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    Benzene compound and pharmaceutical use thereof
    2.
    发明授权
    Benzene compound and pharmaceutical use thereof 有权
    苯化合物及其药物用途

    公开(公告)号：US06372800B1

    公开(公告)日：2002-04-16

    申请号：US09691099

    申请日：2000-10-19

    申请人： Tetsuro Fujita ,  Kunitomo Adachi ,  Toshiyuki Kohara ,  Masatoshi Kiuchi ,  Kenji Chiba ,  Koji Teshima ,  Tadashi Mishina

    发明人： Tetsuro Fujita ,  Kunitomo Adachi ,  Toshiyuki Kohara ,  Masatoshi Kiuchi ,  Kenji Chiba ,  Koji Teshima ,  Tadashi Mishina

    IPC分类号： A61K3135

    CPC分类号： C07C215/56 ,  C07C215/28 ,  C07C215/30 ,  C07C217/64 ,  C07C217/72 ,  C07C219/22 ,  C07C225/16 ,  C07C233/18 ,  C07C233/31 ,  C07C233/36 ,  C07C233/73 ,  C07C271/16 ,  C07C271/18 ,  C07C2601/02

    摘要： A benzene compound of the formula wherein each symbol is as defined in the specification; an optically active isomer or salt thereof, a medicinal composition containing the same, and an immunosuppressant containing the same as the active ingredient. The compound, optically active isomer or salt has an excellent immunosuppressive effect and is useful as an inhibitor for the rejection reaction occurring in organ or bone marrow transplantation, and as a preventive or remedy for articular rheumatism, atopic eczema (dermatitis), Behcet's disease, uveal disease, systemic lupus erythematosus, Sjögren's syndrome, multiple sclerosis, myasthenia gravis, type I diabetes, endocrine ophthalmopathy, primary biliary, cirrhosis, Crohn's disease, glomerulonephritis, sarcoidosis, psoriasis, pemphigus, aplastic anemia, idiopathic thrombocytopenic purpura, allergy, polyarteritis nodosa, progressive systemic sclerosis, mixed connective-tissue disease, aortitis syndrome, polymyositis, dermatomyositis, Wegener's granuloma, ulcerative colitis, active chronic hepatitis, autoimmune hemolytic anemia, Evans' syndrome, bronchial asthma and pollinosis. It is useful also as an antifingal agent and hair growth stimulant.

    摘要翻译： 每个符号的苯甲醛的苯化合物如说明书中所定义; 其光学活性异构体或其盐，含有它们的药用组合物和含有该活性成分的免疫抑制剂。该化合物，旋光异构体或盐具有优异的免疫抑制作用，可用作抑制反应发生的抑制剂 在器官或骨髓移植中，作为关节风湿病，特应性湿疹（皮炎），贝切特氏病，葡萄膜疾病，系统性红斑狼疮，Sjögren综合征，多发性硬化症，重症肌无力，I型糖尿病，内分泌眼病，原发性 胆汁，肝硬化，克罗恩病，肾小球肾炎，结节病，牛皮癣，天疱疮，再生障碍性贫血，特发性血小板减少性紫癜，变态反应，结节性多动脉炎，进行性系统性硬化症，混合性结缔组织病，主动脉炎综合征，多发性肌炎，皮肌炎，韦格纳肉芽肿，溃疡性结肠炎， 活动性慢性肝炎，自身免疫性溶血性贫血， 伊文思综合征，支气管哮喘和花粉症。 它也可用作抗衰老剂和毛发生长兴奋剂。

    2-aminopropane-1,3-diol compounds, medicinal use thereof, and intermediates in synthesizing the same
    4.
    再颁专利
    2-aminopropane-1,3-diol compounds, medicinal use thereof, and intermediates in synthesizing the same 有权
    2-氨基丙烷-1,3-二醇化合物，其药学用途和合成它们的中间体

    公开(公告)号：USRE39072E1

    公开(公告)日：2006-04-18

    申请号：US10410387

    申请日：1998-04-03

    申请人： Kunitomo Adachi ,  Yoshiyuki Aoki ,  Tokushi Hanano ,  Koji Teshima ,  Yukio Hoshino ,  Tetsuro Fujita

    发明人： Kunitomo Adachi ,  Yoshiyuki Aoki ,  Tokushi Hanano ,  Koji Teshima ,  Yukio Hoshino ,  Tetsuro Fujita

    IPC分类号： A61K31/22

    CPC分类号： C07C225/16 ,  C07C215/34 ,  C07C223/02 ,  C07F7/1804

    摘要： The present invention relates to a compound of the general formula wherein R1, R2, R3 and R4 are each a hydrogen or an acyl, a pharmaceutically acceptable acid addition salt thereof or a hydrate thereof; a pharmaceutical comprising this compound; a pharmaceutical composition comprising this compound and a pharmaceutically acceptable carrier; and 2-amino-2-(2-(4-(1-hydroxy-5-phenylpentyl)phenyl)ethyl)propane-1,3-diol or 2-amino-2-(2-(4-formylphenyl)ethyl)propane-1,3-diol, the derivatives of the two compounds whose amino group and/or hydroxy group are(is) protected or a salt thereof. The compound of the present invention shows superior immunosuppressive action with less toxicity and higher safety, and is useful as a drug for prevention or suppression of rejection of organs or bone marrow transplantation, or as a drug for prevention or treatment of various autoimmune diseases or allergic diseases.

    摘要翻译： 本发明涉及以下通式的化合物：其中R 1，R 2，R 3和R 4， 各自为氢或酰基，其药学上可接受的酸加成盐或其水合物; 包含该化合物的药物; 包含该化合物和药学上可接受的载体的药物组合物; 和2-氨基-2-（2-（4-（1-羟基-5-苯基戊基）苯基）乙基）丙烷-1,3-二醇或2-氨基-2-（2-（4-甲酰基苯基）乙基） 丙烷-1,3-二醇，其氨基和/或羟基被保护的两种化合物的衍生物或其盐。 本发明的化合物显示出较好的免疫抑制作用，毒性小，安全性更高，可用作预防或抑制器官​​排斥或骨髓移植的药物，或作为预防或治疗各种自身免疫性疾病或过敏性疾病的药物 疾病

    Remedy for sleep disturbance
    5.
    发明申请
    Remedy for sleep disturbance 失效
    解决睡眠障碍

    公开(公告)号：US20050119308A1

    公开(公告)日：2005-06-02

    申请号：US10508339

    申请日：2003-03-28

    申请人： Koji Teshima ,  Masanori Minoguchi

    发明人： Koji Teshima ,  Masanori Minoguchi

    IPC分类号： A61K31/00 ,  A61K31/454 ,  A61K31/527 ,  A61P25/20 ,  C07D401/04 ,  C07D43/04

    CPC分类号： C07D401/04 ,  A61K31/00 ,  A61K31/454 ,  A61K31/527

    摘要： The present invention has been made based on the finding that a compound acting on the ORL-1 receptor as an agonist acts as a non-photic entrainment factor, and advances the circadian rhythm phase, and provides a novel therapeutic agent for a sleep disorder such as circadian rhythm sleep disorder, more particularly, an agent for the prophylaxis and/or treatment of a sleep disorder, which contains an ORL-1 receptor agonist, and a novel compound useful as such agent for the prophylaxis and/or treatment.

    摘要翻译： 本发明是基于以作为激动剂作用于ORL-1受体的化合物作为非光学夹带因子的化合物的发现而进行的，并且促进了昼夜节律期，并且提供了一种用于睡眠障碍的新型治疗剂， 作为昼夜节律睡眠障碍，更具体地，涉及含有ORL-1受体激动剂的睡眠障碍的预防和/或治疗药物，以及可用作预防和/或治疗剂的新型化合物。

    Agent for prophylaxis or treatment of alcohol dependence or drug dependence
    7.
    发明授权
    Agent for prophylaxis or treatment of alcohol dependence or drug dependence 失效
    用于预防或治疗酒精依赖或药物依赖的药剂

    公开(公告)号：US08207201B2

    公开(公告)日：2012-06-26

    申请号：US12311861

    申请日：2007-10-16

    申请人： Koji Teshima ,  Roberto Ciccocioppo ,  Maurizio Massi

    发明人： Koji Teshima ,  Roberto Ciccocioppo ,  Maurizio Massi

    IPC分类号： A61K31/454

    CPC分类号： A61K31/454

    摘要： The present invention provides an agent for the prophylaxis or treatment of substance abuse and dependence, which contains a compound of the formula (I) represented by (R)-2-{3-[1-(acenaphthen-1-yl)piperidin-4-yl]-2,3-dihydro-2-oxo-benzimidazol-1-yl}-N-methylacetamide, or a pharmaceutically acceptable salt thereof as an active ingredient.

    摘要翻译： 本发明提供了用于预防或治疗药物滥用和依赖性的药剂，其包含由（R）-2- {3- [1-（苊-1-基）哌啶-4-基] 吡啶-4-基] -2,3-二氢-2-氧代 - 苯并咪唑-1-基} -N-甲基乙酰胺或其药学上可接受的盐作为活性成分。

    Remedy for sleep disturbance
    8.
    发明授权
    Remedy for sleep disturbance 失效
    解决睡眠障碍

    公开(公告)号：US08003669B2

    公开(公告)日：2011-08-23

    申请号：US12453057

    申请日：2009-04-28

    申请人： Koji Teshima ,  Masanori Minoguchi

    发明人： Koji Teshima ,  Masanori Minoguchi

    IPC分类号： A61K31/454

    CPC分类号： C07D401/04 ,  A61K31/00 ,  A61K31/454 ,  A61K31/527

    摘要： The present invention has been made based on the finding that a compound acting on the ORL-1 receptor as an agonist acts as a non-photic entrainment factor, and advances the circadian rhythm phase, and provides a novel therapeutic agent for a sleep disorder such as circadian rhythm sleep disorder, more particularly, an agent for the prophylaxis and/or treatment of a sleep disorder, which contains an ORL-1 receptor agonist, and a novel compound useful as such agent for the prophylaxis and/or treatment.

    摘要翻译： 本发明是基于以作为激动剂作用于ORL-1受体的化合物作为非光学夹带因子的化合物的发现而进行的，并且促进了昼夜节律期，并且提供了一种用于睡眠障碍的新型治疗剂， 作为昼夜节律睡眠障碍，更具体地，涉及含有ORL-1受体激动剂的睡眠障碍的预防和/或治疗药物，以及可用作预防和/或治疗剂的新型化合物。

    2-aminopropane-1,3-diol compounds, medicinal use thereof, and intermediates in synthesizing the same
    9.
    发明授权
    2-aminopropane-1,3-diol compounds, medicinal use thereof, and intermediates in synthesizing the same 有权
    2-氨基丙烷-1,3-二醇化合物，其药学用途和合成它们的中间体

    公开(公告)号：US06214873B1

    公开(公告)日：2001-04-10

    申请号：US09402375

    申请日：2000-01-05

    申请人： Kunitomo Adachi ,  Yoshiyuki Aoki ,  Tokushi Hanano ,  Koji Teshima ,  Yukio Hoshino ,  Tetsuro Fujita

    发明人： Kunitomo Adachi ,  Yoshiyuki Aoki ,  Tokushi Hanano ,  Koji Teshima ,  Yukio Hoshino ,  Tetsuro Fujita

    IPC分类号： A61H3122

    CPC分类号： C07C225/16 ,  C07C215/34 ,  C07C223/02 ,  C07F7/1804

    摘要： The present invention relates to a compound of the general formula wherein R1, R2, R3 and R4 are each a hydrogen or an acyl, a pharmaceutically acceptable acid addition salt thereof or a hydrate thereof; a pharmaceutical comprising this compound; a pharmaceutical composition comprising this compound and a pharmaceutically acceptable carrier; and 2-amino-2-(2-(4-(1-hydroxy-5-phenylpentyl)phenyl)ethyl)propane-1,3-diol or 2-amino-2-(2-(4-formylphenyl)ethyl)propane-1,3-diol, the derivatives of the two compounds whose amino group and/or hydroxy group are(is) protected or a salt thereof. The compound of the present invention shows superior immunosuppressive action with less toxicity and higher safety, and is useful as a drug for prevention or suppression of rejection of organs or bone marrow transplantation, or as a drug for prevention or treatment of various autoimmune diseases or allergic diseases.

    摘要翻译： 本发明涉及一般化学式R 1，R 2，R 3和R 4的化合物各自为氢或酰基，其药学上可接受的酸加成盐或其水合物; 包含该化合物的药物; 包含该化合物和药学上可接受的载体的药物组合物; 和2-氨基-2-（2-（4-（1-羟基-5-苯基戊基）苯基）乙基）丙烷-1,3-二醇或2-氨基-2-（2-（4-甲酰基苯基）乙基） 丙烷-1,3-二醇，其氨基和/或羟基被保护的两种化合物的衍生物或其盐。 本发明的化合物显示出较好的免疫抑制作用，毒性小，安全性更高，可用作预防或抑制器官​​排斥或骨髓移植的药物，或作为预防或治疗各种自身免疫性疾病或过敏性疾病的药物 疾病

    Benzene compound and pharmaceutical use thereof
    10.
    发明授权
    Benzene compound and pharmaceutical use thereof 有权
    苯化合物及其药物用途

    公开(公告)号：US06187821B1

    公开(公告)日：2001-02-13

    申请号：US09309818

    申请日：1999-05-12

    申请人： Tetsuro Fujita ,  Kunitomo Adachi ,  Toshiyuki Kohara ,  Masatoshi Kiuchi ,  Kenji Chiba ,  Koji Teshima ,  Tadashi Mishina

    发明人： Tetsuro Fujita ,  Kunitomo Adachi ,  Toshiyuki Kohara ,  Masatoshi Kiuchi ,  Kenji Chiba ,  Koji Teshima ,  Tadashi Mishina

    IPC分类号： A61K31135

    CPC分类号： C07C215/56 ,  C07C215/28 ,  C07C215/30 ,  C07C217/64 ,  C07C217/72 ,  C07C219/22 ,  C07C225/16 ,  C07C233/18 ,  C07C233/31 ,  C07C233/36 ,  C07C233/73 ,  C07C271/16 ,  C07C271/18 ,  C07C2601/02

    摘要： A benzene compound of the formula: wherein each symbol is as defined in the specification; an optically active isomer or salt thereof, a medicinal composition containing the same, and an immunosuppressant containing the same as the active ingredient. The compound, optically active isomer or salt has an excellent immunosuppressive effect and is useful as an inhibitor for the rejection reaction occurring in organ or bone marrow transplantation, and as a preventive or remedy for articular rheumatism, atopic eczema (dermatitis), Behcet's disease, uveal disease, systemic lupus erythematosus, Sjögren's syndrome, multiple sclerosis, myasthenia gravis, type I diabetes, endocrine ophthalmopathy, primary biliary, cirrhosis, Crohn's disease, glomerulonephritis, sarcoidosis, psoriasis, pemphigus, aplastic anemia, idiopathic thrombocytopenic purpura, allergy, polyarteritis nodosa, progressive systemic sclerosis, mixed connective-tissue disease, aortitis syndrome, polymyositis, dermatomyositis, Wegener's granuloma, ulcerative colitis, active chronic hepatitis, autoimmune hemolytic anemia, Evans' syndrome, bronchial asthma and pollinosis. It is useful also as an antifungal agent and hair growth stimulant.

    摘要翻译： 一种下式的苯化合物：其中每个符号如说明书中所定义;光学活性异构体或其盐，含有该化合物的药用组合物和含有该有效成分的免疫抑制剂。化合物，旋光异构体或 盐具有优异的免疫抑制作用，可用作器官或骨髓移植中发生的排斥反应的抑制剂，并且作为关节风湿病，特应性湿疹（皮炎），贝切特氏病，葡萄膜疾病，系统性红斑狼疮， Sjögren综合征，多发性硬化症，重症肌无力，I型糖尿病，内分泌眼病，原发性胆汁性肝硬化，克罗恩病，肾小球性肾炎，结节病，牛皮癣，天疱疮，再生障碍性贫血，特发性血小板减少性紫癜，变态反应，结节性多动脉炎，进行性系统性硬化症 组织病，主动脉炎综合征，多发性肌炎，皮肌炎，威基 r肉芽肿，溃疡性结肠炎，活动性慢性肝炎，自身免疫性溶血性贫血，伊文思综合征，支气管哮喘和花粉症。 它也可用作抗真菌剂和毛发生长兴奋剂。