Patent classifications
C07D513/20
MACROCYCLIC OREXIN RECEPTOR AGONISTS AND USES THEREOF
Provided herein are compounds of Formula (I), (I), or pharmaceutically acceptable salt thereof, wherein m, n, p, A.sub.1, A.sub.2, A.sub.3, A.sub.4, L, R.sub.1, R.sub.2, R.sub.3, R.sub.4, Formula (II), (II), V, X, Y and Z are defined herein. Also provided herein are pharmaceutical compositions comprising a compound of Formula (I) or pharmaceutically acceptable salt thereof, and methods of using a compound of Formula (I) or pharmaceutically acceptable salt thereof, e.g., in the treatment of a disease or disorder that is treatable by administration of an Orexin agonist.
##STR00001##
MACROCYCLIC OREXIN RECEPTOR AGONISTS AND USES THEREOF
Provided herein are compounds of Formula (I), (I), or pharmaceutically acceptable salt thereof, wherein m, n, p, A.sub.1, A.sub.2, A.sub.3, A.sub.4, L, R.sub.1, R.sub.2, R.sub.3, R.sub.4, Formula (II), (II), V, X, Y and Z are defined herein. Also provided herein are pharmaceutical compositions comprising a compound of Formula (I) or pharmaceutically acceptable salt thereof, and methods of using a compound of Formula (I) or pharmaceutically acceptable salt thereof, e.g., in the treatment of a disease or disorder that is treatable by administration of an Orexin agonist.
##STR00001##
Tricyclic compounds as glycogen synthase kinase 3 (GSK3) inhibitors and uses thereof
The present disclosure provides compounds of Formula (I), and salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, and prodrugs thereof. The provided compounds may be useful for inhibiting kinases, e.g., glycogen synthase kinase 3 (GSK3). The provided compounds may be able to selectively inhibit GSK3a, as compared to GSK3P and/or other kinases. The present disclosure further provides pharmaceutical compositions, kits, and methods of use, each of which involve the compounds. The compounds, pharmaceutical compositions, and kits may be useful for treating diseases associated with aberrant activity of GSK3a (e.g., Fragile X syndrome, attention deficit hyperactivity disorder (ADHD), childhood seizure, intellectual disability, diabetes, acute myeloid leukemia (AML), autism, and psychiatric disorder). ##STR00001##
Tricyclic compounds as glycogen synthase kinase 3 (GSK3) inhibitors and uses thereof
The present disclosure provides compounds of Formula (I), and salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, and prodrugs thereof. The provided compounds may be useful for inhibiting kinases, e.g., glycogen synthase kinase 3 (GSK3). The provided compounds may be able to selectively inhibit GSK3a, as compared to GSK3P and/or other kinases. The present disclosure further provides pharmaceutical compositions, kits, and methods of use, each of which involve the compounds. The compounds, pharmaceutical compositions, and kits may be useful for treating diseases associated with aberrant activity of GSK3a (e.g., Fragile X syndrome, attention deficit hyperactivity disorder (ADHD), childhood seizure, intellectual disability, diabetes, acute myeloid leukemia (AML), autism, and psychiatric disorder). ##STR00001##
PIPERIDINE CARBOXAMIDE AZAINDANE DERIVATIVE, METHOD FOR PREPARING SAME, AND USE THEREOF
The present application relates to a substituted piperidine carboxamide azaindane derivative, a method for preparing same, and use of a pharmaceutical composition containing the derivative or a deuterated derivative in medicine. Specifically, the present application relates to a substituted piperidine carboxamide azaindane derivative represented by general formula (I), a method for preparing same, a pharmaceutically acceptable salt thereof, and use thereof as a CGRP receptor antagonist in preventing and/or treating CORP-related diseases, in particular the field of migraine. The definition of each substituent in general formula (I) is the same as that in the specification.
##STR00001##
PIPERIDINE CARBOXAMIDE AZAINDANE DERIVATIVE, METHOD FOR PREPARING SAME, AND USE THEREOF
The present application relates to a substituted piperidine carboxamide azaindane derivative, a method for preparing same, and use of a pharmaceutical composition containing the derivative or a deuterated derivative in medicine. Specifically, the present application relates to a substituted piperidine carboxamide azaindane derivative represented by general formula (I), a method for preparing same, a pharmaceutically acceptable salt thereof, and use thereof as a CGRP receptor antagonist in preventing and/or treating CORP-related diseases, in particular the field of migraine. The definition of each substituent in general formula (I) is the same as that in the specification.
##STR00001##
COMPOUNDS AS SUMO ACTIVATING ENZYME INHIBITORS
Disclosed in the present disclosure are compounds as SUMO activating enzyme inhibitors. Specifically, the present disclosure relates to a compound of general formula (1), a method for preparing same, and use of the compound of general formula (1) and isomers, crystalline forms, pharmaceutically acceptable salts, hydrates or solvates thereof as SAE inhibitors. The compound and the isomer thereof, the crystalline form thereof, the pharmaceutically acceptable salt thereof, the hydrate thereof, or the solvate thereof of the present disclosure can be used in preparing a medicament for treating or preventing a disease related to SAE protein.
##STR00001##
COMPOUNDS AS SUMO ACTIVATING ENZYME INHIBITORS
Disclosed in the present disclosure are compounds as SUMO activating enzyme inhibitors. Specifically, the present disclosure relates to a compound of general formula (1), a method for preparing same, and use of the compound of general formula (1) and isomers, crystalline forms, pharmaceutically acceptable salts, hydrates or solvates thereof as SAE inhibitors. The compound and the isomer thereof, the crystalline form thereof, the pharmaceutically acceptable salt thereof, the hydrate thereof, or the solvate thereof of the present disclosure can be used in preparing a medicament for treating or preventing a disease related to SAE protein.
##STR00001##
RAS INHIBITORS
The disclosure features macrocyclic compounds, and pharmaceutical compositions and protein complexes thereof, capable of inhibiting Ras proteins, and their uses in the treatment of cancers.
RAS INHIBITORS
The disclosure features macrocyclic compounds, and pharmaceutical compositions and protein complexes thereof, capable of inhibiting Ras proteins, and their uses in the treatment of cancers.