Double Bond Between Ring Members Of The Lactone Ring Patents (Class 549/294)
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Patent number: 9790427Abstract: A liquid crystal compound is provided that satisfies at least one physical property, such as high stability to heat and light, a high clearing point (or high maximum temperature), a low minimum temperature of a liquid crystal phase, small viscosity, suitable optical anisotropy, large negative dielectric anisotropy, a suitable elastic constant and good compatibility with other liquid crystal compounds, a liquid crystal composition containing the compound, and a liquid crystal display device including the composition. The liquid crystal compound is represented by formula (1): in which, Ra and Rb are alkyl having 1 to 10 carbons; ring A1, ring A2 and ring A3 are 1,4-cyclohexylene, 1,4-phenylene; and ring N1 is 2,3-difluoro-1,4-phenylene; G is a divalent group represented by formula (pr-1) or (pr-2); in which, Z1, Z2, Z3 and Z4 are a single bond; and a, b and c are 0, 1 or 2.Type: GrantFiled: February 4, 2016Date of Patent: October 17, 2017Assignees: JNC CORPORATION, JNC PETROCHEMICAL CORPORATIONInventors: Teizi Satou, Sakura Tachinami
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Publication number: 20150087846Abstract: A lifestyle disease improving drug that enhances PPAR?, ? and ? agonist activities that includes a compound having the lactone structure in accordance with the chemical formula 6-alkyl-5,6-dihydro-2H-pyran-2-one, the alkyl containing 4, 5, or 6 carbons, and a method for synthesizing the compound. The method includes adding, stepwise, a butyllithium-hexane solution to a diisopropylamine-tetrahydrofuran solution, and then a 6-alkyltetrahydro-2H-pyran-2-one-tetrahydrofuran solution, wherein the alkyl contains 4, 5, or 6 carbons, adding a phenylselenyl choloride-tetrahydrofuran solution to produce a reaction mixture with a phenylselenide, extracting and purifying the phenylselenide, preparing a phenylselenide-tetrahydrofuran solution with the purified phenylselenide, and adding sodium bicarbonate and an aqueous hydrogen peroxide solution to the phenylselenide-tetrahydrofuran solution to produce a reaction mixture including the compound.Type: ApplicationFiled: March 21, 2013Publication date: March 26, 2015Inventor: Munekazu Iinuma
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Publication number: 20130316408Abstract: The invention discloses marine Streptomyces sp., a Pyranosesquiterpene compound, as well as a preparation method and uses thereof. Streptomyces sp. SCSIO 01689 was collected in China Center for Type Culture Collection (CCTCC) (Address: Wuhan University, Wuhan City, China) with the collection number of CCTCC NO: M 2011257 on Jul. 18, 2011. The Streptomyces sp. SCSIO 01689 can produce the Pyranosesquiterpene compound with better anti-Escherichia coli activity and anti-Artemia activity, as well as Cyclo(D)-Pro-(D)-Ile, Cyclo(D)-Pro-(D)-Leu and Cyclo(D)-trans-4-OH-Pro-(D)-Phe with better anti-Vibrio anguillarum activity and anti-Artemia activity, thereby providing a new way for preparing the Cyclo(D)-Pro-(D)-Ile, the Cyclo(D)-Pro-(D)-Leu and the Cyclo(D)-trans-4-OH-Pro-(D)-Phe. The Pyranosesquiterpene compound can be used for preparing anti-Escherichia coli medicaments and anti-Artemia medicaments, as well as preparing condiments as a condiment precursor compound.Type: ApplicationFiled: June 18, 2012Publication date: November 28, 2013Applicant: South China Sea Institute Of Oceanology, Chinese Academy of SciencesInventors: Lijuan Long, Xinpeng Tian, Jie Li, Xiongming Luo, Zhenxiong Qi, Tuan Yin
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Publication number: 20130310450Abstract: The present invention discloses a compound separated from Monascus-fermented rice, the preparation method and uses thereof. Specifically, the present invention discloses a compound represented by the Formula I, or a pharmaceutically acceptable salt thereof, wherein, R1 is selected from the group consisting of hydrogen, hydroxyl, C1-6 straight or branched alkoxyl, (II), (III) and (IV); R2 is hydrogen or C1-6 alkyl; R3 is selected from the group consisting of hydrogen, hydroxyl and C1-6 straight or branched alkoxyl. The present invention further discloses a pharmaceutical composition containing the compound. The compound of the present invention has HMG-CoA reductase inhibition effects.Type: ApplicationFiled: January 10, 2012Publication date: November 21, 2013Applicant: Beijing Peking University WBL Biotech Co., LtdInventors: Zhenwen Duan, Shuren Guo, Xuemei Li, Chunli Liu
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Publication number: 20120215013Abstract: The invention provides a hydrogen storage material comprising a porous carbon material having oxygen-containing functional groups on the surface, and Li bonded to the surface of the porous carbon material. The hydrogen storage material of the invention has more excellent hydrogen storage capacity than the prior art.Type: ApplicationFiled: September 14, 2010Publication date: August 23, 2012Applicant: JX NIPPON OIL & ENERGY CORPORATIONInventors: Ai Minoda, Shinji Oshima, Daisuke Watanabe
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Publication number: 20120190870Abstract: Antitumoral compounds obtained from a porifera, of the family Raspailiidae, genus Lithoplocamia, species lithistoides, and derivatives thereof are provided.Type: ApplicationFiled: June 29, 2011Publication date: July 26, 2012Inventors: Ma Jesús Martín López, Laura Coello Molinero, José Fernando Reyes Benítez, Alberto Rodríguez Vicente, María Garranzo García- Ibarrola, Carmen Murcia Pérez, Andrés Francesch Solloso, Francisco Sánchez Sancho, María del Carmen Cuevas Marchante, Rogelio Fernández Rodríguez
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Publication number: 20120065171Abstract: Novel Fostriecin (or FST) derivatives represented by formula (I), the pharmaceutical compositions and preparation methods thereof. The pharmaceutical uses of these compounds, especially the use for the preparation of pharmaceutical compositions for treating tumor, inhibiting cell over growth, or lowering myocardial infarction and the injury to cells.Type: ApplicationFiled: October 1, 2010Publication date: March 15, 2012Applicants: Dalian University of Technology, BayGen Pharm Technology Co., Ltd.Inventors: Li Tang, Rongguo Qiu
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Patent number: 8093409Abstract: The present invention provides a method for producing a cyclic unsaturated compound, which sufficiently suppresses generation of acyclic unsaturated compounds and permits excellent yield and reaction rate. Such a method for producing a cyclic unsaturated compound is a method for producing a cyclic unsaturated compound by reacting an ?,?-unsaturated carboxylic acid with an unsaturated organic compound, wherein the method comprises a step of reacting the ?,?-unsaturated carboxylic acid with the unsaturated organic compound in the presence of a catalyst.Type: GrantFiled: August 22, 2007Date of Patent: January 10, 2012Assignee: Nippon Shokubai Co., Ltd.Inventor: Koji Yonehara
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Patent number: 8003687Abstract: Esters of compounds in the leptomycin family, having a structure according to formula I where R, R10, R11, R12, R13, and R14 are as defined herein, exhibit anti-tumor properties.Type: GrantFiled: September 11, 2006Date of Patent: August 23, 2011Assignee: Kosan Biosciences IncorporatedInventors: Steven D. Dong, Daniel V. Santi
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Publication number: 20110178169Abstract: The present invention refers to the use of HMP (a secondary metabolite obtained from Aspergillus fungi) as an agent that intensifies the mechanism of macrophage activation, leading to the death of L. (Leishmania) amazonensis, the etiologic agent of cutaneous leishmaniasis. The main mechanism of action of this agent is the activation of the microbicidal activity of host cells, through increased superoxide production, number of lysosomes, actin and microtubule filament polymerization and increased spreading, typical of activated cells. Additionally, HMP represents a molecule of easy acquisition, presents an efficient combat mechanism with no adverse reactions and capacity to inhibit the development of promastigotes and amastigotes forms. Finally, results suggest HMP to be a potential candidate for use against cutaneous leishmaniasis at a minimal concentration of 50 ?g/mL.Type: ApplicationFiled: August 14, 2009Publication date: July 21, 2011Inventors: Alberdan Silva Santos, Edilene Oliveira Da Silva, Jose Luiz Martins do Nascimento, Claudio Naum Alves, Ana Paul Drumond Rodrigues, Antonio Sergio da Costa Carvalho
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Publication number: 20100222382Abstract: Esters of compounds in the leptomycin family, having a structure according to formula I where R, R10, R11, R12, R13, and R14 are as defined herein, exhibit anti-tumor properties.Type: ApplicationFiled: September 11, 2006Publication date: September 2, 2010Applicant: Kosan Biosciences IncorporatedInventors: Steven D Dong, Daniel V. Santi
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Publication number: 20090299009Abstract: The present invention provides a method for producing a cyclic unsaturated compound, which sufficiently suppresses generation of acyclic unsaturated compounds and permits excellent yield and reaction rate. Such a method for producing a cyclic unsaturated compound is a method for producing a cyclic unsaturated compound by reacting an ?,?-unsaturated carboxylic acid with an unsaturated organic compound, wherein the method comprises a step of reacting the ?,?-unsaturated carboxylic acid with the unsaturated organic compound in the presence of a catalyst.Type: ApplicationFiled: August 22, 2007Publication date: December 3, 2009Applicant: Nippon Shokubai Co., Ltd.Inventor: Koji Yonehara
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Patent number: 7622498Abstract: Pesticidal compounds of general formula (I) Wherein ?represents a double bond; A— represents ?C(R5)—C(?O)—, wherein R represents hydrogen or halogen, R1 and R2 represent, independently, hydrogen, halogen, alkoxy, substituted alkoxy or an ester group; or R1 and R2, together with the carbon atoms to which they are attached, represent an oxirane ring; or R1 and R2, taken together, represent an alkylidenedioxy or substituted alkylidenedioxy group; and R3 represents —CH2R6, wherein R6 represents an ester group, oxiranyl, or a group of formula wherein R7 represents hydrogen or alkyl, R8 represents phenylsulfanyl, phenylselenyl, phenylsulfoxy or phenylselenoxy, and R9 represents hydrogen, ethoxycarbonyl or carbamoyl and R4 represents, independently, hydrogen, alkoxy or substituted alkoxy; and methods of making the compounds of formula (I) and methods for controlling pests wherein the pest dies as a result of contact with a compound of formula (I).Type: GrantFiled: August 3, 2007Date of Patent: November 24, 2009Assignees: Instituto Politecnico de Santarem/Escoal Superior Agraria, Faculdade de Ciencias da Universidade de Lisboa, University of NewcastleInventors: Jorge Alberto Guerra Justino, Amelia Pilar Grases Santos Silva Rauter, Tana Lukeba Canda, Richard Wilkins
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Patent number: 7405309Abstract: The invention relates to pyranone derivatives of general formula (I), wherein X is chlorine, bromine or iodine and R1 and R2 is independently a hydrogen atom, an alkyl, cycloalkyl or alkylene, linear or branched group containing 1-20 carbon atoms, optionally substituted by a hydroxyl, amino, ether or halogen group, or R1 and R2 form together a cycle of 5, 6, 7 or 8 members which is optionally substituted by a hydroxyl, amino, ether or halogen group including isomers, enantiomers, diastereoisomers and the mixtures thereof. A method for preparing the inventive derivatives and the therapeutic use thereof, in particular for treating cancer, are also disclosed.Type: GrantFiled: January 14, 2005Date of Patent: July 29, 2008Assignee: Centre National de la Recherche Scientifique (CNRS)Inventors: Joanna Bakala, Denyse Herlem, Emile Benechie, Jérôme Bignon, Françoise Khuong-Huu, Guy Jean Marie Potier, legal representative, Marie-Claude Denise Michèle Zelveyan, legal representative, Catherine Marie Germaine Magnan, legal representative, Odette Drion, legal representative, Pierre Potier
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Patent number: 7314943Abstract: The invention relates to pyran derivatives of formula I and processes and intermediates for their preparation and derivatisation, and the use thereof in liquid-crystalline media.Type: GrantFiled: May 25, 2004Date of Patent: January 1, 2008Assignee: Merck Patent GmbHInventors: Eike Poetsch, Volker Meyer, Werner Binder, Michael Heckmeier, Georg Luessem, Stephan Guertler
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Patent number: 7256158Abstract: The invention relates to new phenyl-substituted cyclic ketoenols of the formula (I) in which Het represents one of the groups ?wherein A, B, D, G, X, Y and Z have the meaning given in the description, several processes and intermediate products for their preparation and their use as pest control agents and herbicides.Type: GrantFiled: August 20, 2004Date of Patent: August 14, 2007Assignee: Bayer AGInventors: Folker Lieb, Hermann Hagemann, Arno Widdig, Michael Ruther, Reiner Fischer, Thomas Bretschneider, Christoph Erdelen, Ulrike Wachendorff-Neumann, Peter Dahmen, Markus Dollinger, Hans Joachim Santel, Alan Graff, Norbert Mencke, Andreas Turberg
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Patent number: 6870058Abstract: Compounds which mimic the chemical and/or biological activity of discodermolide are provided and intermediates useful in their preparation.Type: GrantFiled: December 6, 2000Date of Patent: March 22, 2005Assignee: The Trustees of the University of PennsylvaniaInventors: Amos B. Smith, III, Thomas J. Beauchamp, Matthew J. LaMarche
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Patent number: 6855822Abstract: Benzo[b]furan dimers and processes for their preparation are provided. The invention provides a synthetic process for the preparation of benzo[b]furan dimer using mild reaction conditions, which provides a high substituent tolerance and is appropriate for use in solid phase syntheses for producing a library of benzo[b]furan dimers for biological screening.Type: GrantFiled: June 23, 2003Date of Patent: February 15, 2005Assignee: VivoQuest, Inc.Inventors: Yun Liao, Reza Fathi, Zhen Yang
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Patent number: 6828276Abstract: There are described benzoylcyclohexanediones of the formula I, their preparation, and their use as herbicides and plant growth regulators. In this formula (I), C1, C2, C3 are cyclic radicals, X1 is a hetero atom, X2 is a chain of carbon atoms, L is a chain-like element, R1, R2, R3, R4, R5 are various radicals, and Y and Z are monoatomic bridge elements.Type: GrantFiled: August 30, 2001Date of Patent: December 7, 2004Assignee: Aventis CropScience GmbHInventors: Thomas Seitz, Andreas van Almsick, Lothar Willms, Hermann Bieringer, Thomas Auler, Hubert Menne
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Patent number: 6756013Abstract: The present invention provides a composition having biological activity. The composition includes from about 10 ppm to about 5000 parts iodonium salt. The composition also includes from about 100 ppm to about 300,000 ppm of a compound to act as a carrier of the iodonium compound. The carrier is selected from at least one of polyvinyl alcohols, polyvinyl acetates, polyethylene glycols, ethylene glycol and propylene glycol block copolymers, cellulosic polymers, polyesters, alkyd polymers. The composition also includes from about 50 ppm to about 50,000 ppm of a compound to render the composition compatible with a surface being treated. This component is selected from at least one of di-acids, acid anhydrides, polyfunctional acids, di-ethylene glycol, resorcinol and the like. The composition also includes an appropriate vehicle selected from at least one of water, acidified water, paint, primer, and petroleum distillates.Type: GrantFiled: August 14, 2000Date of Patent: June 29, 2004Assignee: Cornell Development Corporation, LLCInventors: Stephen W. Cornell, David D. Cornell, Paul W. Cornell
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Patent number: 6743927Abstract: The present invention relates to a novel process for producing a &dgr;-lactone of the formula: using an acyl halide of the formula: wherein R1, R2 R3 and X are described herein, as well as novel intermediates. In particular, the present invention relates to a process for enantioselectively producing the (R)-&dgr;-lactone.Type: GrantFiled: February 10, 2003Date of Patent: June 1, 2004Assignee: Roche Colorado CorporationInventors: Michael P. Fleming, Yeun-Kwei Han, Lewis M. Hodges, David A. Johnston, Roger P. Micheli, Kurt Puentener, Chris R. Roberts, Michelangelo Scalone, Mark A. Schwindt, Robert J. Topping
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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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Publication number: 20030236302Abstract: This invention features a 5,6-dihydro-2-pyrone compound of formula (I), wherein R1 is H, OH, or C2˜C5 alkoxyl; and R2 is 2-phenyl ethyl, 2-phenyl ethenyl, 2-heteroaryl ethyl, or 2-heteroaryl ethenyl; in which the phenyl or the heteroaryl is optionally mono-, di-, or tri-substituted with R3, R4, or R5; each of R3, R4, and R5, independently, is Cl, F, Br, I, CN, C1˜C5 alkyl, C1˜C5 alkoxyl, C3˜C5 alkenyloxy, C4˜C6 cycloalkoxyl, C4˜C8 cycloalkyl alkoxyl, C3˜C5 alkoxy alkoxyl, or C1˜C4 alkoxy carbonyl.Type: ApplicationFiled: February 27, 2003Publication date: December 25, 2003Inventors: Shoujun Chen, Lijun Sun, Joel McCleary
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Patent number: 6589984Abstract: There is provided benzofuryl-&agr;-pyrone derivative represented by the following structural formula (I): wherein R1 represents a hydrogen atom or an alkyl group of 1 to 5 carbons; R2 represents hydrogen, —CO—R5 or —SO2R6; R3 represents hydrogen, an alkyl group of 1 to 5 carbons, etc.; and R4 is a substituent attached to the 4-carbon, 5-carbon, 6-carbon or 7 carbon of the benzofuran ring; and their salts. The compounds are useful as therapeutic agent for hypertriglyceridemia, lipid metabolism enhancers, or prophylactic and/or therapeutic agents for arteriosclerosis.Type: GrantFiled: September 11, 2000Date of Patent: July 8, 2003Assignees: Teijin Limited, Microbial Chemistry Research FoundationInventors: Yoshimitsu Naniwa, Hiroshi Imai, Tomohide Ida, Emiko Muratani, Kazuo Kitai, Yoshinori Sugimoto, Tomomi Kosugi, Akiko Takeuchi, Kunihito Watanabe, Takami Tomiyama, Tomio Takeuchi, Masa Hamada
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Patent number: 6545165Abstract: The present invention relates to a novel process for producing a &dgr;-lactone of the formula: using an acyl halide of the formula: wherein R1, R2 R3 and X are described herein, as well as novel intermediates. In particular, the present invention relates to a process for enantioselectively producing the (R)-&dgr;-lactone.Type: GrantFiled: September 22, 2000Date of Patent: April 8, 2003Assignee: Roche Colorado CorporationInventors: Michael P. Fleming, Yeun-Kwei Han, Lewis M. Hodges, David A. Johnston, Roger P. Micheli, Kurt Puentener, Chris R. Roberts, Michelangelo Scalone, Mark A. Schwindt, Robert J. Topping
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Patent number: 6518303Abstract: 2-Phenylpyran-4-one derivatives of formula (I): wherein: R1 represents an alkyl or —NR4R5 group, wherein R4 and R5 each independently represents a hydrogen atom or an alkyl group; R2 represents an alkyl, C3-C7 cycloalkyl, pyridyl, thienyl, naphthyl, tetrahydronaphthyl or indanyl group, or a phenyl group which may be unsubstituted or substituted by one or more halogen atoms or alkyl, trifluoromethyl, hydroxy, alkoxy, methylthio, amino, mono- or dialkylamino, hydroxalkyl or hydroxycarbonyl groups; R3 represents a methyl, hydroxymethyl, alkoxymethyl, C3-C7 cycloalkoxymethyl, benzyloxymethyl, hydroxycarbonyl, nitrile, trifluoromethyl or difluoromethyl group or a CH2—R6 group wherein R6 represents an alkyl group; and X represents a single bond, an oxygen atom, a sulfur atom or a methylene group; or pharmaceutically acceptable salts thereof, processes for their production and synthetic intermediates used in said processes, pharmaceutical compositions containing them and their useType: GrantFiled: March 16, 2001Date of Patent: February 11, 2003Assignee: Almirall Prodesfarma S.A.Inventors: Maria Isabel Crespo Crespo, Juan Miguel Jimenez Mayorga, Carles Puig Duran, Lidia Soca Pueyo
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Patent number: 6465509Abstract: The invention encompasses the novel compounds of Formula I, which are useful in the treatment of cyclooxygenase-2 mediated diseases. The invention also encompasses certain pharmaceutical compositions comprising compounds of Formula I as well as methods of treating cyclooxygenase-2 mediated diseases comprising administering to a patient in need of such treatment a non-toxic therapeutically effective amount of a compound of Formula I.Type: GrantFiled: June 27, 2001Date of Patent: October 15, 2002Assignee: Merck Frosst Canada & Co.Inventors: Chun-Sing Li, Cheuk Kun Lau, Michel Therien, Petpiboon Prasit
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Patent number: 6255276Abstract: The invention is concerned with odorant compositions which contain macrocycles, namely 15- to 17-membered compounds of the formula: wherein the dotted line signifies an optional additional bond, X and Y stand for methylene or C2-12-polymethylene, optionally substituted with an additional methyl group, and A signifies hydrogen or methyl in the case of the unsaturated compounds and methyl in the case of the saturated compounds, with the proviso that the unsaturated compounds are present to more than 80% in the cis form when A signifies hydrogen and are present to more than 50% in the cis form when A signifies methyl, with the exception of Z-oxacyclopentadec-6-en-2-one (15-membered ring), Z-oxacycloheptadec-8-en-2-one (17-membered ring), and Z-oxacycloheptadec-11-en-2-one (17-membered ring), a process for the manufacture of the compounds of formula I and the use of the compounds of formula I as odorants.Type: GrantFiled: February 16, 2000Date of Patent: July 3, 2001Assignee: Givauden Roure (International) S.A.Inventors: Georg Frater, Daniel Helmlinger, Urs Müller
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Patent number: 6242616Abstract: Synthetic methods for lactone-containing compounds such as the discodermolides are provided, as are compounds which mimic the chemical and/or biological activity thereof, and methods and intermediates useful in their preparation.Type: GrantFiled: December 7, 1999Date of Patent: June 5, 2001Assignee: The Trustees of the University of PennsylvaniaInventors: Amos B. Smith, III, Thomas J. Beauchamp, Matthew J. LaMarche, Hirokazu Arimoto
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Patent number: 6239291Abstract: The present invention provides convergent processes for preparing myxopyronins and corallopyronins, compounds useful as antibacterial therapeutics. The present invention also provides novel compositions of matter which are useful for the preparation of pyronin antibiotics.Type: GrantFiled: May 18, 2000Date of Patent: May 29, 2001Assignees: Scriptgen Pharmaceuticals, Inc., Trustees of Boston UniversityInventors: Mark A. Wuonola, Gary R. Gustafson, James S. Panek, Tao Hu, Jennifer V. Schaus
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Patent number: 6211386Abstract: The present invention is a process for the preparation of a compound of the formula: where R3, R4 and n are defined in the specification which comprises hydrogenating a compound of the formula: the E-geometrical isomer thereof or a mixture of the Z- and E-isomers in the presence of catalyst containing Rh, a chiral ligand with at least one phosphorous atom where the hydrogenation is conducted in the presence of a base.Type: GrantFiled: March 14, 2000Date of Patent: April 3, 2001Assignee: Pharmacia & Upjohn CompanyInventors: Mark J. Burk, Nicholas B. Johnson, Bradley D. Hewitt
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Patent number: 6191288Abstract: The present invention provides convergent processes for preparing myxopyronins and corallopyronins, compounds useful as antibacterial therapeutics. The present invention also provides novel compositions of matter which are useful for the preparation of pyronin antibiotics.Type: GrantFiled: September 15, 1999Date of Patent: February 20, 2001Assignee: Anadys Pharmaceuticals, Inc.Inventor: P. Siva Ramamoorthy
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Patent number: 6127551Abstract: The present invention provides convergent processes for preparing myxopyronins and corallopyronins, compounds useful as antibacterial therapeutics. The present invention also provides novel compositions of matter which are useful for the preparation of pyronin antibiotics.Type: GrantFiled: August 9, 1999Date of Patent: October 3, 2000Assignees: Scriptgen Pharmaceuticals, Inc., Trustees of Boston UniversityInventors: Mark A. Wuonola, Gary R. Gustafson, James S. Panek, Tao Hu, Jennifer V. Schaus
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Patent number: 6060507Abstract: Massoialactone is useful for preventing or at least inhibiting growth of a fungus. Accordingly, a fungicidal composition has massoialactone as an active antifungal compound together with an agronomically acceptable carrier therefor. Additional antifungal ingredients can be added to the composition. The composition can be applied to surfaces, including surfaces of plants and plant parts, such as seeds.Type: GrantFiled: August 28, 1997Date of Patent: May 9, 2000Assignee: Horticulture and Food Research Institute of New Zealand LimitedInventors: Robert Anthony Hill, Horace G. Cutler, Stephen Robert Parker
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Patent number: 5942631Abstract: The present invention provides novel haloenol lactones that are effective as active site inhibitors of cholesterol esterase. By inhibiting cholesterol esterase the inhibitors of the present invention provide a new approach to the treatment of hypercholesterolemia through limiting the bioavailability of dietary cholesterol.Type: GrantFiled: April 15, 1998Date of Patent: August 24, 1999Assignee: University Of New MexicoInventors: Lorraine Deck, David L. Vander Jagt
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Patent number: 5808062Abstract: The present invention relates to novel tri- and tetrasubstituted pyrones and related structures which potently inhibit the HIV aspartyl protease blocking HIV infectivity. The pyrone 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 pyrones and of related structures.Type: GrantFiled: October 12, 1994Date of Patent: September 15, 1998Assignee: Warner-Lambert CompanyInventors: John Michael Domagala, Edmund Lee Ellsworth, Elizabeth Lunney, Daniel Fred Ortwine, Kimberly Suzanne Para, Josyula Venkata Nagendra Vara Prasad, Tomi Sawyer, Bradley Dean Tait
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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: 5767147Abstract: This invention relates to novel haloenol lactone compounds. These compounds have the following general structure: ##STR1## in which Ar is an aryl group and Y is a haloenol lactone moiety. The compounds of the invention are useful for the specific measurement of particular isoenzymes of glutathione S-transferase. Measurement of glutathione S-transferase isoenzymes has importance in diagnostic medicine. The compounds of the invention are also useful for treatment of drug resistance in cancer and for preventing herbicide resistance in plants.Type: GrantFiled: April 21, 1995Date of Patent: June 16, 1998Assignee: The Regents of the University of CaliforniaInventors: A. Daniel Jones, Alyson E. Mitchell, Bruce D. Hammock, Jiang Zheng
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Patent number: 5731293Abstract: A compound of the formula (I): ##STR1## wherein R.sup.1 and R.sup.2 are, independently, --CON(R.sup.4)R.sup.5, or a monosaccharide, or acylated monosaccharide group, with the proviso that at least one of R.sup.1 and R.sup.2 is --CON(R.sup.4)R.sup.5, and R.sup.4 and R.sup.5 are, independently, a hydrogen atom, or a hydroxyl, alkyl, aryl, or aralkyl group, or R.sup.4 and R.sup.5 together with the nitrogen atom attached thereto form a 3- to 7-membered saturated cycloaliphatic amino group, and R.sup.3 is a hydrogen atom, or a hydroxyl, alkyl, aryl, aralkyl, or --COOR.sup.8 group, and R.sup.3 is at 3- or 4-position, and R.sup.8 is a hydrogen atom or an alkyl group, or a salt thereof is disclosed. The compound has a function to inhibit a matrix metalloproteinase.Type: GrantFiled: December 28, 1995Date of Patent: March 24, 1998Assignee: Kureha Chemical Industry Co., Ltd.Inventors: Koju Watanabe, Koichi Niimura, Toru Yamazaki, Hiroshi Maruoka
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Patent number: 5481008Abstract: A catalytic process for the manufacture of optically active compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2 are alkyl, which is optionally interrupted by an O atom in a position other than the .alpha.-or .beta.-position, or optionally substituted benzyl,R.sup.3 is hydrogen, lower alkyl, optionally substituted benzyl, --CO--R.sup.4, --COOR.sup.4 or --CONR.sub.2.sup.4, andR.sup.4 is lower alkyl or aryl,comprising asymmetrically hydrogenating a compound of the formula ##STR2## wherein R.sup.1, R.sup.2 and R.sup.3 have the above significance, in the presence of a complex of an optically active, preferably atropisomeric, diphospine ligand with a metal of Group VIII.Type: GrantFiled: August 31, 1994Date of Patent: January 2, 1996Assignee: Hoffmann-La Roche Inc.Inventors: Emil A. Broger, Martin Karpf, Ulrich Zutter
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Patent number: 5420305Abstract: A process for the preparation of a tautomeric mixture of compounds of the formulas ##STR1## wherein W is hydrogen or C.sub.6 H.sub.13, which comprises treating a compound of the formula ##STR2## wherein R is unsubstituted or substituted alkoxy, arylalkoxy, aryloxy or amine and R.sup.1 is hydrogen or when R is alkoxy, substituted alkoxy, substituted amine, unsubstituted or substituted arylalkoxy R.sup.1 can also be metal, with a compound of the formula ##STR3## wherein W is as described above, both X and Y are reducible groups or X is hydrogen and Y is a reducible group or Y is hydrogen and X is a reducible group and, Z is hydroxy or a leaving group to form the compound of formula IV ##STR4## wherein W, X, Y and R are as defined above, the compound of formula IV is treated with a low valent metal to form a tautomeric mixture of compounds of formulas I and Ia, which are useful in the synthesis of tetrahydrolipstatin.Type: GrantFiled: October 4, 1993Date of Patent: May 30, 1995Assignee: Hoffmann-La Roche Inc.Inventors: Keith M. Ramig, John J. Landi, Jr.
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Patent number: 5360918Abstract: A method for controlling insects using nitrophenyl pyrones is described. The pyrones are preferably derived from Streptomyces sp. by a method involving growth and extraction of the pyrones. A novel pyrone, griseulin is also described.Type: GrantFiled: November 22, 1993Date of Patent: November 1, 1994Assignee: Board of Trustees operating Michigan State UniversityInventor: Muraleedharan G. Nair
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Patent number: 5314911Abstract: The present invention relates to a compound represented by the formula I: ##STR1## which was isolated from the culture of Streptomyces prunicolor PA-48153 and has biological activity such as immunosuppressive activity, antitumor activity and antifungal activity.Type: GrantFiled: March 12, 1993Date of Patent: May 24, 1994Assignee: Shionogi Seiyaku Kabushiki KaishaInventors: Tadashi Yoshida, Kenzo Koizumi, Yoshimi Kawamura, Koichi Matsumoto, Hiroshi Itazaki
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Patent number: 5292891Abstract: There are provided novel and optically active 2,2-dimethyl-1,3-dioxin-4-ones which are useful as starting materials for physiologically active compounds, functional materials or the like. Provided are optically active 5,6-epoxyhexanoic acid esters and novel optically active 6-substituted tetrahydropyran-2-one derivatives.Type: GrantFiled: December 15, 1992Date of Patent: March 8, 1994Assignee: Chisso CorporationInventors: Chikara Kaneko, Masayuki Sato
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Patent number: 5256800Abstract: There are provided novel and optically active 2,2-dimethyl-1,3-dioxin-4-ones which are useful as starting materials for physiologically active compounds, functional materials or the like. Furthermore, a method for preparing an optically active compound comprises reacting a racemic 1,3-dioxin-4-one with vinylacetate in the presence of lipase to resolve the racemic compound into optically active compound represented by the formula (3) ##STR1## and an optically active compound represented by the formula (4) ##STR2## which is an antipode of the compound represented by the formula (3).Type: GrantFiled: February 18, 1992Date of Patent: October 26, 1993Assignee: Chisso CorporationInventors: Chikara Kaneko, Masayuki Sato
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Patent number: 5106407Abstract: The present invention discloses the antimicrobial utility of certain iodonium ylide compounds. The particular iodonium ylide compounds are phenyl iodonium ylides having an ortho substituent that stabilizes the positive charge on the polyvalent iodine by a nonbonded electrostatic interaction. The polyvalent iodine is further stabilized by a cyclic 1,3-dicarbonyl anion.Type: GrantFiled: December 4, 1989Date of Patent: April 21, 1992Assignee: The Dow Chemical CompanyInventors: Attila G. Relenyi, Gerald F. Koser, Richard W. Walter, Jr., William J. Kruper, Jr., Ravi B. Shankar, Anthony P. Zelinko
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Patent number: 5091533Abstract: Compounds of the formula: ##STR1## where R.sup.2 contains certain aryls or heteroaryls are effective leukotriene inhibitors.Type: GrantFiled: March 12, 1990Date of Patent: February 25, 1992Assignee: Merck Frosst Canada, Inc.Inventors: Patrice C. Belanger, Claude Dufresne, Brian Fitzsimmons, deceased, Maryann Fitzsimmons, Heir, Yvan Guindon, Cheuk K. Lau, Joshua Rokach, John Schiegetz, Michel Therien, Robert N. Young
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Patent number: 5011944Abstract: .alpha.-Pyrones of the formula I ##STR1## in which R.sup.1 is --CF.sub.3 or --COOR.sup.3 and R.sup.3 is the radical of a C.sub.1 -C.sub.18 alcohol diminished by a hydroxyl group, and R.sup.2 is --F, --Br, --Cl, --CN, --CF.sub.3, C.sub.1 -C.sub.18 alkyl, C.sub.2 -C.sub.18 alkenyl, C.sub.2 -C.sub.18 alkynyl, C.sub.1 -C.sub.18 alkoxy, C.sub.1 -C.sub.18 alkylthio, C.sub.1 -C.sub.18 alkylsulfonyl, C.sub.6 -C.sub.16 aryl, C.sub.7 -C.sub.24 alkaryl, C.sub.7 -C.sub.12 aralkyl, C.sub.8 -C.sub.24 alkaralkyl, C.sub.6 -C.sub.16 aryloxy, C.sub.6 -C.sub.16 arylthio, C.sub.6 -C.sub.16 arylsulfonyl, C.sub.7 -C.sub.24 alkaryloxy, C.sub.7 -C.sub.24 alkarylthio, C.sub.7 -C.sub.24 alkarylsulfonyl, C.sub.7 -C.sub.12 aralkyloxy, C.sub.7 -C.sub.12 aralkylthio, C.sub.7 -C.sub.12 aralkylsulfonyl, C.sub.8 -C.sub.24 alkaralyloxy, C.sub.8 -C.sub.24 alkaralylthio, C.sub.8 -C.sub.24 alkaralylsulfonyl, secondary amine having 2 to 24 C atoms or trialkylsilyl or trialkoxysilyl each of which has 3 to 18 C atoms.Type: GrantFiled: May 24, 1989Date of Patent: April 30, 1991Assignee: Ciba-Geigy CorporationInventors: Vratislav Kvita, Marcus Baumann, Walter Fischer, Carl W. Mayer, Thomas Allmendinger
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Patent number: 5004814Abstract: The invention relates to .alpha.-pyrones of formula I ##STR1## wherein R.sup.1 is chloro or bromo and R.sup.2 is hydrogen, chloro or bromo. The halogen in 4-position can be replaced, for example, by alkoxy, alkylthio or secondary amino. The .alpha.-pyrones are suitable diene components for Diels-Alder reactions.Type: GrantFiled: October 16, 1989Date of Patent: April 2, 1991Assignee: Ciba-Geigy CorporationInventor: Vratislav Kvita
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Patent number: 4918100Abstract: A purified isolate of an actinomycete identified as ATCC 39366 is capable of producing the anti-microbial compound CL-1957B which also exhibits antitumor properties.The antimicrobial compound CL-1957B is produced by cultivating isolate ATCC 39366 under aerobic conditions in a culture medium containing assimilable sources of carbon and nitrogen until a substantial quantity of the CL-1957B compound is produced, and subsequently isolating the compound.The antibiotic compound CL-1957B, its pharmaceutically acceptable salts, the pharmaceutical compositions comprising this substance together with a pharmaceutically acceptable carrier is also disclosed, as are methods of treating microbial infections and tumors in mammals, employing these pharmaceutical compositions.Type: GrantFiled: August 8, 1985Date of Patent: April 17, 1990Assignee: Warner-Lambert CompanyInventors: Gerard C. Hokanson, John P. Schaumberg, James C. French, Josefino B. Tunac