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    2-aminopropane-1,3-diol compounds, medicinal use thereof, and intermediates in synthesizing the same
    1.
    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

    2-aminopropane-1,3-diol compounds, medicinal use thereof, and intermediates in synthesizing the same
    2.
    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

    Benzene compound and pharmaceutical use thereof
    3.
    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。

    Benzene compound and pharmaceutical use thereof
    4.
    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。

    Benzene compound and pharmaceutical use thereof
    5.
    发明授权
    Benzene compound and pharmaceutical use thereof 失效
    苯化合物及其药物用途

    公开(公告)号：US5948820A

    公开(公告)日：1999-09-07

    申请号：US801390

    申请日：1997-02-20

    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： C07C215/28 ,  C07C215/30 ,  C07C215/56 ,  C07C217/64 ,  C07C217/72 ,  C07C219/22 ,  C07C225/16 ,  C07C233/18 ,  C07C233/31 ,  C07C233/36 ,  C07C233/73 ,  C07C271/16 ,  C07C271/18 ,  A61K31/135

    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 ,  C07C2101/02

    摘要： A benzene compound of the formula ##STR1## 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), Beh.cedilla.et's disease, uveal disease, systemic lupus erythematosus, Sjogren'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： 下式的苯化合物其中每个符号如说明书中所定义; 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。 化合物，光学活性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）Beh + 525 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，多发性硬化症， 再生障碍性贫血，特发性血小板减少性紫癜，过敏，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 它也可用作抗真菌剂和毛发生长兴奋剂。

    Hydroformylation of allyl alcohol
    10.
    发明授权
    Hydroformylation of allyl alcohol 失效
    烯丙醇的加氢甲酰化

    公开(公告)号：US5693832A

    公开(公告)日：1997-12-02

    申请号：US266268

    申请日：1994-06-27

    申请人： Tetsuro Fujita ,  Kenichiro Maki ,  Kuniomi Marumo

    发明人： Tetsuro Fujita ,  Kenichiro Maki ,  Kuniomi Marumo

    IPC分类号： C07C45/49 ,  C07D307/20

    CPC分类号： C07D307/20 ,  C07C45/49

    摘要： A process for the hydroformylation of allyl alcohol is disclosed, which comprises reacting allyl alcohol with carbon monoxide and hydrogen in the presence of a rhodium compound and a diphosphine compound represented by formula (I) or (II) ##STR1## wherein R.sup.1 represents an alkyl group or a substituted or unsubstituted aryl group; and R.sup.2 and R.sup.3 each represents an alkyl group or a hydrogen atom.

    摘要翻译： 公开了烯丙醇加氢甲酰化的方法，其包括在铑化合物和由式（I）或（II）表示的二膦化合物存在下使烯丙醇与一氧化碳和氢反应。 >（II）其中R1表示烷基或取代或未取代的芳基; R2和R3各自表示烷基或氢原子。