C07D303/32

Cosmetic Composition Comprising Vetiver Root Extract
20210030663 · 2021-02-04 ·

A cosmetic composition is provided, which comprises a carrier and a Vetiver root extract, in particular an extract from exhausted Vetiver root. This composition provides a stimulation of sebum production, stimulation of sebum antimicrobial, lipids production, activation of adipocytes volume increase, skin hydration, skin tonicity booster, skin fatigue reduction, perilabial wrinkles reduction, skin replumping, and fragrance long-lastingness enhancement.

PROCESS OF PREPARING A PEPTIDE EPOXYKETONE IMMUNOPROTEASOME INHIBITOR, AND PRECURSORS THEREOF
20200407334 · 2020-12-31 ·

Disclosed herein are methods for preparing [(2S,3R)-N-[(2S)-3-(cyclopent-1-en-1-yl)-1-[(2R)-2-methyloxiran-2-yl]-1-oxopropan-2-yl]-3-hydroxy-3-(4-methoxyphenyl)-2-[(2S)-2-[2-(morpholin-4-yl)acetamido]propanamido]propanamide (compound G):

##STR00001##

and precursors thereof.

PROCESS OF PREPARING A PEPTIDE EPOXYKETONE IMMUNOPROTEASOME INHIBITOR, AND PRECURSORS THEREOF
20200407334 · 2020-12-31 ·

Disclosed herein are methods for preparing [(2S,3R)-N-[(2S)-3-(cyclopent-1-en-1-yl)-1-[(2R)-2-methyloxiran-2-yl]-1-oxopropan-2-yl]-3-hydroxy-3-(4-methoxyphenyl)-2-[(2S)-2-[2-(morpholin-4-yl)acetamido]propanamido]propanamide (compound G):

##STR00001##

and precursors thereof.

Inhibitors of HSP90, PI3-Kinase, Proteasome, HDAC, and P97 Pathways for Selective Removal of Senescent Cells in the Treatment of Age Related Conditions
20200360386 · 2020-11-19 ·

Senescent cell medicine encompasses the paradigm that many conditions that are associated with aging or tissue damage are caused or mediated by senescent cells. This disclosure shows that HSP90, pI3-kinase, proteasome, HDAC, and p97 pathways are all active in senescent cells, and can be used as an effective means for removing senescent cells from a target tissue. Exemplary inhibitors of each of these pathways are provided. Also provided is a new genus of p97 inhibitor molecules. The structure includes a core 4 amino pyrimidine ring system, substituted at the 2 position with a nitrogen atom of an amino substituent or a N heterocycle. The 4 amino substituent of the core ring system is optionally linked to a substituted phenyl group. Any of the inhibitors referred to in this disclosure can be screened for senolytic activity and developed for the treatment of conditions such as osteoarthritis, ophthalmic disease, pulmonary disease, and atherosclerosis.

Crystalline salts of peptide epoxyketone immunoproteasome inhibitor

Provided herein is a peptide epoxyketone immunoproteasome inhibitor having a structure: Formula (I) wherein X is a counterion, crystal forms, salts, and processes for making the same, and formulations thereof. ##STR00001##

Crystalline salts of peptide epoxyketone immunoproteasome inhibitor

Provided herein is a peptide epoxyketone immunoproteasome inhibitor having a structure: Formula (I) wherein X is a counterion, crystal forms, salts, and processes for making the same, and formulations thereof. ##STR00001##

Methods and compositions for wound healing

The present invention relates to epoxy-tigliane compounds and their use in promoting wound healing. In particular embodiments, the epoxy-tigliane compounds are epoxy-tigliaen-3-one compounds. Methods of inducing or promoting wound healing as well as methods of reducing scarring and improving cosmetic outcomes upon healing of a wound are described. Compounds and compositions for use in wound healing are also described.

Methods and compositions for wound healing

The present invention relates to epoxy-tigliane compounds and their use in promoting wound healing. In particular embodiments, the epoxy-tigliane compounds are epoxy-tigliaen-3-one compounds. Methods of inducing or promoting wound healing as well as methods of reducing scarring and improving cosmetic outcomes upon healing of a wound are described. Compounds and compositions for use in wound healing are also described.

Processes for the preparation of carfilzomib or pharmaceutically acceptable salts thereof

The present invention relates to an improved process for the preparation of carfilzomib or a pharmaceutically acceptable salt thereof. The present invention also relates to a process for the preparation of amorphous form of carfilzomib.

Process of preparing a peptide epoxyketone immunoproteasome inhibitor, and precursors thereof

Disclosed herein are methods for preparing [(2S,3R)N-[(2S)-3-(cyclopent-1-en-1-yl)-1-[(2R)-2-methyloxiran-2-yl]-1-oxopropan-2-yl]-3-hydroxy-3-(4-methoxyphenyl)-2-[(2S)-2-[2-(morpholin-4-yl)acetamido]propanamido]propanamide (compound G): and precursors thereof. ##STR00001##