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pyrimido [6,1-a] isoquinolin-4-one derived compound, process for preparing same, composition, and use of a compound
专利权人:
VERNALIS DEVELOPMENT LIMITED;VERONA PHARMA PLC.;RHINOPHARMA LIMITED;VERNALIS LIMITED
发明人:
ALEXANDER WILLIAM OXFORD,DAVID JACK
申请号:
BR0009446
公开号:
BRPI0009446B1
申请日:
2000.03.29
申请国别(地区):
BR
年份:
2016
代理人:
摘要:
"compound, process for preparing same, composition, use of a compound, and methods for treating or preventing a disease in a mammal, treating or preventing asthma in a mammal, and treating or preventing" of chronic obstructive pulmonary disease in a mammal ". compounds of formula (1) wherein each R1 and R2 independently represent a C 1-6 alkyl or C 2-7 acyl group; w represents a hydrogen atom or a C 1-3 alkyl alkenyl, C 2-3 alkenyl or C 2-3 alkynyl group; R 6 represents a hydrogen atom or a C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, amino, C 1-6 alkylamino, di (C 1-6) group. ~) alkylamino or C 2-7-acylamino; each of c 1 and R 8 independently represents a hydrogen or halogen atom or a hydroxy, trifluoromethyl, C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, C 2-7 acyl, C C 1-6 alkylthio, C 1-6 alkoxy or C 3-6 cycloalkyl; and R 9 is hydrogen, halogen, hydroxy, trifluoromethyl, C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, C 2-7 acyl, C 1-6 alkylthio, C 1-6 alkoxy or C 3-6 cycloalkyl; x represents och ~ 2 - or a group ??? wherein each of R 3 and R 4 independently represents a hydrogen atom or a C 1-3 alkyl group; each of R 10 and R 11 independently represents a hydrogen atom, a C 1-3 alkyl, C 3-6 cycloalkyl or phenyl group; y represents an oxygen atom or a group chno ~ 2 ~, ncn, nh or nno ~ 2 ~; n is an integer from 2 to 4; or a salt thereof; They are useful for treating respiratory disorders such as asthma. The compounds of the invention have a longer duration of action than the known compound trequinsine (9,10-dimethoxy-3-methyl-2-mesitylimino-2,3,6,7-tetrahydro-4hpyrimidated [6,1-a] isoquinolinone 4-one) and do not have the very bitter taste of trequinsin."composto, processo para preparar o mesmo, composição, uso de um composto, e, métodos para o tratamento ou a prevenção de uma doença em um mamífero, para o tratamento ou a prevenção de asma em um mamífero e para o tratamento ou a prevenção de doença pulmonar obstrutiva crônica em um mamífero". compostos de fórmula geral (1
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