- Arylaminoethyl carbamates as a novel series of potent and selective cathepsin S inhibitors
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We report a novel series of noncovalent inhibitors of cathepsin S. The synthesis of the peptidomimetic scaffold is described and structure-activity relationships of P3, P1, and P1′ subunits are discussed. Lead optimization to a non-peptidic scaffold has r
- Tully, David C.,Liu, Hong,Chatterjee, Arnab K.,Alper, Phil B.,Williams, Jennifer A.,Roberts, Michael J.,Mutnick, Daniel,Woodmansee, David H.,Hollenbeck, Thomas,Gordon, Perry,Chang, Jonathan,Tuntland, Tove,Tumanut, Christine,Li, Jun,Harris, Jennifer L.,Karanewsky, Donald S.
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p. 5107 - 5111
(2007/10/03)
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- INDOLE, INDAZOLE, AND BENZAZOLE DERIVATIVE
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The compound of the formula (I): wherein W is a group of the following formula (VIII) binding to any possible position on the Q: Q is, together with W, a group of the formula: -C(M=C(R3A)-N(R3)-, etc.; R3A is H or optionally substituted lower alkyl; R4, R5, R6, and R7 are independently H or optionally substituted lower alkyl; R1 is optionally substituted lower alkyl, etc.; R2 is H, etc.; R3 is H, etc.; Ar is phenyl, etc., or a pharmaceutically acceptable salt thereof, where these compounds exhibiting β3-adrenoceptor-stimulating activity and being useful as a medicament for treatment of obesity, etc.
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Page/Page column 74
(2010/02/11)
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- COMPOUNDS AND COMPOSITIONS AS CATHEPSIN S INHIBITORS
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The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of Cathepsin S.
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Page/Page column 22-23
(2010/02/14)
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- Simple and efficient preparation of ketones from morpholine amides
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Morpholine-derived amides react with RMgX to give the corresponding ketones in good yield. The mild conditions required and low cost of starting materials make this method very appealing for large scale preparations.
- Martín,Romea,Tey,Urpí,Vilarrasa
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p. 1414 - 1416
(2007/10/03)
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- Nonpeptide Renin Inhibitors Employing a Novel 3-Aza(or oxa)-2,4-dialkyl Glutaric Acid Moiety as a P2/P3 Amide Bond Replacement
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A new series of renin inhibitors has been developed.The inhibitors feature a novel replacement for the P2/P3 dipeptide moiety normally associated with renin inhibitors.The dipeptide replacement was a (2S,4S)-3-aza(or oxa)-2,4-dialkylglutaric acid amide.Ex
- Baker, William R.,Fung, Anthony K. L.,Kleinert, Hollis D.,Stein, Herman H.,Plattner, Jacob J.,et al.
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p. 1722 - 1734
(2007/10/02)
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