509150-43-0Relevant articles and documents
HETEROARYLAMINOISOQUINOLINES, METHODS FOR THEIR PREPARATION AND THERAPEUTIC USES THEREOF
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Page/Page column 115; 116, (2016/08/23)
The application is directed to compounds of formula (IA) : and specifically compounds of formula (I) and their salts and solvates, wherein R1, R11, R12, R13, R4, R5, n, A1, A2, and A3 are as set forth in the specification, as well as to a method for their preparation, pharmaceutical compositions comprising the same, and use thereof for the treatment and/or prevention of conditions associated with the alteration of the activity of β-galactosidase, specially galactosidase beta-1 or GLB1, including GM1 gangliosidoses and Morquio syndrome, type B.
Lead optimization of the VU0486321 series of mGlu1 PAMs. Part 1: SAR of modifications to the central aryl core
Garcia-Barrantes, Pedro M.,Cho, Hyekyung P.,Blobaum, Anna L.,Niswender, Colleen M.,Conn, P. Jeffrey,Lindsley, Craig W.
, p. 5107 - 5110 (2015/11/09)
This Letter describes the lead optimization of the VU0486321 series of mGlu1 positive allosteric modulators (PAMs). While first generation PAMs from Roche were reported in the late 1990s, little effort has focused on the development of mGlu1 PAMs since. New genetic data linking loss-of-function mutant mGlu1 receptors to schizophrenia, bipolar disorder and other neuropsychiatric disorders has rekindled interest in the target, but the ideal in vivo probe, for example, with good PK, brain penetration and low plasma protein binding, for robust target validation has been lacking. Here we describe the first modifications to the central aryl core of the VU0486321 series, where robust SAR was noted. Moreover, structural variants were identified that imparted selectivity (up to >793-fold) versus mGlu4.
USE OF SUBSTITUTED 2,5-DIAMIDOINDOLES FOR THE TREATMENT OF UROLOGICAL DISEASES
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Page 74, (2010/02/07)
The present invention relates to the use of 2,5-diamidoindole derivatives for the preparation of medicaments for treating urological disorders in humans and/or animals.RCK 41-Foreign Countries