Patents Examined by Nicholas S. Rizzo
  • Patent number: 5187160
    Abstract: The invention relates to antimicrobial compounds of the formula: ##STR1## wherein R.sup.1 is amino or a protected amino, R.sup.2 is ethyl, propyl or lower alkenyl,R.sup.3 is COO .theta., carboxy or a protected carboxy,R.sup.4 is hydroxy(lower)alkyl or protected hydroxy(lower)alkyl,R.sup.5 is amino or a protected amino,X.sup..theta. is an anion, andn is 0 or 1,or,R.sup.1, R.sup.3, R.sup.5, X.sup..theta. and n are each as defined above,R.sup.2 is lower alkyl, andR.sup.4 is 3-hydroxypropyl, with proviso that(i) when R.sup.3 is COO.sup..theta., then n is 0, and(ii) when R.sup.3 is carboxy or a protected carboxy, then n is 1,or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: February 23, 1990
    Date of Patent: February 16, 1993
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Kazuo Sakane, Kohji Kawabata, Kenzi Miyai, Yoshiko Inamoto
  • Patent number: 5187179
    Abstract: There are disclosed substituted imidazo[1,2-b][1,2,4]triazole derivatives of Formula I which are useful as angiotensin II antagonists.
    Type: Grant
    Filed: March 22, 1991
    Date of Patent: February 16, 1993
    Assignee: Merck & Co., Inc.
    Inventors: Wallace T. Ashton, Steven M. Hutchins, Malcolm MacCoss
  • Patent number: 5187274
    Abstract: In a process to avoid the formation of waste water in the production of hexamine from ammonia and the stream of gas containing formaldehyde resulting from the catalytic oxidation of methanol on metallic oxide catalysts, or by oxidative dehydrogenation to formaldehyde, the liquid volume during reaction for the production of hexamine is kept constant, and carbon monoxide, the organic components of the exhaust gas and also hydrogen, if present, are oxidized to carbon dioxide and water, thus avoiding an energy-consuming condensation of the condensable components from the stream of exhaust gas and their treatment.
    Type: Grant
    Filed: July 19, 1991
    Date of Patent: February 16, 1993
    Assignee: Josef Meissner GmbH & Co.
    Inventors: Heinrich Hermann, Gunther Pelster, Klaus Degener
  • Patent number: 5186734
    Abstract: Herbicidal bisazinyl compounds of the formula ##STR1## in which A.sup.1 and A.sup.2 are identical or different and represent nitrogen or a C--X group, X representing hydrogen, halogen, alkyl or alkoxy, andQ.sup.1 and Q.sup.2 are identical or different and represent oxygen, sulphur, NH or N-alkyl,(the substituents R, X.sup.1, X.sup.2, Y.sup.1, Y.sup.2 and Z representing a variety of organic radicals).The compounds of the formulas ##STR2## are also new.
    Type: Grant
    Filed: September 11, 1991
    Date of Patent: February 16, 1993
    Assignee: Bayer Aktiengesellschaft
    Inventors: Roland Andree, Mark W. Drewes, Hans-Joachim Santel, Klaus Lurssen, Robert R. Schmidt
  • Patent number: 5185356
    Abstract: A particulate composition comprising an isothiazolinone or isothiazolothione or a salt or complex thereof and a water soluble metal salt. The salt is typically a metal salt, for example the sodium salt of 1,2-benzisothiazolin-3-one and the water soluble metal salt is particularly an alkali metal salt such as disodium hydrogen phosphate. A preferred composition can be obtained by stirring together an isothiazolinone or isothiazolothione, a base and an alkali metal phosphate in the presence of water until a dry particulate product is obtained. The particulate product is typically highly and rapidly soluble in water and may be stored in a container formed from a water soluble material, for example a bag formed from polyvinyl alcohol.
    Type: Grant
    Filed: June 11, 1990
    Date of Patent: February 9, 1993
    Assignee: Imperial Chemical Industries PLC
    Inventors: Bryan S. Backhouse, William A. Fern
  • Patent number: 5185333
    Abstract: A benzazine compound, a geometrical isomer of said benzazine compound, an optical isomer of said benzazine compound, and a pharmaceutically acceptable salt of said benzazine compound, said benzazine compound being represented by formula (I): ##STR1## wherein each symbol is as defined in the specification. Said benzazine compounds exhibit 5-HT.sub.3 receptor antagonistic activity, and 5-HT.sub.1A receptor and/or 5-HT.sub.2 receptor and/or dopamine D.sub.2 receptor blocking activity so that they are useful as drugs for the prophylaxis or treatment of various digestive diseases vomiting and disturbances in central nervous systems and the like. The intermediates for said benzazine compounds are also disclosed.
    Type: Grant
    Filed: June 26, 1991
    Date of Patent: February 9, 1993
    Assignee: Yoshitomi Pharmaceutical Industries, Ltd.
    Inventors: Takeshi Kawakita, Takanobu Kuroita, Takemi Fukuda, Ryuhei Iezawa
  • Patent number: 5185330
    Abstract: A penam derivative represented by the following general formula or a salt thereof: ##STR1## wherein R.sup.1 represents a hydrogen atom, an amino-protecting group or an acyl group; R.sup.2 represents a hydrogen atom or a lower alkyl group; R.sup.3 represents a hydrogen atom, a lower alkoxy group, a lower alkylthio group or a formamido group; R.sup.4 represents a protected or unprotected carboxy group or a craboxylato group; R represents a group of the formula, --NHR.sup.5 or --NR.sup.5 R.sup.6 (in which R.sup.5 and R.sup.6, which may be the same or different, represent protected or unprotected hydroxyl groups, cyano groups, sulfo groups, or unsubstituted or substituted lower alkyl, aryl, acyl, carbamoyl, sulfamoyl, lower alkylsulfonyl or heterocyclic groups) or a group of the formula, --N.dbd.CR.sup.7 R.sup.8 (in which R.sup.7 and R.sup.
    Type: Grant
    Filed: June 20, 1990
    Date of Patent: February 9, 1993
    Assignee: Toyama Chemical Co., Ltd.
    Inventors: Hirokazu Ochiai, Yasuo Watanabe, Yoshiharu Murotani, Hirohiko Fukuda, Osamu Yoshino, Shinzaburo Minami, Toshio Hayashi, Kaishu Momonoi
  • Patent number: 5183929
    Abstract: Disclosed are an advantageous method of industrial production of tert-butyl 3-oxobutylate, which is a useful intermediate for synthesis, characterized by reacting tert-butyl alcohol with diketene in the presence of 4-(tertiary amino) pyridine, and an industrially advantageous method of producing cephalosporin compounds or pharmaceutically acceptable salts thereof, using tert-butyl 3-oxobutylate as an intermediate.
    Type: Grant
    Filed: October 3, 1991
    Date of Patent: February 2, 1993
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Kenzo Naito, Yukio Ishibashi, Haruo Shinbo
  • Patent number: 5183916
    Abstract: Tri-n-butylphosphorothioite is produced on a continuous or semi-continuous by simultaneously adding phosphorus trichloride and butylmercaptan to a reaction vessel at a rate such that an excess of butylmercaptan is present and allowing the resultant mixture to react at a temperature of from about 120.degree. C. to about 150.degree. C. One or more reactors may be employed. This process is particularly advantageous for safety reasons and produces high quality phosphite which may be oxidized without purification to produce S,S,S-tri-n-butylphosphorotrithioate.
    Type: Grant
    Filed: April 14, 1989
    Date of Patent: February 2, 1993
    Assignee: Miles Inc.
    Inventors: Ara H. Zakaryan, Peter E. Newallis, Mark A. Tice
  • Patent number: 5183892
    Abstract: An anthrapyridone compound of the following formula (I), which is useful for coloring synthetic resins: ##STR1## wherein Q is --NH.sub.2, --NHCH.sub.3 or --NHCOZ where Z is phenyl or alkyl which may be substituted; X.sub.1, X.sub.2 and X.sub.3 are each hydrogen, halogen, alkyl, alkoxy, hydroxy, --NHCOR.sup.1, --CONR.sup.2 R.sup.3 m --COR.sup.4, --COOR.sup.5, --SO.sub.2 R.sup.6 or --SO.sub.2 NR.sup.7 R.sup.8 where R.sup.1 and R.sup.4 are each C.sub.1-4 alkyl, R.sup.2 and R.sup.3 are each hydrogen or C.sub.1-4 alkyl, R.sup.5 and R.sup.6 are each alkyl or hydroxyalkyl and R.sup.7 and R.sup.8 are each hydrogen or C.sub.1-4 alkyl, with proviso that when Q is --NHCH.sub.3, X.sub.1, X.sub.2 and X.sub.3 are each hydrogen, halogen, alkoxy, hydroxy, --NHCOR.sup.1, --CONR.sup.2 R.sup.3, --COR.sup.4, --COOR.sup.5, --SO.sub.2 R.sup.6 or --SO.sub.2 NR.sup.7 R.sup.8.Process for producing the anthrapyridone compound is also provided.
    Type: Grant
    Filed: November 30, 1990
    Date of Patent: February 2, 1993
    Assignees: Sumitomo Chemical Company, Limited, Daili Chemical Company, Limited
    Inventors: Toshio Nakamatsu, Masanobu Terao, Shigetoshi Muneishi, Norio Kometani, Yoshiaki Hayashi
  • Patent number: 5182287
    Abstract: Novel heterocyclic alkaloids were isolated from a marine sponge. These compounds, and derivatives thereof, are useful antifungal and antitumor compounds. The novel compounds have the following structures: ##STR1## wherein R.sub.1 =H, alkyl, alkenyl, aryl, benzyl, acyl, benzoyl, or alkali metal;R.sub.2 and R'.sub.2 =O, S, NOX, or NNHX, wherein X is alkyl or aryl.
    Type: Grant
    Filed: August 20, 1991
    Date of Patent: January 26, 1993
    Assignee: Harbor Branch Oceanographic
    Inventors: Geewananda P. Gunawardana, Peter J. McCarthy, Neal S. Burres
  • Patent number: 5182383
    Abstract: The invention relates to new stable, crystalline forms of the t-butylester of ceftazidime of formula ##STR1## and the production thereof.
    Type: Grant
    Filed: February 23, 1990
    Date of Patent: January 26, 1993
    Assignee: Biochemie Gesellschaft m.b.H.
    Inventors: Bernhard C. Prager, Karl Wessely, Werner Veit
  • Patent number: 5182286
    Abstract: Insecticidal and fungicidal substituted 2-[6-(pyrimidinyl)-indol-1-yl]-acrylic esters of the formula ##STR1## in which R.sup.1 represents alkyl, or represents optionally substituted aralkyl,R.sup.2 represents dialkylamino, alkoxy or alkylthio, or represents in each case optionally substituted aralkyloxy or arylalkylthio,R.sup.3 and R.sup.4 in each case independently of one another represent hydrogen, cyano, halogen, or alkyl,R.sup.5, R.sup.6 and R.sup.8 represent hydrogen or other radicals, andR.sup.7 represents optionally substituted pyrimidinyl.The corresponding acetic acid esters are also active.
    Type: Grant
    Filed: January 18, 1991
    Date of Patent: January 26, 1993
    Assignee: Bayer Aktiengesellschaft
    Inventors: Thomas Seitz, Alexander Klausener, Dieter Berg, Ulrike Wachendorff-Neumann, Christoph Erdelen, Gerd Hanssler, Wilhelm Brandes, Stefan Dutzmann
  • Patent number: 5182282
    Abstract: Novel 4-benzyl-1H-indoles of the formula ##STR1## in all diastereoisomeric forms and mixtures thereof having anti-arhythmic activity.
    Type: Grant
    Filed: October 11, 1991
    Date of Patent: January 26, 1993
    Assignee: Roussel Uclaf
    Inventors: Francois Clemence, Jacques Guillaume, Gilles Hamon
  • Patent number: 5180719
    Abstract: Antimicrobial quinolonyl lactam esters comprising a lactam-containing moiety linked, by an ester group, to the 3-carboxy group of a quinolone moiety. These compounds are of the formula: ##STR1## wherein (1) R.sup.3, R.sup.4, and R.sup.5, together with bonds "a" and "b", form certain lactam-containing moieties similar to those known in the art to have antimicrobial activity; and(2) A.sup.2, A.sup.2, A.sup.3, R.sup.7, R.sup.8, and R.sup.9 form any of a variety of quinolone or naphthyridine structures similar to those known in the art to have antimicrobial activity.
    Type: Grant
    Filed: April 29, 1991
    Date of Patent: January 19, 1993
    Assignee: Norwich Eaton Pharmaceuticals, Inc.
    Inventors: Ronald E. White, Thomas P. Demuth, Jr.
  • Patent number: 5180821
    Abstract: Cyclic tetrabenzimidazole, a yellowish, visually non-fluorescent substance, and its chelates, tautomers, ionization and oxidation forms, having utility as chelating agents, catalysts and electrooptic components.
    Type: Grant
    Filed: March 9, 1992
    Date of Patent: January 19, 1993
    Assignee: Moleculon Research Company
    Inventors: Arthur S. Obermayer, James B. Hendrickson, Sajjat Hussoin
  • Patent number: 5179120
    Abstract: A porphycene having the structure ##STR1## wherein each R.sup.1 is, independently, (a) --(CH.sub.2).sub.n --X, where n=1-4, X is OR.sup.2 and R.sup.2 is C.sub.1-6 alkyl, aralkyl or aryl; CN; OH; OSO.sub.2 R.sup.2 ; NH.sub.2 ; NHR.sup.2 ; NR.sub.2.sup.2 ; SH; SR.sup.2 ; S(O).sub.1-2 R.sup.2 ; COOH; CO.sub.2 R.sup.2 ; C(O)NH.sub.2 ; C(O)NHR.sup.2 ; C(O)NR.sub.2.sup.2 ; halogen; or CHO;(b) --(CH.sub.2).sub.m CH.dbd.CH.sub.2 where m is 0-2; or(c) --(CH.sub.2).sub.n --O--G where G is a mono- or oligosaccharide;(d) --(CH.sub.2).sub.2n --X, where X is an amino acid, oligopeptide covalently bonded by an ether-, ester- or amine-bond or --Y--(CH.sub.2).sub.n -porphycene.sup.2 (porphycene.sup.2 being a compound of the same structure and Y is a direct bond; --O--; or --CH.dbd.CH.sub.2); or(e) where one, two or three of the substituents R.sup.1 are C.sub.1-6 alkyl or aryl and the remaining substituents are as above under (a)-(d), and salts and metal complexes thereof.
    Type: Grant
    Filed: June 28, 1991
    Date of Patent: January 12, 1993
    Assignee: Cytopharm, Inc.
    Inventors: Emanuel Vogel, Clemens Richert, Thomas Benninghaus, Martin Muller, Alexander D. Cross
  • Patent number: 5179088
    Abstract: 1-Carba(1-dethia)cephem antibacterial agents possessing a 3-(substituted or unsubstituted)thiazolo group are provided. Further provided is a method for treating bacterial infections in man and other animals and a pharmaceutical formulation utilziing said 1-carba(1-dethia)cephems.
    Type: Grant
    Filed: June 25, 1990
    Date of Patent: January 12, 1993
    Assignee: Eli Lilly and Company
    Inventors: William J. Hornback, John E. Munroe
  • Patent number: 5177095
    Abstract: Substituted triazoles attached through a methylene bridge to novel substituted phenyl derivatives of the Formula I, are useful as angiotensin II antagonists.
    Type: Grant
    Filed: August 13, 1991
    Date of Patent: January 5, 1993
    Assignee: Merck & Co., Inc.
    Inventors: William J. Greenlee, Arthur A. Patchett, David Hangauer, Wallace Ashton, Kenneth J. Fitch, Thomas F. Walsh, Ralph A. Rivero, Daljit S. Dhanoa
  • Patent number: 5177216
    Abstract: The present invention provides a new diastereomer ester compound which is useful as an intermediate in the making of an optically active 3,4-dihydro-3,4-epoxy-2H-1-benzopyran compound.
    Type: Grant
    Filed: May 13, 1991
    Date of Patent: January 5, 1993
    Assignee: Yoshitomi Pharmaceutical Industries, Ltd.
    Inventor: Tsutomu Yamanaka