US2018230079A1PendingUtilityA1
Therapeutic compounds and methods of use thereof
Est. expiryAug 27, 2035(~9.1 yrs left)· nominal 20-yr term from priority
C07C 69/757C07C 313/04C07C 2601/14A61P 25/00C07C 323/61C07C 229/48C07C 62/38C07D 211/22C07C 62/34A61P 29/00C07C 2601/02C07C 2603/74C07C 2601/04C07C 317/44A61P 17/04C07C 2601/08
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Claims
Abstract
and pharmaceutically acceptable salts thereof, wherein the variables RAA, n, ring A, X1, L, m, X2, R2, R3, R4, R5, X, and R6 have the meaning as described herein, and compositions containing such compounds and methods for using such compounds and compositions.
Claims
exact text as granted — not AI-modified1 . A compound of Formula I:
or a salt thereof; wherein
each RA is independently selected from the group consisting of F, Cl, Br, I, —CN, —OR A1 , (X RA )-(6-12 membered aryl), —(X RA )-(5-12 membered heteroaryl), and —R 2 , wherein said 6-12 membered aryl and 5-12 membered heteroaryl of R AA is optionally substituted with from 1 to 5 substitutents independently selected from the group consisting of F, Cl, Br, I, C 1-4 alkyl, C 1-4 haloalkyl, and C 1-4 (halo)alkoxy; R A1 is selected from the group consisting of hydrogen, C 1-8 alkyl, C 2-8 alkenyl, C 1-8 haloalkyl, C 3-8 cycloalkyl, phenyl and benzyl; R A2 is selected from the group consisting of C 1-8 alkyl that is optionally substituted with one or more substituents selected from oxo (═O), fluoro, amino, C 1-4 alkylamino and di(C 1-4 alkyl)amino; X RA is selected from the group consisting of absent, —C(═O)—, and C 1-4 alkylene; wherein any C 1-4 alkylene of X RA is optionally substituted with 1 to 3 substituents selected from the group consisting of C 1-4 alkyl, C 1-4 haloalkyl, and phenyl that is optionally substituted with 1 to 5 substitutents selected from, F, Cl, Br, I, —NH 2 , —OH, —CN, —NO 2 , C 1-4 alkyl, C 1-4 haloalkyl, C 1-4 alkoxy, C 1-4 (halo)alkoxy, C 1-4 alkylamino and C 1-4 dialkylamino;
n is 0, 1, 2, 3, 4, 5, 6, 7, or 8;
ring “A” is a 3-15 membered carbocyclyl, a 6-12 membered aryl, a 5-12 membered heteroaryl, or a 3-15 membered heterocyclyl;
X 1 and X 2 are each independently selected from the group consisting of absent, —S—, —O— and —N(R X )— wherein R x is H, C 1-8 alkyl, or C 1-8 haloalkyl, and wherein if the subscript m is 0 then one of X 1 or X 2 is absent;
L is C 1-6 alkylene, wherein L is optionally substituted with from 1 to 3 substituents independently selected from the group consisting of C 1-4 alkyl, C 1-4 alkoxy, halo, oxo (═O), and C 1-4 haloalkyl;
wherein any two substituents attached to the same atom on L are optionally combined to form a 3- to 5-membered carbocyclic ring;
m is 0 or 1;
R 2 , R 3 , R 4 , and R 5 are each independently selected from the group consisting of H, F, Cl, Br, I, —CN, C 1-8 alkyl, C 3-8 cycloalkyl, C 1-8 haloalkyl and C 1-8 alkoxy;
X is selected from the group consisting of O, S, S═O, SO 2 , N(R N ), C═O, CH 2 , and C═S, wherein R N is selected from the group consisting of H, C 1-6 alkyl and acyl;
ring “B” is selected from the group consisting of cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, and cyclooctyl, wherein ring B is optionally substituted with one or more groups independently selected from C 1-4 alkyl; and
R 6 is hydrogen or C 1-6 alkyl.
2 . The compound of claim 1 wherein the compound of formula (I) is a compound of formula (Ia):
3 . The compound of claim 1 wherein the compound of formula (I) is a compound of formula (Ib):
4 . The compound of claim 1 wherein the compound of formula (I) is a compound of formula (Ic):
5 . The compound of claim 1 wherein the compound of formula (I) is a compound of formula (Id):
6 . The compound of claim 1 wherein the compound of formula (I) is a compound of formula (Ie):
7 . The compound of claim 1 wherein the compound of formula (I) is a compound of formula (If):
8 . The compound of claim 1 wherein the compound of formula (I) is a compound of formula (Ig):
9 . The compound of claim 1 wherein the compound of formula (I) is a compound of formula (Ih):
10 . The compound of claim 1 wherein the compound of formula (I) is a compound of formula (Ij):
11 . The compound of claim 1 , wherein ring “B” is selected from the group consisting of cyclobutyl, cyclopentyl, and cyclohexyl.
12 . The compound of claim 1 wherein the compound of formula (I) is a compound of formula (Ik):
13 . The compound of claim 1 wherein the compound of formula (I) is a compound of formula (Im):
14 . The compound of claim 1 wherein the compound of formula (I) is a compound of formula (In):
15 . The compound of claim 1 wherein the compound of formula (I) is a compound of formula (Io):
16 . The compound of claim 1 wherein the compound of formula (I) is a compound of formula (Ip):
17 . The compound of claim 1 wherein the compound of formula (I) is a compound of formula (Iq):
18 . The compound of claim 1 wherein the compound of formula (I) is a compound of formula (Ir):
19 . The compound of claim 1 wherein the compound of formula (I) is a compound of formula (Is):
20 - 24 . (canceled)
25 . The compound of claim 1 , wherein ring “A” is a 6-15 membered carbocycle.
26 - 43 . (canceled)
44 . A compound selected from the group consisting of:
and salts thereof.
45 . A pharmaceutical composition comprising a compound of formula I as described in claim 1 , or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable excipient.
46 . A method of treating a disease or condition in a mammal selected from the group consisting of pain, depression, cardiovascular diseases, respiratory diseases, and psychiatric diseases, and combinations thereof, wherein the method comprises administering to the mammal in need thereof a therapeutically effective amount of a compound of formula I as described in claim 1 or a pharmaceutically acceptable salt thereof.
47 - 53 . (canceled)Cited by (0)
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