The Bicyclo Ring System Is 1,4-benzodiazepine (including Hydrogenated) Patents (Class 540/504)
  • Publication number: 20100113411
    Abstract: The present invention relates to CGRP antagonists of general formula wherein A, U, V, W, X and R1 to R3 are defined as in claim 1, the tautomers, diastereomers, enantiomers, hydrates, mixtures thereof and the salts thereof as well as the hydrates of the salts, particularly the physiologically acceptable salts thereof with inorganic or organic acids, pharmaceutical compositions containing these compounds, the use thereof and processes for preparing them.
    Type: Application
    Filed: August 6, 2009
    Publication date: May 6, 2010
    Applicant: BOEHRINGER INGELHEIM PHARMA GMBH & CO. KG
    Inventors: Klaus RUDOLF, Stephan Georg MUELLER, Dirk STENKAMP, Philipp LUSTENBERGER, Alexander DREYER, Eckhart BAUER, Marcus SCHINDLER, Kirsten ARNDT, Henri DOODS
  • Publication number: 20100004226
    Abstract: The present invention provides compositions and methods of using stereospecific benzodiazepine derivatives, their salts and prodrugs for the treatment of anxiolytic or convulsant disorders having the side effects of reduced alcohol craving in human alcoholics and a concomitant reduced sedative, hypnotic, muscle relaxant and ataxic side-effects. The invention further provides pharmaceutical compositions for treatment of anxiolytic and convulsant disorders in subjects in need thereof, comprising a compound, prodrug or a salt having a chemical structure represented by any one of Formula I-IV, VI-XI, XV-XVIII and XX-XXI and a pharmaceutically-acceptable carrier.
    Type: Application
    Filed: August 7, 2009
    Publication date: January 7, 2010
    Inventors: James M. Cook, Hao Zhou, Shengming Huang, P.V.V.S. Sarma, Chunchun Zhang
  • Publication number: 20100004227
    Abstract: The present invention relates to novel chemical compounds, methods for their discovery, and their therapeutic use. In particular, the present invention provides benzodiazepine derivatives and related compounds and methods of using benzodiazepine derivatives and related compounds as therapeutic agents to treat a number of conditions associated with the faulty regulation of the processes of programmed cell death, autoimmunity, inflammation, hyperproliferation, and the like.
    Type: Application
    Filed: June 8, 2007
    Publication date: January 7, 2010
    Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN
    Inventor: Gary D. Glick
  • Publication number: 20090253686
    Abstract: The present invention relates to systems and methods for generating new forms of benzodiazepine and benzodiazepine related compounds as well as new compounds and formulations generated by such methods. In particular, the present invention provides high throughput systems and methods for generating and identifying new crystalline benzodiazepine and benzodiazepine related polymorphs and new unsolvated, solvated, and other forms of the compounds that find use as improved drugs and drug formations.
    Type: Application
    Filed: May 27, 2009
    Publication date: October 8, 2009
    Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN
    Inventors: Gary D. Glick, Adam Matzger
  • Patent number: 7598237
    Abstract: This invention provides progesterone receptor modulators having the structure: wherein R1 to R7, X, and Q are as defined in the specification; or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: November 28, 2007
    Date of Patent: October 6, 2009
    Assignee: Wyeth
    Inventors: Puwen Zhang, Jay Edward Wrobel, Eugene Anthony Terefenko, Jeffrey Curtis Kern
  • Publication number: 20090221561
    Abstract: The described invention relates to compounds which modulate cell migration, and find use in, for example, wound healing, cancer progression and angiogenesis.
    Type: Application
    Filed: August 23, 2006
    Publication date: September 3, 2009
    Inventors: Ana Maria Schor, Seth Lawrence Schor, Rodolfo Marquez, David George Norman
  • Publication number: 20090215752
    Abstract: The invention relates to benzodiazepine derivatives having PDE2 inhibitory activities, as well as therapeutic methods of administering said compounds, in particular for treating various diseases of the central or peripheral nervous system. The invention further includes methods of preparing the subject compounds and pharmaceutical compositions containing them.
    Type: Application
    Filed: August 2, 2006
    Publication date: August 27, 2009
    Inventors: Mustapha Abarghaz, Stefano Biondi, Jérôme Duranton
  • Publication number: 20090209473
    Abstract: Angiogenesis may be initiated or increased through the use of gamma-secretase inhibitors. The gamma-secretase inhibitor can be a dipeptide class, sulfonamide class, transition state mimic class, benzodiazepine class, or benzocaprolactam class gamma secretase inhibitor. Methods for initiating and increasing angiogenesis are used for disease prevention and treatment as well as for generating research models.
    Type: Application
    Filed: February 19, 2009
    Publication date: August 20, 2009
    Inventors: Mats Hellstrom, Linda Karlsson-Lindahl, Elisabet Wallgard
  • Publication number: 20090203901
    Abstract: The present invention provides innovative strategies for synthesizing pyrazole ring-functionalized benzodiazepinones. Alternative intermediates and high conversion strategies for forming alpha-aminobenzophenone intermediates involve a combination of aromatic acylation, displacement of electronegative leaving groups with amine, and then N-displacement strategies to produce the desired alpha-aminobenzophenone with primary amine functionality. Reaction strategies are then provided for converting alpha-aminobenzophenones to alpha-aminoamidobenzophenone intermediates with high yield and convenient reaction strategies. These alpha-aminoamidobenzophenone intermediates are then converted into benzodiazepinones. These benzodiazepinones are then converted to pyrazole ring functionalized benzodiazepinones through a series of innovative intermediates and/or reaction strategies.
    Type: Application
    Filed: February 12, 2009
    Publication date: August 13, 2009
    Inventors: Peter J. Harrington, Valerie Grace Paulsen, Charles E. Tucker
  • Patent number: 7572783
    Abstract: The present invention relates to the compounds of Formula I, their preparation and pharmaceutical compositions comprising them. The compounds and pharmaceutical compositions are useful, for example, for the treatment and prevention of obesity, obesity-related disorders and eating disorders.
    Type: Grant
    Filed: August 12, 2005
    Date of Patent: August 11, 2009
    Assignee: Amgen Inc.
    Inventors: Xi Chen, Xiaoqi Chen, Richard Victor Connors, Kang Dai, Ying Fu, Juan C. Jaen, Yong-Jae Kim, Leping Li, Mike E. Lizarzaburu, Jeffrey T. Mihalic, Stephen J. Shuttleworth
  • Patent number: 7566707
    Abstract: The present invention relates to substituted imidazo-pyridinones and imidazo-pyridazinones of general formula wherein Y and R1 to R4 are defined as in claim 1, the tautomers, enantiomers, diastereomers, the mixtures thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).
    Type: Grant
    Filed: June 10, 2004
    Date of Patent: July 28, 2009
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Matthias Eckhardt, Norbert Hauel, Elke Langkopf, Frank Himmelsbach, Iris Kauffmann-Hefner, Mohammad Tadayyon, Michael Mark
  • Publication number: 20090170831
    Abstract: Field of the Invention This invention relates to novel lactams of Formula (I): having drug and bio-affecting properties, their pharmaceutical compositions and methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of A?-peptide, thereby acting to prevent the formation of neurological deposits of amyloid protein. More particularly, the present invention relates to the treatment of neurological disorders related to ?-amyloid production such as Alzheimer's disease and Down's Syndrome.
    Type: Application
    Filed: February 19, 2009
    Publication date: July 2, 2009
    Applicant: BRISTOL-MYERS SQUIBB PHARMA COMPANY
    Inventors: Qi Han, Hong Liu, Richard E. Olson, Michael G. Yang
  • Patent number: 7528249
    Abstract: This invention relates to novel cyclic malonamides having the formula (I): to their pharmaceutical compositions and to their methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of A?-peptide, thereby acting to prevent the formation of neurological deposits of amyloid protein. More particularly, the present invention relates to the treatment of neurological disorders related to ?-amyloid production such as Alzheimer's disease and Down's Syndrome.
    Type: Grant
    Filed: June 19, 2008
    Date of Patent: May 5, 2009
    Assignee: Bristol-Myers Squibb Pharma Company
    Inventors: Richard E. Olson, Michael G. Yang
  • Publication number: 20090093457
    Abstract: Disclosed are substituted xanthines of general formula wherein R1 to R4 are defined hereinbelow, the tautomers, the stereoisomers, the mixtures thereof, the prodrugs thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibitory effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).
    Type: Application
    Filed: December 10, 2008
    Publication date: April 9, 2009
    Applicant: BOEHRINGER INGELHEIM PHARMA GMBH & CO. KG
    Inventors: Frank HIMMELSBACH, Elke LANGKOPF, Matthias ECKHARDT, Roland MAIER, Michael MARK, Mohammad TADAYYON, Ralf R. H. LOTZ
  • Publication number: 20080293700
    Abstract: The present invention relates to novel chemical compounds, methods for their discovery, and their therapeutic use. In particular, the present invention provides benzodiazepine derivatives and methods of using benzodiazepine derivatives as therapeutic agents to treat a number of conditions associated with the faulty regulation of the processes of programmed cell death, autoimmunity, inflammation, and hyperproliferation, and the like.
    Type: Application
    Filed: September 7, 2005
    Publication date: November 27, 2008
    Inventor: Gary D. Glick
  • Publication number: 20080194546
    Abstract: There is provided a compound of formula I: wherein: one or two of X5, X6 and X8 is N, and the others are CH; R7 is selected from halo, ORO1, SRS1, NRN1RN2, NRN7aC(?O)RC1, NRN7bSO2RS2a, an optionally substituted C5-20 heteroaryl group, or an optionally substituted C5-20 aryl group, where RO1 and RS1 are selected from H, an optionally substituted C5-20 aryl group, an optionally substituted C5-20 heteroaryl group, or an optionally substituted C1-7 alkyl group; RN1 and RN2 are independently selected from H, an optionally substituted C1-7 alkyl group, an optionally substituted C5-20 heteroaryl group, an optionally substituted C5-20 aryl group or RN1 and RN2 together with the nitrogen to which they are bound form a heterocyclic ring containing between 3 and 8 ring atoms; RC1 is selected from H, an optionally substituted C5-20 aryl group, an optionally substituted C5-20 heteroaryl group, an optionally substituted C1-7 alkyl group or NRN8RN9, where RN8 and RN9 are independently selected from H, an optionally subs
    Type: Application
    Filed: August 21, 2007
    Publication date: August 14, 2008
    Applicant: KuDOS Pharmaceuticals Limited
    Inventors: Marc Geoffrey Hummersone, Gomez Sylvie, Keith Allan Menear, Graeme Cameron Murray Smith, Karine Malagu, Heather Mary Ellen Duggan, Niall Morrison Barr Martin, Frederic Georges Marie Leroux, Gesine Johanna Hermann, Xiao-Ling Fan Cockcroft
  • Patent number: 7410963
    Abstract: The invention relates to compounds having PDE2 inhibitory activities, as well as therapeutic methods by administering said compounds, in particular for treating various diseases of the central or peripheral nervous system. It further deals with pharmaceutical compositions comprising said compounds and methods for preparing said compounds.
    Type: Grant
    Filed: December 23, 2004
    Date of Patent: August 12, 2008
    Assignee: VIA Pharmaceuticals, Inc.
    Inventors: Mustapha Abarghaz, Stefano Biondi, Jérôme Duranton, Emmanuelle Limanton, Cesare Mondadori, Patrick Wagner
  • Publication number: 20080161292
    Abstract: Inhibitors of poly(ADP-ribose)polymerase, ways to make them and methods of treating patients using them are disclosed.
    Type: Application
    Filed: December 27, 2007
    Publication date: July 3, 2008
    Applicant: Abbott Laboratories
    Inventors: Vincent L. Giranda, Julie M. Miyashiro, Thomas D. Penning, Keith W. Woods
  • Patent number: 7390801
    Abstract: Disclosed are compounds which inhibit ?-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits ?-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.
    Type: Grant
    Filed: May 12, 2006
    Date of Patent: June 24, 2008
    Assignees: Athena Neurosciences, Inc., Eli Lilly and Company
    Inventors: Eugene D. Thorsett, Michael A. Pleiss, Lee H. Latimer, Varghese John, Stephen Freedman, Thomas C. Britton, James A. Audia, Jon K. Reel, Bruce A. Dressman, James J. Droste, Steven S. Henry, Russell D. Stucky, Warren J. Porter
  • Patent number: 7378411
    Abstract: The present invention relates to thienopyrimidinone compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.
    Type: Grant
    Filed: December 2, 2002
    Date of Patent: May 27, 2008
    Assignee: Merck & Co., Inc.
    Inventors: Mark E. Fraley, George D. Hartman, William F. Hoffman
  • Patent number: 7358239
    Abstract: The present invention concerns compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, wherein -Z1-Z2- is a bivalent radical; R1, R2 and R3 are each independently selected from hydrogen, C1-6alkyl, hydroxy, halo and the like; or when R1 and R2 are on adjacent carbon atoms, R1 and R2 taken together may form a bivalent radical of formula; Alk is optionally substituted C1-6alkanediyl; the bivalent radical is a substituted piperidinyl, an optionally substituted pyrrolidinyl, homopiperidinyl, piperazinyl or tropyl; R5 is a radical of formula wherein n is 1 or 2; p1 is 0, and p2 is 1 or 2; or p1 is 1 or 2, and p2 is 0; X is oxygen, sulfur or ?NR9; Y is oxygen or sulfur; R7 is hydrogen, C1-6alkyl, C3-6cycloalkyl, phenyl or phenylmethyl; R8 is C1-6alkyl, C3-6cycloalkyl phenyl or phenylmethyl; R9 is cyano, C1-6alkyl, C3-6cyclo-alkyl, C1-6alkyloxycarbonyl or aminocarbonyl; R10 is hydrogen or C1-6alkyl; and Q is
    Type: Grant
    Filed: March 14, 2005
    Date of Patent: April 15, 2008
    Assignee: Janssen Pharmaceutica, N.V.
    Inventors: Marcel Frans Leopold De Bruyn, Kristof Van Emelen, Piet Tom Bert Paul Wigerinck, Wim Gaston Verschueren
  • Patent number: 7262187
    Abstract: The present invention relates to azolopyrimidinone compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.
    Type: Grant
    Filed: December 2, 2002
    Date of Patent: August 28, 2007
    Assignee: Merck & Co., Inc.
    Inventors: Mark E. Fraley, George D. Hartman, William F. Hoffman
  • Patent number: 7262186
    Abstract: The present invention relates to azolopyriniidinone compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.
    Type: Grant
    Filed: December 2, 2002
    Date of Patent: August 28, 2007
    Assignee: Merck & Co., Inc.
    Inventors: Mark E. Fraley, George D. Hartman, William F. Hoffman
  • Patent number: 7250410
    Abstract: The invention concerns novel benzodiazepine derivatives and their uses in the field of therapeutics particularly for treating pathologies involving the activity of a cyclic nucleotide phosphodiesterase. It also concerns methods for preparing them and novel synthesis intermediates.
    Type: Grant
    Filed: June 7, 2002
    Date of Patent: July 31, 2007
    Assignee: Via Pharmaceuticals, Inc.
    Inventors: Jean-Jacques Bourguignon, Yan Lagouge, Claire Lugnier, Eveline Klotz, Jean-Paul Macher, Pierre Raboisson, Dominique Schultz
  • Patent number: 7244723
    Abstract: The present invention relates to furanopyrimidinone compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.
    Type: Grant
    Filed: December 2, 2002
    Date of Patent: July 17, 2007
    Assignee: Merck & Co., Inc.
    Inventors: Mark E. Fraley, George D. Hartman
  • Patent number: 7238685
    Abstract: The invention relates to novel benzo-fused heterocycles and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and especially their use as endothelin receptor antagonists.
    Type: Grant
    Filed: July 31, 2002
    Date of Patent: July 3, 2007
    Assignee: Actelion Pharmaceuticals Ltd.
    Inventors: Martin Bolli, Christoph Boss, Martine Clozel, Walter Fischli, Thomas Weller, Judith Marfurt
  • Patent number: 7192949
    Abstract: The present invention relates to cycloalkylpyrimidinone compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.
    Type: Grant
    Filed: April 24, 2006
    Date of Patent: March 20, 2007
    Assignee: Merck & Co., Inc.
    Inventors: Mark E. Fraley, Robert M. Garbaccio
  • Patent number: 7067512
    Abstract: The present invention is directed to novel 1,4-benzodiazepines, pharmaceutical compositions thereof, and the use thereof as inhibitors of HDM2-p53 interactions.
    Type: Grant
    Filed: November 13, 2002
    Date of Patent: June 27, 2006
    Inventors: Tianbao Lu, Louis V Lafrance, III, Daniel J Parks, Karen L Milkiewicz, Raul R Calvo, Maxwell D Cummings, Alexander J Kim, Bruce L Grasberger, Theodore E Carver, Jr.
  • Patent number: 7053084
    Abstract: This invention relates to novel lactams having the formula (I): to their pharmaceutical compositions and to their methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of A?-peptide, thereby acting to prevent the formation of neurological deposits of amyloid protein. More particularly, the present invention relates to the treatment of neurological disorders related to ?-amyloid production such as Alzheimer's disease and Down's Syndrome.
    Type: Grant
    Filed: February 17, 2000
    Date of Patent: May 30, 2006
    Assignee: Bristol-Myers Squibb Company
    Inventor: Richard E. Olson
  • Patent number: 6916805
    Abstract: This invention discloses quinoxalinones which display inhibitory effects on serine proteases such as factor Xa, thrombin, and/or factor VIIa. The invention also discloses pharmaceutically acceptable salts and prodrugs of the compounds, pharmaceutically acceptable compositions comprising the compounds, their salts or prodrugs, and methods of using them as therapeutic agents for treating or preventing disease states in mammals characterized by abnormal thrombosis.
    Type: Grant
    Filed: January 4, 2002
    Date of Patent: July 12, 2005
    Assignee: Warner-Lambert Company LLC
    Inventors: Danette Andrea Dudley, Jeremy John Edmunds
  • Patent number: 6838455
    Abstract: Disclosed are compounds which inhibit ?-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits ?-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.
    Type: Grant
    Filed: December 23, 2002
    Date of Patent: January 4, 2005
    Assignees: Athena Neurosciences, Inc., Eli Lilly & Company
    Inventors: James E. Audia, Warren J. Porter, Richard C. Thompson, Stephen C. Wilkie, Douglas R. Stack, Qing Shi
  • Patent number: 6825191
    Abstract: The present invention provides benzodiazepine derivatives of the following formula, analogs thereof and pharmaceutically acceptable salts thereof. The compounds of the present invention have an excellent effect of inhibiting activated blood-coagulation factor X. These compounds are usable as agents for treating various diseases concerned with the activated blood-coagulation factor X.
    Type: Grant
    Filed: March 27, 2003
    Date of Patent: November 30, 2004
    Assignee: Ajinomoto Co., Inc.
    Inventors: Tadakiyo Nakagawa, Munetaka Tokumasu, Kazumi Tashiro, Mitsuo Takahashi, Takashi Kayahara, Shunji Takehana, Yuki Kajigaya, Kaoru Yoshida, Kuniya Sakurai
  • Patent number: 6815543
    Abstract: Oxidation of organic compounds is catalyzed by addition of a catalytic amount of a metalloporphyrin in a non-reactive aprotic solvent.
    Type: Grant
    Filed: February 8, 2002
    Date of Patent: November 9, 2004
    Assignee: Warner-Lambert Company
    Inventor: Patrick Bernardelli
  • Publication number: 20040220180
    Abstract: The present invention relates to novel chemical compounds, methods for their discovery, and their therapeutic use. In particular, the present invention provides benzodiazepine derivatives and methods of using benzodiazepine derivatives as therapeutic agents to treat a number of conditions associated with the faulty regulation of the processes of programmed cell death, autoimmunity, inflammation, and hyperproliferation, and the like.
    Type: Application
    Filed: May 1, 2003
    Publication date: November 4, 2004
    Applicant: The Regents of the University of Michigan
    Inventor: Gary D. Glick
  • Patent number: 6774125
    Abstract: Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.
    Type: Grant
    Filed: October 7, 2002
    Date of Patent: August 10, 2004
    Assignees: Elan Pharmaceuticals, Inc., Eli Lilly & Company
    Inventors: James E. Audia, Richard C. Thompson, Stephen C. Wilkie, Thomas C. Britton, Warren J. Porter, George W. Huffman, Lee H. Latimer
  • Publication number: 20040152888
    Abstract: The invention concerns novel benzodiazepine derivatives and their uses in the field of therapeutics particularly for treating pathologies involving the activity of a cyclic nucleotide phosphodiesterase. It also concerns methods for preparing them and novel synthesis intermediates.
    Type: Application
    Filed: November 26, 2003
    Publication date: August 5, 2004
    Inventors: Jean-Jacques Bourguignon, Yan Lagouge, Claire Lugnier, Eveline Klotz, Jean-Paul Macher, Pierre Raboisson, Dominique Schultz
  • Publication number: 20040138208
    Abstract: Disclosed are compounds, which are bradykinin antagonists and are useful to treat diseases or relieve adverse symptoms associated with disease conditions in mammals mediated by bradykinin. Certain of the compounds exhibit increased potency and are expected to also exhibit an increased duration of action.
    Type: Application
    Filed: October 9, 2003
    Publication date: July 15, 2004
    Inventors: Ryan C. Holcomb, Francine S. Grant, Michael A. Pleiss, Eugene D. Thorsett
  • Publication number: 20040082573
    Abstract: Orally active benzodiazepine derivatives and their salts are disclosed. These compounds and their salts have anxiolytic and anticonvulsant activity with reduced sedative/hypnotic/muscle relaxant/ataxic effects.
    Type: Application
    Filed: March 28, 2003
    Publication date: April 29, 2004
    Inventors: James M. Cook, Qi Huang, Xiaohui He, Xioayan Li, Jianming Yu, Dongmei Han, Snjezana Lelas, John F. McElroy
  • Publication number: 20040043977
    Abstract: Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.
    Type: Application
    Filed: January 6, 2003
    Publication date: March 4, 2004
    Inventors: Jing Wu, Jay S. Tung, Eugene D. Thorsett, Michael A. Pleiss, Jeffrey S. Nissen, Jeffrey Neitz, Lee H. Latimer, Varghese John, Stephen Freedman, Thomas C. Britton, James E. Audia, Jon K. Reel, Thomas E. Mabry, Bruce A. Dressman, Cynthia L. Cwi, James J. Droste, Steven S. Henry, Stacey L. McDaniel, William Leonard Scott, Russell D. Stucky, Warren J. Porter
  • Patent number: 6696438
    Abstract: Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.
    Type: Grant
    Filed: December 12, 2002
    Date of Patent: February 24, 2004
    Assignees: Elan Pharmaceuticals, Inc., Eli Lilly & Company
    Inventors: James E. Audia, Bruce A. Dressman, Qing Shi
  • Publication number: 20040029867
    Abstract: The invention relates to novel compounds of formula (I) containing benzofused heterocyclic sulfonamide derivatives which are effective platelet ADP receptor inhibitors. Such compounds including pharmaceutically acceptable salts are useful in various pharmaceutical compositions for the prevention and/or treatment of cardiovascular disease particularly those related to thrombosis.
    Type: Application
    Filed: April 9, 2003
    Publication date: February 12, 2004
    Inventors: Robert M. Scarborough, Charles K. Marlowe
  • Publication number: 20040024203
    Abstract: Compounds of formula (I) are disclosed. The compounds inhibit the action of gamma secretase, and hence find use in the treatment and prevention of Alzheimer's disease.
    Type: Application
    Filed: April 11, 2003
    Publication date: February 5, 2004
    Inventors: Ian Churcher, Alan John Nadin, Andrew Pate Owens
  • Patent number: 6686350
    Abstract: The present invention relates to novel compounds that are useful for inhibition and prevention of cell adhesion and cell adhesion-mediated pathologies. This invention also relates to pharmaceutical formulations comprising these compounds and methods of using them for inhibition and prevention of cell adhesion and cell adhesion-mediated pathologies. The compounds and pharmaceutical compositions of this invention can be used as therapeutic or prophylactic agents. They are particularly well-suited for treatment of many inflammatory and autoimmune diseases.
    Type: Grant
    Filed: January 25, 1999
    Date of Patent: February 3, 2004
    Assignee: Biogen, Inc.
    Inventors: Zhongli Zheng, Carol L. Ensinger, Steven P. Adams
  • Patent number: 6683075
    Abstract: Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.
    Type: Grant
    Filed: January 6, 2003
    Date of Patent: January 27, 2004
    Assignees: Athena Neurosciences, Inc., Eli Lilly & Company
    Inventors: Jing Wu, Jay S. Tung, Eugene D. Thorsett, Michael A. Pleiss, Jeffrey S. Nissen, R. Jeffrey Neitz, Lee H. Latimer, Varghese John, Stephen Freedman, Thomas C. Britton, James A. Audia, Jon K. Reel, Thomas E. Mabry, Bruce A. Dressman, Cynthia L. Cwi, James J. Droste, Steven S. Henry, Stacey L. McDaniel, William Leonard Scott, Russell D. Stucky, Warren J. Porter
  • Publication number: 20040014964
    Abstract: The present invention describes novel compounds of the formula:
    Type: Application
    Filed: January 21, 2003
    Publication date: January 22, 2004
    Inventors: Edward H. Cheesman, John A. Barrett, Alan P. Carpenter, Milind Rajopadhye, Michael Sworin
  • Patent number: 6653303
    Abstract: Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.
    Type: Grant
    Filed: January 6, 2003
    Date of Patent: November 25, 2003
    Assignees: Athena Neurosciences, Inc., Eli Lilly & Company
    Inventors: Jing Wu, Jay S. Tung, Eugene D. Thorsett, Michael A. Pleiss, Jeffrey S. Nissen, R. Jeffrey Neitz, Lee H. Latimer, Varghese John, Stephen Freedman, Thomas C. Britton, James A. Audia, Jon K. Reel, Thomas E. Mabry, Bruce A. Dressman, Cynthia L. Cwi, James J. Droste, Steven S. Henry, Stacey L. McDaniel, William Leonard Scott, Russell D. Stucky, Warren J. Porter
  • Publication number: 20030186969
    Abstract: The present invention provides benzodiazepine derivatives of the following formula, analogs thereof and pharmaceutically acceptable salts thereof. The compounds of the present invention have an excellent effect of inhibiting activated blood-coagulation factor X. These compounds are usable as agents for treating various diseases concerned with the activated blood-coagulation factor X.
    Type: Application
    Filed: March 27, 2003
    Publication date: October 2, 2003
    Applicant: AJINOMOTO CO. INC
    Inventors: Tadakiyo Nakagawa, Munetaka Tokumasu, Kazumi Tashiro, Mitsuo Takahashi, Takashi Kayahara, Shunji Takehana, Yuki Kajigaya, Kaoru Yoshida, Kuniya Sakurai
  • Publication number: 20030162774
    Abstract: Novel compounds of formula (I) to (VI), which more particularly include sulfonylurea derivatives, sulfonylthiourea derivatives, sulfonylguanidine derivatives, sulfonylcyanoguanidine derivatives, thioacylsulfonamide derivatives, and acylsulfonamide derivatives which are effective platelet ADP receptor inhibitors. These derivatives may be used in various pharmaceutical compositions, and are particularly effective for the prevention and/or treatment of cardiovascular diseases, particularly those diseases related to thrombosis.
    Type: Application
    Filed: January 23, 2003
    Publication date: August 28, 2003
    Applicant: Millennium Pharmaceuticals, Inc.
    Inventors: Robert M. Scarborough, Wolin Huang
  • Publication number: 20030162768
    Abstract: Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.
    Type: Application
    Filed: December 12, 2002
    Publication date: August 28, 2003
    Inventors: James E. Audia, Bruce A. Dressman, Qing Shi
  • Publication number: 20030149262
    Abstract: The present invention describes novel compounds of the formula:
    Type: Application
    Filed: November 26, 2002
    Publication date: August 7, 2003
    Inventors: Edward H. Cheesman, Michael Sworin