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4. 发明专利

CA1292344C PEPTIDES AND THERAPEUTIC APPLICATIONS THEREOF 未知
公开(公告)号：CA1292344C
公开(公告)日：1991-11-19
申请号：CA383284
申请日：1981-08-06
申请人： ROQUES BERNARD
发明人： ROQUES BERNARD , LECOMTE JEANNE-MARIE
IPC分类号： C07K14/655 , A61K38/00 , A61P25/00 , C07K7/06 , C07K14/575 , C07K14/67 , C07K14/70 , A61K37/02
摘要： New peptides and therapeutic applications thereof This invention relates to peptide derivatives of the formula: Tyr - A - Gly - B - C - D (I) in which: A is a D.Ala, AzaGly, Aib, D.Ser., D.Thr, D.Cys, homo Serine,.beta.Phe Ser,.beta.OH Leu, 4OH Ile, ? ,.beta.,? OHNor Val or OH Val residue in which the side-chain OH or SH groups, when same exist, may be free or protected (i) by a straight- or branched-chain alkyl containing 1-6 carbon atoms, (ii) by an unsubstituted phenyl radical or a phenyl radical substituted with one or more fluorine atoms, (iii) by an unsubstituted benzyl radical or a benzyl radical substituted with one or more fluorine atoms, (iv) by an aliphatic acyl radical having 1-6 carbon atoms or an acyl radical COX in which X is a phenyl, benzyl or benzhydryl radical, optionally substituted with one or more fluorine atoms, B is a L.Phe, pF.L.Phe or pentafluoro L.Phe residue, C is a Leu, N.Leu or Ile residue of D or L configuration, D is hydrogen or a group of the formula: or in which n = 0, 1 or 2, R is a hydrogen atom or a radical as defined for the protection of group OH of residue A, Y is a hydrogen atom, a group hydroxy, carboxy, carbamoyl, a group OR1, COOR1 or CONHR1 in which R1 represents a radical as defined for the protection of group OH of residue A, a phosphatidylethanolamine chain or a chain in which n is an integer from 0 to 3, R2 is a hydrogen atom or a straight alkyl radical containing 1-4 carbon atoms, and R3 is a hydrogen or oxygen atom or a straight alkyl residue containing 1-4 carbon atoms, and their pharmaceutically acceptable salts. Said compounds are therapeutically useful, typically as analgesic,psychotropic and anti-diarrheic agents.

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