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1. (WO2001004127) VINYLPYRROLIDINONE DERIVATIVES WITH SUBSTITUTED THIAZOLE RING
Latest bibliographic data on file with the International Bureau   

Pub. No.: WO/2001/004127 International Application No.: PCT/EP2000/006151
Publication Date: 18.01.2001 International Filing Date: 01.07.2000
IPC:
C07D 501/00 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
501
Heterocyclic compounds containing 5-thia-1-azabicyclo [4.2.0] octane ring systems, i.e. compounds containing a ring system of the formula: , e.g. cephalosporins; Such ring systems being further condensed, e.g. 2,3-condensed with an oxygen-, nitrogen- or sulfur-containing hetero ring
Applicants:
ANGEHRN, Peter [CH/CH]; CH (UsOnly)
HEBEISEN, Paul [CH/CH]; CH (UsOnly)
HEINZE-KRAUSS, Ingrid [DE/DE]; DE (UsOnly)
PAGE, Malcolm [GB/CH]; CH (UsOnly)
F. HOFFMANN-LA ROCHE AG [CH/CH]; 124 Grenzacherstrasse CH-4070 Basle, CH (AllExceptUS)
Inventors:
ANGEHRN, Peter; CH
HEBEISEN, Paul; CH
HEINZE-KRAUSS, Ingrid; DE
PAGE, Malcolm; CH
Agent:
KJELLSAA-BERGER, Hanny; 124 Grenzacherstrasse CH-4070 Basle, CH
Priority Data:
99113120.207.07.1999EP
Title (EN) VINYLPYRROLIDINONE DERIVATIVES WITH SUBSTITUTED THIAZOLE RING
(FR) DERIVES DE VINYLPYRROLIDINONE A CYCLE THIAZOLE SUBSTITUE
Abstract:
(EN) The invention is concerned with cephalosporin derivatives of general formula (I) wherein X is chlorine, bromine, fluorine, trifluoromethyl, methyl, carboxy or hydroximethyl; R1 is hydrogen or lower alkanoyl; R2 is hydrogen or an in vivo cleavable group; Y1 is a group -CHR3-; Y2 is one of the groups -CHR3-, -CHR3-CHR3- and -CHOH-CHR3-; R3 is the same or different and selected from hydrogen, hydroxy-lower alkyl and amino-lower alkyl, and readily hydrolyzable ester of compounds of formula I, as well as pharmaceutically acceptable salts of said compounds of formula I and of their esters and salts, with the manufacture of compounds aforesaid; and with their use as pharmaceutically active substances in the treatment and prophylaxis of infectious diseases.
(FR) L'invention concerne des dérivés de céphalosporine représentés par la formule générale (I), dans laquelle X représente chlore, brome, fluor, trifluorométhyle, méthyle, carboxy ou hydroxyméthyle ; R1 désigne hydrogène ou un alcanoyle inférieure ; R2 désigne hydrogène ou un groupe clivable in vivo; Y1 représente un groupe -CHR3- ; Y2 désigne l'un des groupes -CHR3-, -CHR3-CHR3- et - CHOH-CHR3- ; chaque R3 étant identique ou différent et choisi parmi hydrogène, hydroxy-alkyle inférieur et amino-alkyle inférieur. L'invention concerne également un ester rapidement hydrolysable de ces composés de formule I, des sels pharmaceutiquement acceptables desdits composés de formule I et des esters et des sels de ceux-ci. L'invention concerne, en outre, la fabrication des composés susmentionnés, et leur utilisation comme substances pharmaceutiquement actives dans le traitement et la prophylaxie de maladies infectieuses.
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Designated States: AE, AL, AM, AT, AU, AZ, BA, BB, BG, BR, BY, CA, CH, CN, CU, CZ, DE, DK, EE, ES, FI, GB, GD, GE, GH, GM, HR, HU, ID, IL, IN, IS, JP, KE, KG, KP, KR, KZ, LC, LK, LR, LS, LT, LU, LV, MA, MD, MG, MK, MN, MW, MX, NO, NZ, PL, PT, RO, RU, SD, SE, SG, SI, SK, SL, TJ, TM, TR, TT, UA, UG, US, UZ, VN, YU, ZA, ZW
African Regional Intellectual Property Organization (ARIPO) (GH, GM, KE, LS, MW, MZ, SD, SL, SZ, TZ, UG, ZW)
Eurasian Patent Office (AM, AZ, BY, KG, KZ, MD, RU, TJ, TM)
European Patent Office (EPO) (AT, BE, CH, CY, DE, DK, ES, FI, FR, GB, GR, IE, IT, LU, MC, NL, PT, SE)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, GW, ML, MR, NE, SN, TD, TG)
Publication Language: English (EN)
Filing Language: English (EN)