C07K5/06

Substituted imidazo[1,2-a]pyridine compounds as tropomyosin receptor kinase a (TrkA) inhibitors

The present application relates to a series of substituted imidazo[1,2-a]pyridine compounds of formula (I), ##STR00001##
pharmaceutically acceptable salts, pharmaceutically acceptable solvates or stereoisomers thereof, their use as tropomyosin receptor kinase (Trk) family protein kinase inhibitors, method of making and pharmaceutical compositions comprising such compounds.

VAR2CSA-DRUG CONJUGATES

VAR2CSA-drug conjugates having biological activity are disclosed. Methods associated with preparation and use of such conjugates, as well as pharmaceutical compositions comprising such conjugates, are also disclosed.

Compounds for binding to the platelet specific glycoprotein IIb/IIIa and their use for imaging of thrombi

The present invention relates to novel fluorine containing compounds, methods for their preparation, the intermediates of the synthesis, their use as diagnostic agents, especially for imaging of thrombi. The invention relates to positron emission tomography (PET) agents and associated precursor reagents, and methods for producing such radiolaveled agents for imaging of thrombi in a mammalian body. More particularly, the invention relates to small nonpeptide, high-affinity, specific-binding glycoprotein IIb/IIIa antagonists for imaging of thrombi.

Compounds for binding to the platelet specific glycoprotein IIb/IIIa and their use for imaging of thrombi

The present invention relates to novel fluorine containing compounds, methods for their preparation, the intermediates of the synthesis, their use as diagnostic agents, especially for imaging of thrombi. The invention relates to positron emission tomography (PET) agents and associated precursor reagents, and methods for producing such radiolaveled agents for imaging of thrombi in a mammalian body. More particularly, the invention relates to small nonpeptide, high-affinity, specific-binding glycoprotein IIb/IIIa antagonists for imaging of thrombi.

SELECTIVE BCRP/ABCG2 TRANSPORTER INHIBITORS AS AGENTS TO ABOLISH RESISTANCE TO ANTI-CANCER AGENTS

A compound of formula (I):

##STR00001##

or pharmaceutically acceptable enantiomer, salt or solvate thereof, or a mixture thereof, the ring A, and the substituents Z, Y and R.sub.1 being as defined herein.

Antimicrobial compounds and/or modulators of microbial infections and methods of using the same

Some embodiments include compounds that can inhibit the growth of bacterial and/or inhibit or reduce microbial infections caused by one or more microorganisms (e.g., Pseudomonas aeruginosa and Cryptococcus neoformans) and methods of using these compounds to treat microbial infection and outbreaks and/or to reduce the formation of biofilms. Other embodiments include synthesis of the compounds that can inhibit the growth of one or more microorganisms and/or inhibit or reduce microbial infections.

Interval therapy for the treatment of loss of eyesight in humans with glaucoma and other degenerative eye diseases

Methods for the prevention and treatment of ocular disorders, in particular glaucoma, through blocking the toxic effects of β-amyloid (Aβ) derivatives, pharmaceutical compositions for effecting such prevention and interval treatment thereof.

Derivatives of 1-amino-2-cyclobutylethylboronic acid

The present invention provides novel compounds useful as proteasome inhibitors. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases.

Derivatives of 1-amino-2-cyclobutylethylboronic acid

The present invention provides novel compounds useful as proteasome inhibitors. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases.

SYNTHESIS OF BORONIC ESTER AND ACID COMPOUNDS

The invention relates to the synthesis of boronic ester and acid compounds. More particularly, the invention provides improved synthetic processes for the large-scale production of boronic ester and acid compounds, including the peptide boronic acid proteasome inhibitor bortezomib.