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1. 发明授权

US07164024B2 Benzimidazolone derivatives 失效
标题翻译：苯并咪唑酮衍生物
公开(公告)号：US07164024B2
公开(公告)日：2007-01-16
申请号：US10475447
申请日：2002-04-19
申请人： Takeru Yamakawa , Yoshio Ogino , Yufu Sagara , Kenji Matsuda , Akira Naya , Toshifumi Kimura , Norikazu Otake
发明人： Takeru Yamakawa , Yoshio Ogino , Yufu Sagara , Kenji Matsuda , Akira Naya , Toshifumi Kimura , Norikazu Otake
IPC分类号： A61K31/44
CPC分类号： C07D401/14 , C07D409/14
摘要： This invention relates to benzimidazolone derivatives, represented by compounds of a general formula [I] [in which R1 and R2 stand for, e.g., hydrogen atoms; R3a, R3b, R4, R5 stand for, e.g., hydrogen atoms and alkyl groups; R6 stands for e.g., aryl or heteroaryl groups; A ring stands for 5- to 8-membered aliphatic heterocyclic ring containing one nitrogen atom; and Z stands for carbonyl group or sulfonyl group]. The benzimidazolone derivatives of the invention exhibit antagonism to muscarinic acetylcholine receptors, and are useful as treating agent and/or prophylactic of Parkinson's disease, drug-induced parkinsonism, dystonia, akinesia, pancreatitis, bilestone/cholecystitis, biliary dyskinesia, achalasia, pain, itch, cholinergic urticaria, irritable bowel syndrome, vomiting, nausea, dizziness, Meniere's disease, motion sickness and urinary disturbance.
摘要翻译：本发明涉及由通式[I] [其中R 1，R 2和R 2]的化合物代表的例如氢原子的苯并咪唑酮衍生物; R 3a，R 3b，R 4，R 5表示例如氢原子和烷基; R 6表示例如芳基或杂芳基; 环代表含有一个氮原子的5-至8-元脂族杂环; Z代表羰基或磺酰基]。本发明的苯并咪唑酮衍生物对毒蕈碱性乙酰胆碱受体表现出拮抗作用，可用作帕金森病，药物诱发的帕金森综合征，肌张力障碍，运动不良，胰腺炎，胆石，胆囊炎，胆汁运动障碍，贲门失弛缓症，疼痛，瘙痒的治疗剂和/或预防，胆碱能性荨麻疹，肠易激综合征，呕吐，恶心，眩晕，梅尼埃病，运动病和尿紊乱。

2. 发明授权

US07452908B2 Amide derivatives 失效
标题翻译：酰胺衍生物
公开(公告)号：US07452908B2
公开(公告)日：2008-11-18
申请号：US10838340
申请日：2004-05-05
申请人： Yufu Sagara , Minaho Uchiyama , Akira Naya , Toshifumi Kimura , Tomoshige Numazawa , Toru Fujikawa , Norikazu Otake , Kazuhito Noguchi
发明人： Yufu Sagara , Minaho Uchiyama , Akira Naya , Toshifumi Kimura , Tomoshige Numazawa , Toru Fujikawa , Norikazu Otake , Kazuhito Noguchi
IPC分类号： A61K31/445 , C07D211/32
CPC分类号： C07D401/12 , C07D207/16 , C07D211/26 , C07D401/14 , C07D471/10 , C07D493/10
摘要： This invention relates to compounds which are represented by the general formula [I] [in which A stands for a group of the following formula [ao] or [b0] Ar1, Ar2 and Ar3 stand for optionally substituted phenyl; k stands for 0 or 1; m, n and s stand for 0, 1 or 2; R1 stands for hydrogen or optionally substituted lower alkyl; R2, R3, R4 and R5 either stand for hydrogen or optionally substituted lower alkyl, or R2 and R3, or R4 and R5 together stand for trimethylene and the like; R60 stands for hydrogen, alkyl, or the like; R61 and R71 either stand for alkyl and the like, or together stand for trimethylene and the like; X stands for carbonyl or methylene; Y stands for nitrogen or methine; and Q− stands for anion], and the like. The compounds of the invention exhibit selective antagonism to muscarinic M3 receptors, and therefore are useful as safe and effective agents showing little side effect, for treating diseases of the respiratory, urinary and digestive systems.
摘要翻译：本发明涉及由通式[I]表示的化合物[其中A代表下列通式[a]或[b] 0 Ar 1，Ar 2和Ar 3代表任选取代的苯基; k代表0或1; m，n和s代表0,1或2; R 1表示氢或任选取代的低级烷基; R 2，R 3，R 4和R 5均代表氢或任选取代的低级烷基，或 R 2和R 3，或R 4和R 5一起代表三亚甲基等; R 60代表氢，烷基等; R 61和R 71均代表烷基等，或一起代表三亚甲基等; X代表羰基或亚甲基; Y代表氮或次甲基; 和Q ^{代表阴离子]等。本发明的化合物对毒蕈碱M 3受体表现出选择性拮抗作用，因此可用作治疗呼吸，泌尿和消化系统疾病的副作用小的安全有效的药剂。}

3. 发明授权

US06809108B1 Amide derivatives 失效
标题翻译：酰胺衍生物
公开(公告)号：US06809108B1
公开(公告)日：2004-10-26
申请号：US10031716
申请日：2002-03-26
申请人： Yufu Sagara , Minaho Uchiyama , Akira Naya , Toshifumi Kimura , Tomoshige Numazawa , Toru Fujikawa , Norikazu Otake , Kazuhito Noguchi
发明人： Yufu Sagara , Minaho Uchiyama , Akira Naya , Toshifumi Kimura , Tomoshige Numazawa , Toru Fujikawa , Norikazu Otake , Kazuhito Noguchi
IPC分类号： A61K31445
CPC分类号： C07D401/12 , C07D207/16 , C07D211/26 , C07D401/14 , C07D471/10 , C07D493/10
摘要： This invention relates to compounds which are represented by the general formula [I] [in which A stands for a group of the following formula [a0] or [b0] Ar1, Ar2 and Ar3 stand for optionally substituted phenyl; k stands for 0 or 1; m, n and a stand for 0, 1 or 2; R1 stands for hydrogen or optionally substituted lower alkyl; R2, R3, R4 and R5 either stand for hydrogen or optionally substituted lower alkyl, or R2 and R3, or R4 and R5 together stand for trimethylene and the like; R60 stands for hydrogen, alkyl, or the like; R61 and R71 either stand for alkyl and the like, or together stand for trimethylene and the like; X stands for carbonyl or methylene; Y stands for nitrogen or methine; and Q− stands for anion], and the like. The compounds of the invention exhibit selective antagonism to muscarinic M3 receptors, and therefore are useful as safe and effective agents showing little side effect, for treating diseases of the respiratory, urinary and digestive systems.
摘要翻译：本发明涉及由通式[I]表示的化合物[其中A代表下式[a0]或[b0] Ar 1的基团，Ar 2和Ar 3代表任选取代的苯基; k代表0或1; m，n和a代表0,1或2; R 1代表氢或任选取代的低级烷基; R 2，R 3，R 4和R 5分别代表氢或任选取代的低级烷基，或者R 2和R 3，或R 4和R 5，一起代表三亚甲基等; R 60代表氢，烷基等; R 61和R 71代表烷基等，或一起代表三亚甲基等; X代表羰基或亚甲基; Y代表氮或次甲基; 并且Q 1表示阴离子]等。本发明的化合物对毒蕈碱性M3受体表现出选择性拮抗作用，因此可用作治疗副作用小的安全有效药物，用于治疗呼吸道，尿和尿的疾病消化系统。

4. 发明授权

US07875633B2 Phenylpyridone derivative 失效
标题翻译：苯基吡啶酮衍生物
公开(公告)号：US07875633B2
公开(公告)日：2011-01-25
申请号：US11990889
申请日：2006-08-23
申请人： Akira Naya , Toshihiro Sakamoto , Yuji Haga , Norikazu Otake
发明人： Akira Naya , Toshihiro Sakamoto , Yuji Haga , Norikazu Otake
IPC分类号： A61K31/444 , A61K31/4439 , A61K31/5377 , A61K31/4545 , A61P9/00 , A61P25/00 , A61P3/00 , C07D213/64 , C07D401/02 , C07D413/02 , C07D401/14
CPC分类号： C07D213/69 , C07D213/64 , C07D401/10 , C07D413/10
摘要： A compound represented by the formula (I) is contained as an active ingredient: wherein R1 and R2 independently represent a hydrogen atom, a lower alkyl group or the like, or R1 together with a nitrogen atom to which L, Z2 and R1 are attached may form an aliphatic nitrogenated heterocyclic group and R1 and R2 together with a nitrogen atom to which they are attached may form an aliphatic nitrogenated heterocyclic group; X represents a methine group or a nitrogen atom; Y represents —CH2—O—, —CH═CH— or the like; Z1 represents a single bond, a C1-4 alkylene group or the like; Z2 represents a single bond or a C1-4 alkylene group; L represents a methylene group, a C3-8 cycloalkylene group or the like; and Ar represents an aromatic carbocyclic group or the like. The compound is useful as a pharmaceutical for a central nerves system disease, a cardiovascular disease or a metabolic disease.
摘要翻译：作为活性成分，含有式（I）所示的化合物：其中，R 1和R 2分别独立地表示氢原子，低级烷基等，或者与连接有L，Z 2和R 1的氮原子一起形成可以形成脂族氮杂环基，并且R 1和R 2与它们所连接的氮原子一起形成脂族氮杂环基; X表示次甲基或氮原子; Y表示-CH 2 -O-，-CH = CH-等; Z1表示单键，C1-4亚烷基等; Z2表示单键或C1-4亚烷基; L表示亚甲基，C3-8亚环烷基等; Ar表示芳族碳环基等。该化合物可用作中枢神经系统疾病，心血管疾病或代谢疾病的药物。

5. 发明授权

US07732456B2 Pyridone derivative 失效
标题翻译：吡啶酮衍生物
公开(公告)号：US07732456B2
公开(公告)日：2010-06-08
申请号：US10591373
申请日：2005-03-04
申请人： Norikazu Otake , Yuji Haga , Akira Naya , Sayaka Mizutani , Akio Kanatani
发明人： Norikazu Otake , Yuji Haga , Akira Naya , Sayaka Mizutani , Akio Kanatani
IPC分类号： A61K31/444 , C07D401/02
CPC分类号： C07D213/69 , C07D237/16 , C07D239/52 , C07D401/12 , C07D401/14 , C07D403/12 , C07D409/14 , C07D451/02 , C07D471/04
摘要： The invention provides pyridone derivatives represented by a general formula (I) [in the formula, R1 and R2 may be same or different and stands for H, etc., or R1 and R2 may form an aliphatic nitrogen-containing heterocyclic group together with the N to which they bind; X1-X3 may be same or different and stand for methine or N, provided not all of them simultaneously stand for nitrogen; X4-X7 may be same or different and stand for methine or N, provided that three or more of them do not simultaneously stand for N; Y1 and Y3 may be same or different and stand for single bond, —O—, —NR—, —S—, etc; Y2 stands for lower lkylene, etc.; R stands for H, etc., L stands for methylene; Z1 and Z2 may be same or different and stand for single bond or lower alkylene; or R1, L and Z2 may form an aliphatic nitrogen-containing heterocyclic group with the N to which R1 binds; and Ar stands for aromatic carbocyclic group, etc.].
摘要翻译：本发明提供由通式（I）表示的吡啶酮衍生物[在该式中，R 1和R 2可以相同或不同，代表H等，或者R 1和R 2可以与脂族含氮杂环基一起形成他们绑定的N X1-X3可以相同或不同，代替次甲基或N，但不是全部同时代表氮; X4-X7可以相同或不同，代表次甲基或N，条件是它们中的三个或更多不同时代表N; Y1和Y3可以相同或不同，代表单键，-O-，-NR-，-S-等; Y2代表低级亚烷基等; R代表H等，L代表亚甲基; Z 1和Z 2可以相同或不同，代表单键或低级亚烷基; 或R1，L和Z2可以与R1结合的N形成脂族含氮杂环基; 和Ar代表芳族碳环基团等]。

6. 发明申请

US20090137587A1 Phenylpyridone Derivative 失效
标题翻译：苯基吡啶酮衍生物
公开(公告)号：US20090137587A1
公开(公告)日：2009-05-28
申请号：US11990889
申请日：2006-08-23
申请人： Akira Naya , Toshihiro Sakamoto , Yuji Haga , Norikazu Otake
发明人： Akira Naya , Toshihiro Sakamoto , Yuji Haga , Norikazu Otake
IPC分类号： A61K31/444 , C07D213/64 , C07D401/02 , C07D413/02 , A61K31/4439 , A61P9/00 , A61P25/00 , A61P3/00 , C07D401/14 , A61K31/5377 , A61K31/4545
CPC分类号： C07D213/69 , C07D213/64 , C07D401/10 , C07D413/10
摘要： A compound represented by the formula (I) is contained as an active ingredient: wherein R1 and R2 independently represent a hydrogen atom, a lower alkyl group or the like, or R1 together with a nitrogen atom to which L, Z2 and R1 are attached may form an aliphatic nitrogenated heterocyclic group and R1 and R2 together with a nitrogen atom to which they are attached may form an aliphatic nitrogenated heterocyclic group; X represents a methine group or a nitrogen atom; Y represents —CH2—O—, —CH═CH— or the like; Z1 represents a single bond, a C1-4 alkylene group or the like; Z2 represents a single bond or a C1-4 alkylene group; L represents a methylene group, a C3-8 cycloalkylene group or the like; and Ar represents an aromatic carbocyclic group or the like. The compound is useful as a pharmaceutical for a central nerves system disease, a cardiovascular disease or a metabolic disease.
摘要翻译：作为活性成分，含有式（I）所示的化合物：其中，R 1和R 2分别独立地表示氢原子，低级烷基等，或者与连接有L，Z 2和R 1的氮原子一起形成可以形成脂族氮杂环基，并且R 1和R 2与它们所连接的氮原子一起形成脂族氮杂环基; X表示次甲基或氮原子; Y表示-CH 2 -O - ， - CH-CH-等; Z1表示单键，C1-4亚烷基等; Z2表示单键或C1-4亚烷基; L表示亚甲基，C3-8亚环烷基等; Ar表示芳族碳环基等。该化合物可用作中枢神经系统疾病，心血管疾病或代谢疾病的药物。

7. 发明申请

US20070208046A1 Pyridone derivative 失效
标题翻译：吡啶酮衍生物
公开(公告)号：US20070208046A1
公开(公告)日：2007-09-06
申请号：US10591373
申请日：2005-03-04
申请人： Norikazu Otake , Yuji Haga , Akira Naya , Sayaka Mizutani , Akio Kanatani
发明人： Norikazu Otake , Yuji Haga , Akira Naya , Sayaka Mizutani , Akio Kanatani
IPC分类号： A61K31/513 , A61K31/444 , A61K31/4412 , C07D403/02 , C07D401/02
CPC分类号： C07D213/69 , C07D237/16 , C07D239/52 , C07D401/12 , C07D401/14 , C07D403/12 , C07D409/14 , C07D451/02 , C07D471/04
摘要： The invention provides pyridone derivatives represented by a general formula (I) [in the formula, R1 and R2 may be same or different and stands for H, etc., or R1 and R2 may form an aliphatic nitrogen-containing heterocyclic group together with the N to which they bind; X1-X3 may be same or different and stand for methine or N, provided not all of them simultaneously stand for nitrogen; X4-X7 may be same or different and stand for methine or N, provided that three or more of them do not simultaneously stand for N; Y1 and Y3 may be same or different and stand for single bond, —O—, —NR—, —S—, etc; Y2 stands for lower alkylene, etc.; R stands for H, etc., L stands for methylene; Z1 and Z2 may be same or different and stand for single bond or lower alkylene; or R1, L and Z2 may form an aliphatic nitrogen-containing heterocyclic group with the N to which R1 binds; and Ar stands for aromatic carbocyclic group, etc.].
摘要翻译：本发明提供由通式（I）表示的吡啶酮衍生物[在式中，R 1和R 2可以相同或不同，代表H等，或R 1和R 2可以与它们所键合的N一起形成脂族含氮杂环基; X 1 -X 3可以相同或不同，代表次甲基或N，但并不全部同时代表氮; X 4 -X 7可以相同或不同，代表次甲基或N，条件是它们中的三个或更多个不同时代表N; Y 1和Y 3可以相同或不同，代表单键，-O-，-NR-，-S-等; Y 2代表低级亚烷基等; R代表H等，L代表亚甲基; Z 1和Z 2可以相同或不同，代表单键或低级亚烷基; 或R 1，L和Z 2可以与R 1结合的N形成脂族含氮杂环基; 和Ar代表芳族碳环基团等]。

8. 发明授权

US08207169B2 Substituted [1,2,4]triazolo[4′,3′:1,6]pyrido[2,3-b]pyrazines of the formula D 有权
标题翻译：取代的[1,2,4]三唑并[4'，3'：1,6]吡啶并[2,3-b]
公开(公告)号：US08207169B2
公开(公告)日：2012-06-26
申请号：US12995832
申请日：2009-05-28
申请人： Hidetomo Furuyama , Yasuhiro Goto , Nobuhiko Kawanishi , Mark E. Layton , Takashi Mita , Akira Naya , Yoshio Ogino , Yu Onozaki , Kevin J. Rodzinak , Toshihiro Sakamoto , Philip E. Sanderson , Jiabing Wang
发明人： Hidetomo Furuyama , Yasuhiro Goto , Nobuhiko Kawanishi , Mark E. Layton , Takashi Mita , Akira Naya , Yoshio Ogino , Yu Onozaki , Kevin J. Rodzinak , Toshihiro Sakamoto , Philip E. Sanderson , Jiabing Wang
IPC分类号： A61K31/495
CPC分类号： C07D471/14
摘要： The compounds of Formula D are of the class of triazolo-pyrido-pyrazines which are inhibitors of AKT useful for the treatment of cancer
摘要翻译：式D的化合物是三唑并 - 吡啶并吡嗪类，其是可用于治疗癌症的AKT抑制剂

9. 发明申请

US20110092511A1 INHIBITORS OF AKT ACTIVITY 有权
标题翻译： AKT活动的抑制剂
公开(公告)号：US20110092511A1
公开(公告)日：2011-04-21
申请号：US12995832
申请日：2009-05-28
申请人： Hidetomo Furuyama , Yasuhiro Goto , Nobuhiko Kawanishi , Mark E. Layton , Takashi Mita , Akira Naya , Yoshio Ogino , Yu Onozaki , Kevin J. Rodzinak , Toshihiro Sakamoto , Philip E. Sanderson , Jiabing Wang
发明人： Hidetomo Furuyama , Yasuhiro Goto , Nobuhiko Kawanishi , Mark E. Layton , Takashi Mita , Akira Naya , Yoshio Ogino , Yu Onozaki , Kevin J. Rodzinak , Toshihiro Sakamoto , Philip E. Sanderson , Jiabing Wang
IPC分类号： A61K31/4985 , C07D471/14 , A61K31/4375 , C07D403/14 , A61K31/506 , A61P35/00
CPC分类号： C07D471/14
摘要： The instant invention provides for substituted naphthyridine compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms, preferably Akt1. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity especially Akt1 by administering the compound to a patient in need of treatment of cancer.
摘要翻译：本发明提供抑制Akt活性的取代的萘啶化合物。特别地，所公开的化合物选择性地抑制一种或两种Akt同种型，优选Akt1。本发明还提供了包含这种抑制化合物的组合物和通过将该化合物给予需要治疗癌症的患者来抑制Akt活性，尤其是Akt1的方法。

10. 发明授权

US6140338A Chemokine receptor antagonists 失效
标题翻译：趋化因子受体拮抗剂
公开(公告)号：US6140338A
公开(公告)日：2000-10-31
申请号：US147595
申请日：1999-01-29
申请人： Akira Naya , Yufu Owada , Toshihiko Saeki , Kenji Ohwaki , Yoshikazu Iwasawa
发明人： Akira Naya , Yufu Owada , Toshihiko Saeki , Kenji Ohwaki , Yoshikazu Iwasawa
IPC分类号： C07D401/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/12 , C07D417/12 , C07D451/14 , A61K31/453 , A61K31/439 , A61K31/4535
CPC分类号： C07D401/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/12 , C07D417/12 , C07D451/14
摘要： The present invention relates to a compound of the general formula: ##STR1## wherein each of R.sup.1 and R.sup.2 which may be the same or different, is e.g. a hydrogen atom, a halogen atom or a lower alkyl group, X is an oxygen atom, a sulfur atom or CH, Y is CH or a nitrogen atom, and A is e.g. a 1-substituted-4-piperidinyl group, a pharmaceutically acceptable salt thereof, a pharmaceutically acceptable anion-exchange product thereof or a hydrate thereof. The compounds of the present invention have chemokine receptor antagonism, and thus they are useful as treating agents for various diseases relating to chemokine, such as acute inflammatory diseases, chronic inflammatory diseases, acquired immune deficiency syndrome, cancer, ischemic reflow disorder and/or arteriosclerosis.
摘要翻译： PCT No.PCT / JP97 / 02548 Sec。 371日期1999年1月29日第 102（e）日期1999年1月29日PCT提交1997年7月23日PCT公布。第WO98 / 04554号公报日期：1998年2月5日本发明涉及以下通式的化合物：其中R1和R2各自可以相同或不同，氢原子，卤素原子或低级烷基，X是氧原子，硫原子或CH，Y是CH或氮原子，A是例如。 1-取代-4-哌啶基，其药学上可接受的盐，其药学上可接受的阴离子交换产物或其水合物。本发明的化合物具有趋化因子受体拮抗作用，因此它们可用作与趋化因子有关的各种疾病如急性炎性疾病，慢性炎性疾病，获得性免疫缺陷综合征，癌症，缺血性回流病和/或动脉硬化的治疗剂。。

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