US 12,281,126 B2
Inhibitors of cyclin-dependent kinase 7 and uses thereof
Nathanael S. Gray, Boston, MA (US); Tinghu Zhang, Brookline, MA (US); Nicholas Paul Kwiatkowski, Brookline, MA (US); Jie Jiang, Brookline, MA (US); Mingfeng Hao, Hefei (CN); and Zhixiang He, Brookline, MA (US)
Assigned to Dana-Farber Cancer Institute, Inc., Boston, MA (US)
Appl. No. 17/418,353
Filed by Dana-Farber Cancer Institute, Inc., Boston, MA (US)
PCT Filed Dec. 27, 2019, PCT No. PCT/US2019/068835
§ 371(c)(1), (2) Date Jun. 25, 2021,
PCT Pub. No. WO2020/140098, PCT Pub. Date Jul. 2, 2020.
Claims priority of provisional application 62/786,328, filed on Dec. 28, 2018.
Prior Publication US 2022/0089611 A1, Mar. 24, 2022
This patent is subject to a terminal disclaimer.
Int. Cl. C07D 519/00 (2006.01); A61K 31/4162 (2006.01); C07D 487/04 (2006.01)
CPC C07D 519/00 (2013.01) [A61K 31/4162 (2013.01); C07D 487/04 (2013.01)] 15 Claims
 
1. A compound of Formula (I):

OG Complex Work Unit Chemistry
or a pharmaceutically acceptable salt, solvate, hydrate, tautomer, stereoisomer, or isotopically labeled derivative thereof, wherein:
Ring A is aryl, or heteroaryl;
R1 is of the formula —NHC(O)CH═CH2 or L3;
wherein:
L3 is a substituted or unsubstituted C1-4 hydrocarbon chain;
m is 0 or 1;
L is a single bond or —C(═O)—;
one of R9 and R10 is hydrogen and the other is —(CH2) N (CH3)2;
p is 0 or 1 such that when p=0, then D=piperidinyl, 1,2,3,4-tetrahydroisoquinolinyl, or

OG Complex Work Unit Chemistry
and when p=1, then D=tetrahydropyranyl or tetrahydrofuryl;
R11 is substituted or unsubstituted alkyl; and
q is 0 or 1.