10368-35-1Relevant academic research and scientific papers
COMPOUNDS, SALTS THEREOF AND METHODS FOR TREATMENT OF DISEASES
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Paragraph 00253; 00254, (2019/03/12)
The present disclosure relates to compounds according to Formulae (I), (II) and (VIII), useful for treating diseases.
C1 substituted 3, 4 - ISO-quinoline alkaloids of the preparation and its medicinal use
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Paragraph 0066; 0076; 0077, (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.
9 - Substituted derivative of berberine at the preparation and its use in medicine (by machine translation)
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Paragraph 0034; 0042; 0043, (2018/04/03)
The invention belongs to the field of medical technology. The invention relates to a structure of the formula (I) and formula (II) shown by the 9 bit - substituted berberine derivatives and their pharmaceutically acceptable salts thereof and its medical use. After activeness screening tests, the compounds of this invention possess pancrelipase inhibition, develop into the prospect of lipase inhibitors; in addition, the compounds of this invention fat-soluble than berberine increased, so that the development into the prevention or treatment of hyperlipidemia, diabetes, obesity or metabolic syndrome and other diseases in more application prospect. (by machine translation)
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.
AZACYCLIC COMPOUNDS
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Paragraph 0593, (2015/11/09)
Compounds and methods are provided for the treatment of disease conditions in which modification of serotonergic receptor activity has a beneficial effect. In the method, an effective amount of a compound is adminstered to a patient in need of such treatment.
USE OF 4-AMINO-PIPERIDINES FOR TREATING SLEEP DISORDERS
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Page/Page column 125, (2010/11/28)
Inverse agonists and antagonists of serotonin receptors are disclosed for use in treating sleep disorders such as insomnia, and specifically sleep maintenance insomnia. The compound increase slow wave sleep, decrease the number of awakenings after sleep onset, and decrease the time awake after sleep onset.
Azacyclic compounds
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, (2008/06/13)
Compounds and methods are provided for the treatment of disease conditions in which modification of serotonergic receptor activity has a beneficial effect. In the method, an effective amount of a compound is adminstered to a patient in need of such treatment.
Substituted pyridines/pyrimidines, their preparation and their use as pesticides
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, (2008/06/13)
The present invention relates to novel substituted pyridines/pyrimidines of the formula I where A is CH or N; X is NH, O or S(O)qwhere q is 0, 1 or 2; Y1, Y2and Y3independently of one another are a group of the
Synthesis of some new benzimidazole-5(6)-carboxylic acids
Goker,Olgen,Ertan,Akgun,Ozbey,Kendi,Topcu
, p. 1767 - 1773 (2007/10/03)
The title compounds, 1,2-dialkyl-benzimidazole-5(6)-carboxylic acids 34-45 were prepared at four steps; 1) preparation of mono amide derivatives 1-11 by the reaction of methyl 3,4-diaminobenzoate and substituted phenyl or phenoxyacetic acid chlorides; 2) preparation of the methyl benzimidazolecarboxylates 12-22, with zinc chloride and dry hydrogen chloride gas; 3) alkaline hydrolysis of the esters 23-33; and 4) substitution of the imidazole ring with benzyl or p-fluorobenzyl bromide, in alkali medium. 2-Aryl-benzimidazole-5(6)-carboxylic acids 50-53 were prepared via the oxidative condensation of 3,4-diaminobenzoic acid and aromatic aldehydes with cupric ion.
