Inhibitors of JAK

Inventors: Javier de Vicente Fidalgo (Glen Ridge, NJ); Johannes Cornelius Hermann (Jersey City, NJ); Remy Lemoine (San Francisco, CA); Hongju Li (Edison, NJ); Allen John Lovey (North Caldwell, NJ); Eric Brian Sjogren (Mountain View, CA); Michael Soth (Glen Rock, NJ)

Assignee: Hoffmann-La Roche Inc.

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Quick Facts

Patent No.: US 8,618,103
App. No.: 12/878,048
Granted: Dec 31, 2013
Kind: B2

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Abstract

The present invention relates to the use of novel compounds of Formula I, wherein the variables m, n, p, q, Q, r, R, R′, X, X′, Y, Z 1 , Z 2 , and Z 3 are defined as described herein, which inhibit JAK and are useful for the treatment of auto-immune and inflammatory diseases.

Claims (187)

1. A compound of Formula I

wherein:

R is lower alkyl, lower haloalkyl, lower alkoxy, hydroxy lower alkyl, hydroxy, or halogen;

n is 0 or 1;

Z 1 is NH;

Z 2 is CH;

Z 3 is CR 1 ;

R 1 is H, lower alkyl, cycloalkyl, cyano, cyano lower alkyl, or halogen;

X is CH, CR′, or N;

X′ is CH, CR′, or N;

r is 0 or 1;

Y is CH, CR′, or N;

R′ is R′ a or R′ b ;

R′ a is halogen or cyano;

R′ b is lower alkyl, cycloalkyl, heterocycloalkyl, OR″, SR″, S(═O) 2 R″, or NR″R″, optionally substituted with one or more R′ c ;

R′ c is hydroxy, halogen, oxo, cyano, lower alkyl, cycloalkyl, heterocycloalkyl, heteroaryl, carboxy lower alkyl, amino, amino carboxy lower alkyl, lower alkyl amino, lower dialkyl amino, lower haloalkyl, or lower alkoxy;

m is 0 or 1;

R″ is H, lower alkyl, hydroxy lower alkyl, heteroaryl, or lower alkoxy;

Q is H, S(═O) 2 Q 1 , C(═O)Q 2 , C(═O)OQ 3 , or Q 4 ;

Q 1 is lower alkyl, cycloalkyl lower alkyl, lower alkyl amino, lower dialkyl amino, or cycloalkyl, optionally substituted with one or more Q 1′ ;

each Q 1′ is independently halogen, lower alkyl, cyano, or lower alkoxy;

Q 2 is lower alkyl, cycloalkyl lower alkyl, or cycloalkyl, optionally substituted with one or more Q 2′ ;

each Q 2′ is independently halogen, lower alkyl, cyano, or lower alkoxy;

Q 3 is lower alkyl, cycloalkyl lower alkyl, or cycloalkyl, optionally substituted with one or more Q 3′ ;

each Q 3′ is independently halogen, lower alkyl, or lower alkoxy;

Q 4 is lower alkyl, cycloalkyl lower alkyl, heterocycloalkyl, or cycloalkyl, optionally substituted with one or more Q 4′ ;

each Q 4′ is independently halogen, cyano, cyano lower alkyl, lower alkyl, or lower alkoxy;

p is 0, 1, or 2;

q is 1 or 2;

each represents a single bond or a double bond; and

with the proviso that the bonds between Z 1 and Z 2 and Z 2 and Z 3 are not both double bonds and are not both single bonds;

or a pharmaceutically acceptable salt thereof.

2. The compound of claim 1 , having the Formula II

wherein:

R is lower alkyl;

n is 0 or 1;

Z 3 is CR 1 ;

R 1 is H, lower alkyl, or halogen;