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US 2024/0246950 A1Published application
Anilino-Pyrazole Derivatives, Compositions and Methods Thereof
AssigneeEnsem Therapeutics
InventorTao Liu
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Abstract
The invention provides novel anilino-pyrazole derivatives as a cyclin-dependent kinase 2 (CDK2) inhibitors. The invention also provides pharmaceutical compositions comprising the compounds and methods thereof for treating various conditions, diseases and disorders associated with or related to CDK2 activities, or associated with abnormal cell growth, such as tumor growth and cancer.
Claims21
1-89. (canceled)
A compound having the structural Formula I:
- or a pharmaceutically acceptable salt thereof,
- wherein
- Ring A is a 4- to 7-membered carbocyclic ring;
- each of R1 and R2 is independently selected from the group consisting of H, unsubstituted C1-C6 alkyl, and C3-C6 unsubstituted carbocyclic ring;
- or R1 and R2, together with the N atom they are bound to, are joined to form a 4- to 7-membered, unsubstituted heterocyclic ring;
- each R3 is independently selected from the group consisting of halogen, OH, CN, unsubstituted C1-6 alkyl, unsubstituted C1-6 alkoxy, NO2, NRR′, or two R3's, along with the carbon atom(s) they are bound to, form a 3- to 5-membered unsubstituted carbocyclic ring;
- R4 is H, halogen, C1-4 alkyl, CN, NRR′, or C(O)NRR′;
- R5 is
- wherein
- Ring B is a 4- to 7-membered carbocyclic or heterocyclic ring optionally comprising a —S(O)2—, —C(O)—, —S(O)2NR—, —S(O)2NRC(O)—, —C(O)NR—, —OC(O)NR—, or —C(O)NRC(O)— group;
- each of Y1 and Y2 is CR6 or N, and each of Y3 and Y4 is C, CR6 or N;
- provided that not more than one of Y1, Y2, Y3 and Y4 is N, and either Y3 or Y4 is C and being the positions where R5 may be bonded to the rest of the compound;
- each R6 is independently selected from the group consisting of halogen, OH, CN, unsubstituted C1-6 alkyl, unsubstituted C1-4 alkoxy, and C(O)NRR′;
- each R7 is independently selected from the group consisting of halogen, OR, CN, unsubstituted C1-6 alkyl, and unsubstituted C1-4 alkoxy, or two R7's, along with the carbon atom(s) they are bound to, form a 3- to 6-membered unsubstituted carbocyclic or heterocyclic ring;
- each of R and R′ is independently selected from H, unsubstituted C1-6 alkyl, or unsubstituted 4- to 6-membered carbocyclic ring, or where R and R′ are attached to the same N atom, together form an unsubstituted 4- to 6-membered heterocyclic ring;
- i is 0, 1,2, 3,4 or 5;
- and
- k is 0, 1, 2, 3, 4 or 5.
15 more elements
A compound selected from:
- or a pharmaceutically acceptable salt thereof.
A compound selected from
- or a pharmaceutically acceptable salt thereof.
Dependencies are inferred from the claim text.