A61K31/5025

INHIBITORS OF ENL/AF9 YEATS

Methods and compositions for treating leukemia are disclosed. Acylated 6-aminoindoles, acylated 6-aminopyrrolopyridines and acylated 3-aminopyrrolo[3,2-c]pyridazines of the following formula

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inhibit ENL/AF9 YEATS and are therefore useful for treating leukemia.

HETEROCYCLIC COMPOUNDS AS IMMUNOMODULATORS

Disclosed are compounds of Formula (I′), methods of using the compounds as immunomodulators, and pharmaceutical compositions comprising such compounds. The compounds inhibit PD-1/PD-L1 interaction and are useful in treating, preventing or ameliorating diseases or disorders such as cancer or infections.

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HETEROCYCLIC COMPOUNDS AS IMMUNOMODULATORS

Disclosed are compounds of Formula (I′), methods of using the compounds as immunomodulators, and pharmaceutical compositions comprising such compounds. The compounds inhibit PD-1/PD-L1 interaction and are useful in treating, preventing or ameliorating diseases or disorders such as cancer or infections.

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Heterocyclic inhibitors of monocarboxylate transporters

The invention provides compounds of formulae A, B, and C as described herein that inhibit monocarboxylate transporters, such as MCT1 and MCT4. Compounds of the invention can be used for treatment of a condition in a patient, wherein the condition is characterized by the heightened activity or by the high prevalence of MCT1 and/or MCT4, such as cancer or type II diabetes.

Heterocyclic inhibitors of monocarboxylate transporters

The invention provides compounds of formulae A, B, and C as described herein that inhibit monocarboxylate transporters, such as MCT1 and MCT4. Compounds of the invention can be used for treatment of a condition in a patient, wherein the condition is characterized by the heightened activity or by the high prevalence of MCT1 and/or MCT4, such as cancer or type II diabetes.

Heterocyclic inhibitors of monocarboxylate transporters

The invention provides compounds of formulae A, B, and C as described herein that inhibit monocarboxylate transporters, such as MCT1 and MCT4. Compounds of the invention can be used for treatment of a condition in a patient, wherein the condition is characterized by the heightened activity or by the high prevalence of MCT1 and/or MCT4, such as cancer or type II diabetes.

METHOD FOR PRODUCING 3,6-DISUBSTITUTED-IMIDAZO[1,2-B]PYRIDAZINE DERIVATIVE
20230227459 · 2023-07-20 ·

This disclosure relates to a crystal of 3-{4-[(2R)-2-aminopropoxy]phenyl}-N-[(1R)-1-(3-fluorophenyl)ethyl]imidazo[1,2-b]pyridazin-6-amine adipate.

PYRUVATE KINASE ACTIVATORS FOR USE IN TREATING BLOOD DISORDERS

Described herein are compounds that activate pyruvate kinase, pharmaceutical compositions and methods of use thereof. These compounds are represented by Formula (I) wherein R.sup.1, R.sup.2, R.sup.a, R.sup.b, R.sup.j, R.sup.k, and Q are as defined herein.

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PYRUVATE KINASE ACTIVATORS FOR USE IN TREATING BLOOD DISORDERS

Described herein are compounds that activate pyruvate kinase, pharmaceutical compositions and methods of use thereof. These compounds are represented by Formula (I) wherein R.sup.1, R.sup.2, R.sup.a, R.sup.b, R.sup.j, R.sup.k, and Q are as defined herein.

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Methods, compositions, and uses of novel FYN kinase inhibitors
11701353 · 2023-07-18 · ·

The present invention provides methods for inhibiting Fyn kinase, using 5-3-pyridin-2-amine, 6-3-imidazo[1,2-a] pyrazine, 6-3-imidazo[1,2-b] pyridazine, N-(5-imidazo [2,1-b][1,3,4] thiadiazol-2-yl)-amine, 4-3-1H-pyrazolo[3,4-b] pyridine, and N-(3-imidazo [1,2-b] pyridazin-6-yl) amine compounds and methods of treatment, prevention, inhibition or amelioration of diseases and conditions associated with Fyn kinase using such compounds.