Disclosed herein are compounds selective for JAK1, pharmaceutical compositions comprising said compounds, and methods of using said compounds.

The disclosure is directed to compounds of the formula (IA), (I)-(V) and others disclosed herein and uses of such compounds.

The invention provides heterocyclic compounds with quaternary centers and methods of preparing compounds. Methods include the method for the preparation of a compound of Formula (II):

##STR00001##

comprising treating a compound of Formula (I):

##STR00002##

with a transition metal catalyst and under alkylation conditions as valence and stability permit.

The invention provides heterocyclic compounds with quaternary centers and methods of preparing compounds. Methods include the method for the preparation of a compound of Formula (II):

##STR00001##

comprising treating a compound of Formula (I):

##STR00002##

with a transition metal catalyst and under alkylation conditions as valence and stability permit.

A derivative of isocorydine of formula I:

##STR00001##

wherein: R.sub.1

##STR00002##

XN, C, CC; n.sub.1=0, 1 R.sub.2H, R.sub.1 YC, N R.sub.3H, Cl, Br, F, CF.sub.3, OCH.sub.3, CH.sub.3,

##STR00003##

Z H, Cl, F, N; n.sub.2=0, 1 R.sub.4NH.sub.2, CH.sub.2NH.sub.2, NHCO(CH.sub.2).sub.n3CH.sub.3, CH.sub.2NHCO(CH.sub.2).sub.n3CH.sub.3, n.sub.3=0, 1, 2.

This derivative is prepared by amidation condensation reaction between an amino group of NICD and a carbonyl group of an aryl isocyanate, a carboxylic acid, or an acid chloride, or symmetrical amidation condensation reaction between an NICD and an aromatic amino group by solid phosgene. This derivative has anti-cancer activity in vivo and in vitro, and may be used for preventing and treating cancer.

The present invention relates to novel heterocyclicalkyl derivatives having histone deacetylase (HDAC) inhibitory activity, optical isomers thereof or pharmaceutically acceptable salts thereof, the use thereof for the preparation of medicaments, pharmaceutical compositions containing the same, a method for treating diseases using the composition, and methods for preparing the novel heterocyclicalkyl derivatives. The novel heterocyclicalkyl derivatives according to the present invention are selective histone deacetylase (HDAC) inhibitors, and may be effectively used for the treatment of histone deacetylase-mediated diseases, such as cell proliferative diseases, inflammatory diseases, autosomal dominant diseases, genetic metabolic diseases, autoimmune diseases, acute/chronic neurological disease, hypertrophy, heart failure, ocular diseases, or neurodegenerative diseases.

The present invention relates to novel heterocyclicalkyl derivatives having histone deacetylase (HDAC) inhibitory activity, optical isomers thereof or pharmaceutically acceptable salts thereof, the use thereof for the preparation of medicaments, pharmaceutical compositions containing the same, a method for treating diseases using the composition, and methods for preparing the novel heterocyclicalkyl derivatives. The novel heterocyclicalkyl derivatives according to the present invention are selective histone deacetylase (HDAC) inhibitors, and may be effectively used for the treatment of histone deacetylase-mediated diseases, such as cell proliferative diseases, inflammatory diseases, autosomal dominant diseases, genetic metabolic diseases, autoimmune diseases, acute/chronic neurological disease, hypertrophy, heart failure, ocular diseases, or neurodegenerative diseases.

Described are compounds, which are antagonists of the P2Y.sub.14 receptor, for example, a compound of formula (I) in which ring A, R.sup.1, R.sup.2, R.sup.3, and n are as described herein. Also provided are dendron conjugates comprising the compounds, and methods of using the compounds, including a method of treating a disorder, such as inflammation, diabetes, insulin resistance, hyperglycemia, a lipid disorder, obesity, a condition associated with metabolic syndrome, and asthma, and a method of antagonizing P2.sub.14 receptor activity in a cell.

##STR00001##

Provided herein are compounds of formula (A): or a stereoisomer or tautomer thereof, or a pharmaceutically acceptable salt of any of the foregoing, wherein X.sup.1, X.sup.2, X.sup.3, X.sup.4, R.sup.a, R.sup.b, R.sup.c, L, Q, and Y are as defined herein. Also provided are methods of N inhibiting APOL1 and methods of preparing compounds of formula (A). Also provided are methods of inhibiting APOL1 and methods of treating an APOL1-mediated disease, disorder, or condition in an individual.

##STR00001##

The present invention relates to a medicament for treating or preventing a disease related to orexin receptor, especially orexin receptor type 2, comprising a new compound having a urea structure or a pharmaceutically acceptable salt thereof as an active ingredient. In more detail, the present invention relates to a medicament for treating or preventing a disease such as narcolepsy, idiopathic hypersomnia, hypersomnia, sleep apnea syndrome.