790667-50-4

Upstream product

• 50-00-0 formaldehyd 
• 17486-12-3 (E)-but-2-en-1-yltrimethylsilane 
• 90284-71-2 N-benzylammonium trifluoroacetate 
• 34737-89-8 1-Benzyl-3-methyl-4-piperidon 
• 863249-31-4 (3S,4S)-3-methylpiperidin-4-yl pivalate 
• 100-52-7 benzaldehyde 

Downstream Products

• 36173-52-1 (3R,4R)-4-hydroxy-3-methylpiperidine 
• 36173-52-1 rac-trans-3-methylpiperidin-4-ol 
• 955028-90-7 rac-(cis)-tert-butyl 4-hydroxy-3-methylpiperidine-1-carboxylate 
• 955028-90-7 (+/-) tert-butyl trans-4-hydroxy-3-methylpiperidine-1-carboxylate 
• 1610033-94-7 2-((2R,4R)-1-(4-(((3,4-trans)-1-(5-chloro-2-methoxypyridin-4-yl)-3-methylpiperidin-4-yl)oxy)phenyl)-4-(trifluoromethyl)pyrrolidin-2-yl)acetonitrile 
• 88915-34-8 1-benzyl-3-methylpiperidin-4-amine 
• 88915-34-8 (3R,4S)-1-benzyl-3-methylpiperidin-4-amine 
• 955028-90-7 (3,4-trans)-tert-butyl 4-hydroxy-3-methylpiperidine-1-carboxylate 
• 36173-52-1 (3,4-trans)-3-methylpiperidin-4-ol 

Relevant academic research and scientific papers

Enzymatic reduction of α-substituted ketones with concomitant dynamic kinetic resolution

Racemic α-substituted ketones were converted to the corresponding chiral alcohols with high diastereo- and enantioselectivities using enzymatic reduction with concomitant dynamic kinetic resolution. Reductions of N-protected α-amino ketones by microorgani

SUBSTITUTED BICYCLIC COMPOUNDS USEFUL AS T CELL ACTIVATORS

Disclosed are compounds of Formula (I): or a salt thereof, wherein: X is CR6 or N; Y is CR3 or N; R1, R2, R3, R4, R5, R6, R7, and m are defined herein. Also disclosed are methods of using such compounds to inhibit the activity of one or both of diacylglycerol kinase alpha (DGKα) and diacylglycerol kinase zeta (DGKζ), and pharmaceutical compositions comprising such compounds. These compounds are useful in the treatment of viral infections and proliferative disorders, such as cancer.

Discovery of a Potent and Selective CCR4 Antagonist That Inhibits Treg Trafficking into the Tumor Microenvironment

Recruitment of suppressive CD4+ FOXP3+ regulatory T cells (Treg) to the tumor microenvironment (TME) has the potential to weaken the antitumor response in patients receiving treatment with immuno-oncology (IO) agents. Human Treg express CCR4 and can be recruited to the TME through the CC chemokine ligands CCL17 and CCL22. In some cancers, Treg accumulation correlates with poor patient prognosis. Preclinical data suggests that preventing the recruitment of Treg and increasing the population of activated effector T cells (Teff) in the TME can potentiate antitumor immune responses. We developed a novel series of potent, orally bioavailable small molecule antagonists of CCR4. From this series, several compounds exhibited high potency in distinct functional assays in addition to good in vitro and in vivo ADME properties. The design, synthesis, and SAR of this series and confirmation of its in vivo activity are reported.

Discovery of Potent and Orally Bioavailable Dihydropyrazole GPR40 Agonists

G protein-coupled receptor 40 (GPR40) has become an attractive target for the treatment of diabetes since it was shown clinically to promote glucose-stimulated insulin secretion. Herein, we report our efforts to develop highly selective and potent GPR40 agonists with a dual mechanism of action, promoting both glucose-dependent insulin and incretin secretion. Employing strategies to increase polarity and the ratio of sp3/sp2 character of the chemotype, we identified BMS-986118 (compound 4), which showed potent and selective GPR40 agonist activity in vitro. In vivo, compound 4 demonstrated insulinotropic efficacy and GLP-1 secretory effects resulting in improved glucose control in acute animal models.

6,7-DIHYDRO-5H-PYRROLO[3,4-B]PYRIDIN-5-ONE ALLOSTERIC MODULATORS OF THE M4 MUSCARINIC ACETYLCHOLINE RECEPTOR

The present invention is directed to 6,7-dihydro-5H-pyrrolo[3,4-b]pyridine-5-one compounds which are allosteric modulators of the M4 muscarinic acetylcholine receptor. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which M4 muscarinic acetylcholine receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which M4 muscarinic acetylcholine receptors are involved.

PYRROLIDINE GPR40 MODULATORS FOR THE TREATMENT OF DISEASES SUCH AS DIABETES

The present invention provides compounds of Formula (I) or a stereoisomer, a tautomer, a pharmaceutically acceptable salt, a polymorph, or a solvate thereof, wherein all of the variables are as defined herein. These compounds are GPR40 G protein-coupled receptor modulators which may be used as medicaments.

Dihydropyrazole GPR40 modulators

The present invention provides compounds of Formula (I): or a stereoisomer, or a pharmaceutically acceptable salt thereof, wherein all of the variables are as defined herein. These compounds are GPR40 G protein-coupled receptor modulators which may be used as medicaments.

PYRROLIDINE GPR40 MODULATORS

The present invention provides compounds of Formula (I): or a stereoisomer, or a pharmaceutically acceptable salt thereof, wherein all of the variables are as defined herein. These compounds are GPR40 G protein-coupled receptor modulators which may be used as medicaments.

ARYL CARBOXYLIC ACID CYCLOHEXYL AMIDE DERIVATIVES

A compound of formula (I) or a pharmaceutically acceptable salt or prodrug ester thereof: (I) wherein the variants R and X are defined in the specification.

CYCLIC AMINE COMPOUND AND PEST CONTROL AGENT

A pest control agent characterized by containing as an active ingredient a cyclic amine compound represented by the formula (1): (wherein Cy1 represents an (un)substituted five-membered heterocycle or an (un)substituted group represented by the