- Tetrahydroquinoline analogues as muscarinic agonists
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The present invention relates to tetrahydroquinoline compounds as muscarinic receptor agonists; compositions comprising the same; methods of inhibiting an activity of a muscarinic receptor with said compounds; methods of treating a disease condition associated with a muscarinic receptor using said compounds; and methods for identifying a subject suitable for treatment using said compounds.
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Page/Page column 32
(2017/01/05)
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- FUSED IMIDAZOLE AND PYRAZOLE DERIVATIVES AS MODULATORS OF TNF ACTIVITY
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A series of substituted benzimidazole, imidazo[1,2-a]pyridine and pyrazolo[1,5-a]pyridine derivatives, and analogues thereof, being potent modulators of human TNFα activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders.
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Page/Page column 105; 106; 107
(2015/06/25)
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- COMPOUNDS
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A compound of formula (I) or a pharmaceutically acceptable salt or prodrug thereof wherein X is N or CH; Q is NR6 or O; A1 and A2 are independently hydrogen or C1-6 alkyl or may together form a carbonyl group; R1 and R2 are independently hydrogen, halogen, CF3, CN, OR7, OR8, NR8R9, NR8COR10, NR8S02R10, S02NR8R9, SO2R10 or C1-6 alkyl optionally and independently substituted by one or more of hydroxyl, C1-6 alkoxy, halogen or NR8 R9; R 3 is hydrogen, halogen, CF3 or OR 7; R4 is hydrogen, halogen, CF3, OR8, NR8R9, NR8COR10, NR8S02R10 or C1-6 alkyl optionally substituted by hydroxyl, C1-6 alkoxy or NR 8 R 9; or when R3 and R4 are positioned ortho and taken together form -0(CH2)mO-, where m is 1-3; R5 is hydrogen or C1-6 alkyl optionally substituted by hydroxyl, C1-6 alkoxy or NR8 R9; R6 is hydrogen or C1-6 alkyl; R7 is hydrogen or C1-6 alkyl optionally substituted by OR8 or NR8R9; R8 is hydrogen, C1-6 alkyl, optionally substituted by hydroxyl or C1-6 alkoxy or C1-3 alkylphenyl wherein said phenyl group is optionally substituted by one or more substituents selected from halogen, C1-6 alkyl, CF3, OR7, NR8R9 or OCF3; or the groups R8 and R9 when they are attached to a nitrogen atom may together form a 5- or 6-membered ring which optionally contains one further heteroatom selected from NR7, S and O said 5 or 6 membered ring being optionally substituted by hydroxyl or C1-6 alkoxy; or the groups R8 and R9 when they are attached to a nitrogen atom may together form an azetidinyl ring optionally substituted by hydroxyl or C1-6 alkoxy; and R10 is C1-6 alkyl or a phenyl group optionally substituted by one or more substituents selected from halogen, C1-6 alkyl, CF3, OCF3 or OR7; and n is 1 or 2. The use of the compounds in treating amyloid disease is also disclosed.
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- Achieving multi-isoform PI3K inhibition in a series of substituted 3,4-dihydro-2H-benzo[1,4]oxazines
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The SAR and pharmacokinetic profiles of a series of multi-isoform PI3K inhibitors based on a 3,4-dihydro-2H-benzo[1,4]oxazine scaffold are disclosed.
- Perry, Benjamin,Alexander, Rikki,Bennett, Gavin,Buckley, George,Ceska, Tom,Crabbe, Tom,Dale, Verity,Gowers, Lewis,Horsley, Helen,James, Lynwen,Jenkins, Kerry,Crepy, Karen,Kulisa, Claire,Lightfoot, Helen,Lock, Chris,Mack, Stephen,Morgan, Trevor,Nicolas, Anne-Lise,Pitt, Will,Sabin, Verity,Wright, Sara
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scheme or table
p. 4700 - 4704
(2009/04/08)
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- 6-[2-(4-Aryl-1-piperazinyl)ethyl]-2H-1,4-benzoxazin-3(4H)-ones: Dual-acting 5-HT1 receptor antagonists and serotonin reuptake inhibitors
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Investigation of a series 6-[2-(4-aryl-1-piperazinyl)ethyl]-2H-1,4-benzoxazin-3(4H)-ones has led to the discovery of potent 5-HT1A/1B/1D receptor antagonists with and without additional SerT affinity. Modulation of the different target activities gave compounds with a range of profiles suitable for further in vivo characterization.
- Bromidge, Steven M.,Bertani, Barbara,Borriello, Manuela,Faedo, Stefania,Gordon, Laurie J.,Granci, Enrica,Hill, Matthew,Marshall, Howard R.,Stasi, Luigi P.,Zucchelli, Valeria,Merlo, Giancarlo,Vesentini, Alessia,Watson, Jeannette M.,Zonzini, Laura
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scheme or table
p. 5653 - 5656
(2009/06/30)
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- BENZOXAZINONE DERIVATIVES, PREPARATION THEREOF AND USES IN THE TREATMENT OF CNS AND OTHER DISORDERS
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Compounds of formula (I) and pharmaceutically acceptable salts thereof are disclosed:wherein A, R1, R2, R3, p, q, A and X are as defined in the specification. Preparation of the compounds and uses in the treatment of CNS and other disorders, including dep
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