C07D311/76

Substituted bicyclic compounds

Disclosed are compounds of Formulas (I), (II), (III), (IV), and (V): ##STR00001##
and/or a salt thereof, wherein R.sub.1 is OH or OP(O)(OH).sub.2, and X.sub.1, X.sub.2, X.sub.3, R.sub.2, R.sub.2a, R.sub.a, R.sub.b, and R.sub.c are defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein-coupled receptor S1P.sub.1, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.

Substituted bicyclic compounds

Disclosed are compounds of Formulas (I), (II), (III), (IV), and (V): ##STR00001##
and/or a salt thereof, wherein R.sub.1 is OH or OP(O)(OH).sub.2, and X.sub.1, X.sub.2, X.sub.3, R.sub.2, R.sub.2a, R.sub.a, R.sub.b, and R.sub.c are defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein-coupled receptor S1P.sub.1, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.

CHIRAL DIAMINE COMPOUNDS FOR THE PREPARATION OF CHIRAL ALCOHOLS AND CHIRAL AMINES
20170204036 · 2017-07-20 ·

A process for the stereoselective preparation of a chiral alcohol or a chiral amine, the process comprising reacting a first prochiral reactant selected from the group consisting of a ketone, an aldehyde, and an imine, with a second reactant comprising a Grignard reagent, in the presence of a chiral trans-diamine of formula (1) as defined herein:

##STR00001##

Also provided is the use of the chiral trans-diamine of formula (1) in a Grignard reaction and the chiral trans-diamines per se.

CHIRAL DIAMINE COMPOUNDS FOR THE PREPARATION OF CHIRAL ALCOHOLS AND CHIRAL AMINES
20170204036 · 2017-07-20 ·

A process for the stereoselective preparation of a chiral alcohol or a chiral amine, the process comprising reacting a first prochiral reactant selected from the group consisting of a ketone, an aldehyde, and an imine, with a second reactant comprising a Grignard reagent, in the presence of a chiral trans-diamine of formula (1) as defined herein:

##STR00001##

Also provided is the use of the chiral trans-diamine of formula (1) in a Grignard reaction and the chiral trans-diamines per se.

Hydantoin derivatives as Kv3 inhibitors
09669030 · 2017-06-06 · ·

The present invention relates to the prophylaxis of acute noise-induced hearing loss by administering a compound of formula (I): wherein: W is group (Wa), group (Wb) or group (Wc): ##STR00001##

Hydantoin derivatives as Kv3 inhibitors
09669030 · 2017-06-06 · ·

The present invention relates to the prophylaxis of acute noise-induced hearing loss by administering a compound of formula (I): wherein: W is group (Wa), group (Wb) or group (Wc): ##STR00001##

3-Phenyl-7-Hydroxy-Isocoumarins as Macrophage Migration Inhibitory Factor (MIF) Inhibitors
20170144983 · 2017-05-25 ·

Provided herein are 3-phenyl-7-hydroxy-isocoumarin compounds which are MIF inhibitors; compositions comprising said inhibitors and methods for treating or preventing diseases associated with MIF.

3-Phenyl-7-Hydroxy-Isocoumarins as Macrophage Migration Inhibitory Factor (MIF) Inhibitors
20170144983 · 2017-05-25 ·

Provided herein are 3-phenyl-7-hydroxy-isocoumarin compounds which are MIF inhibitors; compositions comprising said inhibitors and methods for treating or preventing diseases associated with MIF.

Process for the synthesis of carboxylic acid derivatives

The present invention discloses one-pot synthesis of various carboxylic acid derivatives using copper catalyst and sodium cyanide as the cyanide source for bringing in carbonylative coupling in a single step.

Process for the synthesis of carboxylic acid derivatives

The present invention discloses one-pot synthesis of various carboxylic acid derivatives using copper catalyst and sodium cyanide as the cyanide source for bringing in carbonylative coupling in a single step.