717878-06-3Relevant articles and documents
NOVEL COMPOUNDS
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Page/Page column 133-134, (2016/04/20)
The present invention relates to novel compounds and methods for the manufacture of inhibitors of deubiquitylating enzymes (DUBs). In particular, the invention relates to the inhibition of ubiquitin C-terminal hydrolase L1 (UCHL1). The invention further relates to the use of DUB inhibitors in the treatment of cancer and other indications. Compounds of the invention include compounds having the formula (I) or a pharmaceutically acceptable salt thereof, wherein R1 to R8 are as defined herein.
Novel orally active NPY Y5 receptor antagonists: Synthesis and structure-activity relationship of spiroindoline class compounds
Sakamoto, Toshihiro,Moriya, Minoru,Tsuge, Hiroyasu,Takahashi, Toshiyuki,Haga, Yuji,Nonoshita, Katsumasa,Okamoto, Osamu,Takahashi, Hirobumi,Sakuraba, Aya,Hirohashi, Tomoko,Shibata, Takunobu,Kanno, Tetsuya,Ito, Junko,Iwaasa, Hisashi,Gomori, Akira,Ishihara, Akane,Fukuroda, Takahiro,Kanatani, Akio,Fukami, Takehiro
experimental part, p. 5015 - 5026 (2009/12/04)
Spiroindoline urea derivatives, designed to act as NPY Y5 receptor antagonists, were synthesized and their structure-activity relationships were investigated. Of these derivatives, compound 3a showed good Y5 binding affinity with favorable pharmacokinetic