52797-99-6Relevant academic research and scientific papers
N-SULFONYL THIAZOLYLPIPERAZINE DERIVATIVES AND RELATED N-SULFONYL HETEROCYCLIC DERIVATIVES FOR THE TREATMENT OF NEURO DEGENERATIVE DISEASES
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Page/Page column 79; sheet 4, (2010/08/08)
This invention provides thiazolylpiperazine derivatives, and N-sulfonyl heterocyclic derivatives including phenyl- and benzyl-thiazolylpiperidine derivatives, and pharmaceutically acceptable salts thereof, which are useful active ingredients for administration in a method for the treatment of an α-synucleopathy such as Parkinson's disease, diffuse Lewy body disease, traumatic brain injury, amyotrophic lateral sclerosis, Niemann-Pick disease, Hallervorden-Spatz syndrome, Down syndrome, neuroaxonal dystrophy, multiple system atrophy and Alzheimer's disease. This invention also provides methods for making such derivatives, and pharmaceutical compositions including such derivatives together with pharmaceutically acceptable excipients.
Potential Thyroliberin Affinity Labels. 1. Chloroacetyl-Substituted Phenylalanylpyrrolidines
Goebel, Richard J.,Currie, Bruce L.,Bowers, Cyril Y.
, p. 366 - 370 (2007/10/02)
Six analogues of thyroliberin (THR) that have a chloroacetyl substituent at the amino terminus have been prepared as potential affinity labels for the TRH receptor.These compounds are N-(chloroacetyl)-L-alanyl-L-phenylalanylpyrrolidine (ClAc-Ala-Phe-Pyrr; 14), N--L-phenylalanyl>pyrrolidine (m-ClAcBz-Phe-Pyrr; 11a), N--L-alanyl-L-phenylalanylpyrrolidine (m-ClAcBz-Ala-Phe-Pyrr; 15a), N--L-phenylalanylpyrrolidine (p-ClAcBz-Phe-Pyrr; 11b), and N--L-alanyl-L-phenylalanylpyrrolidine (p-ClAcBz-Ala-Phe-Pyrr; 15b).Pyroglutamyl-L-phenylalanylpyrrolidine was also synthesized as a model agonist.Weak agonist activity was observed for 11a, 11b, and 15b.These three analogues do not contain the amide group of the pyroglutamyl moiety that was previously thought to be essential for intrinsic activity.No significant antagonist activity was observed for these compounds at the doses tested.
