317319-14-5Relevant academic research and scientific papers
FUSED HETEROCYCLIC COMPOUNDS AND THEIR USE
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Page/Page column 34; 35, (2014/03/25)
The present invention provides compounds of formula (I) and pharmaceutically acceptable salts, hydrates and solvates thereof for use in the treatment of cancer:
5- [4- (AZETIDIN-3-YL0XY) -PHENYL] -2-PHENYL-5H-THIAZ0L0 [5,4-C] PYRIDIN-4-0NE DERIVATIVES AND THEIR USE AS MCH RECEPTOR ANTAGONISTS
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Page/Page column 40, (2008/12/06)
The present invention relates to a melanin concentrating hormone antagonist compound of formula I: wherein "-----" is absent or is optionally a bond; q is 1 or 2; R1 is independently selected from hydrogen, -C1-C2 alkyl, halo, hydroxy, -C1-C2 haloalkyl, -C1-C3 alkoxy, cyano, -O-C3-C4 cycloalkyl, and -OC1-C2 haloalkyl; R2 is selected from the group consisting of hydrogen, -C1-C3 alkyl, hydroxy, -C1-C3 alkoxy, cyano, -C1-C2 haloalkyl, -OC1-C2 haloalkyl, and halo; R3 is selected from the group consisting of hydrogen, -C1-C4 alkyl, -C2-C4 haloalkyl, -C2-C4 alkylOH, -C3-C6 cycloalkyl, -CH2C3-C6 cyxloalkyl, -C2-C4 alkyl-O-C1-C4 alkyl, -C(O)C1-C4 alkyl, -C(O)C1-C4 haloalkyl, -CH2-thiazole, phenyl, benzyl, tetrahydrothiopyranyl, and tetrahydropyranyl, wherein the cycloalkyl, tetrahydrothiopyranyl, tetrahydropyranyl and thiazolyl group is optionally substituted with one or two groups independently selected from the group consisting of halo, hydroxy, C1-C2 alkyl, and -C1-C2 haloalkyl; or a pharmaceutically acceptable salt, enantiomer, diastereomer or mixture thereof,, useful in the treating, preventing or ameliorating of symptoms associated with obesity and related diseases.
Reactions of some ortho and para halogenated aromatic nitriles with ethylenediamine: Selective synthesis of imidazolines
Crane, Louis J.,Anastassiadou, Maria,Stigliani, Jean-Luc,Baziard-Mouysset, Geneviève,Payard, Marc
, p. 5325 - 5330 (2007/10/03)
The reaction of ethylenediamine (EDA) with ortho and/or para halogenated benzonitriles did not lead to the imidazolines expected: a competitive aromatic nucleophilic substitution (SNAr) was observed instead. The selective synthesis of these imidazolines was performed by nucleophilic addition of EDA to thiobenzamide derivatives. The difference in reactivity between the nitrile and thioamide derivatives was estimated by a frontier orbital approach at the RHF/6-31G** level which predicted a greater reactivity of substituted thiobenzamides towards the nucleophilic addition of EDA.
