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1. 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。}

2. 发明申请

US20080090799A1 2-PYRIDINECARBOXAMIDE DERIVATIVE HAVING GK-ACTIVATING EFFECT 有权
标题翻译：具有GK活化作用的2-吡啶甲酰胺衍生物
公开(公告)号：US20080090799A1
公开(公告)日：2008-04-17
申请号：US11973240
申请日：2007-10-05
申请人： Noriaki Hashimoto , Yufu Sagara , Masanori Asai , Teruyuki Nishimura
发明人： Noriaki Hashimoto , Yufu Sagara , Masanori Asai , Teruyuki Nishimura
IPC分类号： A61K31/4439 , A61K31/433 , A61K31/4545 , A61K31/5377 , A61P3/10 , C07D417/14
CPC分类号： C07D417/14
摘要： Compounds of a formula (I) and their pharmaceutically-acceptable salts are disclosed. The compounds have glucokinase-activating effect and are therefore useful for treatment of diabetes and obesity. R1 and R2 each independently represent a lower alkyl group; X1 represent a group of a formula (II-1): wherein: R11 and R12 each independently represent a hydrogen atom or a lower alkyl group, or taken together with the nitrogen atom to which they bond, R11 and R12 may form a 4- to 7-membered nitrogen-containing aliphatic ring (one carbon atom constituting the 4- to 7-membered nitrogen-containing aliphatic ring may be replaced by an oxygen atom), or taken together with a carbon atom in (CH2)m, R11 and R12 may form a 4- to 7-membered nitrogen-containing aliphatic ring; m indicates an integer of from 1 to 3.
摘要翻译：公开了式（I）化合物及其药学上可接受的盐。该化合物具有葡糖激酶活化作用，因此可用于治疗糖尿病和肥胖症。 R 1和R 2各自独立地表示低级烷基; X 1表示式（II-1）的基团：其中：R 11和R 12各自独立地表示氢原子或低级烷基或与它们键合的氮原子一起，R 11和R 12可以形成4-至7-元含氮脂族环（构成4〜7元含氮脂肪族环的一个碳原子可以被氧原子取代），或者与（CH 2 2）m < R 11，R 11和R 12可以形成4-至7-元含氮脂族环; m表示1〜3的整数。

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. 发明申请

US20050176765A1 Ophthalmic compositions for treating ocular hypertension 失效
标题翻译：用于治疗高眼压症的眼用组合物
公开(公告)号：US20050176765A1
公开(公告)日：2005-08-11
申请号：US10515127
申请日：2003-06-17
申请人： Miller Ogidigben , Takeru Yamakawa , Yufu Sagara
发明人： Miller Ogidigben , Takeru Yamakawa , Yufu Sagara
IPC分类号： A61K9/08 , A61K9/10 , A61K31/4545 , A61K31/4747 , A61K45/00 , A61K47/36 , A61P1/04 , A61P9/10 , A61P25/02 , A61P25/04 , A61P25/18 , A61P25/20 , A61P25/28 , A61P27/06 , C07D235/26 , C07D271/10 , C07D271/107 , C07D401/04 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D495/04 , C07D43/14
CPC分类号： C07D271/107 , C07D235/26 , C07D401/04 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D495/04
摘要： This invention relates to selective m1 muscarinic agonist, their use or a formulation thereof in the treatment of glaucoma and/or other conditions which are related to elevated intraocular pressure in the eye of a patient. This invention also relates to the use of such compounds to provide a neuroprotective effect to the eye of mammalian species, particularly humans. In addition, the present invention relates to the use of the compounds in the treatment of dementia such as Alzheimer's disease and vascular dementia, depression, attention deficit disorder, sleep disorder, schizophrenia, pain, ischemia, atrophic gastritis, and atony of gastrointestinal tract.
摘要翻译：本发明涉及选择性m1毒蕈碱激动剂，它们在治疗与患者眼睛中眼内压升高相关的青光眼和/或其他病症中的用途或制剂。本发明还涉及这些化合物对哺乳动物物种尤其是人的眼睛的神经保护作用的用途。此外，本发明涉及该化合物在治疗诸如阿尔茨海默病和血管性痴呆，抑郁症，注意力缺陷障碍，睡眠障碍，精神分裂症，疼痛，局部缺血，萎缩性胃炎和胃肠道疾病的痴呆中的用途。

5. 发明授权

US07279490B2 Ophthalmic compositions for treating ocular hypertension 失效
标题翻译：用于治疗高眼压症的眼用组合物
公开(公告)号：US07279490B2
公开(公告)日：2007-10-09
申请号：US10515127
申请日：2003-06-17
申请人： Miller J Ogidigben , Takeru Yamakawa , Yufu Sagara
发明人： Miller J Ogidigben , Takeru Yamakawa , Yufu Sagara
IPC分类号： A61K31/4545 , C07D401/14
CPC分类号： C07D271/107 , C07D235/26 , C07D401/04 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D495/04
摘要： This invention relates to selective m1 muscarinic agonist, their use or a formulation thereof in the treatment of glaucoma and/or other conditions which are related to elevated intraocular pressure in the eye of a patient. This invention also relates to the use of such compounds to provide a neuroprotective effect to the eye of mammalian species, particularly humans. In addition, the present invention relates to the use of the compounds in the treatment of dementia such as Alzheimer's disease and vascular dementia, depression, attention deficit disorder, sleep disorder, schizophrenia, pain, ischemia, atrophic gastritis, and atony of gastrointestinal tract.
摘要翻译：本发明涉及选择性m1毒蕈碱激动剂，它们在治疗与患者眼睛中眼内压升高相关的青光眼和/或其他病症中的用途或制剂。本发明还涉及这些化合物对哺乳动物物种尤其是人的眼睛的神经保护作用的用途。此外，本发明涉及该化合物在治疗诸如阿尔茨海默病和血管性痴呆，抑郁症，注意力缺陷障碍，睡眠障碍，精神分裂症，疼痛，局部缺血，萎缩性胃炎和胃肠道疾病的痴呆中的用途。

6. 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。

7. 发明授权

US08338460B2 2-pyridinecarboxamide derivative having GK-activating effect 有权
标题翻译：具有GK活化作用的2-吡啶甲酰胺衍生物
公开(公告)号：US08338460B2
公开(公告)日：2012-12-25
申请号：US11973240
申请日：2007-10-05
申请人： Noriaki Hashimoto , Yufu Sagara , Masanori Asai , Teruyuki Nishimura
发明人： Noriaki Hashimoto , Yufu Sagara , Masanori Asai , Teruyuki Nishimura
IPC分类号： A61K31/433 , A61K31/4439 , C07D417/14 , C07D417/10
CPC分类号： C07D417/14
摘要： Compounds of a formula (I) and their pharmaceutically-acceptable salts are disclosed. The compounds have glucokinase-activating effect and are therefore useful for treatment of diabetes and obesity. R1 and R2 each independently represent a lower alkyl group; X1 represent a group of a formula (II-1): wherein: R11 and R12 each independently represent a hydrogen atom or a lower alkyl group, or taken together with the nitrogen atom to which they bond, R11 and R12 may form a 4- to 7-membered nitrogen-containing aliphatic ring (one carbon atom constituting the 4- to 7-membered nitrogen-containing aliphatic ring may be replaced by an oxygen atom), or taken together with a carbon atom in (CH2)m, R11 and R12 may form a 4- to 7-membered nitrogen-containing aliphatic ring; m indicates an integer of from 1 to 3.
摘要翻译：公开了式（I）化合物及其药学上可接受的盐。该化合物具有葡糖激酶活化作用，因此可用于治疗糖尿病和肥胖症。 R1和R2各自独立地表示低级烷基; X 1表示式（II-1）的基团：其中：R 11和R 12各自独立地表示氢原子或低级烷基，或与它们所键合的氮原子一起，R 11和R 12可以形成4- 至7元含氮脂肪族环（构成4〜7元含氮脂肪族环的一个碳原子可以被氧原子取代），或与（CH 2）m，R 11和 R12可以形成4-至7-元含氮脂族环; m表示1〜3的整数。

8. 发明申请

US20100261699A1 N-PYRAZOLE-2-PYRIDINE CARBOXAMIDE DERIVATIVE 审中-公开
标题翻译： N-吡咯-2-吡啶酰胺衍生物
公开(公告)号：US20100261699A1
公开(公告)日：2010-10-14
申请号：US12746567
申请日：2008-12-15
申请人： Noriaki Hashimoto , Teruyuki Nishimura , Yufu Sagara
发明人： Noriaki Hashimoto , Teruyuki Nishimura , Yufu Sagara
IPC分类号： A61K31/4439 , C07D401/14 , A61P3/10
CPC分类号： A61K31/155 , A61K31/427 , A61K31/44 , A61K31/4439 , A61K31/444 , A61K38/28 , A61K38/31 , C07D401/14 , A61K2300/00
摘要： The present invention relates to a compound represented by the formula: or a pharmaceutically acceptable salt thereof, wherein R1 and R2 are each independently a lower alkyl group, X is CH or the like, and X1 is an aminoalkoxy group or the like, which has a glucokinase-activating effect and thus is useful in the treatment of diabetes, obesity, and the like.
摘要翻译：本发明涉及由下式表示的化合物或其药学上可接受的盐，其中R1和R2各自独立地为低级烷基，X为CH等，X1为氨基烷氧基等，其具有葡糖激酶活化作用，因此可用于治疗糖尿病，肥胖症等。

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