C07D471/20

SUBSTITUTED PYRAZOLO[1,5-a]PYRIMIDINES AS BRUTON'S TYROSINE KINASE MODULATORS
20230013862 · 2023-01-19 ·

The invention is fused heterocyclic compounds of formula (I), and salts thereof, compositions thereof, and methods of use therefor. In particular, disclosed herein are certain fused heterocyclic compounds that can be useful for inhibiting protein kinase, including Bruton's tyrosine kinase (Btk), and for treating disorders mediated thereby.

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SUBSTITUTED PYRAZOLO[1,5-a]PYRIMIDINES AS BRUTON'S TYROSINE KINASE MODULATORS
20230013862 · 2023-01-19 ·

The invention is fused heterocyclic compounds of formula (I), and salts thereof, compositions thereof, and methods of use therefor. In particular, disclosed herein are certain fused heterocyclic compounds that can be useful for inhibiting protein kinase, including Bruton's tyrosine kinase (Btk), and for treating disorders mediated thereby.

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MELANOCORTIN 4 RECEPTOR ANTAGONISTS AND USES THEREOF

Described herein are compounds of Formula I:

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and their pharmaceutically acceptable salts, wherein R.sup.1, R.sup.2, R.sup.3, X.sup.1, Y.sup.1, Y.sup.2, Y.sup.3, Y.sup.4 and Y.sup.5 are defined herein; their use as MC4R antagonists; pharmaceutical compositions containing such compounds and salts; the use of such compounds and salts to treat, for example, cachexia, anorexia, or anorexia nervosa; and intermediates and processes for preparing such compounds and salts.

MELANOCORTIN 4 RECEPTOR ANTAGONISTS AND USES THEREOF

Described herein are compounds of Formula I:

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and their pharmaceutically acceptable salts, wherein R.sup.1, R.sup.2, R.sup.3, X.sup.1, Y.sup.1, Y.sup.2, Y.sup.3, Y.sup.4 and Y.sup.5 are defined herein; their use as MC4R antagonists; pharmaceutical compositions containing such compounds and salts; the use of such compounds and salts to treat, for example, cachexia, anorexia, or anorexia nervosa; and intermediates and processes for preparing such compounds and salts.

COMPOUNDS AND COMPOSITIONS FOR INHIBITING THE ACTIVITY OF HIF2-alpha AND THEIR METHODS OF USE

The present invention relates to compounds of formula (I)

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or a pharmaceutically acceptable salt form thereof, wherein the substituents are as defined in the specification; to intermediates in the preparation of the compounds, to pharmaceutical compositions comprising the compounds and to the use of the compounds in the treatment of disease.

COMPOUNDS AND COMPOSITIONS FOR INHIBITING THE ACTIVITY OF HIF2-alpha AND THEIR METHODS OF USE

The present invention relates to compounds of formula (I)

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or a pharmaceutically acceptable salt form thereof, wherein the substituents are as defined in the specification; to intermediates in the preparation of the compounds, to pharmaceutical compositions comprising the compounds and to the use of the compounds in the treatment of disease.

Spiro compounds as inhibitors of KRAS

Disclosed are spirocyclic compounds of Formula I, methods of using the compounds for inhibiting KRAS activity and treating cancer, and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders associated with KRAS activity such as cancer.

Spiro compounds as inhibitors of KRAS

Disclosed are spirocyclic compounds of Formula I, methods of using the compounds for inhibiting KRAS activity and treating cancer, and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders associated with KRAS activity such as cancer.

Heterobicyclic inhibitors of MAT2A and methods of use for treating cancer

The present disclosure provides for compounds according to Formula I or Formula II and their pharmaceutically acceptable salts, stereoisomers, and/or tautomers thereof. Also provided are pharmaceutical compositions and the compounds of formulae I and II for use in methods of treating cancers, via inhibition of MAT2A, including some cancers in which the gene encoding methylthioadenosine phosphorylase (MTAP) is deleted and/or not fully functioning. ##STR00001##

Heterobicyclic inhibitors of MAT2A and methods of use for treating cancer

The present disclosure provides for compounds according to Formula I or Formula II and their pharmaceutically acceptable salts, stereoisomers, and/or tautomers thereof. Also provided are pharmaceutical compositions and the compounds of formulae I and II for use in methods of treating cancers, via inhibition of MAT2A, including some cancers in which the gene encoding methylthioadenosine phosphorylase (MTAP) is deleted and/or not fully functioning. ##STR00001##