Phosphorus Attached Directly Or Indirectly To The Diazine Ring By Nonionic Bonding Patents (Class 544/337)
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Publication number: 20020173490Abstract: Novel bisamidate phosphonate prodrugs of FBPase inhibitors of the Formula IA: 1Type: ApplicationFiled: December 22, 2000Publication date: November 21, 2002Applicant: METABASIS THERAPEUTICS, INC.Inventors: Tao Jiang, Srinivas Rao Kasibhatla, K. Raja Reddy
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Publication number: 20020161227Abstract: A substituted aromatic compound substituted with Q is obtained by reacting a phosphazenium compound represented by formula (1) 1Type: ApplicationFiled: December 20, 2001Publication date: October 31, 2002Inventors: Tadahito Nobori, Setsuko Fujiyoshi, Isao Hara, Takaomi Hayashi, Atsushi Shibahara, Katsuhiko Funaki, Kazumi Mizutani, Shinji Kiyono
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Patent number: 6465643Abstract: The present invention relates to compounds of the formula in which one, two or three of the radicals R1, R2, R3 and R4 are where m and n are an integer from 1 to 10, R5, R6, R7 and R8 are, independently of one another, identical or different and are a straight-chain or branched alkyl radical having 1 to 10 carbon atoms, and the remaining radical(s) R1 to R4 are or —NR9R10, where R9 and R10 are identical or different and are a straight-chain or branched alkyl radical having 1 to 10 carbon atoms, and X− is an inorganic or organic anion or an equivalent of a multiply charged inorganic or organic anion. The invention further relates to mixtures of substances comprising compounds of the formula (1), to a process for preparing the compounds of the formula (1) and to the use thereof.Type: GrantFiled: July 17, 2000Date of Patent: October 15, 2002Assignee: Clariant GmbHInventors: Berthold Schiemenz, Thomas Wessel, Ralf Pfirmann
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Patent number: 6455530Abstract: A method of preparation of optically pure isomers of hydroxyitraconazole, in particular the two cis dioxolane diastereomers of the sec-butyl (S,S)-isomer, and to phosphate and sulfate derivatives thereof is disclosed. Pharmaceutical compositions containing these compounds and to their use for the treatment of fungal infection are also disclosed.Type: GrantFiled: September 18, 2000Date of Patent: September 24, 2002Assignee: Sepracor Inc.Inventors: Patrick Koch, John R. McCullough, Chris H. Senanayake, Gerald J. Tanoury, Yaping Hong
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Patent number: 6451824Abstract: Compounds of formula (I) are suitable for the production of pharmaceuticals for the prophylaxis and therapy of disorders in the course of which an increased activity of matrix-degrading metalloproteinases is involved.Type: GrantFiled: May 8, 1998Date of Patent: September 17, 2002Assignee: Aventis Pharma Deutschland GmbHInventors: Werner Thorwart, Wilfried Schwab, Manfred Schudok, Burkhard Haase
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Publication number: 20020128208Abstract: The disclosed invention is a composition agonists and/or antagonists of V2, V1a or both receptors, in a host, including animals, and especially humans, using a small molecule or its pharmaceutically acceptable salt or prodrug.Type: ApplicationFiled: December 17, 2001Publication date: September 12, 2002Inventors: James P. Snyder, Dennis C. Liotta, Hariharan Venkatesan, Minmin Wang, Matthew C. Davis
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Patent number: 6448401Abstract: An improved process is provided for preparing water-soluble prodrugs of triazole antifungal compounds containing a secondary or tertiary hydroxyl group. More particularly, the improved process is directed toward preparation of water-soluble triazole antifungal compounds are provided having the general formula wherein A is the non-hydroxy portion of a triazole antifungal compound of the type containing a secondary or tertiary hydroxyl group and R and R1 are as defined in the specification.Type: GrantFiled: October 16, 2001Date of Patent: September 10, 2002Assignee: Bristol-Myers Squibb CompanyInventors: Chung-Pin Chen, Timothy Paul Connolly, Laxma Reddy Kolla, John D. Matiskella, Richard H. Mueller, Yadagiri Pendri, Dejah T. Petsch
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Publication number: 20020087030Abstract: A process for preparing polymerizable biaryl derivatives comprises reacting an aromatic comprising a 6-membered ring which bears ester or benzylic OH groups in the 1,4 position with a second aromatic in a palladium-catalyzed cross-coupling reaction to give a biaryl and converting the ester or benzylic OH groups into polymerizable groups in one or more steps. The biaryls obtained are suitable for preparing polymers which are used as electroluminescence materials.Type: ApplicationFiled: October 16, 2001Publication date: July 4, 2002Inventors: Hubert Spreitzer, Willi Kreuder, Heinrich Becker, Jochen Krause
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Patent number: 6399782Abstract: Novel benzimidazole compounds of the following structure and their use as fructose-1,6-bisphosphatase inhibitors is describedType: GrantFiled: April 11, 2000Date of Patent: June 4, 2002Assignee: Metabasis Therapeutics, Inc.Inventors: Srinivas Rao Kasibhatla, K. Raja Reddy, Mark D. Erion, Qun Dang, Gerard R. Scarlato, M. Rami Reddy
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Publication number: 20020065415Abstract: Described are neuroprotective agents of Formula I 1Type: ApplicationFiled: October 4, 2001Publication date: May 30, 2002Inventors: Brian Edward Kornberg, Sham Shridhar Nikam, Michael Francis Rafferty
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Patent number: 6395749Abstract: The present invention provides carboxamine compounds, methods and compositions for inhibiting PARP activity.Type: GrantFiled: September 1, 1998Date of Patent: May 28, 2002Assignee: Guilford Pharmaceuticals Inc.Inventors: Jia-He Li, Jie Zhang
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Publication number: 20020040014Abstract: Novel FBPase inhibitors of the formula I 1Type: ApplicationFiled: March 7, 2001Publication date: April 4, 2002Applicant: Metabasis Therapeutics, Inc.Inventors: Brett C. Bookser, Qun Dang, K. Raja Reddy
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Phosphonic and carboxylic acid derivatives as inhibitors of protein tyrosine phosphatase-1B (PTP-1B)
Patent number: 6365592Abstract: The invention encompasses compounds represented by formula I: as well as compositions and methods of treatment. The compounds are inhibitors of the PTP-1B enzyme.Type: GrantFiled: May 12, 2000Date of Patent: April 2, 2002Assignee: Merck Frosst Canada & Co.Inventors: Yves Leblanc, Claude Dufresne, Patrick Roy, Zhaoyin Wang -
Patent number: 6362172Abstract: Water-soluble prodrugs of triazole antifungal compounds having a secondary or tertiary hydroxy group are provided. More particularly, new water-soluble triazole antifungal compounds are provided having the general formula wherein A is the non-hydroxy portion of a triazole antifungal compound of the type containing a secondary or tertiary hydroxyl group and R and R1 are as defined in the specification.Type: GrantFiled: January 10, 2001Date of Patent: March 26, 2002Assignee: Bristol-Myers Squibb CompanyInventors: Yasutsugu Ueda, John D. Matiskella, Jerzy Golik, Thomas W. Hudyma, Chung-Pin Chen
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Publication number: 20020035092Abstract: Propanoic acid derivatives of formula (1) are described:Type: ApplicationFiled: September 18, 2001Publication date: March 21, 2002Applicant: Celltech Therapeutics LimitedInventors: Rikki Peter Alexander, Barry John Langham, James Thomas Reuberson, Emma Louise Trown, Graham John Warrellow
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Patent number: 6340758Abstract: Described are neuroprotective agents of Formula I wherein R is an amino acid or nitrogen heterocyclic ring which is saturated or unsaturated of from 5 to 8 members which may have additional oxygen or sulfur atoms therein. The other provisions or substituents are described in the specification.Type: GrantFiled: November 25, 1998Date of Patent: January 22, 2002Assignee: Warner-Lambert CompanyInventors: Brian Edward Kornberg, Sham Shridhar Nikam, Michael Francis Rafferty
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Patent number: 6333424Abstract: Compounds having utility in achieving the foregoing objects of the invention are prepared by reacting a 2,2-bis-(disubstituted-phosphoryl)-ethylsulfanyl-acetic acid compound with a pharmaceutically active chemical entity effective to treat the underlying disease state or with non-pharmaceutical entities such as pesticides, insecticides, fungicides or poisons for vermin.Type: GrantFiled: April 8, 1999Date of Patent: December 25, 2001Assignee: Eliza Nor Biopharmaceuticals, Inc.Inventors: Pal Herczegh, John F. Hartmann, Arpad Kovacs, Ferenc J. Sztaricskai, Miklos Hornyak
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Publication number: 20010041691Abstract: Water-soluble prodrugs of triazole antifungal compounds having a secondary or tertiary hydroxy group are provided.Type: ApplicationFiled: January 10, 2001Publication date: November 15, 2001Inventors: Yasutsugu Ueda, John D. Matiskella, Jerzy Golik, Thomas W. Hudyma, Chung-Pin Chen
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Publication number: 20010041690Abstract: The present invention relates to a novel process for making geminal bisphosphonates. The process provides for bisphosphorylation using phosphorus trihalide, phosphorous acid as a reactant/solvent, and a base as an acid acceptor/solvent.Type: ApplicationFiled: January 29, 2001Publication date: November 15, 2001Inventors: Frederick Dana Cazer, William Douglas Cramer, Dennis Michael Billings, Gregory Eugene Parry
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Patent number: 6313294Abstract: The present invention provides a process for preparing an amide, which comprises reacting an amine with an ester in a molten form in the absence of a solvent.Type: GrantFiled: July 8, 1998Date of Patent: November 6, 2001Assignee: Development Center for BiotechnologyInventors: Wen-Chih Chou, Chang-Wei Tan, Shyh-Fong Chen, Hao Ku
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Publication number: 20010034345Abstract: The invention relates to a method of treating dyskinesias associated with dopamine agonist therapy in a mammal which comprises administering to said mammal an effective amount of an antagonist of the AMPA receptor. Dopamine agonist therapy, as referred to in the present invention, is generally used in the treatment of a central nervous system disorder such as Parkinson's disease.Type: ApplicationFiled: September 4, 1998Publication date: October 25, 2001Inventors: J.TIMOTHY GREENAMYRE, BERTRAND L. CHENARD, WILLARD M. WELCH, FRANK S. MENNITI
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Patent number: 6291700Abstract: Sterically hindered phosphoramidates such as N,N′-bis[di-(2,6-xylyl)phosphoryl]piperazine are prepared by the reaction of a sterically hindered diaryl chlorophosphate, such as di-(2,6-xylyl) chlorophosphate, with a basic nitrogen compound containing at least two basic N—H groups, preferably a heterocyclic compound such as piperazine, in the presence of an acid acceptor such as triethylamine. The reaction is conducted in methylene chloride or an aromatic hydrocarbon such as toluene as solvent. If an aromatic hydrocarbon is employed, there is also present at least one dipolar aprotic nitrogen compound, such as 4-dimethylaminopyridine, in an amount effective to increase the reaction rate.Type: GrantFiled: March 30, 2000Date of Patent: September 18, 2001Assignee: General Electric CompanyInventors: James Anthony Cella, John Robert Campbell, Paul Edward Howson
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Patent number: 6277988Abstract: Sterically hindered phosphoramidates such as N,N′-bis[di-(2,6-xylenoxy)phosphinyl]piperazine are prepared by the reaction of a sterically hindered diaryl chlorophosphate, such as di-(2,6-xylyl) chlorophosphate, with a basic nitrogen compound containing at least two basic N—H groups, preferably a heterocyclic compound such as piperazine, in a predominantly liquid, solvent-free reaction mixture. The reaction may be conducted in the melt or in the presence of a non-solvent carrier, typically an aliphatic hydrocarbon. An excess of the basic nitrogen compound is employed as an acid acceptor.Type: GrantFiled: February 29, 2000Date of Patent: August 21, 2001Assignee: General Electric CompanyInventors: John Robert Campbell, James Anthony Cella, Gregory Ronald Gillette, John Edward Kochanowski, Matthew Ladd Reitz
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Patent number: 6248816Abstract: The present invention relates to a polymeric composition suitable for use in films, molded articles and fibers, including microdenier fibers. The polymeric composition comprises a thermoplastic resin in an amount from about 50 weight percent to about 99.9 weight percent of the polymeric composition, and a dye composition in an amount from about 0.1 weight percent to about 50 weight percent of the polymeric composition. The dye composition contains an indanthrone compound as a major component.Type: GrantFiled: May 11, 1999Date of Patent: June 19, 2001Assignee: Eastman Chemical CompanyInventors: Max Allen Weaver, Clarence Alvin Coates, Jr., Jean Carroll Fleischer, Brian Edison Maxwell
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Patent number: 6211182Abstract: This invention discloses novel imidazoles substituted with a six or seven membered heterocyclic ring which contains two nitrogen atoms as part of the heterocyclic ring structure. These compounds have excellent histamine-H3 receptor antagonist activity. Also disclosed are methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such imidazoles as well as methods of using them to treat allergy (for example asthma), inflammation, hypertension, raised intraocular pressure (such as glaucoma)—i.e., a method of lowering intraocular pressure, sleeping disorders, states of hyper and hypomotility and acidic secretion of the gastrointestinal tract, hypo and hyperactivity of the central nervous system (for example, agitation and depression) and other CNS disorders (such as Alzheimer's Disease, schizophrenia, and migraine).Type: GrantFiled: March 8, 1999Date of Patent: April 3, 2001Assignee: Schering CorporationInventors: Wayne Vaccaro, John J. Piwinski, Wing C. Tom, Daniel M. Solomon, Robert G. Aslanian
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Patent number: 6191276Abstract: Sterically hindered phosphoramidates such as N,N′-bis[di-(2,6-xylenoxy)phosphoryl]piperazine are prepared by the reaction of a sterically hindered diaryl chlorophosphate, such as di-(2,6-xylyl) chlorophosphate, with a basic nitrogen compound containing at least two basic N-H groups, preferably a heterocyclic compound such as piperazine, in the presence of calcium oxide as an acid acceptor. The reaction is conducted in the presence of at least one dipolar aprotic solvent.Type: GrantFiled: February 23, 2000Date of Patent: February 20, 2001Assignee: General Electric CompanyInventor: James Anthony Cella
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Patent number: 6177528Abstract: Novel aminomethylphosphine ligands have particular substituents on the central carbon atom. Such ligands form coordination complexes that may be catalysts for the polymerization of monomers or other catalytic induced reactions.Type: GrantFiled: December 14, 1999Date of Patent: January 23, 2001Assignee: Symyx Technologies, Inc.Inventors: Anne Marie LaPointe, Anil Guram, Timothy S. Powers, Bernd Jandeleit, Thomas Boussie, Cheryl Lund
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Patent number: 6166018Abstract: A method of preparation of optically pure isomers of hydroxyitraconazole, in particular the two cis dioxolane diastereomers of the sec-butyl (R,S)-isomer, and to phosphate and sulfate derivatives thereof is disclosed. Pharmaceutical compositions containing these compounds and their use for the treatment of fungal infection are also disclosed.Type: GrantFiled: June 14, 1999Date of Patent: December 26, 2000Assignee: Sepracor Inc.Inventors: John R. McCullough, Chris H. Senanayake, Gerald J. Tanoury, Yaping Hong, Patrick Koch
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Patent number: 6143733Abstract: Quinoxalinedione derivatives ##STR1## as well as their production and use in pharmaceutical agents are described.Type: GrantFiled: May 29, 1997Date of Patent: November 7, 2000Assignee: Schering AktiengesellschaftInventors: Andreas Huth, Martin Kruger, Eckhard Ottow, Dieter Seidelmann, Graham H Jones, Herbert Schneider, Lechoslaw Turski
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Patent number: 6136805Abstract: Quinoxalinedione derivatives of formula (I) ##STR1## are described, and their use in pharmaceutical agents.Type: GrantFiled: February 24, 1998Date of Patent: October 24, 2000Assignee: Scnering AktiengesellschaftInventors: Andreas Huth, Martin Kruger, Eckhard Ottow, Dieter Seidelmann, Roland Neuhaus, Herbert Schneider, Lechoslaw Turski
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Patent number: 6130231Abstract: This invention relates to novel fused heterocycles which are useful as antagonists of the .alpha..sub.v .beta..sub.3 and related integrin receptors, to pharmaceutical compositions containing such compounds, processes for preparing such compounds, and to methods of using these compounds, alone or in combination with other therapeutic agents, for the inhibition of cell adhesion, the treatment of angiogenic disorders, inflammation, bone degradation, cancer metastasis, diabetic retinopathy, thrombosis, restenosis, macular degeneration, and other conditions mediated by cell adhesion and/or cell migration and/or angiogenesis.Type: GrantFiled: November 26, 1997Date of Patent: October 10, 2000Assignee: DuPont PharmaceuticalsInventors: John Wityak, Aleksandra Ewa Tobin
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Patent number: 6127371Abstract: Novel indane and indene derivatives are described which are endothelin receptor antagonists.Type: GrantFiled: October 1, 1999Date of Patent: October 3, 2000Assignee: SmithKline Beecham CorporationInventors: John Duncan Elliott, Deborah Lynne Bryan
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Patent number: 6124295Abstract: Novel compounds of the formula: ##STR1## are disclosed. Compounds of Formula 1.0 are represented by the compounds of formulas: ##STR2## wherein R.sup.1, R.sup.3 and R.sup.4 are each independently selected from halo.Also disclosed are methods of inhibiting farnesyl protein transferase and the growth of abnormal cells, such as tumor cells.Type: GrantFiled: April 27, 1999Date of Patent: September 26, 2000Assignee: Schering CorporationInventors: Arthur G. Taveras, Alan K. Mallams, Adriano Afonso, Ronald J. Doll
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Patent number: 6117873Abstract: Compounds of the formula I ##STR1## in which R.sub.1 is hydroxyl or an aliphatic, araliphatic or aromatic radical,X is a divalent aliphatic, cycloaliphatic, cycloaliphatic-aliphatic, araliphatic, heteroarylaliphatic or aromatic radical,R.sub.2 is hydrogen or an aliphatic or araliphatic radical, alk is lower alkylidene andR.sub.3, R.sub.4 and R.sub.5 independently of one another are hydrogen, lower alkyl, halogen, trifluoromethyl, cyano or nitro,and their salts can be used for the treatment of pathological conditions which respond to blockage of excitatory amino acid receptors, and for the production of pharmaceutical preparations.Type: GrantFiled: April 23, 1999Date of Patent: September 12, 2000Assignee: Novartis AGInventors: Pierre Acklin, Hans Allgeier, Yves Auberson, Silvio Ofner, Siem Jacob Veenstra
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Patent number: 6114336Abstract: This invention relates to a cosmetic composition containing at least one NPY-antagonist component mixed with an excipient for cosmetic preparations.Type: GrantFiled: July 20, 1998Date of Patent: September 5, 2000Assignee: SanofiInventors: Elisabeth Blanc-Ferras, Fran.cedilla.oise Bono Colombie, Bernard Breda, Jean Courregelongue, Catherine Ducasse, Remy Mounier, Paul Raymond, Michel Sabadie, Claudine Serradeil-Le-Gal, Vilain Pol, Jean-Marie Pereillo
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Patent number: 6096743Abstract: A 1,2,3,4-tetrahydroquinoxalinedione derivative represented by the following formula (I) or salt thereof, an NMDA-glycine receptor and/or AMPA receptor antagonist or kainic acid neurotoxicity inhibitor containing the derivative or salt. In addition, a pharmaceutical composition comprising said compound and a pharmaceutically acceptable carrier: ##STR1## wherein the substituents are as described in the specification.Type: GrantFiled: March 5, 1997Date of Patent: August 1, 2000Assignee: Yamanouchi Pharmaceuticals Co., Ltd.Inventors: Jun-ichi Shishikura, Hiroshi Inami, Shuichi Sakamoto, Shin-ichi Tsukamoto, Masao Sasamata, Masamichi Okada, Mitsuo Fujii
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Patent number: 6057323Abstract: Compounds having kappa opioid agonist activity, compositions containing them and method of using them as analgesics and anti-pruritic agents are provided.The compound of formula I, having the structure: ##STR1## wherein R.sub.1, R.sub.2 ;X; and ArY, Z and n are as described in the specification.Type: GrantFiled: October 30, 1998Date of Patent: May 2, 2000Assignee: Adolor CorporationInventors: Wei Yuan Zhang, Alan L. Maycock, Michael Anthony Marella, Virendra Kumar, Forrest Gaul, An-Chih Chang, Deqi Guo
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Patent number: 6057304Abstract: The disclosure relates to quinoxaline derivatives of Formula I ##STR1## wherein R.sup.1, R.sup.4, R.sup.5, R.sup.6, R.sup.7 and R.sup.8 are as defined in the disclosure, as well as their production and use in medicinal agents.Type: GrantFiled: June 5, 1995Date of Patent: May 2, 2000Assignee: Schering AktiengesellschaftInventors: Andreas Huth, Ralph Schmiechen, Ilse Beetz, Ingrid Schumann, Lechoslaw Turski, Peter Andreas Loschmann, David Norman Stephens, Dieter Seidelmann, Martin Kruger, Dieter Rahtz, Peter Holscher
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Patent number: 6043245Abstract: A compound of the formula I ##STR1## wherein G is H or PO.sub.3 H.sub.2 or a pharmaceutical acceptable salt thereof, pharmaceutical compositions containing such compounds and method of using such compounds or pharmaceutical compositions containing them to treat or prevent fungal infection are disclosed.Type: GrantFiled: September 25, 1998Date of Patent: March 28, 2000Assignee: Schering CorporationInventors: Frank Bennett, Viyyoor M. Girijavallabhan, Naginbhai M. Patel, Anil K. Saksena, Ashit Ganguly
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Patent number: 6043363Abstract: Novel aminomethylphosphine ligands have particular substituents on the central carbon atom. Such ligands form coordination complexes that may be catalysts for the polymerization of monomers or other catalytic induced reactions.Type: GrantFiled: March 8, 1999Date of Patent: March 28, 2000Assignee: Symyx Technologies, Inc.Inventors: Anne Marie LaPointe, Anil Guram, Timothy S. Powers, Bernd Jandeleit, Thomas Boussie, Cheryl Lund
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Patent number: 6015800Abstract: A novel series of substituted quinoxaline 2-ones useful as neuroprotective agents are taught. Novel intermediates, processes of preparation, and pharmaceutical compositions containing the compounds are also taught. The compounds are glutamate receptor antagonists and are useful in the treatment of stroke, cerebral ischemia, or cerebral infarction resulting from thromboembolic or hemorrhagic stroke, cerebral vasospasms, hypoglycemia, cardiac arrest, status epilepticus, perinatal asphyxia, anoxia, seizure disorders, pain, Alzheimer's, Parkinson's, and Huntington's Diseases.Type: GrantFiled: May 15, 1998Date of Patent: January 18, 2000Assignee: Warner-Lambert CompanyInventor: Sham Shridhar Nikam
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Patent number: 6004964Abstract: Anti-pruritic pharmaceutical formulations containing kappa agonist compounds and methods of prevention or treatment of pruritus in a mammal with the anti-pruritic formulations.Type: GrantFiled: November 2, 1998Date of Patent: December 21, 1999Assignee: Adolor CorporationInventors: John J. Farrar, An-Chih Chang, Virendra Kumar, Wei Yuan Zhang, Alan Cowan
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Patent number: 5985856Abstract: The present invention is drawn to water soluble derivatives aliphatic acid aromatic secondary and tertiary amine containing drugs. The present invention is further drawn to methods of making water soluble derivatives of aliphatic and aromatic secondary and tertiary amine containing drugs.Type: GrantFiled: December 30, 1998Date of Patent: November 16, 1999Assignee: University of KansasInventors: Valentino Stella, Jeffrey P. Krise, Jan J. Zygmunt, Ingrid Gunda Georg
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Patent number: 5985858Abstract: A phosphonic diester derivative represented by the following formula (1): ##STR1## wherein R.sup.1 represents a cycloalkyl group; a phenyl group which may have 1 to 3 substituents selected from the group consisting of a lower alkoxy group, a lower alkyl group, a halogen atom, a halogen-substituted lower alkyl group, a lower alkanoyl group, a nitro group, a benzoyl group, a cyano group, an N-lower alkylcarbamoyl group, an N-phenyl-lower alkylcarbamoyl group, an N-(halogen-substituted phenyl)carbamoyl group and an N,N-di-lower alkylcarbamoyl group; a 1,3,4-thiadiazol-2-yl group having a halogen-substituted lower alkyl group as a substituent; a thiazolyl group; a pyridyl group which may be substituted by a halogen atom; a benzothiazol-2-yl group having 1 to 2 lower alkoxy groups on the phenyl ring; or a 4,5-dihydrothieno[3,2-e]benzothiazol-2-yl group; R.sup.2 represents a hydrogen atom or a phenyl lower alkyl group; R.sup.3 and R.sup.Type: GrantFiled: June 26, 1998Date of Patent: November 16, 1999Assignee: Otsuka Pharmaceutical Factory, Inc.Inventors: Kazuyoshi Miyata, Yasuhiro Sakai, Yasuo Shoji, Yoshihiko Tsuda, Yasuhide Inoue, Keigo Sato, Shinya Miki
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Patent number: 5968937Abstract: Tricyclic diazepines of the formula: ##STR1## wherein A, B, D, E, F, Y and Z are defined in the specification which compounds have vasopressin and oxytocin antagonist activity.Type: GrantFiled: December 8, 1998Date of Patent: October 19, 1999Assignee: American Cyanamid CompanyInventors: Jay Donald Albright, Marvin Fred Reich, Efren Guillermo Delos Santos
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Patent number: 5962437Abstract: A method of treating viral infections, and in particular HIV-1, hepatitis B virus and herpes viruses, is disclosed. The method comprising administering to a subject in need of such treatment an infection-combating amount of a phospholipid or phospholipid derivative.Type: GrantFiled: May 2, 1997Date of Patent: October 5, 1999Assignee: Wake Forest UniversityInventors: Louis S. Kucera, Susan L. Morris-Natschke, Khalid S. Ishaq
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Patent number: 5962686Abstract: N-Benzylazolium derivatives of the general formula (I), ##STR1## wherein Q is the remainder of an azole compound of the formula II ##STR2## possessing antifungal activity; Z is nitrogen or methine;R.sup.1 and R.sup.2 are each independently a hydrogen atom or a group --OY ?in which Y is a group easily hydrolyzable under physiological condition!;R.sup.3 and R.sup.4 are each independently a hydrogen or halogen atom, lower alkyl, lower alkoxy, lower alkylthio, (lower alkylcarbonyl)thiomethyl, carboxy or methoxycarbonyl; andX.sup.- is a pharmaceutically acceptable anion,as well as salts, hydrates or solvates of the compounds of the general formula (I) have antiftngal properties.Type: GrantFiled: January 8, 1999Date of Patent: October 5, 1999Assignee: Hoffmann-La Roche Inc.Inventors: Shigeyasu Ichihara, Chikako Murasaki, Noriko Ohga, Jun Ohwada, Daisuke Sawada, Nobuo Shimma, Michio Shirai, Isao Umeda
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Patent number: 5952502Abstract: A method of preparation of optically pure isomers of hydroxyitraconazole, in particular the two cis dioxolane diastereomers of the sec-butyl (R,S)-isomer, and to phosphate and sulfate derivatives thereof is disclosed. Pharmaceutical compositions containing these compounds and to their use for the treatment of fungal infection are also disclosed.Type: GrantFiled: November 12, 1997Date of Patent: September 14, 1999Assignee: Sepracor Inc.Inventors: John R. McCullough, Chris H. Senanayake, Gerald J. Tanoury, Yaping Hong, Patrick Koch
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Patent number: 5919965Abstract: A phosphorus ester oligomer having the structure: ##STR1## wherein A can be the same or different in each monomeric unit and each is independently selected from the group consisting of oxygen, sulfur, lower alkyl, alkyl- or aryl-substituted amino and aminoalkyl; B.sub.1 and B.sub.2 can be the same or different and each is independently selected from hydrogen, lower alkyl, a labelling group, a protecting group, a phosphoramidate or a phosphomonoester; R.sub.1 can be the same or different in each monomeric unit, and in at least one of the non-nucleotide monomeric units, R.sub.Type: GrantFiled: January 18, 1995Date of Patent: July 6, 1999Assignee: Genzyme CorporationInventors: Robert Gerard Gentles, Alan F. Cook, Morris Jonathan Rudolph, Reza Fathi
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Patent number: 5914351Abstract: Compounds of the formula ##STR1## wherein Q is a hydrazone derivative;R.sup.1 is hydrogen, halogen, alkyl or alkoxy;R.sup.2 is hydrogen, halogen, alkyl, alkoxy, alkenoxy, alkynyloxy, halomethyl, trifluoromethoxy, alkylthio, nitro or cyano; andR.sup.6 is a substituted carboxamide, carbothioamide, phosphonosoamide, or phosphonothioamide,useful as anti-HIV agents.Type: GrantFiled: December 12, 1997Date of Patent: June 22, 1999Assignees: Uniroyal Chemical Company, Inc., Uniroyal Chemical Co./CIE.Inventors: Walter Gerhard Brouwer, Ewa Maria Osika