C07D235/04

PROCESS AND INTERMEDIATES FOR THE PREPARATION OF BILASTINE

The invention relates to a process for preparing a compound of (III)

##STR00001## wherein X is a leaving group; and R.sup.1 is C.sub.1-C.sub.6 alkyl;
which comprises oxidative rearrangement of a compound of formula (II) or a solvate thereof

##STR00002##

Compounds of formula (III) are key intermediates in the synthesis of Bilastine.

PROCESS AND INTERMEDIATES FOR THE PREPARATION OF BILASTINE

The invention relates to a process for preparing a compound of (III)

##STR00001## wherein X is a leaving group; and R.sup.1 is C.sub.1-C.sub.6 alkyl;
which comprises oxidative rearrangement of a compound of formula (II) or a solvate thereof

##STR00002##

Compounds of formula (III) are key intermediates in the synthesis of Bilastine.

ORGANIC ELECTROLUMINESCENT MATERIALS AND DEVICES

Novel Pt tetradentate complexes having Pt—O bond is disclosed. These complexes are useful as emitters in phosphorescent OLEDs.

ORGANIC ELECTROLUMINESCENT MATERIALS AND DEVICES

Novel Pt tetradentate complexes having Pt—O bond is disclosed. These complexes are useful as emitters in phosphorescent OLEDs.

UNSYMMETRICAL SALTS, CCC-NHC PINCER METAL COMPLEXES, AND METHODS OF MAKING THE SAME
20210179588 · 2021-06-17 ·

Provided herein are unsymmetrical bis(azolium) salts, unsymmetrical CCC—NHC metal complexes, and methods of forming the same. The unsymmetrical bis(azolium) salts include a central aryl ring that is substituted with two heterocyclic rings in an ortho, meta, or para fashion. The unsymmetrical CCC—NHC metal complexes include metalated unsymmetrical bis(azolium) salts. The method of forming the unsymmetrical CCC—NHC metal complexes includes reacting a dihalogenated benzene with a first azole to form a mono(azole)benzene, reacting the mono(azole)benzene with a second azole to form an unsymmetrical bis(azole)benzene, alkylating the unsymmetrical bis(azole)benzene to form an unsymmetrical bis(azolium) salt, and metalating the unsymmetrical bis(azolium) salt to form the unsymmetrical CCC—NHC metal complex. Also provided are a bis-ligated CCC—NHC metal complex and an unsymmetrical bimetallic complex.

ANTIBODY

It has been demonstrated that certain compounds bind to TNF and stabilise a conformation of trimeric TNF that binds to the TNF receptor. Antibodies which selectively bind to complexes of such compounds with TNF superfamily members are disclosed. These antibodies may be used to detect further compounds with the same activity, and as target engagement biomarker.

ANTIBODY

It has been demonstrated that certain compounds bind to TNF and stabilise a conformation of trimeric TNF that binds to the TNF receptor. Antibodies which selectively bind to complexes of such compounds with TNF superfamily members are disclosed. These antibodies may be used to detect further compounds with the same activity, and as target engagement biomarker.

MECHANISM OF ACTION

The invention is in the field of TNF signalling. Compounds have been identified which are capable of modulating signalling of TNF trimers through receptors. Methods of identifying such compounds are therefore provided. The compounds themselves have utility in therapy.

MECHANISM OF ACTION

The invention is in the field of TNF signalling. Compounds have been identified which are capable of modulating signalling of TNF trimers through receptors. Methods of identifying such compounds are therefore provided. The compounds themselves have utility in therapy.

Antibodies binding to trimeric TNF alpha epitopes

It has been demonstrated that certain compounds bind to TNF and stabilise a conformation of trimeric TNF that binds to the TNF receptor. Antibodies which selectively bind to complexes of such compounds with TNF superfamily members are disclosed. These antibodies may be used to detect further compounds with the same activity, and as target engagement biomarker.