Having -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To The Morpholine Ring Patents (Class 514/237.5)
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Publication number: 20040176373Abstract: A method for the treatment of diabetes mellitus, especially Type II diabetes and the cardiac conditions associated with diabetes mellitus in a mammal such as a human, which method comprises administering an effective non-toxic and pharmaceutically acceptable amount of an insulin sensitizer, such as Compound (I), and an agent used in the treatment of the cardiac conditions associated with diabetes mellitus.Type: ApplicationFiled: March 18, 2004Publication date: September 9, 2004Applicant: SmithKline Beecham p.l.c.Inventor: Robin Edwin Buckingham
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Publication number: 20040167126Abstract: Compounds having the formula 1Type: ApplicationFiled: February 19, 2004Publication date: August 26, 2004Inventors: Richard A. Craig, Megumi Kawai, Linda M. Lynch, Jyoti R. Patel, George S. Sheppard, Jieyi Wang, Fan Yang, Nwe Ba-Maung, Xenia Beebe Searle
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Publication number: 20040167128Abstract: Compounds having methionine aminopeptidase-2 inhibitory (MetAP2) are described. Also described are pharmaceutical compositions comprising the compounds, methods of treatment using the compounds, methods of inhibiting angiogenesis, and methods of treating cancer.Type: ApplicationFiled: October 8, 2003Publication date: August 26, 2004Inventors: Kenneth M. Comess, Scott A. Erickson, Jack Henkin, Douglas M. Kalvin, Megumi Kawai, Ki H. Kim, Nwe Y. BaMaung, Chang Hoon Park, George S. Sheppard, Anil Vasudevan, Jieyi Wang, David M. Barnes, Steve D. Fidanze, Lawrence Kolaczkowski, Robert A. Mantei, David C. Park, William J. Sanders, Jason S. Tedrow, Gary T. Wang
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Publication number: 20040167131Abstract: This invention discloses amino acid derivatives which display inhibitory effects on the serine protease factor Xa. The invention also discloses pharmaceutically acceptable salts of the compounds, pharmaceutically acceptable compositions comprising the compounds or their salts, methods for the preparation of the compounds, and methods of using them as therapeutic agents for treating or preventing disease states in mammals characterized by abnormal thrombosis.Type: ApplicationFiled: September 11, 2003Publication date: August 26, 2004Applicant: Pfizer Inc.Inventors: Gary Louis Bolton, Kevin James Filipski, Jeffrey Thomas Kohrt, Frances La, Daniele Marie Leonard
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Publication number: 20040167116Abstract: 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: February 24, 2004Publication date: August 26, 2004Applicant: Vertex Pharmaceuticals IncorporatedInventors: Roger D. Tung, Mark A. Murcko, Govinda Rao Bhisetti
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Publication number: 20040157836Abstract: Compounds having methionine aminopeptidase-2 inhibitory (MetAP2) are described. Also described are pharmaceutical compositions comprising the compounds, methods of treatment using the compounds, methods of inhibiting angiogenesis, and methods of treating cancer.Type: ApplicationFiled: September 23, 2003Publication date: August 12, 2004Inventors: Kenneth M. Comess, Scott A. Erickson, Jack Henkin, Douglas M. Kalvin, Megumi Kawai, Ki H. Kim, Nwe Y. BaMaung, Chang Hoon Park, George S. Sheppard, Anil Vasudevan, Jieyi Wang, David M. Barnes, Steve D. Fidanze, Lawrence Kolaczkowski, Robert A. Mantei, David C. Park, William J. Sanders, Jason S. Tedrow, Gary T. Wang
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Publication number: 20040127477Abstract: The present invention relates to a class of compounds represented by the Formula I 1Type: ApplicationFiled: November 20, 2003Publication date: July 1, 2004Applicant: G. D. Searle & Co.Inventors: Nizal Samuel Chandrakumar, Bipinchandra Nanubhai Desai, Balekudru Devadas, Alan Frank Gasiecki, Renee Huff, Ish K. Khanna, James W. Malecha, Julie M. Miyashiro, Shashidhar N. Rao, Joseph Gerace Rico, Thomas Edward Rogers, Peter Gerrard Ruminski, Mark Andrew Russell, Yi Yu
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Publication number: 20040116414Abstract: This invention is directed to a class of compounds (Formula I) including succinoyl amino pyrazoles, succinoyl amino thiadiazoles, succinoyl amino acid esters, succinoyl amino acid amides, succinoyl amino alcohols, succinoyl amino ketones, succinoyl amino hydantoins, succinoyl anilines, and succinoyl derivatives of privileged structures. The invention is also directed to a pharmaceutical formation comprising such compound in a pharmaceutically acceptable salt form or prodrug thereof. The invention is further directed to a method for inhibiting &bgr;-amyloid peptide release and/or synthesis, a method for inhibiting &ggr;-secretase activity and a method for treating neurological disorders associated with &bgr;-amyloid peptide production. The method comprises administering to a host a pharmaceutical formulation comprising an effective amount of a compound of Formula I. The compounds of Formula I are useful in the prevention and treatment of Alzheimer's disease.Type: ApplicationFiled: May 7, 2003Publication date: June 17, 2004Inventors: Jay S. Tung, Ashley C. Guinn, Eugene D. Thorsett, Michael A. Pleiss
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Publication number: 20040116408Abstract: The present invention is generally drawn to novel isolated therapeutic agents, termed resolving, generated from the interaction between a dietary omega-3 polyunsaturated fatty acid (PUFA) such as eicosapentaenoic acid (EPA) or docosahexaenoic acid (DHA), cyclooxygenase-II (COX-2) and an analgesic, such as aspirin (ASA). Surprisingly, careful isolation of compounds generated from the combination of components in an appropriate environment provide di- and tri-hydroxy EPA or DHA compounds having unique structural and physiological properties. The present invention therefore provides for many new useful therapeutic di- or tri-hydroxy derivatives of EPA or DHA (resolvins) that diminish, prevent, or eliminate inflammation or PMN migration, for example. The present invention also provides methods of use, methods of preparation, and packaged pharmaceuticals for use as medicaments for the compounds disclosed throughout the specification.Type: ApplicationFiled: August 12, 2003Publication date: June 17, 2004Inventor: Charles N. Serhan
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Publication number: 20040110753Abstract: The compounds of the invention are inhibitors of alpha4 containing integrin-mediated binding to ligands such as VCAM-1 and MAdCAM.Type: ApplicationFiled: July 16, 2002Publication date: June 10, 2004Applicant: Genentech, Inc.Inventors: David Y. Jackson, Frederick C. Sailes, Daniel P. Sutherlin
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Publication number: 20040110831Abstract: The invention relates to the compounds of general formula (I), that are present with respect to R1 as racemates as well as L- or D-configured compounds and as E/Z mixtures as well as E or Z isomers and in which the various symbols are defined as in the description and the claims, as well as to the salts thereof, for use as therapeutic agents and for diagnostic purposes. The inventive compounds can be processed to medicaments or to diagnostic agents that are used for the diagnosis, therapy and prevention of urokinase- or urokinase-receptor associated diseases, for example for the treatment of tumors. The compounds are highly efficient in inhibiting growth and/or spread of malign tumors, for example tumor spread of pancreatic cancer, tumor growth of breast cancer and the formation of tumor metastases. The compounds of formula (I) and the salts thereof can be produced by conventional methods.Type: ApplicationFiled: September 18, 2003Publication date: June 10, 2004Inventor: Hugo Ziegler
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Publication number: 20040077616Abstract: The present invention relates to the use of compounds of formula (I) 1Type: ApplicationFiled: October 22, 2002Publication date: April 22, 2004Inventors: Youssef L. Bennani, William H. Bunnelle, Sou-Jen Chang, Sanjay R. Chemburkar, Jinhua Chen, Michael J. Dart, Dilinie P. Fernando, Yi-Yin Ku, Mark Lockwood, Lei Wang
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Publication number: 20040077638Abstract: The invention relates to novel compounds which bind to integrin receptors, their use as ligands of integrin receptors, in particular as ligands of the &agr;v&bgr;3 integrin receptor, and pharmaceutical preparations comprising these compounds.Type: ApplicationFiled: September 8, 2003Publication date: April 22, 2004Inventors: Herve Geneste, Andreas Kling, Arnulf Lauterbach, Claudia Isabella Graef, Thomas Subkoski, Wilfried Hornberger
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Publication number: 20040077646Abstract: Compounds of the formula (I) 1Type: ApplicationFiled: June 2, 2003Publication date: April 22, 2004Inventors: Joe Timothy Bamberg, Tobias Gabriel, Nancy Elisabeth Krauss, Taraneh Mirzadegan, Wylie Solang Palmer, David Bernard Smith
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Publication number: 20040077618Abstract: The present invention relates to the use of compounds of formula (I) 1Type: ApplicationFiled: October 22, 2002Publication date: April 22, 2004Inventors: Youssef L. Bennani, Steve A. Chamberlin, Sanjay R. Chemburkar, Jinhua Chen, Michael J. Dart, Ashok K. Gupta, Lei Wang
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Publication number: 20040077639Abstract: Therapeutic methods for the prevention and treatment of respiratory diseases or conditions are described, the methods including administering to a subject in need thereof a respiratory disease or condition effective amount of a selective inhibitor of inducible nitric oxide synthase.Type: ApplicationFiled: May 16, 2003Publication date: April 22, 2004Inventor: Pamela T. Manning
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Publication number: 20040077617Abstract: The present invention relates to the use of compounds of formula (I) 1Type: ApplicationFiled: October 22, 2002Publication date: April 22, 2004Inventors: Youssef L. Bennani, Sou-Jen Chang, Sanjay R. Chemburkar, Michael J. Dart, Dilinie P. Fernando, Timothy A. Grieme
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Patent number: 6723753Abstract: 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-benzyl-N-phenyl aminoalcohols.Type: GrantFiled: February 7, 2002Date of Patent: April 20, 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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Publication number: 20040072816Abstract: The present invention relates to sulfanilide derivatives of formula (I), in which R1 and R2 are optionally substituted aryl and heteroaryl groups and the other variables are as defined in the claims, for use as pharmaceutically active compounds, as well as pharmaceutical formulations containing such sulfanilide derivatives. Said derivatives are useful in the treatment and/or prevention of preterm labor, premature birth, dysmenorrhea, inappropriate secretion of vasopressin, congestive heart failure, arterial hypertension, liver cirrhosis, nephrotic syndrome and ocular hypertension. In particular, the present invention is related to sulfanilide derivatives displaying a substantial modulatory, in particular antagonistic activity, of the oxytocin and/or vasopressin receptor.Type: ApplicationFiled: September 25, 2003Publication date: April 15, 2004Inventors: Anna Quattropani, Matthias Schwarz, Catherine Joran-Lebrun, Dennis Church, Alexander Scheer
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Patent number: 6720323Abstract: The invention related to colchinol derivatives of the formula (I): Wherein: R1, R2 and R3 are each independently hydroxy, phosphoryloxy (—OPO3H2), C1-4alkoxy or an in vivo hydrolysable ester of hydroxy, with the proviso that at least 2 of R1, R2 and R3 are C1-4alkoxy; A is —CO—, —C(O)O—, —CON(R8)— (wherein R8 is hydrogen, C1-4alkyl, C1-3alkoxyC1-3alkyl, aminoC1-3alkyl or hydroxyC1-3alkyl); a is an integer from 1 to 4 inclusive; Ra and Rb are independently selected from hydrogen, hydroxy and amino; B is —O—, —CO—, N(R9)CO—, —CON(R9)—, —N(R9)C(O)O—, —N(R9)CON(R10)—, —N(R9)SO2—, —SO2N(R9)— or a direct single blond (wherein R9 and R10 are independently selected from hydrogen, C1-4alkyl, C1-3alkoxyC1-3alkyl, aminoC1-3alkyl and hydroxyC1-3alkyl); b is 0 or an integer from 1 to 4 inclusive, (provided that when b is 0, B is a single direct bond); D is carboxy, sulpho, tetrazolyl, imidazoType: GrantFiled: January 7, 2003Date of Patent: April 13, 2004Assignee: Angiogene Pharmaceuticals LimitedInventor: Jean Claude Arnould
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Publication number: 20040063698Abstract: The present invention provides compounds of Formula (I): 1Type: ApplicationFiled: July 31, 2003Publication date: April 1, 2004Inventor: Thomas P. Maduskuie
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Publication number: 20040058904Abstract: The present invention relates to compounds of the general formula (I), processes for their preparation, pharmaceutical compositions containing them as well as their use for the production of pharmaceutical compositions for the treatment of inflammatory diseases.Type: ApplicationFiled: September 29, 2003Publication date: March 25, 2004Inventors: Thomas Rolle, Thomas Lehmann, Markus Albers, Gerhard Hebler, Gerhard Muller, Rudiger Fischer, Masaomi Tajimi, Karl Ziegelbauer, Kevin Bacon, Haruki Hasegawa, Hiromi Okigami
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Publication number: 20040053920Abstract: This invention provides caspase inhibitors of formula I: 1Type: ApplicationFiled: August 21, 2003Publication date: March 18, 2004Inventors: David Bebbington, Ronald Knegtel, Michael Mortimore, David Kay, Julian M.C. Golec
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Publication number: 20040048851Abstract: The compounds of the formula (formula 1) and pharmaceutically acceptable salts thereof and a process for preparing the same and pharmaceutical compositions containing the same are described wherein the substituents have the meaning as specified in the description. The compounds are used as thrombon inhibitors.Type: ApplicationFiled: June 3, 2003Publication date: March 11, 2004Inventors: Uros Urleb, Anamarija Zega, Mojca Stegnar, Bakija Alenka Trampus, Tomas Solmajer, Gregor Mlinsek
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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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Publication number: 20040019038Abstract: Disclosed are novel aromatic compounds which are useful for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases. Also disclosed are pharmaceutical compositions containing and processes of making such compounds.Type: ApplicationFiled: July 21, 2003Publication date: January 29, 2004Applicant: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Pier F. Cirillo, Steffen Breitfelder, Usha R. Patel, John Robert Proudfoot, Alan D. Swinamer, Hidenori Takahashi, Thomas A. Gilmore, Rajiv Sharma
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Publication number: 20030225071Abstract: Compounds of the formula: 1Type: ApplicationFiled: June 11, 2002Publication date: December 4, 2003Inventors: Stacie S. Canan Koch, Therese N. Alexander, Mark Barvian, Gary Bolton, Fredrick E. Boyer, Benjamin J. Burke, Tod Holler, Tanya M. Jewell, Vara Prasad Josyula, David J. Kucera, Maria A. Linton, Jeffrey J. Machak, Lennert J. Mitchell, Sean T. Murphy, Siegfried H. Reich, Donald J. Skalitzky, John H. Tatlock, Michael D. Varney, Scott C. Virgil, Stephen E. Webber, Stephen T. Worland, Michael Melnick
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Patent number: 6649612Abstract: Compounds of formula (I): in which: Ar represents an aromatic or a heteroaromatic radical optionally substituted, in particular, with an alkyl or a carboxyl group, R2 and R3 represent, in particular, H or alkyl, or R2 and R3, taken together, form a 5- or 6-membered ring, R4 and R5 represent, in particular, H or halogen, R6 represents, in particular, H or lower alkyl, and the salts of the compounds of formula (I). These compounds can be used in particular in the treatment of dermatological complaints associated with a keratinization disorder, and for combating ageing of the skin.Type: GrantFiled: August 21, 2001Date of Patent: November 18, 2003Assignee: Galderma Research & DevelopmentInventors: Jean-Michel Bernardon, Philippe Nedoncelle
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Publication number: 20030206935Abstract: The invention relates to novel compounds of formula (I) wherein R1 represents a polymer, aryl or alkyl group. R2 presents a hydrogen atom, a halogen atom, a radical CN, CF3, OH, OCF3, COOH, R7, OR7 or OCOR7, R3 represents an aryl or alkyl halogen, R4 represents an alkyl radical. The invention also relates to a cosmetic composition comprising said compounds and to the use thereof to reduce and/or curb hair loss i.e. to increase and/or stimulate the growth of said hair.Type: ApplicationFiled: April 4, 2003Publication date: November 6, 2003Applicant: L'OrealInventors: Jean-Baptiste Galey, Maria Dalko, Lionel Breton
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Publication number: 20030203890Abstract: The present invention relates generally to methods for treating or preventing nerve injury in a warm-blooded animal caused as a consequence of surgery by administering neurotrophic compounds described below. The invention relates more specifically to methods for treating or preventing nerve injury caused as a consequence of prostate surgery as well as erectile dysfunction.Type: ApplicationFiled: May 29, 2002Publication date: October 30, 2003Inventors: Joseph P. Steiner, Solomon Snyder, Arthur L. Burnett
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Patent number: 6638930Abstract: Substituted heterocycles of the general structural formula: are tachykinin receptor antagonists useful in the treatment of inflammatory diseases, pain or migraine, asthma and emesis, and calcium channel blockers useful in the treatment of cardiovascular conditions such as angina, hypertension or ischemia.Type: GrantFiled: April 17, 2001Date of Patent: October 28, 2003Assignee: Merck & Co. Inc.Inventors: Conrad P. Dorn, Paul E. Finke, Jeffrey J. Hale, Malcolm Maccoss, Sander G. Mills, Shrenik K. Shah, Mark Stuart Chambers, Timothy Harrison, Tamara Ladduwahetty, Brian John Williams
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Publication number: 20030199508Abstract: Compounds of formula I: 1Type: ApplicationFiled: December 20, 2002Publication date: October 23, 2003Inventors: Santiago Conde Ruzafa, Ana Martinez Gil, Daniel Ignacio Perez Fernandez, Maria Concepcion Perez Martin, Francisco Jose Moreno Munoz, Francisco Wandosell Jurado
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Patent number: 6632816Abstract: The present invention provides HIV aspartyl protease inhibitors of the formula; and when the compound of formula I comprises an amino group, pharmaceutically acceptable ammonium salts thereof, wherein n is 3 or 4, wherein R1 may be, for example, iso-butyl, wherein X and Y, same or different, may be, for example, NH2 and F, and wherein R2 and R3 are as defined herein.Type: GrantFiled: December 23, 2002Date of Patent: October 14, 2003Assignee: Pharmacor Inc.Inventors: Brent Richard Stranix, Jean-François Lavallée, Nicolas LeBerre, Valérie Perron
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Publication number: 20030171352Abstract: The present invention relates to compounds of the formula I 1Type: ApplicationFiled: January 24, 2003Publication date: September 11, 2003Applicant: Aventis Pharma Deutschland GmbHInventors: Ursula Schindler, Karl Schoenafinger, Hartmut Strobel
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Publication number: 20030166644Abstract: Use of compounds to inhibit hormone-sensitive lipase, pharmaceutical compositions comprising the compounds, methods of treatment employing these compounds and compositions, and novel compounds. The present compounds are inhibitors of hormone-sensitive lipase and may be useful in the treatment and/or prevention of medical disorders where a decreased activity of hormone-sensitive lipase is desirable.Type: ApplicationFiled: December 13, 2002Publication date: September 4, 2003Inventors: Soren Ebdrup, Johannes Cornelis de Jong, Poul Jacobsen, Holger Claus Hansen, Per Vedso
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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: 20030162778Abstract: The compounds have a structure according to the following Formula (I): 1Type: ApplicationFiled: September 18, 2002Publication date: August 28, 2003Applicant: The Procter and Gamble CompanyInventors: Michael George Natchus, Stanislaw Pikul, Neil Gregory Almstead, Matthew John Laufersweiler, Roger Gunnard Bookland, Joshua Spector Tullis, Biswanath De
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Publication number: 20030161860Abstract: The present invention relates to novel compounds possessing specific hot, pungent and spicy taste when subjected to direct pungency evaluation, which may be useful as food additives and anti-oxidants, however the said compounds do not add to any nutritional value but the synthesised compounds can possess useful pharmacological properties which is expected to find application in new test models for the development of anti-inflammatory drugs, bioavailability enhancers and for the study of hepatic drug metabolising mechanism; also relates to a process for preparing the said compounds.Type: ApplicationFiled: February 7, 2002Publication date: August 28, 2003Inventors: Subhash Chandra Taneja, Surrinder Koul, Jawahir Lal Koul, Beenu Moza, Sukhdev Swami Handa
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Patent number: 6610689Abstract: A compound selected from the group consisting of a compound of formula I a compound of formula II and when the compound of formula I and II comprises an amino group pharmaceutically acceptable ammonium salts thereof, wherein R1, R2, Cx, n, R3, R4, R5, Y are as defined in the specification.Type: GrantFiled: September 17, 2002Date of Patent: August 26, 2003Assignee: Pharmacor Inc.Inventors: Brent Richard Stranix, Gilles Sauvé, Abderrahim Bouzide, Alexandre Coté, Gervais Bérubé, Patrick Soucy, Yongsen Zhao, Jocelyn Yelle
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Publication number: 20030158180Abstract: A compound having the general formula (Ia) and methods of using such compounds for the treatment of diseases and pharmaceutical composition comprising such compounds.Type: ApplicationFiled: October 3, 2002Publication date: August 21, 2003Inventor: Peter Bernstein
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Patent number: 6605626Abstract: 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: GrantFiled: September 21, 2001Date of Patent: August 12, 2003Assignee: Eli Lilly and CompanyInventors: 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
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Publication number: 20030144292Abstract: The compounds have a structure according to the following Formula (I): 1Type: ApplicationFiled: September 18, 2002Publication date: July 31, 2003Inventors: Michael George Natchus, Stanislaw Pikul, Neil Gregory Almstead, Matthew John Laufersweiler, Biswanath De
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Publication number: 20030144234Abstract: The invention discloses cathepsin S as a suitable target for the development of new therapeutics to treat or ameliorate chronic pain. The invention relates to methods to treat and/or ameliorate chronic pain and pharmaceutical compositions therefor comprising modulators with inhibitory effect on cathepsin S enzyme activity and/or cathepsin S gene expression. The invention also relates to a method to identify compounds with therapeutic usefulness to treat chronic pain, comprising identifying compounds that can inhibit cathepsin S activity and/or gene expression which can also reverse the pathological effects of chronic pain in vivo.Type: ApplicationFiled: August 28, 2002Publication date: July 31, 2003Inventors: Francis Paul Buxton, Pamposh Ganju, Christopher Robert Snell, Chuanzheng Song
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Patent number: 6596693Abstract: The present invention is directed to novel dipeptides thereof, represented by the general Formula I: where R1-R3 and AA are defined herein. The present invention relates to the discovery that compounds having Formula I are potent inhibitors of apoptotic cell death. Therefore, the inhibitors of this invention can retard or block cell death in a variety of clinical conditions in which the loss of cells, tissues or entire organs occurs.Type: GrantFiled: August 31, 2000Date of Patent: July 22, 2003Assignee: Cytovia, Inc.Inventors: John F. W. Keana, Sui Xiong Cai, John Guastella, Wu Yang, John A. Drewe, Eckard Weber
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Patent number: 6596752Abstract: The present invention relates to small molecules according to the formula [I]: which are potent inhibitors of &agr;4&bgr;1 mediated adhesion to either VCAM or CS-1 and which can be used for treating or preventing &agr;4&bgr;1 adhesion mediated conditions in a mammal such as a human.Type: GrantFiled: July 12, 2002Date of Patent: July 22, 2003Assignees: Tanabe Seiyaku Co., Ltd., Pharmacia & Upjohn CompanyInventors: Thomas J. Lobl, Bradley R. Teegarden, Alexander Polinsky, Gilbert M. Rishton, Masafumi Yamagishi, Steven Tanis, Jed F. Fisher, Edward W. Thomas, Robert A. Chrusciel
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Publication number: 20030125324Abstract: Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.Type: ApplicationFiled: August 15, 2002Publication date: July 3, 2003Inventors: Andrei W. Konradi, Michael A. Pleiss, Eugene D. Thorsett, Susan Ashwell, Gregory S. Welmaker, Anthony Kreft, Dimitrios Sarantakis, Darren B. Dressen, Francine S. Grant, Christopher Semko, Ying-Zi Xu
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Publication number: 20030119832Abstract: The present invention is in particular related to the use of rivastigmine in the manufacture of a medicament for the treatment of ocular disorders.Type: ApplicationFiled: January 23, 2003Publication date: June 26, 2003Inventor: David Goldblum
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Publication number: 20030119826Abstract: Therapeutic methods for the prevention and treatment of neurodegenerative conditions are described, the methods including administering to a subject in need thereof a neuroprotective effective amount of a selective inhibitor of inducible nitric oxide synthase.Type: ApplicationFiled: September 24, 2001Publication date: June 26, 2003Applicant: Pharmacia CorporationInventors: Pamela T. Manning, Jane R. Connor
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Patent number: 6583165Abstract: The invention provides compounds, compositions and methods relating to novel arylsulfonanilide 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: February 21, 2001Date of Patent: June 24, 2003Assignee: Tularik Inc.Inventor: Jonathan B. Houze
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Publication number: 20030109522Abstract: Therapeutic methods for the prevention and treatment of ophthalmologic conditions are described, the methods including administering to a subject in need thereof a selective inhibitor of inducible nitric oxide synthase.Type: ApplicationFiled: September 24, 2001Publication date: June 12, 2003Inventors: Pamela T. Manning, Jane R. Connor