Patent classifications
C07D211/24
Analogs of pridopidine, their preparation and use
This invention provides an isolated compound having the structure: ##STR00001##
or a salt thereof, processes for making the same and to compositions comprising pridopidine with these compounds.
SSAO INHIBITORS AND USE THEREOF
The application relates to a compound of Formula (I′) or (I):
##STR00001##
or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof, which modulates the activity of SSAO, a pharmaceutical composition comprising a compound of Formula (I′) or (I), and a method of treating or preventing a disease in which SSAO plays a role.
Phenylpiperazine proprotein convertase subtilisin/kexin type 9 (PCSK9) modulators and their use
This invention is related to the field of PCSK9 biology and the composition and methods of use of small organic compounds as ligands for modulation of PCSK9 biological activity. In particular, the invention provides compositions of small organic compounds that modulate circulating levels of low density lipoproteins by altering the conformation of the protein PCSK9. Binding these small organic compound ligands to PCSK9 alters the conformation of the protein, modifying the interaction between PCSK9 and an endogenous low density lipoprotein receptor, and can lead to reduced or increased levels of circulating LDL-cholesterol. High LDL-cholesterol levels are associated with increased risk for heart disease. Low LDL-cholesterol levels may be problematic in other conditions, such as liver dysfunction; thus, there is also utility for small organic compound ligands that can raise LDL levels.
SPIROCYCLIC ROR-GAMMA MODULATORS
Described herein are retinoic acid related-related orphan nuclear receptor (ROR) modulators and methods of utilizing NROR-gamma modulators in the treatment of diseases, disorders or conditions. Also described herein are pharmaceutical compositions containing such compounds.
SPIROCYCLIC ROR-GAMMA MODULATORS
Described herein are retinoic acid related-related orphan nuclear receptor (ROR) modulators and methods of utilizing NROR-gamma modulators in the treatment of diseases, disorders or conditions. Also described herein are pharmaceutical compositions containing such compounds.
Substituted piperidine compound and use thereof
Provided is a substituted piperidine compound having an orexin type 2 receptor agonist activity. A compound represented by the formula (I): ##STR00001##
wherein each symbol is as described in the DESCRIPTION, or a salt thereof has an orexin type 2 receptor agonist activity, and is useful as a prophylactic or therapeutic agent for narcolepsy.
Substituted piperidine compound and use thereof
Provided is a substituted piperidine compound having an orexin type 2 receptor agonist activity. A compound represented by the formula (I): ##STR00001##
wherein each symbol is as described in the DESCRIPTION, or a salt thereof has an orexin type 2 receptor agonist activity, and is useful as a prophylactic or therapeutic agent for narcolepsy.
Piperidine derivatives as liver X receptor beta agonists, compositions, and their use
In its many embodiments, the present invention provides certain piperidine compounds of the Formula (I): and pharmaceutically acceptable salts thereof, wherein X, Y, R.sup.1, R.sup.2, R.sup.3, L, R.sup.4, L.sub.1, Q, and R.sup.5 are as defined herein. The novel compounds of the invention, and pharmaceutically acceptable compositions comprising a compound thereof, are useful as Liver X- receptor (LXR) agonists, and may be useful for treating or preventing pathologies related thereto. Such pathologies include, but are not limited to, inflammatory diseases and diseases characterized by defects in cholesterol and lipid metabolism, such as Alzheimer's disease. ##STR00001##
NOVEL SULFONAMIDE CARBOXAMIDE COMPOUNDS
The present invention relates to compounds of formula (I): Formula (I) wherein Q is selected from O or S; L is a saturated or unsaturated, optionally substituted C.sub.1-C.sub.12 hydrocarbylene group optionally including one or more heteroatoms N, O or S; R.sup.1 is NR.sup.3R.sup.4, OR.sup.5, (CNR.sup.6)R.sup.7, (CO)R.sup.8, CN, N.sub.3, a quaternary ammonium group or an optionally substituted heterocycle; R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7 and R.sup.8 are each independently hydrogen or a saturated or unsaturated, optionally substituted C.sub.1-C.sub.10 hydrocarbyl group optionally including one or more heteroatoms N, O or S; wherein optionally L and R.sup.3, or L and R.sup.4, or R.sup.3 and R.sup.4, or L and R.sup.5, or L and R.sup.6, or L and R.sup.7, or R.sup.6 and R.sup.7, or L and R.sup.8 together with the atom(s) to which they are attached may form a 3- to 12-membered, saturated or unsaturated, optionally substituted cyclic group; and R.sup.2 is a cyclic group substituted at the a-position, wherein R.sup.2 may optionally be further substituted; provided that the atom of L which is attached to the sulfur atom of the sulfonylurea group is a carbon atom and is not a ring atom of a heterocyclic or aromatic group. The present invention further relates to salts, solvates and prodrugs of such compounds, to pharmaceutical compositions comprising such compounds, and to the use of such compounds in the treatment and prevention of medical disorders and diseases, most especially by the inhibition of NLRP.sub.3.
##STR00001##
NOVEL SULFONAMIDE CARBOXAMIDE COMPOUNDS
The present invention relates to compounds of formula (I): Formula (I) wherein Q is selected from O or S; L is a saturated or unsaturated, optionally substituted C.sub.1-C.sub.12 hydrocarbylene group optionally including one or more heteroatoms N, O or S; R.sup.1 is NR.sup.3R.sup.4, OR.sup.5, (CNR.sup.6)R.sup.7, (CO)R.sup.8, CN, N.sub.3, a quaternary ammonium group or an optionally substituted heterocycle; R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7 and R.sup.8 are each independently hydrogen or a saturated or unsaturated, optionally substituted C.sub.1-C.sub.10 hydrocarbyl group optionally including one or more heteroatoms N, O or S; wherein optionally L and R.sup.3, or L and R.sup.4, or R.sup.3 and R.sup.4, or L and R.sup.5, or L and R.sup.6, or L and R.sup.7, or R.sup.6 and R.sup.7, or L and R.sup.8 together with the atom(s) to which they are attached may form a 3- to 12-membered, saturated or unsaturated, optionally substituted cyclic group; and R.sup.2 is a cyclic group substituted at the a-position, wherein R.sup.2 may optionally be further substituted; provided that the atom of L which is attached to the sulfur atom of the sulfonylurea group is a carbon atom and is not a ring atom of a heterocyclic or aromatic group. The present invention further relates to salts, solvates and prodrugs of such compounds, to pharmaceutical compositions comprising such compounds, and to the use of such compounds in the treatment and prevention of medical disorders and diseases, most especially by the inhibition of NLRP.sub.3.
##STR00001##