Abstract: The present invention provides 6-substituted pyridazine compounds of formula (I) which are therapeutically useful as SMARCA2 and/or SMARCA4 degraders. These compounds are useful in the treatment and/or delaying progression of diseases or disorders dependent upon SMARCA2 and/or SMARCA4 in a subject. The present invention also provides preparation of the compounds and pharmaceutical compositions comprising at least one of the compounds of formula (I) or a pharmaceutically acceptable salt, or a stereoisomer or a tautomer or a prodrug thereof.

Abstract: The present invention provides heterocyclic compounds of formula (I), which are therapeutically useful as CBP/EP300 inhibitors. These compounds are useful in the treatment and/or prevention of diseases or disorders mediated by CBP and/or EP300 in an individual. The present invention also provides preparation of the compounds and pharmaceutical compositions comprising at least one of the compounds of formula (I) or a pharmaceutically acceptable salt, or a stereoisomer or a tautomer, an N-oxide or an ester thereof.

Abstract: The present invention provides substituted heterocyclylderivatives of formula (I), which are therapeutically useful, particularly as selective transcriptional CDK inhibitors including CDK7, CDK9, CDK12, CDK13 and CDK18, more particularly transcriptional CDK7 inhibitors. These compounds are useful in the treatment and prevention of diseases and/or disorders associated with selective transcriptional CDKs in a mammal. The present invention also provides preparation of the compounds and pharmaceutical formulations comprising at least one of the substituted heterocyclyl derivatives of formula (I) or a pharmaceutically acceptable salt or a stereoisomer thereof.

Abstract: The present invention provides 5-cyclopropyl-1H-pyrazol-3-yl-amine 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 the preparation of the compounds and pharmaceutical compositions that have at least one of the 5-cyclopropyl-1H-pyrazol-3-yl-amine derivatives of formula (I) or a pharmaceutically acceptable salt, an N-oxide or a stereoisomer thereof.

Abstract: The present invention provides compounds for inhibiting matriptase 2, or a mutant thereof, and compositions and methods of use thereof.

Abstract: The present invention provides substituted pyrazolo[1,3,5] triaziric and pyrazolo[1,5a] pyrimidine derivatives of formula (I), which are therapeutically useful, particularly as selective transcriptional CDK inhibitors including CDK7, CDK9, CDK12, CDK13 and CDK15, more particularly transcriptional CDK7 inhibitors wherein X, ring A, ring B, L1, L2, R1,R2, R3, R4, R6, m, n and p have the meanings given in the specification and pharmaceutically acceptable salts thereof that are useful in the treatment and prevention of disease or disorder associated with selective transcriptional CDKs in a mammal. The present invention also provides preparation of the compounds and pharmaccutical formulations comprising at least one of the substituted pyrazolo [1.5-a] [1-3,5] triazine and pyrazolo[1,5-a] pyrimidine derivatives of formula (I) or a pharmaceutically acceptable salt thereof or a stercoisomer liner thereof.

Abstract: The present invention provides 5-cyclopropyl-1H-pyrazol-3-yl-amine 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 the preparation of the compounds and pharmaceutical compositions that have at least one of the 5-cyclopropyl-1H-pyrazol-3-yl-amine derivatives of formula (I) or a pharmaceutically acceptable salt, an N-oxide or a stereoisomer thereof.

Abstract: The present invention provides substituted heterocyclylderivatives of formula (I), which are therapeutically useful, particularly as selective transcriptional CDK inhibitors including CDK7, CDK9, CDK12, CDK13 and CDK18, more particularly transcriptional CDK7 inhibitors. These compounds are useful in the treatment and prevention of diseases and/or disorders associated with selective transcriptional CDKs in a mammal. The present invention also provides preparation of the compounds and pharmaceutical formulations comprising at least one of the substituted heterocyclyl derivatives of formula (I) or a pharmaceutically acceptable salt or a stereoisomer thereof.

Abstract: The present invention provides substituted pyrazolo[1,5-a][1,3,5]triazine and pyrazolo[1,5-a]pyrimidine derivatives of formula (I), which are therapeutically useful, particularly as selective transcriptional CDK inhibitors including CDK7, CDK9, CDK12, CDK13 and CDK18, more particularly transcriptional CDK7 inhibitors wherein X, ring A, ring B, L1, L2, R1, R2, R3, R4, R6, m, n and p have the meanings given in the specification and pharmaceutically acceptable salts thereof that are useful in the treatment and prevention of diseases or disorder associated with selective transcriptional CDKs in a mammal. The present invention also provides preparation of the compounds and pharmaceutical formulations comprising at least one of the substituted pyrazolo[1,5-a][1,3,5]triazine and pyrazolo[1,5-a]pyrimidine derivatives of formula (I) or a pharmaceutically acceptable salt thereof or a stereoisomer thereof.

Abstract: The present invention provides substituted heterocyclylderivatives of formula (I), which are therapeutically useful, particularly as selective transcriptional CDK inhibitors including CDK7, CDK9, CDK12, CDK13 and CDK18, more particularly transcriptional CDK7 inhibitors. These compounds are useful in the treatment and prevention of diseases and/or disorders associated with selective transcriptional CDKs in a mammal. The present invention also provides preparation of the compounds and pharmaceutical formulations comprising at least one of the substituted heterocyclyl derivatives of formula (I) or a pharmaceutically acceptable salt or a stereoisomer thereof.

Abstract: The present invention provides pyridazine derivatives of formula (I), which are therapeutically useful as SMARCA2/4 degraders. These compounds are useful in the treatment and/or prevention of diseases or disorders dependent upon SMARCA2/4 in a mammal. The present invention also provides preparation of the compounds and pharmaceutical compositions of at least one of the pyridazine derivatives of formula (I) or a pharmaceutically acceptable salt, or a stereoisomer thereof.

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.

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.

Abstract: The present invention provides substituted heterocyclylderivatives of formula (I), which are therapeutically useful, particularly as selective transcriptional CDK inhibitors including CDK7, CDK9, CDK12, CDK13 and CDK18, more particularly transcriptional CDK7 inhibitors. These compounds are useful in the treatment and prevention of diseases and/or disorders associated with selective transcriptional CDKs in a mammal. The present invention also provides preparation of the compounds and pharmaceutical formulations comprising at least one of the substituted heterocyclyl derivatives of formula (I) or a pharmaceutically acceptable salt or a stereoisomer thereof.

Abstract: The present invention provides substituted heterocyclylderivatives of formula (I), which are therapeutically useful, particularly as selective transcriptional CDK inhibitors including CDK7, CDK9, CDK12, CDK13 and CDK18, more particularly transcriptional CDK7 inhibitors. These compounds are useful in the treatment and prevention of diseases and/or disorders associated with selective transcriptional CDKs in a mammal. The present invention also provides preparation of the compounds and pharmaceutical formulations comprising at least one of the substituted heterocyclyl derivatives of formula (I) or a pharmaceutically acceptable salt or a stereoisomer thereof.

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.

Abstract: A compound of formula (I), wherein R3, R4, G, B, M, and Z are as defined in the claims, and pharmaceutically acceptable salts thereof are disclosed. The compounds of formula (1) possess utility as FGFR inhibitors and are useful in the treatment of a condition, where FGFR kinase inhibition is desired, such as cancer.

Abstract: The present invention provides novel spiro[cyclobutane-1,3?-indolin]-2?-one derivatives of formula (I) in which Cy, R1, R2, R4, L, and m have the meaning given in the specification, and pharmaceutically acceptable salts thereof. The compounds of formula (I) are useful as bromodomain inhibitors in the treatment or prevention of diseases or disorders where bromodomain inhibition is desired.

Abstract: The present invention provides substituted heterocyclyl derivatives of formula (I), which are therapeutically useful, particularly as selective transcriptional CDK inhibitors including CDK7, CDK9, CDK12, CDK13 and CDK18, more particularly transcriptional CDK7 inhibitors. These compounds are useful in the treatment and prevention of diseases and/or disorders associated with selective transcriptional CDKs in a mammal. The present invention also provides preparation of the compounds and pharmaceutical formulations comprising at least one of the substituted heterocyclyl derivatives of formula (I) or a pharmaceutically acceptable salt or a stereoisomer thereof.

Abstract: The present invention provides substituted pyrazolo[1,5-a][1,3,5]triazine and pyrazolo[1,5-a]pyrimidine derivatives of formula (I), which are therapeutically useful, particularly as selective transcriptional CDK inhibitors including CDK7, CDK9, CDK12, CDK13 and CDK18, more particularly transcriptional CDK7 inhibitors wherein X, ring A, ring B, L1, L2, R1, R2, R3, R4, R6, m, n and p have the meanings given in the specification and pharmaceutically acceptable salts thereof that are useful in the treatment and prevention of diseases or disorder associated with selective transcriptional CDKs in a mammal. The present invention also provides preparation of the compounds and pharmaceutical formulations comprising at least one of the substituted pyrazolo[1,5-a][1,3,5]triazine and pyrazolo[1,5-a]pyrimidine derivatives of formula (I) or a pharmaceutically acceptable salt thereof or a stereoisomer thereof.