478833-49-7

Upstream product

• 217645-80-2 5-chloro-2-{2-[4-(4-fluoro-benzyl)-(2R,5S)-2,5-dimethyl-piperazin-1-yl]-2-oxo-ethoxy}-benzaldehyde 
• 352-11-4 1-chloromethyl-4-fluorobenzene 
• 217648-11-8 2-chloro-1-[4-(4-fluoro-benzyl)-(2R,5S)-2,5-dimethyl-piperazin-1-yl]-ethanone 
• 2815-34-1 2,5-dimethyl-piperazine 
• 364066-92-2 (2S,5R)-1-(4-fluorobenzyl)-2,5-dimethylpiperazine 
• 5330-38-1 4-chloro-2-hydroxymethylphenol 

Downstream Products

• 478833-52-2 1-((2R,5S)-4-(4-fluorobenzyl)-2,5-dimethylpiperazin-1-yl)-2-(4-chloro-2-(chloromethyl)phenoxy)ethanone 
• 519171-98-3 (2-Methylbenzenesulfonyl)-carbamic acid 5-chloro-2-{2-[4-(4-fluoro-benzyl)-(2R,5S)-2,5-dimethyl-piperazin-1-yl]-2-oxo-ethoxy}-benzyl ester 
• 478833-25-9 (2-(2-((2R,5S)-4-(4-fluorobenzyl)-2,5-dimethylpiperazin-1-yl)-2-oxoethoxy)-5-chlorophenyl)methanesulfonic acid 
• 813446-39-8 (2-(2-((2R,5S)-4-(4-fluorobenzyl)-2,5-dimethylpiperazin-1-yl)-2-oxoethoxy)-5-chlorophenyl)methanesulfonic acid L-arginine cocrystal 

Relevant academic research and scientific papers

Route development and bulk synthesis of CP-865,569

The synthesis of zwitterionic CP-865,569 by three different synthetic routes is described. The first two routes differ in the method of introducing the sulfonic acid at the penultimate step: by sulfite displacement of a benzylic chloride and by oxidation of a benzylic thioacetate. The third route is a convergent route to the drug candidate. The synthesis strategy was primarily driven by the need to introduce the sulfonic acid functionality at the final stage of the synthesis due to the high water solubility and low organic solubility of the desired product.

Piperazinyl CCR1 antagonists-optimization of human liver microsome stability

The synthesis, biological activity, and pharmacokinetic profile of CCR1 antagonists are described.

AMORPHOUS UND CRYSTAL FORMS OF (5-CHLORO-2-{2-

This invention relates to amorphous and crystal salt forms of (5-chloro-2-{2-[4-(4-fluoro--benzyl)-(2R,5S)-2,5-dimethyl-piperazin-1-yl]-2-oxo-ethoxy)-phenyl)-methanesulfonic acid, useful in treating or preventing a disorder or condition by antagonizing th

Methods of using piperazine derivatives

The present invention relates to compounds of the formula I and the pharmaceutically acceptable forms thereof; wherein X, Y, a, b, c, d, R1, R2, R3, R4 and R5 are as defined herein. Moreover, the present invention is also directed at pharmaceutical compositions comprising a compound of the formula I and a pharmaceutically acceptable carrier. Furthermore, the present invention is directed at methods of using the herein described compounds and compositions for treating or preventing a disorder or condition that can be treated or prevented by antagonizing the CCR1 receptor in a mammal.

Novel phosphorus-containing derivatives

A compound of the Formula I a prodrug thereof, or the pharmaceutically acceptable salt of the compound or prodrug; wherein X, Y, a, b, c, d, R1, R2, R3, R4, R5, R6 and R7 are as defined above and are useful to treat inflammation and other immune disorders. The present invention also relates to pharmaceutical compositions that include compounds of Formula I and a pharmaceutically acceptable carrier. Moreover, the present invention relates to methods of using the above-described compounds and compositions to treat and prevent diseases and conditions.

Novel sulfonic acid derivatives

A compound of the formula or the pharmaceutically acceptable salt thereof; wherein X, Y, a, b, c, d, R1, R2, R3 and R5 are as defined above useful to treat inflammation and other immune disorders.

Piperazine derivatives and their use as anti-inflammatory agents

This invention is directed to acyl piperazine derivatives which are useful as anti-inflammatory agents. This invention is also directed to pharmaceutical compositions containing the compounds of the invention, and methods of using the compounds to treat inflammatory disorders in humans.