John Berge - Harlow, GB Richard Jarvest - Stevenage, GB Catherine Simone Victoire Frydrych - Harlow, GB Joseph Guiles - Lafayette CO, US Jian Qiu - Longmont CO, US Theodore M. Tarasow - Longmont CO, US
Assignee:
Replidyne, Inc. - Louisville CO
International Classification:
A61K 31/4709 C07D 215/38 C07D 409/12
US Classification:
514312, 514313, 546153, 546159
Abstract:
Novel substituted thiophenes that are inhibitors of bacterial methionyl t-RNA synthetase (MRS) are disclosed. Also disclosed are method for their preparation and their use in therapy as anti-bacterial agents.
The present invention provides methods for identifying (3-amino-2-oxo-azetidin-1-yl) acetic acid derivatives with anti-PBP2a activity. The method involves the selection of RNA biocatalysts that promote the formation of (3-amino-2-oxo-azetidin-1-yl) acetic acid derivatives with anti-PBP2a activity from component reactants. The invention also provides novel (3-amino-2-oxo-azetidin-1-yl) acetic acid derivatives with anti-PBP2a activity identified by these methods. The invention also provides RNA biocatalysts that are capable of catalyzing the formation of (3-amino-2-oxo-azetidin-1-yl) acetic acid derivatives from component reactants.
Bruce Eaton - Boulder CO, US Theodore Tarasow - Longmont CO, US
Assignee:
INVENUX, INC. - DENVER CO
International Classification:
C12Q001/68 C07H021/04
US Classification:
435/006000, 536/023100
Abstract:
This invention discloses a method for coevolving products from two or more reactants, along with the nucleic acid that can facilitate the reaction for making the products. The invention further discloses the products and facilitating nucleic acids produced by said method.
Nebojsa Janjic - Boulder CO, US Ian Critchley - Lafayette CO, US Joseph Guiles - Lafayette CO, US Theodore Tarasow - Longmont CO, US
International Classification:
A61K031/47 A61K031/4709
US Classification:
514/312000, 514/394000, 514/313000
Abstract:
Disclosed is a pharmaceutical composition comprising an aminoacyl tRNA synthetase inhibitor and another antibacterial agent, including another aminoacyl tRNA synthetase inhibitor.
Substituted Thiophenes With Antibacterial Activity
Novel substituted thiophenes that are inhibitors of bacterial methionyl t-RNA synthetase (MRS) are disclosed. Also disclosed are method for their preparation and their use in therapy as anti-bacterial agents.
Transition Metal Catalyzed Cross-Coupling Of 1-Halo-1-Haloalkene Compounds
Joseph W. Guiles - Lafayette CO, US Jian Qiu - Longmont CO, US Theodore M. Tarasow - Longmont CO, US
Assignee:
REPLIDYNE, INC. - Louisville CO
International Classification:
C07D 333/28
US Classification:
549 78
Abstract:
Methods for introducing a 1-halo-1-haloalkene compound onto an aromatic or heteroaromatic ring are provided, including processes for the production of certain 1-halovinyl aryl or heteroaryl derivatives in which the 1-halovinyl group is either 1-fluoro or 1-chlorovinyl and the aromatic species phenyl or thiophene, the processes including coupling an arylmagnesium species with a dihalo olefin in the presence of a nickel or iron catalyst.
Transition Metal Catalyzed Cross-Coupling Of 1-Halo-1-Haloalkene Compounds
Joseph W. Guiles - Lafayette CO, US Jian Qiu - Longmont CO, US Theodore M. Tarasow - Longmont CO, US
Assignee:
Replidyne, Inc. - Louisville CO
International Classification:
C07D 333/28 C07C 43/225
US Classification:
549 78, 568656
Abstract:
Methods for introducing a 1-halo-1-haloalkene compound onto an aromatic or heteroaromatic ring are provided, including processes for the production of certain 1-halovinyl aryl or heteroaryl derivatives in which the 1-halovinyl group is either 1-fluoro or 1-chlorovinyl and the aromatic species phenyl or thiophene, the processes including coupling an arylmagnesium species with a dihalo olefin in the presence of a nickel or iron catalyst.