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US 8,802,728 B2Granted
Analgesic compounds, methods, and formulations
AssigneeEli Lilly and Company
InventorsJean Marie Defauw, Scott Dale Holmstrom, Shuhui Chen, Yang Zhang, Wentao Wu, Xian Peng, Yujuan Ma, Lun Lu
Life of this patent
Estimating the term…
Abstract
Provided are analgesic compounds, and salts thereof, of formula: (I) wherein A is: (A) Additionally, pharmaceutical formulations and methods of use employing the above compounds are provided.
Claims31
A compound, or salt thereof, of formula I:
- wherein A is
- R1 is hydrogen, C1-C5 alkyl, C1-C5 haloalkyl, C1-C5 alkanol, —(C1-C5 alkyl)phenyl, or phenyl, or a group of the formula —C(O)—R12, where R12 is C1-C5 alkyl, C1-C5 alkoxy, C1-C5 haloalkyl, C1-C5 alkanol, —(C1-C5 alkyl)phenyl, or phenyl;
- R2 is hydrogen, C1-C5 alkyl, C1-C5 alkoxy, halogen, C1-C5 haloalkyl, or C1-C5 haloalkoxy;
- R3 is hydrogen, C1-C5 alkyl, C1-C5 alkoxy, halogen, C1-C5 haloalkyl, or C1-C5 haloalkoxy;
- R4 is hydrogen, C1-C5 alkyl, or —(C1-C5 alkyl)phenyl;
- R5 is hydrogen, C1-C5 alkyl, or —(C1-C5 alkyl)phenyl;
- R6 is hydrogen, hydroxy, or is absent;
- R7 is hydrogen;
- R8 is hydrogen or methyl;
- R9 is hydrogen or methyl;
- R10 is hydrogen;
- R11 is hydrogen or C1-C5 alkyl;
- provided that one of A), B), and C) is present, wherein A), B) and C) are:
- A) R7 and R10 combine to form —CH2— or —(CH2)2—;
- B) R8 and R9 combine to form a cyclopropyl group with the carbon to which they are attached;
- and
- C) R10 and R11 combine to form —CH2— or —(CH2)3.
14 more elements
Dependencies are inferred from the claim text.