C07D207/16

TLR2 MODULATOR COMPOUNDS, PHARMACEUTICAL COMPOSITIONS AND USES THEREOF

The present disclosure relates to compounds which modulate the activity of Toll-like receptor (TLR) proteins, including agonists or activators, partial agonists, and antagonists. Of particular interest of compounds that modulate the activity of TLR2, as well as methods of using such compounds to treat cancer and other disorders associated with a TLR2 pathway.

Methods and compositions for targeting Tregs using CCR8 inhibitors

The present invention provides compounds of Formula (I) which can be used as CCR8 inhibitors, which can be used as treatment or prevention of cancer using CCR8 inhibitors targeted tumor specific T regulatory cells.

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Methods and compositions for targeting Tregs using CCR8 inhibitors

The present invention provides compounds of Formula (I) which can be used as CCR8 inhibitors, which can be used as treatment or prevention of cancer using CCR8 inhibitors targeted tumor specific T regulatory cells.

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PROLINE-LOCKED STAPLED PEPTIDES AND USES THEREOF

The present invention provides a new type of alpha-helix nucleating cross-link (“staple”) formed by olefin metathesis of a proline derivative with an alkenyl side chain and another amino acid derivative with an alkenyl side chain. The proline derivatives as described herein have been found to be strong nucleators of alpha-helix formation. The invention also provides moieties for shielding the free amide N—H's at the N-terminus of an alpha-helix, thereby further stabilizing the helix. The proline derivatives, precursors prior to cross-linking, and the cross-linked peptides are provided as well as methods of using and preparing these compounds and peptides.

PROLINE-LOCKED STAPLED PEPTIDES AND USES THEREOF

The present invention provides a new type of alpha-helix nucleating cross-link (“staple”) formed by olefin metathesis of a proline derivative with an alkenyl side chain and another amino acid derivative with an alkenyl side chain. The proline derivatives as described herein have been found to be strong nucleators of alpha-helix formation. The invention also provides moieties for shielding the free amide N—H's at the N-terminus of an alpha-helix, thereby further stabilizing the helix. The proline derivatives, precursors prior to cross-linking, and the cross-linked peptides are provided as well as methods of using and preparing these compounds and peptides.

COMPOSITIONS AND METHODS AND USES RELATING THERETO

Stable crystal forms comprising lithium ions and the conjugate base of an organic acid which is in the form of anhydrous coordination polymer that exhibit improved in vivo performance with respect to lithium carbonate.

COMPOSITIONS AND METHODS AND USES RELATING THERETO

Stable crystal forms comprising lithium ions and the conjugate base of an organic acid which is in the form of anhydrous coordination polymer that exhibit improved in vivo performance with respect to lithium carbonate.

YAP1 INHIBITORS THAT TARGET THE INTERACTION OF YAP1 WITH OCT4

Binding of the transcriptional co-activator, YAP1, to the transcription factor Oct4, induces Sox2, which is a transcription actor necessary for the self-renewal of stem-like cells from non-small cell lung cancer. The WW domain of YAP1 binds to the PPxY motif of Oct4 to induce Sox2. Delivering a peptide corresponding to the WW domain could prevent the induction of Sox2 and sternness. Similarly, peptides and mimetics of the PPxY motif would be able to inhibit sternness. Disclosed are compounds that affect the Yap1:Oct4 interaction.

SULPHONAMIDES AS METHIONINE METABOLIC PATHWAY INHIBITORS
20230232828 · 2023-07-27 ·

The present invention provides novel sulphonamide inhibitors of cystathionin gamma synthase (CGS), their use as selective and non-selective herbicides, agricultural and non-agricultural herbicides, herbicides in integrated pest management, herbicides for gardening, clearing waste ground, clearing industrial or constructions sites, clearing railways and railway embankments, pesticide, fungicide, agricultural plant stimulant or antimicrobial agent. Also provided is a method for the control of undesired vegetation or clearing areas from the undesired vegetation comprising applying to the locus of said undesired vegetation, to the undesired plants or to a habitat thereof, a herbicidally effective amount of the compound of the present invention.

NOVEL ANALOGS OF PTEROSTILBENE AMINO ACID BEARING CARBONATES FOR TREATING A NON-ALCOHOLIC FATTY LIVER DISEASE AND NONALCOHOLIC STEATOHEPATITIS
20230234912 · 2023-07-27 ·

A series of novel analogs of water soluble pterostilbene amino acid bearing carbonates were synthesized, which show activities in treating a non-alcoholic fatty liver disease and a nonalcoholic steatohepatitis (NASH).