Nitrogen Containing Patents (Class 514/466)
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Patent number: 6838477Abstract: Described herein are compounds related to lactacystin and lactacystin ?-lactone, pharmaceutical compositions containing the compounds, and methods of use.Type: GrantFiled: August 8, 2001Date of Patent: January 4, 2005Assignee: President and Fellows of Harvard CollegeInventors: Stuart L. Schreiber, Robert F. Standaert, Gabriel Fenteany, Timothy F. Jamison
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Publication number: 20040229937Abstract: This invention relates to novel diaryl ureas, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for treating hyper-proliferative and angiogenesis disorders, as a sole agent or in combination with cytotoxic therapies.Type: ApplicationFiled: March 1, 2004Publication date: November 18, 2004Inventors: Jacques Dumas, Wendy Lee, Yuanwei Chen, Lila Adnane, William J. Scott, Sharad Verma, Jianqing Chen, Zhi Chen, Lin Yi
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Patent number: 6818660Abstract: The present invention features calcilytic compounds. “Calcilytic compounds” refer to compounds able to inhibit calcium receptor activity. Also described are the use of calcilytic compounds to inhibit calcium receptor activity and/or achieve a beneficial effect in a patient; and techniques which can be used to obtain additional calcilytic compounds.Type: GrantFiled: October 19, 2001Date of Patent: November 16, 2004Assignee: NPS Pharmaceuticals, Inc.Inventors: Eric G. Del Mar, Robert M. Barmore, Derek Sheehan, Bradford C. Van Wagenen, James F. Callahan, Richard M. Keenan, Nikesh R. Kotecha, Maria Amparo Lago, Linda Sue Southall, Mervyn Thompson
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Patent number: 6812237Abstract: Compounds of the formula (I), wherein R1 is aryl or biaryl; R2 is aryl-lower alkyl, biaryl-lower alkyl, benzo-fused cycloalkyl, cycloalkyl-lower alkyl, bicycloalkyl-lower alkyl, aryloxy-lower alkyl, or aryl-C2-C7-alkyl in which C2-C7-alkyl is interrupted by Y; Y is O, S, SO, SO2, CO or NR6; R3 is hydrogen or lower alkyl; or R2 and R3 combined are C2-C7-alkylene or C2-C7-alkylene interrupted by Y; R4 is hydrogen or lower alkyl; R5 is hydrogen, optionally substituted lower alkyl, aryl-lower alkyl, biaryl-lower alkyl, cycloalkyl-lower alkyl, bicycloalkyl-lower alkyl, aryloxy-lower alkyl, or aryl-C2-C7-alkyl in which C2-C7-alkyl is interrupted by Y; R6 is hydrogen, lower alkyl or aryl-lower alkyl; and pharmaceutically acceptable salts thereof, which are useful as cysteine cathepsin inhibitorsType: GrantFiled: November 7, 2002Date of Patent: November 2, 2004Assignee: Novartis AGInventors: Scott Douglas Cowen, Paul David Greenspan, Leslie Wighton McQuire, Ruben Alberto Tommasi, John Henry Van Duzer
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Patent number: 6762318Abstract: Novel compounds that act to antagonize the action of the glucagon peptide hormone on the glucagon receptor. More particularly, it relates to glucagon antagonists or inverse agonists.Type: GrantFiled: December 3, 2002Date of Patent: July 13, 2004Assignee: Novo Nordisk A/SInventors: Janos Tibor Kodra, Peter Madsen, Jesper Lau, Anker Steen Jorgensen, Inge Thoger Christensen
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Patent number: 6747027Abstract: This invention is directed to proteinase (protease) inhibitors, and more particularly to thiol sulfonamide inhibitors for matrix metalloproteinase 13(MMP-13), compositions of proteinase inhibitors, intermediates for the syntheses of proteinase inhibitors, processes for the preparation of proteinase inhibitors and processes for treating pathological conditions associated with pathological matrix metalloproteinase activity related to MMP-13.Type: GrantFiled: July 22, 1997Date of Patent: June 8, 2004Assignee: Pharmacia CorporationInventors: Gary DeCrescenzo, Zaheer S. Abbas, John N. Freskos, Daniel P. Getman, Robert M. Heintz, Brent V. Mischke, Joseph J. McDonald
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Patent number: 6740665Abstract: Tyrosine kinase inhibitors and pharmaceutical composition comprising the same are disclosed. Methods of treating mammals who have p185 tumors and methods of preventing p185 tumors in mammals at elevated risks of developing such tumors are disclosed. The methods comprise the step of administering effective amounts pharmaceutical compositions comprising a pharmaceutically acceptable carrier or diluent, and, a tyrosine kinase inhibitor to the mammal.Type: GrantFiled: March 12, 2002Date of Patent: May 25, 2004Inventors: Ramachandran Murali, Mark I. Greene
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Publication number: 20040087585Abstract: Nobel PDF inhibitors and novel methods for their use are provided.Type: ApplicationFiled: August 28, 2003Publication date: May 6, 2004Inventors: Jia-Ning Xiang, Siegfried B Christensen, Jinhwa Lee, Daniel J Mercer
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Patent number: 6710089Abstract: The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N-fused-phenyl-N-benzyl aminoalcohols.Type: GrantFiled: May 23, 2002Date of Patent: March 23, 2004Assignee: Pharmacia CorporationInventors: James A. Sikorski, Richard C. Durley, Deborah A. Mischke, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Margaret L. Grapperhaus, Brian S. Hickory, Mark A. Massa, Monica B. Norton, William F. Vernier, Barry L. Parnas, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
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Patent number: 6696442Abstract: This invention is related to carbocyclic and heterocyclic substituted semicarbazones and thiosemicarbazones represented by Formula I: or a pharmaceutically acceptable salt or prodrug thereof, wherein: Y is oxygen or sulfur; R1, R21, R22 and R23 are independently hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, aryl, aminoalkyl, hydroxyalkyl, alkoxyalkyl or carboxyalkyl-82-; or R22 and R23, together with the N, form a heterocycle; A1 and A2 are independently aryl, heteroaryl, saturated or partially unsaturated carbocycle or saturated or partially unsaturated heterocycle, any of which is optionally substituted; X is one or O, S, NR24, CR25R26, C(O), NR24C(O), C(O)NR24, SO, SO2 or a covalent bond; where R24, R25 and R26 are independently hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, aryl, aminoalkyl, hydroxyalkyl, alkoxyalkyl or carboxyalkyl.Type: GrantFiled: June 25, 2002Date of Patent: February 24, 2004Assignee: Euro-Celtique S.A.Inventors: Yan Wang, Sui Xiong Cai, Nancy C. Lan, John F. W. Keana, Victor I. Ilyin
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Patent number: 6689808Abstract: The invention relates to compounds of formula (I): wherein R1 represents alkyl or ureido, R2 represents alkyl or hydrogen, or R1 and R2 together form a 5- or 6-membered ring, R3 represents CN, NO2, NRaR′a, NRaSO2R′a, NRaCZR5 or CZNRaR′a, R4 represents hydrogen or R3, and medicinal products containing the same which are useful in treating or preventing epilepsy and neurodegenerative diseases.Type: GrantFiled: December 26, 2002Date of Patent: February 10, 2004Assignee: Les Laboratoires ServierInventors: Zongru Guo, Fengming Chu, Juntian Zhang, Guangzhong Yang, Bailing Xu, Xinyi Niu, Zhihong Ren, Pierre Lestage, Pierre Renard
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Patent number: 6683210Abstract: Selected bis-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.Type: GrantFiled: March 15, 2002Date of Patent: January 27, 2004Assignee: G. D. Searle & Co.Inventors: Daniel P Getman, Gary A DeCrescenzo, John N Freskos, Michael L Vazquez, James A Sikorski, Balekudru Devadas, Srinivasan Raj Nagarajan, David L Brown, Joseph J McDonald
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Patent number: 6673832Abstract: The invention provides a method of determining whether a compound alleviates vasoconstriction-independent nerve pain mediated by endothelin-1 (ET-1). The method involves (i) determining whether the compound has the ability to inhibit a vasoconstriction-independent ET-1 action, and, if the compound has the inhibitory ability, then ii) determining whether the compound reduces vasoconstriction-independent nerve pain by testing the compound in human patients suffering from pain mediated by the vasoconstriction-independent ET-1 action. The invention also includes a method of determining whether a compound alleviates pain caused by nerve injury in human patients. The method involves (i) determining whether the compound has the ability to inhibit an inflammatory leukocyte response, and, if the compound has the inhibitory ability, then (ii) testing the compound in human patients suffering from pain caused by nerve injury to determine whether the compound alleviates the pain.Type: GrantFiled: May 4, 1998Date of Patent: January 6, 2004Inventor: Gudarz Davar
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Publication number: 20030216384Abstract: The present invention relates to a composition for the treatment and/or prevention of hypertension, said composition comprising an synergistic anti-hypertensive combination of a therapeutically effective amount of at least one angiotensin II inhibitor, and a therapeutically effective amount of at least one nitric oxide donor; said composition optionally further comprising a pharmaceutically acceptable carrier, diluent and/or adjuvant.Type: ApplicationFiled: September 25, 2002Publication date: November 20, 2003Applicant: Northern Sydney Area Health ServiceInventor: Gordon Stokes
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Patent number: 6641810Abstract: FK506 and geldanamycin promote nerve regeneration by a common mechanism that involves the binding of these compounds to polypeptide components of steroid receptor complexes other than the steroid hormone binding portion of the complex (FKBPS52 and hsp90, respectively). These and other agents cause hsp90 dissociation from steroid receptor complexes or block association of hsp90 with steroid receptor complexes.Type: GrantFiled: April 2, 2001Date of Patent: November 4, 2003Assignee: Oregon Health & Science UniversityInventor: Bruce G. Gold
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Patent number: 6642270Abstract: 7-substituted fused ring tetracycline compounds, methods of treating tetracycline responsive states, and pharmaceutical compositions containing the 7-substituted fused ring tetracycline compounds are described.Type: GrantFiled: May 10, 2001Date of Patent: November 4, 2003Assignee: Paratek Pharmaceuticals, Inc.Inventors: Mark L. Nelson, Laura McIntyre
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Patent number: 6638947Abstract: This invention is related to carbocyclic and heterocyclic substituted semicarbazones and thiosemicarbazones represented by Formula I: or a pharmaceutically acceptable salt or prodrug thereof, wherein: Y is oxygen or sulfur; R1, R21, R22 and R23 are independently hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, aryl, aminoalkyl, hydroxyalkyl, alkoxyalkyl or carboxyalkyl; or R22 and R23, together with the N, form a heterocycle; A1 and A2 are independently aryl, heteroaryl, saturated or partially unsaturated carbocycle or saturated or partially unsaturated heterocycle, any of which is optionally substituted; X is one or O, S, NR24, CR25R26, C(O), NR24C(O), C(O)NR24, SO, SO2 or a covalent bond; where R24, R25 and R26 are independently hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, aryl, aminoalkyl, hydroxyalkyl, alkoxyalkyl or carboxyalkyl.Type: GrantFiled: December 6, 2001Date of Patent: October 28, 2003Assignee: Euro-Celtique S.A.Inventors: Yan Wang, Sui Xiong Cai, John F. W. Keana
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Patent number: 6638970Abstract: Novel compounds of the general formula: and pharmaceutically acceptable acid addition salts thereof, wherein the compounds are useful in therapy to protect skeletal muscles against damage resulting from trauma or to protect skeletal muscles subsequent to muscle or systemic diseases such as intermittent claudication, to treat shock conditions, to preserve donor tissue and organs used in transplants, in the treatment of cardiovascular diseases including atrial and ventricular arrhythmias, Prinzmetal's (variant) angina, stable angina, and exercise induced angina, congestive heart disease, and myocardial infarction.Type: GrantFiled: February 22, 2001Date of Patent: October 28, 2003Assignee: CV Therapeutics, Inc.Inventors: Elfaith Elzein, Jeff Zablocki, Tim Marquart
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Patent number: 6617310Abstract: This invention relates generally to phosphate esters of bis-amino acid sulfonamides containing substituted benzyl amines of formula I: or stereoisomeric forms, stereoisomeric mixtures, or pharmaceutically acceptable salt forms thereof, which are useful as HIV protease inhibitors, pharmaceutical compositions comprising the same, and methods of using the same for treating viral infection.Type: GrantFiled: July 18, 2001Date of Patent: September 9, 2003Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Robert F. Kaltenbach, George L. Trainor
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Patent number: 6613803Abstract: This invention is related to carbocyclic and heterocyclic substituted semicarbazones and thiosemicarbazones represented by Formula I: or a pharmaceutically acceptable salt or prodrug thereof, wherein: Y is oxygen or sulfur; R1, R21, R22 and R23 are independently hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, aryl, aminoalkyl, hydroxyalkyl, alkoxyalkyl or carboxyalkyl; or R22 and R23, together with the N, form a heterocycle; A1 and A2 are independently aryl, heteroaryl, saturated or partially unsaturated carbocycle or saturated or partially unsaturated heterocycle, any of which is optionally substituted; X is one or O, S, NR24, CR25R26, C(O), NR24C(O), C(O)NR24, SO, SO2 or a covalent bond; where R24, R25 and R26 are independently hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, aryl, aminoalkyl, hydroxyalkyl, alkoxyalkyl or carboxyalkyl.Type: GrantFiled: October 21, 1999Date of Patent: September 2, 2003Assignee: Euro-Celtique S.A.Inventors: Yan Wang, Sui Xiong Cai, Nancy C. Lan, John F. W. Keana, Victor I. Ilyin, Eckard Weber
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Publication number: 20030134868Abstract: The present invention provides a composition for treating pain. The composition includes a pharmaceutically acceptable analgesic with addictive liability and a GABAergic agent, such as gamma vinyl GABA (GVG) or topiramate, which is effective in reducing or eliminating the addictive liability of the analgesic without interfering with its pain relieving properties.Type: ApplicationFiled: January 2, 2003Publication date: July 17, 2003Inventors: Stephen L. Dewey, Jonathan D. Brodie, Charles R. Ashby
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Publication number: 20030130344Abstract: An adjuvant composition comprising noscapine and its derivatives, for use in the treatment of tumors, cancer, as an adjuvant for vaccines.Type: ApplicationFiled: November 6, 2002Publication date: July 10, 2003Inventors: Judith Kapp, Yong Ke
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Publication number: 20030087957Abstract: Disclosed are novel &agr;-aryl-N-alkylnitrone compounds and pharmaceutical compositions containing such compounds. The disclosed compositions are useful as therapeutics for preventing and/or treating neurodegenerative, autoimmune and inflammatory conditions in mammals and as analytical reagents for detecting free radicals.Type: ApplicationFiled: February 11, 2002Publication date: May 8, 2003Inventors: Judith A. Kelleher, Kirk R. Maples, Alina Dykman, Yong-Kang Zhang, Allan L. Wilcox, Julian Levell
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Publication number: 20030087945Abstract: Compounds of formula (I) 1Type: ApplicationFiled: June 13, 2002Publication date: May 8, 2003Applicant: Aventis Pharma Deutschland GmbHInventors: Werner Thorwart, Wilfried Schwab, Manfred Schudok, Burkhard Haase
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Patent number: 6559179Abstract: This invention relates to the use of compounds as inhibitors of the fatty acid synthase FabH.Type: GrantFiled: February 5, 2002Date of Patent: May 6, 2003Assignee: SmithKline Beecham CorporationInventors: Dimitri Gaitanopoulos, Jack D. Leber, Mei Li, Joseph Weinstock
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Publication number: 20030069304Abstract: The present invention relates to a method for the preparation of citalopram comprising reduction of a compound of formula 1Type: ApplicationFiled: September 9, 2002Publication date: April 10, 2003Applicant: H. Lundbeck A/SInventor: Hans Petersen
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Publication number: 20030064977Abstract: The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.Type: ApplicationFiled: March 8, 2002Publication date: April 3, 2003Applicant: Vertex Pharmaceuticals, Inc.Inventors: Roger D. Tung, Mark A. Murcko, Govinda R. Bhisetti
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Patent number: 6518291Abstract: The present invention relates to a novel class of compounds which are IMPDH inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting IMPDH enzyme activity and consequently, may be advantageously used as therapeutic agents for IMPDH mediated processes. This invention also relates to methods for inhibiting the activity of IMPDH using the compounds of this invention and related compounds.Type: GrantFiled: September 14, 1999Date of Patent: February 11, 2003Assignee: Vertex Pharmaceuticals, IncorporatedInventors: Jeffrey O. Saunders, David M. Armistead, Michael C. Badia, Randy S. Bethiel, Catherine A. Frank, Doug Naegele, Perry M. Novak, David A. Pearlman, Steven M. Ronkin
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Patent number: 6509369Abstract: This invention relates to anti-inflammatory compounds, methods of making such compounds and methods of using such compounds having the following structure:Type: GrantFiled: January 8, 2002Date of Patent: January 21, 2003Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Malcolm K. Scott, Pauline J. Sanfilippo, Louis J. Fitzpatrick, III, Richard Cordova, Kevin Pan, Joseph Meschino
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Patent number: 6509379Abstract: Phenylacetic acid derivatives of the formula I where the variables are as disclosed herein, their salts, processes and intermediates for their preparation, and their use for controlling harmful fungi and animal pests.Type: GrantFiled: April 23, 1998Date of Patent: January 21, 2003Assignee: BASF AktiengesellschaftInventors: Herbert Bayer, Hubert Sauter, Klaus Oberdorf, Wassilios Grammenos, Thomas Grote, Reinhard Kirstgen, Bernd Müller, Ruth Müller, Franz Röhl, Eberhard Ammermann, Volker Harries, Gisela Lorenz, Siegfried Strathmann, Norbert Götz, Albrecht Harreus
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Patent number: 6498172Abstract: 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: GrantFiled: August 20, 1999Date of Patent: December 24, 2002Assignee: Pfizer Inc.Inventors: Kimberly O. Cameron, Bruce A. Lefker, Robert L. Rosati
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Patent number: 6489348Abstract: Fungicidal mixtures comprise as active components a) an amide compound of the formula I A—CO—NR1R2 I in which A, R1 and R2 are as defined in the description, and b) compounds of the formula II, their N-oxide or one of their salts where the substituents R12 to R18 are as defined in the description, and/or c) compounds of the formula III where the substituents X1 to X5 and R19 to R22 are as defined in the description, in a synergistically effective amount.Type: GrantFiled: September 24, 2001Date of Patent: December 3, 2002Assignee: BASF AktiengesellschaftInventors: Klaus Schelberger, Maria Scherer, Karl Eicken, Manfred Hampel, Eberhard Ammermann, Gisela Lorenz, Siegfried Strathmann
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Patent number: 6486198Abstract: The application relates to the use of topiramate and related sulfamates for the treatment and/or prophylaxis of post traumatic stress disorder (PTSD).Type: GrantFiled: March 11, 2002Date of Patent: November 26, 2002Inventor: Jeffrey Berlant
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Publication number: 20020161030Abstract: The following products:Type: ApplicationFiled: January 16, 2002Publication date: October 31, 2002Applicant: Hoechst Marion RousselInventors: Pierre Deprez, Jacques Dumas, Jacques Guillaume
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Patent number: 6458827Abstract: A method of modifying or altering the structure of a 1&agr;-hydroxylated vitamin D compound to increase its biological activity by altering the conformational equilibrium of the A-ring to favor a chair conformation that presents the 1&agr;-hydroxyl in the axial orientation. This is accomplished by either locking the A-ring chair conformation in a geometry having an axially orientated 1&agr;-hydroxyl, or by the addition of one or more substituents to the A-ring which interact with other substituents in the molecule or on the A-ring to provide a driving force to the A-ring to adopt a chair conformation which presents the 1&agr;-hydroxyl in the axial orientation.Type: GrantFiled: July 20, 2001Date of Patent: October 1, 2002Assignee: Wisconsin Alumni Research FoundationInventors: Hector F. DeLuca, Rafal R. Sicinski
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Patent number: 6458843Abstract: This invention is related to carbocyclic and heterocyclic substituted semicarbazones and thiosemicarbazones represented by Formula I: or a pharmaceutically acceptable salt or prodrug thereof, wherein: Y is oxygen or sulfur; R1, R21, R22 and R23 are independently hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, aryl, aminoalkyl, hydroxyalkyl, alkoxyalkyl or carboxyalkyl; or R22 and R23, together with the N, form a heterocycle; A1 and A2 are independently aryl, heteroaryl, saturated or partially unsaturated carbocycle or saturated or partially unsaturated heterocycle, any of which is optionally substituted; X is one or O, S, NR24, CR25R26, C(O), NR24C(O), C(O)NR24, SO, SO2 or a covalent bond; where R24, R25 and R26 are independently hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, aryl, aminoalkyl, hydroxyalkyl, alkoxyalkyl or carboxyalkyl.Type: GrantFiled: October 21, 1999Date of Patent: October 1, 2002Assignee: Euro-Celtique S.A.Inventors: Yan Wang, Sui Xiong Cai, Nancy C. Lan, John F. W. Keana, Victor I. Ilyin, Eckard Weber
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Publication number: 20020137762Abstract: The present invention relates to methods useful for the treatment of neoplastic diseases, tumor cells, and the treatment of cancer delivering compounds of the formula 1Type: ApplicationFiled: January 25, 2002Publication date: September 26, 2002Inventors: Harish C. Joshi, Keqiang Ye, Judith Kapp, Jaren Landen, David Archer, Cheryl Armstrong, Fuqiang Liu
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Patent number: 6451792Abstract: A medical composition containing, as an active constituent, a nitroetheneamine derivative represented by the formula (I): wherein the substituents are as defined in the disclosure, its stereoisomers, its tautomers or a salt thereof.Type: GrantFiled: March 20, 2001Date of Patent: September 17, 2002Assignee: Ishihara Sangyo Kaisha Ltd.Inventors: Fuminori Kato, Keizo Miyata, Hirohiko Kimura, Kazuhiro Yamamoto, Hiroyuki Ikegami, Hiromi Takeo
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Patent number: 6448295Abstract: The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N-fused-phenyl-N-benzyl aminoalcohols.Type: GrantFiled: November 14, 2001Date of Patent: September 10, 2002Assignee: G.D. Searle & Co.Inventors: James A. Sikorski, Richard C. Durley, Deborah A. Mischke, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Margaret L. Grapperhaus, Brian S. Hickory, Mark A. Massa, Monica B. Norton, William F. Vernier, Barry L. Parnas, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
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Publication number: 20020120005Abstract: The present invention relates to the process for the preparation and purification of citalopram (I) 1Type: ApplicationFiled: January 8, 2002Publication date: August 29, 2002Applicant: H. Lundbeck A/SInventors: Marco Villa, Federico Sbrogio, Robert Dancer
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Patent number: 6441028Abstract: A phytomicrobicidal composition comprising such an amount of at least two active ingredient components that a synergistic effect is achieved, together with a suitable carrier material, wherein component I is a compound of the formula I in which: X is CH or N; R is CH3 or cyclopropyl; Y is H, F, Cl, Br, CF3, CF3O, propargyloxy; Z is H, F, Cl, CF3, CF3O; or Y and Z together are a methylenedioxy, a (difluoromethylene)dioxy, an ethylenedioxy, a (trifluoroethylene)dioxy or a benzo group; and wherein component II is a compound selected from the group consisting of II A) metalaxyl, II B) R-metalaxyl, II C) furalaxyl, II D) benalaxyl, II E) ofurace, II F) oxadixyl, II G) cymoxanil and II H) mancozeb.Type: GrantFiled: August 13, 2001Date of Patent: August 27, 2002Assignee: Bayer AktiengesellschaftInventors: Gertrude Knauf-Beiter, Ronald Zeun
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Patent number: 6436914Abstract: Compounds are provided having the formula including pharmaceutically acceptable salts thereof, wherein R1 is lower alkyl, aryl or arylalkyl; A is hydrogen or B is hydrogen, alkyl, alkenyl, or but when A is hydrogen, B may only be R2, R2′, R2″, R3 R3′ and R3″ are as defined herein; m is 0−3. These compounds possess activity at the beta 3 adrenergic receptor in mammals and are useful in the treatment of diabetes, obesity, depression, achalasia and intestinal hypermotility disorders.Type: GrantFiled: July 25, 2001Date of Patent: August 20, 2002Assignee: Bristol-Myers Squibb CompanyInventors: Philip M. Sher, William N. Washburn, Jollie D. Godfrey, Jr.
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Publication number: 20020103192Abstract: Substituted trifluoromethyl ketones, ketooxazoles, ketoamides, ketoesters, and diketones having the formula 1Type: ApplicationFiled: March 14, 2001Publication date: August 1, 2002Inventors: Michael L. Curtin, Steven K. Davidsen, Robin R. Frey, Howard R. Heyman, Michael R. Michaelides, Anil Vasudevan, Carol K. Wada
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Patent number: 6420427Abstract: An aminobutyric acid derivative of the formula (I): (wherein all symbols are as defined in the specification) and salt thereof. salt thereof. The compounds of the formula (I) possess an inhibitory activity on matrix metalloproteinase and are useful for prevention and/or treatment of diseases, for example, rheumatoid diseases, arthrosteitis, unusual bone resorption, osteoporosis, periodontitis, interstitial nephritis, arteriosclerosis, pulmonary emphysema, cirrhosis, cornea injury, metastasis of, invasion of or growth of tumor cells, autoimmune disease (e.g. Crohn's disease, Sjogren's syndrome), disease caused by vascular emigration or infiltration of leukocytes, arterialization, multiple sclerosis, aorta aneurysm, endometriosis.Type: GrantFiled: April 7, 2000Date of Patent: July 16, 2002Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Kanji Takahashi, Tsuneyuki Sugiura
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Patent number: 6407100Abstract: The invention relates to novel compounds of the formula in which R1 is C1-4alkyl and (Y—X) is CH2, C1-2alkylthio-CH═ or C1-2alkyl-ON═ and Z is an aldimino or ketimino group, and to their preparation, as well as fungicidal compositions with such compounds as active substances. The compounds can be employed for controlling fungi in agriculture, in horticulture and in wood preservation.Type: GrantFiled: September 1, 1993Date of Patent: June 18, 2002Assignee: Bayer AktiengesellschaftInventors: Hans Peter Isenring, Bettina Weiss
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Patent number: 6391919Abstract: This invention relates generally to bis-amino acid sulfonamides containing substituted benzyl amines of formula I: or stereoisomeric forms, stereoisomeric mixtures, or pharmaceutically acceptable salt forms thereof, which are useful as HIV protease inhibitors, pharmaceutical compositions and diagnostic kits comprising the same, methods of using the same for treating viral infection or as assay standards or reagents, and intermediates and processes for making the same.Type: GrantFiled: January 12, 2000Date of Patent: May 21, 2002Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Robert F. Kaltenbach, George L. Trainor
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Patent number: 6388131Abstract: The invention provides compounds, compositions and methods relating to novel electrophilic aromatic derivatives and their use as pharmacologically active agents. The compositions find particular use as pharmacological agents in the treatment of disease states, particularly cancer, psoriasis, vascular restenosis, infections, atherosclerosis and hypercholesterolemia, or as lead compounds for the development of such agents.Type: GrantFiled: May 31, 2001Date of Patent: May 14, 2002Assignee: Tularik, Inc.Inventors: Julio Cesar Medina, David Louis Clark, John A. Flygare, Terry J. Rosen, Bei Shan
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Publication number: 20020052405Abstract: This invention provides a method of treating obesity, generalized anxiety disorder, post-traumatic stress disorder, late luteal phase disphoric disorder (premenstrual syndrome), attention deficit disorder, with and without hyperactivity, Gilles de la Tourette syndrome, bulimia nervosa or Shy Drager Syndrome in a mammal by administering to the mammal an effective amount of a hydroxycycloalkanephenethyl amine of the following structural formula: 1Type: ApplicationFiled: November 30, 2001Publication date: May 2, 2002Inventors: Richard L. Rudolph, Albert T. Derivan, Eric A. Muth, G. Virginia Upton
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Patent number: 6376535Abstract: The present invention relates to oxygen-containing heterocyclic compounds represented by the following formula (I): wherein m represents an integer of 0 to 4; R1, R2, R3 and R4 independently represent a hydrogen atom, substituted or unsubstituted lower alkyl, etc.; R5 represents substituted or unsubstituted lower alkoxy etc.; R6 represents a hydrogen atom etc.; and Y represents the following formula (II): wherein R9 represents cyano etc., R10 represents a hydrogen atom etc., R11 represents carboxy etc., and R12 represents a hydrogen atom etc.; and the like; or pharmaceutically acceptable salts thereof.Type: GrantFiled: March 1, 2001Date of Patent: April 23, 2002Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Etsuo Ohshima, Koji Yanagawa, Haruhiko Manabe, Ichiro Miki, Yoshiaki Masuda
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Patent number: 6376538Abstract: 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: GrantFiled: September 19, 1997Date of Patent: April 23, 2002Assignee: Biogen, Inc.Inventors: Steven P. Adams, Ko-Chung Lin, Wen-Cherng Lee, Alfredo C. Castro, Craig N. Zimmerman, Charles E. Hammond, Yu-Sheng Liao, Julio Hernan Cuervo, Juswinder Singh