Chalcogen Attached Indirectly To The Hetero Ring By Nonionic Bonding Patents (Class 549/497)
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Publication number: 20030054246Abstract: An additive compound for oxidizable metal such as zinc is provided.Type: ApplicationFiled: June 17, 2002Publication date: March 20, 2003Inventors: Lin-Feng Li, Dan K. Nguyen
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Publication number: 20030055100Abstract: Compounds are described that bind to tubulin causing tubulin depolymerization and inhibiting tubulin polymerization. The compounds of the invention are therapeutically effective to inhibit cellular proliferation, for example, as effective anti-cancer agents. The compounds can also induce cytotoxicity in cells such as leukemia cells. The chemical structure of the compounds includes a furan, thiophene, thiazole, oxazole, or imidazole group at one end of the molecule (head) and a hydrophobic, aliphatic chain at the other end of the molecule (tail).Type: ApplicationFiled: April 18, 2002Publication date: March 20, 2003Inventors: Fatih M. Uckun, Shyi-Tai M. Jan
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Patent number: 6521765Abstract: Disclosed is a process for the preparation of 3-methyltetrahydrofuran (MeTHF) from 3-(hydroxymethyl)tetrahydrofuran (HOMeTHF) by contacting HOMeTHF with hydrogen in the presence of an acidic, supported catalyst comprising a Group VIII metal.Type: GrantFiled: April 18, 2002Date of Patent: February 18, 2003Assignee: Eastman Chemical CompanyInventors: Alexey Victorovitch Ignatchenko, William Anthony Beavers, Zhufang Liu
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Patent number: 6518440Abstract: A method to produce hydroxymethylfurfural from cellulose contained within lignocellulose solids is disclosed. Hemicellulose contained in lignocellulose solids is converted to furfural. Lignocellulose solids, containing cellulose, is added to a vessel containing an aqueous acidic solution which is employed for hydrolysis of cellulose, contained within lignocellulose solids, to form glucose. Subjecting the glucose to additional hydrolysis to convert glucose and form hydroxymethylfurfural and removing hydroxymethylfurfural from the vessel are procedures applied. Solids remaining from hydrolysis containing lignins are filtered and then extracted with water to remove aqueous acidic solution contained within solids and form an extractate containing dilute aqueous acidic solution. The extactate is combined with a dilute solution of aqueous acidic solution removed from the vessel.Type: GrantFiled: March 5, 2001Date of Patent: February 11, 2003Inventor: Gene E. Lightner
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Publication number: 20020183529Abstract: Tetrahydrofuran compounds of formula (1) wherein the broken line represents a single bond, a divalent organic group, or a structure in which the alicyclic structure in the form of norbornene or tetracyclo[4.4.0.12,5.17,10]dodecene and the tetrahydrofuran cyclic structure share one or two constituent carbon atoms, and k is 0 or 1 are novel and useful as monomers to form base resins for use in chemically amplified resist compositions adapted for micropatterning lithography.Type: ApplicationFiled: April 8, 2002Publication date: December 5, 2002Applicant: Shin-Etsu Chemical Co., Ltd.Inventors: Takeshi Kinsho, Koji Hasegawa, Takeru Watanabe
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Patent number: 6462207Abstract: A series of polyethylene glycol derivatives possessing a diene moiety has been prepared and characterized. The reactivities of these derivatives in various Diels-Alder reactions have been demonstrated. The potential derivatives, which can be made by various Diels-Alder reactions, are expected to be useful in biotechnical applications.Type: GrantFiled: September 14, 2000Date of Patent: October 8, 2002Assignee: Southwest Missouri State UniversityInventor: Reza Sedaghat-Herati
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Patent number: 6458803Abstract: The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N-phenyl-N-heteroaralkyl aminoalcohols.Type: GrantFiled: November 23, 2001Date of Patent: October 1, 2002Assignee: G.D. Searle & Co.Inventors: James A. Sikorski, Richard C. Durley, Deborah A. Mischke, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Margaret L. Grapperhaus, Brian S. Hickory, Mark A. Massa, Monica B. Norton, William F. Vernier, Barry L. Parnas, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
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Publication number: 20020133030Abstract: This invention provides processes for the preparation of a compound of Formula I:Type: ApplicationFiled: May 8, 2002Publication date: September 19, 2002Applicant: Syntex USA, LLCInventors: Jeffrey Allen Campbell, Lawrence Emerson Fisher, Charles Alois Dvorak, Paul Leo McGrane
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Patent number: 6452013Abstract: The present invention of compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, R1 is C1-6alkyloxy, C2-6alkenyloxy or C2-6alkynyl-oxy; R2 is hydrogen, C1-6alkyl C1-6alkyloxy; R3 is hydrogen or halo; R4 is hydrogen or C1-6alkyl; R5 is hydrogen or C1-6alkyl; L is C3-6cycloalkyl, C5-6cycloalkanone, C2-6alkenyl, or L is a radical of formula —Alk—R6—, Alk—X—R7, -Alk-Y—C(═O)—R9, or -Alk-Y—C(═O)—NR11R12 wherein each Alk is C1-12alkanediyl; and R6 is hydrogen, cyano, C1-6alkylsulfonylamino, C3-6cycloalkyl, C5-6cycloalkanone, or a heterocyclic ringsystem; R7 is hydrogen, C1-6alkyl, hydroxyC1-6alkyl, C3-6cycloalkyl, or a heterocyclic ringsystem; X is O, S, SO2 or NR8; said R8 being hydrogen or C1-6alkyl; R9 is hydrogen, C1-6alkyl, C3-6cycloalkyl, C1-6alkyloxy or hydroxy; Y is NR10 or a direct bond; said R10 being hydrogen, or C1-6alkyl; R11 anType: GrantFiled: January 5, 2000Date of Patent: September 17, 2002Assignee: Janssen Pharmaceutica N.V.Inventors: Jean-Paul RenĂ© Marie AndrĂ© Bosmans, Michel Anna Jozef De Cleyn, Michel Surkyn
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Patent number: 6448416Abstract: The present invention is directed to dicyanomethylenedihydrofuran-based electron acceptors which can be used in the preparation of polymeric thin films for waveguide media, and methods of making the same.Type: GrantFiled: June 16, 2000Date of Patent: September 10, 2002Assignee: Corning IncorporatedInventors: Mingqian He, Thomas M. Leslie
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Publication number: 20020099034Abstract: An improved method is described for making 9-deoxy-PGF1-type compounds. In contrast to the prior art, the method is stereoselective and requires fewer steps than the known methods for making these compounds.Type: ApplicationFiled: January 5, 2001Publication date: July 25, 2002Inventors: Robert M. Moriarty, Hitesh Batra
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Patent number: 6420392Abstract: 2,5-Diaryl tetrahydrofurans, 2,5-diaryl tetrahydrothiophenes, 1,3-diaryl cyclopentanes are disclosed that reduce the chemotaxis and respiratory burst leading to the formation of damaging oxygen radicals of polymorphonuclear leukocytes during an inflammatory or immune response. The compounds exhibit this biological activity by acting as PAF receptor antagonists, by inhibiting the enzyme 5-lipoxygenase, or by exhibiting dual activity, i.e., by acting as both a PAF receptor antagonist and inhibitor of 5-lipoxygenase. Also disclosed is a method to treat disorders mediated by PAF and/or leukotrienes that includes administering an effective amount of one or more of the above-identified compounds or a pharmaceutically acceptable salt thereof, optionally in a pharmaceutically acceptable carrier, to a patient in need of such therapy.Type: GrantFiled: October 9, 1996Date of Patent: July 16, 2002Assignee: Millennium Pharmaceuticals, Inc.Inventors: Tesfaye Biftu, Xiong Cai, Sajjat Hussoin, Gurmit Grewal, T Y Shen
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Patent number: 6420419Abstract: L-Ascorbic acid 2-phosphate zinc salt and a salt hydrate thereof having excellent solubility and exhibiting good stability even under weakly acidic conditions. Also disclosed is a process of manufacturing L-ascorbic acid 2-phosphate zinc salt by displacing a cation of a salt of an L-ascorbic acid 2-phosphate other than a zinc salt with a zinc cation. Further disclosed is a composition containing L-ascorbic acid 2-phosphate zinc salt or a salt hydrate thereof as an active ingredient.Type: GrantFiled: June 11, 1998Date of Patent: July 16, 2002Assignee: Showa Denko Kabushiki KaishaInventors: Masahiro Suzuki, Toshi Tsuzuki, Shinobu Ito, Eiji Ogata
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Patent number: 6369102Abstract: Substituted tetrahydrofuran analogs of prostaglandins and methods of their use in treating glaucoma and ocular hypertension are disclosed.Type: GrantFiled: March 6, 2001Date of Patent: April 9, 2002Assignee: Alcon Manufacturing, Ltd.Inventor: Robert D. Selliah
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Publication number: 20020037918Abstract: The present invention provides an efficient synthetic strategy for the preparation of analogs that incorporate important structural elements of the marine natural product curacin A, the compositions and various uses of the compositions. The most active of these compounds at nanomolar concentrations inhibit tubulin polymerization, show growth inhibition activity, inhibited colchicines binding to tubulin and block mitotic progression. The compounds of the present invention represent some of the most potent synthetic curacin A analogs synthesized, with an activity profile rivaling that of the natural product despite the simplified structure, greater water solubility, and increased chemical stability.Type: ApplicationFiled: July 19, 2001Publication date: March 28, 2002Inventors: Peter Wipf, Jonathan T. Reeves, Billy W. Day, Raghavan Balachandran
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Patent number: 6355814Abstract: The present invention relates to a catalytic process for the preparation of 3-hydroxymethyl tetrahydrofuran of formula IV with hydroformylation as one of the key steps. The process comprises reacting 9-hydroxymethyl-7,12-dioxaspiro[5,6]dodecane of the formula III with an alcohol in the presence of an acid catalyst and recovering the 3-hydroxymethyl tetrahydrofuran.Type: GrantFiled: February 28, 2001Date of Patent: March 12, 2002Assignee: Council of Scientific and Industrial Research of IndiaInventors: Pardhasaradhi Malladi, Sri Nagesh Kumar Potluri
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Publication number: 20020028818Abstract: Sulfones of formula I are useful as antiproliferative agents, including, for example, anticancer agents: 1Type: ApplicationFiled: April 12, 2001Publication date: March 7, 2002Inventors: E. Premkumar Reddy, M.V. Ramana Reddy
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Publication number: 20020010337Abstract: The invention relates to novel stilbene compounds having the general formula (I): 1Type: ApplicationFiled: February 21, 2001Publication date: January 24, 2002Inventors: Jean-Michel Bernardon, Bruno Charpentier
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Patent number: 6307067Abstract: Nucleophilic oxygen species, such as primary alcohols, carboxylates, and water, are added to vinyl epoxides in a highly regioselective and enantioselective manner, providing a convenient route to enantiomerically enriched 1,2-diols and oxygen-containing heterocycles. The reaction employs a chiral Pd(0) complex and a borane or borate as co-catalysts Also described are similar additions of nitrogen nucleophiles, and the addition of carbonates to vinyl epoxides using a chiral Pd(0) catalyst.Type: GrantFiled: September 7, 1999Date of Patent: October 23, 2001Assignee: The Board of Trustees of the Leland Stanford Junior UniversityInventors: Ernest John McEachern, Francisco Dean Toste, Barry Martin Trost
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Patent number: 6271425Abstract: A novel process for producing alcohols, characterized by reacting an organic halide represented by the formula R—X (wherein R means an organic residue and X means a halogen atom) with oxygen molecules in the presence of an organotin compound and a reducing agent and optionally in the presence of a free-radical inhibitor in an amount up to 0.3 equivalent based on the organic halide to obtain an alcohol represented by the general formula R—OH (wherein R has the same meaning as the above).Type: GrantFiled: September 7, 1999Date of Patent: August 7, 2001Assignees: Fujisawa Pharmaceutical Co., Ltd.Inventors: Eiichi Nakamura, Masaya Sawamura
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Patent number: 6268513Abstract: The present invention discloses new efficient processes for various bond forming reactions, including Suzuki reactions and aryl aminations. Organic compounds (e.g., ligands), their metal complexes and compositions using those compounds, provide useful catalysts. The invention also relates to performing Suzuki cross coupling reactions with unreactive aryl-chlorides.Type: GrantFiled: August 20, 1999Date of Patent: July 31, 2001Assignee: Symyx Technologies, Inc.Inventors: Anil Guram, Xiaohong Bei
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Patent number: 6225487Abstract: A new ligand having a backbone comprised of PCCC, where the last carbon atom is sp3 hybridized can be combined with a metal or metal precursor compound or formed into a metal-ligand complex to catalyze a number of different chemical transformations, including C—N bond formation.Type: GrantFiled: April 17, 1998Date of Patent: May 1, 2001Assignee: Symyx Technologies, Inc.Inventor: Anil Guram
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Patent number: 6197812Abstract: Substituted tetrahydrofuran analogs of prostaglandins and methods of their use in treating glaucoma and ocular hypertension are disclosed.Type: GrantFiled: November 15, 1999Date of Patent: March 6, 2001Assignee: Alcon Laboratories, Inc.Inventors: Robert D. Selliah, Mark R. Hellberg, Peter G. Klimko, Verney L. Sallee, Paul W. Zinke
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Patent number: 6191292Abstract: The invention relates to precursors of the A-ring of vitamin D, of the formula (I): in which A, R, R1 and R2 are as defined in the specification. The invention also relates to a method of preparing compounds (I) comprising the enzymatic asymmetrization of 3,5-dihydroxybenzoic acid derivatives, as well as intermediates of preparation of said compounds.Type: GrantFiled: December 8, 1999Date of Patent: February 20, 2001Assignee: Laboratoire TheramexInventors: Jean-Claude Pascal, Maurits Vandewalle, Philippe Maillos, Pierre De Clercq
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Patent number: 6166074Abstract: Pharmaceutical compositions which are useful for the treatment of cancer or illnesses which arise due to an abnormally elevated cell proliferation comprise acyl derivatives of aromatic aldehydes, especially arylidene diesters and .alpha.-alkoxyarylidene esters of general formula (I).Type: GrantFiled: October 4, 1996Date of Patent: December 26, 2000Assignee: Norsk Hydro A.S.Inventors: Erik Olai Pettersen, Rolf Olaf Larsen, John Michael Dornish, Bernt B.o slashed.rretzen, Reidar Oftebro, Thomas Ramdahl, Vidar Moen
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Patent number: 6153757Abstract: The invention relates to compounds of formula (1) ##STR1## wherein: Z is O or S; V is a divalent radical which together with C* and N forms a ring having six ring atoms, where each of said ring atoms other than C* and N independently is unsubstituted or substituted by a suitable substituent, and at least one of said other ring atoms is a heteroatom selected from O, N and S, and the remainder is carbon atoms; and Ar is an aryl or heteroaryl group; and pharmaceutically acceptable prodrugs, salts and solvates thereof. The invention further relates to pharmaceutically acceptable prodrugs, salts and solvates of these compounds. The invention also relates to methods of inhibiting the activity of metalloproteinases by administering a compound of formula (1) or a prodrug, salt or solvate thereof. The invention further relates to pharmaceutical compositions comprising an effective amount of these compounds, prodrugs, salts, and solvates.Type: GrantFiled: June 29, 1998Date of Patent: November 28, 2000Assignee: Agouron Pharmaceuticals, Inc.Inventors: Scott E. Zook, Raymond Dagnino, Jr., Michael E. Deason, Steven L. Bender, Michael J. Melnick
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Patent number: 6124476Abstract: The present invention discloses new organic compounds (e.g., ligands), their metal complexes and compositions using those compounds. The invention also relates to the field of catalysis. In particular, this invention relates to new compounds which when combined with suitable metals or metal precursor compounds provide useful catalysts for various bond-forming reactions, including Suzuki cross-coupling reactions. The invention also relates to performing Suzuki cross coupling reactions with unreactive aryl-chlorides.Type: GrantFiled: February 18, 1999Date of Patent: September 26, 2000Assignee: Symyx Technologies, Inc.Inventors: Anil Guram, Xiaohong Bei, Timothy S. Powers, Bernd Jandeleit, Thomas Crevier
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Patent number: 6124344Abstract: The invention relates to the use of derivatives of F-type prostaglandins as ocular hypotensives. The compounds used in accordance with the invention are represented by the following formula I: ##STR1## wherein wavy line attachments indicate either the alpha (.alpha.) or beta (.beta.) configuration; hatched segments indicate a configuration; the solid triangle is used to indicate .beta. configuration; dashed bonds represent a double bond, or a single bond; R is a substituted heteroaryl radical having at least two pendant substituents selected from the group consisting of C.sub.1 to C.sub.6 alkyl; halogen; trifluoromethyl; COR.sup.1 ; COCF.sub.3 ; SO.sub.2 NR.sup.1 ; NO.sub.2 and CN or at least one cyano group; R.sup.1 is hydrogen or a lower alkyl radical having up to six carbon atoms, X is selected from the group consisting of --OR.sup.1 and --N(R.sup.1).sub.2 ; Y is .dbd.Type: GrantFiled: November 19, 1997Date of Patent: September 26, 2000Assignee: Allergan Sales, Inc.Inventor: Robert M. Burk
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Patent number: 6063928Abstract: Novel compounds having the ability to inhibit 5-lipoxygenase enzyme and having the following formula I: ##STR1## and the pharmaceutically acceptable salts thereof, wherein Ar.sup.1 is a heterocyclic moiety which is selected from imidazolyl, pyrrolyl, pyrazolyl, 1,2,3-triazolyl, 1,2,4-triazolyl, indolyl, indazolyl and benzimidazolyl, which is bonded to X.sup.1 through a ring nitrogen atom, and which may be optionally substituted with one or two substituents selected from halo, hydroxy, cyano, amino, C.sub.1-4 alkyl and the like; X.sup.1 is a direct bond or C.sub.1-4 alkylene; Ar.sup.2 is phenylene optionally substituted with halo, hydroxy, cyano, amino and the like; X.sup.2 is --A--X-- or --X--A-- wherein A is a direct bond or C.sub.1-4 alkylene and X is oxy, thio, sulfinyl or sulfonyl; Ar.sup.3 is phenylene, pyridylene, thienylene, furylene, oxazolylene or thiazolylene optionally substituted with one or two substituents selected from halo, hydroxy, cyano, amino, C.sub.1-4 alkyl and the like; R.sup.1 and R.Type: GrantFiled: December 8, 1998Date of Patent: May 16, 2000Assignee: Pfizer IncInventors: Rodney W. Stevens, Takashi Mano, Kazunari Nakao, Yoshiyuki Okumura
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Patent number: 6025392Abstract: Substituted tetrahydrofuran analogs of F-series prostaglandins and methods of their use in treating glaucoma and ocular hypertension are disclosed.Type: GrantFiled: July 2, 1998Date of Patent: February 15, 2000Assignee: Alcon Laboratories, Inc.Inventors: Robert D. Selliah, Mark R. Hellberg, Peter G. Klimko, Verney L. Sallee, Paul W. Zinke
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Patent number: 6020339Abstract: The invention encompasses the novel compound of Formula I useful in the treatment of diseases, including asthma, by raising the level of cyclic adenosine-3',5'-monophosphate (cAMP) through the inhibition of phosphodiesterase IV (PDE IV). ##STR1## The invention also encompasses certain pharmaceutical compositions and methods for treatment of diseases by inhibition of PDE IV, resulting in an elevation of cAMP, comprising the use of compounds of Formula I.Type: GrantFiled: September 28, 1998Date of Patent: February 1, 2000Assignee: Merck & Co., Inc.Inventors: Helene Perrier, Yongxin Han, Christopher Bayly, Dwight Mac Donald, Andre Giroux, Robert N. Young
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Patent number: 6013813Abstract: The present invention deals with the composition of matter and the utilization of certain novel sorbitol guerbet esters which are prepared by the reaction of a guerbet acid and a sorbitol as emulsifiers.Type: GrantFiled: August 24, 1998Date of Patent: January 11, 2000Assignee: Hansotech IncInventor: Anthony J. O'Lenick, Jr.
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Patent number: 6008247Abstract: Compounds according to the formula: ##STR1## wherein: R.sub.1 and R.sub.2 are each independently selected from the group consisting of H, loweralkyl, aryl, alkylaryl, aminoalkyl, aminoaryl, halogen, oxyalkyl, oxyaryl, or oxyarylalkyl; R.sub.3 and R.sub.4 are each independently selected from the group consisting of H, loweralkyl, oxyalkyl, alkylaryl, aryl, oxyaryl, aminoalkyl, aminoaryl, or halogen; and X and Y are located in the para or meta positions and are each selected from the group consisting of H, loweralkyl, oxyalkyl, and ##STR2## wherein: each R.sub.5 is independently selected from the group consisting of H, loweralkyl, alkoxyalkyl, hydroxyalkyl, aminoalkyl, alkylaminoalkyl, cycloalkyl, aryl, or alkylaryl or two R.sub.5 groups together represent C.sub.2 to C.sub.10 alkyl, hydroxyalkyl, or alkylene; and R.sub.Type: GrantFiled: February 27, 1998Date of Patent: December 28, 1999Assignees: The University of North Carolina at Chapel Hill, Georgia State UniversityInventors: David W. Boykin, Richard R. Tidwell, W. David Wilson, Iris Francesconi
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Patent number: 6004903Abstract: Benzoyl derivatives of the formula I ##STR1## where Z is a 5-membered or 6-membered heterocyclic, saturated or unsaturated radical containing one to three hetero atoms selected from the group consisting of oxygen, sulfur and nitrogen,Q is a cyclohexane-1, 3-dione ring bonded in the 2-position and of the formula II, ##STR2## or conventional agricultural salts of the compounds I.Type: GrantFiled: August 14, 1997Date of Patent: December 21, 1999Assignee: Basf AktiengesellschaftInventors: Wolfgang von Deyn, Regina Luise Hill, Uwe Kardorff, Stefan Engel, Martina Otten, Marcus Vossen, Peter Plath, Harald Rang, Albrecht Harreus, Franz Rohl, Helmut Walter, Karl-Otto Westphalen, Ulf Misslitz
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Patent number: 5994397Abstract: Substituted tetrahydrofuran analogs of prostagladins and methods of their use in treating glaucoma and ocular hypertension are disclosed.Type: GrantFiled: April 4, 1997Date of Patent: November 30, 1999Assignee: Alcon Laboratories, Inc.Inventors: Robert D. Selliah, Peter G. Klimko
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Patent number: 5972991Abstract: The invention relates to the use of derivatives of F-type prostaglandins as ocular hypotensives. The PGF derivatives used in accordance with the invention are represented by the following formula I: ##STR1## wherein wavy line attachments indicate either the alpha (.alpha.) or beta (.beta.) configuration; hatched segments indicate .alpha. configuration, solid triangles are used to indicate .beta. configuration, dashed bonds represent a double bond, or a single bond, R is a substituted heteroaryl radical, R.sup.1 is hydrogen or a lower alkyl radical having up to six carbon atoms, X is selected from the group consisting of --OR.sup.1 and --N(R.sup.1).sub.2, Y is =O or represents 2 hydrogen radicals. Certain of the compounds represented by Formula I comprise another aspect of the present invention.Type: GrantFiled: November 3, 1998Date of Patent: October 26, 1999Assignee: AllerganInventor: Robert M. Burk
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Patent number: 5912364Abstract: Disclosed is a process for the preparation of 3-methyltetrahydrofuran (3-MeTHF) which comprises contacting 3-formyltetrahydrofuran with hydrogen in the presence of a catalyst system comprising a Group VIII noble metal or rhenium and a strong acid under hydrogenolysis conditions of temperature and pressure to produce 3-MeTHF. The 3-MeTHF produced in accordance with the present invention is useful as an industrial solvent and, more importantly, as a monomer in the manufacture of polymers such as elastomers.Type: GrantFiled: October 6, 1997Date of Patent: June 15, 1999Assignee: Eastman Chemical CompanyInventor: William Anthony Beavers
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Patent number: 5877333Abstract: A compound having the structure: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, and R.sup.5 are each independently a hydrogen atom, an alkyl group or an aryl group, or wherein R.sup.2 and R.sup.3 together and R.sup.4 and R.sup.5 together are joined as a cycloalkyl group; wherein R.sup.6 is a hydroxyl group, an alkoxyl group, an aralkyloxy group, or --OSi (R.sup.8 R.sup.9 R.sup.10) in which R.sup.8, R.sup.9 and R.sup.10 are each independently an alkyl group or a phosphate salt group and R.sup.7 is a hydrogen atom, a halogen atom, an alkyl group, or an alkoxyl group.Type: GrantFiled: November 5, 1997Date of Patent: March 2, 1999Assignee: Fujirebio Inc.Inventors: Masakatsu Matsumoto, Nobuko Watanabe, Hisako Kobayashi, Hiroshi Ikawa
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Patent number: 5874460Abstract: Compounds of the formula ##STR1## where W is (CH.sub.2).sub.n where n is 1 or 2, or n is 0 and W represents lower alkyl groups attached to each oxygen;m is an integer between 1 and 8;R.sub.1 is COOH or a pharmaceutically acceptable salt thereof, COOR.sub.4, CONR.sub.5 R.sub.6, CONR.sub.5 SO.sub.2 R.sub.7, CH.sub.2 OH, CH.sub.2 OR.sub.7, CH.sub.2 O--COR.sub.7, CH.sub.2 O--CONR.sub.5,R.sub.7, CH.sub.2 OCOOR.sub.7, CH.sub.2 NH.sub.2, CH.sub.2 NR.sub.5 R.sub.6, etc. where R.sub.4 is an alkyl group, or a cycloalkyl group, or R.sub.4 is phenyl or lower alkylphenyl, R.sub.5 and R.sub.6 independently are hydrogen, an alkyl group, etc., R.sub.7 is alkyl of 1 to 10 carbons, phenyl or lower alkylphenyl, R.sub.8 is lower alkyl, and R.sub.9 is divalent alkyl radical of 2-5 carbons, R.sub.10 is an alkyl OR cycloalkyl containing 1 to 5 carbons;R.sub.2 is H, COR.sub.7, R.sub.7, CO--OR.sub.7, CO--NR.sub.5,R.sub.7, PO(OH)OR.sub.7, PO(OR.sub.7).sub.2, POR.sub.7 OH, or POR.sub.7 (OR.sub.7) ;R.sub.Type: GrantFiled: June 9, 1998Date of Patent: February 23, 1999Assignee: Allergan Sales Inc.Inventors: Robert M. Burk, David F. Woodward
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Patent number: 5856531Abstract: Disclosed is a two-step process wherein (1) 2,3-dihydrofuran is reacted with a trialkyl orthoformate in the presence of an acidic catalyst to produce a 2-alkoxy-3-(dialkoxymethyl)tetrahydrofuran intermediate and (2) the intermediate is contacted with hydrogen in the presence of a catalyst system comprising a Group VIII noble metal or rhenium and a strong acid to convert the intermediate to a mixture of 3-methyltetrahydrofuran (3-MeTHF) and 3-(hydroxymethyl)tetrahydrofuran (3-HOMeTHF). The 3-MeTHF produced in accordance with the present invention is useful as an industrial solvent and as a co-monomer in the manufacture of polymers such as elastomers. 3-HOMeTHF may be used as a solvent and in the manufacture of pharmaceutical and agricultural chemicals and acrylate and methacrylate esters for use in preparing polymers such as polyacrylates.Type: GrantFiled: October 6, 1997Date of Patent: January 5, 1999Assignee: Eastman Chemical CompanyInventor: William Anthony Beavers
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Patent number: 5856323Abstract: 2,5-Diaryl tetrahydrofurans, 2,5-diaryl tetrahydrothiophenes, 2,4-diaryl tetrahydrofurans, 2,4-diaryl tetrahydrothiophenes, 1,3-diaryl cyclopentanes, 2,4-diaryl pyrrolidines, and 2,5-diaryl pyrrolidines are disclosed that reduce the chemotaxis and respiratory burst leading to the formation of damaging oxygen radicals of polymorphonuclear leukocytes during an inflammatory or immune response. The compounds exhibit this biological activity by acting as PAF receptor antagonists, by inhibiting the enzyme 5-lipoxygenase, or by exhibiting dual activity, i. e., by acting as both a PAF receptor antagonist and inhibitor of 5-lipoxygenase.A method to treat disorders mediated by PAF or leukotrienes is also disclosed, that includes administering an effective amount of one or more of the above-identified compounds or a pharmaceutically acceptable salt thereof, optionally in a pharmaceutically acceptable carrier.Type: GrantFiled: June 7, 1995Date of Patent: January 5, 1999Assignee: CytoMed, Inc.Inventors: Xiong Cai, Sajjat Hussoin, San-Bao Hwang, David Killian, T. Y. Shen
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Patent number: 5814660Abstract: Substituted tetrahydrofuran analogs of prostaglandins and methods of their use in treating glaucoma and ocular hypertension are disclosed.Type: GrantFiled: June 18, 1997Date of Patent: September 29, 1998Assignee: Alcon Laboratories, Inc.Inventor: Robert D. Selliah
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Patent number: 5808094Abstract: A process for the preparation of mixed crystals of 1,4-diketopyrrolo?3,4-c!pyrroles, consisting of 1 mol each of two different compounds of formula ##STR1## by heating a corresponding mixture in solid form to the temperature range from 220.degree. to 380.degree. C.A and B are, for example, each a group of formula ##STR2## wherein R.sub.1 and R.sub.2 are each independently hydrogen, chloro, bromo, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkylamino, phenyl or --CN,G is --O--, --NR.sub.7 --, --N.dbd.N-- or --SO.sub.2 --,R.sub.3 and R.sub.4 are hydrogen, and R.sub.7 is hydrogen, methyl or ethyl.The mixed crystals and solid solutions obtained are excellently suited for pigmenting high molecular weight material.Type: GrantFiled: July 22, 1997Date of Patent: September 15, 1998Assignee: Ciba Specialty Chemicals CorporationInventors: Jin Mizuguchi, Zhimin Hao, Olof Wallquist, Abul Iqbal
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Patent number: 5808101Abstract: Compounds of the formula ##STR1## where the symbols have the meaning defined in the specification, are capable of lowering intraocular pressure in the eye of a mammal.Type: GrantFiled: November 21, 1997Date of Patent: September 15, 1998Assignee: AllerganInventors: Robert M. Burk, David F. Woodward
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Patent number: 5741914Abstract: Furfuryl alcohol/formaldehyde resins exhibiting high water compatibility and low amounts of volatile organic compounds such as furfuryl alcohol.Type: GrantFiled: May 8, 1995Date of Patent: April 21, 1998Assignee: QO Chemicals, Inc.Inventors: George S. Everett, George R. MacLennan, Michael C. Chen
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Patent number: 5723681Abstract: The present invention relates to novel 3,3-(disubstituted)cyclohexan-1-ol dimers and related compounds, pharmaceutical compositions containing these compounds, and their use in treating allergic and inflammatory diseases and for inhibiting the production of Tumor Necrosis Factor (TNF).Type: GrantFiled: June 23, 1997Date of Patent: March 3, 1998Assignee: SmithKline Beecham CorporationInventors: Siegfried B. Christensen, IV, Joseph M. Karpinski
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Patent number: 5665763Abstract: Compounds of the formula ##STR1## wherein: R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are as defined in the specification,Y is alkylene of 3 to 9 carbon atoms,R.sub.5 is alkoxycarbonyl, alkyltetrazolyl, phenyl or a heterocycle chosen from benzoxazolyl, benzathiazolyl, thiadiazolyl, imidazolyl, dihydroimidazolyl, oxazolyl, thiazolyl, oxadiazolyl, pyrazolyl, oxazolinyl, isoxazolyl, isothiazolyl, furyl, triazolyl, thiophenyl, pyridyl, pyrimidinyl, pyrazinyl, pyridazinyl or any of the above substituted with alkyl, alkoxyalkyl, cycloalkyl, halo alkyl, hydroxyalkyl, alkoxy, hydroxy, halo, furyl, thienyl, fluoroalkyl;or a pharmaceutically acceptable acid addition salts thereof; N-oxides thereof, are useful as antipirconaviral agents.Type: GrantFiled: August 30, 1996Date of Patent: September 9, 1997Assignee: Sanofi, S.A.Inventors: David J. Aldous, Thomas R. Bailey, Guy Dominic Diana, Theodore J. Nitz
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Patent number: 5663367Abstract: Compounds of Formula 1 ##STR1## wherein Z is selected from the group consisting of the radicals shown in Formula 2 and in Formula 3, ##STR2## Y is cycloalkyl or cycloalkenyl of 3 to 8 carbons optionally substituted with one or two R.sub.4 groups, or Y is selected from phenyl, pyridyl, thienyl, furyl, pyrrolyl, pyridazinyl, pyrimidinyl, pyrazinyl, thiazolyl, oxazolyl, and imidazolyl, said groups being optionally substituted with one or two R.sub.4 groups, the divalent Y radical being substituted by the Z and --CR.sub.1 .dbd.CR.sub.1 --CR.sub.1 .dbd.CR.sub.1 groups on adjacent carbons; X is S, O, or NR.sub.5 ; n is 1 or 2; R.sub.1 and R.sub.2 independently are H, lower alkyl or fluoroalkyl; R.sub.3 is hydrogen, lower alkyl, Cl or Br; R.sub.4 is lower alkyl, fluoroalkyl or halogen; R.sub.5 is H or lower alkyl, and B is hydrogen, COOH or a pharmaceutically acceptable salt thereof, COOR.sub.8, CONR.sub.9 R.sub.10, --CH.sub.2 OH, CH.sub.2 OR.sub.11, CH.sub.2 OCOR.sub.11, CHO, CH(OR.sub.12).sub.2, CHOR.sub.Type: GrantFiled: May 31, 1996Date of Patent: September 2, 1997Assignee: AllerganInventors: Vidyasagar Vuligonda, Roshantha A. Chandraratna
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Patent number: 5648486Abstract: 2,5-Diaryl tetrahydrofurans, 2,5-diaryl tetrahydrothiophenes, 2,4-diaryl tetrahydrofurans, 2,4-diaryl tetrahydrothiophenes, 1,3-diaryl cyclopentanes, 2,4-diaryl pyrrolidines, and 2,5-diaryl pyrrolidines are disclosed that reduce the chemotaxis and respiratory burst leading to the formation of damaging oxygen radicals of polymorphonuclear leukocytes during an inflammatory or immune response. The compounds exhibit this biological activity by acting as PAF receptor antagonists, by inhibiting the enzyme 5-lipoxygenase, or by exhibiting dual activity, i.e., by acting as both a PAF receptor antagonist and inhibitor of 5-lipoxygenase.A method to treat disorders mediated by PAF or leukotrienes is also disclosed, that includes administering an effective amount of one or more of the above-identified compounds or a pharmaceutically acceptable salt thereof, optionally in a pharmaceutically acceptable carrier.Type: GrantFiled: May 12, 1993Date of Patent: July 15, 1997Assignee: CytoMed, Inc.Inventors: Xiong Cai, Sajjat Hussoin, San-Bao Hwang, David Killian, T. Y. Shen
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Patent number: 5618941Abstract: Compounds of formula (I) wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are each H or C.sub.1 -C.sub.4 alkyl; R.sup.5 is (CH.sub.2).sub.m NHSO.sub.2 R.sup.6 or (CH).sub.m NHCOR.sup.6 ; R.sup.6 is C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 cycloalkyl optionally substituted by aryl, aryl or heteroaryl; R.sup.7 is H, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, halo, CF.sub.3, OCF.sub.3, CN, CONH.sub.2, or S(O).sub.n (C.sub.1 -C.sub.4 alkyl); X is CH.sub.2, CHCH.sub.3, CH(OH), C(OH)CH.sub.3, C.dbd.CH.sub.2, CO or O; m is 0 or 1 and n is 0, 1 or 2, and their pharmaceutically acceptable salts and biolabile esters, are antagonists of thromboxane A.sub.2 of utility, particulary in combination with a thromboxane synthetase inhibitor, in the treatment of atherosclerosis and unstable angina and for prevention of reocclusion after percutaneous transluminal angioplasty.Type: GrantFiled: March 15, 1995Date of Patent: April 8, 1997Assignee: Pfizer Inc.Inventors: Roger P. Dickinson, Kevin N. Dack, John Steele