Patent classifications
C07D215/54
SUBSTITUTED AMINOBENZYL HETEROARYL COMPOUNDS AS EGFR AND/OR PI3K INHIBITORS
This disclosure is in the field of medicinal chemistry, and relates to a new class of small-molecules having the Formula I,
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or a pharmaceutically acceptable salt or solvate thereof, or an enantiomer, a mixture of enantiomers, a mixture of two or more diastereomers, or an isotopic variant thereof, wherein the variables Ring A, X, R.sub.1a, R.sub.1b, R.sub.2, R.sub.3, R.sub.4, m, n, and p are described herein, which function as dual inhibitors of EGFR proteins and PI3K proteins. The disclosure further relates to the use of the compounds described herein as therapeutics for the treatment of diseases and conditions mediated by EGFR proteins and/or PI3K proteins, such as cancer and other diseases.
Stilbene derivatives for the treatment of CNS and other disorders
The present application discloses stilbene derivative compounds and compositions, and methods for treating ocular diseases, neurological disorders and protein aggregation-related disorders in patients using the compounds and compositions as disclosed herein.
Stilbene derivatives for the treatment of CNS and other disorders
The present application discloses stilbene derivative compounds and compositions, and methods for treating ocular diseases, neurological disorders and protein aggregation-related disorders in patients using the compounds and compositions as disclosed herein.
ACETAMIDO DERIVATIVES AS DNA POLYMERASE THETA INHIBITORS
Disclosed herein are certain acetamido derivatives that are DNA Polymerase Theta (Polθ) inhibitors of Formula (I).
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Also, disclosed are pharmaceutical compositions comprising such compounds and methods of treating diseases treatable by inhibition of Polθ such as cancer, including homologous recombination (HR) deficient cancers.
ACETAMIDO DERIVATIVES AS DNA POLYMERASE THETA INHIBITORS
Disclosed herein are certain acetamido derivatives that are DNA Polymerase Theta (Polθ) inhibitors of Formula (I).
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Also, disclosed are pharmaceutical compositions comprising such compounds and methods of treating diseases treatable by inhibition of Polθ such as cancer, including homologous recombination (HR) deficient cancers.
PDE9 INHIBITOR AND USE THEREOF
The present invention relates to the technical field of pharmaceuticals, and particularly to a PDE9 inhibitor compound of formula (I) or a pharmaceutically acceptable salt or an isomer thereof. The present invention also relates to pharmaceutical formulations, pharmaceutical compositions and use thereof. R.sub.1, R.sub.2, ring A, L, m and n are defined as in the specification. The compound of the present invention can be used in the manufacture of a medicament for treating or preventing the PDE9-mediated related disease.
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KDM1A INHIBITORS FOR THE TREATMENT OF DISEASE
Disclosed herein are new compounds and compositions and their application as pharmaceuticals for the treatment of diseases. Methods of inhibition of KDM1A, methods of increasing gamma globin gene expression, and methods to induce differentiation of cancer cells in a human or animal subject are also provided for the treatment of diseases such as acute myelogenous leukemia.
KDM1A INHIBITORS FOR THE TREATMENT OF DISEASE
Disclosed herein are new compounds and compositions and their application as pharmaceuticals for the treatment of diseases. Methods of inhibition of KDM1A, methods of increasing gamma globin gene expression, and methods to induce differentiation of cancer cells in a human or animal subject are also provided for the treatment of diseases such as acute myelogenous leukemia.
BENZOPYRIDONE HETEROCYCLIC COMPOUND AND USE THEREOF
A compound represented by formula I, or a pharmaceutically acceptable salt thereof, or a stereoisomer thereof, or a tautomer thereof, or a hydrate thereof, or a solvate thereof, or a metabolite thereof, or a prodrug thereof. R.sub.1-R.sub.5 and group A are as defined in the description. The compound is used for the preparation of drugs for treating diseases caused by KRAS G12C mutation and for treating and/or preventing cancers.
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BENZOPYRIDONE HETEROCYCLIC COMPOUND AND USE THEREOF
A compound represented by formula I, or a pharmaceutically acceptable salt thereof, or a stereoisomer thereof, or a tautomer thereof, or a hydrate thereof, or a solvate thereof, or a metabolite thereof, or a prodrug thereof. R.sub.1-R.sub.5 and group A are as defined in the description. The compound is used for the preparation of drugs for treating diseases caused by KRAS G12C mutation and for treating and/or preventing cancers.
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