C07K5/06191

Borylated Di-Peptide Amino Acid compositions for use in Boron Neutron Capture Therapy and methods thereof

Borylated Di-Peptide Amino Acid (“Bdi-AA”) compositions and Di-Peptide Amino Acid (di-AA) compositions and methods of making Bdi-AAs and di-AAs are disclosed herein. Consequently, the Bdi-AAs and di-AAs can be administered to patients as a Neutron Capture Agent and provide a method of treating cancer, immunological disorders, and other disease by utilizing a Neutron Capture Therapy modality.

ENZYME INHIBITORS

The present invention provides compounds of formula (I): Formula (I) compositions comprising such compounds; the use of such compounds in therapy; and methods of treating patients with such compounds; wherein A, Y, n, R1, R2.sup.A, R2.sup.B, R3 and *1 are as defined herein.

##STR00001##

PEPTIDOMIMETICS FOR THE TREATMENT OF CORONAVIRUS AND PICORNAVIRUS INFECTIONS
20220273753 · 2022-09-01 ·

Compounds, compositions and methods for preventing, treating or curing a coronavirus, picornavirus, and/or hepeviridae virus infection in human subjects or other animal hosts. Specific viruses that can be treated include enteroviruses. In one embodiment, the compounds can be used to treat an infection with a severe acute respiratory syndrome virus, such as human coronavirus 229E, SARS, MERS, SARS-CoV-1 (OC43), and SARS-CoV-2. In another embodiment, the methods are used to treat a patient co-infected with two or more of these viruses, or a combination of one or more of these viruses and norovirus.

Delivery systems for controlled drug release

The present invention provides a compound having the structure of Formula (I) or a pharmaceutically acceptable salt, hydrate, solvate, or isomer thereof, for the controlled delivery and release of Agent. ##STR00001##

CYCLEN BASED COMPOUNDS, COORDINATION COMPOUNDS, PEPTIDES, PHARMACEUTICAL PREPARATION, AND USE THEREOF

Cyclen based compounds of general formula (I) are disclosed. X is nitrogen and Y, Z are —CH—, or X, Z are —CH— and Y is nitrogen, or X, Y are —CH— and Z is nitrogen. R.sup.1 is independently selected from H; COOH; benzyloxycarbonyl; fluorenylmethyloxycarbonyl; tert-butoxycarbonyl; methylcarbonyl; trifluoromethylcarbonyl; benzyl; triphenylmethyl; tosyl; mesyl; benzyloxymethyl; phenylsulfonyl; ethoxycarbonyl; 2,2,2-trichloroethyloxycarbonyl; methoxycarbonyl; methoxymethyloxycarbonyl; R.sup.2 is selected from H; methylcarbonyl; tert-butyldimethylsilyl; (C1-C4)alkyl; R.sub.3 is independently selected from H; (C1-C6)alkyl.

Tubulysin analogues as anticancer agents and payloads for antibody-drug conjugates and methods of treatment therewith

In one aspect, the present disclosure provides tubulysin analogs of the formula (I) wherein the variables are as defined herein. In another aspect, the present disclosure also provides methods of preparing the compounds disclosed herein. In another aspect, the present disclosure also provides pharmaceutical compositions and methods of use of the compounds disclosed herein. Additionally, drug conjugates with cell targeting moieties of the compounds are also provided. ##STR00001##

SOLID STATE FORMS OF IVOSIDENIB

Solid state forms of Ivosidenib, processes for preparation thereof, pharmaceutical compositions thereof, and uses thereof are disclosed.

PROTEIN ARGININE METHYLTRANSFERASE 5 (PRMT5) DEGRADATION / DISRUPTION COMPOUNDS AND METHODS OF USE

Disclosed are protein arginine methyltransferase 5 (PRMT5) degradation/disruption compounds including a PRMT5 ligand, a degradation/disruption tag and a linker, and methods for use of such compounds in the treatment of PRMT5-mediated diseases. The PRMT5 degraders disclosed herein offer a novel mechanism for treating PRMT5-mediated diseases compared to small molecule inhibitors of PRMT5 activity.

Tripeptide epoxy ketone protease inhibitors

Provided herein are tripeptide epoxy ketone protease inhibitors, methods of their preparation, related pharmaceutical compositions, and methods of using the same. For example, provided herein are compounds of Formula (X): ##STR00001##
and pharmaceutically acceptable salts and compositions including the same. The compounds and compositions provided herein may be used, for example, in the treatment of diseases including inflammation and neurodegenerative disease.

Difluoroketamide derivatives as HtrA1 inhibitors

The invention provides novel compounds having the general formula (I) ##STR00001##
wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, R.sup.9, R.sup.10, R.sup.11 and R.sup.23 are as described herein, compositions including the compounds and methods of using the compounds.