The -c(=x)- Is Part Of A -c(=x)x- Group, Wherein The X's Are The Same Or Diverse Chalcogens Patents (Class 549/549)
  • Patent number: 11407708
    Abstract: The present invention aims to provide a means by which a cured product to be obtained has a low dielectric loss tangent and higher heat resistance. Specifically, provided are an active ester compound represented by chemical formula (1): (where in chemical formula (1), Ar1 is a substituted or unsubstituted first aromatic ring group, and each Ar2 is independently a substituted or unsubstituted second aromatic ring group, in which at least one of Ar1 and Ar2 has an unsaturated bond-containing substituent, and n is an integer of 2 or 3), a curable composition containing the active ester compound, and a cured product thereof.
    Type: Grant
    Filed: April 24, 2018
    Date of Patent: August 9, 2022
    Assignee: DIC Corporation
    Inventors: Yutaka Satou, Kazuhisa Yamoto
  • Publication number: 20150141252
    Abstract: A method of screening for a plant defense activator, which enhances an immune response of a plant, from at least one candidate substance includes: contacting a plant cell in which a jasmonic acid-dependent defense pathway and a salicylic acid-dependent defense pathway of a plant defense system are capable of working independently from each other, with a candidate substance; contacting the plant cell with a trigger material that induces an immune response; and assaying the plant cell after contacting with the trigger material based on an index representing an immune response, to select a target substance that enhances an immune response of the plant. A method of enhancing an immune response of a plant includes use of a specific compound, and a plant immune response enhancer includes the specific compound.
    Type: Application
    Filed: August 10, 2011
    Publication date: May 21, 2015
    Applicant: Tokyo University of Science Foundation
    Inventors: Kazuyuki Kuchitsu, Takamitsu Kurusu
  • Patent number: 9006249
    Abstract: The present invention provides a compound of formula I?; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, X and n are defined herein. The invention also relates to a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
    Type: Grant
    Filed: June 7, 2012
    Date of Patent: April 14, 2015
    Assignee: Novartis AG
    Inventors: Gary Mark Coppola, Yuki Iwaki, Rajeshri Ganesh Karki, Toshio Kawanami, Gary Michael Ksander, Muneto Mogi, Robert Sun
  • Publication number: 20150045393
    Abstract: The invention provides for novel cysteine protease inhibitors and compositions comprising novel cysteine protease derivatives. The invention further provides for methods for treatment of neurodegenerative diseases comprising administration novel cysteine protease inhibitors or compositions comprising novel cysteine protease inhibitors. In some embodiments, the cysteine protease inhibitors are calpain inhibitors.
    Type: Application
    Filed: February 1, 2013
    Publication date: February 12, 2015
    Inventors: Greg R. Thatcher, Isaac Thomas Schiefer, Ottavio Arancio, Mauro Fa
  • Publication number: 20140031230
    Abstract: An object of the present invention is to provide an auxin biosynthesis inhibitor superior to L-AOPP. The object can be attained by a compound represented by general formula (I): wherein, R1 to R5 and X are the same as defined in the specification or a salt or solvate thereof.
    Type: Application
    Filed: February 28, 2012
    Publication date: January 30, 2014
    Inventors: Yukihisa Shimada, Ko Kikuzato, Megumi Narukawa, Tadao Asami, Kazuo Soeno
  • Publication number: 20130244325
    Abstract: Pro-apoptotic compounds having a tripartite structure: A-L-B are disclosed. In these compounds A is an IBM mimetic moiety; L is a linker and B is a moiety that binds to a protein on the outer mitochondrial membrane. The compounds are useful for inducing cell apoptosis and therefore treating cancer.
    Type: Application
    Filed: September 12, 2012
    Publication date: September 19, 2013
    Applicant: The Rockefeller University
    Inventors: Hermann STELLER, Cristinel SANDU, Anshuman KELKAR, Nidhi GANGADHAR
  • Publication number: 20120252830
    Abstract: The present invention provides a compound of formula I?; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, X and n are defined herein. The invention also relates to a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
    Type: Application
    Filed: June 7, 2012
    Publication date: October 4, 2012
    Applicant: NOVARTIS AG
    Inventors: Gary Mark Coppola, Yuki Iwaki, Rajeshri Ganesh Karki, Toshio Kawanami, Gary Michael Ksander, Muneto Mogi, Robert Sun
  • Patent number: 8163942
    Abstract: The invention relates to purification of (2S,3S)-3-[[(1S)-1-isobutoxymethyl-3-methylbutyl]carbamoyl]oxirane-2-carboxylic acid [hereinafter, referred to as the carboxylic acid] using the salt of the carboxylic acid with an organic amine selected from the group consisting of piperazine, adamantane amines and others. The invention also relates to providing crystalline sodium salt of the carboxylic acid. The sodium salt is usable as a material for preparing medicaments and improved in storage stability, and has the following characteristics: DSC: exothermic peak observed at a temperature in the range of 170 to 175° C. with weight decrease; and characteristic absorption bands of infrared absorption spectrum (KBr tablet): 3255, 2950, 2860, 1670, 1630, 1550, 1460, 1435, 1395, 1365, 1310, 1260, 1110, 890 cm?1.
    Type: Grant
    Filed: September 13, 2010
    Date of Patent: April 24, 2012
    Assignee: Velcura Therapeutics, Inc.
    Inventors: Atsushi Tendo, Toshihiro Takahashi, Tomio Yamakawa, Kazuki Okai, Susumu Nihashi
  • Publication number: 20110275838
    Abstract: The present invention relates to a process for obtaining cinatrins C1 and C3 and derivatives thereof which comprises the hydroxylation of a compound of formula (III).
    Type: Application
    Filed: May 5, 2009
    Publication date: November 10, 2011
    Applicant: CONSEJO SUPERIOR DE INVESTIGACIONES CIENTIFICAS
    Inventors: Pedro Noheda Marin, Luis Miguel Lozano Gordillo, Sergio Maroto Quintana
  • Publication number: 20110212072
    Abstract: Described are a method and a composition for preventing and/or treating a disease related to mitochondrial dysfunction by inhibiting the fatty acid oxidation of one or more cells of an organism. Particularly, the fatty acid oxidation is inhibited by inhibiting the expression and/or activity of the enzyme Camitin-Palmitoyl-Transferase-1 (CPT-1) by means of an arylalkyl- or arlyoxyalkyl-substitued oxirane carboxylic acid or pharmaceutically acceptable salts and derivatives of the arylalkyl-substituted oxirane carboxylic acid.
    Type: Application
    Filed: April 19, 2011
    Publication date: September 1, 2011
    Applicant: MediGene AG
    Inventors: Thomas Henkel, Christoph Rehfuess
  • Publication number: 20110178172
    Abstract: Carnitin-Palmitoyl-Transferase-1 (CPT-1) inhibitor for use in treating and/or preventing disorders caused by delipidation of neural tissue.
    Type: Application
    Filed: June 25, 2009
    Publication date: July 21, 2011
    Applicant: META-IQ APS
    Inventor: Josephus Dirk Nieland
  • Publication number: 20110124891
    Abstract: Compounds of formula (I): are disclosed. In these compounds Y is —CH(OH)—, —CH(NHR6)—, —C(=0)-, —CH?CHCO— or—formula (II)—and R1 and R2 are hydrogen, OH, alkyl, alkoxy, benzyloxy and aryl, and, when Y is —CH(OH)—, additionally alkenyl or alkynyl. Processes for the production of these compounds are also disclosed.
    Type: Application
    Filed: August 16, 2008
    Publication date: May 26, 2011
    Inventors: John Welch, Silvana Ngo, Dong Sung Lim
  • Publication number: 20110105458
    Abstract: Fatty acid inhibitors, pharmaceutical compositions including fatty acid inhibitors, methods for using fatty acid inhibitors to treat a variety of diseases, and methods for preparing fatty acid inhibitors are provided herein.
    Type: Application
    Filed: November 2, 2010
    Publication date: May 5, 2011
    Applicant: COMPLEXA, INC.
    Inventor: Bruce Branchaud
  • Publication number: 20110015262
    Abstract: Methods and compositions for treating inflammatory and proliferative diseases, enabling treatment of MDR tumor cells by using combination of compounds, or a bifunctional compound, that inhibits both fatty acid metabolism and glycolysis. In particular, the invention combines or links a glycolysis inhibitor that is, or that is derived from, hypoglycin A (also referred to as hypoglycine A) and a fatty acid metabolism inhibitor. Preferably, the invention provides bifunctional compounds that link a moiety having the functionality of an oxirane carboxylic acid compound to a moiety having the functionality a hypoglycin A derivative. In specific embodiments, the invention provides a bifunctional compound that links a moiety having the functionality of etomoxir to a moiety having the functionality of hypoglycin A.
    Type: Application
    Filed: April 20, 2006
    Publication date: January 20, 2011
    Inventors: Martha Karen Newell, Evan Newell
  • Publication number: 20110003993
    Abstract: The invention relates to purification of (2S,3S)-3-[[(1S)-1-isobutoxymethyl-3-methylbutyl]carbamoyl]oxirane-2-carboxylic acid [hereinafter, referred to as the carboxylic acid] using the salt of the carboxylic acid with an organic amine selected from the group consisting of piperazine, adamantane amines and others. The invention also relates to providing crystalline sodium salt of the carboxylic acid. The sodium salt is usable as a material for preparing medicaments and improved in storage stability, and has the following characteristics: DSC: exothermic peak observed at a temperature in the range of 170 to 175° C. with weight decrease; and characteristic absorption bands of infrared absorption spectrum (KBr tablet): 3255, 2950, 2860, 1670, 1630, 1550, 1460, 1435, 1395, 1365, 1310, 1260, 1110, 890 cm×1.
    Type: Application
    Filed: September 13, 2010
    Publication date: January 6, 2011
    Applicant: NIPPON CHEMIPHAR CO., LTD.
    Inventors: Atsushi TENDO, Toshihiro TAKAHASHI, Tomio YAMAKAWA, Kazuki OKAI, Susumu NIHASHI
  • Publication number: 20100331545
    Abstract: [Problems] To provide a modulator for signaling of TLR [Means for solving the problems] A medicament containing cathepsin inhibitor such as monosodium (2S,3S)-3-[[(1S)-1-isobutoxymethyl-3-methylbutyl]carbamoyl]oxirane-2-carboxylate as a active ingredient is used as a modulator for signaling of TLR, a therapeutic agent for treating diseases associated with TLR signaling, a therapeutic agent for treating diseases associated with induction of Th17 cells, a therapeutic agent for treating diseases associated with production of IL-6, IL-12, IL-17, or IL-23, or a therapeutic agent for treating systemic lupus erythematosus, lupus nephritis, crohn's disease, psoriasis, or acute disseminated encephalomyelitis.
    Type: Application
    Filed: October 23, 2008
    Publication date: December 30, 2010
    Applicant: NIPPON CHEMIPHAR CO., LTD.
    Inventors: Hiroshi Takayanagi, Masataka Asagiri, Toshitake Hirai
  • Patent number: 7795458
    Abstract: The invention relates to purification of (2S,3S)-3-[[(1S)-1-isobutoxymethyl-3-methylbutyl]carbamoyl]oxirane-2-carboxylic acid [hereinafter, referred to as the carboxylic acid] using the salt of the carboxylic acid with an organic amine selected from the group consisting of piperazine, adamantane amines and others. The invention also relates to providing crystalline sodium salt of the carboxylic acid. The sodium salt is usable as a material for preparing medicaments and improved in storage stability, and has the following characteristics: DSC: exothermic peak observed at a temperature in the range of 170 to 175° C. with weight decrease; and characteristic absorption bands of infrared absorption spectrum (KBr tablet) 3255, 2950, 2860, 1670, 1630, 1550, 1460, 1435, 1395, 1365, 1310, 1260, 1110, 890 cm?1.
    Type: Grant
    Filed: August 21, 2009
    Date of Patent: September 14, 2010
    Assignee: Nippon Chemiphar Co., Ltd
    Inventors: Atsushi Tendo, Toshihiro Takahashi, Tomio Yamakawa, Kazuki Okai, Susumu Nihashi
  • Publication number: 20090312563
    Abstract: The invention relates to purification of (2S,3S)-3-[[(1S)-1-isobutoxymethyl-3-methylbutyl]carbamoyl]oxirane-2-carboxylic acid [hereinafter, referred to as the carboxylic acid] using the salt of the carboxylic acid with an organic amine selected from the group consisting of piperazine, adamantane amines and others. The invention also relates to providing crystalline sodium salt of the carboxylic acid. The sodium salt is usable as a material for preparing medicaments and improved in storage stability, and has the following characteristics: DSC: exothermic peak observed at a temperature in the range of 170 to 175° C. with weight decrease; and characteristic absorption bands of infrared absorption spectrum (KBr tablet) 3255, 2950, 2860, 1670, 1630, 1550, 1460, 1435, 1395, 1365, 1310, 1260, 1110, 890 cm?1.
    Type: Application
    Filed: August 21, 2009
    Publication date: December 17, 2009
    Applicant: NIPPON CHEMIPHAR CO., LTD.
    Inventors: Atsushi TENDO, Toshihiro TAKAHASHI, Tomio YAMAKAWA, Kazuki OKAI, Susumu NIHASHI
  • Patent number: 7585988
    Abstract: The invention relates to purification of (2S,3S)-3-[[(1S)-1-isobutoxymethyl-3-methylbutyl]carbamoyl]oxirane-2-carboxylic acid [hereinafter, referred to as the carboxylic acid] using the salt of the carboxylic acid with an organic amine selected from the group consisting of piperazine, adamantane amines and others. The invention also relates to providing crystalline sodium salt of the carboxylic acid. The sodium salt is usable as a material for preparing medicaments and improved in storage stability, and has the following characteristics: DSC: exothermic peak observed at a temperature in the range of 170 to 175° C. with weight decrease; and characteristic absorption bands of infrared absorption spectrum (KBr tablet): 3255, 2950, 2860, 1670, 1630, 1550, 1460, 1435, 1395, 1365, 1310, 1260, 1110, 890 cm?1.
    Type: Grant
    Filed: April 22, 2004
    Date of Patent: September 8, 2009
    Assignee: Nippon Chemiphar Co., Ltd.
    Inventors: Atsushi Tendo, Toshihiro Takahashi, Tomio Yamakawa, Kazuki Okai, Susumu Nihashi
  • Publication number: 20090149586
    Abstract: The present descriptive report refers to a patent of invention of primary PVC plasticizers composed of epoxidized ethyl and/or isoamyl esters of vegetable oil fatty acids and to the compounds of PVC plasticized with epoxidized bioesters, belonging to the technical field of polymer additives, developed from renewable sources such as vegetable oils and sugar cane, to reduce the cost and improve the properties of PVC compounds. The epoxidized bioesters are suitable to be added to at least one PVC resin and are obtained from a transesterification reaction of at least one type of vegetable oil with ethanol or isoamylic alcohol and subsequent epoxidation, presenting oxirane index equal to or less than 8.
    Type: Application
    Filed: December 9, 2008
    Publication date: June 11, 2009
    Applicant: NEXOLEUM BIODERIVADOS LTDA.
    Inventors: Jacyr Vianna De Quadros Junior, Jose Augusto De Carvalho
  • Publication number: 20080107821
    Abstract: A polymerizable actinic radiation curable composition comprising a photo-acid generating compound and an epoxy compound represented by Formula (1): wherein X represents a divalent group selected form the group consisting of —O—, —S—, —SO—, —SO2—, —CBr2—, —C(CBr3)2—, and —C(CF3)2—; R1 to R18 each independently represent a hydrogen atom, a halogen atom, a hydrocarbon group having 1-8 carbon atoms, provided that the hydrocarbon group may contain an oxygen atom or a halogen atom, or a substituted or unsubstituted alkoxy group having 1-8 carbon atoms.
    Type: Application
    Filed: November 29, 2005
    Publication date: May 8, 2008
    Applicant: KONICA MINOLTA MEDICAL & GRAPHIC, INC.
    Inventors: Nobumasa Sasa, Norio Miura, Kimihiko Ookubo, Takeshi Kurata
  • Patent number: 7279586
    Abstract: The present invention generally relates to at least one precursor compound and derivatives thereof, a process for preparing a taxane, and a baccatin derivative.
    Type: Grant
    Filed: June 4, 2004
    Date of Patent: October 9, 2007
    Assignee: Societe d'etude et de Recherche en Ingenierie Pharmaceutique Seripharm
    Inventors: Luc Chanteloup, Bruno Chauveau, Christine Corbin, Robert Dhal, Sonia Le Guen, Arnaud Lamy, Antoine Leze, Jean-Pierre Robin
  • Patent number: 7078543
    Abstract: The invention relates to processes for preparing oxiranecarboxylic acids and derivatives thereof, in particular to processes which proceed under stereochemical control of the reaction steps, to the oxiranecarboxylic acids prepared according to the invention and derivatives thereof and to their use in pharmaceutical compositions, in particular for treating hyperlipaemia.
    Type: Grant
    Filed: March 28, 2002
    Date of Patent: July 18, 2006
    Assignee: MediGene Aktiengesellschaft
    Inventors: Magnus Cernerud, Kristina Berntsson
  • Patent number: 7060471
    Abstract: The present invention relates to a novel and efficient chemoenzymatic process of preparation of optically active trans alkyl phenylglycidates. The invention particularly discloses a novel process for the chemoenzymatic synthesis of two enantiomers of trans alkyl phenylglycidate i.e.
    Type: Grant
    Filed: March 10, 2004
    Date of Patent: June 13, 2006
    Assignee: Council of Scientific & Industrial Research
    Inventors: Naveen Anand, Munish Kapoor, Subhash Chandra Taneja, Surrinder Koul, Rattan Lal Sharma, Ghulam Nabi Qazi
  • Patent number: 6921832
    Abstract: Optically active fluorine-containing compounds of the formula (1): or of formula (2): are used for producing optically active 3,3,3-trfluoro-2-hydroxy-2-methylpropionic acids.
    Type: Grant
    Filed: November 25, 2003
    Date of Patent: July 26, 2005
    Assignee: Tosoh Corporation
    Inventors: Takuya Miyama, Toshio Naka, Takumi Kagawa
  • Patent number: 6787657
    Abstract: An optically active epoxypropionate derivative of the following formula (1): wherein symbol * represents optically active carbon. Also disclosed is an optically active epoxypropionate derivative of the following formula (2): wherein symbol * represents optically active carbon.
    Type: Grant
    Filed: February 21, 2001
    Date of Patent: September 7, 2004
    Assignee: Tosoh Corporation
    Inventors: Akinori Tanaka, Takumi Kagawa
  • Publication number: 20030216587
    Abstract: A process for the conversion of aldehydes to esters, specifically acrolein or methacrolein to methyl acrylate or methyl methacrylate, respectively. Essentially in the absence of water, an aldehyde is contacted with an oxidizing agent to form an intermediate and then the intermediate is contacted with a diol or an alcohol to form an ester or diester. Preferably, the oxidizing agent is also a chlorinating agent. Specifically, acrolein or methacrolein is contacted with an oxidizing/chlorinating agent, such as t-butyl hypochlorite, and the chlorinated compound is contacted with an alcohol, such as methanol, to form methyl acrylate or methyl methacrylate, respectively. Generally, the order of addition is for the oxidizing agent to be added to the aldehyde, specifically for t-butyl hypochlorite to be added to acrolein or methacrolein, and for the diol or alcohol to be added to the intermediate, specifically for the methanol to be added to the reaction product of acrolein or methacrolein and t-butyl hypochlorite.
    Type: Application
    Filed: May 13, 2002
    Publication date: November 20, 2003
    Applicant: Saudi Basic Industries Corporation (SABIC)
    Inventors: Andrew T. Au, Jean-Pierre Lawanier, David Adam Flosser
  • Patent number: 6500971
    Abstract: An ester compound of formula (1) is provided. R1 is H or methyl, R2 is tertiary C4-20 alkyl, and k=0 or 1. A resist composition comprising as the base resin a polymer resulting from the ester compound is sensitive to high-energy radiation, has excellent sensitivity, resolution, etching resistance and substrate adhesion, and is suited for micropatterning using electron beams or deep-UV.
    Type: Grant
    Filed: June 5, 2001
    Date of Patent: December 31, 2002
    Assignee: Shin-Etsu Chemical Co., Ltd.
    Inventors: Takeru Watanabe, Takeshi Kinsho, Koji Hasegawa, Tsunehiro Nishi, Mutsuo Nakashima, Seiichiro Tachibana, Jun Hatakeyama
  • Publication number: 20020151731
    Abstract: The present invention relates to novel epoxides having the formulas 1
    Type: Application
    Filed: March 11, 2002
    Publication date: October 17, 2002
    Inventor: R. Garth Pews
  • Patent number: 6403638
    Abstract: Compounds having the formulas below, where R is H, lower alkyl, or a pharmaceutically acceptable salt, and where R1 represents i-propyl, t-butyl or n-butyl groups, have selective RXR retionoid agonist activity.
    Type: Grant
    Filed: March 21, 2000
    Date of Patent: June 11, 2002
    Assignee: Allergan Sales, Inc.
    Inventors: Vidyasagar Vuligonda, Kwok Yin Tsang, Jayasree Vasudevan, Roshantha A. Chandraratna
  • Patent number: 6387908
    Abstract: Epoxysuccinamide derivatives of the formula (1): wherein R1 is hydrogen, alkyl, alkenyl, alkynyl, aryl, or aralkyl; R2 is alkyl, alkenyl, alkynyl, aryl, or aralkyl; R3 is hydrogen, alkyl, alkenyl, alkynyl, aryl, aralkyl, heterocyclic, or heterocyclic-alkyl; X is —O— or —NR4— (R4 is hydrogen, alkyl, aryl, aralkyl, heterocyclic, or heterocyclic-alkyl); Y1 is OR5, SR6, or NR7R8; and Y2 is hydrogen or alkyl. The compounds are useful as remedies for bone diseases and arthritis.
    Type: Grant
    Filed: May 5, 2000
    Date of Patent: May 14, 2002
    Assignee: Nippon Chemiphar Co., Ltd.
    Inventors: Yutaka Nomura, Toshihiro Takahashi, Yasushi Yoshino, Koichiro Nishioka
  • Publication number: 20020035279
    Abstract: An ester compound of formula (1) is provided.
    Type: Application
    Filed: June 5, 2001
    Publication date: March 21, 2002
    Applicant: Shin-Etsu Chemical Co., Ltd.
    Inventors: Takeru Watanabe, Takeshi Kinsho, Koji Hasegawa, Tsunehiro Nishi, Mutsuo Nakashima, Seiichiro Tachibana, Jun Hatakeyama
  • Publication number: 20010056163
    Abstract: The present invention relates to macromonomer compounds having the formula (I) where R1 is hydrogen, halogen, and optionally substituted alkyl, aryl, alkylaryl or arylalkyl radical; R2 and R3, which can be similar or different, are hydrogen, halogen, alkyl, aryl, alkylaryl, arylalkyl or alkoxy radical; R4 is an optionally substituted alkyl, aryl, alkylaryl or arylalkyl radical, or —XR5, with R5 being hydrogen, and optionally substituted alkyl, aryl, alkylaryl or aryalkyl; X is oxygen or sulphur; A corresponds to a unit issued from at least one ethylenically unsaturated monomer; and n is comprised between 1 and 10000. The invention also relates to dienic compounds having the formula (II): H2C═CR1—CH═CH—C(R2)(R3)—X2—R6 wherein R1 R2, R3 and X have the same meaning as above and R6 represents R5 or a group —COR7 or —COOR7 with R7 being alkyl, aryl, alkylaryl or arylalkyl.
    Type: Application
    Filed: June 29, 2001
    Publication date: December 27, 2001
    Inventors: Dominique Charmot, Philippe Chaumont, Daniel Colombani
  • Patent number: 6228955
    Abstract: A process for preparing an optically-enriched chiral epoxide of formula I wherein R1, R2 and R3 are each independently selected from H, R, R—CO— and R—O—CO—, each R independently being substantially a hydrocarbon group of up to 20 carbon atoms, and X is an alkyl or cycloalkyl group of up to 10 carbon atoms, provided that —CO—X is not enolisable, which comprises the asymmetric epoxidation of a corresponding prochiral alkene of formula II R1R2C═CR3—CO—X  (II) by reaction with an oxidant in the presence of a chiral catalyst. Many optically-enriched epoxides (I) are novel.
    Type: Grant
    Filed: October 20, 1997
    Date of Patent: May 8, 2001
    Assignee: Chirotech Technology, Ltd.
    Inventors: Stanley Michael Roberts, Brian Michael Adger
  • Patent number: 6187936
    Abstract: A process for the preparation of I: in which R and R1 have the meanings reported in the description, that comprises the enzymatic kinetic resolution by transesterification with aminoalcohols of 3-phenylglycidates of formula I: is described.
    Type: Grant
    Filed: September 20, 1999
    Date of Patent: February 13, 2001
    Assignee: Zambon Group S.p.A.
    Inventors: Marco Villa, Dario Tentorio, Angelo Restelli, Sergio Riva
  • Patent number: 6153589
    Abstract: The present invention is related to compounds, compositions and methods of treating viral infections. Compounds of the present invention have the following general formula: ##STR1## wherein R is selected from --CH.sub.2 OH, --CO.sub.2 R.sup.2, --CONR.sup.3 R.sup.4, or COR.sup.5, wherein R.sup.2 is hydrogen or a lower alkyl group, R.sup.3 and R.sup.4 are each independently hydrogen or a lower alkyl group, R.sup.5 is an amino acid residue bound via a terminal nitrogen or peptide having at least two amino acid residues; and wherein R.sup.1 is C.sub.5 -C.sub.13 alkyl, aryl, aralkyl, aralkyl(lower alkyl)ether, or C.sub.5 -C.sub.13 alkyl(lower alkyl)ether.
    Type: Grant
    Filed: December 15, 1992
    Date of Patent: November 28, 2000
    Assignee: The United States of America as represented by the Department of Health and Human Services
    Inventors: Jeffrey J. Blumenstein, Christopher J. Michejda, Stephen Oroszlan, Terry Copeland
  • Patent number: 6147224
    Abstract: Compounds of Formula 1, Formula 2 or Formula 3 where X is O, S, or (CR.sub.1 R.sub.1).sub.n where n is 0, 1 or 2; Y is a bivalent radical having Formula 4 or Formula 5 where o is an integer from 1 to 4 ##STR1## or Y is a bivalent aryl or 5 or 6 membered heteroaryl radical having 1 to 3 heteroatoms selected from N, S and O, said aryl or heteroaryl groups being unsubstituted, or substituted with 1 to 3 C.sub.1-6 alkyl or with 1 to 3 C.sub.1-6 fluoroalkyl groups; and the remaining symbols have the meaning described in the specification, have RXR selective retinoid agonist-like activity.
    Type: Grant
    Filed: October 1, 1998
    Date of Patent: November 14, 2000
    Assignee: Allergan Sales, Inc.
    Inventors: Vidyasagar Vuligonda, Kwok Yin Tsang, Jayasree Vasudevan, Roshantha A. Chandraratna
  • Patent number: 6143909
    Abstract: Cryptophycin compounds possessing a .beta.-epoxy moiety may be made with high stereoselectivity at various steps in the overall synthetic process. This invention also provides novel intermediates useful in preparing Cryptophycin compounds.
    Type: Grant
    Filed: August 24, 1999
    Date of Patent: November 7, 2000
    Assignee: Eli Lilly and Company
    Inventors: David Warren Hoard, Eric David Moher, Vinod Francis Patel, Bryan Hurst Norman
  • Patent number: 6025506
    Abstract: The invention relates to a process for preparing an optically active trans-compound having formula (1), in which R represents a phenyl group, whether or not substituted, preferably p-methoxyphenyl, and A is derived from an optically active compound, in which an aldehyde having formula (2), in which R is as defined above, is, in the presence of a base, brought into contact with an optically active acetyl compound having formula (3), in which X represents a leaving group and in which A is derived from an amino alcohol, preferably a .beta.-amino alcohol having a rigid structure.Particularly good results were obtained when use was made of a compound having formula (3), in which A is derived from an amino indanol compound having formula (4), in which R.sub.1 and R.sub.2 represent a (hetero)alkyl or (hetero)aryl group, whether or not substituted, having 1-10 C atoms, or R.sub.1 and R.sub.2 constitute an aromatic or aliphatic ring together with the N atom to which they are bound, in particular in which R.sub.
    Type: Grant
    Filed: February 23, 1998
    Date of Patent: February 15, 2000
    Assignee: DSM N.V.
    Inventors: Bernardus Kaptein, Gerardus K. M. Verzijl
  • Patent number: 6013666
    Abstract: This invention relates to a novel oxirane carboxylic acid derivative and thereof manufacturing method. Based on thereof mechanism to inhibit the CPT I, oxirane carboxylic acid derivative of this invention has blood glucose lowering effects so that the derivative may be effectively used as an antidiabetic agent having remarkable antidiabetic activity and less side effects.
    Type: Grant
    Filed: May 11, 1999
    Date of Patent: January 11, 2000
    Assignees: Sang Sup Jew, Kang Ho Kang, Bak Kwang Kim
    Inventors: Sang Sup Jew, Suk Ku Kang, Deuk Joon Kim, Won Ki Kim, Hwa Jung Kim, Chang Kiu Moon, Jeong Hill Park, Young Ger Suh, Bong Jin Lee, Jee Woo Lee, Ki Hwa Jung, Moon Woo Chun, Hoon Huh, Eung Seok Lee, Hyung Ook Kim, Eun Kyung Kim, Sung Jin Kim, Jae Hoon Cheong, Kwang Ho Ko, Bak Kwang Kim
  • Patent number: 5985919
    Abstract: (Het)aryloxy-, -thio- and -aminocrotonates of the formula I ##STR1## where the substituents have the following meanings: U is oxygen, sulfur or amino;V is oxygen, sulfur, amino or alkylamino;X, Y and Z independently of one another are .dbd.N-- or .dbd.CR.sup.3 --;R.sup.1 and R.sup.2 independently of one another are alkyl;R.sup.3 is hydrogen, cyano, nitro, halogen, alkyl, haloalkyl, alkoxy, haloalkoxy, alkylthio and haloalkylthio; andR.sup.4 is an organic radical which is bonded to the skeleton directly or via an oxy, mercapto, amino, carboxyl or carbonylamino group,process for their preparation, and their use.
    Type: Grant
    Filed: October 30, 1997
    Date of Patent: November 16, 1999
    Assignee: BASF Aktiengesellschaft
    Inventors: Thomas Grote, Reinhard Kirstgen, Bernd Muller, Hubert Sauter, Albrecht Harreus, Hartmann Konig, Eberhard Ammermann, Gisela Lorenz, Siegfried Strathmann, Franz Rohl
  • Patent number: 5932752
    Abstract: A process for the preparation of organic compounds through C--C bond forming reaction which comprises reacting a diene with a dienophile in the presence of solid acid based on either yttrium, scandium or lanthanum supported on metal oxide supports such as oxides of zirconium or tin or titanium or iron oxide modified by sulphation as catalysts for a period ranging from 5 to 48 hours and recovering the reaction products from the reaction mixture by filtration and removal of the solvent by evaporation followed by column chromatography.
    Type: Grant
    Filed: May 29, 1996
    Date of Patent: August 3, 1999
    Assignee: Council of Scientific and Industrial Research
    Inventors: Alive Keshavaraja, Vishnumurthy Ramachandra Hegde, Pradeep Kumar, Sooryakant Ganesh Hegde, Arumugamangalam Venkataraman Ramaswamy, Thottappillil Ravindranathan
  • Patent number: 5843992
    Abstract: An epoxysuccinic acid derivative having the following formula: ##STR1## ?wherein R.sup.1 is hydrogen, alkyl, aryl, or aralkyl; each of R.sup.2 and R.sup.3 independently is aryl, aralkyl or alkyl; X is --O-- or --NR.sup.4 --; and R.sup.4 is hydrogen, alkyl, or aralkyl! is useful for prevention and treatment of bone diseases such as osteoporosis, malignant hypercalcemia and Paget's syndrome, and further useful for treatment of osteoarthritis and rheumatoid arthritis which are accompanied by abnormal enhancement of cathepsin L activity, and furthermore useful as a medicine for treating diseases in which cathepsin B and L participate, such as muscular dystrophy and muscular atrophy.
    Type: Grant
    Filed: September 29, 1997
    Date of Patent: December 1, 1998
    Assignee: Nippon Chemiphar Co., Ltd.
    Inventors: Yutaka Nomura, Toshihiro Takahashi, Kaoru Hara, Yasushi Yoshino, Mitsuo Masaki
  • Patent number: 5811458
    Abstract: The invention relates to phenyl propane derivatives of the general formulae: ##STR1## or their mixtures, in which R.sub.1 and R.sub.2 are a branched or straight-chained alkyl residue of the general formula C.sub.n H.sub.2n+1 with n=1-18, for use as a therapeutic agent.
    Type: Grant
    Filed: July 30, 1996
    Date of Patent: September 22, 1998
    Inventors: Jurgen Reichling, Volker Hingst, Ulla Ohlenmacher
  • Patent number: 5786489
    Abstract: A method for esterifying C13 deoxy taxoid intermediates employs three steps, i.e., oxygenation of the C13 deoxy taxoid intermediate to produce a C13 enone taxoid intermediate; reduction of the C13 enone to produce an alcohol; followed by esterification of the C13 alcohol. Key intermediates include C13 deoxy taxoids; C13 enone substituted taxoids; and C1-C2 cyclo carbonate esters of taxoids.
    Type: Grant
    Filed: April 1, 1996
    Date of Patent: July 28, 1998
    Assignee: The Scripps Research Institute
    Inventors: Kyriacos C. Nicolaou, Philippe G. Nantermet, Rodney K. Guy, Hiroaki Ueno
  • Patent number: 5679708
    Abstract: The present invention relates to a compound of the formula: ##STR1## wherein R.sub.1 stands for an optionally esterified or amidated carboxyl group, X stands for an optionally substituted divalent hydrocarbon residue, R.sub.2 stands for hydrogen or an optionally substituted hydrocarbon residue, R.sub.3 stands for an alkyl group which is substituted with a group bonded through O or S(O).sub.n wherein n is 0, 1 or 2, with a proviso that when the partial structural formula: --NH--X--CO-- is leucine residue, R.sub.3 is not 3-hydroxy-3-methylbutyl group nor 4-hydroxy-3-methylbutyl group, or a salt thereof, which is useful as prophylactic and therapeutic agents of bone diseases and as inhibitory agents of thiol protease.
    Type: Grant
    Filed: September 5, 1995
    Date of Patent: October 21, 1997
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Shigetoshi Tsubotani, Masayuki Takizawa, Junji Mizoguchi
  • Patent number: 5677298
    Abstract: Disclosed is a squalene synthetase inhibitor which comprises the compound represented by the formula (I) ##STR1## wherein R.sub.1 stands for H or an optionally substituted hydrocarbon group; R.sub.2 and R.sub.3 independently stand for H, an optionally substituted alkyl group, an optionally substituted phenyl group or an optionally substituted aromatic heterocyclic group; Z stands for a carbon chain containing a double bond or --Z'--C(OH)-- (Z' stands for a bond or a straight-chain or branched alkylene chain); the symbol .........
    Type: Grant
    Filed: August 13, 1996
    Date of Patent: October 14, 1997
    Assignee: Takeda Chemical Industries
    Inventors: Hidefumi Yukimasa, Masakuni Kori, Ryuichi Tozawa, Yasuo Sugiyama
  • Patent number: 5599651
    Abstract: Novel (cyclo)aliphatic epoxy compounds that contain at least one acrylate group in the molecule and at least one cycloaliphatic epoxy group can be used for the production of coating formulations, adhesives, photoresists or in stereolithography. As they contain a cohesive homogeneous network, the three-dimensional objects produced have very good green strength and very good strength properties.
    Type: Grant
    Filed: August 21, 1995
    Date of Patent: February 4, 1997
    Assignee: Ciba-Geigy Corporation
    Inventors: Bettina Steinmann, Jean-Pierre Wolf, Adrian Schulthess, Max Hunziker
  • Patent number: 5569774
    Abstract: Chlorine-substituted olefins I ##STR1## (R.sup.1 =organic radical; R.sup.2 =--CN, --CO--R.sup.3, --CO--S--R.sup.3, --CO--O--R.sup.3 --CO--N(R.sup.4,R.sup.5); R.sup.3 =organic radical; R.sup.4, R.sup.5 =H, organic radical)are prepared by reacting oxiranes II ##STR2## in the presence of a carboxamide (IIIa) or of a lactam (IIIb) in liquid phase with a chlorinating agent (IV). The products I are important intermediates for dyes, drugs and crop protection agents.
    Type: Grant
    Filed: September 20, 1994
    Date of Patent: October 29, 1996
    Assignee: BASF Aktiengesellschaft
    Inventors: Bernd Schaefer, Irene Troetsch-Schaller
  • Patent number: 5556853
    Abstract: A compound of the general formula: ##STR1## wherein R.sup.1 represents a carboxyl group which may optionally be esterified or amidated; R.sup.2 represents a cyclic group which may optionally be substituted or a polar group; n is an integer of 0 to 6; R.sup.3 represents hydrogen or a hydrocarbon residue which may optionally be substituted; R.sup.4 represents (1) a hydrocarbon residue which is substituted by an optionally protected amino group or (2) an alkenyl group; or R.sup.3 and R.sup.4 may be combined with the adjacent nitrogen atom to form a heterocyclic group containing at least two hetero atoms, or a salt thereof.The compound or a salt thereof of the present invention inhibits thiol proteases such as cathepsin L and B and serves well as a prophylactic/therapeutic agent for bone diseases such as osteoporosis.
    Type: Grant
    Filed: October 27, 1994
    Date of Patent: September 17, 1996
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Shigetoshi Tsubotani, Takizawa Masayuki, Shirasaki Mikio, Yukio Fujisawa