157837-04-2Relevant articles and documents
1,4-Benzodiazepines as inhibitors of respiratory syncytial virus
Carter, Malcolm C.,Alber, Dagmar G.,Baxter, Robert C.,Bithell, Sian K.,Budworth, Jo,Chubb, Ann,Cockerill, G. Stuart,Dowdell, Verity C. L.,Henderson, Elisa A.,Keegan, Sally J.,Kelsey, Richard D.,Lockyer, Michael J.,Stables, Jeremy N.,Wilson, Lara J.,Powell, Kenneth L.
, p. 2311 - 2319 (2007/10/03)
Respiratory syncytial virus (RSV) is the cause of one-fifth of all lower respiratory tract infections worldwide and is increasingly being recognized as a serious threat to patient groups with poorly functioning immune systems. Our approach to finding a novel inhibitor of this virus was to screen a 20 000-member diverse library in a whole cell XTT assay. Parallel assays were carried out in the absence of virus in order to quantify any associated cell toxicity. This identified 100 compounds with IC50's less than 50 μM. A-33903 (18), a 1,4-benzodiazepine analogue, was chosen as the starting point for lead optimization. This molecule was moderately active and demonstrated good pharmacokinetic properties. The most potent compounds identified from this work were A-58568 (47), A-58569 (44), and A-62066 (46), where modifications to the aromatic substitution enhanced potency, and A-58175 (42), where the amide linker was modified.
METHOD OF INDUCING CHOLECYSTOKININ AGONIST ACTIVITY USING 1,4-BENZODIAZEPINE COMPOUNDS
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, (2008/06/13)
A method of inducing a Cholescystokinin-A receptor agonist response in a mammal by administering a compound of formula (I), STR1 where R 1 is C 1-C 6 alkyl, C 3-6 cycloalkyl, phenyl, or substituted phenyl; R 2 is C 3-6 alkyl, C 3-6 cycloalkyl, C 3-6 alkenyl, benzyl, phenylC 1-3 alkyl or substituted phenyl; or NR 1 R 2 together form 1,2,3,4-tetrahydroquinoline or benzazepine mono-, di-, or trisubstituted independently with C 1-6 alkyl, C 1-6 alkoxy or halogen substituents; n is an integer selected from the grouping consisting of 0, 1,2 or 3; p is the integer 0 or 1; q is the integer 0 or 1; r is the integer 0 or 1, provided that when q is 0 then r is 0; R 3, R 4, R 5 and R 8 are selected from a variety of substituents; X is nitrogen, nitroso or R 8 ; m is an integer selected from the group consisting of 0, 1, 2 or 3; Y and Z are hydrogen or halogen, novel intermediates, a pharmaceutical composition for treating obesity, gall bladder stasis, disorders of pancreatic secretion, methods for such treatment and processes for preparing compounds of formula (I).
Benzodiazepine derivatives, compositions containing them and their use in therapy
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, (2008/06/13)
Compounds of formula (I), and salts and prodrugs thereof STR1 wherein: R 1 is H, certain optionally substituted C 1.6 alkyl, or C 3-7 cycloalkyl;R 2 is (CH 2) q -tetrazolyl optionally substituted in the tetrazole ring by C 1-4 alkyl, (CH 2) q -imidazolyl