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US 10,894,786 B2Granted
Substituted pyrazole derivatives as selective CDK12/13 inhibitors
AssigneeAurigene Discovery Technologies Limited
InventorsRamulu Poddutoori, Susanta Samajdar, Subhendu Mukherjee
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Abstract
The present invention provides substituted pyrazole derivatives of formula (I) which are therapeutically useful as selective CDK12/13 inhibitors. These compounds are useful in the treatment and/or prevention of diseases and/or disorders associated with CDK12/13 in a mammal. The present invention also provides preparation of the compounds and pharmaceutical compositions with at least one of the substituted pyrazole derivatives of formula (I) or a pharmaceutically acceptable salt, an N-oxide or a stereoisomer thereof.
Claims25
A compound of formula (I):
- or a pharmaceutically acceptable salt, a N-oxide or a stereoisomer thereof;
- wherein,
- ------ is an optional bond;
- each X1, X2 and X3 are independently CR3 or N;
- each Y1 and Y2 are independently C, CH or N;
- R1 is hydrogen or alkyl;
- R2 is
- or —C≡N;
- each R3 is independently selected from hydrogen, halogen, cyano and alkyl;
- R4 is hydrogen, alkyl or —(CH2)n—NRaRb;
- R4′ & R4″ are each independently hydrogen or alkyl;
- R5 is hydrogen or alkyl;
- Ra and Rb are each independently hydrogen or alkyl;
- alternatively, Ra and Rb together with the nitrogen atom to which they are attached form an optionally substituted heterocyclic ring containing 0-2 additional heteroatoms independently selected from N, O and S;
- n is 1 to 3;
- and
- p and q are each independently selected from 0 to 2.
14 more elements
Dependencies are inferred from the claim text.