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Preparation of piperazinyl quinazolines as 5-HT6 modulators.
2007 (English)Patent (Other (popular science, discussion, etc.))Text
Abstract [en]

Title compds. represented by the formula I [wherein Q = (hetero)arylalkyl, (hetero)cycloalkylalkyl or alkyl; B = CH or N; R1 = H, OH, halo, alkyl, etc.; R2 = H, (halo)alkyl, aminocarbonylalkyl, etc.; R3 = H, (halo)alkyl or alkylaryl; R4 = CN, halo, alkoxy, etc.; m = 0-2; n = 0-4; and pharmaceutically acceptable salts, solvates or solvated salts thereof] were prepd. as 5-HT6 modulators. For example, reaction of 2,4-dichloroquinazoline with benzenesulfonamide and followed by reaction with N-methylpiperazine, gave N-[2-(4-methylpiperazin-1-yl)quinazolin-4-yl]benzenesulfonamide in 6% yield. The radioligand binding assay showed II having Ki of 1.4 nM. Thus, I and their pharmaceutical compns. are useful for the treatment of 5-HT6 mediated disorders, such as Alzheimer's disease, schizophrenia, obesity or Parkinson's disease. [on SciFinder(R)]

Place, publisher, year, edition, pages
AstraZeneca AB, Swed. . , 2007. no WO2007108743A2
Keyword [en]
quinazoline piperazinyl benzenesulfonamide prepn 5HT6 modulator, Alzheimer schizophrenia obesity Parkinson disease treatment piperazinylquinazolinyl benzenesulfonamide prepn
National Category
Medicinal Chemistry
URN: urn:nbn:se:uu:diva-270237OAI: oai:DiVA.org:uu-270237DiVA: diva2:888186

CAPLUS AN 2007:1086842(Patent)

Available from: 2015-12-22 Created: 2015-12-22 Last updated: 2015-12-22

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Yngve, Ulrika.
Medicinal Chemistry

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