ANDRIES, KOENRAAD JOZEF LODEWIJK MARCEL,安瑞斯,安瑞斯,KOUL, ANIL,郭安尼,郭安尼,GUILLEMONT, JEROME EMILE GEORGES,古利蒙,古利蒙,PASQUIER, ELISABETH THERESE JEANNE,佩斯儿,佩斯兒
申请号：
TW095120140
公开号：
TWI380819B
申请日:
2006.06.07
申请国别(地区):
TW
年份:
2013
代理人:
摘要：
The present invention relates to the use of a compound for the manufacture of a medicament for the treatment of a bacterial infection, said compound being a compound of formula a pharmaceutically acceptable acid or base addition salt thereof, a stereochemically isomeric form thereof or a N-oxide form thereof, wherein R1 is hydrogen, halo, polyhaloC1-6alkyl, C1-6alkyl, Ar or Het p is an integer equal to 1 or 2 R2 is C1-6alkyloxy, C1-6alkyloxyC1-6alkyloxy or C1-6alkylthio R3 is Ar, Het or Het1 R4 and R5 each independently are hydrogen, C1-6alkyl or benzyl or R4 and R5 together and including the N to which they are attached may form a radical selected from the group of pyrrolidinyl, 2-pyrrolinyl, 3-pyrrolinyl, pyrrolyl, imidazolidinyl, pyrazolidinyl, 2-imidazolinyl, 2-pyrazolinyl, imidazolyl, pyrazolyl, triazolyl, piperidinyl, pyridinyl, piperazinyl, pyridazinyl, pyrimidinyl, pyrazinyl, triazinyl, morpholinyl and thiomorpholinyl, each of said rings may optionally be substituted with C1-6alkyl, halo, polyhaloC1-6alkyl, hydroxy, hydroxyC1-6alkyl, C1-6alkyloxy, amino, mono- or di(C1-6alkyl)amino, C1-6alkylthio, C1-6alkyloxyC1-6alkyl, C1-6alkylthioC1-6alkyl or pyrimidinyl R6 is hydrogen, halo, polyhaloC1-6alkyl, C1-6alkyl, C1-6alkyloxy, C1-6alkylthio or two vicinal R6 radicals may be taken together to form a bivalent radical of formula -CH=CH-CH=CH- r is an integer equal to 1 or 2 R7 is hydrogen, C1-6alkyl, Ar, Het or Het1 provided that the bacterial infection is other than a Mycobacterial infection.本發明係關於使用一種化合物供製造用於治療細菌感染之藥物的用途,此化合物係具有下式化學式之化合物其醫藥上可接受的酸或鹼加成鹽,其立體化學異構物或其N-氧化物型式,其中,R1為氫,鹵基,多鹵基C1-6烷基,C1-6烷基,Ar或Het;p為等於1或2之整數;R2為C1-6烷氧基,C1-6烷氧基C1-6烷氧基或C1-6烷硫基;R3為Ar,Het或Het1;R4與R5各自獨立地為氫,C1-6烷基或苯甲基;或R4與R5一起且包含它們附接著的N可形成挑選自包括下述基之基;吡咯啶基,2-吡咯啉基,3-吡咯啉基,吡咯基,咪唑啶基,吡唑啶基,2-咪唑啉基,2-吡唑啉基,咪唑基,吡唑基,三唑基,六氫吡啶基,吡啶基,六氫吡基,噠基,嘧啶基,吡基,三基,嗎啉基與硫嗎啉基,所述各個環可選擇地經取代下述基:C1-6烷基,鹵基,多鹵基C1-6烷基,羥基,羥基C1-6烷基,C1-6烷氧基,胺基,單-或二(C1-6烷基)胺基,C1-6烷硫基,C1-6烷氧基C1-6烷基,C1-6烷基硫C1-6烷基或嘧啶基;R6為氫,鹵基,多鹵基C1-6烷基,C1-6烷基,C1-6烷氧基,C1-6烷硫基;
