Polycyclo Heterocyclic Ring System Containing Ring Oxygen Patents (Class 548/256)
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Patent number: 7666863Abstract: The present invention relates to benzofuran derivatives and analogs, as well as compositions containing the same and to the use thereof for the treatment or prophylaxis of viral infections and diseases associated therewith, particularly those viral infections and associated diseases caused by the hepatitis C virus.Type: GrantFiled: May 24, 2007Date of Patent: February 23, 2010Assignees: ViroPharma Incorporated, WYETHInventors: Ashis K. Saha, Christopher J Burns, Alfred M. Del Vecchio, Thomas R. Bailey, Jason A. Reinhardt, Bheemashankar A. Kulkarni, Thomas H. Faitg, Hao Feng, Susan R. Rippin, Charles W. Blackledge, David J. Rys, Thomas A. Lessen, John Swestock, Yijun Deng, Theodore J. Nitz
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Publication number: 20100029010Abstract: A compound represented by the following formula (I) or (II): wherein, in the formula (I), R1, R2, R3, and R4 independently represent methyl group or ethyl group; and in the formula (II), R5, R6, R7, and R8 independently represent methyl group or ethyl group and X? represents an anion, and a reagent for measurement of nitric oxide which comprises said compound.Type: ApplicationFiled: October 6, 2009Publication date: February 4, 2010Applicants: SEKISUI MEDICAL Co., Ltd.Inventors: Tetsuo Nagano, Hirotatsu Kojima, Kazuya Kikuchi
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Publication number: 20090306153Abstract: In one embodiment of the present disclosure, an inactivator of protein arginine deiminase 4 is disclosed. The inactivator includes: (I) and x includes F; Cl, and H, y includes OH and NH2, R includes H, an alkyl group, an alkenyl group, an alknyl group, and n is greater than 0.Type: ApplicationFiled: November 7, 2006Publication date: December 10, 2009Applicant: University of South CarolinaInventors: Paul Ryan Thompson, Yuan Luo
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Publication number: 20090220662Abstract: The present invention provides isosorbide derivatives having the formula shown below and certain subgenera or species thereof, as flavor or taste modifiers, particularly, savory (“umami”) taste modifiers, savory flavoring agents and savory flavor enhancers in foods, beverages, and other comestible compositions,Type: ApplicationFiled: March 3, 2009Publication date: September 3, 2009Inventors: Catherine TACHDJIAN, Donald S. Karanewsky, Sara L. Adamski-Werner, Jeffrey M. Yamamoto, Guy Servant
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Patent number: 7579355Abstract: The present invention is directed to compounds which contain a substituted pyridine moeity which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for treating cancer comprising administration of the compounds of the invention.Type: GrantFiled: April 20, 2004Date of Patent: August 25, 2009Assignee: Merck & Co., Inc.Inventors: Mark T. Bilodeau, Mark E. Duggan, John C. Hartnett, Craig W. Lindsley, Zhicai Wu, Zhijian Zhao
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Publication number: 20080280875Abstract: The present invention relates to a compound of formula (I): or a pharmaceutically acceptable salt or solvate thereof, wherein: Ring A is (4-12)-membered heterocyclyl; Ring B is a fused benzene ring selected from the group consisting of: Ring A, ring B, ring C, R1, R1a, R2, R3, R4, L2, n, t, w, and z are as defined in the specification. The invention also relates to pharmaceutical compositions comprising the compounds of formula (I) and methods of treating a condition that is mediated by the modulation of glucokinase, the method comprising administering to a mammal an effective amount of a compound of formula (I).Type: ApplicationFiled: May 9, 2007Publication date: November 13, 2008Inventors: Hao Bai, Simon Bailey, Dilip Ramakant Bhumralkar, Feng C. Bi, Fengli Guo, Mingying He, Paul Stuart Humphries, Anthony Lai Ling, Jihong Lou, Seiji Nukul, Ru Zhou
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Patent number: 7414134Abstract: The invention encompasses novel compounds and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and methods for treatment of diseases mediated by B1 bradykinin receptor.Type: GrantFiled: October 11, 2005Date of Patent: August 19, 2008Assignee: Amgen Inc.Inventors: Benny C. Askew, Jr., Jian J. Chen, Derin C. D'Amico, Thomas Nguyen, Kevin Yang
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Publication number: 20080188521Abstract: The instant invention provides compounds of Formula I which are leukotriene biosynthesis inhibitors. Compounds of Formula I are useful as anti-atherosclerotic, anti-asthmatic, anti-allergic, anti-inflammatory and cytoprotective agents.Type: ApplicationFiled: February 1, 2008Publication date: August 7, 2008Inventors: Erich L. Grimm, Yves Ducharme, Richard Frenette, Richard Friesen, Marc Gagnon, Helene Juteau, Sebastien Laliberte, Bruce MacKay, Yves Gareau
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Publication number: 20080157025Abstract: The invention relates to novel benzotriazole UV-absorbers having a long wavelength shifted absorption spectrum with significant absorbance up to 410-420 nm. Further aspects of the invention are a process for their preparation, a UV stabilized composition containing the new UV-absorbers and the use of the new compounds as UV-light stabilizers for organic materials.Type: ApplicationFiled: January 23, 2006Publication date: July 3, 2008Inventors: Katharina Fritzsche, Adalbert Braig, Markus Frey, Walter Fischer
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Publication number: 20080108141Abstract: A compound represented by the following formula (I) or (II): wherein, in the formula (I), R1, R2, R3, and R4 independently represent methyl group or ethyl group; and in the formula (II), R5, R6, R7, and R8 independently represent methyl group or ethyl group and X— represents an anion, and a reagent for measurement of nitric oxide which comprises said compound.Type: ApplicationFiled: June 4, 2007Publication date: May 8, 2008Applicants: DAIICHI PURE CHEMICALS CO., LTD.Inventors: Tetsuo NAGANO, Hirotatsu KOJIMA, Kazuya KIKUCHI
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Patent number: 6962936Abstract: Described herein are compounds that are useful as protein kinase inhibitors having the formula: where Ht, R2, T, and m are as described in the specification. The compounds are useful for treating diseases in mammals that are alleviated by a protein kinase inhibitor, particularly diseases such as cancer, inflammatory disorders, restenosis, and cardiovascular disease.Type: GrantFiled: April 26, 2002Date of Patent: November 8, 2005Assignee: Vertex Pharmaceuticals IncorporatedInventors: Michael R. Hale, Francois Maltais
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Patent number: 6858607Abstract: The present invention is directed to substituted 4H-chromene and analogs thereof, represented by the general Formula I: or pharmaceutically acceptable salts or prodrugs thereof, wherein: wherein A, R1, R2, R5, X, Y, and Z, are defined herein and B is a fused thiazole, oxazole, 2-imino-imidazole, 2,1,3-thiadiazo-2-one, thiazol-2-one, oxazol-2-one, imidazol-2-thione, thiazol-2-thione, oxazol-2-thione, imidazoline, oxazoline, thiazoline, triazole, oxazine, oxazine-2,3-dione, or piperazine ring. The present invention also relates to the discovery that compounds having Formula I are activators of caspases and inducers of apoptosis. Therefore, the activators of caspases and inducers of apoptosis of this invention can be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.Type: GrantFiled: May 16, 2002Date of Patent: February 22, 2005Assignee: Cytovia, Inc.Inventors: Sui Xiong Cai, Lifen Xu, Richard Storer, Giorgio Attardo
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Publication number: 20040235908Abstract: Disclosed are compounds of the formula: 1Type: ApplicationFiled: June 16, 2004Publication date: November 25, 2004Applicant: Schering CorporationInventors: Arthur G. Taveras, Cynthia J. Aki, Richard W. Bond, Jianping Chao, Michael Dwyer, Johan A. Ferreira, Jonathan A. Pachter, John J. Baldwin, Bernd Kaiser, Ge Li, J. Robert Merritt, Kingsley H. Nelson, Laura L. Rokosz
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Publication number: 20040162324Abstract: The thienylazolylalkoxyethanamines (I) where R1 is a hydrogen atom, a halogen atom or a lower alkyl radical; R2, R3 and R4 represent, independently, a hydrogen atom or a lower alkyl radical; and Az represents a five-member nitrogenated hetercyclic aromatic group, N-methyl-substituted, that contains from one to three nitrogen atoms. They have analgesic activity in mammals, including humans. The compounds (I) can be obtained, for example, by reaction of a derivative of hydroxy-thienylazol (IV) with a derivative of a suitable N-(ethyl)amine. The compounds (IV) are useful intermediates in the synthesis of the compounds (I). The compounds (I) have an application in human and/or veterinary medicine.Type: ApplicationFiled: February 13, 2004Publication date: August 19, 2004Applicant: LABORATORIOS DEL DR. ESTEVE, S.A.Inventors: Ramon Merce-Vidal, Blas Andaluz-Mataro, Jordi Frigola-Constansa
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Publication number: 20040157902Abstract: Novel biphenyl derivatives of the general formula (I), in which A, X, R1, R1′, R1″, R2 R2′, R2″ and n are as defined in Patent claim 1, stereoisomers thereof and physiologically acceptable salts or solvates thereof are novel inhibitors of integrin receptors, in particular of the &agr;v&bgr;3, &agr;v&bgr;5 and/or &agr;v&bgr;6 integrin receptors. The novel compounds can be used as medicaments.Type: ApplicationFiled: November 26, 2003Publication date: August 12, 2004Inventors: Wolfgang Sthle, Alfred Jonczyk, Oliver Schadt, Simon Goodman
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Publication number: 20040152750Abstract: Novel compounds that act to antagonize the action of the glucagon peptide hormone on the glucagon receptor. More particularly, it relates to glucagon antagonists or inverse agonists.Type: ApplicationFiled: December 15, 2003Publication date: August 5, 2004Inventors: Janos Tibor Kodra, Carsten Behrens, Peter Madsen, Anker Steen Jorgensen, Inger Thoger Christensen
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Publication number: 20030236252Abstract: Described are bicycle-substituted cyclohexylamines of Formula (I) and their pharmaceutically acceptable salts thereof. The compounds are antagonists of NMDA receptor channel complexes useful for treating cerebral vascular disorders such as, for example, cerebral ischemia, cardiac arrest, stroke, and Parkinson's specification. disease. The substituents are defined in the specification.Type: ApplicationFiled: November 12, 2002Publication date: December 25, 2003Inventors: Sham Shridhar Nikam, Ian Leslie Scott, Brian Alan Sherer, Lawrence David Wise
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Patent number: 6664399Abstract: Disclosed is an invention concerning triazolyloligosaccharides, oligosaccharides wherein the bonding between the saccharide groups is via a triazole group and methods for their preparation.Type: GrantFiled: August 31, 2000Date of Patent: December 16, 2003Assignee: E. I. du Pont de Nemours & CompanyInventor: Subramaniam Sabesan
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Publication number: 20030139450Abstract: The present invention concerns antiviral compounds, their compositions, and use in the treatment of viral infections. More particularly, the invention provides benzimidazole derivatives for the treatment of respiratory syncytial virus infection.Type: ApplicationFiled: November 7, 2002Publication date: July 24, 2003Inventors: Kuo-Long Yu, Rita Lee Civiello, Mark R. Krystal, Kathleen F. Kadow, Nicholas A. Meanwell
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Patent number: 6469051Abstract: A compound represented by the following general formula: wherein R1 and R2 represent amino groups present at adjacent positions each other on the phenyl ring; R3, R4, R5 and R6 independently represent a C1-6 alkyl group; R7, R8, R9 and R10 independently represent a hydrogen atom, a C1-6 alkyl group, an allyl group, or a halogen atom; R11 represents a hydrogen atom or a C1-18 alkyl group; and X− represents an anion, and an agent for nitric oxide measurement comprising said compound. The compound efficiently reacts with nitric oxide to give a fluorescent compound that emits strong fluorescence by irradiation with excitation light of a long wavelength. This fluorescent compound is characterized in that said compound is detectable in a fluorescence wavelength range hardly influenced by autofluorescence of cells, and its fluorescence intensity is not attenuated under an acidic condition.Type: GrantFiled: December 29, 2000Date of Patent: October 22, 2002Inventors: Tetsuo Nagano, Hirotatsu Kojima
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Patent number: 6441197Abstract: A compound represented by the following formula (I): wherein R1 and R2 represent amino group that substitute at adjacent positions on the phenyl ring, provided that either of R1 and R2 represents a mono(C1-6 alkyl)-substituted amino group and the other represents an unsubstituted amino group; and R3 and R4 independently represent hydrogen atom or an acyl group, and an agent for measurement of nitrogen monoxide which comprises said compound.Type: GrantFiled: January 20, 2000Date of Patent: August 27, 2002Assignees: Daiichi Pure Chemicals Co., Ltd.Inventors: Tetsuo Nagano, Hirotatsu Kojima
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Patent number: 6221604Abstract: The invention provides compositions electron-deficient nitrogen heterocycle-substituted fluorescein dyes and methods in which the dyes are conjugated to substrates and used as detection labels in molecular biology experiments. The electron-deficient nitrogen heterocycles include pyridine, quinoline, pyrazine, and the like. Substrates include polynucleotides, nucleosides, nucleotides, peptides, proteins, carbohydrates, and ligands.Type: GrantFiled: February 7, 2000Date of Patent: April 24, 2001Assignee: PE CorporationInventors: Krishna G. Upadhya, Steven M. Menchen, Weiguo Zhen
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Patent number: 6194438Abstract: The present invention relates to compounds of the formula wherein R1, R2, R3 and R4 are as defined herein. The invention also relates to pharmaceutical compositions containing the compounds of Formula I and to methods of inhibiting abnormal cell growth, including cancer, in a mammal by administering the compounds of Formula I to said mammal.Type: GrantFiled: December 2, 1999Date of Patent: February 27, 2001Assignee: Pfizer Inc.Inventors: Bingwei V. Yang, Joseph P. Lyssikatos
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Patent number: 6096897Abstract: Novel pyrroles, pyrazoles and triazoles, pharmaceutical compositions containing these compounds and their use as endothelin receptor antagonists are described.Type: GrantFiled: June 29, 1999Date of Patent: August 1, 2000Assignee: SmithKline Beecham CorporationInventors: Juan Ignacio Luengo, John Duncan Elliott
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Patent number: 6008219Abstract: This invention relates to compounds of formula (I) ##STR1## which are useful as modulators of D.sub.3 receptors, in particular as antipsychotic agents.Type: GrantFiled: October 29, 1997Date of Patent: December 28, 1999Assignee: SmithKline Beech p.l.c.Inventors: Geoffrey Stemp, Christopher Norbert Johnson
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Patent number: 5874590Abstract: A compound useful for the measurement of nitrogen monoxide under a substantially neutral condition which is represented by the following formula (I): ##STR1## wherein R.sup.1 and R.sup.2 represent amino groups that substitute at adjacent positions on the phenyl ring; R.sup.3 and R.sup.4 independently represent a hydrogen atom or an acyl group; R.sup.5, R.sup.6, R.sup.7, and R.sup.8 independently represent a hydrogen atom, a C.sub.1-6 alkyl group, allyl group, or a halogen atom.Type: GrantFiled: October 17, 1997Date of Patent: February 23, 1999Assignee: Tetsuo NaganoInventors: Tetsuo Nagano, Hirotatsu Kojima
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Patent number: 5698575Abstract: A chromone derivative of the formula (I): ##STR1## wherein R.sup.11 is a pyrazolyl, pyrrolyl, triazolyl, benzotriazolyl, benzimidazolyl, indazolyl, or indolyl group, R.sup.2, R.sup.3, R.sup.4, and R.sup.5 is independently a hydrogen or halogen atom, or a hydroxy or alkoxy group, or an alkoxy group substituted with one or more alkoxy groups, and X is an oxygen or sulfur atom, or a salt thereof is disclosed. The chromone derivative inhibits the activity of matrix metalloproteinase.Type: GrantFiled: August 9, 1996Date of Patent: December 16, 1997Assignee: Kureha Chemical Industry Co., Ltd.Inventors: Koju Watanabe, Tsuyoshi Saito, Koichi Niimura
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Patent number: 5696154Abstract: Provided are brefeldin A derivatives of the formula: ##STR1## wherein one of R.sub.1 and R.sub.2 is H and the other of R.sub.1 and R.sub.2 is a substituent group having 1 to 12 carbon atoms containing a basic nitrogen atom or a quaternary ammonium group, or a salt thereof. These derivatives exhibit good antitumor activity, and are administrable to human patients without the problems associated with brefeldin A.Type: GrantFiled: June 29, 1994Date of Patent: December 9, 1997Assignees: The United States of America as represented by the Department of Health and Human Services, Starks Associates, Inc.Inventors: Louis Malspeis, B. Rao Vishnuvajjala, Jeffrey G. Supko, Charles Theodore Kane, Jr.
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Patent number: 5674894Abstract: The current invention discloses novel amidine derivatives with nitric oxide donating property that can inhibit platelet aggregation and promote vasodilation in a single compound.Type: GrantFiled: May 15, 1995Date of Patent: October 7, 1997Assignee: G.D. Searle & Co.Inventors: Mark G. Currie, Foe S. Tjoeng, Mark E. Zupec
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Patent number: 5612370Abstract: Compounds having the formula ##STR1## and pharmaceutically acceptable salts thereof wherein a, b and d are all carbon atoms or one of a, b and d is a nitrogen atom or --N(O)-- and the others are carbon atoms; Y is a single bond, --CH.sub.2 --, --C(O)--, --O--, --S-- or --N(R.sup.8)--; and R.sup.1 to R.sup.7 are as defined herein. These compounds have potassium channel activating activity and are useful, therefore for example, as cardiovascular agents.Type: GrantFiled: June 7, 1995Date of Patent: March 18, 1997Assignee: Bristol-Myers Squibb CompanyInventor: Karnail S. Atwal
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Patent number: 5571925Abstract: This invention provides novel phenyl and heterocyclic derivatives, their pharmaceutical formulations and their use for antagonizing angiotensin II receptors in mammals.Type: GrantFiled: January 19, 1994Date of Patent: November 5, 1996Assignee: Eli Lilly and CompanyInventors: Sherryl L. Lifer, Winston S. Marshall, Fariborz Mohamadi, Jon K. Reel, Richard L. Simon, Mitchell I. Steinberg, Celia A. Whitesitt
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Patent number: 5565482Abstract: A class of benzopyranopyrazolyl derivatives is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula I ##STR1## wherein A is --(CH.sub.2).sub.m --X--(CH.sub.2).sub.n --; wherein X is S(O).sub.p or O; wherein m is 0 or 1; wherein n is 0 or 1; wherein p is 0 or 1; wherein B is selected from phenyl and five and six membered heteroaryl; wherein R.sup.1 is selected from lower haloalkyl, cyano, formyl, lower alkoxycarbonyl, lower alkoxy, lower N-alkylaminocarbonyl, N-phenylaminocarbonyl, lower N,N-dialkylaminocarbonyl and lower N-alkyl-N-phenylaminocarbonyl; wherein R.sup.2 is phenyl substituted at a substitutable position with a radical selected from lower alkylsulfonyl and sulfamyl; and wherein R.sup.Type: GrantFiled: September 29, 1995Date of Patent: October 15, 1996Assignee: G.D. Searle & Co.Inventors: John J. Talley, Stephen R. Bertenshaw, Matthew J. Graneto, Donald J. Rogier
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Patent number: 5538991Abstract: Phenoxyphenylacetic acids and derivatives of the general structural formula I ##STR1## have endothelin antagonist activity and are useful in treating cardiovascular disorders, such as hypertension, postischemic renal failure, vasospasm, cerebral and cardiac ischemia, myocardial infarction, endotoxic shock, benign prostatic hyperplasia, inflammatory diseases including Raynaud's disease and asthma.Type: GrantFiled: September 14, 1994Date of Patent: July 23, 1996Assignee: Merck & Co., Inc.Inventors: Wallace T. Ashton, Linda L. Chang, William J. Greenlee
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Patent number: 5510362Abstract: A class of substituted imidazole, triazole and tetrazole derivatives of formula (I), wherein the broken circle represents two non-adjacent double bonds in any position in the five-membered ring; two, three or four of V,W,X,Y and Z represent nitrogen and the remainder represent carbon provided that, when two of V,W,X,Y and Z represent nitrogen and the remainder represent carbon, then the said nitrogen atoms are in non-adjacent positions within the five-membered ring; E represents a bond or a straight or branched alkylene chain containing from 1 to 4 carbon atoms; F represents a group of formula (lI); U represents nitrogen or C--R.sup.2 ; B represents oxygen, sulphur or N--R.sup.3 ; are selective agonists of 5--HT.sub.1 -like receptors and are therefore useful in the treatment of clinical conditions, in particular migraine and associated disorders, for which a selective agonist of these receptors is indicated.Type: GrantFiled: September 8, 1994Date of Patent: April 23, 1996Assignee: Merck, Sharp and Dohme LimitedInventors: Victor G. Matassa, Austin J. Reeve, Francine Sternfeld, Helen Routledge, Leslie Street
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Patent number: 5498616Abstract: The present invention is directed to irreversible inhibitors of serine and cysteine proteases which most preferably contain a 1-oxytriazole or 1-oxyimidazole functionality. Methods for the use of the protease inhibitors are also described.Type: GrantFiled: November 4, 1994Date of Patent: March 12, 1996Assignee: Cephalon, Inc.Inventors: John P. Mallamo, Ron Bihovsky, Sankar Chatterjee, Rabindranath Tripathy
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Patent number: 5488064Abstract: Compounds of the formula ##STR1## and pharmaceutically acceptable salts thereof where A is phenyl, naphthyl or dihydro- or tetrahydronaphthyl optionally substituted on the aromatic ring by one to three substituents independently selected from halogen, cyano, trifluoromethyl, nitro, alkoxy, alkylsulfonyl, alkyl, cycloalkyl, aryl or a hydrogen bond donor; B is a bond or an oxygen atom and R.sup.1 to R.sup.4 are as defined herein. These compounds are beta 3 adrenergic receptor agonists and are useful, therefore for example, in the treatment of diabetes, obesity and gastrointestinal diseases.Type: GrantFiled: May 2, 1994Date of Patent: January 30, 1996Assignee: Bristol-Myers Squibb CompanyInventor: Philip M. Sher
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Patent number: 5324833Abstract: Compounds of the formula I, ##STR1## in which 'R.sub.1 is an amino protective group, and n stands for 1 or 2, R.sub.1 denotes hydrogen or an amino protective group, R.sub.2 denotes hydrogen or a carboxyl protective group and R.sub.3 denotes triphenylmethyl, 4-monomethoxy-trityl or 4,4'-dimethoxy-trityl, and reactive carboxylic acid derivatives of such compounds of the formula I in which R.sub.2 stands for hydrogen, are described.These compounds can be used as starting materials for the preparation of peptides. They are more suitable for this than are analogous compounds of the formula I in which R.sub.3 denotes hydrogen or one of the carbamoyl protective groups hitherto customary.Type: GrantFiled: April 13, 1990Date of Patent: June 28, 1994Assignee: Novabiochem AGInventors: Peter Sieber, Bernhard Riniker
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Patent number: 5312852Abstract: 2-(2-Hydroxy-3-perfluoroalkylthiomethyl-5-alkylphenyl)-2H-benzotriazoles are prepared by reacting the Mannich base hydrohalide or quaternary salt of a 2-(2-hydroxy-5-alkylphenyl)-2H-benzotriazole with a perfluoroalkyl mercaptan. The products exhibit outstanding efficacy in protecting organic substrates from light induced deterioration as well as good resistance to loss by volatilization or exudation during the processing of stabilized compositions at elevated temperatures.Type: GrantFiled: July 12, 1993Date of Patent: May 17, 1994Assignee: Ciba-Geigy CorporationInventors: Robert A. Falk, Gregory R. Coughlin
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Patent number: 5223616Abstract: A heterocyclic compound which is useful for dyeing or printing hydrophobic fiber materials and which has the following formula (I), ##STR1##wherein A.sub.1, A.sub.2, A.sub.3 and A.sub.4 are each hydrogen, halogen, alkyl, alkoxy or alkenyl, X.sub.1 is --O-- or the like, R.sub.1 is a methylene or the like, X.sub.2 is a direct linkage or a divalent group of --O--, --S--, --SO--, --SO.sub.2 --, ##STR2## in which R.sub.3 is a hydrogen atom or a C.sub.1-4 alkyl group, ##STR3## in which R.sub.3 is as defined above, T and u are each independently hydrogen or a C.sub.1-4 alkyl, l is O or an integer of 1 to 3, Q is an unsubstituted or substituted 5-, 6- or 7-membered saturated or unsaturated heterocyclic residue, Y is hydrogen, C.sub.1-4 alkyl, a C.sub.1-4 alkoxy group or the like.Type: GrantFiled: November 4, 1991Date of Patent: June 29, 1993Assignee: Sumitomo Chemical Company, Ltd.Inventors: Jun Yamamoto, Junichi Sekihachi, Yosuke Yamamoto, Kazuhiro Machiguchi, Yutaka Kayane
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Patent number: 5164509Abstract: Novel potassium channel activators of the formula ##STR1## where Y, X, X.sub.1, X.sub.2 (N or O), and R.sub.1 -R.sub.4 are as defined herein, are disclosed.Type: GrantFiled: November 26, 1990Date of Patent: November 17, 1992Assignee: E. R. Squibb & Sons, Inc.Inventor: Karnail Atwal
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Patent number: 5102707Abstract: Linear and cyclic diorganopolysiloxanes containing benzotriazole functional groups are well suited for the coating of optical fibers and for lubricating plastics, e.g., PVC.Type: GrantFiled: August 4, 1989Date of Patent: April 7, 1992Assignee: Rhone-Poulenc ChimieInventors: Edith Canivenc, Serge Forestier, Michel Gay, Gerard Lang, Herve Richard
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Patent number: 5053071Abstract: This invention pertains to novel heterocyclic 2,3-dihydrobenzofuran and chromane compounds, including stereoisomers, agriculturally suitable compositions containing them, and their use as broad spectrum herbicides.Type: GrantFiled: May 2, 1990Date of Patent: October 1, 1991Assignee: E. I. Du Pont de Nemours and CompanyInventor: Joseph E. Semple
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Patent number: 5034531Abstract: Novel polycyclic pyranyl compounds, pharmaceutical compositions, and their use as anti-viral agents are disclosed.Type: GrantFiled: December 23, 1988Date of Patent: July 23, 1991Assignee: Schering CorporationInventors: Richard J. Friary, John H. Schwerdt, Ashit K. Ganguly
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Patent number: 5001115Abstract: Prodrugs of bio-active hydroxyaromatic drugs having the structural formula:A pharmaceutically acceptable prodrug of a biologically active, therapeutically effective hydroxyaromatic drug, said prodrug being selected from the group consisting of, (A) compounds having the structural formula:DRUG--O--CR'R"--Z].sub.nwherein:DRUG --O-- is the hydroxyaromatic O-dehydro residue of said drug;R' and R' may be the same or different and may be H, alkyl, aryl or electron withdrawing groups;Z is a displaceable leaving group; andn is an integer in the range of from 1 to 3, and (B) pharmaceutically acceptable salts thereof.Type: GrantFiled: May 17, 1989Date of Patent: March 19, 1991Assignee: University of FloridaInventor: Kenneth B. Sloan
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Patent number: 4996316Abstract: A process for the preparation of tertiary N,N-dimethylamines by the reaction of primary amines, formaldehyde, and hydrogen under pressure and at elevated temperature in the presence of a nickel-containing hydrogenation catalyst in the liquid phase. The hydrogenation catalyst is suspended in a solvent, the nickel concentration is 0.1 to 10% by weight, based on the primary amine. The starting materials are separate from each other, brought to 80.degree. to 150.degree. C. and 1 to 15 MPa and fed into the catalyst suspension simultaneously with stirring and reacted in one step to form the tertiary N,N-dimethylamines.Type: GrantFiled: December 24, 1988Date of Patent: February 26, 1991Assignee: Hoechst AktiengesellschaftInventors: Jurgen Weber, Detlef Kampmann, Claus Kniep
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Patent number: 4954518Abstract: This invention relates to a 4H-1-benzopyran-4-one derivative represented by the formula: ##STR1## or a salt thereof, a process for producing the same and a pharmaceutical composition comprising the same as active ingredient.Type: GrantFiled: October 7, 1988Date of Patent: September 4, 1990Assignee: Toyama Chemical Company, Ltd.Inventors: Shuntaro Takano, Chosaku Yoshida, Takihiro Inaba, Keiichi Tanaka, Ryuko Takeno, Hideyoshi Nagaki, Tomoya Shimotori, Shinji Makino
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Patent number: 4914206Abstract: The present invention provides lankacidin derivatives of the formula ##STR1## and procedures for the production thereof. The lankacidin derivatives [1] show excellent antimicrobial activities and thus can be used for prophylaxis and treatment of infectious disease in animals.Type: GrantFiled: December 15, 1988Date of Patent: April 3, 1990Assignee: Takeda Chemical Industries, LTD.Inventors: Isao Minamida, Naoto Hashimoto
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Patent number: 4881967Abstract: This invention pertains to novel heterocyclic 2,3-dihydrobenzofuran and chromane compounds, including stereoisomers, agriculturally suitable composition containing them, and their use as broad spectrum herbicides.Type: GrantFiled: June 2, 1988Date of Patent: November 21, 1989Assignee: E. I. Du Pont De Nemours and CompanyInventor: Joseph E. Semple
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Patent number: RE39663Abstract: The invention provides compositions electron-deficient nitrogen heterocycle-substituted fluorescein dyes and methods in which the dyes are conjugated to substrates and used as detection labels in molecular biology experiments. The electron-deficient nitrogen heterocycles include pyridine, quinoline, pyrazine, and the like. Substrates include polynucleotides, nucleosides, nucleotides, peptides, proteins, carbohydrates, and ligands.Type: GrantFiled: April 6, 2004Date of Patent: May 29, 2007Assignee: Applera CorporationInventors: Krishna G. Upadhva, Steven M. Menchen, Weiguo Zhen
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Patent number: RE35279Abstract: The present invention relates to novel hydantoin derivatives, processes for producing said hydantoin derivatives, pharmaceutical compositions containing at least one of said hydantoin derivatives as aldose reductase inhibitors and novel intermediate compounds in the synthesis of said hydantoin derivatives.The present invention is based on the selection of a hydantoin which is bonded by a sulfonyl group to various substituents at the 1-position of the hydantoin skeleton.The compounds of the present invention have a strong inhibitory activity against aldose reductase. These compounds are extremely useful for the treatment and/or prevention of various forms of diabetic complications based on the accumulation of polyol metabolites.Type: GrantFiled: February 17, 1994Date of Patent: June 18, 1996Assignee: Mochida Pharmaceutical Co., Ltd.Inventors: Ei Mochida, Kimihiro Murakami, Kazuo Kato, Katsuaki Kato, Jun Okuda, Ichitomo Miwa