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    Inhibiting lipoxygenase with pyrazolone derivatives
    8.
    发明授权
    Inhibiting lipoxygenase with pyrazolone derivatives 失效
    用吡唑啉酮衍生物抑制脂氧合酶

    公开(公告)号：US4670460A

    公开(公告)日：1987-06-02

    申请号：US808582

    申请日：1985-12-13

    申请人： Mithat Mardin ,  Friedel Seuter ,  Elisabeth Perzborn ,  Klaus Schlossmann ,  Dieter Mayer ,  Volker Fiedler

    发明人： Mithat Mardin ,  Friedel Seuter ,  Elisabeth Perzborn ,  Klaus Schlossmann ,  Dieter Mayer ,  Volker Fiedler

    IPC分类号： A61K31/415

    CPC分类号： A61K31/415

    摘要： A method of inhibiting lipoxygenase in a patient, for the prophylaxis and/or treatment of ischaemias and disorders in cardiac rhythm, inflammations of the skin and the eye, and of rheumatic, allergic and asthmatic diseases, oedemas, pulmonary embolisms, pulmonary hypertension, shock lung, oxygen intoxications and ulcerations which comprises administering to such patient an effective amount of a compound of the formula ##STR1## wherein R represents an aryl or heteroaryl radical which has 6 to 12 C atoms and optionally contains 1 to 3 identical or different substituents from the group comprising halogen, trifluoromethyl, alkyl, alkenyl, alkoxy, alkylamino, cyano, trifluoromethoxy, nitro, hydroxyl, SO.sub.n -alkyl (n=0 to 2) or SO.sub.n -trifluoromethyl (n=0 to 2), alkyl, alkenyl and alkoxy in each case being understood as meaning radicals with 1 to 4 C atoms,R.sup.1 represents hydrogen or a hydrocarbon radical which has 1 to 18 C atoms and optionally contains a hydroxyl, ether, ester or carboxyl group and optionally 1 to 3 halogen atoms,R.sup.2 has the meaning of R.sup.1 or represents radical ##STR2## R.sup.3 represents hydrogen or an acyl or sulphonyl radical with in each case 1 to 15 C atoms andX represents one of the groups --O--CH.sub.2 --CH.sub.2 --, --S--CH.sub.2 --CH.sub.2 --, --CH.sub.2 --CH.sub.2 --CH.sub.2 --, --CH.sub.2 --CH.sub.2 --, --CH.sub.2 or ##STR3## the oxygen or sulphur atom being bonded to the radical R, and with the provisio that X does not represent --O--CH.sub.2 --CH.sub.2 -- if R=.beta.-naphthyl, R.sup.1 =CH.sub.3 and R.sup.2 =R.sup.3 =H.

    摘要翻译： 一种在患者体内抑制脂氧合酶的方法，用于预防和/或治疗心脏节律，皮肤和眼睛炎症以及风湿性，过敏性和哮喘性疾病，oedemas，肺栓塞，肺动脉高压，休克 肺，氧中毒和溃疡，其包括向此类患者施用有效量的式（I）化合物，其中R表示具有6至12个C原子并且任选地含有1至3个相同或相同或相同的1至3个的芳基或杂芳基， 硝基，羟基，SO1-烷基（n = 0至2）或SO 3 - 三氟甲基（n = 0至2）的不同取代基，烷基，环烷基， 烯基和烷氧基在每种情况下被理解为含有1至4个C原子的基团，R 1表示氢或具有1至18个C原子并且任选地含有羟基，醚，酯或羧基的烃基 p和任选的1至3个卤素原子，R 2具有R 1的含义或表示基团R 3表示氢或酰基或磺酰基，在每种情况下为1至15个C原子，X表示基团-O-CH 2 -CH 2 - ， - CH 2 -CH 2 - ， - CH 2 -CH 2 - ， - CH 2 -CH 2 - ， - CH 2或者 - 或者与基团R键合的氧原子或硫原子， 如果R =β-萘基，R1 = CH3，R2 = R3 = H，则不表示-O-CH2-CH2-。

    1H-pyrido-(2,3-b) (1,4)-thiazines
    10.
    发明授权
    1H-pyrido-(2,3-b) (1,4)-thiazines 失效
    1H-吡啶并（2,3-b）（1,4） - 噻嗪

    公开(公告)号：US4861878A

    公开(公告)日：1989-08-29

    申请号：US927909

    申请日：1986-11-06

    申请人： Gerd Fengler ,  Alexander Klausener ,  Hans-Josef Buysch ,  Mithat Mardin ,  Bernhard Pelster

    发明人： Gerd Fengler ,  Alexander Klausener ,  Hans-Josef Buysch ,  Mithat Mardin ,  Bernhard Pelster

    IPC分类号： A61K31/54 ,  A61P11/00 ,  A61P29/00 ,  A61P37/08 ,  C07D513/04

    CPC分类号： C07D513/04

    摘要： New potent lipoxygenase inhibitors which are 1H-pyrido-[2,3-b][1,4] thiazines are disclosed. The new thiazines are of the formula ##STR1## in which R.sup.1 denotes hydrogen, halogen, optionally substituted alkyl or alkoxy or the group ##STR2## in which R.sup.5 and R.sup.6 are identical or different and denote hydrogen, optionally substituted alkyl or aryl, or can be linked to form a 5- or 6-membered heterocyclic ring,R.sup.2 and R.sup.3 are identical or different and denote hydrogen or optionally substituted alkyl or alkoxy andR.sup.4 denotes hydroxyl, the group ##STR3## in which R.sup.5 and R.sup.6 have the abovementioned meaning, or, in the case where R.sup.3 denotes hydrogen or optionally substituted alkoxy, also denotes optionally substituted alkoxy.

    摘要翻译： 公开了新的有效的脂氧合酶抑制剂，它们是1H-吡啶并[2,3-b] [1,4]噻嗪。 新的噻嗪类具有式“IMAGE”，其中R 1表示氢，卤素，任选取代的烷基或烷氧基或其中R 5和R 6相同或不同并表示氢，任选取代的烷基或芳基或可以 连接形成5-或6-元杂环，R2和R3相同或不同，表示氢或任选取代的烷基或烷氧基，R4表示羟基，其中R5和R6具有上述含义的基团 或者在R3表示氢或任选取代的烷氧基的情况下，也表示任选取代的烷氧基。