IP Library Granted Patent US 9,242,976
Granted Patent B2
US 9,242,976 · App. 14/371,463 · Granted Jan 26, 2016

Thiazolyl- or thiadiazolyl-substituted pyridyl compounds useful as kinase inhibitors

Inventors: Venkatram Reddy Paidi (Bangalore, IN); Sreekantha Ratna Kumar (Bangalore, IN); Abhisek Banerjee (West Bengal, IN); Ramesh Sistla (Bangalore, IN); Satheesh Kesavan Nair (Bangalore, IN); William J. Pitts (Newtown, PA); John Hynes (Washington Crossing, PA)
Assignee: Bristol-Myers Squibb Company
C07D417/14C07D413/04C07D413/14C07D417/04C07D471/04C07D487/04
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Quick Facts
Patent No.
US 9,242,976
App. No.
14/371,463
Granted
Jan 26, 2016
Kind
B2
Abstract

Compounds having the following formula (I) or an enantiomer, diastereomer or a pharmaceutically-acceptable salt thereof, wherein X is N or C—R 7 , are useful as kinase modulators, including IRAK-4 modulation.

Claims (26)

1. A compound having the following formula:

or a stereoisomer or pharmaceutically-acceptable salt thereof, wherein

X is N;

R is —C(═O)—R 1 , —C(═O)O—R 1 or —C(═O)NR 11 —R 1 ;

R 1 is piperidinyl substituted with 0-3 R 1a ;

R 1a is hydrogen, —OCF 3 , —CN, —(CH 2 ) r OR b , —(CH 2 ) r C(O)R b , —(CH 2 ) r C(O)OR b , —(CH 2 ) r OC(O)R b , —(CH 2 ) r NR 11 R 11 , —(CH 2 ) r C(O)NR 11 R 11 , —(CH 2 ) r NR b C(O)R c , —(CH 2 ) r NR b C(O)OR c , —S(O) p NR 11 R11, —NR b S(O) p R c , —S(O) 2 R c , or C 1-6 alkyl substituted with 0-2 R a ;

R 2 is benzo[d]thiazolyl;

R 3 is propyl substituted with 0-3 R 3a ;

R 3a is —OH or phenyl;

R 11 at each occurrence is hydrogen;

R a is R d , F, Cl, Br, OCF 3 , CF 3 , CHF 2 , or CN;

R b is R e , C 1-6 alkyl, or C 1-6 haloalkyl;

R c is CH 3 ;

R d is hydrogen;

R e is hydrogen;

p is 0, 1, or 2; and

r is 0, 1, or 2.

2. The compound of claim 1 , or a stereoisomer or pharmaceutically-acceptable salt thereof, wherein R 2 is

3. The compound according to claim 1 , or a stereoisomer or pharmaceutically-acceptable salt thereof, wherein R 3 is —CH(CH 3 ) 2 .

4. The compound according to claim 1 , or a stereoisomer or pharmaceutically-acceptable salt thereof, wherein R 1a is —OH or —NH 2 .

5. The compound according to claim 1 or a stereoisomer or pharmaceutically acceptable salt thereof, wherein:

R is —C(═O)—R 1 ;

R 1 is piperidinyl substituted with 0-1 R 1a ; and

R 1a is hydrogen, —OH, or —NH 2 .

6. The compound according to claim 1 , or a stereoisomer or pharmaceutically-acceptable salt thereof, wherein said compound is selected from

7. A pharmaceutical composition comprising one or more compounds according to claim 1 and a pharmaceutically acceptable carrier or diluent.

Continuity (2)
Provisional Application 61586148 · Jan 13, 2012
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