Patents Examined by Paul M. Coughlan, Jr.
  • N-Unsaturated fatty acid amides of tryptophan ester homologues and anti-cholesteric use thereof
    Patent number: 4448785
    Abstract: Ethylenically unsaturated fatty acid amides of tryptophan derivatives e.g. .alpha.-[1-oxo-9-octadecenylamino)]-1H-indole-3-propanoic acid, ethyl ester, are useful as pharmaceutical agents and are obtainable by reacting a mixed anhydride of a long chain unsaturated carboxylic acid with an appropriate tryptophan ester.
    Type: Grant
    Filed: June 24, 1982
    Date of Patent: May 15, 1984
    Assignee: Sandoz, Inc.
    Inventors: Faizulla G. Kathawala, John G. Heider
  • Purification of ceforanide
    Patent number: 4448958
    Abstract: Crude cephalosporin 7-[.alpha.-(2-aminomethylphenyl)acetamido]-3-[(1-carboxymethyltetrazol-5-y lthio)methyl]-3-cephem-4-carboxylic acid is purified by converting it to its salt with benzyldimethylamine, recovering said salt and from it regenerating said cephalosporin in purified form.
    Type: Grant
    Filed: October 20, 1982
    Date of Patent: May 15, 1984
    Assignee: Bristol-Myers Company
    Inventors: Paul D. Sleezer, Richard R. Smith
  • Process for the production of bis(4-hydroxyphenyl)biphenyl disulfone
    Patent number: 4449003
    Abstract: The present invention relates to a process for the production of bis(4-hydroxyphenyl)biphenyl disulfone.
    Type: Grant
    Filed: April 2, 1982
    Date of Patent: May 15, 1984
    Assignee: Mobay Chemical Corporation
    Inventor: John R. Sanderson
  • 3-Carbamoyloxymethylcephem derivatives, and antibacterial drugs containing same
    Patent number: 4448775
    Abstract: The invention provides 3-carbamoyloxymethylcephem derivatives represented by the general formula: ##STR1## wherein R.sub.1 represents hydrogen atom or trichloroacetyl group, R.sub.2 represents hydrogen atom or methoxy group, and R.sub.3 represents hydrogen atom or hydroxyl group, or pharmaceutically acceptable salt thereof. The cephem derivatives of the invention are useful as antibacterial drugs.
    Type: Grant
    Filed: September 23, 1982
    Date of Patent: May 15, 1984
    Assignee: Eisai Co., Ltd.
    Inventors: Shigeto Negi, Yoshimasa Machida, Hiroshi Yamauchi, Isao Saito, Yoshikazu Hasagawa, Tamio Kawamura
  • 7-[2-Alkoxyimino-2-(5-amino-1,2,4-thiadiazol-3-yl)acetamido]-3-cephems
    Patent number: 4447429
    Abstract: This invention relates to novel cephem compounds of high antimicrobial activity of the formula ##STR1## wherein R.sup.1 is amino or a protected amino,R.sup.2 is lower alkyl,R.sup.3 is hydrogen or lower alkyl,R.sup.4 is hydrogen, acyloxy(lower)alkyl or acylthio(lower)alkyl andR.sup.5 is carboxy or a protected carboxy.
    Type: Grant
    Filed: December 5, 1980
    Date of Patent: May 8, 1984
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Tsutomu Teraji, Kazuo Sakane, Jiro Goto
  • Hydroxy and hydroperoxy tetrahydropyrimidines
    Patent number: 4447606
    Abstract: This invention relates to 5-hydroperoxy and/or 5-hydroxy derivatives of 2,2,4,4-dipentamethylene 5,6-tetramethylene 2,3,4,5-tetrahydropyrimidines; and to the preparation thereof. The compounds of this invention have utility as corrosion inhibitors.
    Type: Grant
    Filed: April 9, 1979
    Date of Patent: May 8, 1984
    Assignee: Petrolite Corporation
    Inventor: Bernardus A. Oude Alink
  • 1,2,3,4-Tetrahydroisoquinolines 6.10,7,8 dihydroxy substitute-1-methylanilino and use as smooth muscle relaxants
    Patent number: 4447436
    Abstract: 1,2,3,4-Tetrahydroisoquinolines having the formula: ##STR1## wherein R.sub.1 and R.sub.2 are each hydrogen, lower alkyl, lower alkenyl, acyl, aryl or ar(lower)alkyl, in which aryl and the aryl moiety of the ar(lower)alkyl may contain at least one substituent selected from the group consisting of halogen, lower alkoxy, amino, nitro, hydroxy, acyloxy, ar(lower)alkoxy, lower alkylenedioxy, halo(lower)alkyl, acylamino, ar(lower)alkylamino and aryl, and pharmaceutically acceptable salts thereof, having a relaxant activity on smooth muscles.
    Type: Grant
    Filed: January 4, 1980
    Date of Patent: May 8, 1984
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Teiji Kishimoto, Hiromu Kochi, Masayuki Kato
  • N-Substituted thioxobenzothiazolines
    Patent number: 4447618
    Abstract: The present invention relates to compounds of the formula ##STR1## wherein: T is hydrogen, lower alkyl, halo, --CF.sub.3, --CN or --NO.sub.2 ; x is 1 or 2; n is 1 or 2; m is zero or 1; when m is 1, R is hydrogen, lower alkyl, halo (lower) alkyl, lower alkenyl, halo (lower) alkenyl, benzyl, phenyl, carbamoyl (lower) alkyl, cyano (lower) alkyl or agriculturally acceptable salts; when m is zero, R is ##STR2## R.sub.1 and R.sub.2 independently equal hydrogen, lower alkyl, lower alkenyl, lower alkoxy (lower) alkyl or phenyl; R.sub.3 is hydrogen or lower alkyl; a is 4, 5 or 6.
    Type: Grant
    Filed: July 5, 1979
    Date of Patent: May 8, 1984
    Assignee: Monsanto Company
    Inventor: John J. D'Amico
  • Di(tri-lower alkylstannyl)pyrimidine derivative and a process for producing the same
    Patent number: 4447605
    Abstract: The present invention relates to a novel process for producing pyrimidine nucleosides by a reaction between bis(tri-lower alkylstannyl)-5-halogenouracil and 2-substituted tetrahydrofurane. The novel process of the present invention makes it possible to obtain, depending upon the manner of substitution of tetrahydrofurane residue on two nitrogen atoms N.sub.1 and N.sub.3 of 5-halogenouracil, N.sub.1 -mono-substituted compound, N.sub.3 -mono-substituted compound and N.sub.1,N-di-substituted compound among which the last can be converted by hydrolysis thereof into N.sub.1 -mono-substituted compound. The present invention further relates to novel N.sub.3 -mono-substituted compounds and N.sub.1,N.sub.3 -di-substituted compounds obtained by such process. The present invention still further relates to novel bis-(tri-lower alkylstannyl)-5-halogenouracil used in the present invention as a raw compound.
    Type: Grant
    Filed: July 28, 1981
    Date of Patent: May 8, 1984
    Assignee: Rikagaku Kenkyusho
    Inventors: Masanao Matsui, Tomoya Ogawa
  • 10-Substituted 5-cyanomethylene-dibenzo[A,B]-cycloheptenes, their preparations, and therapeutic agents containing these compounds
    Patent number: 4447610
    Abstract: 10-Substituted 5-cyanomethylene-dibenzo[a,d]-cycloheptenes, their pure cis- and trans-isomers, their N-oxides and their pharmaceutically tolerated addition salts with acids, processes for their preparation, therapeutic agents containing these compounds and their use as drugs, especially as sedatives, hypnotics or tranquilizers.
    Type: Grant
    Filed: February 25, 1981
    Date of Patent: May 8, 1984
    Assignee: BASF Aktiengesellschaft
    Inventors: Gerd Steiner, Hans P. Hofmann, Horst Kreiskott, Hans-Juergen Teschendorf, Dieter Lenke
  • Cephalosporin antibiotics
    Patent number: 4446317
    Abstract: The invention provides novel antibiotic cefuroxime esters of the formula ##STR1## (wherein R is a primary or secondary alkyl group containing 1 to 4 carbon atoms). These compounds are useful as orally administrable broad spectrum antibiotics.
    Type: Grant
    Filed: January 27, 1982
    Date of Patent: May 1, 1984
    Assignee: Glaxo Operations U.K. Limited
    Inventors: Michael Gregson, Richard B. Sykes
  • Cationic naphtholactam dyestuffs
    Patent number: 4446326
    Abstract: Cationic dyestuffs of the general formula ##STR1## wherein R represents hydrogen or an alkyl radical with a maximum of 8 C atoms, which is optionally substituted by non-ionic radicals,R.sup.1 represents hydrogen or an alkyl radical with a maximum of 4 C atoms, which is optionally substituted by non-ionic radicals, andAn.sup.- represents an anion, and whereinthe benzene rings and naphthalene rings can contain non-ionic radicals which are customary in dyestuff chemistry,are used for dyeing natural and synthetic cationically dyeable fibres, and paper.
    Type: Grant
    Filed: September 30, 1981
    Date of Patent: May 1, 1984
    Assignee: Bayer Aktiengesellschaft
    Inventor: Alfred Brack
  • Cephalosporin derivative and pharmaceutical composition containing the derivative
    Patent number: 4446137
    Abstract: A compound having the general formula (I) is derived from a cephalosporin; ##STR1## wherein R' is a hydrogen atom, an alkyl group having 1 to 4 atoms or an alkali metal and R is --CH.sub.2 COOR', --CH.sub.2 CH.sub.2 SR', ##STR2## or --CH.sub.2 CH.sub.2 COOR' wherein R' is defined above. A pharmaceutical composition containing the compound is excellent in an antibacterial activity, the activity being recovered by the action of an activating enzyme in a living body although the compound per se shows a low activity against the beneficial bacterial colonies in a living body.
    Type: Grant
    Filed: September 16, 1982
    Date of Patent: May 1, 1984
    Assignee: Kureha Kagaku Kogyo Kabushiki Kaisha
    Inventors: Shigeaki Muto, Kouichi Niimura, Takao Ando, Masahiko Fujii, Takao Furusho, Chikao Yoshikumi
  • 10 Oxo-4,5-dihydro-10H-benzo 5,6 cycloheph[1,2-B]pyrryls
    Patent number: 4444981
    Abstract: A compound of formula (II): ##STR1## wherein R is a C.sub.1-4 alkyl group;R.sub.1 is a hydrogen atom or a C.sub.1-4 alkyl group;R.sub.2 is a hydrogen or halogen atom, or a C.sub.1-4 alkyl, C.sub.1-4 alkoxy or C.sub.1-4 alkylthio group;and pro-drugs thereof; and the pharmaceutically acceptable salts of the compounds of formula (II) and of their pro-drugs; has useful anti-inflammatory and analgesic activity.
    Type: Grant
    Filed: July 25, 1980
    Date of Patent: April 24, 1984
    Assignee: Beecham Group Limited
    Inventor: Alexander C. Goudie
  • 7-Heteroaryl[1,2,4]triazolo[1,5-a]pyrimidines
    Patent number: 4444774
    Abstract: This disclosure describes 7-heteroaryl[1,2,4]triazolo[1,5-a]pyrimidines which are useful as anxiolytic agents.
    Type: Grant
    Filed: July 29, 1982
    Date of Patent: April 24, 1984
    Assignee: American Cyanamid Company
    Inventors: John P. Dusza, Jay D. Albright
  • Imidazobenzothiadiazepines
    Patent number: 4444688
    Abstract: 5-Diazacycloalkyl-imidazo[2,1-b][1,3,5]benzothiadiazepines, e.g. those of the formula ##STR1## the N-oxides and salts thereof are neuroleptic agents, lacking extrapyramidal side-effects.
    Type: Grant
    Filed: August 9, 1982
    Date of Patent: April 24, 1984
    Assignee: Ciba-Geigy Corporation
    Inventor: Isidoros Vlattas
  • Production of 3-pyrrolin-2-ones
    Patent number: 4443616
    Abstract: Pyrrolidin-2-ones are produced by hydrogenation of 3-pyrrolin-2-ones, which latter compounds could not prior to this invention be easily obtained. These 3-pyrrolin-2-ones with various substituents are produced by ring closure of N-aroylmethyl-acetamides. The ring closure is effected in basic media under nitrogen.
    Type: Grant
    Filed: April 21, 1981
    Date of Patent: April 17, 1984
    Assignee: The Purdue Frederick Company
    Inventor: Peter Hofer
  • Benzofuran derivatives, process for their preparation and their therapeutic applications
    Patent number: 4443468
    Abstract: This invention relates to compounds having the general formula: ##STR1## in which ##STR2## is selected from: a radical ##STR3## in which R'.sub.1 is hydrogen and R'.sub.2 is selected from hydrogen; C.sub.1-6 alkyl; C.sub.2-6 alkenyl; C.sub.2-6 alkynyl; phenyl; phenyl C.sub.1-6 alkyl; mono-, di- and trimethoxyphenyl C.sub.1-6 alkyl; C.sub.1-6 alkoxy; benzyloxy; di-C.sub.1-6 alkylamino-C.sub.1-6 alkyl; C.sub.1-6 hydroxyalkyl; C.sub.1-6 alkyloxycarbonyl-C.sub.1-6 alkyl; or R'.sub.1 and R'.sub.2 are joined to form a heterocyclic ring;and their pharmacologically acceptable inorganic and organic acid addition salts.Said compounds are therapeutically useful for the treatment of dysrhythmia.
    Type: Grant
    Filed: March 5, 1982
    Date of Patent: April 17, 1984
    Assignee: Laboratoires Jacques Logeais
    Inventors: J. Georges Maillard, Jacky Legeai
  • Hydrogenated isoquinolines and peripheral vascular disease treating compositions thereof
    Patent number: 4442108
    Abstract: 1-(3,4-Dialkoxybenzyl)-6,7-dialkoxyl-1,2,3,4-tetrahydro- and 3,4-dihydroisoquinolines wherein the alkoxy groups in the benzyl ring are different from those in the isoquinoline nucleus and one contains from 2 to 6 carbon atoms while the other contains from 3 to 6 carbon atoms are useful in the treatment of peripheral vascular disease. A typical embodiment is 1-(3,4-diethexybenzyl)-6,7-diisopropoxy-3,4-dihydroisoquinoline hydrochloride.
    Type: Grant
    Filed: September 10, 1981
    Date of Patent: April 10, 1984
    Assignee: Laboratoires Sobio S.A. of Immeuble Perisud
    Inventors: Jean-Bernard Le Polles, Michel Martin, Guy Nadler, Edmond Saias
  • Development restrainer release compounds
    Patent number: 4442290
    Abstract: There are described novel compounds which are represented by the formula ##STR1## wherein R is ##STR2## A is sulfur or selenium; X represents the nonmetallic atoms necessary to form a nucleus which completes a five or six membered heterocyclic moiety; R.sub.1 is H or lower alkyl; R.sub.2 is H or a hydrolyzable group; and R.sub.3 is H, alkyl or a hydrolyzable group. The compounds are useful in photographic applications and provide controlled release of a photographically useful material during processing of photographic elements with an aqueous alkaline processing composition.
    Type: Grant
    Filed: March 29, 1982
    Date of Patent: April 10, 1984
    Assignee: Polaroid Corporation
    Inventors: James R. Bartels-Keith, Anthony J. Puttick