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EP0300423A2
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EP
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Cephalosporin compound, method of its production and composition for prevention and treatment of bacterial infectious diseases
Assignee: Kyoto Pharmaceutical Industries Ltd
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Filing: 1988-07-19
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Granted: —
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Expires: 2008-07-19
Abstract
Abstract A cephalosporin compound represented by the formula (I): wherein R' represents a hydrogen atom or a-amino acid residue (ester bonding), its ester, or its pharmacologically acceptable salt, which is useful as a preventive, therapeutic drug for bacterial infections as well as an intermediate for the synthesis of other cephalosporin compounds, a method of its production, a pharmaceutical composition for prevention and treatment of bacterial infectious diseases and method for the treatment of bacterial infectious diseases.
Inventors
- 👤 Susumu Nishizawa
- 👤 Hiroyuki Muro
- 👤 Masayasu Kasai
- 👤 Satoru Hatano
- 👤 Syouzi 202 Nakagawa Co.Op. 5 Kamiya
- 👤 Nobuharu Kakeya
- 👤 Kazuhiko Kitao
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-11-09 20:57
CPC Classifications
C; C07; C07D; C07D501/00; C07D501/14; C07D501/16; C07D501/20; C07D501/24; C07D501/36
Claims Analysis
Total Claims: 10
Claim 1
Independent Claim
28 words
(1) A cephalosporin compound represented by the formula (I): wherein R' represents a hydrogen atom or a-amino acid residue (ester bonding), its ester, or its pharmacologically acceptable salt.
Claim 2
Dependent Claim
15 words
(2) The compound as claimed in Claim (1) wherein R 1 is a hydrogen atom.
Claim 3
Dependent Claim
18 words
(3) The compound as claimed in Claim (1) wherein R 1 is an a-amino acid residue (ester bonding).
Claim 4
Dependent Claim
19 words
(4) The compound as claimed in Claim (3) wherein an a-amino acid residue is a neutral amino acid residue.
Claim 5
Dependent Claim
19 words
(5) The compound as claimed in Claim (1) wherein a carboxy group in the formula (I) forms as ester.
Claim 6
Dependent Claim
50 words
(6) The compound as claimed in Claim (5) wherein the hydrogen atom of the carboxy group in the formula (1) is substituted by an alkyl group, phthalxyl 5-methyl-1,3-dioxol-2-on-4-ylmethyl or a group represented by the formula: wherein R2 represents an alkyl group and R3 represents an alkyl group or alkoxy group.
Claim 7
Dependent Claim
34 words
(7) The compound as claimed in Claim (1) which is chosen from the compounds listed below. * 7-D-(-)Mandelamido-3-(1,2,4-thiadiazol-5-yl)thiomethyl-3-cephem-4-carboxylic acid * Pivaloyloxymethyl 7-D-(-)mandelamido-3-(1,2,4-thiadiazol-5-yl)thiomethyl-3-cephem-4-carboxylate * Pivaloyloxymethyl 7-[D-O-(L-alanyl)mandelamido]-3-[(1,2,4-thiadiazole-5-yl)thiomethyl]-3-cephem-4-carboxylate hydrochloride * (5-Methyl-1,3-dioxol-2-on-4-yl)methyl 7-[D-O-(L-alanyl)mandelamido]-3-[(1,2,4-thiadiazol-5-yl)thiomethyl]-3-cephem-4-carboxylate hydrochloride * 1-Ethoxycarbonyloxyethyl 7-[D-O-(L-alanyl)mandelamido]-3-[(1,2,4-thiadiazol-5-yl)thiomethyl]-3-cephem-4-carboxylate hydrochloride
Claim 8
Dependent Claim
167 words
(8) The production method for a cephalosporin compound represented by the formula (I): , its ester, or its pharmacologically acceptable salt, characterized by: (a) reaction between a compound represented by the formula (II): or the formula (II-1): and a compound represented by the formula (III): , its ester or its salt; (b) nucleophilic substitution reaction of 3-position Y of a compound represented by the formula (VI): , its ester or its salt, with 1,2,4-thiadiazol-5-thiol; (c) reaction between a compound represented by the formula (I-1): . its ester or its salt and a compound represented by the formula (VIII): ; or (d) reaction between a compound represented by the formula (1-2): and a compound represented by the formula (V): In the above formulae, R 1 represents a hydrogen atom or a-amino acid residue (ester bonding); R 4 represents a group introduced by the esterification; R 5 represents an a-amino acid residue; X represents a carboxy-reactive group such as halogen, alkylsulfonate or arylsulfonate; and Y represents a nucleophilic residue.
Claim 9
Dependent Claim
43 words
(9) A composition for prevention and treatment of bacterial infections, comprising an effective amount of at least one compound selected from the cephalosporin compound as claimed in Claim (1), its ester or its pharmacologically acceptable salt, and one or more pharmaceutically acceptable additives.
Claim 10
Dependent Claim
32 words
(10) A method for treatment of bacterial infectious diseases caused by Gram-positive bacteria or Gram-negative bacteria, which comprises administering of an effective amount of a cephalosporin compound as claimed in Claim 1.
References Cited (Backward Citations)
No citation records indexed.
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