IP Library Granted Patent US 11,135,222
Granted Patent B2
US 11,135,222 · App. 14/948,078 · Granted Oct 5, 2021

Aurora kinase inhibitors

Inventors: Justin Gabriel Meyerowitz (San Francisco, CA); William Clay Gustafson (San Francisco, CA); William A. Weiss (San Francisco, CA); Nicholas T. Hertz (San Francisco, CA); Kevan M. Shokat (San Francisco, CA)
Assignee: THE REGENTS OF THE UNIVERSIITY OF CALIFORNIA
A61K31/506C07D403/12
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Quick Facts
Patent No.
US 11,135,222
App. No.
14/948,078
Granted
Oct 5, 2021
Kind
B2
Abstract

Disclosed herein inter alia are compositions and methods useful in the treatment of cancer and for modulating the activity of Aurora A kinase and/or a Myc family protein.

Claims (15)

1. A compound, or a pharmaceutically acceptable salt thereof, having the formula:

wherein

R 1 is a substituted or unsubstituted C 5 cycloalkyl, substituted or unsubstituted 5 to 6 membered heteroaryl;

R 2 is hydrogen, halogen, —CF 3 , —CCl 3 , —CN, —OH, —NH 2 , —COOH, —CONH 2 , —NO 2 , —SH, —SO 2 Cl, —SO 3 H, —SO 4 H, —SO 2 NH 2 , —NHNH 2 , —ONH 2 , —NHC(O)NHNH 2 , —NHC(O)NH 2 , —NHSO 2 H, —NHC(O)H, —NHC(O)OH, —NHOH, —OCH 3 , —OCF 3 , —OCHF 2 , —C(O)CH 3 , substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl;

R 3 is independently halogen, —CF 3 , —CCl 3 , —CN, —OH, —NH 2 , —COOH, —CONH 2 , —NO 2 , —SH, —SO 2 Cl, —SO 3 H, —SO 4 H, —SO 2 NH 2 , —NHNH 2 , —ONH 2 , —NHC(O)NHNH 2 , —NHC(O)NH 2 , —NHSO 2 H, —NHC(O)H, —NHC(O)OH, —NHOH, —OCH 3 , —OCF 3 , —OCHF 2 , —C(O)CH 3 , unsubstituted alkyl, or unsubstituted heteroalkyl; and

n is independently an integer from 0 to 5.

2. The compound of claim 1 , wherein R 1 is an unsubstituted cyclopentyl or unsubstituted furanyl.

3. The compound of claim 1 , wherein R 2 is hydrogen, halogen, —CF 3 , —CCl 3 , —CN, —OH, —NH 2 , —COOH, —CONH 2 , —NO 2 , —SH, —SO 2 Cl, —SO 3 H, —SO 4 H, —SO 2 NH 2 , —NHNH 2 , —ONH 2 , —NHC(O)NHNH 2 , —NHC(O)NH 2 , —NHSO 2 H, —NHC(O)H, —NHC(O)OH, —NHOH, —OCH 3 , —OCF 3 , —OCHF 2 , —C(O)CH 3 , substituted or unsubstituted C 1 -C 8 alkyl, substituted or unsubstituted 2 to 8 membered heteroalkyl, substituted or unsubstituted C 3 -C 8 cycloalkyl, substituted or unsubstituted 3 to 8 membered heterocycloalkyl, substituted or unsubstituted C 6 -C 10 aryl, or substituted or unsubstituted 5 to 10 membered heteroaryl.

4. The compound of claim 1 , wherein R 2 is hydrogen or unsubstituted C 1 -C 4 alkyl.

5. The compound of claim 1 , wherein R 3 is independently halogen, —CF 3 , —CCl 3 , —CN, —OH, —NH 2 , —COOH, —CONH 2 , —NO 2 , —SH, —SO 2 Cl, —SO 3 H, —SO 4 H, —SO 2 NH 2 , —NHNH 2 , —ONH 2 , —NHC(O)NHNH 2 , —NHC(O)NH 2 , —NHSO 2 H, —NHC(O)H, —NHC(O)OH, —NHOH, —OCH 3 , —OCF 3 , —OCHF 2 , —C(O)CH 3 , unsubstituted C 1 -C 4 alkyl, or unsubstituted 2 to 4 membered heteroalkyl.

6. The compound of claim 1 , wherein the compound has the formula:

7. The compound of claim 1 , wherein the compound has the formula:

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

9. The compound of claim 1 , wherein R 1 is a substituted or unsubstituted C 5 cycloalkyl.

10. The compound of claim 9 , wherein R 1 is unsubstituted cyclopentyl.

Assignments (2)
CONFIRMATORY LICENSE Recorded Jun 13, 2016
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 038966/0799 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 19, 2015
From: MEYEROWITZ, JUSTIN GABRIEL; GUSTAFSON, WILLIAM CLAY; WEISS, WILLIAM A.; HERTZ, NICHOLAS T.; SHOKAT, KEVAN M.
To: THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
Reel/Frame 037335/0243 →
Continuity (3)
Continuation PCTUS2014039238 · May 22, 2014
Provisional Application 61826409 · May 22, 2013
Related Publication 20160250211A1 · Sep 1, 2016
Cited By (1)
US 12,551,482