1624302-00-6Relevant articles and documents
2-ACYLAMINOTHIAZOLE DERIVATIVE AND SALT THEREOF
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, (2016/01/25)
[Problem] A compound which is useful as an active ingredient of a pharmaceutical composition for treating storage dysfunctions, voiding dysfunctions, and lower urinary tract diseases is provided. [Means for Solution] The present inventors have found that a thiazole derivative having pyrazine-2-carbonylamino substituted at the 2-position is an excellent muscarinic M3 receptor positive allosteric modulator, and is useful as an agent for preventing and/or treating bladder or urinary tract diseases, related to bladder contraction by a muscarinic M3 receptor, thereby completing the present invention. The 2-acylaminothiazole derivative or a salt thereof of the present invention can be used as an agent for preventing and/or treating bladder or urinary tract diseases, related to bladder contraction by a muscarinic M3 receptor, for example, voiding dysfunctions such as underactive bladder.
Towards a new synthetic entry into the Iboga-alkaloid family
Frauenfelder, Christine,Borschberg, Hans-Juerg
, p. 1753 - 1765 (2007/10/03)
A novel retrosynthetic concept is presented that, in principle, allows access to many hitherto not accessible representatives of the Iboga-alkaloid family. The flexibility required by this approach is provided through a highly convergent assembly of the target, which allows for a control over the substitution pattern of the indole sub-system, as well as over the relative configuration of the aliphatic core of these alkaloids. The key step for the construction of the latter consists in an intramolecular nitrone-olehn 1,3-dipolar cycloaddition reaction of 26 to yield the crucial tricyclic isoxazolidine derivative 28.