54544-67-1Relevant articles and documents
INDAZOLAMIDE DERIVATIVES
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Page/Page column 18, (2010/10/19)
Novel indazole derivatives of the formula (I), in which R1-R3 have the meanings indicated in claim 1, are HSP90 inhibitors and can be used for the preparation of a medicament for the treatment of diseases in which the inhibition, regulation and/or modulation of HSP90 plays a role.
Design and synthesis of novel 2,3-dihydro-1H-isoindoles with high affinity and selectivity for the dopamine D3 receptor
Austin, Nigel E,Avenell, Kim Y,Boyfield, Izzy,Branch, Clive L,Hadley, Michael S,Jeffrey, Phillip,Johnson, Christopher N,Macdonald, Gregor J,Nash, David J,Riley, Graham J,Smith, Alexander B,Stemp, Geoffrey,Thewlis, Kevin M,Vong, Antonio K.K,Wood, Martyn D
, p. 685 - 688 (2007/10/03)
Starting from the tetrahydroisoquinoline SB-2770111, a novel series of 5-substituted-2,3-dihydro-1H-isoindoles has been designed. Subsequent optimisation resulted in identification of 19. which has high affinity for the dopamine D3 receptor (pKi 8.3) and ≥ 100-fold selectivity over other aminergic receptors. In rat studies 19 was brain penetrant with an excellent pharmacokinetic profile (oral bioavailability 77%. t1/2 5.2h).