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US 9,233,913 B2Granted
Amino acid derivatives for the treatment of neuropathic pain
AssigneeXianqi Kong
InventorsXianqi Kong, Nigel Levens, Serge Lamothe, Mohammed Atfani, Stephane Ciblat, Lucie Jette
Life of this patent
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Abstract
The invention relates to compounds, to compositions comprising the same and uses thereof for the prevention or treatment of pain, e.g neuropathic pain while having neutral or beneficial effect on metabolic parameters.
Claims19
A method for treating neuropathic pain in a subject in need thereof, comprising administering a compound or a pharmaceutically acceptable salt or ester thereof to the subject, the compound being selected from a compound of Formula IV:
- wherein,
- X is O, NH, or S;
- R1 is hydrogen, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C3-6cycloalkyl, C3-6heterocycloalkyl, C6aryl, or C5-9heteroaryl;
- R2 is hydrogen, or an N-protecting group;
- R8 and R9 are each independently hydrogen, C1-12alkyl, C6-10aryl, NH2, NHR6, NR6R7, OR6, halide, cycloalkyl, alkylenyl, arylalkyl, or R8 and R9 are taken together with their adjacent atoms to form a spiro or fused heterocycloalkyl or heteroaryl group, or R8 and R9 are attached to the same carbon atom and together with the adjacent carbon atom form a carbonyl;
- R4, R6 and R7 are each independently hydrogen, C1-12alkyl, or C6-10aryl;
- and
- p is an integer from 1 to 2;
- wherein when R1, R2, R4, R6, R7, R8 or R9 is a group selected from alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, aryl, or heteroaryl, then said alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, aryl, or heteroaryl group may be unsubstituted or substituted with a group selected from the group consisting of acyl, unsubstituted amino, alkylamino, dialkylamino, arylamino, diarylamino, alkylarylamino, acylamino, carbamoyl, ureido, alkylcarbonyloxy, arylcarbonyloxy, alkoxycarbonyloxy, alkoxycarbonyl, carboxy, carboxylate, aminocarbonyl, mono and dialkylaminocarbonyl, cyano, azido, halogen, hydroxyl, nitro, trifluoromethyl, thio, alkylthio, arylthio, alkylthiocarbonyl, thiocarboxylate, lower alkyl, lower alkenyl, lower alkynyl, cycloalkyl, heterocycloalkyl, aryl, heteroaryl, lower alkoxy, aryloxy, aryloxycarbonyloxy, benzyloxy, benzyl, sulfinyl, alkylsulfinyl, sulfonyl, sulfate, sulfonate, sulfonamide, phosphate, phosphonato, phosphinato, oxo, guanidine, imino, and formyl;
- such that neuropathic pain is treated in the subject;
- wherein the neuropathic pain is associated with epilepsy.
8 more elements
A method for treating neuropathic pain in a subject in need thereof, comprising administering a compound or a pharmaceutically acceptable salt or ester thereof to the subject, the compound being selected from a compound of Formula IV:
- wherein,
- X is O, NH, or S;
- R1 is hydrogen, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C3-6cycloalkyl, C3-6heterocycloalkyl, C6aryl, or C5-9heteroaryl;
- R2 is hydrogen, or an N-protecting group;
- R8 and R9 are each independently hydrogen, C1-12alkyl, C6-10aryl, NH2, NHR6, NR6R7, OR6, halide, cycloalkyl, alkylenyl, arylalkyl, or R8 and R9 are taken together with their adjacent atoms to form a spiro or fused heterocycloalkyl or heteroaryl group, or R8 and R9 are attached to the same carbon atom and together with the adjacent carbon atom form a carbonyl;
- R4, R6 and R7 are each independently hydrogen, C1-12alkyl, or C6-10aryl;
- and
- p is an integer from 1 to 2;
- wherein when R1, R2, R4, R6, R7, R8 or R9 is a group selected from alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, aryl, or heteroaryl, then said alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, aryl, or heteroaryl group may be unsubstituted or substituted with a group selected from the group consisting of acyl, unsubstituted amino, alkylamino, dialkylamino, arylamino, diarylamino, alkylarylamino, acylamino, carbamoyl, ureido, alkylcarbonyloxy, arylcarbonyloxy, alkoxycarbonyloxy, alkoxycarbonyl, carboxy, carboxylate, aminocarbonyl, mono and dialkylaminocarbonyl, cyano, azido, halogen, hydroxyl, nitro, trifluoromethyl, thio, alkylthio, arylthio, alkylthiocarbonyl, thiocarboxylate, lower alkyl, lower alkenyl, lower alkynyl, cycloalkyl, heterocycloalkyl, aryl, heteroaryl, lower alkoxy, aryloxy, aryloxycarbonyloxy, benzyloxy, benzyl, sulfinyl, alkylsulfinyl, sulfonyl, sulfate, sulfonate, sulfonamide, phosphate, phosphonato, phosphinato, oxo, guanidine, imino, and formyl;
- such that neuropathic pain is treated in the subject;
- wherein the neuropathic pain is associated with post-herpetic neuralgia.
8 more elements
Dependencies are inferred from the claim text.