HUMAN GLUCAGON-LIKE-PEPTIDE-1 MODULATORS AND THEIR USE IN THE TREATMENT OF DIABETES AND RELATED CONDITIONS
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Abstract
The present invention provides novel human glucagon-like peptide-1 (GLP-1)-receptor modulators that have biological activity similar or superior to native GLP-1 peptide and thus are useful for the treatment or prevention of diseases or disorders associated with GLP activity. Further, the present invention provides novel, chemically modified peptides that not only stimulate insulin secretion in type II diabetics, but also produce other beneficial insulinotropic responses. These synthetic peptide GLP-1 receptor modulators exhibit increased stability to proteolytic cleavage making them ideal therapeutic candidates for oral or parenteral administration. The peptides of this invention show desirable pharmacokinetic properties and desirable potency in efficacy models of diabetes.
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Citations
28 Claims
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1. A compound of Formula VIa:
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2. A compound of Formula VIIa:
- 3. A method for treating or delaying the progression or onset of diabetes, diabetic retinopathy, diabetic neuropathy, diabetic nephropathy, wound healing, insulin resistance, hyperglycemia, hyperinsulinemia, Syndrome X, diabetic complications, elevated blood levels of free fatty acids or glycerol, hyperlipidemia, obesity, hypertriglyceridemia, atherosclerosis or hypertension, which comprises administering to a mammalian species in need of treatment a therapeutically effective amount of a pharmaceutical composition comprising an isolated polypeptide comprising SEQ ID NO:
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5. A method for treating or delaying the progression or onset of diabetes, diabetic retinopathy, diabetic neuropathy, diabetic nephropathy, wound healing, insulin resistance, hyperglycemia, hyperinsulinemia, Syndrome X, diabetic complications, elevated blood levels of free fatty acids or glycerol, hyperlipidemia, obesity, hypertriglyceridemia, atherosclerosis or hypertension, which comprises administering to a mammalian species in need of treatment a therapeutically effective amount of a pharmaceutical composition comprising an isolated polypeptide of SEQ ID NO:
- 93.
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6. A method for administering a polypeptide of SEQ ID NO:
- 93, comprising the parenteral administration of a formulation comprising a polypeptide of SEQ ID NO;
93. - View Dependent Claims (8, 9, 10)
- 93, comprising the parenteral administration of a formulation comprising a polypeptide of SEQ ID NO;
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7. A method for administering a polypeptide of SEQ ID NO:
- 93, comprising the non-parenteral administration of a formulation comprising a polypeptide of SEQ ID NO;
93.
- 93, comprising the non-parenteral administration of a formulation comprising a polypeptide of SEQ ID NO;
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11. A polypeptide comprising a sequence selected from the group consisting of SEQ ID NOs:
- 17, 60, 64, 78, 80, and 90.
- View Dependent Claims (13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28)
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12. A pharmaceutical composition, comprising a polypeptide selected from the group consisting of SEQ ID NOs:
- 17, 60, 64, 78, 80 and 90 and a pharmaceutically acceptable carrier thereof.
Specification