281234-93-3

Upstream product

• 79421-43-5 N-(4-cyanophenyl)-4-hydroxypiperidine 
• 5382-16-1 4-HYDROXYPIPERIDINE 
• 619-42-1 4-methoxycarbonylphenyl bromide 
• 73775-92-5 piperidin-4-yl acetate 
• 109384-19-2 t-butyl 4-hydroxy piperidine-1-carboxylate 
• 850452-53-8 2-methylpropan-2-yl 4-(acetyloxy)piperidine-1-carboxylate 
• 403-33-8 methyl 4-flurobenzoate 
• 1103500-41-9 methyl 4-(4-hydroxypiperidin-1-yl)benzoate 

Downstream Products

• 1616960-91-8 4-(4-hydroxypiperidin-1-yl)-N-(2-(2-methyl-1H-indol-1-yl)ethyl)benzamide 

Relevant academic research and scientific papers

ANDROGEN RECEPTOR PROTEIN DEGRADERS WITH A TRICYCLIC CEREBLON LIGAND

The present disclosure provides compounds represented by Formula I : A-L-B 1 I, and the salts or solvates thereof, wherein A, L, and B1 are as defined in the specification. ompounds having Formula I are androgen receptor degraders useful for the treatment of ancer and other diseases.

Strategies toward Discovery of Potent and Orally Bioavailable Proteolysis Targeting Chimera Degraders of Androgen Receptor for the Treatment of Prostate Cancer

Proteolysis targeting chimera (PROTAC) small-molecule degraders have emerged as a promising new type of therapeutic agents, but the design of PROTAC degraders with excellent oral pharmacokinetics is a major challenge. In this study, we present our strategies toward the discovery of highly potent PROTAC degraders of androgen receptor (AR) with excellent oral pharmacokinetics. Employing thalidomide to recruit cereblon/cullin 4A E3 ligase and through the rigidification of the linker, we discovered highly potent AR degraders with good oral pharmacokinetic properties in mice with ARD-2128 being the best compound. ARD-2128 achieves 67% oral bioavailability in mice, effectively reduces AR protein and suppresses AR-regulated genes in tumor tissues with oral administration, leading to the effective inhibition of tumor growth in mice without signs of toxicity. This study supports the development of an orally active PROTAC AR degrader for the treatment of prostate cancer and provides insights and guidance into the design of orally active PROTAC degraders.

C-3 NOVEL TRITERPENONE WITH C-17 REVERSE AMIDE DERIVATIVES AS HIV INHIBITORS

The present invention relates to C-3 novel triterpenone with C-17 reverse amide compounds of Formula (I); and pharmaceutically acceptable salts thereof, wherein ring Formula (II), R1, R2, R3, R4, R5, R6, R7, 'n' and 'm' are as defined in Formula (I). The invention also relates to C-3 novel triterpenone with C-17 reverse amide derivatives, related compounds, and pharmaceutical compositions useful for the therapeutic treatment of viral diseases and particularly HIV mediated diseases.

SUBSTITUTED (AMINOIMINOMETHYL OR AMINOMETHYL) BENZOHETEROARYL COMPOUNDS

This invention is directed to an (aminoiminomethyl or aminomethyl) benzoheteroaryl compound of formula I which is useful for inhibiting the activity of Factor Xa by combining said compound with a composition containing Factor Xa. The present invention is also directed to compositions containing compounds of the formula I, methods for their preparation, their use, such as in inhibiting the formation of thrombin or for treating a patient suffering from, or subject to, a disease state associated with a physiologically detrimental excess amount of thrombin.