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US 11,633,394 B2Granted
Substituted alkynylene compounds as anticancer agents
AssigneeAurigene Oncology Limited
InventorsDinesh Chikkanna, Vinayak V. Khairnar, Muralidhara Ramachandra, Leena Khare Satyam
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Abstract
The present invention relates to substituted alkynylene compounds represented by the compounds of formula (I), pharmaceutically acceptable salts and stereoisomers thereof. The present invention further provides the therapeutic uses of the compounds of formula (I) as anti-cancer agents.
Claims30
A compound of formula (I)
- or a pharmaceutically acceptable salt or a stereoisomer thereof;
- wherein,
- A represents aryl or heteroaryl;
- X represents N—Ry or absent;
- Y represents O, S or NCN;
- B represents aryl, cycloalkyl or heterocycloalkyl;
- wherein the aryl, cycloalkyl or heterocycloalkyl are optionally substituted with one or more groups selected from alkyl, halo and oxo;
- R1 represents unsubstituted alkyl;
- R2 represents hydrogen or unsubstituted alkyl;
- or R1 and R2 together with the carbon atoms to which they are attached form 3- to 5-membered cycloalkyl ring;
- R3 represents —C(O)Ra, —S(O)2Ra, —NHS(O)2Ra, —NRbC(O)Ra, ═NORa, heteroaryl, heterocycloalkyl or (heterocycloalkyl)alkyl-;
- wherein the heteroaryl and heterocycloalkyl are optionally substituted with one or more groups selected from alkyl, halo, oxo and —C(O)Rx;
- R4 represents alkyl, halo, haloalkyl, cyano, alkoxy, aryloxy, hydroxyalkyl, acetylene, acyl, hydroxy, cycloalkyl or —N(Rx)2;
- wherein the alkoxy is unsubstituted or substituted with unsubstituted phenyl, and the cycloalkyl is optionally substituted with alkyl;
- Ra represents alkyl, alkenyl, haloalkyl, cycloalkyl or heterocycloalkyl;
- wherein the alkyl, alkenyl, haloalkyl, cycloalkyl and heterocycloalkyl are optionally substituted with one or more groups selected from alkyl, halo, aryl, cycloalkyl, haloalkyl, amino, amido, alkylamino, aminoalkyl, hydroxyl, cyano, alkoxy, alkoxyaryl, aryloxy, hydroxyalkyl, carboxylic acid, ester, thioester, oxo(═O) and —C(O)Rx;
- Rx represents hydrogen, alkyl, alkenyl, acyl or —C(O)-cycloalkyl;
- Ry represents hydrogen or alkyl;
- Rb represents hydrogen, alkyl or alkenyl;
- ‘m’ represents 0, 1, 2 or 3.
17 more elements
A compound selected from:
- Example
- Structure
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- or a pharmaceutically acceptable salt or a stereoisomer thereof.
84 more elements
Dependencies are inferred from the claim text.