Polycyclo Ring System Having The Seven-membered Hetero Ring As One Of The Cyclos Patents (Class 514/212.04)
  • Publication number: 20080275024
    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: Application
    Filed: June 19, 2008
    Publication date: November 6, 2008
    Applicant: BRISTOL-MYERS SQUIBB PHARMA COMPANY
    Inventors: Richard E. Olson, Michael G. Yang
  • Patent number: 7429578
    Abstract: Compounds of the formula below are poly(ADP-ribosyl)transferase (PARP) inhibitors, and are useful as therapeutics in treatment of cancers and the amelioration of the effects of stroke, head trauma, and neurodegenerative disease. As cancer therapeutics, the compounds of the invention may be used, e.g., in combination with cytotoxic agents and/or radiation.
    Type: Grant
    Filed: September 6, 2005
    Date of Patent: September 30, 2008
    Assignees: Agouron Pharmaceuticals, Inc., Cancer Research Campaign Technology Limited
    Inventors: Stephen Evan Webber, Stacie S. Canan-Koch, Jayashree Tikhe, Lars Henrik Thoresen
  • Publication number: 20080233132
    Abstract: The present invention relates to methods for treating multiple sclerosis by combining immunotherapy with myelin repair.
    Type: Application
    Filed: November 2, 2007
    Publication date: September 25, 2008
    Inventors: Stephen D. Miller, Terra J. Frederick
  • Patent number: 7425551
    Abstract: The invention relates to malonamide derivatives of formula wherein A1, A2, R1, R2, R3, and R4 are as defined herein and to pharmaceutically acceptable acid addition salts, optically pure enantiomers, racemates or diastereomeric mixtures thereof for the treatment of Alzheimer's disease.
    Type: Grant
    Filed: March 22, 2007
    Date of Patent: September 16, 2008
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Alexander Flohr, Roland Jakob-Roetne, Wolfgang Wostl
  • Publication number: 20080214522
    Abstract: Compounds of the formula (I): wherein A, B, D, M, Ar, W, X, Y, Z and R1 are as defined herein, are useful in the prevention and treatment of hepatitis C infections. The compounds, their preparation, pharmaceutical compositions containing them and their use in medicine are disclosed.
    Type: Application
    Filed: December 19, 2007
    Publication date: September 4, 2008
    Applicant: Istituto di Ricerche di Biologia Molecolare P. Angeletti SpA
    Inventors: Ian Stansfield, Uwe Koch, Joerg Habermann, Frank Narjes
  • Patent number: 7375099
    Abstract: The invention relates to malonamide derivatives of formula wherein each of the variables are as defined in the specification and to pharmaceutically acceptable acid addition salts thereof. The compounds are ?-secretase inhibitors. Thus, the invention also relates to pharmaceutical compositions containing these compounds and to a method of treating Alzheimer's disease by administering the compounds of the invention.
    Type: Grant
    Filed: January 29, 2004
    Date of Patent: May 20, 2008
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Guido Galley, Annick Goergler, Helmut Jacobsen, Eric Argirios Kitas, Jens-Uwe Peters
  • Patent number: 7351701
    Abstract: The invention relates to trycyclic lactam indole derivatives and triacyclic lactam benzimodole derivatives and their use in inhibiting the activity of PARP enzyme. The invention also relates to the use of these compounds in the preparation of medicaments.
    Type: Grant
    Filed: July 23, 2004
    Date of Patent: April 1, 2008
    Assignees: Cancer Research Technology Limited, Pfizer, Inc.
    Inventors: Thomas Helleday, Nicola Curtin
  • Patent number: 7304049
    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: September 19, 2005
    Date of Patent: December 4, 2007
    Assignee: Bristol-Myers Squibb Pharma Company
    Inventor: Richard E. Olson
  • Publication number: 20070225273
    Abstract: The invention relates to malonamide derivatives of formula wherein A1, A2, R1, R2, R3, and R4 are as defined herein and to pharmaceutically acceptable acid addition salts, optically pure enantiomers, racemates or diastereomeric mixtures thereof for the treatment of Alzheimer's disease.
    Type: Application
    Filed: March 22, 2007
    Publication date: September 27, 2007
    Inventors: Alexander Flohr, Roland Jakob-Roetne, Wolfgang Wostl
  • Patent number: 7268126
    Abstract: The present invention relates to novel polymorphic and amorphous forms of a phosphate salt of 8-fluoro-2-{4-[(methylamino)methyl]phenyl}-1,3,4,5-tetrahydro-6H-azepino[5,4,3-cd]indol-6-one, and to processes for their preparation. Such polymorphic forms may be a component of a pharmaceutical composition and may be used to treat a mammalian disease condition mediated by poly(ADP-ribose) polymerase activity including the disease condition such as cancer.
    Type: Grant
    Filed: September 21, 2005
    Date of Patent: September 11, 2007
    Assignees: Agouron Pharmaceuticals, Inc., Cancer Research Technology Ltd.
    Inventors: Jia Liu, Naresh Nayyar, Ming Guo, Zhen-Ping Wu, Bennett Chaplin Borer, Aparna Nadig Srirangam, Mark Bryan Mitchell, Yi Li, Jan-Jon Chu
  • Patent number: 7166587
    Abstract: The present invention provides compounds of the general formula wherein R4 is one of the following groups ?and R1, R2, R3, R7, R8, and R9 are as defined in the specification and pharmaceutically acceptable salts, optically pure enantiomers, racemates or diastereomeric mixtures thereof. The compounds are useful for the treatment of Alzheimer's disease.
    Type: Grant
    Filed: September 27, 2004
    Date of Patent: January 23, 2007
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Alexander Flohr, Guido Galley, Roland Jakob-Roetne, Eric Argirios Kitas, Jens-Uwe Peters, Wolfgang Wostl
  • Patent number: 7160875
    Abstract: The invention relates to malonamide derivatives of formula wherein each of the variables are as defined herein and to pharmaceutically acceptable acid addition salts, optically pure enantiomers, racemates and diastereomeric mixtures thereof. These compounds are ?-secretase inhibitors and may be used for the treatment of Alzheimer's disease.
    Type: Grant
    Filed: September 2, 2004
    Date of Patent: January 9, 2007
    Assignee: Hoffmann-La Rache Inc.
    Inventors: Alexander Flohr, Guido Galley, Roland Jakob-Roetne, Eric Argirios Kitas, Jens-Uwe Peters, Wolfgang Wostl
  • Patent number: 7153847
    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 12, 2003
    Date of Patent: December 26, 2006
    Assignees: Athena Neurosciences, Inc., Eli Lilly and Company
    Inventors: Jing Wu, Jay S. Tung, Jeffrey S. Nissen, R. Jeffrey Neitz, James A. Audia, Thomas E. Mabry
  • Patent number: 7105508
    Abstract: The invention relates to novel compounds which bind to integrin receptors, and to the preparation thereof and the use thereof as drugs.
    Type: Grant
    Filed: August 1, 2000
    Date of Patent: September 12, 2006
    Assignee: Abbott GmbH & Co. KG
    Inventors: Andreas Kling, Hervé Geneste, Udo Lange, Arnulf Lauterbach, Claudia Isabella Graef, Thomas Subkowski, Uta Holzenkamp, Helmut Mack, Jens Sadowski, Wilfried Hornberger, Volker Laux
  • Patent number: 6960576
    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: November 4, 2002
    Date of Patent: November 1, 2005
    Assignee: Bristol-Myers Squibb Pharma Company
    Inventors: Richard E. Olson, Hong Liu, Lorin A. Thompson
  • Patent number: 6958329
    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: November 4, 2002
    Date of Patent: October 25, 2005
    Assignee: Bristol-Myers Squibb Pharma Company
    Inventor: Richard E. Olson
  • Patent number: 6958330
    Abstract: Disclosed are polycyclic ?-amino-?-caprolactams and related compounds which are useful as synthetic intermediates in the preparation of inhibitors of ?-amyloid peptide release and/or its synthesis.
    Type: Grant
    Filed: June 14, 2001
    Date of Patent: October 25, 2005
    Assignees: Elan Pharmaceuticals, Inc., Eli Lilly and Company
    Inventors: James E. Audia, Thomas E. Mabry, Jeffrey A. Nissen, Stacey L. McDaniel, Warren J. Porter
  • Patent number: 6906056
    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 that include 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: March 20, 2003
    Date of Patent: June 14, 2005
    Assignees: Elan Pharmaceuticals, Inc., Eli Lilly & Company
    Inventors: Richard C. Thompson, Stephen Wilkie, Douglas R. Stack, Eldon E. Vanmeter, Qing Shi, Thomas C. Britton, James E. Audia, Jon K. Reel, Thomas E. Mabry, Bruce A. Dressman, Cynthia L. Cwi, Steven S. Henry, Stacey L. McDaniel, Russell D. Stucky, Warren J. Porter
  • Patent number: 6900199
    Abstract: 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: Grant
    Filed: October 14, 2003
    Date of Patent: May 31, 2005
    Assignee: Bristol-Myers Squibb Pharma Company
    Inventors: Qi Han, Hong Liu, Richard E. Olson, Michael G. Yang
  • Publication number: 20040254159
    Abstract: Compounds having the formula 1
    Type: Application
    Filed: February 25, 2004
    Publication date: December 16, 2004
    Inventors: Lisa A. Hasvold, Laura Hexamer, Gaoquan Li, Nan-Horng Lin, Hing Sham, Gerard M. Sullivan, Le Wang, Ping Xia
  • Patent number: 6696436
    Abstract: The invention provides B-ring expanded estra-1,3,5(10)-triene compounds of general formula (1) which modulate the polymerization of tubulin and/or the depolymerization of microtubules. The compounds have anti-angiogenic and anti-tumor activity. The invention also provides methods of preparing the compounds, and methods of using the compounds for the treatment of cancer or other mammalian diseases characterized by undesirable angiogenesis. The compounds of the invention are also expected to have utility as research tools.
    Type: Grant
    Filed: August 16, 2002
    Date of Patent: February 24, 2004
    Assignee: The United States of America as represented by the Department of Health and Human Services
    Inventors: Ernest Hamel, Mark S. Cushman
  • Patent number: 6638925
    Abstract: New derivatives of benzazepine, particularly of benzofuro[3a,3,2,ef][2]benzazepin of the general formula (I) and new compounds of the general formula (III) Drugs, containing compounds of formulas (I) and/or (III), which can be used successfully for the treatment of Alzheimer's disease and related dementia conditions, as well as for the treatment of Langdon-Down syndrome, are also described.
    Type: Grant
    Filed: February 11, 1999
    Date of Patent: October 28, 2003
    Assignee: Sanochemia Ltd.
    Inventors: Laszlo Czollner, Johannes Frohlich, Ulrich Jordis, Bernhard Kuenburg
  • Patent number: 6635632
    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 22, 1997
    Date of Patent: October 21, 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: 20030153550
    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: October 7, 2002
    Publication date: August 14, 2003
    Inventors: James E. Audia, Richard C. Thompson, Stephen C. Wilkie, Thomas C. Britton, Warren J. Porter, George W. Huffman, Lee H. Latimer
  • Publication number: 20030149022
    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 23, 2002
    Publication date: August 7, 2003
    Inventors: James E. Audia, Warren J. Porter, Richard C, Thompson, Stephen C. Wilkie, Douglas R. Stack, Qing Shi
  • Patent number: 6602866
    Abstract: This invention discloses and claims a series of mercaptoacetylamide derivatives of formula I. Also disclosed and claimed are pharmaceutical compositions incorporating these compounds and processes for preparing said compounds.
    Type: Grant
    Filed: April 8, 2002
    Date of Patent: August 5, 2003
    Assignee: Aventis Pharma Deutschland GmbH
    Inventors: Gary A. Flynn, Barbara A. Anderson, Manfred Gerken, Bernd Jablonka, Heinz-Werner Kleemann, Wolfgang Linz, Werner Seiz, Bernhard Seuring
  • Patent number: 6579867
    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: July 27, 2001
    Date of Patent: June 17, 2003
    Assignees: Athena Neurosciences, Inc., Eli Lilly & Company
    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 A. Audia, Jon K. Reel, Thomas E. Mabry, Bruce A. Dressman, James J. Droste, Steven S. Henry, Stacey L. McDaniel, Russell D. Stucky, Warren J. Porter
  • Patent number: 6559141
    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: July 27, 2001
    Date of Patent: May 6, 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
  • Patent number: 6552013
    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: June 22, 1999
    Date of Patent: April 22, 2003
    Assignees: Elan Pharmaceuticals, Inc., Eli Lilly and Company
    Inventors: James E. Audia, Warren J. Porter, Richard C. Thompson, Stephen C. Wilkie, Douglas R. Stack, Qing Shi
  • Patent number: 6544978
    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: July 27, 2001
    Date of Patent: April 8, 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
  • Patent number: 6541466
    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: July 27, 2001
    Date of Patent: April 1, 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
  • Patent number: 6528505
    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: June 22, 1999
    Date of Patent: March 4, 2003
    Assignees: Elan Pharmaceuticals, Inc., Eli Lilly & Company
    Inventors: James E. Audia, Bruce A. Dressman, Qing Shi
  • Patent number: 6509331
    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: June 21, 1999
    Date of Patent: January 21, 2003
    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: 20020173504
    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: July 27, 2001
    Publication date: November 21, 2002
    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: 6468996
    Abstract: The present invention relates to compounds of the general formula (I) The compounds are useful in the treatment and/or prevention of conditions mediated by nuclear receptors, in particular the Peroxisome Proliferator-Activated Receptors (PPAR).
    Type: Grant
    Filed: October 19, 1999
    Date of Patent: October 22, 2002
    Assignees: Novo Nordisk A/S, Dr. Reddy's Research Foundation
    Inventors: Lone Jeppesen, Paul Stanley Bury, Per Sauerberg
  • Publication number: 20020151539
    Abstract: The present invention relates to novel N-substituted azaheterocyclic compounds of the general formula 1
    Type: Application
    Filed: March 14, 2002
    Publication date: October 17, 2002
    Inventors: Tine Krogh Jorgensen, Knud Erik Andersen, Rolf Hohlweg, Uffe Bang Olsen, Erik Fischer, Zdenek Polivka, Kaler Sindelar
  • Publication number: 20020151538
    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: July 27, 2001
    Publication date: October 17, 2002
    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 A. Audia, Jon K. Reel, Thomas E. Mabry, Bruce A. Dressman, James J. Droste, Steven S. Henry, Stacey L. McDaniel, Russell D. Stucky, Warren J. Porter
  • Patent number: 6395728
    Abstract: The invention relates to a method for the treatment or prevention of a condition or disease selected from the group consisting of hypertension, (acute and chronic) congestive heart failure, left ventricular dysfunction and hypertrophic cardiomyopathy, myocardial infarction and its sequelae, supraventricular and ventricular arrhythmias, atrial fibrillation or atrial flutter, atherosclerosis, angina (whether stable or ustable), renal insufficiency (diabetic and non-diabetic), heart failure, angina pectoris, diabetessecondary aldosteronism, primary and secondary pulmonary hyperaldosteronism, primary and pulmonary hypertension, renal failure conditions, such as diabetic nephropathy,glomerulonephritis, scleroderma, glomerular sclerosis, proteinuria of primary renal disease, and also renal vascular hypertension, diabetic retinopathy, the management of other vascular disorders, such as migraine, Raynaud's disease, luminal hyperplasia, cognitive dysfunction (such as Alzheimer's), and stroke, comprising admi
    Type: Grant
    Filed: January 9, 2001
    Date of Patent: May 28, 2002
    Assignee: Novartis AG
    Inventors: Randy Lee Webb, Marc de Gasparo
  • Publication number: 20020061874
    Abstract: This invention relates to novel lactams having the Formula (I): 1
    Type: Application
    Filed: April 3, 2001
    Publication date: May 23, 2002
    Inventors: Michael G. Yang, Hong Liu
  • Patent number: 6387893
    Abstract: Spirotricyclic azacycloalkyl compounds and pharmaceutically acceptable salts thereof are disclosed. The synthesis of these compounds is also described. One application of these compounds, which are alpha 1a adrenergic receptor antagonists, is in the treatment of benign prostatic hyperplasia. These compounds are selective in their ability to relax smooth muscle tissue enriched in the alpha 1a receptor subtype without at the same time inducing hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia can be achieved.
    Type: Grant
    Filed: September 27, 2000
    Date of Patent: May 14, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Ben E. Evans, Jacob M. Hoffman, Kevin F. Gilbert, Kenneth E. Rittle
  • Publication number: 20020052360
    Abstract: This invention relates to novel lactams having the formula (I): 1
    Type: Application
    Filed: March 14, 2001
    Publication date: May 2, 2002
    Inventors: Richard E. Olson, Hong Liu, Lorin A. Thompson III
  • Publication number: 20020042412
    Abstract: A new class of cyclin dependent kinase inhibitors that also have antiproliferative activity in human tumor cell line assays are described.
    Type: Application
    Filed: December 14, 2000
    Publication date: April 11, 2002
    Inventors: Daniel W. Zaharevitz, Rick P. Gussio, Ravi K. Jalluri, Edward A. Sausville, Conrad Kunick, Laurent Meijer
  • Publication number: 20020025955
    Abstract: This invention relates to novel lactams of Formula (I): 1
    Type: Application
    Filed: April 11, 2001
    Publication date: February 28, 2002
    Inventors: Qi Han, Hong Liu, Richard E. Olson, Michael G. Yang