2-(pyrazol-3-yl)carbapenem derivatives

Organic compounds -- part of the class 532-570 series – Organic compounds – Heterocyclic carbon compounds containing a hetero ring...

Reexamination Certificate

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Reexamination Certificate

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07045619

ABSTRACT:
A compound of formula (I):whereinRαis hydrogen, optionally substituted (C1-6)alkyl or optionally substituted aryl;Rβis hydrogen, optionally substituted (C1-6)alkyl or optionally substituted aryl; orRαand Rβtogether form an optionally substituted 5 or 6 membered heterocyclic ring with or without additional heteroatoms;R1is (C1-6)alkyl which is unsubstituted or substituted by fluoro, a hydroxy group which is optionally protected by a removable hydroxy protecting group, or by an amino group which is optionally protected by a removable amino protecting group;R2is hydrogen or methyl; and—CO2R3is carboxy or a carboxylate anion or the group R3is a removable carboxy protecting group. This invention also relates to processes for its preparation, intermediates and pharmaceutical compositions comprising compounds of formula (I). Compounds of formula (I) which include pharmaceutically acceptable salts or pharmaceutically acceptable in vivo hydrolysable esters thereof have a broad spectrum of anti-bacterial activity and show good stability towards DHP-1.

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Chemical Abstracts 114:247039u Preparation of 1-azabicyclo[3.2.0]hept-2-ene-2-=carboxylic acid compounds antimicrobial agents.
Chemistry in Action, Michael Freemantle (MacMillan), p 537.
Daniels, T.C. et al. Textbook of Organic Medicinal and Pharmaceutical Chemistry, ed. by Wilson, C.O. et al. (Lippinott Co., Philadelphia), pp. 31-33, 1997.
Hawley's Condensed Chemical Dictionary, Twelfth Edition, pp. 21-22.
Dewent WPI Prontant for JP92040357.

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