Peptides and therapeutic applications thereof

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United States of America Patent

PATENT NO 4407794
SERIAL NO

06289383

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ATTORNEY / AGENT: (SPONSORED)

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Abstract

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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, .alpha.,.beta.,.gamma. 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: ##STR1## 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 OR.sub.1, COOR.sub.1 or CONHR.sub.1 in which R.sub.1 represents a radical as defined for the protection of group OH of residue A, a phosphatidylethanolamine chain or a chain ##STR2## in which n is an integer from 0 to 3, R.sub.2 is a hydrogen atom or a straight alkyl radical containing 1-4 carbon atoms, and R.sub.3 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 an analgesic, psychotropic and anti-diarrheic agents.

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Patent Owner(s)

Patent OwnerAddress
CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (CNRS) A FRENCH BODY CORPORATE15 QUAI ANATOLE FRACE PARIS 75700

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Inventor(s)

Inventor Name Address # of filed Patents Total Citations
Lecomte, Jeanne-Marie Paris, FR 65 682
Roques, Bernard Saint Maurice, FR 24 356

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