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PEPTIDE AGONISTS OF GLP-1 ACTIVITY

  • US 20140336356A1
  • Filed: 12/03/2013
  • Published: 11/13/2014
  • Est. Priority Date: 07/12/1999
  • Status: Abandoned Application
First Claim
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1. A peptide conjugate comprising a peptide X selected from the group consisting of (a) an exendin having at least 90% homology to exendin-4;

  • (b) a variant of said exendin wherein said variant comprises a modification selected from the group consisting of between one and five deletions at positions 34-39 and contains a Lys at position 40 having a lipophilic substituent;

    or (c) GLP-1 (7-36) (SEQ ID NO;

         114) or GLP-1 (7-37) (SEQ ID NO;

         123) having at least one modification selected from the group consisting of;

    (i) substitution of D-alanine, glycine or alpha-amino isobutyric acid for alanine at position 8 and (ii) a lipophilic substituent; and

    Z, a peptide sequence of 4-20.amino acid units covalently bound to said variant, wherein each amino acid unit in said peptide sequence, Z is selected from the group consisting of Ala, Leu, Ser, Thr, Tyr, Asn, Gin, Asp, Glu, Lys, Arg, His, Met, Orn, and amino acid units of the general formula I —

    NH—

    C(R1)(R2)—

    C(═

    O)-(1) wherein R1 and R2 are selected from the group consisting of hydrogen, C1-6-alkyl, phenyl, and phenyl-methyl, wherein C1-6-alkyl is optionally substituted with from one to three substituents selected from halogen, hydroxy, amino, cyano, nitro, sulfono, and carboxy, and phenyl and phenyl-methyl is optionally substituted with from one to three substituents selected from C1-6-alkyl, C2-6-alkenyl, halogen, hydroxy, amino, cyano, nitro, sulfono, and carboxy, or R1 and R2 together with the carbon atom to which they are bound form a cyclopentyl, cyclohexyl, or cycloheptyl ring, e.g. 2,4-diaminobutanoic acid and 2,3-diaminopropanoic acid; and

    a pharmaceutically acceptable salt or the c-terminal amide of said peptide conjugate, with the proviso that x is not exendin-4 or exendin-3.

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