88965-67-7Relevant academic research and scientific papers
(1 R,2 R)-N-(1-cyanocyclopropyl)-2-(6-methoxy-1,3,4,5-tetrahydropyrido[4,3- b]indole-2-carbonyl)cyclohexanecarboxamide (AZD4996): A potent and highly selective cathepsin k inhibitor for the treatment of osteoarthritis
Dossetter, Alexander G.,Beeley, Howard,Bowyer, Jonathan,Cook, Calum R.,Crawford, James J.,Finlayson, Jonathan E.,Heron, Nicola M.,Heyes, Christine,Highton, Adrian J.,Hudson, Julian A.,Jestel, Anja,Kenny, Peter W.,Krapp, Stephan,Martin, Scott,MacFaul, Philip A.,McGuire, Thomas M.,Gutierrez, Pablo Morentin,Morley, Andrew D.,Morris, Jeffrey J.,Page, Ken M.,Ribeiro, Lyn Rosenbrier,Sawney, Helen,Steinbacher, Stefan,Smith, Caroline,Vickers, Madeleine
, p. 6363 - 6374 (2012)
Directed screening of nitrile compounds revealed 3 as a highly potent cathepsin K inhibitor but with cathepsin S activity and very poor stability to microsomes. Synthesis of compounds with reduced molecular complexity, such as 7, revealed key SAR and demonstrated that baseline physical properties and in vitro stability were in fact excellent for this series. The tricycle carboline P3 unit was discovered by hypothesis-based design using existing structural information. Optimization using small substituents, knowledge from matched molecular pairs, and control of lipophilicity yielded compounds very close to the desired profile, of which 34 (AZD4996) was selected on the basis of pharmacokinetic profile.
PYRAZOLE DERIVATIVES AS MALT1 INHIBITORS
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Paragraph 1231-1233, (2020/01/04)
Disclosed are compounds, compositions and methods for treating of diseases, syndromes, conditions, and disorders that are affected by the modulation of MALT 1. Such compounds are represented by Formula (I) as follows: wherein R1, R2, R3, R4, R5, and G, are defined herein.
Novel Compound - 827
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Page/Page column 20, (2009/01/23)
The present invention relates to compounds and compositions for treating diseases associated with cysteine protease activity. The compounds are reversible inhibitors of cysteine proteases, including cathepsins B, K, C, F, H, L, O, S, W and X. Of particular interest are diseases associated with Cathepsin K.
Prostaglandin D2 receptor antagonists
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, (2008/06/13)
Certain tetrahydrocarbazole-1-acetic acid derivatives are potent and selective antagonists of the prostaglandin D2 receptor, and are therefore useful in the treatment of allergic conditions such as allergic rhinitis.
Method and compositions for the treatment of allergic conditions using PGD2 receptor antagonists
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, (2008/06/13)
Prostaglandin D2 receptor antagonists in conjunction with an antihistamine and/or a leukotriene antagonist are useful in the treatment of allergic conditions.
