Patents Examined by Jacqueline Haley
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Patent number: 5670656Abstract: 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: GrantFiled: May 24, 1996Date of Patent: September 23, 1997Assignee: Zeneca LimitedInventors: John Michael Cox, Kevin James Gillen, Russell Martin Ellis, Shaheen Khatoon Vohra, Stephen Christopher Smith, Ian Richard Matthews
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Patent number: 5668087Abstract: 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: GrantFiled: March 15, 1996Date of Patent: September 16, 1997Assignee: Nihon Bayer Agrochem K.K.Inventors: Toshio Goto, Yoshinori Kitagawa, Seishi Ito, Katsuhiko Shibuya, Kazuhiro Ukawa, Yoshiko Kyo, Natsuko Minegishi
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Patent number: 5665754Abstract: 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: GrantFiled: September 20, 1993Date of Patent: September 9, 1997Assignee: Glaxo Wellcome Inc.Inventors: Paul Lawrence Feldman, Jeffrey Alan Stafford
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Patent number: 5665889Abstract: 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: GrantFiled: January 22, 1996Date of Patent: September 9, 1997Assignee: Industrial Technology Research InstituteInventors: Shiao-Jung Chu, Pine-Sci Kuo, Chu-Chang Dai, Hsi-Yen Hsu, Ching-Tang Lin
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Patent number: 5663348Abstract: 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: GrantFiled: July 19, 1995Date of Patent: September 2, 1997Assignee: Nissan Chemical Industries Ltd.Inventors: Hiroshi Kashihara, Mikio Suzuki, Yoshio Ohara
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Patent number: 5661159Abstract: 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: GrantFiled: August 2, 1994Date of Patent: August 26, 1997Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Masaaki Matsuo, Kazuo Okumura, Shinji Shigenaga
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Patent number: 5661175Abstract: 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: GrantFiled: June 20, 1995Date of Patent: August 26, 1997Inventors: Yoel Kashman, Dolores G. Gravalos
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Patent number: 5658935Abstract: 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: GrantFiled: January 17, 1996Date of Patent: August 19, 1997Assignee: Hoechst AktiengesellschaftInventors: Otmar Klingler, Gerhard Zoller, Bernd Jablonka, Melitta Just, Gerhard Breipohl, Jochen Knolle, Wolfgang Konig
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Patent number: 5658861Abstract: 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: GrantFiled: May 11, 1995Date of Patent: August 19, 1997Assignee: Dowell Schlumberger IncorporatedInventors: Erik B. Nelson, Vernon G. Constien, Kay E. Cawiezel
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Patent number: 5658940Abstract: 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: GrantFiled: October 6, 1995Date of Patent: August 19, 1997Assignee: Celgene CorporationInventors: George W. Muller, Mary Shire
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Patent number: 5659039Abstract: 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: GrantFiled: February 23, 1995Date of Patent: August 19, 1997Assignee: Mitsui Toatsu Chemicals, Inc.Inventors: Akira Ogiso, Rihoko Imai, Tsutami Misawa, Ryu Oi, Yoriaki Matsuzaki, Hisato Itoh
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Patent number: 5656654Abstract: 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: GrantFiled: June 22, 1994Date of Patent: August 12, 1997Assignee: Farmitalia Carlo Erba S.r.l.Inventors: Franco Buzzetti, Antonio Longo, Maria Gabriella Brasca, Fabrizio Orzi, Angelo Crugnola, Dario Ballinari, Mariangela Mariani
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Patent number: 5656759Abstract: 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: GrantFiled: June 7, 1995Date of Patent: August 12, 1997Assignee: Sony CorporationInventors: Kengo Ito, Masanobu Hida, Kaori Isaji
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Patent number: 5654257Abstract: 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: GrantFiled: February 15, 1996Date of Patent: August 5, 1997Assignee: Nihon Bayer Agrochem K.K.Inventors: Toshio Goto, Yoshinori Kitagawa, Seishi Ito, Katsuhiko Shibuya, Tatsuya Yamaoka, Chieko Ueno, Yoshiko Kyo
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Patent number: 5654316Abstract: 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: GrantFiled: June 6, 1995Date of Patent: August 5, 1997Assignee: Schering CorporationInventors: Nicholas I. Carruthers, Cheryl A. Alaimo
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Patent number: 5654440Abstract: 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: GrantFiled: March 15, 1996Date of Patent: August 5, 1997Assignee: Agency of Industrial Science & Technology, Ministry of International Trade & IndustryInventors: Katsuya Kato, Shozo Fujii, Masato Katayama, Hiroshi Kimoto
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Patent number: 5654326Abstract: 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: GrantFiled: June 6, 1995Date of Patent: August 5, 1997Assignee: Eli Lilly and CompanyInventors: Nicholas J. Bach, Robert D. Dillard, Susan E. Draheim
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Patent number: 5652198Abstract: 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: GrantFiled: March 6, 1996Date of Patent: July 29, 1997Assignee: Nihon Bayer Agrochem K.K.Inventors: Toshio Goto, Seishi Ito, Yukiyoshi Watanabe, Shin-ichi Narabu, Akihiko Yanagi
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Patent number: 5650379Abstract: 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: GrantFiled: June 5, 1995Date of Patent: July 22, 1997Assignee: Marathon Oil CompanyInventor: Robert D. Sydansk
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Patent number: 5650406Abstract: 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: GrantFiled: October 8, 1996Date of Patent: July 22, 1997Assignee: Asahi Kasei Kogyo Kabushiki KaishaInventors: Nobuyuki Takahashi, Daisuke Mochizuki