Patents Examined by David E. Wheeler
  • Patent number: 4001243
    Abstract: Certain substituted 6,7-dihydro-1-oxo-1H,5H-benzo[ij]-quinolizine-2-carboxylic acids and hydrazides, esters, amides and salts thereof, intermediates therefor, and a process for their preparation are described; the compounds are active as anti-microbial agents.
    Type: Grant
    Filed: January 22, 1975
    Date of Patent: January 4, 1977
    Assignee: Riker Laboratories, Inc.
    Inventor: John F. Gerster
  • Patent number: 4001244
    Abstract: 1-Aryl-3,4-dihydro-2(1H)-isoquinolinecarbonyl chlorides, useful in the preparation of the corresponding carboxamides, are described herein. The subject compounds can be prepared by reacting an 1-aryl-3,4-dihydro-2(1H)-isoquinoline with phosgene.
    Type: Grant
    Filed: April 25, 1975
    Date of Patent: January 4, 1977
    Assignee: G. D. Searle & Co.
    Inventor: Peter K. Yonan
  • Patent number: 4001245
    Abstract: The title compound possesses pharmacological activity as an anti-inflammatory agent.
    Type: Grant
    Filed: December 2, 1975
    Date of Patent: January 4, 1977
    Assignee: Morton-Norwich Products, Inc.
    Inventor: Thomas J. Schwan
  • Patent number: 4001225
    Abstract: This invention relates to new cephalosporanic acid derivatives and pharmaceutically acceptable salts thereof which possess antibacterial activity, pharmaceutical composition of the same and processes for the preparation thereof.
    Type: Grant
    Filed: January 30, 1975
    Date of Patent: January 4, 1977
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventor: Hirokichi Harada
  • Patent number: 4001235
    Abstract: 2-Amino-1,4-dihydropyridines bearing a carbonyl function in the 5-position and being optionally substituted by lower alkyl or phenyl in the 6-position, and the corresponding 2-amino-1,4,5,6,7,8-hexahydro-5-oxoquinolines, which derivatives are further substituted by a carbonyl group in the 3-position and optionally substituted in the 4-position by lower alkyl, phenyl, substituted phenyl or a heterocyclic group are antihypertensive agents and coronary vessel dilators. The compounds, of which 2-amino-6-methyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylic acid 3,5-diethyl ester is a representative embodiment, are prepared through condensation of an ylideneacetoacetic acid ester and an amidine.
    Type: Grant
    Filed: September 5, 1974
    Date of Patent: January 4, 1977
    Assignee: Bayer Aktiengesellschaft
    Inventors: Horst Meyer, Friedrich Bossert, Wulf Vater, Kurt Stoepel
  • Patent number: 4000133
    Abstract: A cephalosporanic acid derivative possessing antibacterial activity and pharmaceutically acceptable salts thereof, and processes for preparing same, having the general formula ##STR1## wherein R.sub.1 is hydrogen, aryl or a heterocyclic groupR.sub.2 is pyridyl or styryl, andR.sub.3 is hydrogen, alkylthio or an unsubstituted or alkyl substituted heterocyclic group.
    Type: Grant
    Filed: June 3, 1974
    Date of Patent: December 28, 1976
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Kazuo Kariyone, Osamu Nishiwaki, Kunikazu Takai
  • Patent number: 4000134
    Abstract: Compounds of the formula ##STR1## wherein R is H, heterocyclic thio, pyridinium, carbamoyloxy or acetoxy; Y is H, Cl or Br; and pharmaceutically acceptable salts and esters thereof are effective antibacterial agents.
    Type: Grant
    Filed: August 23, 1973
    Date of Patent: December 28, 1976
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Joseph Edward Dolfini
  • Patent number: 4000141
    Abstract: Cationic dyestuffs of the formula ##STR1## IN WHICH R represents alkyl, alkenyl, alkinyl, cycloalkyl, aralkyl or aryl,R.sub.1 represents hydrogen or an alkyl, alkenyl, alkinyl, cycloalkyl or aralkyl radical andAn.sup.- represents an anion, processes for their preparation and their use for dyeing, printing and bulk dyeing of natural and synthetic materials.
    Type: Grant
    Filed: October 11, 1974
    Date of Patent: December 28, 1976
    Assignee: Bayer Aktiengesellschaft
    Inventor: Hans Peter Kuhlthau
  • Patent number: 3998950
    Abstract: Derivatives of 7-aminocephalosporanic acid of the formula: ##STR1## wherein the carbon atom marked with an asterisk represents an asymmetry center of the molecule, A represents an aromatic nucleus, preferably phenyl which may be substituted by alkyl having 1-4 carbon atoms, halogen, hydroxy or alkoxy having 1-4 carbon atoms, or a heterocyclic nucleus, preferably 2- or 3-thiophene which may be, for example, substituted by halogen, R represents a hydrogen atom or a straight or branched chain lower alkyl radical, R.sub.1 represents a hydrogen atom, a hydroxy group, an acetoxy or pyridinium group. The invention includes the compounds as such or in the form of separated epimers as well as the corresponding pharmaceutically acceptable salts with alkali or alkaline-earth metals, with suitable organic bases or corresponding suitable organic or inorganic acid addition salts. Also method of preparing same. The compounds have powerful antibacterial action against gram-positive and gram-negative bacteria.
    Type: Grant
    Filed: March 28, 1975
    Date of Patent: December 21, 1976
    Assignee: ISF S.p.A.
    Inventors: Renato Broggi, Giuseppe Libassi, Giorgio Pifferi
  • Patent number: 3998808
    Abstract: This invention discloses new chemical compositions of matter having the formula: ##STR1## wherein A is a saturated or mono unsaturated aliphatic hydrocarbon chain having from 3 to 7 carbon atoms which optionally contains a maximum of three substituents selected from the group consisting of alkyl, alkoxy and halogen; and n is an integer from 1 to 3. This invention further discloses an insecticidal and fungicidal composition which comprises an inert carrier and, as an essential active ingredient, in a quantity toxic to insects and fungi, a compound of the above description; and a method for the control of insects and fungi which comprises applying to the locus of said insects or fungi an insecticidal and fungicidal composition heretofore described.
    Type: Grant
    Filed: May 18, 1971
    Date of Patent: December 21, 1976
    Assignee: Velsicol Chemical Corporation
    Inventors: Sidney B. Richter, Alfred A. Levin
  • Patent number: 3997542
    Abstract: Compounds useful as antiamebic agents are 1-(Ac.sub.1)-5-R-6-(Ac.sub.2 O)-1,2,3,4-tetrahydroquinolines (I), where Ac.sub.1 is haloacetyl, dihaloacetyl or trihaloacetyl with halo being chloro or bromo, R is hydrogen, chloro or bromo, and Ac.sub.2 is hydrogen, Ac.sub.1, alkanoyl having from one to sixteen carbon atoms, benzoyl, 2(or 3)-thenoyl, 2(or 3)-furoyl or N-(lower-alkyl)carbamoyl. Said compounds are prepared: by reacting 1,2,3,4-tetrahydro-6-quinolinol with an acyl halide of the formula Ac.sub.1 -halogen to produce 1-(Ac.sub.1)-1,2,3,4-tetrahydro-6-quinolinol having formula I where R and Ac.sub.2 are each hydrogen, Ac.sub.1 is defined as in formula I and halide is chloride or bromide; by reacting said 1-(Ac.sub.1)-1,2,3,4-tetrahydro-6-quinolinol with a chlorinating or brominating agent to produce the corresponding 1-(Ac.sub.1)-5-chloro(or bromo)-1,2,3,4-tetrahydro-6-quinolinol where Ac.sub.1 is defined as in claim 1; and, by reacting 1-(Ac.sub.
    Type: Grant
    Filed: June 23, 1975
    Date of Patent: December 14, 1976
    Assignee: Sterling Drug Inc.
    Inventor: Denis Mahlon Bailey
  • Patent number: 3996216
    Abstract: 3-Heterothio(formylamino)acetylamino cephalosporin derivatives of the general formula ##STR1## wherein R is hydrogen, lower alkyl, phenyl-lower alkyl, tri(lower alkyl)silyl, trihaloethyl, a salt forming ion or the group ##STR2## R.sub.1 is hydrogen, lower alkyl, cyclo-lower alkyl, unsaturated cyclo-lower alkyl, phenyl, substituted phenyl, furyl, pyridyl or thienyl; R.sub.2 is a five or six membered nitrogen, sulfur and/or oxygen containing heterocyclic ring system; R.sub.3 is lower alkyl, phenyl or phenyl-lower alkyl; and R.sub.4 is hydrogen or lower alkyl; are useful antibacterial agents.
    Type: Grant
    Filed: May 28, 1975
    Date of Patent: December 7, 1976
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Hermann Breuer, Uwe D. Treuner
  • Patent number: 3996219
    Abstract: 3-Heterothio(.alpha.-thiocarbonylamino)cephalosporin derivatives of the general formula ##STR1## wherein R is hydrogen, lower alkyl, phenyl-lower alkyl, tri(lower alkyl)silyl, trihaloethyl, a salt forming ion or the group ##STR2## R.sub.1 is hydrogen, lower alkyl, cyclo-lower alkyl, unsaturated cyclo-lower alkyl, phenyl, substituted phenyl or thienyl; R.sub.2 and R.sub.5 each is hydrogen or lower alkyl; R.sub.3 is a five or six membered nitrogen, sulfur and/or oxygen containing ring system; and R.sub.4 is lower alkyl, phenyl or phenyl-lower alkyl; are useful as antibacterial agents.
    Type: Grant
    Filed: May 28, 1975
    Date of Patent: December 7, 1976
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Hermann Breuer, Uwe D. Treuner
  • Patent number: 3994887
    Abstract: Cephalosporin compounds with 3-substituted ureido or -thioureido group at position 7 and hydrogen or heterocyclicthiomethyl groups at position 3 are prepared. These compounds are antibacterial agents.
    Type: Grant
    Filed: June 4, 1975
    Date of Patent: November 30, 1976
    Assignee: Recherche et Industrie Therapeutiques (R.I.T.)
    Inventors: Pierre Crooij, Alain Colinet
  • Patent number: 3994889
    Abstract: 3-Heterothio(.alpha.-thiocarbonylamino)-7.alpha.-methoxycephalosporin derivatives of the general formula ##SPC1##Wherein R is hydrogen, lower alkyl, phenyl-lower alkyl, tri(lower alkyl)silyl, trihaloethyl, a salt forming ion or the group ##EQU1## R.sub.1 is hydrogen, lower alkyl, cyclo-lower alkyl, unsaturated cyclo-lower alkyl, phenyl, substituted phenyl or thienyl; R.sub.2 and R.sub.5 each is hydrogen or lower alkyl; R.sub.3 is a five or six membered nitrogen, sulfur and/or oxygen containing ring system, and R.sub.4 is lower alkyl, phenyl or phenyl-lower alkyl; are useful as antibacterial agents.
    Type: Grant
    Filed: May 28, 1975
    Date of Patent: November 30, 1976
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Hermann Breuer, Uwe D. Treuner
  • Patent number: 3994886
    Abstract: Cephalosporin compounds with 3-substituted ureido or -thioureido group at position 7 and hydrogen or heterocyclicthiomethyl groups at position 3 are prepared. These compounds are antibacterial agents.
    Type: Grant
    Filed: June 3, 1975
    Date of Patent: November 30, 1976
    Assignee: Recherche et Industrie Therapeutiques (R.I.T.)
    Inventors: Pierre Crooij, Alain Colinet
  • Patent number: 3995040
    Abstract: New cyclopenteno-quinolone derivatives of the formula ##SPC1##WhereinR is a saturated or unsaturated aliphatic hydrocarbyl, e.g., alkyl and alkenyl,X is hydrogen or alkyl, andY is halogen, azido, alkylthio, alkyl-sulfonyl, or nitrile or unsubstituted or substituted (e.g., alkyl mono or di-substituted) amino;And the pharmacologically compatible salts thereof; are outstandingly effective as bacteriostats in mammals.
    Type: Grant
    Filed: July 14, 1975
    Date of Patent: November 30, 1976
    Assignee: Boehringer Mannheim G.m.b.H.
    Inventors: Alfred Rhomberg, Herbert Berger, Kurt Stach, Wolfgang Vomel, Winfriede Sauer
  • Patent number: 3993646
    Abstract: A process for producing a 2-cephem or 3-cephem derivative compound of the formula: ##SPC1##Wherein R.sub.1 represents a substituted or unsubstituted amino radical and R.sub.4 represents hydrogen or a radical selected from the group consisting of carboxy, protected carboxy, ester, acid amide, acid anhydride, acid halide, acid azide and carboxy salt, and the dotted line indicates the alternate bond structure providing 3-cephem or 2-cephem, which comprises:Reacting a halogenated derivative selected from the group consisting of a halogenated penam derivative having the formula: ##SPC2##A halogenated cepham derivative of the formula: ##SPC3##Wherein X represents a halogen atom, R.sub.3 represents a radical selected from the group consisting of carboxy, protected carboxy, ester, acid amide, acid anhydride, acid halide, acid azide and carboxy salt, and R.sub.1 is as defined above, or mixtures thereof with a dehydrohalogenoic acid reagent.
    Type: Grant
    Filed: January 4, 1974
    Date of Patent: November 23, 1976
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Takashi Kamiya, Yoshihisa Saito, Tsutomu Teraji, Osamu Nakaguti, Teruo Oku, Hitoshi Nakamura, Masashi Hashimoto
  • Patent number: 3992386
    Abstract: Phenoxyacetic acids of the formula ##SPC1##Wherein R.sub.1 is H or alkyl of 1-4 carbon atoms; R.sub.2 is H, or when R.sub.4 is Q, also alkyl of 1-4 carbon atoms; R.sub.3 is methyl, phenyl or chlorophenyl; and R.sub.4 is piperidino, isoindolino, 1,2,3,4-tetrahydroquinolino, 1-R.sub.5 -1,2,3,4-tetrahydro-4-quinolyl, 4-piperidinophenyl, 4-piperidinophenoxy, 1-pyrryl, or Q, wherein R.sub.5 is H or alkyl of 1-4 carbon atoms; and Q is 4-oxo-1,2,3,4-tetrahydroquinolino, 4-hydroxy-1,2,3,4-tetrahydroquinolino, 4-chromanyl, 4-thiochromanyl or 1-phenyl-1,2,3,4-tetrahydro-4-quinolyl; and the salts thereof, possess cholesterol level-lowering activity.
    Type: Grant
    Filed: March 8, 1974
    Date of Patent: November 16, 1976
    Assignee: Merck Patent Gesellschaft mit beschrankter Haftung
    Inventors: Erich Schacht, Werner Mehrhof, Herbert Nowak, Zdenek Simane, Detlev Kayser
  • Patent number: 3992540
    Abstract: Novel 3-quinoline-carboxamides of the formula ##SPC1##Wherein R is selected from the group consisting of halogen, --CF.sub.3, --OCF.sub.3 and --SCF.sub.3 in the 7- or 8-position, R.sub.1 is selected from the group consisting of hydrogen and acyl of an aliphatic carboxylic acid of 2 to 4 carbon atoms, R.sub.3 is selected from the group consisting of hydrogen and alkyl of 1 to 4 carbon atoms and R.sub.2 is selected from the group consisting of thiazloyl, pyridinyl and oxazolyl and their non-toxic, pharmaceutically acceptable acid addition salts having analgesic activity and their preparation and novel intermediates.
    Type: Grant
    Filed: July 28, 1975
    Date of Patent: November 16, 1976
    Assignee: Roussel-UCLAF
    Inventors: Francois Clemence, Roger Deraedt, Andre Allais, Odile Le Martret