Additional Nitrogen Containing Hetero Ring (e.g., Thiazetidine, Etc.) Patents (Class 544/111)
  • Patent number: 5176737
    Abstract: A herbicidal compound of formula (I): ##STR1## in which Ar is an optionally substituted aryl or heterocyclic ring system:R.sup.1 and R.sup.2 are independently selected from H, optionally substituted alkyl, alkenyl or akynyl, halogen, NR.sup.a R.sup.b, or R.sup.1 and R.sup.2 together with the carbon to which they are attached form an optionally substituted alkenyl or cycloalkyl group;R.sup.3 is CO.sub.2 R.sup.4, CN, COR.sup.4, CH.sub.2 OR.sup.4, CH.sub.4 (OH)R.sup.4, CH(OR.sup.4)R.sup.5, CH.sub.2 OSO.sub.6 R.sup.4, CH.sub.2 OSO.sub.6 R.sub.4, CH.sub.2 ONR.sup.6 R.sup.7, CSNH.sub.2, COSR.sup.4, SCOR.sup.4, COHNSO.sub.2 R.sup.4, CONR.sup.6 R.sup.7, CONHNR.sup.6 R.sup.7, CONHN.sup.+ R.sup.6 R.sup.7 R.sup.8 Y.sup.-2, CO.sub.2.sup.- M.sup.+ or COON.dbd.CR.sup.6 R.sup.7 ;M.sup.+ is an agriculturally acceptable cation;Y.sup.- is an agriculturally acceptable anion;R.sup.4, and R.sup.5 are independently selected from H or an optionally substituted alkyl, aryl, alkenyl or alkynyl group;R.sup.6, R.sup.7, R.sup.8, R.sup.
    Type: Grant
    Filed: February 7, 1991
    Date of Patent: January 5, 1993
    Assignee: Imperial Chemical Industries PLC
    Inventors: Ewan J. T. Chrystal, John E. D. Barton, David Cartwright, Christopher J. Mathews
  • Patent number: 5159072
    Abstract: A method of heating dichloromethane laden streams to prevent discharge into the environment by contacting the laden stream with N,N-dialkyldithiocarbamate salt in the presence of oxygen and water.
    Type: Grant
    Filed: October 5, 1990
    Date of Patent: October 27, 1992
    Assignee: Eastman Kodak Company
    Inventor: Arunas V. Kavaliunas
  • Patent number: 5136868
    Abstract: Herbicidal aryltetrazolinones and thiones of the formula ##STR1## in which W is oxygen or sulfur; R is alkyl, fluoroalkyl, alkenyl, haloalkenyl, cyanoalkyl, alkylthioalkyl, haloalkoxyalkyl, trifluoromethylthio or alkoxyalkyl; one of X.sup.1 and X.sup.2 is fluorine, chlorine, or bromine and the other is fluorine, chlorine, bromine, alkyl, nitro or haloalkyl; and Z is a group selected from a variety of substituents including 2-propynyloxy as disclosed and exemplified.
    Type: Grant
    Filed: December 28, 1989
    Date of Patent: August 11, 1992
    Assignee: FMC Corporation
    Inventor: George Theodoridis
  • Patent number: 5103006
    Abstract: Novel compounds of the formula ##STR1## wherein X is sulfur or oxygen, R.sub.2 is aryl or heterocyclo and R.sub.1 is as defined herein, are disclosed. Compounds of formula I possess calcium channel activating activity.
    Type: Grant
    Filed: August 21, 1990
    Date of Patent: April 7, 1992
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: George C. Rovnyak, Spencer D. Kimball
  • Patent number: 5101032
    Abstract: Cycloalkylidene dyes have the formula ##STR1## where m is 0 or 1,L is a chemical bond or C.sub.1 -C.sub.2 -alkylene, which may be substituted,R.sup.1 is hydrogen, C.sub.1 -C.sub.20 -alkyl, which may be phenyl-substituted, substituted or unsubstituted phenyl, naphthyl or C.sub.3 -C.sub.7 -cycloalkyl,Y is oxygen or two hydrogens,X.sup.1 is oxygen andX.sup.2 is C.sub.1 -C.sub.8 -alkanoyloxy, substituted or unsubstituted benzoyloxy, C.sub.1 -C.sub.6 -trialkylsilyloxy or a radical of the formula OR.sup.1 or NR.sup.2 R.sup.3, where R.sup.1 is as defined above and R.sup.2 and R.sup.3 are identical or different and each is independently of the other C.sub.1 -C.sub.20 -alkyl, which may be phenyl-substituted, substituted or unsubstituted phenyl, naphthyl, or C.sub.3 -C.sub.7 -cycloalkyl or R.sup.2 and R.sup.3 together with the nitrogen atom joining them are saturated heterocyclyl, or else one of R.sup.2 and R.sup.3 is hydrogen, or X.sup.1 and X.sup.
    Type: Grant
    Filed: October 22, 1990
    Date of Patent: March 31, 1992
    Assignee: BASF Aktiengesellschaft
    Inventors: Hans-Dieter Martin, Bernhard Albert, Knut Kessel
  • Patent number: 5068231
    Abstract: A method of treating animals to obtain muscle relaxation and/or to relieve anxiety is disclosed utilizing novel and known 3-aryloxy and 3-arylthioazetidinecarbonxamides having the formula: ##STR1## wherein Z is oxygen or sulfur; B is oxygen or sulfur; Ar is pyridyl or halo substituted pyridyl, phenyl or substituted phenyl; R.sup.1 and R.sup.2 are hydrogen, loweralkyl, aryl, allyl groups, propargyl, cycloalkyl, loweralkylcycloalkyl, cycloakylloweralkyl, arylloweralkyl and diloweralkylaminoalkyl, and R.sup.1 and R.sup.2 when taken together with the adjacent nitrogen atom may form a heterocyclic amine radical; R.sup.3 is hydrogen, loweralkyl, aryl or arylloweralkyl, and the geometrical isomers thereof and pharmaceutical salts thereof and hydrates thereof when they are possible.
    Type: Grant
    Filed: October 22, 1986
    Date of Patent: November 26, 1991
    Assignee: A. H. Robins Company Incorporated
    Inventors: Chandler R. Taylor, Jr., Albert D. Cale. Jr., David N. Johnson, Harold F. Stauffer. Jr.
  • Patent number: 5053430
    Abstract: Novel compounds having the general formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are as defined herein. These compounds are useful in the treatment of schizophrenia.
    Type: Grant
    Filed: September 22, 1989
    Date of Patent: October 1, 1991
    Assignee: Boehringer Ingelheim KG
    Inventors: Matthias Grauert, Herbert Merz, Joachim Mierau, Gunter Schingnitz, Claus Schneider
  • Patent number: 5041440
    Abstract: Novel dithiolane derivatives of formula: ##STR1## wherein X is, a C.sub.2 -C.sub.7 alkylcarbonyl group, benzoyl group, benzoyl group substituted with 1-3 groups selected from halogen, C.sub.1 -C.sub.4 alkyl, and C.sub.1 -C.sub.4 alkoxy; Y represents C.sub.2 -C.sub.7 alkylcarbonyl group, C.sub.2 -C.sub.7 alkoxycarbonyl group or cyano group; and R represents di (C.sub.1 -C.sub.4 alkylamino) group, morpholino group or piperidino group, are produced by reacting glyoxal sodium bisulfite adduct with amine compounds in the presence of acids and then with dithiolates. The dithiolane derivatives can activate liver functions and are effective for treatment and prophylaxis of hepatitis and other hepatic disorders.
    Type: Grant
    Filed: August 22, 1989
    Date of Patent: August 20, 1991
    Assignee: Nihon Nohyaku Co., Ltd.
    Inventors: Shuhei Kubota, Kunikazu Hiraga, Keisuke Nakayama, Matazaemon Uchida
  • Patent number: 5021413
    Abstract: Analgesic compounds are of the general formula (I): ##STR1## in which, R.sup.1 and R.sup.2 each represents hydrogen or C.sub.1 -C.sub.6 alkyl, or R.sup.1 and R.sup.2 together with the nitrogen atom to which they are attached form a heterocycle; E represents methylene, sulfur, oxygen or imino group optionally substituted with C.sub.1 -C.sub.6 alkyl or aralkyl; ring A is aryl or heteroaryl ring, optionally substituted; R.sup.3 is hydrogen or C.sub.1 -C.sub.6 alkyl and R.sup.4 is hydrogen or R.sup.3 and R.sup.4 together represent a group of formula (IV):--(CR.sup.a R.sup.a).sub.m --C(.dbd.Y)-- (IV)(wherein R.sup.a and R.sup.a is C.sub.1 -C.sub.6 alkyl or hydrogen, up to a maximum of 3 alkyl groups, m is 1, 2, or 3, and Y is two hydrogens or oxygen); provided that when E represents a methylene group, then R.sup.3 is a C.sub.1 -C.sub.6 alkyl group or R.sup.3 and R.sup.4 together represent a group of the formula (IV).
    Type: Grant
    Filed: August 22, 1989
    Date of Patent: June 4, 1991
    Assignee: Sankyo Company Limited
    Inventors: Atsusuke Terada, Yoshio Iizuka, Kazuyuki Wachi, Kenji Fujibayashi
  • Patent number: 5011831
    Abstract: Quinolinecarboxylic acid derivatives of the formula (I) ##STR1## and pharmaceutically acceptable salts thereof wherein R.sup.1 is hydrogen, straight or branch chain lower alkyl or phenyl unsubstituted or substituted by one or more halo moieties; R.sup.2 is hydrogen or straight or branch chain lower alkyl; and ##STR2## is a 5- or 6-membered ring wherein the nitrogen atom is the only heteroatom or where there is a second heteroatom selected from the group consisting of nitrogen, oxygen and sulfur, said 5- or 6-membered ring being unsubstituted or substituted by lower alkyl, amino or mono- or di-lower alkyl amino are useful for treating bacterial infections in humans and animals.
    Type: Grant
    Filed: November 7, 1988
    Date of Patent: April 30, 1991
    Assignee: Nippon Shinyaku Co. Ltd.
    Inventors: Masahiro Kise, Masahiko Kitano, Masakuni Ozaki, Kenji Kazuno, Masahito Matsuda, Ichiro Shirahase, Yoshifumi Tomii
  • Patent number: 4996318
    Abstract: The amino-9,10-secosteroids ##STR1## of the present invention contain an amino group attached to the terminal carbon atom of the C.sub.17 -side chain and are useful as pharmaceutical agents for treating a number of conditions including spinal trauma, mild and/or moderate to severe head injury, etc.
    Type: Grant
    Filed: September 19, 1989
    Date of Patent: February 26, 1991
    Assignee: The Upjohn Company
    Inventors: Martin Gall, Robert I. Higuchi
  • Patent number: 4994570
    Abstract: Indicators for the detection of thio groups are disclosed together with processes for the preparation of such indicators.
    Type: Grant
    Filed: May 29, 1990
    Date of Patent: February 19, 1991
    Assignee: Miles Inc.
    Inventors: Holger Heidenreich, Klaus Wehling
  • Patent number: 4958023
    Abstract: There are provided gastric antiulcer and cytoprotective substituted N-phenyl-2-pyridinecarbothioamides. The process for their production and formulation is disclosed.
    Type: Grant
    Filed: June 29, 1989
    Date of Patent: September 18, 1990
    Assignee: American Home Products Corporation
    Inventors: William A. Kinney, Nancy E. Lee
  • Patent number: 4956359
    Abstract: Novel 3-aryloxy and 3-arylthioazetidinecarboxamides having utility in a method of treating convulsions and epilepsy and compositions therefor are disclosed having the formula: ##STR1## wherein Z is oxygen or sulfur; B is oxygen or sulfur; Ar is pyridyl or halo-substituted-pyridyl, phenyl or substituted phenyl; R.sup.1 and R.sup.2 are selected from hydrogen, loweralkyl, aryl, allyl, substituted allyl, propargyl, cycloalkyl, loweralkylcycloalkyl, cycloalkylloweralkyl, arylloweralkyl, diloweralkylaminoloweralkyl, and R.sup.1 and R.sup.2 when taken with the adjacent nitrogen atom may form a heterocyclic radical; R.sup.3 is hydrogen, loweralkyl, aryl or arylloweralkyl, and the geometrical isomers thereof, excepting that when R.sup.3 is hydrogen, Z is oxygen, B is oxygen, and Ar is phenyl or phenyl substituted by trifluoromethyl or aminocarbonyl, then R.sup.1 and R.sup.2 cannot be a combination of hydrogen and loweralkyl, and the further exception that when R.sup.
    Type: Grant
    Filed: October 22, 1986
    Date of Patent: September 11, 1990
    Assignee: A. H. Robins Company, Inc.
    Inventors: Chandler R. Taylor, Jr., Albert D. Cale, Jr., Harold F. Stauffer, Jr.
  • Patent number: 4925845
    Abstract: Gem 3 dialkyl or spiro 4 aryl or heteroaryl 5 heterocyclic 3 H indoles and their pharmaceutically acceptable salts are prepared. They are useful for reducing blood pressure producing a positive inotropic action influencing thrombocyte aggregation and improving microcirculation. Hydrazinophenyl heterocyclic intermeidates are also disclosed.
    Type: Grant
    Filed: February 24, 1988
    Date of Patent: May 15, 1990
    Assignee: Boehringer Mannheim GmbH
    Inventors: Alfred Mertens, Wolfgang von der Saal, Lothar Kling, Bernd Muller-Beckmann
  • Patent number: 4898941
    Abstract: A process for preparing a diphenylalkene derivative of the formula [II] ##STR1## which comprises oxidizing a diphenylalkanoic acid derivative of the formula [I] ##STR2## wherein R.sub.1 and R.sub.2 are each substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aralkyl or substituted or unsubstituted aryl, R.sub.1 and R.sub.2 may form a heteroring together theirwith or with an adjacent benzene ring, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8, R.sub.9, R.sub.10 and R.sub.11 are each hydrogen atom, halogen atom, substituted or unsubstituted alkyl, substituted or unsubstituted hydroxyl or substituted or unsubstituted amino, R.sub.12 and R.sub.13 are each hydrogen atom or substituted or unsubstituted alkyl, X is carboxyl, amide, ester or halide thereof.
    Type: Grant
    Filed: August 11, 1987
    Date of Patent: February 6, 1990
    Assignee: Kanzaki Paper Manufacturing Co., Ltd.
    Inventors: Nobuo Kanda, Haruo Omura, Yukihiro Abe, Mitsuru Kondo
  • Patent number: 4882328
    Abstract: Compounds of the formula ##STR1## and pharmaceutically acceptable salts thereof, R.sup.1 is hydrogen, alkyl or phenyl unsubstituted or substituted by one or two halo moieties, R.sup.2 is hydrogen or alkyl, A CX wherein X is halo, B is O or NR.sup.3 wherein R.sup.3 is hydrogen, alkyl, acyl, haloacyl, 2alkoxycarbonyl or (5-methyl-2-oxo-1,3-dioxolen-4-yl) methyl are useful for treating bacterial infections in humans and animals.
    Type: Grant
    Filed: September 22, 1988
    Date of Patent: November 21, 1989
    Assignee: Nippon Shinyaku Co. Ltd.
    Inventors: Masahiro Kise, Masakuni Ozaki, Kenji Kazuno, Yoshifumi Tomii, Jun Segawa, Shoji Yasufuki
  • Patent number: 4833139
    Abstract: There are disclosed compounds of the formula ##STR1## where R.sub.1 is loweralkoxycarbonyl, --CH.sub.2 OH or --CONR.sub.3 R.sub.4, R.sub.3 and R.sub.4 being independently hydrogen, loweralkyl or arylloweralkyl; and R.sub.2 is --CH.sub.2 CH.dbd.CH.sub.2, ##STR2## R.sub.5 and R.sub.6 being independently loweralkyl or alternatively the group -NR.sub.5 R.sub.6 as a whole being ##STR3## R.sub.7 being hydrogen, loweralkyl or arylloweralkyl; which are useful for enhancing cholinergic activity in mammals and hence for the treatment of various memory dysfunctions characterized by decreased cholinergic function such as Alzheimer's disease.
    Type: Grant
    Filed: July 5, 1988
    Date of Patent: May 23, 1989
    Assignee: Hoechst-Roussel Pharmaceuticals, Inc.
    Inventor: Lawrence L. Martin
  • Patent number: 4820842
    Abstract: The present invention provides a process for preparing a 5-cyano-2-substituted-1,4-dihydropyridine compound having cardiovascular activity.
    Type: Grant
    Filed: September 11, 1987
    Date of Patent: April 11, 1989
    Assignee: Warner-Lambert Company
    Inventors: Kevin R. Anderson, Ila Sircar
  • Patent number: 4814445
    Abstract: The present invention provides novel mitomycin analogs containing a disulfide group and processes for the preparation thereof. These compounds are mitomycin A analogs in which the 7-alkoxy group bears an organic substituent incorporating a disulfide group. Mitomycin A is an antibiotic of established utility, and the 7-O-substituted mitosane analogs thereof have similar utility.
    Type: Grant
    Filed: February 25, 1988
    Date of Patent: March 21, 1989
    Assignee: Bristol-Myers Company
    Inventors: Dolatrai M. Vyas, Terrence W. Doyle, Richard A. Partyka
  • Patent number: 4808750
    Abstract: Novel fluorophenoxyphenoxypropionates and derivatives thereof possess herbicidal activity selectively in the presence of broadleaf crops. Preemergent and postemergent applications are contemplated.
    Type: Grant
    Filed: July 14, 1986
    Date of Patent: February 28, 1989
    Assignee: The Dow Chemical Company
    Inventors: Richard B. Rogers, B. Clifford Gerwick, III
  • Patent number: 4772622
    Abstract: Novel diamino oxadiazoles, wherein one of the amine functions is connected to a basicly-substituted heterocyclic group through a linear or cyclic connecting group, which are useful for the suppression of gastric acid secretions in mammals. Compositions employing these compounds and processes for the preparation of such compounds from known N-cyano-S-methylisothiourea precursors by treatment with hydroxylamine and for alkylation of amine groups are also disclosed.
    Type: Grant
    Filed: June 16, 1986
    Date of Patent: September 20, 1988
    Assignee: Merck & Co., Inc.
    Inventors: Susan F. Britcher, William C. Lumma, Jr.
  • Patent number: 4758575
    Abstract: Novel substituted tetrahydro-, hexahydro- and octahydro-[3,4'-bi-2H-pyrrole]-2,2'-diones of the formula ##STR1## in which each of R.sub.1 and R.sub.
    Type: Grant
    Filed: June 25, 1987
    Date of Patent: July 19, 1988
    Assignee: Ciba-Geigy Corporation
    Inventor: Romeo Paioni
  • Patent number: 4757151
    Abstract: Certain 2-substituted-[2-substituted-amino]-N-arylalkyl-3-[indol-3-yl]propanamides demonstrate activity as appetite suppressants. The compounds, pharmaceutical compositions, and a method of suppressing appetite are disclosed.
    Type: Grant
    Filed: September 30, 1986
    Date of Patent: July 12, 1988
    Assignee: Warner-Lambert Company
    Inventor: David C. Horwell
  • Patent number: 4743595
    Abstract: A process for efficiently preparing 2-amino-5-nitrophenol derivatives in which benzoxazole derivatives are subjected to nucleophilic substitution reaction at the 5 position thereof to obtain corresponding benzoxazole derivatives, and the oxazole ring of the benzoxazole derivatives is then subjected to ring-opening to obtain 2-amino-5-nitrophenol derivatives. The 2-amino-5-nitrophenol derivatives are useful as industrial starting materials, reducing agents or antioxidants and intermediates for cyan-image-forming couplers.
    Type: Grant
    Filed: June 12, 1985
    Date of Patent: May 10, 1988
    Assignee: Fuji Photo Film Co., Ltd.
    Inventors: Isamu Itoh, Mitsunori Ono, Hidetoshi Kobayashi, Kazuyoshi Yamakawa
  • Patent number: 4707305
    Abstract: This invention provides a novel class of naphthoquinodimethane compositions. Illustrative of the invention is 11,11-di(n-hexyldecylamino)-12,12-dicyano-2,6-naphthoquinodimethane: ##STR1## An invention naphthoquinodimethane compound has utility as a nonlinear optical component in an electrooptic light modulator device.
    Type: Grant
    Filed: May 19, 1986
    Date of Patent: November 17, 1987
    Assignee: Celanese Corporation
    Inventors: Eui W. Choe, Alan Buckley, Anthony F. Garito
  • Patent number: 4689414
    Abstract: Cardiovascular activity is exhibited by compounds having the formula ##STR1## and pharmaceutically acceptable salts thereof, wherein R.sub.1 is alkyl, cycloalkyl, aryl, heterocyclo, --(CH.sub.2).sub.n --Y.sub.2, --(CH.sub.2).sub.p --Y.sub.3 or halo substituted alkyl;R.sub.2 is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, --(CH.sub.2).sub.n --Y.sub.1, or halo substituted alkyl;R.sub.3 is hydrogen, alkyl, cycloalkyl, aryl, heterocyclo, --(CH.sub.2).sub.n --Y.sub.2, --(CH.sub.2).sub.p --Y.sub.3, or halo substituted alkyl;R.sub.4 is aryl or heterocyclo;R.sub.5 is hydrogen, alkyl, aryl, arylalkyl, cyano, nitro, ##STR2## Y.sub.1 is cycloalkyl, aryl, heterocyclo, hydroxyl, alkoxy, aryl-(CH.sub.2).sub.m --O--, mercapto, alkylthio, aryl-(CH.sub.2).sub.m --S--, amino, substituted amino, carbamoyl, ##STR3## Y.sub.2 is cycloalkyl, aryl, heterocyclo, carbamoyl, ##STR4## amino, or substituted amino; m is 0 or an integer of 1 to 6;n is an integer of 1 to 6; andp is an integer of 2 to 6.
    Type: Grant
    Filed: February 24, 1986
    Date of Patent: August 25, 1987
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Karnail Atwal
  • Patent number: 4684656
    Abstract: Cardiovascular activity is exhibited by compounds having the formula ##STR1## and pharmaceutically acceptable salts thereof wherein X is oxygen or sulfur;R.sub.1 is alkyl, cycloalkyl, aryl, heterocyclo, --(CH.sub.2).sub.n --Y.sub.1, or halo substituted alkyl;R.sub.2 is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, --(CH.sub.2).sub.n --Y.sub.1, or halo substituted alkyl;R.sub.3 is hydrogen, alkyl, cycloalkyl, aryl, heterocyclo, --(CH.sub.2).sub.n --Y.sub.2, --(CH.sub.2).sub.p --Y.sub.3, or halo substituted alkyl;R.sub.4 is aryl or heterocyclo;Y.sub.1 is cycloalkyl, aryl, heterocyclo, hydroxyl, alkoxy, aryl--(CH.sub.2).sub.m --O--, mercapto, alkylthio, aryl--(CH.sub.2).sub.m --S--, amino, substituted amino, carbamoyl, ##STR2## Y.sub.2 is cycloalkyl, aryl, heterocyclo, carbamoyl, ##STR3## Y.sub.3 is hydroxyl, alkoxy, aryl--(CH.sub.2).sub.m --O--, mercapto, alkylthio, aryl--(CH.sub.2).sub.
    Type: Grant
    Filed: March 14, 1986
    Date of Patent: August 4, 1987
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Karnail Atwal
  • Patent number: 4684644
    Abstract: The present invention is directed to a class of basic monocarboxyamide derivatives of actagardine. Actagardine (INN) is an antibiotic substance produced by actinoplanes strains such as Actinoplanes Sp. ATCC 31048 and Actinoplanes Sp. ATCC 31049 which are described in U.S. Pat. No. 4,022,884. Actagardine shows antimicrobial in vitro and in vivo activity against gram-positive organisms. Its complete chemical structure is not yet known but there is only information on its chemical functions and main fragments. In particular, it has been found that actagardine has two carboxylic functions and a primary amino function and can therefore be represented as follows: ##STR1## The compounds of the invention are monoamide derivatives at one of the carboxy functions of actagardine.
    Type: Grant
    Filed: March 21, 1986
    Date of Patent: August 4, 1987
    Assignee: Gruppo Lepetit S.p.A.
    Inventors: Adriano Malabarba, Bruno Cavalleri
  • Patent number: 4683228
    Abstract: A guanidine derivative of the formula I: ##STR1## in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, ring X and D are a variety of radicals defined in the specification and A is a 3-8C alkylene chain which is substituted by a hydroxy radical and into which is optionally inserted, as part of the backbone of the chain, one or two groups selected from oxygen and sulphur atoms and NH and 1-6C N-alkyl radicals; and the pharmaceutically-acceptable acid additions salts thereof. Pharmaceutical compositions and methods of manufacture are also described. The compound of the formula I is a histamine H-2 antagonist and is therefore useful in ulcer therapy.
    Type: Grant
    Filed: January 22, 1985
    Date of Patent: July 28, 1987
    Assignees: ICI Americas Inc., Imperial Chemical Industries PLC
    Inventors: Karin M. Kirkland, Derrick M. Mant
  • Patent number: 4670592
    Abstract: A bisbiguanide compound of the formula:R.sup.1 R.sup.2 N.C(:NR.sup.6)NH.C(:NH)NH.CH.sub.2 X-- --(CH.sub.2).sub.3 NH.C(:NH)NH.C(:NR.sup.7)NR.sup.3 R.sup.4 Vor a tautomer thereof, wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 which may be the same or different, are each hydrogen, a 1-16C alkyl radical, a 2-16C alkoxyalkyl radical, a 3-12C cycloalkyl radical, a (3-12C cycloalkyl)-(1-4C alkyl) radical, or an optionally substituted phenyl or phenyl(1-4C alkyl) radical, or R.sup.1 and R.sup.2 and the nitrogen atom to which they are attached, or R.sup.3 and R.sup.4 and the nitrogen atom to which they are attached, which may be the same or different, are each a 1-azetidinyl, 1-pyrrolidinyl, piperidino, hexamethyleneimino, heptamethyleneimino, morpholino or 4-(1-8C alkanoyl)-1-piperazinyl radical each of which may bear 1-3C alkyl substituents; each of R.sup.6 and R.sup.7, which may be the same or different, is hydrogen or a 1-8C alkyl radical; and X is a substituted ethylene or ethylidene radical of the formula:--CH.
    Type: Grant
    Filed: May 7, 1984
    Date of Patent: June 2, 1987
    Assignee: Imperial Chemical Industries PLC
    Inventors: Murdoch A. Eakin, Philip N. Edwards, Michael S. Large
  • Patent number: 4663453
    Abstract: The invention relates to benzopyrrolobenzodiazepines and quinobenzodiazepines of the formula ##STR1## where X and Y may be the same or different and each is hydrogen, halogen, CF.sub.3, lower alkyl, lower alkoxy, lower alkylthio and lower alkylsulfonyl, p and q are independently 1 or 2; R.sub.1 is hydrogen when R.sub.2 is bonded to R.sub.3 to form a --(CH.sub.2).sub.m --CH.sub.2 -- group or a --CH.dbd.CH-- group; R.sub.3 is hydrogen when R.sub.1 is bonded to R.sub.2 to form a --(CH.sub.2).sub.m --CH.sub.2 -- group or a --CH.dbd.CH-- group; m is 1 or 2; R.sub.4 is NR.sub.5 R.sub.6 wherein R.sub.5 is hydrogen or lower alkyl and R.sub.6 is hydrogen, lower alkyl or a group of the formula (CH.sub.2).sub.n NR.sub.7 R.sub.8 wherein R.sub.7 and R.sub.8 are lower alkyl, and n is 2 or 3, ##STR2## wherein R.sub.9 is lower alkyl, ##STR3## wherein R.sub.10 is CH.sub.2 CH.sub.2 OH, lower alkyl, phenyl, phenyl substituted by halogen, CF.sub.
    Type: Grant
    Filed: August 28, 1985
    Date of Patent: May 5, 1987
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Edward J. Glamkowski, Yulin Chiang
  • Patent number: 4659721
    Abstract: Alkanol derivatives corresponding to the general formula IR.sup.1 R.sup.2 N--(CH.sub.2).sub.m --Q--CH.sub.2 X--CH.sub.2 --Y--(CH.sub.2).sub.n --NHR.sup.3 (I)which have a highly selective action on histamine-H.sub.2 receptors are described. Due to this action, these compounds may advantageously be used for treatment of diseases caused by raised gastric secretion.
    Type: Grant
    Filed: January 22, 1985
    Date of Patent: April 21, 1987
    Assignee: Ludwig Heumann & Co. GmbH
    Inventors: Helmut Schickaneder, Stefan Postius, Istvan Szelenyi, Peter Morsdorf, Rolf Herter, Kurt H. Ahrens
  • Patent number: 4656180
    Abstract: Diamine derivatives corresponding to the general formula IR.sup.1 R.sup.2 N--(CH.sub.2).sub.m --Q--A--NH--R--NH--B--Q'--(CH.sub.2).sub.n NR.sup.3 R.sup.4 (I)which have a highly selective action on histamine-H.sub.2 receptors and are therefore suitable for use as anti-ulcerative agents are described. Processes for the preparation of these compounds and pharmaceutical preparations containing these compounds are also described.
    Type: Grant
    Filed: March 5, 1985
    Date of Patent: April 7, 1987
    Assignee: Ludwig Heumann & Co., GmbH
    Inventors: Stefan Postius, Rolf Herter, Peter Morsdorf, Helmut Schickaneder, Istvan Szelenyi, Kurt H. Ahrens
  • Patent number: 4647561
    Abstract: Compounds of formula ##STR1## wherein R.sub.4 is aryl or heterocyclo are disclosed. These compounds are useful as cardiovascular agents and especially as anti-hypertensive agents.
    Type: Grant
    Filed: August 5, 1985
    Date of Patent: March 3, 1987
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Karnail Atwal
  • Patent number: 4647675
    Abstract: Novel compounds of the general formula I ##STR1## where A.sup..crclbar. is an anion, R is hydrogen or unsubstituted or substituted alkyl or cycloalkyl, R.sup.1 and R.sup.2 independently of one another are each hydrogen or unsubstituted or substituted alkyl or cycloalkyl, or one of the radicals may furthermore be aryl, or R.sup.1 and R.sup.2, together with the nitrogen atom, form a saturated heterocyclic structure, the radicals R.sup.3 independently of one another are each hydrogen or C.sub.1 -C.sub.4 -alkyl, R.sup.4 and R.sup.5 independently of one another are each unsubstituted or substituted alkyl or cycloalkyl, or one of the radicals may furthermore be hydrogen, aryl or hetaryl, R.sup.4 and R.sup.5, together with the nitrogen atom, form a saturated heterocyclic structure, n is 1, 2 or 3, X is hydrogen, chlorine, bromine, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy or nitro and Y is hydrogen or chlorine, are particularly useful for dyeing paper stocks.
    Type: Grant
    Filed: July 11, 1985
    Date of Patent: March 3, 1987
    Assignee: BASF Aktiengesellschaft
    Inventors: Udo Mayer, Andreas Oberlinner
  • Patent number: 4608435
    Abstract: New benzo-1,4-quinones and salts thereof with organic or inorganic acid and bases have the formula I ##STR1## wherein p is 1 or 2 and q is 0 or 1, provided that p+q is 1 or 2, R is a residue of formula II ##STR2## wherein Q is selected from the residues --CO.sub.2 R.sub.4, --CON(R.sub.4)(R.sub.5), --OR.sub.5, --OCOR.sub.7, --N(R.sub.8)(R.sub.9), --PO(OR.sub.10)([O].sub.x R.sub.11), --SO.sub.2 R.sub.12, --CN, Halogen, --NO.sub.2 or --COR.sub.13, n is an integer from 1 to 20, k is 1 or 2 and x is 0 or 1, and R.sub.1 to R.sub.5 and R.sub.7 to R.sub.13 are as defined in the specification.The compounds of formula I are useful in photographic materials such as bleaching inhibitors in films of photographic silver dye bleach materials.
    Type: Grant
    Filed: April 28, 1983
    Date of Patent: August 26, 1986
    Assignee: Ciba-Geigy AG
    Inventor: Frederick H. Howell
  • Patent number: 4602087
    Abstract: The distyrylbiphenyls of the formula ##STR1## in which X and X' independently of one another are a direct bond, oxygen, sulfur, --O--C.sub.1-3 -alkylene-CON(R.sub.4)--CON(R.sub.4)--, --O--C.sub.1-3 alkylene-COO--, OCO or --COO--, with the proviso that if n+n'=O, X and X' may not be --CON(R.sub.4)-- or O--C.sub.1-3 -alkylene-CON(R.sub.4)--, and if n+n'=2 and X and X' are --CON(R.sub.4)-- or --COO--, A.sup..crclbar. may not be a phosphite or phosphonate anion, and Y and Y' independently of one another are C.sub.1-20 -alkyene, R.sub.1 and R.sub.1 ' independently of one another are unsubstituted or substituted C.sub.1-8 -alkyl or C.sub.3-4 -alkenyl, R.sub.1 together with R.sub.2, or R.sub.1 ' together with R.sub.2 ', is a heterocyclic ring, R.sub.2 and R.sub.2 ' independently of one another are unsubstituted or substituted C.sub.1-8 -alkyl or C.sub.3-4 -alkenyl, or R.sub.2 together with R.sub.1, or R.sub.2 ' together with R.sub.1 ', is a heterocyclic ring, or R.sub.1 and R.sub.2, or R.sub.1 ' and R.sub.
    Type: Grant
    Filed: May 18, 1984
    Date of Patent: July 22, 1986
    Assignee: Ciba-Geigy Corporation
    Inventors: Christian Luthi, Hans R. Meyer, Kurt Weber
  • Patent number: 4595539
    Abstract: Certain 2-substituted-2-penem-3-carboxylic acid compounds and pharmaceutically-acceptable salts thereof can be prepared from the appropriate xanthate or trithiocarbonate by desulfurization and addition of an electrophilic sulfur compound followed by halogenation and ring closure. The corresponding desulfurized and halogenated olefinic intermediates are disclosed.
    Type: Grant
    Filed: June 10, 1983
    Date of Patent: June 17, 1986
    Assignee: Pfizer Inc.
    Inventor: Ernest S. Hamanaka
  • Patent number: 4587048
    Abstract: The present invention relates to a novel process for the manufacture of 4-thioazetidinone compounds of the formula ##STR1## in which R.sub.1.sup.a represents an amino-protecting group and R.sub.1.sup.b represents hydrogen or an acyl radical Ac, or in which R.sub.1.sup.a and R.sub.1.sup.b together represent a bivalent acyl radical, R.sub.2.sup.A represents an etherified hydroxy group, R.sub.3 represents methyl, hydroxy, etherified or esterified hydroxy, cyano, tertiary amino or nitro, X represents hydrogen or halogen, and Y represents a group --SR.sub.4 or --SO.sub.2 --R.sub.5 in which R.sub.4 represents an optionally substituted heteroaryl radical or the acyl radical of an organic carboxylic or thiocarboxylic acid and R.sub.5 represents an optionally substituted hydrocarbon radical, or, when R.sub.3 represents hydroxy or methyl, tautomers thereof. Compounds of the formula I are manufactured by reacting compounds of the formula III with a nitrosating agent and a compound of the formula IV.
    Type: Grant
    Filed: April 20, 1984
    Date of Patent: May 6, 1986
    Assignee: Ciba-Geigy Corporation
    Inventor: Gottfried Sedelmeier
  • Patent number: 4576749
    Abstract: Antibacterial activity is exhibited by 2-azetidinones having a 3-acylamino substituent and a 1-substituent of the formula ##STR1## (or a salt or ester thereof).
    Type: Grant
    Filed: April 13, 1984
    Date of Patent: March 18, 1986
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Robert Zahler, William H. Koster, William A. Slusarchyk
  • Patent number: 4562201
    Abstract: The present invention relates to new compounds of the formula ##STR1## where X is ##STR2## alkylene, or --S-- where R.sub.1 is hydrogen, alkyl, or aryl; W is hydrogen, hydroxy, amino, alkyloxy, aryloxy, O-alkyl, or O-aralkyl; (Y).sub.A is --CH.sub.2 NR.sub.2 R.sub.3 where R.sub.2 and R.sub.3 may be hydrogen, substituted alkyls, aryls, or together with N form a 5 to 7 membered heterocyclic group; and Ar is a substituted or unsubstituted aryl. These compounds are useful in the treatment of various cardiac arrhythmias.
    Type: Grant
    Filed: July 26, 1982
    Date of Patent: December 31, 1985
    Assignee: American Hospital Supply Corporation
    Inventors: David M. Stout, William L. Matier
  • Patent number: 4533497
    Abstract: N-ethylidene azetidinones are new antibiotic compounds. They are produced from the reaction of a Grignard reagent with a cephalosporin substituted at the 3 position with a chloro, oxy, amino or sulfide moieties.
    Type: Grant
    Filed: December 27, 1982
    Date of Patent: August 6, 1985
    Assignee: Eli Lilly and Company
    Inventor: Douglas O. Spry
  • Patent number: 4532348
    Abstract: 1-(Substituted phenylthiocarbamyl) 3,3-disubstituted formamidine compounds having the structural formula ##STR1## wherein n is 1, 2 or 3,R is alkyl having 1 to 6 carbon atoms, alkoxy having 1 to 6 carbon atoms, alkylthio having 1 to 4 carbon atoms, halogen, nitro, acyl having 1 to 4 carbon atoms, hydroxyl and ##STR2## wherein R.sup.3 and R.sup.4 have the same meaning as R.sup.1 and R.sup.2 defined below,R.sup.1 and R.sup.2 are the same or different and are alkyl having 1 to 6 carbon atoms, or taken together represent the chain --(CH.sub.2).sub.p --(X).sub.m --(CH.sub.2).sub.q and forming a ring structure with the nitrogen to which they are bound wherein p is 1, 2 or 3, q is 2 or 3, X represents --O--, --S--, --SO--, --SO.sub.2 --, --NR.sup.3 --, R.sup.3 is hydrogen or alkyl having 1 to 6 carbon atoms, and m is 0 or 1 and their use as pharmaceutical agents.
    Type: Grant
    Filed: July 16, 1980
    Date of Patent: July 30, 1985
    Assignee: Stauffer Chemical Company
    Inventors: Ferenc M. Pallos, Jack R. DeBaun, Eugene G. Teach
  • Patent number: 4528379
    Abstract: In a process for the preparation of a substituted thiadiazolyloxyacetamide of the formula ##STR1## in which R.sup.1 and R.sup.2 each independently is hydrogen, alkyl, alkenyl, alkenyl, alkinyl, optionally substituted cycloalkyl or cycloalkenyl, halogenoalkyl, alkoxyalkyl, alkoxy, aralkyl or optionally substituted aryl, orR.sup.1 and R.sup.2, together with the nitrogen atom to which they are bonded, form an optionally substituted heterocyclic structure which can contain further hetero atoms,One of X and Y is a nitrogen atom and the other a C-R.sup.3 a grouping, andR.sup.
    Type: Grant
    Filed: July 18, 1983
    Date of Patent: July 9, 1985
    Assignee: Bayer Aktiengesellschaft
    Inventors: Reimer Colln, Karl H. Mohrmann
  • Patent number: 4504663
    Abstract: The present invention concerns novel heterocyclic aminoalcoyl derivatives having the formula: ##STR1## wherein n=1, 2 or 3; A represents a nitrogen atom or the CH group, X=CH.sub.2 or CH.sub.2 O; R represents a phenyl nucleus possibly substituted; NR.sub.1 R.sub.2 =amino, methylamino, N,N-dialkylamino or an heterocyclic radical; and R.sub.3 =H, halogen, alkyl, alkyloxy or methoxy.These derivatives are useful as drugs, especially as analgesics and antidepressants.
    Type: Grant
    Filed: November 15, 1983
    Date of Patent: March 12, 1985
    Assignee: Delalande S.A.
    Inventors: Gerard H. Moinet, Philippe L. Dostert, Guy R. Bourgery
  • Patent number: 4478598
    Abstract: The amphoteric styrene derivatives correspond to the formula ##STR1## in which X is oxygen, sulfur, a direct bond, --SO.sub.2 N(R.sub.5 --, --CON(R.sub.5 -- or --COO--, Y.sub.1 and Y.sub.2 independently of one another are C.sub.1 -C.sub.4 -alkylene or hydroxypropylene, R.sub.1 and R.sub.2 independently of one another are C.sub.1 -C.sub.4 -alkyl or, together with the N atom, are a pyrrolidine, piperidine, hexamethyleneimine or morpholine ring, and R.sub.1, together with R.sub.5, is also a piperazine ring, R.sub.3 and R.sub.4 are hydrogen, C.sub.1-4 -alkyl, chlorine, C.sub.1-4 -alkoxy or C.sub.3-4 -alkenyl or together, in the o-position relative to one another, are a trimethylene or tetramethylene group, R.sub.5 is hydrogen, C.sub.1-4 -alkyl or cyanoethyl or, together with R.sub.1, is a piperazine ring, Q is --COO or --SO.sub.3 and n is the number 1 or 2, and can be prepared by reacting the corresponding amine compounds with a halide of the formula Hal--Y.sub.
    Type: Grant
    Filed: February 22, 1982
    Date of Patent: October 23, 1984
    Assignee: Ciba-Geigy Corporation
    Inventors: Hans R. Meyer, Max Morf
  • Patent number: 4469687
    Abstract: The invention relates to new chemical compounds corresponding to the following formula ##STR1## in which R is a non-hydrolyzable radical and Az represents aziridinyl ##STR2## These compounds may be used as medicaments.
    Type: Grant
    Filed: September 9, 1981
    Date of Patent: September 4, 1984
    Assignee: Agence Nationale de Valorisation de la Recherche
    Inventors: Jean-Francois Labarre, Francois Sournies, Johan C. van de Grampel, Adriaan A. Van Der Huizen
  • Patent number: 4463001
    Abstract: The present invention relates to new 6-substituted 6H-dibenzo [b,d]pyran derivatives, to a process for their preparation and pharmaceutical and veterinary compositions containing them.
    Type: Grant
    Filed: October 1, 1981
    Date of Patent: July 31, 1984
    Assignee: Farmitalia Carlo Erba S.p.A.
    Inventors: Piero Melloni, Paolo Salvadori, Pier P. Lovisolo
  • Patent number: 4431851
    Abstract: The present invention concerns compounds of the formula ##STR1## wherein n=1, 2 or 3; and R' represents phenyl or orthofluorophenyl. Said compounds are used as intermediates in the preparation of heterocyclic aminoalkyl derivatives which are useful as analgesics and antidepressants.
    Type: Grant
    Filed: March 8, 1983
    Date of Patent: February 14, 1984
    Assignee: Delalande S.A.
    Inventors: Gerard H. Moinet, Philippe L. Dostert, Guy R. Bourgery