Patents Assigned to OPKO Health, Inc.
  • HYDROCHLORIDE SALTS OF 8-[{1-(3,5-BIS-(TRIFLUOROMETHYL)PHENYL)-ETHOXY}-METHYL]-8-PHENYL-1,7-DIAZA-SPIRO[4.5]DECAN-2-ONE AND PREPARATION PROCESS THEREFOR
    Publication number: 20190375751
    Abstract: Disclosed are hydrochloride and tosylate crystalline salt forms of (5S,8S)-8-[{(1R)-1-(3,5-Bis-(trifluoromethyl)phenyl)-ethoxy}-methyl]-8-phenyl-1,7-diazaspiro[4.5]decan-2-one, represented by Formula I and methods of preparing the same.
    Type: Application
    Filed: January 9, 2019
    Publication date: December 12, 2019
    Applicant: OPKO Health, Inc.
    Inventors: Mengwei Hu, Sunil Paliwal, Neng-Yang Shih, Frank Bruno Guenter, Ingrid Mergelsberg
  • Hydrochloride salts of 8-[1-(3,5-bis-(trifluoromethyl)phenyl)-ethoxymethyl]-8-phenyl-1,7-diazaspiro[4,5]decan-2-one and preparation process therefor
    Patent number: 10196394
    Abstract: Disclosed are hydrochloride and tosylate crystalline salt forms of (5S,8S)-8-[{(1R)-1-(3,5-Bis-(trifluoromethyl)phenyl)-ethoxy}-methyl]-8-phenyl-1,7-diazaspiro[4.5]decan-2-one, represented by Formula I and methods of preparing the same.
    Type: Grant
    Filed: April 10, 2015
    Date of Patent: February 5, 2019
    Assignee: OPKO Health, Inc.
    Inventors: Mengwei Hu, Sunil Paliwal, Neng-Yang Shih, Frank Bruno Guenter, Ingrid Mergelsberg
  • Process and intermediates for the synthesis of 8-[{1-(3,5-bis-(trifluoromethyl)phenyl)-ethoxy}-methyl]-8-phenyl-1,7-diaza-spiro[4.5]decan-2-one compounds
    Patent number: 10000493
    Abstract: This application discloses a process to synthesize 8-({1-(3,5-Bis-(trifluoromethyl)phenyl)-ethoxy)-methyl]-8-pheny-1,7-diazaspiro[4.5]decan-2-one comprising reacting a compound of the Formula 27a-sulfonate with zinc in the presence of acetic acid.
    Type: Grant
    Filed: February 12, 2016
    Date of Patent: June 19, 2018
    Assignee: OPKO Health, Inc.
    Inventors: Ingrid Mergelsberg, Dominik Hermann Scherer, Monika Erika Huttenloch, Hon-Chung Tsui, Sunil Paliwal, Neng-Yang Shih
  • NKantagonists
    Patent number: 9969711
    Abstract: A compound having the general structure shown in Formula I: or pharmaceutically acceptable salts and/or solvates thereof are useful in treating diseases or conditions mediated by NK1 receptors, for example various physiological disorders, symptoms or diseases, including emesis, depression, anxiety and cough.
    Type: Grant
    Filed: October 14, 2016
    Date of Patent: May 15, 2018
    Assignee: OPKO Health, Inc.
    Inventors: Anandan Palani, Xianhai Huang, Dong Xiao, Sunil Paliwal, Hon-Chung Tsui, Michelle Laci Wrobleski, Ashwin U. Rao, Cheng Wang, Sapna S. Shah, Neng-Yang Shih
  • Process and intermediates for the synthesis of 8-[{1-(3,5-bis-(trifluoromethyl)phenyl)-ethoxy}-methyl]-8-phenyl-1,7-diaza-spiro[4.5]decan-2-one compounds
    Patent number: 9822116
    Abstract: This application discloses a novel process to synthesize 8-[{1-(3,5-Bis-(trifluoromethyl)phenyl)-ethoxy}-methyl]-8-phenyl-1,7-diaza-spiro[4.5]decan-2-one compounds, which may be used, for example, as NK-1 inhibitor compounds in pharmaceutical preparations, intermediates useful in said process, and processes for preparing said intermediates; also disclosed is a process for removal of metals from N-heterocyclic carbine metal complexes.
    Type: Grant
    Filed: February 1, 2016
    Date of Patent: November 21, 2017
    Assignee: OPKO Health, Inc.
    Inventors: George G. Wu, Gerald Werne, Xiaoyong Fu, Robert K. Orr, Frank Xing Chen, Jian Cui, Victoria M. Sprague, Fucheng Zhang, Ji Xie, Liansheng Zeng, Louis Peter Castellanos, Yuyin Chen, Marc Poirier, Ingrid Mergelsberg
  • NKantagonists
    Patent number: 9688693
    Abstract: A NK1 antagonist having the formula (I), wherein Ar1 and Ar2 are optionally substituted phenyl or heteroaryl, X1 is an ether, thio or imino linkage, R4 and R5 are not both H or alkyl, and the remaining variables are as defined in the specification, useful for treating a number of disorders, including emesis, depression, anxiety and cough. Pharmaceutical compositions. Methods of treatment and combinations with other agents are also disclosed.
    Type: Grant
    Filed: July 25, 2014
    Date of Patent: June 27, 2017
    Assignee: OPKO Health, Inc.
    Inventors: Sunil Paliwal, Gregory A. Reichard, Cheng Wang, Dong Xiao, Hon-Chung Tsui, Neng-Yang Shih, Juan D. Arredondo, Michelle Laci Wrobleski, Anandan Palani
  • Identification of small molecules recognized by antibodies in subjects with neurodegenerative diseases
    Patent number: 9551721
    Abstract: The present invention provides for the identification of individuals having neurodegenerative diseases (ND). Peptoids recognized by Parkinson's Disease- and Alzheimer's Disease-specific antibodies are identified, allowing one to diagnose or predict ND in subjects.
    Type: Grant
    Filed: June 1, 2010
    Date of Patent: January 24, 2017
    Assignees: The Board of Regents of the University of Texas System, OPKO Health, Inc.
    Inventors: Muralidhar Reddy Moola, Dwight German, Steven Connell, Rosemary Wilson, Johnnie Wilson, Thomas Kodadek
  • NKantagonists
    Patent number: 9469629
    Abstract: A compound having the general structure shown in Formula I: or pharmaceutically acceptable salts and/or solvates thereof are useful in treating diseases or conditions mediated by NK1 receptors, for example various physiological disorders, symptoms or diseases, including emesis, depression, anxiety and cough.
    Type: Grant
    Filed: June 13, 2014
    Date of Patent: October 18, 2016
    Assignee: OPKO Health, Inc.
    Inventors: Anandan Palani, Xianhai Huang, Dong Xiao, Sunil Paliwal, Hon-Chung Tsui, Michelle Laci Wrobleski, Ashwin U. Rao, Cheng Wang, Sapna S. Shah, Neng-Yang Shih
  • HYPERSULFATED DISACCHARIDE FORMULATIONS
    Publication number: 20160250242
    Abstract: Hypersulfated disaccharides with utility in asthma or asthma related disorders are disclosed. The compounds are formulated with agents that enhance the oral delivery of the hypersulfated disaccharides. The delivery agents are selected from the group consisting of natural or synthetic polymers having ionic side chains as well as other compounds or types of compounds that improve the bioavailability of the disaccharides relative to delivery of the drug without such agents. The hypersulfated disaccharides are made from heparin or salts thereof.
    Type: Application
    Filed: May 13, 2016
    Publication date: September 1, 2016
    Applicant: OPKO Health, Inc.
    Inventor: Tahir AHMED
  • Pharmaceutical formulations: salts of 8-[1-3,5-bis-(trifluoromethyl)phenyl)-ethoxy-methyl]-8-phenyl-1,7-diaza-spiro[4.5]decan-2-one and treatment methods using the same
    Patent number: 9345692
    Abstract: Pharmaceutical formulations containing salts of (5S,8S)-8-[{(1R)-1-(3,5-Bis-(trifluoromethyl)phenyl]-ethoxy}-methyl]-8-phenyl-1,7-diazaspiro[4.5]decan-2-one, represented by Formula I, are disclosed. Disclosed also are methods of treatment utilizing such dosage forms.
    Type: Grant
    Filed: March 19, 2013
    Date of Patent: May 24, 2016
    Assignee: OPKO Health, Inc.
    Inventors: Zhihui Qiu, Larisa Reyderman
  • Process and intermediates for the synthesis of 8-[{1-(3,5-bis-(trifluoromethyl)phenyl)-ethoxy}-methyl]-8-phenyl-1,7-diaza-spiro[4.5]decan-2-one compounds
    Patent number: 9260428
    Abstract: This application discloses a process to synthesize 8-({1-(3,5-Bis-(trifluoromethyl)phenyl)-ethoxy)-methyl]-8-pheny-1.7-diaza-spiro[4.5]decan-2-one comprising reacting a compound of the Formula 27a-sulfonate with zinc in the presence of acetic acid.
    Type: Grant
    Filed: September 27, 2013
    Date of Patent: February 16, 2016
    Assignee: OPKO Health, Inc.
    Inventors: Ingrid Mergelsberg, Dominik Hermann Scherer, Monika Erika Huttenloch, Hon-Chung Tsui, Sunil Paliwal, Neng-Yang Shih
  • Process and intermediates for the synthesis of 8-[{1-(3,5-bis-(trifluoromethyl)phenyl)-ethoxy}-methyl]-8-phenyl-1,7-diaza-spiro[4.5]decan-2-one compounds
    Patent number: 9249144
    Abstract: This application discloses a novel process to synthesize 8-[{1-(3,5-Bis-(trifluoromethyl)phenyl)-ethoxy}-methyl]-8-phenyl-1,7-diaza-spiro[4.5]decan-2-one compounds, which may be used, for example, as NK-1 inhibitor compounds in pharmaceutical preparations, intermediates useful in said process, and processes for preparing said intermediates; also disclosed is a process for removal of metals from N-heterocyclic carbine metal complexes.
    Type: Grant
    Filed: October 1, 2013
    Date of Patent: February 2, 2016
    Assignee: OPKO Health, Inc.
    Inventors: George G. Wu, Gerald Werne, Xiaoyong Fu, Robert K. Orr, Frank Xing Chen, Jian Cui, Victoria M. Sprague, Fucheng Zhang, Ji Xie, Liansheng Zeng, Louis Peter Castellanos, Yuyin Chen, Marc Poirier, Ingrid Mergelsberg
  • Intravenous formulations of neurokinin-1 antagonists
    Patent number: 9101615
    Abstract: Pharmaceutical compositions for intravenous administration comprising the compound of Formula I or pharmaceutically acceptable salts, hydrates or prodrugs thereof are described herein. Methods of preparing the pharmaceutical compositions and methods for treating nausea and/or emesis with the pharmaceutical compositions are also described herein.
    Type: Grant
    Filed: August 13, 2010
    Date of Patent: August 11, 2015
    Assignee: OPKO Health, Inc.
    Inventors: Jiansheng Wan, Pranav Gupta, David Monteith, Soumendu Bhattacharya
  • Hypersulfated disaccharide formulations
    Patent number: 9006211
    Abstract: Hypersulfated disaccharides with utility in asthma or asthma related disorders are disclosed. The compounds are formulated with agents that enhance the oral delivery of the hypersulfated disaccharides. The delivery agents are selected from the group consisting of natural or synthetic polymers having ionic side chains as well as other compounds or types of compounds that improve the bioavailability of the disaccharides relative to delivery of the drug without such agents. The hypersulfated disaccharides are made from heparin or salts thereof.
    Type: Grant
    Filed: August 28, 2013
    Date of Patent: April 14, 2015
    Assignee: OPKO Health, Inc.
    Inventor: Tahir Ahmed
  • NK1 antagonists
    Patent number: 8796299
    Abstract: A NK1 antagonist having the formula (I), wherein Ar1 and Ar2 are optionally substituted phenyl or heteroaryl, X1 is an ether, thio or imino linkage, R4 and R5 are not both H or alkyl, and the remaining variables are as defined in the specification, useful for treating a number of disorders, including emesis, depression, anxiety and cough. Pharmaceutical compositions. Methods of treatment and combinations with other agents are also disclosed.
    Type: Grant
    Filed: September 24, 2012
    Date of Patent: August 5, 2014
    Assignee: OPKO Health, Inc.
    Inventors: Sunil Paliwal, Gregory A. Reichard, Cheng Wang, Dong Xiao, Hon-Chung Tsui, Neng-Yang Shih, Juan D. Arredondo, Michelle Laci Wrobleski, Anandan Palani
  • NK1 antagonists
    Patent number: 8754216
    Abstract: A compound having the general structure shown in Formula I: or pharmaceutically acceptable salts and/or solvates thereof are useful in treating diseases or conditions mediated by NK1 receptors, for example various physiological disorders, symptoms or diseases, including emesis, depression, anxiety and cough.
    Type: Grant
    Filed: September 26, 2011
    Date of Patent: June 17, 2014
    Assignee: OPKO Health, Inc.
    Inventors: Sapna S. Shah, Anandan Palani, Xianhai Huang, Dong Xiao, Sunil Paliwal, Hon-Chung Tsui, Michelle Laci Wrobleski, Ashwin U. Rao, Cheng Wang, Neng-Yang Shih
  • PHARMACEUTICAL FORMULATIONS: SALTS OF 8-[1-3,5-BIS-(TRIFLUOROMETHYL)PHENYL)-ETHOXYMETHYL]-8-PHENYL-1,7-DIAZA-SPIRO[4.5]DECAN-2-ONE AND TREATMENT METHODS USING THE SAME
    Publication number: 20140088128
    Abstract: Pharmaceutical formulations containing salts of (5S,8S)-8-[{(1R)-1-(3,5-Bis-(trifluoromethyl)phenyl]-ethoxy}-methyl]-8-phenyl-1,7-diazaspiro[4.5]decan-2-one, represented by Formula I, are disclosed. Disclosed also are methods of treatment utilizing such dosage forms.
    Type: Application
    Filed: March 19, 2013
    Publication date: March 27, 2014
    Applicant: OPKO Health, Inc.
    Inventor: OPKO Health, Inc.
  • Process and Intermediates for the Synthesis of 8-[-methyl]-8-phenyl-1,7-diaza-spiro[4.5]decan-2-one Compounds
    Publication number: 20140031549
    Abstract: This application discloses a novel process to synthesize 8-[{1-(3,5-Bis-(trifluoromethyl)phenyl)-ethoxy}-methyl]-8-phenyl-1,7-diaza-spiro[4.5]decan-2-one compounds, which may be used, for example, as NK-1 inhibitor compounds in pharmaceutical preparations, intermediates useful in said process, and processes for preparing said intermediates; also disclosed is a process for removal of metals from N-heterocyclic carbine metal complexes.
    Type: Application
    Filed: October 1, 2013
    Publication date: January 30, 2014
    Applicant: OPKO Health, Inc.
    Inventors: George G. Wu, Gerald Werne, Xiaoyong Fu, Robert K. Orr, Frank Xing Chen, Jian Cui, Victoria M. Sprague, Fucheng Zhang, Ji Xie, Liansheng Zeng, Louis Peter Castellanos, Yuyin Chen, Marc Poirier, Ingrid Mergelsberg
  • PROCESS AND INTERMEDIATES FOR THE SYNTHESIS OF 8-[-METHYL]-8-PHENYL-1,7-DIAZA-SPIRO[4.5]DECAN-2-ONE COMPOUNDS
    Publication number: 20140024834
    Abstract: This application discloses a process to synthesize 8-({1-(3,5-Bis-(trifluoromethyl)phenyl)-ethoxy)-methyl]-8-pheny-1.7-diaza-spiro[4.5]decan-2-one comprising reacting a compound of the Formula 27a-sulfonate with zinc in the presence of acetic acid.
    Type: Application
    Filed: September 27, 2013
    Publication date: January 23, 2014
    Applicant: OPKO HEALTH, INC.
    Inventors: Ingrid MERGELSBERG, Dominik Hermann SCHERER, Monika Erika HUTTENLOCH, Hon-Chung TSUI, Sunil PALIWAL, Neng-Yang SHIH
  • HYPERSULFATED DISACCHARIDE FORMULATIONS
    Publication number: 20130345167
    Abstract: Hypersulfated disaccharides with utility in asthma or asthma related disorders are disclosed. The compounds are formulated with agents that enhance the oral delivery of the hypersulfated disaccharides. The delivery agents are selected from the group consisting of natural or synthetic polymers having ionic side chains as well as other compounds or types of compounds that improve the bioavailability of the disaccharides relative to delivery of the drug without such agents. The hypersulfated disaccharides are made from heparin or salts thereof.
    Type: Application
    Filed: August 28, 2013
    Publication date: December 26, 2013
    Applicant: OPKO Health, Inc.
    Inventor: Tahir AHMED