73873-63-9Relevant academic research and scientific papers
The discovery of a series of N-substituted 3-(4-piperidinyl)-1,3- benzoxazolinones and oxindoles as highly brain penetrant, selective muscarinic M1 agonists
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
scheme or table, p. 5434 - 5438 (2011/02/21)
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
COMPOUNDS WHICH HAVE ACTIVITY AT M1 RECEPTOR AND THEIR USES IN MEDICINE
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Page/Page column 88-89, (2009/04/25)
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.
BENZIMIDAZOLES WHICH HAVE ACTIVITY AT M1 RECEPTOR AND THEIR USES IN MEDICINE
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, (2008/06/13)
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.
Stereochemistry of Alkylation of Carboxylic Acid Salt and Ester α Anions Derived from Cyclic Systems.
Krapcho, A.Paul,Dundulis, Edward A.
, p. 3236 - 3245 (2007/10/02)
A stereochemical study of the alkylation of α-lithiated carboxylate salts and esters has been performed.The α anions derived from the bicyclic acids exo-1, endo-1, and 7 (R=H) and the esters 4 and 7 (R=CH3) yield predominantly exo alkylation.As an example, the α anion derived from ester 7 (R=CH3) on treatment with CH3I yields exo-8 (R=R'=CH3) and endo-9 (R=R'=CH3) in a 97:3 ratio, a highly stereoselective reaction.Addition of TMEDA to the reactions involving the α anions derived from exo- or endo-1 did not change the stereochemical alkylation results.The α anions derived from the substituted cyclohexanecarboxylic acids 10, 13, 16, 19, or 22 (where R=H in each case) on methylation yield more axial methylation (axial/equatorial ratios of 0.4-2.7) than the α anions derived from the methyl esters corresponding to these acids.The α anions from the esters yield predominantly equatorial methylated products (e/a ratios varying from 4 to 9).The reasons for the different stereochemical results are discussed.
