Patents Examined by Jacqueline Haley
  • Patent number: 5670656
    Abstract: A process for the preparation of a compound of general formula II: ##STR1## wherein R.sup.1 is hydrogen, or C.sub.1 -C.sub.10 hydrocarbyl or heterocyclyl having 3 to 8 ring atoms, either of which may optionally be substituted; each R.sup.2, R.sup.3, R.sup.4 and R.sup.5 is independently hydrogen or C.sub.1 -C.sub.4 alkyl; A is an optionally substituted aromatic or heteroaromatic ring system; and R.sup.21 is hydrogen, halogen, OH or OCONHR.sup.1, wherein R.sup.1 is as defined above; the process comprising cyclizing a compound of general formula III: ##STR2## wherein A, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.21 are as defined in general formula II and R.sup.25 is a leaving group such as a halogen atom; under basic conditions.
    Type: Grant
    Filed: May 24, 1996
    Date of Patent: September 23, 1997
    Assignee: Zeneca Limited
    Inventors: John Michael Cox, Kevin James Gillen, Russell Martin Ellis, Shaheen Khatoon Vohra, Stephen Christopher Smith, Ian Richard Matthews
  • Patent number: 5668087
    Abstract: Herbicidal 1-alkenyltetrazolinones of the formula: ##STR1## wherein R.sup.1 represents the group: ##STR2## or the group: ##STR3## R.sup.2 and R.sup.3, independently of one another, represent C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl which may optionally be substited by methyl, C.sub.2-4 alkenyl, C.sub.2-5 alkynyl, phenyl which may optionally be substituted or aralkyl which may optionally be substituted, orR.sup.2 and R.sup.3 may optionally form, together with the N-atom to which they are bonded, a heterocyclic ring which may optionally be substituted, and novel intermediates therefor.
    Type: Grant
    Filed: March 15, 1996
    Date of Patent: September 16, 1997
    Assignee: Nihon Bayer Agrochem K.K.
    Inventors: Toshio Goto, Yoshinori Kitagawa, Seishi Ito, Katsuhiko Shibuya, Kazuhiro Ukawa, Yoshiko Kyo, Natsuko Minegishi
  • Patent number: 5665754
    Abstract: Novel pyrrolidine compounds which are useful for inhibiting the function of Type IV phosphodiesterase (PDE-IV) as well as methods for making the same are disclosed. Applications in treating inflammatory diseases and other diseases involving elevated levels of cytokines, as well as central nervous system (CNS) disorders, are also disclosed.
    Type: Grant
    Filed: September 20, 1993
    Date of Patent: September 9, 1997
    Assignee: Glaxo Wellcome Inc.
    Inventors: Paul Lawrence Feldman, Jeffrey Alan Stafford
  • Patent number: 5665889
    Abstract: The present invention relates to a method for the production of N-vinyl-2-pyrrolidone with high selectivity. The method is characterized in subjecting 2-pyrrolidone and acetylene to vinylation by using hydroxy end-capped ether oligomers having a molecular weight less than 1000 or linear diols having at least 4 carbon atoms as co-catalysts under the catalyzation of alkali metal salts. At a vinylation temperature of 100.degree.-200 .degree. C., a reaction pressure of 7.5-30 atm and a reaction time period of 3-20 hours, N-vinyl-2-pyrrolidones are obtained with yields above 90%.
    Type: Grant
    Filed: January 22, 1996
    Date of Patent: September 9, 1997
    Assignee: Industrial Technology Research Institute
    Inventors: Shiao-Jung Chu, Pine-Sci Kuo, Chu-Chang Dai, Hsi-Yen Hsu, Ching-Tang Lin
  • Patent number: 5663348
    Abstract: An optically active .beta.-aminoalkoxyborane complex of the formula (I): ##STR1## wherein R.sup.1 is C.sub.1 -C.sub.8 alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.7 -C.sub.11 aralkyl or C.sub.6 -C.sub.10 aryl, R.sup.2 is hydrogen, C.sub.1 -C.sub.8 alkyl, C.sub.3 -C.sub.7 cycloalkyl or C.sub.7 -C.sub.11 aralkyl, or R.sup.1 and R.sup.2 together form (CH.sub.2).sub.n wherein n is 3 or 4, and Ar is naphthyl, anthryl or phenanthryl, which may be substituted by from 1 to 3 substituents selected from the group consisting of halogen, nitro, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl, C.sub.7 -C.sub.11 aralkyl, C.sub.6 -C.sub.10 aryl, C.sub.1 -C.sub.6 alkoxy and styrene polymer substituents.
    Type: Grant
    Filed: July 19, 1995
    Date of Patent: September 2, 1997
    Assignee: Nissan Chemical Industries Ltd.
    Inventors: Hiroshi Kashihara, Mikio Suzuki, Yoshio Ohara
  • Patent number: 5661159
    Abstract: This invention relates to new quinolylbenzofuran derivatives having activities as leukotrien and Slow Reacting Substance of Anaphylaxis antagonists and inhibitors and represented by the general formula (I): ##STR1## wherein R.sup.1 is halogen, etc.,R.sup.2 is hydrogen or halogen,R.sup.3 is hydrogen, halogen, hydroxy, lower alkyl or lower alkoxy,R.sup.4 is hydrogen, acyl, cyano, nitro, substituted or unsubstituted aryl, or substituted or unsubstituted lower alkyl,R.sup.5 is hydrogen, hydroxy, lower alkyl or lower alkoxy,A is lower alkylene, lower alkenylene or a single bond,X is a single bond, O, NH, S, SO or SO.sub.2, andY is O or S,provided that when R.sup.3 is hydrogen, R.sup.4 is hydrogen,R.sup.5 is hydrogen, A is a single bond and X is a single bond, then R.sup.1 is halogen, etc.,and pharmaceutically acceptable salts thereof to processes for the preparation thereof and to a pharmaceutical composition comprising the same.
    Type: Grant
    Filed: August 2, 1994
    Date of Patent: August 26, 1997
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Masaaki Matsuo, Kazuo Okumura, Shinji Shigenaga
  • Patent number: 5661175
    Abstract: Three cytotoxic peptides, the known compound Jaspamide and two new peptides, hemiasterlin (Compound 2) and geodiamolide TA (Compound 3), have been isolated from the sponge Hemiasterella minor. The structures of the three were determined by interpreting the NMR and mass spectra. Hemiasterlin (Compound 2) is a novel linear tripeptide embodying two unique, new natural amino acids and geodiamolide TA (Compound 3) is a newly discovered higher homolog of geodiamolides A-F.
    Type: Grant
    Filed: June 20, 1995
    Date of Patent: August 26, 1997
    Inventors: Yoel Kashman, Dolores G. Gravalos
  • Patent number: 5658935
    Abstract: The invention concerns heterocyclic compounds of the general formula (I) in which A, B, R, R.sup.2, R.sup.3, W, Y, Z.sup.1, Z.sup.2 and r are as defined in the description, methods of preparing them and their use as inhibitors of thrombocyte aggregation, the metastization of carcinoma cells and the binding of osteoclasts on bone surfaces.
    Type: Grant
    Filed: January 17, 1996
    Date of Patent: August 19, 1997
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Otmar Klingler, Gerhard Zoller, Bernd Jablonka, Melitta Just, Gerhard Breipohl, Jochen Knolle, Wolfgang Konig
  • Patent number: 5658861
    Abstract: The crosslinking of galactomannan gum fracturing fluids by borate ion is delayed for high-temperature applications by encapsulating the boron with a polymer coating. The crosslink-delay time is further adjusted by varying the concentration of an organic polyol. The polyol also acts as a stabilizer for the crosslinked fluid at elevated temperatures. Low pumping friction pressures are achieved by the delay in the crosslinking with the boron available at high temperatures to add high-temperature stability to the fracturing fluid at temperatures ranging up to about 350.degree. F.
    Type: Grant
    Filed: May 11, 1995
    Date of Patent: August 19, 1997
    Assignee: Dowell Schlumberger Incorporated
    Inventors: Erik B. Nelson, Vernon G. Constien, Kay E. Cawiezel
  • Patent number: 5658940
    Abstract: Novel succinimides and maleimides are inhibitors of tumor necrosis factor .alpha. and phosphodiesterase and can be used to combat cachexia, endotoxic shock, retrovirus replication, asthma, and inflammatory conditions. A typical embodiment is methyl 3-(3',4',5',6'-tetrahydrophthalimido)-3-(3",4"-dimethoxyphenyl)propionate.
    Type: Grant
    Filed: October 6, 1995
    Date of Patent: August 19, 1997
    Assignee: Celgene Corporation
    Inventors: George W. Muller, Mary Shire
  • Patent number: 5659039
    Abstract: Novel quinophthalone compounds, which are represented by the following formula (1): ##STR1## R.sub.1 -R.sub.5 each independently represents a hydrogen or halogen atom or a hydroxy, linear or branched alkyl, substituted or unsubstituted cycloalkyl, halogenated alkyl, alkoxyalkyl, alkoxy, nitro, amino, alkylamino, carboxyl, alkoxycarbonyl, aminocarbonyl, alkylaminocarbonyl, alkylcarbonylamino, alkylcarbonyloxy or cyano group; R.sub.6 -R.sub.17 each independently represents a hydrogen or halogen atom or a hydroxyl, alkyl, halogenated alkyl, alkoxy, nitro, amino, alkylamino, carboxyl, alkoxycarbonyl, aminocarbonyl, alkylaminocarbonyl, alkylcarbonyloxy or cyano group; m and n each stands for 0 or 1; and A represents a substituent, are yellow orange dyestuffs suitable for polarizing films.
    Type: Grant
    Filed: February 23, 1995
    Date of Patent: August 19, 1997
    Assignee: Mitsui Toatsu Chemicals, Inc.
    Inventors: Akira Ogiso, Rihoko Imai, Tsutami Misawa, Ryu Oi, Yoriaki Matsuzaki, Hisato Itoh
  • Patent number: 5656654
    Abstract: Arylidene and heteroarylidene oxindole derivatives of formula (I) ##STR1## wherein, subject to provisos, Y is a bicyclic ring system chosen from naphthalene, tetralin, quinoline and isoquinoline;R is hydrogen or an oxo (.dbd.O) group when Y is tetralin; orR is hydrogen when Y is naphthalene, quinoline or isoquinoline;each of R.sup.1 and R.sup.2 independently is hydrogen, C.sub.1 -C.sub.6 alkyl or C.sub.2 -C.sub.6 alkanoyl;m is zero, 1 or 2;n is zero, 1, 2 or 3;each of R.sup.3 and R.sup.4 independently is hydrogen, halogen, cyano, C.sub.1 -C.sub.6 alkyl, carboxy, nitro or --NR.sup.6 R.sup.7 in which each of R.sup.6 and R.sup.7 independently is hydrogen or C.sub.1 -C.sub.6 alkyl;R.sup.5 is hydrogen or C.sub.1 -C.sub.6 alkyl; and their pharmaceutically acceptable salts, which are useful as tyrosine kinase inhibitors.
    Type: Grant
    Filed: June 22, 1994
    Date of Patent: August 12, 1997
    Assignee: Farmitalia Carlo Erba S.r.l.
    Inventors: Franco Buzzetti, Antonio Longo, Maria Gabriella Brasca, Fabrizio Orzi, Angelo Crugnola, Dario Ballinari, Mariangela Mariani
  • Patent number: 5656759
    Abstract: When the counter ion of hydrophilic cationic dyes is substituted with an organic anion including a sulfosuffinate anion such as diethylhexylsulfonate anion, an alkylbenzenesulfonate anion such as a dodecylbenzenesulfonate, an alkylsulfate anion such as a laurylsulfate anion, or a soap anion such as a laurylsulfate anion, the cationic dyes are imparted with hydrophobicity. An ink layer 3 containing the hydrophobic cationic dye is formed on a support 2 to provide a thermal transfer ink ribbon 10.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: August 12, 1997
    Assignee: Sony Corporation
    Inventors: Kengo Ito, Masanobu Hida, Kaori Isaji
  • Patent number: 5654257
    Abstract: 1-cycloalkenyltetrazolinone derivatives of the following herbicidal formula ##STR1## R.sup.1 is cycloalkenyl which may optionally be substituted by halogen C.sub.1-4 alkyl, or bicycloalkenyl which may optionally be substituted by halogen or C.sub.1-4 alkyl, andR.sup.2 and R.sup.3 each independently is alkyl, cycloalkyl, phenyl (optionally substituted by a member selected from the group consisting of nitro, cyano, halogen, alkyl, haloalkyl, alkoxy, haloalkoxy and alkylthio), alkenyl and alkynyl,orR.sup.2 and R.sup.3 together with the N-atom to which they are bonded form, a 5- or 6-membered heterocyclic ring which may optionally contain a further hetero atom, said heterocyclic ring optionally being benzo-condensed, or a C-.sub.
    Type: Grant
    Filed: February 15, 1996
    Date of Patent: August 5, 1997
    Assignee: Nihon Bayer Agrochem K.K.
    Inventors: Toshio Goto, Yoshinori Kitagawa, Seishi Ito, Katsuhiko Shibuya, Tatsuya Yamaoka, Chieko Ueno, Yoshiko Kyo
  • Patent number: 5654316
    Abstract: The invention relates to compounds of the formula ##STR1## wherein X, i, j, n, n', A, A', R.sub.2, R.sub.3, and U are as described herein. The compounds of the invention are NK.sub.1 or NK.sub.2 or NK.sub.3 receptor antagonists and as such are useful in the treatment of diseases such as asthma.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: August 5, 1997
    Assignee: Schering Corporation
    Inventors: Nicholas I. Carruthers, Cheryl A. Alaimo
  • Patent number: 5654440
    Abstract: An optically active (+)-4,4,4-trifluoro-3-(indole-3-)butyric acid is produced by a method which consists essentially of causing 2,2,2-trifluoroethanol to react on a racemic modification 4,4,4-trifluoro-3-(indole-3-)butyric acid thereby forming a reaction solution containing the trifluoroethyl ester of the butyric acid, causing an enzyme having an esterase activity to act on the reaction solution thereby forming an optically active (+)-4,4,4-trifluoro-3-(indole-3-)butyric acid, and thereafter separating the reaction product from the reaction solution.
    Type: Grant
    Filed: March 15, 1996
    Date of Patent: August 5, 1997
    Assignee: Agency of Industrial Science & Technology, Ministry of International Trade & Industry
    Inventors: Katsuya Kato, Shozo Fujii, Masato Katayama, Hiroshi Kimoto
  • Patent number: 5654326
    Abstract: A class of novel 1H-indole-3-glyoxylamides is disclosed together with the use of such indole compounds for inhibiting sPLA.sub.2 mediated release of fatty acids for treatment of conditions such as septic shock.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: August 5, 1997
    Assignee: Eli Lilly and Company
    Inventors: Nicholas J. Bach, Robert D. Dillard, Susan E. Draheim
  • Patent number: 5652198
    Abstract: Selective herbicidal tetrazolinones of the formula ##STR1## wherein X is hydrogen or halogen,Y is hydrogen or C.sub.1-4 alkyl,R.sup.1 is C.sub.1-4 alkyl, andR.sup.2 is cycloheptyl or cyclooctyl.and synergistic mixtures thereof.
    Type: Grant
    Filed: March 6, 1996
    Date of Patent: July 29, 1997
    Assignee: Nihon Bayer Agrochem K.K.
    Inventors: Toshio Goto, Seishi Ito, Yukiyoshi Watanabe, Shin-ichi Narabu, Akihiko Yanagi
  • Patent number: 5650379
    Abstract: A process and composition are provided for permeability reduction in a hydrocarbon-bearing formation to improve hydrocarbon recovery therefrom. The process includes placement of a crosslinked polymer gel in the treatment region preceded by surface preparation of a gelation solution which is the gel precursor. The gelation solution contains a crosslinkable polymer, a chromium(III)/carboxylate complex crosslinking agent, a carboxylate salt delaying agent and an aqueous solvent. The gel is placed in the treatment region by injecting the gelation solution into a well bore in fluid communication with the formation, displacing it into the desired treatment region and gelling the solution to completion forming the permeability-reducing gel in situ. The gelation rate is retarded in a controlled manner by adjusting the composition or concentration of the delaying agent in the gelation solution.
    Type: Grant
    Filed: June 5, 1995
    Date of Patent: July 22, 1997
    Assignee: Marathon Oil Company
    Inventor: Robert D. Sydansk
  • Patent number: 5650406
    Abstract: A compound represented by general formula (1) or an innocuous salt thereof, a process for producing the same, and a schizophrenia remedy containing the same as the active ingredient (wherein the nitrogeneous ring B represents 3-azabicyclo [3.2.2] nonan-3-yl or 4-azatricyclo [4.3.1.1.sup.3.8 ] undecan-4-yl; and R represents hydrogen, lower alkyl, lower alkoxy, hydroxy or halogen). The above compound and salt have a high affinity for sigma-binding sites and are useful as an antischizophrenic drug.
    Type: Grant
    Filed: October 8, 1996
    Date of Patent: July 22, 1997
    Assignee: Asahi Kasei Kogyo Kabushiki Kaisha
    Inventors: Nobuyuki Takahashi, Daisuke Mochizuki