263888-56-8Relevant articles and documents
NOVEL MORPHOLINYL AMINE COMPOUNDS FOR THE TREATMENT OF AUTOIMMUNE DISEASE
-
Paragraph 0204; 0205, (2020/03/26)
The present invention relates to compounds of formula (I), wherein R1, R2 and R3 are as described herein, and their pharmaceutically acceptable salt, enantiomer or diastereomer thereof, and compositions including the compounds and methods of using the compounds.
S1P RECEPTORS MODULATORS
-
Page/Page column 139, (2010/04/30)
The invention relates to novel compounds that have S1P receptor modulating activity and, preferably, apoptotic activity and/or anti proliferative activity against cancer cells and other cell types. Further, the invention relates to a pharmaceutical comprising at least one compound of the invention for the treatment of diseases and/or conditions caused by or associated with inappropriate S1P receptor modulating activity or expression, for example, cancer. A further aspect of the invention relates to the use of a pharmaceutical comprising at least one compound of the invention for the manufacture of a medicament for the treatment of diseases and/or conditions caused by or associated with inappropriate S1P receptor modulating activity or expression such as cancer.
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).