623564-46-5Relevant academic research and scientific papers
Bicyclic 6-alkylidene-penems as class-D beta-lactamases inhibitors
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Page/Page column 18, (2010/11/25)
This invention relates to certain bicyclic 6-alkylidene penems which act as a inhibitor of class-D enzymes. β-Lactamases hydrolyze β-lactam antibiotics, and as such serve as the primary cause of bacterial resistance. The compounds of the present invention when combined with β-lactam antibiotics will provide an effective treatment against life threatening bacterial infections. In accordance with the present invention there are provided compounds of general formula I or a pharmaceutically acceptable salt or in vivo hydrolyzable ester R5 thereof: wherein: One of A and B denotes hydrogen and the other an optionally substituted fused bicyclic heteroaryl group; and X═O or S.
Selective hydrolysis of ethyl 5,6-dihydro-4H-pyrrolo[1,2-b]pyrazole-2- carboxylate and ethyl 5,6-dihydro-4H-pyrrolo[1,2-b]pyrazole-3-carboxylate as a key step in the large-scale synthesis of bicyclic heteroaryl carboxyaldehydes
Nikitenko,Winkley,Zeldis,Kremer,Chan,Strong,Jennings,Jirkovsky,Blum,Khafizova,Grosu,Venkatesan
, p. 712 - 716 (2012/12/22)
The isomeric mixture of ethyl 5,6-dihydro-4H-pyrrolo[1,2-b]-pyrazole-2- and -3-carboxylates (14 and 15), derived from a proline meso-ionic synthon, demonstrated remarkably different stabilities towards alkaline hydrolysis. On that basis, a non-chromatographic, highly efficient method for their large-scale separation was developed. The desired isomer 14 was converted into 5,6-dihydro-4H-pyrrolo[1,2-b]pyrazole-2-carbaldehyde, a key intermediate in the synthesis of bicyclic heteroaryl-substituted 6-alkylidene penems.
Process for preparing 6-alkylidene penem derivatives
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, (2008/06/13)
The present invention provides a process of making compounds of formula I, which are useful for the treatment of bacterial infection or disease.
Process for synthesizing beta-lactamase inhibitor intermediates
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Page 16-17, (2008/06/13)
There is provided a process for the preparation of bicyclicheteroaryl carboxaldehydes having the structural Formula I where X and Y are defined in the specification The bicyclic heteroaryl carboxaldehydes are useful as intermediates in the preparation of β-lactamase inhibitors.
BICYCLIC 6-ALKYLIDENE-PENEMS AS ?-LACTAMASES INHIBITORS
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Page/Page column 67-68, (2008/06/13)
The present invention provides a compound of Formula (I), pharmaceutical compositions and the use thereof for the treatment of bacterial infection or disease in a patient in need thereof.
PROCESS FOR PREPARING 6-ALKYLIDENE PENEM DERIVATIVES
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Page/Page column 96, (2010/02/07)
The present invention provides a process of making compounds of Formula (I), which are useful for the treatment of bacterial infection or disease.
