Nitrogen Or Chalcogen Attached Indirectly To The Hetero Ring By Nonionic Bonding Patents (Class 549/72)
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Patent number: 7094911Abstract: 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. The compounds according to the invention have the formula (1) wherein R1, R2, U, V, A, B, W, R3, C and R4 have the meaning as defined in the claims.Type: GrantFiled: October 31, 2002Date of Patent: August 22, 2006Assignee: Bayer AktiengesellschaftInventors: Markus Albers, Klaus Urbahns, Andrea Vaupel, Michael Härter, Delf Schmidt, Beatrix Stelte-Ludwig, Christoph Gerdes, Elke Stahl, Jörg Keldenich, Ulf Brueggemeier, Klemens Lustig
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Patent number: 7041702Abstract: The present invention relates to pharmaceutically acceptable compounds, including acylguanidine compounds, and methods of treatment and pharmaceutical compositions that utilize or comprise one or more such compounds. Compounds of the invention are particularly useful for the treatment or prophylaxis of neurological injury and neurodegenerative disorders.Type: GrantFiled: October 20, 1998Date of Patent: May 9, 2006Assignee: Scion Pharmaceuticals, Inc.Inventors: Graham J. Durant, Seetharamaiyer Padmanabhan
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Patent number: 7034053Abstract: The present invention disclosed compounds of Formula I. The present invention also discloses beta-3 agonists of formula I and methods for treating beta-3 mediated diseases and condition using the compounds of formula I, in particular methods for treating diabetes or obesity.Type: GrantFiled: December 17, 2001Date of Patent: April 25, 2006Assignee: SmithKline Beecham CorporationInventors: David N. Deaton, Barry George Shearer, David Edward Uehling
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Patent number: 7019024Abstract: The invention provides a pharmaceutical for treatment of neurological and neuropsychiatric disorders comprising a compound of the formula: or a pharmaceutically acceptable salt thereof.Type: GrantFiled: January 9, 2001Date of Patent: March 28, 2006Assignee: Allelix Neuroscience Inc.Inventors: Vassil Iliya Ognyanov, Laurence A. Borden, Stanley Charles Bell, Jing Zhang
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Patent number: 6982279Abstract: Compounds of the formulae IA and Ib. in which X, R(1), R(2), R(3), R(4), R(5), R(6), R(7), R(30) and R(31) have the meanings indicated in the claims, are very particularly suitable as novel antiarrhythmic active compounds, in particular for the treatment and prophylaxis of atrial arrhythmias, e.g. atrial fibrillation (AF) or atrial flutters.Type: GrantFiled: December 12, 2001Date of Patent: January 3, 2006Assignee: Aventis Pharm Deutschland GmbHInventors: Stefan Peukert, Joachim Brendel, Horst Hemmerle, Heinz-Werner Kleemann
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Patent number: 6960594Abstract: A novel compound which inhibits certain integrins, particularly ?v integrins. Additionally, the novel compound may be used in a method of treating tumors or cancer which comprises administering a pharmaceutically effective amount of the compound to a patient. Additionally, the novel compound may be used in a method of inhibiting angiogensis. Finally, a method of producing the novel compound is disclosed.Type: GrantFiled: January 16, 2002Date of Patent: November 1, 2005Assignee: Shire BioChem Inc.Inventors: Denis Labrecque, Serge Lamothe, Marc Courchesne, Laval Chan, Giorgio Attardo, Karen Meerovitch
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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: 6887903Abstract: The compounds of formula 1 wherein R and R2 are as defined in the disclosure, are useful in the prevention and treatment of tissue damage due to exacerbated recruitment of polymorphonuclear neutrophils (PMN leukocytes) at the inflammatory sites.Type: GrantFiled: October 14, 1999Date of Patent: May 3, 2005Assignee: Dompe S.p.A.Inventors: Riccardo Bertini, Cinzia Bizzarri, Vilma Sabbatini, Gianfranco Caselli, Marcello Allegretti, Maria Candida Cesta, Carmelo Gandolfi, Marco Mantovanini, Francesco Colotta, Stefano Porzio
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Patent number: 6878743Abstract: The present invention provides compounds having formula (I): and pharmaceutically acceptable derivatives thereof, wherein A, B, D, E, G, J, n, and R1 are as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof as caspase inhibitors and for the treatment of disorders caused by excessive apoptotic activity.Type: GrantFiled: September 17, 2002Date of Patent: April 12, 2005Assignee: Sunesis Pharmaceuticals, Inc.Inventors: Ingrid Choong, Matthew Burdett, Warren DeLano, Daniel Erlanson, Dennis Lee, Willard Lew
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Patent number: 6875790Abstract: The present invention relates to cyclic sulfone moiety-containing hydroxyethylamine protease inhibitor compounds and pharmaceutical or method of use therefor, particularly as an inhibitor of HIV protease.Type: GrantFiled: February 20, 2003Date of Patent: April 5, 2005Assignees: G. D. Searle & Co., Pharmacia Corporation (Monsanto Corporation)Inventors: Deborah E. Bertenshaw, Daniel Getman, Robert M. Heintz, John J. Talley, Kathryn L. Reed, Robert Alan Chrusciel, Michael Clare
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Patent number: 6852882Abstract: Novel PDF inhibitors and novel methods for their use are provided.Type: GrantFiled: June 4, 2002Date of Patent: February 8, 2005Assignee: SmithKline Beecham CorporationInventors: Siegfried B. Christensen, IV, Maxwell D. Cummings, Joseph M. Karpinski
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Patent number: 6835745Abstract: This invention provides estrogen receptor modulators of formula I, having the structure wherein, R1, R2, R3, X, and Y are as defined in the specification, or a pharmaceutically acceptable salt thereof.Type: GrantFiled: January 10, 2003Date of Patent: December 28, 2004Assignee: WyethInventors: Richard D. Coghlan, William F. Fobare, Heather A. Harris, James C. Keith, Jr., Leo M. Albert
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Patent number: 6812237Abstract: Compounds of the formula (I), wherein R1 is aryl or biaryl; R2 is aryl-lower alkyl, biaryl-lower alkyl, benzo-fused cycloalkyl, cycloalkyl-lower alkyl, bicycloalkyl-lower alkyl, aryloxy-lower alkyl, or aryl-C2-C7-alkyl in which C2-C7-alkyl is interrupted by Y; Y is O, S, SO, SO2, CO or NR6; R3 is hydrogen or lower alkyl; or R2 and R3 combined are C2-C7-alkylene or C2-C7-alkylene interrupted by Y; R4 is hydrogen or lower alkyl; R5 is hydrogen, optionally substituted lower alkyl, aryl-lower alkyl, biaryl-lower alkyl, cycloalkyl-lower alkyl, bicycloalkyl-lower alkyl, aryloxy-lower alkyl, or aryl-C2-C7-alkyl in which C2-C7-alkyl is interrupted by Y; R6 is hydrogen, lower alkyl or aryl-lower alkyl; and pharmaceutically acceptable salts thereof, which are useful as cysteine cathepsin inhibitorsType: GrantFiled: November 7, 2002Date of Patent: November 2, 2004Assignee: Novartis AGInventors: Scott Douglas Cowen, Paul David Greenspan, Leslie Wighton McQuire, Ruben Alberto Tommasi, John Henry Van Duzer
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Patent number: 6811833Abstract: A 4-membered compound is represented by the following formula (I) is disclosed (in the formula, X1 and X2 each independently represent an oxygen atom, a sulfur atom or a substituted or unsubstituted imino group, Y1 and Y2 each independently represent a single bond, an oxygen atom or a substituted or unsubstituted imino group, B1 and B2 each independently represent an optionally substituted aliphatic, aliphatic carbonyl, aromatic or aromatic carbonyl group having 1-20 carbon atoms, and A1 and A2 each independently represent a group represented by the following formula (II) (Ar1, Ar2 and Ar3 each independently represent a cyclic group having 5-14 carbon atoms, L1 and L2 each independently represent a single bond or a divalent linking group, and p represents an integer of 0-2)). There is also disclosed a birefringence medium containing a 4-membered compound represented by the formula (I) and an optical element comprising the birefringence medium.Type: GrantFiled: September 17, 2002Date of Patent: November 2, 2004Assignee: Fuji Photo Film Co., Ltd.Inventors: Naoyuki Nishikawa, Kentaro Toyooka
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Patent number: 6803384Abstract: A compound of formula Id and pharmaceutically acceptable salts and esters thereof, wherein the substituent designations are as provided in the specification. Compounds of the invention are useful for treating reperfusion injury.Type: GrantFiled: January 22, 2003Date of Patent: October 12, 2004Assignee: Hoffmann-La Roche Inc.Inventors: Nader Fotouhi, Paul Gillespie, Robert William Guthrie, Sherrie Lynn Pietranico-Cole, Weiya Yun
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Patent number: 6784173Abstract: Compounds of formula I wherein A, R1 and R2 are defined in the specification. These compounds are useful as HDAC inhibitors. Also disclosed are methods of making and using said compounds.Type: GrantFiled: June 11, 2002Date of Patent: August 31, 2004Assignee: Hoffmann-La Roche Inc.Inventors: Ulrike Leser-Reiff, Tim Sattelkau, Gerd Zimmermann
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Publication number: 20040138270Abstract: The present invention describes compounds of the general formula I 1Type: ApplicationFiled: December 10, 2003Publication date: July 15, 2004Inventors: Georg Fertig, Frank Herting, Matthias Koerner, Manfred Kubbies, Anja Limberg, Ulrike Reiff, Michael Weidner
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Patent number: 6716881Abstract: The present invention provides carbanilides of formula (I), wherein A, Q, R, X, Z and m are as defined herein. A plurality of processes for preparing these compounds is provided, along with methods of using the compounds to control microorganisms in crops and in the protection of materials. The compounds of the present invention also find use in controlling animal pests.Type: GrantFiled: May 30, 2002Date of Patent: April 6, 2004Assignee: Bayer AktiengesellschaftInventors: Hans-Ludwig Elbe, Bernd-Wieland Krüger, Robert Markert, Ralf Tiemann, Dietmar Kuhnt, Stefan Dutzmann, Klaus Stenzel, Christoph Erdelen, Martin Kugler, Hans-Ulrich Buschhaus
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Publication number: 20040063673Abstract: This invention provides compounds defined by Formula IType: ApplicationFiled: August 5, 2003Publication date: April 1, 2004Inventor: Adam Richard Johnson
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Patent number: 6677369Abstract: This application relates to a compound of formula I (or a prodrug thereof or a pharmaceutically acceptable salt of the compound or prodrug thereof) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well as a process for its preparation and intermediates therefor.Type: GrantFiled: April 25, 2002Date of Patent: January 13, 2004Assignee: 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, 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: 20030220389Abstract: The invention relates to O-substituted 6-methyl-tramadol derivatives, to methods for producing them, to medicaments containing these compounds, to the use of O-substituted 6-methyl-tramadol derivatives for producing medicaments for treating pain and other symptoms or diseases, and to methods of treatment using the medicaments.Type: ApplicationFiled: March 31, 2003Publication date: November 27, 2003Applicant: GRUENENTHAL GMBHInventors: Helmut Buschmann, Babette-Yvonne Koegel, Elmar Friderichs, Dagmar Kaulartz
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Publication number: 20030220390Abstract: The invention relates to 5-amino-1-pentene-3-ol substituted derivatives, a method for the production thereof, medicaments containing said compounds, the use of substituted 5-amino-1-pentene-3-ol derivatives for the production of medicaments, and methods of treatment using the medicaments.Type: ApplicationFiled: March 31, 2003Publication date: November 27, 2003Applicant: GRUENENTHAL GMBHInventors: Helmut Buschmann, Corinna Maul, Bernd Sundermann, Utz-Peter Jagusch, Michael Haurand, Boris Chizh
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Patent number: 6627652Abstract: Process of treatment of mammals, including humans to treat diseases or conditions of the type which are normally treated with retinoid-like compounds is disclosed, with pharmaceutical compositions containing an active compound which is a selective agonist of the RXR retinoid receptor sites in preference to the RAR retinoid receptor sites. A compound is defined to be a selective agonist of the RXR receptor site if the compound is at least approximately ten times more effective as an agonist in the RXR receptor sites than in the RAR receptor sites.Type: GrantFiled: April 20, 1995Date of Patent: September 30, 2003Assignee: Allergan, Inc.Inventor: Roshantha A. S. Chandraratna
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Patent number: 6610729Abstract: The present invention relates to a hydroxamic acid derivative of the formula (I) wherein each symbol is as defined in the specification, a pharmacologically acceptable salt thereof, a pharmaceutical composition containing the derivative or a salt thereof, and to pharmaceutical use thereof. The hydroxamic acid derivative and a pharmacologically acceptable salt thereof of the present invention have an inhibitory activity of TNF &agr; production, and are useful for, for example, the prophylaxis and treatment of the diseases such as autoimmune diseases and inflammatory diseases (e.g., sepsis, MOF, rheumatoid arthritis, Crohn's disease, cachexia, myasthenia gravis, systemic lupus erythematosus, asthma, I type diabetes, psoriasis and the like), and the like.Type: GrantFiled: November 22, 2000Date of Patent: August 26, 2003Assignee: Mitsubishi Pharma CorporationInventors: Tomokazu Gotou, Shinji Takeda, Kazuhiro Maeda, Tomohiro Yoshida, Naoki Sugiyama, Tadahiro Takemoto
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Publication number: 20030153609Abstract: The present invention is directed C2-disubstituted indan-1-ones of the Formula I, 1Type: ApplicationFiled: August 29, 2002Publication date: August 14, 2003Applicant: Aventis Pharma Dutschlan GmbH.Inventors: Gerhard Jaehne, Volker Krone, Martin Bickel, Matthias Gossel
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Patent number: 6605730Abstract: The invention relates to compounds of the formula R1, R2, and n have the meanings set forth in the disclosure, that are useful as intermediates for nematicidal pyrazoles.Type: GrantFiled: August 15, 2001Date of Patent: August 12, 2003Assignee: Nihon Bayer Agrochem K.K.Inventors: Katsuaki Wada, Takuya Gomibuchi, Yuichi Otsu, Katsuhiko Shibuya, Takahisa Abe, Wolfram Andersch, Achim Harder, Peter Lösel
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Patent number: 6600052Abstract: A novel process for preparing 3,4-di(carbocyclyl or heterocyclyl)thiophenes comprising reacting a compound of Formula IV: with a ring cyclizing reagent to form the compound of Formula V to yield a compound of Formula V: wherein R1, R2 and R3 are as defined in the specification.Type: GrantFiled: April 20, 2001Date of Patent: July 29, 2003Assignee: Pharmacia CorporationInventors: David L. Brown, Cindy L. Ludwig
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Publication number: 20030120085Abstract: Benzamidoxime derivatives of the formula I 1Type: ApplicationFiled: October 1, 2002Publication date: June 26, 2003Inventors: Karl Eicken, Joachim Rheinheimer, Frank Wetterich, Eberhard Ammermann, Gisela Lorenz, Siegfried Strathmann
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Patent number: 6566366Abstract: Compounds of the formula and salts thereof wherein the substituents are defined as in accordance with the specification useful for the treatment of tumor growth, osteoporosis, inflammation and cardiovascular disorders.Type: GrantFiled: March 6, 2001Date of Patent: May 20, 2003Assignees: Aventis Pharma Deutschland GmbH, Genentech, Inc.Inventors: Karl-Heinz Scheunemann, Jochen Knolle, Amuschirwan Peyman, David William Will, Denis Carniato, Jean-Francois Gourvest, Thomas Gadek, Robert McDowell, Sarah Catherine Bodary, Robert Andrew Cuthbertson
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Patent number: 6566508Abstract: Disclosed are novel coumarin based fluorogenic compounds useful in assaying for biological activity. Specifically, these fluorogenic compounds exhibit fluorescence at particular wavelengths when cleaved by target enzymes. Preferred compounds include sugar and peptide derivatives of umbelliferone derivatives bearing a heterocyclic five membered ring at the 3-position. These compounds can be used for rapidly detecting food pathogens and for determining sterilization effectiveness. The compounds may also be used in a form bounded to a polymeric support or to a biomolecule or macromolecule.Type: GrantFiled: March 11, 2002Date of Patent: May 20, 2003Assignee: 3M Innovative Properties CompanyInventors: James Gregory Bentsen, Christopher Allen Mickelson, Orlin Bruce Knudson, Kevin Michael Lewandowski
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Patent number: 6552203Abstract: The present invention relates to cyclic sulfone moiety-containing hydroxyethylamine protease inhibitor compounds and pharmaceutical or method of use therefor, particularly as an inhibitor of HIV protease.Type: GrantFiled: October 11, 2001Date of Patent: April 22, 2003Assignee: Monsanto CompanyInventors: Deborah E. Bertenshaw, Daniel Getman, Robert M. Heintz, John J. Talley, Kathryn L. Reed, Robert Alan Chrusciel, Michael Clare
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Patent number: 6534680Abstract: Dicarboxylic acid crystals are prepared from a solution containing at least one organic dicarboxylic acid in a process in which at least one anionic polyelectrolyte having a molecular weight of at least 2000 is added to the solution before or during the crystallization.Type: GrantFiled: October 27, 1999Date of Patent: March 18, 2003Assignee: BASF AktiengesellschaftInventors: Matthias Rauls, Dieter Baumann, Hermann Wistuba, Bernhard Otto
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Patent number: 6534532Abstract: The invention concerns novel carbanilides of formula (I), in which A, Q, R, X, Z and m have the meanings given in the description. The invention further concerns a plurality of processes for preparing these substances, in their use as microbiocides for controlling undesirable microorganisms both in crop protection and in the protection of materials. Additionally, they are suitable for controlling animal pests.Type: GrantFiled: September 18, 2001Date of Patent: March 18, 2003Assignee: Bayer AktiengesellschaftInventors: Hans-Ludwig Elbe, Bernd-Wieland Krüger, Robert Markert, Ralf Tiemann, Dietmar Kuhnt, Stefan Dutzmann, Klaus Stenzel, Christoph Erdelen, Martin Kugler, Hans-Ulrich Buschhaus
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Patent number: 6509369Abstract: This invention relates to anti-inflammatory compounds, methods of making such compounds and methods of using such compounds having the following structure:Type: GrantFiled: January 8, 2002Date of Patent: January 21, 2003Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Malcolm K. Scott, Pauline J. Sanfilippo, Louis J. Fitzpatrick, III, Richard Cordova, Kevin Pan, Joseph Meschino
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Patent number: 6509379Abstract: Phenylacetic acid derivatives of the formula I where the variables are as disclosed herein, their salts, processes and intermediates for their preparation, and their use for controlling harmful fungi and animal pests.Type: GrantFiled: April 23, 1998Date of Patent: January 21, 2003Assignee: BASF AktiengesellschaftInventors: Herbert Bayer, Hubert Sauter, Klaus Oberdorf, Wassilios Grammenos, Thomas Grote, Reinhard Kirstgen, Bernd Müller, Ruth Müller, Franz Röhl, Eberhard Ammermann, Volker Harries, Gisela Lorenz, Siegfried Strathmann, Norbert Götz, Albrecht Harreus
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Patent number: 6498185Abstract: This invention is directed to compounds of formula (III): wherein B, C, D, E, R1, R2 and R3 are disclosed herein. These compounds are disclosed as being useful as anti coagulants.Type: GrantFiled: August 3, 2000Date of Patent: December 24, 2002Assignee: Berlex Laboratories, Inc.Inventors: Damian O. Arnaiz, Yuo-Ling Chou, Brian D. Griedel, Rushad E. Karanjawala, Monica J. Kochanny, Wheeseong Lee, Amy Mei Liang, Michael M. Morrissey, Gary B. Phillips, Karna Lyn Sacchi, Steven T. Sakata, Kenneth J. Shaw, R. Michael Snider, Shung C. Wu, Bin Ye, Zuchun Zhao
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Patent number: 6492412Abstract: 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: June 29, 2001Date of Patent: December 10, 2002Assignee: Pfizer, Inc.Inventors: Kimberly O. Cameron, Hua Z. Ke, Bruce A. Lefker, Robert L. Rosati, David D. Thompson
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Patent number: 6479550Abstract: &agr;-Sulfenimino acid derivatives of formula I including the optical isomers thereof and mixtures of such isomers, wherein A is cycloalkyl, cycloalkenyl, aryl or heteroaryl, each optionally substituted, B is a direct bond or optionally substituted alkylene, E is hydrogen or optionally substituted aryl, R is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, aryl or arylalkyl, each optionally substituted, and T is NH or oxygen, have been found to be useful for controlling or preventing the infestation of plants by phytopathogenic microorganisms, especially fungi. The invention relates the novel compounds and also to the preparation thereof and to the use of the compounds for plant protection, and to compositions suitable for applying the novel compounds in agricultural techniques.Type: GrantFiled: July 16, 2001Date of Patent: November 12, 2002Assignee: Syngenta Crop Protection, Inc.Inventors: André Jeanguenat, Martin Zeller, Hugo Ziegler
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Patent number: 6465060Abstract: Tetrahydrothiophene derivatives of the formula (I) R1—X—(A1—M1)a—(A2—M2)b—A3—Y—T—Z—R2 (I) where the symbols and indices have the following meanings, for example: T is undirected and is tetrahydrothiophene-2,5-diyl or tetrahydrothiophene-2,4-diyl R1 is hydrogen or a straight-chain or branched C1-20-alkyl or C2-20-alkenyl radical (with or without asymmetric carbon atoms), R2 is hydrogen or a straight-chain or branched alkyl radical (with or without asymmetric carbon atoms) having 1 to 20 carbon atoms, X is a single bond, —O—, OC(═O)—, —C(═O)O— or —OC(═O)O— Y is —OC(═O)—, —SC(═O)—, —OCH2— or —CH2CH2— Z is a single bond or —O— A1, A2 and A3 are undirected different and are each, independently of one another phenylene-1,4-diyl, M1 and M2 are undirected and are each, independently of one another —OC(&boxHType: GrantFiled: November 7, 2000Date of Patent: October 15, 2002Assignee: Clariant International Ltd.Inventors: Rainer Wingen, Barbara Hornung, Wolfgang Schmidt
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Patent number: 6455520Abstract: The invention concerns amide derivatives of formula (I) wherein R3 is (1-6C)alkyl or halogeno; m is 0-3, p is 0-2 and q is 0-4; each of R1 and R2 is a group such as hydroxy, halogeno, trifluoromethyl and cyano; R4 is a basic group such as amino, (1-6C)alkylamino, di-[(1-6C)alkyl]amino, di-[(1-6C)alkyl]amino-(1-6C)alkyl, di-[(1-6C)alkyl]amino-(2-6C)alkoxy, heteroaryl, heteroaryloxy, heteroaryl-(1-6C)alkoxy, heterocyclyl, heterocyclyloxy and heterocyclyl-(1-6C)alkoxy; and Q2 is a group such as heteroaryl, heteroaryloxy or heteroaryl-(1-6C)alkoxy which is optionally substituted; or pharmaceutically-acceptable salts or in-vivo-cleavable esters thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases or medical conditions mediated by cytokines.Type: GrantFiled: March 23, 2001Date of Patent: September 24, 2002Assignee: Astra Zeneca ABInventors: Dearg S Brown, George R Brown
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Publication number: 20020132833Abstract: This invention provides novel compounds that are effective as inhibitors of caspase and cellular apoptosis. The invention also provides methods for using the compounds to treat caspase-mediated diseases in mammals.Type: ApplicationFiled: April 3, 2001Publication date: September 19, 2002Inventors: Julian M.C. Golec, Paul Charifson, Guy Brenchley
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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: 6448290Abstract: The sulfonamide or carboamide derivatives of the formula (I) and a pharmaceutical composition which comprise them as an active ingredient: (wherein A ring, B ring is carbocyclic ring, heterocyclic ring; Z1 is —COR1, —CH═CH—COR1 etc.; Z2 is H, alkyl etc.; Z3 is single bond, alkylene; Z4 is SO2, CO; Z5 is alkyl, phenyl, heterocyclic ring etc.; R2 is CONR8, O, S, NZ6, Z7-alkylene, alkylene etc.; R3 is H, alkyl, halogen, CF3 etc.; R4 is H, (substituted) alkyl etc.; n, t is 1-4). The compounds of the formula (I) can bind to receptors of PGE2 and show antagonistic activity against the action thereof or agonistic activity. Therefore, they are considered to be useful as medicine for inhibition of uterine contraction, analgesics, antidiarrheals, sleep inducers, medicine for increase of vesical capacity or medicine for uterine contraction, cathartic, suppression of gastric acid secretion, antihypertensive or diuretic agents.Type: GrantFiled: June 18, 1999Date of Patent: September 10, 2002Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Shuichi Ohuchida, Yuuki Nagao
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Patent number: 6441023Abstract: Matrix metalloproteinases (MMPs) are a group of enzymes that have been implicated in the pathological destruction of connective tissue and basement membranes. These zinc containing endopeptidases consist of several subsets of enzymes including collagenases, stromelysins and gelatinases. TNF-&agr; converting enzyme (TACE), a pro-inflmatory cytokine, catalyzes the formation of TNF-&agr; from membrane bound TNF-&agr; precursor protein. It is expected that small molecule inhibitors of MMPs and TACE therefore have the potential for treating a variety of disease states.Type: GrantFiled: July 3, 2001Date of Patent: August 27, 2002Assignee: American Home Products CorporationInventors: Aranapakam Mudumbai Venkatesan, Jannie Lea Baker, Jeremy Ian Levin
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Patent number: 6429317Abstract: The present invention provides novel indane-like compounds which can be useful for treating psychosis and other conditions associated with the modulation of a muscarinic receptor. The invention provides formulations and methods for using the novel compounds.Type: GrantFiled: September 5, 2000Date of Patent: August 6, 2002Assignee: Eli Lilly and CompanyInventors: Sean P. Hollinshead, Michael A. Staszak, John S. Ward, Joseph W. Wilson, Bret E. Huff, Philip F. Hughes, Jose S. Mendoza, Charles H. Mitch
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Patent number: 6426355Abstract: Compounds having the formula: wherein R1-R5, X and G are described herein and which are useful in the treatment of diseases associated with herpes viruses including human cytomegalovirus, herpes simplex viruses, Epstein-Barr virus, varicella-zoster virus, human herpesviruses-6 and -7, and Kaposi herpesvirus.Type: GrantFiled: September 27, 2000Date of Patent: July 30, 2002Assignee: American Home ProductsInventors: Jonathan Bloom, Kevin Curran, Martin DiGrandi, Russell Dushin, Thomas Jones, Stanley Lang, Adma Ross, Eugene A. Terefenko, Bryan O'Hara
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Patent number: 6414013Abstract: Compounds which are 3-aminocarbonyl-2-carboxamido-thiophene derivatives of formula (I): wherein R1 and R2 are, independently from each other, hydrogen, halogen or an optionally substituted group selected from aryl, straight or branched C1-C6 alkyl or aryl C1-C6 alkyl; or, taken together with the thiophene bond to which they are linked, R1 and R2 form a —(CH2)m—(NR4)n—(CH2)p— group wherein m and p are, each independently, an integer form 1 to 3, n is 0 or 1 and m+n+p is an integer from 3 to 5; and R4 is hydrogen or an optionally substituted straight or branched C1-C6 alkyl group; R3 is a group, optionally further substituted, selected from: i) straight or branched C1-C8 alkyl, C2-C6 alkenyl, C2-C6 alkynyl or C2-C6 alkylcarbonyl; ii) aryl; iii) 3 to 7 membered carbocycle; iv) 5 to 7 membered heterocycle with from 1 to 3 heteroatoms selected from nitrogen, oxygen and sulphur; or a pharmaceutically acceptable salt thereof; are useful in the treatment of diseasesType: GrantFiled: June 19, 2000Date of Patent: July 2, 2002Assignee: Pharmacia & Upjohn S.p.A.Inventors: Daniele Fancelli, Paolo Pevarello, Mario Varasi
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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: 6372779Abstract: This invention relates to anti-inflammatory compounds, methods of making such compounds and methods of using such compounds having the following structure:Type: GrantFiled: December 28, 1998Date of Patent: April 16, 2002Assignee: Ortho Pharmaceutical CorporationInventors: Malcolm K. Scott, Pauline J. Sanfilippo, Louis J. Fitzpatrick, III, Richard Cordova, Kevin Pan, Joseph Meschino
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Patent number: 6372895Abstract: Disclosed are novel coumarin based fluorogenic compounds useful in assaying for biological activity. Specifically, these fluorogenic compounds exhibit fluorescence at particular wavelengths when cleaved by target enzymes. Preferred compounds include sugar and peptide derivatives of umbelliferone derivatives bearing a heterocyclic five membered ring at the 3-position. These compounds can be used for rapidly detecting food pathogens and for determining sterilization effectiveness. The compounds may also be used in a form bounded to a polymeric support or to a biomolecule or macromolecule.Type: GrantFiled: July 7, 2000Date of Patent: April 16, 2002Assignee: 3M Innovative Properties CompanyInventors: James Gregory Bentsen, Christopher Allen Mickelson, Orlin Bruce Knudson, Kevin Michael Lewandowski