Chalcogen Attached Indirectly To The Hetero Ring By Nonionic Bonding Patents (Class 549/427)
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Patent number: 7145015Abstract: Benzocycloheptenes of formula (I), in which R1, R2 and Y have the meanings that indicated herein, exhibit selective estrogenic activity on bones and are suitable for the production of pharmaceutical agents, especially for prophylaxis and therapy of osteoporosis:Type: GrantFiled: April 11, 2005Date of Patent: December 5, 2006Assignee: Schering AGInventors: Rolf Bohlmann, Jorg Kroll, Hermann Kuenzer, Christa Hegele-Hartung, Monika Lessl, Rosemarie Lichtner, Yukishige Nishino
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Patent number: 7081347Abstract: A method for assessing aspirin resistance and relative risk of a cardiovascular event in a patient taking aspirin is provided. The concentration of 11-dehydro-thromboxane B2 in a urine sample is measured and compared to a set of standardized quartile concentrations. A concentration of urinary 11-dehydro-thromboxane B2 that falls within the second, third, or fourth quartile is indicative of aspirin resistance and an elevated risk of a recurrent cardiovascular event.Type: GrantFiled: September 24, 2003Date of Patent: July 25, 2006Assignee: McMaster UniversityInventors: Salim Yusuf, Jack Hirsh, John Eikelboom
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Patent number: 7064221Abstract: This invention provides a process for producing a pyran efficiently with high productivity and simplified production facilities. The process for producing a pyran comprises reacting aldehyde (I) represented by: R1—CHO??(I) wherein is a single or double bond and R1 represents an alkyl or alkenyl group having 1 to 12 carbon atoms, an optionally alkyl- or alkoxy-substituted aryl group having 6 to 12 carbon atoms in total, etc., to react isoprenol to produce pyran (II), wherein water in a reactor is maintained in an amount of 0.25 wt % or less while the conversion of that which has the lower charged total number of moles between aldehyde (I) and isoprenol is less than 50%.Type: GrantFiled: August 11, 2004Date of Patent: June 20, 2006Assignee: Kao CorporationInventors: Kazuki Naito, Koji Mine
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Patent number: 6958395Abstract: The present invention relates to a method by which saccharide compounds can be prepared in a very easy way. This method comprises the steps of: (a) attaching at least one saccharide to a cyclic or acyclic diene, (b) reacting the saccharide-containing diene obtained in step (a) or a commercially available saccharide-containing diene with a dienophile by Diels-Alder reaction.Type: GrantFiled: August 22, 2001Date of Patent: October 25, 2005Assignee: Deutsches Krebsforschungszentrum Stiftung des Offentlichen RechtsInventors: Manfred Wiessler, Hans-Christian Kliem, Bernd Sauerbrei, Birgit Schmauser
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Patent number: 6902777Abstract: A liquid-crystalline mediums which contain one or more compounds of the formula A and at least one compound of the formula B wherein compounds of formula A contain at least one ring selected from and in which Ra, Rb, ring A and ring B, Y, Z1, Z2, a, L1, L2, L3, L4, L5, L6, L7, L8 and L9 are as defined herein, are suitable for use in twisted nematic (TN) and supertwisted nematic (STN) liquid-crystal displays. Such displays have very short response times and good steepnesses and angle dependencies.Type: GrantFiled: December 22, 2003Date of Patent: June 7, 2005Assignee: Merck Patent GmbHInventors: Harald Hirschmann, Eike Poetsch, Peer Kirsch, Sabine Schoen
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Patent number: 6867323Abstract: Improved methods for generating a —C—C— bond by cross-coupling of a transferable group with an acceptor group. The transferable group is a substituent of an organosilicon nucleophile and the acceptor group is provided as an organic electrophile. The reaction is catalyzed by a Group 10 transition metal complex (e.g., Ni, Pt or Pd), particularly by a palladium complex. Certain methods of this invention use improved organosilicon nucleophiles which are readily prepared, can give high product yields and exhibit high stereoselectivity. Methods of this invention employ activating ions such as halides, hydroxide, hydride and silyloxides. In specific embodiments, organosilicon nucleophilic reagents of this invention include siloxanes, particularly cyclic siloxanes. The combination of the cross-coupling reactions of this invention with ring-closing metathesis, hydrosilylation and intramolecular hydrosilylation reactions provide useful synthetic strategies that have wide application.Type: GrantFiled: June 6, 2001Date of Patent: March 15, 2005Assignee: The Board of Trustees of the University of IllinoisInventors: Scott E. Denmark, Jun Young Choi, Daniel Wehrli, Zhicai Wu, Luc Neuville, Weitao Pan, Ramzi F. Sweis, Zhigang Wang, Shyh-Ming Yang
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Patent number: 6864254Abstract: An inhibitor for 20-hydroxyeicosatetraenoic acid production which comprises as the active ingredient a specific hydroxyformamidine derivative or a pharmacologically acceptable salt thereof. It is useful especially as a remedy for kidney diseases, cerebrovascular diseases, or circulatory diseases. The novel hydroxyformamidine derivative or pharmacologically acceptable salt thereof is also provided.Type: GrantFiled: November 1, 2000Date of Patent: March 8, 2005Assignee: Taisho Pharmaceutical Co., Ltd.Inventors: Masakazu Sato, Noriyuki Miyata, Takaaki Ishii, Yuko Kobayashi, Hideaki Amada
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Patent number: 6841709Abstract: The present invention is to provide a technology to establish a new cycle-based organic chemical industry, which may be called a polymer cascade (polymer reflux industry) wherein the polymer substances shall not remain the final products, but still give birth to synthetic materials as raw materials for chemical industry and produce useful organic compounds.Type: GrantFiled: October 30, 2001Date of Patent: January 11, 2005Inventor: Masaaki Yoshida
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Patent number: 6835845Abstract: A is a novel methine compound, for example, which is represented by the following formula (I): wherein R1, R2, R3, R4 and R5 each represents a hydrogen atom or a substituent; X represents an oxygen atom, a sulfur atom, or N—R6; Z represents —NR7R8, or —OG; R6, R7 and R8 each represents a hydrogen atom or a substituent; G represents a hydrogen atom, a cation or a substituent; L1, L2 and L3 each represents a substituted or unsubstituted methine group; n represents 1 or 2; and W represents an electron attractive group. Also, a material for organic luminescence element and organic luminescence element using the same are disclosed.Type: GrantFiled: July 26, 2002Date of Patent: December 28, 2004Assignee: Fuji Photo Film Co., Ltd.Inventors: Hisashi Okada, Terukazu Yanagi
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Patent number: 6833462Abstract: An acrylate compound of formula (4): is produced by allowing an acrylic acid compound of formula (1): to react with an unsaturated compound of formula (2) or (3): In formulae (1) through (4), R1 and R2 are H or F, R3 is H, F, or an alkyl, alkenyl, fluoroalkyl or fluoroalkenyl group, R4 and R5 are H, halogen, or an alkyl, alkenyl, halogenated alkyl or halogenated alkenyl group; and X and Y are an unsubstituted or substituted hydrocarbon group, and dashed line - - - means that X and Y may be bonded together to form a cyclic structure.Type: GrantFiled: November 26, 2002Date of Patent: December 21, 2004Assignee: Tosoh CorporationInventors: Shinichi Ishikawa, Hisao Eguchi
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Patent number: 6818638Abstract: Mevinolin derivatives wherein the lactone ring is modified have interesting pharmaceutical properties, particularly in preventing or treating disorders or diseases mediated by LFA-1/ICAM-1 interactions.Type: GrantFiled: July 11, 2002Date of Patent: November 16, 2004Assignee: Novartis AGInventors: Rolf Baenteli, Wilfried Bauer, Sylvain Cottens, Claus Ehrhardt, Ulrich Hommel, Jörg Kallen, Josef Gottfried Meingassner, François Nuninger, Gabriele Weitz Schmidt
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Patent number: 6812352Abstract: Multidentate phosphite ligands are disclosed for use in reactions such as hydrocyanation and isomerization. The catalyst compositions made therefrom and the various catalytic processes which employ such multidentate phosphite ligands are also disclosed. In particular, the ligands have heteroatom-containing substituents on the carbon attached to the ortho position of the terminal phenol group.Type: GrantFiled: April 9, 2002Date of Patent: November 2, 2004Assignee: Invista North America S.a.r.l.Inventors: Kristina Ann Kreutzer, Wilson Tam, J. Michael Garner, John Ronald Boyles
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Patent number: 6762198Abstract: Disclosed are compounds which are inhibitors of metalloproteases and which are effective in treating conditions characterized by excess activity of these enzymes. In particular, the compounds have a structure according to the following Formula (I): where J, M, Q, T, W, X, Z, R1, R2, R3, R4, R4′, R5, R6, R6′, R7, m, and n have the meanings described in the specification. This invention also includes optical isomers, diastereomers and enantiomers of the formula above, and pharmaceutically-acceptable salts, biohydrolyzable amides, esters, and imides thereof. Also disclosed are pharmaceutical compositions comprising these compounds, and methods of treating or preventing metalloprotease-related maladies using the compounds or the pharmaceutical compositions.Type: GrantFiled: March 25, 2003Date of Patent: July 13, 2004Assignee: The Procter & Gamble CompanyInventors: Menyan Cheng, Neil Gregory Almstead, Michael George Natchus, Stanislaw Pikul, Biswanath De
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Publication number: 20040073050Abstract: The present invention relates to substituted cyclohexenes, to their use as well as to their preparation method. These compounds have powerful long lasting natural fruity grapefruit notes with minty and fresh green tonalities.Type: ApplicationFiled: May 23, 2003Publication date: April 15, 2004Inventor: Andreas Goeke
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Patent number: 6713507Abstract: The present invention relates to novel ether compounds, compositions comprising ether compounds, and methods useful for treating and preventing cardiovascular diseases, dyslipidemias, dysproteinemias, and glucose metabolism disorders comprising administering a composition comprising an ether compound. The compounds, compositions, and methods of the invention are also useful for treating and preventing Alzheimer's Disease, Syndrome X, peroxisome proliferator activated receptor-related disorders, septicemia, thrombotic disorders, obesity, pancreatitis, hypertension, renal disease, cancer, inflammation, and impotence. In certain embodiments, the compounds, compositions, and methods of the invention are useful in combination therapy with other therapeutics, such as hypocholesterolemic and hypoglycemic agents.Type: GrantFiled: October 11, 2001Date of Patent: March 30, 2004Assignee: Esperion Therapeutics, Inc.Inventors: Jean-Louis Henri Dasseux, Carmen Daniela Oniciu
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Patent number: 6696569Abstract: Novel compounds comprising a C—C double bond substituted at one carbon with two oxygen or sulfur atom-containing groups are disclosed. The compounds are useful in methods and compositions for generating chemiluminescence by reaction with a peroxidase enzyme and a peroxide. The chemiluminescence thus produced can be used as a detectable signal in assays for peroxidase enzymes and in assays employing enzyme-labeled specific binding pairs.Type: GrantFiled: April 11, 2001Date of Patent: February 24, 2004Assignee: Lumigen, Inc.Inventors: Hashem Akhavan-Tafti, Zahra Arghavani, Renuka DeSilva
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Patent number: 6686348Abstract: A compound of formula (I): wherein: R1 represents hydrogen, halogen, alkyl or alkoxy, X represents oxygen, sulphur or NR wherein R represents hydrogen or alkyl, A represents any one of the groups described in the description, their isomers and addition salts thereof with a pharmaceutically acceptable acid or base and medicinal products containing the same are useful as metalloprotease inhibitor.Type: GrantFiled: December 21, 2001Date of Patent: February 3, 2004Assignee: Les Laboratoires ServierInventors: Guillaume De Nanteuil, Alain Benoist, Philippe Pastoureau, Massimo Sabatini, John Hickman, Alain Pierre, Gordon Tucker
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Publication number: 20030139613Abstract: An acrylate compound of formula (4): 1Type: ApplicationFiled: November 26, 2002Publication date: July 24, 2003Applicant: TOSOH CORPORATIONInventors: Shinichi Ishikawa, Hisao Eguchi
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Patent number: 6566381Abstract: Heterocyclic substituted compounds having the general structure: which are inhibitors of metalloproteases and which are effective in treating conditions characterized by excess activity of these enzymes.Type: GrantFiled: March 1, 2000Date of Patent: May 20, 2003Assignee: The Procter & Gamble CompanyInventors: Menyan Cheng, Neil Gregory Almstead, Michael George Natchus, Stanislaw Pikul, Biswanath De
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Publication number: 20030080323Abstract: Disclosed is a novel methine compound, for examples, which is represented by the following formula (I): 1Type: ApplicationFiled: July 26, 2002Publication date: May 1, 2003Applicant: FUJI PHOTO FILM CO., LTD.Inventors: Hisashi Okada, Terukazu Yanagi
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Patent number: 6541655Abstract: Complexes of a selected class of chiral ligands with molybdenum, tungsten or chromium, preferably molybdenum, are effective as catalysts in highly enantioselective and regioselective alkylation of allylic substrates.Type: GrantFiled: September 7, 2001Date of Patent: April 1, 2003Assignee: The Board of Trustees of the Leland Stanford Junior UniversityInventors: Barry M. Trost, Iwao Hachiya
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Patent number: 6525206Abstract: Featured compounds have high monoamine transport affinity and are characterized by one of the following two general formulas set out above. The compounds bind selectively or non-selectively to monoamine transporters. The compounds are useful to treat various medical indications including attention deficit hyperactivity disorder (ADHD), Parkinson's disease, cocaine addiction, smoking cessation, weight reduction, obsessive-compulsive disorder, various forms of depression, traumatic brain injury, stroke, and narcolepsy.Type: GrantFiled: October 17, 2000Date of Patent: February 25, 2003Assignees: President and Fellows of Harvard College, Organix, Inc.Inventors: Peter C. Meltzer, Paul Blundell, Pinglang Wang, Bertha K. Madras
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Patent number: 6482950Abstract: Squarylium compounds of the formula: wherein Q1 and Q2 are each independently a pyrylium, thiopyrylium, selenopyrylium, benzpyrylium, benzthiopyrylium or benzselenopyrylium nucleus, and R1 and R2 are each independently an aliphatic or cycloaliphatic group, can be prepared by reacting a squaric acid derivative of the formula: with a compound of the formula Q2CH2R2 in the presence of a base. The derivatives of Formula II may be prepared by condensing a 2,3,4,4-tetrahalocyclobut-2-en-1-one with a compound of the formula Q1CH2R1 in the presence of a base to produce a compound of the formula: wherein Q1 and R1 are as defined above, and X represents chlorine or bromine, and hydrolyzing the compound of Formula III.Type: GrantFiled: June 6, 1995Date of Patent: November 19, 2002Assignee: Polaroid CorporationInventors: Paulina P. Garcia, John W. Lee, John L. Marshall, Donald A. McGowan, Anthony J. Puttick, Thomas K. Spencer, Stephen G. Stroud, Stephen J. Telfer, Michael J. Zuraw
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Patent number: 6472422Abstract: The invention provides a compound of formula (I): wherein R1, R2, R3, and Y have any of the meanings defined in the specification; as well a pharmaceutical composition comprising a compound of formula I; intermediates and methods useful for preparing a compound of formula I; and therapeutic methods for treating drug addiction, Parkinson's disease or depression comprising administering a compound of formula I, to a mammal in need of such treatment.Type: GrantFiled: January 25, 2001Date of Patent: October 29, 2002Assignee: Georgetown UniversityInventors: Alan P. Kozikowski, Gian Luca Araldi
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Patent number: 6458474Abstract: Disclosed is a novel methine compound, for example, which is represented by the following formula (I): wherein R1, R2, R3, R4 and R5 each represents a hydrogen atom or a substituent; X represents an oxygen atom, a sulfur atom, or N—R6; Z represents —NR7R8, or —OG; R6, R7 and R8 each represents a hydrogen atom or a substituent; G represents a hydrogen atom, a cation or a substituent; L1, L2 and L3 each represents a substituted or unsubstituted methine group; n represents 1 or 2; and W represents an electron attractive group.Type: GrantFiled: March 18, 1999Date of Patent: October 1, 2002Assignee: Fuji Photo Film Co., Ltd.Inventors: Hisashi Okada, Terukazu Yanagi
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Patent number: 6420573Abstract: This invention provides processes for the preparation of a compound of Formula I: Y—C(═O)—C(R1)(R2)—CH2—S(O)nR3 wherein: Y is hydroxy or XONX, where each X is independently hydrogen, lower alkyl or lower acyl; R1 is hydrogen or lower alkyl; R2 is hydrogen, lower alkyl, aryl, aralkyl, cycloalkyl, cycloalkylalkyl, or R1 and R2 together with the carbon atom to which they are attached form a cycloalkyl or heterocyclo group; R3 is aryl; and n is 0, 1 or 2. The invention also provides novel aryl haloalkyl sulfide intermediates useful for the preparation of compounds of Formula I and novel methods of preparing aryl alkyl sulfides.Type: GrantFiled: November 9, 2001Date of Patent: July 16, 2002Assignee: Syntex (U.S.A.) LLPInventors: Jeffrey Allen Campbell, Lawrence Emerson Fisher, Charles Alois Dvorak, Paul Leo McGrane
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Patent number: 6395910Abstract: The present invention provides a production method of a 5-phthalancarbonitrile compound, which comprises the use of a novel compound of the formula [I] wherein X is chlorine atom, bromine atom or iodine atom, as a key intermediate. The method of the present invention imposes small environmental burden (without use of a reagent imposing great burden on the environment, such as heavy metal, metal cyanide, thionyl chloride and the like) and is safe. The inventive method is based on a completely new strategy which is different from conventional production methods of 5-phthalancarbonitrile compound.Type: GrantFiled: July 20, 2001Date of Patent: May 28, 2002Assignee: Sumika Fine Chemicals Co., Ltd.Inventors: Tetsuya Ikemoto, Masami Igi
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Patent number: 6384237Abstract: A novel pyrylium compound is represented by the general formula (I): wherein X is oxygen or sulfur, Y− is a monovalent anion, n is an integer of 2 or 3, and M is hydrogen or an alkali metal. This pyrylium compound functions as a labeling agent by intermolecular bonding to nucleic acids, and as a fluorescence label having a chemical bond with the nucleic acids and an excitation wavelength in a visible light region.Type: GrantFiled: July 24, 2000Date of Patent: May 7, 2002Assignee: Canon Kabushiki KaishaInventors: Tomohiro Suzuki, Tadashi Okamoto, Nobuko Yamamoto
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Patent number: 6376429Abstract: Benzoylcyclohexanediones of the formula (I), process for their preparation and their use as herbicides and plant growth regulators are described. In this formula (I), R11, R2, R3, R4, R5, R6 and R7 are various radicals, L is an alkylene chain, and Y and Z are a monoatomic bridge element.Type: GrantFiled: October 7, 1999Date of Patent: April 23, 2002Assignee: Hoechst Schering AgrEvo GmbHInventors: Andreas Van Almsick, Lothar Willms, Thomas Auler, Hermann Bieringer, Christopher Rosinger
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Patent number: 6376468Abstract: The invention pertains to novel peptide analogs suitable for inhibiting protein:prenyl transferases. As such they are therapeutically useful in e.g. inhibiting oncogenesis and other unwanted cell proliferation, and in supressing aberrant high signal transduction. The analogs comply with the following formula: in which: R1 is hydrogen or a thiol-protecting group; R2 and R3 are independently hydrogen or C1-C4 alkyl; R4 is hydrogen, C1-C4 alkyl, C1-C4 acyl or peptidyl; R5 is hydrogen or C1-C4 alkyl; R6 is hydrogen or optionally substituted C1-C6 alkyl; A is a direct bond or an optionally substituted C1-C4 alkylene chain; Y represents an oxo group or two hydrogen atoms; Z is oxygen, sulphur, imino or C1-C5 alkyl-, aryl- or acylimino; M is 0, 1 or 2; N is 0 or 1.Type: GrantFiled: February 3, 2000Date of Patent: April 23, 2002Assignees: Nederlandse Organisatie Voor Toegepast-Natuurwetenschappelijk Onderzoek TNO, Rijksuniversiteit LeidenInventors: Herman Steven Overkleeft, Steven Hendrik Leonard Verhelst, Nicolaas Johannes Meeuwenoord, Elsbet Jantine Pieterman, Louis Hartog Cohen, Mark Overhand, Gijsbert Arie Van der Marel, Jacobus Hubertus Van Boom
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Patent number: 6350431Abstract: This invention provides a physiologically tolerable light imaging contrast agent compound having a molecular weight in the range 500 to 5000000 and containing at least two chromophores having delocalized electron systems as well as at least one polyalkylene oxide (PAO) moiety having a molecular weight in the range 60 to 100000.Type: GrantFiled: October 28, 1999Date of Patent: February 26, 2002Assignee: Nycomed Imaging ASInventors: Robert Allen Snow, Paul Mark Henrichs, Daniel Joseph Delecki, William Anthony Sanderson, Vinay Chandrakant Desai, Edward Bacon, Kenneth Robert Hollister, Eric Paul Hohenschuh
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Patent number: 6337411Abstract: Compounds of the formula I are suitable for the production of pharmaceuticals for the prophylaxis and therapy of conditions whose course involves an increased activity of matrix-degrading enzymes, in particular stromelysin.Type: GrantFiled: December 15, 2000Date of Patent: January 8, 2002Assignee: Aventis Pharma Deutschland GmbHInventors: Cordula Hopmann, Martin Albert Knauf, Klaus-Ulrich Weithmann, Joachim Wink
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Publication number: 20010039287Abstract: A treatment process is disclosed that comprises administering an effective amount of an aromatic sulfone hydroxamic acid that exhibits excellent inhibitory activity of one or more matrix metalloprotease (MMP) enzymes, such as MMP-2, MMP-9 and MMP-13, while exhibiting substantially less inhibition at least of MMP-1 to a host having a condition associated with pathological matrix metalloprotease activity. Also disclosed are metalloprotease inhibitor compounds having those selective activities, processes for manufacture of such compounds and pharmaceutical compositions using an inhibitor.Type: ApplicationFiled: February 24, 1999Publication date: November 8, 2001Inventors: THOMAS E BARTA, DANIEL P BECKER, TERRI L BOEHM, GARY A DECRESCENZO, CLARA I WILLAMI1, JOSEPH J MCDONALD, JOHN N FRESKOS, DANIEL P GETMAN, GUNNAR J HANSON
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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: 6271399Abstract: Indane and indene compounds are described which are endothelin receptor antagonists.Type: GrantFiled: June 2, 1995Date of Patent: August 7, 2001Assignee: SmithKline Beecham CorporationInventors: Russell Donovan Cousins, John Duncan Elliott, Maria Amparo Lago, Jack Dale Leber, Catherine Elizabeth Peishoff
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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: 6057342Abstract: The present application describes amidinophenyl-pyrrolidines, -pyrrolines, and -isoxazolidines and derivatives thereof of formula I: ##STR1## or pharmaceutically acceptable salt forms thereof, wherein one of D and D' may be C(.dbd.NH)NH.sub.2 and the other H, and J.sup.1 and J.sup.2 may be O or CH.sub.2, which are useful as inhibitors of factor Xa.Type: GrantFiled: July 7, 1997Date of Patent: May 2, 2000Assignee: Dupont Pharmaceutical Co.Inventors: John Matthew Fevig, Donald Joseph Phillip Pinto, Mimi Lifen Quan, Petrus Fredericus Wilhelmus Stouten
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Patent number: 6040274Abstract: 2- Aroylcyclohexanediones I ##STR1## where X, Y=O or S;Ar=phenyl or heteroaryl in each case having 1-4 substituents: halogen, cyano, nitro, --N.dbd.N--Ph, C.sub.1 -C.sub.4 -alkoxycarbonyl, --N(R.sup.9)--COR.sup.10, --N(R.sup.9)--SO.sub.2 --R.sup.11, --SO.sub.2 --N(R.sup.9)R.sup.10, --S(O).sub.m --R.sup.8 or opt. subst. C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy, C.sub.1 -C.sub.4 -haloalkyl or C.sub.1 -C.sub.4 -haloalkoxy;two adjacent C atoms of the phenyl or heteroaryl ring can also be bridged by means of a chain --C(R.sup.12).dbd.C(R.sup.13)--C(R.sup.14).dbd.C(R.sup.15)--, --Z.sup.1 --C(R.sup.12).dbd.N--, --Z.sup.1 --N.dbd.C(R.sup.12)--, --Z.sub.1 --C(R.sup.12).dbd.C(R.sup.13)--, --Z.sup.1 --C(R.sup.12).dbd.C(R.sup.13)--C(R.sup.14,R.sup.15)--, --Z.sup.1 --C (R.sup.12,R.sup.13)--C(R.sup.14,R.sup.15)--, --Z.sup.1 --C(R.sup.12,R.sup.13)--C(R.sup.14 R.sup.15)--Z.sup.2 --, --C(R.sup.12,R.sup.13)--Z.sup.1 --C(R.sup.14,R.sup.15)--C(R.sup.16,R.sup.17)--, --Z.sup.1 --N(R.sup.20)--Z.sup.2 --, --Z.sup.1 --Z.sup.Type: GrantFiled: March 18, 1997Date of Patent: March 21, 2000Assignee: BASF AktiengesellschaftInventors: Jurgen Kast, Marcus Vossen, Wolfgang von Deyn, Stefan Engel, Regina Luise Hill, Uwe Kardorff, Martina Otten, Peter Plath, Helmut Walter, Karl-Otto Westphalen, Ulf Misslitz
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Patent number: 6015899Abstract: Products are described which can be obtained by reacting components a), b) and c), where component a) is a compound of the formula I or a mixture of compounds of the formula I, component b) is a compound of the formula II or a mixture of compounds of the formula II and component c) is a compound of the formula III or a mixture of compounds of the formula III, ##STR1## in which the general symbols are as defined in claim 1, the compound of the formula I being, for example, pentaerythritol, thiodiethylene glycol, 1,4-butanediol, 1,4-propanediol, diethylene glycol, triethylene glycol, diethanolamine or glycerol, the compound of the formula II being, for example, sunflower oil or coconut fat, and the compound of the formula III being, for example, methyl 3-(3',5'-di-tert-butyl-4'-hydroxyphenyl)propionate. The abovementioned products can be used as liquid antioxidants in polymers and lubricants.Type: GrantFiled: April 21, 1997Date of Patent: January 18, 2000Assignee: Ciba Specialty Chemicals CorporationInventors: Paul Dubs, Roger Martin, Samuel Evans
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Patent number: 5968908Abstract: The invention is novel analogs of 9-cis-retinoic acid which are useful for the treatment and prevention of coronary artery disease and to protect against premature atherosclerosis by increasing HDL levels. The invention includes processes for preparing the novel 9-cis-retinoic acid analogs.Type: GrantFiled: November 14, 1995Date of Patent: October 19, 1999Assignee: American Cyanamid CompanyInventors: Joseph William Epstein, Feng Ling Qing, Gary Harold Birnberg, Adam Matthew Gilbert
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Patent number: 5968962Abstract: A compound of the formula (I): ##STR1## or pharmaceutical acceptable salts thereof wherein X is NR.sub.1, S(O).sub.g, or O; R.sub.1 is H, C.sub.1-6 alkyl optionally substituted with one or more OH, CN, or halo, or R.sub.1 is --(CH.sub.2).sub.h -- aryl, --COR.sub.1--1, --COOR.sub.1-2, --CO--(CH.sub.2).sub.h --COR.sub.1--1, C.sub.1-6 alkyl sulfonyl, --SO.sub.2 --(CH.sub.2).sub.h --aryl, or --(CO).sub.i --Het; R.sub.2 is H, C.sub.1-6 alkyl, --(CH.sub.2).sub.h --aryl, or halo; R.sub.3 and R.sub.4 are the same or different and are H or halo; R.sub.5 is H, C.sub.1-12 alkyl optionally substituted with one or more halo, C.sub.3-12 cycloalkyl, C.sub.1-6 alkoxy. The compounds are useful antimicrobial agents.Type: GrantFiled: August 13, 1996Date of Patent: October 19, 1999Assignee: Pharmacia & Upjohn CompanyInventors: Richard C. Thomas, Toni-Jo Poel, Michael R. Barbachyn
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Patent number: 5932595Abstract: The present invention relates to compounds of Formula I: ##STR1## that are matrix metalloprotease inhibitors, pharmaceutical compositions containing them, methods for their use and methods of preparing these compounds.Type: GrantFiled: December 18, 1996Date of Patent: August 3, 1999Assignees: Syntex (U.S.A.) Inc., Agouron Pharmaceuticals, Inc.Inventors: Steven Lee Bender, Chris Allen Broka, Jeffrey Allen Campbell, Arlindo Lucas Castelhano, Lawrence Emerson Fisher, Robert Than Hendricks, Keshab Sarma
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Patent number: 5919950Abstract: Squarylium compounds of the formula: ##STR1## wherein Q.sup.1 and Q.sup.2 are each independently a pyrylium, thiopyrylium, selenopyrylium, benzpyrylium, benzthiopyrylium or benzselenopyrylium nucleus, and R.sup.1 and R.sup.2 are each independently an aliphatic or cycloaliphatic group, can be prepared by reacting a squaric acid derivative of the formula: ##STR2## with a compound of the formula Q.sup.2 CH.sub.2 R.sup.2 in the presence of a base.Type: GrantFiled: April 23, 1993Date of Patent: July 6, 1999Assignee: Polaroid CorporationInventors: Paulina P. Garcia, John W. Lee, John L. Marshall, Donald A. McGowan, Anthony J. Puttick, Thomas K. Spencer, Stephen G. Stroud, Stephen J. Telfer, Michael J. Zuraw
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Patent number: 5834508Abstract: A novel ketone derivative (I) which possesses a potent inhibitory activity against thiol protease such as papain, cathepsin B, cathepsin H, cathepsin L, calpain or the like with excellent properties regarding oral absorbance, tissue transference and cell membrane permeability, and are clinically useful in the treatment of various diseases such as muscular dystrophy, amyotrophy. Also provided are a process for producing the compound (I) and a pharmaceutical composition containing the same.Type: GrantFiled: February 6, 1997Date of Patent: November 10, 1998Assignee: Mitsubishi Chemical CorporationInventors: Ryoichi Ando, Naoko Ando, Hirokazu Masuda, Yasuhiro Morinaka, Chizuko Takahashi, Yoshikuni Tamao, Akihiro Tobe
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Patent number: 5789440Abstract: The present invention relates to novel 5,6-dihydropyrone derivatives and related structures which potently inhibit the HIV aspartyl protease blocking HIV infectivity. The 5,6-dihydropyrone derivatives are useful in the development of therapies for the treatment of bacterial and viral infections and diseases, including AIDS. The present invention is also directed to methods of synthesis of multifunctionalized 5,6-dihydropyrones and of related structures.Type: GrantFiled: October 12, 1994Date of Patent: August 4, 1998Assignee: Warner-Lambert CompanyInventors: Edmund Lee Ellsworth, Elizabeth Lunney, Bradley Dean Tait
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Patent number: 5767295Abstract: The invention provides an efficient process for producing a 2-substituted optically active 2,3-dihydro-4H-pyran-4-one comprising subjecting an aldehyde, which is not bulky and cannot be expected an electronic interaction with a catalyst, such as acetaldehyde, and a Danishefsky diene to a highly enantio-selective asymmetric hetero Diels-Alder reaction in the presence of an asymmetric catalyst readily obtainable from inexpensive starting materials.Type: GrantFiled: July 8, 1996Date of Patent: June 16, 1998Assignee: Kaneka CorporationInventors: Masura Mitsuda, Junzo Hasegawa
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Patent number: 5760073Abstract: The substituted 4H-pyrans are prepared by reacting either aldehydes or ylidene compounds with suitably substituted .beta.-diketones. The substituted 4H-pyrans according to the invention are suitable as active compounds in medicaments, in particular for the treatment of disorders of the central nervous system.Type: GrantFiled: August 7, 1996Date of Patent: June 2, 1998Assignee: Bayer AktiengesellschaftInventors: Klaus Urbahns, Hans-Georg Heine, Bodo Junge, Frank Mauler, Thomas Glaser, Reilinde Wittka, Jean-Marie-Viktor De Vry
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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: 5705527Abstract: An amino acid compound of the formula: R.sup.1 NH--CH(R.sup.2)--COHN--A--ONO.sub.2, wherein R.sup.1 represents a hydrogen atom, a C.sub.1 -C.sub.7 alkanoyl group, a C.sub.1 -C.sub.6 alkoxycarbonyl group, a C.sub.6 -C.sub.10 arylcarbonyl group, a C.sub.7 -C.sub.13 aralkylcarbonyl group, a C.sub.7 -C.sub.13 aralkyloxycarbonyl group or a 5- or 6-membered aromatic heterocyclic carbonyl group; R.sup.2 represents a substituted C.sub.1 -C.sub.6 alkyl group; and A represents a C.sub.2 -C.sub.5 alkylene group; and pharmacologically acceptable salts thereof. The amino acid compound has an excellent vasodilator action for collateral vessels and is useful for treating angina pectoris.Type: GrantFiled: April 20, 1995Date of Patent: January 6, 1998Assignee: Sankyo Company, LimitedInventors: Sadao Ishihara, Fujio Saito, Takao Yoshioka, Hiroyuki Koike, Shigeki Miyake, Hiroshi Mizuno
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Patent number: RE37035Abstract: Phenylacetic acid benzylamides having the following general structure wherein the substituents are defined herein, are disclosed, which compounds are hypoglcemic agents.Type: GrantFiled: October 7, 1997Date of Patent: January 30, 2001Assignee: Boehringer Ingelheim KGInventors: Wolfgang Grell, Rudolf Hurnaus, Gerhart Griss, Robert Sauter, Manfred Reiffen, Eckhard Rupprecht