Patents by Inventor Dolatrai M. Vyas

Dolatrai M. Vyas 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).

  • Macrocycles and macrocycle stabilized peptides
    Patent number: 9169295
    Abstract: The invention provides methods of preparing macrocycles including macrocycle stabilized peptides (MSPs). Macrocycles and MSPs are prepared according to nucleophilic capture of an iminoquinomethide type intermediate generated from a suitably substituted 2-amino-thiazol-5-yl carbinol. The preferred nucleophile may be selected from an electron rich aromatic moiety in the case of macrocycles and, in the case of MSPs, at least one amino acid comprises an electron rich aromatic moiety. In addition, the concept can be extended to other related 5-membered heterocyclic systems in place of the thiazole, such as imidazole or oxazole. The conditions for the generation of the corresponding iminoquinomethide type intermediates may be similar or different than the conditions used for the 2-amino-thiazol-5-yl carbinol.
    Type: Grant
    Filed: October 13, 2011
    Date of Patent: October 27, 2015
    Assignee: Bristol-Myers Squibb Company
    Inventors: Mark G. Saulnier, Dolatrai M. Vyas, David R. Langley, David B. Frennesson
  • Azaindazole compounds
    Patent number: 8673922
    Abstract: Disclosed are azaindazole compounds of Formula (I), or pharmaceutically acceptable salts thereof, wherein W is CR4 or N; and R1, R2, R3, and R4 are defined herein. Also disclosed are methods of using such compounds in the treatment of at least one CYP17 associated condition, such as, for example, cancer, and pharmaceutical compositions comprising such compounds.
    Type: Grant
    Filed: July 14, 2011
    Date of Patent: March 18, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: Upender Velaparthi, David B. Frennesson, Mark G. Saulnier, Joel F. Austin, Audris Huang, James Aaron Balog, Dolatrai M. Vyas
  • Pyrrolotriazine kinase inhibitors
    Patent number: 8592579
    Abstract: The invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase activity thereby making them useful as anticancer agents and for the treatment of Alzheimer's Disease.
    Type: Grant
    Filed: August 7, 2012
    Date of Patent: November 26, 2013
    Assignee: Bristol-Myers Squibb Company
    Inventors: Mark D. Wittman, Harold Mastalerz, Kurt Zimmermann, Mark G. Saulnier, Upender Velaparthi, Dolatrai M. Vyas, Guifen Zhang, Walter Lewis Johnson, David B. Frennesson, Xiaopeng Sang, Peiying Liu, David R. Langley
  • MACROCYCLES AND MACROCYCLE STABILIZED PEPTIDES
    Publication number: 20130281657
    Abstract: The invention provides methods of preparing macrocycles including macrocycle stabilized peptides (MSPs). Macrocycles and MSPs are prepared according to nucleophilic capture of an iminoquinomethide type intermediate generated from a suitably substituted 2-amino-thiazol-5-yl carbinol. The preferred nucleophile may be selected from an electron rich aromatic moiety in the case of macrocycles and, in the case of MSPs, at least one amino acid comprises an electron rich aromatic moiety. In addition, the concept can be extended to other related 5-membered heterocyclic systems in place of the thiazole, such as imidazole or oxazole. The conditions for the generation of the corresponding iminoquinomethide type intermediates may be similar or different than the conditions used for the 2-amino-thiazol-5-yl carbinol.
    Type: Application
    Filed: October 13, 2011
    Publication date: October 24, 2013
    Applicant: Bristol-Myers Squibb Company
    Inventors: Mark G. Saulnier, Dolatrai M. Vyas, David R. Langley, David B. Frennesson
  • AZAINDAZOLE COMPOUNDS
    Publication number: 20130184254
    Abstract: Disclosed are azaindazole compounds of Formula (I), or pharmaceutically acceptable salts thereof, wherein W is CR4 or N; and R1, R2, R3, and R4 are defined herein. Also disclosed are methods of using such compounds in the treatment of at least one CYP17 associated condition, such as, for example, cancer, and pharmaceutical compositions comprising such compounds.
    Type: Application
    Filed: July 14, 2011
    Publication date: July 18, 2013
    Inventors: Upender Velaparthi, David B. Frennesson, Mark G. Saulnier, Joel F. Austin, Audris Huang, James Aaron Balog, Dolatrai M. Vyas
  • PYRROLOTRIAZINE KINASE INHIBITORS
    Publication number: 20120302747
    Abstract: The invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase activity thereby making them useful as anticancer agents and for the treatment of Alzheimer's Disease.
    Type: Application
    Filed: August 7, 2012
    Publication date: November 29, 2012
    Inventors: Mark D. Wittman, Harold Mastalerz, Kurt Zimmermann, Mark G. Saulnier, Upender Velaparthi, Dolatrai M. Vyas, Guifen Zhang, Walter Lewis Johnson, David B. Frennesson, Xiaopeng Sang, Peiying Liu, David R. Langley
  • Pyrrolotriazine kinase inhibitors
    Patent number: 8212031
    Abstract: The invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit protein kinase activity thereby making them useful as anticancer agents.
    Type: Grant
    Filed: March 4, 2009
    Date of Patent: July 3, 2012
    Assignee: Bristol-Myers Squibb Company
    Inventors: Upender Velaparthi, Dolatrai M. Vyas
  • PYRROLOTRIAZINE KINASE INHIBITORS
    Publication number: 20110124623
    Abstract: The invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase activity thereby making them useful as anticancer agents and for the treatment of Alzheimer's Disease.
    Type: Application
    Filed: January 28, 2011
    Publication date: May 26, 2011
    Inventors: Mark D. Wittman, Harold Mastalerz, Kurt Zimmermann, Mark G. Saulnier, Upender Velaparthi, Dolatrai M. Vyas, Guifen Zhang, Walter Lewis Johnson, David B. Frennesson, Xiaopeng Sang, Peiying Liu, David R. Langley
  • Pyrrolotriazine kinase inhibitors
    Patent number: 7879855
    Abstract: The invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase activity thereby making them useful as anticancer agents and for the treatment of Alzheimer's Disease.
    Type: Grant
    Filed: March 26, 2009
    Date of Patent: February 1, 2011
    Assignee: Bristol-Myers Squibb Company
    Inventors: Mark D. Wittman, Harold Mastalerz, Kurt Zimmermann, Mark G. Saulnier, Upender Velaparthi, Dolatrai M. Vyas, Guifen Zhang, Walter Lewis Johnson, David B. Frennesson, Xiaopeng Sang, Peiying Liu, David R. Langley
  • PYRROLOTRIAZINE KINASE INHIBITORS
    Publication number: 20110003821
    Abstract: The invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit protein kinase activity thereby making them useful as anticancer agents.
    Type: Application
    Filed: March 4, 2009
    Publication date: January 6, 2011
    Inventors: Upender Velaparthi, Dolatrai M. Vyas
  • PYRROLOTRIAZINE KINASE INHIBITORS
    Publication number: 20090239838
    Abstract: The invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase activity thereby making them useful as anticancer agents and for the treatment of Alzheimer's Disease.
    Type: Application
    Filed: March 26, 2009
    Publication date: September 24, 2009
    Inventors: Mark D. Wittman, Harold Mastalerz, Kurt Zimmermann, Mark G. Saulnier, Upender Velaparthi, Dolatrai M. Vyas, Guifen Zhang, Walter Lewis Johnson, David B. Frennesson, Xiaopeng Sang, Peiying Liu, David R. Langley
  • Pyrrolotriazine kinase inhibitors
    Patent number: 7534792
    Abstract: The invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase activity thereby making them useful as anticancer agents and for the treatment of Alzheimer's Disease.
    Type: Grant
    Filed: July 5, 2007
    Date of Patent: May 19, 2009
    Assignee: Bristol-Myers Squibb Company
    Inventors: Mark D. Wittman, Harold Mastalerz, Kurt Zimmermann, Mark G. Saulnier, Upender Velaparthi, Dolatrai M. Vyas, Guifen Zhang, Walter Lewis Johnson, David B. Frennesson, Xiaopeng Sang, Peiying Liu, David R. Langley
  • PYRROLOTRIAZINE COMPOUNDS USEFUL AS KINASE INHIBITORS AND METHODS OF TREATING KINASE-ASSOCIATED CONDITIONS THEREWITH
    Publication number: 20090062288
    Abstract: The invention relates to at least one pyrrolotriazine derivative, at least one pharmaceutical composition comprising at least one pyrrolotriazine derivative, and at least one method of using at least one pyrrolotriazine derivative to treat at least one kinase associated condition.
    Type: Application
    Filed: October 28, 2008
    Publication date: March 5, 2009
    Inventors: Harold Mastalerz, Dolatrai M. Vyas, George L. Trainor, Ashvinikumar V. Gavai
  • Pyrrolotriazine compounds useful as kinase inhibitors and methods of treating kinase-associated conditions therewith
    Patent number: 7442700
    Abstract: The invention relates to at least one pyrrolotriazine derivative, at least one pharmaceutical composition comprising at least one pyrrolotriazine derivative, and at least one method of using at least one pyrrolotriazine derivative to treat at least one kinase associated condition.
    Type: Grant
    Filed: June 27, 2006
    Date of Patent: October 28, 2008
    Assignee: Bristol-Myers Squibb Company
    Inventors: Harold Mastalerz, Dolatrai M. Vyas, George L. Trainor, Ashvinikumar V. Gavai
  • PYRROLOTRIAZINE KINASE INHIBITORS
    Publication number: 20080009497
    Abstract: The invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase activity thereby making them useful as anticancer agents and for the treatment of Alzheimer's Disease.
    Type: Application
    Filed: July 5, 2007
    Publication date: January 10, 2008
    Inventors: Mark D. Wittman, Harold Mastalerz, Kurt Zimmermann, Mark G. Saulnier, Upender Velaparthi, Dolatrai M. Vyas, Guifen Zhang, Walter Lewis Johnson, David B. Frennesson, Xiaopeng Sang, Peiying Liu, David R. Langley
  • Pyrrolotriazine compounds
    Patent number: 7102003
    Abstract: The present invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The compounds of the invention inhibit tyrosine kinase activity of growth factor receptors such as HER1, HER2 and HER4 thereby making them useful as antiproliferative agents. The compounds are also useful for the treatment of other diseases associated with signal transduction pathways operating through growth factor receptors.
    Type: Grant
    Filed: June 21, 2005
    Date of Patent: September 5, 2006
    Assignee: Bristol-Myers Squibb Company
    Inventors: Ashvinikumar V. Gavai, Harold Mastalerz, Jean-Paul Daris, Pierre Dextraze, Philippe Lapointe, Edward H. Ruediger, Dolatrai M. Vyas, Guifen Zhang
  • Neurotrophic difluoroamide agents
    Patent number: 6239146
    Abstract: The present invention relates to the design, synthesis, and the peptidyl-prolyl isomerase (PPIase or rotamase) inhibitory activity of novel &agr;,&agr;-difluoroacetamido compounds that are neurotrophic agents (i.e. compounds capable of stimulating growth or proliferation of nervous tissue) and that bind to immunophilins such as FKBP12 and inhibit their rotamase activity. This invention also relates to pharmaceutical compositions comprising these compounds.
    Type: Grant
    Filed: June 9, 2000
    Date of Patent: May 29, 2001
    Assignee: Bristol-Myers Squibb Company
    Inventors: Vivekananda M. Vrudhula, Gene M. Dubowchik, Bireshwar Dasgupta, Dolatrai M. Vyas
  • Neurotrophic difluoroamide agents
    Patent number: 6096762
    Abstract: The present invention relates to the design, synthesis, and the peptidyl-prolyl isomerase (PPIase or rotamase) inhibitory activity of novel .alpha.,.alpha.-difluoroacetamido compounds that are neurotrophic agents (i.e. compounds capable of stimulating growth or proliferation of nervous tissue) and that bind to immunophilins such as FKBP12 and inhibit their rotamase activity. This invention also relates to pharmaceutical compositions comprising these compounds.
    Type: Grant
    Filed: May 21, 1999
    Date of Patent: August 1, 2000
    Assignee: Bristol-Myers Squibb Company
    Inventors: Vivekananda M. Vrudhula, Gene M. Dubowchik, Bireshwar Dasgupta, Dolatrai M. Vyas
  • 6-thio-substituted paclitaxels
    Patent number: 5977386
    Abstract: The present invention concerns novel paclitaxel derivatives, their use as antitumor agents, and pharmaceutical formulations.
    Type: Grant
    Filed: November 26, 1997
    Date of Patent: November 2, 1999
    Assignee: Bristol-Myers Squibb Company
    Inventors: Andrew J. Staab, John F. Kadow, Dolatrai M. Vyas, Mark D. Wittman, Harold A. Mastalerz
  • 7-methylthiooxomethyl and 7-methylthiodioxomethyl paclitaxels
    Patent number: 5902822
    Abstract: The present invention concerns novel paclitaxel derivatives, their use as antitumor agents, and pharmaceutical formulations.
    Type: Grant
    Filed: February 18, 1998
    Date of Patent: May 11, 1999
    Assignee: Bristol-Myers Squibb Company
    Inventors: Jerzy Golik, Dolatrai M. Vyas