C07D207/16

PREPARATION METHOD OF A HIGH-OPTICAL-PURITY CHIRAL OXO-AZA-CYCLOALKANE COMPOUND
20230064377 · 2023-03-02 ·

A preparation method of a high-optical-purity chiral oxo-aza-cycloalkane compound comprises the steps of: (R or S)N-substituent P-2-alkoxycarbonylalkyliminodiacetic acid diester as the raw material is cyclized in the presence of a solvent and a cyclization reagent (lewis acid-lewis base) to obtain high-optical-purity N-substituent P -2- (R or S)- substituent G oxo-aza-cycloalkane or the salt thereof through thermal decarboxylation or hydrolysis decarboxylation reaction; the specific type of cyclization reagent used in the present invention is conductive to the preparation of the high-optical-purity target product, easily recoverable, with reduced waste liquid discharge, green, and environment-friendly, which contributes to green industrial production.

COMPOSITIONS AND METHODS FOR PREPARING REGIO- AND STEREOSELECTIVE ALICYCLIC ALKENE ISOTOPOLOGUES AND STEREOISOTOPOMERS

A method for preparing isotopologues and/or stereoisotopomers of cyclic and heterocyclic alkenes and dienes is described. The method provides regio- and/or stereospecific addition of hydrogen, deuterium, tritium and a variety of other substituents to arenes, heteroarenes, and alicyclic compounds that have multiple carbon-carbon double bonds, thereby providing discrete isotopologues and stereoisotopomers of cyclic and heterocyclic alkenes and dienes with high isotopic purity and in high enantiomeric excess. Also described are isotopologues and stereoisotopomers of cyclic and heterocyclic alkenes and dienes, such as isotopologues and stereoisotopomers of cyclohexene and tetrahydropyridine, as well as products thereof, such as isotopologues and stereoisotopomers of piperidines and piperidine-containing compounds, such as methylphenidate. In addition, a method of determining the absolute configuration of stereoisotopomers of cyclohexenes is described.

METHODS OF MANUFACTURING A BIFUNCTIONAL COMPOUND
20230069491 · 2023-03-02 ·

This disclosure pertains to the preparation of bifunctional compounds (e.g., Compound 1), intermediates in the preparation of such compounds, and preparation of such intermediates.

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FERROPTOSIS INHIBITORS - DIARYLAMINE PARA-ACETAMIDES
20230159492 · 2023-05-25 · ·

Provided are compounds that inhibit ferroptosis activity, or modulate or inhibit a disease associated with ferroptosis dysregulation, such as neuropathy, ischemia reperfusion injury, acute kidney failure and cancer, including corresponding sulfonamides, and pharmaceutically acceptable salts, hydrates and stereoisomers thereof. The compounds are employed in pharmaceutical compositions, and methods of making and use, including treating a person in need thereof with an effective amount of the compound or composition, and detecting a resultant improvement in the person's health or condition.

DIMERS FOR USE IN SYNTHESIS OF PEPTIDOMIMETICS
20230159450 · 2023-05-25 ·

Dimers for use in synthesis of peptidomimetics are described. Uses of dimers as synthons in synthesis of azapeptides and other peptidomimetics, azapeptides and other peptidomimetics synthesized from the dimers and uses of azapeptides and other peptidomimetics are also described.

DIMERS FOR USE IN SYNTHESIS OF PEPTIDOMIMETICS
20230159450 · 2023-05-25 ·

Dimers for use in synthesis of peptidomimetics are described. Uses of dimers as synthons in synthesis of azapeptides and other peptidomimetics, azapeptides and other peptidomimetics synthesized from the dimers and uses of azapeptides and other peptidomimetics are also described.

Methods and Compositions for Targeting Tregs using CCR8 Inhibitors
20230159446 · 2023-05-25 ·

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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NOVEL SMALL MOLECULE INHIBITORS OF TEAD TRANSCRIPTION FACTORS

The present disclosure compounds, as well as their compositions and methods of use. The compounds inhibit the activity of the TEAD transcription factor, and are useful in the treatment of diseases related to the activity of TEAD transcription factor including, e.g., cancer and other diseases.

NOVEL SMALL MOLECULE INHIBITORS OF TEAD TRANSCRIPTION FACTORS

The present disclosure compounds, as well as their compositions and methods of use. The compounds inhibit the activity of the TEAD transcription factor, and are useful in the treatment of diseases related to the activity of TEAD transcription factor including, e.g., cancer and other diseases.

Guanidine compounds and use thereof

The present invention relates to guanidine compounds for inhibiting mitochondrial oxidative phosphorylation (OXPHOS) and use thereof. More specifically, the present invention relates to a pharmaceutical composition for preventing or treating a OXPHOS-related disease, particularly cancer, by inhibiting mitochondrial oxidative phosphorylation and reprogramming cellular metabolism.