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Page 1
Selective non zinc binding inhibitors of MMP13.
De Savi C, Morley AD, Ting A, Nash I, Karabelas K, Wood CM, James M, Norris SJ, Karoutchi G, Rankine N, Hamlin G, Macfaul PA, Ryan D, Baker SV, Hargreaves D, Gerhardt S. De Savi C, et al. Among authors: gerhardt s. Bioorg Med Chem Lett. 2011 Jul 15;21(14):4215-9. doi: 10.1016/j.bmcl.2011.05.075. Epub 2011 May 27. Bioorg Med Chem Lett. 2011. PMID: 21669521
Dipeptidyl nitrile inhibitors of Cathepsin L.
Asaad N, Bethel PA, Coulson MD, Dawson JE, Ford SJ, Gerhardt S, Grist M, Hamlin GA, James MJ, Jones EV, Karoutchi GI, Kenny PW, Morley AD, Oldham K, Rankine N, Ryan D, Wells SL, Wood L, Augustin M, Krapp S, Simader H, Steinbacher S. Asaad N, et al. Among authors: gerhardt s. Bioorg Med Chem Lett. 2009 Aug 1;19(15):4280-3. doi: 10.1016/j.bmcl.2009.05.071. Epub 2009 May 27. Bioorg Med Chem Lett. 2009. PMID: 19515558
Design of selective Cathepsin inhibitors.
Bethel PA, Gerhardt S, Jones EV, Kenny PW, Karoutchi GI, Morley AD, Oldham K, Rankine N, Augustin M, Krapp S, Simader H, Steinbacher S. Bethel PA, et al. Among authors: gerhardt s. Bioorg Med Chem Lett. 2009 Aug 15;19(16):4622-5. doi: 10.1016/j.bmcl.2009.06.090. Epub 2009 Jun 27. Bioorg Med Chem Lett. 2009. PMID: 19616430
The discovery of N-cyclopropyl-4-methyl-3-[6-(4-methylpiperazin-1-yl)-4-oxoquinazolin-3(4H)-yl]benzamide (AZD6703), a clinical p38α MAP kinase inhibitor for the treatment of inflammatory diseases.
Brown DS, Cumming JG, Bethel P, Finlayson J, Gerhardt S, Nash I, Pauptit RA, Pike KG, Reid A, Snelson W, Swallow S, Thompson C. Brown DS, et al. Among authors: gerhardt s. Bioorg Med Chem Lett. 2012 Jun 15;22(12):3879-83. doi: 10.1016/j.bmcl.2012.04.116. Epub 2012 May 2. Bioorg Med Chem Lett. 2012. PMID: 22608965
Discovery of a potent, selective, and orally bioavailable acidic 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor: discovery of 2-[(3S)-1-[5-(cyclohexylcarbamoyl)-6-propylsulfanylpyridin-2-yl]-3-piperidyl]acetic acid (AZD4017).
Scott JS, Bowker SS, Deschoolmeester J, Gerhardt S, Hargreaves D, Kilgour E, Lloyd A, Mayers RM, McCoull W, Newcombe NJ, Ogg D, Packer MJ, Rees A, Revill J, Schofield P, Selmi N, Swales JG, Whittamore PR. Scott JS, et al. Among authors: gerhardt s. J Med Chem. 2012 Jun 28;55(12):5951-64. doi: 10.1021/jm300592r. Epub 2012 Jun 19. J Med Chem. 2012. PMID: 22691057
Novel acidic 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor with reduced acyl glucuronide liability: the discovery of 4-[4-(2-adamantylcarbamoyl)-5-tert-butyl-pyrazol-1-yl]benzoic acid (AZD8329).
Scott JS, deSchoolmeester J, Kilgour E, Mayers RM, Packer MJ, Hargreaves D, Gerhardt S, Ogg DJ, Rees A, Selmi N, Stocker A, Swales JG, Whittamore PR. Scott JS, et al. Among authors: gerhardt s. J Med Chem. 2012 Nov 26;55(22):10136-47. doi: 10.1021/jm301252n. Epub 2012 Nov 7. J Med Chem. 2012. PMID: 23088558
164 results