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1. 发明申请

US20120225866A1 NITROGEN-CONTAINING COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS THEREOF FOR THE TREATMENT OF ATRIAL FIBRILLATION 有权
标题翻译：含氮化合物及其治疗ATRIAL FIBRILLATION的药物组合物
公开(公告)号：US20120225866A1
公开(公告)日：2012-09-06
申请号：US13388442
申请日：2010-08-20
申请人： Kunio Oshima , Shuuji Matsumura , Hokuto Yamabe , Naohiro Isono , Noriaki Takemura , Shinichi Taira , Takashi Oshiyama , Yasuhiro Menjo , Tsuyoshi Nagase , Masataka Ueda , Yasuo Koga , Sunao Nakayama , Kenji Tsujimae , Toshiyuki Onogawa , Kuninori Tai , Motohiro Itotani
发明人： Kunio Oshima , Shuuji Matsumura , Hokuto Yamabe , Naohiro Isono , Noriaki Takemura , Shinichi Taira , Takashi Oshiyama , Yasuhiro Menjo , Tsuyoshi Nagase , Masataka Ueda , Yasuo Koga , Sunao Nakayama , Kenji Tsujimae , Toshiyuki Onogawa , Kuninori Tai , Motohiro Itotani
IPC分类号： A61K31/5513 , C07D493/10 , A61P9/06 , C07D243/14
CPC分类号： C07D491/048 , C07D213/38 , C07D215/227 , C07D243/12 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07D495/04
摘要： The present invention provides a novel diazepine compound that blocks the IKur current or the Kv1.5 channel potently and more selectively than other K+ channels. The present invention relates to a diazepine compound represented by General Formula (1) or a salt thereof, wherein R1, R2, R3, and R4 are each independently hydrogen, lower alkyl, cyclo lower alkyl or lower alkoxy lower alkyl; R2 and R3 may be linked to form lower alkylene; A1 is lower alkylene optionally substituted with one or more substituents selected from the group consisting of hydroxyl and oxo; Y1 and Y2 are each independently —N═ or —CH═; and R5 is group represented by wherein R6 and R7 are each independently hydrogen or organic group; R6 and R7 may be linked to form a ring together with the neighboring group —XA—N—XB—; XA and XB are each independently a bond, lower alkylene, etc.
摘要翻译：本发明提供了一种新颖的二氮杂类化合物，其比其他K +通道有效地和选择性地阻断IK电流或Kv1.5通道。本发明涉及由通式（1）表示的二氮杂化合物或其盐，其中R 1，R 2，R 3和R 4各自独立地为氢，低级烷基，环低级烷基或低级烷氧基低级烷基; R2和R3可以连接形成低级亚烷基; A1是任选被一个或多个选自羟基和氧代的取代基取代的低级亚烷基; Y1和Y2各自独立地为-N =或-CH =; 并且R 5为其中R 6和R 7各自独立地为氢或有机基团的基团; R6和R7可以与相邻基团-XA-N-XB-一起形成环; XA和XB各自独立地为键，低级亚烷基等

2. 发明授权

US08822453B2 Nitrogen-containing compounds and pharmaceutical compositions thereof for the treatment of atrial fibrillation 有权
标题翻译：含氮化合物及其药物组合物用于治疗房颤
公开(公告)号：US08822453B2
公开(公告)日：2014-09-02
申请号：US13388442
申请日：2010-08-20
申请人： Shuuji Matsumura , Hokuto Yamabe , Naohiro Isono , Noriaki Takemura , Takashi Oshiyama , Tsuyoshi Nagase , Masataka Ueda , Kuninori Tai
发明人： Shuuji Matsumura , Hokuto Yamabe , Naohiro Isono , Noriaki Takemura , Takashi Oshiyama , Tsuyoshi Nagase , Masataka Ueda , Kuninori Tai
IPC分类号： C07D243/12 , C07D409/12 , C07D495/04 , A61K31/551 , A61K31/4985 , A61P9/06 , C07D401/14 , C07D471/04 , C07D403/12 , C07D403/14 , C07D401/12
CPC分类号： C07D491/048 , C07D213/38 , C07D215/227 , C07D243/12 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07D495/04
摘要： The present invention provides a novel diazepine compound that blocks the IKur current or the Kv1.5 channel potently and more selectively than other K+ channels. The present invention relates to a diazepine compound represented by General Formula (1) or a salt thereof, wherein R1, R2, R3, and R4 are each independently hydrogen, lower alkyl, cyclo lower alkyl or lower alkoxy lower alkyl; R2 and R3 may be linked to form lower alkylene; A1 is lower alkylene optionally substituted with one or more substituents selected from the group consisting of hydroxyl and oxo; Y1 and Y2 are each independently —N═ or —CH═; and R5 is group represented by wherein R6 and R7 are each independently hydrogen or organic group; R6 and R7 may be linked to form a ring together with the neighboring group —XA—N—XB—; XA and XB are each independently a bond, lower alkylene, etc.
摘要翻译：本发明提供了一种新颖的二氮杂类化合物，其比其他K +通道有效地和选择性地阻断IK电流或Kv1.5通道。本发明涉及由通式（1）表示的二氮杂化合物或其盐，其中R 1，R 2，R 3和R 4各自独立地为氢，低级烷基，环低级烷基或低级烷氧基低级烷基; R2和R3可以连接形成低级亚烷基; A1是任选被一个或多个选自羟基和氧代的取代基取代的低级亚烷基; Y1和Y2各自独立地为-N =或-CH =; 并且R 5为其中R 6和R 7各自独立地为氢或有机基团的基团; R6和R7可以与相邻基团-XA-N-XB-一起形成环; XA和XB各自独立地为键，低级亚烷基等

3. 发明授权

US08106086B2 Indoledione derivative 有权
标题翻译：吲哚二酮衍生物
公开(公告)号：US08106086B2
公开(公告)日：2012-01-31
申请号：US12532182
申请日：2008-03-27
申请人： Toshiyuki Takahashi , Tsuyoshi Nagase , Nagaaki Sato
发明人： Toshiyuki Takahashi , Tsuyoshi Nagase , Nagaaki Sato
IPC分类号： A61K31/4155 , C07D403/02
CPC分类号： C07D403/04
摘要： A compound represented by the general formula (I-a): [wherein R1a and R2a each means hydrogen, lower cycloalkyl, lower alkyl, etc.; R3a means hydrogen, lower cycloalkyl, lower alkyl, etc.; R4a and R5a each means lower alkyl, lower cycloalkyl, etc. or R4a and R5a are bonded to each other to form lower cycloalkylidene; and R6a means lower alkyl, lower haloalkyl, etc.]. This compound functions as an LCE inhibitor and is useful as a therapeutic agent for various circulatory diseases, nervous diseases, metabolic diseases, reproductive diseases, digestive tract diseases, neoplasm, infectious diseases, etc.
摘要翻译：由通式（I-a）表示的化合物：[其中R 1a和R 2a各自表示氢，低级环烷基，低级烷基等; R3a表示氢，低级环烷基，低级烷基等; R4a和R5a各自表示低级烷基，低级环烷基等，或者R4a和R5a彼此键合形成较低环烷叉基; R6a表示低级烷基，低级卤代烷基等〕。该化合物作为LCE抑制剂起作用，可用作各种循环系统疾病，神经疾病，代谢疾病，生殖疾病，消化道疾病，肿瘤，感染性疾病等的治疗剂。

4. 发明申请

US20110009622A1 LONG-CHAIN FATTY ACYL ELONGASE INHIBITOR COMPRISING ARYLSULFONYL DERIVATIVE AS ACTIVE INGREDIENT 有权
标题翻译：包含ARYLSULFONYL衍生物作为活性成分的长链脂肪ACYL ELONGASE抑制剂
公开(公告)号：US20110009622A1
公开(公告)日：2011-01-13
申请号：US12933444
申请日：2009-04-17
申请人： Makoto Jitsuoka , Tsuyoshi Nagase , Nagaaki Sato , Daisuke Tsukahara
发明人： Makoto Jitsuoka , Tsuyoshi Nagase , Nagaaki Sato , Daisuke Tsukahara
IPC分类号： C07D223/06 , C07D413/12 , C07D265/30 , C07D239/38 , C07D487/08 , C07D241/18 , C07D221/22 , C07D498/04 , C07D471/04 , C07D413/04 , C07D401/04 , C07D401/12 , C07D211/96 , C07D211/54 , C07D213/56 , C07D249/12 , C07D235/14 , C07D403/12 , C07D231/18 , C07D207/48 , C07C311/16 , C07C237/20 , C07D413/14
CPC分类号： C07D211/96 , C07C311/16 , C07C311/19 , C07C311/20 , C07C317/44 , C07C2601/02 , C07C2601/14 , C07D207/48 , C07D213/70 , C07D213/75 , C07D231/40 , C07D231/52 , C07D239/38 , C07D249/12 , C07D265/28 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/12 , C07D413/04 , C07D453/06 , C07D471/04 , C07D471/06 , C07D471/08 , C07D487/04 , C07D487/08 , C07D491/04 , C07D491/08
摘要： [Problem] To provide compounds useful as preventives or remedies for circular system disorders, nervous system disorders, metabolic disorders, reproduction system disorders, digestive system disorders, neoplasm, infectious diseases, etc., or as herbicides.[Means for Solution] A long-chain fatty acyl elongase inhibitor comprising, as the active ingredient thereof, a compound or a pharmaceutically-active salt thereof of a formula (I): [wherein W represents a hydrogen atom, a C1-6 alkyl, etc.; X represents an aryl, a heteroaryl, etc.; n indicates 0 or 1; Z represents a hydrogen atom, a C1-6 alkyl, etc.; A1, A2, A3 and A4 each independently represent CH or N].
摘要翻译： [问题]提供可用作循环系统疾病，神经系统疾病，代谢紊乱，繁殖系统疾病，消化系统疾病，肿瘤，感染性疾病等的预防药物或补救剂的化合物或作为除草剂。 [解决方案]长链脂肪酰基延伸酶抑制剂，其包含作为其活性成分的式（I）的化合物或其药物活性盐：[其中W表示氢原子，C 1-6烷基等等 X表示芳基，杂芳基等; n表示0或1; Z表示氢原子，C1-6烷基等; A1，A2，A3和A4各自独立地表示CH或N]。

5. 发明申请

US20090209562A1 Fused ring 4-oxopyrimidine derivative 有权
公开(公告)号：US20090209562A1
公开(公告)日：2009-08-20
申请号：US12378163
申请日：2009-02-11
申请人： Tsuyoshi Nagase , Nagaaki Sato , Akio Kanatani , Shigeru Tokita
发明人： Tsuyoshi Nagase , Nagaaki Sato , Akio Kanatani , Shigeru Tokita
IPC分类号： A61K31/517 , C07D239/88 , A61P25/00
CPC分类号： C07D239/91 , A61K31/517 , A61K31/55 , A61K45/06 , C07D401/12 , C07D403/12 , C07D471/04 , C07D487/08 , A61K2300/00
摘要： The present invention provides a compound represented by formula (I) below, or a pharmaceutically acceptable salt thereof, which, having histamine H3 receptor antagonist or inverse agonist activity, is useful in the prophylaxis or therapy of metabolic diseases, circulatory diseases, or nervous system diseases. [where, for example, Ar is a divalent group formed by eliminating two hydrogen atoms from benzene, X1 is a nitrogen atom, sulfur atom or oxygen atom, R1 is a 5- to 6-membered heteroaryl group, Ring A is a 5- to 6-membered heteroaryl ring, R2 and R3 are amino groups or alkylamino groups, and X2 is represented by formula (II): (where R4 and R5 are lower alkyl groups, and n is an integer from 2 to 4).]

6. 发明申请

US20050182045A1 Fused ring 4-oxopyrimidine derivative 有权
标题翻译：稠环4-氧代嘧啶衍生物
公开(公告)号：US20050182045A1
公开(公告)日：2005-08-18
申请号：US11058444
申请日：2005-02-14
申请人： Tsuyoshi Nagase , Nagaaki Sato , Akio Kanatani , Shigeru Tokita
发明人： Tsuyoshi Nagase , Nagaaki Sato , Akio Kanatani , Shigeru Tokita
IPC分类号： A61K31/4725 , A61K31/517 , A61K31/519 , A61K31/55 , A61K45/06 , A61P1/16 , A61P3/04 , A61P3/06 , A61P3/10 , A61P3/12 , A61P5/00 , A61P9/00 , A61P9/04 , A61P9/10 , A61P9/12 , A61P13/12 , A61P19/06 , A61P25/02 , A61P25/08 , A61P25/14 , A61P25/16 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/32 , A61P25/36 , A61P43/00 , C07D217/24 , C07D239/70 , C07D239/91 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/12 , C07D471/04 , C07D487/08 , C07D43/02
CPC分类号： C07D239/91 , A61K31/517 , A61K31/55 , A61K45/06 , C07D401/12 , C07D403/12 , C07D471/04 , C07D487/08 , A61K2300/00
摘要： The present invention provides a compound represented by formula (I) below, or a pharmaceutically acceptable salt thereof, which, having histamine H3 receptor antagonist or inverse agonist activity, is useful in the prophylaxis or therapy of metabolic diseases, circulatory diseases, or nervous system diseases. [where, for example, Ar is a divalent group formed by eliminating two hydrogen atoms from benzene, X1 is a nitrogen atom, sulfur atom or oxygen atom, R1 is a 5- to 6-membered heteroaryl group, Ring A is a 5- to 6-membered heteroaryl ring, R2 and R3 are amino groups or alkylamino groups, and X2 is represented by formula (II): (where R4 and R5 are lower alkyl groups, and n is an integer from 2 to 4).]
摘要翻译：本发明提供下述式（I）表示的化合物或其药学上可接受的盐，其具有组胺H3受体拮抗剂或反向激动剂活性，可用于预防或治疗代谢性疾病，循环系统疾病或神经系统疾病 [其中，例如，Ar为通过从苯中除去两个氢原子形成的二价基团，X 1是氮原子，硫原子或氧原子，R 1是 5-至6-元杂芳基，环A为5-至6-元杂芳基环，R 2和R 3为氨基或烷基氨基，和 X 2由式（II）表示：其中R 4和R 5是低级烷基，n是2的整数至4）。]

7. 发明授权

US08268842B2 Fused ring 4-oxopyrimidine derivative 有权
标题翻译：稠环4-氧代嘧啶衍生物
公开(公告)号：US08268842B2
公开(公告)日：2012-09-18
申请号：US12378163
申请日：2009-02-11
申请人： Tsuyoshi Nagase , Nagaaki Sato , Akio Kanatani , Shigeru Tokita
发明人： Tsuyoshi Nagase , Nagaaki Sato , Akio Kanatani , Shigeru Tokita
IPC分类号： A61K31/519 , A61K31/517 , A01N43/54
CPC分类号： C07D239/91 , A61K31/517 , A61K31/55 , A61K45/06 , C07D401/12 , C07D403/12 , C07D471/04 , C07D487/08 , A61K2300/00
摘要： The present invention provides a compound represented by formula (I) below, or a pharmaceutically acceptable salt thereof, which, having histamine H3 receptor antagonist or inverse agonist activity, is useful in the prophylaxis or therapy of metabolic diseases, circulatory diseases, or nervous system diseases. [where, for example, Ar is a divalent group formed by eliminating two hydrogen atoms from benzene, X1 is a nitrogen atom, sulfur atom or oxygen atom, R1 is a 5- to 6-membered heteroaryl group, Ring A is a 5- to 6-membered heteroaryl ring, R2 and R3 are amino groups or alkylamino groups, and X2 is represented by formula (II): (where R4 and R5 are lower alkyl groups, and n is an integer from 2 to 4).]
摘要翻译：本发明提供下述式（I）表示的化合物或其药学上可接受的盐，其具有组胺H3受体拮抗剂或反向激动剂活性，可用于预防或治疗代谢性疾病，循环系统疾病或神经系统疾病 [其中，例如，Ar为通过从苯中除去2个氢原子形成的二价基团，X 1为氮原子，硫原子或氧原子，R 1为5〜6元杂芳基，环A为5- 至6元杂芳基环，R 2和R 3为氨基或烷基氨基，X 2由式（II）表示：（其中R 4和R 5为低级烷基，n为2至4的整数）。

8. 发明授权

US08124807B2 Sulfonyl-substituted 6-membered ring derivative 有权
标题翻译：磺酰取代的6元环衍生物
公开(公告)号：US08124807B2
公开(公告)日：2012-02-28
申请号：US12745761
申请日：2008-12-16
申请人： Tsuyoshi Nagase , Takahide Sasaki , Toshiyuki Takahashi
发明人： Tsuyoshi Nagase , Takahide Sasaki , Toshiyuki Takahashi
IPC分类号： C07C233/10 , C07D213/62 , C07D239/38
CPC分类号： C07C317/44 , C07C2601/14 , C07D211/54 , C07D213/71 , C07D213/75 , C07D233/84 , C07D239/38 , C07D277/36 , C07D285/125 , C07D401/12 , C07D417/12
摘要： [Problem]To provide a compound that is useful as an agent in the prevention and treatment of circulatory system, nervous system, metabolic, reproductive system, and gastrointestinal diseases.[Means for Resolution]A compound or a pharmaceutically acceptable salt thereof represented by the following Formula (I): [wherein, Z represents formula (II-1), (II-2), or (II-3), wherein m and n are 0, 1, or 2, Y represents CR3 or N, R1 represents a C1-6 alkyl, C3-8 cycloalkyl, etc., R2 represents phenyl or a heteroaryl, etc., R3 and R4 each independently represent a hydrogen atom, a C1-6 alkyl, etc., M1, M2, M3, and M4 each independently represent a hydrogen atom, a C1-6 alkyl, etc.]
摘要翻译： [问题]提供可用作预防和治疗循环系统，神经系统，代谢，生殖系统和胃肠道疾病的药剂的化合物。 [解决方法]由下式（I）表示的化合物或其药学上可接受的盐：[其中，Z表示式（II-1），（II-2）或（II-3），其中m和 n为0,1或2，Y表示CR 3或N，R 1表示C 1-6烷基，C 3-8环烷基等，R 2表示苯基或杂芳基等，R 3和R 4各自独立地表示氢原子，C 1-6烷基等，M 1，M 2，M 3和M 4各自独立地表示氢原子，C 1-6烷基等]

9. 发明申请

US20100249147A1 SULFONYL-SUBSTITUTED 6-MEMBERED RING DERIVATIVE 有权
标题翻译： SULFONYL取代的6会议室衍生
公开(公告)号：US20100249147A1
公开(公告)日：2010-09-30
申请号：US12745761
申请日：2008-12-16
申请人： Tsuyoshi Nagase , Takahide Sasaki , Toshiyuki Takahashi
发明人： Tsuyoshi Nagase , Takahide Sasaki , Toshiyuki Takahashi
IPC分类号： A61K31/497 , C07C233/10 , A61K31/167 , C07D213/62 , A61K31/4402 , C07D239/38 , A61K31/505 , A61P3/04 , A61P3/10 , A61P1/16
CPC分类号： C07C317/44 , C07C2601/14 , C07D211/54 , C07D213/71 , C07D213/75 , C07D233/84 , C07D239/38 , C07D277/36 , C07D285/125 , C07D401/12 , C07D417/12
摘要： [Problem] To provide a compound that is useful as an agent in the prevention and treatment of circulatory system, nervous system, metabolic, reproductive system, and gastrointestinal diseases.[Means for Resolution] A compound or a pharmaceutically acceptable salt thereof represented by the following Formula (I): [wherein, Z represents formula (II-1), (II-2), or (II-3), wherein m and n are 0, 1, or 2, Y represents CR3 or N, R1 represents a C1-6 alkyl, C3-8 cycloalkyl, etc., R2 represents phenyl or a heteroaryl, etc., R3 and R4 each independently represent a hydrogen atom, a C1-6 alkyl, etc., M1, M2, M3, and M4 each independently represent a hydrogen atom, a C1-6 alkyl, etc.]
摘要翻译： [问题]提供可用作预防和治疗循环系统，神经系统，代谢，生殖系统和胃肠道疾病的药剂的化合物。 [解决方法]由下式（I）表示的化合物或其药学上可接受的盐：[其中，Z表示式（II-1），（II-2）或（II-3），其中m和 n为0,1或2，Y表示CR 3或N，R 1表示C 1-6烷基，C 3-8环烷基等，R 2表示苯基或杂芳基等，R 3和R 4各自独立地表示氢原子，C 1-6烷基等，M 1，M 2，M 3和M 4各自独立地表示氢原子，C 1-6烷基等]

10. 发明授权

US07790731B2 Crystal form of 2-methyl-3-{4-[3-(1-pyrrolidinyl)propoxy]phenyl}-5-trifluoromethyl-4(3H)-quinazolinone 失效
标题翻译： 2-甲基-3- {4- [3-（1-吡咯烷基）丙氧基]苯基} -5-三氟甲基-4（3H） - 喹唑啉酮的晶型
公开(公告)号：US07790731B2
公开(公告)日：2010-09-07
申请号：US11884138
申请日：2006-02-13
申请人： Akio Kanatani , Nagaaki Sato , Tsuyoshi Nagase , Shigeru Tokita
发明人： Akio Kanatani , Nagaaki Sato , Tsuyoshi Nagase , Shigeru Tokita
IPC分类号： A61K31/517
CPC分类号： C07D239/91 , A61K31/517 , A61K45/06
摘要： The present invention is directed to a form I crystal of 2-methyl 3-{4-[3-(1-pyrrolidinyl)propoxy]phenyl}-5-trifluoromethyl-4(3H)-quinazolinone that is useful for example in the treatment of sleep disorders or various sleep disorder-associated diseases.
摘要翻译：本发明涉及例如在治疗中有用的2-甲基3- {4- [3-（1-吡咯烷基）丙氧基]苯基} -5-三氟甲基-4（3H） - 喹唑啉酮的I型晶体的睡眠障碍或各种睡眠障碍相关疾病。

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