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1. 发明专利

JPH04360899A PRODUCTION OF BIOACTIVE PENTAPEPTIDE 失效
公开(公告)号：JPH04360899A
公开(公告)日：1992-12-14
申请号：JP15949291
申请日：1991-06-04
申请人： TANABE SEIYAKU CO
发明人： MATSUMOTO KAZUO , HAYASHI MASAAKI , HIRAMATSU KEN
IPC分类号： C07K1/02 , C07K1/06 , C07K1/113 , C07K5/08 , C07K7/06
摘要： PURPOSE:To obtain the subject peptides having an allergy blocking effect with industrial advantage by condensing L-aspartyl-L-prolyl-L-arginine in which the side chains are protected with an amino-protected L-aspartyl-L-serine and subsequently eliminating the protecting groups. CONSTITUTION:A tripeptide (e.g. N-t-butoxycarbonyl-(beta benzyl-L-aspartyl-L- prolyl-NG-nitro-L-arginine benzyl ester) represented by formula I (R and R are carboxylic group-protecting group; R is guanidino group-protecting group; R is amino-protecting group) is, after removal of the amino-protecting groups from the aspartic acid part thereof, subjected to fragment condensation with an amino-protected type dipeptide (e.g. N-t-butoxycarbonyl-beta-benzyl-L-aspartyl-L- serine) of formula II (R is amino-protecting group; R is carboxyl-protecting group) to obtain a pentapeptide of formula III. The protecting groups are subsequently eliminated, thus obtaining the objective L-aspartyl-L-serin-L-aspartyl-L- prolyl-L-arginine) of formula IV.

2. 发明专利

JPH02262561A 失效
公开(公告)号：JPH02262561A
公开(公告)日：1990-10-25
申请号：JP31394089
申请日：1989-12-01
申请人： TANABE SEIYAKU CO
发明人： MATSUMOTO KAZUO , HAYASHI MASAAKI , NUMANAMI KENICHI , SATO TADASHI , TAKADA ISAO
IPC分类号： C07D233/64 , A61K31/415 , A61K38/00 , A61P37/00 , C07D233/54 , C07D401/12 , C07K1/02 , C07K1/113 , C07K5/02 , C07K5/06 , C07K5/065 , C07K5/08 , C07K5/087
摘要： NEW MATERIAL:The compound of formula I (R is branched alkyl, branched alkyloxy or aryl-substituted lower alkyloxy; R and R are H or lower alkyl; R and R are phenyl-substituted alkyl; R is H or lower alkoxycarbonyl; R is H or lower alkylthio substituted with nitrogen-containing heterocyclic group; X and X are CH, OCH or N; A is lower alkoxycarbonyl, hydroxymethyl, etc.) and its salt. EXAMPLE:N-tert-butoxycarbonyl-L-phenylalanyl-L-phenylalanyl-L-histidine methyl ester. USE:A treating agent and preventive for arthrorheumatism, multiple sclerosis, systemic lupus erythematosus, etc. PREPARATION:The objective compound of formula I can be produced by condensing a compound of formula II, its salt or its reactive derivative with a compound of formula III or its salt.

3. 发明专利

JPH02101065A IMIDAZOLINE DERIVATIVE 失效
公开(公告)号：JPH02101065A
公开(公告)日：1990-04-12
申请号：JP25339188
申请日：1988-10-06
申请人： TANABE SEIYAKU CO
发明人： MATSUMOTO KAZUO , SUZUKI MAMORU , YAMAMOTO KOZO , TAKADA ISAO , IWAZAWA YOSHIRO
IPC分类号： C07D233/06 , A61K31/415 , A61K31/44 , A61K31/4427 , A61P37/00 , C07D233/20 , C07D233/22 , C07D233/54 , C07D233/64 , C07D401/04
摘要： NEW MATERIAL:An imidazoline derivative expressed by formula I (R is halogenophenyl, lower alkylphenyl or pyridyl; X and X are H or lower alkoxy) or salt thereof. EXAMPLE:cis-2-(4-Chlorophenyl)-4,5-diphenylimidazoline. USE:Immune controlling agent useful as remedy and/or preventive for articular rheumatism, multiple sclerosis, systemic lupus erythematosus, rheumatic fever, having low toxicity and exhibiting high safeness as a medicine. PREPARATION:A compound expressed by formula II or salt thereof is condensed with a compound expressed by formula III (R' is lower alkyl) or salt thereof to provide the compound expressed by formula I. Furthermore, the above- mentioned compound or salt thereof activates migration of inflammatory macrophage, especially staying in chronic inflammation site and causing a tissue disorder to cause the macrophage to withdraw from the inflammation site and simultaneously recover a function of lowered suppressor T cell.

4. 发明专利

JPS6111940B2 JPS6111940B2 - 失效
公开(公告)号：JPS6111940B2
公开(公告)日：1986-04-05
申请号：JP7227575
申请日：1975-06-13
申请人： Tanabe Seiyaku Co
发明人： MYOSHI SOJI , MATSUMOTO KAZUO , IWASAKI TAMEO , HORIKAWA HIROSHI
IPC分类号： C25B3/02 , C07C67/00 , C07C231/00 , C07C231/12 , C07C233/47

5. 发明专利

JPS6034951A IMIDAZOLE DRIVATIVE AND ITS PREPARATION 失效
公开(公告)号：JPS6034951A
公开(公告)日：1985-02-22
申请号：JP14667884
申请日：1984-07-13
申请人： TANABE SEIYAKU CO
发明人： MATSUMOTO KAZUO , IWAZAWA YOSHIROU
IPC分类号： C07D233/58 , A61K31/415 , A61P25/04 , A61P29/00 , C07D233/54 , C07D233/64 , C07D263/34 , C07D307/52 , C07D333/00 , C07D333/22 , C07D405/04 , C07D409/04 , C07D409/14 , C07D413/04
摘要： NEW MATERIAL:An imidazole derivative of formula I [R is furyl, thienyl, phenyl, halogenophenyl, lower alkylphenyl, lower alkoxyphenyl; R is thienyl, halogenophenyl, lower alkylphenyl, (trifluoro-lower-alkyl)phenyl; Y is monoflurormethyl, difluoromethyl, trifluoromethyl] or its salt. EXAMPLE:2-(4-Chlorophenyl)-4-phenyl-5-(2-fluoroethyl)imidazole. USE:It has anti-inflammatory, analgesic and antipyretic actions and is used as a drug for treatment of inflammation in organs such as skeleton muscles or joints, e.g., rheumatism, gout, arthritis, and bone fracture. It is low-toxicity and free from side-effects such as formation of peptic ulcers. PREPARATION:A novel compound of formula IV is obtained from a compound of formula II (X is halogen) and another compound of formula III (R is ester residue) and the product is allowed to react with ammonia or the like to give the compound of formula I .

6. 发明专利

JPS59172488A Antilipemic agent 失效
标题翻译：抗生素
公开(公告)号：JPS59172488A
公开(公告)日：1984-09-29
申请号：JP4654683
申请日：1983-03-18
申请人： Tanabe Seiyaku Co Ltd
发明人： MATSUMOTO KAZUO , TAKASHIMA KOUKI
IPC分类号： C07D413/04 , A61K31/42 , A61P3/06 , A61P7/02
摘要： PURPOSE: An antilipemic agent, containing a specific furyloxazolylacetic acid derivative as an active constituent, and having reducing action on blood serum cholesterol and blood serum triglyceride and further inhibitory action on blood platelet agglutination without side effects, e.g. hepatic function disorder, etc.
CONSTITUTION: An antilipemic agent containing a furyloxazolylacetic acid derivative (salt) of formula I [R
1 is 1W6C alkyl, 5W6C cycloalkyl or (substituted) phenyl; R
2 is H or 1W12C alkyl] as an active constituent. The compound of formula I (group R
2 is R
3 ) can be prepared by cyclizing a 3-acylaminopropionic acid derivative of formula II (R
3 is 1W12C alkyl) through dehydration. The antilipemic agent is administered usually in 1W20mg/kg/day dose.
COPYRIGHT: (C)1984,JPO&Japio
摘要翻译：目的：含有特定的呋喃并唑基乙酸衍生物作为活性成分的抗疲劳剂，对血清胆固醇和血清甘油三酸酯具有降低作用，并且对血小板凝集的进一步抑制作用无副作用，例如，肝功能障碍等。构成：含有式I的呋喃并唑基乙酸衍生物（盐）的抗血药剂[R 1]为1-6C烷基，5-6C环烷基或（取代）苯基; R 2为H或1-12C烷基]作为活性成分。式I化合物（基团R 2为R 3）可以通过脱水将环状式II的3-酰基氨基丙酸衍生物（R 3为1-12C烷基）环化来制备。抗疲劳剂通常以1-20mg / kg /天的剂量施用。

7. 发明专利

JPS57175156A ALPHA-ISOCYANO-BETA-PHENYLPROPONIC AMIDE DERIVATIVE, ITS PREPARATION AND AGRICULTURAL AND GARDENING FUNGICDE 失效
公开(公告)号：JPS57175156A
公开(公告)日：1982-10-28
申请号：JP5883681
申请日：1981-04-17
申请人： TANABE SEIYAKU CO
发明人： YONEDA NAOTO , MATSUMOTO KAZUO , TAKIGUCHI KAZUO , YAMADA KUNIHIKO
IPC分类号： C07C241/00 , A01N47/40 , C07C67/00 , C07C291/10 , C07D295/16
摘要： NEW MATERIAL:A compound shown by the formulaI(R is H, alkyl; R is cycloalkyl; or R and R are linked to N to form pyrrolidino, piperidino, morpholino; ring A is phenyl, or phenyl having 1-3 substituent groups selected from alkyl, alkoxy, halogen, and nitro). EXAMPLE:alpha-Isocyano-beta-phenylpropionic acid cyclohexyl amide. USE:An agricultural and gardening fungicide. Having improved activity against powdery milder of cucumbers and leaf mold of tomatoes. PROCESS:An alpha-isocyano-beta-phenylpropionic acid compound shown by the formula II (Y is ester residue, alkali metal atom) is condensed with an amine shown by the formula III in a solvent such as methanol, benzene, etc. at 0-100 deg.C, to give a compound shown by the formulaI.

8. 发明专利

JPS5470285A PRODUCTION OF 44HYDROXYISOCARBOSTYRYLL33CARBOXYLIC ANALOG 失效
公开(公告)号：JPS5470285A
公开(公告)日：1979-06-05
申请号：JP13703577
申请日：1977-11-14
申请人： TANABE SEIYAKU CO
发明人： MIYOSHI SOUJI , YONEDA NAOTO , MATSUMOTO KAZUO , SUZUKI MAMORU , NUMANAMI KENICHI
IPC分类号： C07D217/26
摘要： PURPOSE:The reaction product from phthalic anhydride and an alpha-isocyanoacetate ester is, directly or after hydrolysis with an alkali, hydrolyzed with an acid to produce through simple processes title compound useful as an intermediate for synthesizing medicines and agricultural chemicals. CONSTITUTION:The reaction between phthalic anhydride of formula II and an alpha- isocyanoacetic ester of formula III in a solvent such as tetrahydrofuran or dioxane is conducted in the presence of a base such as 1,8-diazabicyclo (5,4,0)undecene-7 to form 5-(2-caroxyphenyl)oxazol-4-carboxylic ester of formula IV. Then the ester is hydrolyzed with an acid such as hydrochloric or hydrobromic acid to afford the objective compound of formula I. Or the compound of formula IV is hydrolyzed with an alkali such as KOH, NaOH with subsequent hydrolysis using an acid to form the objective compound of formual I-B.

9. 发明专利

JPS5365876A PYRROLE DERIVS* AND PROCESS FOR THEIR PREPARATION 失效
公开(公告)号：JPS5365876A
公开(公告)日：1978-06-12
申请号：JP14259076
申请日：1976-11-26
申请人： TANABE SEIYAKU CO
发明人： MIYOSHI SOUJI , YONEDA NAOTO , MATSUMOTO KAZUO , SUZUKI MAMORU , SAKAI KAZUO
IPC分类号： A61K31/40 , A61P25/04 , A61P29/00 , C07D207/32
摘要： PURPOSE:Pyrrole derivs. of formula I (NR R is dialkylamino or heteromonocyclic amino at the 2-, 3-or 4-position of the benzene ring), e.g. 3-(4dimethylaminophenyl) pyrrole.

10. 发明专利

JPS5353617A AAISOCYANO FATTY ACID AMIDE DERIVATIVES AND PROCESS FOR PREPARATION OF THESAME 失效
公开(公告)号：JPS5353617A
公开(公告)日：1978-05-16
申请号：JP12750576
申请日：1976-10-23
申请人： TANABE SEIYAKU CO
发明人： MIYOSHI SOUJI , YONEDA NAOTO , MATSUMOTO KAZUO , SUZUKI MAMORU
IPC分类号： A01N47/40 , A01N37/34 , A01N37/44 , A61K31/495 , A61P29/00 , C07C67/00 , C07C241/00 , C07C291/10 , C07D295/18
摘要： PURPOSE:alpha-Isocyano fatty acid amide derivatives I (one of R and R is H, and the other is alkyl, cycloalkyl, etc.; R and R together with N or O at the terminal position or together with the adjacent N form a heterocyclic ring), e.g. alpha-isocyanoacetic acid-n-propylamide.

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