1082373-80-5Relevant articles and documents
Aliphatic cycloalkyl derivatives Preparation method, pharmaceutical composition and application thereof
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Paragraph 0121-0124, (2020/12/14)
The invention discloses an aliphatic cycloalkyl derivative, a preparation method thereof, a pharmaceutical composition and an application thereof. The invention provides an aliphatic cycloalkyl derivative represented by a formula I or a pharmaceutically a
Overcoming hERG issues for brain-penetrating cathepsin S inhibitors: 2-Cyanopyrimidines. Part 2
Irie, Osamu,Kosaka, Takatoshi,Kishida, Masashi,Sakaki, Junichi,Masuya, Keiichi,Konishi, Kazuhide,Yokokawa, Fumiaki,Ehara, Takeru,Iwasaki, Atsuko,Iwaki, Yuki,Hitomi, Yuko,Toyao, Atsushi,Gunji, Hiroki,Teno, Naoki,Iwasaki, Genji,Hirao, Hajime,Kanazawa, Takanori,Tanabe, Keiko,Hiestand, Peter C.,Malcangio, Marzia,Fox, Alyson J.,Bevan, Stuart J.,Yaqoob, Mohammed,Culshaw, Andrew J.,Hart, Terance W.,Hallett, Allan
scheme or table, p. 5280 - 5284 (2009/05/07)
We describe here orally active and brain-penetrant cathepsin S selective inhibitors, which are virtually devoid of hERG K+ channel affinity, yet exhibit nanomolar potency against cathepsin S and over 100-fold selectivity to cathepsin L. The new
COMPOUNDS AND COMPOSITIONS USEFUL AS CATHEPSIN S INHIBITORS
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Page/Page column 49, (2008/06/13)
The present invention relates to the use of a 2-cyanopyrimidine compound of the formula (I), wherein R1, R2, R3 and X are as defined in the specification and in the claims, in free form or in salt form, and , where possible, in tautomeric form, as an inhibitor of the activity of cathepsin S.