On December 27, 2007, Arnold, James; Berg, Stefan; Chessari, Gianni; Congreve, Miles; Edwards, Phil; Holenz, Joerg; Kers, Annika; Kolmodin, Karin; Murray, Christopher; Patel, Sahil; Rakos, Laszlo; Rotticci, Didier; Sylvester, Mark; Oehberg, Liselotte published a patent.Computed Properties of 908267-63-0 The title of the patent was Substituted isoindoles as BACE inhibitors and their preparation, pharmaceutical compositions and use in the treatment of cognitive impairment, Alzheimers disease, neurodegeneration and dementia. And the patent contained the following:
This invention relates to compounds having the structural formula I and to their pharmaceutically acceptable salt, compositions and methods of use. These compounds provide a treatment or prophylaxis of cognitive impairment, Alzheimer disease, neurodegeneration and dementia. Compounds of formula I wherein R1 is H, NO2, CN, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl;, CONH-C1-6 alkyl, etc.; R2 is Me, (un)substituted C0-3 alkyl-C3-6 cycloalkyl, NO2, CN, substituted C2-4 alkenyl, etc.; R3 is H, halo, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-6 cycloalkyl, etc.; m is 0, 1, 2, and 3; and their pharmaceutically acceptable salts, solvates, salts of solvates thereof are claimed. Example compound II•TFA was prepared by Suzuki cross-coupling of [3-(3-bromo-4-hydroxyphenyl)-3-(4-methoxyphenyl)-3H-isoindol-1-yl]carbamic acid tert-Bu ester with 3-methoxyphenylboronic acid; the resulting [3-(6-hydroxy-3′-methoxybiphenyl-3-yl)-3-(4-methoxyphenyl)-3H-isoindol-1-yl]carbamic acid tert-Bu ester underwent hydrolysis to give compound II•TFA. All the invention compounds were evaluated for their BACE inhibitory activity. From the assay, it was determined that compound II exhibited an IC50 value of 67 nM. The experimental process involved the reaction of 4-Bromo-2-isopropylpyridine(cas: 908267-63-0).Computed Properties of 908267-63-0
The Article related to substituted isoindole preparation bace inhibitor, treatment alzheimer disease neurodegeneration dementia cognitive impairment isoindole preparation, Heterocyclic Compounds (One Hetero Atom): Indoles, Indolizines, Carbazoles, and Other Arenopyrroles and other aspects.Computed Properties of 908267-63-0