Having -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To The Hetero Ring Patents (Class 549/450)
  • Patent number: 11603497
    Abstract: 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: Grant
    Filed: January 23, 2020
    Date of Patent: March 14, 2023
    Assignee: CLARIANT INTERNATIONAL LTD
    Inventors: Antonio Pedro de Oliveira Felho, Aline Yae Kina, Grahame N. Taylor, Fabian Schneider, Julie Murison, Stefan Hauck, Mike Sahl, Matthias Krull, Jonathan James Wylde
  • Publication number: 20140155635
    Abstract: 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: Application
    Filed: October 29, 2013
    Publication date: June 5, 2014
    Applicant: KOREA INSTITUTE OF SCIENCE AND TECHNOLOGY
    Inventors: Tae Bo SIM, Ho Jong Yoon, Ji Nyeo Kim
  • Publication number: 20120130092
    Abstract: 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: Application
    Filed: December 6, 2011
    Publication date: May 24, 2012
    Inventors: Teruhiko Ishikawa, Seiki Saito, Takayuki Kudoh, Kotaro Suto, Hironori Nishiuchi, Makoto Okada, Masatoshi Taniguchi
  • Patent number: 8148554
    Abstract: 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: Grant
    Filed: August 12, 2010
    Date of Patent: April 3, 2012
    Assignee: Eisai R&D Management Co., Ltd.
    Inventors: Boris M. Seletsky, Melvin J. Yu, Wanjun Zheng
  • Patent number: 7825126
    Abstract: 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: Grant
    Filed: September 2, 2005
    Date of Patent: November 2, 2010
    Assignee: The United States of America as represented by the Department of Health and Human Services
    Inventors: Kenneth A. Jacobson, Bhalchandra V. Joshi, Susanna Tchilibon
  • Publication number: 20100273968
    Abstract: 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: Application
    Filed: December 17, 2008
    Publication date: October 28, 2010
    Applicant: SOLVAY SOLEXIS S.P.A.
    Inventors: Giuseppe Marchionni, Vito Tortelli
  • Publication number: 20080262230
    Abstract: 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: Application
    Filed: March 29, 2006
    Publication date: October 23, 2008
    Applicant: Nippon Zoki Pharmaceutical Co., LTD.
    Inventors: Kunihiko Higashiura, Takashi Ogino, Kazuhito Furukawa
  • Patent number: 7271274
    Abstract: 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: Grant
    Filed: April 20, 2005
    Date of Patent: September 18, 2007
    Assignee: AhteroGenics, Inc.
    Inventors: Charles Q. Meng, M. David Weingarten
  • Patent number: 7060727
    Abstract: 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: Grant
    Filed: December 11, 2003
    Date of Patent: June 13, 2006
    Assignee: XenoPort, Inc.
    Inventor: Mark A. Gallop
  • Patent number: 6844375
    Abstract: 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: Grant
    Filed: August 23, 2001
    Date of Patent: January 18, 2005
    Assignee: Dainippon Ink and Chemicals, Inc.
    Inventors: Helmut Hartl, Rainer B. Frings, Gerwald F. Grahe
  • Patent number: 6809091
    Abstract: 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: Grant
    Filed: June 28, 2000
    Date of Patent: October 26, 2004
    Assignee: Takara Bio Inc.
    Inventors: Yoko Tatsumi, Hiroaki Sagawa, Hiromu Ohnogi, Eiji Kobayashi, Hua-Kang Wu, Nobuto Koyama, Katsushige Ikai, Ikunoshin Kato
  • Publication number: 20040192758
    Abstract: The present invention relates to compounds of the general formula (II) and salts and physiologically functional derivatives thereof, 1
    Type: Application
    Filed: December 17, 2003
    Publication date: September 30, 2004
    Applicant: 4SC AG
    Inventors: Johann Leban, Stefan Tasler
  • Publication number: 20040087806
    Abstract: Disclosed are novel processes for preparing 1,3-dioxolane nucleosides of general formula I and II: 1
    Type: Application
    Filed: August 6, 2003
    Publication date: May 6, 2004
    Inventors: Jinfa Du, Kyoichi A. Watanabe
  • Patent number: 6706899
    Abstract: 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 same
    Type: Grant
    Filed: September 5, 2001
    Date of Patent: March 16, 2004
    Assignee: Department of Science and Technology, Technology Bhavan
    Inventors: Ibrahim Ibnu Saud, Tom Thomas Puthiyaparampil
  • Patent number: 6503940
    Abstract: 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: Grant
    Filed: July 31, 2001
    Date of Patent: January 7, 2003
    Assignees: 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
  • Patent number: 6495217
    Abstract: 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: Grant
    Filed: October 4, 1999
    Date of Patent: December 17, 2002
    Assignee: Merck Patent GmbH
    Inventor: Louise Farrand
  • Patent number: 6486200
    Abstract: 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: Grant
    Filed: July 7, 2000
    Date of Patent: November 26, 2002
    Assignees: 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
  • Patent number: 6388104
    Abstract: 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: Grant
    Filed: October 5, 2000
    Date of Patent: May 14, 2002
    Assignee: Dainippon Ink and Chemicals, Inc.
    Inventors: Helmut Hartl, Rainer B. Frings, Gerwald F. Grahe
  • Patent number: 6376684
    Abstract: 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: Grant
    Filed: November 13, 2000
    Date of Patent: April 23, 2002
    Assignee: Sepracor Inc.
    Inventors: Chris Hugh Senanayake, Paul T. Grover
  • Patent number: 6291513
    Abstract: 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: Grant
    Filed: July 5, 2000
    Date of Patent: September 18, 2001
    Assignee: Monsanto company
    Inventors: Wendell G. Phillips, Michael K. Mao, Chun Ma, Thomas L. Fevig
  • Patent number: 6200997
    Abstract: 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: Grant
    Filed: January 25, 1999
    Date of Patent: March 13, 2001
    Assignee: BASF Aktiengesellschaft
    Inventors: 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
  • Patent number: 6197817
    Abstract: 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: Grant
    Filed: January 22, 1999
    Date of Patent: March 6, 2001
    Assignee: Selectus Pharmaceuticals, Inc.
    Inventors: William L. Matier, Shyam Patil
  • Patent number: 6177576
    Abstract: A novel composition for supplementing the human diet having a polyol-derived pyruvate (2-keto-propionic-acid) moeity as a component.
    Type: Grant
    Filed: August 5, 1998
    Date of Patent: January 23, 2001
    Inventor: Michael J. Arnold
  • Patent number: 5990158
    Abstract: 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: Grant
    Filed: November 3, 1997
    Date of Patent: November 23, 1999
    Assignee: Kotobuki Seiyaku Co., Ltd.
    Inventors: Tsuyoshi Tomiyama, Akira Tomiyama, Takashi Yanagisawa, Atsushi Noda, Yoshinori Kobayashi
  • Patent number: 5880295
    Abstract: 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: Grant
    Filed: June 19, 1996
    Date of Patent: March 9, 1999
    Assignee: DuPont Pharmaceuticals Company
    Inventor: Robert Frank Kaltenbach, III
  • Patent number: 5846907
    Abstract: 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: Grant
    Filed: July 30, 1997
    Date of Patent: December 8, 1998
    Assignee: BASF Aktiengesellschaft
    Inventors: 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
  • Patent number: 5846906
    Abstract: 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: Grant
    Filed: July 30, 1997
    Date of Patent: December 8, 1998
    Assignee: BASF Aktiengesellschaft
    Inventors: 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
  • Patent number: 5834498
    Abstract: 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: Grant
    Filed: October 7, 1996
    Date of Patent: November 10, 1998
    Assignee: Allergan
    Inventor: Robert M. Burk
  • Patent number: 5770620
    Abstract: 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: Grant
    Filed: October 16, 1995
    Date of Patent: June 23, 1998
    Assignee: Ontogen Corporation
    Inventors: Adnan M. M. Mjalli, Xiaodong Cao, Edmund J. Moran
  • Patent number: 5733887
    Abstract: 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: Grant
    Filed: November 20, 1995
    Date of Patent: March 31, 1998
    Assignee: Pfizer Inc.
    Inventor: Nigel Derek Walshe
  • Patent number: 5693827
    Abstract: 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: Grant
    Filed: June 7, 1995
    Date of Patent: December 2, 1997
    Assignees: Uniroyal Chemical Company, Inc., Uniroyal Chemical Ltd/Ltee
    Inventors: 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
  • Patent number: 5616711
    Abstract: 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: Grant
    Filed: August 6, 1993
    Date of Patent: April 1, 1997
    Assignee: Fujirebio Inc.
    Inventors: Hiroshi Ikawa, Hajime Matsumoto, Masakatsu Matsumoto, Yasuo Sekine, Masato Nishimura, Akihiko Hosoda
  • Patent number: 5571932
    Abstract: 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: Grant
    Filed: November 21, 1995
    Date of Patent: November 5, 1996
    Assignee: Ausimont S.p.A.
    Inventors: Walter Navarrini, Vito Tortelli, Pasqua Colaianna, Julio A. Abusleme
  • Patent number: 5559252
    Abstract: 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: Grant
    Filed: June 30, 1994
    Date of Patent: September 24, 1996
    Assignee: The DuPont Merck Pharmaceutical Company
    Inventor: Robert F. Kaltenbach III
  • Patent number: 5523320
    Abstract: 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: Grant
    Filed: January 3, 1995
    Date of Patent: June 4, 1996
    Assignee: Ohgen Research Laboratories, Ltd.
    Inventor: Kiyoshi Akiyama
  • Patent number: 5488166
    Abstract: 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: Grant
    Filed: January 23, 1995
    Date of Patent: January 30, 1996
    Assignee: Virginia Tech Intellectual Properties, Inc.
    Inventor: Tomas Hudlicky
  • Patent number: 5395947
    Abstract: 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: Grant
    Filed: September 14, 1993
    Date of Patent: March 7, 1995
    Assignee: Sunkyong Industries, Ltd.
    Inventors: Dae-Kee Kim, Ganghyeok Kim, Jongsik Gam, Yong B. Cho, Hun T. Kim, Joo H. Tai, Key H. Kim
  • Patent number: 5371069
    Abstract: 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: Grant
    Filed: April 17, 1992
    Date of Patent: December 6, 1994
    Assignee: Giuaudan-Roure Corporation
    Inventors: Philip A. Christenson, Paul J. Riker, Denise A. Anderson, John M. Yurecko, Jr.
  • Patent number: 5306844
    Abstract: 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: Grant
    Filed: May 11, 1990
    Date of Patent: April 26, 1994
    Assignee: Mitsubishi Gas Chemical Company, Inc.
    Inventors: Fumio Toda, Koichi Tanaka
  • Patent number: 5302587
    Abstract: 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: Grant
    Filed: September 9, 1991
    Date of Patent: April 12, 1994
    Assignee: Toray Industries, Inc.
    Inventors: Go Hata, Masato Mutoh, Hideyuki Hashimoto
  • Patent number: 5268491
    Abstract: 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: Grant
    Filed: October 16, 1992
    Date of Patent: December 7, 1993
    Assignee: Zambon Group S.p.A.
    Inventors: Marco Villa, Paolo Cavalleri
  • Patent number: 5256664
    Abstract: 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: Grant
    Filed: April 28, 1992
    Date of Patent: October 26, 1993
    Assignee: Bristol-Myers Squibb Company
    Inventors: Robert F. Mayol, George M. Luke
  • Patent number: 5235074
    Abstract: 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: Grant
    Filed: March 6, 1992
    Date of Patent: August 10, 1993
    Assignee: Ausimont S.p.A.
    Inventors: Walter Navarrini, Simonetta Fontana, Vittorio Montanari
  • Patent number: 5233058
    Abstract: 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: Grant
    Filed: October 21, 1991
    Date of Patent: August 3, 1993
    Assignee: E. I. Du Pont de Nemours and Company
    Inventors: Douglas R. Anton, William B. Farnham, Ming-Hong Hung, Ronald J. McKinney
  • Patent number: 5227500
    Abstract: There are disclosed halogenated dioxolanes of a specified formula, dioxoles made therefrom, polymers of the dioxoles, and processes for making the dioxolanes.
    Type: Grant
    Filed: July 17, 1991
    Date of Patent: July 13, 1993
    Assignee: E. I. Du Pont de Nemours and Company
    Inventor: Carl G. Krespan
  • Patent number: 5225576
    Abstract: 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: Grant
    Filed: June 7, 1991
    Date of Patent: July 6, 1993
    Assignee: Ausimont S.p.A
    Inventors: Walter Navarrini, Simonetta Fontana, Vittorio Montanari
  • Patent number: 5217991
    Abstract: 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: Grant
    Filed: May 28, 1992
    Date of Patent: June 8, 1993
    Assignee: G. D. Searle & Co.
    Inventors: Gunnar J. Hanson, John S. Baran, Dave Weissing, Mark Russell
  • Patent number: 5216013
    Abstract: 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: Grant
    Filed: July 16, 1992
    Date of Patent: June 1, 1993
    Assignee: G. D. Searle & Co.
    Inventor: Gunnar J. Hanson
  • Patent number: 5214167
    Abstract: 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: Grant
    Filed: February 18, 1992
    Date of Patent: May 25, 1993
    Assignee: E. I. Du Pont de Nemours and Company
    Inventors: Ming-Hong Hung, Paul R. Resnick
  • Patent number: 5177222
    Abstract: 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: Grant
    Filed: November 5, 1990
    Date of Patent: January 5, 1993
    Assignee: BASF Aktiengesellschaft
    Inventors: Helmut Guembel, Joachim Paust, Karin Sperling-Vietmeier, Rainer Becker