402958-32-1Relevant academic research and scientific papers
A METHOD FOR THE PREPARATION OF 3-AMINO-N-CYCLOPROPYL-2-HYDROXYL-HEXANAMIDE
-
Page/Page column 24, (2014/01/08)
The present invention discloses a method for preparing 3-amino-N-cyclopropyl-2-hydroxyl-hexanamide. The invention relates to the technical field of the preparation of pharmaceutical intermediates. The method uses trans-2-hexenoic acid as the starting material, through the steps of epoxidation, ring-opening by nitrile, amidation, etc., to obtain the final product 3-amino-N-cyclopropyl-2-hydroxyl-hexanamide. The method uses easily-obtainable materials, requires mild reactive conditions, and adopts stable processes. Therefore it is suitable for large scale industrial production.
CATHEPSIN INHIBITORS FOR THE TREATMENT OF BONE CANCER AND BONE CANCER PAIN
-
, (2012/11/13)
The present invention is directed to methods of using compounds that are inhibitors of cysteine proteases, in particular, of both cathepsins S and K and optionally further cathepsins B and/or L in treating bone cancer. The present invention is directed to pharmaceutical compositions comprising these compounds for treating bone cancer and bone cancer pain, especially the pain associated with metastasis. A single compound can be used to ameliorate the pain, the injury to bone, while also reducing tumor growth, the risk of metastasis and/or invasiveness of the cancer.
TERTIARY AMINE SUBSTITUTED PEPTIDES USEFUL AS INHIBITORS OF HCV REPLICATION
-
Page/Page column 17, (2010/12/18)
The present invention provides tertiary amine substituted peptides of Formula (I) useful as inhibitors of HCV replication. The variables R and R1-R12 in Formula I are described herein. The invention also includes methods for preparing such compounds. The present invention further includes pharmaceutical compositions containing tertiary amine substituted peptides and methods for using such compounds, including methods for using the compounds to treat hepatitis C infection.
HCV PROTEASE INHIBITORS
-
Page/Page column 18, (2008/12/04)
This invention relates to the compounds of formula (I) shown below. Each variable in formula (I) is defined in the specification. These compounds can be used to treat hepatitis C virus infection.
Discovery of a novel bicycloproline P2 bearing peptidyl α-ketoamide LY514962 as HCV protease inhibitor
Yip, Yvonne,Victor, Frantz,Lamar, Jason,Johnson, Robert,Wang, Q. May,Barket, Donna,Glass, John,Jin, Ling,Liu, Lifei,Venable, Daryl,Wakulchik, Mark,Xie, Congping,Heinz, Beverly,Villarreal, Elcira,Colacino, Joe,Yumibe, Nathan,Tebbe, Mark,Munroe, John,Chen, Shu-Hui
, p. 251 - 256 (2007/10/03)
We describe herein the design, syntheses and evaluation of a number of bicycloproline P2 bearing HCV protease inhibitors endowed with impressive enzyme potency, enzyme selectivity, cellular activity and favorable ADME profiles.
P1 and P3 optimization of novel bicycloproline P2 bearing tetrapeptidyl α-ketoamide based HCV protease inhibitors
Victor, Frantz,Lamar, Jason,Snyder, Nancy,Yip, Yvonne,Guo, Deqi,Yumibe, Nathan,Johnson, Robert B.,Wang, Q. May,Glass, John I.,Chen, Shu-Hui
, p. 257 - 261 (2007/10/03)
With the aim of discovering potent and selective HCV protease inhibitors, we synthesized and evaluated a series of 1a based tetrapeptidyl ketoamides with additional modification(s) at P1′, P1, and P3 positions. As a result of this effort, we found that re
