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Novel scaffold for cathepsin K inhibitors |
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| Authors: | Teno Naoki Miyake Takahiro Ehara Takeru Irie Osamu Sakaki Junichi Ohmori Osamu Gunji Hiroki Matsuura Naoko Masuya Keiichi Hitomi Yuko Nonomura Kazuhiko Horiuchi Miyuki Gohda Keigo Iwasaki Atsuko Umemura Ichiro Tada Sachiyo Kometani Motohiko Iwasaki Genji Cowan-Jacob Sandra W Missbach Martin Lattmann René Betschart Claudia |
| Affiliation: | Novartis Institutes for BioMedical Research, Ohkubo 8, Tsukuba, Ibaraki, Japan. naoki.teno@novartis.com |
| Abstract: | Pyrrolopyrimidine, a novel scaffold, allows to adjust interactions within the S3 subsite of cathepsin K. The core intermediate 10 facilitated the P3 optimization and identified highly potent and selective cathepsin K inhibitors 11-20. |
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