Patents by Inventor Bernard R. Neustadt

Bernard R. Neustadt has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).

  • Patent number: 8822480
    Abstract: The present invention relates to Bicyclic Heterocycle Derivatives of Formula (I), compositions comprising a Bicyclic Heterocycle Derivative, and methods of using the Bicyclic Heterocycle Derivatives for treating or preventing obesity, diabetes, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of a G-protein coupled receptor (GPCR) such as GPR119 in a patient.
    Type: Grant
    Filed: July 15, 2009
    Date of Patent: September 2, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Santhosh Francis Neelamkavil, Craig D. Boyle, Samuel Chackalamannil, William J. Greenlee, Bernard R. Neustadt, Andrew W. Stamford
  • Patent number: 8815876
    Abstract: The present invention relates to Bicyclic Heterocycle Derivatives, compositions comprising a Bicyclic Heterocycle Derivative, and methods of using the Bicyclic Heterocycle Derivatives for treating or preventing obesity, diabetes, a diabetic complication, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of a G protein-coupled receptor (GPCR) in a patient. The compounds are of structure (I).
    Type: Grant
    Filed: July 15, 2009
    Date of Patent: August 26, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Santhosh Francis Neelamkavil, Craig D. Boyle, Bernard R. Neustadt, Samuel Chackalamannil, William J. Greenlee
  • Patent number: 8722882
    Abstract: The present invention relates to Pyriraidine Derivatives of formula (I), compositions comprising a Pyrimidine Derivative, and methods of using the Pyrimidine Derivatives for treating or preventing obesity, diabetes, a diabetic complication, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of a G protein-coupled receptor (GPCR) in a patient.
    Type: Grant
    Filed: December 21, 2009
    Date of Patent: May 13, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Bernard R. Neustadt, Andrew Stamford, Jinsong Hao, Charles Lee Jayne, Yan Xia
  • Patent number: 8435994
    Abstract: The present invention relates to certain fused tricyclic heteroaryl rings compounds of the Formula (I) (also referred to herein as the “Fused Tricyclic Compounds”), wherein M, Q, U, W, X, Y, Z, R1, R2, and R3, and rings C and D are as herein described. The present invention also provides compositions comprising at least one Fused Tricyclic Compound, and use of such compounds in the treatment of central nervous system diseases or disorders such as Parkinson's disease.
    Type: Grant
    Filed: November 12, 2010
    Date of Patent: May 7, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Joel M. Harris, Bernard R. Neustadt, Andrew W. Stamford
  • Publication number: 20130096141
    Abstract: Compounds of structural formula I: are GPR119 agonists and are useful for the treatment, control or prevention of disorders responsive to agonism of GPR119, such as metabolic-related disorders such as type I diabetes, type II diabetes, inadequate glucose tolerance, insulin resistance, hyperglycemia, hyperlipidemia, hypertriglyceridemia, hypercholesterolemia, dyslipidemia or syndrome X. The compounds are also reported as being useful for controlling weight gain, controlling food intake, and inducing satiety in mammals.
    Type: Application
    Filed: June 14, 2011
    Publication date: April 18, 2013
    Inventors: Bernard R. Neustadt, Hong Liu
  • Patent number: 8415353
    Abstract: Compounds of the Formula (I), where W represents CH or N; and Q represents —CN, —C(?NOH)NH2, —CONHR1 or various herein described heterocyclic radicals; as well as pharmaceutically acceptable salts, solvates, esters and prodrugs thereof are adenosine A2a receptor antagonists and, therefore, are useful in the treatment of central nervous system diseases, in particular Parkinson's disease.
    Type: Grant
    Filed: March 3, 2009
    Date of Patent: April 9, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Joel M. Harris, Bernard R. Neustadt, Hong Liu, Jinsong Hao, Andrew W. Stamford
  • Patent number: 8410122
    Abstract: The present invention relates to Bicyclic Heterocycle Derivatives, compositions comprising a Bicyclic Heterocycle Derivative, and methods of using the Bicyclic Heterocycle Derivatives for treating or preventing obesity, diabetes, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of a GPCR in a patient.
    Type: Grant
    Filed: December 21, 2009
    Date of Patent: April 2, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Joel M. Harris, Bernard R. Neustadt, Andrew Stamford, Hong Liu
  • Patent number: 8318751
    Abstract: The present invention relates to Pyrimidinone Derivatives, compositions comprising a Pyrimidinone Derivative, and methods of using the Pyrimidinone Derivatives for treating or preventing obesity, diabetes, a metabolic disease, a cardiovascular disease or a disorder related to the activity of GPR119 in a patient.
    Type: Grant
    Filed: April 17, 2008
    Date of Patent: November 27, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Craig D. Boyle, Samuel Chackalamannil, Claire M. Lankin, Unmesh G. Shah, Bernard R. Neustadt, Hong Liu, Andrew W. Stamford
  • Publication number: 20120232073
    Abstract: The present invention relates to Fused Bicyclic Pyrimidine Derivatives, compositions comprising a Fused Bicyclic Pyrimidine Derivative, and methods of using the Fused Bicyclic Pyrimidine Derivatives for treating or preventing obesity, diabetes, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of a G-protein coupled receptor (GPCR) in a patient.
    Type: Application
    Filed: November 16, 2010
    Publication date: September 13, 2012
    Inventors: Santhosh Francis Neelamkavil, Dipshikha Biswas, Samuel Chackalamannil, Bernard R. Neustadt, Andrew Stamford, Hong Liu
  • Publication number: 20120232086
    Abstract: The present invention relates to certain fused tricyclic heteroaryl rings compounds of the Formula (I) (also referred to herein as the “Fused Tricyclic Compounds”), wherein M, Q, U, W, X, Y, Z, R1, R2, and R3, and rings C and D are as herein described. The present invention also provides compositions comprising at least one Fused Tricyclic Compound, and use of such compounds in the treatment of central nervous system diseases or disorders such as Parkinson's disease.
    Type: Application
    Filed: November 12, 2010
    Publication date: September 13, 2012
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: Joel M. Harris, Bernard R. Neustadt, Andrew W. Stampford
  • Patent number: 8222259
    Abstract: Compounds of the Formula I wherein R1 and R2 together with the carbon atoms to which they are bonded optionally form a further heteroaromatic ring of the formula (II) as well as pharmaceutically acceptable salts, solvates, esters and prodrugs thereof are adenosine A2a receptor antagonists and, therefore, are useful in the treatment of central nervous system diseases, in particular Parkinson's disease.
    Type: Grant
    Filed: March 3, 2009
    Date of Patent: July 17, 2012
    Assignee: Schering Corporation
    Inventors: Joel M. Harris, Bernard R. Neustadt, Jinsong Hao, Andrew W. Stamford
  • Publication number: 20120040975
    Abstract: The present invention relates to Bridged Bicyclic Heterocycle Derivatives, compositions comprising a Bridged Bicyclic Heterocycle Derivative, and methods of using the Bridged Bicyclic Heterocycle Derivatives for treating or preventing obesity, diabetes, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of a GPCR in a patient.
    Type: Application
    Filed: April 1, 2010
    Publication date: February 16, 2012
    Inventors: Santhosh Francis Neelamkavil, Bernard R. Neustadt, Andrew Stamford, Yan Xia, Joel M. Harris, Craig D. Boyle, Samuel Chackalamannil, Dipshikha Biswas, Hong Liu, Jinsong Hao, Claire M. Lankin, Unmesh Shah
  • Patent number: 8114879
    Abstract: The use of CCR5 antagonists of the formula or a pharmaceutically acceptable salt thereof, wherein R is optionally substituted phenyl, pyridyl, thiophenyl or naphthyl; R1 is hydrogen or alkyl; R2 is substituted phenyl, substituted heteroaryl, naphthyl fluorenyl, diphenylmethyl or optionally substituted phenyl- or heteroaryl-alkyl; R3 is hydrogen, alkyl, alkoxyalkyl, cycloalkyl, cycloalkylalkyl, or optionally substituted phenyl, phenylalkyl, naphthyl, naphthylalkyl, heteroaryl or heteroarylalkyl; R4, R5 and R7 are hydrogen or alkyl; R6 is hydrogen, alkyl or alkenyl; for the treatment of HIV, solid organ transplant rejection, graft v.
    Type: Grant
    Filed: March 26, 2008
    Date of Patent: February 14, 2012
    Assignee: Schering Corporation
    Inventors: Bahige M. Baroudy, John W. Clader, Hubert B. Josien, Stuart W. McCombie, Brian A. McKittrick, Michael W. Miller, Bernard R. Neustadt, Anandan Palani, Elizabeth M. Smith, Ruo Steensma, Jayaram R. Tagat, Susan F. Vice, Mark A. Laughlin, Eric Gilbert, Marc A. Labroli
  • Publication number: 20110263624
    Abstract: The present invention relates to Bicyclic Heterocycle Derivatives, compositions comprising a Bicyclic Heterocycle Derivative, and methods of using the Bicyclic Heterocycle Derivatives for treating or preventing obesity, diabetes, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of a GPCR in a patient.
    Type: Application
    Filed: December 21, 2009
    Publication date: October 27, 2011
    Applicant: Schering Corporation
    Inventors: Joel M. Harris, Bernard R. Neustadt, Andrew Stamford, Hong Liu
  • Publication number: 20110263570
    Abstract: The present invention relates to Pyriraidine Derivatives of formula (I), compositions comprising a Pyrimidine Derivative, and methods of using the Pyrimidine Derivatives for treating or preventing obesity, diabetes, a diabetic complication, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of a G protein-coupled receptor (GPCR) in a patient.
    Type: Application
    Filed: December 21, 2009
    Publication date: October 27, 2011
    Applicant: Schering Corporation
    Inventors: Bernard R. Neustadt, Andrew Stamford, Jinsong Hao, Charles Lee Jayne, Yan Xia
  • Publication number: 20110166167
    Abstract: The present invention relates to Bicyclic Heterocycle Derivatives, compositions comprising a Bicyclic Heterocycle Derivative, and methods of using the Bicyclic Heterocycle Derivatives for treating or preventing obesity, diabetes, a diabetic complication, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of a G protein-coupled receptor (GPCR) in a patient. The compounds are of structure (I).
    Type: Application
    Filed: July 15, 2009
    Publication date: July 7, 2011
    Applicant: Schering Corporation
    Inventors: Santhosh Francis Neelamkavil, Craig D. Boyle, Bernard R. Neustadt, Samuel Chackalamannil, William J. Greenlee
  • Publication number: 20110166165
    Abstract: The present invention relates to Bicyclic Heterocycle Derivatives of Formula (I), compositions comprising a Bicyclic Heterocycle Derivative, and methods of using the Bicyclic Heterocycle Derivatives for treating or preventing obesity, diabetes, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of a G-protein coupled receptor (GPCR) such as GPR119 in a patient.
    Type: Application
    Filed: July 15, 2009
    Publication date: July 7, 2011
    Applicant: Schering Corporation
    Inventors: Santhosh Francis Neelamkavil, Craig D. Boyle, Samuel Chackalamannil, William J. Greenlee, Bernard R. Neustadt, Andrew W. Stamford
  • Publication number: 20110152256
    Abstract: Compounds of the Formula I wherein R1 and R2 together with the carbon atoms to which they are bonded optionally form a further heteroaromatic ring of the formula (II) as well as pharmaceutically acceptable salts, solvates, esters and prodrugs thereof are adenosine A2a receptor antagonists and, therefore, are useful in the treatment of central nervous system diseases, in particular Parkinson's disease.
    Type: Application
    Filed: March 3, 2009
    Publication date: June 23, 2011
    Inventors: Joel M. Harris, Bernard R. Neustadt, Hong Liu, Jinsong Hao, Andrew W. Stamford
  • Publication number: 20110118286
    Abstract: The present invention relates to Bicyclic Heterocycle Derivatives of Formula (I), compositions comprising a Bicyclic Heterocycle Derivative, and methods of using the Bicyclic Heterocycle Derivatives for treating or preventing obesity, diabetes, a diabetic complication, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of a G protein-coupled receptor (GPCR) in a patient.
    Type: Application
    Filed: July 15, 2009
    Publication date: May 19, 2011
    Inventors: Santhosh Francis Neelamkavil, Craig D. Boyle, Joel M. Harris, Andre Stamford, Jinsong Hao, Bernard R. Neustadt, Samuel Chackalamannil, Yan Xia, Wiliam J. Greenlee
  • Patent number: RE44205
    Abstract: Compounds having the structural formula I or a pharmaceutically acceptable salt thereof, wherein R is optionally substituted phenyl, cycloalkenyl, or heteroaryl; X is alkylene or —C(O)CH2—; Y is —N(R2)CH2CH2N(R)3)—, —OCH2CH2N(R2)—, —O—, —S—, —CH2S—, —(CH2)2—NH—, or optionally substituted ?m and n are 2-3, and Q is nitrogen or optionally substituted carbon; and Z is optionally substituted phenyl, phenylalkyl or heteroaryl, diphenylmethyl, R6—C(O)—, R6—SO2—, R6—OC(O)—, R7—N(R8)—C(O)—, R7—N(R8)—C(S)—, ?phenyl-CH(OH)—, or phenyl-C(?NOR2)—; or when Q is CH, phenylamino or pyridylamino; or Z and Y together are substituted piperidinyl or substituted phenyl; and R2, R3, R6, R7, and R8 are as defined in the specification are disclosed, their use in the treatment of Parkinson's disease, alone or in combination with other agents for treating Parkinson's disease, and pharmaceutical compositions comprising them; also disclosed are a processes for preparing intermediates useful for preparing comp
    Type: Grant
    Filed: April 6, 2012
    Date of Patent: May 7, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Bernard R. Neustadt, Neil Lindo, William J. Greenlee, Deen Tulshian, Lisa S. Silverman, Yan Xia, Craig D. Boyle, Samuel Chackalamannil