Additional Chalcogen Attached Directly Or Indirectly To The Diazine Ring By Nonionic Bonding Patents (Class 544/318)
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Publication number: 20080145453Abstract: The invention concerns molecules of formula (I), drugs containing same and their use as anti-cancer agents.Type: ApplicationFiled: March 14, 2006Publication date: June 19, 2008Inventors: Roman Lopez, Bernard Rousseau, Frank Kozielsky, Dimitrios Skoufias, Salvatore De Bonis
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Publication number: 20080139505Abstract: The present invention provides compounds of formula (I): pharmaceutical compositions thereof, and methods of using the same, processes or preparing the same, and intermediates thereof.Type: ApplicationFiled: November 15, 2005Publication date: June 12, 2008Inventors: Thomas Daniel Aicher, Guillermo S. Cortez, Todd Michael Groendyke, Albert Khilevich, James Allen Knobelsdorf, Fredrik Pehr Marmsater, Jeffrey Michael Schkeryantz, Tony Pisal Tang, Nicholas Andrew Magnus
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Publication number: 20080125589Abstract: It was found that a fluoro derivative can be produced by reacting a hydroxy derivative with sulfuryl fluoride (SO2F2) in the presence of an organic base or in the presence of an organic base and “a salt or complex comprising an organic base and hydrogen fluoride”. According to the present production process, it is not necessary to use perfluoroalkanesulfonyl fluoride, which is not preferable in industrial use, and it is possible to advantageously produce optically-active fluoro derivatives, which are important intermediates of medicines, agricultural chemicals and optical materials, specifically 4-fluoroproline derivatives, 2?-deoxy-2?-fluorouridine derivatives, optically-active ?-fluorocarboxylate derivatives, and the like, even in a large scale.Type: ApplicationFiled: March 17, 2006Publication date: May 29, 2008Applicant: CENTRAL GLASS COMPANY, LIMITEDInventors: Akihiro Ishii, Takashi Ootsuka, Manabu Yasumoto, Hideyuki Tsuruta, Kenjin Inomiya, Koji Ueda, Kaori Mogi
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Publication number: 20080119651Abstract: Pyrimidine-5-carboxylates of formula: wherein R is C1-4 alkyl, R1 is C1-4 alkyl, trifluoromethyl, R2 is hydrogen or C1-4 alkyl and X is hydroxy, chlorine or bromine, are prepared from certain 3-oxoalkanoates of formula (II): with urea and orthoesters of formula (III) R2C(OR). The intermediate 2-acyl-3-ureidoacrylate, without being isolated, is reacted to give a 2-hydroxypyrimidine-5-carboxylate[(I), X?OH] or a hydrate thereof, which is optionally converted into the corresponding chloro or bromo compound (I, X?Cl, Br).Type: ApplicationFiled: November 4, 2005Publication date: May 22, 2008Inventors: Laurent Ducry, Bruno Rittiner
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Patent number: 7358239Abstract: The present invention concerns compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, wherein -Z1-Z2- is a bivalent radical; R1, R2 and R3 are each independently selected from hydrogen, C1-6alkyl, hydroxy, halo and the like; or when R1 and R2 are on adjacent carbon atoms, R1 and R2 taken together may form a bivalent radical of formula; Alk is optionally substituted C1-6alkanediyl; the bivalent radical is a substituted piperidinyl, an optionally substituted pyrrolidinyl, homopiperidinyl, piperazinyl or tropyl; R5 is a radical of formula wherein n is 1 or 2; p1 is 0, and p2 is 1 or 2; or p1 is 1 or 2, and p2 is 0; X is oxygen, sulfur or ?NR9; Y is oxygen or sulfur; R7 is hydrogen, C1-6alkyl, C3-6cycloalkyl, phenyl or phenylmethyl; R8 is C1-6alkyl, C3-6cycloalkyl phenyl or phenylmethyl; R9 is cyano, C1-6alkyl, C3-6cyclo-alkyl, C1-6alkyloxycarbonyl or aminocarbonyl; R10 is hydrogen or C1-6alkyl; and Q isType: GrantFiled: March 14, 2005Date of Patent: April 15, 2008Assignee: Janssen Pharmaceutica, N.V.Inventors: Marcel Frans Leopold De Bruyn, Kristof Van Emelen, Piet Tom Bert Paul Wigerinck, Wim Gaston Verschueren
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Publication number: 20080064704Abstract: The invention relates to novel heterocyclic derivatives of the general formula (I), processes for their preparation, and their use in medicaments, especially for the treatment of chronic obstructive pulmonary diseases, acute coronary syndrome, acute myocardial infarction and heart failure development.Type: ApplicationFiled: February 15, 2005Publication date: March 13, 2008Applicant: Bayer HealthCare AGInventors: Heike Gielen-Haertwig, Barbara Albrecht, Jorg Keldenich, Volkhart Li, Josef Pernerstorfer, Karl-Heinz Schlemmer, Leila Telan
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Patent number: 7288544Abstract: Achiral pyrimidine derivatives and pyridine derivatives of the following formulae or analogs thereof have selective N-type calcium channel antagonistic activity and showed analgesic action when they were taken orally.Type: GrantFiled: March 14, 2003Date of Patent: October 30, 2007Assignee: Ajinomoto Co., Inc.Inventors: Seiji Ohno, Kayo Otani, Seiji Niwa, Satoshi Iwayama, Akira Takahara, Hajime Koganei, Yukitsugu Ono, Shinichi Fujita, Tomoko Takeda, Masako Hagihara, Akiko Okajima
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Patent number: 7244692Abstract: The invention relates to novel substituted benzoylcyclohexanediones of formula (I) in which A1 represents a single bond or represents alkanediyl (alkylene) having 1 to 3 carbon atoms, A2 represents alkanediyl (alkylene) having 1 to 3 carbon atoms, and R1, R2, R3, R4 and R5 are each as defined in the disclosure, and to novel intermediates, to processes for their preparation and to their use as herbicides.Type: GrantFiled: September 20, 2004Date of Patent: July 17, 2007Assignee: Bayer AktiengesellschaftInventors: Klaus-Helmut Müller, Hans-Georg Schwarz, Stefan Lehr, Otto Schallner, Dorothee Hoischen, Mark Wilhelm Drewes, Peter Dahmen, Dieter Feucht, Rolf Pontzen
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Patent number: 7238697Abstract: The present invention relates to novel pyridylpyrimidines of the formula in which R1, R2, X, n, Y, Z and R have the meanings given in the disclosure, to a plurality of processes for preparing these compounds, and to their use for controlling pests. This invention further relates to novel intermediates and process for their preparation.Type: GrantFiled: February 11, 2002Date of Patent: July 3, 2007Assignee: Bayer CropScience AGInventors: Thomas Bretschneider, Mazen Es-Sayed, Rüdiger Fischer, Fritz Maurer, Christoph Erdelen, Peter Lösel
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Patent number: 7232905Abstract: The present invention provides a process for the preparation of substituted dihydropyrimidinones using polyaniline salts as reusable catalysts, which comprises reacting an aldehyde, a ?-keto ester and urea/thiourea in the presence of a polyaniline salt catalyst and separating the substituted dihydropyrimidinone obtained.Type: GrantFiled: March 26, 2004Date of Patent: June 19, 2007Assignee: Council of Scientific and Industrial ResearchInventors: Palaniappan Srinivasan, Vaidya J. Rao, Gangadasu Banda
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Patent number: 7192572Abstract: A composition comprising (a) from 0.005% to 0.5% by weight of a cooling compound; (b) from 0.1% to 10% by weight of an emulsifiable substance; (c) from 0.15% to 15% by weight of a surfactant; (d) optionally up to 5% by weight, preferably from 0.05% to 5% by weight of a cosurfactant.Type: GrantFiled: December 18, 2003Date of Patent: March 20, 2007Assignee: Conopco, Inc.Inventors: Ingrid Anne Marie Appelqvist, Mark Emmett Malone, Asish Nandi
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Patent number: 7179812Abstract: The present invention provides compounds of formula (I): their pharmaceutically acceptable salts or esters, enantiomeric forms, diastereoisomers and racemates, the preparation of the above-mentioned compounds, pharmaceutical compositions containing them and their manufacture, as well as the use of the above-mentioned compounds in the control or prevention of illnesses such as cancer.Type: GrantFiled: March 31, 2005Date of Patent: February 20, 2007Assignee: Hoffmann-la Roche Inc.Inventors: Birgit Bossenmaier, Walter-Gunar Friebe, Wolfgang Jenni, Matthias Rueth, Edgar Voss
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Patent number: 7157580Abstract: Aminopyrimidine and aminopyridine (I) compounds, compositions and methods useful in the treatment of inflammatory, metabolic or malignant conditions, are provided hereinType: GrantFiled: October 18, 2004Date of Patent: January 2, 2007Assignee: Roche Palo Alto LLCInventors: Ronald Charles Hawley, Sharada Shenvi Labadie, Eric Brian Sjogren, Francisco Xavier Talamas
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Patent number: 7148349Abstract: Compounds of Formula I, their preparation and synthetic intermediates, and their use in the synthesis of prodrugs: wherein: V and L are trans relative to one another; V is selected from group consisting of carbocyclic aryl, substituted carbocyclic aryl, heteroaryl, and substituted heteroaryl; and L is a leaving group selected from the group consisting of halogen, alkyl sulfonate, aryloxy optionally substituted with 1–2 substituents, N-containing heteroaryl, and N-hydroxy-nitrogen containing heteroaryl; and salts thereof.Type: GrantFiled: October 31, 2003Date of Patent: December 12, 2006Assignee: Metabasis Therapeutics, Inc.Inventors: K. Raja Reddy, William Craigo, Zhili Sun, Serge Boyer, Bheemarao G. Ugarkar
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Patent number: 7119097Abstract: A compound of the formula pharmaceutically acceptable salts and enantiomers thereof and pharmaceutical compositions containing this compound, its pharmaceutically acceptable salts and enantiomers are claimed.Type: GrantFiled: March 16, 2006Date of Patent: October 10, 2006Assignee: Abbott GmbH & Co. KGInventors: Hartmut Riechers, Dagmar Klinge, Wilhelm Amberg, Andreas Kling, Stefan Muller, Ernst Baumann, Joachim Rheinheimer, Uwe Josef Vogelbacher, Wolfgang Wernet, Liliane Unger, Manfred Raschack
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Patent number: 7109148Abstract: A stem/leaf desiccant for crop plants which comprises as an active ingredient, a compound of formula (I): wherein X represent CH or nitrogen; Z represents halogen; A represents oxygen, sulfur, or NH; R1 represents hydroxyl, C1–C7 alkoxy, C3–C7 alkenyloxy, C3–C7 alkynyloxy, C5–C7 cycloalkoxy, {(C1–C7 alkoxy)carbonyl} C1–C3 alkoxy, (C1–C7 alkylamino)oxy, {di(C1–C7 alkyl)amino}oxy, (C3–C7 alkylideneamino)oxy, C1–C7 alkylamino, di(C1–C7 alkyl)amino, C3–C7 alkenylamino, C3–C7 alkynylamino, C5–C7 cycloalkylamino, {(C1–C7 alkoxy)carbonyl} C1–C3 alkylamino, or (C1–C7 alkoxy)amino; R2 is hydrogen or methyl; and R3 is hydrogen, halogen, C1–C3 alkyl, or C1–C3 alkoxy; a method for desiccating a crop plant and a method for harvesting a crop by using the stem/leaf desiccant.Type: GrantFiled: May 31, 2001Date of Patent: September 19, 2006Assignee: Sumitomo Chemical Company, LimitedInventor: Nobuaki Mito
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Patent number: 7109205Abstract: Carboxylic acid derivatives where R–R6, X, Y and Z have the meanings stated in the description, and the preparation thereof, are described. The novel compounds are suitable for controlling diseases.Type: GrantFiled: June 24, 2003Date of Patent: September 19, 2006Assignee: Abbott GmbH & Co. KGInventors: Hartmut Riechers, Dagmar Klinge, Wilhelm Amberg, Andreas Kling, Stefan Müller, Ernst Baumann, Joachim Rheinheimer, Uwe Josef Vogelbacher, Wolfgang Wernet, Liliane Unger, Manfred Raschack
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Patent number: 7109334Abstract: A process for producing predominantly cis nucleosides or nucleoside analogues and derivatives of formula (A): wherein R1 is a pyrimidine base or a pharmaceutically acceptable derivative thereof and Q is oxygen, carbon or sulphur, comprising a coupling step of the pyrimidine base with a molecule of formula (B) described herein in a suitable coupling solvent, in the presence of catalytic amounts of an element or combination of elements of groups IB or IIB of the periodic table, a tertiary amine and a Lewis acid to obtained an intermediate of formula (D) which is deprotected in the subsequent step to generate the product of formula (A).Type: GrantFiled: June 14, 2002Date of Patent: September 19, 2006Assignee: Shire BioChem, Inc.Inventor: Qing Yu
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Patent number: 7105520Abstract: Phenylalanine derivatives of the following formulae and analogues thereof have an antagonistic activity to ?4 integrin.Type: GrantFiled: September 23, 2002Date of Patent: September 12, 2006Assignee: Ajinomoto Co., Inc.Inventors: Nobuyasu Suzuki, Toshihiko Yoshimura, Hiroyuki Izawa, Shingo Makino, Eiji Nakanishi, Masahiro Murata, Takashi Tsuji
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Patent number: 7105527Abstract: The present invention is directed to a method and composition of treating or preventing viral infections, in particular, human immunodeficiency virus (HIV) and hepatitis B virus (HBV) infections, in human patients or other animal hosts, comprising the administration of N4-acyl-2?,3?-dideoxy-5-fluorocytidine or N4-acyl-2?,3?-didehydro-2?,3?-dideoxy-5-fluorocytidine, and pharmaceutically acceptable salts, prodrugs, and other derivatives thereof.Type: GrantFiled: December 13, 2002Date of Patent: September 12, 2006Inventors: Michael J. Otto, Junxing Shi, Kyoichi A. Watanabe
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Patent number: 7026327Abstract: The invention provides the compounds of formula (I) in which: R1 is selected from the group consisting of H, C1-6alkyl, C1-2alkyl substituted by one to five fluorine atoms, C3-6alkenyl, C3-6alkynyl, C3-10cycloalkylC0-6alkyl, C4-12bridged cycloalkyl, A(CR4R5)n and B(CR4R5)n; R2 is C1-2alkyl substituted by one to five fluorine atoms; R3 is selected from the group consisting of C1-6alkyl, NH2 and R7CONH; R4 and R5 are independently selected from H or C1-6alkyl; A is an unsubstituted 5- or 6-membered heteroaryl or an unsubstituted 6-membered aryl, or a 5- or 6-membered heteroaryl or a 6-membered aryl substituted by one or more R6; R6 is selected from the group consisting of halogen, C1-6alkyl, C1-6alkyl substituted by one more fluorine atoms, C1-6alkoxy, C1-6alkoxy substituted by one or more F, NH2SO2 and C1-6alkylSO2; B is selected from the group consisting of where defines the point of attachment of the ring; R7 is selected from the group consisting of H, C1-6alkyl, C1-6alkoxy, C1-6alkylOC1-6alkylType: GrantFiled: May 23, 2002Date of Patent: April 11, 2006Assignee: Glaxo Group LimitedInventors: Alan Naylor, Jeremy John Payne, Neil Anthony Pegg
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Patent number: 7022701Abstract: The present invention provides a compound of formula I and the use thereof for the therapeutic treatment of disorders relating to or affected by the 5-HT6 receptor.Type: GrantFiled: April 20, 2004Date of Patent: April 4, 2006Assignee: WyethInventors: Derek Cecil Cole, Joseph Raymond Stock, William Joseph Lennox, Ping Zhou
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Patent number: 7019002Abstract: The invention provides pyrido[2,3-d]pyrimidin-7(8H)-one telomerase inhibitors of the formula where R1, R2 are as defined herein. The invention also provides methods for preparing the compounds of formula I, methods of using the compounds to treat diseases such as cancer, and pharmaceutical compositions comprising the compounds.Type: GrantFiled: December 4, 2002Date of Patent: March 28, 2006Assignee: Pharmacia & Upjohn, S.p.A.Inventors: Mauro Angiolini, Dario Ballinari, Domenico Fusar Bassini, Luisella Bonomini, Markus Gude, Maria Menichincheri, Jurgen Moll, Jean-Yves Trosset
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Patent number: 6939965Abstract: Processes for the preparation of 1,3-oxathiolane nucleosides are provided that include reacting a 5-O-protected-oxymethyl-1,3-oxathiolane with a silylated nucleoside in the presence of (Cl)3Ti(isopropoxide). Using the processes described herein, the compounds can be provided as isolated enantiomers.Type: GrantFiled: February 11, 2003Date of Patent: September 6, 2005Assignees: Gilead Sciences, Inc., Emory UniversityInventors: George R. Painter, Dennis C. Liotta, Merrick R. Almond, Darryl G. Cleary, José D. Soria, Marcos Sznaidman
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Patent number: 6933301Abstract: A therapeutic composition is provided that comprises a 1-R1-phenyl, 4-R2-phenyl substituted 1,2,3,6-tetrahydropyrimidine-2-one cold receptor agonist in a therapeutically effective amount. The cold receptor agonist may be represented by the general formula 1-[R1-phenyl]-4-[R2-phenyl]-1,2,3,6-tetrahydropyrimidine-2-one wherein: R1 is -hydroxy, -chloro, -fluoro, -alkyl, -acetoxy, -trifluoromethyl; and R2 is -nitro, -chloro, -fluoro, -alkyl, -trifluoromethyl. Therapeutic compositions of the invention when formulated for delivery to the mucous membranes of the nose and throat alleviate the sensations of airway obstruction and provide symptomatic relief of upper airway breathing disorders.Type: GrantFiled: October 8, 2002Date of Patent: August 23, 2005Inventor: Edward T. Wei
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Patent number: 6927193Abstract: Substituted aryl ether derived compounds represented by the general structure (I) are described. X and Y are independent of each other and are represented by hydrogen, halogen, cyano, nitro, (C1-4)alkyl, (C1-4)haloalkyl, or (C1-4)haloalkoxy; Z is oxygen or sulfur; Q is selected form Q1 to Q6; Also described are the processes for the manufacture of these compounds and agriculturally suitable compositions containing these as active ingredients which are useful as herbicides for general or selective pre-emergent or post-emergent control of undesired plant species and defoliants.Type: GrantFiled: March 3, 2003Date of Patent: August 9, 2005Assignee: Ishihara Sangyo Kaisha, Ltd.Inventors: Sandeep Gupta, Masamitsu Tsukamoto, Mark Read
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Patent number: 6924251Abstract: The invention relates to novel substituted benzoylcyclohexanediones of the general formula (I), in which m, n, A, R1, R2, R3, R4 and Z are each as defined in the description, and also to processes for their preparation and to their use as herbicides.Type: GrantFiled: July 13, 1999Date of Patent: August 2, 2005Assignee: Bayer AktiengesellschaftInventors: Hans-Georg Schwarz, Klaus-Helmut Müller, Stefan Lehr, Otto Schallner, Mark Wilhelm Drewes, Dieter Feucht, Rolf Pontzen, Ingo Wetcholowsky, Heinz-Jürgen Wroblowsky
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Patent number: 6921767Abstract: The present invention relates to a class of compounds represented by the Formula I or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising compounds of the Formula I, and methods of selectively inhibiting or antagonizing the ?v?3 and/or ?v?5 integrin.Type: GrantFiled: December 20, 2002Date of Patent: July 26, 2005Assignee: Pharmacia CorporationInventors: Nagarajan R. Srinivasan, Ish Kumar Khanna, Michael Clare, Alan Gasiecki, Thomas Rogers, Barbara Chen, Mark Russell, Hwang-Fun Lu, Yu Yi, Renee M. Huff, Bipinchandra N. Desai, Balekudru Devadas, Mihir D. Parikh, Thomas Penning
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Patent number: 6919347Abstract: Bradykinin B1-receptor antagonists of formula are disclosed. The compounds are useful for treating diseases associated with inappropriate bradykinin receptor activity, such as diabetic vasculopathy, inflammation, pain, hyperalgesia, asthma, rhinitis, septic shock, atherosclerosis and multiple sclerosis. Pyrimidines, triazines, and anilines in which Q is imidazolyl or pyrrolyl are particularly preferred.Type: GrantFiled: January 14, 2002Date of Patent: July 19, 2005Assignee: Pharmacopeia Drug Discovery, Inc.Inventors: Michael H. J. Ohlmeyer, John J. Baldwin, Roland E. Dolle, III, Vidyadhar Paradkar, Jorge Gabriel Quintero, Gonghua Pan
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Patent number: 6919348Abstract: A therapeutic composition is provided that comprises a 1-R1-phenyl, 4-R2-phenyl substituted 1,2,3,6-tetrahydropyrimidine-2-one cold receptor agonist in a therapeutically effective amount and preferably further comprises one or more pharmaceutically active drugs such as an anti-inflammatory glucocorticosteroid, a sympathomimetic amine decongestant, an anti-histamine, a local anesthetic, menthol or a menthol analog, and mixtures thereof. The cold receptor agonist may be represented by the general formula 1-[R1-phenyl]-4-[R2-phenyl]-1,2,3,6-tetrahydropyrimidine-2-one wherein: R1 is -hydroxy, -chloro, -fluoro, -alkyl, -acetoxy, -trifluoromethyl; and R2 is -nitro, -chloro, -fluoro, -alkyl, -trifluoromethyl. Therapeutic compositions of the invention elicit long-lasting cooling or soothing, particularly when formulated for delivery to suppress the sensations of itch and pain, such as for delivery to inflamed skin, to the mucous membranes of the anogenital areas, and to the enteric mucosa.Type: GrantFiled: May 2, 2002Date of Patent: July 19, 2005Inventor: Edward T. Wei
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Patent number: 6855716Abstract: Dihydropyrimidine derivatives of the following formula or analogs thereof have selective N-type calcium channel antagonistic activity, and they are used as therapeutic agents for various diseases participating in the N-type calcium channels.Type: GrantFiled: December 26, 2001Date of Patent: February 15, 2005Assignee: Ajinomoto Co., Inc.Inventors: Seiji Ohno, Akiko Okajima, Seiji Niwa, Morikazu Kito, Akira Takahara, Yukitsugu Ono, Yuki Kajigaya, Tomoko Takeda, Hajime Koganei
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Patent number: 6838415Abstract: The invention relates to novel substituted benzoylisoxazoles of the general formula (I), in which n represents the number 0, 1, 2 or 3, A represents a single bond or represents alkanediyl (alkylene), R1 represents hydrogen or represents in each case optionally substituted alkyl, alkenyl or cycloalkyl, R2 represents hydrogen, cyano, carbamoyl, halogen, or represents in each case optionally substituted alkyl, alkylcarbonyl, alkoxy, alkoxycarbonyl or alkylthio, alkylsulphinyl or alkylsulphonyl, R3 represents hydrogen, nitro, cyano, carboxyl, carbamoyl, thiocarbamoyl, halogen, or represents in each case optionally substituted alkyl, alkoxy, alkylthio, alkylsulphinyl, alkylsulphonyl, alkylamino, dialkylamino or dialkylaminosulphonyl, R4 represents nitro, cyano, carboxyl, carbamoyl, thiocarbamoyl, halogen, or represents in each case optionally substituted alkyl, alkoxy, alkylthio, alkylsulphinyl, alkylsulphonyl, alkylamino, dialkylamino or dialkylaminosulphonyl, and Z represents an optionally substituted 4-Type: GrantFiled: April 20, 2000Date of Patent: January 4, 2005Assignee: Bayer AktiengesellschaftInventors: Klaus-Helmut Müller, Stefan Lehr, Otto Schallner, Hans-Georg Schwarz, Heinz-Jürgen Wroblowsky, Mark Wilhelm Drewes, Dieter Feucht, Rolf Pontzen, Ingo Wetcholowsky
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Patent number: 6835216Abstract: Compounds, preferably 5-pyrimidinol and 3-pyridinol derivatives, that act as effective chain breaking antioxidants of both the lipid and water-soluble variety (analogous to the natural Vitamins E and C), many of which are more reactive toward peroxyl radicals than the most potent form of Vitamin E. These compounds may exhibit many chemopreventive effects associated with conditions in which free radical-mediated cellular damage or disruption is implicated and Vitamins E and C are shown to have protective effects. Additionally, these compounds should be excellent oxidation inhibitors as additives to fuels, lubricants, rubber, polymers, chemicals, solvents and foodstuffs.Type: GrantFiled: June 26, 2001Date of Patent: December 28, 2004Assignee: Vanderbilt UniversityInventors: Derek A. Pratt, Luca Valgimigli, Gino A. DiLabio
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Patent number: 6831081Abstract: The present invention provides a compound of formula as described herein, which are useful as antiviral agents, in particular, as agents against viruses of the herpes family.Type: GrantFiled: August 27, 2003Date of Patent: December 14, 2004Assignee: Pharmacia & UpjohnInventors: Mark E. Schnute, Fred L. Ciske, Michael J. Genin, Joseph Walter Strohbach, Suvit Thaisrivongs
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Patent number: 6818648Abstract: The present invention provides novel compounds, and pharmaceutical compositions thereof, and methods of using same in the treatment of affective disorders, anxiety, depression, post-traumatic stress disorders, eating disorders, supranuclear palsey, irritable bowl syndrome, immune supression, Alzheimer's disease, gastrointestinal diseases, anorexia nervosa, drug and alcohol withdrawal symptoms, drug addiction, inflammatory disorders, or fertility problems. The novel compounds provided by this invention are those of formula: wherein R1, R3, R5, Q, Z, Y, V, X and X′ are as defined herein.Type: GrantFiled: March 17, 2003Date of Patent: November 16, 2004Assignee: Bristol-Myers Squibb PharmaInventors: Robert John Chorvat, Parthasarathi Rajagopalan
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Patent number: 6787539Abstract: The invention relates to compounds of the formula wherein R1 is lower alkyl, lower alkoxy, pyridinyl, pyrimidinyl, phenyl, —S-lower alkyl, —S(O)2-lower alkyl, —N(R)—(CH2)n—N(R)2, —O—(CH2)n—N(R)2, —N(R)2, or a cyclic tertiary amine of the group which may contain one additional heteroatom, selected from N, O or S, and wherein this group may be connected with the pyrimidine ring via the linker —O(CH2)n—; R2 is hydrogen, lower alkyl, lower alkoxy, halogen or trifluoromethyl; R3/R3′ is, independently from each other, hydrogen or lower alkyl; R4 is independently from each other halogen, trifluoromethyl or lower alkoxy; R5 is hydrogen or lower alkyl; R is, independently from each other, hydrogen or lower alkyl; X is —C(O)N(R)— or —N(R)C(O)—; Y is —O—, —S—, —SO2—, - or —N(R)—; n is 1,2,3 or 4; and m is 0,1 or 2; or a pharmaceuticType: GrantFiled: October 15, 2001Date of Patent: September 7, 2004Assignee: Hoffmann-La Roche Inc.Inventor: Heinz Stadler
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Patent number: 6787544Abstract: Nitrogen-containing heterocyclic carboxamide derivatives represented by the following general formula: wherein ring A is a substituted or unsubstituted pyrazine, pyrimidine, pyridazine or triazine ring; R1 is O or OH; R2 is a hydrogen atom, an acyl group or a substituted or unsubstituted carbamoylalkyl or carboxyalkyl group; and the broken line represents a single bond or a double bond; or salts thereof are useful for preventing and treating virus infections and especially influenza virus infections.Type: GrantFiled: February 20, 2001Date of Patent: September 7, 2004Assignee: Toyama Chemical Co., Ltd.Inventors: Yousuke Furuta, Hiroyuki Egawa, Nobuhiko Nomura
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Patent number: 6784171Abstract: The invention concerns a process for the manufacture of tert-butyl (E)-(6-[2-4-(4-fluorophenyl)-6-isopropyl-2-[methyl(methylsulfonyl)amino]pyrimidin-5-yl]vinyl)-(4R, 6S)-2,2-dimethyl(1,3-dioxan-4-yl) acetate, the novel starting material used in said process and the use of the process in the manufacture of a pharmaceutical.Type: GrantFiled: July 2, 2003Date of Patent: August 31, 2004Assignee: AstraZenecaInventors: Nigel P Taylor, Loius J Diorazio, Haruo Koike, Mikio Kabaki
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Patent number: 6780868Abstract: Compounds of formula (I): wherein: V represents a single bond or a linear or branched (C1-C6)alkylene chain, M represents a single bond or a linear or branched (C1-C6)alkylene chain, A and E each represents nitrogen or CH, but at least one of the two groups A or E represents nitrogen, W represents a group of formula (i): X represents carbonyl, G1 represents a linear C3 alkylene chain optionally containing a double bond and/or being optionally substituted by a hydroxyl group, their isomers, their hydrates, their solvates, and additional salts thereof with a pharmaceutically acceptable acid, and medicinal products containing the same which are useful in the treatment of diseases or pathological conditions in which endothelial dysfunction is known.Type: GrantFiled: February 20, 2003Date of Patent: August 24, 2004Assignee: Les Laboratoires ServierInventors: Jean-Louis Peglion, Christophe Poitevin, Jean-Paul Vilaine, Nicole Villeneuve, Marie-Pierre Bourguignon, Catherine Thollon
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Patent number: 6777418Abstract: The current invention provide novel retinoid compounds and methods for their synthesis, methods of treating or preventing emphysema, cancer and dermatological disorders and pharmaceutical compositions suitable for the treatment or prevention of emphysema, cancer and dermatological disorders.Type: GrantFiled: October 1, 2001Date of Patent: August 17, 2004Assignee: Syntex (U.S.A.) LLCInventors: Jean-Marc Lapierre, David Mark Rotstein, Eric Brian Sjogren
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Patent number: 6770642Abstract: The present invention provides a compound of formula I and the use thereof for the therapeutic treatment of disorders relating to or affected by the 5-HT6 receptor.Type: GrantFiled: December 19, 2002Date of Patent: August 3, 2004Assignee: WyethInventors: Derek Cecil Cole, Joseph Raymond Stock, William Joseph Lennox, Ping Zhou
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Publication number: 20040142930Abstract: 1.Type: ApplicationFiled: November 4, 2003Publication date: July 22, 2004Inventors: Koichiro Yamada, Kenji Matsuki, Kenji Omori, Kohei Kikkawa
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Publication number: 20040138242Abstract: This invention is directed to dihydropyrimidines which are selective antagonists for human &agr;1a receptors. This invention is also related to uses of these compounds for relaxing lower urinary tract tissue, treating benign prostatic hyperplasia and for the treatment of any disease where the antagonism of the &agr;1a receptor may be useful. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.Type: ApplicationFiled: November 6, 2003Publication date: July 15, 2004Applicants: Merck and Co., Inc., Synaptic Pharmaceutical CorporationInventors: Donghui Cui, Margaret R. Davis, Michael Dunn, Ben E. Evans, Hanumath P. Kari, Bharat Lagu, Dhanapalan Nagarathnam, Kamlesh P. Vyas, Kanyin Zhang
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Patent number: 6743801Abstract: A therapeutic composition is provided that comprises a 1-R1-phenyl, 4-R2-phenyl substituted 1,2,3,6-tetrahydropyrimidine-2-one sensory nerve receptor agonist in a therapeutically effective amount. The sensory nerve receptor agonist may be represented by the general formula 1-[R1-phenyl]-4-[R2-phenyl]-1,2,3,6-tetrahydropyrimidine-2-one wherein: R1 is -hydroxy, -chloro, -fluoro, -alkyl, -acetoxy, -trifluoromethyl; and R2 is -nitro, -chloro, -fluoro, -alkyl, -trifluoromethyl. Therapeutic compositions of the invention reduce pain, itch, and a sense of discomfort, when formulated for topical delivery to the human lips, mouth, and to the anorectal area.Type: GrantFiled: August 29, 2002Date of Patent: June 1, 2004Inventor: Edward T. Wei
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Patent number: 6710045Abstract: The present invention relates to novel heterocyclic fluoroalkenyl thioethers of the formula (I) in which m represents integers from 3 to 10, n represents 0, 1 or 2 and Het represents the following, in each case optionally substituted, groupings: to processes for their preparation and to their use as pesticides.Type: GrantFiled: May 12, 2003Date of Patent: March 23, 2004Assignee: Bayer CropScience AGInventors: Udo Kraatz, Bernd Gallenkamp, Albrecht Marhold, Peter Wolfrum, Wolfram Andersch, Christoph Erdelen, Andreas Turberg, Olaf Hansen, Achim Harder
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Publication number: 20040023999Abstract: Compounds of Formula (IA) and Formula (IB) 1Type: ApplicationFiled: March 21, 2003Publication date: February 5, 2004Applicant: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Younes Bekkali, Rajashehar Betageri, Mario G. Cardozo, Thomas A. Gilmore, Christian Hanke Justus Joachim Harcken, Thomas M. Kirrane, Daniel Kuzmich, John Robert Proudfoot, Doris Riether, Hidenori Takahashi, David S. Thomson, Ji Wang, Renee Zindell, Hossein Razavi
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Patent number: 6686369Abstract: The present invention relates to carboxylic acid derivatives of the formula where the radicals have the meanings stated in the description, to the preparation of these compounds and to their use as drugs.Type: GrantFiled: October 8, 1998Date of Patent: February 3, 2004Assignee: Abbott GmbH & Co., KGInventors: Dagmar Klinge, Wilhelm Amberg, Ernst Baumann, Andreas Kling, Hartmut Riechers, Liliane Unger, Manfred Raschack, Stefan Hergenröder, Sabine Schult
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Publication number: 20040002476Abstract: The invention is a compound, composition, use for and a method of treating Flaviviridae (Hepacivirus, Flavirius, Pestivirus) infections, including BVDV and HCV, or abnormal cellular proliferation, including malignant tumors, in a host including animals, and especially humans, using a &bgr;-D or &bgr;-L nucleoside of general formula (I)-(XX), or their pharmaceutically acceptable salt or prodrug thereof.Type: ApplicationFiled: February 13, 2003Publication date: January 1, 2004Inventors: Lieven J. Stuyver, Junxing Shi, Kyoichi A. Watanabe
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Patent number: 6653258Abstract: Fungicidal compounds of the formula (I): and stereoisomers thereof, wherein R1 is optionally substituted aryl or optionally substituted heteroaryl; Y is oxygen, sulphur or NR4; R2, R3 and R4, which may be the same or different, are hydrogen, C1-4 alkyl or C2-4 alkenyl; X is halogen, C1-4 alkyl, C2-4 alkenyl, C1-4 alkoxy, nitro or cyano, and n is 0 or an integer of 1 to 4; provided that when Y is oxygen, n is 0 and R1 is unsubstituted phenyl at least one of R2 and R3 is other than hydrogen or methyl.Type: GrantFiled: March 27, 1995Date of Patent: November 25, 2003Assignee: Syngenta LimitedInventors: John M Clough, Christopher R A Godfrey, Paul J de Fraine, Michael G Hutchings, Vivienne M Anthony
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Patent number: RE39265Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.Type: GrantFiled: November 9, 2000Date of Patent: September 5, 2006Assignee: Aventis Pharmaceuticals Inc.Inventors: Joseph T. Strupczewski, Kenneth J. Bordeau, Edward J. Glamkowski, Yulin Chiang, Grover C. Helsley