IP Library Granted Patent US 9,580,427
Granted Patent B2
US 9,580,427 · App. 14/118,541 · Granted Feb 28, 2017

Kinase inhibitors

Inventors: John William Taunton, Jr. (San Francisco, CA); Jesse McFarland (Oakland, CA); Shyam Krishnan (San Francisco, CA); Jonathan Choy (Lafayette, CA)
Assignee: The Regents of the University of California
C07D487/04C07D215/54C07D235/08C07D239/48C07D239/94C07D401/12C07D401/14C07D403/04C07D403/12C07D405/12C07D405/14C07D417/12C07D471/04
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Quick Facts
Patent No.
US 9,580,427
App. No.
14/118,541
Granted
Feb 28, 2017
Kind
B2
Abstract

Provided herein are compounds such as the compounds having the structure of Formula (XI) and methods of using the same, such as methods of inhibiting kinases.

Claims (29)

1. A compound having the structure of Formula (XI):

wherein:

the dashed lines are optionally a bond;

y is an integer from 0 to 2;

j is an integer from 0 to 3;

f is 0 or 1;

Z 1 , Z 2 , and Z 3 are —N— or —CH—, provided that at least one and not more than two of Z 1 , Z 2 , and Z 3 are simultaneously N;

Ar is a monocyclic or fused bicyclic (C 6 -C 10 ) aryl, monocyclic or fused bicyclic 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O or S, monocyclic (C 3 -C 10 )cycloalkyl or 4 to 8 membered heterocycloalkyl containing 1-4 heteroatoms selected from N, O or S and is optionally fused to monocyclic aryl or heteroaryl as defined above and can contain one to two —CO— groups in the ring;

R 12 is hydrogen, (C 1 -C 6 ) unsubstituted saturated alkyl, hydroxy, unsubstituted saturated (C 1 -C 6 ) alkoxy, halogen, halo substituted (C 1 -C 6 ) saturated alkyl, or unsubstituted saturated (C 1 -C 6 ) haloalkoxy;

R 14 is hydrogen, (C 1 -C 6 ) unsubstituted saturated alkyl, hydroxy, —O(C 1 -C 6 ) unsubstituted saturated alkyl, halogen, unsubstituted saturated (C 1 -C 6 ) haloalkyl, or unsubstituted saturated (C 1 -C 6 ) haloalkoxy;

L 1 is —C(O)— or —SO 2 —;

L 4 is a bond, —O—, —NH—, or methylene;

ring A is azetidinyl, pyrrolidinyl, piperidinyl, or piperazinyl optionally substituted with methyl or fluoro;

L 11 is —O—, —CO—, —CH 2 —, —S—, —SO—, —SO 2 —, —NR 15C —, —NR 15C CO—, —CONR 15C —, —NR 15C SO 2 —, —SO 2 NR 15C —, or —NR 15C CONR 15D —, wherein each R 15C and R 15D is independently hydrogen or C 1 -C 6 unsubstituted saturated alkyl;

R 23 is hydrogen, (C 1 -C 6 ) unsubstituted saturated alkyl, hydroxy, unsubstituted saturated (C 1 -C 6 ) alkoxy, halo, unsubstituted saturated (C 1 -C 6 ) haloalkyl, unsubstituted saturated (C 1 -C 6 ) haloalkoxy, carboxy, —COO—(C 1 -C 6 ) unsubstituted saturated alkyl, cyano, —CONH 2 , or —NR x R y where R x is hydrogen and R y is hydrogen, (C 1 -C 6 ) unsubstituted saturated alkyl, unsubstituted saturated (C 3 -C 6 ) cycloalkyl, unsubstituted saturated (C 3 -C 6 )cycloalkyl-(C 1 -C 6 ) unsubstituted saturated alkyl, —COR wherein R is (C 1 -C 6 ) unsubstituted saturated alkyl, or —SO 2 —(C 1 -C 6 ) unsubstituted saturated alkyl;

R 2 and R 3 are independently (C 1 -C 6 ) unsubstituted saturated alkyl, unsubstituted saturated (C 1 -C 6 ) haloalkoxy, (C 1 -C 6 ) saturated alkyl which is substituted with one, two, or three substituents independently selected from hydroxyl, unsubstituted saturated (C 1 -C 6 ) alkoxy, carboxy, cyano, —COO—(C 1 -C 6 ) unsubstituted saturated alkyl, —S—(C 1 -C 6 ) unsubstituted saturated alkyl, —SO 2 —(C 1 -C 6 ) unsubstituted saturated alkyl, halo, —CONR″R′ or NR″R′ where each R″ is hydrogen, (C 1 -C 6 ) unsubstituted saturated alkyl, (C 3 -C 6 ) unsubstituted saturated cycloalkyl, (C 1 -C 6 ) saturated alkyl substituted with one, two, or three hydroxy or one to three unsubstituted saturated (C 1 -C 6 ) alkoxy and R′ is hydrogen, (C 1 -C 6 ) unsubstituted saturated alkyl, unsubstituted saturated (C 3 -C 6 ) cycloalkyl or 4 to 8 membered heterocycloalkyl containing 1-4 heteroatoms selected from N, O or S and which is optionally substituted with one or two groups independently selected from (C 1 -C 6 ) unsubstituted saturated alkyl, hydroxyl, unsubstituted saturated (C 1 -C 6 ) alkoxy, —S—(C 1 -C 6 ) unsubstituted saturated alkyl, —SO 2 —(C 1 -C 6 ) unsubstituted saturated alkyl, or halo, or R 2 and R 3 together with the carbon atom to which they are attached form (C 3 -C 6 ) unsubstituted saturated cycloalkyl; and

R 4 is R 18 -substituted or unsubstituted alkyl, R 18 -substituted or unsubstituted heteroalkyl, R 18 -substituted or unsubstituted cycloalkyl, R 18 -substituted or unsubstituted heterocycloalkyl, R 18 -substituted or unsubstituted aryl, or R 18 -substituted or unsubstituted heteroaryl, wherein

R 18 is independently halogen, —CN, —OH, —SH, —NH 2 , —COOH, —NO 2 , —CONH 2 , —CF 3 , unsubstituted alkyl, unsubstituted heteroalkyl, unsubstituted cycloalkyl, unsubstituted heterocycloalkyl, unsubstituted aryl, or unsubstituted heteroaryl.

2. The compound of claim 1 , wherein L 11 is —O—.

3. The compound of claim 2 , wherein R 12 is absent, methyl, fluoro, or trifluoromethyl.

4. The compound of claim 3 , wherein R 14 is independently absent, unsubstituted saturated (C 1 -C 6 ) alkyl, unsubstituted saturated (C 1 -C 6 ) alkoxy, halo, unsubstituted saturated (C 1 -C 6 ) haloalkyl or unsubstituted saturated (C 1 -C 6 ) haloalkoxy.

5. The compound of claim 4 , wherein R 23 is independently absent, unsubstituted saturated (C 1 -C 6 ) alkyl, unsubstituted saturated (C 1 -C 6 ) alkoxy, halo, unsubstituted saturated (C 1 -C 6 ) haloalkyl, unsubstituted saturated (C 1 -C 6 ) haloalkoxy, or cyano.

6. The compound of claim 5 , wherein L 4 is a bond or methylene.

7. The compound of claim 6 , wherein L 1 is —C(O)— and ring A is piperidinyl optionally substituted with methyl or fluoro.

8. The compound of claim 7 , wherein R 2 and R 3 are independently unsubstituted saturated C 1 -C 6 alkyl or together form (C 3 -C 6 ) unsubstituted saturated cycloalkyl.

9. The compound of claim 8 , wherein Ar is unsubstituted phenyl or phenyl substituted at least one of a meta or para position.

10. A pharmaceutical composition comprising a compound of claim 1 or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable excipient.

11. A method for treating leukemia, multiple myeloma, lymphoma, non-small cell lung cancer, pancreatic cancer or rheumatoid arthritis, said method comprising administering to a subject in need thereof an effective amount of a compound of claim 1 .

12. The compound according to claim 1 , said compound selected from the group consisting of:

Assignments (4)
CONFIRMATORY LICENSE Recorded Sep 11, 2017
From: UNIVERSITY OF CALIFORNIA, SAN FRANCISCO
To: NATIONAL INSTITUTES OF HEALTH (NIH), U.S. DEPT. OF HEALTH AND HUMAN SERVICES (DHHS), U.S. GOVERNMENT
Reel/Frame 043811/0262 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 29, 2016
From: TAUNTON, JOHN WILLIAM
To: THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
Reel/Frame 040805/0478 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 16, 2016
From: CHOY, JONATHAN
To: THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
Reel/Frame 040642/0411 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 20, 2015
From: TAUNTON, JACK; KRISHNAN, SHYAM; MCFARLAND, JESSE
To: THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
Reel/Frame 035678/0919 →
Continuity (2)
Provisional Application 61487233 · May 17, 2011
Related Publication 20140323464A1 · Oct 30, 2014