Patents by Inventor Lawrence R. Marcin

Lawrence R. Marcin 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).

  • Publication number: 20210246136
    Abstract: The present invention provides compounds of Formula (I): or stereoisomers, tautomers, or pharmaceutically acceptable salts or solvates thereof, wherein all the variables are as defined herein. These compounds are antagonists to ?v-containing integrins. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating a disease, disorder, or condition associated with dysregulation of ?v-containing integrins, such as pathological fibrosis, transplant rejection, cancer, osteoporosis, and inflammatory disorders, by using the compounds and pharmaceutical compositions.
    Type: Application
    Filed: March 25, 2021
    Publication date: August 12, 2021
    Inventors: Pratik Devasthale, Fang Moore, Guohua Zhao, Susan Nicole Pieniazek, Kumaravel Selvakumar, Suresh Dhanusu, Manoranjan Panda, Lawrence R. Marcin
  • Patent number: 11014922
    Abstract: The present invention provides compounds of Formula (I): or stereoisomers, tautomers, or pharmaceutically acceptable salts or solvates thereof, wherein all the variables are as defined herein. These compounds are antagonists to ?v-containing integrins. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating a disease, disorder, or condition associated with dysregulation of av-containing integrins, such as pathological fibrosis, transplant rejection, cancer, osteoporosis, and inflammatory disorders, by using the compounds and pharmaceutical compositions.
    Type: Grant
    Filed: November 7, 2017
    Date of Patent: May 25, 2021
    Assignee: Bristol-Myers Squibb Company
    Inventors: Pratik Devasthale, Fang Moore, Guohua Zhao, Susan Nicole Pieniazek, Kumaravel Selvakumar, Suresh Dhanusu, Manoranjan Panda, Lawrence R. Marcin
  • Publication number: 20190270741
    Abstract: The present invention provides compounds of Formula (I): or stereoisomers, tautomers, or pharmaceutically acceptable salts or solvates thereof, wherein all the variables are as defined herein. These compounds are antagonists to ?v-containing integrins. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating a disease, disorder, or condition associated with dysregulation of ?v-containing integrins, such as pathological fibrosis, transplant rejection, cancer, osteoporosis, and inflammatory disorders, by using the compounds and pharmaceutical compositions.
    Type: Application
    Filed: November 7, 2017
    Publication date: September 5, 2019
    Applicant: BRISTOL-MYERS SQUIBB COMPANY
    Inventors: Pratik DEVASTHALE, Fang MOORE, Guohua ZHAO, Susan Nicole PIENIAZEK, Kumaravel SELVAKUMAR, Suresh DHANUSU, Manoranjan PANDA, Lawrence R. MARCIN
  • Patent number: 10112944
    Abstract: Disclosed are compounds of Formula (I) or a salt thereof, wherein: X is CR6 or N; W is: (i) —(CR3R3)1-4— or (ii) —(CR3R3)x-Y—(CR3R3)y-; and Y, R1, R2, R3, R5, R6, R7, x, and y are define herein. Also disclosed are methods of using such compounds as modulators of TNF?, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating inflammatory and autoimmune diseases.
    Type: Grant
    Filed: March 17, 2016
    Date of Patent: October 30, 2018
    Assignee: Bristol-Myers Squibb Company
    Inventors: Lawrence R. Marcin, Stephen T. Wrobleski, T.G. Murali Dhar
  • Publication number: 20180072728
    Abstract: Disclosed are compounds of Formula (I) or a salt thereof, wherein: X is CR6 or N; W is: (i) —(CR3R3)1-4— or (ii) —(CR3R3)x-Y—(CR3R3)y-; and Y, R1, R2, R3, R5, R6, R7, x, and y are define herein. Also disclosed are methods of using such compounds as modulators of TNF?, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating inflammatory and autoimmune diseases.
    Type: Application
    Filed: March 17, 2016
    Publication date: March 15, 2018
    Inventors: Lawrence R. MARCIN, Stephen T. WROBLESKI, Murali T.G. DHAR
  • Patent number: 9738642
    Abstract: The disclosure generally relates to compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds modulate the mGluR2 receptor and may be useful for the treatment of various disorders of the central nervous system.
    Type: Grant
    Filed: September 18, 2014
    Date of Patent: August 22, 2017
    Assignee: Bristol-Myers Squibb Company
    Inventors: Lawrence R. Marcin, Mendi A. Higgins, Joanne J. Bronson, F. Christopher Zusi, John E. Macor, Min Ding
  • Publication number: 20160237081
    Abstract: The disclosure generally relates to compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds modulate the mGluR2 receptor and may be useful for the treatment of various disorders of the central nervous system.
    Type: Application
    Filed: September 18, 2014
    Publication date: August 18, 2016
    Inventors: Lawrence R. Marcin, Mendi A. Higgins, Joanne J. Bronson, F. Christopher Zusi, John E. Macor, Min Ding
  • Patent number: 8604024
    Abstract: Compounds of formula (I), including pharmaceutically acceptable salts thereof, are set forth herein: wherein X is selected from the group of CH2, O, and NR2; m=0 or 1; R1 at each instance is selected from the group of halogen, hydroxy, amino, C1-4alkylamino, C1-4dialkylamino, haloC1-4 alkyl, CN, C1-C6 alkyl or cycloalkyl, C1-C6 alkoxy, and C2-C4 alkynyl; L is a bond, —NHCO—, —NH—, or L and Z together can be absent; Z is a C6-C10-aryl group or a 5-10 membered heterocyclic group which can be further substituted with from 0-3 substituents selected from the group of halogen, haloC1-4 alkoxy, 4-methoxyphenyl, hydroxy, amino, C1-4alkylamino, C1-4dialkylamino, haloC1-4 alkyl, CN, C1-C6 alkyl or cycloalkyl, C1-C6 alkoxy, and C2-C4 alkynyl; R2 is selected from the group of hydrogen, benzyl, C1-C6 alkyl or cycloalkyl, C1-C6 alkoxy, acetyl, and methanesulfonyl; and R3, R4 and R5 are independently selected from hydrogen or C1-4alkyl.
    Type: Grant
    Filed: May 22, 2012
    Date of Patent: December 10, 2013
    Assignee: Bristol-Myers Squibb Company
    Inventors: Lorin A. Thompson, III, Jianliang Shi, Yong-Jin Wu, Lawrence R. Marcin, Ramkumar Rajamani, Mendi A. Higgins
  • Patent number: 8513253
    Abstract: There is provided a series of novel ?-(N-sulfonamido)acetamide compounds of the Formula (I) wherein R, R1, R2 and R3 are defined herein, which are inhibitors of ?-amyloid peptide (?-AP) production and are useful in the treatment of Alzheimer's Disease and other conditions affected by anti-amyloid activity.
    Type: Grant
    Filed: July 21, 2010
    Date of Patent: August 20, 2013
    Assignee: Bristol-Myers Squibb Company
    Inventors: Michael F. Parker, Katharine E. McElhone, Robert A. Mate, Joanne J. Bronson, Yonghua Gai, Carl P. Bergstrom, Lawrence R. Marcin, John E. Macor
  • Publication number: 20130131051
    Abstract: Compounds of formula (I), including pharmaceutically acceptable salts thereof, are set forth herein: wherein X is selected from the group of CH2, O, and NR2; m=0 or 1; R1 at each instance is selected from the group of halogen, hydroxy, amino, C1-4alkylamino, C1-4dialkylamino, haloC1-4 alkyl, CN, C1-C6 alkyl or cycloalkyl, C1-C6 alkoxy, and C2-C4 alkynyl; L is a bond, —NHCO—, —NH—, or L and Z together can be absent; Z is a C6-C10-aryl group or a 5-10 membered heterocyclic group which can be further substituted with from 0-3 substituents selected from the group of halogen, haloC1-4 alkoxy, 4-methoxyphenyl, hydroxy, amino, C1-4alkylamino, C1-4dialkylamino, haloC1-4 alkyl, CN, C1-C6 alkyl or cycloalkyl, C1-C6 alkoxy, and C2-C4 alkynyl; R2 is selected from the group of hydrogen, benzyl, C1-C6 alkyl or cycloalkyl, C1-C6 alkoxy, acetyl, and methanesulfonyl; and R3, R4 and R5 are independently selected from hydrogen or C1-4alkyl.
    Type: Application
    Filed: May 22, 2012
    Publication date: May 23, 2013
    Inventors: LORIN A. THOMPSON, III, Jianliang Shi, Yong-Jin Wu, Lawrence R. Marcin, Ramkumar Rajamani, Mendi A. Higgins
  • Patent number: 8349880
    Abstract: The present disclosure provides a series of compounds of the formula (I) which reduce ?-amyloid peptide (?-AP) production and are useful in the treatment of Alzheimer's Disease and other conditions affected by ?-amyloid peptide (?-AP) production.
    Type: Grant
    Filed: January 7, 2010
    Date of Patent: January 8, 2013
    Assignee: Bristol-Myers Squibb Company
    Inventors: Lawrence R. Marcin, Lorin A. Thompson, III, Kenneth M. Boy, Jason M. Guernon, Mendi A. Higgins, Jianliang Shi, Yong-Jin Wu, Yunhui Zhang, John E. Macor
  • Patent number: 8350084
    Abstract: The present invention provides a novel alpha-(N-sulfonamido)acetamide compound, its pharmaceutical composition, processes thereof and a method for the treatment of Alzheimer's disease and other conditions associated with ?-amyloid peptide.
    Type: Grant
    Filed: November 18, 2011
    Date of Patent: January 8, 2013
    Assignee: Bristol-Myers Squibb Company
    Inventors: John E. Starrett, Jr., Kevin W. Gillman, Richard E. Olson, Lawrence R. Marcin, Bang-Chi Chen, Huiping Zhang
  • Publication number: 20120088925
    Abstract: The present invention provides a novel alpha-(N-sulfonamido)acetamide compound, its pharmaceutical composition, processes thereof and a method for the treatment of Alzheimer's disease and other conditions associated with ?-amyloid peptide.
    Type: Application
    Filed: November 18, 2011
    Publication date: April 12, 2012
    Inventors: John E. Starrett, JR., Kevin W. Gillman, Richard E. Olson, Lawrence R. Marcin, Bang-Chi Chen, Huiping Zhang
  • Publication number: 20110105485
    Abstract: There is provided a series of novel ?-(N-sulfonamido)acetamide compounds of the Formula (I) wherein R, R1, R2 and R3 are defined herein, which are inhibitors of ?-amyloid peptide (?-AP) production and are useful in the treatment of Alzheimer's Disease and other conditions affected by anti-amyloid activity.
    Type: Application
    Filed: July 21, 2010
    Publication date: May 5, 2011
    Inventors: Michael F. Parker, Katharine E. McElhone, Robert A. Mate, Joanne J. Bronson, Yonghua Gai, Carl P. Bergstrom, Lawrence R. Marcin, John E. Macor
  • Patent number: 7902218
    Abstract: There is provided a series of tetrahydroisoquinoline diaminopropane compounds of Formula (I) or a stereoisomer; or a pharmaceutically acceptable salt thereof, wherein R, R8 and R9 are as defined herein, their pharmaceutical compositions and methods of use. These compounds inhibit the processing of amyloid precursor protein (APP) by ?-secretase and, more specifically, inhibit the production of A?-peptide. The present disclosure is directed to compounds useful in the treatment of neurological disorders related to ?-amyloid production, such as Alzheimer's disease and other conditions affected by anti-amyloid activity.
    Type: Grant
    Filed: December 6, 2007
    Date of Patent: March 8, 2011
    Assignee: Bristol-Myers Squibb Company
    Inventors: Lorin A. Thompson, III, Kenneth M. Boy, Jianliang Shi, John E. Macor, Andrew C. Good, Lawrence R. Marcin
  • Publication number: 20110015175
    Abstract: The present disclosure provides a series of compounds of the formula (I) which reduce ?-amyloid peptide (?-AP) production and are useful in the treatment of Alzheimer's Disease and other conditions affected by ?-amyloid peptide (?-AP) production.
    Type: Application
    Filed: January 7, 2010
    Publication date: January 20, 2011
    Inventors: Lawrence R. Marcin, Lorin A. Thompson, III, Kenneth M. Boy, Jason M. Guernon, Mendi A. Higgins, Jianliang Shi, Yong-Jin Wu, Yunhui Zhang, John E. Macor
  • Patent number: 7786122
    Abstract: There is provided a series of novel ?-(N-sulfonamido)acetamide compounds of the Formula (I) wherein R, R1, R2 and R3 are defined herein, which are inhibitors of ?-amyloid peptide (?-AP) production and are useful in the treatment of Alzheimer's Disease and other conditions affected by anti-amyloid activity.
    Type: Grant
    Filed: October 11, 2007
    Date of Patent: August 31, 2010
    Assignee: Bristol-Myers Squibb Company
    Inventors: Michael F. Parker, Katharine E. McElhone, Robert A. Mate, Joanne J. Bronson, Yonghua Gai, Carl P. Bergstrom, Lawrence R. Marcin, John E. Macor
  • Patent number: 7772221
    Abstract: There is provided a series of macrocyclic diaminopropanes of Formula (I) or a stereoisomer; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, m, n, W, X, Y, Z and L as defined herein, their pharmaceutical compositions and methods of use. These novel compounds inhibit the processing of amyloid precursor protein (APP) by ?-secretase and, more specifically, inhibit the production of A?-peptide. The present disclosure is directed to compounds useful in the treatment of neurological disorders related to ?-amyloid production, such as Alzheimer's disease and other conditions affected by anti-amyloid activity.
    Type: Grant
    Filed: January 25, 2008
    Date of Patent: August 10, 2010
    Assignee: Bristol-Meyers Squibb Company
    Inventors: Lawrence R. Marcin, Andrew C. Good, Yong-Jin Wu, Dmitry S. Zuev, Richard E. Olson, Nenghui Wang
  • Publication number: 20080194535
    Abstract: There is provided a series of macrocyclic diaminopropanes of Formula (I) or a stereoisomer; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, m, n, W, X, Y, Z and L as defined herein, their pharmaceutical compositions and methods of use. These novel compounds inhibit the processing of amyloid precursor protein (APP) by ?-secretase and, more specifically, inhibit the production of A?-peptide. The present disclosure is directed to compounds useful in the treatment of neurological disorders related to ?-amyloid production, such as Alzheimer's disease and other conditions affected by anti-amyloid activity.
    Type: Application
    Filed: January 25, 2008
    Publication date: August 14, 2008
    Inventors: Lawrence R. Marcin, Andrew C. Good, Yong-Jin Wu, Dmitry S. Zuev, Richard E. Olson, Nenghui Wang
  • Publication number: 20080153868
    Abstract: There is provided a series of tetrahydroisoquinoline diaminopropane compounds of Formula (I) or a stereoisomer; or a pharmaceutically acceptable salt thereof, wherein R, R8 and R9 are as defined herein, their pharmaceutical compositions and methods of use. These compounds inhibit the processing of amyloid precursor protein (APP) by ?-secretase and, more specifically, inhibit the production of A?-peptide. The present disclosure is directed to compounds useful in the treatment of neurological disorders related to ?-amyloid production, such as Alzheimer's disease and other conditions affected by anti-amyloid activity.
    Type: Application
    Filed: December 6, 2007
    Publication date: June 26, 2008
    Inventors: Lorin A. Thompson, Kenneth M. Boy, Jianliang Shi, John E. Macor, Andrew C. Good, Lawrence R. Marcin