10368-35-1Relevant articles and documents
C1 substituted 3, 4 - ISO-quinoline alkaloids of the preparation and its medicinal use
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, (2019/03/28)
The invention belongs to the field of medical technology. The invention relates to a structure of the formula (I) indicated by the C1 substituted 3, 4 - ISO alkaloid or its pharmaceutically acceptable salt preparation method and medical use thereof. The invention to BOC - L - phenylalanine as raw materials, with 3, 4 - dimethoxyphenethylamine to N - acylated condensation and then remove the BOC group gets the (S)- 2 - amino - N - (3, 4 - dimethyl practiced with ethyl) - 3 - benzyl amide intermediate 1, intermediate 1 or phenethylamine derivatives with the prepared containing different substituent phenyllacetyl carries out amidation reaction, finally loop Bischler - Napieralski reaction. After activeness screening tests, the compounds of this invention possess pancrelipase inhibition, in the development into a lipase inhibitor and for preventing or treating hyperlipidemia, diabetes, obesity or metabolic syndrome and other diseases has a good application prospect.
COMPOUNDS, SALTS THEREOF AND METHODS FOR TREATMENT OF DISEASES
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Paragraph 00410-00411, (2019/03/12)
The present disclosure relates to compounds according to Formula (I), useful for treating diseases.
Discovery of a Potent, Selective T-type Calcium Channel Blocker as a Drug Candidate for the Treatment of Generalized Epilepsies
Bezen?on, Olivier,Heidmann, Bibia,Siegrist, Romain,Stamm, Simon,Richard, Sylvia,Pozzi, Davide,Corminboeuf, Olivier,Roch, Catherine,Kessler, Melanie,Ertel, Eric A.,Reymond, Isabelle,Pfeifer, Thomas,De Kanter, Ruben,Toeroek-Schafroth, Michael,Moccia, Luca G.,Mawet, Jacques,Moon, Richard,Rey, Markus,Capeleto, Bruno,Fournier, Elvire
supporting information, p. 9769 - 9789 (2017/12/26)
We report here the discovery and pharmacological characterization of N-(1-benzyl-1H-pyrazol-3-yl)-2-phenylacetamide derivatives as potent, selective, brain-penetrating T-type calcium channel blockers. Optimization focused mainly on solubility, brain penetration, and the search for an aminopyrazole metabolite that would be negative in an Ames test. This resulted in the preparation and complete characterization of compound 66b (ACT-709478), which has been selected as a clinical candidate.