7-position Substituent Contains Hetero Ring Patents (Class 514/206)
-
Patent number: 4950661Abstract: The present invention relates to derivatives of the cephalosporin family, of formula: ##STR1## in which: X is an oxygen atom or a sulfur atomn is zero, 1 or 2.R.sub.1, R.sub.2 and R.sub.3 each designate, a hydrogen atom or else R.sub.1 and R.sub.2 designate a hydrogen atom or a methyl group, and R.sub.3 designates a carboxyl or cyclopropyl group, or elseR.sub.1 and R.sub.2 taken together with the carbon atom to which they are linked form a cyclobutyl or cyclopentyl group and R.sub.3 is a carboxyl group.B is the residue of a primary or secondary amine;their preparation process and application in therapeutics.Type: GrantFiled: April 28, 1988Date of Patent: August 21, 1990Assignee: SANOFIInventors: Dominique Olliero, Ali Salhi
-
Patent number: 4946837Abstract: A compound of the formula; ##STR1## wherein R.sup.0 stands for nitrogen-containing heterocyclic group, acyl group or amino-protecting group, Z stands for S, S.fwdarw.O, O or CH.sub.2, R.sup.4 stands for hydrogen atom, methoxy group or formamido group, R.sup.13 stands for hydrogen atom, methyl group, hydroxyl group or halogen atom and A stands for an optionally substituted thiazol-3-yl group forming a fused ring at the 4,5-position or a physiologically or pharmaceutically acceptable salt or ester thereof.This compound is novel and has excellent antibacterial activity.Type: GrantFiled: May 12, 1988Date of Patent: August 7, 1990Assignee: Takeda Chemical Industries, Ltd.Inventors: Akio Miyake, Masahiro Kondo, Masahiko Fujino
-
Patent number: 4943568Abstract: Antibacterially active novel cephalosporins of the formula ##STR1## in which R.sup.1 represents alkyl, alkenyl, alkoxy, alkylthio, halogen, trifluoromethyl or trifluoromethoxy,R.sup.2 represents hydrogen or an organic radical,R.sup.3 represents hydrogen, alkyl, alkenyl, alkoxy, alkylthio, halogen, hydroxymethyl or ethers or esters thereof, or various organothiomethyl or substituted aminomethyl radicals, andR.sup.4 represents COO.sup.- or COOH, or salts thereof.Type: GrantFiled: November 21, 1986Date of Patent: July 24, 1990Assignee: Bayer AktiengesellschaftInventors: Michael Boberg, Rolf Angerbauer, Karl G. Metzger, Hans-Joachim Zeiler
-
Patent number: 4943567Abstract: Cephalosporin compounds represented by the general formula (I): ##STR1## wherein R.sup.1 and R.sup.5 independently represent a hydrogen atom or a protective group for an amino group; R.sup.2 represents an alkyl group or a cycloalkyl group; R.sup.3 represents a hydrogen atom, a lower alkenyl group, an alkanoyloxymethyl group, a carbamoyloxymethyl group, a heterocyclic thiomethyl group or a heterocyclic methyl group; R.sup.4 represents a hydrogen atom or an ester residue; and X represents CH or a nitrogen atom and pharmacologically acceptable addition salts thereof, intermediate compounds used in the synthesis process of these compounds, production methods of these compounds and pharmaceutical compositions containing these compounds.Type: GrantFiled: May 27, 1988Date of Patent: July 24, 1990Assignee: Kyoto Pharmaceutical Industries, Ltd.Inventors: Susumu Nishizawa, Hiroyuki Muro, Masayasu Kasai, Satoru Hatano, Syouzi Kamiya, Nobuharu Kakeya, Kazuhiko Kitao
-
Patent number: 4921850Abstract: A 3-propenylcephem derivative of the following formula: ##STR1## wherein R.sub.1 represents a fluoro-substituted lower alkyl group or a cyano-substituted lower alkyl group, and A represents a cyclic or an acylic ammonio group, or a pharmaceutically acceptable salt thereof, exhibiting excellent anti-bacterial activities against both Gram-positive bacteria and Gram-negative bacteria; Process for the preparation thereof; Anti-bacterial composition; Intermediate for the 3-propenylcephem derivative; and Process for the preparation of the intermediate.Type: GrantFiled: October 13, 1987Date of Patent: May 1, 1990Assignee: Eisai Co., Ltd.Inventors: Takashi Kamiya, Toshihiko Naito, Shigeto Negi, Yuuki Komatu, Yasunobu Kai, Takaharu Nakamura, Isao Sugiyama, Yoshimasa Machida, Seiichiro Nomoto, Kyosuke Kitoh, Kanemasa Katsu, Hiroshi Yamauchi
-
Patent number: 4919932Abstract: A pharmaceutical formulation having a synergistic anti-bacterial activity and comprising(a) a cephalosporin derivative or a physiologically acceptable salt or ester thereof and(b) a penem antibiotic of the basic structure (B) ##STR1## or a physiologically acceptable salt or ester thereof, a process for preparing such a formulation and its use for the treatment of bacterial infections.Type: GrantFiled: June 2, 1987Date of Patent: April 24, 1990Assignee: Hoechst AktiengesellschaftInventors: Michael Limbert, Elmar Schrinner, Gerhard Seibert
-
Patent number: 4918070Abstract: A cephalosporin derivative having the formula: ##STR1## wherein R.sup.1 is a substituted amino group, X is an alkylene group, R.sup.2 is an aryl or heterocyclic group which may be substituted and R.sup.3 is a hydrogen atom, a negative charge or a residue of an ester which can form a pharmaceutically acceptable ester hydrolyzable in a living body; or a pharmaceutically acceptable salt thereof.Type: GrantFiled: February 26, 1988Date of Patent: April 17, 1990Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Susumu Nakagawa, Hiroshi Fukatsu, Yoshiaki Katoh, Satoshi Murase
-
Patent number: 4918068Abstract: There are provided new cephem compounds (synisomers) represented by the following general formula (I): ##STR1## wherein R.sup.1 means a lower group, R.sup.2 denotes an ester-forming group of the carboxyl group, and the 4-methylthiazolyl group and the cephem moiety are cis to each other relative to the carbon-carbon double bond of the substituted vinyl group in the side chain at the 3-position of the cephem nucleus. The cephem compounds exhibit strong antibacterial activities not only against resistant strains of bacteria and gram-negative bacteria but also against gram-positive bacteria and moreover have very low toxicity.Type: GrantFiled: February 26, 1987Date of Patent: April 17, 1990Assignee: Meiji Seika Kaisha, Ltd.Inventors: Yuichi Yamamoto, Kunio Atsumi, Kenji Sakagami, Takashi Yoshida, Ken Nishihata, Sinichi Kondo
-
Patent number: 4914091Abstract: Adamantane 1 carbonyloxymethyl 7.beta.-[2-(2-aminothiazol-4-yl)-(Z)-2-methoxyiminoacetamido]-3-[(1,2,3-th iadiazol-5 yl)-thiomethyl]ceph-3-em-4 carboxylate is disclosed. It and other esters are used as orally administered anti bacterials".Type: GrantFiled: April 2, 1984Date of Patent: April 3, 1990Assignee: American Cyanamid CompanyInventors: William V. Curran, Adma S. Ross
-
Patent number: 4904652Abstract: The compound 7[2-(aminothiazol-4-yl)-2-methyoxyiminoacetamido]-methylthiomethyl-3-cephe m-4-carboxylic acid or carboxylic ester thereof, or a pharmaceutically acceptable salt thereof is disclosed as an antimicrobial agent.Type: GrantFiled: October 9, 1985Date of Patent: February 27, 1990Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Takao Takaya, Hisashi Takasugi, Takashi Masugi, Hideaki Yamanaka, Kohji Kawabata
-
Patent number: 4902683Abstract: Crystalline hydrohalide salts of the cephalosporin antibiotic ceftiofur, processes for their manufacture, and pharmaceutical compositions containing one of these salts are provided.Type: GrantFiled: February 17, 1989Date of Patent: February 20, 1990Assignee: The Upjohn CompanyInventors: Mahendra I. Amin, Jay A. Campbell
-
Patent number: 4898858Abstract: New cephalosporin derivatives of a general formula (I) and non-toxic salts and non-toxic esters thereof are provided: ##STR1## (wherein R represents an acyclic or cyclic lower alkyl group having 1-6 carbon atoms, which may optionally be substituted by a halogen atom; the steric configuration as asterisked (*) includes an optical-active (R)-form or (S)-form or an optical-inactive (RS)-form; n is 0 or 1, n.sup.1 is 0 to 3, n.sup.2 is 0 to 3; and when n.sup.1 is 0, n.sup.2 is 3; when n.sup.1 is 1, n.sup.2 is 2; when n.sup.1 is 2, n.sup.2 is 1; when n.sup.1 is 3, n.sup.2 is 0).The new derivatives of the formula (I) and non-toxic salts and esters thereof have high bactericidal activity with broad antibacterial spectra, and these are useful as active ingredients in bactericides.Type: GrantFiled: November 10, 1986Date of Patent: February 6, 1990Assignees: Meiji Seika Kaisha Ltd., Susumu MitsuhashiInventors: Seiji Shibahara, Tsuneo Okonogi, Yasushi Murai, Toshiaki Kudo, Takashi Yoshida, Ken Nishihata, Shinichi Kondo
-
Patent number: 4888332Abstract: The present invention relates to novel cephalosporin derivatives, processes for preparing thereof, compositions for preventing and/or treating infectious diseases which comprise the novel cephalosporin derivatives as active components, and the intermediate compounds in the synthesis of cephalosporin derivatives and processes for producing thereof.The novel cephalosporin derivatives according to the present invention contain condensed heterocyclic groups, particularly a triazolopyrimidine ring or a thiadiazolopyrimidine ring as substituents at the 3-position of the cephem skeleton, and a hydroxyimino, an alkyloxyimino or an acyloxyimino moiety as substituents at the 7-position of the cephem skeleton.The compounds of the present invention containing the aforementioned substituents have a strong antibacterial activity against gram-negative bacteria and also against gram-positive bacteria including methicillin-resistant Staphylococcus aureus.Type: GrantFiled: December 28, 1984Date of Patent: December 19, 1989Assignee: Mochida Pharmaceutical Co., Ltd.Inventors: Haruo Ohnishi, Hiroshi Kosuzume, Masahiro Mizota, Yasuo Suzuki, Ei Mochida
-
Patent number: 4880798Abstract: The present invention relates to novel cephalosporin derivatives, processes for preparing thereof, compositions for preventing and/or treating infectious diseases which comprise the novel cephalosporin derivatives as active components, and the intermediate compounds in the synthesis of cephalosporin derivatives and processes for producing thereof.The present invention is based on the selection of groups containing a condensed heterocyclic ring, particularly a triazolopyrimidine ring, as substitutents at the 3-position of the cephem skeleton, and of groups containing a carboxyl and hydroxy substituted phenylmethyloxyimino moiety, particularly a (carboxy substituted catechol)methyloxyimino moiety, as substituents at the 7-position of the cephem skeleton.The compounds of the present invention containing the aforementioned substituents have a strong antibacterial activity against Gram-negative bacteria and also against Gram-positive bacteria including methicillin-resistant Staphylococcus aureus.Type: GrantFiled: November 20, 1987Date of Patent: November 14, 1989Assignee: Mochida Pharmaceutical Co., Ltd.Inventors: Kazuo Kato, Kimihiro Murakami, Hidenori Mochizuki, Ei Mochida
-
Patent number: 4880797Abstract: A compound having the formula: ##STR1## wherein R is a vinyl, phenyl or aralkyl group which may be substituted; or a pharmaceutically acceptable salt, physiologically hydrolyzable ester or solvate thereof.Type: GrantFiled: March 20, 1987Date of Patent: November 14, 1989Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Susumu Nakagawa, Ryuji Mitomo, Ryosuke Ushijima
-
Patent number: 4880796Abstract: An antimicrobial preparation of D-7-[.alpha.-(4-hydrooxy-6-methylnicotinamido)-4-hydroxyphenylacetamido]-3 -(1-methyltetrazol-5-yl)thiomethyl-.DELTA..sup.3 -cephem-4-sodium carboxylate (hereinafter referred to as "Compound A" of enhanced stability is disclosed, which comprises a microbially effective amount of Compund A and a stabilizer selected from the class consisting of benzoic acid, sodium benzoate and nicotinamide.Type: GrantFiled: April 9, 1987Date of Patent: November 14, 1989Assignees: Sumitomo Chemical Company, Limited, Yamanouchi Pharmaceutical Co., Ltd.Inventors: Yoshiya Yamahira, Yoshiko Okuzawa, Keiji Fujioka, Shigeji Sato, Reimei Ishikawa
-
Patent number: 4871730Abstract: A cephem compound of the formula: ##STR1## wherein R.sup.1 is a group of the formula: ##STR2## in which R.sup.5 is amino or protected amino, R.sup.6 is hydrogen, lower alkyl, lower alkenyl, lower alkynyl, carboxy(lower) alkyl, protected carboxy(lower) alkyl, cyclo(lower) alkyl or cyclo (lower)alkenyl, and Z is CH or N;R.sup.2 is hydrogen, phenyl, pyridyl which may have a lower alkyl group, or cyano; andR.sup.3 is carboxy or protected carboxy; and pharmaceutically acceptable salt thereof.Type: GrantFiled: November 24, 1986Date of Patent: October 3, 1989Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Takao Takaya, Zenzaburo Tozuka, Nobuyoshi Yasuda, Kohji Kawabata
-
Patent number: 4866055Abstract: The present invention relates to novel cephalosporin derivatives and their crystalline form, processes for preparing thereof, compositions for treating and/or preventing infectious diseases which comprise the novel cephalosporin derivatives as active components, and the intermediate compounds in the synthesis of cephalosporin derivatives and processes for producing thereof.The present invention is based on the selection of a triazolopyrimidine ring as substituent at the 3-position of the cephem skeleton, and a 2-carboxy-4,5-dihydroxyphenylmethyloxyimino moiety as substituent at the 7-position of the cephem skeleton.The compounds of the present invention containing these substituents have a wide antibacterial spectrum against Gram-negative bacteria including Pseudomonas aeruginosa and Gram-positive bacteria including methicillin-resistant Staphylococcus aureus. These compounds are extremely useful for the treatment of infectious diseases.Type: GrantFiled: November 16, 1987Date of Patent: September 12, 1989Assignee: Mochida Pharmaceutical Co., Ltd.Inventors: Kazuo Kato, Kimihiro Murakami, Hidenori Mochizuki, Ei Mochida
-
Patent number: 4864022Abstract: A compound of the formula; ##STR1## wherein R.sup.1 is an amino group which may be protected, R.sup.3 is a hydrogen atom or an optionally substituted hydrocarbon residue; Z is S, S.fwdarw.O, O or CH.sub.2, R.sup.4 is a hydrogen atom, methoxy group or formamido group, R.sup.13 is a hydrogen atom, methyl group, hydroxyl group or halogen atom and A.sym. is an optionally substituted imidazolium-1-yl group forming a condensed ring at the 2,3- or 3,4-position or a pharmaceutically acceptable salt or ester thereof is novel and has excellent antibacterial activity.Type: GrantFiled: February 28, 1986Date of Patent: September 5, 1989Assignee: Takeda Chemical Industries, Ltd.Inventors: Akio Miyake, Masahiro Kondo, Masahiko Fujino
-
Patent number: 4861769Abstract: A compound of the formula: ##STR1## wherein R.sup.1 is lower alkyl, lower alkanoyl, aryl, ar(lower)alkyl or a heterocyclic group, each of which may have suitable substituent(s),R.sup.2 is carboxy or protected carboxy,R.sup.3 is hydrogen, halogen, hydroxy, lower alkoxy, acyloxy, lower alkylthio, lower alkenyl, lower alkenylthio, lower alkynyl, heterocyclicthio or a heterocyclic group, in which lower alkylthio, lower alkenyl, lower alkenylthio, heterocyclicthio and a heterocyclic group may have suitable substituent(s),R.sup.4 and R.sup.5 are each hydrogen, halogen or arylthio,A is lower alkylene, andn is an integer of 0 or 1,and a pharmaceutically acceptable salt thereof, processes for preparation thereof and pharmaceutical composition comprising the same.Type: GrantFiled: February 12, 1986Date of Patent: August 29, 1989Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Takao Takaya, Zenzaburo Tozuka, Nobuyoshi Yasuda, Shintaro Nishimura
-
Patent number: 4857521Abstract: A cephalosporin derivative represented by the formula ##STR1## wherein R is an organic residue known on .beta.-lactam antibiotics and Q is a radical of ##STR2## dotted-line means a possible double bond, R.sub.1 is hydrogen or monovalent substituent, R.sub.2, R.sub.3 and R.sub.4 are mono-valent substituent, respectively,a salt thereof, a process for the manufacture thereof and a pharmaceutical agent comprising same.Type: GrantFiled: January 23, 1987Date of Patent: August 15, 1989Assignee: Sanwa Kagaku Kenkyusho Co., Ltd.Inventors: Masayasu Kurono, Yutaka Baba, Takahiko Mitani, Masao Onishi, Yasuaki Kondo, Kiichi Sawai
-
Patent number: 4841044Abstract: Cephalosporin derivatives represented by the general formula ##STR1## wherein R is a hydrogen atom or a lower alkyl group having 1 to 4 carbon atoms, R' is a hydrogen atom, a lower alkyl group having 1 to 4 carbon atoms, a cycloalkyl group having 5 or 6 carbon atoms or a benzyl group, or R and R' together with the nitrogen atom to which they are attached form a tetrahydropyridinyl group, a morpholinyl group or pyrroridinyl group, and the non-toxic salts thereof are disclosed. These compounds are useful as antibacterial agents.Type: GrantFiled: December 18, 1986Date of Patent: June 20, 1989Assignee: Taisho Pharmaceutical Co., Ltd.Inventors: Yoshiaki Watanabe, Chihiro Yokoo, Masami Goi, Akira Onodera, Mitsuo Murata, Hiroshi Fukushima, Minoru Taguchi, Kaoru Sota
-
Patent number: 4840945Abstract: The present invention relates to novel cephalosporin derivatives, processes for preparing thereof, compositions for preventing and/or treating infectious diseases which comprise the novel cephalosporin derivatives as active components, and the intermediate compounds in the synthesis of cephalosporin derivatives and processes for producing thereof.The present invention is based on the selection of groups containing a condensed heterocyclic ring, particularly a triazolopyrimidine ring or a thiadiazolopyrimidine ring, as substituents at the 3-position of the cephem skeleton, and of groups containing a catechol moiety, particularly a catechol carboxymethyloxyimino moiety or a catechol carboxyimino moiety, as substituents at the 7-position of the cephem skeleton.The compounds of the present invention containing the aforementioned substituents have a strong antibacterial activity against Gram-negative bacteria and also against Gram-positive bacteria including methicillin-resistant Staphylococcus aureus.Type: GrantFiled: March 10, 1986Date of Patent: June 20, 1989Assignee: Mochida Pharmaceutical Co., Ltd.Inventors: Haruo Ohnishi, Hiroshi Kosuzume, Masahiro Mizota, Yasuo Suzuki, Ei Mochida
-
Patent number: 4839351Abstract: A compound of the general formula: ##STR1## wherein R.sup.0 is hydrogen, a nitrogen-containing heterocyclic group, an acyl group or an amino-protective group; A is S, S.fwdarw.O, O or CH.sub.2 ; R.sup.4 is hydrogen, methoxy group or formamido group; R.sup.13 is hydrogen, methyl, hydroxyl or a halogen; and A is an optionally substituted condensed cyclic group formed by combining an imidazole or pyrazole ring with 5- or 6-membered nitrogen-containing aromatic heterocyclic ring to share a C-N bond with each other,or a salt or ester thereof.and a process for preparing the same and a pharmaceutical composition thereof are disclosed.Type: GrantFiled: December 12, 1986Date of Patent: June 13, 1989Assignee: Takeda Chemical Industries, Ltd.Inventors: Tatsuo Nishimura, Yoshinobu Yoshimura, Akio Miyake, Naoto Hashimoto
-
Patent number: 4839350Abstract: A class of new caphalosporin compounds (syn-isomer) is now provided, which is useful as antibacterial agent and is represented by the general formula (I) ##STR1## wherein R.sup.1 is an amino group or a protected amino group; R.sup.2 is a lower alkyl group, a carboxymethyl group or a protected carboxymethyl group; R.sup.3 is a hydrogen atom, a salt-forming cation or a carboxyl-protecting group; A is an unsubstituted or substituted phenyl group, an unsubstituted or substituted furyl group, an unsubstituted or substituted thiazolyl group or an unsubstituted or substituted 3-lower-alkylthiazolio group, and a pharmaceutically acceptable salt or ester thereof.Type: GrantFiled: April 7, 1987Date of Patent: June 13, 1989Assignees: Meiji Seika Kaisha, Ltd., Susumu MitsuhashiInventors: Kunio Atsumi, Kenji Sakagami, Yuichi Yamamoto, Takashi Yoshida, Ken Nishihata, Shinichi Kondo, Shunzo Fukatsu
-
Patent number: 4833134Abstract: Cephem compounds of the formula: ##STR1## wherein Q stands for a nitrogen atom or CH, R.sup.1 stands for a hydrogen atom or an optionally substituted lower alkyl group, R.sup.2 stands for a hydrogen atom or a lower alkyl group, A stands for a sulfur atom or NH, and n denotes an integral number ranging from 2 to 4, or salts thereof, and processes for producing them. The compounds (I) or salts thereof show not only excellent antibacterial activities against a wide range of pathogenic bacteria from gram-positive to gram-negative ones, including a variety of strains isolated clinically but also hydrophilic properties, and therefore they are excellent antibiotic substances having desirable water-solubility when used as injections.Type: GrantFiled: August 13, 1987Date of Patent: May 23, 1989Assignee: Takeda Chemical Industries, Ltd.Inventors: Shoji Kishimoto, Kiminori Tomimatsu, Michiyuki Sendai
-
Patent number: 4833242Abstract: Novel cephalosporin derivatives and salts thereof are disclosed. These compounds exhibit excellent antimicrobial activity against a wide variety of Gram-negative and Gram-positive bacteria and also have other excellent characteristics as a medicine such as stability and low toxicity. These compounds can be administered in a form of subcutaneous, intravenous or intramuscular injections.Type: GrantFiled: April 17, 1985Date of Patent: May 23, 1989Assignee: Daiichi Seiyaku Co., Ltd.Inventors: Minoru Furukawa, Hiroaki Tagawa, Takeshi Hayano, Akio Ejima
-
Patent number: 4822786Abstract: A cephalosporin compound having the formula: ##STR1## wherein R.sub.1 is a hydrogen atom, a halogen atom, a methoxy group, a substituted or unsubstituted vinyl group, or --CH.sub.2 --A wherein A is a hydrogen atom, an azido group, an acyloxy group, a carbamoyloxy group, a subsituted or unsubstituted heterocyclic group (wherein the hetrocyclic ring is a 5- or 6-membered heterocyclic ring having from 1 to 4 oxygen, nitrogen or sulfur atoms), or a substituted or unsubstituted heterocyclic thio group (wherein the heterocyclic ring is a monocyclic or bicyclic heterocyclic ring having from 1 to 5 oxygen, nitrogen or sulfur atoms), or a pharmaceutically acceptable salt thereof.Type: GrantFiled: June 17, 1987Date of Patent: April 18, 1989Assignee: Kaken Pharmaceutical Co., Ltd.Inventors: Yoshiyuki Zama, Nobuo Ishiyama, Tsuneo Saita, Takanobu Naito, Masao Hirose, Masaaki Yokoyama, Taiji Asano, Hisato Senda, Keiji Sekine, Shigeru Sanai
-
Patent number: 4810702Abstract: Cephalosporin compounds having 2-(2-aminothiazol-4-yl)-2{(1S)-carboxyethoxyimino}acetyl group on the side chain at the 7-position thereof and 1-ethylpyridinium-4-ylthiomethyl group on the side chain at the 3-position thereof or non-toxic salts thereof are excellent antibacterial agents for mammals including human. The cephalosporin derivatives have low toxicity.Type: GrantFiled: December 11, 1987Date of Patent: March 7, 1989Assignee: Meiji Seika Kaisha, Ltd.Inventors: Seiji Shibahara, Tsuneo Okonogi, Yasushi Murai, Toshiaki Kudo, Takashi Yoshida, Ken Nishihata, Shinichi Kondo
-
Patent number: 4800199Abstract: Cephalosporins active as antibacterial agents, and processes for synthesis of such agents, are disclosed.Type: GrantFiled: October 20, 1986Date of Patent: January 24, 1989Assignee: American Cyanamid CompanyInventors: Robert Babine, Ving J. Lee
-
Patent number: 4797395Abstract: A compound of the formula ##STR1## wherein (1) R.sub.1 is a lower alkyl group of 2 to 6 carbon atoms or a cycloalkyl group of 5 to 7 carbon atoms and R.sub.2 is a cycloalkyl group of 5 to 7 carbon atoms or a lower alkyl group of 1 to 3 carbon atoms which is substituted by a cycloalkyl group of 5 to 7 carbon atoms or by a phenyl group, or (2) R.sub.1 is a cycloalkyl group of 5 to 7 carbon atoms and R.sub.2 is a lower alkyl group of 1 to 5 carbon atoms, or a pharmaceutically acceptable salt thereof, processes for preparing the same and a pharmaceutical composition thereof are provided. The compound can orally be applied as antibiotics having improved bioavailability.Type: GrantFiled: July 18, 1986Date of Patent: January 10, 1989Assignee: Takeda Chemical Industries, Ltd.Inventors: Akio Miyake, Yoshinobu Yoshimura, Mitsuo Numata
-
Patent number: 4786633Abstract: A cephalosporin compound of the formula: ##STR1## wherein: R.sup.2 is a group of the formula: ##STR2## R.sup.4 is a lower alkenyl group, a lower alkyl group or a lower alkyl group substituted with a member selected from the group consisting of cyano, lower alkylthio, 2-(lower alkyl)-1,3,4-thiadiazol-5-yl, carbamoyl, thiocarbamoyl, and N-lower alkyl(thiocarbamoyl) andR.sup.5 and R.sup.6 are each a hydrogen atom or a lower alkyl group, or a pharmaceutically acceptable salt thereof, is disclosed. These compounds have antimicrobial activity.Type: GrantFiled: June 3, 1987Date of Patent: November 22, 1988Assignee: Tanabe Seiyaku Co., Ltd.Inventors: Mitsuyoshi Wagatsuma, Toyonari Oine, Totaro Yamaguchi
-
Patent number: 4784995Abstract: A cephalosporin compound of the formula: ##STR1## wherein R.sup.1 is a protected or unprotected amino group;either one of R.sup.2 and R.sup.3 is a substituted or unsubstituted lower alkylthio group; sulfamoyl group; a lower alkylsulfonyl group; sulfo group; a substituted or unsubstituted amino group; a lower alkyl group; a lower alkyl group having a substituent selected from a lower alkylthio group, amino group and an acylamino group; a halogen atom; carboxy group or a lower alkoxy group; andthe other one of R.sup.2 and R.sup.3 is hydrogen atom; carbamoyl group; a substituted or unsubstituted amino group; a lower alkyl group or a hydroxy-lower alkyl group; orR.sup.2 and R.sup.3 are combined together to form a lower alkylene group;or a salt thereof and processes for preparing the same are disclosed. The cephalosporin compound (I) is useful as an antimicrobial agent.Type: GrantFiled: June 8, 1987Date of Patent: November 15, 1988Assignee: Tanabe Seiyaku Co., Ltd.Inventors: Toyonari Oine, Mitsuyoshi Wagatsuma, Totaro Yamaguchi
-
Patent number: 4761410Abstract: The invention relates to antimicrobial compounds of the formula: ##STR1## wherein R.sup.1 is amino or a protected amino group,R.sup.2 is carboxy or a protected carboxy group andR.sup.3 is thiadiazolylthiomethyl or thiadiazolylthiomethyl substituted with lower alkyl, and pharmaceutically acceptable salts thereof.Type: GrantFiled: December 31, 1985Date of Patent: August 2, 1988Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Takao Takaya, Kazuo Sakane, Kenzi Miyai, Teruaki Matuo
-
Patent number: 4761409Abstract: A cephem derivative represented by the general formula ##STR1## wherein R.sup.1 represents hydrogen or methyl, R.sup.2 represents carboxyl or esterified carboxyl, and n represents 0 or 1, or a pharmaceutically acceptable salt thereof; intermediates for the cephem derivative or salt thereof; processes for producing these compounds; and a pharmaceutical composition and method for preventing or treating bacterial infectious diseases, wherein the cephem derivative or the salt thereof is used.Type: GrantFiled: August 5, 1985Date of Patent: August 2, 1988Assignee: Sumitomo Pharmaceuticals Company, LimitedInventors: Hirotada Yamada, Naruhito Masai, Shinji Ueda, Takao Okuda, Masuhiro Kato, Masatomo Fukasawa, Masataka Fukumura
-
Patent number: 4760059Abstract: The rectal absorption of the beta-lactam antibiotic ceftriaxone in a solid dosage form is enhanced with chenodeoxycholic acid or its sodium salt, in the presence of a carrier consisting of a mixture of two or more glycerides of C.sub.12 to C.sub.18 fatty acids.Type: GrantFiled: August 5, 1985Date of Patent: July 26, 1988Assignee: Hoffmann-La Roche Inc.Inventors: Charanjit Behl, Joel Unowsky
-
Patent number: 4758556Abstract: Cephem derivatives of the general formula ##STR1## in which the R.sub.2 O group is in the syn-position, a process for their manufacture and pharmaceutical formulations which are active against bacterial infections and contain these compounds.Type: GrantFiled: March 30, 1978Date of Patent: July 19, 1988Assignee: Hoechst AktiengesellschaftInventors: Walter Durckheimer, Dieter Bormann, Eberhard Ehlers, Elmar Schrinner, Rene Heymes
-
Patent number: 4758557Abstract: Cephalosporin compounds represented by the following formula (I) and pharmaceutically acceptable salts thereof have a broad bactericidal spectrum against various pathogenic bacteria including Psuedomonas aeruginosa and are useful as bactericidal remedies for pathogenic diseases of human and animals: ##STR1## wherein A represents an unsubstituted or substituted pyridylthio group of a formula (I-1); ##STR2## or an unsubstituted or substituted pyridiniumthio group of a formula (I-2): ##STR3## or an unsubstituted or substituted pyridinium group of a formula (I-3); ##STR4## or a 5- or 6-membered heterocyclicthio or bicycloheterocyclicthio group of a formula (I-4):--S--Het (I-4).Type: GrantFiled: June 9, 1986Date of Patent: July 19, 1988Assignee: Meiji Seika Kaisha, Ltd.Inventors: Takashi Tsuruoka, Katsuyoshi Iwamatsu, Kiyoaki Katano, Hiroko Ogino, Ryoichi Okamoto, Takashi Yoshida, Masaji Sezaki, Fumio Kai, Shigeharu Inoue, Shinichi Kondo
-
Patent number: 4749694Abstract: Novel lysine esters used as absorption enhancing agents for gastrointestinally and rectally administered drugs. Also provided are processes for preparation of said lysine ester compounds as well as pharmaceutical formulations and methods for their use as absorption enhancing agents.Type: GrantFiled: April 26, 1984Date of Patent: June 7, 1988Assignee: Merck & Co., Inc.Inventors: Joseph A. Fix, Stefano A. Pogany
-
Patent number: 4748170Abstract: An antibacterial 7beta-(carboxyalkenoyl)amino-3-cephem-4-carboxylic acid represented by the following formula: ##STR1## (wherein R is aryl or a heterocyclic group; R.sup.1 is hydrogen or halogen;R.sup.2 is a single bond, alkylene, or thiaalkylene;R.sup.3 is a hydrogen atom or carboxy modifying group;R.sup.4 is hydrogen or methoxy;R.sup.5 is hydrogen or a 3-substituent of cephalosporins;R.sup.6 is a hydrogen atom or carboxy modifying group; andX is oxygen, sulfur, or sulfinyl)a pharmaceutical composition containing the same, and a method for treating a bacterial infection with the same.Type: GrantFiled: February 20, 1986Date of Patent: May 31, 1988Assignee: Shionogi & Co., Ltd.Inventor: Yoshio Hamashima
-
Patent number: 4748163Abstract: Antibacterially active and animal growth-promoting novel .beta.-lactam compounds of the formula ##STR1## in which R.sup.1 represents the radical ##STR2## Y representing N or CR.sup.9, or Y--R.sup.7 representing >C.dbd.O or >C.dbd.N--R.sup.7,Z representing O, S, or NR.sup.10, andR.sup.2 represents hydrogen or a protective group.Type: GrantFiled: February 21, 1986Date of Patent: May 31, 1988Assignee: Bayer AktiengesellschaftInventors: Gunter Schmidt, Hans-Joachim Zeiler, Karl G. Metzger
-
Patent number: 4748172Abstract: Cephalosporin compounds substituted in the 7-position by a 2-(5- or 6-membered heterocyclic)-2-oximinoacetylamino group and in the 3-position with an imidazolo, oxazolo or thiazolopyridinium-methyl group are broad spectrum antibiotics highly effective in combating bacterial infections of gram-negative and gram-positive microorganisms. The cephalosporins are best prepared by reacting a silylated 7-[2-(heterocyclic)-2-oximinoacetylamino-3-iodomethyl-3-cephem-4-carboxyli c acid with an imidazolopyridine, an oxazolopyridine or a thiazolopyridine. Pharmaceutical formulations comprising a compound of the invention and a method for treating bacterial infections comprising their use are also provided.Type: GrantFiled: January 12, 1987Date of Patent: May 31, 1988Assignee: Eli Lilly and CompanyInventor: Allen S. Katner
-
Patent number: 4735938Abstract: Antibiotically active penicillins and cephalosporins of the formula ##STR1## in which Z is hydrogen or lower alkoxy,n is 1 or 2,Y, in the form of the free acid, is ##STR2## X is --S--, --n--, --SO-- or --SO.sub.2 --, T is an organic radical, hydrogen or halogen,A is hydroxyl, optionally substituted alkyl, a substituted or unsubstituted phenyl ring, an optionally substituted polycyclic aromatic ring, an optionally substituted 5-membered or 6-membered heterocyclic ring with nitrogen, oxygen and/or sulphur as hetero atoms in the ring, or an optionally substituted polycyclic heterocyclic ring,or non-toxic pharmaceutically tolerated salts thereof.Type: GrantFiled: July 10, 1986Date of Patent: April 5, 1988Assignee: Bayer AktiengesellschaftInventors: Michael Boberg, Karl G. Metzger, Hans-Joachim Zeiler
-
Patent number: 4734407Abstract: Antibacterially active and animal growth-regulating novel .beta.-lactam compounds of the formula ##STR1## in which R.sup.1 represents an optionally substituted radical of the formula ##STR2## Z represents oxygen, sulphur or --N--R.sup.Type: GrantFiled: March 10, 1986Date of Patent: March 29, 1988Assignee: Bayer AktiengesellschaftInventors: Gunter Schmidt, Hans-Joachim Zeiler, Karl G. Metzger
-
Patent number: 4734408Abstract: The crystalline sulfate dihydrate, dimethylacetamide hydrate and dimethylformamide hydrate solvates of the antibiotic syn-7-[2-(2-aminothiazol-4-yl)-2-methoxyiminoacetamido]-3-(3-methyl-3H-imi dazolo[4,5-c]pyridinium-5-ylmethyl)-3-cephem-4-carboxylate are provided.Type: GrantFiled: December 17, 1986Date of Patent: March 29, 1988Assignee: Eli Lilly and CompanyInventor: Allen S. Katner, deceased
-
Patent number: 4734409Abstract: Disclosed herein are a cephalosporin derivative represented by the formula (I): ##STR1## wherein R.sup.1 represents a halogenoalkyl group, a salt and ester thereof, a process for producing the same, and a pharmaceutical composition and an antibacterial agent comprising the same.Type: GrantFiled: February 15, 1985Date of Patent: March 29, 1988Assignee: Kureha Kagaku Kogyo Kabushiki KaishaInventors: Shigeaki Muto, Chikao Yoshikumi, Takao Furusho, Isamu Motokawa, Yoko Onishi, Akihiko Kanno, Takayoshi Fujii, Takao Ando
-
Patent number: 4732753Abstract: Suppositories containing as the active substance a therapeutically effective amount of ceftriaxone, a pharmaceutically compatible salt thereof or a hydrate of one of these compounds, a stabilizer consisting of a mono-, di- or triglyceride of a C.sub.12 -C.sub.18 -fatty acid or of a mixture of such glycerides, a potentiator consisting of an aliphatic C.sub.2 -C.sub.18 -fatty acid, a mono-, di- or triglyceride of a C.sub.2 -C.sub.12 -fatty acid, a partial ester or complete ester of propylene glycol, polyethylene glycol or a carbohydrate with a C.sub.2 -C.sub.12 -fatty acid, a pharmaceutically compatible ester or ether thereof or of a mixutre of the said potentiators and, if desired, customary therapeutically inert adjuvants for suppositories, and their manufacture are described. These have valuable antimicrobial properties.Type: GrantFiled: February 11, 1985Date of Patent: March 22, 1988Assignee: Hoffmann-La Roche Inc.Inventor: Walter Fuller
-
Patent number: 4731360Abstract: Acylcarnitine used as a nasal, buccal, sublingual and vaginal drug absorption enhancing vehicle for poorly absorbed drugs.Type: GrantFiled: August 16, 1985Date of Patent: March 15, 1988Assignee: Merck & Co., Inc.Inventors: Jose Alexander, A. J. Repta, Joseph A. Fix
-
Patent number: 4729989Abstract: Choline ester salts are used as drug absorption enhancing agents for orally and rectally administered drugs.Type: GrantFiled: June 28, 1985Date of Patent: March 8, 1988Assignee: Merck & Co., Inc.Inventors: Jose Alexander, Joseph A. Fix
-
Patent number: 4729992Abstract: A compound of the formula: ##STR1## or a pharmaceutical acceptable salt thereof, processes for preparing the same and a pharmaceutical composition containing the compound or the salt thereof mentioned above are provided. The compound has antibiotic activity and has improved absorbability.Type: GrantFiled: April 19, 1985Date of Patent: March 8, 1988Assignee: Tatsuo Chemical Ind., Ltd.Inventors: Tatsuo Nishimura, Yoshinobu Yoshimura, Mitsuo Numata