Patents by Inventor Robert M. Borzilleri

Robert M. Borzilleri 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).

  • TGF-beta inhibitors
    Patent number: 11352360
    Abstract: Disclosed are imidazole and thiazole compounds, as well as pharmaceutical compositions and methods of use thereof. One embodiment is a compound having the structure and pharmaceutically acceptable salts, prodrugs and N-oxides thereof (and solvates and hydrates thereof), wherein X, A, Z, R1 and R? are as described herein. In certain embodiments, a compound disclosed herein inhibits TGF-?, and can be used to treat disease by blocking TGF-? signaling.
    Type: Grant
    Filed: March 21, 2019
    Date of Patent: June 7, 2022
    Assignees: Rigel Pharmaceuticals, hic., Bristol-Myers Squibb Company
    Inventors: Todd Kinsella, Marina Gelman, Hui Hong, Ihab S. Darwish, Rajinder Singh, Jiaxin Yu, Robert M. Borzilleri, Upender Velaparthi, Peiying Liu, Chetan Padmakar Dame, Hasibur Rahaman, Jayakumar Sankara Warrier
  • TGF beta receptor antagonists
    Patent number: 10961239
    Abstract: The invention relates generally to compounds of formula (I) that modulate the activity of TGF?R-1 and TGF?R-2, pharmaceutical compositions containing said compounds and methods of treating proliferative disorders and disorders of dysregulated apoptosis, such as cancer, utilizing the compounds of the invention.
    Type: Grant
    Filed: January 3, 2018
    Date of Patent: March 30, 2021
    Assignee: Bristol-Myers Squibb Company
    Inventors: Robert M. Borzilleri, Upender Velaparthi, Chetan Padmakar Darne, Peiying Liu, Manjunatha Narayana Rao Kamble, Balaji Seshadri, Raju Mannoori, Hasibur Rahaman, Jayakumar Sankara Warrier
  • TGF-Beta Inhibitors
    Publication number: 20200031832
    Abstract: Disclosed are imidazole and thiazole compounds, as well as pharmaceutical compositions and methods of use thereof. One embodiment is a compound having the structure and pharmaceutically acceptable salts, prodrugs and N-oxides thereof (and solvates and hydrates thereof), wherein X, A, Z, R1 and R? are as described herein. In certain embodiments, a compound disclosed herein inhibits TGF-?, and can be used to treat disease by blocking TGF-? signaling.
    Type: Application
    Filed: March 21, 2019
    Publication date: January 30, 2020
    Inventors: Todd Kinsella, Marina Gelman, Hui Hong, Ihab S. Darwish, Rajinder Singh, Jiaxin Yu, Robert M. Borzilleri, Upender Velaparthi, Peiying Liu, Chetan Padmakar Darne, Hasibur Rahaman, Jayakumar Sankara Warrier
  • TGF BETA RECEPTOR ANTAGONISTS
    Publication number: 20190337942
    Abstract: The invention relates generally to compounds of formula (I) that modulate the activity of TGF?R-1 and TGF?R-2, pharmaceutical compositions containing said compounds and methods of treating proliferative disorders and N disorders of dysregulated apoptosis, such as cancer, utilizing the compounds of the invention.
    Type: Application
    Filed: January 3, 2018
    Publication date: November 7, 2019
    Inventors: Robert M. Borzilleri, Upender Velaparthi, Chetan Padmakar Darne, Peiying Liu, Manjunatha Narayana Rao Kamble, Balaji Seshadri, Raju Mannoori, Hasibur Rahaman, Jayakumar Sankara Warrier
  • TGF Beta RECEPTOR ANTAGONISTS
    Publication number: 20190292179
    Abstract: The invention relates generally to compounds that modulate the activity of TGF?R-1 and TGF?R-2, pharmaceutical compositions containing said compounds and methods of treating proliferative disorders and disorders of dysregulated apoptosis, such as cancer, utilizing the compounds of the invention.
    Type: Application
    Filed: July 19, 2017
    Publication date: September 26, 2019
    Inventors: Robert M. Borzilleri, Peiyung Liu, Andrew J. Tebben, Upender Velaparthi, Hasibur Rahaman, Gopikishan Tonukunuru, Jayakumar Sankara Warrier
  • TGF beta receptor antagonists
    Patent number: 10399987
    Abstract: The invention relates generally to compounds that modulate the activity of TGF?R-1 and TGF?R-2, pharmaceutical compositions containing said compounds and methods of treating proliferative disorders and disorders of dysregulated apoptosis, such as cancer, utilizing the compounds of the invention.
    Type: Grant
    Filed: July 27, 2016
    Date of Patent: September 3, 2019
    Assignee: Bristol-Myer Squibb Company
    Inventors: Lalgudi S. Harikrishnan, Brian E. Fink, Robert M. Borzilleri, Gopikishan Tonukunuru, Jayakumar Sankara Warrier
  • TGF? receptor antagonist
    Patent number: 10336761
    Abstract: The invention relates generally to compounds that modulate the activity of TGF?R-1 and TGF? R-2, pharmaceutical compositions containing said compounds and methods of treating proliferative disorders and disorders of dysregulated apoptosis, such as cancer, utilizing the compounds of the invention.
    Type: Grant
    Filed: July 21, 2016
    Date of Patent: July 2, 2019
    Assignee: Bristol-Myers Squibb Company
    Inventors: Lalgudi S. Harikrishnan, Brian E. Fink, Robert M. Borzilleri, Gopikishan Tonukunuru, Hasibur Rahaman, Jayakumar Sankara Warrier, Balaji Seshadri
  • TGF beta receptor antagonists
    Patent number: 10292985
    Abstract: The invention relates generally to compounds that modulate the activity of TGFBETA R-1 and TGFBETA R-2, pharmaceutical compositions containing said compounds and methods of treating proliferative disorders and disorders of dysregulated apoptosis, such as cancer, utilizing the compounds of the invention.
    Type: Grant
    Filed: August 30, 2016
    Date of Patent: May 21, 2019
    Assignee: Bristol-Myers Squibb Company
    Inventors: Robert M. Borzilleri, Brian E. Fink, Lalgudi S. Harikrishnan, Jayakumar Sankara Warrier
  • TGF-? inhibitors
    Patent number: 10287295
    Abstract: Disclosed are imidazole and thiazole compounds, as well as pharmaceutical compositions and methods of use thereof. One embodiment is a compound having the structure and pharmaceutically acceptable salts, prodrugs and N-oxides thereof (and solvates and hydrates thereof), wherein X, A, Z, R1 and R? are as described herein. In certain embodiments, a compound disclosed herein inhibits TGF-?, and can be used to treat disease by blocking TGF-? signaling.
    Type: Grant
    Filed: January 2, 2018
    Date of Patent: May 14, 2019
    Assignees: Rigel Pharmaceuticals, Inc., Bristol-Meyers Squibb Company
    Inventors: Todd Kinsella, Marina Gelman, Hui Hong, Ihab S. Darwish, Rajinder Singh, Jiaxin Yu, Robert M. Borzilleri, Upender Velaparthi, Peiying Liu, Chetan Padmakar Darne, Hasibur Rahaman, Jayakumar Sankara Warrier
  • Benzodiazepine dimers, conjugates thereof, and methods of making and using
    Patent number: 10112975
    Abstract: Benzodiazepine dimers having a structure represented by wherein R1 is wherein the variables in formulae (I), (Ia), and (Ib) are as defined in the application. Such dimers are useful as anti-cancer agents, especially when used in an antibody-drug conjugate (ADC).
    Type: Grant
    Filed: October 17, 2017
    Date of Patent: October 30, 2018
    Assignee: Briston-Myers Squibb Company
    Inventors: Yong Zhang, Ivar M. McDonald, Naidu S. Chowdari, Tram N. Huynh, Robert M. Borzilleri, Sanjeev Gangwar
  • Tubulysin analogs and methods of making and use
    Patent number: 10077287
    Abstract: Tubulysin analogs of the formula (I) where R1, R2 R3, R4, R5, R6, R7, and Y are as defined herein, are anti-mitotic agents that can be used in the treatment of cancer, especially when conjugated to a targeting moiety.
    Type: Grant
    Filed: August 24, 2015
    Date of Patent: September 18, 2018
    Assignee: Bristol-Myers Squibb Company
    Inventors: Heidi L. Perez, Donna Wei, Robert M. Borzilleri, Sanjeev Gangwar, Gretchen M. Schroeder, Heng Cheng, Robert J. Schmidt
  • TGF BETA RECEPTOR ANTAGONISTS
    Publication number: 20180250303
    Abstract: The invention relates generally to compounds of formula (I) that modulate the activity of TGF?R-1 and TGF?R-2, pharmaceutical compositions containing said compounds and methods of treating proliferative disorders and disorders of dysregulated apoptosis, such as cancer, utilizing the compounds of the invention.
    Type: Application
    Filed: August 23, 2016
    Publication date: September 6, 2018
    Inventors: Robert M. Borzilleri, Brian E. Fink, Lalgudi S. Harikrishnan, Upender Velaparthi, Vishweshwaraiah Baligar, Hasibur Rahaman, Jayakumar Sankara Warrier
  • TGF BETA RECEPTOR ANTAGONISTS
    Publication number: 20180243312
    Abstract: The invention relates generally to compounds that modulate the activity of TGFBETA R-1 and TGFBETA R-2, pharmaceutical compositions containing said compounds and methods of treating proliferative disorders and disorders of dysregulated apoptosis, such as cancer, utilizing the compounds of the invention.
    Type: Application
    Filed: August 30, 2016
    Publication date: August 30, 2018
    Inventors: Robert M. BORZILLERI, Brian E. Fink, Lalgudi S. Harikrishnan, Jayakumar Sankara Warrier
  • TGF BETA RECEPTOR ANTAGONISTS
    Publication number: 20180215761
    Abstract: The invention relates generally to compounds that modulate the activity of TGF?R-1 and TGF? R-2, pharmaceutical compositions containing said compounds and methods of treating proliferative disorders and disorders of dysregulated apoptosis, such as cancer, utilizing the compounds of the invention.
    Type: Application
    Filed: July 21, 2016
    Publication date: August 2, 2018
    Inventors: Lalgudi S. HARIKRISHNAN, Brian E. FINK, Robert M. BORZILLERI, Gopikishan TONUKUNURU, Hasibur RAHAMAN, Jayakumar SANKARA WARRIER, Balaji SESHADRI
  • TGF BETA RECEPTOR ANTAGONISTS
    Publication number: 20180215762
    Abstract: The invention relates generally to compounds that modulate the activity of TGF?R-1 and TGF?R-2, pharmaceutical compositions containing said compounds and methods of treating proliferative disorders and disorders of dysregulated apoptosis, such as cancer, utilizing the compounds of the invention.
    Type: Application
    Filed: July 27, 2016
    Publication date: August 2, 2018
    Inventors: Lalgudi S. HARIKRISHNAN, Brian E. Fink, Robert M. Borzilleri, Gopikishan Tonukunuru, Jayakumar Sankara Warrier
  • GDF-8 inhibitors
    Patent number: 9981944
    Abstract: Disclosed are 2,2?-bipyridyl compounds, as well as pharmaceutical compositions and methods of use thereof. One embodiment is a compound having the structure and pharmaceutically acceptable salts, prodrugs and N-oxides thereof (and solvates and hydrates thereof), wherein R1, Z and n are as described herein. In certain embodiments, a compound disclosed herein inhibits GDF8, and can be used to treat disease by blocking GDF8 signaling.
    Type: Grant
    Filed: February 15, 2016
    Date of Patent: May 29, 2018
    Assignees: RIGEL PHARMACEUTICALS, INC, BRISTOL-MYERS SQUIBB COMPANY
    Inventors: Pingyu Ding, Marina Gelman, Todd Kinsella, Rajinder Singh, Somasekhar Bhamidipati, Upender Velaparthi, Robert M. Borzilleri, Hasibur Rahaman, Jayakumar Sankara Warrier
  • TGF-Beta Inhibitors
    Publication number: 20180127426
    Abstract: Disclosed are imidazole and thiazole compounds, as well as pharmaceutical compositions and methods of use thereof. One embodiment is a compound having the structure and pharmaceutically acceptable salts, prodrugs and N-oxides thereof (and solvates and hydrates thereof), wherein X, A, Z, R1 and R? are as described herein. In certain embodiments, a compound disclosed herein inhibits TGF-?, and can be used to treat disease by blocking TGF-? signaling.
    Type: Application
    Filed: January 2, 2018
    Publication date: May 10, 2018
    Inventors: Todd Kinsella, Marina Gelman, Hui Hong, Ihab S. Darwish, Rajinder Singh, Jiaxin Yu, Robert M. Borzilleri, Upender Velaparthi, Peiying Liu, Chetan Darne, Hasibur Rahaman, Jayakumar Sankara Warrier
  • BENZODIAZEPINE DIMERS, CONJUGATES THEREOF, AND METHODS OF MAKING AND USING
    Publication number: 20180079781
    Abstract: Benzodiazepine dimers having a structure represented by wherein R1 is wherein the variables in formulae (I), (Ia), and (Ib) are as defined in the application. Such dimers are useful as anti-cancer agents, especially when used in an antibody-drug conjugate (ADC).
    Type: Application
    Filed: October 17, 2017
    Publication date: March 22, 2018
    Inventors: Yong ZHANG, Ivar M. MCDONALD, Naidu S. CHOWDARI, Tram N. HUYNH, Robert M. BORZILLERI, Sanjeev GANGWAR
  • Macrocyclic benzodiazepine dimers, conjugates thereof, preparation and uses
    Patent number: 9902740
    Abstract: Macrocyclic benzodiazepine dimers having a structure represented by formula I where A and B are independently according to formulae Ia or Ib and the other variables in formulae I, Ia, and Ib are as defined in the application. Such dimers are useful as anti-cancer agents, especially when used as the drug component in an antibody-drug conjugate (ADC).
    Type: Grant
    Filed: May 26, 2017
    Date of Patent: February 27, 2018
    Assignee: Bristol-Myers Squibb Company
    Inventors: Yong Zhang, Robert M. Borzilleri, Andrew J. Tebben, Erik M. Stang, Andrew F. Donnell, Gretchen M. Schroeder, Heidi L. Perez, Donna D. Wei
  • HETEROARYLENE-BRIDGED BENZODIAZEPINE DIMERS, CONJUGATES THEREOF, AND METHODS OF MAKING AND USING
    Publication number: 20180037581
    Abstract: Benzodiazepine dimers having a structure represented by wherein X comprises a heteroaromatic moiety and is as further defined in the application; R1 is and the other variables in formulae (I), (Ia), and (Ib) are as defined in the application. Such dimers are useful as anti-cancer agents, especially when used in an antibody-drug conjugate (ADC).
    Type: Application
    Filed: October 17, 2017
    Publication date: February 8, 2018
    Inventors: Ivar M. MCDONALD, Naidu S. CHOWDARI, Walter Lewis JOHNSON, Yong ZHANG, Robert M. BORZILLERI, Sanjeev GANGWAR