A61K47/6801

IONIC POLYMERS COMPRISING BIOLOGICALLY ACTIVE COMPOUNDS
20210128591 · 2021-05-06 · ·

Compounds useful as biologically active compounds are disclosed. The compounds have the following structure (I): structure (I) or a stereoisomer, tautomer or salt thereof, wherein R.sup.1, R.sup.2, R.sup.3, L, L.sup.1, L.sup.2, L.sup.3, L.sup.4, M and n are as defined herein. Methods associated with preparation and use of such compounds are also provided.

##STR00001##

De-immunised anti-ERBB3 antibodies

Provided herein are antibody molecules that bind specifically to ERBB3 and related nucleic acid molecules, vectors and host cells. Also provided herein are medical uses of such antibody molecules.

ANTI-PD-L1 ANTIBODIES AND ANTIBODY-DRUG CONJUGATES
20210101982 · 2021-04-08 ·

Provided are novel anti-PD-L1 antibodies and antibody-drug conjugates and methods of using such anti-PD-L1 antibodies and antibody-drug conjugates to treat cancer.

Cyclopentane-based modulators of STING (stimulator of interferon genes)

Compounds of the general formula (I): ##STR00001##
or a pharmaceutically acceptable salt thereof, processes for the preparation of these compounds, compositions containing these compounds, and the uses of these compounds.

ANTI-HUMAN PD-L1 ANTIBODIES AND THEIR USES

An anti-PD-L1 antibody, or an antigen-binding fragment thereof, comprising: a heavy chain variable region comprising the three CDRs with the sequences of SEQ ID NOs: 2-4, 6-8, 10-12, 14-16, or 18-20; and/or a light chain variable region comprising the three CDRs with the sequences of SEQ ID NOs: 22-24, 26-28, 30-32, 34-36, or 38-40, wherein the antibody is a chimeric, humanized, composite, or human antibody.

ALK5 INHIBITORS, CONJUGATES, AND USES THEREOF

ALK5 inhibitor compounds, conjugates, and pharmaceutical compositions for use in the treatment of disease, such as cancer, are disclosed herein. The disclosed compounds are useful, among other things, in the treating of cancer and fibrosis and modulating ALK5. Additionally, compounds incorporated into a conjugate with an antibody construct are described herein.

SELECTIVE DRUG RELEASE FROM INTERNALIZED CONJUGATES OF BIOLOGICALLY ACTIVE COMPOUNDS
20210138077 · 2021-05-13 ·

The invention relates to conjugates of biologically active compounds, wherein such a conjugate is comprised of a sequence of amino acids containing a tripeptide that confers selective cleavage by tumor tissue homogenate for release of free drug and/or improves biodistribution into the tumor tissue in comparison to normal tissue homogenate from the same species, wherein the normal tissue is the site of an adverse event associated with administration to a human subject in need thereof of a therapeutically effective amount of a comparator conjugate whose amino acid sequence is a dipeptide known to be selectively cleavable by Cathepsin B.

TGFßR1 INHIBITOR-ASGR ANTIBODY CONJUGATES AND USES THEREOF

Various conjugates and compositions thereof are disclosed for use in the treatment of a liver disease, such as liver cancer and liver fibrosis. The compositions comprise conjugates, wherein the conjugates are comprised of an antibody or antibody construct specific for ASGR1 or ASGR2 attached to a TGFβR1 inhibitor via a linker. Additionally provided are the methods of preparation of the conjugates and compositions thereof.

THERAPEUTIC MOLECULES

The invention relates to binding molecules that bind specifically to prostate specific membrane antigen (PSMA), in particular, single human variable heavy chain domain antibodies and related methods for treatment of cancer.

COMPOSITIONS COMPRISING A FATTY ACID OIL MIXTURE AND A FREE FATTY ACID, AND METHODS AND USES THEREOF

Compositions comprising a fatty acid oil mixture and at least one free fatty acid, and uses thereof are disclosed. Further disclosed are preconcentrates capable of forming a self-nanoemulsifying drug delivery system (SNEDDS), a self-microemulsifying drug delivery system (SMEDDS) or self-emulsifying drug delivery systems (SEDDS) in an aqueous solution. Preferred fatty acids are eicosapentaenoic acid (EPA) and docosahexaenoic acid (DHA) in a form chosen from ethyl ester and triglyceride.