C07D309/22

BIARYL KINASE INHIBITORS
20190367508 · 2019-12-05 ·

The present disclosure is generally directed to compounds which can inhibit AAK1 (adaptor associated kinase 1), compositions comprising such compounds, and methods for inhibiting AAK1.

Asymmetric addition reactions

Processes of forming C.sub.sp2C.sub.sp3 bonds at the allylic carbon of a cyclic allylic compound starting material are disclosed, in which a racemic mixture of a cyclic allylic compound having a leaving group attached to the allylic carbon is reacted with a compound having a nucleophilic carbon atom in the presence of a Rh(I), Pd(II) or Cu(I) pre-catalyst and a chiral ligand. The reaction products containing the newly-formed C.sub.sp2C.sub.sp3 bond are generated in high stereoisomeric excess, and may therefore serve as important organic building blocks in the preparation of new agrochemicals and pharmaceuticals.

Asymmetric addition reactions

Processes of forming C.sub.sp2C.sub.sp3 bonds at the allylic carbon of a cyclic allylic compound starting material are disclosed, in which a racemic mixture of a cyclic allylic compound having a leaving group attached to the allylic carbon is reacted with a compound having a nucleophilic carbon atom in the presence of a Rh(I), Pd(II) or Cu(I) pre-catalyst and a chiral ligand. The reaction products containing the newly-formed C.sub.sp2C.sub.sp3 bond are generated in high stereoisomeric excess, and may therefore serve as important organic building blocks in the preparation of new agrochemicals and pharmaceuticals.

RESCORCINOLS, METHODS FOR THEIR MANUFACTURE, AND USES THEREOF

The present invention relates to a group of resorcinol derivatives as a pharmaceutically active compounds and methods of preparation thereof. Resorcinol derivatives have been used to treat various diseases and disorders. While such treatments hold promise, there remains a need in the art for more effective treatments and this has been brought about by way of the resorcinol derivative of the invention.

RESCORCINOLS, METHODS FOR THEIR MANUFACTURE, AND USES THEREOF

The present invention relates to a group of resorcinol derivatives as a pharmaceutically active compounds and methods of preparation thereof. Resorcinol derivatives have been used to treat various diseases and disorders. While such treatments hold promise, there remains a need in the art for more effective treatments and this has been brought about by way of the resorcinol derivative of the invention.

BIARYL KINASE INHIBITORS
20190048006 · 2019-02-14 ·

The present disclosure is generally directed to compounds which can inhibit AAK1 (adaptor associated kinase 1), compositions comprising such compounds, and methods for inhibiting AAK1.

BIARYL KINASE INHIBITORS
20190048006 · 2019-02-14 ·

The present disclosure is generally directed to compounds which can inhibit AAK1 (adaptor associated kinase 1), compositions comprising such compounds, and methods for inhibiting AAK1.

CATECHOL O-METHYLTRANSFERASE ACTIVITY INHIBITING COMPOUNDS

Compounds of formula (I), wherein R.sub.1 is as defined in the claims, exhibit COMT enzyme inhibiting activity and are thus useful as COMT inhibitors. Methods of treatment and pharmaceutical dosage forms are also disclosed.

CATECHOL O-METHYLTRANSFERASE ACTIVITY INHIBITING COMPOUNDS

Compounds of formula (I), wherein R.sub.1 is as defined in the claims, exhibit COMT enzyme inhibiting activity and are thus useful as COMT inhibitors. Methods of treatment and pharmaceutical dosage forms are also disclosed.

Biaryl kinase inhibitors

The present disclosure is generally directed to compounds which can inhibit AAK1 (adaptor associated kinase 1), compositions comprising such compounds, and methods for inhibiting AAK1.