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MACROCYCLIC QUINAZOLINE DERIVATIVES, THEIR PREPARATION PROCESS, PHARMACEUTICAL COMPOSITION UNDERSTANDING THEM
专利权人:
Janssen Pharmaceutica N.V.
发明人:
Carsten Schultz-Fademrecht,Eddy Jean Edgard Freyne,Frederik Jan Rita Rombouts,Gaston Stanislas Marcella Diels,Marc Willems,Peter Jacobus Johannes Antonius Buijnsters,Peter Ten Holte,Timothy Pietro Sur
申请号:
BRPI0410714
公开号:
BRPI0410714B1
申请日:
2004.05.25
申请国别(地区):
BR
年份:
2019
代理人:
摘要:
"quinazoline derivatives". The present invention relates to compounds of the formula: n-oxide forms, pharmaceutically acceptable addition salts and stereochemically isomeric forms thereof, wherein: z represents nh; y represents -C- 3-9-alkyl-, -C- 2-9-alkenyl-, -C- 3-7-alkyl-co-nh optionally substituted by amino, mono- or di (C 1-4 ~ C 1-4 alkyloxycarbonylamino-, C 3-7 alkenyl-co-n- optionally substituted by amino, mono- or di (C 1-4 alkyl) amino- or C 1-4 alkyloxycarbonylamino- 1-4-alkyloxycarbonylamino-, C 1-5-5-alkyl-nr-13-C-1-5-alkyl-, C-1-5-alkyl-nr-14 ^ -co-C-1-5 ~ C 1-6 alkyl-C 1-6 alkyl-C 1-5 alkyl-C 1-6 alkyl-C 1-6 alkyl-C 1- 1-5 alkyl-C 1- 1-3 alkyl nh-co-het ^ 20 ^ -, -c-1-2-alkyl-co-het ^ 21 ^ co-, -c-1-2-alkyl-nh-co-cr ^ 16 ^ r ^ 17 ^ - nh-, -c-1-2-alkyl-co-nh-cr-18 ^ r ^ 19 ^ -co-, -c-1-2-alkyl-co-nr-20 ^ -c-1-3 ~ C1-6 alkyl-co-C1-3-3 alkyl-nh-; x ^ 1 ^ is a direct bond, or O-alkylated or ~ c ~ 1-2; X ^ 2 ^ represents a direct bond, -co-C 1- 1-2-alkyl-, nr ^ 12 ^, - nr ^ 12 ^ -C-1-2-alkyl-, -on = ch- or -c- 1-2-alkyl-; R2 and R2 each independently represent hydrogen or halo; R3 represents hydrogen; R4 is hydrogen or C1-4 alkyloxy; R 12 and R 13 each independently represent hydrogen or C 1-4 alkyl; R 14 and R 15 represent hydrogen; R 16 and R 17 each independently represent hydrogen or C 1-4 alkyl; R 18 and R 19 each independently represent hydrogen or C 1-4 alkyl optionally substituted by phenyl or hydroxy; R 20 and R 21 each independently represent hydrogen or C 1-4 alkyl optionally substituted by C 1-4 alkyloxy; het ^ 20 ^, het ^ 21 ^ and het ^ 22 ^ each independently represent a heterocycle selected from the group consisting of pyrrolidinyl, 2-pyrrolidinonyl or piperidinyl optionally substituted by hydroxy."derivados de quinazolina". a presente invenção se refere a compostos da fórmula: as formas de n-óxido, os sais de adição farmaceuticamente aceitáveis e as formas estereoquimicamente isoméricas do mesmo, em que: z representa nh; y representa -c~ 3
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