C07K5/06

Dipeptidomimetics as inhibitors of human immunoproteasomes
11202817 · 2021-12-21 · ·

The compounds of the present invention are represented by the following compounds having Formula I: ##STR00001##
where the substituents R.sup.1, R.sup.4, L, M, X, Y, and s are as defined herein. The compounds of the present invention are also represented by the following compounds having Formula (Ia), Formula (Ib), or Formula (Ic): ##STR00002##
where the substituents R.sup.1-R.sup.4, R.sup.x, R.sup.y, X, Y, and s are as defined herein. These compounds are used in the treatment of cancer, immunologic disorders, autoimmune disorders, neurodegenerative disorders, or inflammatory disorders or for providing immunosuppression for transplanted organs or tissues.

Dipeptidomimetics as inhibitors of human immunoproteasomes
11202817 · 2021-12-21 · ·

The compounds of the present invention are represented by the following compounds having Formula I: ##STR00001##
where the substituents R.sup.1, R.sup.4, L, M, X, Y, and s are as defined herein. The compounds of the present invention are also represented by the following compounds having Formula (Ia), Formula (Ib), or Formula (Ic): ##STR00002##
where the substituents R.sup.1-R.sup.4, R.sup.x, R.sup.y, X, Y, and s are as defined herein. These compounds are used in the treatment of cancer, immunologic disorders, autoimmune disorders, neurodegenerative disorders, or inflammatory disorders or for providing immunosuppression for transplanted organs or tissues.

COMPOUNDS CONTAINING DEUTERIUM
20210388024 · 2021-12-16 · ·

The invention provides a compound of formula (I), or a pharmaceutically acceptable salt thereof (Formula I), wherein, each R.sup.1—R.sup.30 is independently selected from the group consisting of H and deuterium, and at least one of R.sup.1—R.sup.30 is deuterium with an abundance level greater than the naturally occurring abundance of deuterium. The invention also provides pharmaceutical compositions containing the compounds, and uses of the compounds.

##STR00001##

SYNTHESIS OF BORONIC ESTER AND ACID COMPOUNDS

The invention relates to the synthesis of boronic ester and acid compounds. More particularly, the invention provides improved synthetic processes for the large-scale production of boronic ester and acid compounds, including the peptide boronic acid proteasome inhibitor bortezomib.

Cyclic peptides as protein targeting agents

Peptides having activity as protein binding agents are disclosed. The peptides have the following structure (I): ##STR00001##
including stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, wherein R, R.sup.1, L.sup.1, L.sup.2, G, M, Y.sup.1Y.sup.2 and SEQ are as defined herein. Methods associated with preparation and use of such peptides, as well as pharmaceutical compositions comprising such peptides, are also disclosed.

Cyclic peptides as protein targeting agents

Peptides having activity as protein binding agents are disclosed. The peptides have the following structure (I): ##STR00001##
including stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, wherein R, R.sup.1, L.sup.1, L.sup.2, G, M, Y.sup.1Y.sup.2 and SEQ are as defined herein. Methods associated with preparation and use of such peptides, as well as pharmaceutical compositions comprising such peptides, are also disclosed.

Tripeptide compound, preparation method therefor, and application thereof

Provided are a tripeptide compound, a preparation method therefor, and an application thereof. The structure of the related compound is represented by formula (I). The provided compound has angiotensin converting enzyme inhibiting bioactivity, and the compound and a pharmaceutical composition thereof play a role in preventing and treating hypertension and other cardiocerebral vascular system diseases.

SMAC mimetic

A SMAC mimetic and pharmaceutical compositions thereof and methods of use.

SMAC mimetic

A SMAC mimetic and pharmaceutical compositions thereof and methods of use.

BORONATE ESTER COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS THEREOF

The present invention provides novel compounds useful as proteasome inhibitors. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases.