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    • 2. 发明授权
    • Quinoline derivatives
    • 喹啉衍生物
    • US06605616B1
    • 2003-08-12
    • US09621486
    • 2000-07-21
    • Anders BjörkStig JönssonTomas FexGunnar Hedlund
    • Anders BjörkStig JönssonTomas FexGunnar Hedlund
    • A61K314704
    • C07D215/56
    • The invention is related to compounds of general formula (I) wherein R is methyl, ethyl, n-propyl, iso-propyl, n-butyl or allyl; R′ is methyl, methoxy, fluoro, chloro, bromo, azido, trifluorometlhyl, or OCHxFy, wherein x=0−2, y=1−3 with the. proviso that x+y=3; R″ is hydrogen, fluoro or chloro; with the proviso that R″ is fluoro or chloro only when R′ is fluoro or chloro; R4 is hydrogen or pharmaceutically acceptable inorganic or organic cations; R5 is dimethylamino or nitro; R6 is hydrogen; and when R′ is azido R5 is also ethyl, n-propyl, iso-propyl, methoxy, ethoxy, chloro, bromo, trifluoromethyl, OCHxFy, wherein x=0−2, y=1−3 with the proviso that x+y=3, or R5 and R6 taken together are methylenedioxy; and any tautomer thereof. The invention also relates to pharmaceutical compositions containing a compound of the general formula (I) together with a pharmaceutically acceptable carrier. Included are also processes for the preparation of the compounds of formula (I), as well as methods for the treatment of mammals suffering from diseases resulting from autoimmunity and pathological inflammation by administering of a compound having the formula (I) to said mammal.
    • 本发明涉及通式(I)的化合物,其中R是甲基,乙基,正丙基,异丙基,正丁基或烯丙基; R'是甲基,甲氧基,氟,氯,溴,叠氮基,三氟甲基或OCH x Fy,其中x = 0-2,y = 1-3。 条件是x + y = 3; R“是氢,氟或氯; 条件是仅当R'为氟或氯时R“为氟或氯; R4是氢或药学上可接受的无机或有机阳离子; R5是二甲基氨基或硝基; R6是氢; 当R'为叠氮基时,R 5也是乙基,正丙基,异丙基,甲氧基,乙氧基,氯,溴,三氟甲基,OCH x Fy,其中x = 0-2,y = 1-3,条件是x + y = 3,或R5和R6一起是亚甲二氧基; 及其互变异构体。 本发明还涉及含有通式(I)的化合物与药学上可接受的载体的药物组合物。 还包括制备式(I)化合物的方法,以及通过向所述哺乳动物施用具有式(I)的化合物来治疗患有由自身免疫和病理性炎症引起的疾病的哺乳动物的方法。
    • 3. 发明授权
    • Drugs for the treatment of malignant tumors
    • US06395750B1
    • 2002-05-28
    • US09694757
    • 2000-10-24
    • Gunnar HedlundKarl JanssonStig JönssonAnders Björk
    • Gunnar HedlundKarl JanssonStig JönssonAnders Björk
    • A61K3147
    • A61K31/47C07D215/54C07D215/56
    • The invention relates to a method for the treatment of tumors in mammals by the administration of compounds of the general formula (I) wherein A is O41 or NR42 R43 wherein R41 is hydrogen or a pharmaceutically acceptable inorganic or organic cation, or CORA wherein RA is alkyl and aryl; R42 and R43 are hydrogen, C1-C4-alkyl, cyclopropyl, cyclopentyl or cyclohexyl; or R42 is benzyl or phenethyl, optionally mono- or disubstituted by methyl, iso-propyl methoxy, fluoro, chloro, bromo, dimethylamino, trifluoromethyl or nitro and R43 is hydrogen; or R42 and R43 form a 5- or 6-membered ring; or R42 is CORB wherein RB is alkyl or aryl, —CH2N(CH3)2 or —CH2CH2COOH or CORB is a 2-acyloxymethylbenzoyl group wherein RC is methyl, ethyl, phenyl or benzyl; R42 is COORD wherein RD is C1-C4-alkyl, phenyl or benzyl; or R42 is —CH2OCO-tert.-butyl or R42 is CONRFRG wherein RF and RG are C1-C4-alkyl; or R42 is CXNHRE wherein X is O or S and RE is C1-C4-alkyl, C2-C4-alkyl functionalized with an tertiary amino group, or phenyl, optionally functionalised with a p-chloro group; or R42 is CH2NRHRI wherein RH and RI are C1-C4-alkyl and RH and RI form a morpholine ring and R43 is hydrogen, C1-C2-alkyl or cyclopropyl; R is hydrogen, C1-C4-alkyl or allyl; with the proviso that R is not hydrogen when A is OR41; R′ is hydrogen, methyl, methoxy, fluoro, chloro, bromo, cyano, nitro, azido, trifluoromethyl, or OCHxFy, wherein x=0-2, y=1-3 with the proviso that x+y=3; and that R′ is not hydrogen when R is methyl and A is OR41; R″ is hydrogen, fluoro or chloro, with the proviso that R″ is fluoro or chloro only when R′ is fluoro or chloro; R5 is hydrogen, C1-C3-alkyl; methoxy, ethoxy, thio-C1-C3-alkyl fluoro, chloro, bromo, trifluoromethyl, nitro, amino, dimethylamino or OCHxFy, or OCH2CHxFy wherein x=0-2, y=1-3 with the proviso that x+y=3 and that R5 is not fluoro or amino when A is OR41; and that R5 is hydrogen only when A is NR42 R43 and R′ is trifluoromethyl; R6 is hydrogen; or R5 and R6 taken together are methylenedioxy, or any tautomer, optical isomer or racemate thereof. The invention also comprises novel compounds, therapeutic compositions and processes for the preparation of the compounds of formula I.