Having -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To The Hetero Ring Patents (Class 549/450)
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Patent number: 11603497Abstract: This invention provides a composition comprising I. at least one reaction product between a nitrogen-free monohydric alcohol and an aldehyde or ketone, and II. at least one reaction product between a monosaccharide having 3 to 6 carbon atoms and/or an oligosaccharide being formed by oligomerization of monosaccharides having 3 to 6 carbon atoms and an aldehyde or ketone, and optionally III. at least one reaction product from III.a) formaldehyde, and III.b) an amine, selected from the group consisting of primary alkyl amines having 1 to 4 carbon atoms, and primary hydroxy alkyl amines having 2 to 4 carbon atoms, and optionally IV. at least one solid suppression agent selected from the group consisting of IV(a). alkali or alkaline earth metal hydroxides IV(b). mono-, di- or tri-hydroxy alkyl, aryl or alkylaryl amines, IV(c). mono-, di- or tri-alkyl, aryl or alkylaryl primary, secondary and tertiary amines or IV(d). multifunctional amines and IV(e). mixtures of compounds of groups IV(a) to IV(c).Type: GrantFiled: January 23, 2020Date of Patent: March 14, 2023Assignee: CLARIANT INTERNATIONAL LTDInventors: Antonio Pedro de Oliveira Felho, Aline Yae Kina, Grahame N. Taylor, Fabian Schneider, Julie Murison, Stefan Hauck, Mike Sahl, Matthias Krull, Jonathan James Wylde
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Publication number: 20140155635Abstract: Disclosed are a novel resorcyclic acid lactone compound with inhibitory activity against protein kinases, a pharmaceutically acceptable salt thereof, a method for the synthesis thereof, and a pharmaceutical composition for the treatment and prevention of various cancer diseases comprising the same as an active ingredient. The novel resorcyclic acid lactone compound is useful as a therapeutic for cancer diseases, especially blood cancer, inter alia, acute myeloid leukemia (AML).Type: ApplicationFiled: October 29, 2013Publication date: June 5, 2014Applicant: KOREA INSTITUTE OF SCIENCE AND TECHNOLOGYInventors: Tae Bo SIM, Ho Jong Yoon, Ji Nyeo Kim
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Publication number: 20120130092Abstract: It is possible to produce oseltamivir safely and stably in large quantities by using as a starting material tartaric acid, mannitol or arabinose, via dihydroxyhexenoic acid ester of the formula (4c).Type: ApplicationFiled: December 6, 2011Publication date: May 24, 2012Inventors: Teruhiko Ishikawa, Seiki Saito, Takayuki Kudoh, Kotaro Suto, Hironori Nishiuchi, Makoto Okada, Masatoshi Taniguchi
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Patent number: 8148554Abstract: The invention provides methods and compositions for use in treating diseases associated with excessive cellular proliferation, such as cancer, and intermediates for the synthesis of such compositions.Type: GrantFiled: August 12, 2010Date of Patent: April 3, 2012Assignee: Eisai R&D Management Co., Ltd.Inventors: Boris M. Seletsky, Melvin J. Yu, Wanjun Zheng
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Patent number: 7825126Abstract: Disclosed are (N)-methanocarba adenine nucleosides of the formula: as highly potent A3 adenosine receptor agonists, pharmaceutical compositions comprising such nucleosides, and a method of use of these nucleosides, wherein R1-R6 are as defined in the specification. These nucleosides are contemplated for use in the treatment a number of diseases, for example, inflammation, cardiac ischemia, stroke, asthma, diabetes, and cardiac arrhythmias. The invention also provides compounds that are agonists of both A1 and A3 adenosine receptors for use in cardioprotection.Type: GrantFiled: September 2, 2005Date of Patent: November 2, 2010Assignee: The United States of America as represented by the Department of Health and Human ServicesInventors: Kenneth A. Jacobson, Bhalchandra V. Joshi, Susanna Tchilibon
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Publication number: 20100273968Abstract: The invention pertains to a process for preparing compounds of formula (I-A) or (I-B) here below: by reaction of perfluoroallylfluorosulfate (FAFS) of formula (II): with at least one hypofluorite of formula (II-A) or (II-B): wherein: RF in formulae (I-A) and (II-A) is a monovalent fluorocarbon C1-C20 group, optionally comprising oxygen catenary atoms, optionally comprising functional groups comprising heteroatoms (e.g. —SO2F groups); R?F in formulae (I-B) and (II-B) is a divalent fluorocarbon C1-C6 group, preferably a group of formula wherein X1 and X2, equal to or different from each other, are independently a fluorine atom or a C1-C3 fluorocarbon group. The FAFS-hypofluorite adducts of formulae (I-A) and (I-B) can be produced with high selectivity so as to access useful intermediates which can further be reacted taking advantage of the un-modified fluorosulfate group chemistry.Type: ApplicationFiled: December 17, 2008Publication date: October 28, 2010Applicant: SOLVAY SOLEXIS S.P.A.Inventors: Giuseppe Marchionni, Vito Tortelli
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Publication number: 20080262230Abstract: Disclosed is a novel benzyloxypropylamine derivative having an excellent tachykinin receptor antagonistic effect. This compound shows a good transfer into the blood and a long blood half-life in the blood kinetic test using a guinea pig orally administered with the compound and is stable in an animal plasma. The compound also shows a high transfer to the central nervous system when it is orally administered to a guinea pig at a certain dose. Accordingly, the benzyloxypropylamine derivative is quite useful as a novel anti-tachykinin agent.Type: ApplicationFiled: March 29, 2006Publication date: October 23, 2008Applicant: Nippon Zoki Pharmaceutical Co., LTD.Inventors: Kunihiko Higashiura, Takashi Ogino, Kazuhito Furukawa
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Patent number: 7271274Abstract: The invention relates to compounds, pharmaceutical compositions comprising the compounds, and methods of using the compounds, wherein the compounds are of the following Formulas: or a pharmaceutically acceptable salt, ester or prodrug thereof, wherein the substituents are defined in the application. The invention further provides methods of treatment of inflammatory disorders by administering the compounds.Type: GrantFiled: April 20, 2005Date of Patent: September 18, 2007Assignee: AhteroGenics, Inc.Inventors: Charles Q. Meng, M. David Weingarten
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Patent number: 7060727Abstract: The present invention relates generally to prodrugs of fused GABA analogs, pharmaceutical compositions of prodrugs of fused GABA analogs, methods of making prodrugs of fused GABA analogs and methods of using prodrugs of fused GABA analogs and pharmaceutical compositions of prodrugs of fused GABA analogs to treat or prevent various diseases.Type: GrantFiled: December 11, 2003Date of Patent: June 13, 2006Assignee: XenoPort, Inc.Inventor: Mark A. Gallop
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Patent number: 6844375Abstract: The invention relates to: 4-methylene-1,3-dioxolanes of the general formula (I) wherein R1 denotes hydrogen, C5-C6-cycloalkyl or C1-C4-alkyl; m and n, which may be the same or different, denote 0 or 1, whereby m?n, o denotes 2, 3 or 4 depending on the valency of the group X; and X denotes a C—C single bond, straight-chain or branched C1-C18-alkylene, C5-C6-cycloalkylene, C8-C18-arylalkylene, —CH2(OCH2CH2)pOCH2—, —CH2(OCH(CH3)CH2)pOCH2—, wherein p is an integer from 0 to 100; a process for their production; and intermediate products used. Moreover, compositions capable of emission-free, photocationic cross-linking, which comprise 4-methylene-1,3-dioxolanes of the general formula (I) and their use for the production of solvent-resistant and transparent films.Type: GrantFiled: August 23, 2001Date of Patent: January 18, 2005Assignee: Dainippon Ink and Chemicals, Inc.Inventors: Helmut Hartl, Rainer B. Frings, Gerwald F. Grahe
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Patent number: 6809091Abstract: A method for the manufacture of a substance having an apoptosis-inducing ability characterized in including a step of subjecting at least one compound selected from the following (a), (b), (c) and (d) [excluding uronic acid and/or uronic acid derivatives; and compounds which contain uronic acid and/or uronic acid derivatives] to a heating treatment: (a) pentose; (b) pentose derivatives; (c) compounds containing pentose; (d) compounds containing pentose derivatives.Type: GrantFiled: June 28, 2000Date of Patent: October 26, 2004Assignee: Takara Bio Inc.Inventors: Yoko Tatsumi, Hiroaki Sagawa, Hiromu Ohnogi, Eiji Kobayashi, Hua-Kang Wu, Nobuto Koyama, Katsushige Ikai, Ikunoshin Kato
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Publication number: 20040192758Abstract: The present invention relates to compounds of the general formula (II) and salts and physiologically functional derivatives thereof, 1Type: ApplicationFiled: December 17, 2003Publication date: September 30, 2004Applicant: 4SC AGInventors: Johann Leban, Stefan Tasler
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Publication number: 20040087806Abstract: Disclosed are novel processes for preparing 1,3-dioxolane nucleosides of general formula I and II: 1Type: ApplicationFiled: August 6, 2003Publication date: May 6, 2004Inventors: Jinfa Du, Kyoichi A. Watanabe
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Patent number: 6706899Abstract: The present invention relates to a novel acyclic chiral compound of Garcinia acid of formula I, Wherein: R2=R5=lower aryl ester or alkyl ester or substituted aryl alcohol or alkyl alcohol R3=substituted aryl ester or alkyl ester or substituted aryl alcohol R1=R4=hydroxyl or And a process for preparing the sameType: GrantFiled: September 5, 2001Date of Patent: March 16, 2004Assignee: Department of Science and Technology, Technology BhavanInventors: Ibrahim Ibnu Saud, Tom Thomas Puthiyaparampil
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Patent number: 6503940Abstract: A methods of treating an infection comprises administering a therapeutically effective amount of a compound described by the Formula (I): wherein: X may be O, S, or NR′ wherein R′ is H or loweralkyl, R1 and R2 may be independently selected from the group consisting of H, loweralkyl, oxyalkyl, alkoxyalkyl, cycloalkyl, aryl, hydroxyalkyl, aminoalkyl, and alkylaminoalkyl; R3 and R4 are each independently selected from the group consisting of H, loweralkyl, halogen, oxyalkyl, oxyaryl, and oxyarylalkyl; R5 is represented by a formula selected from the group consisting of: wherein: X1, X2, and X3 are independently selected from O and S; and R6 and R7 are independently selected from the group consisting of loweralkyl, aryl, alkylaryl, oxyaryl, an ester-containing substituent, and oxyalkyl; or a pharmaceutically acceptable salt thereof.Type: GrantFiled: July 31, 2001Date of Patent: January 7, 2003Assignees: The University of North Carolina at Chapel Hill, Georgia State University Research Foundation, Inc.Inventors: David W. Boykin, M. Syed Rahmathullah, Richard R. Tidwell, James E. Hall
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Patent number: 6495217Abstract: The invention relates to chiral compounds of formula I wherein R1, R2, X, Y1 and Y2 have the meanings defined herein, as well as to liquid crystalline mixtures comprising at least one chiral compound of formula I.Type: GrantFiled: October 4, 1999Date of Patent: December 17, 2002Assignee: Merck Patent GmbHInventor: Louise Farrand
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Patent number: 6486200Abstract: A methods of treating an infection comprises administering a therapeutically effective amount of a compound described by the Formula (I): wherein: X may be O, S, or NR′ wherein R′ is H or loweralkyl; R1 and R2 may be independently selected from the group consisting of H, loweralkyl, oxyalkyl, alkoxyalkyl, cycloalkyl, aryl, hydroxyalkyl, aminoalkyl, and alkylaminoalkyl; R3 and R4 are each independently selected from the group consisting of H, loweralkyl, halogen, oxyalkyl, oxyaryl, and oxyarylalkyl; R5 is represented by a formula selected from the group consisting of: wherein: X1, X2, and X3 are independently selected from O and S; and R6 and R7 are independently selected from the group consisting of loweralkyl, aryl, alkylaryl, oxyaryl, an ester-containing substituent, and oxyalkyl; or a pharmaceutically acceptable salt thereof.Type: GrantFiled: July 7, 2000Date of Patent: November 26, 2002Assignees: The University of North Carolina at Chapel Hill, Georgia State University Research Foundation, Inc.Inventors: David W. Boykin, M. Syed Rahmathullah, Richard R. Tidwell, James E. Hall
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Patent number: 6388104Abstract: Novel 4-methylene-1,3-dioxolanes of the general formula I in which R1 denotes hydrogen or alkyl, X denotes a single bond, C1-C18 alkylene, cycloalkylene, arylalkylene, —CH2(OCH2CH2)n— or —CH2(OCH(CH3)CH2)n—, in which n is an integer from 1 to 100, and Z means a functional group selected from among —OH, —COOR′ or —OCOR′, in which R′ denotes hydrogen or C1-C8 alkyl, are described, as are a process for the production thereof and the intermediates used in this process.Type: GrantFiled: October 5, 2000Date of Patent: May 14, 2002Assignee: Dainippon Ink and Chemicals, Inc.Inventors: Helmut Hartl, Rainer B. Frings, Gerwald F. Grahe
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Patent number: 6376684Abstract: A process for preparing an alkyl phenylglycolic acid is disclosed. It follows the sequence of condensing a substituted acetaldehyde with mandelic acid to provide a 5-phenyl-1,3-dioxolan-4-one, which is condensed with an alkyl ketone or aldehyde to provide a 5-(1-hydroxyalkyl)-5-phenyl-1,3-dioxolan-4-one, which is dehydrated to a 5-(1-alkenyl)-5-phenyl-1,3-dioxolan-4-one. The 5-(1-alkenyl)-5-phenyl-1,3-dioxolan-4-one may be hydrolyzed and reduced to an &agr;-alkylphenylglycolic acid or the hydrolysis and reduction steps may be reversed. The process enables the production of single enantiomers of cyclohexylphenylglycolic acid (CHPGA). An analogous process for racemic CHPGA is disclosed employing racemic mandelic acid and acetone. Novel intermediates in the process are also disclosed.Type: GrantFiled: November 13, 2000Date of Patent: April 23, 2002Assignee: Sepracor Inc.Inventors: Chris Hugh Senanayake, Paul T. Grover
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Patent number: 6291513Abstract: The fungicidal compound 4,5-dimethyl-N-2-propenyl-2-(trimethylsilyl)-3-thiophenecarboxamide (Formula (I)) has shown superior and unexpected control of the growth of the soil-borne fungus Gaeumannomyces graminis (Gg). The present invention provides a novel compound for synthesizing the compound of Formula (I) which uses the compound 4-hydroxy-4,5-dimethyl-2-trimethylsilanyl-dihydrothiophene-3-carboxylic acid allylamide (Formula (II)) as well as novel compounds of synthesizing the allylamide. In addition, Formula (II) itself has unexpectedly been found to provide control of Gg.Type: GrantFiled: July 5, 2000Date of Patent: September 18, 2001Assignee: Monsanto companyInventors: Wendell G. Phillips, Michael K. Mao, Chun Ma, Thomas L. Fevig
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Patent number: 6200997Abstract: The present invention relates to heterocyclyl-substituted phenyl compounds of the formula I, where the substituents have the following meanings: Y is halogen, C1-C4-alkyl, C1-C4-haloalkyl or C1-C4-alkoxy; n is 0, 1 or 2, where the radicals Y may be different if n=2; E is a group A or B, where # denotes the bond to the phenyl ring, and G R&agr;, R&bgr;, Y, n, T and Z are each as defined in the description.Type: GrantFiled: January 25, 1999Date of Patent: March 13, 2001Assignee: BASF AktiengesellschaftInventors: Andreas Gypser, Hubert Sauter, Herbert Bayer, Markus Gewehr, Wassilios Grammenos, Thomas Grote, Roland Götz, Bernd Müller, Arne Ptock, Franz Röhl, Volker Harries, Eberhard Ammermann, Gisela Lorenz, Siegfried Strathmann
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Patent number: 6197817Abstract: Disclosed are compounds of the formula: R represents hydrogen or is a C-3 to C-6 cycloalkyl or C-4 to C-10 straight or branched carbon chain alkyl-cycloalkyl or a group —B—D, where B is C-2 to C-10 straight or branched carbon chain alkyl and D is hydroxy or alkyloxy or 2,3-dihydroxypropyl or 2,3-dialkyloxypropyl or 2,2-dialkyl-1,3-dioxolane-5-methyl, where alkyl is C-1 to C-10 straight or branched carbon chain; W represents CH(CH3)CH2—, C(CH3)2CH2—; Z represents hydrogen, —NHCOR2, —NHCONR2R3 or —NHSO2R2 or —NHSO2NR2R3 or —NHCOOR4 wherein R4 is alkyl of from 1 to about 6 carbon atoms, alkoxyalkyl wherein the alkyl groups may be the same or different and contain from 1 to about 6 carbon atoms, alkoxyaryl, cycloalkyl of from 3 to about 8 carbon atoms.Type: GrantFiled: January 22, 1999Date of Patent: March 6, 2001Assignee: Selectus Pharmaceuticals, Inc.Inventors: William L. Matier, Shyam Patil
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Patent number: 6177576Abstract: A novel composition for supplementing the human diet having a polyol-derived pyruvate (2-keto-propionic-acid) moeity as a component.Type: GrantFiled: August 5, 1998Date of Patent: January 23, 2001Inventor: Michael J. Arnold
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Patent number: 5990158Abstract: New therapeutic agents of carboxylic acid derivatives are disclosed, which are represented by the compounds of the following formula (I) or its pharmaceutically acceptable salts, ##STR1## These compounds are useful as a matrix metalloproteinases (MMPs) inhibitors.Type: GrantFiled: November 3, 1997Date of Patent: November 23, 1999Assignee: Kotobuki Seiyaku Co., Ltd.Inventors: Tsuyoshi Tomiyama, Akira Tomiyama, Takashi Yanagisawa, Atsushi Noda, Yoshinori Kobayashi
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Patent number: 5880295Abstract: The present invention provides a process for the preparation of compounds of formula (V) below, and analogs thereof, which are useful as intermediates for the synthesis of HIV protease inhibitors, including cyclic ureas.Type: GrantFiled: June 19, 1996Date of Patent: March 9, 1999Assignee: DuPont Pharmaceuticals CompanyInventor: Robert Frank Kaltenbach, III
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Patent number: 5846907Abstract: Pyrazol-4-ylbenzoyl compounds of the formula I ##STR1## where Z is a 5- or 6-membered heterocyclic saturated or unsaturated radical, Q is a pyrazole ring and L and M are as defined in the specification, their use as herbicidal compounds and to processes for preparing the compounds.Type: GrantFiled: July 30, 1997Date of Patent: December 8, 1998Assignee: BASF AktiengesellschaftInventors: Wolfgang von Deyn, Regina Luise Hill, Uwe Kardorff, Stefan Engel, Martina Otten, Marcus Vossen, Peter Plath, Harald Rang, Albrecht Harreus, Hartmann Konig, Helmut Walter, Karl-Otto Westphalen, Ulf Misslizt
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Patent number: 5846906Abstract: Herbicidally active phenyldiketone compounds of the formula I ##STR1## in which the substituents have the following meanings: L and M are hydrogen, C.sub.1 -C.sub.6 -alkyl, C.sub.2 -C.sub.6 -alkenyl, C.sub.2 -C.sub.6 -alkynyl, C.sub.1 -C.sub.4 -alkoxy, it being possible for these groups to be unsubstituted or substituted by one to five halogen atoms or C.sub.1 -C.sub.4 -alkoxy, or halogen, cyano, nitro, a group --(Y).sub.n --S(O).sub.m R.sup.7 or a group --(Y).sub.n --CO--R.sup.8,Z is a 5- or 6-membered heterocyclic saturated or unsaturated radical which has one to three hetero atoms selected from the group consisting of oxygen, sulfur or nitrogen and which is unsubstituted or substituted by halogen, cyano, nitro, a group --CO--R.sup.8, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -haloalkyl, C.sub.3 -C.sub.8 -cycloalkyl, C.sub.1 -C.sub.4 -alkoxy, C.sub.1 -C.sub.4 -haloalkoxy, C.sub.1 -C.sub.4 -alkylthio, C.sub.1 -C.sub.4 -haloalkylthio, di-C.sub.1 -C.sub.Type: GrantFiled: July 30, 1997Date of Patent: December 8, 1998Assignee: BASF AktiengesellschaftInventors: Wolfgang von Deyn, Regina Luise Hill, Uwe Kardorff, Stefan Engel, Martina Otten, Marcus Vossen, Peter Plath, Harald Rang, Albrecht Harreus, Hartmann Konig, Helmut Walter, Karl-Otto Westphalen, Ulf Misslitz
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Patent number: 5834498Abstract: The invention relates to the use of derivatives of F-type prostaglandins as ocular hypotensives. The PGF derivatives used in accordance with the invention are represented by the following formula I: ##STR1## wherein wavy line attachments indicate either the alpha (.alpha.) or beta (.beta.) configuration; hatched segments indicate .alpha. configuration, solid triangles are used to indicate .beta. configuration, dashed bonds represent a double bond, or a single bond, R is a substituted heteroaryl radical, R.sup.1 is hydrogen or a lower alkyl radical having up to six carbon atoms, X is selected from the group consisting of --OR.sup.1 and --N(R.sup.1).sub.2, Y is .dbd.O or represents 2 hydrogen radicals. Certain of the compounds represented by Formula I comprise another aspect of the present invention.Type: GrantFiled: October 7, 1996Date of Patent: November 10, 1998Assignee: AllerganInventor: Robert M. Burk
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Patent number: 5770620Abstract: The present invention provides novel protein tyrosine phosphatase modulating compounds having an aryl acrylic acid structure, compositions comprising the compounds, and methods of making and using the same.Type: GrantFiled: October 16, 1995Date of Patent: June 23, 1998Assignee: Ontogen CorporationInventors: Adnan M. M. Mjalli, Xiaodong Cao, Edmund J. Moran
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Patent number: 5733887Abstract: Antiparasitic compounds of the formula (I) ##STR1## where the broken lines between the 3-4 and 4-5 positions represent optional bonds and either (i) the 3-4 optional bond is present; the 4-5 optional bond is absent, R.sup.7 is absent and R.sup.6 is halogen atom, an isothiocyanate group, a diazo group, a thioureido group of formula NHCSNR.sup.15 R.sup.16 where R.sup.15 and R.sup.16 are independently H, C.sub.1 -C.sub.8 alkyl, cycloalkyl, aryl or aralkyl groups, an azido group or a C.sub.1 -C.sub.8 alkylcarbonyl-thio group, or (ii) the 4-5 optional bond is present, the 3-4 optional bond is absent, R.sup.6 is absent and R.sup.7 is a mercapto, C.sub.1 -C.sub.8 alkylthio, oxo, optionally substituted oximino or C.sub.1 -C.sub.8 alkylcarbonylthio group; or R.sup.7 is absent and R.sup.6 is CN, with the provisos that the compounds where R.sup.6 is .alpha.-fluoro and R.sup.2 is CH(CH.sub.3).sub.2, CH(CH.sub.3)C.sub.2 H.sub.5, C(CH.sub.3).dbd.CHCH.sub.3, C(CH.sub.3).dbd.CHC.sub.2 H.sub.5 and C(CH.sub.3).dbd.CHCH(CH.sub.Type: GrantFiled: November 20, 1995Date of Patent: March 31, 1998Assignee: Pfizer Inc.Inventor: Nigel Derek Walshe
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Patent number: 5693827Abstract: A method of inhibiting the growth or replication of viruses of the HIV group is disclosed. Also disclosed are compounds useful in the method and pharmaceutical formulations incorporating such compounds. The method involves the use of compounds having the general formula: ##STR1## wherein the substituent groups are as defined in the specification.Type: GrantFiled: June 7, 1995Date of Patent: December 2, 1997Assignees: Uniroyal Chemical Company, Inc., Uniroyal Chemical Ltd/LteeInventors: William Ashley Harrison, Gary Edward Jewell, Ethel Ellen Felauer, Mark Achiel Dekeyser, Dong Dao-Cong, James Anthony McGuiness, Anupama Mishra, Walter Gerhard Brouwer, Derek James McPhee
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Patent number: 5616711Abstract: A method of producing an aminobutene derivative of formula (I) by allowing a butenol derivative of formula (II) to react with an amide derivative of formula (III) is disclosed. The aminobutene derivative of formula (I) can be deprotected to produce an aminobutene derivative of formula (I-1) or an aminobutene derivative of formula (I-2): ##STR1## The aminobutene derivative of formula (I-A) can also be deprotected to produce the aminobutene derivative of formula (I-B). Any or all of the above aminobutene derivatives are useful as intermediates for producing anti-ulcer drugs, and anti-ulcer drugs having an inhibitory effect on gastric acid secretion based on the antagonism against histamine H.sub.2 receptor.Type: GrantFiled: August 6, 1993Date of Patent: April 1, 1997Assignee: Fujirebio Inc.Inventors: Hiroshi Ikawa, Hajime Matsumoto, Masakatsu Matsumoto, Yasuo Sekine, Masato Nishimura, Akihiko Hosoda
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Patent number: 5571932Abstract: The invention relates to new thermoprocessable copolymers of tetrafluoroethylene constituted by perfluoromethylvinylether (0.5-13% by weight), a fluorinated dioxole (0.05-3%) and tetrafluoroethylene (difference to 100%), particularly useful for coating electric cables by melt extrusion.It relates also to new perfluorodioxoles of formula ##STR1## wherein R.sub.F is a C.sub.1 -C.sub.5, perfluoroalkyl radical; X.sub.1 and X.sub.2 are, independently from each other, F or CF.sub.3 ; and their homopolymers and copolymers, in particular thermoprocessable copolymers as defined above.Type: GrantFiled: November 21, 1995Date of Patent: November 5, 1996Assignee: Ausimont S.p.A.Inventors: Walter Navarrini, Vito Tortelli, Pasqua Colaianna, Julio A. Abusleme
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Patent number: 5559252Abstract: The present invention provides a process for the preparation of compounds of formula (V) below, and analogs thereof, which are useful as intermediates for the synthesis of HIV protease inhibitors, including cyclic ureas.Type: GrantFiled: June 30, 1994Date of Patent: September 24, 1996Assignee: The DuPont Merck Pharmaceutical CompanyInventor: Robert F. Kaltenbach III
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Patent number: 5523320Abstract: N-methyldeacetylcolchiceinamide derivatives represented by the formula ##STR1## wherein R denotes a residue obtained by removing COOH from a C.sub.3 -C.sub.7 sugar carboxylic acid, and hydroxyl groups present in the residue may properly be protected with a protecting group for a hydroxyl group.The N-methyldeacetylcolchiceinamide derivatives have less toxicity and strong effect for inhibiting proliferation of tumor cells, and are expected to be used as a carcinostatic.Type: GrantFiled: January 3, 1995Date of Patent: June 4, 1996Assignee: Ohgen Research Laboratories, Ltd.Inventor: Kiyoshi Akiyama
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Patent number: 5488166Abstract: Provided by the present invention is a process for the biocatalytic synthesis of optically pure sphingosines from achiral starting material. The stereoisomers of sphingosine are prepared from chiral arene diols using stereospecific reaction techniques to obtain the desired sphingosine or derivative thereof.Type: GrantFiled: January 23, 1995Date of Patent: January 30, 1996Assignee: Virginia Tech Intellectual Properties, Inc.Inventor: Tomas Hudlicky
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Patent number: 5395947Abstract: Disclosed herein are novel platinum(II) complexes having a potent anti-tumor activity which are represented by the formula (1), ##STR1## wherein R.sub.1 and R.sub.2, which may be the same or different, are a hydrogen atom or a C.sub.1-4 alkyl group, respectively, or jointly form a cycloalkane group together with the carbon atom attached thereto; two Xs jointly form a group represented by formula (a) or (b) wherein, R.sub.3 is a hydrogen atom or a methyl group; R.sub.4 and R.sub.5, which may be the same or different, are a hydrogen atom or a C.sub.1-4 alkyl group, respectively, or jointly form a cyclobutane together with the carbon thereto; and the absolute configurations at the respective chiral centers in the 4,5-bis(aminomethyl)-1,3-dioxolane moiety are (4R,5R) or (4S,5S); processes for the preparing the same; and their use for treating animal or human cancer.Type: GrantFiled: September 14, 1993Date of Patent: March 7, 1995Assignee: Sunkyong Industries, Ltd.Inventors: Dae-Kee Kim, Ganghyeok Kim, Jongsik Gam, Yong B. Cho, Hun T. Kim, Joo H. Tai, Key H. Kim
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Patent number: 5371069Abstract: The present invention provides organoleptic compositions which upon thermolyis, hydrolysis or both, release an odorant molecule. They find utility, for example, in tobacco, in tobacco paper, and as additives to food, beverages or gum. The compositions contain one or more dicarboalkoxy dioxolane derivatives having the following formula: ##STR1## wherein R.sup.1 and R.sup.2 are, independently, --CO.sub.2 R.sup.3 wherein R.sup.3 is --H.sub.3 or lower alkyl, provided that in at least one of R.sup.1 and R.sup.2, R.sup.3 is lower alkyl; wherein Z is a direct bond, or --CH.dbd.C(R.sup.4)--; where R.sup.4 is --H or alkyl group; and Y is ##STR2## where R.sup.5 and R.sup.6 are independently --H, lower alkyl or --OR.sup.7 where R.sup.7 is --H or lower alkyl.Type: GrantFiled: April 17, 1992Date of Patent: December 6, 1994Assignee: Giuaudan-Roure CorporationInventors: Philip A. Christenson, Paul J. Riker, Denise A. Anderson, John M. Yurecko, Jr.
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Patent number: 5306844Abstract: A d- or l-tartaric acid amide derivative serving as a host compound and a method of producing the amide derivative which combines with a guest compound to form a clathrate compound and which is expressed by the following Formula (A) or (B): ##STR1##Type: GrantFiled: May 11, 1990Date of Patent: April 26, 1994Assignee: Mitsubishi Gas Chemical Company, Inc.Inventors: Fumio Toda, Koichi Tanaka
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Patent number: 5302587Abstract: A novel platinum (II) complex represented by the following formula (A): ##STR1## wherein R.sub.1 represents C.sub.1 -C.sub.5 lower hydrocarbon group, R.sub.2 and R.sub.3 represents hydrogen atom or C.sub.1 -C.sub.3 lower hydrocarbon group, the configuration of 1,2-diaminocyclohexane being cis, trans-l- or trans-d-. Since the platinum (II) complex has a strong anti-tumor activity and its toxicity is low, it is useful as an agent for treating malignant tumor.Type: GrantFiled: September 9, 1991Date of Patent: April 12, 1994Assignee: Toray Industries, Inc.Inventors: Go Hata, Masato Mutoh, Hideyuki Hashimoto
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Patent number: 5268491Abstract: A process for the selective dehalogenation in position 5 of the naphthalenic nucleus of compounds of formula ##STR1## (wherein X, X.sub.1 and R have the meanings reported in the description) by treatment with a dehalogenating agent selected among hydrogen sulfide, aliphatic thiols or mixtures thereof in an inert anhydrous solvent at acid pH.Type: GrantFiled: October 16, 1992Date of Patent: December 7, 1993Assignee: Zambon Group S.p.A.Inventors: Marco Villa, Paolo Cavalleri
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Patent number: 5256664Abstract: 2-(3-[4-(3-Halophenyl)-1-piperazinyl]propyl derivatives of certain 4-alkyl- or 4-phenoxyalkyl-2,4-dihydro-3H-1,2,4-triazol-3-ones and triazol-3,5-diones are psychotropic agents having promise as antidepressants by virtue of their receptor site binding affinity profiles and animal pharmacology.Type: GrantFiled: April 28, 1992Date of Patent: October 26, 1993Assignee: Bristol-Myers Squibb CompanyInventors: Robert F. Mayol, George M. Luke
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Patent number: 5235074Abstract: This invention process for preparing 1,3-dioxolanes of formula: ##STR1## wherein; X.sub.1, X.sub.2, X.sub.3 and X.sub.4, like or different from one another, represent F, Cl, Br, I, CF.sub.2 OSO.sub.2 F, SO.sub.2 F, C(O)F, H, perhaloalkyl or oxyperhaloalkyl radicals containing from 1 to 5 carbon atoms,X.sub.5 and X.sub.6, like or different from each other, represent F or CF.sub.3. Said process is characterized in that a bis(fluoroxy)perfluoroalkane is reacted, at a temperature ranging from -140.degree. C. to +60.degree. C., with a halogenated olefin.This invention also relates to new 1,3-dioxolanes of formula (I) belonging to the class defined hereinbefore.Type: GrantFiled: March 6, 1992Date of Patent: August 10, 1993Assignee: Ausimont S.p.A.Inventors: Walter Navarrini, Simonetta Fontana, Vittorio Montanari
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Patent number: 5233058Abstract: Partially fluorinated compounds of specified formulas that are useful as chemical intermediates and monomers are disclosed. Partially fluorinated polymers prepared from one of these compounds are also disclosed. Fluoro-2,2-dimethyldioxolanes and copolymers thereof are further disclosed.Type: GrantFiled: October 21, 1991Date of Patent: August 3, 1993Assignee: E. I. Du Pont de Nemours and CompanyInventors: Douglas R. Anton, William B. Farnham, Ming-Hong Hung, Ronald J. McKinney
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Patent number: 5227500Abstract: There are disclosed halogenated dioxolanes of a specified formula, dioxoles made therefrom, polymers of the dioxoles, and processes for making the dioxolanes.Type: GrantFiled: July 17, 1991Date of Patent: July 13, 1993Assignee: E. I. Du Pont de Nemours and CompanyInventor: Carl G. Krespan
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Patent number: 5225576Abstract: This invention relates to a process for preparing 1,3-dioxolanes of formula: ##STR1## wherein; X.sub.1, X.sub.2, X.sub.3 and X.sub.4, like or different from one another, represent F, Cl, Br, I, CF.sub.2 OSO.sub.2 F, SO.sub.2 F, C(O)F, H, perhaloalkyl or oxyperhaloalkyl radicals containing from 1 to 5 carbon atoms,X.sub.5 and X.sub.6, like or different from each other, represent F or CF.sub.3. Said process is characterized in that a bis(fluoroxy)perfluoroalkane is reacted, at a temperature ranging from -140.degree. C. to +60.degree. C., with a halogenated olefin.This invention also relates to new 1,3-dioxolanes of formula (I) belonging to the class defined hereinbefore.Type: GrantFiled: June 7, 1991Date of Patent: July 6, 1993Assignee: Ausimont S.p.AInventors: Walter Navarrini, Simonetta Fontana, Vittorio Montanari
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Patent number: 5217991Abstract: Non-peptidyl compounds characterized generally as cycloalkyl/cycloalkylalkyl-N-terminal cycloalkoxy-C-terminal amino hydroxy .beta.-amino acid derivatives are useful as renin inhibitors for treatment of hypertension. Compounds of particular interest are of the formula ##STR1## wherein R.sub.1 is selected from cycloalkyl and cycloalkylalkyl groups, wherein said cycloalkyl group contains three to about eight carbon atoms and the acyclic alkyl portion of said cycloalkylalkyl group contains one to about eight carbon atoms; wherein each of R.sub.2 and R.sub.4 is independently selected from hydrido and methyl; wherein R.sub.3 is methyl or ethyl: wherein R.sub.5 is cyclohexylmethyl; wherein R.sub.6 and R.sub.Type: GrantFiled: May 28, 1992Date of Patent: June 8, 1993Assignee: G. D. Searle & Co.Inventors: Gunnar J. Hanson, John S. Baran, Dave Weissing, Mark Russell
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Patent number: 5216013Abstract: Non-peptidyl compounds characterized generally as heterocyclic acyl aminodiol .beta.-amino acid derivatives are useful as renin inhibitors for treatment of hypertension. Compounds of particular interest are compounds of the formula ##STR1## wherein R.sub.1 is selected from aryl and aralkyl groups represented by ##STR2## and wherein R.sub.1 may be further selected from heteroaryl and heteroaralkyl represented by ##STR3## wherein each of T and A is independently selected from N and CH; wherein n is a number selected from zero through five, inclusive; wherein X is selected from oxygen atom, methylamino and NH; wherein each of Y and Z is independently selected from chloro, fluoro, methoxy and dimethylamino; wherein Q is oxygen atom; and wherein each of T and A is independently selected from N and CH; wherein each of R.sub.2 and R.sub.4 is independently selected from hydrido and methyl; wherein R.sub.3 is selected from methyl and ethyl; wherein R.sub.5 is cyclohexylmethyl; wherein R.sub.6 is hydroxy; wherein R.Type: GrantFiled: July 16, 1992Date of Patent: June 1, 1993Assignee: G. D. Searle & Co.Inventor: Gunnar J. Hanson
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Patent number: 5214167Abstract: Process comprising heating a dioxole at 100.degree.-400.degree. C. for a sufficient time to convert the dioxole to an epoxide, for example, bis-2,2-trifluoromethyl-4,5-difluoro-1,3-dioxole to 2,3-epoxy-3-trifluoromethyl-4-trifluorobutyryl fluoride.Type: GrantFiled: February 18, 1992Date of Patent: May 25, 1993Assignee: E. I. Du Pont de Nemours and CompanyInventors: Ming-Hong Hung, Paul R. Resnick
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Patent number: 5177222Abstract: 1,1-Dialkoxy-2-oxo-6-aryl-3,5-alkadienes of the general formula I ##STR1## where Ar is a phenyl, biphenyl or naphthyl radical which may be substituted by one, two or three C.sub.1 -C.sub.4 -alkyl groups, C.sub.1 -C.sub.4 -alkoxy groups, hydroxyl groups, phenoxy groups, amino groups which may be mono- or di-C.sub.1 -C.sub.4 -alkyl-substituted, halogen atoms or a methylenedioxy group, the substituents being identical or different,R.sup.1 is hydrogen or C.sub.1 -C.sub.8 -alkyl,R.sup.2 is hydrogen, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.10 -alkoxycarbonyl or C.sub.1 -C.sub.10 -acyl,the radicals R.sup.3 are C.sub.1 -C.sub.8 -alkyl groups which may be bonded to one another with formation of a five-membered or six-membered ring andR.sup.4 is hydrogen or C.sub.1 -C.sub.4 -alkyl, are used as sunscreen agents in cosmetic preparations.Type: GrantFiled: November 5, 1990Date of Patent: January 5, 1993Assignee: BASF AktiengesellschaftInventors: Helmut Guembel, Joachim Paust, Karin Sperling-Vietmeier, Rainer Becker