C07K5/06026

METAL COMPOUND HAVING PHASE TRANSFORMATION AND METHOD OF PREPARING THE SAME
20220041461 · 2022-02-10 · ·

The present invention relates to a metal phase transformation compound and a method for preparing the same.

ANTIVIRAL COMPOUNDS

The invention provides a compound of formula I, formula II, or formula III:

##STR00001##

or a salt thereof, wherein R.sup.1-R.sup.10 have any of the values described in the specification, as well as compositions comprising a compound of formula I. The compounds are useful as HIV-1 CA-targeting molecules and as antiviral agents.

PYRROLOBENZODIAZEPINE CONJUGATES
20210316006 · 2021-10-14 ·

A compound of formula (I) wherein R.sup.L is a linker for connection to a cell binding agent.

##STR00001##

METAL DI-AMINO ACID CHELATES OR METAL TRI-AMINO ACID CHELATES
20210369768 · 2021-12-02 ·

The present disclosure relates to metal di-amino acid chelates and metal tri-amino acid chelates.

REPROGRAMMING UROKINASE INTO AN ANTIBODY-RECRUITING ANTICANCER AGENT
20210284988 · 2021-09-16 ·

The present invention relates to chimeric (preferably, bifunctional) compounds, compositions comprising those compounds and methods of treating cancer in a patient or subject, especially including metastatic cancer where cancer cells exhibit ovrexpression (heightened expression) of cell surface urokinase-type plasminogen activator receptor (urokinase receptor) compared to normal (non-cancerous) cells. The compounds preferably covalently bind to the urokinase receptor and recruit native antibodies of the patient or subject where the antibodies can selectively degrade and/or deactivate targeted cancer cells through antibody-dependent cellular phagocytosis and/or antibody-dependent cellular cytotoxicity (ADCC) against a large number and variety of cancers, thus providing cancer cell death and/or an inhibition of growth, elaboration and/or metastasis of the cancer, including remission and cure of the patient's cancer.

PPAR agonists and methods of use thereof

Provided herein are deuterated compounds and compositions useful in increasing PPARδ activity. The compounds have a formula ##STR00001##
where L.sup.5 comprises at least one deuterium. Exemplary species include ##STR00002##
The compounds and compositions provided herein are useful for the treatment of PPARδ related diseases (e.g., muscular diseases, vascular disease, demyelinating disease, and metabolic diseases).

NON-PEPTIDIC CELL-PENETRATING MOTIFS

Disclosed are compounds that can penetrate the mitochondrial membrane and that are able to deliver cargo (e.g., therapeutic agents) specifically to the mitochondria.

AMIDE COMPOUND HAVING BET PROTEOLYSIS-INDUCING ACTION AND MEDICINAL APPLICATION THEREOF

Provided are a compound superior in a cytotoxic action on cancer cells, an action inducing degradation of BET protein in cancer cells, and an inhibitory action on the binding of BET protein and acetylated histone, and useful as an anticancer agent, a BET protein degradation inducer or a BET protein inhibitor. A compound represented by the following formula (I)

##STR00001##

wherein each symbol is as defined in the specification, or a pharmacologically acceptable salt thereof

COATING FILM-FORMING COMPOSITION

A composition that can more readily form a coating film exhibiting excellent moisture-retaining property. A coating film-forming composition including at least one lipidic peptide compound composed of a low-molecular-weight lipidic peptide or a pharmaceutically usable salt thereof. The lipidic peptide compound may preferably be a compound prepared by bonding of a peptide moiety having an amino acid repeating structure to a lipidic moiety having a C.sub.9-23 aliphatic group.

FAP-activated proteasome inhibitors for treating solid tumors

Disclosed are proteasome inhibitors, fibroblast activation protein (FAP)-activated prodrugs of proteasome inhibitors, and pharmaceutically acceptable salts of the inhibitors and prodrugs. Also disclosed are related pharmaceutical compositions, and methods of using the inhibitors and prodrugs and compositions thereof, for example, in treating cancer or other cell proliferative diseases. In vitro and in vivo methods of quantifying the expression of FAP in a biopsy sample and a mammal, respectively, are also disclosed.