Patents Examined by Paul M. Coughlan, Jr.
  • Patent number: 4423213
    Abstract: The invention relates to novel 7-acylamino-3-vinylcephalosporanic acid derivatives of antimicrobial activity, and to methods of preparation thereof from novel intermediate compounds of the formula: ##STR1## in which R.sub.C is amino or a group of the formula: ##STR2## wherein R.sup.8 is aryl,A.sup.12 is lower alkylene having a group of the formula: .dbd.N.about.OR.sup.4, wherein R.sup.4 is hydrogen, cyclo(lower) alkenyl, lower alkynyl, lower alkenyl, lower alkenyl substituted by carboxy or a protected carboxy group, lower alkyl, or lower alkyl substituted by one or more substituent(s) selected from carboxy, a protected carboxy group, amino, a protected amino group, cyano, phosphono, a protected phosphono group and a heterocyclic group which may have suitable substituent(s),R.sup.a is a protected amino group,R.sup.b is a protected carboxy group,R.sup.c and R.sup.d are combined to form oxo or a protected oxo group, and X.sup.1 is halogen, andR.sup.
    Type: Grant
    Filed: May 7, 1981
    Date of Patent: December 27, 1983
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Takao Takaya, Hisashi Takasugi, Takashi Masugi, Hideaki Yamanaka, Kohji Kawabata
  • Patent number: 4421912
    Abstract: A compound of the formula: ##STR1## wherein R.sup.1 represents hydrogen or an alkyl group, X represents oxygen or sulfur or a group of formula --NR.sup.2 (where R.sup.2 is hydrogen or an alkyl group and in the case of alkyl, it may form a ring jointed with R.sup.1), and Y represents acetoxy group or a group of formula --SR.sup.3 (where R.sup.3 is a nitrogen-containing heterocyclic group), or a pharmaceutically acceptable salt thereof, is found to have a broad antimicrobial spectrum and, in particular, effective against gram-negative bacteria including Escherichia coli, Klebsiella pneumoniae, Proteus vulgaris, Proteus morganii, as well as gram positive ones. Thus, these compounds may be used for antimicrobial agents in therapeutical purposes.
    Type: Grant
    Filed: February 18, 1981
    Date of Patent: December 20, 1983
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Mitsuo Numata, Isao Mimamida, Masayoshi Yamaoka, Mitsuru Shiraishi, Toshio Miyawaki
  • Patent number: 4421913
    Abstract: An improvement in the production of methotrexate as set out in Ellard U.S. Pat. No. 4,080,325. It has been found that magnesium oxide facilitates the coupling reaction by acting as an acid acceptor. The dense grade of magnesium oxide is preferred in molar proportions of 2 to 4 moles of magnesium oxide per mole of 2,4-diamino-6-hydroxymethylpteridine. Further, the triphenylphosphine oxide which is generated by hydrolysis of the protecting groups is removed from the reaction stream by utilization of toluene or BTX-type solvents.
    Type: Grant
    Filed: December 11, 1981
    Date of Patent: December 20, 1983
    Assignee: The United States of America as represented by the Secretary of the Department of Health and Human Services
    Inventors: James A. Ellard, James A. Webster
  • Patent number: 4420478
    Abstract: Novel syn isomers of oximes of 3-azidomethyl-7-amino-thiazolyl-cephalosporanic acids of the formula ##STR1## wherein R is selected from the group consisting of hydrogen, alkyl of 1 to 4 carbon atoms, unsaturated alkyl of 2 to 4 carbon atoms, benzoyl and --(CH.sub.2).sub.n --R.sub.1, n is an integer from 1 to 4, R.sub.1 is selected from the group consisting of NH.sub.2 and --COOA' and A' and A are selected from the group consisting of hydrogen, alkali metal, alkaline earth metal, magnesium, --NH.sub.4, an easily cleavable ester group and a non-toxic, pharmaceutically acceptable organic amine and their non-toxic, pharmaceutically acceptable acid addition salts having antibiotic activity and a novel process and novel intermediates for their preparation.
    Type: Grant
    Filed: April 9, 1979
    Date of Patent: December 13, 1983
    Assignee: Roussel Uclaf
    Inventors: Rene Heymes, Andre Lutz
  • Patent number: 4420325
    Abstract: This invention relates to benzylsulfonylureas which are active pre- and post-emergence herbicides.
    Type: Grant
    Filed: April 22, 1982
    Date of Patent: December 13, 1983
    Assignee: E. I. Du Pont de Nemours & Company
    Inventor: Richard F. Sauers
  • Patent number: 4418199
    Abstract: Novel tricyclic imidyl derivatives, for example those of the formula ##STR1## [n=1 or 2, Y=a bridge member and X=a functional group] are described. The novel tricyclic imidyl derivatives are suitable for the preparation of photocrosslinkable polymers by incorporation into existing polymer chains or by building up the polymer chain from tricyclic imidyl derivatives, according to the definition, with suitable functional groups X by polymerization or polycondensation. The photocrosslinkable polymers obtained by this means can be used, for example, to produce printing plates for the offset printing process and especially as photoresists.
    Type: Grant
    Filed: February 16, 1982
    Date of Patent: November 29, 1983
    Assignee: Ciba-Geigy Corporation
    Inventors: Hans Zweifel, Walter Schilling, Angelo Storni, Daniel Bellus
  • Patent number: 4417058
    Abstract: Novel tricyclic imidyl derivatives, for example those of the formula ##STR1## [n=1 or 2, Y=a bridge member and X=a functional group] are described. The novel tricyclic imidyl derivatives are suitable for the preparation of photocrosslinkable polymers by incorporation into existing polymer chains or by building up the polymer chain from tricyclic imidyl derivatives, according to the definition, with suitable functional groups X by polymerization or polycondensation. The photocrosslinkable polymers obtained by this means can be used, for example, to produce printing plates for the offset printing process and especially as photoresists.
    Type: Grant
    Filed: February 16, 1982
    Date of Patent: November 22, 1983
    Assignee: Ciba-Geigy Corporation
    Inventors: Hans Zweifel, Walter Schilling, Angelo Storni, Daniel Bellus
  • Patent number: 4415562
    Abstract: New cephalosporins of the general formula: ##STR1## in which R is alkyl, L-2-amino-2-carboxyethyl, phenyl or various heterocyclic rings, R' is a hydrogen atom or a radical of the general formula: ##STR2## and R.degree. is hydrogen, alkyl, vinyl, cyanomethyl or a carboxyalkyl radical of the general formula: ##STR3## and also their salts, their preparation and the pharmaceutical compositions in which they are present.
    Type: Grant
    Filed: November 19, 1981
    Date of Patent: November 15, 1983
    Assignee: Rhone-Poulenc Industries
    Inventors: Daniel Farge, Pierre L. Roy, Claude Moutonnier, Jean-Francois Peyronel
  • Patent number: 4415735
    Abstract: The invention provides new cephalosporins of the general formula: ##STR1## in which n=0 or 1, R.sub.4 is an amine-protecting radical, R.sup.a.sub.5 and R.sup.b.sub.5, which are identical or different, are hydrogen atoms or alkyl radicals, or form an alkylene radical of 2 or 3 carbon atoms, R.sup.c.sub.5 is a hydrogen atom or an acid-protecting radical and R.sub.2 is an acid-protecting radical or a radical which can easily be removed by an enzymatic method. The compounds of formula (I) are in the form of a 3-oxoethyl-bicyclooct-2-ene or -bicyclooct-3-ene or a 3-oxoethylidenebicyclooctane if n=0, and in the form of a 3-oxoethylbicyclooct-2-ene or a 3-oxoethylidenebicyclooctane if n=1. They are useful as intermediates for the preparation of pharmaceutically active cephalosporins.
    Type: Grant
    Filed: November 19, 1981
    Date of Patent: November 15, 1983
    Assignee: Rhone-Poulenc Industries
    Inventors: Daniel Farge, Pierre L. Roy, Claude Moutonnier, Jean-Francois Peyronel
  • Patent number: 4415575
    Abstract: Heterocyclic carbamates are disclosed which have potent gastric secretion inhibitory properties. The heterocyclic substituent is a pyridyl group or a 6-membered heterocycle with two nitrogen heteroatoms, which may be optionally substituted. Further substituents on the carbamate nitrogen and oxygen atoms are also disclosed. The compounds have profound effects on the inhibition of gastric secretions in the gastro-intestinal tract, and compositions for such uses are also disclosed.
    Type: Grant
    Filed: February 5, 1982
    Date of Patent: November 15, 1983
    Assignee: Merck & Co., Inc.
    Inventors: William A. Bolhofer, John D. Prugh
  • Patent number: 4414387
    Abstract: Cephapirin acetylcysteinate having antibacterial activity. Said salt is obtained by reacting an aqueous solution of cephapirin with an aqueous solution of acetylcysteine. To isolate the salt, the aqueous solution is submitted to lyophilization.
    Type: Grant
    Filed: May 13, 1982
    Date of Patent: November 8, 1983
    Inventors: Renato Broggi, Marco Falciani
  • Patent number: 4414216
    Abstract: There are disclosed tetrahydrofuran compounds and analogs thereof of the formula: ##STR1## and pharmaceutically acceptable acid addition salts thereof, wherein X is oxygen or sulfur, R.sup.1 and R.sup.2 are each hydrogen, halogen, lower alkyl or lower alkoxy, and Am is a group of the formula: ##STR2## wherein Z is oxygen or sulfur, R.sup.3 is hydrogen or halogen, R.sup.4 is hydrogen, lower alkyl or phenyl which may be substituted by 1 to 3 substituents at any position(s) on the phenyl nucleus, each substituent being independently selected from halogen, lower alkyl and lower alkoxy, and R.sup.5 is hydrogen or lower alkyl. Such compounds are useful as neuroleptics.
    Type: Grant
    Filed: June 21, 1982
    Date of Patent: November 8, 1983
    Assignee: Yoshitomi Phamaceutical Industries, Ltd.
    Inventors: Takeshi Kawakita, Yasuaki Chihara, Takemi Fukuda, Michihide Setoguchi, Tetsuya Tahara
  • Patent number: 4414394
    Abstract: Novel tricyclic imidyl derivatives, for example those of the formula ##STR1## [n=1 or 2, Y=a bridge member and X=a functional group] are described. The novel tricyclic imidyl derivatives are suitable for the preparation of photocrosslinkable polymers by incorporation into existing polymer chains or by building up the polymer chain from tricyclic imidyl derivatives, according to the definition, with suitable functional groups X by polymerization or polycondensation. The photocrosslinkable polymers obtained by this means can be used, for example, to produce printing plates for the offset printing process and especially as pohtoresists.
    Type: Grant
    Filed: February 16, 1982
    Date of Patent: November 8, 1983
    Assignee: Ciba-Geigy Corporation
    Inventors: Hans Zweifel, Walter Schilling, Angelo Storni, Daniel Bellus
  • Patent number: 4411898
    Abstract: A 3,7-disubstituted-3-cephem-4-carboxylic acid of the general formula: ##STR1## having antibacterial activity, processes for preparing same, and pharmaceutical compositions thereof for treating infectious diseases in humans and animals.
    Type: Grant
    Filed: April 29, 1981
    Date of Patent: October 25, 1983
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Takao Takaya, Masayoshi Murata
  • Patent number: 4412070
    Abstract: There is presented compounds of the formula ##STR1## wherein X represents the 1,2,5,6-tetrahydro-2-methyl- 5,6-dioxo-as-triazin-3-yl group or its corresponding tautomeric form, the 2,5-dihydro-6-hydroxy-2-methyl-5-oxo-as-triazin-3-yl group, and the readily hydrolyzable esters, readily hydrolyzable ethers and salts of the compounds and hydrates of the compounds of formula I or of their esters, ethers and salts. Also provided is a method of their manufacture and intermediates therefor as well as corresponding pharmaceutical preparations.
    Type: Grant
    Filed: September 28, 1981
    Date of Patent: October 25, 1983
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Roland Reiner
  • Patent number: 4411839
    Abstract: Novel 1-substituted pyrimidinediones and thiopyrimidineones, synthesis thereof and intermediates therefor, useful as control agents for pests.
    Type: Grant
    Filed: May 27, 1982
    Date of Patent: October 25, 1983
    Assignee: Zoecon Corporation
    Inventors: George R. Lindahl, III, Clive A. Henrick
  • Patent number: 4411690
    Abstract: Fused [1,2,4]oxadiazolylidenebenzenesulfonamides such as 2-chloro-N-(5,7-dimethyl-2H-[1,2,4]oxadiazolo-[2,3-a]pyrimidin-2-ylidene)b enzenesulfonamide and 2-chloro-N-(7-methoxy-5-methyl-2H-[1,2,4]oxadiazolo-[2,3-a][1,3,5]triazin- 2-ylidene)benzenesulfonamide are general and selective pre- or post-emergence herbicides and can be useful in regulating plant growth.
    Type: Grant
    Filed: December 3, 1981
    Date of Patent: October 25, 1983
    Assignee: E. I. Du Pont de Nemours & Co.
    Inventor: Chi-Ping Tseng
  • Patent number: 4411897
    Abstract: The invention relates to the novel crystalline hydrochloride and the crystalline hydrobromide of 7.beta.-[2-(2-amino-4-thiazolyl)-2-methoxyiminoacetamido]-3-cephem-4-carbo xylic acid pivaloyloxymethyl ester, a process for the production thereof, and pharmaceutical preparations that contain these compounds.
    Type: Grant
    Filed: January 15, 1981
    Date of Patent: October 25, 1983
    Assignee: Ciba-Geigy Corporation
    Inventor: Riccardo Scartazzini
  • Patent number: 4410522
    Abstract: Novel penicillins and cephalosporins and non-toxic salts thereof, which contain a mono- or di-oxo- or thioxo-piperazino(thio)carbonylamino group in molecule. These compounds are valuable antibacterial compounds for use in mammals including man. This disclosure relates to such compounds and a process for the preparation thereof.
    Type: Grant
    Filed: October 12, 1977
    Date of Patent: October 18, 1983
    Assignee: Toyama Chemical Co., Ltd.
    Inventors: Isamu Saikawa, Shuntaro Takano, Chosaku Yoshida, Okuta Takashima, Kaishu Momonoi, Seietsu Kuroda, Miwako Komatsu, Takashi Yasuda, Yutaka Kodama
  • Patent number: 4409217
    Abstract: The invention relates to new cephem compounds, of high antimicrobial activity of the formula: ##STR1## wherein R.sup.1 is amino or protected amino,R.sup.2 is carboxy(lower)alkyl or protected carboxy(lower)alkyl,R.sup.3 is halogen or lower alkoxy, andR.sup.4 is carboxy or protected carboxy,and a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: September 26, 1980
    Date of Patent: October 11, 1983
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Takao Takaya, Hisashi Takasugi, Toshiyuki Chiba, Kiyoshi Tsuji