- SUBSTITUTED IMIDAZOLE CARBOXAMIDES AND THEIR USE IN THE TREATMENT OF MEDICAL DISORDERS
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The invention provides substituted imidazole carboxamides and related compounds, compositions containing such compounds, medical kits, and methods for using such compounds and compositions to treat a medical disorder, e.g., cancer, lysosomal storage disorder, neurodegenerative disorder, inflammatory disorder, in a patient.
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Paragraph 00454
(2021/04/01)
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- Coupling process and intermediates useful for preparing cephalosporins
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The process of the present invention and the preparation of the compound of the present invention are illustrated in the following reaction schemes. Except where otherwise indicated, in the reaction schemes and discussion that follow, substituents R1, R2, R3, L, A1, A2 and X are as defined above unless otherwise described. This invention relates to a novel process for the preparation of 3-cyclic-ether-substituted cephalosporins of formula I wherein the group CO2R1 is a carboxylic acid or a carboxylate salt and R2 has the formula: wherein A1 is selected from the group consisting of C6-10aryl, C1-10heteroaryl and C1-10heterocyclyl; A2 is selected from the group consisting of hydrogen, C1-6alkyl, C3-10cycloalkyl, C6-10aryl, C1-6alkyl(CO)(C1-6)alkyl-O—, HO(CO)(C1-6)alkyl, mono-(C6-10aryl)(C1-6alkyl), di-(C6-10aryl)(C1-6alkyl) and tri-(C6-10aryl)(C1-6alkyl); from a zwitterionic compound of formula II; or from a compound of formula V: wherein R2 is as defined above and R3 is para-nitrobenzyl or allyl. The invention also relates to the preparation of the above compounds of formulae II and V.
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- Process and ester derivatives useful for preparation of cephalosporins
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This invention relates a process for preparing a compound of formula (I) wherein R1 is para-nitrobenzyl or allyl; and X is halo, which is useful to prepare 3-cyclic-ether-substituted cephalosporins, from trimethylphosphinic compounds. This invention also relates to compounds useful in such process.
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- Cephalosporins and homologues, preparations and pharmaceutical compositions
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β-Lactam antibiotics of formula (I) or a salt thereof, wherein R1 is hydrogen, methoxy or formamido; R2 is an acyl group; CO2 R3 is a carboxy group or a carboxylate anion, or R3 is a readily removable
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