84359-50-2

Upstream product

• 470689-98-6 4-diphenylaminopiperidine-1-carboxylic acid tert-butyl ester 
• 125541-22-2 1-(tert-butoxycarbonyl)-4-phenylaminopiperidine 
• 79099-07-3 N-tert-butyloxycarbonylpiperidin-4-one 
• 62-53-3 aniline 
• 108-86-1 bromobenzene 

Downstream Products

• 685530-67-0 4'-cyano-4-diphenylamino-[1,4']bipiperidinyl-1'-carboxylic acid tert-butyl ester 
• 470690-00-7 4-diphenylamino-[1,4']bipiperidinyl-1'-carboxylic acid tert-butyl ester 
• 1416053-66-1 (2R)-1-[4-(diphenylamino)piperidin-1-yl]-3-(quinolin-5-yloxy)propan-2-ol 
• 1610999-33-1 3-[4-(diphenylamino)piperidin-1-yl]-N-(3-methoxyphenyl)-N-methylpropanamide 

Relevant academic research and scientific papers

HETEROCYCLICALKYL DERIVATIVE COMPOUNDS AS SELECTIVE HISTONE DEACETYLASE INHIBITORS AND PHARMACEUTICAL COMPOSITIONS COMPRISING THE SAME

The present invention relates to novel heterocyclicalkyl derivatives having histone deacetylase (HDAC) inhibitory activity, optical isomers thereof or pharmaceutically acceptable salts thereof, the use thereof for the preparation of medicaments, pharmaceutical compositions containing the same, a method for treating diseases using the composition, and methods for preparing the novel heterocyclicalkyl derivatives. The novel heterocyclicalkyl derivatives according to the present invention are selective histone deacetylase (HDAC) inhibitors, and may be effectively used for the treatment of histone deacetylase-mediated diseases, such as cell proliferative diseases, inflammatory diseases, autosomal dominant diseases, genetic metabolic diseases, autoimmune diseases, acute/chronic neurological disease, hypertrophy, heart failure, ocular diseases, or neurodegenerative diseases.

Synthesis of 5-oxyquinoline derivatives for reversal of multidrug resistance

The inhibition of ABC (ATP binding cassette) transporters is considered a powerful tool to reverse multidrug resistance. Zosuquidar featuring a difluorocyclopropyl-annulated dibenzosuberyl moiety has been found to be an inhibitor of the P-glycoprotein, one of the best-studied multidrug efflux pumps. Twelve 5-oxyisoquinoline derivatives, which are analogues of zosuquidar wherein the dibenzosuberyl-piperazine moiety is replaced by either a diarylaminopiperidine or a piperidone-derived acetal or thioacetal group, have been synthesized as pure enantiomers. Their inhibitory power has been evaluated for the bacterial multidrugresistance ABC transporter LmrCD and fungal Pdr5. Four of the newly synthesized compounds reduced the transport activity to a higher degree than zosuquidar, being up to fourfold more efficient than the lead compound in the case of LmrCD and about two times better for Pdr5.

Orally Bioavailable Competitive CCR5 Antagonists

The chemokine receptor CCR5 plays an important role in inflammatory and autoimmune disorders as well as in transplant rejection by affecting the trafficking of effector T cells and monocytes to diseased tissues. Antagonists of CCR5 are believed to be of potential therapeutic value for the disorders mentioned above and HIV infection. Here we report on the structure-activity relationship of a new series of highly potent and selective competitive CCR5 antagonists. While all compounds tested were inactive on rodent CCR5, this series includes compounds that cross-react with the cynomolgus monkey (cyno) receptor. One of these compounds, i.e., 26n, has good PK properties in cynos, and its overall favorable profile makes it a promising candidate for in vivo profiling in transplantation and other disease models.