The Chalcogen, X, Is Part Of A -c(=x)x- Group, Wherein The X's Are The Same Or Diverse Chalcogens Patents (Class 546/335)
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Publication number: 20030149083Abstract: Specified phenylalanine derivatives and analogues thereof have an antagonistic activity to &agr; 4 integrin. They are used as therapeutic agents for various diseases concerning &agr; 4 integrin.Type: ApplicationFiled: May 20, 2002Publication date: August 7, 2003Applicant: AJINOMOTO CO. INCInventors: Yasuhiro Tanaka, Toshihiko Yoshimura, Hiroyuki Izawa, Chieko Ejima, Mitsuhiko Kojima, Yuko Satake, Eiji Nakanishi, Nobuyasu Suzuki, Shingo Makino, Manabu Suzuki, Masahiro Murata
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Publication number: 20030135053Abstract: The invention relates to novel bicyclic aromatic compounds which have the general formula (I): 1Type: ApplicationFiled: January 2, 2003Publication date: July 17, 2003Inventor: Jean-Michel Bernardon
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Publication number: 20030130523Abstract: A family of substituted chiral allosteric effectors of hemoglobin is useful for delivering more oxygen to hypoxic and ischemic tissues by reducing the oxygen affinity of hemoglobin in whole blood.Type: ApplicationFiled: September 10, 2002Publication date: July 10, 2003Inventors: Donald J. Abraham, Gajanan S. Joshi, Stephen J. Hoffman, Melissa Grella, Richmond Danso-Danquah, Amal Yousseff, Martin Safo, Sanjeev Kulkarni
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Patent number: 6586466Abstract: The present invention provides compounds which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, and methods for treating diseases of excessive bone loss or cartilage or matrix degradation, including osteoporosis; gingival disease including gingivitis and periodontitis; arthritis, more specifically, osteoarthritis and rheumatoid arthritis; Paget's disease; hypercalcemia of malignancy; and metabolic bone disease, comprising inhibiting said bone loss or excessive cartilage or matrix degradation by administering to a patient in need thereof a compound of the present invention.Type: GrantFiled: April 20, 2001Date of Patent: July 1, 2003Assignee: SmithKline Beecham CorporationInventor: Dennis Shinji Yamashita
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Patent number: 6586463Abstract: Compounds having the general structure: which are useful for the treatment of a variety of diseases and conditions, such as bone disorders.Type: GrantFiled: September 4, 2001Date of Patent: July 1, 2003Assignee: The Procter & Gamble CompanyInventors: Mitchell Anthony deLong, David Lindsey Soper, John August Wos, Biswanath De
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Publication number: 20030120073Abstract: Protein tyrosine phosphatases (PTPs) are implicated in a number of disease processes, including autoimmune diseases, glucose intolerance, diabetes, obesity and certain types of proliferative diseases such as cancer and psoriasis. The present invention discloses novel &agr;-ketocarboxylic acid inhibitors of PTPs, methods for synthesizing said inhibitors, and methods for using pharmaceutical compositions of the inhibitors to treat PTP-mediated disorders, diseases or dysfunctions. The compositions described herein can also be used as diagnostic and screening tools to elucidate complex signal transduction pathways involving PTPs or to identify PTP-mediated disease states.Type: ApplicationFiled: April 5, 2002Publication date: June 26, 2003Inventor: Christopher T. Seto
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Publication number: 20030092746Abstract: Compounds of Formula I are antagonists of VLA-4 and/or &agr;4&bgr;7, and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These compounds may be formulated into pharmaceutical compositions and are suitable for use in the treatment of AIDS-related dementia, allergic conjunctivitis, allergic rhinitis, Alzheimer's disease, asthma, atherosclerosis, autologous bone marrow transplantation, certain types of toxic and immune-based nephritis, contact dermal hypersensitivity, inflammatory bowel disease including ulcerative colitis and Crohn's disease, inflammatory lung diseases, inflammatory sequelae of viral infections, meningitis, multiple sclerosis, multiple myeloma, myocarditis, organ transplantation, psoriasis, pulmonary fibrosis, restenosis, retinitis, rheumatoid arthritis, septic arthritis, stroke, tumor metastasis, uveititis, and type I diabetes.Type: ApplicationFiled: May 21, 2001Publication date: May 15, 2003Inventors: William K. Hagmann, Stephen E. DeLaszlo, Theodore Kamenecka, Malcolm MacCoss
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Publication number: 20030065185Abstract: Disclosed are compounds which bind VLA-4. Certain of these compounds aslo inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA4. 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: April 8, 2002Publication date: April 3, 2003Inventors: Eugene D. Thorsett, Christopher M. Semko, Michael A. Pleiss, Louis John Lombardo, Francine S. Grant, Darren B. Dressen, Michael S. Dappen
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Publication number: 20030065187Abstract: The present invention relates to copper-catalyzed carbon-heteroatom and carbon-carbon bond-forming methods. In certain embodiments, the present invention relates to copper-catalyzed methods of forming a carbon-nitrogen bond between the nitrogen atom of an amide or amine moiety and the activated carbon of an aryl, heteroaryl, or vinyl halide or sulfonate. In additional embodiments, the present invention relates to copper-catalyzed methods of forming a carbon-nitrogen bond between a nitrogen atom of an acyl hydrazine and the activated carbon of an aryl, heteroaryl, or vinyl halide or sulfonate. In other embodiments, the present invention relates to copper-catalyzed methods of forming a carbon-nitrogen bond between the nitrogen atom of a nitrogen-containing heteroaromatic, e.g., indole, pyrazole, and indazole, and the activated carbon of an aryl, heteroaryl, or vinyl halide or sulfonate.Type: ApplicationFiled: April 24, 2002Publication date: April 3, 2003Inventors: Stephen L. Buchwald, Artis Klapars, Jon C. Antilla, Gabriel E. Job, Martina Wolter, Fuk Y. Kwong, Gero Nordmann, Edward J. Hennessy
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Publication number: 20030060624Abstract: The present invention relates to processes for the preparation of any of the intermediate 1,3-substituted indenes of the formulae (Ia), (Ib) and (Ic) or a mixture thereof: 1Type: ApplicationFiled: April 17, 2002Publication date: March 27, 2003Inventor: Robert A. Singer
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Publication number: 20030013657Abstract: Certain known and novel pyruvate derivatives are particularly active in restoring or preserving metabolic integrity in oxidatively competent cells that have been subjected to oxygen deprivation. These pyruvate-derived compounds include, but are not limited to oximes, amides, pyruvate analogues, modified pyruvate analogues, esters of pyruvate (e.g., polyol-pyruvate esters, pyruvate thioesters, glycerol-pyruvate esters and dihydroxyacetone-pyruvate esters). Such pyruvate derivatives (including single tautomers, single stereoisomers and mixtures of tautomers and/or stereoisomers, and the pharmaceutically acceptable salts thereof) are useful in the manufacture of pharmaceutical compositions for treating a number of conditions characterized by oxidative stress.Type: ApplicationFiled: May 3, 2002Publication date: January 16, 2003Inventors: Bing Wang, Guy Miller, Satyanarayana Janagani
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Publication number: 20020198400Abstract: A process for the synthesis of a compound of the formula 1Type: ApplicationFiled: July 15, 2002Publication date: December 26, 2002Inventors: Ahmed F. Abdel-Magid, Judith H. Cohen, Cynthia A. Maryanoff, Frank John Villani, Hua M. Zhong
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Patent number: 6498172Abstract: This invention relates to prostaglandin agonists, methods of using such prostaglandin agonists, pharmaceutical compositions containing such prostaglandin agonists and kits containing such prostaglandin agonists. The prostaglandin agonists are useful for the treatment of bone disorders including osteoporosis.Type: GrantFiled: August 20, 1999Date of Patent: December 24, 2002Assignee: Pfizer Inc.Inventors: Kimberly O. Cameron, Bruce A. Lefker, Robert L. Rosati
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Publication number: 20020187993Abstract: Energy-reversible acyl conjugates, intermediates, and related compositions are disclosed.Type: ApplicationFiled: January 31, 2002Publication date: December 12, 2002Inventors: Carl W. Gilbert, Eleanor B. McGowan, Kirby S. Black, T. Gregory P. Harper
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Publication number: 20020165230Abstract: This invention encompasses the novel compounds of Formula I, which are useful in the treatment of caspase-3 mediated diseases.Type: ApplicationFiled: September 7, 2001Publication date: November 7, 2002Inventors: Yongxin Han, Andre Giroux, Erich L. Grimm, Renee Aspiotis, Cameron Black
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Patent number: 6441177Abstract: Tertiary amines of the formula wherein A1, A2, A3, A4, M, p, T and Q are as defined herein, and acid addition salts thereof, have antimycotic and cholesterol-lowering activity.Type: GrantFiled: December 16, 1999Date of Patent: August 27, 2002Assignee: Hoffmann-La Roche Inc.Inventors: Johannes Aebi, Henrietta Dehmlow, Jacques Himber, Synèse Jolidon, Hans Lengsfeld, Olivier Morand, Gérard Schmid, Yu-Hua Ji
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Patent number: 6417368Abstract: The invention provides a resin-immobilized imine represented by the following formula: P—Q—N—═CH—R I [in the formula, P represents the principal chain of a resin polymer; Q represents a substituted or unsubstituted hydrocarbon side chain or a substituted or unsubstituted hydrocarbon side chain with a heteroatom interposed therein; R represents a substituted or unsubstituted hydrocarbon group or heterocyclic group] and a resin-immobilized &bgr;-aminocarbonyl compound of the following formula: which can be released as &bgr;-aminocarbonyl compound from the solid phase; and the invention also provide a resin-immobilized amine of the following formula: —P—Q1—O—Q2—NH2 III [Q1 and Q2 independently represent a hydrocarbon chain such as arylene, alkylenearylene or arylenealkylene], which is essential for solid state synthesis; and the invention has enabled the solid state synthesis of &bgr;-amType: GrantFiled: November 8, 2000Date of Patent: July 9, 2002Assignee: Japan Science and Technology CorporationInventors: Shu Kobayashi, Yoji Aoki
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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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Publication number: 20020068829Abstract: The present invention is directed to a process for preparing 3S-3-amino-3-aryl propionic acid and derivatives thereof.Type: ApplicationFiled: October 29, 2001Publication date: June 6, 2002Inventors: Lorraine Scott, Frank John Villani, Donald G. Walker
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Publication number: 20020062026Abstract: N-methyleneglycinates of formula (I) 1Type: ApplicationFiled: November 15, 2001Publication date: May 23, 2002Applicant: DEGUSSA AGInventors: Stefan Eils, Kai Rossen, Wilfried Jahn, Ingo Klement
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Patent number: 6392050Abstract: The invention relates to a process for preparing substituted pyridines in a simple and cost-effective manner in good yields by reacting substituted 1,4-dihydropyridines with methyl nitrite in the presence of an acid that contains less than 20% by weight of oxidizing components.Type: GrantFiled: June 4, 2001Date of Patent: May 21, 2002Assignee: Bayer AktiengesellschaftInventors: Norbert Lui, Hans Panskus, Albert Schnatterer
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Publication number: 20020058832Abstract: An efficient and selective process, capable of scale-up, to make itaconate derivatives of formula (IV), and/or succinate derivatives of formula (V) and/or (VI) by asymmetric hydrogenation of the itaconate derivatives.Type: ApplicationFiled: October 15, 2001Publication date: May 16, 2002Inventors: Andrew Michael Derrick, Nicholas Murray Thomson
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Publication number: 20020058804Abstract: The present invention provides a compound that includes an active therapeutic agent attached to a blocking moiety that is sensitive to the catalytic action of molecules having retro-aldol and retro-Michael catalytic activity, methods for making such compounds and methods of converting such compounds to active therapeutic agents using molecules having aldolase activity.Type: ApplicationFiled: June 18, 2001Publication date: May 16, 2002Applicant: The Scripps Research InstituteInventors: Carlos F. Barbas, Doron Shabat, Christoph Rader, Benjamin List, Richard A. Lerner
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Publication number: 20020049332Abstract: The invention includes selected novel optically active &agr;-amino ketones which either are themselves useful or are intermediates for the preparation of known ketomethylene pseudopeptides useful as antibiotics, antibiotic enhancers, or enzyme inhibitors. Further, the present invention provides a method for dehydrogenation/asymmetrical hydrogenation to obtain essentially pure antipodes of ketomethylene pseudopeptides having two chiral centers.Type: ApplicationFiled: October 11, 2001Publication date: April 25, 2002Inventor: John J. Talley
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Publication number: 20020035136Abstract: Compounds of formula (I) 1Type: ApplicationFiled: August 22, 2001Publication date: March 21, 2002Inventors: Gang Liu, Yihong Li, David A. Janowick, Zhonghua Pei
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Patent number: 6355634Abstract: 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: June 7, 1995Date of Patent: March 12, 2002Assignee: Bayer AktiengesellschaftInventors: Hans Peter Isenring, Bettina Weiss
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Patent number: 6355618Abstract: The present invention is directed to novel dipeptide thereof, represented by the general Formula I: where R1-R3, X and Y are defined herein. The present invention also relates to the discovery that compounds having Formula I are potent inhibitors of caspases and 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: April 7, 2000Date of Patent: March 12, 2002Assignee: Cytovia, Inc.Inventors: Sui Xiong Cai, Eckard Weber, Yan Wang, Gordon B. Mills, Douglas R. Green
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Patent number: 6337398Abstract: Succinoylamino hydroxyethylamino sulfonyl urea derivatives of the formula: wherein the substituents are as defined in the specification, are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: October 13, 1995Date of Patent: January 8, 2002Assignee: G.D. Searle & Co.Inventors: Michael L Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, Eric T. Sun
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Patent number: 6337417Abstract: The invention provides N-phenyltetrahydrophthalamic acid derivatives represented by the general formula [I], methods of producing the same, herbicides containing the same as the effective components, imidoylchloride derivatives as the intermediate products and methods of producing the same, wherein X and Y each individually represent hydrogen atoms or halogen atoms, R1 represents a lower alkoxycarbonylalkylthio group, R2 represents a lower alkyl group, a halogenated lower alkyl group or a substituted or unsubstituted phenyl group, and R3 represents a lower alkoxy group, a lower alkenyloxy group, a lower alkynyloxy group, or a lower alkoxyalkoxy group. The herbicides of the present invention, which are very useful, can be widely applied to upland, paddy field, orchard, turf, forest, non-crop land, etc., and are not harmful to crops.Type: GrantFiled: June 15, 1998Date of Patent: January 8, 2002Assignee: Central Glass Co., Ltd.Inventors: Tetsuo Takematsu, Takeo Komata, Takashi Kume, Yumiko Kohda, Kiyoshi Suzuki, Matsue Kawamura, Yukio Ikeda, Kaoru Mori
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Patent number: 6337306Abstract: Phenoxyacetic acid derivatives of the formula: wherein R1, R2, Xn and A are as defined herein, and a process for preparing the derivatives. The derivatives are used as herbicides.Type: GrantFiled: November 5, 1999Date of Patent: January 8, 2002Assignee: Rhone-Poulenc AgroInventors: Norio Sasaki, Atsushi Go, Hideshi Mukaida, Yukiko Oe
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Patent number: 6331554Abstract: Picornaviral 3C protease inhibitors of formula I, obtainable by chemical synthesis, that inhibit or block the biological activity of the picornaviral 3C protease are described. These compounds, as well as pharmaceutical compositions that contain these compounds, are suitable for treating patients or hosts infected with one or more picornaviruses.Type: GrantFiled: October 20, 1999Date of Patent: December 18, 2001Assignee: Agouron Pharmaceuticals, Inc.Inventors: Peter S. Dragovich, Thomas J. Prins, Ru Zhou
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Patent number: 6329523Abstract: Novel compounds having the formula: wherein the constituent variables are defined herein. The compounds are constructed to include a central aromatic, aliphatic, or heterocyclic ring system. Attached to the central ring system are two linear groups having nitrogenous moieties that are derivatized with chemical functional groups. The ring system can include further nitrogenous moieties, either as ring atoms or on pendant groups attached to the ring, that may also be derivatized with chemical functional groups. The totality of the chemical functional groups imparts certain conformational and other properties to the these compounds. In accordance with certain embodiments of the invention, libraries of such compounds are prepared utilizing permutations and combinations of the chemical functional groups and the nitrogenous moieties to build complexity into the libraries.Type: GrantFiled: March 10, 1999Date of Patent: December 11, 2001Assignee: ISIS Pharmaceuticals, Inc.Inventors: Phillip Dan Cook, Haoyun An
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Patent number: 6319925Abstract: Oxime ethers of formula (I) in which a) X is an N atom and Y is an oxygen atom or NH, or b) X is CH and Y is an oxygen atom, in which furthermore R1 is C1-C4alkyl; R2 is hydrogen, C1-C4alkyl or cyclopropyl; and in which R3 and R4 are as defined herein, are fungicidal, acaricidal and insecticidal active ingredients for agriculture. They can be employed as formulated crop protection compositions.Type: GrantFiled: December 22, 1997Date of Patent: November 20, 2001Assignee: Bayer AktiengesellschaftInventor: Hugo Ziegler
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Publication number: 20010041709Abstract: The present invention relates to compounds of formula (I) 1Type: ApplicationFiled: January 26, 2001Publication date: November 15, 2001Inventors: John Patrick Mogensen, Per Sauerberg, Paul Stanley Bury, Lone Jeppesen, Ingrid Pettersson
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Patent number: 6316459Abstract: O-Benzyloxime ethers of the formula I where X is substituted or unsubstituted CH2, NOalkyl Y is O, S, NR5 R1, R2, R5 are H, alkyl Z1, Z2 are H, halogen, methyl, methoxy, cyano R3, R4 are hydrogen, cyano, substituted or unsubstituted alkyl, alkenyl, cycloalkyl, cycloalkenyl, alkynyl, alkoxy, haloalkoxy, alkylthio, benzylthio, alkylcarbonyl, substituted or unsubstituted phenylcarbonyl, substituted or unsubstituted benzylcarbonyl, alkoxycarbonyl, substituted or unsubstituted phenoxycarbonyl, substituted or unsubstituted benzyloxycarbonyl, N(R6)2, where R6 is H, alkyl, substituted or unsubstituted phenyl, —CO—N(R7)2, where R7 is H, substituted or unsubstituted alkyl, substituted or unsubstituted aryl, substituted or unsubstituted aryloxy, substituted or unsubstituted arylthio, substituted or unsubstituted hetaryl, substituted or unsubstituted hetaryloxy, substituted or unsubstituted hetarylthio, substituted or unsubstituted heterocyclyl, substituted or unsubstituted heterocyType: GrantFiled: October 25, 1994Date of Patent: November 13, 2001Inventors: Siegbert Brand, Uwe Kardorff, Reinhard Kirstgen, Bernd Mueller, Klaus Oberdorf, Hubert Sauter, Gisela Lorenz, Eberhard Ammermann, Christoph Kuenast, Albrecht Harreus
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Patent number: 6313339Abstract: Certain cyclopropyl oxime ethers substituted by aryl and heterocyclic moieties possess broad spectrum fungicidal and insecticidal properties. These compounds are disclosed along with compositions containing these compounds and methods for controlling fungi and insects by the use of a fungitoxic or insecticidal amount of these compounds.Type: GrantFiled: February 17, 2000Date of Patent: November 6, 2001Inventors: Ronald Ross, Jr., Duyan Vuong Nguyen, Steve Howard Shaber
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Patent number: 6313122Abstract: This application relates to a compound of formula (I), a pharmaceutically acceptable salt of the compound, or a prodrug thereof, as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well as a process for its preparation and intermediates therefor.Type: GrantFiled: March 20, 2000Date of Patent: November 6, 2001Assignee: 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: 20010029300Abstract: A process for the synthesis of a compound of the formula 1Type: ApplicationFiled: May 15, 2001Publication date: October 11, 2001Inventors: Ahmed F. Abdel-Magid, Judith H. Cohen, Cynthia A. Maryanoff, Frank John Villani, Hua M. Zhong
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Patent number: 6288071Abstract: Pesticidally active cyclohexadienyl derivative compounds of the formula I that are esters, oximes or amides are claimed. These compounds may be used as fungicides, acaricides and insecticides in plant protection.Type: GrantFiled: December 10, 1998Date of Patent: September 11, 2001Assignee: Bayer AktiengesellschaftInventors: Henry Szczepanski, Martin Zeller, Ottmar Franz Hüter
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Patent number: 6258956Abstract: A process for the synthesis of a compound of the formula wherein R1 is aryl, heteroaryl, substituted aryl or substituted heteroaryl and R2 is hydrogen, alkyl or aralkyl, or salt thereof.Type: GrantFiled: March 21, 2000Date of Patent: July 10, 2001Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Ahmed F. Abdel-Magid, Judith H. Cohen, Cynthia A. Maryanoff, Frank John Villani, Jr., Hua M. Zhong
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Patent number: 6242637Abstract: The invention relates to compounds of the formula in which: A is a divalent radical selected from: A1) —O—CO— A2) —CH2—O—CO— A3) —O—CH2—CO— A4) —O—CH2—CH2— A5) —N(R1)—CO— A6) —N(R1)—CO—CO— A7) —N(R1)—CH2—CH2— A8) —O—CH2— in which: R1 is a hydrogen or a (C1-C4)-alkyl; and Am is a nitrogen-containing heterocycle.Type: GrantFiled: October 20, 1998Date of Patent: June 5, 2001Assignee: Sanofi-SynthelaboInventors: Xavier Emonds-Alt, Isabelle Grossriether, Patrick Gueule, Vincenzo Proietto, Didier Van Broeck
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Patent number: 6225288Abstract: Compounds represented by formula I: as well as pharmaceutically acceptable salts, esters and hydrates thereof are disclosed along with pharmaceutical compositions and methods of treatment. The compounds are useful as inhibitors of caspase-3, which is implicated in modulating apoptosis.Type: GrantFiled: March 16, 2000Date of Patent: May 1, 2001Assignee: Merk Frosst Canada & Co.Inventors: Yongxin Han, Andre Giroux, Erich Grimm, Renee Aspiotis, Sebastien Francoeur, Robert Zamboni, Petpiboon Prasit, Christopher Bayly, Dan McKay, Cameron Black
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Patent number: 6197770Abstract: Disclosed are compounds which are inhibitors of metalloproteases and which are effective in treating conditions characterized by excess activity of these enzymes. In particular, the compounds have a structure according to the following Formula (I): where X, W, Z, A, G, R1, R2, R3, R4, R5, R5′ and k have the meanings described in the specification. This invention also includes optical isomers, diastereomers and enantiomers of the formula above, and pharmaceutically-acceptable salts, biohydrolyzable amides, esters, and imides thereof Also described are pharmaceutical compositions comprising these compounds, and methods of treating or preventing metalloprotease-related maladies using the compounds or the pharmaceutical compositions.Type: GrantFiled: March 1, 2000Date of Patent: March 6, 2001Assignee: The Procter & Gamble Co.Inventors: Michael George Natchus, Roger Gunnard Bookland, Neil Gregory Almstead, Stanislaw Pikul, Biswanath De, Menyan Cheng
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Patent number: 6166051Abstract: Compounds of formula (I) wherein R, R.sub.1, R.sub.2, R.sub.3 have the meanings reported in the description, processes for their preparation and pharmaceutical compositions which contain them as active ingredients are described. The compounds of formula (I) are endowed with a mixed ACE-inhibitory and NEP-inhibitory activity and are useful in the treatment of cardiovascular diseases.Type: GrantFiled: June 23, 1998Date of Patent: December 26, 2000Assignee: Zambon Group S.p.A.Inventors: Franco Pellacini, Stefano Romagnano, Gabriele Norcini, Francesco Santangelo, Claudio Semeraro
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Patent number: 6166050Abstract: Compounds of the formula ##STR1## which inhibit leukocyte adhesion mediated by interaction of the .alpha..sub.4 .beta..sub.1 integrin (VLA-4) with its counterreceptor VCAM-1, and their use for the treatment of inflammatory and autoimmune diseases.Type: GrantFiled: December 10, 1999Date of Patent: December 26, 2000Assignee: American Home Products CorporationInventors: Louis J. Lombardo, Joan Sabalski
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Patent number: 6156774Abstract: Mercapto amino acid derivatives of formula (I), wherein R is hydrogen, a salt-forming cation of a in vivo hydrolysable ester-forming group; R.sub.1 is selected from (a) and (b) in which A is a monocyclic aryl or heteroaryl ring and B is a monocyclic aryl, alicyclic or heterocyclic ring, C and D are independently --Z.sub.p --(CR.sub.8 CR.sub.9).sub.q -- or --(CR.sub.8 CR.sub.9).sub.q --Z.sub.p -- where p is 0 or 1, q is 0 to 3 provided that p+q in C is not 0, R.sub.8 and R.sub.9 are independently hydrogen or (C.sub.1-6)alkyl or together represent oxo and Z is O, NR.sub.10 or S(O).sub.x where R.sub.10 is hydrogen, (C.sub.1-6)alkyl or aryl(C.sub.1-6)alkyl and x is 0-2, and wherein C and D are linked ortho to one another on each of the rings A and B in formula (b); R.sub.2 is hydrogen, (C.sub.1-6)alkyl or aryl(C.sub.1-6)alkyl; R.sub.3 is hydrogen, (C.sub.1-6)alkyl optionally substituted by up to three halogen atoms, (C.sub.3-7)cycloalkyl, fused aryl(C.sub.3-7)cycloalkyl, (C.sub.3-7)cycloalkyl(C.sub.2-6)alkyl, (C.Type: GrantFiled: April 7, 1999Date of Patent: December 5, 2000Assignee: SmithKline Beecham P.L.C.Inventors: John Hargreaves Bateson, Desmond John Best, Brian Peter Clarke, Martin Leonard Gilpin, David Witty
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Patent number: 6140353Abstract: N-(4-carbamimidophenylamino) phenylglycineamide derivative compounds having the formula: ##STR1## in which E, g.sup.1, g.sup.2, Q, R and X.sup.1 to X.sup.4 are each as defined in the description, and hydrates or solvates and physiologically acceptable salts thereof can be used as inhibitors of the formation of the coagulation factors Xa, IXa and thrombin induced by the factor VIIa and by the tissue factor. These compounds can be used as medicaments for the treatment and/or prevention of thromboses, apoplexy, cardiac infarction, inflammation and arteriosclerosis or as antitumor agents.Type: GrantFiled: December 2, 1998Date of Patent: October 31, 2000Assignee: Hoffmann-La Roche Inc.Inventors: Jean Ackermann, Katrin Grobke, Yu-Hua Ji, Sabine Wallbaum, Lutz Weber
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Patent number: 6124361Abstract: The present invention relates to compounds of the formula I, as defined in the specification, pharmaceutical compositions containing such compounds the use of such compounds to treat neurological and psychiatric disorders.Type: GrantFiled: December 29, 1998Date of Patent: September 26, 2000Assignee: Pfizer IncInventor: Bertrand L. Chenard
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Patent number: 6121268Abstract: Compounds with fungicidal properties having formula I ##STR1## where m and n are 0 or 1 provided that m+n is 1; X is hydrogen, halo, (C.sub.1 -C.sub.4)alkyl, or (C.sub.1 -C.sub.4)alkoxy; R is an optionally-substituted alkyl, cycloalkyl, alkenyl, alkynyl, alkoxy, aryl, aralkyl, or heterocyclic group; R.sub.1 and R.sub.2 are hydrogen, optionally-substituted alkyl, cycloalkyl, cyano, carboxy alkyl, or aryl; at least one of R.sub.1 and R.sub.2 is hydrogen; and R.sub.3 is alkyl or haloalkyl.Type: GrantFiled: November 23, 1998Date of Patent: September 19, 2000Assignee: Rohm and Haas CompanyInventors: Ronald Ross, Ted Tsutomo Fujimoto, Edward Michael Szapacs, Steven Howard Shaber
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Patent number: 6080839Abstract: The invention relates to a novel labeling reactant, suitable for labeling of a biospecific binding reactant using solid-phase synthesis. The invention further concerns new labeling methods. The novel labeling reactant has the formula (I) ##STR1## wherein -A- is a bivalent aromatic structure capable of absorbing light or energy and transferring the excitation energy to a lanthanide ion after the product made by the said solid-phase synthesis has been released from the used solid support, deprotected and converted to a lanthanide chelate;-G- is a bridge replacing a hydrogen atom in A;R is a protected amino acid residue --CH(NHX)COOH, where X is a transient protecting group, or its active ester, where said ester is e.g. an N-hydroxysuccinimido, p-nitrophenol or pentafluorophenol ester; andR' is --COOR'" where R'" is an alkyl of 1 to 4 carbon atoms, phenyl or benzyl, which phenyl or benzyl can be substituted or unsubstituted.Type: GrantFiled: June 25, 1998Date of Patent: June 27, 2000Assignee: Wallac OyInventors: Harri Takalo, Jari Hovinen, Veli-Matti Mukkala, Paivi Liitti, Heikki Mikola