Abstract: The present disclosure provides 2,4-disubstituted thiazoles of the general structure shown below that are agonists of G-protein coupled receptor (IC-GPCR2). Also, provided are compositions comprising these compounds as well as methods for using these compounds in a variety of applications including diabetes and metabolic disorders.
Type:
Grant
Filed:
August 14, 2009
Date of Patent:
July 24, 2012
Assignee:
Metabolex Inc.
Inventors:
Xin Chen, Peng Cheng, L. Edward Clemens, Jeffrey D. Johnson, Jingyuan Ma, Alison Murphy, Imad Nashashibi, Christopher J. Rabbat, Jiangao Song, Maria E. Wilson, Yan Zhu, Zuchun Zhao
Abstract: The present invention provides crystalline solid and amorphous forms of (?)-halofenate. The crystalline solid forms may be used in various pharmaceutical compositions, and are particularly effective for the prevention and/or treatment of conditions associated with blood lipid deposition in a mammal, particularly those diseases related to Type 2 diabetes and hyperlipidemia. The invention also relates to a method for preventing or treating Type 2 diabetes and hyperlipidemia in a mammal comprising the step of administering a therapeutically effective amount of crystalline solid and amorphous forms of (?)-halofenate.
Type:
Grant
Filed:
April 20, 2006
Date of Patent:
June 19, 2012
Assignees:
Metabolex, Inc., DiaTex, Inc.
Inventors:
Edward D. Daugs, Eric J. Hagen, Jason A. Hanko, David H. Louks
Abstract: Compounds and methods are provided for the treatment of, inter alia, Type II diabetes and other diseases associated with poor glycemic control.
Type:
Grant
Filed:
July 10, 2008
Date of Patent:
May 22, 2012
Assignee:
Metabolex Inc.
Inventors:
Jingyuan Ma, Christopher J. Rabbat, Jiangao Song, Xin Chen, Imad Nashashibi, Zuchun Zhao, Aaron Novack, Dong Fang Shi, Peng Cheng, Yan Zhu, Alison Murphy
Abstract: Aryl GPR119 agonists are provided. These compounds are useful for the treatment of diabetic diseases, including Type II diabetes and other diseases associated with poor glycemic control.
Type:
Application
Filed:
June 16, 2009
Publication date:
December 1, 2011
Applicant:
METABOLEX, INC.
Inventors:
Jiangao Song, Jingyuan Ma, Christopher J. Rabbat, Imad Nashashibi, Xin Chen, Zuchun Zhao
Abstract: The present invention provides a compounds the formula (IV): and methods for producing an ?-(phenoxy)phenylacetic acid compound of the formula: wherein R1 is a member selected from the group consisting of: each R2 is a member independently selected from the group consisting of (C1-C4)alkyl, halo, (C1-C4)haloalkyl, amino, (C1-C4)aminoalkyl, amido, (C1-C4)amidoalkyl, (C1-C4)sulfonylalkyl, (C1-C4)sulfamylalkyl, (C1-C4)alkoxy, (C1-C4)heteroalkyl, carboxy and nitro; the subscript n is 1 when R1 has the formula (a) or (b) and 2 when R1 has the formula (c) or (d); the subscript m is an integer of from 0 to 3; * indicates a carbon which is enriched in one stereoisomeric configuration; and the wavy line indicates the point of attachment of R1; and compounds.
Abstract: The present invention provides the use of (?)(3-trihalomethylphenoxy)(4-halophenyl)acetic acid derivatives and compositions in the treatment of insulin resistance, Type 2 diabetes and hyperlipidemia.
Abstract: The present invention provides the use of (?)(3-trihalomethylphenoxy)(4-halophenyl)acetic acid derivatives and compositions in the treatment of insulin resistance, Type 2 diabetes, hyperlipidemia and hyperuricemia.
Abstract: The present invention is directed to certain novel compounds represented by Formula (I) and pharmaceutically acceptable salts, solvates, hydrates and prodrugs thereof. The present invention is also directed to methods of making and using such compounds and pharmaceutical compositions containing such compounds to treat or control a number of diseases mediated by PPAR such as glucose metabolism, lipid metabolism and insulin secretion, specifically Type 2 diabetes, hyperinsulinemia, hyperlipidemia, hyperuricemia, hypercholesteremia, atherosclerosis, one or more risk factors for cardiovascular disease, Syndrome X, hypertriglyceridemia, hyperglycemia, obesity and eating disorders.
Type:
Application
Filed:
October 7, 2009
Publication date:
April 8, 2010
Applicant:
Metabolex, Inc.
Inventors:
Yan ZHU, Jingyuan Ma, Peng Cheng, Zuchun Zhao, Francine M. Gregoire, Vera A. Rakhmanova
Abstract: Substituted phenylacetic acids, phenylethanols and related compounds are provided that are useful in treating or controlling a number of diseases associated with glucose metabolism, lipid metabolism and insulin secretion.
Abstract: Compounds, compositions, and methods relating to 5-ethyl-2-{4-[4-(4-tetrazol-1-yl-phenoxymethyl)-thiazol-2-yl]-piperidin-1-yl}-pyrimidine or a pharmaceutically acceptable salt thereof are provided for the treatment of Type II diabetes and other diseases associated with poor glycemic control.
Type:
Grant
Filed:
December 26, 2007
Date of Patent:
December 29, 2009
Assignee:
Metabolex Inc.
Inventors:
Xin Chen, Peng Cheng, L. Edward Clemens, Jeffrey D. Johnson, Jingyuan Ma, Alison Murphy, Imad Nashashibi, Christoper J. Rabbat, Jiangao Song, Maria E. Wilson, Yan Zhu, Zuchun Zhao
Abstract: The present invention is directed to certain novel compounds represented by Formula (I) and pharmaceutically acceptable salts, solvates, hydrates and prodrugs thereof. The present invention is also directed to methods of making and using such compounds and pharmaceutical compositions containing such compounds to treat or control a number of diseases mediated by PPAR such as glucose metabolism, lipid metabolism and insulin secretion, specifically Type 2 diabetes, hyperinsulinemia, hyperlipidemia, hyperuricemia, hypercholesteremia, atherosclerosis, one or more risk factors for cardiovascular disease, Syndrome X, hypertriglyceridemia, hyperglycemia, obesity and eating disorders.
Type:
Grant
Filed:
August 11, 2005
Date of Patent:
November 24, 2009
Assignee:
Metabolex Inc.
Inventors:
Yan Zhu, Jingyuan Ma, Peng Cheng, Zuchun Zhao, Francine M. Gregoire, Vera A. Rakhmanova
Abstract: The present invention provides the use of (?) (3-trihalomethylphenoxy) (4-halophenyl) acetic acid derivatives and compositions in the treatment of insulin resistance, Type 2 diabetes, hyperlipidemia and hyperuricemia.
Abstract: The present invention provides a methods and compounds for producing an enantiomerically enriched ?-(phenoxy)phenylacetic acid compound of the formula: from a mixture of its enantiomers, where R1 is alkyl or haloalkyl and X is halide.
Abstract: The present invention provides compositions and methods for diagnosing and treating diabetes, insulin resistance and dyslipidemia. In particular, the invention provides methods of identifying modulators of AKR1C as well as methods of diagnosing diabetes by measuring the levels of AKR1C or 9?, 11?-PGF2? in a patient.
Type:
Grant
Filed:
December 16, 2002
Date of Patent:
March 31, 2009
Assignee:
Metabolex, Inc.
Inventors:
Steve Waters, Shonna Moodie, Brian Lavan, Thomas A. Gustafson
Abstract: Compounds and methods are provided for the treatment of, inter alia, Type II diabetes and other diseases associated with poor glycemic control. The compounds of the invention are orally active.
Type:
Application
Filed:
December 26, 2007
Publication date:
February 26, 2009
Applicant:
Metabolex, Inc.
Inventors:
Xin Chen, Peng Cheng, L. Edward Clemens, Jeffrey D. Johnson, Jingyuan Ma, Alison Murphy, Imad Nashashibi, Christopher J. Rabbat, Jiangao Song, Maria E. Wilson, Yan Zhu, Zuchun Zhao
Abstract: The present invention provides polynucleotides encoding potassium channels as well as methods of using the potassium channels to treat and diagnose diabetes and a predisposition for diabetes.
Type:
Grant
Filed:
March 3, 2006
Date of Patent:
February 17, 2009
Assignee:
Metabolex, Inc.
Inventors:
Jeffrey D. Johnson, John F. Palma, Anthony C. Schweitzer, John E. Blume
Abstract: The invention provides apoptosis signaling kinase related kinase (ASKRK) nucleic acid and polypeptide sequences and methods of using such sequences to identify modulators of ASKRK. Such modulators can be used for the treatment of diabetes or for delaying the onset of diabetes. The invention also provides methods of diagnosing diabetes or pre-diabetes and methods of making a prognosis based on the detection of ASKRK nucleic acids and proteins.
Type:
Grant
Filed:
September 7, 2007
Date of Patent:
January 20, 2009
Assignee:
Metabolex, Inc.
Inventors:
Jeffrey D. Johnson, Yun-Ping Zhou, Kimberly Marlen