C07D223/08

Phenyl-(aza)cycloalkyl carboxylic acid GPR120 modulators

The present invention provides compounds of Formula (I): ##STR00001##
or a stereoisomer, or a pharmaceutically acceptable salt thereof, wherein all of the variables are as defined herein. These compounds are GPR120 G protein-coupled receptor modulators which may be used as medicaments.

Low molecular weight cyclic amine containing cationic lipids for oligonucleotide delivery

The instant invention provides for novel cationic lipids that can be used in combination with other lipid components such as cholesterol and PEG-lipids to form lipid nanoparticles with oligonucleotides. It is an object of the instant invention to provide a cationic lipid scaffold that demonstrates enhanced efficacy along with lower liver toxicity as a result of lower lipid levels in the liver. The present invention employs low molecular weight cationic lipids comprising at least one short lipid chain to enhance the efficiency and tolerability of in vivo delivery of siRNA.

Low molecular weight cyclic amine containing cationic lipids for oligonucleotide delivery

The instant invention provides for novel cationic lipids that can be used in combination with other lipid components such as cholesterol and PEG-lipids to form lipid nanoparticles with oligonucleotides. It is an object of the instant invention to provide a cationic lipid scaffold that demonstrates enhanced efficacy along with lower liver toxicity as a result of lower lipid levels in the liver. The present invention employs low molecular weight cationic lipids comprising at least one short lipid chain to enhance the efficiency and tolerability of in vivo delivery of siRNA.

DUAL NAV1.2/5HT2a INHIBITORS FOR TREATING CNS DISORDERS

Compounds of formula I:

##STR00001##

are disclosed, as are pharmaceutical compositions containing such compounds. Methods of treating neurological or psychiatric disorders in a patient in need are also disclosed. Such disorders include depression, bipolar disorder, pain, schizophrenia, obsessive compulsive disorder, addiction, social disorder, attention deficit hyperactivity disorder, an anxiety disorder, autism, a cognitive impairment, or a neuropsychiatric symptom such as apathy, depression, anxiety, psychosis, aggression, agitation, impulse control disorders, and sleep disorders in neurological disorders such as Alzheimer's and Parkinson's diseases.

DUAL NAV1.2/5HT2a INHIBITORS FOR TREATING CNS DISORDERS

Compounds of formula I:

##STR00001##

are disclosed, as are pharmaceutical compositions containing such compounds. Methods of treating neurological or psychiatric disorders in a patient in need are also disclosed. Such disorders include depression, bipolar disorder, pain, schizophrenia, obsessive compulsive disorder, addiction, social disorder, attention deficit hyperactivity disorder, an anxiety disorder, autism, a cognitive impairment, or a neuropsychiatric symptom such as apathy, depression, anxiety, psychosis, aggression, agitation, impulse control disorders, and sleep disorders in neurological disorders such as Alzheimer's and Parkinson's diseases.

Histone deacetylase inhibitors

Provided herein are compounds and methods for inhibiting histone deacetylase (HDAC) enzymes (e.g., HDAC1, HDAC2, and HDAC3).

Histone deacetylase inhibitors

Provided herein are compounds and methods for inhibiting histone deacetylase (HDAC) enzymes (e.g., HDAC1, HDAC2, and HDAC3).

CATIONIC LIPID

The present invention provides novel cationic lipids having excellent encapsulation and delivery stability of nucleic acid medicines. Provided is a compound represented by Formula (I) or a pharmacologically acceptable salt thereof. In the Formula (I), R.sup.1 is a substituted or unsubstituted formula: (CH.sub.2).sub.aL.sub.1(CH.sub.2).sub.bCH.sub.3; R.sup.2 is a substituted or unsubstituted C5-C20 alkyl group or a substituted or unsubstituted formula: (CH.sub.2).sub.cL.sub.2(CH.sub.2).sub.aCH.sub.3; L.sup.1 and L.sup.2 are each independently C(?O)O, OC(?O), or OC(?O)O; a, b, c, and d are each independently an integer of at least 1, and the total of a and b and the total of c and d are each an integer of 5 to 25; R.sup.3 to R.sup.7 are each independently a hydrogen atom, a substituted or unsubstituted C.sup.1-C.sup.6 alkyl group, or the like; R.sup.8, R.sup.9, and R.sup.10 are each a hydrogen atom; the constituent atoms in the Formula (I) may form a ring; Z is OC(?O), C(?O)O, OC(?O)O, or the like; and X is O or S.

Heterocyclic amides as kinase inhibitors

Disclosed are compounds having the formula: ##STR00001## wherein X, Y, Z.sup.1, Z.sup.2, Z.sup.3, Z.sup.4, R.sup.5, R.sup.A, m, A. L, and B are as defined herein, and methods of making and using the same.

Heterocyclic amides as kinase inhibitors

Disclosed are compounds having the formula: ##STR00001## wherein X, Y, Z.sup.1, Z.sup.2, Z.sup.3, Z.sup.4, R.sup.5, R.sup.A, m, A. L, and B are as defined herein, and methods of making and using the same.