1830-42-8Relevant academic research and scientific papers
SHORT-ACTING BENZODIAZEPINE DERIVATIVES, PREPARATION METHOD THEREFOR, AND USE THEREOF
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, (2018/11/21)
The present invention relates to a benzodiazepine derivative of Formula I as a short-acting anesthetic, a pharmaceutical composition comprising the same, a kit comprising the same, a preparation method thereof, an method of anesthesia using the same and use thereof in the manufacture of an anesthetic medicament.
SHORT-ACTING BENZODIAZEPINES
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Page/Page column 11-12, (2008/06/13)
It has now been found that compounds of the present invention as described in Benzodiazepine derivatives of Formula (I) containing a carboxylic ester moiety and thereby capable of being inactivated by nonspecific tissue esterases in an organ-independent elimination mechanism and thereby providing a more predictable and reproducible pharmacodynamic profile. The compounds of the present invention are suitable for therapeutic purposes, including sedative-hypnotic, anxiolytic, muscle relaxant and anticonvulsant purposes and are useful to be administered intravenously in the following clinical settings: preoperative sedation, anxiolysis, and amnestic use for perioperative events; conscious sedation during short diagnostic, operative or endoscopic procedures; as a component for the induction and maintenance of general anesthesia, prior and/or concomitant to the administration of other anesthetic agents; ICU sedation.
QUINOLINONE DERIVATIVES AS INHIBITORS OF C-FMS KINASE
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Page/Page column 42-43, (2010/02/10)
The invention is directed to compounds of Formulae I and II: (I) (II) wherein R1, R2, R3, R5, R6, Y1, Y2, Y3, Y4 and X are set forth in the specification, as well as solvates, hydrates, tautomers or pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase.
ARYL SULFONAMIDES
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Page 45-46, (2008/06/13)
Compounds are provided that act as potent antagonists of the CCR9 receptor, and which have been further confirmed in animal testing for inflammation, one of the hallmark disease states for CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR9-mediated diseases, and as controls in assays for the identification of CCR9 antagonists.
Relating the structure, activity, and physical properties of ultrashort-acting benzodiazepine receptor agonists
Pacofsky, Gregory J.,Stafford, Jeffrey A.,Cox, Richard F.,Cowan, Jill R.,Dorsey Jr., George F.,Gonzales, Stephen S.,Kaldor, Istvan,Koszalka, George W.,Lovell, George G.,McIntyre, Maggie S.,Tidwell, Jeffrey H.,Todd, Dan,Whitesell, Graham,Wiard, Robert P.,Feldman, Paul L.
, p. 3219 - 3222 (2007/10/03)
The ultrashort-acting benzodiazepine (USA BZD) agonists reported previously have been structurally modified to improve aqueous solubility. Lactam-to-amidine modifications, replacement of the C5-haloaryl ring, and annulation of heterocycles are presented. These analogues retain BZD receptor potency and full agonism profiles.
The synthesis of substituted 2-aminophenyl heterocycic ketones
Fryer,Zhang,Rios
, p. 985 - 992 (2007/10/02)
The synthesis of substituted 2-aminophenyl heterocyclic ketones, key intermediates to the preparation of 1,4-benzodiazepines has been achieved in one step and in good, yield from the corresponding anthranilic acid, by treatment with heterocyclic lithium reagents and chlorotrimethylsilane.
1-POLYHALOGENOALKYL-2-OXO-1,3-DIHYDRO-2H-1,4-BENZODIAZEPINES
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, (2014/02/11)
This invention relates to 2-oxo-1,3-dihydro-2H-1,4-dibenziodiazepines, and the 4-N-oxides thereof, having a polyfluoroalkyl radical attached at the 1-position thereof, to their use as muscle relaxants, as sedatives, an anticonvulsants, and as anti-anxiety agents and to the intermediates useful in the preparation thereof. The compounds may be prepared by N-polyfluoroalkylating the appropriately substituted 2-oxo-1,3-dihydro-2H-1,4-benzodiazepines. Alternate methods for the synthesis of the compounds of this invention are also described
