Having -c(=x)-, Wherein X Is Chalcogen, Attached Indirectly To Ring Carbon Of The Five-membered Hetero Ring By An Acyclic Carbon Or Acyclic Carbon Chain (e.g., Indole-3-acetic Acid, Etc.) Patents (Class 548/494)
  • Publication number: 20030105088
    Abstract: This invention relates to new compounds, pharmaceutical compositions and diagnostic kits comprising such compounds, and methods of using such compounds for inhibiting NAALADase enzyme activity, detecting diseases where NAALADase levels are altered, effecting neuronal activity, effecting TGF-&bgr; activity, inhibiting angiogenesis, and treating glutamate abnormalities, diabetic neuropathy, pain, compulsive disorders, prostate diseases, cancers and glaucoma.
    Type: Application
    Filed: January 17, 2002
    Publication date: June 5, 2003
    Applicant: GUILFORD PHARMACEUTICALS INC.
    Inventors: Takashi Tsukamoto, Pavel Majer, Doris Stoermer, Barbara S. Slusher
  • Publication number: 20030087762
    Abstract: The present invention provides compounds and compositions capable of stimulating plant growth, regeneration of plant cells and tissues, and transformation of plant cells and tissues, comprising mono- and multi-substituted auxinic analogues of indole-3-acetic acid (IAA) comprising substituent groups such as halo-, alkyl-, alkoxy-, acyl-, acylamido- and acyloxy-groups. The invention relates to a method of using such mono- and multi-substituted auxinic analogues of IAA to affect growth, regeneration or transformation in monocotyledonous and dicotyledonous plants, as well as in transgenic plant tissues. The invention also contemplates the use of these auxinic IAA analogues in the presence of other plant growth regulators, such as cytokinin, etc., to enhance plant growth.
    Type: Application
    Filed: February 6, 2001
    Publication date: May 8, 2003
    Applicant: Life Technologies, Inc.
    Inventors: Jhy-Jhu Lin, Jianqing Lan, Nacyra Assad-Garcia
  • Publication number: 20030088111
    Abstract: In accordance with the present invention, there are provided normal modified forms of nonsteroidal anti-inflamamatory drugs. Modified NSAIDs according to the invention provide a new class of anti-inflammatory agent which provide the therapeutic benefits of NSAIDs while causing a much lower incidence of side-effects then typically observed with such agents.
    Type: Application
    Filed: March 12, 2002
    Publication date: May 8, 2003
    Applicant: Medinox, Inc.
    Inventors: Ching-San Lai, Tingmin Wang
  • Publication number: 20030078289
    Abstract: A compound of the formula 1
    Type: Application
    Filed: September 24, 2002
    Publication date: April 24, 2003
    Inventors: Gary E. Aspnes, Yuan-Ching P. Chiang
  • Publication number: 20030065007
    Abstract: Non-peptide acetamide derivatives of Formula I are specific NK1 antagonists, 1
    Type: Application
    Filed: October 9, 2002
    Publication date: April 3, 2003
    Inventors: Mark Wallace Creswell, Michael Higginbottom, David Christopher Horwell, Russel Andrew Lewthwaite, Martyn Clive Pritchard, Jennifer Raphy
  • Publication number: 20030055263
    Abstract: The present application relates to the use of the carboxylic acid derivatives of general formula
    Type: Application
    Filed: July 10, 2002
    Publication date: March 20, 2003
    Applicant: Boehringer Ingelheim Pharma KG
    Inventors: Henning Priepke, Iris Kauffmann-Hefner, Norbert Hauel, Klaus Damm, Andreas Schnapp
  • Patent number: 6534535
    Abstract: Novel compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds of formula (I) below: are useful in vitro or in vivo for preventing or treating coagulation disorders.
    Type: Grant
    Filed: August 10, 2000
    Date of Patent: March 18, 2003
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Bing-Yan Zhu, Robert M. Scarborough, Lane Clizbe, Brandon Doughan, Zhaozhong Jon Jia, Kim Kane-Maguire, Charles Marlowe, Yonghong Song, Ting Su, Willy Teng, Penglie Zhang
  • Patent number: 6531485
    Abstract: This invention relates to prostaglandin agonists, methods of using such prostaglandin agonists, pharmaceutical compositions containing such prostaglandin agonists and kits containing such prostaglandin agonists. The prostaglandin agonists are useful for the treatment of bone disorders including osteoporosis.
    Type: Grant
    Filed: December 16, 1999
    Date of Patent: March 11, 2003
    Assignee: Pfizer Inc.
    Inventors: Kimberly O. Cameron, Paul A. DaSilva-Jardine
  • Publication number: 20030045728
    Abstract: Indol-3-yl derivatives of the general formula I 1
    Type: Application
    Filed: August 9, 2002
    Publication date: March 6, 2003
    Inventors: Matthias Wiesner, Simon Goodman, Rudolf Gottschlich
  • Publication number: 20030045560
    Abstract: This invention provides novel compounds, pharmaceutical compositions and methods of treating thrombotic disorders in mammals, the compounds having the formula: 1
    Type: Application
    Filed: June 13, 2002
    Publication date: March 6, 2003
    Applicant: Wyeth
    Inventors: Thomas Joseph Commons, Susan Christman Croce, Richard Page Woodworth, Eugene John Trybulski, Hassan Mohmoud Elokdah, David LeRoy Crandall
  • Publication number: 20030040625
    Abstract: This invention provides a class of therapeutic compounds and methods for the treatment of mammals with physiological disorders, such as for example a frequently occurring type of essential hypertension, which are critically associated with the decreased binding of magnesium to the plasma membranes of their cells. These methods consist of administering to a mammal in need of such treatment a compound selected from a series of disubstituted trans, trans 1,3-butadienes, 1,3-disubstituted perhydrobutadienes, 1,2-disubstituted trans ethylenes and 1,2 disubstituted ethanes and disubstitutedpropanes, each of which embodies, in common, the unique structural feature essential for the biological activity of these compounds. This invention also provides for pharmaceutical formulations that employ these novel compounds.
    Type: Application
    Filed: August 29, 2002
    Publication date: February 27, 2003
    Inventor: Ibert Clifton Wells
  • Publication number: 20030018062
    Abstract: The present invention provides hydroxamate compounds which are deacetylase inhibitors. The compounds are suitable for pharmaceutical compositions having anti-proliferative properties.
    Type: Application
    Filed: August 31, 2001
    Publication date: January 23, 2003
    Inventors: Stacy W. Remiszewski, Kenneth W. Bair, Richard W. Versace, Lawrence B. Perez, Michael A. Green, Lidia C. Sambucetti, Sushil Sharma
  • Publication number: 20030018053
    Abstract: Disclosed are substituted indolealkanoic acids useful in the treatment of chronic complications arising from diabetes mellitus. Also disclosed are pharmaceutical compositions containing the compounds and methods of treatment employing the compounds, as well as methods for their synthesis.
    Type: Application
    Filed: June 28, 2002
    Publication date: January 23, 2003
    Applicant: The Institute for Pharmaceutical Discovery LLC.
    Inventors: Michael Jones, David Gunn, John Jones, Michael Van Zandt
  • Patent number: 6506759
    Abstract: N-heterocyclic moiety containing hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
    Type: Grant
    Filed: October 31, 2000
    Date of Patent: January 14, 2003
    Assignee: Monsanto Company
    Inventors: John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, Kathryn L. Reed, Ko-Chung Lin, John Nicholas Freskos, Michael Clare, Donald Joseph Rogier, Jr., Robert M. Heintz, Michael L. Vazquez, Richard A. Mueller
  • Publication number: 20030008895
    Abstract: This invention relates to prostaglandin agonists, methods of using such prostaglandin agonists, pharmaceutical compositions containing such prostaglandin agonists and kits containing such prostaglandin agonists. The prostaglandin agonists are useful for the treatment of bone disorders including osteoporosis.
    Type: Application
    Filed: December 16, 1999
    Publication date: January 9, 2003
    Inventors: KIMBERLY O CAMERON, PAUL A. DASILVA-JARDINE
  • Patent number: 6500851
    Abstract: This application relates to a compound of formula I (or a prodrug thereof or a pharmaceutically acceptable salt of the compound or prodrug thereof) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well as a process for its preparation and intermediates therefor.
    Type: Grant
    Filed: February 22, 2002
    Date of Patent: December 31, 2002
    Assignee: Eli Lilly and Company
    Inventors: Douglas Wade Beight, Trelia Joyce Craft, Jeffry Bernard Franciskovich, Theodore Goodson, Jr., Steven Edward Hall, David Kent Herron, Valentine Joseph Klimkowski, Jeffrey Alan Kyle, John Joseph Masters, David Mendel, Guy Milot, Jason Scott Sawyer, Robert Theodore Shuman, Gerald Floyd Smith, Anne Louise Tebbe, Jennifer Marie Tinsley, Leonard Crayton Weir, James Howard Wikel, Michael Robert Wiley, Ying Kwong Yee
  • Patent number: 6472418
    Abstract: Non-peptide acetamide derivatives of Formula I are specific NK1 antagonist, where R is aryl, R1 and R2 are H or alkyl, m, n and q are integers from 0 to 4, X is NR8 or NHCONH, R3 and R9 are H or alkyl, R4 is naphthyl or indolyl, R5 and R2 are H or alkyl, and R6 is aryl. The compounds are useful agents for treating inflammatory and allergic disorders, pain, anxiety, depression, schizophrenia and emesis.
    Type: Grant
    Filed: June 18, 2001
    Date of Patent: October 29, 2002
    Assignee: Warner-Lambert Company
    Inventors: Mark Wallace Creswell, Michael Higginbottom, David Christopher Horwell, Russel Andrew Lewthwaite, Martyn Clive Pritchard, Jennifer Raphy
  • Publication number: 20020132792
    Abstract: Aryl-substituted indirubin derivatives, their production and their intermediate products for production, as well as their use as medications for treating cancer, such as solid tumors and leukemia; auto-immune diseases, such as psoriasis, alopecia and multiple sclerosis, chemotherapy agent-induced alopecia and mucositis; cardiovascular diseases, such as stenoses, arterioscleroses and restenoses; infectious diseases, such as, e.g., those caused by unicellular parasites, such as trypanosoma, toxoplasma or plasmodium, or those caused by fungi; nephrological diseases, such as, e.g., glomerulonephritis; chronic neurodegenerative diseases, such as Huntington's disease, amyotrophic lateral sclerosis, Parkinson's disease, AIDS dementia and Alzheimer's disease; acute neurodegenerative diseases, such as ischemias of the brain and neurotraumas; viral infections, such as, e.g., cytomegalic infections, herpes, hepatitis B and C, and HIV diseases, are described.
    Type: Application
    Filed: November 29, 2001
    Publication date: September 19, 2002
    Applicant: Schering AG
    Inventors: Olaf Prien, Andreas Steinmeyer, Gerhard Siemeister, Rolf Jautelat
  • Publication number: 20020119971
    Abstract: The invention relates to new hydroxyindoles of the Formula, 1
    Type: Application
    Filed: February 21, 2002
    Publication date: August 29, 2002
    Inventors: Norbert Hofgen, Ute Egerland, Hildegard Poppe, Degenhard Marx, Stefan Szelenyi, Thomas Kronbach, Emmanuel Polymeropoulos, Sabine Heer
  • Publication number: 20020115651
    Abstract: The invention relates to new hydroxyindoles of the Formula, 1
    Type: Application
    Filed: February 21, 2002
    Publication date: August 22, 2002
    Inventors: Norbert Hofgen, Ute Egerland, Hildegard Poppe, Degenhard Marx, Stefan Szelenyi, Thomas Kronbach, Emmanuel Polymeropoulos, Sabine Heer
  • Publication number: 20020111351
    Abstract: The invention relates to nets hydroxyindoles of the Formula, 1
    Type: Application
    Filed: February 21, 2002
    Publication date: August 15, 2002
    Inventors: Norbert Hofgen, Ute Egerland, Hildegard Poppe, Degenhard Marx, Stefan Szelenyi, Thomas Kronbach, Emmanuel Polymeropoulos, Sabine Heer
  • Publication number: 20020107241
    Abstract: The present invention relates N-heterocyclic derivatives for treating or preventing neuronal damage associated with neurological diseases. The invention also provides compositions comprising the compounds of the present invention and methods of utilizing those compositions for treating or preventing neuronal damage.
    Type: Application
    Filed: January 3, 2002
    Publication date: August 8, 2002
    Inventors: David Lauffer, Brian Ledford, Michael Mullican
  • Publication number: 20020103138
    Abstract: We have discovered a method of modifying the tumor cell microenvironment to reduce or prevent the establishment, growth or metastasis of malignant cells comprising administering to a patient having malignant cells a pharmaceutically effective amount of a PAR-1 inhibitor and optionally a PAR-2 inhibitor to prevent or reduce activation of normal cells within the tumor microenvironment. This method also has the effect in some patients of modulating the immune system to facilitate a more efficient immune response to malignant cells and maybe coupled with cytokine therapy and T-cell therapy to enhance the patient's immune response to the malignant cells.
    Type: Application
    Filed: May 25, 2001
    Publication date: August 1, 2002
    Inventors: Michael D'Andrea, Claudia Derian, Hal Brent Woodrow
  • Patent number: 6423738
    Abstract: A method for treating circadian rhythm phase disorders is described. The invention provides methods to specifically advance or delay the phase of certain circadian rhythms in humans. The disclosed methods relate to the administration of melatonin at times determined with relation to the time of dim light endogenous melatonin onset. Embodiments capable of alleviating the effects of jet lag, winter depression and shift-work sleep disturbance are provided.
    Type: Grant
    Filed: May 30, 2000
    Date of Patent: July 23, 2002
    Assignee: Oregon Health & Sciences University
    Inventors: Alfred J. Lewy, Robert L. Sack
  • Publication number: 20020087007
    Abstract: There is provided a process for preparing a pharmacologically acceptable salt of N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanyl-amino acid which comprises condensing an amino acid and N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanine.
    Type: Application
    Filed: November 21, 2001
    Publication date: July 4, 2002
    Applicant: Kaneka Corporation
    Inventors: Yasuyoshi Ueda, Koichi Kinoshita, Tadashi Moroshima, Yoshifumi Yanagida, Yoshihide Fuse
  • Patent number: 6384220
    Abstract: Para-aryl or heteroaryl substituted phenyl amides which are active as glucokinase activators to increase insulin secretion which makes them useful for treating type II diabetes.
    Type: Grant
    Filed: May 1, 2001
    Date of Patent: May 7, 2002
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Wendy Lea Corbett, Nancy-Ellen Haynes, Ramakanth Sarabu
  • Patent number: 6384235
    Abstract: The present application describes a process for preparing compounds of the indole type of the formula in which A is a hydrocarbon radical which, together with the carbons to which it is attached, forms a substituted or unsubstituted mono- or polycyclic aromatic system which may contain one or more heteroatoms from the group consisting of N, O and S, and R1, R2 independently of one another are H, a saturated, linear or branched aliphatic C1-C20-hydrocarbon radical, an unsaturated, linear or branched aliphatic C2-C20-hydrocarbon radical, a saturated or unsaturated, unsubstituted or alkyl-substituted cycloaliphatic C3-C20-hydrocarbon radical or an aromatic C5-C20-hydrocarbon radical, where these radicals may contain in their molecular skeleton one or more heteroatoms from the group consisting of the halogens, N, P, O, S, Si, Sn and B and may be substituted or unsubstituted, by cyclization of alkynylaminoaromatics of the formula in which R1 and R2 are as defined in formula (I)
    Type: Grant
    Filed: February 14, 2001
    Date of Patent: May 7, 2002
    Assignee: BASF Aktiengesellschaft
    Inventors: Jochem Henkelmann, Jan-Dirk Arndt
  • Patent number: 6372759
    Abstract: This application relates to a compound of formula (I), a pharmaceutically acceptable salt of the compound, or a prodrug thereof, as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well as a process for its preparation and intermediates therefor.
    Type: Grant
    Filed: March 20, 2000
    Date of Patent: April 16, 2002
    Assignee: Eli Lilly and Company
    Inventors: Douglas Wade Beight, Trelia Joyce Craft, Jeffry Bernard Franciskovich, Theodore Goodson, Steven Edward Hall, David Kent Herron, Valentine Joseph Klimkowski, Jeffrey Alan Kyle, John Joseph Masters, David Mendel, Guy Milot, Jason Scott Sawyer, Robert Theodore Shuman, Gerald Floyd Smith, Anne Louise Tebbe, Jennifer Marie Tinsley, Leonard Crayton Weir, James Howard Wikel, Michael Robert Wiley, Ying Kwong Yee
  • Patent number: 6355810
    Abstract: Disclosed are multibinding compounds which inhibit 3-hydroxy-3-methylglutaryl coenzyme A reductase (HMG-COA reductase), the rate limiting enzyme in cholesterol biosynthesis. The multibinding compounds of this invention containing from 2 to 10 ligands covalently attached to one or more linkers. Each ligand is a moiety capable of binding to HMG-CoA reductase and the distance between ligands is at least 10 Å. The multibinding compounds of this invention are useful in the treatment and prevention of hypercholesterolemia, hyperlipidemia, atherosclerosis and the like.
    Type: Grant
    Filed: June 4, 1999
    Date of Patent: March 12, 2002
    Assignee: Advanced Medicine, Inc.
    Inventors: John H. Griffin, Michael R. Leadbetter, Donald E. Schmidt, Jr.
  • Publication number: 20020002286
    Abstract: The subject invention involves a solid-phase process for the synthesis of indole compounds comprising the steps:
    Type: Application
    Filed: February 8, 2001
    Publication date: January 3, 2002
    Inventors: Daniel Michael Ketcha, Lawrence Joseph Wilson
  • Patent number: 6326501
    Abstract: A process for manufacturing a methylated indole compounds of the formula: where R1 is selected from the group consisting of halogen, C1-C6 alkyl, C1-C6 alkenyl, —OCH3, —NO2, —CHO, —CO2CH3, and —CN, and R2 is selected from the group consisting of C1-C6 alkyl, —CO2CH3, —CN, —CHO, —NH2, —N(C1-C6 alkyl)2, —(CH2)nCOOH, and —(CH2)nCN, where n is an integer from 1 to 4, inclusive, involves reacting a compound of the formula: with dimethyl carbonate in the presence of a base or a catalyst at ambient pressure.
    Type: Grant
    Filed: April 5, 2001
    Date of Patent: December 4, 2001
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Xinglong Jiang
  • Patent number: 6316487
    Abstract: The subject invention pertains to novel compounds, and compositions comprising the compounds, for the treatment of cardiac arrhythmias. The subject invention further concerns a method of making the novel compounds. The novel compounds are rapidly metabolized analogs of amiodarone, having the distinct and advantageous characteristic of being metabolized to a less lipophilic compound. The new compounds can have particular utility for treating life-threatening ventricular tachyarrhythmias, especially in patients with congestive heart failure (CHF). The product can also provide effective management for ventricular arrhythmias and supraventricular arrhythmias, including atrial fibrillation and re-entrant tachyarrhythmias involving accessory pathways.
    Type: Grant
    Filed: October 6, 2000
    Date of Patent: November 13, 2001
    Assignee: Aryx Therapeutics
    Inventors: Pascal Druzgala, Peter G. Milner
  • Publication number: 20010034454
    Abstract: Methoxy and ethoxy substituted 3-aroyl-2-arylbenzo[b]thiophenes and benzo[b]thiophene analogues are described for use in inhibiting tubulin polymerization. The compounds' use for treating tumor cells is also described.
    Type: Application
    Filed: December 15, 2000
    Publication date: October 25, 2001
    Applicant: BYLOR UNIVERSITY AND ARIZONA DESEASE CONTROL RESEARCH COMMISSION
    Inventors: Kevin G. Pinney, George R. Pettit, Vani P. Mocharla, Maria del Pilar Mejia, Anupama Shirali
  • Patent number: 6306890
    Abstract: A compound of the formula where: n, and X are as defined in the specification, and the compound possesses selectivity for inhibition of cyclooxygenase-2.
    Type: Grant
    Filed: August 30, 1999
    Date of Patent: October 23, 2001
    Assignee: Vanderbilt University
    Inventors: Amit S. Kalgutkar, Lawrence J. Marnett
  • Patent number: 6291508
    Abstract: Mono- or polyenic carboxylic acid derived compounds of the formula (1-I) or a physiologically acceptable salt thereof: Z—(CR3═CR2)n—COOR1  (1-I) wherein R1 is hydrogen or a carboxyl-protecting group; R2 and R3 are each independently hydrogen, halogen, linear lower alkyl, branched lower alkyl linear lower alkoxy, branched lower alkoxy or aryl, m is 1 to 3 and Z is a group or their salts have the potent ability to bind to retinoic acid receptors thus useful in treating psoriasis and rheumatoid arthritis.
    Type: Grant
    Filed: September 23, 1999
    Date of Patent: September 18, 2001
    Assignee: Eisai Co., Ltd.
    Inventors: Shigeki Hibi, Kouichi Kikuchi, Hiroyuki Yoshimura, Mitsuo Nagai, Katsuya Tagami, Shinya Abe, Ieharu Hishinuma, Junichi Nagakawa, Norimasa Miyamoto, Takayuki Hida, Aichi Ogasawara, Seiko Higashi, Kenji Tai, Takashi Yamanaka, Makoto Asada
  • Patent number: 6284897
    Abstract: A method for the crystallization of tryptophan, comprising storing a tryptophan solution at a pH of 8 to 13 and at a temperature of room temperature to 100° C. for 0.5 hour to 1 week and then, followed by crystallization.
    Type: Grant
    Filed: January 9, 2001
    Date of Patent: September 4, 2001
    Assignee: Ajinomoto Co., Inc.
    Inventors: Ichiro Fuke, Shuichi Endo, Seiji Funatsu
  • Patent number: 6277833
    Abstract: Substituted triols are prepared by reducing appropriately substituted carboxylic esters. The substituted triols can be used as active substances in medicaments.
    Type: Grant
    Filed: September 24, 1998
    Date of Patent: August 21, 2001
    Assignee: Bayer Aktiengesellschaft
    Inventors: Rolf Angerbauer, Peter Fey, Walter Hübsch, Thomas Philipps, Hilmar Bischoff, Hans-Peter Krause, Jörg Petersen von Gehr, Delf Schmidt
  • Publication number: 20010012851
    Abstract: Nitric oxide releasing oxindole prodrugs are described which are useful in methods of treating or preventing pain, inflammation, fever, or gastrointestinal lesions in a patient in need of such treatment, or of modifying an inflammatory disease or condition by favorably affecting the outcome thereof in said patient, wherein there is administered to said patient a therapeutically effective amount of a compound of Formula (I): 1
    Type: Application
    Filed: July 29, 1999
    Publication date: August 9, 2001
    Inventors: KRISTIN M. LUNDY, MICHAEL T. CLARK
  • Patent number: 6265591
    Abstract: A process for preparing 1H-indole-3-glyoxamides useful for inhibiting SPLA2 and novel intermediates useful in the preparation of such compounds.
    Type: Grant
    Filed: September 27, 2000
    Date of Patent: July 24, 2001
    Assignee: Eli Lilly and Company
    Inventors: Benjamin Alan Anderson, Nancy Kay Harn
  • Patent number: 6252084
    Abstract: A class of novel 1H-indole-3-acetamides is disclosed together with the use of such indole compounds for inhibiting sPLA2 mediated release of fatty acids for treatment of conditions such as septic shock.
    Type: Grant
    Filed: October 31, 1997
    Date of Patent: June 26, 2001
    Assignee: Eli Lilly and Company
    Inventors: Nicholas J. Bach, Robert D. Dillard, Susan E. Draheim, Robert B. Hermann, Richard W. Schevitz
  • Patent number: 6218419
    Abstract: The subject application concerns novel compounds with useful biological properties. For example, these compounds can be used as antinflammatory, anti-proliferative, immunomodulatory, and/or neuroprotective agents. Specific examples of the compounds of the subject invention include Secobatzelline A and Secobatzelline B, which can be isolated from marine sponges.
    Type: Grant
    Filed: July 8, 1999
    Date of Patent: April 17, 2001
    Assignee: Harbor Branch Oceanographic Institution, Inc.
    Inventors: Sarath P. Gunasekera, Peter J. McCarthy, Ross E. Longley, Shirley A. Pomponi, Amy E. Wright
  • Patent number: 6184244
    Abstract: This invention is directed to novel (N-substituted) indole ICE/ced-3-inhibitor compounds. The invention is also directed to pharmaceutical compositions of such indole compounds, plus the use of such compositions in the treatment of patients suffering inflammatory, autoimmune and neurodegenerative diseases, for the prevention of ischemic injury.
    Type: Grant
    Filed: June 30, 1999
    Date of Patent: February 6, 2001
    Assignee: Idun Pharmaceuticals, Inc.
    Inventors: Donald S. Karanewsky, Xu Bai
  • Patent number: 6169103
    Abstract: Fluorine-substituted biphenyl butyric acid compounds and derivatives are described as well as acid methods for the preparation and pharmaceutical compositions of same, which are useful as inhibitors of matrix metalloproteinases, particularly gelatinase A, stromelysin-1, and collagenase-3, and for the treatment of atherosclerotic plaque rupture, aortic aneurism, heart failure, restenosis, periodontal disease, corneal ulceration, treatment of burns, decubital ulcers, wound healing, cancer, inflammation, pain, arthritis, osteoporosis, multiple sclerosis, renal disease, and other autoimmune or inflammatory disorders dependent upon tissue invasion by leukocytes or other activated migrating cells, acute and chronic neurodegenerative disorders including stroke, head trauma, spinal cord injury, Alzheimer's disease, amyotrophic lateral sclerosis, cerebral amyloid angiopathy, AIDS, Parkinson's disease, Huntington's disease, prion diseases, myasthenia gravis, and Duchenne's muscular dystrophy.
    Type: Grant
    Filed: February 24, 1999
    Date of Patent: January 2, 2001
    Assignee: Warner-Lambert
    Inventors: Claude Forsey Purchase, Jr., Bruce David Roth, Gerald Paul Schielke, Lary Craswell Walker, Andrew David White
  • Patent number: 6166050
    Abstract: Compounds of the formula ##STR1## which inhibit leukocyte adhesion mediated by interaction of the .alpha..sub.4 .beta..sub.1 integrin (VLA-4) with its counterreceptor VCAM-1, and their use for the treatment of inflammatory and autoimmune diseases.
    Type: Grant
    Filed: December 10, 1999
    Date of Patent: December 26, 2000
    Assignee: American Home Products Corporation
    Inventors: Louis J. Lombardo, Joan Sabalski
  • Patent number: 6159989
    Abstract: There are disclosed compounds of formula (I) ##STR1## and pharmaceutically acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety of sex-hormone related and other conditions in both men and women.
    Type: Grant
    Filed: December 15, 1999
    Date of Patent: December 12, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Lin Chu, Mark Goulet, Thomas F. Walsh, Matthew J. Wyvratt, Stephanie L. Witkin
  • Patent number: 6159995
    Abstract: Compounds of formula (I) ##STR1## are suitable for the production of pharmaceuticals for the prophylaxis and therapy of disorders in the course of which an increased activity of matrix-degrading metalloproteinases is involved.
    Type: Grant
    Filed: May 8, 1998
    Date of Patent: December 12, 2000
    Assignee: Aventis Pharma Deutschland GmbH
    Inventors: Werner Thorwart, Wilfried Schwab, Manfred Schudok, Burkhard Haase, Bernhard Neises, Gunter Billen
  • Patent number: 6150394
    Abstract: Compounds having a metalloproteinase inhibitory activity, represented by the formula (I), its optically active isomers, their pharmaceutically acceptable salts, or hydrates thereof.
    Type: Grant
    Filed: July 22, 1998
    Date of Patent: November 21, 2000
    Assignee: Shionogi & Co., Ltd.
    Inventors: Fumihiko Watanabe, Hiroshige Tsuzuki, Mitsuaki Ohtani
  • Patent number: 6130240
    Abstract: Described is a novel compound and method, useful for treatment of cardiac arrhythmias, especially useful in patients with congestive heart failure (CHF). A process for synthesizing the novel compound is also described.
    Type: Grant
    Filed: December 14, 1998
    Date of Patent: October 10, 2000
    Assignee: Aryx Therapeutics, Inc.
    Inventor: Pascal Druzgala
  • Patent number: 6077849
    Abstract: Compounds of formula I: ##STR1## as well as tautomers, pharmaceutically acceptable salts, hydrates, prodrugs and reduced forms are disclosed. The compounds are useful for the treatment and prevention of diabetes mellitus, and in particular, for the treatment or prevention of hyperglycemia in diabetic patients.
    Type: Grant
    Filed: March 29, 1999
    Date of Patent: June 20, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Kun Liu, Harold B. Wood, Anthony B. Jones, Bei Zhang
  • Patent number: 6075150
    Abstract: .alpha.-ketoamide compounds useful for treating disorders mediated by 20S proteasome in mammals having the following formula: wherein X.sub.2 is Ar or Ar--X.sub.3 wherein X.sub.3 is --C.dbd.O, or --CH.sub.2 CO--, and wherein Ar is phenyl, substituted phenyl, indole, substituted indoles, and any other heteroaryls; R.sub.1, and R.sub.2 are each individually selected from the side chains of the known natural .alpha.-amino acids and unnatural amino acids, hydrogen, 1-10 carbon linear and branched alkyl, 1-10 carbon linear and branched substituted alkyl, aryl, substituted aryl, 1-10 carbon linear, branched substituted aryl, alkoxyaryl, 3-8 carbon cycloalkyl, heterocycle substituted heterocycle, heteroaryl and substituted heteroaryl; X.sub.1 is selected from hydroxide, monoalkylamino, dialkylamino, alkoxide, arylkoxide and ##STR1## wherein X.sub.4 is hydroxide, arylamino, monoalkylamino, dialkylamino, alkoxide, or arylalkoxide; and R.sub.3 is selected from the known natural .alpha.
    Type: Grant
    Filed: January 26, 1998
    Date of Patent: June 13, 2000
    Assignee: CV Therapeutics, Inc.
    Inventors: Lisa Wang, Robert T. Lum, Steven R. Schow, Alison Joly, Suresh Kerwar, Michael M Wick