Patent classifications
C07D249/16
PROCESS FOR THE CYCLOADDITION OF A HETERO(ARYL) 1,3-DIPOLE COMPOUND WITH A (HETERO)CYCLOALKYNE
A process is provided, comprising reacting a (hetero)aryl 1,3-dipole compound with a (hetero)cycloalkyne, wherein the (hetero)aryl 1,3-dipole compound comprises a 1,3-dipole functional group bonded to a (hetero)aryl group, and wherein the (hetero)aryl 1,3-dipole compound is a (hetero)aryl azide or a (hetero)aryl diazo compound; wherein:
(i) the (hetero)aryl group of the (hetero)aryl 1,3-dipole compound comprises a substituent
(ii) the (hetero)aryl group of the (hetero)aryl 1,3-dipole compound is an electron-poor (hetero)aryl group
and wherein the (hetero)cycloalkyne is a (hetero)cyclooctyne or a (hetero)cyclononyne according to Formula (1). The invention also relates to the products obtainable by the process according to the invention.
BIS-OCTAHYDROPHENANTHRENE CARBOXAMIDE DERIVATIVES AND PROTEIN CONJUGATES THEREOF FOR USE AS LXR AGONISTS
Provided herein are compounds or payloads, linker-payloads, antibody-drug conjugates, and compositions, and methods for the treatment of diseases and disorders associated with the liver X receptor, including bis-octahydrophenanthrene carboxamides and protein (e.g., antibody) drug conjugates thereof.
BIS-OCTAHYDROPHENANTHRENE CARBOXAMIDE DERIVATIVES AND PROTEIN CONJUGATES THEREOF FOR USE AS LXR AGONISTS
Provided herein are compounds or payloads, linker-payloads, antibody-drug conjugates, and compositions, and methods for the treatment of diseases and disorders associated with the liver X receptor, including bis-octahydrophenanthrene carboxamides and protein (e.g., antibody) drug conjugates thereof.
Bicyclic sulfones and sulfoxides and methods of use thereof
The invention provides novel compounds having the general formula I: ##STR00001##
wherein R.sup.1, R.sup.B1, R.sup.B2, n, p, q, the A ring and the B ring are as described herein, pharmaceutical compositions including the compounds, and methods of using the compounds.
Bicyclic sulfones and sulfoxides and methods of use thereof
The invention provides novel compounds having the general formula I: ##STR00001##
wherein R.sup.1, R.sup.B1, R.sup.B2, n, p, q, the A ring and the B ring are as described herein, pharmaceutical compositions including the compounds, and methods of using the compounds.
Compositions and methods concerning immune tolerance
The present disclosure provides compositions comprising mannose-fused antigens to target mannose receptors. The compositions may be used to prevent immunity or reduce an immune response protein-based drugs that would otherwise elicit an immune response.
Compositions and methods concerning immune tolerance
The present disclosure provides compositions comprising mannose-fused antigens to target mannose receptors. The compositions may be used to prevent immunity or reduce an immune response protein-based drugs that would otherwise elicit an immune response.