79134-92-2Relevant academic research and scientific papers
SMALL MOLECULE MODULATORS OF IL-17
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Page/Page column 82-83, (2020/09/30)
The present invention relates to a compound according to formula I and pharmaceutically acceptable salts, hydrates, or solvates thereof. The invention further relates to, to said compounds for use in therapy, to pharmaceutical compositions comprising said
AMINO-ACID ANILIDES AS SMALL MOLECULE MODULATORS OF IL-17
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Page/Page column 90, (2020/07/14)
The present invention relates to a compound according to formula I (I) and pharmaceutically acceptable salts, hydrates, or solvates thereof. The invention further relates to said compounds for use in therapy, to pharmaceutical compositions comprising said compounds, to methods of treating diseases, e.g. dermal diseases, with said compounds, and to the use of said compounds in the manufacture of medicaments.
Glycine transporter-1 inhibitors
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Page/Page column 33, (2008/06/13)
The present invention provides compounds that are glycine transporter 1 (hereinafter referred to as GlyT-1) inhibitors and are therefore useful for the treatment of diseases treatable by inhibition of GlyT1 such as cognitive disorders associated with Schizophrenia, ADHD (attention deficit hyperactivity disorder), MCI (mild cognitive impairment), and the like. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.
Mechanistic Evidence regarding the Magnesium Halide Transformation of Cyclopropylmethanols into Homoallylic Halides
McCormick, J. P.,Fitterman, Alan S.,Barton, Donald L.
, p. 4708 - 4712 (2007/10/02)
Cyclopropylmethanols are converted into homoallylic halides in high yield by treatment with magnesium bromide or iodide in refluxing, anhydrous diethyl ether.For uncovering of the details of the reaction mechanism, (cyclopropylphenylmethoxy)magnesium bromide (3a) was prepared by treatment of cyclopropylphenylmethanol (1) with hydridomagnesium bromide.Alkoyoxymagnesium bromide 3a was stable in refluxing diethyl ether and was not changed when treated with tetrabutylammonium bromide but was transformed into 4-bromo-1-phenyl-1-butene by treatment with hydrogen bromide or magnesium bromide.These results, together with first-order kinetics for the reaction of magnesium halide with 1, suggest a mechanism involving rapid formation of an intermediate ion pair (4), a magnesium oxonium bromide, which undergoes rate-determining ring opening to give homoallylic halide.A Hammett study of the reaction of substituted cyclopropylphenylmethanols with magnesium iodide provides a p value of -1.82, revealing substantial positive charge development on the carbinol carbon in the latter step.This investigation provides one of only a very few reported examples of Hammett studies used to probe positive charge development for a reaction carried out in anhydrous diethyl ether.
