IP Library Granted Patent US 9,359,349
Granted Patent B2
US 9,359,349 · App. 14/491,929 · Granted Jun 7, 2016

Substituted quinazolines as kinase inhibitors

Inventors: Pingda Ren (San Diego, CA); Yi Liu (San Diego, CA); Troy Edward Wilson (Rolling Hills Estates, CA)
Assignee: INTELLIKINE LLC
C07D471/04A61K31/517C07D239/42C07D239/84C07D239/94C07D401/12C07D401/14C07D403/04
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Quick Facts
Patent No.
US 9,359,349
App. No.
14/491,929
Granted
Jun 7, 2016
Kind
B2
Abstract

The present invention provides compounds of Formula I that modulate PI3 kinase activity and methods of treatment of diseases and conditions associated with PI3 kinase activity.

Claims (22)

1. A compound of Formula II:

or a pharmaceutically acceptable salt thereof, wherein

W 4 is N;

R 1 is unsubstituted methyl or methyl substituted with one or more fluoro;

R 2 is aryl, or heteroaryl, each independently substituted with OH or halo;

R 4 is hydrogen; and

R 5 is hydrogen, alkyl, aryl or heteroaryl, wherein the alkyl, aryl or heteroaryl is optionally substituted;

or R 4 and R 5 , taken together with the nitrogen atom to which they are attached form an optionally substituted heteroaryl ring;

wherein, when a moiety is optionally substituted, substituents are each independently selected from R a , —OR b , amino, halo, cyano, nitro, oxo, acyl, alkoxycarbonyl, aminocarbonyl, —OCOR b ,—OCO 2 R a , —OCONR b R c , sulfanyl, sulfinyl, and sulfonyl;

each R a is independently C 1 -C 6 alkyl, cycloalkyl, heterocycloalkyl, alkenyl, alkynyl, aryl, or heteroaryl;

each R b is independently hydrogen or C 1 -C 6 alkyl, cycloalkyl, heterocycloalkyl, aryl, or heteroaryl; and

each R c is independently hydrogen or C 1 -C 4 alkyl; or

R b and R c together with the nitrogen to which they are attached form a heterocycloalkyl group.

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

3. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein R 1 is methyl substituted with one or more fluoro.

4. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein R 2 is aryl, substituted at one or both meta positions.

5. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein R 2 is a bicyclic aryl or bicyclic heteroaryl.

6. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein R 5 is alkyl, aryl, or heteroaryl, each of which is optionally substituted.

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

8. The pharmaceutical composition of claim 7 wherein the composition is formulated as a solid, semi-solid, liquid, or aerosol dosage form.

9. A compound selected from the group consisting of:

or a pharmaceutically acceptable salt thereof.

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 24, 2021
From: INTELLIKINE LLC
To: TAKEDA PHARMACEUTICAL COMPANY LIMITED
Reel/Frame 056754/0087 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 14, 2015
From: REN, PINGDA; LIU, YI; WILSON, TROY EDWARD
To: INTELLIKINE LLC
Reel/Frame 035406/0144 →
Continuity (4)
Continuation 14139723 · Dec 23, 2013
Continuation 12677098
Provisional Application 60997922 · Oct 4, 2007
Related Publication 20150141442A1 · May 21, 2015