Biological profile of L-745,870, a selective antagonist with high affinity for the dopamine D4 receptor

…, N Curtis, JJ Kulagowski, PD Leeson, M Ridgill… - … of Pharmacology and …, 1997 - ASPET
L-745,870,(3-{[4-(4-chlorophenyl)piperazin-1-yl]methyl}-1Hpyrollo[2,3-b] pyridine, was
identified as a selective dopamine D4 receptor antagonist with excellent oral bioavailability and …

3'-(Arylmethyl)-and 3'-(aryloxy)-3-phenyl-4-hydroxyquinolin-2 (1H)-ones: orally active antagonists of the glycine site on the NMDA receptor

…, IM Mawer, AM Moseley, MP Ridgill… - Journal of medicinal …, 1994 - ACS Publications
Antagonists of the JV-methyl-D-aspartate (NMDA) subtype of excitatory amino acid receptor
have demon-strated promising potential for the treatment of a variety of neurological and …

L-745,870, a subtype selective dopamine D4 receptor antagonist, does not exhibit a neuroleptic-like profile in rodent behavioral tests

…, PD Leeson, S Patel, CI Ragan, M Ridgill… - … of Pharmacology and …, 1997 - ASPET
This study examined the high-affinity, selective dopamine D 4 receptor antagonist, L-745,870
(3-{[4-(4-chlorophenyl)piperazin-1-yl]methyl}-1H-pyrrolo[2,3-b]pyridine) in rodent …

2-Aryl indole NK1 receptor antagonists: optimisation of the 2-aryl ring and the indole nitrogen substituent

…, GJ Hollingworth, MM Kurtz, MP Ridgill… - Bioorganic & medicinal …, 2001 - Elsevier
… Author links open overlay panel Kevin Dinnell a , Gary G Chicchi d , Madhumeeta J Dhar
c , Jason M Elliott a , Gregory J Hollingworth a , Marc M Kurtz d , Mark P Ridgill a , Wayne …

Amino acid bioisosteres: design of 2-quinolone derivatives as glycine-site N-methyl-D-aspartate receptor antagonists

…, JJ Kulagowski, IM Mawer, MP Ridgill… - Bioorganic & Medicinal …, 1993 - Elsevier
3-Substituted-2-quinoloners (6–8) have been identified as glycine-site N-methyl-D-aspartate
receptor antagonists. It is proposed that the α-phenyl lactam unit in the potent 4-hydroxy-3-…

Synthesis and SAR of 2-and 3-substituted 7-azaindoles as potential dopamine D4 ligands

…, JJ Kulagowski, PD Leeson, MP Ridgill… - Bioorganic & medicinal …, 1999 - Elsevier
7-azaindole compounds bearing a cyclic amine moiety linked by a one or two carbon chain
attached at the 2- or 3-position were synthesised and evaluated as potential dopamine D 4 …

Regioselective rapid analogue syntheses of 1-methyl-3, 5-diarylpyrazoles via palladium-catalysed coupling to 3 (5)-pyrazolyl nonaflates

S Bourrain, M Ridgill, I Collins - Synlett, 2004 - thieme-connect.com
Regioselective rapid analogue syntheses of 1-methyl-3, 5-diarylpyrazoles were developed,
based on Pd-catalysed couplings to 1-methyl-3 (5)-arylpyrazole nonaflates, which offered an …

4, 4-Disubstituted cyclohexylamine NK1 receptor antagonists II

…, GJ Hollingworth, MM Kurtz, MP Ridgill… - Bioorganic & medicinal …, 2002 - Elsevier
… Author links open overlay panel Laura C Cooper a , Emma J Carlson b , Jose L Castro a ,
Gary G Chicchi c , Kevin Dinnell a , Jerry Di Salvo c , Jason M Elliott a , Gregory J …

2-Aryl indole NK1 antagonists: optimisation of the amide substituent

…, JM Elliott, M Kurtz, D Morrison, MP Ridgill… - Bioorganic & medicinal …, 2001 - Elsevier
The in vivo properties of a series of 2-arylindole NK 1 antagonists have been improved, by
modification of the amide substituent. The 1-(2-methoxyphenyl)piperazine amide was …

4, 4-Disubstituted cyclohexylamine NK1 receptor antagonists I

…, K Dinnell, GJ Hollingworth, MP Ridgill… - Bioorganic & medicinal …, 2002 - Elsevier
A series of novel 4,4-disubstituted cyclohexylamine based NK 1 antagonists is described.
The effect of changes to the C 1 –C 4 relative stereochemistry on the cyclohexane ring and …