Patents Represented by Attorney, Agent or Law Firm Kenneth B. Rubin
-
Patent number: 6589952Abstract: 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: GrantFiled: July 13, 2001Date of Patent: July 8, 2003Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Rajagopal Bakthavatchalam, Richard G. Wilde, Paul J. Gilligan
-
Patent number: 6448261Abstract: Corticotropin releasing factor (CRF) antagonists of formula I; and their use in treating anxiety, depression, and other psychiatric and neurological disorders.Type: GrantFiled: March 14, 2000Date of Patent: September 10, 2002Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Rajagopal Bakthavatchalam, Argyrios Georgios Arvanitis, James Peter Beck, Gary Avonn Cain, Robert John Chorvat, Paul Joseph Gilligan, Richard Eric Olson
-
Patent number: 6399609Abstract: Corticotropin releasing factor (CRF) antagonists of formula I: and their use in treating anxiety, depression, and other psychiatric and neurological disorders.Type: GrantFiled: May 11, 2000Date of Patent: June 4, 2002Assignee: Bristol-Myers Squibb Pharma CompanyInventor: Richard Gerald Wilde
-
Patent number: 6365589Abstract: 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: GrantFiled: June 25, 1999Date of Patent: April 2, 2002Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Paul Joseph Gilligan, Richard Eric Olson, William Eric Frietze
-
Patent number: 6362344Abstract: 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: GrantFiled: September 26, 2000Date of Patent: March 26, 2002Assignee: Bristol-Myers Squibb Pharma CompanyInventor: William A. Nugent
-
Patent number: 6342503Abstract: 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: GrantFiled: January 7, 1998Date of Patent: January 29, 2002Assignee: DuPont Pharmaceuticals CompanyInventors: 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: 6326368Abstract: 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: GrantFiled: March 13, 1997Date of Patent: December 4, 2001Assignee: DuPont Pharmaceuticals CompanyInventors: Robert John Chorvat, Parthasarathi Rajagopalan
-
Patent number: 6326162Abstract: 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: GrantFiled: July 24, 1998Date of Patent: December 4, 2001Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Jeffrey A. Miller, Elizabeth C. Arner, Robert A. Copeland, Gary L. Davis, Ruiqin Liu, Michael Pratta, Micky D. Tortorella
-
Patent number: 6294671Abstract: 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: GrantFiled: August 20, 1999Date of Patent: September 25, 2001Assignee: DuPont Pharmaceuticals CompanyInventor: William Eric Frietze
-
Patent number: 6271380Abstract: 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: GrantFiled: December 28, 1999Date of Patent: August 7, 2001Assignee: DuPont Pharmaceuticals CompanyInventors: Paul Joseph Gilligan, Rajagopal Bakthavatchalam
-
Patent number: 6262081Abstract: 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: GrantFiled: July 8, 1999Date of Patent: July 17, 2001Assignee: DuPont Pharmaceuticals CompanyInventor: Robert Zaczek
-
Patent number: 6258809Abstract: 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: GrantFiled: March 3, 2000Date of Patent: July 10, 2001Assignee: DuPont Pharmaceuticals CompanyInventors: Parthasarathi Rajagopalan, Robert John Chorvat, Rajagopal Bakthavatchalam, James Peter Beck, Paul Joseph Gilligan, Richard Eric Olson
-
Patent number: 6187918Abstract: 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: GrantFiled: March 10, 2000Date of Patent: February 13, 2001Assignee: DuPont Pharmaceuticals CompanyInventor: William A. Nugent
-
Patent number: 6143743Abstract: 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: GrantFiled: July 2, 1998Date of Patent: November 7, 2000Assignee: Dupont Pharmaceuticals CompanyInventors: Richard Gerald Wilde, Rajagopal Bakthavatchalam, James Peter Beck, Argyrios Georgious Arvanitis
-
Patent number: 6136833Abstract: 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: GrantFiled: January 11, 1999Date of Patent: October 24, 2000Assignee: Dupont Pharmaceuticals CompanyInventors: Sherif Ibrahim Farag Badawy, Donna Lynn Gilbert
-
Patent number: 6136809Abstract: 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: GrantFiled: January 28, 1998Date of Patent: October 24, 2000Assignee: Dupont PharmaceuticalsInventors: Paul Gilligan, Robert Chorvat
-
Patent number: 6124463Abstract: The present invention describes novel benzimidazoles of formula: ##STR1## or pharmaceutically acceptable salt forms thereof, which are useful as CRF antagonists.Type: GrantFiled: June 14, 1999Date of Patent: September 26, 2000Assignee: DuPont PharmaceuticalsInventors: James Peter Beck, Matthew Allen Curry
-
Patent number: 6124289Abstract: 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: GrantFiled: July 23, 1997Date of Patent: September 26, 2000Assignee: Dupont Pharmaceuticals Co.Inventors: Liqi He, Paul Joseph Gilligan, Argyrios Georgios Arvanitis, Robert John Chorvat
-
Patent number: 6124300Abstract: 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: GrantFiled: March 20, 1997Date of Patent: September 26, 2000Assignee: DuPont PharmaceuticalsInventors: Parthasarathi Rajagopalan, Robert John Chorvat, Rajagopal Bakthavatchalam, James Peter Beck, Paul Joseph Gilligan, Richard Eric Olson
-
Patent number: 6107301Abstract: 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'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: ##STR1## wherein R.sup.1, R.sup.3, R.sup.4, R.sup.5, Z, Y, V, X, X', J, K, L, and M are as defined herein.Type: GrantFiled: August 5, 1997Date of Patent: August 22, 2000Assignee: Dupont Pharmaceuticals CompanyInventors: Paul Edward Aldrich, Argyrios Georgios Arvanitis, Rajagopal Bakthavatchalam, James Peter Beck, Robert Scott Cheeseman, Robert John Chorvat, Paul Joseph Gilligan, Carl Nicholas Hodge, Zelda Rakowitz Wasserman