Patents Examined by C. Warren Ivy
  • Patent number: 5792792
    Abstract: The invention relates to borneol derivatives of general formula I ##STR1## in which R.sup.1 means C(O)--CH(OR.sup.6)--CH(NHR.sup.7)--R.sup.8,R.sup.2 means hydrogen, --OH, C.sub.1 -C.sub.10 alkyl, C.sub.1 -C.sub.10 alkoxy, --OC(O)R.sup.9a, --OSO.sub.2 R.sup.9a, --OP(O)(OH).sub.2, NHR.sup.9a, NR.sup.9a R.sup.9b,R.sup.3 means hydrogen, --OH, C.sub.1 -C.sub.10 alkoxy, --OC(O)R.sup.9b, --OSO.sub.2 R.sup.9b, --OP(O)(OH).sub.2, orR.sup.2, R.sup.3 together mean an oxygen atom,R.sup.4 means hydrogen, C.sub.1 -C.sub.10 alkyl, --(CH.sub.2).sub.n --OR.sup.11a,R.sup.5 means hydrogen, C.sub.1 -C.sub.10 alkyl, --(CH.sub.2).sub.p --OR.sup.11b, orR.sup.4, R.sup.5 together mean an oxygen atom, a=CHR.sup.10 group,n means 0 to 8,p means 1 to 8,R.sup.7 means --C(O)R.sup.12, --SO.sub.2 R.sup.12, --C(O)OR.sup.12, --C(O)NHR.sup.9d, --C(O)NR.sup.9d R.sup.9e, ##STR2## R.sup.8 means aryl, R.sup.9a-e, R.sup.12 are the same or different and mean C.sub.1 -C.sub.10 alkyl, C.sub.4 -C.sub.8 cycloalkyl, aryl, C.sub.7 -C.sub.16 aralkyl,R.sup.
    Type: Grant
    Filed: January 3, 1997
    Date of Patent: August 11, 1998
    Assignee: Schering Aktiengesellschaft
    Inventors: Ulrich Klar, Hermann Graf, Gunter Neef, Siegfried Blechert
  • Patent number: 5792876
    Abstract: A process is described for producing acetals comprising reacting an aldehyde or a ketone with an alcohol in the presence of a titanium compound having an acetylacetone as a ligand, or in the presence of a compound selected from the group consisting of stannous chloride dihydrate, cerium chloride hexahydrate and bismuth chloride. The process can be used in the synthesis of unstable acetals or when water exists in the reaction mixture, and therefore the process can be used for a wide variety of applications.
    Type: Grant
    Filed: November 6, 1996
    Date of Patent: August 11, 1998
    Assignee: Kuraray Co., Ltd.
    Inventors: Hideharu Iwasaki, Masahiko Kitayama, Takashi Onishi
  • Patent number: 5789604
    Abstract: New antibacterial agents produced by fungal culture 07F275, of which the compound designated 07F275 alpha having the following structure: ##STR1## is representative. Methods for the fermentation, recovery and purification from crude solutions are also disclosed.
    Type: Grant
    Filed: May 12, 1993
    Date of Patent: August 4, 1998
    Assignee: American Cyanamid Company
    Inventors: Cedric John Pearce, Robert West, Gerhard Schlingmann
  • Patent number: 5789405
    Abstract: An oxaspiro ?2,5!octane derivative of the formula: ##STR1## useful in inhibiting angiogenesis in solid tumors.
    Type: Grant
    Filed: June 5, 1991
    Date of Patent: August 4, 1998
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Teruo Oku, Chiyoshi Kasahara, Takehiko Ohkawa, Masashi Hashimoto
  • Patent number: 5789624
    Abstract: Hydroformylation of alkenes to aldehydes in the presence of a rhodium complex catalyst is improved by the addition of a novel bidentate ligand of the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.1 ' and R.sub.2 ' are organic radicals selected from alicyclic, aliphatic and aromatic groups of which at least one is preferably substituted with at least one electronegative moiety and the methylene groups are present at the trans-2,3 positions on the norbomane moiety. The invention also provides a novel method for producing the bidentate ligand and novel intermediate phosphine oxide and phosphinous acid compounds.
    Type: Grant
    Filed: April 10, 1996
    Date of Patent: August 4, 1998
    Assignee: Hoechst Celanese Corporation
    Inventors: Jerry D. Unruh, Brigitte E. Segmuller, Gabriel R. Chapa, Kent E. Pryor
  • Patent number: 5786368
    Abstract: Novel N-alkyl derivatives of deoxygalactonojirimycin are provided in which said alkyl contains from 3-6 carbon atoms. These novel compounds are useful for selectively inhibiting glycolipid synthesis.
    Type: Grant
    Filed: January 17, 1996
    Date of Patent: July 28, 1998
    Assignee: Monsanto Company
    Inventors: Frances M. Platt, Gabrielle R. Neises, Raymond A. Dwek, Terry D. Butters
  • Patent number: 5786378
    Abstract: This invention relates to neurotrophic low molecular weight, small molecule heterocyclic thioesters and ketones having an affinity for FKBP-type immunophilins, and their use as inhibitors of the enzyme activity associated with immunophilin proteins, particularly peptidyl-prolyl isomerase, or rotamase, enzyme activity.
    Type: Grant
    Filed: September 25, 1996
    Date of Patent: July 28, 1998
    Assignee: GPI Nil Holdings, Inc.
    Inventors: Gregory S. Hamilton, Jia-He Li
  • Patent number: 5783702
    Abstract: Cisapride, i.e. cis-4-amino-5-chloro-N-?1-?3-(4 fluoro-phenoxy)propyl!-3-methoxy-4-piperidinyl!-2-methoxy-benzamide, and similar benzamide derivatives, are prepared from novel 1-aryloxyalkyl- or 1-aralkyl-3-arylcarbonyloxy-4-oxo-piperidines, by nuclear substituent re arrangement involving acyl transfer under animal forming conditions, to give the corresponding 1-aryloxyalkyl- or 1-aralkyl-3-hydroxy-4-lower alkoxy-4-arylamido piperidine. This in turn is readily converted to the corresponding 3-oxo-4-arylamido-piperidine by reaction with strong organic acid, which can then be reduced, deprotected and 3-methylated to give the final compound, e.g. cisapride.
    Type: Grant
    Filed: August 21, 1996
    Date of Patent: July 21, 1998
    Assignee: Torcan Chemical Ltd.
    Inventors: Yee-Fung Lu, Clarke Slemon, Raymond So, Jan Oudenes, Teng-Ko Ngooi
  • Patent number: 5783731
    Abstract: A process to reduce carbonyl impurities in a carbonylation reaction for the production of acetic acid is described. The methyl iodide recycle stream which is directed to a carbonylation reactor for carbonylating methanol or methyl acetate to acetic acid, is treated to remove carbonyl impurities by reacting the methyl iodide stream formed in the reaction with an aqueous amino compound which reacts with the carbonyls to form water soluble nitrogenous derivatives, separating an organic methyl iodide phase from an aqueous derivative phase and distilling the methyl iodide phase to remove heavier impurities. The treatment of the methyl iodide recycle stream to the carbonylation reactor has been found to greatly reduce the carbonyls present in the acetic acid product. The formation of nitrile from the nitrogenous derivative during distillation may be minimized by adding water to the system.
    Type: Grant
    Filed: September 11, 1995
    Date of Patent: July 21, 1998
    Assignee: Hoechst Celanese Corporation
    Inventors: Darrell Andrew Fisher, Michael L. Karnilaw, Kenneth Paul Kidwell, Melchior Albert Meilchen, Valerie Santillan, Mark O. Scates, G. Paull Torrence, Richard F. Vogel, Jr., R. Jay Warner
  • Patent number: 5780636
    Abstract: The invention relates to a process for the preparation of intermediates useful in the preparation of (1R,2R)-2-(3-pyridyl)-N-alkyltetrahydro-2H-thiopyran-2-carbothioamide 1-oxides, which possess useful pharmaceutical properties, for example antihypertensive properties, and to intermediates and pharmaceutical products prepared using said process.
    Type: Grant
    Filed: January 5, 1996
    Date of Patent: July 14, 1998
    Assignee: Rhone-Poulenc Rorer Limited
    Inventors: Philippe Pitchen, David Michael Thompson
  • Patent number: 5780466
    Abstract: The invention relates to compounds of the formula ##STR1## in which: A is a divalent radical selected from:A.sub.1) --O--CO--A.sub.2) --CH.sub.2 --O--CO--A.sub.3) --O--CH.sub.2 --CO--A.sub.4) --O--CH.sub.2 --CH.sub.2 --A.sub.5) --N(R.sub.1)--CO--A.sub.6) --N(R.sub.1)--CO--CO--A.sub.7) --N(R.sub.1)--CH.sub.2 --CH.sub.2 --A.sub.8) --O--CH.sub.2 --in which:R.sub.1 is a hydrogen or a (C.sub.1 -C.sub.4)-alkyl; andAm is a nitrogen-containing heterocycle.
    Type: Grant
    Filed: August 27, 1996
    Date of Patent: July 14, 1998
    Assignee: Sanofi
    Inventors: Xavier Emonds-Alt, Isabelle Grossriether, Patrick Gueule, Vincenzo Proietto, Didier Van Broeck, Joelle Taillades
  • Patent number: 5780666
    Abstract: A process is described for the preparation of (+)-2-(3,4-dichlorophenyl)-4-hydroxybutylamine (I) by reaction of 3,4-dichlorophenylacetic acid (II) with an alkali metal halogenoacetate, treatment of the 3-cyano-3-(3,4-dichlorophenyl)propionic acid (III) with D-(-)-N-methylglucamine, with second-order asymmetric conversion, hydrolysis of the D-(-)-N-methylglucamine salt of (-)-3-cyano-3-(3,4-dichlorophenyl,)propionic acid and enantioconservative reduction of the resulting levorotatory cyanoacid with a borane.
    Type: Grant
    Filed: February 7, 1996
    Date of Patent: July 14, 1998
    Assignee: Sanofi
    Inventors: Marcel Descamps, Joel Radisson, Anne-Archard Gilles
  • Patent number: 5780700
    Abstract: A process for the preparation of olefinically unsaturated compounds by catalytic oxidation, ie oxidative dehydrogenation by transferring oxygen from a previously oxidized oxygen carrier acting as catalyst, in the absence of molecular oxygen, the catalyst being regenerated after exhaustion, wherein, during the operating phase of the catalyst (oxidation/dehydration partial step), the residence time, space velocity and/or temperature of the reactants in the reactor is/are adjusted, ie, controlled, continuously or in discrete steps, in a manner appropiate to the momentary state of activity of the redox catalyst by adjusting--continuously or stepwise--the residence time of the reactants in the freshly regenerated catalyst (ie at the commencement of the reaction) to a shorter time, and/or the temperature to a lower value, than the corresponding parameter(s) in the partially reduced catalyst.
    Type: Grant
    Filed: September 13, 1995
    Date of Patent: July 14, 1998
    Assignee: BASF Aktiengesellschaft
    Inventors: Alfred Hagemeyer, Thomas Lautensack, Otto Watzenberger, Axel Deimling
  • Patent number: 5780490
    Abstract: Compounds of formula (I): ##STR1## wherein: R.sup.1 is hydrogen or alkyl; R.sup.2 is alkylene; R.sup.3 is hydrogen, alkyl, alkoxy, alkylthio, halogen, nitro group, amino group, monoalkylamino, dialkylamino, aryl, or aralkyl; X is aryl, or aromatic heterocyclic; Y is oxygen, sulfur or a group of formula >N--R.sup.4, in which R.sup.4 is hydrogen, alkyl or acyl; and Z is a group of formula (Za), (Zb), (Zc) or (Zd): ##STR2## and salts thereof can be used to treat or prevent are included those arising from hyperlipidemia, hyperglycemia, obesity, impaired glucose tolerance (IGT), insulin resistant non-IGT (NGT), non-diagnostic glucose tolerance, insulin resistance, diabetic complications, fatty liver, polycystic ovary syndrome (PCOS) and gestational diabetes mellitus (GDM); in addition the compounds of the present invention have aldose reductase inhibitory activity.
    Type: Grant
    Filed: June 18, 1997
    Date of Patent: July 14, 1998
    Assignee: Sankyo Company, Limited
    Inventors: Hiroaki Yanagisawa, Takashi Fujita, Koichi Fujimoto, Takao Yoshioka, Kunio Wada, Minoru Oguchi, Toshihiko Fujiwara, Hiroyoshi Horikoshi
  • Patent number: 5776958
    Abstract: Compounds of general formula (1): ##STR1## wherein Y is a halogen atom or a group --OR.sup.1 where R.sup.1 is an optionally substituted alkyl group;X is --O--, --S-- or --N(R.sup.8)--, where R.sup.8 is a hydrogen atom or an alkyl group;R.sup.2 is an optionally substituted alkyl, alkenyl, cycloalkyl or cycloalkenyl group;R.sup.3 is a hydrogen or halogen atom or an --OR.sup.9 group, where R.sup.9 is a hydrogen atom or an optionally substituted alkyl, alkenyl, alkoxyalkyl, or alkanoyl group, or a formyl, carboxamido or thiocarboxamido group;R.sup.4 is a group --(CH.sub.2).sub.n Ar, where Ar is a monocyclic or bicyclic aryl group optionally containing one or more heteroatoms selected from oxygen, sulphur or nitrogen atoms and n is zero or an integer 1,2 or 3;R.sup.5 is a C.sub.3-9 carbocyclic ketone optionally containing one or more heteroatoms selected from oxygen, sulphur or nitrogen atoms;R.sup.6 is a hydrogen atom or an optionally substituted alkyl group;R.sup.
    Type: Grant
    Filed: December 21, 1994
    Date of Patent: July 7, 1998
    Assignee: Celltech Therapeutics, Limited
    Inventors: Graham John Warrellow, Ewan Campbell Boyd, Rikki Peter Alexander, Michael Anthony William Eaton
  • Patent number: 5777172
    Abstract: A process comprising the reaction of an optionally substituted benzene with thiophosgene in the presence of a Friedel Crafts catalyst for the preparation of the equivalent optionally substituted benzophenthione. The benzophenthiones are converted into the equivalent benzophenone derivatives by hydrolysis.
    Type: Grant
    Filed: November 18, 1996
    Date of Patent: July 7, 1998
    Assignee: Zeneca Limited
    Inventors: Michael Charles Henry Standen, Nicholas Charles Evens
  • Patent number: 5776948
    Abstract: Antibacterial fluoroquinoline derivatives and salts thereof of the following formula are stable and have low toxicity and high photostability and low cytotoxicity under light irradiation: ##STR1## wherein R.sub.1 is hydrogen or lower alkyl;R.sub.2 is hydrogen, optionally protected amino, optionally protected aminocarbonyl or optionally protected carboxyl;R.sub.5 is halogen, lower alkyl or optionally protected hydroxyl or is the same as R.sub.2 ;R.sub.6 is lower alkyl;A is CH.sub.2, optionally protected nitrogen or oxygen;andn and m are each an integer of from 0 to 4, provided that n +m is an integer of from 1 to 4.
    Type: Grant
    Filed: October 9, 1996
    Date of Patent: July 7, 1998
    Assignee: Chugai Seiyaku Kabushiki Kaisha
    Inventors: Takeshi Yokota, Masayuki Haramura, Akira Okamachi, Toshihiko Makino
  • Patent number: 5777152
    Abstract: 2-Aryl-2-chloramalonic diester is prepared by reacting 2-arylmalonic diesters with aqueous hypochlorite in the presence of an inert solubilizer at pH 8 to 14.
    Type: Grant
    Filed: February 29, 1996
    Date of Patent: July 7, 1998
    Assignee: Huels Aktiengesellschaft
    Inventors: Christoph Theis, Radu Bordeianu, Wilfried Latz
  • Patent number: 5777151
    Abstract: Mono- or polycarboxylic acid esters are prepared by reacting a salt of such carboxylic acid with an organic halocompound, e.g., a (cyclo)alkyl, (cyclo)alkenyl, aryl or aralkyl halide, in an aqueous reaction medium, in the presence of a catalytically effective amount of a phase transfer catalyst, for example an onium salt.
    Type: Grant
    Filed: September 24, 1992
    Date of Patent: July 7, 1998
    Assignee: Rhone-Poulenc Chimie
    Inventor: Michel Crochemore
  • Patent number: 5777175
    Abstract: Propylene oxide is added to an active hydrogen compound in the presence of an alkali metal hydroxide catalyst in an amount of from 0.05 to 0.5 mole per mole of the active hydrogen compound at a reaction temperature of from 60.degree. to 98.degree. C. at a reaction pressure less than or equal to 4 kg/cm.sup.2 to prepare a polyoxyalkylene polyol which has a hydroxyl value of from 10 to 35 mg KOH/g, a monool content less than or equal to 15 mol %, a Head-to-Tail bond selectivity greater than or equal to 96 percent, and low viscosity. A polymer polyol is prepared by polymerizing an ethylenically unsaturated monomer in the polyoxyalkylene polyol. A flexible polyurethane foam is prepared by reacting the polyoxyalkylene polyol or the polymer polyol with an organic polyisocyanate compound in the presence of a foaming agent, a catalyst, a surfactant, a crosslinking agent and other additives.
    Type: Grant
    Filed: April 12, 1995
    Date of Patent: July 7, 1998
    Assignee: Mitsui Toatsu Chemicals, Inc.
    Inventors: Kazuhiko Ohkubo, Tomoki Tsutsui, Yoshitsugu Sakaki, Tamotsu Kunihiro, Ariko Nishikawa, Tsukuru Izukawa, Kaoru Ueno, Seijiro Sakai, Yukichi Tanaka