10-04-2014 дата публикации
Номер: US20140099316A1
Автор:
Aradhye Jayraj D.,
Berrebi-Bertrand Isabelle,
Capet Marc,
Desai Japan Nitinkumar,
Lecomte Jeanne-Marie,
Pal Ranjan Kumar,
Panchal Bhavesh M.,
Pathak Sandeep Pankajbhai,
Pillai Muthukumaran Natarajan,
Prajapati Kaushik Dhanjubhai,
Rana Dijixa Chandubhai,
ROBERT Philippe,
SAMANTA Biswajit,
Schwartz Jean-Charles,
Thennati Rajamannar
Принадлежит:
The present invention relates to novel compounds acting as agonists at S1P (sphingosine-1-phosphate) receptors, compositions containing these compounds, use of these compounds in medicine and their process of preparation. 2. The compound according to claim 1 , wherein Ar is a disubstituted phenyl group.4. The compound according to claim 1 , wherein R1 is selected from:{'sub': 2', '2', '2', '2', '2', '2', '2', '2', '2', '3', '2', '2, 'methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, secondarybutyl, tertiary butyl, n-pentyl, isopentyl, n-hexyl, isohexyl, hydroxymethyl, hydroxyethyl, hydroxypropyl, methoxymethyl, ethoxymethyl, methoxyethyl, vinyl, allyl, methoxyethoxymethyl, ethoxyethoxymethyl, ethoxyethoxyethyl, Phenyl, benzyl, benzyloxymethyl, benzyloxyethyl, —CH-[Ph(o-F)], —CH-[Ph(m-F)], —CH-[Ph(p-F)], —CH-[Ph(o-OMe)], —CH-[Ph(m-OMe)], or —CH-[Ph(p-OMe)], methoxybutyl, methoxyethoxymethyl, methoxyethoxyethyl, —CH-[Ph(o,o-F)], —CH-[Ph(m-CF)], —CH-furyl, —CH-pyridyl, (2-methoxy-phenoxy)-ethyl, 4-methoxy-benzyl, isopropoxy methyl, cyclopentyloxymethyl, thiophen-2-ylmethyl, cyclopropylmethyl, 2-morpholin-4-yl-ethyl, 3-piperidin-1-yl-propyl, 3-pyrrolidin-1-yl-propyl.'}5. The compound according to claim 1 , wherein R2 is H.6. The compound according to claim 1 , wherein R3 is selected from phenyl claim 1 , cyclohexyl claim 1 , cyclopentyl claim 1 , isobutyl claim 1 , isopropoxy.7. The compound according to which is selected from:1-{4-[5-(3-chloro-4-cyclohexylphenyl)-[1,2,4]-oxadiazol-3-yl]benzyl}-4-methylpiperidine-4-carboxylic acid1-{4-[5-(3-chloro-4-isobutylphenyl)-[1,2,4]-oxadiazol-3-yl]benzyl}-4-methylpiperidine-4-carboxylic acid1-{4-[5-(3-chloro-4-cyclopentylphenyl)-[1,2,4]-oxadiazol-3-yl]benzyl}-4-methylpiperidine-4-carboxylic acid1-{4-[5-(2-Chlorobiphenyl-4-yl)-[1,2,4]-oxadiazol-3-yl]benzyl}-4-methylpiperidine-4-carboxylic acid1-{4-[5-(3-chloro-4-cyclopentylphenyl)-[1,2,4]-oxadiazol-3-yl]benzyl}-4-methoxymethylpiperidine-4-carboxylic acid1-{4-[5-(3-chloro-4- ...
Подробнее