Patents Represented by Attorney, Agent or Law Firm Kenneth B. Rubin
  • Patent number: 6589952
    Abstract: Provided herein are novel imidazo[1,2-a]pyrazines of Formula I: wherein: X is CHR5, NR5, O, S, S(O)n or a single bond, wherein n is equal to 0, 1 or 2; D is aryl or heteroaryl attached through an unsaturated carbon atom and wherein said aryl or heteroaryl is optionally substituted at any available position with from 1-5 of A1, A2, A3, A4 and A5; R2 is C1-4 alkyl or C3-8 cycloalkyl, each of which is optionally substituted with from 1-3 hydroxy, halogen or C1-4 alkoxy, or wherein when X is a bond, R2 is optionally also CN, CF3, C2F5, C1-4 alkyl or C3-8 cycloalkyl, each of which C1-4 alkyl or C3-8 cycloalkyl is optionally substituted with from 1-3 hydroxy, halogen and C1-4 alkoxy; as well as compositions containing the same, useful in the treatment of, for example, neurological and psychological disorders characterized by corticotropin releasing factor (CRF) overexpression.
    Type: Grant
    Filed: July 13, 2001
    Date of Patent: July 8, 2003
    Assignee: Bristol-Myers Squibb Pharma Company
    Inventors: Rajagopal Bakthavatchalam, Richard G. Wilde, Paul J. Gilligan
  • Patent number: 6448261
    Abstract: Corticotropin releasing factor (CRF) antagonists of formula I; and their use in treating anxiety, depression, and other psychiatric and neurological disorders.
    Type: Grant
    Filed: March 14, 2000
    Date of Patent: September 10, 2002
    Assignee: Bristol-Myers Squibb Pharma Company
    Inventors: Rajagopal Bakthavatchalam, Argyrios Georgios Arvanitis, James Peter Beck, Gary Avonn Cain, Robert John Chorvat, Paul Joseph Gilligan, Richard Eric Olson
  • Patent number: 6399609
    Abstract: Corticotropin releasing factor (CRF) antagonists of formula I: and their use in treating anxiety, depression, and other psychiatric and neurological disorders.
    Type: Grant
    Filed: May 11, 2000
    Date of Patent: June 4, 2002
    Assignee: Bristol-Myers Squibb Pharma Company
    Inventor: Richard Gerald Wilde
  • Patent number: 6365589
    Abstract: The present invention describes novel imidazo-pyridines, -pyridazines, and -triazines of formula I: wherein A and B can be C or N and D is aryl or heteroaryl or pharmaceutically acceptable salt forms thereof, which are useful as CRF antagonists.
    Type: Grant
    Filed: June 25, 1999
    Date of Patent: April 2, 2002
    Assignee: Bristol-Myers Squibb Pharma Company
    Inventors: Paul Joseph Gilligan, Richard Eric Olson, William Eric Frietze
  • Patent number: 6362344
    Abstract: Chiral aminoalcohol catalysts and methods for their preparation are provided. The first catalyst is prepared via selective hydrogenation of one of two benzene rings in a precursor. The aminoalcohol promotes the asymmetric addition of organozinc reagents to aldehydes to afford optically active alcohols or their esters. The second catalyst is prepared by selective dialkylation of 3-exo-aminoisoborneol with a 2-haloethyl ether. The aminoalcohol promotes the addition of organozinc reagents to aliphatic aldehydes containing a &bgr;-branch with greatly enhanced enantioselectivity relative to DAIB.
    Type: Grant
    Filed: September 26, 2000
    Date of Patent: March 26, 2002
    Assignee: Bristol-Myers Squibb Pharma Company
    Inventor: William A. Nugent
  • Patent number: 6342503
    Abstract: The present invention provides novel compounds, compounds and pharmaceutical compositions thereof, and methods of using same in the treatment of affective disorders, anxiety, depression, post-traumatic stress disorders, eating disorders, supranuclear palsy, irritable bowel syndrome, immune suppression, Alzheimer'disease, gastrointestinal diseases, anorexia nervosa, drug and alcohol withdrawal symptoms, drug addiction, inflammatory disorders, or fertility problems. The novel compounds provided by this invention are those of formula: wherein R1, R3, R4, R5, Z, Y, V, X, X′, J, K, L, and M are as defined herein.
    Type: Grant
    Filed: January 7, 1998
    Date of Patent: January 29, 2002
    Assignee: DuPont Pharmaceuticals Company
    Inventors: Paul Edward Aldrich, Argyrios Georgios Arvanitis, Robert Scott Cheeseman, Robert John Chorvat, Thomas Eugene Christos, Paul Joseph Gilligan, Dimitri Emil Grigoriadis, Carl Nicholas Hodge, Paul John Krenitsky, Everett Latham Scholfield, Sang William Tam, Zelda Rakowitz Wasserman
  • Patent number: 6326162
    Abstract: This invention is directed to assays to determine the presence or absence of proteins that exhibit aggrecanase or ADMP activity. This invention also relates to peptides that acts as a substrates for ADMPs, their use in various assays to determine the presence or absence of ADMP activity, and their use as inhibitors of ADMP activity.
    Type: Grant
    Filed: July 24, 1998
    Date of Patent: December 4, 2001
    Assignee: Bristol-Myers Squibb Pharma Company
    Inventors: Jeffrey A. Miller, Elizabeth C. Arner, Robert A. Copeland, Gary L. Davis, Ruiqin Liu, Michael Pratta, Micky D. Tortorella
  • Patent number: 6326368
    Abstract: The present invention provides novel compounds, and pharmaceutical compositions thereof, and methods of using same in the treatment of affective disorders, anxiety, depression, post-traumatic stress disorders, eating disorders, supranuclear palsey, irritable bowl syndrome, immune supression, Alzheimer's disease, gastrointestinal diseases, anorexia nervosa, drug and alcohol withdrawal symptoms, drug addiction, inflammatory disorders, or fertility problems. The novel compounds provided by this invention are those of formula: wherein R1, R3, R5, Q, Z, Y, V, X and X′ are as defined herein.
    Type: Grant
    Filed: March 13, 1997
    Date of Patent: December 4, 2001
    Assignee: DuPont Pharmaceuticals Company
    Inventors: Robert John Chorvat, Parthasarathi Rajagopalan
  • Patent number: 6294671
    Abstract: The present invention describes novel isoxazolo[1,5-a]pyrimidines of formula: wherein R is an aromatic or heteroaromatic ring, or pharmaceutically acceptable salt form thereof, which are useful as CRF antagonists.
    Type: Grant
    Filed: August 20, 1999
    Date of Patent: September 25, 2001
    Assignee: DuPont Pharmaceuticals Company
    Inventor: William Eric Frietze
  • Patent number: 6271380
    Abstract: Corticotropin releasing factor (CRF) antagonists of formula I: and their use in treating anxiety, depression, and other psychiatric, neurological disorders as well as treatment of immunological, cardiovascular or heart-related diseases and colonic hypersensitivity associated with psychopathological disturbance and stress.
    Type: Grant
    Filed: December 28, 1999
    Date of Patent: August 7, 2001
    Assignee: DuPont Pharmaceuticals Company
    Inventors: Paul Joseph Gilligan, Rajagopal Bakthavatchalam
  • Patent number: 6262081
    Abstract: The invention relates to a method of treating neurological disorders associated with neurotransmitter deficit in a mammal comprising administering to the mammal a therapeutically effective amount of a combination of: (i) at least one neurotransmitter release enhancer, and (ii) at least one acetylcholinesterase inhibitor. The invention also relates to compositions and kits containing the same.
    Type: Grant
    Filed: July 8, 1999
    Date of Patent: July 17, 2001
    Assignee: DuPont Pharmaceuticals Company
    Inventor: Robert Zaczek
  • Patent number: 6258809
    Abstract: Novel compounds and pharmaceutical compositions thereof, and methods of using same in treating anxiety, depression, and other psychiatric and neurological disorders. The novel compounds provided by this invention are those of the following formulae: wherein R1, R13, X, Y, Z, G and Q are as defined herein.
    Type: Grant
    Filed: March 3, 2000
    Date of Patent: July 10, 2001
    Assignee: DuPont Pharmaceuticals Company
    Inventors: Parthasarathi Rajagopalan, Robert John Chorvat, Rajagopal Bakthavatchalam, James Peter Beck, Paul Joseph Gilligan, Richard Eric Olson
  • Patent number: 6187918
    Abstract: Novel chiral aminoalcohol catalysts and methods for their preparation are provided. The first catalyst is prepared via selective hydrogenation of one of two benzene rings in a precursor. The aminoalcohol promotes the asymmetric addition of organozinc reagents to aldehydes to afford optically active alcohols or their esters. The second catalyst is prepared by selective dialkylation of 3-exo-aminoisoborneol with a 2-haloethyl ether. The aminoalcohol promotes the addition of organozinc reagents to aliphatic aldehydes containing a &bgr;-branch with greatly enhanced enantioselectivity relative to DAIB.
    Type: Grant
    Filed: March 10, 2000
    Date of Patent: February 13, 2001
    Assignee: DuPont Pharmaceuticals Company
    Inventor: William A. Nugent
  • Patent number: 6143743
    Abstract: Corticotropin releasing factor (CRF) antagonists of formula (I): ##STR1## and their use in treating psychiatric disorders and neurological diseases, anxiety-related disorders, post-traumatic stress disorder, supranuclear palsy and feeding disorders as well as treatment of immunological, cardiovascular or heart-related diseases and colonic hypersensitivity associated with psychopathological disturbance and stress in mammals.
    Type: Grant
    Filed: July 2, 1998
    Date of Patent: November 7, 2000
    Assignee: Dupont Pharmaceuticals Company
    Inventors: Richard Gerald Wilde, Rajagopal Bakthavatchalam, James Peter Beck, Argyrios Georgious Arvanitis
  • Patent number: 6136833
    Abstract: Provided is a pharmaceutical composition comprising a tablet or capsule containing a pharmacologically effective amount of a pharmaceutical compound, or a pharmaceutically acceptable salt thereof, having an amidine-based group and an optional ester group, a pharmaceutically acceptable solid carrier, and a pharmaceutically acceptable acid in an amount to modify the pH of the composition to substantially that of the compound at pH of maximum stability.Such a composition is prepared by adding water during formulation manufacture and contacting the compound during formulation manufacture with a pharmaceutically acceptable acid having a pH in a saturated aqueous solution substantially that of the compound at pH of maximum stability.
    Type: Grant
    Filed: January 11, 1999
    Date of Patent: October 24, 2000
    Assignee: Dupont Pharmaceuticals Company
    Inventors: Sherif Ibrahim Farag Badawy, Donna Lynn Gilbert
  • Patent number: 6136809
    Abstract: Corticotropin releasing factor (CRF) antagonists of formula I or II: ##STR1## and their use in treating anxiety, depression, and other psychiatric, neurological disorders as well as treatment of immunological, cardiovascular or heart-related diseases and colonic hypersensitivity associated with psychopathological disturbance and stress.
    Type: Grant
    Filed: January 28, 1998
    Date of Patent: October 24, 2000
    Assignee: Dupont Pharmaceuticals
    Inventors: Paul Gilligan, Robert Chorvat
  • Patent number: 6124300
    Abstract: Novel compounds and pharmaceutical compositions thereof, and methods of using same in treating anxiety, depression, and other psychiatric and neurological disorders. The novel compounds provided by this invention are those of the following formulae: ##STR1## wherein R.sup.1, R.sup.13, X, Y, Z, G and Q are as defined herein.
    Type: Grant
    Filed: March 20, 1997
    Date of Patent: September 26, 2000
    Assignee: DuPont Pharmaceuticals
    Inventors: Parthasarathi Rajagopalan, Robert John Chorvat, Rajagopal Bakthavatchalam, James Peter Beck, Paul Joseph Gilligan, Richard Eric Olson
  • Patent number: 6124289
    Abstract: Corticotropin releasing factor (CRF) antagonists of formula I or II: ##STR1## and their use in treating anxiety, depression, and other psychiatric, neurological disorders as well as treatment of immunological, cardiovascular or heart-related diseases and colonic hypersensitivityassociated with psychopathological disturbance andstress.
    Type: Grant
    Filed: July 23, 1997
    Date of Patent: September 26, 2000
    Assignee: Dupont Pharmaceuticals Co.
    Inventors: Liqi He, Paul Joseph Gilligan, Argyrios Georgios Arvanitis, Robert John Chorvat
  • Patent number: 6124463
    Abstract: The present invention describes novel benzimidazoles of formula: ##STR1## or pharmaceutically acceptable salt forms thereof, which are useful as CRF antagonists.
    Type: Grant
    Filed: June 14, 1999
    Date of Patent: September 26, 2000
    Assignee: DuPont Pharmaceuticals
    Inventors: James Peter Beck, Matthew Allen Curry
  • Patent number: 6107294
    Abstract: The present invention describes novel thiazolo[4,5-d]pyrimidines of formula: ##STR1## wherein R.sup.3 is a substituted aromatic or heteroaromatic group, or pharmaceutically acceptable salt forms thereof, which are useful as CRF antagonists.
    Type: Grant
    Filed: March 31, 1999
    Date of Patent: August 22, 2000
    Assignee: Dupont Pharmaceuticals
    Inventor: James Peter Beck