5964-48-7Relevant academic research and scientific papers
Discovery of the first M5-selective and CNS penetrant negative allosteric modulator (NAM) of a muscarinic acetylcholine receptor: (S)-9b-(4-chlorophenyl)-1-(3,4-difluorobenzoyl)-2,3-dihydro-1 H -imidazo[2,1- a ]isoindol-5(9b H)-one (ML375)
Gentry, Patrick R.,Kokubo, Masaya,Bridges, Thomas M.,Kett, Nathan R.,Harp, Joel M.,Cho, Hyekyung P.,Smith, Emery,Chase, Peter,Hodder, Peter S.,Niswender, Colleen M.,Daniels, J. Scott,Conn, P. Jeffrey,Wood, Michael R.,Lindsley, Craig W.
, p. 9351 - 9355 (2013)
A functional high throughput screen and subsequent multidimensional, iterative parallel synthesis effort identified the first muscarinic acetylcholine receptor (mAChR) negative allosteric modulator (NAM) selective for the M5 subtype. ML375 is a
The discovery of 1,2,3,9b-tetrahydro-5H-imidazo[2,1-a]isoindol-5-ones as a new class of respiratory syncytial virus (RSV) fusion inhibitors. Part 1
Bond, Silas,Draffan, Alistair G.,Fenner, Jennifer E.,Lambert, John,Lim, Chin Yu,Lin, Bo,Luttick, Angela,Mitchell, Jeffrey P.,Morton, Craig J.,Nearn, Roland H.,Sanford, Vanessa,Stanislawski, Pauline C.,Tucker, Simon P.
, p. 969 - 975 (2015/02/19)
Respiratory syncytial virus (RSV) is a major cause of respiratory tract infections in infants, young children and adults. Compound 1a (9b-(4-chlorophenyl)-1-(4-fluorobenzoyl)-1,2,3,9b-tetrahydro-5H-imidazo[2,1-a]isoindol-5-one) was identified as an inhibitor of A and B strains of RSV targeting the fusion glycoprotein. SAR was developed by systematic exploration of the phenyl (R1) and benzoyl (R2) groups. Furthermore, introduction of a nitrogen at the 8-position of the tricyclic core resulted in active analogues with improved properties (aqueous solubility, protein binding and log D) and excellent rat pharmacokinetics (e.g., rat oral bioavailability of 89% for compound 17).
POLYCYCLIC AGENTS FOR THE TREATMENT OF RESPIRATORY SYNCYTIAL VIRUS INFECTIONS
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Page/Page column 41, (2010/02/12)
Compounds of formula (I), and their use as in the treatment of infections involving viruses of the Pneumovirinae sub-family (RSV) are disclosed. In the formula ring (A) may be phenyl, pyridyl etc., (B-C) may be CH2-CH2etc., (R1) may be phenyl and substituted forms thereof, (R2) may be assorted substituents.
Polycyclic amino derivatives of pyrrolidone and piperidone
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, (2008/06/13)
A series of compounds of the formula STR1 have been found to exhibit useful pharmacological properties, e.g. antiinflammatory and analgetic activity.
5H-imidazo[2,1-a]isoindol-5-one compounds
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, (2008/06/13)
A new class of chemical compounds whose members exert an appetite suppressant and mood elevating effect in man has been invented. This class is defined as being composed of those compounds having the 1-substituted-2,5-benzodiazocine structure, fully saturated in the nonbenzenoid portion, and whose nitrogens are tervalent. Members of this class are prepared by condensing an orthobenzoylbenzoic acid or ester thereof with an ethylenediamine and reducing with a metallic alkaline hydride the product thus obtained.
