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Organic compounds

  • US 4,291,022 A
  • Filed: 05/23/1980
  • Issued: 09/22/1981
  • Est. Priority Date: 03/11/1975
  • Status: Expired due to Term
First Claim
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1. A compound of formula I, ##STR53## wherein R1 is (i) H,(ii) NH2,(iii) H--Ala--NH--;

  • H--Tyr--NH--;

    H--Cys--NH--;

    H--Val--NH--;

    H--Lys--NH--;

    H--(α

    -amino-isobutyryl)--NH--;

    H--Phe--NH(iv) NH2 --NH--CO--NH--;

    (v) C6 H5.NH--CO--Gly--NH--;

    H--Ala--Gly--NH--;

    H--Val--Gly--NH--;

    H--α

    --phenyl--Gly--NH--,(vi) R2 --A--CO--NH--, whereinR2 is lower alkyl, phenyl, or phenyl substituted by halogen, hydroxy, amino lower alkyl or lower alkoxy,A is a direct bond, alkylene containing up to 6 carbon atoms or --NH--,(vii) R2 --Ala--NH--;

    R2 --Ala--Gly--NH--;

    wherein R2 is as defined above,(viii) C6 H5.AI.CO--M--NH--, whereinAI is an alkylene chain of up to 6 carbon atoms, and--M-- is --(mono- or di-Hal)--Phe, --Gly-- or --Ala--,(ix) T--(mono- or di-Hal)--Phe--NH, wherein T-- is H--, H--Val-- or benzoyl--,(x) ##STR54## wherein AI is as defined above, and--L-- is --Val--(mono- or di-Hal)-- Phe--α

    --phenyl--Gly--, andn is an integer between 4 and 10,each B is hydrogen or the two radicals B form a direct bond,X is --Lys--, or --Nle--, andY is --Asn--, --Gln-- or --Thr--, andZ signifies the radicals;

    (i) --CO--asparaginol;

    --CO--leucinol;

    --CO--iso-leucinol;

    --CO--valinol;

    --CO--norleucinol;

    --CO--glutaminol;

    --CO--threoninol;

    (ii) --CO--Leu;

    --CO--Ser;

    --CO--Iso--Leu;

    --CO--Val, and their corresponding amides, wherein the amide portion signifies the radical --CO--NR4 R5 (wherein R4 and R5 independently are hydrogen or lower alkyl) or the radical ##STR55## (wherein n is as defined above);

    (iii) --CO--ThrOR3 or --CO--SerOR3 (wherein R3 is lower alkyl);

    or(iv) --CO--NH--(CH2)k --OH (wherein k is an integer between 2 and

         6), or ##STR56## (wherein 11 and 12 independently signify a whole number from 1 to

         6);

    wherein in formula I the unit containing radicals R1, X, Y and Z, as well as in the remaining units of the peptide sequence, at least one unit may be present in D form,with the proviso that when R1 is H--Cys--NH or H--(D)--Cys--NH, B--B is other than a direct bond,or a pharmaceutically acceptable acid addition salt or complex thereof.

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