1,2-oxazoles (including Hydrogenated) Patents (Class 546/272.1)
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Patent number: 7067538Abstract: The present invention relates to sulfones that are useful in the treatment of chemokine-mediated disorders. In certain embodiments, the present invention concerns the compounds that are MCP-1 receptor antagonists.Type: GrantFiled: May 21, 2003Date of Patent: June 27, 2006Assignee: Warner-Lambert Company, LLCInventors: Larry D. Bratton, Alexander J. Bridges, David T. Connor, Steven R. Miller, Yuntao Song, Kuai-Lin Sun, Bharat K. Trivedi, Paul C. Unangst
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Patent number: 7060710Abstract: The present invention provides compounds of formula I: in which: one of X and Y is a nitrogen atom substituted by a group R6? and the other is a carbon atom substituted by an isoxazole group substituted on its carbon atoms by groups R3 and R4; one of R6 and R6? is hydrogen; either all of W1, W2, W3 and W4 are carbon or one of W1, W2, W3 and W4 is nitrogen and the rest are carbon; and R1 and R2 are, independently, a small group, heteroaromatic ring or a 4–7 membered cyclic amine ring; processes for making them; pharmaceutical composition containing them; their use in therapy, particularly for enhancing cognition in conditions such as Alzheimer's Disease; and methods of treatment using them.Type: GrantFiled: November 22, 2002Date of Patent: June 13, 2006Assignee: Merck Sharp & Dohme Ltd.Inventors: Tamara Ladduwahetty, Angus Murray MacLeod, Kevin John Merchant, Francine Sternfeld
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Patent number: 7056932Abstract: The invention is concerned with novel heterocyclyl substituted 1-alkoxy acetic acid derivatives of formula (I) wherein R1 to R6 and A are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit the formation of coagulation factors Xa, IXa and thrombin induced by factor VIIa and tissue factor and can be used as medicaments.Type: GrantFiled: December 10, 2004Date of Patent: June 6, 2006Assignee: Hoffman-La Roche Inc.Inventors: Luca Claudio Gobbi, Katrin Groebke Zbinden, Peter Mohr, Ulrike Obst
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Patent number: 7022650Abstract: A description is given of 4-trifluoromethylpyrazolyl-substituted pyridines and pyrimidines of formula (I) and of their use as herbicides. In this formula (I) R1, R2, R3 and R4 are various radicals, A is an aromatic or heteroaromatic radical, and Z is a nitrogen or carbon atom.Type: GrantFiled: July 24, 2003Date of Patent: April 4, 2006Assignee: Bayer CropScience GmbHInventors: Michael Gerhard Hoffmann, Hendrik Helmke, Lothar Willms, Thomas Auler, Hermann Bieringer, Hubert Menne
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Patent number: 7015236Abstract: An N-heteroaryl-4-(haloalkyl)nicotinamide derivative represented by formula (I): [wherein R represents a C1–C6 haloalkyl group; R1 represents a hydrogen atom, a C1–C6alkyl group which may be substituted a C2–C6 alkenyl group or an acyl group; X represents a group represented by formula C—R2, or a nitrogen atom; R2 and R3 each independently represent a hydrogen atom, a halogen atom, a C1–C6 alkyl group which may be substituted, a C3–C7 cycloalkyl group, a C2–C6 alkenyl group, a C3–C7 cycloalkenyl group, a formyl group, a group represented by formula CH?NOR4, a cyano group, a phenyl group which may be substituted, a heterocyclic group which may be substituted, a C1–C6 alkoxy group which may be substituted, a C1–C6 alkylthio group or a phenoxy group]; or a salt thereof, a pesticide containing it as an active component, a method for producing it and intermediates thereof.Type: GrantFiled: November 19, 2002Date of Patent: March 21, 2006Assignee: Sankyo Agro Company, LimitedInventors: Shigeru Mio, Hideshi Okui
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Patent number: 6987189Abstract: A method of making a compound of Formula VI: wherein Tr is a triphenyl group; R1, R2 and R3 are each independently selected from the group consisting of H, C1–C4 alkyl, C1–C4 alkoxy, aryl, heteroaryl, and arylalkyl; R4 is C2–C6 alkyl, and R5 and R6 are each independently H or C1–C4 alkyl, involves the step of reacting a compound of Formula V: with Tr-OH to produce a compound of Formula VI. The compounds of Formula VI are useful as intermediates in the manufacture of antibiotic agents. Methods of making compounds of Formula V, and intermediates made or used in the foregoing methods, are also described.Type: GrantFiled: September 28, 2004Date of Patent: January 17, 2006Assignee: North Carolina State UniversityInventors: Daniel L. Comins, Shenlin Huang
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Patent number: 6974826Abstract: The present invention relates to certain substituted heterocycles of Formula (I) which are useful in the treatment of diseases related to lipid and carbohydrate metabolism, such as type 2 diabetes, adipocyte differentiation, uncontrolled proliferation, such as lymphoma, Hodgkin's Disease, leukemia, breast cancer, prostate cancer or cancers in general; and inflammation, such as osteoarthritis, rheumatoid arthritis, Crohn's Disease or Inflammatory Bowel Disease.Type: GrantFiled: July 19, 2004Date of Patent: December 13, 2005Assignees: Incyte San Diego Inc., Ortho McNeil Pharmaceutical Inc.Inventors: Magnus Pfahl, Catherine Tachdjian, Hussien A. Al-Shamma, Andrea Fanjul, David P. M. Pleynet, Lyle W. Spruce
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Patent number: 6964975Abstract: The present invention relates to novel isoxazole and thiazole compounds having an excellent lysophosphatidic acid (LPA) receptor antagonistic activity represented by general formula [1] or salts thereof: wherein R1 and R2 represents an optionally substituted alkyl group or the like; R3 represents a hydrogen atom or the like; R4 represent a group selected from the group consisting of (I) optionally substituted phenyl, aryl, or heterocycle, (II) substituted or nonsubstituted alkyl, and (III) substituted or nonsubstituted alkenyl, alternatively, R3 and R4 may form a ring structure together with a carbon atom to which they bind; and X represents an oxygen atom or a sulfur atom, provided that, when R3 is a hydrogen atom, R4 represents a group other than methyl, and the use thereof as a medicine.Type: GrantFiled: February 19, 2001Date of Patent: November 15, 2005Assignee: Kirin Beer Kabushiki KaishaInventors: Akihiro Ueno, Rika Nagao, Tomoko Watanabe, Hideo Ohta, Mikio Yagi
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Patent number: 6916933Abstract: Compounds of Formula I have activity as inhibitors of binding between VCAM-1 and cells expressing VLA-4 and are useful for treating disease whose symptoms and or damage are related to the binding of VCAM-1 to cells expressing VLA-4.Type: GrantFiled: September 24, 2003Date of Patent: July 12, 2005Assignee: Hoffman-La Roche Inc.Inventors: Gerald Lewis Kaplan, Achyutharao Sidduri, Jefferson Wright Tilley
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Patent number: 6908923Abstract: Certain substituted benzamide derivatives of Formula I: selectively modulate the cardiac sarcomere, for example by potentiating cardiac myosin, and are useful in the treatment of systolic heart failure including congestive heart failure.Type: GrantFiled: December 20, 2002Date of Patent: June 21, 2005Assignee: Cytokinetics, Inc.Inventors: Fady Malik, Adam Lewis Tomasi, Bainian Feng, Erica Anne Kraynack, Kathleen A. Elias, Pu-Ping Lu, Whitney Walter Smith, Xiangping Qian, David J. Morgans, Jr.
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Patent number: 6875871Abstract: Disclosed are novel compounds that are useful and effective as photoaffinity probes and methods of using oxazolidinone photoaffinity probes.Type: GrantFiled: February 6, 2003Date of Patent: April 5, 2005Assignee: Pharmacia & Upjohn CompanyInventors: Lisa Marie Thomasco, Robert C. Gadwood
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Patent number: 6852745Abstract: Novel biphenyl sulfonamide compounds which are combined angiotensin and endothelin receptor antagonists are claimed along with methods of using such compounds in the treatment of conditions such as hypertension and other diseases, as well as pharmaceutical compositions containing such compounds.Type: GrantFiled: September 26, 2003Date of Patent: February 8, 2005Assignee: Bristol-Myers Squibb CompanyInventors: Natesan Murugesan, John E. Tellew, John E. Macor, Zhengxiang Gu
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Patent number: 6835741Abstract: Novel biphenyl sulfonamide compounds which are combined angiotensin and endothelin receptor antagonists are claimed along with methods of using such compounds in the treatment of conditions such as hypertension and other diseases, as well as pharmaceutical compositions containing such compounds.Type: GrantFiled: September 26, 2003Date of Patent: December 28, 2004Assignee: Bristol-Myers Squibb CompanyInventors: Natesan Murugesan, John E. Tellew, John E. Macor, Zhengxiang Gu
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Patent number: 6800642Abstract: Compounds of the formula: useful for treatment of disorders such as schizophrenia, schizoaffective disorder, bipolar disorder, Parkinson's disease, L-DOPA induced pychoses and dyskinesias, Tourette's syndrome and hyperprolactinemia and in the treatment of drug addiction such as the addiction to ethanol, nicotine or cocaine and related illnesses.Type: GrantFiled: April 24, 2002Date of Patent: October 5, 2004Assignee: WyethInventors: Megan Tran, Gary P. Stack
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Patent number: 6790846Abstract: Isoxazolone compounds having the generic structure: are used to treat disease associated with unwanted cytokine activity, including rheumatoid arthritis, osteoarthritis, diabetes, HIV/AIDS, inflammatory bowel disease, Crohn's disease, ulcerative colitis, congestive heart, hypertension, chronic obstructive pulmonary disease, septic shock syndrome, tuberculosis, adult respiratory distress, asthma, atherosclerosis, muscle degeneration, periodontal disease, cachexia, Reiter's syndrome, gout, acute synovitis, anorexia and bulimia nervosa fever, malaise, myalgia and headaches.Type: GrantFiled: May 7, 2002Date of Patent: September 14, 2004Assignee: The Procter & Gamble CompanyInventors: Michael Philip Clark, Jane Far-Jine Djung, Steven Karl Laughlin, Joshua Spector Tullis, Michael George Natchus, Biswanath De
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Publication number: 20040162427Abstract: The invention relates to the use of compounds of formula (I) as medicaments, to the novel compounds of formula (I) themselves, and to a method for the production thereof.Type: ApplicationFiled: April 12, 2004Publication date: August 19, 2004Inventors: Ulrich Rosentreter, Thomas Krmer, Andrea Vaupel, Walter Hbsch, Nicole Diedrichs, Thomas Krahn, Klaus Dembowsky, Johannes Stasch
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Publication number: 20040158067Abstract: 3-substituted-6-aryl pyridines of Formula I are provided: 1Type: ApplicationFiled: November 7, 2003Publication date: August 12, 2004Applicant: Neurogen CorporationInventors: Alan J. Hutchison, Jun Yuan, Kyungae Lee, George D. Maynard, Bertrand L. Chenard, Nian Liu, Qin Guo, Zihong Guo, Peter Hrnciar
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Publication number: 20040157842Abstract: The present invention relates to the potentiation of glutamate receptor function using certain sulphonamide derivatives. It also relates to novel sulphonamide derivatives, to processes for their preparation and to pharmaceutical compositions containing them.Type: ApplicationFiled: February 6, 2004Publication date: August 12, 2004Inventors: Macklin Brian Arnold, Paul Leslie Ornstein, Richard Lee Simon, Hamideh Zarrinmayeh, Dennis Michael Zimmerman
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Publication number: 20040147525Abstract: Compounds of the formula (I) below, or pharmacologically acceptable salts, esters or other derivatives thereof: 1Type: ApplicationFiled: July 22, 2003Publication date: July 29, 2004Applicant: SANKYO COMPANY, LIMITEDInventors: Tomio Kimura, Kazumasa Aoki, Akira Nakao
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Patent number: 6759419Abstract: The present invention relates to substituted pyrrolidinone compounds of formula 1, wherein n is 0 or 1; Aza is a heterocycle optionally substituted with C1-4 alkyl, or C1-4 alkyl substituted with a heterocycle, which represents a saturated or unsaturated five- or six-membered ring having nitrogen(s) as a heteroatom, which are muscarinic acetylcholine receptor agonists and useful as nootropics and therapeutic agents for cerebral neural diseases such as Alzheimer's disease; and pharmaceutically acceptable salts thereof; processes for the preparation thereof; and pharmaceutical compositions comprising these compounds or salts.Type: GrantFiled: October 18, 2002Date of Patent: July 6, 2004Assignee: Korea Institute of Science and TechnologyInventors: Youseung Kim, Soon Bang Kang, Gyochang Keum, Min Seok Jang, Jae Yang Kong, Dae Young Jeong, Taeg-Su Jang
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Publication number: 20040122037Abstract: The invention concerns substituted isoxazolines derivatives according to Formula (I): wherein X=CH?2#191, N—R7, S or O, R1, R2 and R3 are certain specific substituents, Pir is an optionally substituted piperidyl or piperazyl radical and R3 represents an optionally substituted aromatic homocyclic or heterocyclic ring system including a partially or completely hydrogenated hydrocarbon chain of maximum 6 atoms long with which the ring system is attached to the Pir radical and which may contain one or more heteroatoms selected from the group of O, N and S ; a process for their preparation, pharmaceutical compositions comprising them and their use as a medicine, in particular for the treatment of depression and/of anxiety and disorders of body weight.Type: ApplicationFiled: August 21, 2003Publication date: June 24, 2004Inventors: Jose Ignacio Andres-Gil, Francisco Javier Fernandez-Gadea, Manuel Jesus Alcazar-Vaca, Jose Maria Cid-Nunez, Joaquin Pastor-Fernandez, Antonius Adrianus Henrikus Petrus Megens, Godelieve Maria Heylen, Xavier Jean Michel Langlois, Margaretha Henrica Maria Bakker, Thomas Horst Wolfgang Steckler
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Publication number: 20040116440Abstract: Bombesin receptor antagonists are provided which are useful for the diagnosis, prevention, or treatment of male sexual dysfunction in humans and animals, female sexual dysfunction in humans and animals, anxiety and panic disorders, social phobia, depression, psychoses, sleeping disorders, memory impairment, pulmonary hypertension, lung repair and lung development disorders, cancer including prostate cancer and pancreatic cancer, hepatic porphyria, gastrointestinal secretory disturbances, gastrointestinal disorders including colitis, Crohn's disease and inflammatory bowel disease, emesis, anorexia, pain, seasonal affective disorders, feeding disorders, or pruritus.Type: ApplicationFiled: December 4, 2003Publication date: June 17, 2004Inventors: Michael Higginbottom, Martyn Clive Pritchard, Herman Thijs Stock
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Publication number: 20040116473Abstract: Novel isothiazole and isoxazole compounds, including derivatives thereof, to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use are described. The compounds of the present invention are potent inhibitors of transforming growth factor (“TGF”)-&bgr; signaling pathway. They are useful in the treatment of various TGF-related disease states including, for example, cancer, and fibrotic diseases.Type: ApplicationFiled: September 17, 2003Publication date: June 17, 2004Applicant: Pfizer IncInventors: Michael J. Munchhof, Laura C. Blumberg
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Publication number: 20040102498Abstract: Isoxazole estrogen receptor agonist and antagonist compounds having unexpected and surprising activity in modulating estrogen receptor activity are described. In addition, methods and compositions for treating or preventing estrogen receptor-mediated disorders are disclosed. The compounds, methods, and compositions of the invention have utility in preventing or treating estrogen receptor-mediated disorders such as osteoporosis, breast and endometrial cancers, atherosclerosis, and Alzheimer's disease.Type: ApplicationFiled: November 13, 2003Publication date: May 27, 2004Inventors: Verena D. Huebner, Xiaodong Lin, Ian James, Liya Chen, Manoj Desai, Jennifer C. Moore, Beata Krywult, Thayalan Navaratnam, Rajinder Singh, Rob Trainor, Liang Wang
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Publication number: 20040097499Abstract: The present invention provides certain amide, carbamate and urea derivatives useful for potentiating glutamate receptor function in a mammal and therefore, useful for treating a wide variety of conditions, such as psychiatric and neurological disorders.Type: ApplicationFiled: July 3, 2003Publication date: May 20, 2004Inventors: MacKlin Brian Arnold, David Michael Bender, Thomas John Bleisch, Winton Dennis Jones, Paul Leslie Ornstein, Hamid H. Zarrinmayeh, Dennis Michael Zimmerman
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Publication number: 20040097729Abstract: Compounds of the formula (I) in which the substituents are as defined in claim 1 are suitable for use as herbicides.Type: ApplicationFiled: December 6, 2002Publication date: May 20, 2004Inventors: Andrew Edmunds, Alain De Mesmaeker, Christoph Luthy, Jurgen Schaetzer
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Publication number: 20040072873Abstract: The present invention provides antibacterial agents of formula I described herein.Type: ApplicationFiled: August 1, 2003Publication date: April 15, 2004Inventors: Robert C. Gadwood, Jason M. Ochoada
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Patent number: 6706743Abstract: The instant invention provides &bgr;3 adrenergic receptor agonists of structural Formula (I), the stereoisomers and prodrugs thereof, and the pharmaceutically acceptable salts of the compounds, stereoisomers and prodrugs, wherein Ar, R, R1, R2, R3, R4, R5, R6, R7, R8, X, and Y, are as defined herein.Type: GrantFiled: March 5, 2003Date of Patent: March 16, 2004Assignee: Pfizer IncInventors: Robert F. Day, Jennifer A. Lafontaine
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Publication number: 20040030132Abstract: The present invention relates to biphenyl and biphenyl-analogous compounds, their preparation and use as pharmaceutical compositions, as integrin antagonists and in particular for the production of pharmaceutical compositions for the treatment and prophylaxis of cancer, arteriosclerosis, restenosis, osteolytic disorders such as osteoporosis and ophthalmic diseases.Type: ApplicationFiled: October 31, 2002Publication date: February 12, 2004Inventors: Markus Albers, Klaus Urbahns, Andrea Vaupel, Michael Harter, Delf Schmidt, Beatrix Stelte-Ludwig, Christoph Gerdes, Elke Stahl, Jorg Keldenich, Ulf Brueggemeier, Klemens Lustig
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Patent number: 6689888Abstract: The present invention provides processes useful in the preparation of certain &bgr;3-adrenergic receptor agonists of the structural formula the pharmaceutically acceptable salts thereof, and the hydrates of said pharmaceutically acceptable salts, wherein HET is as described herein. The invention further provides intermediates useful in the preparation of such agonists, and processes useful in the production of such intermediates.Type: GrantFiled: February 20, 2003Date of Patent: February 10, 2004Assignee: Pfizer Inc.Inventors: Robert J. Chambers, Robert W. Dugger, Ming Kang, Yong Tao, John W. Wong
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Patent number: 6686382Abstract: Thienyl-, furyl-, pyrrolyl- and phenylsulfonamides, formulations of pharmaceutically-acceptable derivatives thereof and methods for modulating or altering the activity of the endothelin family of peptides are provided. In particular, N-(isoxazolyl)thienylsulfonamides, N-(isoxazolyl)furylsulfonamides, N-(isoxazolyl)pyrrolylsulfonamides and N-(isoxazolyl)phenylsulfonamides, formulations thereof and methods using these sulfonamides for inhibiting the binding of an endothelin peptide to an endothelin receptor by contacting the receptor with the sulfonamide are provided. Methods for treating endothelin-mediated disorders by administering effective amounts of one or more of these sulfonamides or pharmaceutically acceptable derivatives thereof that inhibit the activity of endothelin are also provided.Type: GrantFiled: December 29, 2000Date of Patent: February 3, 2004Assignee: Encysive Pharmaceuticals Inc.Inventors: Chengde Wu, Natalie Blok, George W. Holland
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Publication number: 20040019059Abstract: The present invention is concerned with the compounds of formula 1Type: ApplicationFiled: March 31, 2003Publication date: January 29, 2004Inventors: Eddy Jean Edgard Freyne, Jose Ignacio Andres-Gil, Frederik Dirk Deroose, Davy Petrus Franciscus Maria Petit, Maria Encarnacion Matesanz-Ballesteros, Rosa Maria Alvarez Escobar
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Patent number: 6677341Abstract: The invention relates to substituted aryl and heteroaryl (R)-Chiral Halogenated 1-Substitutedamino-(n+1)-Alkanol 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. Novel high yield, stereoselective processes for the preparation of the chiral substituted alkanol compounds from chiral and achiral intermediates are described. Preferred (R)-Chiral 1-Substitutedamino-(n+1)-Alkanol compounds are substituted (R)-Chiral heteroaryl aminoalcohols.Type: GrantFiled: December 12, 2001Date of Patent: January 13, 2004Assignee: Pharmacia CorporationInventors: James A. Sikorski, Richard C. Durley, Margaret L. Grapperhaus, Mark A. Massa, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Brian S. Hickory, Monica B. Norton, William F. Vernier, Deborah A. Mischke, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
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Patent number: 6673818Abstract: Methods of treating cyclooxygenase-2 mediated disorders comprising administering to a subject a therapeutically effective amount of one or more fluoro-substituted benzenesulfonyl compounds corresponding to Formula I: wherein A, X, n, R1, R2, and R3 are as described in the specification, and novel fluoro-substituted benzenesulfonyl compounds within Formula I.Type: GrantFiled: April 16, 2002Date of Patent: January 6, 2004Assignee: Pharmacia CorporationInventors: David L. Brown, Matthew J. Graneto, Cindy L. Ludwig, John M. Molyneaux, John J. Talley
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Patent number: 6668527Abstract: There is disclosed a genus of non-peptidyl compounds, wherein said compounds are VLA-4 inhibitors useful in treating inflammatory, autoimmune, and respiratory diseases, and wherein said compounds comprise a compound of Formula (1.0.Type: GrantFiled: June 12, 2002Date of Patent: December 30, 2003Assignee: Pfizer Inc.Inventors: Allen J. Duplantier, Louis S. Chupak, Anthony J. Milici, Wan F. Lau
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Patent number: 6667331Abstract: There is disclosed a genus of non-peptidyl compounds, wherein said compounds are VLA-4 inhibitors useful in treating inflammatory, autoimmune, and respiratory diseases, and wherein said compounds comprise a compound of Formula (1.0.Type: GrantFiled: June 12, 2002Date of Patent: December 23, 2003Assignee: Pfizer IncInventors: Allen J. Duplantier, Louis S. Chupak, Anthony J. Milici, Wan F. Lau
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Publication number: 20030216386Abstract: The invention relates to isoxazole and oxadiazole compounds of Formulae I and II, 1Type: ApplicationFiled: April 10, 2003Publication date: November 20, 2003Inventors: Michele A. Weidner-Wells, Todd C. Henninger, Dennis J. Hlasta
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Patent number: 6649635Abstract: The present invention relates to novel heteroaryl-carboxamides which modulate the activity of protein tyrosine kinases and therefore are expected to be useful in the treatment of abnormal protein tyrosine kinase activity driven disorders including cancer.Type: GrantFiled: September 7, 2001Date of Patent: November 18, 2003Assignee: Sugen, Inc.Inventors: Gerald McMahon, Peng Cho Tang, Laura Kay Shawver, Klaus Peter Hirth
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Patent number: 6639078Abstract: The present invention includes nuclear receptor heterodimer and nuclear receptor-coactivator pepetide assays for identifying ligands for nuclear receptors, utilizing scintillation proximity and fluorescence resonance energy transfer (FRET), and methods of using identified ligands.Type: GrantFiled: June 18, 2001Date of Patent: October 28, 2003Assignee: SmithKline Beecham CorporationInventors: Curt Dare Haffner, Patrick Reed Maloney, Timothy Mark Wilson
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Publication number: 20030195241Abstract: Described herein are compounds that are useful as protein kinase inhibitors, especially inhibitors of ERK, having the formula: 1Type: ApplicationFiled: October 15, 2002Publication date: October 16, 2003Inventors: Michael Hale, James Janetka, Francois Maltais, Jingrong Cao, Robert Mashal
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Publication number: 20030186989Abstract: Compounds useful as inhibitors of PDE4 in the treatment of diseases regulated by the activation and degranulation of eosinophils, especially asthma, chronic bronchitis, and chronic obstructive pulmonary disease, of Formula (1.0.Type: ApplicationFiled: July 24, 2002Publication date: October 2, 2003Inventors: Anthony Marfat, Robert James Chambers
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Publication number: 20030187028Abstract: Isoxazoles are highly effective anti-viral agents. Combinations of isoxazoles, dihydropyrimidines and/or lamivudine and, optionally, interferon inhibit the proliferation of HBV viruses better than conventional agents.Type: ApplicationFiled: January 21, 2003Publication date: October 2, 2003Inventors: Michael Brands, Susanne Nikolic, Peter Eckenberg, Marcus Bauser, Johannes Kaulen, Arnold Paessens, Erwin Graef, Olaf Weber, Stefan Lottmann, Karl-Heinz Schlemmer
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Publication number: 20030176439Abstract: The present invention relates to compounds of the formula I, 1Type: ApplicationFiled: June 26, 2002Publication date: September 18, 2003Applicant: Aventis Pharma Dutschland GmbHInventors: Manfred Schudok, Otmar Klingler, Hans-Peter Nestler, Hans Matter, Herman Schreuder, Hauke Szillat
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Publication number: 20030162813Abstract: Provided are compounds, processes and synthetic intermediates useful for the preparation of compounds of the formula I and IX 1Type: ApplicationFiled: October 11, 2002Publication date: August 28, 2003Applicant: Onconova Therapeutics, Inc.Inventors: M. V. Ramana Reddy, Stanley C. Bell
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Patent number: 6610692Abstract: Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure: or a pharmaceutically acceptable salt thereof, wherein b is NY or O; c is CY2 or N; d is CY3 or N; e is CY4 or N; f is CY5 or N; g is CY6 or N; Y4, Y5, and Y6 are independently hydrogen, C1-4 alkyl, or halogen; Y1 and Y2 are independently hydrogen, C1-4 alkyl, C3-7 cycloalkyl, halogen, NH2, OH or C1-4 alkoxy, and Y3 is hydrogen, C1-4 alkyl, C3-7 cycloalkyl, halogen, —CN, NH2, OH or C1-4 alkoxy; A is and W, W1, R1, R3, R4, R5, X and Z are defined in the specification.Type: GrantFiled: October 28, 1999Date of Patent: August 26, 2003Assignee: Merck & Co., Inc.Inventors: Philip E. Sanderson, Bruce D. Dorsey, Terry A. Lyle, Matthew G. Stanton, Donnette Staas, Adel M. Naylor-Olsen, Craig Coburn, Matthew M. Morrissette
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Publication number: 20030149078Abstract: Methods of treating cyclooxygenase-2 mediated disorders comprising administering to a subject a therapeutically effective amount of one or more fluoro-substituted benzenesulfonyl compounds corresponding to Formula I: 1Type: ApplicationFiled: December 13, 2002Publication date: August 7, 2003Applicant: Pharmacia CorporationInventors: David L. Brown, Matthew J. Graneto, Cindy L. Ludwig, John M. Molyneaux, John J. Talley
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Publication number: 20030139408Abstract: The invention relates to a compound of formula (I): 1Type: ApplicationFiled: November 27, 2002Publication date: July 24, 2003Inventors: Otto Meth-Cohn, Chu-Yi Yu, Pierre Lestage, Marie-Cecile Lebrun, Daniel-Henri Caignard, Pierre Renard
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Patent number: 6593349Abstract: Compounds, compositions and methods are provided which are useful in the treatment of diseases through the modulation of potassium ion flux through voltage-dependent potassium channels. More particularly, the invention provides bisarylamines, compositions and methods that are useful in the treatment of central or peripheral nervous system disorders (e.g., migraine, ataxia, Parkinson's disease, bipolar disorders, trigeminal neuralgia, spasticity, mood disorders, brain tumors, psychotic disorders, myokymia, seizures, epilepsy, hearing and vision loss, Alzheimer's disease, age-related memory loss, learning deficiencies, anxiety and motor neuron diseases) and as neuroprotective agents (e.g., to prevent stroke and the like) by opening potassium channels associated with the onset or recurrence of the indicated conditions.Type: GrantFiled: March 11, 2002Date of Patent: July 15, 2003Assignee: ICAgen, Inc.Inventors: Grant Andrew McNaughton-Smith, George Salvatore Amato
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Patent number: 6583141Abstract: The present invention is concerned with the compounds of formula wherein m, n and p are each independently 0 or 1 and q is 0, 1, 2, 3, 4 or 5; —A1═A2—A3═A4— is a pyridinylidene, pyridazinylidene, pyrimidinylidene, pyrazinylidene or phenylidene; B represents an amide, ketone or oxadiazole; D represents Ar or Het; Q represents a covalent direct bond or a ketone, —N—, —O—, —CR5R6—, amide ethenyl, imine, sulfonyl, sulfinyl, 3-oxobutenyl, pyrazole, isoxazole or thiazole; L represents Ar or Het; R1 represents hydrogen, halo, hydroxy, C(2-6)alkenyl, C(2-6)alkynyl, C(3-6)cycloalkyl, C(3-6)cycloalkenyl, cyano, guanidine, nitro, NR17R18, an optionally substituted C(1-6)alkyl or C(1-6)alkyloxy; R2 and R3 each independently represent hydrogen, halo, C(1-6)alkyloxy or an optionally substituted C(1-6)alkyl; R5 and R6 each independently represent hydrogen, hydroxy, halo, an optionally substituted C(1-6)alkyl, C(2-6)alkenyl, C(2-6)alkynyl, C(3-Type: GrantFiled: April 6, 2001Date of Patent: June 24, 2003Assignee: Janssen Pharmaceutica, N.V.Inventors: Eddy Jean Edgard Freyne, José Ignacio Andrés-Gil, Frederik Dirk Deroose, Davy Petrus Franciscus Maria Petit, Maria Encarnacion Matesanz-Ballesteros, Rosa Maria Alvarez Escobar
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Publication number: 20030114491Abstract: The present invention relates to substituted pyrrolidinone compounds of formula 1, 1Type: ApplicationFiled: October 18, 2002Publication date: June 19, 2003Inventors: Youseung Kim, Soon Bang Kang, Gyochang Keum, Min Seok Jang, Jae Yang Kong, Dae Young Jeong