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    • 5. 发明申请
    • Quinoline Derivatives as Antibacterial Agents
    • 喹啉衍生物作为抗菌剂
    • US20100197727A1
    • 2010-08-05
    • US11917091
    • 2006-06-26
    • Koenraad Jozef Lodewijk Marcel AndriesAnil KoulDavid Francis Alain LancoisMagali Madeleine Simone MotteJérôme Emile Georges Guillemont
    • Koenraad Jozef Lodewijk Marcel AndriesAnil KoulDavid Francis Alain LancoisMagali Madeleine Simone MotteJérôme Emile Georges Guillemont
    • A61K31/47C07D215/227C07D409/06A61K31/4709C07D401/06C07D215/36A61P31/04
    • C07D409/06A61K31/47A61K31/4709C07D215/227C07D215/36C07D401/06
    • Use of a compound for the manufacture of a medicament for the treatment of a bacterial infection provided that the bacterial infection is other than a Mycobacterial infection, said compound being a compound of formula (Ia) or (Ib) a N-oxide, a tautomeric form or a stereochemically isomeric form thereof wherein A− is a counter ion; R1 is hydrogen, halo, haloalkyl, cyano, hydroxy, Ar, Het, alkyl, alkyloxy, alkylthio, alkyloxyalkyl, alkylthioalkyl, Ar-alkyl or di(Ar)alkyl; p is 1 to 4; R2 is hydrogen, hydroxy, mercapto, alkyloxy, alkyloxyalkyloxy, alkylthio, mono or di(alkyl)amino or wherein Y is CH2, O, S, NH or N-alkyl; R3 is alkyl, Ar, Ar-alkyl, Het or Het-alkyl; q is 0 to 4; R4 and R5 each independently are hydrogen, alkyl or benzyl; or R4 and R5 may be taken together including the N to which they are attached; R6 is hydrogen, halo, haloalkyl, hydroxy, Ar, alkyl, alkyloxy, alkylthio, alkyloxyalkyl, alkylthioalkyl, Ar-alkyl or di(Ar)alkyl; or two vicinal R6 radicals may be taken together to form —CH═CH—CH═CH—; r is 1 to 5; R7 is hydrogen, alkyl, Ar or Het; R8 is hydrogen or alkyl; R9 is oxo; or R8 and R9 taken together form —CH═CH—N═; R10 is alkyl, alkylcarbonyl, Ar, Ar-alkyl, Ar-carbonyl, Het1-alkyl or Het1-carbonyl.
    • 使用化合物制造用于治疗细菌感染的药物,只要细菌感染不是分枝杆菌感染,所述化合物是式(Ia)或(Ib)的化合物,N-氧化物,互变异构体 形式或其立体化学异构体形式,其中A-是抗衡离子; R 1是氢,卤素,卤代烷基,氰基,羟基,Ar,Het,烷基,烷氧基,烷硫基,烷氧基烷基,烷硫基烷基,芳烷基或二(Ar) p为1〜4; R2是氢,羟基,巯基,烷氧基,烷氧基烷氧基,烷硫基,一或二(烷基)氨基或其中Y是CH2,O,S,NH或N-烷基; R3是烷基,Ar,Ar-烷基,Het或Het-烷基; q为0〜4; R4和R5各自独立地为氢,烷基或苄基; 或R4和R5可以一起包括它们所连接的N; R 6是氢,卤素,卤代烷基,羟基,Ar,烷基,烷氧基,烷硫基,烷氧基烷基,烷硫基烷基,芳烷基或二(Ar) 或两个连位的R6基团可以一起形成-CH = CH-CH = CH-; r为1〜5; R7是氢,烷​​基,Ar或Het; R8是氢或烷基; R9是氧代; 或R8和R9一起形成-CH = CH-N =; R10是烷基,烷基羰基,Ar,Ar-烷基,Ar-羰基,Het1-烷基或Het1-羰基。
    • 7. 发明授权
    • Mycobacterial inhibitors
    • 分枝杆菌抑制剂
    • US07902225B2
    • 2011-03-08
    • US10596270
    • 2005-01-21
    • Jérôme Emile Georges GuillemontElisabeth Therese Jeanne PasquierDavid Francis Alain Lancois
    • Jérôme Emile Georges GuillemontElisabeth Therese Jeanne PasquierDavid Francis Alain Lancois
    • C07D215/38A61K31/04
    • C07D215/14C07D215/227C07D215/38C07D401/04C07D401/12C07D401/14C07D405/04C07D405/06C07D405/12C07D405/14C07D409/04C07D409/14
    • The present invention relates to novel substituted quinoline derivatives according to the general Formula (Ia) or the general Formula (Ib) the pharmaceutically acceptable acid or base addition salts thereof, the quaternary amines thereof, the stereochemically isomeric forms thereof the tautomeric forms thereof and the N-oxide forms thereof. The claimed compounds are useful for the treatment of mycobacterial diseases. In particular, compounds are claimed in which, independently from each other, R1 is halo; p=1; R2 is optionally substituted alkyloxy, alkyl, Ar, Het, or a radical of formula R3 is optionally substituted Ar or Het; q=1, R4 and R5 each independently are alkyl; R6 is hydrogen or a radical of formula r is equal to 0 or 1 and R7 is hydrogen or Ar. Also claimed is a composition comprising a pharmaceutically acceptable carrier and, as active ingredient, a therapeutically effective amount of the claimed compounds, the use of the claimed compounds or compositions for the manufacture of a medicament for the treatment of mycobacterial diseases and a process for preparing the claimed compounds.
    • 本发明涉及根据通式(Ia)或通式(Ib)的新的取代喹啉衍生物,其药学上可接受的酸或碱加成盐,其季胺,其互变异构形式的立体化学异构形式和 N-氧化物形式。 所要求保护的化合物可用于治疗分枝杆菌病。 特别地,要求保护的化合物,其中R1彼此独立地为卤素; p = 1; R 2是任选取代的烷氧基,烷基,Ar,Het或式R3的基团是任选取代的Ar或Het; q = 1,R4和R5各自独立地为烷基; R6是氢或式r的基团等于0或1,而R7是氢或Ar。 还要求保护的是包含药学上可接受的载体和作为活性成分的治疗有效量的要求保护的化合物的组合物,所要求保护的化合物或组合物在制备用于治疗分枝杆菌疾病的药物中的用途以及制备方法 要求保护的化合物。