Back to results
US 2020/0087239 A1Published application
Therapeutic compounds and methods of use thereof
AssigneesGenentech, Inc., Xenon Pharmaceuticals Inc.
InventorsIvan William HEMEON, Brian Salvatore SAFINA, Daniel SUTHERLIN
Life of this patent
Estimating the term…
Abstract
The invention provides compounds having the general formula I: 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.
Claims1
A compound of Formula I:
- or a salt thereof;
- wherein
- each RAA is independently selected from the group consisting of F, Cl, Br, I, —CN, —ORA1, —(XRA)-(6-12 membered aryl), —(XRA)-(5-12 membered heteroaryl), and —RA2, wherein said 6-12 membered aryl and 5-12 membered heteroaryl of RAA is optionally substituted with from 1 to 5 substitutents independently selectd from the group consisting of F, Cl, Br, I, C1-4 alkyl, C1-4 haloalkyl, and C1-4(halo)alkoxy;
- RA1 is selected from the group consisting of hydrogen, C1-8 alkyl, C2-8 alkenyl, C1-8 haloalkyl, C3-8 cycloalkyl, phenyl and benzyl;
- RAA2 is selected from the group consisting of C1-8 alkyl that is optionally substituted with one or more substituents selected from oxo (=O), fluoro, amino, C1-4 alkylamino and di(C1-4alkyl)amino;
- XRA is selected from the group consisting of absent, —C(=O)—, and C1-4 alkylene;
- wherein any C1-4 alkylene of XRA is optionally substituted with 1 to 3 substituents selected from the group consisting of C1-4 alkyl, C1-4 haloalkyl, and phenyl that is optionally substituted with 1 to 5 substitutents selected from, F, Cl, Br, I, —NH2, —OH, —CN, —NO2, C1-4 alkyl, C1-4 haloalkyl, C1-4 alkoxy, C1-4(halo)alkoxy, C1-4 alkylamino and C1-4 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;
- X1 and X2 are each independently selected from the group consisting of absent, —S—, —O— and —N(RX)— wherein Rx is H, C1-8 alkyl, or C1-8 haloalkyl, and wherein if the subscript m is 0 then one of X1 or X2 is absent;
- L is C1-6 alkylene, wherein L is optionally substituted with from 1 to 3 substituents independently selected from the group consisting of C1-4 alkyl, C1-4 alkoxy, halo, oxo (=O), and C1-4 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;
- R2, R3, R4, and R5 are each independently selected from the group consisting of H, F, Cl, Br, I, —CN, C1-8 alkyl, C3-8 cycloalkyl, C1-8 haloalkyl and C1-8 alkoxy;
- X is selected from the group consisting of O, S, S=O, SO2, N(RN), C=O, CH2, and C=S, wherein RN is selected from the group consisting of H, C1-6 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 C1-4 alkyl;
- and
- R6 is hydrogen or C1-6 alkyl.
15 more elements
Dependencies are inferred from the claim text.