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US 2013/0158057 A1Published application
Aminopyrimidine derivatives as lrrk2 modulators
AssigneeGenentech, Inc.
InventorsCharles Baker-Glenn, Mark Chambers, Bryan K. Chan, Anthony Estrada, Zachary Kevin Sweeney
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Abstract
Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, n. X, R1, R2, R3, R4 and R5 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of diseases associated with LRRK2 receptor, such as Parkinson's disease.
Claims21
A compound of formula I:
- or pharmaceutically acceptable salts thereof,
- wherein:
- m is from 0 to 3;
- X is:
- —NRa—;
- —O—;
- or —S(O)r— wherein r is from 0 to 2 and Ra is hydrogen or C1-6alkyl;
- Y is C or N;
- R1 is:
- C1-6alkyl;
- C1-6alkenyl;
- C1-6alkynyl;
- halo-C1-6alkyl;
- C1-6alkoxy-C1-6alkyl;
- hydroxy-C1-6alkyl;
- amino-C1-6alkyl;
- C1-6alkylsulfonyl-C1-6alkyl;
- C3-6cycloalkyl optionally substituted with C1-6alkyl;
- C3-6cycloalkyl-C1-6alkyl wherein the C3-6cycloalkyl portion is optionally substituted with C1-6alkyl;
- tetrahydrofuranyl;
- tetrahydrofuranyl-C1-6alkyl;
- oxetanyl;
- or oxetan-C1-6alkyl;
- or R1 and Ra together with the atoms to which they are attached may form a three to six membered ring that may optionally include an additional heteroatom selected from O, N and S, and which is substituted with oxo, halo or C1-6alkyl;
- R2 is:
- halo;
- C1-6alkoxy;
- cyano;
- C1-6alkynyl;
- C1-6alkenyl;
- halo-C1-6alkyl;
- halo-C1-6alkoxy;
- C3-6cycloalkyl wherein the C3-6cycloalkyl portion is optionally substituted with C1-6alkyl;
- C3-6cycloalkyl-C1-6alkyl wherein the C3-6cycloalkyl portion is optionally substituted with C1-6alkyl;
- tetrahydrofuranyl;
- tetrahydrofuranyl-C1-6alkyl;
- acetyl;
- oxetanyl;
- or oxetan-C1-6alkyl;
- R3 and R4 each independently is:
- halo;
- C1-6alkyl;
- C1-6alkoxy;
- C3-6cycloalkyloxy;
- halo-C1-6 alkyl;
- or halo-C1-6alkoxy;
- and
- R5 is a 5-membered heteroaryl group optionally substituted one or more times with R6;
- and
- R6 is:
- C1-6alkyl;
- C3-6cycloalkyl;
- C3-6cycloalkyl-C1-6alkyl;
- halo;
- halo-C1-6alkyl;
- C1-6alkoxy;
- heterocyclyl;
- oxo;
- or —C(O)—NRbRc wherein Rb and Rc each independently is hydrogen or —C1-6alkyl.
56 more elements
Dependencies are inferred from the claim text.