Patent classifications
C07D261/20
Substituted benzofuran, benzopyrrole, benzothiophene, and structurally related complement inhibitors
Disclosed are compounds of formulae I and II, and pharmaceutically acceptable salts and prodrugs thereof, which are inhibitors of the complement system. Also provided are pharmaceutical compositions comprising such a compound, and methods of using the compounds and compositions in the treatment or prevention of a disease or condition characterized by aberrant complement system activity. ##STR00001##
Substituted benzofuran, benzopyrrole, benzothiophene, and structurally related complement inhibitors
Disclosed are compounds of formulae I and II, and pharmaceutically acceptable salts and prodrugs thereof, which are inhibitors of the complement system. Also provided are pharmaceutical compositions comprising such a compound, and methods of using the compounds and compositions in the treatment or prevention of a disease or condition characterized by aberrant complement system activity. ##STR00001##
Fused cyclooctyne compounds and their use in metal-free click reactions
The invention relates to fused cyclooctyne compounds, and to a method for their preparation. The invention also relates to a conjugate wherein a fused cyclooctyne compound according to the invention is conjugated to a label, and to the use of these conjugates in bioorthogonal labeling, imaging and/or modification, such as for example surface modification, of a target molecule. The invention further relates to a method for the modification of a target molecule, wherein a conjugate according to the invention is reacted with a compound comprising a 1,3-dipole or a 1,3-(hetero)diene.
Benzothiophene and benzothiazole compounds and methods of use thereof
Compounds having activity as inhibitors of G12C mutant KRAS protein are provided. The compounds have the following structure (I) or a pharmaceutically acceptable salt, stereoisomer or prodrug thereof, wherein B, Z, R.sup.a, R.sup.b, R.sup.c, R.sup.1, L, L.sup.1 and E are as defined herein. Methods associated with preparation and use of such compounds, pharmaceutical compositions comprising such compounds and methods to modulate the activity of G12C mutant KRAS protein for treatment of disorders, such as cancer, are also provided. ##STR00001##
Heterocyclic compounds for the treatment of arenavirus
The invention relates to compounds of structural formula I ##STR00001## wherein A, D, and E are independently N or C—R.sup.3, G, H, and J are independently N or C, K is N or C—H, L is N, N—R.sup.3 or C—R.sup.3, and A, D, E, G, H, J, K, and L together cannot have more than 4 N, R.sup.1 is selected from (C.sub.6 to C.sub.10) aryl, (C.sub.2 to C.sub.9) heteroaryl, and 5-indolyl, wherein each of the said (C.sub.6 to C.sub.10) aryl and (C.sub.2 to C.sub.9) heteroaryl is substituted with at least one R.sup.4a group, and wherein said (C.sub.2 to C.sub.9) heteroaryl is C-attached, and R.sup.2 is selected from the group consisting of ##STR00002##
METHODS AND MATERIALS FOR INCREASING OR MAINTAINING NICOTINAMIDE MONONUCLEOTIDE ADENYLYL TRANSFERASE-2 (NMNAT2) POLYPEPTIDE LEVELS
This document provides methods and materials for increasing or maintaining NMNAT2 polypeptide levels within cells. For example, compounds (e.g., organic compounds) having the ability to increase or maintain NMNAT2 polypeptide levels within cells, formulations containing compounds having the ability to increase or maintain NMNAT2 polypeptide levels within cells, methods for making compounds having the ability to increase or maintain NMNAT2 polypeptide levels within cells, methods for making formulations containing compounds having the ability to increase or maintain NMNAT2 polypeptide levels within cells, methods for increasing or maintain NMNAT2 polypeptide levels within cells, and methods for treating mammals (e.g., humans) having a condition responsive to an increase in NMNAT2 polypeptide levels are provided (or for preventing said condition).
Aliphatic acid amide derivative
The present invention relates to a compound represented by formula (1): ##STR00001##
the compound having antagonist activity against serotonin 5-HT.sub.2A receptors and serotonin 5-HT.sub.7 receptors; or a pharmaceutically acceptable salt of the compound. (In the formula, Z is a nitrogen atom and the like; Y is carbonyl and the like; m and n are 1 and the like; R.sup.1a through R.sup.1d, R.sup.2a through R.sup.2d, and R.sup.4a through R.sup.4d are a hydrogen atom and the like; R.sup.3 is alkyl and the like; and Q is a specific bicyclic group.)
Compounds
A compound of formula (I), or a pharmaceutical salt thereof:
##STR00001##
Compounds
A compound of formula (I), or a pharmaceutical salt thereof:
##STR00001##
SMALL MOLECULES TARGETING THE INTRINSICALLY DISORDERED STRUCTURAL ENSEMBLE OF ALPHA-SYNUCLEIN PROTECT AGAINST DIVERSE ALPHA-SYNUCLEIN MEDIATED DYSFUNCTIONS
Provided herein are pharmaceutical compositions and methods for treatment or prevention of synucleinopathies with small-molecule inhibitors of pathogenic α-synuclein activity having the Formula (I). Also, provide are methods for identifying novel compounds for modulating α-synuclein activity.