Having -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To The Thiazole Ring Patents (Class 548/200)
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Publication number: 20040176427Abstract: A compound of formula (1) and pharmaceutically acceptable salts, solvates and hydrolysable esters thereof: wherein R1 and R2 are independently H or C1-3 alkyl or R1 and R2 which are bonded to the same carbon atom may together with the carbon atom to which they are bonded form a 3-5 membered cycloalkyl ring; X1 represents O or S; Each R3, R4, R8 and R9 independently represents H, halogen, —CH3 and OCH3; R5 represents H or C1-6 alkyl or R4 and R5 together form a 3-6 member cycloalkyl ring. X2 represents NH, NCH3 or O; One of Y and Z is N, and the other is O or S; R6 represents phenyl or pyridyl (wherein the N is in position 2 or 3) and is optionally substituted by one more halogen, CF3, C1-6 straight or branched alkyl (optionally substituted by halogen), with the provision that when R6 is pyridyl, the N is unsubstituted.Type: ApplicationFiled: April 29, 2004Publication date: September 9, 2004Inventors: Bernard Dumaitre, Romain Luc Gosmini
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Patent number: 6787522Abstract: Compounds of formula (I) are antibacterials: wherein: R1 represents hydrogen, or C1-C6 alkyl or C1-C6 alkyl substituted by one or more halogen atoms; R2 represents a group R10—(X)n—(ALK)m— wherein R10 represents hydrogen, or a C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, cycloalkyl, aryl, or heterocyclyl group, any of which may be unsubstituted or substituted by (C1-C6)alkyl, (C1-C6)alkoxy, hydroxy, mercapto, (C1-C6)alkylthio, amino, halo (including fluoro, chloro, bromo and iodo), trifluoromethyl, cyano, nitro, —COOH, —CONH2, —COORA, —NHCORA, —CONHRA, —NHRA, —NRARB, or —CONRARB wherein RA and RB are independently a (C1-C6)alkyl group, and ALK represents a straight or branched divalent C1-C6 alkylene, C2-C6 alkenylene, or C2-C6 alkynylene radical, and may be interrupted by one or more non-adjacent —NH—, —O— or —S— linkages, X represents —NH—, —O— or —S—, anType: GrantFiled: April 30, 2002Date of Patent: September 7, 2004Assignee: British Biotech PharmaceuticalsInventors: Michael George Hunter, Raymond Paul Beckett, John Martin Clements, Mark Whittaker, Stephen John Davies, Lisa Marie Pratt, Zoe Marie Spavold, Steven Launchbury
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Publication number: 20040171842Abstract: Compounds of the formula: 1Type: ApplicationFiled: December 4, 2003Publication date: September 2, 2004Applicant: Pfizer IncInventors: David John Kucera, Robert William Scott
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Publication number: 20040171840Abstract: A process for preparing &agr;-functionalized thiazolidines or oxazolidines, each of which are oxycarbonyl-functionalized in the 4-position, by adding a base to a reaction mixture comprising an oxycarbonyl-functionalized thiazolidine or oxazolidine and an electrophile at a temperature of greater than −40° C.Type: ApplicationFiled: February 24, 2004Publication date: September 2, 2004Applicant: Consortium fur Elektrochemische Industrie GmbHInventors: Dieter Heldmann, Jurgen Stohrer
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Publication number: 20040167341Abstract: The present invention relates to novel compounds of formula (I):, their use for inhibiting serine proteases, such as dipeptidyl peptidases, such as dipeptidyl peptidase IV (DPP-IV) and to methods for their production and their therapeutic utility.Type: ApplicationFiled: December 19, 2003Publication date: August 26, 2004Inventors: Curt Dale Haffner, Darryl Lynn McDougald, Armarjit Sab Randhawa, Steven Michael Reister, David N Deaton, Martin James Lenhard
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Publication number: 20040167191Abstract: The present invention provides compounds of the formula: 1Type: ApplicationFiled: February 13, 2004Publication date: August 26, 2004Inventors: Hans-Ulrich Demuth, Torsten Hoffmann, Ulrich Heiser
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Patent number: 6770656Abstract: The present invention is related to substituted amine derivatives notably for use as pharmaceutically active compounds, as well as to pharmaceutical formulations containing such amine derivatives of formula (I). Said substituted amine derivatives are efficient modulators, in particular inhibitors, of the Bax function and/or activation. The present invention is furthermore related to novel substituted amine derivatives as well as methods of their preparation.Type: GrantFiled: December 26, 2002Date of Patent: August 3, 2004Assignee: Applied Research Systems ARS Holding N.V.Inventors: Serge Halazy, Matthias Schwarz, Bruno Antonsson, Agnes Bombrun, Jean-Claude Martinou, Dennis Church
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Publication number: 20040138265Abstract: The invention concerns novel carboxamides of formula (I) wherein A is (A1), (A2), (A3), (A4), (A5); Q is (Q1), (Q2), (Q3), (Q4), (Q5), (Q6); R1 is CH2 R2, CH2CH═CHR2, CH═C═CHR2 or COR3; R2 is hydrogen, C1-C6alkyl, C1-C6haloalkyl, C2-C6alkenyl, C2-C6alkynyl, C3-C7cycloalkyl, COOC1-C4alkyl, COOC3-C6alkenyl, COOC3-C6alkynyl or CN; R3 is C1-C6alkyl, C1-C6alkyl substituted by halogen, C1-C6alkoxy or C1-C6haloalkoxy; or is C1-C6alkylthio, C1-C6haloalkylthio, C1-C6alkoxy, C1-C6haloalkoxy; C3-C6alkenyloxy or C3-C6haloalkenyloxy; C3-C6haloalkenyloxy; C3-C6alkynyloxy or C3-C6haloalkynyloxy; R4 is methyl, CF2Cl, CF3, CF2H, CFH2, Cl or Br, R5 is methyl, CF3, CH2OCH3 or CH2OCF3; R6 is hydrogen, fluoro, CF3 or methyl; R7 is hydrogen, methyl or halogen; and Z is phenyl, halophenyl, C5-C7cycloalkyl, C5-C7acycloalkyl substituted by C1-C3alkyl, C1C3haloalkyl or halogen, or a group of the form —CHR8—CH2—CHR9R10 wherein R8, R9 and R10 are independently of each other C1-C3alkyl.Type: ApplicationFiled: January 12, 2004Publication date: July 15, 2004Inventors: Harald Walter, Stephan Trah
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Publication number: 20040138268Abstract: Novel aminoalkylthiazole derivatives of Formula I are described which are openers of KCNQ potassium channels and are useful in the treatment of disorders responsive to the opening of the KCNQ potassium channels, including pain and migraine.Type: ApplicationFiled: December 9, 2003Publication date: July 15, 2004Inventors: Kenneth M. Boy, Yong-Jin Wu
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Patent number: 6759412Abstract: The present invention relates to compounds according to the general formula (I), wherein R1-R4 have the meanings given in the description, A is CH2, CHOH or CH—(C1-C3-alkyl), B, C and D are independently CH2 or CH—(C1-C3-alkyl), and R5 is an aryl or heteroaryl group, possibly substituted by the substituents listed in the description.Type: GrantFiled: February 13, 2002Date of Patent: July 6, 2004Assignee: Aventis Pharma Deutschland GmbHInventors: Hartmut Strobel, Paulus Wohlfart
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Publication number: 20040110831Abstract: The invention relates to the compounds of general formula (I), that are present with respect to R1 as racemates as well as L- or D-configured compounds and as E/Z mixtures as well as E or Z isomers and in which the various symbols are defined as in the description and the claims, as well as to the salts thereof, for use as therapeutic agents and for diagnostic purposes. The inventive compounds can be processed to medicaments or to diagnostic agents that are used for the diagnosis, therapy and prevention of urokinase- or urokinase-receptor associated diseases, for example for the treatment of tumors. The compounds are highly efficient in inhibiting growth and/or spread of malign tumors, for example tumor spread of pancreatic cancer, tumor growth of breast cancer and the formation of tumor metastases. The compounds of formula (I) and the salts thereof can be produced by conventional methods.Type: ApplicationFiled: September 18, 2003Publication date: June 10, 2004Inventor: Hugo Ziegler
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Patent number: 6747047Abstract: This invention provides compounds of Formula (1), their N-oxides and agriculturally suitable salts wherein A, B, J, R1, R2, R3 and R4 and n are as defined in the disclosure. Also disclosed are methods for controlling arthropods comprising contacting the arthropods or their environment with an arthropodicidally effective amount of a compound of Formula (1) and compositions containing the compounds of Formula (1).Type: GrantFiled: August 28, 2002Date of Patent: June 8, 2004Assignee: E.I. du Pont de Nemours and CompanyInventors: George P. Lahm, Brian J. Myers, Thomas P. Selby, Thomas M. Stevenson
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Publication number: 20040106802Abstract: The invention discloses a novel series of compound represented by general formula (I), 1Type: ApplicationFiled: November 26, 2003Publication date: June 3, 2004Applicant: TORRENT PHARMACEUTICALS LTD.Inventor: Alangudi Sankaranarayanan
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Publication number: 20040106656Abstract: The present invention is directed to compounds which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.Type: ApplicationFiled: September 24, 2003Publication date: June 3, 2004Inventors: Wallace T Ashton, Charles G Caldwell, Hyun O Ok, Emma R Parmee, Ann E Weber
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Publication number: 20040106655Abstract: The present invention aims at providing compounds having therapeutic effects due to a DPP-IV inhibitory action, and satisfactory as pharmaceutical products.Type: ApplicationFiled: February 10, 2003Publication date: June 3, 2004Inventors: Hiroshi Kitajima, Hiroshi Sakashita, Fumihiko Akahoshi, Yoshiharu Hayashi
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Patent number: 6740647Abstract: Novel five-membered heterocyclic amidines, their preparation and use as competitive inhibitors of trypsin-like serine proteases, especially thrombin and kininogenases such as kallikrein. Pharmaceutical compositions which contain the compounds as active ingredients, and use of the compounds as thrombin inhibitors, anticoagulants and antiinflammatory agents.Type: GrantFiled: June 21, 2000Date of Patent: May 25, 2004Assignee: Abbott GmbH & Co., KGInventors: Dorit Baucke, Udo Lange, Helmut Mack, Werner Seitz, Hans Wolfgang Höffken, Wilfried Hornberger
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Publication number: 20040097732Abstract: PDF inhibitors and novel methods for their use are provided.Type: ApplicationFiled: August 28, 2003Publication date: May 20, 2004Inventors: Kelly M Aubart, Jia-Ning Xiang, Siegfried B Christensen, XIangmin Liao, Maxwell D Cummings
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Publication number: 20040092559Abstract: The invention provides compounds of the formula I 1Type: ApplicationFiled: October 14, 2003Publication date: May 13, 2004Inventors: Lawrence Hamann, David Augeri
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Publication number: 20040082628Abstract: The present invention relates to acylated arylcycloalkylamines, to pharmaceutical compositions comprising such compounds, to methods for the stimulation of the expression of endothelial NO synthase, and methods of treatment comprising administering such compounds.Type: ApplicationFiled: August 7, 2003Publication date: April 29, 2004Applicant: AVENTIS PHARMA DEUTSCHLAND GMBHInventors: Hartmut Strobel, Paulus Wohlfart, Peter Below
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Patent number: 6716843Abstract: Compound of formula (I): wherein: represents an optionally substituted, 5-membered, nitrogen-containing heterocycle, R1 represents hydrogen, alkyl, acyl, prolyl, alanyl, histidylprolyl or phenylalanylprolyl, Ak represents an alkylene or heteroalkylene chain, X represents a single bond or optionally substituted phenylene, R2 represents optionally substituted alkyl, (C3-C10)cycloalkyl, or —NR2aR2b wherein R2a and R2b, which may be the same or different, each represent hydrogen or alkyl or, together with the nitrogen atom carrying them, form a nitrogen-containing heterocycle, Y represents R3 represents hydrogen or a group selected from alkyl, (C3-C7) cycloalkyl and aryl, R4, R5 and R6, which may be the same or different, each represent hydrogen or alkyl, or R4 and R6, or R5 and R6, together with the atoms carrying them, form an imidazolidine or dihydrobenzimidazole ring, its optical isomers and addition salts thereof with a pharmaceuticallyType: GrantFiled: March 28, 2002Date of Patent: April 6, 2004Assignee: Les Laboratoires ServierInventors: Guillaume De Nanteuil, Bernard Portevin, Alain Benoist, Nigel Levens, Olivier Nosjean, Bernadette Husson-Robert
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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: 20040063935Abstract: The present invention is to provide an aliphatic nitrogen-containing 5-membered ring compound represented by the formula [I]: 1Type: ApplicationFiled: April 4, 2003Publication date: April 1, 2004Inventors: Kosuke Yasuda, Hiroshi Morimoto, Saburo Kawanami, Masataka Hikota, Takeshi Matsumoto, Kenji Arakawa
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Publication number: 20040059110Abstract: The present invention provides cystine derivatives, which may be in a free form, a salt form, a solvate form. The cystine derivatives of the present invention may be used to suppress activation of inflammatory factors. Accordingly, the present invention provides: compositions containing the cystine derivatives; a method for suppressing the activation of inflammatory factors by administering the composition; a method for preventing, ameliorating and/or therapeutically treating diseases, skin injuries or disorders involved in the activation of inflammatory factors by administering the composition; a method for preventing, delaying, ameliorating and/or therapeutically treating skin change via aging or aesthetically unfavorable skin change as induced or promoted by inflammatory factors by administering the composition; and pharmaceutical agents containing the cystine derivatives.Type: ApplicationFiled: August 4, 2003Publication date: March 25, 2004Applicant: AJINOMOTO CO., INC.Inventors: Takashi Nakano, Manabu Kitazawa, Keiji Iwasaki, Kazutami Sakamoto
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Patent number: 6710056Abstract: An amidinophenylpyruvic acid derivative of the following formula, analogs thereof and pharmaceutically acceptable salts thereof have an excellent antagonistic effect against activated blood coagulation factor VII.Type: GrantFiled: June 5, 2002Date of Patent: March 23, 2004Assignee: Ajinomoto Co., Inc.Inventors: Masayuki Sugiki, Kazuyuki Sagi, Kohichi Fujita, Takashi Kayahara, Shunji Takehana, Kuniya Sakurai, Kazumi Tashiro
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Patent number: 6706742Abstract: Compound selected from those of formula (I): wherein: represents an optionally substituted 5-membered nitrogen-containing heterocycle, Ak represents an alkylene chain, X represents a single bond or phenylene, R1 and R2, which may be identical or different, each represent hydrogen or alkyl, R3 represents alkyl, nitro or cyano, Y represents NR4 or CHNO2, R4 represents hydrogen or alkyl, its tautomers when they exist, its optical isomers, and addition salts thereof with a pharmaceutically acceptable acid, with the exclusion of compounds wherein, simultaneously, represents an unsubstituted 5-membered nitrogen-containing heterocycle, Ak represents —(CH2)3—, X represents a single bond, Y represents NH and R3 represents nitro. Medicinal products containing the same which are useful as dipeptidyl peptidase IV inhibitors.Type: GrantFiled: May 15, 2002Date of Patent: March 16, 2004Assignee: Les Laboratories ServierInventors: Guillaume De Nanteuil, Bernard Portevin, Alain Benoist, Nigel Levens, Olivier Nosjean, Bernadette Husson-Robert, Michelle Boulanger
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Publication number: 20040049035Abstract: Novel pyrrole derivatives of formula (I) wherein X is oxygen or sulfur; R1 is C1-C4alkyl unsubstituted or substituted, with the exception of CF3; C3-C6cycloalkyl unsubstituted or substituted; or halogen; R2 is hydrogen, C1-C4alkyl unsubstituted or substituted, C1-C4alkoxy unsubstituted or substituted, cyano or halogen; R3 is C1-C4alkyl unsubstituted or substituted; and A is orthosubstituted aryl; orthosubstituted heteroaryl; bicycloaryl unsubstituted or substituted; or bicycloheteroaryl unsubstituted or substituted. The novel compounds have plant-protective properties and are suitable for protecting plants against infestations by phytopathogenic microorganisms.Type: ApplicationFiled: October 8, 2002Publication date: March 11, 2004Inventors: Harald Walter, Hermann Schneider
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Patent number: 6685617Abstract: The present invention relates to compound of formula (I), that are potent inhibitors of &agr;4&bgr;1 mediated adhesion to either VCAM or CS-1 and which could be useful for the treatment of inflammatory diseases. Specifically, the molecules of the present invention can be used for treating or preventing &agr;4&bgr;1 adhesion mediated conditions in a mammal such as a human. This method may comprise administering to a mammal or a human patient an effective amount of the compound or composition as explained in the present specification.Type: GrantFiled: March 9, 2001Date of Patent: February 3, 2004Assignees: Pharmacia & Upjohn Company, Tanabe Seiyaku Co., Ltd.Inventors: James Blinn, Robert Chrusciel, Jed Fisher, Steven Tanis, Edward Thomas, Thomas Lobl, Bradley Teegarden
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Patent number: 6680337Abstract: The present invention provides cyclopentane heptanoic acid, 2 heteroaryl alkyl or alkenyl derivatives which may be substituted in the 1-position with hydroxyl, alkyloxy, amino and amido groups, e.g. 1-OH cyclopentane heptanoic acid, 2 heteroarylalkenyl derivatives. In particular, these derivatives are 7-[5-hydroxy-2-(heteroatom-substituted hydroxyhydrocarbyl)-3-hydroxycyclopentyl] heptanoic or heptenoic acids and amine, amide, ether, ester and alchohol derivatives of said acids wherein one or more of said hydroxy groups are replaced with an ether group. These compounds are potent ocular hypotensive and are particularly suited for the management of glaucoma.Type: GrantFiled: March 7, 2003Date of Patent: January 20, 2004Assignee: Allergan, Inc.Inventor: Robert M. Burk
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Patent number: 6667318Abstract: The invention relates to novel compounds having formula (I) wherein Cy, X, Y, L and R1-6 are as defined herein. The compounds bind CD11/CD18 adhesion receptors such as Lymphocyte Function-associated Antigen-1 (LFA-1) and are therefore useful for treating disorders mediated by LFA-1 such as inflammation and autoimmune diseases.Type: GrantFiled: November 26, 2001Date of Patent: December 23, 2003Assignee: Genentech, Inc.Inventors: Daniel J. Burdick, Mark S. Stanley, David Oare, Mark E. Reynolds, Thomas R. Gadek, James C. Marsters
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Publication number: 20030229231Abstract: Non-natural amino acids such as 2-alkylated amino acids allow for the synthesis of a wider variety of peptidal and non-peptidal pharmaceutically active agents. A method of preparing a 2-alkylcysteine involves condensing cysteine with an aryl nitrile to form a 2-arylthiazoline-4-carboxylic acid, followed by alkylating the 2-arylthiazoline-4-carboxylic acid at the 4-position. The present invention also discloses a method of preparing a class of iron chelating agents related to desferrithiocin, all of which contain a thiazoline ring. In this method, an aryl nitrile or imidate is condensed with cysteine or a 2-alkyl cysteine.Type: ApplicationFiled: May 15, 2003Publication date: December 11, 2003Applicant: Genzyme CorporationInventors: Mukund S. Chorghade, Mukund K. Gurjar, Bhanu M. Chanda, Joseph Cherian
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Publication number: 20030225102Abstract: The invention discloses a novel series of compound represented by general formula (I), 1Type: ApplicationFiled: April 8, 2003Publication date: December 4, 2003Applicant: TORRENT PHARMACEUTICALS LTD.Inventor: Alangudi Sankaranarayanan
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Publication number: 20030225255Abstract: Disclosed is a prodrugs of the formula: 1Type: ApplicationFiled: January 18, 2002Publication date: December 4, 2003Inventors: Jeannette C. Roberts, Britta H. Wilmore, Pamela B. Cassidy, Pamela K. Dominick, Megan D. Short
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Publication number: 20030216450Abstract: Compounds according to general formula (1), wherein R1 is H or CN, X1 is S, O, SO2 or CH2, X2 is O, S or CH2, X3 is NR5 or a carbonyl or thiocarbonyl group and R4 is R6R7N, R8(CH2)qOC(═O), R8(CH2)qOC(═S), R6R7NC(═O), R6R7NC(═S); R8(CH2)qC(═O), R8(CH2)qC(═S) or R8(CH2)qSO2, m is 1-3 and n is 0-4 are new. The compounds of the invention are inhibitors of dipeptidyl peptidase IV. Pharmaceutical compositions of the compounds of the invention, or pharmaceutically acceptable salts thereof, are useful in the treatment of,inter alia, type 2 diabetes.Type: ApplicationFiled: January 9, 2003Publication date: November 20, 2003Inventors: David Michael Evans, Gary Robert William Pitt
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Publication number: 20030203951Abstract: The present invention relates to novel compounds that can be used as antiinflammatory, immunomodulatory and antiproliferatory agents. In particular the invention refers to new compounds which inhibit dihydroorotate dehydrogenase (DHODH), a process for their manufacture, pharmaceutical compositions containing them and to their use for the treatment and prevention of diseases, in particular their use in diseases where there is an advantage in inhibiting dihydroorotate dehydrogenase (DHODH).Type: ApplicationFiled: July 9, 2002Publication date: October 30, 2003Applicant: 4SC AGInventors: Johan Leban, Bernd Kramer, Wael Saeb, Gabriel Garcia
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Publication number: 20030204095Abstract: The present invention provides a process for the preparation of 4-methyl-5-formyl-thiazole of the formula (I) 1Type: ApplicationFiled: December 5, 2002Publication date: October 30, 2003Applicant: Orchid Chemicals & Pharmaceuticals LimitedInventors: Pandurang Balwant Deshpande, Parven Kumar Luthra, Rajesh Vyas, Ramakrishna Kamma
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Publication number: 20030195354Abstract: An amide compound given by formula [I]: 1Type: ApplicationFiled: December 12, 2002Publication date: October 16, 2003Inventor: Hiroshi Sakaguchi
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Patent number: 6627624Abstract: Disclosed are compounds of the formula: or the pharmaceutically acceptable non-toxic salts thereof wherein the A, B, C, D, X, R1, R2, R3, R4, R5, and R6, are variables defined herein, which compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAa brain receptors, and are therefore useful in the diagnosis and treatment of anxiety, Down Syndrome, sleep, cognitive and seizure disorders, depression, overdose with benzodiazepine drugs, and enhancement of memory and alertness.Type: GrantFiled: March 31, 2000Date of Patent: September 30, 2003Assignee: Neurogen CorporationInventors: Robert W. DeSimone, Alan Hutchison, Kenneth Shaw, Daniel L. Rosewater
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Publication number: 20030171595Abstract: The invention relates to novel thienylsulphonylamino(thio)carbonyl compounds of the formula (I), 1Type: ApplicationFiled: October 31, 2002Publication date: September 11, 2003Inventors: Klaus-Helmut Muller, Ernst Rudolf F. Gesing, Mark Wilhelm Drewes, Johannes Rudolf Jansen, Rolf Kirsten, Joachim Kluth, Klaus Konig
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Publication number: 20030166944Abstract: Peptide derivatives useful as inhibitors of activity of thyrotropin-releasing hormone-degrading ectoenzyme (TRH-DE) disclosed.Type: ApplicationFiled: August 19, 2002Publication date: September 4, 2003Applicant: The Provost, Fellows and Scholars of the College of th HolyInventor: Julie A. Kelly
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Publication number: 20030162820Abstract: The present invention provides compounds of the formula: 1Type: ApplicationFiled: September 16, 2002Publication date: August 28, 2003Inventors: Hans-Ulrich Demuth, Torsten Hoffmann, Ulrich Heiser
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Patent number: 6610707Abstract: Compounds of the formula: wherein R1, Y, W, A and R2 are as defined above are inhibitors of rotamase enzymes in particular FKBP-12 and FKBP-52. The compounds therefore moderate neuronal regeneration and outgrowth and can be used for treating neurological disorders arising from neurodegenerative diseases and nerve damage.Type: GrantFiled: September 1, 1999Date of Patent: August 26, 2003Assignee: Pfizer Inc.Inventors: David John Bull, Robert John Maguire, Michael John Palmer, Martin James Wythes
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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: 20030153507Abstract: Compounds of the formula: 1Type: ApplicationFiled: June 11, 2002Publication date: August 14, 2003Inventors: Stacie S. Canan-Koch, Therese N. Alexander, Mark Barvian, Gary Bolton, Frederick E. Boyer, Benjamin J. Burke, Tod Holler, Tanya M. Jewell, Vara Prasad Josyula, David J. Kucera, Maria A. Linton, Jeffrey J. Machak, Lennert J. Mitchell, Sean T. Murphy, Siegfried H. Reich, Donald J. Skalitzky, John H. Tatlock, Michael D. Varney, Scott C. Virgil, Stephen E. Webber, Stephen T. Worland, Michael Melnick
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Patent number: 6605608Abstract: The present invention relates to the compounds of the formula (I) and salts thereof (all the symbols are the same meanings as described in the specification). The compounds of the formula (I) possess inhibitory activity of N-type calcium channel, so they are useful as drug for prevention and/or treatment of cerebral infarct, transient ischemic attack, encephalomyelopathy after cardiac operation, spinal angiopathy, hypertension with stress, neurosis, epilepsy, asthma and pollakiuria etc. or agent for the treatment of pain.Type: GrantFiled: December 22, 2000Date of Patent: August 12, 2003Assignee: Ono Pharmaceutical Co., LtdInventors: Takuya Seko, Masashi Kato
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Publication number: 20030144262Abstract: This invention relates to a series of N-heterocyclyl hydrazides of Formula I, 1Type: ApplicationFiled: October 4, 2002Publication date: July 31, 2003Inventors: Zhihua Sui, Mark Macielag, James Lanter
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Patent number: 6593312Abstract: A compound of formula (I): wherein: represents an optionally substituted saturated carbon ring having from 4 to 8 ring members, R1 and R4, which may be identical or different, each represents hydrogen or acyl, R2 and R3, which may be identical or different, each represents hydrogen or alkyl, R5 and R6, which may be identical or different, each represents hydrogen or alkyl, or R5 and R6 together, with the nitrogen atom carrying them, form an optionally substituted nitrogen-containing heterocycle, stereoisomers thereof, and also addition salts thereof with a pharmaceutically acceptable acid. Medicinal products containing the same which are useful for treatment of glucose intolerance or of disorders associated with hyperglycaemia.Type: GrantFiled: June 18, 2002Date of Patent: July 15, 2003Assignee: Les Laboratoires ServierInventors: Michel Wierzbicki, Jean-Marie Fourquez, Nigel Levens, Bernadette Husson-Robert, Olivier Nosjean, Michelle Boulanger
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Patent number: 6592781Abstract: A novel composition of thiazolidines of the following formula and a method to prepare the same are disclosed. The method involves reacting a dihydrothiazole with a mixture comprising formic acid and an aldehyde. These new thiazolidines are useful as corrosion inhibitors.Type: GrantFiled: May 29, 2002Date of Patent: July 15, 2003Assignee: Baker Hughes IncorporatedInventors: Bernardus Antonius Maria Oude Alink, Benjamin T. Outlaw
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Patent number: 6589962Abstract: Certain &agr;-hydroxy-&ggr;-[[(carbocyclic- or heterocyclic-substituted)amino]carbonyl]alkanamide derivatives are described as inhibitors of HIV protease and inhibitors of HIV replication. These compounds are useful in the prevention or treatment of infection by HIV and the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described. These compounds are effective against HIV viral mutants which are resistant to HIV protease inhibitors currently used for treating AIDS and HIV infection.Type: GrantFiled: April 16, 2002Date of Patent: July 8, 2003Assignee: Merck & Co., Inc.Inventors: James R Tata, Zhijian Lu, Subharekha Raghavan, Tracy T. Huening, Thomas A. Rano, Mark G. Charest
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Patent number: 6586602Abstract: Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, wherein the disease may be, for example, 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: GrantFiled: January 14, 2002Date of Patent: July 1, 2003Inventors: Eugene D. Thorsett, Christopher M. Semko, Michael A. Pleiss, Louis John Lombardo, Andrei W. Konradi, Francine S. Grant, Darren B. Dressen, Michael S. Dappen
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Publication number: 20030109705Abstract: Accordingly, the present invention provides a compound of Formula I, or tautomers or isomers thereof, 1Type: ApplicationFiled: February 27, 2002Publication date: June 12, 2003Inventor: Jonas Grina