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Aliphatic cyclic amino acids are fundamental building blocks of modern medicinal chemistry. The combination of readily functionalized amine and carboxyl groups attached to a chiral central core along with one or two potentially diverse side chains provides a unique three-dimensional structure with a high degree of functionality. This makes them invaluable as starting materials for syntheses of complex molecules, highly diverse elements for SAR campaigns, integral components of peptidomimetic drugs, and potential drugs on their own”. (Reference: Mark A. T. Blaskovich J. Med. Chem. 2016, 59, 10807−10836)
For example, the following 6 drugs which are under active clinical development or marketed, consist of different units of aliphatic cyclic amino acids.
ARN-509 / Phase III
AR Antagonist
Asunaprevir / Launched – 2014
HCV NS3 NS4A Protease Inhibitors
AZD-5363 / Phase II
PKB Inhibitors
ONC1-13B / IND Filed
Androgen Receptor Antagonists
Ibodutant / Phase III
Tachykinin NK2 Antagonists
CR-845 / Phase II
kappa-Opioid Agonists

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China & India
Business Development Team
Tel: +86-400 025 5188
Fax: +86-25 8691 8232
E-mail: sales_china@pharmablock.com

US & Europe
Dr. Shuhai Zhao
Tel: +1-408 735 7571 / 408 921 9969
Fax: +1-408 550 1891
E-mail: salesusa@pharmablock.com

Other Countries
Michelle Gong / Qingling Hu
Tel: +86-25 8691 8086 / 8691 8288
Fax: +86-25 8691 8232
E-mail: sales@pharmablock.com

 
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