Chalcogen Bonded Directly To Ring Carbon Of The Five-membered Hetero Ring (e.g., Adrenochrome, Etc.) Patents (Class 514/421)
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Publication number: 20030069299Abstract: Indolinones of general formula I 1Type: ApplicationFiled: November 1, 2001Publication date: April 10, 2003Inventors: Rainer Walter, Armin Heckel, Gerald Roth, Joerg Kley, Gisela Schnapp, Martin Lenter, Jacobus Van Meel, Walter Spevak, Ulrike Weyer-Czernilofsky
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Publication number: 20030060499Abstract: A therapeutic method for preserving the dopaminergic function of patients suffering from Parkinson's disease, which method comprises administering an effective amount of ropinirole or a pharmaceutically acceptable salt or solvate thereof to a human or animal patient in need thereof. Typically, said patient has had Parkinson's disease for a period of less than three years since diagnosis.Type: ApplicationFiled: July 29, 2002Publication date: March 27, 2003Inventor: Ian Frederic Tulloch
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Patent number: 6528513Abstract: Compounds and compositions are provided which are useful for the treatment of viral infections, particularly human Cytomegalovirus infection. The compounds include novel pyrimidine-based derivatives.Type: GrantFiled: December 15, 2000Date of Patent: March 4, 2003Assignee: Tularik INCInventors: Timothy D. Cushing, Heather L. Mellon, Juan C. Jaen, John A. Flygare, Shi-Chang Miao, Xiaoqi Chen, Jay P. Powers
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Publication number: 20030039704Abstract: The invention provides a method of treating or preventing rosacea, comprising topical administration, of a pharmaceutical preparation comprising a nonsteroidal anti-inflammatory drug (NSAID).Type: ApplicationFiled: March 15, 2002Publication date: February 27, 2003Inventors: Moshe Arkin, Marcel Zighelboim, Ilana Lavon, Amira Zeevi
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Patent number: 6518281Abstract: Novel amides and imides are inhibitors of tumor necrosis factor&agr; and phosphodiesterase and can be used to combat cachexia, endotoxic shock, retrovirus replication, asthma, and inflammatory conditions.Type: GrantFiled: July 20, 2001Date of Patent: February 11, 2003Assignee: Celgene CorporationInventors: George W. Muller, Mary Shire
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Patent number: 6492366Abstract: A compound selected from those of formula (I): wherein: R1 and R2 each independently represent hydrogen or, alkyl, T1 and T2 each independently represent alkylene, G represents a heterocyclic group selected of formula (&agr;): wherein: W1 to W5 and X1 to X4 are so defined in the description. Medicinal products containing the same are useful as serotonin-reuptake inhibitors.Type: GrantFiled: October 11, 2000Date of Patent: December 10, 2002Assignee: Les Laboratoires ServierInventors: Gilbert Lavielle, Olivier Muller, Mark Millan, Didier Cussac, Anne Dekeyne
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Publication number: 20020169198Abstract: This invention relates to methods of co-administering compounds of formula 1 which are agonists of the progesterone receptor which have the general structure: 1Type: ApplicationFiled: April 5, 2002Publication date: November 14, 2002Applicant: WYETHInventors: Andrew Fensome, Puwen Zhang, Marci C. Koko, Lin Zhi, Todd K. Jones, Jay E. Wrobel, Christopher M. Tegley, James P. Edwards, Edward G. Melenski
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Patent number: 6458825Abstract: Compounds related to lactacystin and lactacystin lactone, pharmaceutical compositions containing the compounds, and methods of use.Type: GrantFiled: August 15, 2000Date of Patent: October 1, 2002Assignee: President and Fellows of Harvard CollegeInventors: Gabriel Fenteany, Timothy F. Jamison, Stuart L. Schreiber, Robert F. Standaert
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Patent number: 6451841Abstract: The invention relates to a method of combating insects and parasites, and in particular acarids, the method comprising a step of diffusing a composition that includes permethrin in a solvent. The method is such that a composition is diffused in a chamber to be treated, the composition comprising permethrin and tetramethrin in a solvent, and it is diffused in such a manner that the solvent is entirely in the gaseous state.Type: GrantFiled: January 12, 2001Date of Patent: September 17, 2002Assignee: Produits BergerInventors: Jannick Lehoux, Corinne Gomez
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Patent number: 6441019Abstract: This invention provides compounds of the formula: wherein A and B are independent substituents selected from S, CH or N; provided that when A is S, B is CH or N; and when B is S, A is CH or N; and A and B cannot both be CH; and when A and B both equal N, one N may be optionally substituted with an C1 to C6 alkyl group; R1 and R2 are independent substituents selected from the group of H, C1 to C6 alkyl, substituted C1 to C6 alkyl, C2 to C6 alkenyl, substituted C2 to C6 alkenyl, C2 to C6 alkynyl, substituted C2 to C6 alkynyl, C3 to C8 cycloalkyl, substituted C3 to C8 cycloalkyl, aryl, substituted aryl, heterocyclic, substituted heterocyclic, CORA, or NRBCORA; or R1 and R2 are fused to form optionally substituted 3 to 8 membered spirocyclic alkyl, alkenyl or heterocyclic ring, the heterocyclic ring containing one to three heteroatoms selected from the group of O, S and N; or pharmaceutically useful salts thereof.Type: GrantFiled: July 17, 2001Date of Patent: August 27, 2002Assignees: Wyeth, Ligand Pharmaceuticals, Inc.Inventors: Arthur A. Santilli, Andrew Q. Viet, Puwen Zhang, Andrew Fensome, Jay E. Wrobel, James P. Edwards, Todd K. Jones, Christopher M. Tegley, Lin Zhi
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Publication number: 20020103250Abstract: The present invention provides a method of treating Restless Legs Syndrome in human or animal patient, which method comprises administering to said patient an effective amount of ropinirole or a pharmaceutically acceptable salt or solvate thereof. Preferably, a dose of ropinirole or a pharmaceutically acceptable salt or solvate thereof is administered to the patient 1 to 3 hours before the patient goes to bed. A typical dose comprises 0.1 mg-5 mg of ropinirole. The invention also provides a pharmaceutical composition for use in the treatment of Restless Legs Syndrome which comprises an effective amount of ropinirole or a pharmaceutically acceptable salt or solvate thereof and a pharmaceutically acceptable carrier.Type: ApplicationFiled: March 22, 2002Publication date: August 1, 2002Applicant: SmithKline Beecham CorporationInventor: Kapil Dev Sethi
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Publication number: 20020099075Abstract: The invention provdes methods of reducing tissue damage resulting from ischemia which comprise administering to a mammal in need of such reduction an effective amount of a combination, or a pharmaceutical composition comprising such combination, of an NHE-1 inhibitor and a second compound selected from the group consisting of: (a) a complement modulator, (b) a metabolic modulator, (c) an anti-apoptotic agent, (d) a nitric oxide synthase-related agent, and (e) an enzyme/protein modulator.Type: ApplicationFiled: January 17, 2002Publication date: July 25, 2002Inventors: Wayne R. Tracey, Roger J. Hill
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Publication number: 20020099048Abstract: A bicyclolactam compound of the formula (1) is disclosed, which has an excellent anxiolytic effect, is high in safety, and is useful as an effective component of medicinals which are greatly diminished in side effects such as hypnotic, muscle relaxant and sedative effects 1Type: ApplicationFiled: January 10, 2002Publication date: July 25, 2002Applicant: Taiho Pharmaceutical Company LimitedInventors: Junji Yamamoto, Takashi Arima, Nobuo Kasahara, Masato Nanri, Kazuo Ogawa, Ichiro Yamawaki, Manabu Kaneda
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Publication number: 20020068735Abstract: This invention provides a progesterone receptor antagonist of formula 1 having the structure 1Type: ApplicationFiled: January 9, 2002Publication date: June 6, 2002Applicant: American Home Products CorporationInventors: Mark A. Collins, Valerie A. Mackner, Jay E. Wrobel, Lin Zhi, Todd K. Jones, James P. Edwards, Christopher M. Tegley
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Patent number: 6395764Abstract: This invention involves compounds having the following structure: wherein: a) R1 is hydrogen; or alkyl; bond (a) is a single or a double bond; b) R2 and R3 are each independently selected from hydrogen; unsubstituted C1-C3 alkanyl, alkenyl or alkynyl; cycloalkanyl, cycloalkenyl; unsubstituted C1-C3 alkylthio or alkoxy; hydroxy; thio; nitro; cyano; amino; C1-C3 alkylamino or C1-C3 dialkylamino and halo; c) R4, R5 and R6 are each independently selected from hydrogen; unsubstituted C1-C3 alkanyl, alkenyl or alkynyl; cycloalkanyl, cycloalkenyl; unsubstituted C1-C3 alkylthio or alkoxy; hydroxy; thio; nitro; cyano; amino; C1-C3 alkylamino or C1-C3 dialkylamino; halo; and 2-imidazolinylamino; and wherein one and only one of R4, R5 and R6 is 2-imidazolinylamino; d) R7 is selected from hydrogen; unsubstituted C1-C3 alkanyl, alkenyl or alkynyl; cycloalkanyl, cycloalkenyl; unsubstituted C1-C3 alkylthio or alkoxy; hydroxy; thio; nitro; cyano; amino; C1-C3 alkylamino or C1-C3 dialkylamino and halo;Type: GrantFiled: October 17, 2000Date of Patent: May 28, 2002Assignee: The Procter & Gamble CompanyInventors: Raymond Todd Henry, Russell James Sheldon, William Lee Seibel
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Patent number: 6365608Abstract: Fungicidal mixtures comprise as active components a) an amide compound of the formula I A—CO—NR1R2 I in which A is an aryl group or an aromatic or non-aromatic, 5- or 6-membered heterocycle which has from 1 to 3 hetero atoms selected from O, N and S; where the aryl group or the heterocycle may or may not have 1, 2 or 3 substituents which are selected, independently of one another, from alkyl, halogen, CHF2, CF3, alkoxy, haloalkoxy, alkylthio, alkylsulfynyl and alkylsulfonyl; R1 is a hydrogen atom; R2 is a phenyl or cycloalkyl group which may or may not have 1, 2 or 3 substituents which are selected, independently of one another, from alkyl, alkenyl, alkynyl, alkoxy, alkenyloxy, alkynyloxy, cycloalkyl, cycloalkenyl, cycloalkyloxy, cycloalkenyloxy, phenyl and halogen, where the aliphatic and cycloaliphatic radicals may be partially or fully halogenated and/or the cycloaliphatic radicals may be substituted by from 1 to 3 alkyl groups and where the phenyl group may have from 1Type: GrantFiled: June 19, 2000Date of Patent: April 2, 2002Assignee: BASF AktiengesellschaftInventors: Klaus Schelberger, Maria Scherer, Karl Eicken, Manfred Hampel, Eberhard Ammermann, Gisela Lorenz, Siegfried Strathmann
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Patent number: 6355668Abstract: A bicyclolactam compound of the formula (1) is disclosed, which has an excellent anxiolytic effect, is high in safety, and is useful as an effective component of medicinals which are greatly diminished in side effects such as hypnotic, muscle relaxant and sedative effects A bicyclolactam derivative represented by the following formula (1) is also disclosed, and is useful as an effective component of an anxiolytic agentType: GrantFiled: August 28, 2000Date of Patent: March 12, 2002Assignee: Taiho Pharmaceutical Co., Ltd.Inventors: Junji Yamamoto, Takashi Arima, Nobuo Kasahara, Masato Nanri, Kazuo Ogawa, Ichiro Yamawaki, Manabu Kaneda
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Publication number: 20020019435Abstract: The invention relates to a method of combating insects and parasites, and in particular acarids, the method comprising a step of diffusing a composition that includes permethrin in a solvent. The method is such that a composition is diffused in a chamber to be treated, the composition comprising permethrin and tetramethrin in a solvent, and it is diffused in such a manner that said solvent is entirely in the gaseous state.Type: ApplicationFiled: January 12, 2001Publication date: February 14, 2002Inventors: Jannick Lehoux, Corinne Gomez
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Patent number: 6342610Abstract: Thienyl-, furyl- and pyrrolyl-sulfonamides and methods for modulating or altering the activity of the endothelin family of peptides are provided. In particular, N-(isoxazolyl)thienylsulfonamides, N-(isoxazolyl)furylsulfonamides and N-(isoxazolyl)pyrrolylsulfonamides and methods using these sulfonamides for inhibiting the binding of an endothelin peptide to an endothelin receptor by contacting the receptor with the sulfonamide are provided. Methods for treating endothelin-mediated disorders by administering effective amounts of one or more of these sulfonamides or prodrugs thereof that inhibit or increase the activity of endothelin are also provided.Type: GrantFiled: November 7, 1997Date of Patent: January 29, 2002Assignee: Texas Biotechnology Corp.Inventors: Ming Fai Chan, Chengde Wu, Bore Gowda Raju, Timothy Kogan, Erik Joel Verner, Rosario Silvestre Castillo, Venkatachalapathi Yalamoori, Adam Kois, Vitukudi Narayanaiyengar Balaji
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Patent number: 6288104Abstract: There is disclosed the use of mesembrine and related compounds (e.g. mesembranol, mesembranone) as scrotonin-uptake inhibitors, pharmaceutical compositions comprising such compounds or dry material or an extract of plants from the Mesembryanthemaceae family (e.g. Sceletium (Aizoaceae) tortuosum) containing a standardized content of said compounds, for use in the treatment of depressive states, psychological or psychiatric disorders with an anxiety component, alcohol and drug dependence, bulimia nervosa and obsessive-compulsive disorders. Also disclosed are new derivatives of mesembrine.Type: GrantFiled: March 22, 1999Date of Patent: September 11, 2001Assignee: African Natural Health CCInventors: Nigel Peter Gericke, Ben-Erik Van Wyk
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Publication number: 20010020035Abstract: Disclosed are compounds of the formula 1Type: ApplicationFiled: June 1, 1998Publication date: September 6, 2001Inventors: PAMELA ALBAUGH, GANG LIU, ALAN HUTCHISON
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Patent number: 6277875Abstract: The present invention is directed to metho s for the treatment of human patients afflicted with fibromyalgia using a non-ergot dopamine receptor D2/D3 agonist. In particular, patients are treated with a therapeutically effective amount of tetrahydro-benzthiazole or 3(H)-indolone compounds that are dopamine agonists. More specifically, the compounds 2-amino-6-n-propylamino-4,5,6,7-tetrahydrobenzo-thiazole or 4-[2-(dipropylamino)-ethyl]-1,3-dihydro-2H-indol-2-one are administered to fibromyalgia patients to reduce the musculoskeletal pain symptoms associated with fibromyalgia.Type: GrantFiled: July 17, 2000Date of Patent: August 21, 2001Inventor: Andrew J. Holman
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Patent number: 6271199Abstract: This invention is directed to treating ischemia by administering proteasome inhibitors, ubiquitin pathway inhibitors, agents that interfere with the activation of NF-&kgr;B via the ubiquitin proteasome pathway, or mixtures thereof.Type: GrantFiled: November 24, 1998Date of Patent: August 7, 2001Assignee: Millennium Pharmaceuticals, Inc.Inventors: Stephen J Brand, Alfred L. Goldberg, Louis Plamondon, Francois Soucy, Peter J. Elliott
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Publication number: 20010006964Abstract: New active compound combinations of valinamide derivatives of the formula (I) 1Type: ApplicationFiled: February 5, 2001Publication date: July 5, 2001Inventors: Heinz-Wilhelm Dehne, Wilhelm Brandes, Karl-Heinz Kuck, Thomas Seitz
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Patent number: 6228878Abstract: Disclosed are compounds of formula I: wherein X is selected from oxygen, sulfur and NR; wherein R is selected from hydrogen, loweralkyl and CH2CH2COAr1; and Z is hydrogen; straight or branched chain alkyl having 1-6 carbon atoms; or Z and R1, R2 or R3 together represent CH2; CH2CH2; CH2O; or CH2S forming a five or six membered ring and such ring may be optionally substituted with loweralkyl or phenyl; R24 is hydrogen; loweralkyl, or optionally substituted phenyl; each R10 is selected from hydrogen and loweralkyl; and Ar1 represents an aryl group or optionally substituted phenyl, thienyl or optionally substituted thienyl; or the pharmaceutically acceptable salts thereof, useful for preventing or decreaseing the production of abnormally phosphorylated paired helical filament (PHF) epitopes associated with Alzheimer's Disease and, therefore, useful for treating Alzheimer's Disease.Type: GrantFiled: August 10, 1999Date of Patent: May 8, 2001Assignee: Molecular Geriatrics CorporationInventors: John Francis DeBernardis, Daniel Joseph Kerkman
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Patent number: 6218421Abstract: A method for promoting smoking cessation, which method comprises administrating an effective, non-toxic amount of ropinirole or a pharmaceutically acceptable salt or solvate thereof to a human in need thereof. Said ropinirole is preferably administered orally or transdermally. Also provided is a medicament for use in smoking cessation that comprises ropinirole. Said medicament may be a tablet for oral use or a transdermal patch containing ropinirole.Type: GrantFiled: July 1, 1999Date of Patent: April 17, 2001Assignee: SmithKline Beecham p.l.c.Inventor: Stephen Eldon King
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Patent number: 6218422Abstract: Provided are compositions comprising 1-methyl-2-nitro-3-[(3-tetrahydrofuryl)methyl]guanidine and 3,4,5,6-tetrahydrophthalimidomethyl chrysanthemate, as well as a method of controlling cockroaches.Type: GrantFiled: April 20, 2000Date of Patent: April 17, 2001Assignee: Sumitomo Chemical Company, LimitedInventor: Satoshi Sembo
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Patent number: 6201008Abstract: The present invention provides a pesticidal composition which comprises 4-bromo-2-(4-chlorophenyl)-1-ethoxymethyl-5-trifluromethylpyrrole-3-carbonitrile and at least one pyrethroidal compound as active ingredients, and an inert carrier, and an insecticidal/acaricidal method applying 4-bromo-2-(4-chlorophenyl)-1-ethoxymethyl-5-trifluoromethylpyrrole-3-carbonitrile and at least one pyrethroidal compound to noxious insects, acarina, or the locus where noxious insects or acarina inhabit.Type: GrantFiled: June 29, 1999Date of Patent: March 13, 2001Assignee: Sumitomo Chemical Co. Ltd.Inventors: Yoji Takada, Izumi Fujimoto
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Patent number: 6158438Abstract: A method of chronically instrumenting an animal enabling one to simulate congestive heart failure. This invention also relates to method for assessing the effects of a test compound on cardiac function and systemic vascular dynamics.Type: GrantFiled: February 4, 1999Date of Patent: December 12, 2000Assignee: Merck & Co., Inc.Inventor: You-Tang Shen
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Patent number: 6160003Abstract: 1,3,6-Trihydro-6-Aza-3-Oxapentalen-2-One Derivatives of Formula I are useful for inducing or promoting apoptosis and for arresting uncontrolled neoplastic cell proliferation, and are specifically useful in the arresting and treatment of neoplasia: ##STR1## Wherein R.sub.1 and R.sub.2 are independently selected from the group consisting of hydrogen, lower alkyl, and benzyl,R.sub.3 and R.sub.4 are selected from the group consisting of substituted or unsubstituted phenyl, and the like,R.sub.5 is selected from the group consisting of hydrogen, lower alkyl, and the like,Y is selected from the group consisting of CH.sub.2, C.dbd.O, CH--OH; m is an integer from 0-3; X is selected from the group consisting of CH.sub.2, C.dbd.O, CH--OH, and SO.sub.2 ; and n is an integer from 0-2.Type: GrantFiled: February 26, 1999Date of Patent: December 12, 2000Assignee: Cell Pathways, Inc.Inventors: Gerhard Sperl, Rifat Pamukcu
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Patent number: 6130241Abstract: The invention provides an insect- or acarid-repellent formulation comprising a compound of formula (I), wherein R represents straight or branched chain C.sub.2-10 alkyl, straight or branched chain C.sub.2-10 alkenyl, or straight or branched chain C.sub.2-10 alkynyl, which groups are optionally substituted by one or more groups selected from halogen, C.sub.4-8 cycloalkyl and C.sub.4-8 cycloalkenyl; and a suitable adjuvant, diluent or carrier.Type: GrantFiled: March 10, 1999Date of Patent: October 10, 2000Assignee: Pfizer Inc.Inventor: Darren John Schulz
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Patent number: 6121306Abstract: Racemic (.+-.)-1-azobicyclo[2.2.1]heptan-3-one may be efficiently resolved into its (1S,4R)- and (1R,4S)-1-azabicyclo[2.2.1]heptan-3-one isomers by formation of di-p-toluoyl hemitartrate salts by combination with di-p-toluoyl-L-tartaric acid and di-p-toluoyl-D-tartaric acid, respectively. Selective crystallization using one of the di-p-toluoyltartaric acids in less than stoichiometric amount in a suitable solvent mixture allows isolation of the desired isomer as its respective di-p-toluoyl hemitartrate in high isomeric purity. The isolated hemitartrates are storage stable and may be used as such in the preparation of pharmaceuticals and other biologically active compounds, or may be used to provide the free base of the respective 1-azabicyclo[2.2.1]heptan-3-one isomer.Type: GrantFiled: September 29, 1999Date of Patent: September 19, 2000Assignee: Warner-Lambert CompanyInventor: Denis Martin Sobieray
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Patent number: 6090835Abstract: Fungicidal mixtures, comprisinga.1) a phenyl-benzylether of the formula I.a, I.b or I.c, ##STR1## or a.1) a carbamate of the formula I.d, ##STR2## where X is CH and N, n is 0, 1 or 2 and R is halogen, C.sub.1 -C.sub.4 -alkyl and C.sub.1 -C.sub.4 -haloalkyl, it being possible for the radicals R to be different when n is 2, andb) a dicarboximide-type fungicide (II)in a synergistically active amount.Type: GrantFiled: September 14, 1998Date of Patent: July 18, 2000Assignee: BASF AktiengesellschaftInventors: Klaus Schelberger, Maria Scherer, Hubert Sauter, Manfred Hampel, Joachim Leyendecker, Eberhard Ammermann, Gisela Lorenz, Siegfried Strathmann, Peter Irwin, Randall Evan Gold
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Patent number: 6083515Abstract: Nonsteroidal antiinflammatory drugs which have been substituted with a nitrogen monoxide group; compositions comprising (i) a nonsteroidal antiinflammatory drug, which can optionally be substituted with a nitrogen monoxide group and (ii) a compound that directly donates, transfers or releases a nitrogen monoxide group (preferably as a charged species, particularly nitrosonium); and methods of treatment of inflammation, pain, gastrointestinal lesions and/or fever using the compositions are disclosed. The compounds and compositions protect against the gastrointestinal, renal and other toxicities that are otherwise induced by nonsteroidal antiinflammatory drugs.Type: GrantFiled: January 22, 1999Date of Patent: July 4, 2000Assignee: NitroMed, Inc.Inventors: David S. Garvey, L. Gordon Letts, H. Burt Renfroe, Sang William Tam
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Patent number: 6083970Abstract: Fungicidal mixtures, comprisinga.sub.1) at least one compound from the group selected from oxime ethers of the formula I ##STR1## where the substituents have the following meanings: X is oxygen or amino (NH);Y is CH or N;Z is oxygen, sulfur, amino (NH) or C.sub.1 -C.sub.4 -alkylamino (N--C.sub.1 -C.sub.4 -alkyl);R' is C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -haloalkyl, C.sub.3 -C.sub.6 -alkenyl, C.sub.2 -C.sub.6 -haloalkenyl, C.sub.3 -C.sub.6 -alkynyl, C.sub.3 -C.sub.6 -haloalkynyl, C.sub.3 -C.sub.6 -cycloalkylmethyl, or is benzyl which can be partially or fully halogenated and/or can have attached to it one to three of the following radicals: cyano, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -haloalkyl, C.sub.1 -C.sub.4 -alkoxy, C.sub.1 -C.sub.4 -haloalkoxy and C.sub.1 -C.sub.4 -alkylthio;a.sub.2) carbamates of the formula II ##STR2## where T is CH or N, n is 0, 1 or 2 and R is halogen, C.sub.1 -C.sub.4 -alkyl or C.sub.1 -C.sub.Type: GrantFiled: October 22, 1998Date of Patent: July 4, 2000Assignee: BASF AktiengesellschaftInventors: Ruth Muller, Herbert Bayer, Hubert Sauter, Eberhard Ammermann, Gisela Lorenz, Siegfried Strathmann, Klaus Schelberger, Maria Scherer, Joachim Leyendecker, Bernd Muller
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Patent number: 6075044Abstract: The use of certain heterocyclic derivatives for treating parasitic protozoa infections in mammals, in particular bovine trichomoniasis and giardiasis, is disclosed.Type: GrantFiled: July 17, 1998Date of Patent: June 13, 2000Assignee: The Regents of the University of CaliforniaInventors: Ching C. Wang, John Somoza, Jon P. Page, Ronaldus Marcellus Alphonsus Knegtel, Irwin D. Kuntz, Connie M. Oshiro, A. Geoffrey Skillman
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Patent number: 6042842Abstract: The present invention relates to cosmetic compositions, in particular make-up cosmetic compositions, comprising a novel red pigment with an intense and saturated color which does not generate free radicals. This novel pigment is a diketopyrrolopyrrole (DPP) of formula: ##STR1## in which R.sub.1 and R.sub.2 independently represent a hydrogen atom, a C.sub.1 to C.sub.18 alkyl radical, a C.sub.3 to C.sub.12 alkenyl radical, a C.sub.2 to C.sub.5 alkoxycarbonyl radical or a phenyl radical which is optionally substituted by a halogen and R.sub.3 and R.sub.4 independently represent a hydrogen atom, a C.sub.1 to C.sub.18 alkyl radical, a C.sub.1 to C.sub.4 alkoxy radical, a halo radical or a phenyl radical, or a --SO.sub.3 M group with M being a hydrogen atom, a metal atom or an ammonium group, it being possible for the alkyl, alkenyl and alkoxy radicals to be linear or branched.Type: GrantFiled: March 26, 1999Date of Patent: March 28, 2000Assignee: L'Oreal S.A.Inventors: Patricia Lemann, Jean-Christophe Simon
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Patent number: 6020360Abstract: The invention is drawn to a novel use of a group of known compounds with the formula shown below, ##STR1## wherein R.sub.1, R.sub.2 =hydrogen, substituted or unsubstituted alkyl, cycloalkyl, acyl, aryl, aralkyl, or heterocyclic group; R.sub.3 =hydrogen, alkyl, cycloalkyl, aralkyl, aryl or heterocyclic group, the salts thereof, the compositions thereof and their use as medicaments, particularly in the treatment of human and animal cancers.Type: GrantFiled: September 18, 1996Date of Patent: February 1, 2000Inventors: John M. Webster, Jianxiong Li, Genhui Chen
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Patent number: 5994344Abstract: There are described according to the invention compounds of formula (I) (relative stereochemistry indicated), wherein R.sub.1, R.sub.2, R.sub.3 and X are as defined in the specification, together with processes for preparing them, compositions containing them and their use as pharmaceuticals. Compounds of formula (I) are indicated inter alia for the treatment of chronic bronchitis.Type: GrantFiled: September 25, 1998Date of Patent: November 30, 1999Assignee: Glaxo Wellcome Inc.Inventors: Michael Dennis Dowle, Harry Finch, Lee Andrew Harrison, Graham George Inglis, Martin Redpath Johnson, Simon John Fawcett Macdonald, Pritom Shah, Robin Andrew Smith
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Patent number: 5990105Abstract: The present invention relates to novel compounds of the general formula ##STR1## wherein R.sup.1 is hydrogen;R.sup.2 is hydrogen, trifluoromethyl or lower alkyl;R.sup.3 is hydrogen or amino; orR.sup.1 and R.sup.2 or R.sup.3 and R.sup.2 taken together are --CH.dbd.CH--CH.dbd.CH--;Z is pyrimidin-4-yl, pyridin-4-yl, pyridin-2-yl or phenyl;R.sup.4, R.sup.5 are each independently hydrogen, lower alkyl, trifluoromethyl, halogen, lower alkoxy, nitrilo, amino, lower alkyl-amino, di-lower alkyl-amino, piperazinyl, morpholinyl, pyrrolidinyl, vinyl, C.sub.3 -C.sub.6 cycloalkyl, C.sub.3 -C.sub.6 cycloalkenyl, t-buthylethinyl, hydroxyalkylethinyl, phenylethinyl, naphthyl, thiophenyl, or phenyl, which may be substituted by halogen, lower alkoxy, lower alkyl, trifluoromethyl or nitro, or a group --NH(CH.sub.2).sub.n NR.sup.6 R.sup.7, --N(CH.sub.3)(CH.sub.2).sub.n NR.sup.6 R.sup.7, --NH(CH.sub.2).sub.n -morpholin-4-yl or --NH(CH.sub.2).sub.n OH;n is 2-4R.sup.6 and R.sup.Type: GrantFiled: January 15, 1999Date of Patent: November 23, 1999Assignee: Hoffmann-La Roche Inc.Inventors: Michael Bos, Walter Hunkeler, Claus Riemer
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Fungicidal mixtures of an oxime ether carboxylic acid amide with an N-trichloromethyl thiophtalimide
Patent number: 5965599Abstract: A fungicidal mixture comprisinga) an oxime ether carboxamide of the formula I ##STR1## where R is hydrogen or halogen and b) a phthalimide derivative selected from the group consisting of the compounds II and III ##STR2## in a synergistically active amount.Type: GrantFiled: January 22, 1998Date of Patent: October 12, 1999Assignee: BASF AtiengesellschaftInventors: Barbara Schwalge, Ruth Muller, Herbert Bayer, Hubert Sauter, Eberhard Ammermann, Gisela Lorenz, Siegfried Strathmann -
Patent number: 5962503Abstract: There is provided the use of a cholinesterase inhibitor in the manufacture of a medicament for topical administration for use in the treatment of xerostomiaType: GrantFiled: December 13, 1996Date of Patent: October 5, 1999Assignee: Astra AktiebolagInventors: Jorgen Ekstrom, Herbert Helander
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Patent number: 5927283Abstract: A family of compounds has been found to be useful for right-shifting hemoglobin towards a low oxygen affinity state. The effect has particular application in a wide variety of treatments including hypoxia, hypothermia, ischemia, stroke, ARDS, COPD, surgical blood loss, acute nonvolemic hemodilutions, wounds, diabetic ulcers, chronic leg ulcers, pressure sores, tissue transplants, and sepsis. The compounds are capable of acting on hemoglobin in whole blood.Type: GrantFiled: May 8, 1997Date of Patent: July 27, 1999Assignee: Virginia Commonwealth UniversityInventors: Donald J. Abraham, Michael Gerber
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Patent number: 5922762Abstract: There are described new active compound combinations of a compound of the formula (I) ##STR1## with known fungicidal active compounds, and their use for the control of phytopathogenic fungi.Type: GrantFiled: May 1, 1997Date of Patent: July 13, 1999Assignee: Bayer AktiengesellschaftInventors: Wilhelm Brandes, Heinz-Wilhelm Dehne, Stefan Dutzmann, Karl-Heinz Kuck, Bernd-Wieland Kruger
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Patent number: 5906207Abstract: A method of chronically instrumenting an animal enabling one to simulate congestive heart failure. A method for assessing the effects of a test compound on cardiac function and systemic vascular dynamics.Type: GrantFiled: March 27, 1997Date of Patent: May 25, 1999Assignee: Merck & Co., Inc.Inventor: You-Tang Shen
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Patent number: 5877201Abstract: A fungicidal mixture containinga) the oxime ether carboxylic acid ester of the formula I ##STR1## and b) a phthalimide derivative selected from the group of compounds II and III ##STR2## in a synergistically active amount.Type: GrantFiled: December 16, 1996Date of Patent: March 2, 1999Assignee: BASF AktiengesellschaftInventors: Eberhard Ammermann, Gisela Lorenz, Dietrich Mappes, Klaus Schelberger, Manfred Hampel
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Patent number: 5866582Abstract: Fungicidal combination comprising a compound A which is iprodione, vinclozoline or procymidone, and a compound B which is cyprodinil, also known as 2-phenylamino-4-cyclopropyl-6-methylpyrimidine, fungicidal compositions comprising same, and method of preventing fungal attacks on crops.Type: GrantFiled: February 19, 1997Date of Patent: February 2, 1999Assignee: Rhone-Poulenc AgrochimieInventor: Patrice Duvert
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Patent number: 5843912Abstract: The present invention relates to compositions comprising analogues of purine nucleosides containing a ring-expanded ("fat") heterocyclic ring, in place of purine, and an unmodified or modified sugar residue, pharmaceutically acceptable derivatives of such compositions, as well as methods of use thereof. In particular, these compositions may be utilized in the treatment of certain cancers, bacterial, fungal, parasitic, and viral infections, including, but not limited to, Acquired Immunodeficiency Syndrome (AIDS) and hepatitis.Type: GrantFiled: August 23, 1995Date of Patent: December 1, 1998Assignees: Universy of Maryland, NabiInventors: Ramachandra Hosmane, Barry Burns
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Patent number: 5843981Abstract: A mixture of a pyrethrin, a pyethroid, and one or more synergists is applied to dust mites in a substrate, such as carpeting, in order to kill the dust mites.Type: GrantFiled: November 18, 1996Date of Patent: December 1, 1998Inventor: Jeffery D. Miller
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Patent number: 5827872Abstract: The invention is drawn to novel antibiotics, xenomins of the formula shown below, ##STR1## wherein R.sub.1 =hydrogen; R.sub.2 =an unsubstituted acyl group; R.sub.3 =hydrogen or alkyl, produced by Xenorhabdus species, the salts thereof, the compositions thereof and their use as medicaments and/or agrochemicals, particularly in the treatment of infectious diseases involving microorganisms susceptible to them, including drug-resistant Staphylococcus, and in the treatment of human and animal cancers.Type: GrantFiled: August 23, 1996Date of Patent: October 27, 1998Inventors: John M. Webster, Jianxiong Li, Genhui Chen