105211-75-4Relevant academic research and scientific papers
BICYCLIC COMPOUNDS USEFUL AS CATHEPSIN S INBHIBITORS
-
Page/Page column 39, (2010/11/29)
Compounds of formula (I), wherein R1, R2, R3, Ra and E are are defined within, and pharmaceutically acceptable salts, solvates, hydrates and N-oxides thereof having utility in the treatment of disorders mediated by cathepsin S.
CATHEPSIN S INHIBITORS
-
Page/Page column 94, (2010/11/08)
Compounds of the formula (I) where R1 is C1-C4 straight or branched alkyl, optionally substituted with up to three substituents selected from halo and hydroxy; R2 is halo, hydroxy, methyloxy, or C1-C2 alkyl, which alkyl is optionally substituted with up to three halogens or an hydroxy or a methyloxy; D is - C3-C7 alkylene-, thereby defining a cycloalkyl ring; E is -C(=O)-, -S(=O)m-, -NRdS(=O)m-, -NRaC(=O)-, -OC(=O)-, R3 is an optionally substituted carbocyclic or heterocyclic ring R10 is H, ORc, SRc or together with the gem H is =O or (ORc)2; Ra is independently selected from H, C1-C4 alkyl; have utility in the inhibition of cathepsin S and are thus useful pharmaceuticals against disorders such as autoimmune disorders and chronic pain.
Novel 8-substituted dipyridodiazepinone inhibitors with a broad-spectrum of activity against HIV-1 strains resistant to non-nucleoside reverse transcriptase inhibitors
O'Meara, Jeff A.,Yoakim, Christiane,Bonneau, Pierre R.,B?s, Michael,Cordingley, Michael G.,Déziel, Robert,Doyon, Louise,Duan, Jianmin,Garneau, Michel,Guse, Ingrid,Landry, Serge,Malenfant, Eric,Naud, Julie,Ogilvie, William W.,Thavonekham, Bounkham,Simoneau, Bruno
, p. 5580 - 5588 (2007/10/03)
A series of novel 8-substituted dipyridodiazepinone-based inhibitors were investigated for their antiviral activity against wild type human immunodeficiency virus (HIV-1) and the clinically prevalent K103N/Y181C mutant virus. Our efforts have resulted in a series of benzoic acid analogues that are potent inhibitors of HIV-1 replication against a panel of HIV-1 strains resistant to non-nucleoside reverse transcriptase inhibitors (NNRTIs). Furthermore, the combination of good antiviral potency, a broad spectrum of activity, and an excellent pharmacokinetic profile provides strong justification for the further development of compound 7 as a potential treatment for wild type and NNRT1-resistant HIV-1 infection.
Quinclidine derivatives as squalene synthase inhibitors
-
, (2008/06/13)
Quinuclidine derivatives of formula, and their pharmaceutically acceptable salts, in which: R1 is hydrogen or hydroxy; R2 is hydrogen; pr R1 and R2 are joined together so that CR1 -CR2 is a
