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US 2003/0119790 A1Published application
Substituted phenol compounds useful for anesthesia and sedation
AssigneeTheravance, Inc.
InventorsThomas E. Jenkins, Yu-Hua Ji, Huiwei Wu, Jennifer Bolton
Life of this patent
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Abstract
The invention provides substituted phenol compounds and pharmaceutical compositions containing substituted phenol compounds which are useful for inducing or maintaining anesthesia or sedation in a mammal. This invention also provides methods for inducing or maintaining anesthesia or sedation in a mammal using substituted phenol compounds.
Claims23
A pharmaceutical composition comprising a pharmaceutically acceptable carrier and a compound selected from the group consisting of:
- 19
- wherein
- R1 and R2 are each independently (C1-C8)alkyl, (C3-C8)cycloalkyl, or (C3-C8)cycloalkyl(C1-C8)alkyl;
- L is selected from the group consisting of covalent bond and a hydrocarbylene group containing from 1 to 12 carbon atoms and optionally containing from 1 to 5 heteroatoms selected from the group consisting of oxygen, nitrogen, and sulfur;
- and
- R3 is selected from the group consisting of —C(═O)ORa, —C(═O)SRa, —P(═O)(ORa)2, —C(═O)OCH2C(═O)N(Ra)2, and —C(═O)OC(═O)Ra wherein each Ra is independently selected from a hydrocarbyl group containing from 1 to 20 carbon atoms and optionally containing from 1 to 5 heteroatoms selected from the group consisting of halo, nitrogen, oxygen and sulfur;
- or a pharmaceutically acceptable salt thereof.
4 more elements
A compound of formula (V):
- 23
- wherein L is a covalent bond, methylene, or ethylene;
- and
- R3 is selected from the group consisting of —C(═O)ORa, —C(═O)SRa, —P(═O)(ORa)2, —C(═O)OCH2C(═O)N(Ra)2, and —C(═O)OC(═O)Ra wherein each Ra is independently selected from a hydrocarbyl group containing from 1 to 20 carbon atoms and optionally containing from 1 to 5 heteroatoms selected from the group consisting of halo, nitrogen, oxygen and sulfur;
- provided when L is a covalent bond, R3 is not —C(═O)ORawherein Ra is methyl, ethyl, 1,2-dibromoethyl, but-2-enyl, hexadecyl, stearyl, or benzyl;
- and
- provided when L is ethylene, R3 is not —C(═O)ORawherein Ra is methyl or stearyl;
- or a pharmaceutically acceptable salt thereof.
5 more elements
A compound of formula (X):
- 24
- wherein
- R4 is (C1-C5)alkyl, (C2-C5)alkenyl, or (C2-C5)alkynyl;
- R5 is (C1-C6)alkyl, (C3-C8)cycloalkyl, or (C3-C8)cycloalkyl(C1-C6)alkyl;
- and R6 is methyl;
- or R5 and R6 together with the carbon atom to which they are attached form a (C3-C8)cycloalkyl;
- and
- Ra is (C1-C8)alkyl, (C2-C8)alkenyl, (C2-C8)alkynyl or (C3-C8)cycloalkyl.
5 more elements
Dependencies are inferred from the claim text.