Patents Examined by Joseph P. Brust
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Patent number: 5457119Abstract: New hapalindole-type alkaloids called A89271 A-F and I are antifungal and antitumor agents. Methods for preparing them and for preparing hapalindoles G and H by culturing the blue-green alga Fischerella ambigua ATCC 55210 are provided. Methods for preparing A89271 factors B and F by culturing the blue-green alga Hapalosiphon hibernicus ATCC 55225 and a biologically pure culture of this alga are also provided. Further provided are methods and compositions for the inhibition of fungal growth and the treatment of susceptible neoplasms.Type: GrantFiled: July 8, 1994Date of Patent: October 10, 1995Assignee: Eli Lilly and CompanyInventors: Roseanne Bonjouklian, Richard E. Moore, Gregory M. L. Patterson, Tim A. Smitka
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Patent number: 5430171Abstract: T-butyl (R)-(-)-4-cyano-3-hydroxybutyrate having an optical purity of 99%ee or higher and a process for producing the same are disclosed, the process comprising cyanogenation of a t-butyl (S)-(-)-4-halogeno-3-hydroxybutyrate obtained by enantioselective hydrogenation of a t-butyl 4-halogenoacetoacetate. Recrystallization of the resulting crude product gives the optically active compound with high optical purity.Type: GrantFiled: July 11, 1994Date of Patent: July 4, 1995Assignee: Takasago International CorporationInventors: Shigeru Mitsuhashi, Kazutoshi Sakurai, Hidenori Kumobayashi
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Patent number: 5424319Abstract: Non-peptidyl compounds characterized generally as .alpha.-succinamidoacyl aminodiols having a piperidinyl-type group at the N-terminus are useful as renin inhibitors for the treatment of hypertension.Type: GrantFiled: December 16, 1993Date of Patent: June 13, 1995Assignee: G.D. Searle & Co.Inventors: Gunnar J. Hanson, John S. Baran
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Patent number: 5411957Abstract: Non-peptidyl compounds characterized generally as .alpha.-succinamidoacyl aminodiols having a 3-azabicyclo[3.2.2]-nonanyl-type group at the N-terminus are useful as renin inhibitors for the treatment of hypertension.Type: GrantFiled: January 25, 1994Date of Patent: May 2, 1995Assignee: G.D. Searle & Co.Inventors: Gunnar J. Hanson, John S. Baran
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Patent number: 5391768Abstract: Methods for purifying 1,4-dioxan-2-one includes dissolving a crude reaction product containing 1,4-dioxan-2-one in an aliphatic ester solvent, forming crystals of 1,4-dioxan-2-one, and filtering the mixture to recover solids containing crystalline 1,4-dioxan-2-one which is relatively pure compared to the crude reaction product.Type: GrantFiled: March 25, 1993Date of Patent: February 21, 1995Assignee: United States Surgical CorporationInventor: Ying Jiang
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Patent number: 5380875Abstract: Provided are N-(9-fluorenylmethoxycarbonyl)-4-substituted proline derivatives represented by the following formula (I): ##STR1## wherein Q is O or S, R represents a particular monovalent group, and T represents H or --C(CH.sub.3).sub.3. Where T is H, the derivatives can each be prepared by reacting a corresponding electron attractive compound with N-(9-fluorenylmethoxycarbonyl)-4-hydroxyproline in the presence of a coupling reagent. The derivatives in which T stands for --(CH.sub.3).sub.3 can each be prepared by reacting the corresponding N-(9-fluorenylmethoxy-carbonyl)-4-hydroxyproline derivative with isobutylene in the presence of a catalytic amount of sulfuric acid. The staring material, N-(9-fluorenylmethoxycarbonyl)-4-hydroxyproline, can be purified by adsorbing it on anhydrous magnesium sulfate.Type: GrantFiled: May 4, 1994Date of Patent: January 10, 1995Assignee: Hitachi Chemical Company, Ltd.Inventors: Yasuo Yamamoto, Yoshiaki Harushima, Akira Nagai
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Patent number: 5336682Abstract: Fungicidally active compounds of the formula ##STR1## and stereoisomers thereof, wherein A is the group .dbd.CW-- or a nitrogen atom, B is the group .dbd.CX-- or a nitrogen atom, D is the group .dbd.CY-- or a nitrogen atom, and E is the group .dbd.CZ-- or a nitrogen atom, wherein W, X, Y and Z, which may be the same or different, are, for example, hydrogen, halogen, nitro, nitrile, or other defined groups and wherein R.sup.1 and R.sup.2 are alkyl, cycloalkyl, alkenyl, alkynyl, optionally substituted aryl, optionally substituted aralkyl, cycloalkyl groups, or optionally substituted heteroaromatic, and V is oxygen or sulfur.Type: GrantFiled: December 10, 1991Date of Patent: August 9, 1994Assignee: Imperial Chemical Industries Public Limited CompanyInventors: Paul deFraine, Brian K. Snell, Kevin Beautement, Vivienne M. Anthony, John M. Clough
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Patent number: 5336777Abstract: Compounds of the general formula ##STR1## are cyclised to the corresponding isothiazolinone using a carbonyl halide of the formula RCOX where R is halogen or alkyl and X is halogen. R.sup.3 and R.sup.4 are preferably such as to form a 5 or 6 membered ring. Useful carbonyl halides are phosgene and propionyl chloride.Type: GrantFiled: November 5, 1992Date of Patent: August 9, 1994Assignee: Zeneca LimitedInventors: Frank S. Moffatt, David Winstanley
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Patent number: 5321169Abstract: A novel tetracyclic cyclohexylcyclohexene derivatives represented by formula: ##STR1## wherein ##STR2## n, X and Y are as defined in the specifications, are disclosed. The compounds are useful as electroptic display materials.Type: GrantFiled: May 11, 1993Date of Patent: June 14, 1994Assignee: Dainippon Ink and Chemicals, Inc.Inventors: Yasuyuki Tanaka, Haruyoshi Takatsu, Kiyohumi Takeuchi, Yuji Tamura
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Patent number: 5310935Abstract: The synthesis of optically active 5-oxygenated (3S)-1,3-dimethyloxindole-3-acetic acids ##STR1## and their use in the synthesis of optically active (3aS-cis)-eseroline and (3aS-cis)-N.sup.1 -benzylnoreseroline, which are important intermediates in the synthesis of compounds related to (3aS-cis)-physostigmine and carbamate analogs, and of (3aS-cis)-N.sup.1 -benzylnor- and N.sup.1 -norphysostigmine and their carbamate analogs.Type: GrantFiled: June 30, 1992Date of Patent: May 10, 1994Assignee: Pharmagroup InternationalInventors: Arnold Brossi, Danilo C. Massari, Qian-Sheng Yu
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Patent number: 5306725Abstract: A stabilized isothiazolone liquid formulation including:an isothiazolone compound represented by the formula (I): ##STR1## (where X represents a hydrogen atom or halogen atom, and Y represents a lower alkyl group), anda mixed solvent containing 50-99.9 wt. % of a glycol-type solvent and 50-0.1 wt. % of an amide-type compound represented by the formula (II): ##STR2## where R.sub.1 represents a hydrogen atom or a lower alkyl group, R.sub.2 and R.sub.3 each represent a lower alkyl group, R.sub.1 may bond to R.sub.2 or R.sub.3 to form a nitrogen-containing heterocycle),the compound of the formula (I) being dissolved in the mixed solvent of which amount is at least sufficient to dissolve the compound of the formula (I).Type: GrantFiled: October 30, 1992Date of Patent: April 26, 1994Assignee: Katayama Chemical Inc.Inventors: Yoichi Sano, Katsuji Tsuji, Sakae Katayama, deceased
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Patent number: 5292918Abstract: A process for preparing an (S,S) or (R,R) diastereoisomer of the formula: ##STR1## or salts, esters or amides thereof, wherein R.sup.3 and R.sup.4 independently represent hydrogen, alkyl, aryl or aryl substituted with halogen, alkyl, nitro or alkoxy, and n and m independently represent integers from one to six, comprising combining a cyanide compound of the formula:M.sup.1 C.tbd.N (III)wherein M.sup.1 is hydrogen, trimethylsilyl or a metal, with an optional proton source, a solvent and a Lewis acid of the formula:M.sup.2 X.sub.4, AlCl.sub.3 or BF.sub.3 (IV)wherein M.sup.2 is Sn or Ti and X represents chloro, bromo, fluoro or iodo, with an .alpha.-amino acid compound or salts or esters thereof, followed by addition of an acyl or acetal compound to give the diastereoisomer of formula (X).Type: GrantFiled: October 6, 1992Date of Patent: March 8, 1994Assignee: Schering CorporationInventors: Jacques Gosteli, Ingrid Mergelsberg, Markus Tanner
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Patent number: 5268497Abstract: A process for the production of an ethylenically unsaturated nitrile from a hydrocarbon feed stream comprised of a mixture of an alkene and an alkane by reaction with an oxygen-containing gas and ammonia. The alkene is converted to unsaturated nitrile by reaction with the oxygen and ammonia in the presence of a suitable catalyst in an ammoxidation reactor; the nitrile product is recovered from the product stream; some of the byproduct carbon oxides and some of the inert gas introduced into the system with the reactants are removed from product stream and the remainder of this stream, now rich in unreacted alkene and alkane, and containing the rest of the byproduct gases and inert gases is introduced into a reactor which contains a catalyst that causes alkane contained in the gas stream to convert to the corresponding alkene. The effluent from the dehydrogenation reactor is recycled to the ammoxidation reactor.Type: GrantFiled: February 24, 1992Date of Patent: December 7, 1993Assignee: The BOC Group, Inc.Inventor: Ramakrishnan Ramachandran
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Patent number: 5264584Abstract: Novel dialkoxymethylimidazolidine derivatives of the formula (1) ##STR1## are described. Also, a preparation process of the derivatives and insecticidal compositions comprising the same are set forth.Type: GrantFiled: September 14, 1992Date of Patent: November 23, 1993Assignee: Mitsui Toatsu Chemicals, Inc.Inventors: Kenji Kodaka, Katsutoshi Kinoshita, Michihiko Nakaya, Koichi Ebihara, Shirou Shiraishi, Eiichi Yamada, Satoshi Numata
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Patent number: 5262431Abstract: A novel prolinal derivative of general formula: ##STR1## [wherein A represents a group of the general formula: ##STR2## (wherein one of R.sup.1 and R.sup.2 represents hydrogen atom and the other represents alkyl group of from 2 to 5 carbon atoms, alkoxy group of from 1 to 5 carbon atom(s), phenyl group, benzyl group, cycloalkyl group of from 4 to 6 carbon atoms or (cycloalkyl group of from 4 to 6 carbon atoms)--methyl group or R.sup.1 and R.sup.2 each represents, same or different, alkyl group of from 1 to 4 carbon atom(s).) or a group of the general formula: ##STR3## (wherein m represents an integer of from 3 to 6.) n represents an integer of from 3 to 10.D represents carbocyclic or heterocyclic ring unsubstituted or substituted by from one to three of halogen atom, nitro group, trifluoromethyl group, alkyl or alkoxy group of from 1 to 4 carbon atom(s).]possess inhibitory activity on prolyl endopeptidase, and therefore be useful for treating and/or preventing agent for amnesia.Type: GrantFiled: February 19, 1992Date of Patent: November 16, 1993Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Masaaki Toda, Shuichi Ohuchida, Hiroyuki Ohno
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Patent number: 5254578Abstract: Compounds of the formula: ##STR1## in which: R.sup.1 is a trifluoromethyl or a pentafluoroethyl;R.sup.2 is ##STR2## in which R.sup.4 is hydrogen; .alpha.-.beta. is a carbon-carbon single bond;and pharmaceutically acceptable salts thereof, have antihypertensive activity and can thus be used for the treatment and prophylaxis of cardiovascular diseases.Type: GrantFiled: November 9, 1992Date of Patent: October 19, 1993Assignee: Sankyo Company, LimitedInventors: Toshihiko Hashimoto, Hidekazu Masuko, Hiroyuki Koike, Toshio Sada
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Patent number: 5219852Abstract: Substituted thiazoles, oxazoles and 2-hydroxy morpholine compounds useful in the treatment of diabetes mellitus and obesity are described.Type: GrantFiled: December 18, 1991Date of Patent: June 15, 1993Assignee: Dr. Karl Thomae GmbHInventors: Manfred Reiffen, Rudolf Hurnaus, Robert Sauter, Wolfgang Grell, Eckhard Rupprecht
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Patent number: 5206240Abstract: Spirocycles of general structural formula: ##STR1## are Class III antiarrhythmic agents.Type: GrantFiled: June 3, 1991Date of Patent: April 27, 1993Assignee: Merck & Co., Inc.Inventors: John J. Baldwin, Jason M. Elliott, David A. Claremon, Gerald S. Ponticello, David C. Remy, Harold G. Selnick
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Patent number: 5202455Abstract: The present invention relates to a process for the liquid-phase preparation of nitriles from aliphatic dicarboxylic acids at temperatures of about 200.degree. to 350.degree. C. using ammonia in the presence of a phosphoric acid-based catalyst, wherein an adsorbent for the catalyst is added to the reaction mixture.Type: GrantFiled: September 6, 1991Date of Patent: April 13, 1993Assignee: Huels AktiengesellschaftInventor: Karl Schmitz
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Patent number: 5177242Abstract: The reaction time and ease of handling of reactants in the known process of forming optically active (S)-cyanohydrins by reacting aldehydes with hydrocyanic acid in the presence of the enzyme S-oxynitrilase and a solvent may be significantly improved over the known methods when the solution of aldehydes and acid is passed through a porous membrane comprising a polymeric resinous binder having finely divided filler particles dispersed throughout the binder to which the S-oxynitrilase enzyme has been chemically bound.Type: GrantFiled: December 17, 1991Date of Patent: January 5, 1993Assignee: FMC CorporationInventors: Stephen W. Andruski, Bruce Goldberg