Patents Examined by John Kight
  • Patent number: 6063810
    Abstract: Compounds of formula (I), wherein A is a hydrogen atom or a hydroxyl group; B is a hydrogen atom or a C.sub.1-8 alkyl, C.sub.1-8 alkenyl, C.sub.1-8 fluoroalkyl or C.sub.1-8 perfluoroalkyl group; each of R.sub.1, R.sub.2 and R.sub.5, which are the same or different, is a hydrogen atom, a halogen such as chlorine, bromine or fluorine, a C.sub.1-8 alkyl, C.sub.1-8 alkenyl, C.sub.3-8 cycloalkyl, C.sub.3-8 cycloalkenyl, C.sub.6, C.sub.10 or C.sub.14 aryl, C.sub.1-6 alkoxycarbonyl, C.sub.1-6 hydroxyalkyl, C.sub.1-6 alkoxyalkyl, C.sub.1-6 alkoxy, C.sub.1-8 fluoroalkyl or C.sub.1-8 perfluoroalkyl group, or R.sub.1 and R.sub.2 taken together form a C.sub.3-8 cycloalkyl, C.sub.3-8 cycloalkenyl or C.sub.6, C.sub.10 or C.sub.14 aryl ring, except for compounds in which R.sub.1 and R.sub.2 are both hydrogen; each of R.sub.3 and R.sub.4, which are the same or different, is a hydrogen atom or a C.sub.1-8 alkyl, C.sub.1-8 alkenyl, C.sub.3-8 cycloalkyl or C.sub.3-8 cycloalkenyl group, or R.sub.3 and R.sub.
    Type: Grant
    Filed: August 31, 1998
    Date of Patent: May 16, 2000
    Assignee: Synthelabo
    Inventors: Christophe Philippo, Gilles Courtemanche, Eykmar Fett, Marie Claire Orts, Philippe Bovy, Stephen Eric O'Connor, Anne Marie Galzin
  • Patent number: 6063927
    Abstract: Piperidine compounds, processes for preparing them, pharmaceutical compositions comprising them and their use in therapy are disclosed.
    Type: Grant
    Filed: April 23, 1999
    Date of Patent: May 16, 2000
    Assignee: SmithKline Beecham plc
    Inventors: Andrew Simon Craig, Alan David Jones, Deirdre O'Keeffe, Neal Ward
  • Patent number: 6063938
    Abstract: Disclosed is a process for producing .epsilon.-caprolactone which comprises distilling a reaction mixture obtained by oxidation of cyclohexanone to separate impurities, wherein .epsilon.-caprolactone separated in a rectifying column is contacted with an oxygen-containing gas and then distilled. Thereby, a high quality of .epsilon.-caprolactone of in which no coloration occurs during long time preservation can be produced by industrial advantages.
    Type: Grant
    Filed: July 25, 1997
    Date of Patent: May 16, 2000
    Assignee: Mitsubishi Gas Chemical Company, Inc.
    Inventors: Kazuo Tanaka, Kengi Nakaya, Atsushi Ohkoshi, Hideaki Fujita
  • Patent number: 6063181
    Abstract: 1,7-Disubstituted perylene-3,4,9,10-tetracarboxylic dianhydrides I and perylere-3,4,9,10-tetracarboxylic acids Ia ##STR1## where L.sup.1, L.sup.2 independently of one another are 1,2-ethylene, 1,2-ethenylene and 1,2-ethynylene, andR.sup.1, R.sup.2 independently of one another are hydrogen or substituted or unsubstituted C.sub.1 -C.sub.30 -alkyl,their preparation and use as pigments, laser dyes and precursors for preparing fluorescent dyes, polymeric colorants, pigments and pigment additives, and also 1,7-disubstituted perylene-3,4,9,10-tetracarboxylic diimides (VI) as their intermediates.
    Type: Grant
    Filed: June 18, 1998
    Date of Patent: May 16, 2000
    Assignee: BASF Aktiengesellschaft
    Inventors: Arno Bohm, Harald Arms, Georg Henning, Peter Blaschka
  • Patent number: 6060483
    Abstract: The present invention provides the new use in the treatment of neurodegenerative diseases with ergoline derivatives of formula (I) ##STR1## wherein R.sub.1 represents a hydrogen atom or a linear or branched C.sub.1 -C.sub.5 alkyl or C.sub.2 -C.sub.5 alkenyl group optionally substituted with a C.sub.3 -C.sub.7 cycloalkyl, a hydroxy group or a R.sub.3 -substituted phenyl group wherein R.sub.3 is a hydroxy or a hydroxymethyl group; R.sub.2 represents a hydrogen atom or a linear or branched C.sub.1 -C.sub.5 alkyl or a C.sub.2 -C.sub.5 alkenyl group optionally substituted with a hydroxy group, or a R.sub.3 -substituted phenyl group wherein R.sub.3 is as above defined, or with a C.sub.1 -C.sub.5 alkoxy group; the symbols--at positions 2,3 and 8, 9 independently denote a single or double chemical bond and Z represents a group (CH.sub.2).sub.n OH, wherein n is 0 or an integer from 1 to 3, or a group C(R.sub.4).sub.2 OH wherein R.sub.4 is a C.sub.1 -C.sub.
    Type: Grant
    Filed: December 28, 1998
    Date of Patent: May 9, 2000
    Assignee: Pharmacia & Upjohn S.p.A.
    Inventors: Sergio Mantegani, Enzo Brambilla, Nicola Carfagna, Mario Varasi
  • Patent number: 6060628
    Abstract: A manufacturing method for 1,1,1,3,3-pentafluoropropane in which the method is composed of:step A wherein 2,3-dichloro-1,1,1,3,3-pentafluoropropane is reduced with hydrogen under the presence of hydrogenation catalyst in gaseous phase;step B wherein all of the products of the said step A are introduced into a cooler condenser, so that either a component of hydrogen and hydrogen chloride as non-condensation component and another compoment of 1,1,1,3,3-pentafluoropropane as condensation components or a component of hydrogen as non-condensation component and another component of hydrogen chloride and 1,1,1,3,3-pentafluoropropane as condensation component are obtained;step C wherein hydrogen is separated from the non-condensation component of the said step B, and it is recycled to the said step A; andstep D wherein 1,1,1,3,3-pentafluoropropane is separated from the condensation component of the said step B.
    Type: Grant
    Filed: August 26, 1997
    Date of Patent: May 9, 2000
    Assignee: Daikin Industries Ltd.
    Inventors: Hirokazu Aoyama, Noriaki Shibata, Akinori Yamamoto
  • Patent number: 6057333
    Abstract: Discorhabdin compounds are derived from marine sponges of the genus Batzella or prepared by synthetic methods. These compounds, and pharmaceutical compositions containing them as active ingredients, are useful as immunomodulatory, antitumor agents, and/or caspase inhibitors.
    Type: Grant
    Filed: July 24, 1998
    Date of Patent: May 2, 2000
    Assignee: Harbor Branch Oceanographic Institution, Inc.
    Inventors: Sarath P. Gunaskera, Peter J. McCarthy, Shirley A. Pomponi, Amy E. Wright, Ross E. Longley
  • Patent number: 6057441
    Abstract: This invention concerns the compounds of formula (I), ##STR1## the N-oxide forms, the pharmaceutically acceptable addition salts and the stereoisomeric forms thereof, wherein n is zero to 6; p and q are zero to 4; r is zero to 5; R.sup.1 and R.sup.2 each independently are hydrogen; optionally substituted C.sub.1-6 alkyl; C.sub.1-6 alkylcarbonyl; halomethylcarbonyl; or R.sup.1 and R.sup.2 taken together with the nitrogen atom to which they are attached may form a morpholinyl ring or an optionally substituted heterocycle; each R.sup.3 and R.sup.4 independently are halo, cyano, hydroxy, halomethyl, halomethoxy, carboxyl, nitro, amino, mono- or di(C.sub.1-6 alkyl)amino, C.sub.1-6 alkylcarbonylamino, aminosulfonyl, mono- or di(C.sub.1-6 alkyl)aminosulfonyl, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy, C.sub.1-6 alkylcarbonyl, C.sub.1-6 alkyloxycarbonyl; each R.sup.5 independently is C.sub.1-6 alkyl, cyano or halomethyl; X is CR.sup.6 R.sup.7, NR.sup.8, O, S, S(.dbd.O) or S(.dbd.O).sub.
    Type: Grant
    Filed: October 6, 1998
    Date of Patent: May 2, 2000
    Assignee: Janssen Pharmaceutica, N.V.
    Inventors: Pilar Gil-Lopetegui, Francisco Javier Fernandez-Gadea, Theo Frans Meert
  • Patent number: 6057371
    Abstract: The invention relates to methods for the treatment of central nervous system disorders, gastrointestinal disorders, drug abuse, angina, migraine, hypertension and depression by administering a pharmaceutical composition comprising an effective amount of certain sigma receptor ligands to a patient in need of such treatment. The invention further relates to novel sigma receptor ligands having high binding to the sigma receptor and pharmaceutical compositions thereof. Unexpectedly, certain of the sigma receptor ligands of the present invention have selectivity for the sigma receptor over the DA, PCP and 5-HT.sub.1A receptors.
    Type: Grant
    Filed: June 10, 1992
    Date of Patent: May 2, 2000
    Assignee: Virginia Commonwealth University
    Inventor: Richard A. Glennon
  • Patent number: 6054464
    Abstract: A compound of formula ##STR1## X is O or S; Y is O or S; G and D are independently nitrogen or carbon with the proviso that no more than one of G, D, or E is nitrogen; E is N or C--R.sub.4 ; R.sub.1 is hydrogen or methyl; R.sub.2 is hydrogen or fluoro; R.sub.3 is hydrogen, halogen, C.sub.1 to C.sub.3 alkyl, --OR.sub.5, --CN, --CONH.sub.2, --CO.sub.2 R.sub.5, --NR .sub.5 R.sub.6 or phenyl optionally substituted with one to three of the following substituents: halogen, C.sub.1 to C.sub.3 alkyl, --NO.sub.2, --CN, or --OCH.sub.3 ; R.sub.4 is hydrogen, halogen, C.sub.1 to C.sub.3 alkyl, --OR.sub.5, --CN, --CONH.sub.2, --CO.sub.2 R.sub.5, --NR.sub.5 R.sub.6 or phenyl optionally substituted with one to three of the following substituents: halogen, C.sub.1 to C.sub.3 alkyl, --NO.sub.2, --CN, or --OCH.sub.3 ;or R.sub.2 and R.sub.3 or R.sub.3 and R.sub.4 may together represent a fused phenyl ring optionally substituted with one or two of the following substituents: halogen, C.sub.1 to C.sub.3 alkyl, --NO.sub.
    Type: Grant
    Filed: March 26, 1999
    Date of Patent: April 25, 2000
    Assignee: Astra Aktiebolag
    Inventors: John Macor, Edwin Wu
  • Patent number: 6054586
    Abstract: A process for preparing 4-methylenepiperidine having a formula (VII): ##STR1## which comprises reacting an isonipecotate having a formula (I): ##STR2## wherein R.sup.1 is methyl group or ethyl group, with an acylating agent having a formula (II): R.sup.2 X or a formula (II'): (R.sup.2).sub.2 O wherein R.sup.2 is benzoyl group or acetyl group and X is chlorine atom or bromine atom, in the presence or the absence of a base, reducing the resulting ester having a formula (III): ##STR3## wherein R.sup.1 and R.sup.2 are the same as defined above, with sodium borohydride or lithium borohydride in an organic solvent containing methanol, reacting the resulting alcohol with a halogenating agent without any solvent or in an organic solvent in the presence or the absence of a base, reacting the resulting halide with a dehydrohalogenating agent in an organic solvent and hydrolyzing the resulting methylene compound having a formula (VI): ##STR4## wherein R.sup.
    Type: Grant
    Filed: March 26, 1998
    Date of Patent: April 25, 2000
    Assignee: Kaken Pharmaceutical Co., Ltd.
    Inventor: Takanobu Naito
  • Patent number: 6051711
    Abstract: A method for synthesizing swainsonine salts and intermediates thereof comprising subjecting a compound of the formula I ##STR1## wherein R.sup.2 and R.sup.2' are the same or different and represent alkyl, halogen, alkenyl, alkoxy, cycloalkyl or aryl which may be substituted, to acid hydrolysis in the presence of a C.sub.1-4 alkanol to obtain a crystalline salt of swainsonine; and optionally, recrystallizing the swainsonine salt from a C.sub.1-4 alkanol. The reaction may be used in combination with one or more additional reaction steps.
    Type: Grant
    Filed: October 23, 1998
    Date of Patent: April 18, 2000
    Assignee: GLYCODesign Inc.
    Inventors: Francois Tropper, Rajan N. Shah, Pradeep Sharma
  • Patent number: 6051731
    Abstract: Compounds of the formula ##STR1## where the symbols have the meaning described in the application, have retinoid-like or retinoid antagonist-like biological activity.
    Type: Grant
    Filed: September 4, 1997
    Date of Patent: April 18, 2000
    Assignee: Allergan Sales, Inc.
    Inventors: Vidyasagar Vuligonda, Min Teng, Richard L. Beard, Alan T. Johnson, Yuan Lin, Roshantha A. Chandraratna
  • Patent number: 6051561
    Abstract: Carrier compounds and compositions therewith which are useful in the delivery of active agents are provided. Methods of administration and preparation are provided as well.
    Type: Grant
    Filed: February 7, 1997
    Date of Patent: April 18, 2000
    Assignee: Emisphere Technologies Inc.
    Inventors: Andrea Leone-Bay, Eric Wang, Donald J. Sarubbi, Harry Leipold
  • Patent number: 6048985
    Abstract: A method of stabilizing borane-tetrahydrofuran complex comprises the step of maintaining the temperature of the borane-tetrahydrofuran complex at or below 20.degree. C. A method of reacting a borane reagent with a substrate comprises the steps of heating the borane reagent and the substrate in a reaction vessel and preventing escape of evolved diborane from the reaction vessel. Preferably, a reaction vessel containing a borane reagent and a substrate is maintained under at greater than atmospheric pressure with back-pressure regulation.
    Type: Grant
    Filed: December 22, 1998
    Date of Patent: April 11, 2000
    Assignee: Mine Safety Appliances Company
    Inventors: Elizabeth R. Burkhardt, Joseph A. Corella, II
  • Patent number: 6048868
    Abstract: The present invention provides .beta.-carboline derivatives useful as components of cosmetic, medicinal, and pharmaceutical compositions. The medicinal and pharmaceutical compositions can be used to induce hypnotic activity in a subject. Methods of producing the .beta.-carboline derivatives are provided as well.
    Type: Grant
    Filed: March 17, 1998
    Date of Patent: April 11, 2000
    Assignees: Cemaf, Laboratories Besins Iscovesco
    Inventors: J-Bernard Fourtillan, Marianne Fourtillan, Jean-Claude Jacquesy, Marie-Paule Jouannetaud, Bruno Violeau, Omar Karam
  • Patent number: 6046261
    Abstract: A piperidine compound having excellent blooming resistance represented by the formula (I) ##STR1## (wherein, R.sub.1, R.sub.2 and R.sub.3 each independently represent a hydrogen atom, lower alkyl group, cycloalkyl group having 5 to 7 carbon atoms or an acyl group having 2 to 18 carbon atoms. R.sub.4 represents an acyl group having 2 to 18 carbon atoms.) is provided, and a method for producing the piperidine compound and use thereof as a stabilizer for an organic material are also provided.
    Type: Grant
    Filed: August 10, 1998
    Date of Patent: April 4, 2000
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Kazusige Okamoto, Motohiko Sammizzo, Mitsuo Shimode
  • Patent number: 6045720
    Abstract: A compound expressed by the following formula (1) and a liquid crystalline composition with using it are provided: ##STR1## wherein, either one of rings A, B and C denotes ##STR2## remaining two of them denote each independently ##STR3## R denotes an alkyl group or an alkoxy group with 4-16 carbon atoms, R* denotes ##STR4## in which, R.sub.1 denotes CH.sub.3, CF.sub.3, CH.sub.2 F or CHF.sub.2, R.sub.2 denotes an alkyl group with 1-10 carbon atoms and m denotes 2-12.The said compound exhibits a ferroelectric liquid crystalline phase and an antiferroelectric liquid crystalline phase by itself.
    Type: Grant
    Filed: December 4, 1998
    Date of Patent: April 4, 2000
    Assignee: Chisso Corporation
    Inventors: Ryushi Shundo, Shinichi Saito, Eiji Okabe, Hideo Saito
  • Patent number: 6045991
    Abstract: Compounds which generate red chemiluminescence on reaction with a phosphatase enzyme are provided as well as intermediates useful for their preparation. The chemiluminescent compounds comprise a luciferin ring system and an exocyclic enol phosphate group where the position on the luciferin ring system adjacent to the double bond is disubstituted. The chemiluminescent compounds are useful alone or within compositions containing a cationic aromatic compound in methods for producing chemiluminescence. The chemiluminescent reactions can be applied in assays for phosphatase enzymes and in assays employing enzyme-labeled specific binding pairs.
    Type: Grant
    Filed: May 3, 1999
    Date of Patent: April 4, 2000
    Assignee: Lumigen, Inc.
    Inventor: Hashem Akhavan-Tafti
  • Patent number: 6046342
    Abstract: The present invention provides pyromellitic dianhydride derivatives represented as formula I: ##STR1## wherein, R is C.sub.1-24 alkyl.The pyromellitic dianhydride derivatives of the invention can be used as monomers for the synthesis of polyimides, ladder poly(imidazopyrrolone)s, crosslinked polyamides and polyesters. The present invention also provides a novel process for preparing the pyromellitic dianhydride derivatives as formula I.
    Type: Grant
    Filed: March 24, 1999
    Date of Patent: April 4, 2000
    Assignee: Korea Advanced Institute of Science and Technology
    Inventors: Jin Chul Jung, Kyung-Hoon Lee