24
申请号：US10543915
申请日：2004-02-06
申请人： Naoaki Kanaya , Hiroaki Ishihara , Youichi Kimura , Takashi Ishiyama , Yuichi Ochiai
发明人： Naoaki Kanaya , Hiroaki Ishihara , Youichi Kimura , Takashi Ishiyama , Yuichi Ochiai
IPC分类号： A61K31/497 , C07D237/00 , C07D237/02
CPC分类号： A61K31/551 , A61K31/4439 , A61K31/4545 , A61K31/496 , A61K31/501 , A61K31/5377 , A61K31/541 , C07D231/14 , C07D401/04 , C07D401/14 , C07D403/04 , C07D413/14 , C07D493/04
摘要： The present invention is directed to a strong platelet aggregation-inhibiting agent which does not inhibit COX-1 or COX-2. Further, the present invention provides compounds represented by formula (I), salts of the compounds, and solvates or hydrates of the compounds or the salts. Also provided are medicaments containing any of the compounds, salts, or solvates and preventive and/or therapeutic agents for ischemic diseases, containing any of the compounds, salts, or the solvates or hydrates.
摘要翻译：本发明涉及不抑制COX-1或COX-2的强烈的血小板聚集抑制剂。此外，本发明提供由式（I）表示的化合物，化合物的盐，化合物或其盐的溶剂合物或水合物。还提供了含有任何化合物，盐或溶剂化物的药物，以及含有任何化合物，盐或溶剂合物或水合物的缺血性疾病的预防和/或治疗剂。

6. 发明申请

US20060189591A1 Five-membered heterocyclic derivative 审中-公开
标题翻译：五元杂环衍生物
公开(公告)号：US20060189591A1
公开(公告)日：2006-08-24
申请号：US10553982
申请日：2004-04-20
申请人： Toru Okayama , Kouichi Uoto , Takashi Ishiyama , Naoaki Kanaya , Youichi Kimura , Hiroaki Ishihara , Toshiyuki Watanabe , Kunihiko Fujii
发明人： Toru Okayama , Kouichi Uoto , Takashi Ishiyama , Naoaki Kanaya , Youichi Kimura , Hiroaki Ishihara , Toshiyuki Watanabe , Kunihiko Fujii
IPC分类号： C07D413/02 , C07D403/02 , A61K31/55 , A61K31/454 , A61K31/422 , A61K31/4178
CPC分类号： C07D401/14 , A61K31/4439 , A61K31/4545 , A61K31/497 , A61K31/499 , A61K31/501 , A61K31/5377 , A61K31/553
摘要： The present invention relates to a compound represented by formula (I): a salt of the compound, or a solvate of the compound or the salt; a drug containing any of the compounds, the salts, and the solvates; a preventive and/or therapeutic agent for an ischemic disease containing any of the compounds, the salts, and the solvates; and a platelet coagulation inhibitor containing any of the compounds, the salts, and the solvates. The compound of the present invention is useful as a strong platelet coagulation inhibitor without inhibiting COX-1 or COX-2.
摘要翻译：本发明涉及由式（I）表示的化合物：化合物的盐或化合物或其盐的溶剂合物; 含有任何化合物，盐和溶剂合物的药物; 含有任何化合物，盐和溶剂合物的缺血性疾病的预防和/或治疗剂; 和含有任何化合物，盐和溶剂合物的血小板凝血抑制剂。本发明的化合物可用作强抑制血小板凝血抑制剂而不抑制COX-1或COX-2。

7. 发明授权

US5866577A Aromatic amidine derivatives and salts thereof 失效
标题翻译：芳族脒衍生物及其盐
公开(公告)号：US5866577A
公开(公告)日：1999-02-02
申请号：US924504
申请日：1997-09-05
申请人： Takayasu Nagahara , Naoaki Kanaya , Kazue Inamura , Yukio Yokoyama
发明人： Takayasu Nagahara , Naoaki Kanaya , Kazue Inamura , Yukio Yokoyama
IPC分类号： A61K31/155 , A61K31/165 , A61K31/19 , A61K31/195 , A61K31/215 , A61K31/235 , A61K31/33 , A61K31/40 , A61K31/4025 , A61K31/443 , A61K31/4433 , A61K31/445 , A61K31/4465 , A61K31/451 , A61K31/495 , A61K31/50 , A61K31/505 , A61P7/02 , A61P43/00 , C07C255/52 , C07C255/54 , C07C255/56 , C07C255/58 , C07C257/18 , C07C323/31 , C07C323/32 , C07D207/09 , C07D207/12 , C07D209/04 , C07D211/22 , C07D211/44 , C07D211/46 , C07D239/02 , C07D239/20 , C07D241/02 , C07D307/78 , C07D307/79 , C07D307/80 , C07D307/84 , C07D333/60 , C07D333/68 , C07D401/12 , C07D403/10 , C07D403/12 , C07D405/12 , C07D409/10 , C07D409/12 , C07D417/12 , C07D521/00
CPC分类号： C07D307/79 , C07C257/18 , C07D207/12 , C07D211/22 , C07D211/46 , C07D231/12 , C07D233/56 , C07D249/08 , C07D307/80 , C07D307/81 , C07D333/60 , C07D401/12 , C07D403/12 , C07D405/12 , C07D407/12 , C07D409/12 , C07D417/12
摘要： An anticoagulant agent which comprises, as an active ingredient, an aromatic amidine derivative represented by the following general formula (1) or a salt thereof: ##STR1## wherein the group represented by ##STR2## is a group selected from indolyl, benzofuranyl, benzothienyl, benzimidazolyl, benzoxazolyl, benzothiazolyl, naphthyl, tetrahydronaphthyl and indanyl; X is a single bond, an oxygen atom, a sulfur atom or a carbonyl group; and Y is a saturated or unsaturated 5- or 6-membered heterocyclic moiety or cyclic hydrocarbon moiety optionally having a substituent group, an amino group optionally having a substituent group or an aminoalkyl group optionally having a substituent group.The inventive compound has a high anticoagulant capacity based on its excellent FXa inhibition activity.
摘要翻译：作为活性成分，含有下述通式（1）表示的芳香族脒衍生物或其盐的抗凝血剂：其中，由“IMAGE”表示的基团是选自吲哚基，苯并呋喃基，苯并噻吩基，苯并咪唑基，苯并恶唑基，苯并噻唑基，萘基，四氢萘基和茚满基; X是单键，氧原子，硫原子或羰基; Y是任选具有取代基的任选具有取代基的氨基或任选具有取代基的氨基烷基的饱和或不饱和的5-或6-元杂环部分或环烃部分。基于其优异的FXa抑制活性，本发明化合物具有高抗凝血能力。

8. 发明授权

US5962695A Aromatic amidine derivatives and salts thereof 失效
标题翻译：芳族脒衍生物及其盐
公开(公告)号：US5962695A
公开(公告)日：1999-10-05
申请号：US131235
申请日：1998-08-07
申请人： Takayasu Nagahara , Naoaki Kanaya , Kazue Inamura , Yukio Yokoyama
发明人： Takayasu Nagahara , Naoaki Kanaya , Kazue Inamura , Yukio Yokoyama
IPC分类号： A61K31/155 , A61K31/165 , A61K31/19 , A61K31/195 , A61K31/215 , A61K31/235 , A61K31/33 , A61K31/40 , A61K31/4025 , A61K31/443 , A61K31/4433 , A61K31/445 , A61K31/4465 , A61K31/451 , A61K31/495 , A61K31/50 , A61K31/505 , A61P7/02 , A61P43/00 , C07C255/52 , C07C255/54 , C07C255/56 , C07C255/58 , C07C257/18 , C07C323/31 , C07C323/32 , C07D207/09 , C07D207/12 , C07D209/04 , C07D211/22 , C07D211/44 , C07D211/46 , C07D239/02 , C07D239/20 , C07D241/02 , C07D307/78 , C07D307/79 , C07D307/80 , C07D307/84 , C07D333/60 , C07D333/68 , C07D401/12 , C07D403/10 , C07D403/12 , C07D405/12 , C07D409/10 , C07D409/12 , C07D417/12 , C07D521/00
CPC分类号： C07D307/79 , C07C257/18 , C07D207/12 , C07D211/22 , C07D211/46 , C07D231/12 , C07D233/56 , C07D249/08 , C07D307/80 , C07D307/81 , C07D333/60 , C07D401/12 , C07D403/12 , C07D405/12 , C07D407/12 , C07D409/12 , C07D417/12
摘要： An anticoagulant agent which comprises, as an active ingredient, an aromatic amidine derivative represented by the following general formula (1) or a salt thereof: ##STR1## wherein the group represented by ##STR2## is a group selected from indolyl, benzofuranyl, benzothienyl, benzimidazolyl, benzoxazolyl, benzothiazolyl, naphthyl, tetrahydronaphthyl and indanyl; X is a single bond, an oxygen atom, a sulfur atom or a carbonyl group; and Y is a saturated or unsaturated 5- or 6-membered heterocyclic moiety or cyclic hydrocarbon moiety optionally having a substituent group, an amino group optionally having a substituent group or an aminoalkyl group optionally having a substituent group.The inventive compound has a high anticoagulant capacity based on its excellent FXa inhibition activity.
摘要翻译：作为活性成分，含有下述通式（1）所示的芳香族脒衍生物或其盐的抗凝血剂，其特征在于，所述基团为选自吲哚基，苯并呋喃基，苯并噻吩基，苯并咪唑基，苯并恶唑基，苯并噻唑基，萘基，四氢萘基和茚满基; X是单键，氧原子，硫原子或羰基; Y是任选具有取代基的任选具有取代基的氨基或任选具有取代基的氨基烷基的饱和或不饱和的5-或6-元杂环部分或环烃部分。基于其优异的FXa抑制活性，本发明化合物具有高抗凝血能力。

9. 发明授权

US5620991A Aromatic amidine derivatives and salts thereof 失效
标题翻译：芳族脒衍生物及其盐
公开(公告)号：US5620991A
公开(公告)日：1997-04-15
申请号：US471173
申请日：1995-06-06
申请人： Takayasu Nagahara , Naoaki Kanaya , Kazue Inamura , Yukio Yokoyama
发明人： Takayasu Nagahara , Naoaki Kanaya , Kazue Inamura , Yukio Yokoyama
IPC分类号： A61K31/155 , A61K31/165 , A61K31/19 , A61K31/195 , A61K31/215 , A61K31/235 , A61K31/33 , A61K31/40 , A61K31/4025 , A61K31/443 , A61K31/4433 , A61K31/445 , A61K31/4465 , A61K31/451 , A61K31/495 , A61K31/50 , A61K31/505 , A61P7/02 , A61P43/00 , C07C255/52 , C07C255/54 , C07C255/56 , C07C255/58 , C07C257/18 , C07C323/31 , C07C323/32 , C07D207/09 , C07D207/12 , C07D209/04 , C07D211/22 , C07D211/44 , C07D211/46 , C07D239/02 , C07D239/20 , C07D241/02 , C07D307/78 , C07D307/79 , C07D307/80 , C07D307/84 , C07D333/60 , C07D333/68 , C07D401/12 , C07D403/10 , C07D403/12 , C07D405/12 , C07D409/10 , C07D409/12 , C07D417/12 , C07D521/00 , C07D211/06
CPC分类号： C07D307/79 , C07C257/18 , C07D207/12 , C07D211/22 , C07D211/46 , C07D231/12 , C07D233/56 , C07D249/08 , C07D307/80 , C07D307/81 , C07D333/60 , C07D401/12 , C07D403/12 , C07D405/12 , C07D407/12 , C07D409/12 , C07D417/12
摘要： An anticoagulant agent which comprises, as an active ingredient, an aromatic amidine derivative represented by the following general formula (1) or a salt thereof: ##STR1## wherein the group represented by ##STR2## is a group selected from indolyl, benzofuranyl, benzothienyl, benzimidazolyl, benzoxazolyl, benzothiazolyl, naphthyl, tetrahydronaphthyl and indanyl; X is a single bond, an oxygen atom, a sulfur atom or a carbonyl group; and Y is a saturated or unsaturated 5- or 6-membered heterocyclic moiety or cyclic hydrocarbon moiety optionally having a substituent group, an amino group optionally having a substituent group or an aminoalkyl group optionally having a substituent group.The inventive compound has a high anticoagulant capacity based on its excellent FXa inhibition activity.
摘要翻译：作为活性成分，含有下述通式（1）表示的芳香族脒衍生物或其盐的抗凝血剂：其中，由“IMAGE”表示的基团是选自吲哚基，苯并呋喃基，苯并噻吩基，苯并咪唑基，苯并恶唑基，苯并噻唑基，萘基，四氢萘基和茚满基; X是单键，氧原子，硫原子或羰基; Y是任选具有取代基的任选具有取代基的氨基或任选具有取代基的氨基烷基的饱和或不饱和的5-或6-元杂环部分或环烃部分。基于其优异的FXa抑制活性，本发明化合物具有高抗凝血能力。

10. 发明授权

US5576343A Aromatic amidine derivatives and salts thereof 失效
公开(公告)号：US5576343A
公开(公告)日：1996-11-19
申请号：US468304
申请日：1995-06-06
申请人： Takayasu Nagahara , Naoaki Kanaya , Kazue Inamura , Yukio Yokoyama
发明人： Takayasu Nagahara , Naoaki Kanaya , Kazue Inamura , Yukio Yokoyama
IPC分类号： A61K31/155 , A61K31/165 , A61K31/19 , A61K31/195 , A61K31/215 , A61K31/235 , A61K31/33 , A61K31/40 , A61K31/4025 , A61K31/443 , A61K31/4433 , A61K31/445 , A61K31/4465 , A61K31/451 , A61K31/495 , A61K31/50 , A61K31/505 , A61P7/02 , A61P43/00 , C07C255/52 , C07C255/54 , C07C255/56 , C07C255/58 , C07C257/18 , C07C323/31 , C07C323/32 , C07D207/09 , C07D207/12 , C07D209/04 , C07D211/22 , C07D211/44 , C07D211/46 , C07D239/02 , C07D239/20 , C07D241/02 , C07D307/78 , C07D307/79 , C07D307/80 , C07D307/84 , C07D333/60 , C07D333/68 , C07D401/12 , C07D403/10 , C07D403/12 , C07D405/12 , C07D409/10 , C07D409/12 , C07D417/12 , C07D521/00
CPC分类号： C07D307/79 , C07C257/18 , C07D207/12 , C07D211/22 , C07D211/46 , C07D231/12 , C07D233/56 , C07D249/08 , C07D307/80 , C07D307/81 , C07D333/60 , C07D401/12 , C07D403/12 , C07D405/12 , C07D407/12 , C07D409/12 , C07D417/12
摘要： An anticoagulant agent which comprises, as an active ingredient, an aromatic amidine derivative represented by the following general formula (1) or a salt thereof: ##STR1## wherein the group represented by ##STR2## is a group selected from indolyl, benzofuranyl, benzothienyl, benzimidazolyl, benzoxazolyl, benzothiazolyl, naphthyl, tetrahydronaphthyl and indanyl; X is a single bond, an oxygen atom, a sulfur atom or a carbonyl group; and Y is a saturated or unsaturated 5- or 6-membered heterocyclic moiety or cyclic hydrocarbon moiety optionally having a substituent group, an amino group optionally having a substituent group or an aminoalkyl group optionally having a substituent group.The inventive compound has a high anticoagulant capacity based on its excellent FXa inhibition activity.

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