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3-UROISOQUINOLEIN-8-YLE DERIVES
专利权人:
ACTELION PHARMACEUTICALS LTD
发明人:
HUBSCHWERLEN, CHRISTIAN,PANCHAUD, PHILIPPE,GUDE, MARKUS
申请号:
MA36339
公开号:
MA35048B1
申请日:
2013.10.11
申请国别(地区):
MA
年份:
2014
代理人:
摘要:
the invention relates to derivatives of 3 - ur u00c9idoisoquinol u00c9in - acetate of formula (i), wherein r1 is alkyl or cyclopropyl haloalkyle; r2 is h, halogen, acetate pyrimidin pyridazin-3 (4, 5) or an acetate group optionally substitu u00c9 of pyridin-3 acetate, acetate or ph u00c9nyle pyridin - 4. r3 is alkyl, alcynyl (e) aminoalkyle, carbamoylalkyle carbamoylalkyle, methyl -, alkoxy, haloalcoxy, alcynyloxy.(4 hydroxybut - 2 - a - 1 - [(4 - aminobut) oxy) - 2 - a 1 yl) oxy dim u00c9thylaminoalcoxy, carbamoylalcoxy, alkylamino, cycloalkyl, cycloalkylalkyle, cycloalkylalcoxy, hydroxyalkyle, hydroxyalcoxy, alcoxyalkyle, alcoxyalcoxy, carboxyalkyle, carboxyalcoxy, alcoxycarbonylalcoxy, aryl, benzyl, or h u00c9t u00c9roaryle. nzyloxy, 2 dihydroxypropoxy cyano u00c9thoxy, 2,3 -, 3,4 - dihydroxybutoxy, ch2ra, ch2ch2rb, - (ch2) n - c (o) o - r & d- (ch2) n - and (or) c (o) o - d, - o (ch2) n - and (or) c (o) o - r - (ch2) n - or - o - (ch2) n -; r is cyano, ac u00c9tylamino or n no dim u00c9thylamino is cyano or carbamoyl; rb and rc are h or methyl; r is alkyl) - pyrrolidin-3-yl; is pip u00c9ridin - yl acetate, acetate, pip u00c9ridin - 3 - 1 - yl, morpholin oxopyrrolidin - 1, 2 - 5 - oxopy acetate. rrolidin) acetate, 2.5 - dioxopyrrolidin - 1 - 2 - 1 oxoimidazolidin acetate, acetate.4 - (tert butoxy) - carbonyl) pip u00c9razin - 1, 4 - (acetate, cyclohexyl or h u00c9t u00c9roaryle aminom u00c9thyl); r4 is h or methyl; and salts of these compounds. these compounds are useful in the prevention or treatment of bacterial infections.L'INVENTION CONCERNE DES DÉRIVÉS DE 3-URÉIDOISOQUINOLÉIN-8-YLE DE FORMULE I, DANS LAQUELLE R1 EST ALKYLE, HALOALKYLE OU CYCLOPROPYLE; R2 EST H, HALOGÈNE, PYRIDAZIN-4-YLE, PYRIMIDIN-5-YLE OU UN GROUPE FACULTATIVEMENT SUBSTITUÉ DE PYRIDIN-3-YLE, PYRIDIN-4-YLE OU PHÉNYLE; R3 EST ALKYLE, ALCYNYLE, AMINOALKYLE, CARBAMOYLALKYLE, MÉTHYL-CARBAMOYLALKYLE, ALCOXY, HALOALCOXY, ALCYNYLOXY, (4-HYDROXYBUT-2-YN-1-YL)OXY, (4-AMINOBUT-2-YN-1-YL)OXY, DIMÉTHYLA
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