C07D233/54

Chiral synthesis method for producing cis-imidazoline compounds for pharmaceutical use

This invention provides a method for enantioselective synthesis of cis-imidazolines and related structures through chiral resolution. A chiral acid is used to separate enantiomeric precursors of the cis-imidazolines from a racemic mixture by selective crystallization. Both enantiomers can be cyclized into the desired cis-imidazoline by complementary pathways. Compounds can be synthesized according to the invention with an enantiomeric excess as high as 99%. Cis-imidazolines such as Nutlin-3a prepared according to this invention may be used for treating cancer, killing senescent cells, or treating senescence-associated conditions.

Chiral synthesis method for producing cis-imidazoline compounds for pharmaceutical use

This invention provides a method for enantioselective synthesis of cis-imidazolines and related structures through chiral resolution. A chiral acid is used to separate enantiomeric precursors of the cis-imidazolines from a racemic mixture by selective crystallization. Both enantiomers can be cyclized into the desired cis-imidazoline by complementary pathways. Compounds can be synthesized according to the invention with an enantiomeric excess as high as 99%. Cis-imidazolines such as Nutlin-3a prepared according to this invention may be used for treating cancer, killing senescent cells, or treating senescence-associated conditions.

Pesticidally active heterocyclic derivatives with sulphur containing substituents

Compounds of formula (I), wherein the substituents are as defined in claim 1, and the agrochemically acceptable salts, stereoismers, enantiomers, tautomers and N-oxides of those compounds, can be used as insecticides and can be prepared in a manner known per se. ##STR00001##

Pesticidally active heterocyclic derivatives with sulphur containing substituents

Compounds of formula (I), wherein the substituents are as defined in claim 1, and the agrochemically acceptable salts, stereoismers, enantiomers, tautomers and N-oxides of those compounds, can be used as insecticides and can be prepared in a manner known per se. ##STR00001##

AMIDO-SUBSTITUTED CYCLOHEXANE DERIVATIVES

The present invention relates to amido-substituted cyclohexane compounds of general formula (I), in which A, R.sup.4, R.sup.6, R.sup.7, R.sup.8, R.sup.9, R.sup.10 and R.sup.11 are as defined herein, to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of neoplasms, as a sole agent or in combination with other active ingredient.

##STR00001##

INHIBITORS OF ALPHA-AMINO-BETA-CARBOXYMUCONIC ACID SEMIALDEHYDE DECARBOXYLASE
20180134667 · 2018-05-17 ·

The present disclosure discloses compounds capable of modulating the activity of -amino--carboxymuconic acid semialdehyde decarboxylase (ACMSD), which are useful for the prevention and/or the treatment of diseases and disorders associated with defects in NAD.sup.+ biosynthesis, e.g., metabolic disorders, neurodegenerative diseases, chronic inflammatory diseases, kidney diseases, and diseases associated with ageing. The present application also discloses pharmaceutical compositions comprising said compounds and the use of such compounds as a medicament.

Metabotropic glutamate receptor negative allosteric modulators (NAMS) and uses thereof

Provided herein are small molecule active metabotropic glutamate subtype-2 and -3 receptor negative allosteric modulators (NAMs), compositions comprising the compounds, and methods of using the compounds and compositions.

COMPOUNDS AND METHODS FOR IDO AND TDO MODULATION AND INDICATIONS THEREFOR

Disclosed are compounds of Formula I(a):

##STR00001##

or a pharmaceutically acceptable salt, a solvate, a tautomer, an isomer or a deuterated analog thereof, wherein R.sup.4, R.sup.5, R.sup.6, R.sup.7, G.sup.1, G.sup.2 and Ring A are as described in any of the embodiments described in this disclosure; compositions thereof; and uses thereof.

ANESTHETIC COMPOUNDS AND RELATED METHODS OF USE

Provided herein are compounds according to formula (I):

##STR00001##

Provided herein is also a pharmaceutical composition comprising a compound according to formula (I) and a pharmaceutically acceptable carrier, and a method for providing anesthesia in a subject by administering such a pharmaceutical composition.

ANESTHETIC COMPOUNDS AND RELATED METHODS OF USE

Provided herein are compounds according to formula (I):

##STR00001##

Provided herein is also a pharmaceutical composition comprising a compound according to formula (I) and a pharmaceutically acceptable carrier, and a method for providing anesthesia in a subject by administering such a pharmaceutical composition.