102308-48-5Relevant academic research and scientific papers
Benzenesulphonamide derivatives, method for production and use thereof for treatment of pain
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Page/Page column 18, (2008/06/13)
The present invention concerns novel benzenesulphonamide compounds, defined by formula I and the description, their method of preparation and their use in therapy.
Therapeutic agents
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, (2008/06/13)
Compounds of formula I STR1 and pharmaceutically acceptable salts thereof in which R1, R2 and R3 independently represent hydrogen, hydroxy, halo, alkyl or alkoxy; ALK1 represents a C2-6 alkylene chain optionally substituted by one or more C1-2 alkyl groups; Y represents a piperidine ring which is attached through nitrogen to ALK1 ; R4 represents hydrogen or a C1-4 alkyl group; the broken line in --- represents a bond, or is absent and the free valency on Y is taken up by hydrogen and the free valency on CR4 is taken up by hydrogen or a C1-4 alkyl group; ALK2 is absent or represents a C1-4 alkylene chain optionally substituted by one or more C1-2 alkyl groups; and R5 and R6 independently represent hydrogen, alkyl, phenyl, alkyl (optionally substituted) or R5 and R6 together with the nitrogen atom to which they are attached represent a saturated 3-7 membered heterocyclic ring (with a proviso); are disclosed which are antiinflammatory, antiallergic and immunomodulatory agents. Compositions containing these compounds and processes to prepare these compounds are also disclosed.
Synthesis and structure-activity relationship of some 5- [[[(dialkylamino)alkyl]-1-piperidinyl]acetyl]-10,11-dihydro-5H- benzo[b,e][1,4]diazepin-11-ones as M2-selective antimuscarinics
Cohen,Baumgold,Jin,De la Cruz,Rzeszotarski,Reba
, p. 162 - 165 (2007/10/02)
A series of 5-[[[(dialkylamino)alkyl]-1-piperidinyl]acetyl]-10,11-dihydro- 5H-dibenzo[b,e][1,4]-diazepin-11-ones were prepared as potential M2- selective ligands. The compounds were evaluated for their affinity and selectivity for the muscarinic cholinergic receptor. The best M2-selective antimuscarinic agent studied is 5-[[4-[4-(diethylamino)butyl]-1- piperidinyl]acetyl]-10,11-dihydro-5H-dibenzo[b,e][1,4]diazepin-11-one, which is approximately 10 times more potent at M2 receptors than previously known compounds such as 11-[[4-[4-(diethylamino)butyl]-1-piperidinyl]acetyl]-5,11- dihydro-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one (AQ-RA 741).
