Patents Examined by Gerald A. Schwartz
  • Patent number: 4048228
    Abstract: Substituted cyanamidic compounds as exemplified by N-(diphenylmethylidene)cyanamide may be prepared by reacting nitrogen-containing compounds having the formula: ##STR1## in which R.sub.1 and R.sub.2 are selected from the group consisting of hydrogen, aryl, alkyl possessing from 1 to about 30 carbon atoms, cycloalkyl possessing from about 5 to about 12 carbon atoms in the ring, alkyl-substituted cycloalkyl, aryl-substituted cycloalkyl, alkaryl and aralkyl radicals and R.sub.3 is selected from the group consisting of hydrogen, alkyl possessing from 1 to about 30 carbon atoms, aryl, cycloalkyl possessing from 5 to about 12 carbon atoms in the ring, alkyl-substituted cycloalkyl, aryl-substituted cycloalkyl and bicycloalkyl radicals with cyanamide and a compound selected from the group consisting of an acid-acting compound, an alkyl halide and an alkyl sulfate.
    Type: Grant
    Filed: January 12, 1977
    Date of Patent: September 13, 1977
    Assignee: UOP Inc.
    Inventor: James P. Shoffner
  • Patent number: 4046904
    Abstract: A penicillin of the formula: ##STR1## (i.e. 6-[D-2-(3-hydroxypyridazine-4-carbonamido)-2-(p-hydroxyphenyl)acetamido]pe nicillanic acid), which is valuable as an antibacterial agent, a nutritional supplement in animal feeds and a therapeutic agent in poultry and mammals including man and is especially useful in the treatment of infectious diseases caused by Gram-positive and Gram-negative bacteria.
    Type: Grant
    Filed: February 13, 1976
    Date of Patent: September 6, 1977
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Hirotada Yamada, Hisao Tobiki, Norihiko Tanno, Kozo Shimago, Kosaku Okamura, Takenari Nakagome, Toshiaki Komatsu, Akio Izawa, Hiroshi Noguchi, Kenji Irie, Yasuko Eda
  • Patent number: 4046903
    Abstract: This invention relates to a semi-synthetic penicillin having at least one .pi.-aromatic, organometallic complex of a transition metal such as ferrocene, attached, preferably in the 6 position, to a penicillin nucleus which optionally carries further substituents.
    Type: Grant
    Filed: October 20, 1975
    Date of Patent: September 6, 1977
    Inventors: Eva Irene Edwards, Roger Epton, George Marr
  • Patent number: 4046759
    Abstract: There disclose new penicillin esters and S-oxides thereof which are of value as intermediates for the preparation of various cephalosporin antibiotics.
    Type: Grant
    Filed: August 25, 1975
    Date of Patent: September 6, 1977
    Inventor: Toshiyasu Ishimaru
  • Patent number: 4045486
    Abstract: Azomethines having the formula ##STR1## wherein R is hydrogen, alkyl or alkoxy,m denotes an integer of from 1 to 4, andThe m R radicals are the same or different,Are prepared by condensing cyclohexanone and a primary aromatic amine in the presence of an acid ion exchanger.
    Type: Grant
    Filed: May 12, 1976
    Date of Patent: August 30, 1977
    Assignee: Bayer Aktiengesellschaft
    Inventors: Hermann-Dieter Krall, Hans-Helmut Schwarz
  • Patent number: 4045481
    Abstract: Disclosed is a process for preparing chlorinated isocyanide dichlorides comprising reacting an olefin with at least equimolar quantities of chlorine and cyanogen chloride at a temperature of from -30.degree. C to about 70.degree. C in the presence of a Friedel-Crafts catalyst.
    Type: Grant
    Filed: July 17, 1975
    Date of Patent: August 30, 1977
    Assignee: Bayer Aktiengesellschaft
    Inventor: Dieter Arlt
  • Patent number: 4045485
    Abstract: 2-(2'-Naphthyl) acetaldehyde derivatives optionally substituted at the 2 position and/or positions C-1',4',5',7' or 8'; and/or position C-6' or positions C-5' and 7' exhibit anti-inflammatory, analgesic, antipyretic and anti-pruritic activity.
    Type: Grant
    Filed: November 5, 1976
    Date of Patent: August 30, 1977
    Assignee: Syntex Corporation
    Inventors: John H. Fried, Ian T. Harrison
  • Patent number: 4045432
    Abstract: Antidepressant 1,1a,6,10b-tetrahydrodibenzo-[a,e]-cyclopropa-[c]-cyclohepten-6-substitute d oximes and their pharmaceutically suitable salts useful for alleviating depression in mammals.
    Type: Grant
    Filed: March 15, 1976
    Date of Patent: August 30, 1977
    Assignee: E. I. Du Pont de Nemours and Company
    Inventor: Roy Teruyuki Uyeda
  • Patent number: 4045574
    Abstract: D-homo-20-ketopregnanes of the formula ##STR1## wherein R.sub.1 is oxygen, ##STR2## in which R.sub.5 is hydrogen or lower acyl; R.sub.2 is hydrogen or methyl; R.sub.3 is oxygen, ##STR3## or two hydrogen atoms; R.sub.4 is hydrogen, hydroxy or acyloxy; R.sub.6 is hydrogen or methyl; and R.sub.7 is hydrogen, acetyl, hydroxy or lower acyloxy in the .alpha.- or .beta.-position possess CNS-depressant activity, including anesthesia upon parenteral administration, and are produced by hydrogenating the corresponding steroids having double bonded C.sub.5 and/or C.sub.16 carbon atoms.
    Type: Grant
    Filed: November 29, 1974
    Date of Patent: August 30, 1977
    Assignee: Schering Aktiengesellschaft
    Inventors: Ulrich Kerb, Rudolf Wiechert, Klaus Kieslich, Karl Petzoldt, Helmut Wachtel, Dieter Palenschat, Reinhard Horowski, Gert Paschelke, Wolfgang Kehr
  • Patent number: 4044000
    Abstract: 6-Alkoxylated-6-acylamidopenicillanic acids and 7-alkoxylated-7-acylamidocephalosporin acids and esters thereof, are provided by reacting a 6-acylamidopenicillanic acid ester or a 7-acylamidocephalosporin ester under anhydrous conditions at -90.degree. C. to -15.degree. C. with an alkali metal salt of a lower alkyl alcohol in the presence of an excess of the corresponding alcohol to produce, in situ, the anionic form of the antibiotic which on halogenation with a positive halogen compound, e.g. t-butyl hypochlorite, yields the compound of the invention. Compounds of the invention, e.g. 6-methoxy-6-phenoxy-acetamidopenicillanic acid and 7-methoxy-7-[2-(2-thienyl)acetamido]cephalosporanic acid are useful antibiotics.
    Type: Grant
    Filed: August 23, 1976
    Date of Patent: August 23, 1977
    Assignee: Eli Lilly and Company
    Inventor: Gary A. Koppel
  • Patent number: 4042582
    Abstract: Mixtures of mono- and disazomethine compounds are obtained by reacting 1.2 to 2.5 mols of an optionally substituted m-phenylene diamine with 2 mols of one or more optionally substituted 2-hydroxy-1-naphthaldehydes. The products are pigments having superior properties than the components.
    Type: Grant
    Filed: March 25, 1975
    Date of Patent: August 16, 1977
    Assignee: Hoechst Aktiengesellschaft
    Inventor: Theodor Papenfuhs
  • Patent number: 4039579
    Abstract: The present invention relates to 2-[1-imino-2-(methylsulfinyl)ethyl]phenols and 3-[1-imino-2-(methylsulfinyl)ethyl]-2-naphthalenols having the following structural formulas: ##STR1## wherein X is hydrogen, lower alkyl, halogen, lower alkoxy or hydroxy; Y is hydrogen, lower alkyl or cycloalkyl.These compounds exhibit antibacterial activity, particularly against gram-positive bacteria, and are useful in the treatment of bacterial infections caused by these organisms.
    Type: Grant
    Filed: December 8, 1976
    Date of Patent: August 2, 1977
    Assignee: Warner-Lambert Company
    Inventors: David T. Connor, Patricia A. Young, Max VON Strandtmann
  • Patent number: 4038316
    Abstract: Novel acylhydroximyl halides are provided and prepared by contacting a nitroalkanone with a halogen acid in the presence of an organic acid or alcohol.
    Type: Grant
    Filed: December 8, 1975
    Date of Patent: July 26, 1977
    Assignee: Texaco Inc.
    Inventors: Roger G. Duranleau, John M. Larkin
  • Patent number: 4038317
    Abstract: The present invention relates to a compound selected from the group consisting of compounds of formula: ##STR1## in which: R.sup.1 is selected from the group consisting of phenyl, phenyl substituted by a radical selected from C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, halogen, nitro, amino and cyano, and naphthyl,R.sup.2 is selected from the group consisting of hydrogen, C.sub.1 -C.sub.4 alkyl, and phenyl, or, together with the carbon atom to which they are attached, R.sup.1 and R.sup.2 form a polycyclic ring selected from the rings derived from fluorene, xanthene, indane, tetrahydronaphthalene, dihydrodibenzocycloheptene and dibenzocycloheptene,R.sup.3 is selected from the group consisting of isopropyl and tert. butyl, and a pharmaceutically acceptable acid addition salt thereof.Such a compound is useful as anti-hypertensive drug.
    Type: Grant
    Filed: February 10, 1976
    Date of Patent: July 26, 1977
    Assignee: Seperic
    Inventors: Camille Georges Wermuth, Jean Schwartz
  • Patent number: 4038271
    Abstract: [[[(2,4-Dioxo-1-imidazolidinyl)amino]carbonyl]amino]-acetylpenicillin derivatives of the formula ##STR1## wherein R is hydrogen, lower alkyl, phenyl-lower alkyl, tri(lower alkyl)silyl, a salt forming ion, or the group ##STR2## R.sub.1 is hydrogen or methoxy; R.sub.2, R.sub.3 and R.sub.5 each are independently selected from hydrogen and lower alkyl; R.sub.4 is hydrogen, lower alkyl, cycloalkyl, cycloalkenyl, cycloalkadienyl, phenyl, phenyl-lower alkyl, substituted phenyl, substituted phenyl-lower alkyl, or certain heterocyclic groups; R.sub.6 is lower alkyl; are disclosed. These compounds are useful as antibacterial agents.
    Type: Grant
    Filed: November 8, 1976
    Date of Patent: July 26, 1977
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Hermann Breuer, Uwe D. Treuner
  • Patent number: 4036829
    Abstract: Lactonyl esters of Penicillins of the formula ##STR1## WHEREIN R.sup.1 is an antibacterially active penicillin-completing side chain; R is hydrogen, methyl or phenyl; and Ra, Rb, Rc, Rd are hydrogen, lower alkyl, lower alkoxy, halo, and nitro, provided that when R is hydrogen and R.sup.1 is D-.alpha.-aminophenylacetamido and Ra, Rb, Rc, and Rd are not all hydrogen are disclosed to possess antibacterial properties.
    Type: Grant
    Filed: August 5, 1976
    Date of Patent: July 19, 1977
    Assignee: Beecham Group Limited
    Inventors: Harry Ferres, John Peter Clayton
  • Patent number: 4036846
    Abstract: The present invention discloses novel 6-acylamino-2,2-dimethyl-3-phosphonopenams and certain lower alkyl esters thereof possessing antibacterial activity, methods for their production, and intermediates therefor; the production comprises the steps of reacting 6-triphenylmethylamino-2,2-dimethylpenam-3-carboxylic acid with lead tetraacetate to form the corresponding 3-acetoxy compound, the latter is converted to .alpha.-triphenylmethylamino-5,5-dimethyl-3-thiazoline-2-acetic acid which is condensed with dimethyl phosphite to produce .alpha.-triphenylmethylamino-5,5-dimethyl-4(0,0-dimethylphosphono)-thiazol idine-2-acetic acid which is cyclized to 6-triphenylmethylamino-2,2-dimethyl-3-(0,0-dimethylphosphono)penam and the latter is subsequently deblocked and acylated.
    Type: Grant
    Filed: October 29, 1976
    Date of Patent: July 19, 1977
    Assignee: Pfizer Inc.
    Inventor: Wayne E. Barth
  • Patent number: 4036847
    Abstract: A penam derivative having the formula: ##STR1## wherein X represents a halogen atom, and wherein R.sub.1 represents an amino or acylamino, and R.sub.3 represents a radical selected from the group consisting of carboxy, ester, acid amide, acid anhydride, acid halide, and acid azide.
    Type: Grant
    Filed: August 5, 1976
    Date of Patent: July 19, 1977
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Takashi Kamiya, Yoshihisa Saito, Tsutomu Teraji, Osamu Nakaguti, Teruo Oku, Hitoshi Nakamura, Masashi Hashimoto
  • Patent number: 4035381
    Abstract: The alkali metal salts of the reaction products of ampicillin or amoxicillin with 5-formyl-2-furansulfonic acid are found to be stable, useful water-soluble forms of the penicillin antibiotics especially advantageous for parenteral administration.
    Type: Grant
    Filed: October 26, 1976
    Date of Patent: July 12, 1977
    Assignee: Bristol-Myers Company
    Inventors: Murray Arthur Kaplan, William Joseph Gottstein, Alphonse P. Granatek
  • Patent number: RE29349
    Abstract: A new family of organic thermotropic nematic compounds comprising N-(para-substituted alkoxy-benzylidene)-anilines having also a para-n-butyl substituent on the aniline ring. These compounds have the following structural formula: ##STR1## wherein R is a straight chain alkyl group containing 1 to 4 carbon atoms and R' is n-butyl. Synthesis involves combining the desired p-substituted benzaldehyde and p-n-butyl aniline in equimolar proportions in anhydrous ethyl alcohol with glacial acetic acid as catalyst. The resulting homologous series of compounds are useful as materials which undergo a change in optical properties under the influence of externally applied energy, preferred members of which, either individually or in binary mixtures, have melting points near room temperature, a broad nematic mesomorphic temperature range within an overall range of about 0.degree. to about 70.degree. C., low viscosity in the nematic phase, good stability, and substantially no color.
    Type: Grant
    Filed: September 2, 1975
    Date of Patent: August 9, 1977
    Assignee: Minnesota Mining and Manufacturing
    Inventor: Elwood L. Strebel