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    Biaryl derivatives
    2.
    发明授权
    Biaryl derivatives 失效
    双芳基衍生物

    公开(公告)号：US07858800B2

    公开(公告)日：2010-12-28

    申请号：US11629730

    申请日：2005-06-29

    申请人： Hiroshi Kawamoto ,  Satoru Ito ,  Atsushi Satoh ,  Yasushi Nagatomi ,  Yukari Hirata ,  Toshifumi Kimura ,  Gentaroh Suzuki ,  Akio Sato ,  Hisashi Ohta

    发明人： Hiroshi Kawamoto ,  Satoru Ito ,  Atsushi Satoh ,  Yasushi Nagatomi ,  Yukari Hirata ,  Toshifumi Kimura ,  Gentaroh Suzuki ,  Akio Sato ,  Hisashi Ohta

    IPC分类号： C07D401/00 ,  A61K31/44

    CPC分类号： C07D401/14 ,  C07D249/06 ,  C07D271/04 ,  C07D401/04 ,  C07D417/04

    摘要： The present invention relates to a compound represented by the formula (I): or a pharmaceutically acceptable salt thereof, wherein: R1 is a linear or branched alkoxy group, a cycloalkoxy group, a linear or branched lower alkyl group, etc.; R2 is halogen atom, a lower alkyl group, etc.; Q1 is carbon atom or nitrogen atom; Q2 is carbon atom which may be substituted with oxo group; the formula (III):   (II) is a single bond or a double bond; A is a group selected from the group consisting of the substitutent group α; and R5 is hydrogen atom, a lower alkyl group, cyano group, an alkoxy group or a trialkylsilyl group; having an mGluR1 inhibiting action and being useful as treatment and/or prevention of convulsion, acute pain, cerebral disturbance such as cerebral infarction or transient cerebral ischemia onset, anxiety, chemical dependency or Parkinson's disease.

    摘要翻译： 本发明涉及由式（I）表示的化合物或其药学上可接受的盐，其中：R1是直链或支链烷氧基，环烷氧基，直链或支链低级烷基等; R2是卤原子，低级烷基等; Q1是碳原子或氮原子; Q2是可以被氧代基取代的碳原子; 式（III）：（II）是单键或双键; A是选自由取代基α组成的组的基团; R5为氢原子，低级烷基，氰基，烷氧基或三烷基甲硅烷基; 具有mGluR1抑制作用，并且可用作治疗和/或预防惊厥，急性疼痛，脑梗塞如脑梗死或暂时性脑缺血发作，焦虑，化学依赖或帕金森病。

    Biaryl derivatives
    3.
    发明申请
    Biaryl derivatives 失效
    双芳基衍生物

    公开(公告)号：US20070191389A1

    公开(公告)日：2007-08-16

    申请号：US11629730

    申请日：2005-06-29

    申请人： Hiroshi Kawamoto ,  Satoru Ito ,  Atsushi Satoh ,  Yasushi Nagatomi ,  Yukari Hirata ,  Toshifumi Kimura ,  Gentaroh Suzuki ,  Akio Sato ,  Hisashi Ohta

    发明人： Hiroshi Kawamoto ,  Satoru Ito ,  Atsushi Satoh ,  Yasushi Nagatomi ,  Yukari Hirata ,  Toshifumi Kimura ,  Gentaroh Suzuki ,  Akio Sato ,  Hisashi Ohta

    IPC分类号： A61K31/496 ,  A61K31/454 ,  A61K31/4439 ,  C07D413/02 ,  C07D403/02

    CPC分类号： C07D401/14 ,  C07D249/06 ,  C07D271/04 ,  C07D401/04 ,  C07D417/04

    摘要： The present invention relates to a compound represented by the formula (I): or a pharmaceutically acceptable salt thereof, wherein: R1 is a linear or branched alkoxy group, a cycloalkoxy group, a linear or branched lower alkyl group, etc.; R2 is halogen atom, a lower alkyl group, etc.; Q1 is carbon atom or nitrogen atom; Q2 is carbon atom which may be substituted with oxo group; the formula (III):   (II) is a single bond or a double bond; A is a group selected from the group consisting of the substitutent group α; and R5 is hydrogen atom, a lower alkyl group, cyano group, an alkoxy group or a trialkylsilyl group; having an mGluR1 inhibiting action and being useful as treatment and/or prevention of convulsion, acute pain, cerebral disturbance such as cerebral infarction or transient cerebral ischemia onset, anxiety, chemical dependency or Parkinson's disease.

    摘要翻译： 本发明涉及由式（I）表示的化合物或其药学上可接受的盐，其中：R 1是直链或支链烷氧基，环烷氧基，直链或支链低级 烷基等; R 2是卤素原子，低级烷基等; Q 1是碳原子或氮原子; Q 2是可以被氧代基取代的碳原子; 公式（III）：<？in-line-formula description =“In-line Formulas”end =“lead”？> （II）<？in-line-formula description =”In-line 公式“end =”tail“？>是单键或双键; A是选自由取代基组α组成的组的组; R 5是氢原子，低级烷基，氰基，烷氧基或三烷基甲硅烷基; 具有mGluR1抑制作用，并且可用作治疗和/或预防惊厥，急性疼痛，脑梗塞如脑梗死或暂时性脑缺血发作，焦虑，化学依赖或帕金森病。

    Substituted imidazolidinone derivatives
    4.
    发明授权
    Substituted imidazolidinone derivatives 失效
    取代的咪唑啉酮衍生物

    公开(公告)号：US06699880B1

    公开(公告)日：2004-03-02

    申请号：US10110638

    申请日：2002-04-15

    申请人： Takeru Yamakawa ,  Makoto Ando ,  Seita Koito ,  Kenji Ohwaki ,  Toshifumi Kimura ,  Toshihiko Saeki ,  Mitsuru Miyaji ,  Yuki Iwahori ,  Toru Fujikawa ,  Norikazu Otake ,  Kazuhito Noguchi

    发明人： Takeru Yamakawa ,  Makoto Ando ,  Seita Koito ,  Kenji Ohwaki ,  Toshifumi Kimura ,  Toshihiko Saeki ,  Mitsuru Miyaji ,  Yuki Iwahori ,  Toru Fujikawa ,  Norikazu Otake ,  Kazuhito Noguchi

    IPC分类号： A61K31445

    CPC分类号： C07D401/14

    摘要： This invention relates to the compounds represented by the general formula [I], [in which A—D signify optionally substituted methine group(s) or nitrogen atom; E signifies oxygen or sulfur atom; signify optionally substituted mono- or bi-cyclic aliphatic nitrogen-containing heterocyclic group(s); R1 signifies lower alkenyl, lower alkynyl, cyclo(lower alkyl), lower alkanoyl, lower alkoxycarbonyl, optionally substituted lower alkyl and the like; and R2 signifies lower alkyl]. The compounds of the present invention exhibit an action to stimulate muscarinic acetylcholine receptors M4, and are useful as analgesic for diseases accompanying pain such as cancerous pain, migraine, gout, chronic rheumatism, chronic pain or neuralgia; or as agents for treating tolerance to narcotic analgesics represented by morphine, dependence on narcotic analgesics represented by morphine, itching, dementia, irritable bowel syndrome, schizophrenia, glaucoma, pollakiuria, urinary incontinence, cholelithiasis, cholecystitis, functional dyspepsia and reflux esophagitis.

    摘要翻译： 本发明涉及由通式[I]表示的化合物，其中A-D表示任选取代的次甲基或氮原子; E表示氧或硫原子;表示任选取代的单环或双环脂族含氮杂环基; R 1表示低级烯基，低级炔基，环（低级烷基），低级烷酰基，低级烷氧基羰基，任意取代的低级烷基等; 本发明化合物表现出刺激毒蕈碱性乙酰胆碱受体M4的作用，可作为镇痛药用于伴随疼痛的疾病，例如癌性疼痛，偏头痛，痛风，慢性风湿病，慢性疼痛或慢性疼痛。 神经痛; 或作为治疗由吗啡代表的麻醉止痛药的耐受性的药剂，以吗啡，瘙痒，痴呆，肠易激综合征，精神分裂症，青光眼，尿频尿症，尿失禁，胆石病，胆囊炎，功能性消化不良和反流性食管炎为代表的麻醉止痛药的依赖。

    Benzimidazolone derivatives
    8.
    发明授权
    Benzimidazolone derivatives 失效
    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。

    Amide derivatives
    9.
    发明授权
    Amide derivatives 失效
    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。

    Amide derivatives
    10.
    发明授权
    Amide derivatives 失效
    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。