- 2-AZABICYCLO[3.1.1] DERIVATIVES AS ANTAGONISTS OF THE OREXIN-1 AND OREXIN-2 RECEPTORS
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There is provided a compound of formula I, wherein L1, R1, R2, R5, X, A and B have meanings given in the description, and pharmaceutically acceptable salts, solvates and prodrugs thereof, which compounds are useful as antagonists of the orexin-1 and orexin-2 receptors or as selective antagonists of the orexin-1 receptor, and thus, in particular, in the treatment or prevention of inter alia substance dependence, addiction, anxiety disorders, panic disorders, binge eating, compulsive disorders, impulse control disorders, cognitive impairment and Alzheimer's disease.
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Page/Page column 80; 81
(2019/05/15)
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- ISOQUINOLINES AS INHIBITORS OF HPK1
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Isoquinoline compounds and their use as inhibitors of HPK1 (hematopoietic kinase 1) are described. The compounds are useful in treating HPK1-dependent disorders and enhancing an immune response. Also described are methods of inhibitng HPK1, methods of treating HPK1-dependent disorders, methods for enhancing an immune response, and methods for preparing the isoquinoline compounds.
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Paragraph 1042; 1043
(2018/10/21)
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- 1,3-Dipropyl-8-(1-phenylacetamide-1H-pyrazol-3-yl)-xanthine derivatives as highly potent and selective human A2B adenosine receptor antagonists
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A new series of 1,3-dipropyl-8-(1-phenylacetamide-1H-pyrazol-3-yl)-xanthine derivatives has been identified as potent A2B adenosine receptor antagonists. The products have been evaluated for their binding affinities for the human A2B, A1, A2A, and A3 adenosine receptors. N-(4-chloro-phenyl)-2-[3-(2,6-dioxo-1,3-dipropyl-2,3,6,7-tetrahydro-1H-purin-8-yl)-5-methyl-pyrazol-1-yl] (11c) showed a high affinity for the human A2B adenosine receptor Ki = 7 nM and good selectivity (A1, A2A, A3/A2B > 140). Synthesis and SAR of this novel class of compounds is presented herein.
- Tabrizi, Mojgan Aghazadeh,Baraldi, Pier Giovanni,Preti, Delia,Romagnoli, Romeo,Saponaro, Giulia,Baraldi, Stefania,Moorman, Allan R.,Zaid, Abdel Naser,Varani, Katia,Borea, Pier Andrea
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p. 2419 - 2430
(2008/09/21)
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