Patents Examined by Joseph P. Brust
  • Patent number: 5457119
    Abstract: 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: Grant
    Filed: July 8, 1994
    Date of Patent: October 10, 1995
    Assignee: Eli Lilly and Company
    Inventors: Roseanne Bonjouklian, Richard E. Moore, Gregory M. L. Patterson, Tim A. Smitka
  • Patent number: 5430171
    Abstract: 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: Grant
    Filed: July 11, 1994
    Date of Patent: July 4, 1995
    Assignee: Takasago International Corporation
    Inventors: Shigeru Mitsuhashi, Kazutoshi Sakurai, Hidenori Kumobayashi
  • Patent number: 5424319
    Abstract: 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: Grant
    Filed: December 16, 1993
    Date of Patent: June 13, 1995
    Assignee: G.D. Searle & Co.
    Inventors: Gunnar J. Hanson, John S. Baran
  • Patent number: 5411957
    Abstract: 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: Grant
    Filed: January 25, 1994
    Date of Patent: May 2, 1995
    Assignee: G.D. Searle & Co.
    Inventors: Gunnar J. Hanson, John S. Baran
  • Patent number: 5391768
    Abstract: 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: Grant
    Filed: March 25, 1993
    Date of Patent: February 21, 1995
    Assignee: United States Surgical Corporation
    Inventor: Ying Jiang
  • Patent number: 5380875
    Abstract: 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: Grant
    Filed: May 4, 1994
    Date of Patent: January 10, 1995
    Assignee: Hitachi Chemical Company, Ltd.
    Inventors: Yasuo Yamamoto, Yoshiaki Harushima, Akira Nagai
  • Patent number: 5336777
    Abstract: 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: Grant
    Filed: November 5, 1992
    Date of Patent: August 9, 1994
    Assignee: Zeneca Limited
    Inventors: Frank S. Moffatt, David Winstanley
  • Patent number: 5336682
    Abstract: 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: Grant
    Filed: December 10, 1991
    Date of Patent: August 9, 1994
    Assignee: Imperial Chemical Industries Public Limited Company
    Inventors: Paul deFraine, Brian K. Snell, Kevin Beautement, Vivienne M. Anthony, John M. Clough
  • Patent number: 5321169
    Abstract: 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: Grant
    Filed: May 11, 1993
    Date of Patent: June 14, 1994
    Assignee: Dainippon Ink and Chemicals, Inc.
    Inventors: Yasuyuki Tanaka, Haruyoshi Takatsu, Kiyohumi Takeuchi, Yuji Tamura
  • Patent number: 5310935
    Abstract: 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: Grant
    Filed: June 30, 1992
    Date of Patent: May 10, 1994
    Assignee: Pharmagroup International
    Inventors: Arnold Brossi, Danilo C. Massari, Qian-Sheng Yu
  • Patent number: 5306725
    Abstract: 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: Grant
    Filed: October 30, 1992
    Date of Patent: April 26, 1994
    Assignee: Katayama Chemical Inc.
    Inventors: Yoichi Sano, Katsuji Tsuji, Sakae Katayama, deceased
  • Patent number: 5292918
    Abstract: 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: Grant
    Filed: October 6, 1992
    Date of Patent: March 8, 1994
    Assignee: Schering Corporation
    Inventors: Jacques Gosteli, Ingrid Mergelsberg, Markus Tanner
  • Patent number: 5268497
    Abstract: 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: Grant
    Filed: February 24, 1992
    Date of Patent: December 7, 1993
    Assignee: The BOC Group, Inc.
    Inventor: Ramakrishnan Ramachandran
  • Patent number: 5264584
    Abstract: 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: Grant
    Filed: September 14, 1992
    Date of Patent: November 23, 1993
    Assignee: Mitsui Toatsu Chemicals, Inc.
    Inventors: Kenji Kodaka, Katsutoshi Kinoshita, Michihiko Nakaya, Koichi Ebihara, Shirou Shiraishi, Eiichi Yamada, Satoshi Numata
  • Patent number: 5262431
    Abstract: 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: Grant
    Filed: February 19, 1992
    Date of Patent: November 16, 1993
    Assignee: Ono Pharmaceutical Co., Ltd.
    Inventors: Masaaki Toda, Shuichi Ohuchida, Hiroyuki Ohno
  • Patent number: 5254578
    Abstract: 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: Grant
    Filed: November 9, 1992
    Date of Patent: October 19, 1993
    Assignee: Sankyo Company, Limited
    Inventors: Toshihiko Hashimoto, Hidekazu Masuko, Hiroyuki Koike, Toshio Sada
  • Patent number: 5219852
    Abstract: Substituted thiazoles, oxazoles and 2-hydroxy morpholine compounds useful in the treatment of diabetes mellitus and obesity are described.
    Type: Grant
    Filed: December 18, 1991
    Date of Patent: June 15, 1993
    Assignee: Dr. Karl Thomae GmbH
    Inventors: Manfred Reiffen, Rudolf Hurnaus, Robert Sauter, Wolfgang Grell, Eckhard Rupprecht
  • Patent number: 5206240
    Abstract: Spirocycles of general structural formula: ##STR1## are Class III antiarrhythmic agents.
    Type: Grant
    Filed: June 3, 1991
    Date of Patent: April 27, 1993
    Assignee: Merck & Co., Inc.
    Inventors: John J. Baldwin, Jason M. Elliott, David A. Claremon, Gerald S. Ponticello, David C. Remy, Harold G. Selnick
  • Patent number: 5202455
    Abstract: 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: Grant
    Filed: September 6, 1991
    Date of Patent: April 13, 1993
    Assignee: Huels Aktiengesellschaft
    Inventor: Karl Schmitz
  • Patent number: 5177242
    Abstract: 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: Grant
    Filed: December 17, 1991
    Date of Patent: January 5, 1993
    Assignee: FMC Corporation
    Inventors: Stephen W. Andruski, Bruce Goldberg