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    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

    申请人： ABBOTT LABORATORIES

    发明人： Chu, Daniel T. ,  Plattner, Jacob J. ,  Klein, Larry L. ,  Shen, Linus L.

    IPC分类号： C07C333/06 ,  C07D513/04 ,  C07D519/00 ,  A61K31/435

    CPC分类号： C07D513/04 ,  C07C333/06 ,  C07C2601/02 ,  C07D513/14

    摘要： 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.

    摘要翻译： 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。

    Glaucoma treatment
    3.
    发明公开
    Glaucoma treatment 失效
    青光眼治疗

    公开(公告)号：EP0311012A3

    公开(公告)日：1990-07-11

    申请号：EP88116399.2

    申请日：1988-10-04

    申请人： ABBOTT LABORATORIES

    发明人： Stein, Herman H. ,  Crowley, Steven R. ,  Plattner, Jacob J.

    IPC分类号： A61K38/07

    CPC分类号： A61K38/553 ,  Y10S514/913 ,  Y10S530/86

    摘要： A method and a composition for treating or reducing and/or controlling intraocular pressure comprising administering an effective amount of a renin inhibiting compound of the formula:
    wherein A is a substituent; W is CO or CHOH and U is CH₂ or NR₂ wherein R₂ is hydrogen or loweralkyl; with the proviso that when W is CHOH then U is CH₂; R₁ is loweralkyl, cycloalkyl, benzyl, (alpha,­alpha)-dimethylbenzyl, 4-hydroxybenzyl, 4-methoxybenzyl, halobenzyl, (1-naphthyl)methyl, (2-naphthyl)methyl, (4-imidazoyl)methyl, phenethyl, 1-benzyloxyethyl, phenoxy, thiophenoxy or anilino; R₃ is loweralkyl, loweralkenyl, ((alkoxy)alkoxy)alkyl, carboxyalkyl, (thioalkoxy)alkyl, benzyl or heterocyclic ring substituted methyl; and R₄ is a substituted amino group; or pharmaceutically acceptable salts or esters thereof. Also disclosed are compositions, methods and kits for treating glaucoma or reducing and/or controlling intraocular pressure wherein the renin inhibiting compound is administered in combination with a beta-adrenergic antagonist, a steroidal antiinflammatory agent or an angiotensin converting enzyme inhibiting compound.

    摘要翻译： 用于治疗或减少和/或控制眼内压的方法和组合物，其包括施用有效量的下式的肾素抑制化合物：其中A是取代基; W是CO或CHOH，U是CH 2或NR 2，其中R 2是氢或低级烷基; 条件是当W是CHOH时，则U是CH 2; R 1是低级烷基，环烷基，苄基，（α，α-）二甲基苄基，4-羟基苄基，4-甲氧基苄基，卤代苄基，（1-萘基）甲基，（2-萘基）甲基，（4-咪唑基）甲基，苯乙基， 苄氧基乙基，苯氧基，硫代苯氧基或苯胺基; 低级链烯基，（（烷氧基）烷氧基）烷基，羧基烷基，（硫代烷氧基）烷基，苄基或杂环取代的甲基; 并且R 4是取代的氨基; 或其药学上可接受的盐或酯。 还公开了用于治疗青光眼或降低和/或控制眼内压的组合物，方法和试剂盒，其中肾素抑制化合物与β-肾上腺素能拮抗剂，甾体抗炎剂或血管紧张素转化酶抑制化合物组合施用。

    Tricyclic quinoline antineoplastic agents
    5.
    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

    申请人： ABBOTT LABORATORIES

    发明人： Chu, Daniel T. ,  Plattner, Jacob J. ,  Klein, Larry L. ,  Shen, Linus L.

    IPC分类号： C07C333/06 ,  C07D513/04 ,  C07D519/00 ,  A61K31/435

    CPC分类号： C07D513/04 ,  C07C333/06 ,  C07C2601/02 ,  C07D513/14

    摘要： 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.

    摘要翻译： 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。

    Glaucoma treatment
    8.
    发明公开
    Glaucoma treatment 失效
    Behandlung von Glaukom。

    公开(公告)号：EP0311012A2

    公开(公告)日：1989-04-12

    申请号：EP88116399.2

    申请日：1988-10-04

    申请人： ABBOTT LABORATORIES

    发明人： Stein, Herman H. ,  Crowley, Steven R. ,  Plattner, Jacob J.

    IPC分类号： A61K38/07

    CPC分类号： A61K38/553 ,  Y10S514/913 ,  Y10S530/86

    摘要： A method and a composition for treating or reducing and/or controlling intraocular pressure comprising administering an effective amount of a renin inhibiting compound of the formula:
    wherein A is a substituent; W is CO or CHOH and U is CH₂ or NR₂ wherein R₂ is hydrogen or loweralkyl; with the proviso that when W is CHOH then U is CH₂; R₁ is loweralkyl, cycloalkyl, benzyl, (alpha,­alpha)-dimethylbenzyl, 4-hydroxybenzyl, 4-methoxybenzyl, halobenzyl, (1-naphthyl)methyl, (2-naphthyl)methyl, (4-imidazoyl)methyl, phenethyl, 1-benzyloxyethyl, phenoxy, thiophenoxy or anilino; R₃ is loweralkyl, loweralkenyl, ((alkoxy)alkoxy)alkyl, carboxyalkyl, (thioalkoxy)alkyl, benzyl or heterocyclic ring substituted methyl; and R₄ is a substituted amino group; or pharmaceutically acceptable salts or esters thereof.
    Also disclosed are compositions, methods and kits for treating glaucoma or reducing and/or controlling intraocular pressure wherein the renin inhibiting compound is administered in combination with a beta-adrenergic antagonist, a steroidal antiinflammatory agent or an angiotensin converting enzyme inhibiting compound.

    摘要翻译： 一种用于治疗或减少和/或控制眼内压的方法和组合物，包括给予有效量的下列化学式的肾素抑制化合物：其中A是取代基的 W是CO或CHOH，U是CH 2或NR 2，其中R 2是氢或低级烷基; 条件是当W是CHOH时，则U是CH 2; R1是低级烷基，环烷基，苄基，（α，α） - 二甲基苄基，4-羟基苄基，4-甲氧基苄基，卤代苄基，（1-萘基）甲基，（2-萘基）甲基，（4-咪唑基）甲基，苯乙基 苄氧基乙基，苯氧基，硫代苯氧基或苯胺基; R3是低级烷基，低级烯基，（（烷氧基）烷氧基）烷基，羧基烷基，（硫代烷氧基）烷基，苄基或杂环取代的甲基; R4为取代氨基; 或其药学上可接受的盐或酯。 还公开了用于治疗青光眼或降低和/或控制眼内压的组合物，方法和试剂盒，其中肾素抑制化合物与β-肾上腺素能拮抗剂，甾族抗炎药或血管紧张素转化酶抑制化合物联合施用。