Tricyclic quinoline antineoplastic agents
    1.
    发明公开
    Tricyclic quinoline antineoplastic agents 失效
    Dreizyklische Chinoline als antineoplastische Wirkstoffe。

    公开(公告)号:EP0424802A2

    公开(公告)日:1991-05-02

    申请号:EP90119985.1

    申请日:1990-10-18

    CPC classification number: C07D513/04 C07C333/06 C07C2601/02 C07D513/14

    Abstract: Isothiazolo-quinoline derivatives of the formula I which may exist as tautomers (formula II) are described which are cytotoxic for various tumor cell lines and are useful in the treatment of neoplastic diseases.
    wherein R is selected from (a) lower alkyl, (b) haloalkyl, (c) lowercycloalkyl, (d) alkylamino, (e) an aromatic heterocyclic group and (f) a phenyl group; W, X and Z are independently selected from hydrogen, halogen and lower alkyl; and Y is selected from a (a) phenyl group, (b) -NR₂R₃, (c) a bicyclic N-containing heterocyclic group, and (d) -OR₁₀, wherein R₁₀ is hydrogen, lower alkyl or a phenyl group;
    or any two of W, X, Y and Z taken together form a fused, substituted or unsubstituted, aromatic group or heterocyclic group.

    Abstract translation: 描述了可以以互变异构体(式II)存在的式I的异噻唑并喹啉衍生物,其对各种肿瘤细胞系是细胞毒性的,并且可用于治疗肿瘤性疾病。 其中R选自(a)低级烷基,(b)卤代烷基,(c)低级环烷基,(d)烷基氨基,(e)芳族杂环基和(f)苯基; W,X和Z独立地选自氢,卤素和低级烷基; 并且Y选自(a)苯基,(b)-NR2R3,(c)双环含氮杂环基和(d)-OR10,其中R10是氢,低级烷基或苯基; 或W,X,Y和Z中的任意两个一起形成稠合,取代或未取代的芳族基团或杂环基。

    Tricyclic quinoline antineoplastic agents
    2.
    发明公开
    Tricyclic quinoline antineoplastic agents 失效
    三环喹啉类抗肿瘤药物

    公开(公告)号:EP0424802A3

    公开(公告)日:1992-05-06

    申请号:EP90119985.1

    申请日:1990-10-18

    CPC classification number: C07D513/04 C07C333/06 C07C2601/02 C07D513/14

    Abstract: Isothiazolo-quinoline derivatives of the formula I which may exist as tautomers (formula II) are described which are cytotoxic for various tumor cell lines and are useful in the treatment of neoplastic diseases.
    wherein R is selected from (a) lower alkyl, (b) haloalkyl, (c) lowercycloalkyl, (d) alkylamino, (e) an aromatic heterocyclic group and (f) a phenyl group; W, X and Z are independently selected from hydrogen, halogen and lower alkyl; and Y is selected from a (a) phenyl group, (b) -NR₂R₃, (c) a bicyclic N-containing heterocyclic group, and (d) -OR₁₀, wherein R₁₀ is hydrogen, lower alkyl or a phenyl group;
    or any two of W, X, Y and Z taken together form a fused, substituted or unsubstituted, aromatic group or heterocyclic group.

    Abstract translation: 描述了可以互变异构体形式存在的式I异噻唑并喹啉衍生物(式II),其对各种肿瘤细胞系具有细胞毒性,并可用于治疗肿瘤疾病。 (a)低级烷基,(b)卤代烷基,(c)低级环烷基,(d)烷基氨基,(e)芳族杂环基和(f)苯基; W,X和Z独立地选自氢,卤素和低级烷基; (a)苯基,(b)-NR 2 R 3,(c)双环含N杂环基和(d)-OR 10,其中R 10是氢,低级烷基或苯基; 或者W,X,Y和Z中的任意两个一起形成稠合的取代或未取代的芳族基团或杂环基团。

    6-O-substituted ketolides having antibacterial activity
    4.
    发明公开
    6-O-substituted ketolides having antibacterial activity 失效
    具有抗菌活性的6-O-取代的酮内酯

    公开(公告)号:EP1291353A1

    公开(公告)日:2003-03-12

    申请号:EP02024560.1

    申请日:1997-09-02

    CPC classification number: C07H17/08 Y02P20/55

    Abstract: Antimicrobial compounds having the formula (II)as well as pharmaceutically acceptable salts, esters or prodrugs thereof; pharmaceutical compositions comprising such compounds; methods of treating bacterial infections by the administration of such compounds; and processes for the preparation of the compounds.

    Abstract translation: 具有式(II)的抗微生物化合物及其药学上可接受的盐,酯或前药; 包含此类化合物的药物组合物 通过施用这些化合物来治疗细菌感染的方法; 和制备这些化合物的方法。

    Process for the preparation of quinoline antibacterial compounds
    9.
    发明公开
    Process for the preparation of quinoline antibacterial compounds 失效
    Verfahren zur Herstellung von antibakteriellen Chinolin-Verbindungen。

    公开(公告)号:EP0350950A1

    公开(公告)日:1990-01-17

    申请号:EP89112960.3

    申请日:1989-07-14

    CPC classification number: C07D401/04

    Abstract: A process for preparing substituted 7-(piperazin-1-yl)-4-oxo-1,4-dihydro-3-quinoline carboxylic acid derivative antibacterial agents by reacting a carbamate protected piperazine derivative with a 7-halo-4-oxo-1,4-dihydro-quinoline carboxylic acid derivative.

    Abstract translation: 通过使氨基甲酸酯保护的哌嗪衍生物与7-卤代-4-氧代-1,4-二氢-3-喹啉羧酸衍生物抗菌剂反应制备取代的7-(哌嗪-1-基)-4-氧代-1,4-二氢-3-喹啉羧酸衍生物抗菌剂的方法, 1,4-二氢 - 喹啉羧酸衍生物。

    7-(2-Methyl-4-aminopyrrolidinyl)naphthyridine and quinoline compounds
    10.
    发明公开
    7-(2-Methyl-4-aminopyrrolidinyl)naphthyridine and quinoline compounds 失效
    7-(2-甲基-4-氨基吡咯烷基)萘啶和Chenolin-Verbindungen。

    公开(公告)号:EP0302371A2

    公开(公告)日:1989-02-08

    申请号:EP88112103.2

    申请日:1988-07-27

    CPC classification number: C07D401/04 C07D471/04 Y02P20/55

    Abstract: Naphthyridine and quinoline compounds having the formula:
    wherein A is CH or N; Z is an amine having the formula:
    R is o , p -difluorophenyl or p -fluorophenyl; and R₁ is hydrogen or a carboxy protecting group. The compounds of the invention have antibacterial activity and improved solubility and pharmacokinetic properties.

    Abstract translation: 萘啶和喹啉化合物,其具有下式:其中A是CH或N; Z是具有下式的胺: R是邻,对二氟苯基或对氟苯基; 并且R 1是氢或羧基保护基。 本发明的化合物具有抗菌活性和改善的溶解度和药代动力学性质。

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