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    Novel mycobacterial inhibitors
    1.
    发明申请
    Novel mycobacterial inhibitors 有权
    新型分枝杆菌抑制剂

    公开(公告)号：US20070082895A1

    公开(公告)日：2007-04-12

    申请号：US10596386

    申请日：2005-01-21

    申请人： Jerome Guillemont ,  Elisabeth Pasquier

    发明人： Jerome Guillemont ,  Elisabeth Pasquier

    IPC分类号： A61K31/541 ,  A61K31/5377 ,  C07D417/14 ,  C07D413/14

    CPC分类号： C07D413/06 ,  C07D413/14

    摘要： The present invention relates to novel substituted quinoline derivatives according to the general formula (Ia) or the general formula (Ib) salts, quaternary amines, stereochemically isomeric forms, tautomeric forms and N-oxide forms thereof, wherein R1 is hydrogen, halo, haloalkyl, cyano, hydroxy, Ar, Het, alkyl, alkyloxy, alkylthio, alkyloxyalkyl, alkylthioalkyl, Ar-alkyl or di(Ar)alkyl; p is 1, 2, 3 or 4; R2 is hydrogen, hydroxy, thio, alkyloxy, alkyloxyalkyloxy, alkylthio, mono or di(alkyl)amino or a radical of formula R3 is alkyl, Ar, Ar-alkyl, Het or Het-alkyl; R4 is hydrogen, alkyl or benzyl; R5 is hydrogen, halo, haloalkyl, hydroxy, Ar, alkyl, alkyloxy, alkylthio, alkyloxyalkyl, alkylthioalkyl, Ar-alkyl or di(Ar)alkyl; or two vicinal R5 radicals may be taken together to form together with the phenyl ring to which they are attached a naphthyl; r is 1, 2, 3, 4 or 5; R6 is hydrogen, alkyl, Ar or Het; R7 is hydrogen or alkyl; R8 is oxo; or R7 and R8 taken together form the radical CH═CH—N═; Z is CH2 or C(═O). The claimed compounds are useful for the treatment of mycobacterial diseases, particularly those diseases caused by pathogenic mycobacteria such as M. tuberculosis, M. bovis, M. avium, M. smegmatis and M. marinum. Also claimed is a pharmaceutical composition containing a compound of the present invention, 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.

    摘要翻译： 本发明涉及根据通式（Ia）或通式（Ib）的新的取代喹啉衍生物，其盐，季胺，立体化学异构形式，互变异构形式和N-氧化物形式，其中R 1， 烷基，烷氧基，烷硫基，烷氧基烷基，烷硫基烷基，芳烷基或二（Ar）烷基; p为1,2,3或4; R 2是氢，羟基，硫代，烷氧基，烷氧基烷氧基，烷硫基，一或二（烷基）氨基或式R 3的基团是烷基，Ar，Ar- 烷基，Het或Het-烷基; R 4是氢，烷基或苄基; R 5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）烷基; 或两个邻位R 5个基团可以与它们所连接的苯环一起形成萘基; r为1,2,3,4或5; R 6是氢，烷基，Ar或Het; R 7是氢或烷基; R 8是氧代; 或R 7和R 8一起形成基团CH-CH-N-; Z是CH 2或C（-O）。 所要求保护的化合物可用于治疗分枝杆菌疾病，特别是由致病性分枝杆菌引起的疾病如结核分枝杆菌，牛分枝杆菌，鸟分枝杆菌，耻垢分枝杆菌和马氏海马。 还要求保护的是含有本发明化合物，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的药物组合物及其制备方法。

    Novel mycobacterial inhibitors
    2.
    发明申请
    Novel mycobacterial inhibitors 有权
    新型分枝杆菌抑制剂

    公开(公告)号：US20070093478A1

    公开(公告)日：2007-04-26

    申请号：US10596270

    申请日：2005-01-21

    申请人： Jerome Guillemont ,  Elisabeth Pasquier ,  David Lancois

    发明人： Jerome Guillemont ,  Elisabeth Pasquier ,  David Lancois

    IPC分类号： A61K31/541 ,  A61K31/5377 ,  A61K31/496 ,  A61K31/4709 ,  C07D417/02 ,  C07D413/02 ,  C07D403/02

    CPC分类号： C07D215/14 ,  C07D215/227 ,  C07D215/38 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D405/04 ,  C07D405/06 ,  C07D405/12 ,  C07D405/14 ,  C07D409/04 ,  C07D409/14

    摘要： 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 tautomers 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 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.

    摘要翻译： 本发明涉及根据通式（Ia）或通式（Ib）的其取代的喹啉衍生物，其药学上可接受的酸或碱加成盐，其季胺，其互变异构体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R 1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R 3的基团是任选取代的Ar或Het; q = 1，R 4和R 5各自独立地为烷基; R 6是氢或式的基团等于0或1，R 7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。

    HIV INHIBITING 5-CARBO- OR HETEROCYCLYL SUBSTITUTED PYRIMIDINES
    8.
    发明申请
    HIV INHIBITING 5-CARBO- OR HETEROCYCLYL SUBSTITUTED PYRIMIDINES 有权

    公开(公告)号：US20070208022A1

    公开(公告)日：2007-09-06

    申请号：US11576068

    申请日：2005-09-29

    申请人： Jerome Guillemont ,  Jan Heeres ,  Paulus Lewi

    发明人： Jerome Guillemont ,  Jan Heeres ,  Paulus Lewi

    IPC分类号： A61K31/5377 ,  A61K31/53 ,  A61K31/506 ,  C07D403/02 ,  C07D413/02

    CPC分类号： C07D403/12 ,  C07D239/48 ,  C07D239/50 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/14 ,  C07D417/12

    摘要： HIV replication inhibitors of formula (I) N-oxides, a pharmaceutically acceptable addition salts, a quaternary amines or a stereoisomeric forms thereof, wherein -a1=a2-a3=a4- is —CH═CH—CH═CH—, —N═CH—CH═CH—, —N═CH—N═CH—, —N═CH—CH═N—, —N═N—CH═CH—; -b1=b2-b3=b4- is —CH═CH—CH═CH—, —N═CH—CH═CH—, —N═CH—N═CH—, —N═CH—CH═N—, —N═N—CH═CH—; R1 is hydrogen; aryl; formyl; C1-6alkylcarbonyl; optionally substituted C1-6alkyl; C1-6alkyloxycarbonyl; R2 is OH; halo; optionally substituted C1-6alkyl, C2-6alkenyl or C2-6alkynyl; substituted carbonyl; carboxyl; CN; nitro; amino; substituted amino; polyhalomethyl; polyhalo methylthio; —S(═O)rR6; C(═NH)R6; R2a is CN; amino; substituted amino; optionally substituted C1-6alkyl; halo; optionally substituted C2-6alkyloxy; substituted carbonyl; —CH═N—NH—C(═O)—R16; optionally substituted C1-6alkyloxy C1-6alkyl; substituted C2-6alkenyl or C2-6alkynyl; —C(═N—O—R8)—C1-4alkyl; R7 or —X3—R7; X1 is —NR1—, —O—, —C(═O)—, CH2, —CHOH—, —S—, —S(═O)r—; R3 is CN; amino; C1-6alkyl; halo; optionally substituted C1-6alkyloxy; substituted carbonyl; —CH═N—NH—C(═O)—R16; substituted C1-6alkyl; optionally substituted C1-6alkyloxy C1-6alkyl; substituted C2-6alkenyl or C2-6alkynyl; —C(═N—O—R8)—C1-4alkyl; R7; —X3—R7; R4 is halo; OH; optionally substituted C1-6alkyl, C2-6alkenyl or C2-6alkynyl; C3-7cycloalkyl; C1-6alkyloxy; CN; nitro; polyhalo C1-6alkyl; polyhalo C1-6alkyloxy; substituted carbonyl; formyl; amino; mono- or di(C1-4alkyl)amino or R7; R5 is —Y—CqH2q-L or —CqH2q—Y—CrH2r-L; L is aryl or Het; processes for the preparation of these compounds, pharmaceutical compositions comprising these compounds as active ingredient and the use of these compounds for the prevention or the treatment of HIV infection.