C07D403/00

Process for making hydroxylated cyclopentylpyrimidine compounds

The invention provides processes for preparing a compound of formula I ##STR00001##
and salts thereof, wherein R.sup.1 is defined herein, and compounds and intermediates of said formula.

Trisubstituted bicyclic heterocyclic compounds with kinase activities and uses thereof

Trisubstituted bicyclic heterocyclic compounds (e.g., chromenones and quinolines) and pharmaceutical compositions,that modulate kinase activity, including PI3 kinase activity, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein.

METHODS FOR PREPARATION OF QUINAZOLINE DERIVATIVES

Methods for preparing compounds having the following structure (I):

##STR00001##

or a pharmaceutically acceptable salt, stereoisomer, or tautomer thereof, wherein R.sup.1, R.sup.2a, R.sup.2b, R.sup.3a, R.sup.3b, R.sup.4a, R.sup.4b and R.sup.4c, are as defined herein are provided. Related compounds and methods for making the same are also provided.

HOLE TRANSPORT COMPOSITIONS AND RELATED DEVICES AND METHODS (I)

A composition comprising: at least one compound comprising a hole transporting core, wherein the core is covalently bonded to a first arylamine group and also covalently bonded to a second arylamine group different from the first, and wherein the compound is covalently bonded to at least one intractability group, wherein the intractability group is covalently bonded to the hole transporting core, the first arylamine group, the second arylamine group, or a combination thereof, and wherein the compound has a molecular weight of about 5,000 g/mole or less. Blended mixtures of arylamine compounds, including fluorene core compounds, can provide good film formation and stability when coated onto hole injection layers. Solution processing of OLEDs is a particularly important application.

4-(3-cyanophenyl)-6-pyridinylpyrimidine mGlu5 modulators

The disclosures herein relate to novel compounds of formula wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 and n are defined here, and their use in treating, preventing, ameliorating, controlling or reducing the risk of inflammation, neurological or psychiatric disorders associated with modulating mGlu5 receptor function. ##STR00001##

Substituted aminopyrimidine compounds and methods of use

The invention relates to the preparation and use of new aminopyrimidine derivatives as drug candidates in free form or in pharmaceutically acceptable salt form and formulations thereof for the modulation of a disorder or disease which is mediated by the activity of the PI3K enzymes. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of disorders or diseases, such as disorders of immunity and inflammation in which PI3K enzymes play a role in leukocyte function, and hyperproliferative disorders associated with PI3K activity, including but not limited to leukemias and solid tumors, in mammals, especially humans.

Substituted aminopyrimidine compounds and methods of use

The invention relates to the preparation and use of new aminopyrimidine derivatives as drug candidates in free form or in pharmaceutically acceptable salt form and formulations thereof for the modulation of a disorder or disease which is mediated by the activity of the PI3K enzymes. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of disorders or diseases, such as disorders of immunity and inflammation in which PI3K enzymes play a role in leukocyte function, and hyperproliferative disorders associated with PI3K activity, including but not restricted to leukemias and solid tumors, in mammals, especially humans.

Therapeutic compounds and related methods of use

Methods of treating disorders using compounds that modulate striatal-enriched tyrosine phosphatase (STEP), such as those of formula (III), and composition thereof are described herein. Exemplary disorders include schizophrenia and cognitive deficit. ##STR00001##

TRPV1 antagonists including dihydroxy substituent and uses thereof

The disclosure relates to Compounds of Formula (I) ##STR00001##
and pharmaceutically acceptable derivatives thereof, where R.sub.1, R.sub.4, R.sub.8, R.sub.9, and m are as defined herein, compositions comprising an effective amount of a Compound of Formula (I) or a pharmaceutically acceptable derivative thereof, and methods for treating or preventing a condition such as pain, pain associated with osteoarthritis, osteoarthritis, UI, an ulcer, IBD, and IBS, comprising administering to an animal in need thereof an effective amount of a Compound of Formula (I) or a pharmaceutically acceptable derivative thereof.

Compounds as diacylglycerol acyltransferase inhibitors
09624174 · 2017-04-18 · ·

Compounds of Formula (I) are inhibitors of acyl coenzyme A: diacylglycerol acyltransferase 1 (DGAT-1), useful in the treatment of obesity, obesity related disorders, genetic (Type 1, Type 5 hyperlipidemia) and acquired forms of hypertriglyceridemia or hyperlipoproteinemia-related disorders, caused by but not limited to lipodystrophy, hypothyroidism, medications (beta blockers, thiazides, estrogen, glucocorticoids, transplant) and other factors (pregnancy, alcohol intake), hyperlipoproteinemia, chylomicronemia, dyslipidemia, non-alcoholic steatohepatitis, diabetes, insulin resistance, metabolic syndrome, cardiovascular outcomes, angina, excess hair growth (including syndromes associated with hirsutism), nephrotic syndrome, fibrosis such as mycocardial, renal and liver fibrosis, hepatitis C virus infection and acne or other skin disorders. ##STR00001##