C07D209/60

Tricyclic sulfones as RORγ modulators

There are described RORγ modulators of the formula (I), ##STR00001##
and formula (II) ##STR00002##
or stereoisomers, tautomers, pharmaceutically acceptable salts, solvates, or prodrugs thereof, wherein all substituents are defined herein. Also provided are pharmaceutical compositions comprising the same. Such compounds and compositions are useful in methods for modulating RORγ activity in a cell and methods for treating a subject suffering from a disease or disorder in which the subject would therapeutically benefit from modulation of RORγ activity, for example, autoimmune and/or inflammatory disorders.

Tricyclic sulfones as RORγ modulators

There are described RORγ modulators of the formula (I), ##STR00001##
and formula (II) ##STR00002##
or stereoisomers, tautomers, pharmaceutically acceptable salts, solvates, or prodrugs thereof, wherein all substituents are defined herein. Also provided are pharmaceutical compositions comprising the same. Such compounds and compositions are useful in methods for modulating RORγ activity in a cell and methods for treating a subject suffering from a disease or disorder in which the subject would therapeutically benefit from modulation of RORγ activity, for example, autoimmune and/or inflammatory disorders.

Heteroaryl Rheb inhibitors and uses thereof

The present invention provides compounds of general Formula I and I′: ##STR00001## ##STR00002##
compositions thereof, and methods of using same to treat Rheb-mediated disorders.

Cyanine-containing compounds for cancer imaging and treatment

This invention relates generally to cyanine-containing compounds; pharmaceutical compositions comprising cyanine-containing compounds; and methods of using cyanine-containing compounds for cancer cell imaging, cancer cell growth inhibition, and detecting cancer cells, for example. Compounds of the invention are preferentially taken up by cancer cells as compared to normal cells. This allows many uses in the cancer treatment, diagnosis, tracking and imaging fields.

Cyanine-containing compounds for cancer imaging and treatment

This invention relates generally to cyanine-containing compounds; pharmaceutical compositions comprising cyanine-containing compounds; and methods of using cyanine-containing compounds for cancer cell imaging, cancer cell growth inhibition, and detecting cancer cells, for example. Compounds of the invention are preferentially taken up by cancer cells as compared to normal cells. This allows many uses in the cancer treatment, diagnosis, tracking and imaging fields.

WATER-SOLUBLE COMPOUND FOR DETECTION OF BETA-AMYLOID
20220155310 · 2022-05-19 ·

The present invention relates to a water-soluble compound for the detection of beta-amyloid, and a production method thereof. The compound according to the present invention has excellent water-soluble properties, and thus can provide a water-soluble formulation for the detection of beta-amyloid. Accordingly, there is an effect that the compound can be useful as a composition for the detection of beta-amyloid through retinal imaging.

WATER-SOLUBLE COMPOUND FOR DETECTION OF BETA-AMYLOID
20220155310 · 2022-05-19 ·

The present invention relates to a water-soluble compound for the detection of beta-amyloid, and a production method thereof. The compound according to the present invention has excellent water-soluble properties, and thus can provide a water-soluble formulation for the detection of beta-amyloid. Accordingly, there is an effect that the compound can be useful as a composition for the detection of beta-amyloid through retinal imaging.

Synthetic process

The invention generally relates to a process for preparing compounds, including Compound of Formula (I), useful as key intermediates in the preparation of compounds having RORγt antagonist properties. ##STR00001##

Synthetic process

The invention generally relates to a process for preparing compounds, including Compound of Formula (I), useful as key intermediates in the preparation of compounds having RORγt antagonist properties. ##STR00001##

Method for the synthesis of monoprotected bifunctional prodrugs and antibody drug conjugates based thereon as well as a method for preparing antibody drug conjugates

The present invention relates to a method for the synthesis of compounds useful in the preparation of antibody drug conjugates (ADC), namely, monoprotected dimeric bifunctional prodrugs based on duocarmycin analogs. In a further aspect, compounds obtained by the method according to the present invention are provided. The monoprotected bifunctional prodrug is used for preparing antibody drug conjugates composed of an antibody moiety and the monoprotected bifunctional prodrug. The antibody compound conjugates thus obtained are provided. Further, a method of preparing an antibody drug conjugate composed of two identical or two different antibody moieties is provided as well as the antibody compound conjugate containing two different antibody moieties accordingly. These conjugates can be used in pharmaceutical compositions, in particular, for use in treatment of tumors, e.g. for use in ADC therapy.