Abstract: New compounds are disclosed which have utility in the treatment of a variety of metabolic related conditions in a patient. The compounds of this invention have the structure (I): wherein R1, R2, R3, n, p, q, and Ar are as defined herein, including stereoisomers, and pharmaceutically acceptable salts thereof. Also disclosed are pharmaceutical compositions comprising a compound of this invention, as well as methods relating to the use thereof in a patient in need thereof.
Type:
Application
Filed:
June 23, 2010
Publication date:
July 7, 2011
Applicants:
BOEHRINGER INGELHEIM INTERNATIONAL GMBH, NEUROCRINE BIOSCIENCES, INC.
Inventors:
Brian DYCK, Joe A. TRAN, Junko TAMIYA, Florence JOVIC, Troy VICKERS, Chen CHEN, Nicole HARRIOTT, Timothy COON, Neil J. ASHWEEK
Abstract: New compounds are disclosed which have utility in the treatment of a variety of metabolic related conditions in a patient. The compounds of this invention have the structure (I): wherein X1, X2, X3, X4, Y1, Y2, A, R1, R2, R3, R4, m, n, p, and q are as defined herein, including stereoisomers, esters, and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof in a patient in need thereof.
Type:
Application
Filed:
June 23, 2010
Publication date:
January 27, 2011
Applicants:
BOEHRINGER INGELHEIM INTERNATIONAL GMBH, NEUROCRINE BIOSCIENCES, INC.
Abstract: CRF receptor antagonists are disclosed which may have utility in the treatment of a variety of disorders, including the treatment of disorders manifesting hypersecretion of CRF in mammals, such as stroke. The CRF receptor antagonists of this invention have the following structure: and pharmaceutically acceptable salts, esters, solvates, stereoisomers and prodrugs thereof, wherein R1, R2, n, R5, Ar, and Het are as defined herein. Compositions containing a CRF receptor antagonists in combination with a pharmaceutically acceptable carrier are also disclosed, as well as methods for use of the same.
Type:
Grant
Filed:
October 17, 2005
Date of Patent:
January 26, 2010
Assignees:
Neurocrine Bioscience, Inc., SB Cork
Inventors:
Marion Lanier, Manisha Moorjani, John Edward Tellew, John P. Williams
Abstract: The present invention generally relates to the polymorph Form 2 of [3-(4-methoxy-2-methyl-phenyl)-2,5-dimethyl-pyrazolo[1,5-a]pyrimidin-7-yl]-[(S)-1-(3-methyl-[1,2,4]oxadiazol-5-yl)-propyl]-amine. The present invention also relates to pharmaceutical compositions comprising the same and methods of using the same.
Type:
Application
Filed:
September 28, 2006
Publication date:
December 11, 2008
Applicants:
SB PHARMCO PUERTO RICO INC., NEUROCRINE BIOSCIENCES INC.
Abstract: GnRH receptor antagonists are disclosed that have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: wherein A, Q, R1, R2, R3a, R3b, R4, R5, R6 and n are as defined herein, including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.
Type:
Grant
Filed:
September 11, 2006
Date of Patent:
December 9, 2008
Assignee:
Neurocrine Biosciences, Inc.
Inventors:
Yun-Fei Zhu, Chen Chen, Fabio C. Tucci, Zhiqiang Guo, Timothy D. Gross, Martin Rowbottom, R. Scott Struthers
Abstract: Polymorph Form III of N-methyl-N-(3-{3-[2-thienylcarbonyl]-pyrazol-[1,5-?]-pyrimidin-7-yl}phenyl)acetamide, and use thereof as a sedative-hypnotic, anxiolytic, anticonvulsant, and/or skeletal muscle relaxant agent. Related compositions and methods are also disclosed, particularly with regard to treatment of insomnia.
Type:
Grant
Filed:
December 15, 2004
Date of Patent:
December 2, 2008
Assignee:
Neurocrine Biosciences, Inc.
Inventors:
Scott E. Zook, Donald Hettinger, Henry R. DuBois, III
Abstract: Compounds having utility as GnRH receptor antagonists and for treatment of a variety of sex-hormone related conditions in both men and women. Such compounds have the following structure (I): (I) wherein R1a, R1b, R1c, R2a, R2b, R3, R4, R5, R6, R7, n and X are as defined herein, including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of structure (I) in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.
Type:
Application
Filed:
May 13, 2005
Publication date:
October 23, 2008
Applicant:
NEUROCRINE BIOSCIENCES, INC.
Inventors:
Yun-Fei Zhu, Zhiqiang Gou, Mi Chen, Liren Zhao
Abstract: The present invention provides compounds of formula (I) including stereoisomers, prodrugs and pharmaceutically acceptable salts or solvates thereof to processes for their preparation, to pharmaceutical compositions containing them and to their use in the treatment of conditions mediated by corticotrophin-releasing factor (CRF).
Type:
Grant
Filed:
April 7, 2004
Date of Patent:
September 23, 2008
Assignees:
SB Pharmaco Puerto Rico Inc., Neurocrine Biosciences Inc.
Inventors:
Romano Di Fabio, Fabio Maria Sabbatini, Yves St-Denis
Abstract: GnRH receptor antagonists are disclosed that have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: wherein R1a, R1b, R1c, R2a, R2b, R3, R4, R5, R6 and X are as defined herein, including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.
Type:
Grant
Filed:
January 25, 2007
Date of Patent:
September 2, 2008
Assignee:
Neurocrine Biosciences, Inc.
Inventors:
Zhiqiang Guo, Yongsheng Chen, Dongpei Wu, Chen Chen, Warren Wade, Wesley J. Dwight, Charles Q. Huang, Fabio C. Tucci
Abstract: CRF receptor antagonists are disclosed which may have utility in the treatment of a variety of disorders, including the treatment of disorders manifesting hypersecretion of CRF in mammals. The CRF receptor antagonists of this invention have the following structure: (I); and pharmaceutically acceptable salts, esters, solvates, stereoisomers and prodrugs thereof, wherein R1, R2a, R2b, Y, Het, n, o, R6, Ar and R7 are as defined herein. Compositions containing a CRF receptor antagonist in combination with a pharmaceutically acceptable carrier are also disclosed, as well as methods for use of the same.
Type:
Application
Filed:
October 19, 2005
Publication date:
August 14, 2008
Applicant:
NEUROCRINE BIOSCIENCES, INC.
Inventors:
Marion Lanier, Zhiyong Luo, Manisha Moorjani, John Edward Tellew, John P. Williams, Xiaohu Zhang
Abstract: Compounds having the following structure (I): including stereoisomers, prodrugs, and pharmaceutically acceptable salts, esters and solvates thereof, wherein R1, R2, R3a, R3b, L1, L2 and n are as defined herein. Such compounds generally function as H1 receptor ligands, and thus have utility as sleep inducing agents. Pharmaceutical compositions containing a compound of structure (I), as well as methods relating to the use thereof, are also disclosed.
Abstract: A novel hydrate form of N-methyl-N-(3-{3-[2-thienylcarbonyl]-pyrazol-[1,5-?]-pyrimidin-7-yl}phenyl)acetamide (“Compound No. 1”) and processes related to the use thereof in the synthesis of a polymorphic form of Compound No. 1.
Abstract: Monoamine re-uptake inhibitors and more specifically serotonin and noradrenaline re-uptake inhibitors are disclosed that have utility in the treatment of disorders of the central or peripheral nervous system in both men and women. The compounds of this invention have the structure: wherein R1, R2, R3, R4, R5, R6, m, n, W, X, Y, and Z are as defined herein, including stereoisomers, prodrugs and pharmaceutically acceptable salts, esters and solvates thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for inhibiting monoamine re-uptake in a subject in need thereof.
Type:
Grant
Filed:
June 7, 2006
Date of Patent:
May 27, 2008
Assignee:
Neurocrine Biosciences, Inc.
Inventors:
Joseph Pontillo, Yinghong Gao, Warren S. Wade, Dongpei Wu, Wendy K. Eccles
Abstract: 4-Aminopyrimidine derivatives of formula (I) FORMULA heteroaryl groups, including pharmaceutically acceptable salts thereof, wherein R1 and R2 are adenosine A2A receptor antagonists useful in the treatment of movement disorders such as Parkinson's disease.
Type:
Application
Filed:
December 14, 2004
Publication date:
March 6, 2008
Applicant:
Neurocrine Biosciences, Inc.
Inventors:
Maria Isabel Crespo Crespo, Maria Prat Quinones, Siliva Gual Roig, Julio Cesar Castro Palomino Laria, Deborah H. Slee
Abstract: GnRH receptor antagonists are disclosed that have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: wherein R1a, R1b, R2a, R2b, R3, R4, R5, R6, R7 and X are as defined herein, including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.
Type:
Grant
Filed:
June 2, 2006
Date of Patent:
February 12, 2008
Assignee:
Neurocrine Biosciences, Inc.
Inventors:
Yun-Fei Zhu, Collin Regan, Jaimie K Rueter, Zhiqiang Guo, Yongsheng Chen, Charles Q Huang
Abstract: CRF receptor antagonists are disclosed which have utility in the treatment of a variety of disorders in mammals, including the treatment of disorders, such as stroke, manifesting hypersecretion of CRF. The CRF receptor antagonists of this invention have the following structure: including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof, wherein R1, R2, R5, Ar, and Het are as defined herein. Compositions containing a CRF receptor antagonist in combination with a pharmaceutically acceptable carrier are also disclosed, as well as methods for use of the same.
Type:
Application
Filed:
December 20, 2004
Publication date:
December 20, 2007
Applicants:
SB Pharmco Puerto Rico Inc and Neurocrine Biosciences, Inc., Neurocrine Biosciences, Inc.,, SB Pharmco Puerto Rico
Inventors:
John Williams, Zhiyong Luo, John Tellew
Abstract: A novel hydrate form of N-methyl-N-(3-{3-[2-thienylcarbonyl]-pyrazol-[1,5-?]-pyrimidin-7-yl}phenyl)acetamide (“Compound No. 1”) and processes related to the use thereof in the synthesis of a polymorphic form of Compound No. 1.
Abstract: The present invention relates to tricyclic pyridines compounds of formula (I) including stereoisomers, prodrugs and pharmaceutically acceptable salts or solvates thereof:
Type:
Grant
Filed:
July 15, 2002
Date of Patent:
September 25, 2007
Assignees:
SB Pharmco Puerto Rico Inc., Neurocrine Biosciences Inc.
Inventors:
Romano Di Fabio, Collin F Regan, Yves St-Denis, Fabrizio Micheli, Michael K Schwaebe
Abstract: GnRH receptor antagonists are disclosed that have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: wherein A, Q, R1, R2, R3a, R3b, R4, R5, R6 and n are as defined herein, including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.
Type:
Application
Filed:
September 11, 2006
Publication date:
September 6, 2007
Applicant:
Neurocrine Biosciences, Inc.
Inventors:
Yun-Fei Zhu, Chen Chen, Fabio Tucci, Zhiqiang Guo, Timothy Gross, Martin Rowbottom, R. Struthers
Abstract: GnRH receptor antagonists are disclosed that have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: wherein R1a, R1b, R1c, R2a, R2b, R3, R4, R5, R6 and X are as defined herein, including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.