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1. 发明专利

DE69321823T2 未知
公开(公告)号：DE69321823T2
公开(公告)日：1999-06-02
申请号：DE69321823
申请日：1993-10-18
申请人： YOSHITOMI PHARMACEUTICAL , TAITO CO
发明人： FUJITA TETSURO , SASAKI SHIGEO , YONETA MASAHIKO , MISHINA TADASHI , ADACHI KUNITOMO , CHIBA KENJI
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 , C07C219/04 , A61K31/13 , A61K31/195
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 , R , R and R , 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.

2. 发明专利

DK0627406T3 未知
公开(公告)号：DK0627406T3
公开(公告)日：1999-07-12
申请号：DK93923035
申请日：1993-10-18
申请人： TAITO CO , YOSHITOMI PHARMACEUTICAL
发明人： MISHINA TADASHI , ADACHI KUNITOMO , CHIBA KENJI , FUJITA TETSURO , SASAKI SHIGEO , YONETA MASAHIKO
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 , A61K31/13 , A61K31/195 , C07C219/04
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 , R , R and R , 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.

3. 发明专利

CA2126337A1 2-AMINO-1,3-PROPANEDIOL COMPOUND AND IMMUNOSUPPRESSANT 未知
公开(公告)号：CA2126337A1
公开(公告)日：1994-04-28
申请号：CA2126337
申请日：1993-10-18
申请人： YOSHITOMI PHARMACEUTICAL , TAITO CO
发明人： FUJITA TETSURO , SASAKI SHIGEO , YONETA MASAHIKO , MISHINA TADASHI , ADACHI KUNITOMO , CHIBA KENJI
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 , C07C215/02 , A61K31/13 , C07C317/32 , A61K31/38 , A61K31/44
摘要： 2-Amino-1,3-propanediol compounds of the formula (I) (see formula I) wherein R is an optionally substituted straight- or branched carbon chain, an optionally substituted aryl, an optionally substituted cycloalkyl or the like, and R2, R3, R4 and R5 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.

4. 发明专利

JPH11310556A NOVEL PROCESS FOR PRODUCING 2-AMINO-2-(2-(4OCTYLPHENYL) ETHYL) PROPANE-1,3-DIOL 失效
公开(公告)号：JPH11310556A
公开(公告)日：1999-11-09
申请号：JP11871198
申请日：1998-04-28
申请人： YOSHITOMI PHARMACEUTICAL
发明人： MISHINA TADASHI , OBARA TOSHIYUKI , ADACHI KUNITOMO
IPC分类号： C07C213/00 , C07C215/08 , C07C231/12 , C07C233/31
摘要： PROBLEM TO BE SOLVED: To provide a novel production process for 2-amino-2-[2-(4octylphenyl) ethyl]propane-1,3-diol that is useful as an immunosuppressant agent. SOLUTION: The 2-amino-2-[2-(4-octylphenyl)ethyl]propane-1,3-diol can produced by reacting diethyl acetamidemalonate with a (2-haloethyl)benzene to form 2-acetamide-2-phenyl-ethyl malonate, after reduction, acetyulating it, further introducing an octyanoyl group to give 2-acetamide-2-acetoxymethyl-4-(4 octanoylphenyl)butyl acetate followed by hydrolysis and reduction of the product, as the intermediates in the individual steps can be crystallized and the production steps can be shortened.

5. 发明专利

JPH1180026A NEW IMMUNOSUPPRESSANT, ITS USE AND ITS IDENTIFICATION 失效
公开(公告)号：JPH1180026A
公开(公告)日：1999-03-23
申请号：JP23727397
申请日：1997-09-02
申请人： YOSHITOMI PHARMACEUTICAL
发明人： CHIBA KENJI , ADACHI KUNITOMO
IPC分类号： G01N33/49 , A61K31/13 , A61K31/135 , A61K45/00 , A61P37/06
摘要： PROBLEM TO BE SOLVED: To obtain the subject suppressant which is safely usable with low toxicity, can be used together with usual immunosuppressive compounds without adverse drug reactions and is useful for inhibiting the rejection reaction in transplantation and preventing and treating autoimmune diseases by formulating a specific compound which promotes lymphocyte homing toward mesenteries, peripheral lymph tissues or Peyer patches. SOLUTION: The objective suppressant preferably not inhibiting the production of T-cell interleukin-2 is obtained by particularly formulating 2- aminopropane-1,3-diol, its homolog, analog or derivative, particularly a compound of formula I (R is a carbon chain; R -R are each H, an alkyl, etc.), particularly 2-amino-2[2-(4-octylphenyl)ethyl]propane-1,3-diol hydrochloride, or a benzene compound, its homolog, analog or derivative, particularly a compound of formula II [W, R , X and Y are each H and the like; Z is a single bond and the like; (m) is 1 and 2; (n) is 2 and 3].

6. 发明专利

JPH0276879A CIS-2,6-DIAZABICYCLO(3.3.0)OCTANE DERIVATIVE AND USE APPLICATION THEREOF AS MEDICINE 失效
公开(公告)号：JPH0276879A
公开(公告)日：1990-03-16
申请号：JP13840489
申请日：1989-05-31
申请人： YOSHITOMI PHARMACEUTICAL
发明人： ARITA MASAFUMI , ADACHI KUNITOMO , SAITO TADAMASA , FUKUMASU YOSHITAKA , HAGA KEIICHIRO
IPC分类号： A61K31/40 , A61P1/04 , A61P7/02 , A61P9/00 , A61P25/28 , C07D487/04
摘要： NEW MATERIAL:Compounds of formula I (X is O, S, NH or N; X1 is alkylene or alkenylene where ring is formed together with N in case of X is N; Y is alkylene; Y1 is H, alkyl or alkenyl; Y2 is H, alkyl, alkenyl, alkynyl, aryl, aralkyl, heterocycle, etc.; A is H or OH which may have protecting group) R, R1 and R2 are H or alkyl; Z is O or S). EXAMPLE:7-(3-Methoxycarbonylpropylthio)-2-(3alpha-hydroxyoctyl)-cis-2,6- diazabicyclo[3.3.0]oct-6-en-3-one. USE:An antithrombotic agent. An agent for protection of brain. Especially useful as an antiulcer agent. PREPARATION:For example, a compound of formula II is reacted with a compound of formula III (R7 is group reactive with carbonyl, halogen, alkoxy, etc.) to obtain a compound of formula I where X is S.

7. 发明专利

AT172711T 未知
公开(公告)号：AT172711T
公开(公告)日：1998-11-15
申请号：AT93923035
申请日：1993-10-18
申请人： YOSHITOMI PHARMACEUTICAL
发明人： FUJITA TETSURO , SASAKI SHIGEO , YONETA MASAHIKO , MISHINA TADASHI , ADACHI KUNITOMO , CHIBA KENJI
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 , C07C219/04
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 , R , R and R , 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.

8. 发明公开

EP0778263A4 BENZENE COMPOUND AND MEDICINAL USE THEREOF 失效
标题翻译： BENZOLDERIVATE UND DEREN MEDIZINISCHE VERWENDUNG
公开(公告)号：EP0778263A4
公开(公告)日：1997-10-22
申请号：EP95928630
申请日：1995-08-22
申请人： YOSHITOMI PHARMACEUTICAL
发明人： FUJITA TETSURO , ADACHI KUNITOMO , KOHARA TOSHIYUKI , KIUCHI MASATOSHI , CHIBA KENJI , TESHIMA KOJI , MISHINA TADASHI
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： C07C217/64 , C07C215/28 , C07C215/30 , C07C215/56 , 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 represented by general formula (I) (wherein each symbol is as defined in the specification), an optical isomer or salt thereof, a medicinal composition containing the same, and an immunosuppressant containing the same as the active ingredient. The compound, 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：由通式（I）表示的苯化合物（其中各符号如说明书中所定义），其光学异构体或其盐，含有其的药物组合物和含有其的免疫抑制剂作为活性成分。该化合物，异构体或盐具有优异的免疫抑制作用，并且可用作器官或骨髓移植中发生的排斥反应的抑制剂，并作为关节风湿病，特应性湿疹（皮炎），白塞病，葡萄膜炎，全身性红斑狼疮，干燥综合征，多发性硬化症，重症肌无力，I型糖尿病，内分泌性眼病，原发性胆汁性肝硬化，克罗恩氏病，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，过敏症，多动脉炎结节，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，埃文斯综合征，支气管哮喘和花粉症。它也可用作抗真菌剂和毛发生长刺激剂。

9. 发明专利

DE69321823D1 未知
公开(公告)号：DE69321823D1
公开(公告)日：1998-12-03
申请号：DE69321823
申请日：1993-10-18
申请人： YOSHITOMI PHARMACEUTICAL
发明人： FUJITA TETSURO , SASAKI SHIGEO , YONETA MASAHIKO , MISHINA TADASHI , ADACHI KUNITOMO , CHIBA KENJI
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 , C07C219/04 , A61K31/13 , A61K31/195
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 , R , R and R , 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.

10. 发明专利

CA2198383A1 BENZENE COMPOUND AND PHARMACEUTICAL USE THEREOF 未知
公开(公告)号：CA2198383A1
公开(公告)日：1996-02-29
申请号：CA2198383
申请日：1995-08-22
申请人： YOSHITOMI PHARMACEUTICAL
发明人： FUJITA TETSURO , ADACHI KUNITOMO , KOHARA TOSHIYUKI , KIUCHI MASATOSHI , CHIBA KENJI , TESHIMA KOJI , MISHINA TADASHI
IPC分类号： A61K31/135 , A61K31/16 , A61K31/22 , A61K31/27 , C07C215/28 , C07C217/64 , C07C219/22 , C07C225/16 , C07C233/18 , C07C271/16
摘要： A benzene compound represented by general formula (I) (wherein each symbol is as defined in the specification), an optical isomer or salt thereof, a medicinal composition containing the same, and an immunosuppressant containing the same as the active ingredient. The compound, 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.

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