IP Library Granted Patent US 9,783,531
Granted Patent B2
US 9,783,531 · App. 15/105,411 · Granted Oct 10, 2017

Thiazole-substituted aminoheteroaryls as spleen tyrosine kinase inhibitors

Inventors: Michelle R. Machacek (Brookline, MA); Eric T. Romeo (Allston, MA); Alan B. Northrup (Reading, MA); Michael D. Altman (Needham, MA)
Assignee: Merck Sharp & Dohme Corp.
C07D417/12A61K31/427A61K31/433A61K31/5377A61K45/06
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Quick Facts
Patent No.
US 9,783,531
App. No.
15/105,411
Granted
Oct 10, 2017
Kind
B2
Abstract

The invention provides certain thiazole-substituted aminoheteroaryl compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein R 1 , R 3 , R 5 , R 6 , A, Cy and the subscripts r, s, and t are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk).

Claims (35)

1. A compound of the Formula (I)

or a pharmaceutically acceptable salt thereof, wherein

ring A is

R 1 is

C 3 -C 6 cycloalkyl;

R 3 is selected from the group consisting of

(a) H;

(b) C 1 -C 3 alkyl;

(c) C 1 -C 3 alkoxy; and

(d) halo;

ring C y is cyclobutyl or cyclohexyl;

R 5 is —C(O)OH;

R 6 is C 1 -C 3 alkyl or halo;

the subscript r is 1;

the subscripts is 0 or 1; and

the subscript t is 0, 1, 2, 3, 4, or 5.

2. The compound of claim 1 or a pharmaceutically acceptable salt thereof, wherein R 3 is H or methyl.

3. The compound of claim 1 or a pharmaceutically acceptable salt thereof, wherein

R 3 is methyl.

4. The compound of claim 1 or a pharmaceutically acceptable salt thereof, wherein C y is cyclobutyl and the subscripts s and t are both 0.

5. The compound of claim 1 or a pharmaceutically acceptable salt thereof, wherein

C y is cyclohexyl;

R 5 is —C(O)OH;

R 6 is methyl;

the subscripts is 1; and

the subscript t is 0, 1, or 2.

6. The compound of claim 1 or a pharmaceutically acceptable salt thereof, wherein the compound is selected from the group consisting of:

1-(5-{3-[(1-cyclohexyl-1H-1,2,4-triazol-3-yl)amino]-5-methylphenyl}-1,3-thiazol-2-yl)cyclobutanol;

1-(5-{3-[(1-cyclobutyl-1H-1,2,4-triazol-3-yl)amino]-5-methylphenyl}-1,3-thiazol-2-yl)cyclobutanol;

1-(5-{3-[(1-cyclobutyl-1H-1,2,4-triazol-5-yl)amino]-5-methylphenyl}-1,3-thiazol-2-yl)cyclobutanol;

cis-4-(5-{3-[(1-cyclobutyl-1H-1,2,4-triazol-5-yl)amino]-5-methylphenyl}-1,3-thiazol-2-yl)-4-hydroxycyclohexanecarboxylic acid;

(1R,4S)-4-(5-{3-[(1-cyclobutyl-1H-1,2,4-triazol-3-yl)amino]-5-methylphenyl}-1,3-thiazol-2-yl)-4-hydroxy-2,2-dimethylcyclohexanecarboxylic acid; and

(1S,4R)-4-(5-{3-[(1-cyclobutyl-1H-1,2,4-triazol-3-yl)amino]-5-methylphenyl}-1,3-thiazol-2-yl)-4-hydroxy-2,2-dimethylcyclohexanecarboxylic acid.

7. A pharmaceutical composition comprising the compound of claim 1 or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier.

8. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein the compound is cis-4-(5-{3-[(1-cyclobutyl-1H-1,2,4-triazol-3-yl)amino]-5-methylphenyl}-1,3-thiazol-2-yl)-4-hydroxy-2,2-dimethylcyclohexanecarboxylic acid.

Assignments (2)
MERGER Recorded Aug 8, 2022
From: MERCK SHARP & DOHME CORP.
To: MERCK SHARP & DOHME LLC
Reel/Frame 061102/0145 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 29, 2016
From: MACHACEK, MICHELLE R.; ROMEO, ERIC T.; NORTHRUP, ALAN B.; ALTMAN, MICHAEL D.
To: MERCK SHARP & DOHME CORP.
Reel/Frame 039042/0193 →
Continuity (2)
Provisional Application 61918980 · Dec 20, 2013
Related Publication 20160311813A1 · Oct 27, 2016