Merck + Co., Inc.

Vtv Therapeutics LLC

Tung M Fong

Catherine D Strader

Ruey-Ruey C Huang

Maria Carmen Valcarce Lopez

Leonardus H T Van Der Ploeg

Leonardus H Van Der Ploeg

Michael R Tota

The present invention relates to the use of liver-selective glucokinase activators and a GLP1 analog in restoring insulin sensitivity and treating type II diabetes, including reducing body weight in subjects undergoing type II diabetes treatment.

Glucokinase activator compositions for the treatment of diabetes

The present invention relates to pharmaceutical compositions comprising {2-[3-cyclohexyl-3-(trans-4-propoxy-cyclohexyl)-ureido]-thiazol-5-ylsulfanyl}-acetic acid (FRI-1) in combination with an anti-diabetic drug selected from the group consisting of metformin, sitagliptin or exenatide. The present invention also relates to the use of the pharmaceutical compositions in restoring insulin sensitivity and treating type II diabetes, including reducing body weight in subjects undergoing type II diabetes treatment.

Novel polypeptides derived from the C-terminal region of the human and mouse agouti related transcript (ART) proteins are provided. Also provided are DNA sequences encoding the novel C-terminal polypeptides. The novel C-terminal polypeptides can be used to inhibit the binding of melanocyte stimulating hormones to melanocortin receptors. Methods of identifying inhibitors of the binding of ART protein to melanocortin receptors are also provided.

C-terminal region of agouti-related transcript (ART) protein

The present invention relates to rhesus monkey DNA molecules encoding the melanocortin-5 receptor protein, recombinant vectors comprising DNA molecules encoding rhesus MC-5R, recombinant host cells which contain a recombinant vectors encoding rhesus MC-5R, the rhesus MC-5R protein encoded by the DNA molecule, and methods of identifying selective agonists and antagonists of rhesus MC-5R.

DNA molecules encoding the melanocortin 5 receptor protein from rhesus monkey

Mutant ob receptors have been made which a) lack a functional first CK-F3 domain; b) lack a functional second CK-F3 domain or c) lack a functional intracellular domain. These receptors may be used in various assays, such as a transactivation assay to identify novel ligands.

Mutant OB receptors and nucleotides encoding them

A recombinant human neurokinin-3 receptor (hereinafter identified as human NK3R) is disclosed which has been prepared by polymerase chain reaction techniques. Also disclosed is the complete sequence of human NK3R complementary DNA; expression systems, including a CHO (chinese hamster ovarian cell line) stable expression system; and an assay using the CHO expression system. Human NK3R can be used in an assay to identify and evaluate entities that bind to the neurokinin-3 receptor.

Method for measuring human neurokinin-3 receptor ligand binding

Human neurokinin-3 receptor

Recombinant human neurokinin-1 receptor (human NKIR) is disclosed which has been isolated by polymerase chain reaction techniques. Also disclosed is the complete sequence of human NKIR cDNA, expression systems containing said isolated cDNA, including a CHO (Chinese Hamster Ovarian Cell Line) stable expression systems, and an assay using the CHO eexpression system. NKIR, also known as substance P receptor, can be used in an assay to identify and evaluate entities that bind substance P receptor. The assay can also be used in conjunction with diagnosis and therapy to determine the body fluid concnetration of substance P in arthritis patients.

DNA encoding the human neurokinin-1 receptor

Recombinant human neurokinin-1 receptor (hereinafter identified as human NK1R) has been prepared by polymerase chain reaction techniques. The complete sequence of human NK1R complementary DNA has been identified. Expression systems, including a CHO (chinese hamster ovarian cell line) stable expression system; and an assay using the CHO expression system have been developed. NK1R, also known as substance P receptor, may be used in an assay to identify and evaluate entities that bind to the substance P receptor. The assay may also be used in conjunction with diagnosis and therapy to determine the body fluid concentration of substance P antagonists in arthritis patients.

Human neurokinin-1 receptor

A novel recombinant human neurokinin-1 receptor short form (hereinafter identified as human NK1R sF) is disclosed which has been prepared by polymerase chain reaction techniques. Also disclosed is the complete sequence of human NK1R sF complementary DNA; expression systems, including a CHO (Chinese hamster ovarian cell line) stable expression system; and an assay using the CHO expression system. NK1R sF, can be used in an assay to identify and evaluate entities that bind substance P receptor or NK1R sF. The assay can also be used in conjunction with diagnosis and therapy to determine the body fluid concentration of substance P antagonists in arthritis patients.

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Somerset, NJ, United States of America

Tung M Fong