Chalcogen Bonded Directly To The Oxazine Ring Patents (Class 544/92)
  • Patent number: 4446319
    Abstract: Novel aminocyclitols, namely the compounds of the formula ##STR1## wherein X is hydroxyl group, a halogen or an acyloxy group; Y is hydrogen or a halogen; and OR.sup.1 is an optionally protected hydroxyl group; and their production.These aminocyclitols are important intermediates for preparing valiolamine having .alpha.-glucosidase inhibitory activity.
    Type: Grant
    Filed: April 26, 1982
    Date of Patent: May 1, 1984
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Satoshi Horii, Hiroshi Fukase
  • Patent number: 4443598
    Abstract: Intermediates for preparing an antibacterial 1-dethia-1-oxacephalosporins which are represented by the following formula: ##STR1## wherein R is a monovalent group (minus the carbonyl) from an acyl derived from a carboxylic or carbonic acid;Y.sup.1 is a divalent group of the following formula: ##STR2## wherein COB is carboxy or protected carboxy;X is hydrogen or a nucleophilic group; andZ is a leaving groupare prepared from a compound of the following formula: ##STR3## wherein R and Y.sup.1 are as defined above by the action of an acid. The new compounds of this invention shown by the following formula: ##STR4## wherein A is amino or substituted amino;E is hydrogen or methoxy; andY is a divalent group of the following formula: ##STR5## in which COB, X, and Z are as defined above are convertible into other compounds of the same formula by applying conventional methods in .beta.-lactam chemistry.
    Type: Grant
    Filed: May 4, 1982
    Date of Patent: April 17, 1984
    Assignee: Shionogi & Co., Ltd.
    Inventors: Mitsuru Yoshioka, Uyeo Shoichiro, Yoshio Hamashima, Ikuo Kikkawa, Teruji Tsuji, Wataru Nagata
  • Patent number: 4363651
    Abstract: 4H-3,1-Benzoxazine derivatives of the formula ##STR1## where R.sup.1, R.sup.2 and Y have the meanings given in the description, and their use for controlling undesired plant growth.
    Type: Grant
    Filed: September 25, 1981
    Date of Patent: December 14, 1982
    Assignee: BASF Aktiengesellschaft
    Inventors: Gerhard Hamprecht, Bruno Wuerzer
  • Patent number: 4344945
    Abstract: New piperidine derivatives which have a useful pharmacological activity such as hypotensive activity are prepared.
    Type: Grant
    Filed: March 9, 1981
    Date of Patent: August 17, 1982
    Assignee: Kyowa Hakko Kogyo Co., Ltd.
    Inventors: Masayuki Teranishi, Hiroyuki Obase, Haruki Takai, Kazuhiro Kubo, Yutaka Kasuya
  • Patent number: 4341778
    Abstract: The invention relates to compounds of general formula I ##STR1## (wherein R.sub.1 and R.sub.2, which may be the same or different, each represents a hydrogen atom or a (C.sub.1 -C.sub.4) alkyl group;R.sub.3 and R.sub.4, which may be the same or different, each represents a hydrogen, fluorine or chlorine atom or a hydroxy, methyl, ethyl or (C.sub.1 -C.sub.4) alkoxy group, or R.sub.3 together with R.sub.4 represents a methylenedioxy group;R.sub.5 and R.sub.6, which may be the same or different, each represents a hydrogen atom or a methyl group;R.sub.7 represents a group of formula ##STR2## R represents a hydrogen atom or a (C.sub.1 -C.sub.4) alkyl group; R.sub.8 represents a fluorine or chlorine atom or a (C.sub.1 -C.sub.4) alkyl, (C.sub.1 -C.sub.4) alkylthio, hydroxymethyl, CONHR.sub.11, SO.sub.2 NHR.sub.11, OR.sub.12, methoxycarbonyl, ethoxycarbonyl or NHSO.sub.2 CH.sub.3 group;R.sub.9 represents a hydrogen, fluorine or chlorine atom or a OR.sub.12 group;R.sub.
    Type: Grant
    Filed: July 6, 1981
    Date of Patent: July 27, 1982
    Assignee: C. H. Boehringer Sohn
    Inventors: Anton Mentrup, Kurt Schromm, Ernst-Otto Renth, Wolfgang Hoefke, Wolfram Gaida, Ilse Streller, Armin Fugner
  • Patent number: 4321371
    Abstract: Substituted N-benzoylanthranilic acid derivatives of the formula I ##STR1## and their anhydro compounds, of the formula II ##STR2## where R.sup.1 is substituted phenyl,R.sup.2 is hydrogen, nitro, cyano or halogen,X is hydrogen, halogen, nitro or cyano, or is alkyl, haloalkyl, alkoxy, haloalkoxy, haloalkylmercapto or alkylmercapto, each of 1 to 4 carbon atoms, andY is --OR.sup.6 or ##STR3## where R.sup.6 is hydrogen, or is alkyl, alkenyl or alkynyl each of up to 4 carbon atoms, or is one equivalent of an alkaline earth metal cation, of an alkali metal cation or of an ammonium ion which is unsubstituted or is substituted by alkyls of 1 to 4 carbon atoms, andR.sup.7 and R.sup.8 independently of one another are hydrogen or alkyl of 1 to 4 carbon atoms, herbicides containing these compounds, and processes for controlling undesired plant growth by means of these compounds.
    Type: Grant
    Filed: August 15, 1980
    Date of Patent: March 23, 1982
    Assignee: BASF Aktiengesellschaft
    Inventors: Adolf Parg, Bruno Wuerzer, Gerhard Hamprecht
  • Patent number: 4315766
    Abstract: 4H-3,1-Benzoxazine derivatives of the formula ##STR1## where R.sup.1, R.sup.2 and Y have the meanings given in the specification, and their use for controlling unwanted plant growth in numerous crops, such as cereals, Indian corn, soybeans and cotton.
    Type: Grant
    Filed: April 8, 1980
    Date of Patent: February 16, 1982
    Assignee: BASF Aktiengesellschaft
    Inventors: Gerhard Hamprecht, Bruno Wuerzer
  • Patent number: 4314078
    Abstract: Preparation of a compound of the following formula (I): ##STR1## wherein R.sup.1 is alkyl of 1 to 12 carbons, from the compound of the following formula (II): ##STR2## by the steps of coupling (II) with 3,4-dichlorobenzotrifluoride; reacting the --NH.sub.2 and COOH groups with a COX.sub.2 compound, X being a leaving group, to produce a heterocycle; opening the heterocycle with an alkanesulphonamide; and oxidizing the resultant --NH.sub.2 group to an --NO.sub.2 to yield a compound of formula (I). Novel intermediates are also described. Compounds of formula (I) are useful as selective pre- and post-emergent herbicides.
    Type: Grant
    Filed: April 2, 1981
    Date of Patent: February 2, 1982
    Assignee: ICI Americas Inc.
    Inventors: Walter M. Kruse, John F. Stephen
  • Patent number: 4313000
    Abstract: The invention comprises the preparation of a compound of the following formula (I): ##STR1## wherein R.sup.1 is alkyl of 1 to 12 carbons, from the compound of the following formula (II): ##STR2## by the steps of coupling (II) with 3,4-dichlorobenzotrifluoride; reacting the --NH.sub.2 group with an XCOOR compound, X being a leaving group with R an organic moiety; oxidizing the --CH.sub.3 group to a --COOH group; cyclization to produce a heterocycle with loss --OR; opening the heterocycle with an alkanesulphonamide; and oxidizing the resultant --NH.sub.2 group to an NO.sub.2 to yield a compound of formula (I). Novel intermediates are also described. Compounds of formula (I) are useful as selective pre- and post-emergent herbicides.
    Type: Grant
    Filed: April 2, 1981
    Date of Patent: January 26, 1982
    Assignee: ICI Americas Inc.
    Inventors: Walter M. Kruse, John F. Stephen
  • Patent number: 4301283
    Abstract: A process for preparing 2-oxo-dihydrobenzo[d][1,3]oxazines (also named 1,4-dihydro-2H-3,1-benzoxazin-2-ones) which process comprises treating a suspension or solution of a 2-carbamoyl-benzyl alcohol in a substantially water-immiscible organic medium with aqueous alkaline hypochlorite or hypobromite having a pH of at least 11 in the presence of a phase transfer catalyst; and conversion of the 2-oxo-dihydrobenzo[d][1,3]oxazines to corresponding 2-amino-benzyl alcohols which are useful as intermediates in the production of dyes, pharmaceuticals and herbicides.
    Type: Grant
    Filed: September 10, 1980
    Date of Patent: November 17, 1981
    Assignee: Sterling Drug Inc.
    Inventors: John G. Thorpe, Peter G. Urben
  • Patent number: 4295875
    Abstract: New tetrahydro-1,3-oxazines of the formula ##STR1## where R denotes linear or branched haloalkyl of up to 3 carbon atoms, R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are identical or different and each denotes hydrogen or linear or branched alkyl of up to 3 carbon atoms, R.sup.6 denotes hydrogen or linear or branched alkyl of up to 8 carbon atoms, R.sup.7 denotes hyrogen, linear or branched alkyl of up to 8 carbon atoms, alkoxyalkyl of up to 6 carbon atoms or dialkoxyalkyl of up to 8 carbon atoms, and R.sup.6 and R.sup.7 may together form a methylene chain of 4 or 5 carbon atoms.The compounds are antagonistic agents and, as such, increase the tolerance of herbicidal acetanilides by crop plants. Herbicidal agents containing the tetrahydro-1,3-oxazines in combination with haloacetanilides are suitable for combating unwanted plant growth in Indian corn and cereal crops.
    Type: Grant
    Filed: March 24, 1980
    Date of Patent: October 20, 1981
    Assignee: BASF Aktiengesellschaft
    Inventors: Karl Eicken, Wolfgang Rohr, Hans J. Pander, Bruno Wuerzer
  • Patent number: 4293495
    Abstract: 4R,4'R bis[1-(2-N-3-methyl-4-al-Z-but-2-ene-oate)-2-oxo-3S-acylamino azetidine]disulfide compounds are prepared by reacting the corresponding 7.alpha.-acylamino-2.alpha.-alkoxy-3-methyl-3-cephem-4-carboxylates first with an N-chloro halogenating agent, e.g., N-chlorosuccinimide, then with an aqueous suspension of mercury dichloride and cadmium carbonate. The disulfide compounds produced in this invention are intermediates in the synthesis of the biologically active 7.beta.-acylamino-7.alpha.-alkoxy-3-methyl 1-oxa .beta.-lactam antibiotic compounds.
    Type: Grant
    Filed: April 7, 1980
    Date of Patent: October 6, 1981
    Assignee: Eli Lilly and Company
    Inventors: Stjepan Kukolja, Janice L. Pfeil
  • Patent number: 4293493
    Abstract: Azetidinone alcohol disulfides are synthesized by reduction of the corresponding aldehydes. The azetidinone alcohol disulfides are the substrates for a process which cyclizes these compounds to 1-oxa .beta.-lactam compounds, employing a cyclizing reagent chosen from the class consisting of divalent mercury salts or trivalent phosphine compounds. The 1-oxa .beta.-lactam compounds produced by this process are intermediates in the synthesis of 1-oxa .beta.-lactam antibiotics.
    Type: Grant
    Filed: April 7, 1980
    Date of Patent: October 6, 1981
    Assignee: Eli Lilly and Company
    Inventors: Stjepan Kukolja, Janice L. Pfeil
  • Patent number: 4279823
    Abstract: Simple arenes, aryl alcohols, aryl acids and aryl amides are reacted with an electrophilic thallium salt to provide arylthallium intermediates; and thereafter, the arylthallium compound is directly carbonylated by reacting with carbon monoxide in the presence of a noble metal carbonylation catalyst, such as palladium halide salts. The carbonylation reaction provides an excellent yield at room temperature and atmospheric pressure and is catalytic with respect to the noble metal salt.
    Type: Grant
    Filed: December 11, 1979
    Date of Patent: July 21, 1981
    Assignee: Iowa State University Research Foundation, Inc.
    Inventor: Richard C. Larock
  • Patent number: 4276295
    Abstract: Novel 3-aromatic moiety substituted-4(3H)-quinazolinone derivatives useful as a vasodilators, hypotensive and antiatherosclerotic agents having the formula of ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4 and Q are as defined in the accompanying specification or its acid addition salt; and a process for producing the same.
    Type: Grant
    Filed: December 14, 1979
    Date of Patent: June 30, 1981
    Assignee: Masayuki Ishikawa
    Inventors: Masayuki Ishikawa, Hiromichi Tanaka, Yukuo Eguchi, Shigeru Ito, Yoshimi Takashima, Masahiko Kobayashi
  • Patent number: 4268510
    Abstract: The invention relates to novel heterocyclic trichloromethyl derivatives, particularly 2-trichloromethyl-substituted quinazoline, benzo[d]-[1,3]-oxazine and benzo[e]-[1,3]-oxazine derivatives, for example 1,2-dihydro-2-trichloromethylquinazolin-4-one. The compounds of the invention are at least as effective as prior art trichloromethyl derivatives, which reduce the production of methane during the rumen metabolism of ruminant animals, and increase the formation of propionate at the expense of acetate, and hence improve the animals' rate of growth and their efficiency of food utilization.
    Type: Grant
    Filed: August 28, 1979
    Date of Patent: May 19, 1981
    Assignee: Imperial Chemical Industries Limited
    Inventors: Francis T. Boyle, Michael A. Taylor
  • Patent number: 4264597
    Abstract: Compounds of the formula ##STR1## wherein X is --O--or --S--;R.sup.1 is amino or a substituted amino group;R.sup.2 is carboxy or a protected carboxy group; and the heavy solid line means single or double bond; the compounds are useful in the treatment of infectious diseases particularly fungal infection, in human beings and animals.
    Type: Grant
    Filed: May 30, 1979
    Date of Patent: April 28, 1981
    Inventors: Masashi Hashimoto, Keiji Hemmi, Matsuhiko Aratani, Hidekazu Takeno, Daijiro Hagiwara
  • Patent number: 4252804
    Abstract: Compounds of the formula I ##STR1## wherein m and n are 0, 1 or 2, X represents oxygen, imino, benzylimino, or morpholinoethylimino, Y represents CO, CONH, COO or SO.sub.2, and NR.sub.1 R.sub.2 represents a dimethylamino, diethylamino, dipropylamino, dibutylamino, allylamino, isobutenylamino, cyclopentylamino, cyclohexylamino, cycloheptylamino, cyclooctylamino, N-methyl N-cyclopentylamino, N-methyl N-cyclohexylamino, N-allyl N-cyclohexylamino, adamantylamino, diethoxyethylamino, dimethylaminoethylamino, dimethylaminopropylamino, N-methyl N-dimethylaminopropyl-amino, benzylamino, 3,4,5-trimethoxybenzylamino, phenethylamino, p-chlorophenethylamino, tetrahydrofurfurylamino, tetrahydropyranylmethylamino, pyrrolidino, isoxazolidinyl, piperidino, 4-hydroxypiperidino, 4-m-chlorophenyl-4-hydroxypiperidino, homopiperidino, 1,2,3,6-tetrahydropyridyl, morpholino, 2-methylmorpholino, 2,6-dimethylmorpholino, 2-morpholinoethylamino, thiamorpholino, piperazino, 4-methylpiperazino, 4-(.alpha.
    Type: Grant
    Filed: January 13, 1978
    Date of Patent: February 24, 1981
    Assignee: Metabio-Joullie
    Inventors: Maurice Joullie, Gabriel Maillard, Lucien Lakah, Christian J. M. Warolin
  • Patent number: 4232147
    Abstract: 4-N-acylfortimicin B-1,5-carbamates represented by the formula ##STR1## wherein R is acyl and R.sub.1 is hydrogen or benzyloxycarbonyl.
    Type: Grant
    Filed: September 26, 1979
    Date of Patent: November 4, 1980
    Assignee: Abbott Laboratories
    Inventors: John S. Tadanier, Jerry R. Martin
  • Patent number: 4230846
    Abstract: A 1,5-fortimicin B carbamate represented by the formula: ##STR1## wherein each R is hydrogen or monocyclicaryloxycarbonyl and R.sub.1 is selected from the group consisting of: loweralkyl, hydroxyloweralkyl, hydrogen, aminoloweralkyl, N-loweralkylaminoloweralkyl, N,N-diloweralkylaminoloweralkyl, trihaloalkoxycarbonyl, an amino acid residue and an N-protected amino acid residue and the pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: September 26, 1979
    Date of Patent: October 28, 1980
    Assignee: Abbott Laboratories
    Inventors: John S. Tadanier, Jerry R. Martin
  • Patent number: 4221814
    Abstract: A terephthalic acid monoamide derivative of the formula: ##STR1## (wherein R is a straight- or branched-chain lower alkyl group; R' and R" may be the same or different, and represent a hydrogen atom, or a straight- or branched-chain lower alkyl group) or pharmaceutically acceptable salts thereof are disclosed. A process for preparing such terephthalic acid monoamide derivative or its salts, as well as an anti-allergic agent containing such derivative or its salts as an effective ingredient are also disclosed.
    Type: Grant
    Filed: June 1, 1979
    Date of Patent: September 9, 1980
    Assignee: Chugai Seiyaku Kabushiki Kaisha
    Inventors: Sakae Takaku, Takashi Mori, Yasushi Murakami, Yoshiyuki Ohsugi, Shigeyuki Kataoka, Yasuhisa Takeda, Takashi Matsuno, Yoshimitsu Iida, Akiko Ariga, Akira Okazaki, Kazuo Igusa, Toshichika Ogasawara, Minoru Shindo
  • Patent number: 4218462
    Abstract: Disclosed are 1-substituted-6-(1-hydroxyethyl)-2-(2-aminoethylthio)-1-carbadethiapen-2-e m-3-carboxylic acids (I) and their pharmaceutically acceptable salts and esters which are useful as antibiotics; such compounds are prepared by total synthesis. ##STR1## wherein R.sup.1 is, inter alia, substituted and unsubstituted alkyl, aryl and aralkyl.
    Type: Grant
    Filed: October 24, 1978
    Date of Patent: August 19, 1980
    Assignee: Merck & Co., Inc.
    Inventors: Burton G. Christensen, David H. Shih
  • Patent number: 4211702
    Abstract: Penicillin and cephalosporin imino halides are prepared by reacting of 6-acylaminopenicillins or 7-acylamino cephalosporins with a novel chlorinating compound derived from a triaryl phosphite and chlorine or bromine. The imino halide products are intermediates in the preparation of antibiotic compounds.
    Type: Grant
    Filed: February 1, 1979
    Date of Patent: July 8, 1980
    Assignee: Eli Lilly and Company
    Inventors: Lowell D. Hatfield, Larry C. Blaszczak, Jack W. Fisher
  • Patent number: 4187375
    Abstract: A new process for preparing oxazine ring compounds comprises cyclization of an azetidinone-1-hydroxyacetate in the presence of a proton source.
    Type: Grant
    Filed: October 27, 1978
    Date of Patent: February 5, 1980
    Assignee: SmithKline Corporation
    Inventors: Thomas F. Buckley, John G. Gleason
  • Patent number: 4183855
    Abstract: Intermediates (I) for preparing a potent antibacterial, 1-oxadethiacephalosporin, are shown by the following formula ##STR1## (wherein R is a group of acyl-minus-carbonyl derived from a carboxylic or carbonic acid;COB is carboxy or protected carboxy;X is hydrogen or a nucleophilic group;Y is a nucleophilic group; andZ is a leaving group)and prepared from the corresponding exomethylene compound (II) by addition of a compound of formula: Y-Z (in which Y and Z are as defined above).
    Type: Grant
    Filed: February 24, 1978
    Date of Patent: January 15, 1980
    Assignee: Shionogi & Co., Ltd.
    Inventors: Mitsuru Yoshioka, Shoichiro Uyeo, Teruji Tsuji, Yoshio Hamashima, Ikuo Kikkawa, Wataru Nagata
  • Patent number: 4180668
    Abstract: 6-Amino-4H-s-triazolo[4,3-a][1,4]benzodiazepines of the formula ##STR1## wherein R is hydrogen or C.sub.1 to C.sub.3 -alkyl, R.sub.1 is hydrogen or halogen, and the two R.sub.2 groups are taken together with the nitrogen to which they are bonded to complete a nitrogen ring moiety selected from the group consisting of pyrrolidino, piperidino, morpholino and 3,6-dihydro-1(2H)-pyridyl, and the pharmacologically acceptable salts thereof, are central nervous system depressant drugs which are useful in effective dosages in domestic and zoo animals for their calming and tranquilizing uses during shipment and to reduce aggressive behavior. In man these compounds are potentially useful for controlling anxiety and schizophrenia and for their sedative, muscle relaxant and anti-convulsant activity.
    Type: Grant
    Filed: June 8, 1977
    Date of Patent: December 25, 1979
    Assignee: The Upjohn Company
    Inventor: Jackson B. Hester, Jr.
  • Patent number: 4160099
    Abstract: Labile quaternary ammonium salts of the following formula (I) and (II) are provided: ##STR1## wherein ##STR2## represents a tertiary aliphatic amine; wherein ##STR3## represents an unsaturated amine; wherein R represents a member selected from the group consisting of a hydrogen atom, a C.sub.1 -C.sub.8 open chain or cyclo alkyl group, a C.sub.1 -C.sub.8 alkoxyalkyl group, a C.sub.1 -C.sub.8 acyloxyalkyl group, a C.sub.1 -C.sub.8 haloalkyl group, a C.sub.1 -C.sub.8 carboxyalkyl group, a C.sub.2 -C.sub.8 alkenylphenyl group, an aryl group, and a substituted aryl group, whose substituents are selected from the group consisting of a halogen atom, an O-lower alkyl (C.sub.1 -C.sub.4) group, an O-acyl group, a nitro group, a carboxyl group, and a carboethoxy group; wherein R.sub.1 which may be the same or different, represents any member defined by R above with the proviso that R.sub.
    Type: Grant
    Filed: September 20, 1976
    Date of Patent: July 3, 1979
    Assignee: Interx Research Corporation
    Inventor: Nicolae S. Bodor
  • Patent number: 4159330
    Abstract: 3,4-Dihydro-4-oxo-quinazoline derivatives substituted in the 2-position by a substituted phenyl group are disclosed. The derivatives possess anti-allergy properties and can be used for the treatment of allergic conditions.
    Type: Grant
    Filed: December 2, 1977
    Date of Patent: June 26, 1979
    Assignee: Carlo Erba S.p.A.
    Inventors: Gianfederico Doria, Ciriaco Romeo, Piernicola Giraldi, Francesco Lauria, Maria L. Corno, Piero Sberze, Marcello Tibolla
  • Patent number: 4140789
    Abstract: A compound of the formula ##STR1## in which R.sub.1 denotes optionally substituted lower akyl which is optionally branched at the linking carbon atom, R.sub.2 represents hydrogen or lower alkanoyl and R.sub.3 is a group of the formula --R.sub.3.sup.a -(R.sub.3.sup.b).sub.n -- (Ia), in which R.sub.3.sup.1 represents the radical of the formula --N(R.sub.4)-- or --O-- and R.sub.4 represents hydrogen or lower alkyl, R.sub.3.sup.b denotes the radical of the formula --CH.sub.2 -- or, if R.sub.3.sup.a represents --N(R.sub.4)--, denotes the radical of the formula --C(.dbd.O)-- and n represents nought or 1, and a group of the formula Ia, in which n represents 1, can be linked to the carbonyl group of the carbamoyl grouping either via the group R.sub.3.sup.a or the group R.sub.3.sup.b, or acid addition salts thereof, which can be used pharmaceutically can be used as beta-receptor blocking agents for the treatment of disorders in the cardiac rhythm and coronary heart diseases.
    Type: Grant
    Filed: December 16, 1976
    Date of Patent: February 20, 1979
    Assignee: Ciba-Geigy Corporation
    Inventors: Knut A. Jaeggi, Franz Ostermayer, Herbert Schroter
  • Patent number: 4116953
    Abstract: Compounds of the formula ##STR1## in which K is the radical of a coupling component;X is hydrogen, chloro, bromo, methyl or nitro; andY is hydrogen, chloro, bromo or methyl.The compounds are eminently suitable as pigments for coloring printing inks, surface coatings and resins with exceptional fastness properties.
    Type: Grant
    Filed: September 16, 1976
    Date of Patent: September 26, 1978
    Assignee: BASF Aktiengesellschaft
    Inventors: Peter Dimroth, Helmut Junge, Peter Tonne, Rolf Urtel
  • Patent number: 4089956
    Abstract: A new series of 7-acylamino-8-oxo-3-oxa-1-azabicyclo-[4.2.0]octane-2-carboxylic acid derivatives is described which compounds have antibacterial activity especially against certain Gram negative organisms.
    Type: Grant
    Filed: September 8, 1976
    Date of Patent: May 16, 1978
    Assignee: SmithKline Corporation
    Inventors: Thomas Francis Buckley, John Gerald Gleason
  • Patent number: 4073614
    Abstract: A mixture of a triphenylmethane compound represented by the formula (Ia) ##STR1## AND A TRIPHENYLMETHANE COMPOUND REPRESENTED BY THE FORMULA (Ib) ##STR2## WHEREIN R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 and X are as defined hereinafter, useful as a color former.
    Type: Grant
    Filed: July 8, 1975
    Date of Patent: February 14, 1978
    Assignee: Hodogaya Chemical Co., Ltd.
    Inventors: Minoru Ozutsumi, Yoshihide Miyazawa, Masahiko Yamaguchi
  • Patent number: 4074050
    Abstract: A triphenylmethane compound represented by the formula (Ia) ##STR1## OR A MIXTURE THEREOF, WHEREIN R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 and X are as defined hereinafter, useful as a color former.
    Type: Grant
    Filed: March 16, 1977
    Date of Patent: February 14, 1978
    Assignee: Hodogaya Chemical Co., Ltd.
    Inventors: Minoru Ozutsumi, Yoshihide Miyazawa, Masahiko Yamaguchi
  • Patent number: 4056619
    Abstract: 1-Substituted-2-(2-pyridinyl)ethanone N-oxides having the formula I or II: ##STR1## wherein R.sub.1 is hydrogen or lower alkyl; R.sub.2 and R.sub.3 are each hydrogen, halogen, hydroxy, lower alkyl, lower alkoxy, or benzyloxy; R.sub.4 is halogen, hydroxy, lower alkyl, lower alkoxy, benzyloxy, ortho-amino, ortho-lower alkylamino, ortho-alkanoylamino or ortho-benzoylamino; and R.sub.5 is hydrogen, halogen, hydroxy, lower alkyl, lower alkoxy or benzyloxy; the pharmaceutically acceptable acid addition salts thereof, and a process for the preparation thereof, are described. The compounds of this invention are useful for the treatment of allergic conditions and for the treatment of hyperacidity.
    Type: Grant
    Filed: September 8, 1975
    Date of Patent: November 1, 1977
    Assignee: Warner-Lambert Company
    Inventors: David T. Connor, Patricia A. Young, Maximilian VON Strandtmann
  • Patent number: 4044010
    Abstract: Compounds of the formfulas ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, m and n and X are as hereinafter set forth,Are described. The compounds of formulas I and Ia are useful as neuroleptic agents.
    Type: Grant
    Filed: February 4, 1976
    Date of Patent: August 23, 1977
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Max Gerecke, Jean-Pierre Kaplan, Emilio Kyburz