IP Library Granted Patent US 9,453,028
Granted Patent B2
US 9,453,028 · App. 14/754,415 · Granted Sep 27, 2016

Protein kinase C inhibitors and uses thereof

Inventors: Haoran Zhao (Foster City, CA); Rao Kolluri (Foster City, CA); Carlos Valdez (San Ramon, CA); Kin Tso (San Francisco, CA); Rajinder Singh (Belmont, CA); John Ramphal (Union City, CA)
Assignee: Rigel Pharmaceuticals, Inc.
C07D498/04A61K31/5383C07D498/14
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Quick Facts
Patent No.
US 9,453,028
App. No.
14/754,415
Granted
Sep 27, 2016
Kind
B2
Abstract

This disclosure concerns compounds which are useful as inhibitors of protein kinase C (PKC) and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of PKC. This disclosure also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.

Claims (11)

1. A compound selected from the group consisting of:

N2-(4,4-dimethyl-4H-benzo[b]tetrazolo[1,5-d][1,4]oxazin-8-yl)-5-fluoro-N4-(2,2,6,6-tetramethylpiperidin-4-yl)pyrimidine-2,4-diamine; and

N2-(4,4-dimethyl-4H-benzo[b]tetrazolo[1,5-d][1,4]oxazin-8-yl)-5-fluoro-N4-(1,2,2,6,6-pentamethylpiperidin-4-yl)pyrimidine-2,4-diamine,

or a salt or stereoisomer thereof.

2. The compound of claim 1 , wherein the compound is:

N2-(4,4-dimethyl-4H-benzo[b]tetrazolo[1,5-d][1,4]oxazin-8-yl)-5-fluoro-N4-(2,2,6,6-tetramethylpiperidin-4-yl)pyrimidine-2,4-diamine.

3. The compound of claim 1 , wherein the compound is:

N2-(4,4-dimethyl-4H-benzo[b]tetrazolo[1,5-d][1,4]oxazin-8-yl)-5-fluoro-N4-(1,2,2,6,6-pentamethylpiperidin-4-yl)pyrimidine-2,4-diamine.

4. A pharmaceutical composition comprising a compound of claim 1 and a pharmaceutically acceptable carrier.

5. A pharmaceutical composition comprising a compound of claim 2 and a pharmaceutically acceptable carrier.

6. A pharmaceutical composition comprising a compound of claim 3 and a pharmaceutically acceptable carrier.

Assignments (2)
SECURITY INTEREST Recorded Aug 25, 2022
From: RIGEL PHARMACEUTICALS, INC.
To: MIDCAP FINANCIAL TRUST
Reel/Frame 061327/0712 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 22, 2015
From: ZHAO, HAORAN; KOLLURI, RAO; VALDEZ, CARLOS; TSO, KIN; SINGH, RAJINDER; RAMPHAL, JOHN
To: RIGEL PHARMACEUTICALS, INC.
Reel/Frame 036152/0777 →
Continuity (5)
Continuation 13760666 · Feb 6, 2013
Continuation 12687054 · Jan 13, 2010
Provisional Application 61145021 · Jan 15, 2009
Provisional Application 61147353 · Jan 26, 2009
Related Publication 20150376203A1 · Dec 31, 2015