IP Library Granted Patent US 9,714,247
Granted Patent B2
US 9,714,247 · App. 15/276,604 · Granted Jul 25, 2017

Multiple kinase pathway inhibitors

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Quick Facts
Patent No.
US 9,714,247
App. No.
15/276,604
Granted
Jul 25, 2017
Kind
B2
Abstract

Kinase with inhibitory activity against kinases disposed in multiple signaling pathways and their therapeutic uses.

Claims (25)

1. A compound having the following Structural Formula (I):

or a pharmaceutically acceptable salt or tautomer thereof, wherein:

R1 is a nitrogen-containing six-membered heteroaryl in which at least one ring nitrogen atom is adjacent to the carbon linking R1 to the amino group, substituted with 1, 2, or 3 groups independently selected from the group consisting of:

(C1-C3)alkylamino(C2-C3)alkoxyl;

(C1-C3) dialkylamino(C2-C3)alkoxyl;

(C1-C3)alkylamino(C2-C3)alkylamino;

(C1-C3)dialkylamino(C2-C3)alkylamino;

(C1-C3)alkylamino(C2-C3)dialkylamino;

(C1-C3)dialkylamino(C2-C3)dialkylamino; and

R2 is:

hydrogen;

C1-C6 alkyl, optionally substituted with 1, 2, or 3 groups selected from hydroxyl, methoxyl, ethoxyl, methylamino, N,N-dimethyl amino, ethylamino, N,N-diethylamino and methylsulfanyl; or

a three- to six-membered cycloalkyl, optionally substituted with 1, 2, or 3 groups selected from hydroxyl, methoxyl, ethoxyl, methylamino, N,N-dimethyl amino, ethylamino, N,N-diethylamino and methylsulfanyl;

R3 is phenyl, optionally substituted with 1, 2, or 3 substituents selected from the group consisting of fluoro, chloro, hydroxyl, methyl, methoxyl, —SCH 3 and trifluoromethyl.

2. The compound of claim 1 , wherein R1 is pyridyl.

3. The compound of claim 1 , wherein R1 is substituted with (C1-C3) dialkylamino(C2-C3)alkoxyl or (C1-C3)dialkylamino(C2-C3)alkylamino.

4. The compound of claim 1 , wherein R1 is substituted with a substituent having one of the following structures:

5. The compound of claim 1 , wherein R2 is methyl, ethyl or isopropyl.

6. The compound of claim 1 , wherein R2 is cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl.

7. The compound of claim 1 , wherein R3 has one of the following structures:

8. The compound of claim 1 , wherein the compound has one of the following structures:

9. A pharmaceutical composition comprising:

(a) a pharmaceutically acceptable vehicle; and

(b) a compound of any of claim 1 , or a pharmaceutically acceptable salt or tautomer thereof.

10. A method of inhibiting kinase activity, comprising contacting a Bruton's tyrosine kinase with a compound of claim 1 , or a pharmaceutically acceptable salt or tautomer thereof, thereby inhibiting kinase activity of the Bruton's tyrosine kinase.

Assignments (1)
SECURITY INTEREST Recorded Nov 17, 2016
From: TOLERO PHARMACEUTICALS, INC.
To: SUMITOMO DAINIPPON PHARMA CO., LTD.
Reel/Frame 040362/0884 →