ETOMIDATE ANALOGUES WITH IMPROVED PHARMACOKINETIC AND PHARMACODYNAMIC PROPERTIES

摘要

The invention is directed to compounds according to formula (I):;;where R1 is L1C(O)OT or L1C(O)OL2C(O)OT; R2 is a substituted or unsubstituted C1-C10 alkyl, C2-C10 alkenyl, or C2-C10 alkynyl, or R1; n is an integer from 0 to 5; each R3 is independently halogen or R2; L1 and L2 are each independently a bond, a substituted or unsubstituted C1-C10 alkylene, C2-C10 alkenylene, or C2-C10 alkynylene; and T is H, a substituted or unsubstituted C1-C10 alkyl, C2-C10 alkenyl, or C2-C10 alkynyl, nitrophenol, or cyclopropyl. The invention is also directed to a pharmaceutical composition comprising a compound according to formula (I) and a pharmaceutically acceptable carrier, and to methods for providing anesthesia in mammals by administering such a pharmaceutical composition.

主权项

1. A compound according to formula (I)wherein,
R1 is L1C(O)OT or L1C(O)OL2C(O)OT; R2 is a substituted or unsubstituted C1-C10 alkyl, C2-C10 alkenyl, or C2-C10 alkynyl, or R1; n is an integer from 0-5; each R3 is independently halogen or R2; L1 and L2 are each independently a bond, a substituted or unsubstituted C1-C10 alkylene, C2-C10 alkenylene, or C2-C10 alkynylene, wherein the backbone of alkylene may contain one or more heteroatoms; T is H, a substituted or unsubstituted C1-C10 alkyl, C2-C10 alkenylene, C2-C10 alkynylene, nitrophenol, or cyclopropyl, wherein the backbone of alkyl may contain one or more heteroatoms; and pharmaceutically acceptable salts, stereoisomer mixtures, and enantiomers thereof, provided that when R1 is L1C(O)OT, R2 is CH3, R3 fluorine, n is 1, and T is CH2CH3, L1 is not a bond.