Patents Represented by Attorney Dayton R. Stemple
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Patent number: 4599426Abstract: 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: GrantFiled: September 13, 1983Date of Patent: July 8, 1986Assignee: Fujisawa Pharmaceutical Co.Inventors: Takashi Kamiya, Kunihiko Tanaka, Tsutomu Teraji, Yoshiharu Nakai
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Patent number: 4576753Abstract: 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: GrantFiled: July 9, 1984Date of Patent: March 18, 1986Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Takashi Kamiya, Masashi Hashimoto, Osamu Nakaguti
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Patent number: 4544653Abstract: 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: GrantFiled: March 6, 1978Date of Patent: October 1, 1985Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Takao Takaya, Takashi Masugi, Hisashi Takasugi, Hiromu Kochi
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Patent number: 4544751Abstract: 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: GrantFiled: July 9, 1982Date of Patent: October 1, 1985Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Takao Takaya, Hisashi Takasugi, Toshiyuki Chiba, Zenzaburo Tozuka
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Patent number: 4543356Abstract: 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: GrantFiled: January 3, 1983Date of Patent: September 24, 1985Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Ikuo Ueda, Masayuki Kato, Masanobu Nagano
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Patent number: 4525478Abstract: 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: GrantFiled: September 3, 1982Date of Patent: June 25, 1985Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventor: Yoshinari Sato
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Patent number: 4506076Abstract: 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: GrantFiled: April 29, 1981Date of Patent: March 19, 1985Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Takashi Kamiya, Kunihiko Tanaka, Tsutomu Teraji, Yoshiharu Nakai
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Patent number: 4493833Abstract: Preparation of pharmaceutical composition comprising, treatment of human and animal diseases with, and compound of, 3,7-disubstituted-3-cephem-4-carboxylic acid.Type: GrantFiled: August 25, 1981Date of Patent: January 15, 1985Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Takao Takaya, Takashi Masugi, Hisashi Takasugi, Hiromu Kochi
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Patent number: 4487767Abstract: 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: GrantFiled: May 19, 1982Date of Patent: December 11, 1984Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Takao Takaya, Takashi Masugi, Hisashi Takasugi, Hiromu Kochi
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Patent number: 4473566Abstract: 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: GrantFiled: October 31, 1980Date of Patent: September 25, 1984Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Takao Takaya, Takashi Masugi, Hisashi Takasugi, Hiromu Kochi
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Patent number: 4472309Abstract: 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: GrantFiled: August 25, 1981Date of Patent: September 18, 1984Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Takashi Kamiya, Masashi Hashimoto, Osamu Nakaguti, Teruo Oku, Yoshiharu Nakai, Hidekazu Takeno
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Patent number: 4472300Abstract: 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: GrantFiled: March 13, 1980Date of Patent: September 18, 1984Assignee: 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
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Patent number: 4440766Abstract: 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: GrantFiled: August 10, 1981Date of Patent: April 3, 1984Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Takashi Kamiya, Kunihiko Tanaka, Yoshiharu Nakai, Kazuo Sakane
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Patent number: 4431643Abstract: 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: GrantFiled: March 1, 1982Date of Patent: February 14, 1984Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Takao Takaya, Takashi Masugi, Hisashi Takasugi, Hiromu Kochi
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Patent number: 4429126Abstract: 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: GrantFiled: June 4, 1982Date of Patent: January 31, 1984Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Ikuo Ueda, Masayuki Kato, Masanobu Nagano
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Patent number: 4411898Abstract: 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: GrantFiled: April 29, 1981Date of Patent: October 25, 1983Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Takao Takaya, Masayoshi Murata
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Patent number: 4401989Abstract: 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: GrantFiled: July 19, 1982Date of Patent: August 30, 1983Inventor: Telesforo Tulli
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Patent number: 4393070Abstract: 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: GrantFiled: December 4, 1980Date of Patent: July 12, 1983Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Yoshinari Sato, Tsutomu Teraji
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Patent number: 4377580Abstract: 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: GrantFiled: November 25, 1980Date of Patent: March 22, 1983Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Ikuo Ueda, Masayuki Kato, Masanobu Nagano
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Patent number: 4370334Abstract: 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: GrantFiled: December 4, 1980Date of Patent: January 25, 1983Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventor: Yoshinari Sato