Patent classifications
C07D419/14
DRUG ANTIBODY CONJUGATES
Drug conjugates having formula [D-(X).sub.b-(AA).sub.w-(T).sub.g-(L)-].sub.n-Ab wherein: D is a drug moiety having the following formula (I) or a pharmaceutically acceptable salt, ester, solvate, tautomer or stereoisomer thereof, (I) wherein D is covalently attached via a hydroxy or amine group to (X).sub.b if any, or (AA).sub.w if any, or to (T).sub.g if any, or (L); that are useful in the treatment of cancer.
##STR00001##
MATERIALS FOR ORGANIC ELECTROLUMINESCENT DEVICES
The present invention relates to compounds of the formula (1) which are suitable for use in electronic devices, in particular organic electroluminescent devices, and to electronic devices which comprise these compounds.
##STR00001##
MATERIALS FOR ORGANIC ELECTROLUMINESCENT DEVICES
The present invention relates to compounds of the formula (1) which are suitable for use in electronic devices, in particular organic electroluminescent devices, and to electronic devices which comprise these compounds.
##STR00001##
ARYL HYDROCARBON RECEPTOR MODULATORS
The disclosure discloses an aryl hydrocarbon receptor modulators of formula (I), and pharmaceutically acceptable salts,
##STR00001## R is H, CN, CH.sub.2(OH)R.sub.0, C.sub.mH.sub.2m+1, C.sub.nH.sub.2n-1, C.sub.nH.sub.2n-3,
##STR00002##
two R.sub.a is independently H, or two R.sub.a together form O or NW.sub.3R.sub.1; A is a C.sub.6 to C.sub.10 aromatic ring, or a C.sub.2 to C.sub.10 heteroaromatic ring containing 1 to 5 heteroatom from N, O and S, or 4 to 7 membered non-aromatic heterocyclic ring containing 1 to 3 heteroatom from N, O and S and CN, which are with no substituent or substituted by 1 or 3 R; Q is R, or a C.sub.6 to C.sub.10 aromatic ring or a C.sub.2 to C.sub.10 heteroaromatic ring containing 1 to 5 heteroatom selected from N, O and S, which are with no substituent or substituted by 1 or 3 R; R is R.sub.c connected with C or R.sub.N connected with N.
SOLID FORMS COMPRISING 4-AMINO-2-(2,6-DIOXOPIPERIDINE-3-YL)ISOINDOLINE-1,3-DIONE AND A COFORMER, COMPOSITIONS AND METHODS OF USE THEREOF
Provided herein are solid forms comprising (a) 4-amino-2-(2,6-dioxopiperidine-3-yl)isoindoline-1,3-dione and (b) a coformer. Pharmaceutical compositions comprising the solid forms (e.g., cocrystals) and methods for treating, preventing and managing various disorders are also disclosed.
SOLID FORMS COMPRISING 4-AMINO-2-(2,6-DIOXOPIPERIDINE-3-YL)ISOINDOLINE-1,3-DIONE AND A COFORMER, COMPOSITIONS AND METHODS OF USE THEREOF
Provided herein are solid forms comprising (a) 4-amino-2-(2,6-dioxopiperidine-3-yl)isoindoline-1,3-dione and (b) a coformer. Pharmaceutical compositions comprising the solid forms (e.g., cocrystals) and methods for treating, preventing and managing various disorders are also disclosed.
ARYL HYDROCARBON RECEPTOR MODULATOR
Disclosed is an aryl hydrocarbon receptor modulator of formula (I), and a pharmaceutically acceptable salt thereof, wherein
##STR00001##
R is H, CN, CH.sub.2(OH)R.sub.0, C.sub.mH.sub.2m+1, C.sub.nH.sub.2n-1, C.sub.nH.sub.2n-3,
##STR00002##
two R.sub.a are independently H or two R.sub.a together form O or NW.sub.3R.sub.1; A is a C.sub.6 to C.sub.10 aromatic ring unsubstituted or substituted with 1 to 3 R, or a C.sub.2-C.sub.10 heteroaromatic ring interrupted by 1 to 5 heteroatoms selected from N, O, and S or a 4 to 7 membered nonaromatic heterocyclic ring containing CN and interrupted by 1 to 3 heteroatoms selected from N, O, and S, with either one unsubstituted or substituted with 1 to 3 R; Q is R, or is a C.sub.6 to C.sub.10 aromatic ring or a C.sub.2 to C.sub.10 heteroaromatic ring unsubstituted or substituted with 1 to 3 R and interrupted by 1 to 5 heteroatoms selected from N, O, and S; and R is R.sub.c which is C-attached or R.sub.N which is N-attached. The compounds of formula (I) of the present invention can regulate AhR activity, and can be used to inhibit the growth of cancer cells and inhibit the metastasis and invasion of tumor cells.
Inhibitors of KEAP1-Nrf2 protein-protein interaction
Sultam compounds, pharmaceutical compositions containing them, methods of making them, and methods of using them including methods for treating disease states, disorders, and conditions associated with the KEAP1-Nrf2 interaction, such as inflammatory bowel disease, including Crohn's disease and ulcerative colitis.
INHIBITORS OF MYELOPEROXIDASE
The specification generally relates to compounds of Formula (I), (Ia), and (Ib):
##STR00001## and pharmaceutically acceptable salts thereof, where X, Y.sup.1, Y.sup.2, Y.sup.3, Y.sup.4, and Y.sup.5 and X.sup.1, X.sup.2, r, and q, have any of the meanings defined herein, together with compositions containing them and their use in therapy. The compounds are inhibitors of the enzyme MPO, and are thereby particularly useful in the treatment or prophylaxis of diseases or conditions in which modulation of the activity of the enzyme myeloperoxidase (MPO) is desirable, including diseases with inflammatory, cardiovascular, respiratory, renal, hepatic and/or neurological components, as well as neutrophilic driven diseases.
INHIBITORS OF MYELOPEROXIDASE
The specification generally relates to compounds of Formula (I), (Ia), and (Ib):
##STR00001## and pharmaceutically acceptable salts thereof, where X, Y.sup.1, Y.sup.2, Y.sup.3, Y.sup.4, and Y.sup.5 and X.sup.1, X.sup.2, r, and q, have any of the meanings defined herein, together with compositions containing them and their use in therapy. The compounds are inhibitors of the enzyme MPO, and are thereby particularly useful in the treatment or prophylaxis of diseases or conditions in which modulation of the activity of the enzyme myeloperoxidase (MPO) is desirable, including diseases with inflammatory, cardiovascular, respiratory, renal, hepatic and/or neurological components, as well as neutrophilic driven diseases.