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1. 发明授权

US06214873B1 2-aminopropane-1,3-diol compounds, medicinal use thereof, and intermediates in synthesizing the same 有权
标题翻译： 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. 再颁专利

USRE39072E1 2-aminopropane-1,3-diol compounds, medicinal use thereof, and intermediates in synthesizing the same 有权
标题翻译： 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

3. 发明授权

US06455528B1 Piperazine compounds and medicinal use thereof 失效
标题翻译：哌嗪类化合物及其医药用途
公开(公告)号：US06455528B1
公开(公告)日：2002-09-24
申请号：US09529491
申请日：2000-04-14
申请人： Kunitomo Adachi , Yoshiyuki Aoki , Tokushi Hanano , Hiroshi Morimoto , Masao Hisadome
发明人： Kunitomo Adachi , Yoshiyuki Aoki , Tokushi Hanano , Hiroshi Morimoto , Masao Hisadome
IPC分类号： A61K31506
CPC分类号： C07D239/42 , C07C2601/02 , C07D213/74 , C07D233/88 , C07D239/47 , C07D239/48 , C07D239/50 , C07D239/52 , C07D239/545 , C07D277/42 , C07D295/135
摘要： The present invention relates to a piperazine compound of the formula wherein R1 and R2 are each hydrogen, halogen, lower alkyl, lower alkoxy, amino, substituted amino, nitro, hydroxy or cyano, R3, R4 and R5 are each hydrogen, halogen, lower alkyl, lower alkoxy, nitro, amino, substituted amino or hydroxy, R6 and R7 are each hydrogen, lower alkyl, lower alkyl substituted by halogen, aralkyl, acyl or lower acyl substituted by halogen, R8 and R9 are each hydrogen or lower alkyl, Y is lower alkylene and the like, and ring A is phenyl, pyrimidyl, thiazolyl, pyridyl, pyrazyl or imidazolyl, a pharmaceutically acceptable salt thereof and pharmaceutical agents containing these compounds. The compound of the present invention has superior TNF-&agr; production inhibitory effect and/or IL-10 production promoting effect, and, since it is free of or shows only strikingly reduced expression of an effect on the central nervous system, the compound is useful as a highly safe and superior TNF-&agr; production inhibitor an/or IL-10 production promoter and is useful as an agent for the prophylaxis or treatment of various diseases caused by abnormal TNF-&agr; production, diseases curable with IL-10, such as chronic inflammatory diseases, acute inflammatory diseases, inflammatory diseases due to infection, autoimmune diseases, allergic diseases, and TNF-&agr; mediated diseases.
摘要翻译：本发明涉及式R 1和R 2的哌嗪化合物各自为氢，卤素，低级烷基，低级烷氧基，氨基，取代的氨基，硝基，羟基或氰基，R 3，R 4和R 5各自为氢，卤素，低级烷基，低级烷氧基，硝基，氨基，取代的氨基或羟基，R6和R7各自为氢，低级烷基，被卤素取代的低级烷基，芳烷基，酰基或被卤素取代的低级酰基，R8和R9分别为氢或低级烷基，Y 是低级亚烷基等，环A是苯基，嘧啶基，噻唑基，吡啶基，吡唑基或咪唑基，其药学上可接受的盐和含有这些化合物的药物。本发明的化合物具有优异的TNF-α产生抑制作用和/或IL-10产生促进作用，并且由于其没有或显示出仅显着降低对中枢神经系统的作用的表达，所以该化合物是有用的作为高度安全和优越的TNF-α产生抑制剂和/或IL-10产生促进剂，并且可用作预防或治疗由异常TNF-α产生引起的各种疾病的药剂，可用IL-10固化的疾病，例如慢性炎性疾病，急性炎性疾病，感染引起的炎性疾病，自身免疫疾病，过敏性疾病和TNF-α介导的疾病。

4. 发明申请

US20060167014A1 Piperazine compounds and medicinal use thereof 审中-公开
标题翻译：哌嗪类化合物及其医药用途
公开(公告)号：US20060167014A1
公开(公告)日：2006-07-27
申请号：US11298980
申请日：2005-12-12
申请人： Kunitomo Adachi , Yoshiyuki Aoki , Tokushi Hanano , Hiroshi Morimoto , Masao Hisadome
发明人： Kunitomo Adachi , Yoshiyuki Aoki , Tokushi Hanano , Hiroshi Morimoto , Masao Hisadome
IPC分类号： A61K31/495 , C07D241/04
CPC分类号： C07D239/42 , C07C2601/02 , C07D213/74 , C07D233/88 , C07D239/47 , C07D239/48 , C07D239/50 , C07D239/52 , C07D239/545 , C07D277/42 , C07D295/135
摘要： The present invention relates to a piperazine compound of the formula wherein R1 and R2 are each hydrogen, halogen, lower alkyl, lower alkoxy, amino, substituted amino, nitro, hydroxy or cyano, R3, R4 and R5 are each hydrogen, halogen, lower alkyl, lower alkoxy, nitro, amino, substituted amino or hydroxy, R6 and R7 are each hydrogen, lower alkyl, lower alkyl substituted by halogen, aralkyl, acyl or lower acyl substituted by halogen, R8 and R9 are each hydrogen or lower alkyl, Y is lower alkylene and the like, and ring A is phenyl, pyrimidyl, thiazolyl, pyridyl, pyrazyl or imidazolyl, a pharmaceutically acceptable salt thereof and pharmaceutical agents containing these compounds. The compound of the present invention has superior TNF-α production inhibitory effect and/or IL-10 production promoting effect, and, since it is free of or shows only strikingly reduced expression of an effect on the central nervous system, the compound is useful as a highly safe and superior TNF-α production inhibitor an/or IL-10 production promoter and is useful as an agent for the prophylaxis or treatment of various diseases caused by abnormal TNF-α production, diseases curable with IL-10, such as chronic inflammatory diseases, acute inflammatory diseases, inflammatory diseases due to infection, autoimmune diseases, allergic diseases, and TNF-α mediated diseases.
摘要翻译：本发明涉及下式的哌嗪化合物其中R 1和R 2各自为氢，卤素，低级烷基，低级烷氧基，氨基，取代的氨基，硝基，羟基或氰基，R 3，R 4和R 5各自为氢，卤素，低级烷基，低级烷氧基，硝基，氨基，取代的氨基或羟基，R 6和R 7各自为氢，低级烷基，被卤素取代的低级烷基，芳烷基，酰基或被卤素取代的低级酰基， 8和R 9各自为氢或低级烷基，Y为低级亚烷基等，环A为苯基，嘧啶基，噻唑基，吡啶基，吡唑基或咪唑基，其药学上可接受的盐和含有这些化合物的药剂。本发明的化合物具有优异的TNF-α产生抑制作用和/或IL-10产生促进作用，并且由于其没有或显示出仅显着降低对中枢神经系统的作用的表达，所以该化合物是有用的作为高度安全和优越的TNF-α产生抑制剂和/或IL-10产生促进剂，并且可用作预防或治疗由异常TNF-α产生引起的各种疾病的药剂，可用IL-10固化的疾病，例如慢性炎性疾病，急性炎性疾病，感染引起的炎性疾病，自身免疫疾病，过敏性疾病和TNF-α介导的疾病。

5. 发明授权

US06372800B1 Benzene compound and pharmaceutical use thereof 有权
标题翻译：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。

6. 发明授权

US06187821B1 Benzene compound and pharmaceutical use thereof 有权
标题翻译：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。

7. 发明授权

US5948820A Benzene compound and pharmaceutical use thereof 失效
标题翻译：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。

8. 发明授权

US5719176A 2-amino-1,3-propanediol compound and immunosuppressant 失效
标题翻译： 2-氨基-1,3-丙二醇化合物和免疫抑制剂
公开(公告)号：US5719176A
公开(公告)日：1998-02-17
申请号：US725890
申请日：1996-10-02
申请人： Tetsuro Fujita , Shigeo Sasaki , Masahiko Yoneta , Tadashi Mishina , Kunitomo Adachi , Kenji Chiba
发明人： Tetsuro Fujita , Shigeo Sasaki , Masahiko Yoneta , Tadashi Mishina , Kunitomo Adachi , Kenji Chiba
IPC分类号： A01N33/02 , A01N43/40 , A01N43/60 , A01N57/00 , C07C215/10 , C07C215/18 , C07C215/20 , C07C215/24 , C07C215/26 , C07C215/28 , C07C215/34 , C07C215/42 , C07C215/54 , C07C215/56 , C07C215/68 , C07C217/28 , C07C217/30 , C07C217/34 , C07C217/48 , C07C217/52 , C07C217/64 , C07C217/72 , C07C217/76 , C07C219/06 , C07C219/24 , C07C219/30 , C07C225/04 , C07C225/06 , C07C225/10 , C07C225/14 , C07C225/16 , C07C229/22 , C07C229/38 , C07C229/46 , C07C233/18 , C07C233/31 , C07C233/35 , C07C233/36 , C07C233/41 , C07C233/43 , C07C233/47 , C07C237/06 , C07C237/24 , C07C237/30 , C07C251/38 , C07C271/20 , C07C271/24 , C07C271/28 , C07C323/25 , C07C323/30 , C07C323/32 , C07C323/34 , C07C323/41 , C07D207/06 , C07D207/09 , C07D207/32 , C07D207/325 , C07D207/335 , C07D211/14 , C07D211/26 , C07D213/38 , C07D213/40 , C07D233/54 , C07D237/08 , C07D239/26 , C07D241/12 , C07D261/08 , C07D263/32 , C07D265/30 , C07D275/02 , C07D277/28 , C07D279/12 , C07D295/13 , C07D295/135 , C07D307/52 , C07D309/32 , C07D317/28 , C07D333/20 , C07D521/00 , C07C711/00
CPC分类号： C07D207/325 , C07C215/10 , C07C215/18 , C07C215/20 , C07C215/24 , C07C215/26 , C07C215/28 , C07C215/34 , C07C215/42 , C07C215/54 , C07C215/56 , C07C215/68 , C07C217/28 , C07C217/30 , C07C217/34 , C07C217/48 , C07C217/52 , C07C217/64 , C07C217/72 , C07C217/76 , C07C219/06 , C07C219/24 , C07C219/30 , C07C225/04 , C07C225/06 , C07C225/10 , C07C225/14 , C07C225/16 , C07C229/22 , C07C229/38 , C07C229/46 , C07C233/18 , C07C233/31 , C07C233/35 , C07C233/36 , C07C233/41 , C07C233/43 , C07C233/47 , C07C237/06 , C07C237/24 , C07C237/30 , C07C251/38 , C07C271/20 , C07C271/24 , C07C271/28 , C07C323/25 , C07C323/30 , C07C323/32 , C07C323/34 , C07C323/41 , C07D207/06 , C07D207/09 , C07D207/335 , C07D211/14 , C07D211/26 , C07D213/38 , C07D213/40 , C07D231/12 , C07D233/56 , C07D233/64 , C07D237/08 , C07D239/26 , C07D241/12 , C07D249/08 , C07D261/08 , C07D263/32 , C07D265/30 , C07D275/02 , C07D277/28 , C07D279/12 , C07D295/13 , C07D295/135 , C07D307/52 , C07D309/32 , C07D317/28 , C07D333/20 , C07C2101/08 , C07C2101/14
摘要： A 2-amino-1,3-propanediol compound represented by general formula (I) or a pharmaceutically acceptable salt thereof, and an immunosuppressant containing the same as the active ingredient. In said formula R represents optionally substituted linear or branched carbon chain, optionally substituted aryl or optionally substituted cycloalkyl; and R.sup.2, R.sup.3, R.sup.4 and R.sup.5, which may be the same or different from one another, represent each hydrogen, alkyl, aralkyl, acyl or alkoxycarbonyl. The compound is immunodepressant and useful as an inhibitor against rejection in organ or bone marrow transplantation, as a preventive or remedy for autoimmune diseases and so forth, or a reagent in the medical and pharmaceutical fields. ##STR1##
摘要翻译：由通式（I）表示的2-氨基-1,3-丙二醇化合物或其药学上可接受的盐，和含有该活性成分的免疫抑制剂。在所述式中，R代表任选取代的直链或支链碳链，任选取代的芳基或任选取代的环烷基; 可以相同或不同的R 2，R 3，R 4和R 5表示氢，烷基，芳烷基，酰基或烷氧基羰基。该化合物是免疫抑制剂，可用作作为器官或骨髓移植排斥反应的抑制剂，作为自身免疫疾病等的预防或补救剂，或医药领域的试剂。（一）

9. 发明授权

US5952316A 2-amino-1,3-propanediol compound and immunosuppressant 失效
标题翻译： 2-氨基-1,3-丙二醇化合物和免疫抑制剂
公开(公告)号：US5952316A
公开(公告)日：1999-09-14
申请号：US911602
申请日：1997-08-14
申请人： Tetsuro Fujita , Shigeo Sasaki , Masahiko Yoneta , Tadashi Mishina , Kunitomo Adachi , Kenji Chiba
发明人： Tetsuro Fujita , Shigeo Sasaki , Masahiko Yoneta , Tadashi Mishina , Kunitomo Adachi , Kenji Chiba
IPC分类号： A01N33/02 , A01N43/40 , A01N43/60 , A01N57/00 , C07C215/10 , C07C215/18 , C07C215/20 , C07C215/24 , C07C215/26 , C07C215/28 , C07C215/34 , C07C215/42 , C07C215/54 , C07C215/56 , C07C215/68 , C07C217/28 , C07C217/30 , C07C217/34 , C07C217/48 , C07C217/52 , C07C217/64 , C07C217/72 , C07C217/76 , C07C219/06 , C07C219/24 , C07C219/30 , C07C225/04 , C07C225/06 , C07C225/10 , C07C225/14 , C07C225/16 , C07C229/22 , C07C229/38 , C07C229/46 , C07C233/18 , C07C233/31 , C07C233/35 , C07C233/36 , C07C233/41 , C07C233/43 , C07C233/47 , C07C237/06 , C07C237/24 , C07C237/30 , C07C251/38 , C07C271/20 , C07C271/24 , C07C271/28 , C07C323/25 , C07C323/30 , C07C323/32 , C07C323/34 , C07C323/41 , C07D207/06 , C07D207/09 , C07D207/32 , C07D207/325 , C07D207/335 , C07D211/14 , C07D211/26 , C07D213/38 , C07D213/40 , C07D233/54 , C07D237/08 , C07D239/26 , C07D241/12 , C07D261/08 , C07D263/32 , C07D265/30 , C07D275/02 , C07D277/28 , C07D279/12 , C07D295/13 , C07D295/135 , C07D307/52 , C07D309/32 , C07D317/28 , C07D333/20 , C07D521/00 , C07P211/00 , C07P401/00
CPC分类号： C07D207/325 , C07C215/10 , C07C215/18 , C07C215/20 , C07C215/24 , C07C215/26 , C07C215/28 , C07C215/34 , C07C215/42 , C07C215/54 , C07C215/56 , C07C215/68 , C07C217/28 , C07C217/30 , C07C217/34 , C07C217/48 , C07C217/52 , C07C217/64 , C07C217/72 , C07C217/76 , C07C219/06 , C07C219/24 , C07C219/30 , C07C225/04 , C07C225/06 , C07C225/10 , C07C225/14 , C07C225/16 , C07C229/22 , C07C229/38 , C07C229/46 , C07C233/18 , C07C233/31 , C07C233/35 , C07C233/36 , C07C233/41 , C07C233/43 , C07C233/47 , C07C237/06 , C07C237/24 , C07C237/30 , C07C251/38 , C07C271/20 , C07C271/24 , C07C271/28 , C07C323/25 , C07C323/30 , C07C323/32 , C07C323/34 , C07C323/41 , C07D207/06 , C07D207/09 , C07D207/335 , C07D211/14 , C07D211/26 , C07D213/38 , C07D213/40 , C07D231/12 , C07D233/56 , C07D233/64 , C07D237/08 , C07D239/26 , C07D241/12 , C07D249/08 , C07D261/08 , C07D263/32 , C07D265/30 , C07D275/02 , C07D277/28 , C07D279/12 , C07D295/13 , C07D295/135 , C07D307/52 , C07D309/32 , C07D317/28 , C07D333/20 , C07C2101/08 , C07C2101/14
摘要： 2-Amino-1,3-propanediol compounds of the formula (I) ##STR1## wherein R is an optionally substituted straight- or branched carbon chain, an optionally substituted aryl, an optionally substituted cycloalkyl or the like, and R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are the same or different and each is a hydrogen, an alkyl, an aralkyl, an acyl or an alkoxycarbonyl, pharmaceutically acceptable salts thereof and immunosuppressants comprising these compounds as active ingredients.The 2-amino-1,3-propanediol compounds of the present invention show immunosuppressive action and are useful for suppressing rejection in organ or bone marrow tranplantation, prevention and treatment of autoimmune diseases or as reagents for use in medicinal and pharmaceutical fields.
摘要翻译：式（I）的2-氨基-1,3-丙二醇化合物，其中R是任选取代的直链或支链碳链，任选取代的芳基，任选取代的环烷基等，以及R 2，R 3，R 4和R 5 各自为氢，烷基，芳烷基，酰基或烷氧基羰基，其药学上可接受的盐和包含这些化合物作为活性成分的免疫抑制剂。本发明的2-氨基-1,3-丙二醇化合物显示免疫抑制作用，可用于抑制器官或骨髓移植中的排斥反应，预防和治疗自身免疫性疾病或用作药物和药物领域的试剂。

10. 发明授权

US5604229A 2-amino-1,3-propanediol compound and immunosuppressant 失效
标题翻译： 2-氨基-1,3-丙二醇化合物和免疫抑制剂
公开(公告)号：US5604229A
公开(公告)日：1997-02-18
申请号：US244942
申请日：1994-06-17
申请人： Tetsuro Fujita , Shigeo Sasaki , Masahiko Yoneta , Tadashi Mishina , Kunitomo Adachi , Kenji Chiba
发明人： Tetsuro Fujita , Shigeo Sasaki , Masahiko Yoneta , Tadashi Mishina , Kunitomo Adachi , Kenji Chiba
IPC分类号： A01N33/02 , A01N43/40 , A01N43/60 , A01N57/00 , C07C215/10 , C07C215/18 , C07C215/20 , C07C215/24 , C07C215/26 , C07C215/28 , C07C215/34 , C07C215/42 , C07C215/54 , C07C215/56 , C07C215/68 , C07C217/28 , C07C217/30 , C07C217/34 , C07C217/48 , C07C217/52 , C07C217/64 , C07C217/72 , C07C217/76 , C07C219/06 , C07C219/24 , C07C219/30 , C07C225/04 , C07C225/06 , C07C225/10 , C07C225/14 , C07C225/16 , C07C229/22 , C07C229/38 , C07C229/46 , C07C233/18 , C07C233/31 , C07C233/35 , C07C233/36 , C07C233/41 , C07C233/43 , C07C233/47 , C07C237/06 , C07C237/24 , C07C237/30 , C07C251/38 , C07C271/20 , C07C271/24 , C07C271/28 , C07C323/25 , C07C323/30 , C07C323/32 , C07C323/34 , C07C323/41 , C07D207/06 , C07D207/09 , C07D207/32 , C07D207/325 , C07D207/335 , C07D211/14 , C07D211/26 , C07D213/38 , C07D213/40 , C07D233/54 , C07D237/08 , C07D239/26 , C07D241/12 , C07D261/08 , C07D263/32 , C07D265/30 , C07D275/02 , C07D277/28 , C07D279/12 , C07D295/13 , C07D295/135 , C07D307/52 , C07D309/32 , C07D317/28 , C07D333/20 , C07D521/00 , C07C211/00
CPC分类号： C07D207/325 , C07C215/10 , C07C215/18 , C07C215/20 , C07C215/24 , C07C215/26 , C07C215/28 , C07C215/34 , C07C215/42 , C07C215/54 , C07C215/56 , C07C215/68 , C07C217/28 , C07C217/30 , C07C217/34 , C07C217/48 , C07C217/52 , C07C217/64 , C07C217/72 , C07C217/76 , C07C219/06 , C07C219/24 , C07C219/30 , C07C225/04 , C07C225/06 , C07C225/10 , C07C225/14 , C07C225/16 , C07C229/22 , C07C229/38 , C07C229/46 , C07C233/18 , C07C233/31 , C07C233/35 , C07C233/36 , C07C233/41 , C07C233/43 , C07C233/47 , C07C237/06 , C07C237/24 , C07C237/30 , C07C251/38 , C07C271/20 , C07C271/24 , C07C271/28 , C07C323/25 , C07C323/30 , C07C323/32 , C07C323/34 , C07C323/41 , C07D207/06 , C07D207/09 , C07D207/335 , C07D211/14 , C07D211/26 , C07D213/38 , C07D213/40 , C07D231/12 , C07D233/56 , C07D233/64 , C07D237/08 , C07D239/26 , C07D241/12 , C07D249/08 , C07D261/08 , C07D263/32 , C07D265/30 , C07D275/02 , C07D277/28 , C07D279/12 , C07D295/13 , C07D295/135 , C07D307/52 , C07D309/32 , C07D317/28 , C07D333/20 , C07C2101/08 , C07C2101/14
摘要： 2-Amino-1,3-propanediol compounds of the formula (I) ##STR1## wherein R is an optionally substituted straight- or branched carbon chain, an optionally substituted aryl, an optionally substituted cycloalkyl or the like, and R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are the same or different and each is a hydrogen, an alkyl, an aralkyl, an acyl or an alkoxycarbonyl, pharmaceutically acceptable salts thereof and immunosuppressants comprising these compounds as active ingredients.The 2-amino-1,3-propanediol compounds of the present invention show immunosuppressive action and are useful for suppressing rejection in organ or bone marrow tranplantation, prevention and treatment of autoimmune diseases or as reagents for use in medicinal and pharmaceutical fields.
摘要翻译： PCT No.PCT / JP93 / 01515 Sec。 371日期：1994年6月17日 102（e）日期1994年6月17日PCT提交1993年10月18日PCT公布。出版物WO94 / 08943 日期1994年4月28日 - 式（I）的氨基-1,3-丙二醇化合物其中R是任选取代的直链或支链碳链，任选取代的芳基，任选取代的环烷基或 R 2，R 3，R 4和R 5相同或不同，各自为氢，烷基，芳烷基，酰基或烷氧基羰基，其药学上可接受的盐和包含这些化合物作为活性成分的免疫抑制剂。本发明的2-氨基-1,3-丙二醇化合物显示免疫抑制作用，可用于抑制器官或骨髓移植中的排斥反应，预防和治疗自身免疫性疾病或用作药物和药物领域的试剂。

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