Plural Double Bonds Between Ring Members Of The Oxazole Ring Patents (Class 548/247)
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Patent number: 6624167Abstract: Pharmaceutical compositions incorporate compounds that are capable of affecting nicotinic cholinergic receptors. A wide variety of conditions and disorders, and particularly conditions and disorders associated with dysfunction of the central and autonomic nervous systems can be treated using pharmaceutical compositions incorporating compounds in which an aromatic ring is bridged with an ethylenic or acetylenic unit to an azabicyclic moiety.Type: GrantFiled: August 4, 2000Date of Patent: September 23, 2003Assignee: Targacept, Inc.Inventors: Thomas Jeffrey Clark, Balwinder Singh Bhatti
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Publication number: 20030176708Abstract: This invention is in the field of antiinflammatory pharmaceutical agents and specifically relates to compounds, compositions and methods for treating disorders mediated by cyclooxygenase-2 or 5-lipoxygenase, such as inflammation.Type: ApplicationFiled: December 12, 2002Publication date: September 18, 2003Applicant: Pharmacia CorporationInventors: John J. Talley, James A. Sikorski, Matthew J. Graneto, Jeffery S. Carter, Bryan H. Norman, Balekudru Devadas, Hwang-Fun Lu
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Patent number: 6616989Abstract: Isoxazole derivatives of the formula (I) where the symbols and indices have the following meanings, for example: T is X is S or O R1 and R2 are identical or different and are each hydrogen, F, CN or a straight-chain or branched C1-C20-alkyl or C2-C20-alkenyl radical (with or without asymmetric carbon atoms), A1 and A2 are undirected and identical or different and are each phenylene-1,4-diyl, M1 is undirected and is —OC(═O)—, —OCH2—, —SC(═O)—, —SCH2—, —CH2CH2—, —OC(═O)CH2CH2—, —OCH2CH2CH2—, —C≡C—, —(CH2)4— or a single bond; a is 0 or 1, are used in liquid-crystal mixtures.Type: GrantFiled: November 7, 2000Date of Patent: September 9, 2003Assignee: Clariant International Ltd.Inventors: Wolfgang Schmidt, Barbara Hornung, Rainer Wingen
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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: 6610858Abstract: The present invention relates to processes for the conversion of nitriles to amidines in the preparation of compounds which are antagonists of the platelet glycoprotein IIb/IIIa fibrinogen receptor complex. The compounds described herein are potent thrombolytics and useful for the inhibition of platelet aggregation in the treatment of thromboembolic disorders.Type: GrantFiled: April 25, 2002Date of Patent: August 26, 2003Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Philip Ma, Pasquale N. Confalone, Hui-Yin Li
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Patent number: 6608209Abstract: A process is described for preparing isoxazoles of the formula I wherein R1 is hydrogen, C1-C6-alkyl, R2 is C1-C6-alkyl, R3, R4, R5 are hydrogen, C1-C6-alkyl, or R4 and R5 together form a bond, R6 is a heterocyclic ring, n is 0, 1 or 2; in which an intermediate of the formula VI is prepared, followed by halogenation, thiomethylation, oxidation and acylation to give compounds of formula I. Novel intermediates for preparing the intermediates are described.Type: GrantFiled: June 27, 2002Date of Patent: August 19, 2003Assignee: BASF AktiengesellschaftInventors: Joachim Rheinheimer, Wolfgang von Deyn, Joachim Gebhardt, Michael Rack, Rene Lochtman, Norbert Götz, Michael Keil, Matthias Witschel, Helmut Hagen, Ulf Misslitz, Ernst Baumann
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Patent number: 6593363Abstract: The present invention relates to diterpene derivatives prepared from the components which are extracted from Acanthopanax Koreanum and represented by Chemical Formula (1).Type: GrantFiled: September 15, 2000Date of Patent: July 15, 2003Assignees: Sae Han Pharm. Co., Ltd.Inventors: Young Ger Suh, Young Hoon Choi, Hye Kyung Lee, Young Ho Kim, Hyoung Sup Park
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Fungicidal agents containing pyrrolidones as their active agents and use thereof for treating plants
Patent number: 6586369Abstract: Agrochemical compositions having fungicidal action and comprising as active compounds compounds of the formula I where R1 is hydrogen, C1-C6-alkyl, C1-C6-alkylcarbonyl, formyl or C1-C6-haloalkylcarbonyl; R2 is halogen, C1-C6-alkylthio, C1-C6-alkoxy, C3-C6-cycloalkyl-C1-C6-alkoxy, C1-C6-alkoxy-C1-C6-alkyl, halo-C1-C6-alkoxy, C1-C6-alkylsulfonyl, C1-C6-alkylsulfinyl, halo-C1-C6-alkylsulfonyl, cyano or a radical NR13R14; R3-R12 are hydrogen, halogen, C1-C8-cycloalkyl, C1-C6-alkyl, halo-C1-C6-alkyl, C1-C6-alkoxy, halo-C1-C6-alkoxy, C1-C6-alkylsulfonyl, halo-C1-C6-alkylsulfonyl, formyl, C1-C6-alkylcarbonyl, cyano, C1-C6-alkylthio or phenyl, which may be unsubstituted or substituted by halogen, C1-C6-alkyl or halo-C1-C6-alkyl, R13 is hydrogen, C1-C6-alkyl, R14 is C1-C6-alkyl, C1-C8-cycloalkyl or, together with R13 and the nitrogen atom to which they are attached, a saturated or unsaturated heterocyclic five- or six-membered ring which contains one or two heteroatoms selected from the group coType: GrantFiled: August 20, 2002Date of Patent: July 1, 2003Assignee: BASF AktiengesellschaftInventors: Joachim Rheinheimer, Karl Eicken, Ingo Rose, Thomas Grote, Eberhard Ammermann, John-Bryan Speakman, Siegfried Strathmann, Gisela Lorenz -
Patent number: 6586452Abstract: The present invention relates to novel nodulosporic acid derivatives, which are acaricidal, antiparasitic, insecticidal and anthelmintic agents.Type: GrantFiled: July 9, 2001Date of Patent: July 1, 2003Assignee: Merck & Co., Inc.Inventors: Thomas Shih, Steven L. Colletti, Michael H. Fisher, Peter T. Meinke, Howard C. H. Kuo, Prasun K. Chakravarty, Matthew J. Wyvratt, Sriram Tyagarajan, Richard Berger
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Publication number: 20030114501Abstract: Arylisoxazoline derivatives, processes for their preparation and their use as pesticidesType: ApplicationFiled: March 22, 2002Publication date: June 19, 2003Inventors: Ralf Braun, Oswald Ort, Karl-Josef Haack, Matthias Eckhardt, Waltraud Hempel, Maria-Theresia Thonessen
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Patent number: 6579880Abstract: The invention relates to isoxazole and oxadiazole compounds of Formulae I and II, pharmaceutical compositions containing the compounds, and methods for their production and use. These compounds are effective in inhibiting the action of IL-8 and are thus useful as anti-inflammatory agents for a variety of diseases.Type: GrantFiled: June 6, 2001Date of Patent: June 17, 2003Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Michele A. Weidner-Wells, Todd C. Henninger, Dennis J. Hlasta
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Publication number: 20030105334Abstract: The present disclosure provides a method for the preparation of aromatic sulfonyl halides by contacting a substituted phenyl compound with a halosulfonic acid and trifluoroacetic acid. The present disclosure further provides a method for the preparation of 4-[5-methyl-3-phenylisoxazol-4-yl]benzenesulfonamide which is useful in treating cyclooxygenase-2 related disorders.Type: ApplicationFiled: October 2, 2002Publication date: June 5, 2003Inventors: Leo J. Letendre, Sastry A. Kunda, Donald J. Gallagher, Lisa M. Seaney, Kathleen McLaughlin
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Publication number: 20030105331Abstract: Derivatives of C2-substituted indan-1-ol compounds, processes for their preparation and their use are disclosed.Type: ApplicationFiled: August 30, 2002Publication date: June 5, 2003Inventors: Gerhard Jaehne, Volker Krone, Martin Bickel, Matthias Gossel
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Publication number: 20030096842Abstract: This invention relates to compounds of formula (I) that inhibit farnesylation of gene products through inhibition of the enzyme farnesyl-protein transferase (FPTase). The invention also relates to methods of manufacturing the compounds, pharmaceutical compositions and methods of treating diseases, especially cancer, which are mediated through farnesylation.Type: ApplicationFiled: June 20, 2002Publication date: May 22, 2003Inventors: James Michael Wardleworth, Francis Thomas Boyle, Zbigniew Matusiak
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Patent number: 6559100Abstract: Substituted 2-benzoylcyclohexane-1,3-diones of the formula I where: R1 and R2 are each hydrogen, mercapto, nitro, halogen, cyano, thiocyanato, C1-C6-alkyl, C1-C6-haloalkyl, C1-C6-alkoxy, C2-C6-alkenyl, C2-C6-alkynyl, —OR3, —OCOR3, —OSO2R3, —S(O)nR3, —SO2OR3, —SO2N(R3)2, —NR3SO2R3 or —NR3COR3; R3 is hydrogen, C1-C6-alkyl, C1-C6-haloalkyl, C2-C6-alkenyl, C2-C6-alkynyl, phenyl or phenyl-C1-C6-alkyl; where the abovementioned alkyl radicals may be partially or fully halogenated and/or may carry one to three of the following groups: hydroxyl, mercapto, amino, cyano, R3, —OR3, —SR3, —N(R3)2, ═NOR3, —OCOR3, —SCOR3, —NR3COR3, —CO2R3, —COSR3, —CON(R3)2, C1-C4-alkyliminooxy, C1-C4-alkoxyamino, C1-C4-alkylcarbonyl, C1-C4-alkoxy-C2-C6-alkoxycarbonyl, C1-C4-alkylsulfonyl, heterocyclyl, heterocyclyloxy, phenyl, benzyl, hetaryl, phenoxy, benzyloxy and hetaryloxy, where the eight last mentioned radicType: GrantFiled: February 7, 2000Date of Patent: May 6, 2003Assignee: BASF AktiengesellschaftInventors: Stefan Engel, Joachim Rheinheimer, Ernst Baumann, Wolfgang von Deyn, Regina Luise Hill, Guido Mayer, Ulf Misslitz, Oliver Wagner, Matthias Witschel, Martina Otten, Helmut Walter, Karl-Otto Westphalen
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Patent number: 6555559Abstract: The present invention provides novel PGI2 derivatives and an anti Helicobacter agent, a platelet function potentiating agent or a cervical ripening agent containing any of the derivatives.Type: GrantFiled: August 1, 2000Date of Patent: April 29, 2003Assignee: Toray Industries, Inc.Inventors: Hisanori Wakita, Naohiro Yamada, Hitoshi Hatakeyama, Takeshi Ishigaki, Noriyuki Hirano, Takeshi Mori
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Publication number: 20030073722Abstract: This invention is in the field of antiinflammatory pharmaceutical agents and specifically relates to compounds, compositions and methods for treating disorders mediated by cyclooxygenase-2 or 5-lipoxygenase, such as inflammation.Type: ApplicationFiled: July 8, 2002Publication date: April 17, 2003Applicant: Pharmacia CorporationInventors: John J. Talley, James A. Sikorski, Matthew J. Graneto, Bryan H. Norman, Balekudru Devadas, Hwang-Fun Lu
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Publication number: 20030065012Abstract: 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: April 25, 2002Publication date: April 3, 2003Applicant: Chiron CorporationInventors: 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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Patent number: 6531610Abstract: A retroviral protease inhibiting compound of the formula: is disclosed.Type: GrantFiled: July 20, 2000Date of Patent: March 11, 2003Assignee: Abbott LaboratoriesInventors: Dale J. Kempf, Daniel W. Norbeck
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Patent number: 6531498Abstract: The invention relates to compounds of formula I and to their physiologically acceptable salts and solvates which act as phosphodiesterse VII inhibitors and are thus useful for the treatment of allergic disorders, asthma, chronic bronchitis, atopic dermatitis, psoriasis and other skin disorders, inflammatory disorders, autoimmune diseases, rheumatoid arthritis, multiple sclerosis, Crohn's disease, diabetes mellitus or ulcerative colitis, osteoporosis, transplant rejection reactions, cachexia, tumor growth, tumor metastases, sepsis, memory disturbances, atherosclerosis and AIDS.Type: GrantFiled: May 3, 2002Date of Patent: March 11, 2003Assignee: Merck PatentgesellschaftInventors: Hans-Michael Eggenweiler, Rochus Jonas, Michael Wolf, Michael Gassen, Thomas Welge
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Patent number: 6525099Abstract: The present invention provides certain N-substituted sulfonamide 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: GrantFiled: January 23, 2001Date of Patent: February 25, 2003Assignee: Eli Lilly and CompanyInventors: Macklin Brian Arnold, Winton Dennis Jones, Paul Leslie Ornstein, Hamideh Zarrinmayeh, Dennis Michael Zimmerman
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Patent number: 6518266Abstract: The present invention is directed to novel pyrazole derivatives and their use as pesticidal agents. The pyrazole derivatives have Formula I: or a salt thereof, where R1 represents R5O, R5SO2, R5SO or R5S in which R5 is as defined herein; X is halo, cyano, C1-6 alkoxycarbonyl, C2-6 alkynyl, optionally substituted C6-14 aryl or an optionally substituted 5- to 7-membered heteroaromatic ring linked to thiazole via a carbon-carbon bond; R2 is hydrogen, amino, chloro, bromo, iodo, cyano, C1-6 alkoxy, C1-6 alkyl or C6-10 aryl; and R3-R7 each represent hydrogen, halogen, straight- or branched-chain C1-4 alkyl or C1-4 alkoxy, either of which is unsubstituted or substituted by one or more halogen atoms, straight- or branched-chain C1-4 alkylthio or C1-4 alkylsulphinyl, either of which is substituted by one or more halogen atoms, nitro, cyano, or straight- or branched-chain C1-4 alkylsulphonyl group which is unsubstituted or substituted by one or more halogen atoms.Type: GrantFiled: July 21, 2000Date of Patent: February 11, 2003Assignees: 3-Dimensional Pharmaceuticals, Heska CorporationInventors: Daljit S. Dhanoa, Dario Doller, Sanath Meegalla, Richard M. Soll, Nancy Wisnewski, Gary Silver, Dan T. Stinchcomb, R. Lee Seward, Dimitris Agrafiotis, Deyou Sha
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Publication number: 20030022865Abstract: The present invention relates to novel sulfoxide and bis-sulfoxide compounds, compositions comprising sulfoxide and bis-sulfoxide compounds, and methods useful for treating and preventing cardiovascular diseases, dyslipidemias, dysproteinemias, and glucose metabolism disorders comprising administering a composition comprising an ether compound. The compounds, compositions, and methods of the invention are also useful for treating and preventing Alzheimer's Disease, Syndrome X, peroxisome proliferator activated receptor-related disorders, septicemia, thrombotic disorders, obesity, pancreatitis, hypertension, renal disease, cancer, inflammation, and impotence. In certain embodiments, the compounds, compositions, and methods of the invention are useful in combination therapy with other therapeutics, such as hypocholesterolemic and hypoglycemic agents.Type: ApplicationFiled: October 11, 2001Publication date: January 30, 2003Inventors: Jean-Louis Henri Dasseux, Carmen Daniela Oniciu
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Patent number: 6512121Abstract: This invention is in the field of antiinflammatory pharmaceutical agents and specifically relates to compounds, compositions and methods for treating disorders mediated by cyclooxygenase-2 or 5-lipoxygenase, such as inflammation.Type: GrantFiled: June 11, 2001Date of Patent: January 28, 2003Assignee: G.D. Searle & Co.Inventors: John J Talley, James A Sikorski, Matthew J Graneto, Jeffrey S Carter, Bryan H Norman, Balekudru Devadas, Hwang-Fun Lu
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Publication number: 20030018013Abstract: The present invention relates to novel ether compounds, compositions comprising ether compounds, and methods useful for treating and preventing cardiovascular diseases, dyslipidemias, dysproteinemias, and glucose metabolism disorders comprising administering a composition comprising an ether compound. The compounds, compositions, and methods of the invention are also useful for treating and preventing Alzheimer's Disease, Syndrome X, peroxisome proliferator activated receptor-related disorders, septicemia, thrombotic disorders, obesity, pancreatitis, hypertension, renal disease, cancer, inflammation, and impotence. In certain embodiments, the compounds, compositions, and methods of the invention are useful in combination therapy with other therapeutics, such as hypocholesterolemic and hypoglycemic agents.Type: ApplicationFiled: October 11, 2001Publication date: January 23, 2003Inventors: Jean-Louis Henri Dasseux, Carmen Daniela Oniciu
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Patent number: 6503912Abstract: The present application relates to novel guanidine derivatives of the formula (I) in which R1 represents a five- or six-membered heterocyclic group; R2 represents hydrogen or alkyl, R3 represents the groupings —OR4, —OCOR5, —OCOOR6, —OCONR7R8 and —OSO2R9, where R4, R5 and R6 independently of one another represent alkyl, alkoxyalkyl, halogenoalkyl, alkenyl, alkinyl, alkylaminoalkyl, dialkylaminoalkyl, optionally substituted cycloalkyl and in each case optionally substituted phenyl or benzyl, R7 and R8 independently of one another represent hydrogen, alkyl, alkenyl and in each case optionally substituted phenyl or benzyl and R9 represents alkyl or optionally substituted phenyl, A represents the groupings —CH2CH2—, (CH2)3 and —CH═CH— and z represents cyano or nitro, with the proviso that, if Z represents NO2 and A represents —CH2CH2—, the radical R2 represents hydrogen; and the compound of the formula (I) in whichType: GrantFiled: June 28, 2000Date of Patent: January 7, 2003Assignee: Bayer AktiengesellschaftInventors: Klaus Wagner, Christoph Erdelen, Wolfram Andersch, Ulrike Wachendorff-Neumann, Andreas Turberg, Norbert Mencke
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Publication number: 20030004200Abstract: A stable crystalline form of 4-[5-methyl-3-phenylisoxazol-4-yl]benzenesulfonamide is described. This crystal structure, designated Form B, is more stable, has favorable handling properties and is characterized by its melting point, x-ray and other physical characterizations.Type: ApplicationFiled: July 26, 2002Publication date: January 2, 2003Applicant: G.D. Searle & Co.Inventors: John J. Talley, John R. Medich, Kathleen T. McLaughlin, Henry T. Gaud, Edward E. Yonan
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Patent number: 6495582Abstract: Described herein are compounds that are useful as protein kinase inhibitors, especially inhibitors of ERK, having the formula: where A, B, R1, R2, T and Ht are described in the specification. The compounds are useful for treating diseases in mammals that are alleviated by a protein kinase inhibitor, particularly diseases such as cancer, inflammatory disorders, restenosis, and cardiovascular disease.Type: GrantFiled: September 14, 2001Date of Patent: December 17, 2002Assignee: Vertex Pharmaceuticals IncorporatedInventors: Michael Hale, James Janetka, Francois Maltais, Jingrong Cao, Robert Mashal
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Patent number: 6495580Abstract: Compounds, compositions and methods are provided for the prophylaxis and treatment of infections caused by viruses of the Pneumovirinae subfamily of Paramyxoviridae and diseases associated with such infections.Type: GrantFiled: October 18, 1999Date of Patent: December 17, 2002Assignee: ViroPharma IncorporatedInventors: Theodore J. Nitz, Daniel C. Pevear
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Patent number: 6492396Abstract: The present invention is directed to chemical compositions of substituted thioacetamides, processes for the preparation thereof and uses of the compositions in the treatment of diseases.Type: GrantFiled: May 15, 2001Date of Patent: December 10, 2002Assignee: Cephalon, Inc.Inventors: Edward R. Bacon, Sankar Chatterjee, Derek Dunn, John P. Mallamo, Jeffry L. Vaught, Matthew S. Miller
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Patent number: 6492402Abstract: The present invention relates to a compound having formula I: and pharmaceutically acceptable salts thereof. The compounds of formula I and pharmaceutical compositions containing them are of the class of thrombin inhibitors which are useful as anticoagulants.Type: GrantFiled: December 29, 1999Date of Patent: December 10, 2002Assignee: LG Life Sciences, Ltd.Inventors: Koo Lee, Won Hyuk Jung, Cheol Won Park, Sang Koo Lee, Sun Hwa Lee, Hee Dong Park
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Publication number: 20020177618Abstract: Described herein are compounds that are useful as protein kinase inhibitors, especially inhibitors of ERK, having the formula: 1Type: ApplicationFiled: September 14, 2001Publication date: November 28, 2002Inventors: Michael Hale, James Janetka, Francois Maltais, Jingrong Cao, Robert Mashal
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Patent number: 6479529Abstract: Chemically stable pharmaceutical formulations comprising a therapeutically effective amount of a material of formula I are provided which formulations contain a stabilizer system comprising an organic carboxylic acid containing more than 1 carboxylic acid group and an antioxidant. The preferred organic carboxylic acid is citric acid and the preferred antioxidants are ascorbic acid and butylated hydroxytoluene, which antioxidants are preferred to be used in admixture. The chemically stable pharmaceutical formulations are particularly useful for treating Irritable Bowel Syndrome (IBS) in mammals and comprises administering to the mammal needing treatment an effective dose of the above chemically stable pharmaceutical formulation. The stabilizer system is also effective for use in other pharmaceutical formulations containing active ingredients having oxidizable groups such as amino, phenolic, hydryoxyl amino, aldehyde, unsaturated compounds, sulfoxide, sulfone and mercapto.Type: GrantFiled: April 12, 1999Date of Patent: November 12, 2002Assignee: Shire US Inc.Inventor: Philip C. Lang
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Publication number: 20020156290Abstract: A novel process for preparing the compounds of the formula I 1Type: ApplicationFiled: May 9, 2002Publication date: October 24, 2002Inventors: Michael Rack, Norbert Gotz, Helmut Hagen, Wolfgang von Deyn, Ernst Baumann, Rene Lochtman, Joachim Gebhardt
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Patent number: 6451824Abstract: Compounds of formula (I) are suitable for the production of pharmaceuticals for the prophylaxis and therapy of disorders in the course of which an increased activity of matrix-degrading metalloproteinases is involved.Type: GrantFiled: May 8, 1998Date of Patent: September 17, 2002Assignee: Aventis Pharma Deutschland GmbHInventors: Werner Thorwart, Wilfried Schwab, Manfred Schudok, Burkhard Haase
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Patent number: 6448201Abstract: Benzoylcyclohexanediones and benzoylpyrazoles, their preparation and their use as herbicides and plant growth regulators. There are described benzoyl compounds of the formula (I), their preparation and their use as herbicides and plant growth regulators. In this formula (I), R1, R2, R3 and R4 are various radicals, X is an alkylene chain which may contain a hetero atom and Het is a heterocycle or heteroaromatic ring.Type: GrantFiled: November 2, 2000Date of Patent: September 10, 2002Assignee: Aventis CropScience GmbHInventors: Thomas Seitz, Lothar Willms, Thomas Auler, Hermann Bieringer, Felix Thürwächter
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Patent number: 6448281Abstract: A compound of the formula I: wherein: X is CH or N; Y is O or S; Z is OH, NH2, NMeR3, NHR3; OR3 or 5- or 6-membered heterocycle, having 1 to 4 heteroatoms selected from O, N and S, said heterocycle being optionally substituted with from 1 to 4 substituents; A is N, COR7 or CR5, wherein R5 is H, halogen, or (C1-6) alkyl and R7 is H or (C1-6 alkyl), with the proviso that X and A are not both N; R6 is H, halogen, (C1-6 alkyl) or OR7, wherein R7 is H or (C1-6 alkyl); R1 is selected from the group consisting of 5- or 6-membered heterocycle having 1 to 4 heteroatoms selected from O, N, and S, phenyl, phenyl(C1-3)alkyl, (C2-6)alkenyl, phenyl(C2-6)alkenyl, (C3-6)cycloalkyl, (C1-6)alkyl, CF3, 9- or 10-membered heterobicycle having 1 to 4 heteroatoms selected from O, N and S, wherein said heterocycle, phenyl, phenyl(C2-6)alkenyl and phenyl(C1-3)alkyl), alkenyl, cycloalkyl, (C1-6)alkyl, and heterobicycle are all optionally substituted with from 1 to 4 substituents; R2 is selected from (C1-6)alkyl, (CType: GrantFiled: July 3, 2001Date of Patent: September 10, 2002Assignee: Boehringer Ingelheim (Canada) Ltd.Inventors: Pierre Louis Beaulieu, Gulrez Fazal, James Gillard, George Kukolj, Volkhard Austel
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Patent number: 6441014Abstract: A stable crystalline form of 4-[5-methyl-3-phenylisoxazol-4-yl]benzenesulfonamide is described. This crystal structure, designated Form B, is more stable, has favorable handling properties and is characterized by its melting point, x-ray and other physical characterizations.Type: GrantFiled: December 19, 2000Date of Patent: August 27, 2002Assignee: G.D. Searle & Co.Inventors: John J Talley, John R Medich, Kathleen T McLaughlin, Henry T Gaud, Edward E Yonan
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Patent number: 6440899Abstract: Cyclohexenonedioxothiochromanoyl derivatives of the formula I where X is oxygen, sulfur, S═O, S(═O)2, CR4R5, C═O or C═NR6, the other substituents are as defined in the specification, and and agriculturally useful salts thereof; processes for preparing the cyclohexenonedioxotheiochromanoyl derivatives; compositions comprising them, and the use of these derivatives or of compositions comprising them for controling undesirable piants.Type: GrantFiled: October 30, 2000Date of Patent: August 27, 2002Assignee: BASF AktiengesellschaftInventors: Matthias Witschel, Klaus Langemann, Wolfgang von Deyn, Ulf Misslitz, Ernst Baumann, Stefan Engel, Guido Mayer, Ulf Neidlein, Oliver Wagner, Roland Götz, Martina Otten, Karl-Otto Westphalen, Helmut Walter
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Publication number: 20020114770Abstract: The present invention relates to certain resorcinol derivatives and their use as skin lightening agents.Type: ApplicationFiled: September 7, 2001Publication date: August 22, 2002Inventors: Stuart E. Bradley, Eric W. Collington, Mathhew C. Fyfe, Martin J. Procter, Colin P. Sambrook Smith
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Patent number: 6432994Abstract: Thienyl-, furyl- and pyrrolyl-sulfonamides, pharmaceutically-acceptable salts of sulfonamides, formulations of salts and the sulfonamides, and methods for modulating or altering the activity of the endothelin family of peptides using the formulations and sulfonamides are provided. In particular, formulations of sodium salts of N-(isoxazolyl)thienylsulfonamides, N-(isoxazolyl)furylsulfonamides and N-(isoxazolyl)pyrrolylsulfonamides are provided. A process of preparing an alkali metal salt of a hydrophobic sulfonamide is provided. The process includes the step of dissolving a free sulfonamide in an organic solvent in the presence of a saturated alkali metal salt solution and recovering the formed sulfonamide salt from the organic phase.Type: GrantFiled: March 27, 2000Date of Patent: August 13, 2002Assignee: Texas Biotechnology CorporationInventors: Chengde Wu, Natalie Blok, Timothy Kogan, Karin Keller, Patricia Woodard
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Patent number: 6420567Abstract: Thienyl-, furyl- and pyrrolyl-sulfonamides, formulations of pharmaceutically-acceptable salts 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 and N-(isoxazolyl)pyrrolylsulfonamides, 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 prodrugs thereof that inhibit the activity of endothelin are also provided.Type: GrantFiled: September 26, 1997Date of Patent: July 16, 2002Assignee: Texas Biotechnology CorporationInventors: Chengde Wu, Bore Gowda Raju, Timothy Kogan, Natalie Blok
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Patent number: 6417219Abstract: The invention provides compounds which are useful as inhibitors of metalloproteases, and which are effective in treating conditions characterized by excess activity of these enzymes. In particular, the present invention relates to a compound having a structure according to Formula (I). Also disclosed are compounds, pharmaceutical compositions and methods of treating diseases characterized by metalloprotease activity using these compounds or the pharmaceutical compositions containing them.Type: GrantFiled: August 26, 1997Date of Patent: July 9, 2002Assignee: The Proctor & Gamble CompanyInventors: Michael George Natchus, Biswanath De, Stanislaw Pikul, Neil Gregory Almstead, Roger Gunnard Bookland, Yetunde Olabisi Taiwo, Menyan Cheng
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Patent number: 6414004Abstract: 3-Substituted-5-Aryl-4-Isoxazolecarboritriles having anti-viral activity.Type: GrantFiled: December 21, 2000Date of Patent: July 2, 2002Assignee: Universita' Degli Studi di CataniaInventors: Ernesto Geremia, Gianna Tempera, Angelo Castro, Adriana Garozzo, Francesco Guerrera, Rossella Maria Campagna
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Publication number: 20020077316Abstract: The present invention relates to novel sulfide and disulfide compounds, compositions comprising sulfide and disulfide compounds, and methods useful for treating and preventing cardiovascular diseases, dyslipidemias, dysproteinemias, and glucose metabolism disorders comprising administering a composition comprising an ether compound. The compounds, compositions, and methods of the invention are also useful for treating and preventing Alzheimer's Disease, Syndrome X, peroxisome proliferator activated receptor-related disorders, septicemia, thrombotic disorders, obesity, pancreatitis, hypertension, renal disease, cancer, inflammation, and impotence. In certain embodiments, the compounds, compositions, and methods of the invention are useful in combination therapy with other therapeutics, such as hypocholesterolemic and hypoglycemic agents.Type: ApplicationFiled: October 11, 2001Publication date: June 20, 2002Inventors: Jean-Louis Henri Dasseux, Carmen Daniela Oniciu
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Patent number: 6407103Abstract: The present invention relates to the synthesis of a new class of indeno[1,2-c]pyrazol-4-ones of formula (I): that are potent inhibitors of the class of enzymes known as cyclin dependent kinases, which relate to the catalytic subunits cdk1-9 and their regulatory subunits know as cyclins A-H. This invention also provides a novel method of treating cancer or other proliferative diseases by administering a therapeutically effective amount of one of these compounds or a pharmaceutically acceptable salt form thereof. Alternatively, one can treat cancer or other proliferative diseases by administering a therapeutically effective combination of one of the compounds of the present invention and one or more other known anti-cancer or anti-proliferative agents.Type: GrantFiled: December 6, 2000Date of Patent: June 18, 2002Assignee: Bristol-Myers Squibb Pharma CompanyInventors: David A. Nugiel, David J. Carini, Susan V. Di Meo, Eddy W. Yue
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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: 6407268Abstract: 4-Benzoylpyrazoles of the formula I where: R1 and R2 are each hydrogen, mercapto, nitro, halogen, cyano, thiocyanato, C1-C6-alkyl, C1-C6-haloalkyl, C1-C6-alkoxy, C2-C6-alkenyl, C2-C6-alkynyl, —OR10, —OCOR10, —OSO2R10, —S(O)nR10, —SO2OR10, —SO2NR3R10, —NR10SO2R10 or —NR10COR; Q is a pyrazole of the formula II, which is attached in position 4 and, Substituted 4-benzoylpyralozoles.Type: GrantFiled: June 6, 2000Date of Patent: June 18, 2002Assignee: BASF AktiengesellschaftInventors: Stefan Engel, Ernst Baumann, Wolfgang von Deyn, Regina Luise Hill, Uwe Kardorff, Guido Mayer, Martina Otten, Joachim Rheinheimer, Oliver Wagner, Matthias Witschel, Ulf Misslitz, Helmut Walter
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Patent number: 6403791Abstract: A compound of the formula wherein R1 is C1-3 alkyl optionally substituted with one or more fluorines; R2 is C1-6 alkyl, cycloalkyl or NR4R5; R3 is a pyrazole, imidazole or isoxazole group of partial formula (A), (B) or (C) NR4R5 is a nitrogen-containing heterocyclic ring; R6 is C1-3 alkyl; and R7 and R8, which are the same or different, each represents C1-3 alkyl, halogen, CF3 or CN; or a pharmaceutically-acceptable salt thereof.Type: GrantFiled: February 9, 2001Date of Patent: June 11, 2002Assignee: Darwin Discovery, Ltd.Inventors: Hazel Joan Dyke, Alan Findlay Haughan, Christopher Lowe, George Martin Buckley, Richard John Davenport, Andrew Sharpe, Hannah Jayne Kendall, Verity Margaret Sabin, John Gary Montana, Catherine Louise Picken
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Patent number: 6399784Abstract: The present invention relates to processes for the conversion of nitrites to amidines in the preparation of compounds which are antagonists of the platelet glycoprotein IIb/IIIa fibrinogen receptor complex. The compounds described herein are potent thrombolytics and useful for the inhibition of platelet aggregation in the treatment of thromboembolic disorders.Type: GrantFiled: January 10, 2001Date of Patent: June 4, 2002Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Philip Ma, Pasquale N. Confalone, Hui-Yin Li