168077-29-0Relevant articles and documents
NOVEL BENZAMIDINE COMPOUND
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Page/Page column 32-33, (2008/06/13)
A novel compound, or a pharmaceutically acceptable salt thereof, represented by the formula (1) wherein the characters are as defined in the description. Thus, there can be provided an activated blood coagulation factor X inhibitor and a novel anti(blood)
Use of oxido-squalene cyclase inhibitors to lower blood cholesterol
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, (2008/06/13)
PCT No. PCT/GB96/01985 Sec. 371 Date Feb. 13, 1998 Sec. 102(e) Date Feb. 13, 1998 PCT Filed Aug. 14, 1996 PCT Pub. No. WO97/06802 PCT Pub. Date Feb. 27, 1997A compound of formula (I), or a pharmaceutically acceptable salt thereof, wherein G, T1, T2 and T3 are selected from CH and N; provided that T2 and T3 are not both CH; A is selected from a direct bond and (1-4C)alkylene; X is selected from oxy, thio, sulphinyl, sulphonyl, carbonyl, carbonylamino, N-di-(1-6C)alkylcarbonylamino, sulphonamido, methylene, (1-4C)alkylmethylene and di-(1-6C)alkylmethylene, and when T2 is CH, X may also be selected from aminosulphonyl and oxycarbonyl; and Q is selected from (5-7C)cycloalkyl, a heterocyclic moiety containing up to 4 heteroatoms selected from nitrogen, oxygen and sulphur, phenyl, naphthyl, phenyl(1-4C)alkyl and phenyl(2-6C)alkenyl; for the manufacture of a medicament for treating diseases or medical conditions in which an inhibition of oxido-squalene cyclase is desirable.
A novel series of 4-piperidinopyridine and 4-piperidinopyrimidine inhibitors of 2,3-oxidosqualene cyclase-lanosterol synthase
Brown,Hollinshead,Stokes,Waterson,Clarke,Foubister,Glossop,McTaggart,Mirrlees,Smith,Wood
, p. 4964 - 4972 (2007/10/03)
A novel series of 4-piperidinopyridines and 4-piperidinopyrimidines showed potent and selective inhibition of rat 2,3-oxidosqualene cyclase-lanosterol synthase (OSC) (e.g. 26 IC50 rat = 398 ± 25 nM, human = 112 ± 25 nM) and gave selective oral inhibition of rat cholesterol biosynthesis (26 ED80 = 1.2 ± 0.3 mg/kg, n = 5; HMGCoA reductase inhibitor simvastatin ED80 = 1.2 ± 0.3 mg/kg, n = 5). The piperidinopyrimidine OSC inhibitors have a significantly lower pKa than the corresponding pyridine or the previously reported quinuclidine OSC inhibitor series. This indicates that other novel OSC inhibitors may be found in analogues of this series across a broader pKa range (6.0-9.0). These series may yield novel hypocholesterolemic agents for the treatment of cardiovascular disease.