Title:
CATHEPSIN K INHIBITOR, AND PREPARATION METHOD THEREFOR AND USE THEREOF
Document Type and Number:
WIPO Patent Application WO/2023/138695
Kind Code:
A1
Abstract:
The present invention relates to a cathepsin K inhibitor having a structure as shown in formula (0) and/or formula (II), wherein cyanopyrimidine or a ketone serving as an electrophilic group is a key group to exert a good inhibition effect on cathepsin K. Further provided are a method for preparing the cathepsin K inhibitor and the use thereof. The provided cathepsin K inhibitor has a relatively high inhibition effect and selectivity, and is expected to be used for treating diseases including thyroid diseases, cardiovascular diseases, bone diseases and gingival diseases.
Inventors:
WANG JINXIN (CN)
ZHANG GUIMIN (CN)
WANG KE (CN)
YAO JINGCHUN (CN)
PAN LIHONG (CN)
ZHANG GUIMIN (CN)
WANG KE (CN)
YAO JINGCHUN (CN)
PAN LIHONG (CN)
Application Number:
PCT/CN2023/073612
Publication Date:
July 27, 2023
Filing Date:
January 28, 2023
Export Citation:
Assignee:
SHANDONG NEW TIME PHARMACEUTICAL CO LTD (CN)
International Classes:
C07D471/04; A61K31/341; A61K31/437; A61K31/506; A61P9/00; A61P19/10; A61P35/00; C07D247/02; C07D309/16
Foreign References:
| CN1678613A | 2005-10-05 | |||
| CN101687864A | 2010-03-31 | |||
| JPH05194418A | 1993-08-03 | |||
| CN106478564A | 2017-03-08 |
Other References:
DATABASE Registry CAS; 30 August 2016 (2016-08-30), ANONYMOUS : "4-Pyrimidinecarbonitrile, 2-[[(3-bromophenyl) methyl]methylamin o]- ", XP093080139, retrieved from STN Database accession no. 1982714-07-7
TENO, N. ; IRIE, O. ; MIYAKE, T. ; GOHDA, K. ; HORIUCHI, M. ; TADA, S. ; NONOMURA, K. ; KOMETANI, M. ; IWASAKI, G. ; BETSCHART, C.: "New chemotypes for cathepsin K inhibitors", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, ELSEVIER, AMSTERDAM NL, vol. 18, no. 8, 15 April 2008 (2008-04-15), Amsterdam NL , pages 2599 - 2603, XP022606355, ISSN: 0960-894X, DOI: 10.1016/j.bmcl.2008.03.036
MILTZ, WOLFGANG ET AL.: "Design and Synthesis of Potent and Orally Active GPR4 Antagonists with Modulatory Effects on Nociception, Inflammation, and Angiogenesis", BIOORGANIC & MEDICINAL CHEMISTRY, vol. 25, no. 16, 29 June 2017 (2017-06-29), XP085133595, DOI: 10.1016/j.bmc.2017.06.050
TENO, N. ; IRIE, O. ; MIYAKE, T. ; GOHDA, K. ; HORIUCHI, M. ; TADA, S. ; NONOMURA, K. ; KOMETANI, M. ; IWASAKI, G. ; BETSCHART, C.: "New chemotypes for cathepsin K inhibitors", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, ELSEVIER, AMSTERDAM NL, vol. 18, no. 8, 15 April 2008 (2008-04-15), Amsterdam NL , pages 2599 - 2603, XP022606355, ISSN: 0960-894X, DOI: 10.1016/j.bmcl.2008.03.036
MILTZ, WOLFGANG ET AL.: "Design and Synthesis of Potent and Orally Active GPR4 Antagonists with Modulatory Effects on Nociception, Inflammation, and Angiogenesis", BIOORGANIC & MEDICINAL CHEMISTRY, vol. 25, no. 16, 29 June 2017 (2017-06-29), XP085133595, DOI: 10.1016/j.bmc.2017.06.050
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