Sulfur Containing Hetero Ring (e.g., Thioxane, Etc.) Patents (Class 544/145)
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Publication number: 20040019084Abstract: The invention concerns novel lipoic acid derivatives, which have an inhibiting action with respect to NO-synthase enzymes producing nitrogen monoxide NO and/or are agents enabling the regeneration of antioxidants or entities trapping reactive oxygen species (ROS) and intervening in a more general manner in the redox status of thiol groups. The invention also concerns methods for preparing them, pharmaceutical compositions containing them and their use for therapeutic purposes, particularly their use as NO-synthase inhibitors and/or as agents acting more generally in the redox status of thiol groups.Type: ApplicationFiled: April 21, 2003Publication date: January 29, 2004Applicant: SOCIETE DE CONSEILS DE RECHERCHES ET D'APPLICATION SCIENTIFIQUES (S.C.R.A.S)Inventors: Jeremiah Harnett, Michel Auguet, Pierre-Etienne Chabrier de Lassauhyere
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Publication number: 20030232819Abstract: The present invention provides novel tropane compounds and methods for their use.Type: ApplicationFiled: March 27, 2003Publication date: December 18, 2003Inventors: Paul Blundell, Peter C. Meltzer, Bertha K. Madras
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Publication number: 20030232827Abstract: This invention to antagonists that inhibit transporters and receptors. The invention also relates to partial inhibitors of transporters and receptors that allow partial transport or partial binding of a compound to the transporter or receptor. The invention also relates to compounds that differentially prevent transport or binding through a transporter or to a receptor. The invention also relates to the use of these compounds for treating certain diseases and disorders.Type: ApplicationFiled: February 10, 2003Publication date: December 18, 2003Inventors: Peter C. Meltzer, Bertha K. Madras, Paul Blundell, Shanghao Lui
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Publication number: 20030216570Abstract: Compounds of the formula 1Type: ApplicationFiled: April 30, 2002Publication date: November 20, 2003Inventors: Jayasree Vasudevan, Dehua Huang, Vidyasagar Vuligonda, Roshantha S. Chandraratna
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Publication number: 20030212061Abstract: The present invention relates to a group of aza-thioxanthenone compounds having antitumor activity, and processes for their preparation. Compositions containing the aza-thioxanthenone compounds and methods of treating tumors and cancer in mammals with the compounds of the present invention are also disclosed.Type: ApplicationFiled: March 12, 2002Publication date: November 13, 2003Inventor: Simon N. Haydar
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Patent number: 6638930Abstract: Substituted heterocycles of the general structural formula: are tachykinin receptor antagonists useful in the treatment of inflammatory diseases, pain or migraine, asthma and emesis, and calcium channel blockers useful in the treatment of cardiovascular conditions such as angina, hypertension or ischemia.Type: GrantFiled: April 17, 2001Date of Patent: October 28, 2003Assignee: Merck & Co. Inc.Inventors: Conrad P. Dorn, Paul E. Finke, Jeffrey J. Hale, Malcolm Maccoss, Sander G. Mills, Shrenik K. Shah, Mark Stuart Chambers, Timothy Harrison, Tamara Ladduwahetty, Brian John Williams
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Publication number: 20030181445Abstract: The invention provides novel compounds of the formula I below: 1Type: ApplicationFiled: January 17, 2003Publication date: September 25, 2003Applicant: H. Lundbeck A/SInventors: Ejner Knud Moltzen, Garrick Paul Smith, Christian Krog-Jensen, Klaus Peter Bogeso
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Publication number: 20030171372Abstract: The invention provides a method, compounds, and compositions for inhibiting the replication or proliferation of a virus. In accordance with the invention, at least one cannabichromene derivative is exposed to the virus, a host cell, or an infected cell under conditions sufficient to inhibit the replication or proliferation of the virus.Type: ApplicationFiled: January 16, 2003Publication date: September 11, 2003Applicant: Immugen Pharmaceuticals, Inc.Inventor: Craig R. Travis
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Publication number: 20030166650Abstract: There is provided novel cinnamide derivatives of Formula I 1Type: ApplicationFiled: May 31, 2002Publication date: September 4, 2003Inventors: Yong-Jin Wu, Li-Quang Sun, Jie Chen, Huan He, Alexandre L'Heureux, Pierre Dextraze, Jean-Paul Daris, Gene G. Kinney, Steven I. Dworetzky, Piyasena Hewawasam
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Publication number: 20030158194Abstract: The subject invention pertains to novel compounds (and salts thereof), and compositions comprising the compounds, for the treatment of cardiac arrhythmias. The subject invention further concerns methods of making the novel compounds. The novel compounds are rapidly metabolized analogs of amiodarone, having the distinct and advantageous characteristic of being metabolized to a less lipophilic compound. This results in an improved safety profile. The new compounds have particular utility for treating life-threatening ventricular tachyarrhythmias, especially in patients with congestive heart failure (CHF). The compounds also provide effective management for ventricular arrhythmias and supraventricular arrhythmias, including atrial fibrillation and re-entrant tachyarrhythmias involving accessory pathways.Type: ApplicationFiled: December 10, 2002Publication date: August 21, 2003Inventor: Pascal Druzgala
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Publication number: 20030158191Abstract: The invention provides cannabinol derivatives and pharmaceutical preparations thereof.Type: ApplicationFiled: December 22, 2002Publication date: August 21, 2003Inventor: Craig R. Travis
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Patent number: 6608057Abstract: Disclosed are cathepsin S reversible inhibitory compounds of the formulas (I),(Ia) and (II),(IIa) as defined herein. The compounds are useful for treating autoimmune diseases.Type: GrantFiled: October 24, 2001Date of Patent: August 19, 2003Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Charles L. Cywin, Michel J. Emmanuel, Tina Morwick, Denice M. Spero, David S. Thomson, Yancey D. Ward
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Publication number: 20030153557Abstract: The present invention relates to thienyl substituted acylguanidine derivatives, such as compounds of formula (I) in which R1, R2, R4, R6, A, B and D have the meanings indicated in the claims, their physiologically tolerable salts and their prodrugs. The compounds of the present invention are valuable pharmaceutical active compounds. They are vitronectin receptor antagonists and inhibitors of bone resorption by osteoclasts. They are suitable, for example, for the therapy and prophylaxis of diseases which are caused at least partially by an undesired extent of bone resorption, for example of osteoporosis. The invention furthermore relates to processes for the preparation of thienyl substituted acylguanidines, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.Type: ApplicationFiled: November 14, 2002Publication date: August 14, 2003Applicant: Aventis Pharma Deutschland GmbH and 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: 6605637Abstract: The invention concerns novel lipoic acid derivatives, which have an inhibiting action with respect to NO-synthase enzymes producing nitrogen monoxide NO and/or are agents enabling the regeneration of antioxidants or entities trapping reactive oxygen species (ROS) and intervening in a more general manner in the redox status of thiol groups. The invention also concerns methods for preparing them, pharmaceutical compositions containing them and their use for therapeutic purposes, particularly their use as NO-synthase inhibitors and/or as agents acting more generally in the redox status of thiol groups.Type: GrantFiled: September 27, 2001Date of Patent: August 12, 2003Assignee: Societe de Conseils de Recherches et d'Applications Scientifiques (S.C.R.A.S.)Inventors: Jeremiah Harnett, Michel Auguet, Pierre-Etienne Chabrier de Lassauniere
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Publication number: 20030149030Abstract: A compound of the formula 1Type: ApplicationFiled: December 10, 2002Publication date: August 7, 2003Inventors: Alexander Alanine, Alexander Flohr
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Publication number: 20030130279Abstract: The present invention relates to compounds with the formula (I) 1Type: ApplicationFiled: November 22, 2002Publication date: July 10, 2003Inventors: Guido Kurz, Marianne Nilsson, Jerk Vallgarda, Meredith Williams
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Publication number: 20030105096Abstract: The present invention relates to the therapeutic use of non-amine tropane analogues that bind to the SERT to treat neuropsychiatric disorders.Type: ApplicationFiled: February 28, 2002Publication date: June 5, 2003Inventors: Bertha K. Madras, Peter C. Meltzer
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Patent number: 6544990Abstract: The present invention discloses disubstiuted 4-oxo-1,4-dihydro-3-quinolinecarboxamide derivatives. The compounds are useful as antiviral agents, in particular, as agents against viruses of the herpes family.Type: GrantFiled: February 27, 2002Date of Patent: April 8, 2003Assignee: Pharmacia & Upjohn CompanyInventors: Valerie A. Vaillancourt, Joseph Walter Strohbach, Audris Huang
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Patent number: 6525086Abstract: The present invention relates to compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, A, X, T, Q, Z, U, Y, Ar, p and n are as defined in the specification. These compounds are useful in the treatment and/or prevention of conditions mediated by nuclear receptors, in particular the Peroxisome Proliferator-Activated Receptors (PPAR).Type: GrantFiled: March 14, 2001Date of Patent: February 25, 2003Assignee: Novo Nordisk A/SInventors: Lone Jeppesen, Paul Stanley Bury, Per Sauerberg
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Publication number: 20020198193Abstract: The present invention relates to novel compounds of formula (I): 1Type: ApplicationFiled: May 6, 2002Publication date: December 26, 2002Applicant: LABORATOIRES FOURNIER S.A.Inventors: Veronique Barberousse, Soth Samreth
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Patent number: 6498274Abstract: The invention concerns the use of amide derivatives of formula (I) wherein: R1 and R2 are substituents such as hydroxy, C1-6alkoxy, mercapto, C1-6alkylthio, amino, C1-6alkylamino and di-(C1-6alkyl)amino; m and p are independently 0-3R3 is C1-4alkyl; q is 0-4; and R4 is aryl or cycloalkyl; or a pharmaceutically acceptable salt thereof in the manufacture of a medicament for use in the treatment of diseases or medical conditions mediated by cytokinesType: GrantFiled: March 7, 2000Date of Patent: December 24, 2002Assignee: Zeneca LimitedInventors: Dearg S Brown, George R Brown, Philip Cohen
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Publication number: 20020173645Abstract: The present invention is directed to chemical processes for preparing 2-aryl-6-hydroxy-3-[4-(2-aminoethoxy)benzoyl]benzo[b]-thiophenes. The present invention is also directed to crystalline solvates and a non-solvated crystalline form of 6-hydroxy-2-(4-hydroxyphenyl)-3-[4-(2-piperidinoethoxy)benzoyl]-benzo[b]thiophene hydrochloride, as well as processes for their preparation.Type: ApplicationFiled: February 26, 2002Publication date: November 21, 2002Inventor: Wayne Douglas Luke
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Publication number: 20020156077Abstract: Novel non-steroidal estrogen receptor ligands and methods of synthesis are disclosed. The novel molecules are intended for use in therapeutic preparations for the treatment of estrogen receptor related disease states. The compounds specified are tetra-cyclic derivatives and have been shown to be antiproliferative against human estrogen-dependent cancer cells and to have good binding affinity for the estrogen receptor.Type: ApplicationFiled: August 21, 2001Publication date: October 24, 2002Inventors: Jonathan Martin Schmidt, Julie Mercure, Jeffry Lawrence Lowell, Stefan Kwiatkowski, Krzysztof Pupek, Shuguang Zhu, John Whelan, Natalie Lazarowych
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Patent number: 6440958Abstract: This invention is directed to a class of acrylic and propionic acid compounds and their use in the treatment of post-menopausal symptoms and restenosis. In other embodiments, the invention is directed to intermediates and to processes for the preparation of the acrylic and propionic acid compounds.Type: GrantFiled: June 25, 1996Date of Patent: August 27, 2002Assignee: Eli Lilly and CompanyInventors: Charles David Jones, Alan David Palkowitz, Kenneth Jeff Thrasher
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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: 20020091150Abstract: The present invention is a compound of formula 1Type: ApplicationFiled: December 10, 2001Publication date: July 11, 2002Inventors: Konrad Bleicher, Vincent Mutel, Eric Vieira, Jurgen Wichmann, Thomas Johannes Woltering
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Publication number: 20020068739Abstract: The present invention relates to the compounds of formula (I) in which X, R1, R2 and R3 are as defined in claim 1. These compounds are cholesteryl acyl transferase (ACAT) inhibitors.Type: ApplicationFiled: November 1, 2001Publication date: June 6, 2002Applicant: Merck Patent Gesellschaft mit beschrankter HaftungInventors: Diedier Festal, Jean Yves Nioche, Guy Augert, Jacques Deserprit
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Patent number: 6391901Abstract: This application relates to novel compounds of formula I (and their pharmaceutically acceptable salts), as defined herein, processes and intermediates for their preparation, pharmaceutical formulations comprising the novel compounds of formula I, and the use of defined compounds of formula I as thrombin inhibitors.Type: GrantFiled: January 21, 2000Date of Patent: May 21, 2002Assignee: Eli Lilly and CompanyInventors: Nickolay Y Chirgadze, Michael L Denney, Matthew J Fisher, Robert J Foglesong, Richard W Harper, Mary G Johnson, Ho-Shen Lin, Michael P Lynch, Jefferson R McCowan, Shawn C Miller, Alan D Palkowitz, Michael E Richett, Daniel J Sall, Gerald F Smith, Kumiko Takeuchi, Minsheng Zhang
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Patent number: 6392040Abstract: The compounds of formula I are useful in treating gastrointestinal disorders associated with antagonizing the motilin receptor. The compounds compete with erythromycin and motilin for the motilin receptor. In addition the compounds are antagonists of the contractile smooth muscle response to those ligands.Type: GrantFiled: March 9, 2001Date of Patent: May 21, 2002Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Robert H. Chen, Min A. Xiang
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Publication number: 20020045764Abstract: Novel tubulin binding compounds having potent tubulin depolymerization activity and inhibitory activity against tubulin polymerization. The compounds are effective agents for inhibiting cellular proliferation, for example, in cancer cells. The compounds are adapted to interact favorably with a novel tubulin binding pocket, which pocket is useful for screening of anti-tubulin, anti-proliferation, and anti-cancer drugs.Type: ApplicationFiled: June 28, 2001Publication date: April 18, 2002Applicant: Parker Hughes InstituteInventors: Fatih M. Uckun, Shyi-Tai Jan, Chen Mao
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Patent number: 6358885Abstract: This invention relates to certain phenylheterocyclic compounds, herbicidal compositions thereof and a method for their use as general and selective preemergent or postemergent herbicides or plant growth regulants.Type: GrantFiled: April 15, 1999Date of Patent: March 19, 2002Assignees: Mississippi State University, Research Technology Corporation Mississippi StateInventors: Thomas P. Selby, Thomas M. Stevenson
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Patent number: 6352987Abstract: 8,8a-Dihydroindeno[1,2-d]thiazole derivatives which carry in the 2-position a substituent having a sulfonamide structure or sulfone structure; processes for their preparation and their use as medicaments The invention relates to polycyclic dihydrothiazoles and to their physiologically acceptable salts and physiologically functional derivatives. Compounds of formula I, in which the radicals are as defined above, and their physiologically acceptable salts and processes for their preparation are described. The compounds are suitable, for example, as anorectics.Type: GrantFiled: February 26, 2001Date of Patent: March 5, 2002Assignee: Aventis Pharma Deutschland GmbHInventors: Gerhard Jaehne, Hans Jochen Lang, Matthias Gossel, Martin Bickel
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Patent number: 6342512Abstract: Sulfonylcarboxamide derivatives of formula I, their physiologically acceptable salts and/or physiologically functional derivatives, methods of making these compounds, their use for preparing medicines for the prevention and treatment of hyperlipidemia and arteriosclerotic disorders. The compounds of formula I have the following structure: in which the radicals are as defined and their physiologically acceptable salts and physiologically functional derivatives are described.Type: GrantFiled: September 1, 2000Date of Patent: January 29, 2002Assignee: Aventis Pharma Deutschland GmbHInventors: Reinhard Kirsch, Hans-Ludwig Schaefer, Eugen Falk, Horst Hemmerle
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Patent number: 6313164Abstract: Compounds of the formula (I): wherein one of m and n is 0, and the other is 0, 1 or 2; k is 0 or 1 to 12; R1 is hydrogen, a substituent which is an aryl or a heterocyclic, or an optionally substituted alkyl group; A is a single bond, an oxygen atom, a carbonyl group or a group of the formula —N(R2)CO—, —N(R2)CS—, —N(R2)SO2—, —CON(R2)N(R3)CO—, —CON(R2)CO—, —CON(R2)CS—, —CON(R2)SO2—, —O—CO—, —ON(R2)CO—, —ON(R2)SO2—, —O—CON(R2)N(R3)CO—, —O—CON(R2)CO—, —O—CON(R2)SO2—, —CO—O—, —CO—CO—, —CO—CON(R2)N(R3)CO—, —CO—CON(R2)CO—, —CO—CON(R2)SO2—, —N(R2)O—, —N(R2)COCO—, —N(R2)N(R3)CO—, —N(R2)N(R3)SO2—, —N(R2)CON(R3)N(R4)CO—, —N(R2)CON(R3)CO—, —N(R2)CON(R3)SO2&mdasType: GrantFiled: July 15, 1999Date of Patent: November 6, 2001Assignee: Sankyo Company, LimitedInventors: Takashi Fujita, Tomihisa Yokoyama
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Patent number: 6284756Abstract: This application relates to novel compounds of formula I (and their pharmaceutically acceptable salts), as defined herein, processes and intermediates for their preparation, pharmaceutical formulations comprising the novel compounds of formula I, and the use of the compounds of formula I as thrombin inhibitors.Type: GrantFiled: January 21, 2000Date of Patent: September 4, 2001Assignee: Eli Lilly and CompanyInventors: Nickolay Y Chirgadze, Richard W Harper, Todd J Kohn, Ho-Shen Lin, Jefferson R McCowan, Alan D Palkowitz, Daniel J Sall, Gerald F Smith, Kumiko Takeuchi, Michael R Wiley, Minsheng Zhang
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Patent number: 6166006Abstract: This invention is to provide a compound of the formula: ##STR1## wherein R.sup.1 is an optionally substituted 5- to 6-membered ring: C is a divalent group of the formula: ##STR2## wherein the ring A is an optionally substituted 5- to 6-membered aromatic ring, X is an optionally substituted C, N or O atom, and the ring B is an optionally substituted 5- to 7-membered ring; Z is a chemical bond or a divalent group; R.sup.2 is (1) an optionally substituted amino group in which a nitrogen atom may form a quaternary ammonium, etc., or a salt thereof, which is useful for antagonizing MCP-1 receptor.Type: GrantFiled: December 17, 1998Date of Patent: December 26, 2000Assignee: Takeda Chemical Industries, Ltd.Inventors: Mitsuru Shiraishi, Takahito Kitayoshi, Yoshio Aramaki, Susumu Honda, Tsuneo Oda
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Patent number: 6150358Abstract: A compound of formula (I): ##STR1## wherein Ra represents linear or branched (C.sub.1 -C.sub.8)alkylene,Rb represents single bond, or linear or branched (C.sub.1 -C.sub.6)alkylene,Z represents thiocarbamate, or thioamide, each being optionally substituted,T represents optionally substituted morpholino,its isomers, and pharmaceutically-acceptable acid or base addition salts thereof, and medicinal products containing the same which are useful in the treatment of disease for which the use of anti-oxidation agent is required.Type: GrantFiled: December 14, 1999Date of Patent: November 21, 2000Assignee: Adir et CompagnieInventors: Solo Goldstein, Claude Guillonneau, Yves Charton, Pierre Lestage, Brian Lockhart
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Patent number: 6133262Abstract: This application relates to novel compounds of formula I (and their pharmaceutically acceptable salts), as defined herein, processes and intermediates for their preparation, pharmaceutical formulations comprising the novel compounds of formula I, and the use of the compounds of formula I as thrombin inhibitors.Type: GrantFiled: October 28, 1999Date of Patent: October 17, 2000Assignee: Eli Lilly and CompanyInventors: Jefferson Ray McCowan, John Eldon Toth, Daniel Jon Sall
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Patent number: 6133288Abstract: The present invention provides compounds of formula I and II: ##STR1## wherein X is --O--, --S--, or --NR.sup.5 --;Y is --O--, --S--, --CH.sub.2 --, --CH.sub.2 CH.sub.2 --, --CH.dbd.CH--, or --NR.sup.5 --;B is --CH.sup.2 -- or --CO--;R.sup.1, R.sup.2, and R.sup.3 are each independently --H, --OH, --O(C.sub.1 -C.sub.4 alkyl), --OCOC.sub.6 H.sub.5, --OCO(C.sub.1 -C.sub.6 alkyl), --OSO.sub.2 (C.sub.4 -C.sub.6 alkyl), --OSO.sub.2 CF.sub.3, Cl, or F;n is 1 or 2;W is CH.sub.2 or C.dbd.O;R.sup.4 is 1-piperidinyl, 2-oxo-1-piperidinyl, 1-pyrrolidinyl, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidinyl, 2-oxo-1-pyrrolidinyl, 4-morpholino, dimethylamino, diethylamino, or 1-hexamethyleneimino;R.sup.5 is C.sub.1 -C.sub.3 alkyl, --COC.sub.6 H.sub.5, --CO(C.sub.1 -C.sub.6 alkyl), --C(O)OC.sub.6 H.sub.5, --C(O)O(C.sub.1 -C.sub.6 alkyl), --SO.sub.2 (C.sub.1 -C.sub.6 alkyl), --SO.sub.2 C.sub.6 H.sub.5, or --SO.sub.2 CF.sub.3 ;or a pharmaceutically acceptable salt or solvate thereof.Type: GrantFiled: November 9, 1999Date of Patent: October 17, 2000Assignee: Eli Lilly and CompanyInventor: Timothy Alan Grese
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Patent number: 6087359Abstract: A thioaryl sulfonamide hydroxamic acid compound that inter alia inhibits matrix metalloprotease activity is disclosed as are a treatment process that comprises administering a contemplated thioaryl sulfonamide hydroxamic acid compound in a MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity.Type: GrantFiled: September 10, 1999Date of Patent: July 11, 2000Inventors: Daniel P. Getman, Daniel P. Becker, Thomas E. Barta, Clara I. Villamil, Susan L. Hockerman, Louis J. Bedell, Hui Li, John N. Freskos, Robert M. Heintz, Joseph J. McDonald, Gary A. DeCrescenzo
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Patent number: 6060468Abstract: The present invention relates to novel N-substituted azaheterocyclic compounds of the general formula ##STR1## wherein X, Y, Z, R.sup.1, R.sup.1a, R.sup.2, R.sup.2a, p, r and s are as defined in the detailed part of the present description or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation as well as their use for treatment of indications caused by or related to secretion and circulation of insulin antagonising peptides.Type: GrantFiled: October 3, 1997Date of Patent: May 9, 2000Assignee: Novo Nordisk A/SInventors: Tine Krogh J.o slashed.rgensen, Erik Fischer, Rolf Hohlweg, Knud Erik Andersen, Uffe Bang Olsen, Zdenek Polivka, Vladimir Valenta, Karel Sindelar
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Patent number: 6025495Abstract: The present invention provides processes for the regioselective alkylation of benzothiophenes.Type: GrantFiled: April 29, 1998Date of Patent: February 15, 2000Assignee: Eli Lilly and CompanyInventors: John McNeill McGill, III, Randal Scott Miller
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Patent number: 6013663Abstract: A compound of formula (I): ##STR1## wherein one of m and n represents 0, and the other represents 0, 1 or 2; k represents 0 or 1 to 12; R.sup.1 is hydrogen, an aryl, a heterocyclic, an alkyl, a hydroxy or --OR.sup.7, wherein R.sup.7 is an alkyl, an alkenyl or an aralkyl; A is --CON(R.sup.2)SO.sub.2--, wherein R.sup.2 is hydrogen, an alkyl or an aralkyl; B is a single bond; and pharmaceutically acceptable salts thereof. The compounds have the ability to enhance the activity of glutathione reductase and can therefore be used for the treatment and prevention of a variety of diseases including cataracts.Type: GrantFiled: March 31, 1998Date of Patent: January 11, 2000Assignee: Sankyo Company, LimitedInventors: Takashi Fujita, Tomihisa Yokoyama
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Patent number: 5977098Abstract: The invention provides a compound of formula I: ##STR1## or a pharmaceutically acceptable salt or solvate thereof; pharmaceutical formulations containing a compound of formula I, and methods of using a compound of formula I for the inhibition of bone loss or bone resorption and for treatment of cardiovascular-related pathological conditions.Type: GrantFiled: June 30, 1998Date of Patent: November 2, 1999Assignee: Eli Lilly and CompanyInventor: Alan David Palkowitz
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Patent number: 5922706Abstract: Substituted heterocycles of the general structural formula: ##STR1## are tachykinin receptor antagonists useful in the treatment of inflammatory diseases, pain or migraine, asthma and emesis, and calcium channel blockers useful in the treatment of cardiovascular conditions such as angina, hypertension or ischemia.Type: GrantFiled: November 13, 1997Date of Patent: July 13, 1999Assignee: Merck & Co., Inc.Inventors: Conrad P. Dorn, Jeffrey J. Hale, Malcolm Maccoss, Sander G. Mills, Shrenik K. Shah, Tamara Ladduwahetty
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Patent number: 5914351Abstract: Compounds of the formula ##STR1## wherein Q is a hydrazone derivative;R.sup.1 is hydrogen, halogen, alkyl or alkoxy;R.sup.2 is hydrogen, halogen, alkyl, alkoxy, alkenoxy, alkynyloxy, halomethyl, trifluoromethoxy, alkylthio, nitro or cyano; andR.sup.6 is a substituted carboxamide, carbothioamide, phosphonosoamide, or phosphonothioamide,useful as anti-HIV agents.Type: GrantFiled: December 12, 1997Date of Patent: June 22, 1999Assignees: Uniroyal Chemical Company, Inc., Uniroyal Chemical Co./CIE.Inventors: Walter Gerhard Brouwer, Ewa Maria Osika
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Patent number: 5866577Abstract: An anticoagulant agent which comprises, as an active ingredient, an aromatic amidine derivative represented by the following general formula (1) or a salt thereof: ##STR1## wherein the group represented by ##STR2## is a group selected from indolyl, benzofuranyl, benzothienyl, benzimidazolyl, benzoxazolyl, benzothiazolyl, naphthyl, tetrahydronaphthyl and indanyl; X is a single bond, an oxygen atom, a sulfur atom or a carbonyl group; and Y is a saturated or unsaturated 5- or 6-membered heterocyclic moiety or cyclic hydrocarbon moiety optionally having a substituent group, an amino group optionally having a substituent group or an aminoalkyl group optionally having a substituent group.The inventive compound has a high anticoagulant capacity based on its excellent FXa inhibition activity.Type: GrantFiled: September 5, 1997Date of Patent: February 2, 1999Assignee: Daiichi Pharmaceutical Co., Ltd.Inventors: Takayasu Nagahara, Naoaki Kanaya, Kazue Inamura, Yukio Yokoyama
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Patent number: 5856341Abstract: The invention provides benzo?b!indenothiophene compounds of formula I ##STR1## wherein, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, and R.sup.6, are as defined in the specification, intermediates, formulations, and methods of inhibiting bone loss or bone resorption, particularly osteoporosis, cardiovascular-related pathological conditions including hyperlipidemia and related cardiovascular pathologies, and estrogen-dependent cancer.Type: GrantFiled: September 19, 1997Date of Patent: January 5, 1999Assignee: Eli Lilly and CompanyInventors: Michael Gregory Bell, Brian Stephen Muehl, Mark Alan Winter
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Patent number: 5856520Abstract: A novel substituted benzenedithiol metal complex represented by the general formula (1) is provided. The substituted benzenedithiol metal complex is useful as a singlet oxygen quencher and as an optical data recording medium per se. ##STR1## wherein M is a transition metal; A.sup.+ is a quaternary ammonium group; and R is an organic group selected from the group consisting of organic groups represented by the formulae (i), (ii), (iii) and (iv): ##STR2## (wherein R.sup.1 is an alkyl group having 1 to 4 carbon atoms), ##STR3## (wherein n is 3, 4 or 5), ##STR4## (wherein R.sup.2 is one of a hydrogen atom and a substitutent having 1 to 4 carbon atoms).Type: GrantFiled: October 20, 1997Date of Patent: January 5, 1999Assignee: Sumitomo Seika Chemicals Co., Ltd.Inventors: Kazuyoshi Hirako, Satoshi Kimura, Michio Suzuki
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Patent number: 5843940Abstract: The invention provides benzothiophene compounds, formulations, and methods of inhibiting bone loss or bone resorption, particularly osteoporosis, and cardiovascular-related pathological conditions including hyperlipidemia, and estrogen-dependent cancer.Type: GrantFiled: October 23, 1997Date of Patent: December 1, 1998Assignee: Eli Lilly and CompanyInventors: George Joseph Cullinan, Brian Stephen Muehl