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    • 2. 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.
    • 8. 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。
    • 9. 发明授权
    • Vibrating tamper having a single control lever
    • 振动篡改具有单个控制杆
    • US06419420B2
    • 2002-07-16
    • US09726356
    • 2000-12-01
    • Gunnar Hedlund
    • Gunnar Hedlund
    • E01C1935
    • E01C19/36Y10T74/18936Y10T74/1896Y10T74/18992Y10T74/20213Y10T74/20396Y10T74/2042
    • The invention is directed to a vibrating tamper having a single control lever. The single control lever (4) can be set by an operator to any one of three releasably fixed positions with a snap-action detent device holding the control lever in the position selected by the operator. In the first position, the engine ignition is short-circuited, a fuel valve is closed, a fuel tank venting valve is closed and the throttle is fully closed. In the second position, the engine ignition circuit is enabled, the fuel tank venting valve is open, the fuel valve is open and the throttle control is in a starting/idling position. In the third position, the engine ignition circuit is enabled, the fuel tank venting valve is open, the fuel valve is open and the throttle control is in full-throttle position.
    • 本发明涉及具有单个控制杆的振动捣固器。 单个控制杆(4)可以由操作者设置为三个可释放地固定的位置中的任何一个,其中快动定位装置将控制杆保持在操作者选择的位置。 在第一位置,发动机点火被短路,燃料阀关闭,燃料箱排放阀关闭并且节流阀完全关闭。 在第二位置,启动发动机点火电路,燃油箱排气阀打开,燃油阀打开,油门控制处于启动/空转位置。 在第三位置,启动发动机点火电路,燃油箱排气阀打开,燃油阀打开,油门控制处于全油门位置。
    • 10. 发明授权
    • Quinoline derivatives
    • 喹啉衍生物
    • US6121287A
    • 2000-09-19
    • US352887
    • 1999-07-14
    • Anders BjorkStig JonssonTomas FexGunnar Hedlund
    • Anders BjorkStig JonssonTomas FexGunnar Hedlund
    • A61K31/47A61P29/00A61P37/02C07D215/56A61K31/4704C07D215/36
    • C07D215/56A61K31/47
    • The invention is related to compounds of general formula (I) ##STR1## wherein R is Me, Et, n-Pr, iso-Pr, n-Bu, iso-Bu, sec.-Bu or allyl; R' is hydrogen, Me, MeO, fluoro, chloro, brorno, CF.sub.3, or OCH.sub.x F.sub.y ; R" is hydrogen or fluoro, with the proviso that R" is fluoro when R' is fluoro; and further when R' and R" are both hydrogen, R is not Me; R.sub.4 is selected from hydrogen and pharmaceutically acceptable inorganic and organic cations; R.sub.5 is selected from MeS, EtS, n-PrS, iso-PrS, MeSO, EtSO, MeSO.sub.2 and EtSO.sub.2 ; wherein x=0-2, y=1-3 with the proviso that x+y=3; and Me is methyl, Et is ethyl, Pr is propsy and Bu is butyl; and any tautomer, optical isomer and racemate 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为Me,Et,n-Pr,异Pr,n-Bu,异-B Bu,sec.-Bu或烯丙基; R'是氢,Me,MeO,氟,氯,Brorno,CF 3或OCH x F y; R“是氢或氟,条件是当R'是氟时,R”是氟; 而且当R'和R“均为氢时,R不为Me; R4选自氢和药学上可接受的无机和有机阳离子; R5选自MeS,EtS,n-PrS,iso-PrS,MeSO,EtSO,MeSO2和EtSO2; 其中x = 0-2,y = 1-3,条件是x + y = 3; Me是甲基,Et是乙基,Pr是活检,Bu是丁基; 和其互变异构体,光学异构体和外消旋体。 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。