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US 2018/0008604 A1Published application
Covalent inhibitors of cdk-7
AssigneeNewave Pharmaceutical Inc.
InventorsYi Chen, Yan Lou
Life of this patent
Estimating the term…
Abstract
The disclosure includes compounds of Formula (I) wherein R0, R1, R2, R3, R4, R5, and L are defined herein. Also disclosed is a method for treating a neoplastic disease, autoimmune disease, and inflammatory disorder with these compounds.
Claims10
A compound of Formula (I), or an N-oxide thereof, or a pharmaceutically acceptable salt, solvate, polymorph, tautomer, stereoisomer, an isotopic form, or a prodrug of said compound of Formula (I) or N-oxide thereof:
- wherein
- A is cycloalkyl, heterocycloalkyl, cycloalkenyl, heterocycloalkenyl, aryl, heteroaryl, fused hetero-bicyclic, or spiro-heterocyclic;
- each of B, and C, independently, is cycloalkyl, cycloalkenyl, heterocycloalkyl, heterocycloalkenyl, aryl, or heteroaryl;
- each of Z1, Z2, Z3, and Z4 independently, is a bond, (CRaRb)p, (CRaRb)pN(Ra)(CRaRb)q, N(Ra)(CRaRb)qN(Ra), (CRaRb)pO(CRaRb)q, (CRaRb)pC═C(CRaRb)q, (CRaRb)pC≡C(CRaRb)q, C(Ra)═N, O, S, C(O), N(Ra), S(O2), OC(O), C(O)O, OSO2, S(O2)O, C(O)S, SC(O), C(O)C(O), C(O)N(Ra), N(Ra)C(O), S(O2)N(Ra), N(Ra)S(O2), OC(O)O, OC(O)S, OC(O)N(Ra), OC(O)N(Ra)(CRaRb)p+1N(Ra)(CRaRb)q, N(Ra)C(O)O, N(Ra)C(O)S, N(Ra)C(O)N(Rb), (CRaRb)pN(Ra)C(O)(CRaRb)q, or (CRaRb)pC(O)N(Ra)(CRaRb)q;
- each of m, n, p, and q independently, is 0, 1, 2, 3, or 4;
- Warhead is
- L1 is N(R7) if the atom which L1 connects to ring A is a carbon atom;
- or L1 is a direct bond if ring A is a heterocycloalkyl, heterocycloalkenyl, or heteroaryl and the atom which L1 connects to ring A is a nitrogen atom;
- L2 is (CRaRb)sC═C(CRaRb)r in which each of r, and s independently, is 1, 2, 3, or 4;
- each of W1, and W2 independently, is C(R4) or N;
- each of R1, R2, R3, R4, R5, R6, and R7, independently, is H, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, heterocycloalkyl, heterocycloalkenyl, aryl, heteroaryl, halo, nitro, oxo, cyano, —ORa, —SRa, —NRbRc, —C(O)Ra, —S(O)Ra, —SO2Ra, —P(O)RbRc, —C(O)N(Rb)Rc, —N(Rb)C(O)Rc, —C(O)ORa, —OC(O)Ra, —SO2N(Rb)Rc, —N(Rb)SO2Rc, -alkyl-Ra, -alkyl-C(O)Ra, -alkyl-NRbRc, -alkyl-C(O)N(Rb)Rc, -alkyl-N(Rb)RcC(O), or -alkyl-N(Rb)SO2Rc;
- and
- each of Ra, Rb, Ra, Rb, and Rc, independently, is H, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, heterocycloalkyl, heterocycloalkenyl, aryl, heteroaryl, halo, cyano, amine, nitro, hydroxy, —C(O)NHOH, alkoxy, alkoxyalkyl, haloalkyl, hydroxyalkyl, aminoalkyl, alkylcarbonyl, alkoxycarbonyl, alkylcarbonylamino, dialkylamino, or alkylamino.
10 more elements
Dependencies are inferred from the claim text.