- The discovery of a series of N-substituted 3-(4-piperidinyl)-1,3- benzoxazolinones and oxindoles as highly brain penetrant, selective muscarinic M1 agonists
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A series of N-substituted 3-(4-piperidinyl)-1,3-benzoxazolinones and oxindoles are reported which were found to be potent and selective muscarinic M1 agonists. By control of the physicochemical characteristics of the series, particularly the li
- Johnson, Dale J.,Forbes, Ian T.,Watson, Steve P.,Garzya, Vincenzo,Stevenson, Graeme I.,Walker, Graham R.,Mudhar, Harminder S.,Flynn, Sean T.,Wyman, Paul A.,Smith, Paul W.,Murkitt, Graham S.,Lucas, Adam J.,Mookherjee, Claudette R.,Watson, Jeannette M.,Gartlon, Jane E.,Bradford, Andrea M.,Brown, Fiona
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scheme or table
p. 5434 - 5438
(2011/02/21)
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- COMPOUNDS WHICH HAVE ACTIVITY AT M1 RECEPTOR AND THEIR USES IN MEDICINE
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Compounds of formula (I) or a salt thereof are provided: wherein R4, R5, R6, Q, A, Y and R are as defined in the description. Uses of the compounds as medicaments and in the manufacture of medicaments for treating psychotic disorders, cognitive impairments and Alzheimer's Disease are disclosed. The invention further discloses pharmaceutical compositions comprising the compounds.
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Page/Page column 89-90
(2009/04/25)
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- BENZIMIDAZOLES WHICH HAVE ACTIVITY AT M1 RECEPTOR AND THEIR USES IN MEDICINE
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Compounds of formula (I), salts and solvates are provided: formula (I), wherein Q, R and R6 are as defined in the claims. Uses of the compounds for therapy, for example in the treatment of psychotic disorders and cognitive impairment, are also disclosed.
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