C07C237/12

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.

Compositions and methods relating to salts of specialized pro-resolving mediators

The present invention relates to compounds of Formulas I-IV, which are salts of special lipid mediators of inflammation, compositions containing same, and methods of using same in the treatment of various diseases and disorders characterized by chronic or excessive inflammation, or both. Provided are pharmaceutical compositions adapted to deliver the compounds the lower gastrointestinal tract and methods of using same as monotherapy in the treatment of inflammatory diseases or disorders of the lower gastrointestinal tract, and in combination therapy with 5-aminosalicylate.

Compositions and methods relating to salts of specialized pro-resolving mediators

The present invention relates to compounds of Formulas I-IV, which are salts of special lipid mediators of inflammation, compositions containing same, and methods of using same in the treatment of various diseases and disorders characterized by chronic or excessive inflammation, or both. Provided are pharmaceutical compositions adapted to deliver the compounds the lower gastrointestinal tract and methods of using same as monotherapy in the treatment of inflammatory diseases or disorders of the lower gastrointestinal tract, and in combination therapy with 5-aminosalicylate.

Method for producing amide compound

Provided is a novel method for producing amide compounds at high stereochemical selectivities. The method according to the present invention for producing amide compounds is provided with an amidation step for reacting, in the presence of a catalyst comprising a metal compound, an amino compound with an aminoester compound represented by general formula (1) to amidate the ester group in the aminoester compound.

Method for producing amide compound

Provided is a novel method for producing amide compounds at high stereochemical selectivities. The method according to the present invention for producing amide compounds is provided with an amidation step for reacting, in the presence of a catalyst comprising a metal compound, an amino compound with an aminoester compound represented by general formula (1) to amidate the ester group in the aminoester compound.

Method for producing amide compound

Provided is a novel method for producing amide compounds at high stereochemical selectivities. The method according to the present invention for producing amide compounds is provided with an amidation step for reacting, in the presence of a catalyst comprising a metal compound, an amino compound with an aminoester compound represented by general formula (1) to amidate the ester group in the aminoester compound.

LIPID NANOPARTICLE COMPOSITION
20220153686 · 2022-05-19 ·

Provided herein are lipids that can be used in combination with other lipid components, such as neutral lipids, cholesterol and polymer conjugated lipids, to form lipid nanoparticles for delivery of therapeutic agents (e.g., nucleic acid molecules) for therapeutic or prophylactic purposes, including vaccination.

LIPID NANOPARTICLE COMPOSITION
20220153686 · 2022-05-19 ·

Provided herein are lipids that can be used in combination with other lipid components, such as neutral lipids, cholesterol and polymer conjugated lipids, to form lipid nanoparticles for delivery of therapeutic agents (e.g., nucleic acid molecules) for therapeutic or prophylactic purposes, including vaccination.

Modulators of Sestrin-GATOR2 interaction and uses thereof

The present invention provides compounds, compositions thereof, and methods of using the same.