Abstract: The present application discloses a process for the preparation of a halofenate compound of the formula (III) or a salt thereof: wherein R, X and X? are as defined herein, the process comprising contacting a compound of formula (Ia) with a compound of formula (Ib) and N,N?-dicyclohexylcarbodiimide under conditions sufficient to form the compound of formula (III).
Abstract: Methods of treating gout flares comprising administering a composition comprising a first urate-lowering agent are disclosed. In some aspects, the first urate-lowering agent is (?)-halofenate, (?)-halofenic acid, or a pharmaceutically acceptable salt thereof. Other aspects provide for methods of reducing the number, duration, frequency or intensity of gout flares experienced by a subject.
Type:
Application
Filed:
August 7, 2013
Publication date:
May 8, 2014
Applicant:
Metabolex, Inc.
Inventors:
Brian Edward Lavan, Gopal Chandra Saha, Brian K. Roberts, Charles A. McWerther
Abstract: GPR120 agonists are provided. These compounds are useful for the treatment of metabolic diseases, including Type II diabetes and diseases associated with poor glycemic control.
Type:
Application
Filed:
October 15, 2013
Publication date:
May 1, 2014
Applicant:
Metabolex, Inc.
Inventors:
Dong Fang Shi, Jiangao Song, Christopher J. Rabbat, Jingyuan Ma, Aaron Novack, Imad Nashashibi, Xin Chen
Abstract: Crystalline salts of 5-ethyl-2-{4-[4-(4-tetrazol-1-yl-phenoxymethyl)-thiazol-2-yl]-piperidin-1-yl}-pyrimidine, compositions thereof, methods for their preparation, and methods for their use are disclosed.
Type:
Application
Filed:
March 28, 2013
Publication date:
February 6, 2014
Applicant:
Metabolex, Inc.
Inventors:
Jiangao SONG, Charles A. McWherter, Fang Ma, Mark Andres, Igor Ivanisevic, Ekaterina Albert, Patricia Andres
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:
Application
Filed:
July 10, 2013
Publication date:
January 23, 2014
Applicants:
Diatex, Inc., Metabolex, Inc.
Inventors:
Edward D. Daugs, Eric J. Hagen, Jason A. Hanko, David H. Louks
Abstract: GPR120 agonists are provided. These compounds are useful for the treatment of metabolic diseases, including Type II diabetes and diseases associated with poor glycemic control.
Type:
Grant
Filed:
October 5, 2012
Date of Patent:
December 3, 2013
Assignee:
Metabolex, Inc.
Inventors:
Dong Fang Shi, Jiangao Song, Christopher J. Rabbat, Jingyuan Ma, Aaron Novack, Imad Fayek Nashashibi, Xin Chen, Phuongly Pham
Abstract: The present invention is directed to a novel process for the preparation of (4-chloro-phenyl)-(3-trifluoromethyl-phenoxy)-acetic acid 2-acetylamino-ethyl ester, useful in the treatment of metabolic disorders and further to a process for the preparation of (4-chloro-phenyl)-(3-trifluoromethyl-phenoxy)-acetic acid, a synthesis intermediate.
Type:
Grant
Filed:
April 3, 2009
Date of Patent:
September 24, 2013
Assignee:
Metabolex, Inc.
Inventors:
Diego Broggini, Hartmut Burghard Zinser
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:
May 11, 2012
Date of Patent:
August 13, 2013
Assignees:
Metabolex, Inc.
Inventors:
Edward D. Daugs, Eric J. Hagen, Jason A. Hanko, David H. Louks
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: GPR120 agonists are provided. These compounds are useful for the treatment of metabolic diseases, including Type II diabetes and diseases associated with poor glycemic control.
Type:
Grant
Filed:
October 4, 2012
Date of Patent:
July 2, 2013
Assignee:
Metabolex, Inc.
Inventors:
Dong Fang Shi, Jiangao Song, Jingyuan Ma, Aaron Novack, Phuongly Pham, Imad Fayek Nashashibi, Christopher J. Rabbat, Xin Chen
Abstract: GPR120 agonists are provided. These compounds are useful for the treatment of metabolic diseases, including Type II diabetes and diseases associated with poor glycemic control.
Abstract: GPR120 agonists are provided. These compounds are useful for the treatment of metabolic diseases, including Type II diabetes and diseases associated with poor glycemic control.
Abstract: Crystalline salts of 5-ethyl-2-{4-[4-(4-tetrazol-1-yl-phenoxymethyl)-thiazol-2-yl]-piperidin-1-yl}-pyrimidine, compositions thereof, methods for their preparation, and methods for their use are disclosed.
Type:
Grant
Filed:
September 20, 2010
Date of Patent:
April 2, 2013
Assignee:
Metabolex, Inc.
Inventors:
Jiangao Song, Charles A. McWherter, Fang Ma, Mark Andres, Igor Ivanisevic, Ekaterina Albert, Patricia Andres
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: GPR120 agonists are provided. These compounds are useful for the treatment of metabolic diseases, including Type II diabetes and diseases associated with poor glycemic control.
Type:
Grant
Filed:
December 17, 2009
Date of Patent:
November 13, 2012
Assignee:
Metabolex Inc.
Inventors:
Dong Fang Shi, Jiangao Song, Jingyuan Ma, Aaron Novack, Phuongly Pham, Imad Fayek Nashashibi, Christopher J. Rabbat, Xin Chen
Abstract: GPR120 agonists are provided. These compounds are useful for the treatment of metabolic diseases, including Type II diabetes and diseases associated with poor glycemic control.
Type:
Grant
Filed:
June 16, 2010
Date of Patent:
October 30, 2012
Assignee:
Metabolex Inc.
Inventors:
Dong Fang Shi, Jiangao Song, Jingyuan Ma, Aaron Novack, Phuongly Pham, Imad Fayek Nashashibi, Christopher J. Rabbat, Xin Chen
Abstract: Compounds, compositions, and methods of avoiding edema while treating or preventing PPAR?-mediated diseases, including cancer, using derivatives and prodrugs are provided.
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:
Grant
Filed:
November 16, 2009
Date of Patent:
October 16, 2012
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 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:
Application
Filed:
May 11, 2012
Publication date:
September 13, 2012
Applicants:
Diatex, Inc., Metabolex, Inc.
Inventors:
Edward D. Daugs, Eric J. Hagen, Jason A. Hanko, David H. Louks