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    • 5. 发明授权
    • Quinoline derivatives as antibacterial agents
    • 喹啉衍生物作为抗菌剂
    • US07709498B2
    • 2010-05-04
    • US11296918
    • 2005-12-08
    • Koenraad Jozef Lodewijk Marcel AndriesAnil KoulJérôme Emile Georges GuillemontElisabeth Therese Jeanne Pasquier
    • Koenraad Jozef Lodewijk Marcel AndriesAnil KoulJérôme Emile Georges GuillemontElisabeth Therese Jeanne Pasquier
    • C07D215/38
    • C07D215/227A61K31/47A61K31/4709A61K31/496A61K31/497A61K31/501A61K31/506A61K31/53A61K31/5377A61K31/541C07D215/36C07D401/04C07D401/06C07D401/12C07D405/04C07D405/06C07D409/06Y02A50/473
    • The present invention relates to a method for the treatment of a bacterial infection comprising administering a therapeutically effective amount of a compound of formula or 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 to bacterial infection is other than a Mycobacterial infection.
    • 本发明涉及一种治疗细菌感染的方法,包括给予治疗有效量的式的化合物或其药学上可接受的酸或碱加成盐,其立体化学异构形式或其N-氧化物形式,其中 R 1是氢,卤素,多卤代C 1-6烷基,C 1-6烷基,Ar或Het; p是等于1或2的整数; R2是C1-6烷氧基,C1-6烷氧基C1-6烷氧基或C1-6烷硫基; R3是Ar,Het或Het1; R 4和R 5各自独立地为氢,C 1-6烷基或苄基; 或R4和R5一起并且包括它们所连接的N可以形成选自吡咯烷基,2-吡咯啉基,3-吡咯啉基,吡咯基,咪唑烷基,吡唑烷基,2-咪唑啉基,2-吡唑啉基,咪唑基,吡唑基 三唑基,哌啶基,吡啶基,哌嗪基,哒嗪基,嘧啶基,吡嗪基,三嗪基,吗啉基和硫代吗啉基,每个所述环可任选被C 1-6烷基,卤素,多卤代C 1-6烷基,羟基,羟基C 1-6烷基,C 1-6烷氧基, 氨基,单或二(C 1-6烷基)氨基,C 1-6烷硫基,C 1-6烷氧基C 1-6烷基,C 1-6烷硫基C 1-6烷基或嘧啶基; R 6是氢,卤素,多卤代C 1-6烷基,C 1-6烷基,C 1-6烷氧基,C 1-6烷硫基; 或两个连位的R6基团可以一起形成式-CH = CH-CH = CH-的二价基团; r是等于1或2的整数; R7是氢,C1-6烷基,Ar,Het或Het1; 只要细菌感染不是分枝杆菌感染。