Patents Represented by Attorney Dayton R. Stemple
  • Patent number: 4599426
    Abstract: The present invention relates to new 3,7-disubstituted-3-cephem-4-carboxylic acid compounds and pharmaceutically acceptable salts thereof which have antimicrobial activities and to processes for preparation thereof, to pharmaceutical compositions comprising the same, and to a method of using the same therapeutically in the treatment of infectious diseases in humans and animals.This division relates to intermediate compounds, namely amino or amido-thiazolyl, substituted oxyimino disubstituted acetic acid of the formula: ##STR1## wherein R.sup.1 is amino or a protected amino group;R.sup.2 is --CONH--R.sup.5 or --HNCO--R.sup.5,R.sup.5 is aryl or heterocyclic, either of which may be substituted, andA is lower alkylene, or a salt thereof.
    Type: Grant
    Filed: September 13, 1983
    Date of Patent: July 8, 1986
    Assignee: Fujisawa Pharmaceutical Co.
    Inventors: Takashi Kamiya, Kunihiko Tanaka, Tsutomu Teraji, Yoshiharu Nakai
  • Patent number: 4576753
    Abstract: This invention relates to new 2-azetidinone compounds, which have antimicrobial activities, and to processes for the preparation thereof, and more particularly, this invention provides new 2-azetidinone compounds, especially ones having various substituted carboxyalkyl radicals at the first position and having various groups at the fourth position of the azetidinone nucleus, which have antimicrobial activities against various pathogenic microorganisms and are useful as antibiotics in treatment for microbial infections in mammals including human beings and animals.
    Type: Grant
    Filed: July 9, 1984
    Date of Patent: March 18, 1986
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Takashi Kamiya, Masashi Hashimoto, Osamu Nakaguti
  • Patent number: 4544653
    Abstract: The present invention relates to a 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. New cephems disclosed herein are ##STR1## wherein R.sup.1 is ##STR2## R.sup.2 is lower alkyl, R.sup.3 is carboxy, R.sup.4 is carbamoyloxy methyl which may be substituted with a trihalo- (lower) alkanoyl; and R.sup.7 is amino, lower alkanoylamino or halo (lower)alkanoylamino.
    Type: Grant
    Filed: March 6, 1978
    Date of Patent: October 1, 1985
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Takao Takaya, Takashi Masugi, Hisashi Takasugi, Hiromu Kochi
  • Patent number: 4544751
    Abstract: 3,7-disubstituted-3-cephem-4-carboxylic acid compounds having bacteriostatic properties and the following formula: ##STR1## in which R.sup.1 is thiadiazolyl or isothiazolyl, each of which may have suitable substituent(s), or thiazolyl; R.sup.2 is hydrogen or lower alkyl; R.sup.3 is carboxy or protected carboxy; R.sup.4 is hydrogen, acyloxy or a heterocyclicthio group which may have suitable substituent(s); and R.sup.5 is hydrogen or lower alkoxy, process for making same and treating infectious diseases therewith.
    Type: Grant
    Filed: July 9, 1982
    Date of Patent: October 1, 1985
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Takao Takaya, Hisashi Takasugi, Toshiyuki Chiba, Zenzaburo Tozuka
  • Patent number: 4543356
    Abstract: This invention is directed to new quinazoline derivatives of the following formula having use in the treatment of symptoms associated with allergic manifestations. ##STR1## wherein R.sub.a.sup.1 and R.sub.b.sup.1 are C.sub.2 -C.sub.7 alkoxycarbonyl or R.sub.a.sup.1 and R.sub.b.sup.1 is linked together to form a group of the formula: ##STR2## R.sup.2 and R.sup.3 are hydrogen, C.sub.1 -C.sub.6 alkyl, halogen, nitro, amino, C.sub.1 -C.sub.6 alkoxy, phenoxy, C.sub.1 -C.sub.6 alkylthio, C.sub.1 -C.sub.6 alkylpiperazinyl, C.sub.1 -C.sub.18 alkanoylamino, di(C.sub.1 -C.sub.6)alkanoylamino, C.sub.3 -C.sub.9 alkoxalylamino, C.sub.4 -C.sub.8 cycloalkylcarbonylamino, C.sub.3 -C.sub.7 cycloalkyl(C.sub.1 -C.sub.6)alkanoylamino, benzamido, phenyl(C.sub.1 -C.sub.6)alkanoylamino, C.sub.1 -C.sub.6 alkylsulfonylamino or di(C.sub.1 -C.sub.6)alkylamino which may be substituted with hydroxy,A.sup.1 is a group of the formula: ##STR3## in which R.sup.4 is hydrogen C.sub.1 -C.sub.6 alkyl, hydroxy, C.sub.1 -C.sub.6 alkoxy, C.sub.
    Type: Grant
    Filed: January 3, 1983
    Date of Patent: September 24, 1985
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Ikuo Ueda, Masayuki Kato, Masanobu Nagano
  • Patent number: 4525478
    Abstract: 1,4-Dihydropyridine derivatives of the general formula ##STR1## having vasodilating and anti-hypertensive activity, processes for preparing same, and pharmaceutical compositions thereof for treating cardiovascular diseases.
    Type: Grant
    Filed: September 3, 1982
    Date of Patent: June 25, 1985
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventor: Yoshinari Sato
  • Patent number: 4506076
    Abstract: The present invention relates to new 3,7-disubstituted-3-cephem-4-carboxylic acid compounds and pharmaceutically acceptable salts thereof which have antimicrobial activities and to processes for preparation thereof, to pharmaceutical compositions comprising the same, and to a method of using the same therapeutically in the treatment of infectious diseases in humans and animals.This division relates to intermediate compounds, namely amino or amido-thiazolyl, substituted oxyimino disubstituted acetic acid of the formula: ##STR1## wherein R.sup.1 is amino or a protected amino group;R.sup.2 is --CONH--R.sup.5, --NHCO--R.sup.5, or ##STR2## R.sup.5 is aryl or heterocyclic, either of which may be substituted, R.sup.6 is hydrogen or lower alkyl, andA is lower alkylene, or a salt thereof.
    Type: Grant
    Filed: April 29, 1981
    Date of Patent: March 19, 1985
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Takashi Kamiya, Kunihiko Tanaka, Tsutomu Teraji, Yoshiharu Nakai
  • Patent number: 4493833
    Abstract: Preparation of pharmaceutical composition comprising, treatment of human and animal diseases with, and compound of, 3,7-disubstituted-3-cephem-4-carboxylic acid.
    Type: Grant
    Filed: August 25, 1981
    Date of Patent: January 15, 1985
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Takao Takaya, Takashi Masugi, Hisashi Takasugi, Hiromu Kochi
  • Patent number: 4487767
    Abstract: Bacteriostatic cephem compounds and processes for preparing same having the formula: ##STR1## wherein R.sup.1 is amino or protected amino,R.sup.2 is lower alkyl, amino(lower)alkyl, protected amino(lower)alkyl, hydroxy(lower)alkyl, protected hydroxy(lower)alkyl, lower alkylthio(lower)alkyl, carboxy(lower)alkyl, esterified carbony(lower)alkyl, (C.sub.3 -C.sub.8)cycloalkyl, lower alkenyl or lower alkynyl,R.sup.3 is a heterocyclic group substituted with amino(lower)alkyl, protected amino(lower)alkyl, hydroxy(lower)alkyl or both amino and lower alkyl,R.sup.4 is carboxy or protected carboxy, provided that R.sup.3 is a heterocyclic group substituted with hydroxy(lower)alkyl or both amino and lower alkyl, when R.sup.2 is lower alkyl, and its pharmaceutically acceptable salt.
    Type: Grant
    Filed: May 19, 1982
    Date of Patent: December 11, 1984
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Takao Takaya, Takashi Masugi, Hisashi Takasugi, Hiromu Kochi
  • Patent number: 4473566
    Abstract: 7-(.alpha.,.alpha.-disubstituted-acetamido)-3-substituted-3-cephem-4-carbox ylic acids having antibacterial properties and the following formula are disclosed: ##STR1## wherein R.sup.1 is hydrogen, halogen, hydroxy, nitro, lower alkoxy or acylamino, R.sup.2 is hydrogen or acyl andR.sup.3 is lower alkanoyloxy, carbamoyloxy which may have lower alkyl, aryl or protective group for amino or a heterocyclicthio which may have lower alkyl.
    Type: Grant
    Filed: October 31, 1980
    Date of Patent: September 25, 1984
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Takao Takaya, Takashi Masugi, Hisashi Takasugi, Hiromu Kochi
  • Patent number: 4472300
    Abstract: New antimicrobial azetidinone derivatives and their salt of the formula: ##STR1## wherein R.sub.1 amino or acylamino, and A is selected from a variety of groups.
    Type: Grant
    Filed: March 13, 1980
    Date of Patent: September 18, 1984
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Takashi Kamiya, Yoshihisa Saito, Masashi Hashimoto, Osamu Nakaguti, Teruo Oku, Youichi Shiokawa, Takao Takaya, Tadaaki Komori, Tsutomu Teraji, Keiji Hemmi, Hisashi Takasugi
  • Patent number: 4472309
    Abstract: This invention relates to new 2-azetidinone compounds, which have antimicrobial activities, and to processes for the preparation thereof, and more particularly, this invention provides new 2-azetidinone compounds, especially ones having various substituted carboxyalkyl radicals at the first position and having various group at the fourth position of the azetidinone nucleus, which have antimicrobial activity against various pathogenic microorganisms and are useful as antibiotics in treatment for microbial infections in mammals including human beings and animals.
    Type: Grant
    Filed: August 25, 1981
    Date of Patent: September 18, 1984
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Takashi Kamiya, Masashi Hashimoto, Osamu Nakaguti, Teruo Oku, Yoshiharu Nakai, Hidekazu Takeno
  • Patent number: 4440766
    Abstract: 3,7-Disubstituted-3-cephem-4-carboxylic acid compounds and pharmaceutical salts thereof having antibacterial properties in the treatment of animals and processes for preparing the compounds.
    Type: Grant
    Filed: August 10, 1981
    Date of Patent: April 3, 1984
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Takashi Kamiya, Kunihiko Tanaka, Yoshiharu Nakai, Kazuo Sakane
  • Patent number: 4431643
    Abstract: The present invention relates to new syn-isomers of 3,7-disubstituted-3-cephem-4-carboxylic acid compounds, pharmaceutically acceptable salts thereof, and pharmaceutical compositions comprising the same, which have antibacterial activities in the treatment of infectious diseases in human beings and animals.
    Type: Grant
    Filed: March 1, 1982
    Date of Patent: February 14, 1984
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Takao Takaya, Takashi Masugi, Hisashi Takasugi, Hiromu Kochi
  • Patent number: 4429126
    Abstract: Quinazoline derivatives of the formulae: ##STR1## wherein A.sup.1 is ##STR2## A.sup.2 is ##STR3## R.sup.1 is hydrogen, carboxy or esterified carboxy, R.sub.a.sup.1 and R.sub.b.sup.1 are esterified carboxy,R.sup.2 and R.sup.3 are hydrogen, alkyl, halogen, nitro, amino, alkoxy, aryloxy, alkylthio, alkylpiperazinyl, acylamino or dialkylamino which may be substituted with hydroxy,R.sup.4 is hydrogen, alkyl, hydroxy, alkoxy, alkenyloxy, dialkylamino or 2,2-dialkoxycarbonylvinylaminoR.sub.a.sup.4 is hydrogen, alkyl, hydroxy, alkoxy, alkenyloxy or dialkylamino,R.sup.5 is alkyl or alkenyl, andR.sup.6 is carboxy or esterified carboxy.
    Type: Grant
    Filed: June 4, 1982
    Date of Patent: January 31, 1984
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Ikuo Ueda, Masayuki Kato, Masanobu Nagano
  • Patent number: 4411898
    Abstract: A 3,7-disubstituted-3-cephem-4-carboxylic acid of the general formula: ##STR1## having antibacterial activity, processes for preparing same, and pharmaceutical compositions thereof for treating infectious diseases in humans and animals.
    Type: Grant
    Filed: April 29, 1981
    Date of Patent: October 25, 1983
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Takao Takaya, Masayoshi Murata
  • Patent number: 4401989
    Abstract: Television and FM radio antenna apparatus with a tuneable circuit to be coupled with a building wiring system and thus supplement or replace conventional interior or exterior antennas.
    Type: Grant
    Filed: July 19, 1982
    Date of Patent: August 30, 1983
    Inventor: Telesforo Tulli
  • Patent number: 4393070
    Abstract: 1,4-dihydropyridine derivatives of the general formula: ##STR1## having vasodilating and anti-hypertensive activity, processes for preparing same, and pharmaceutical compositions thereof for treating cardiovascular diseases.
    Type: Grant
    Filed: December 4, 1980
    Date of Patent: July 12, 1983
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Yoshinari Sato, Tsutomu Teraji
  • Patent number: 4377580
    Abstract: Quinazoline derivatives of the formulae: ##STR1## wherein A.sup.1 is ##STR2## A.sup.2 is ##STR3## R.sup.1 is hydrogen, carboxy or esterified carboxy, R.sub.a.sup.1 and R.sub.b.sup.1 are esterified carboxy,R.sup.2 and R.sup.3 are hydrogen, alkyl, halogen, nitro, amino, alkoxy, aryloxy, alkylthio, alkylpiperazinyl, acylamino or dialkylamino which may be substituted with hydroxy,R.sup.4 is hydrogen, alkyl, hydroxy, alkoxy, alkenyloxy, dialkylamino or 2,2-dialkoxycarbonylvinylaminoR.sub.a.sup.4 is hydrogen, alkyl, hydroxy, alkoxy, alkenyloxy or dialkylamino,R.sup.5 is alkyl or alkenyl, andR.sup.6 is carboxy or esterified carboxy.
    Type: Grant
    Filed: November 25, 1980
    Date of Patent: March 22, 1983
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Ikuo Ueda, Masayuki Kato, Masanobu Nagano
  • Patent number: 4370334
    Abstract: 1,4-Dihydropyridine derivatives of the general formula ##STR1## having vasodilating and anti-hypertensive activity, processes for preparing same, and pharmaceutical compositions thereof for treating cardiovascular diseases.
    Type: Grant
    Filed: December 4, 1980
    Date of Patent: January 25, 1983
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventor: Yoshinari Sato