Patents Examined by David E. Wheeler
  • Patent number: 4203898
    Abstract: Amide derivatives of VLB, leurosidine, leurocristine and related dimeric alkaloids are useful as anti viral and anti-neoplastic agents or as intermediates in the preparation of such agents.
    Type: Grant
    Filed: October 25, 1978
    Date of Patent: May 20, 1980
    Assignee: Eli Lilly and Company
    Inventors: George J. Cullinan, Koert Gerzon
  • Patent number: 4202893
    Abstract: Novel alkyloximes of 7-amino-thiazolyl-acetamidocephalosporanic acids of the formula ##STR1## wherein R is selected from the group consisting of alkyl of 1 to 5 carbon atoms, cycloalkyl of 3 to 5 carbon atoms and --CH.sub.2 --SR', R' is selected from the group consisting of acyl of an alkanoic acid of 2 to 4 carbon atoms, 1-methyl-tetrazolyl and 2-methyl-1,3,4-thiadiazolyl, R.sub.1 is selected from the group consisting of hydrogen and a group easily removeable by acid hydrolysis or hydrogenolysis, R.sub.2 is selected from the group consisting of alkyl of 1 to 4 carbon atoms and alkenyl and alkynyl of 2 to 4 carbon atoms, A is selected from the group consisting of hydrogen, an alkali metal cation, an equivalent of an alkaline earth metal or magnesium, an organic amine base cation and an ester group easily removeable by acid hydrolysis or hydrogenolysis with the proviso that when R.sub.1 is hydrogen, A is not an ester group easily removeable by hydrogenolysis or acid hydrolysis and the wavy line means that OR.
    Type: Grant
    Filed: May 12, 1977
    Date of Patent: May 13, 1980
    Assignee: Roussel Uclaf
    Inventors: Rene Heymes, Andre Lutz
  • Patent number: 4200744
    Abstract: Novel 7.alpha.-methoxy-cephalosporins and non-toxic salts thereof, which contain a di-oxo-piperazinyl-carbonylamino group in molecule. These compounds are valuable antibacterial compounds for use in mammals including man. This disclosure relates to such compounds and methods for producing the same.
    Type: Grant
    Filed: October 27, 1977
    Date of Patent: April 29, 1980
    Assignee: Toyama Chemical Company, Limited
    Inventors: Isamu Saikawa, Shuntaro Takano, Hiroyuki Imaizumi, Isamu Takakura, Hirokazu Ochiai, Takashi Yasuda, Hideo Taki, Masuru Tai, Yutaka Kodama
  • Patent number: 4200751
    Abstract: Lactone electron donative color-forming agents of quinoline-carboxylic acid are disclosed having the general formulae (I) and (II) ##STR1## wherein A and B represent a variety of chemical moieties, X represents halo- or nitro- and n.sup.1 is an integer of 0-4. The color-forming agents are useful in recording materials of the pressure-sensitive and heat-sensitive varieties, and the like.
    Type: Grant
    Filed: November 21, 1977
    Date of Patent: April 29, 1980
    Assignee: Yamamoto Kagaku Gosei Co., Ltd.
    Inventors: Seiji Ikegami, Yoshihiro Hatano
  • Patent number: 4200745
    Abstract: Cephalosporin compounds of the formula ##STR1## wherein R and R.sub.2 are hydrogen or protecting groups, R.sub.1 is hydrogen or methoxy, R.sub.3 is hydrogen or C.sub.1 -C.sub.4 alkyl and R.sub.4 is C.sub.1 -C.sub.4 alkyl, are broad spectrum antibiotics or intermediates thereto.
    Type: Grant
    Filed: December 20, 1977
    Date of Patent: April 29, 1980
    Assignee: Eli Lilly and Company
    Inventor: Allen S. Katner
  • Patent number: 4199504
    Abstract: Bridged vinca dimers in which two indole-dihydro-indole C-3 carboxamides are linked through the nitrogen atom of a carboxamide group, useful as oncolytic agents.
    Type: Grant
    Filed: May 15, 1978
    Date of Patent: April 22, 1980
    Assignee: Eli Lilly and Company
    Inventors: Robert A. Conrad, Koert Gerzon
  • Patent number: 4199505
    Abstract: A process for the preparation of alkaloids of the leurosine type having the formula I ##STR1## and the acid addition salts thereof. In the formula I R is hydrogen or methyl. The compounds prepared according to the invention are known compounds showing cytostatic activity.
    Type: Grant
    Filed: May 19, 1978
    Date of Patent: April 22, 1980
    Assignee: Richter Gedeon Vegyeszeti Gyar Rt.
    Inventors: Csaba Szantay, Lajos Szabo, Katalin Honty, Katalin Nogradi, Karola Jovanovics, Eszter Dezseri, Lajos Dancsi, Csaba Lorincz, Bela Szarvady, Lajos Kovacs
  • Patent number: 4197298
    Abstract: 7-[2-(2-aminothiazol-4-yl)-2-(syn)-methoxyiminoacetamido]cephalosporanic acid derivatives of the formula; ##STR1## wherein R.sup.1 NH is an amino group which may optionally be protected; COOR.sup.2 is a carboxyl group which may optionally be esterified; X is oxygen, sulfur or an imino group which may optionally be substituted; B is hydrogen or a hydroxyl, amino, thiol or hydrocarbon group which may optionally be substituted, or a salt thereof, are novel, .beta.-lactamase-resistant and low-toxicity compounds which display excellent activity against a broad spectrum of microorganisms including Gram-negative bacteria such as Escherichia coli, Serratia marcescens, Proteus rettgeri, Enterobacter cloacae, Citrobacter freundii. Thus, these compounds can be used for antibacterial agents in therapeutical purpose.
    Type: Grant
    Filed: February 14, 1978
    Date of Patent: April 8, 1980
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Michihiko Ochiai, Akira Morimoto, Yoshihiro Matsushita
  • Patent number: 4197243
    Abstract: The compounds of this invention are strong central nervous system depressants, in particular strong antipsychotics.
    Type: Grant
    Filed: May 15, 1978
    Date of Patent: April 8, 1980
    Assignee: Yamanouchi Pharmaceutical Co., Ltd.
    Inventors: Masuo Murakami, Kozo Takahashi, Yasufumi Hirata, Mutsuo Takashima, Sumio Iwanami, Osamu Hasegawa, Yoshihisa Nozaki, Shiro Tachikawa, Masaaki Takeda, Shinji Usuda
  • Patent number: 4191688
    Abstract: C-3 Carboxamides of leurosine, leuroformine, 4-desacetylleurosine and 4-desacetylleuroformine, useful as antitumor agents.
    Type: Grant
    Filed: June 12, 1978
    Date of Patent: March 4, 1980
    Assignee: Eli Lilly and Company
    Inventors: Robert A. Conrad, George J. Cullinan, Jean C. Miller, Koert Gerzon
  • Patent number: 4179502
    Abstract: 2-Hydroxyiminoacetamide compounds of the following formula and salts thereof: ##STR1## [wherein X is S, O or an imino group which may optionally be substituted; B is a hydrogen atom or a hydroxyl, amino, mercapto or hydrocarbon residue group which may optionally be substituted; and COOR is a carboxyl group which may optionally be esterified] and pharmaceutically acceptable salts thereof are novel and useful as antibacterial agents.
    Type: Grant
    Filed: February 14, 1978
    Date of Patent: December 18, 1979
    Inventors: Mitsuo Numata, Isao Minamida, Susumu Tsushima
  • Patent number: 4172198
    Abstract: New cephalosporin compounds of the formula: ##STR1## wherein R.sub.1 is hydrogen or hydroxy, R.sub.2 is a substituted alkanoyl group, R.sub.3 is hydrogen, carbamoyloxy, alkanoyloxy or a heterocyclic-thio group which may have suitable substituents, and R.sub.4 is carboxy or protected carboxy.
    Type: Grant
    Filed: August 15, 1977
    Date of Patent: October 23, 1979
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Takashi Kamiya, Tsutomu Teraji, Keiji Hemmi, Jiro Goto
  • Patent number: 4167506
    Abstract: A group of novel polynuclear heterocyclic compounds having a diazaphenalene skeleton. These compounds assume orange to reddish violet colors according to the types of substituents on the diazaphenalene skeleton, and have excellent thermal stability and weatherability and good dispersibility in polymeric materials. They are useful as orange to reddish violet pigments, especially for coloring polymeric materials.
    Type: Grant
    Filed: September 13, 1977
    Date of Patent: September 11, 1979
    Assignee: Teijin Limited
    Inventors: Keizo Shimada, Toshiaki Harada, Masahiro Koga, Shizuo Nagahama, Hiroyoshi Minematsu, Hidetsugu Yoshida
  • Patent number: 4166115
    Abstract: The present invention relates to new syn-isomer of 3,7-disubstituted-3-cephem-4-carboxylic acid compounds and pharmaceutically acceptable salts thereof. More particularly, it relates to new syn-isomer of 3,7-disubstituted-3-cephem-4-carboxylic acid compounds and pharmaceutically acceptable salts thereof which have antibacterial activities and to processes for the preparation thereof, to pharmaceutical composition comprising the same, and to a method of using the same therapeutically in the treatment of infectious diseases in human beings and animals.
    Type: Grant
    Filed: February 11, 1977
    Date of Patent: August 28, 1979
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Takao Takaya, Takashi Masugi, Hisashi Takasugi, Hiromu Kochi
  • Patent number: 4162314
    Abstract: Novel .beta.-lactam antibiotics are compounds of the formula: ##STR1## wherein R is alkyl of up to 6 carbon atoms or, when A is oxygen, R is hydrogen; A is oxygen or --OCO--; Z is ##STR2## R.sup.1 is hydrogen, acetoxy or S-Het; Het is 1,2,3-triazol-5-yl, 1-methyltetrazol-5-yl, 1,3,4-thiadiazol-2-yl or 2-methyl-1,3,4-thiadiazol-5-yl; and n is an integer from 0 to 8; or a readily-cleavable ester or physiologically-acceptable salt thereof.
    Type: Grant
    Filed: June 13, 1977
    Date of Patent: July 24, 1979
    Assignee: Merck Patent Gesellschaft mit beschrankter Haftung
    Inventors: Rudolf Gottschlich, Rolf Gericke, Horst Juraszyk, Jurgen Seubert, Wighard Strehlow, Helmut Wahlig, Rolf Bergmann, Elvira Dingeldein
  • Patent number: 4160767
    Abstract: 3-Spiro-5"-oxazolidine-2",4"-dione derivatives of Vinca alkaloids, useful as anti-tumor agents and as intermediates.
    Type: Grant
    Filed: August 21, 1978
    Date of Patent: July 10, 1979
    Assignee: Eli Lilly and Company
    Inventors: Jean C. Miller, Gerald E. Gutowski
  • Patent number: 4160086
    Abstract: A class of .alpha.-carboxy-3-heterocyclicthio cephems have an unusually high level of antibacterial activity against a wide variety of Gram-positive and Gram-negative organisms.
    Type: Grant
    Filed: April 8, 1975
    Date of Patent: July 3, 1979
    Assignee: Beecham Group Limited
    Inventors: George Burton, Elzbieta Watson
  • Patent number: 4160093
    Abstract: 6-Ethyl-6,9-dihydro-9-oxopyrazolo[3,4-f]quinoline-8-carboxylic acid of the formula: ##STR1## is useful as an antibacterial agent.
    Type: Grant
    Filed: April 24, 1978
    Date of Patent: July 3, 1979
    Assignee: Morton-Norwich Products, Inc.
    Inventors: Thomas J. Schwan, Raymond Freedman
  • 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: 4159269
    Abstract: 3-Spiro-5"-oxazolidine-2",4"-dione derivatives of Vinca alkaloids, useful as anti-tumor agents, synthesized from a C-3 carboxamide and a dialkyl carbonate.
    Type: Grant
    Filed: March 3, 1978
    Date of Patent: June 26, 1979
    Assignee: Eli Lilly and Company
    Inventor: Jean C. Miller