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14 条记录 (耗时 0.042 秒)

    Drugs for the treatment of malignant tumors
    1.
    发明授权
    Drugs for the treatment of malignant tumors 有权

    公开(公告)号：US06395750B1

    公开(公告)日：2002-05-28

    申请号：US09694757

    申请日：2000-10-24

    申请人： Gunnar Hedlund ,  Karl Jansson ,  Stig Jönsson ,  Anders Björk

    发明人： Gunnar Hedlund ,  Karl Jansson ,  Stig Jönsson ,  Anders Björk

    IPC分类号： A61K3147

    CPC分类号： A61K31/47 ,  C07D215/54 ,  C07D215/56

    摘要： 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.

    Quinoline derivatives
    3.
    发明授权
    Quinoline derivatives 有权
    喹啉衍生物

    公开(公告)号：US06605616B1

    公开(公告)日：2003-08-12

    申请号：US09621486

    申请日：2000-07-21

    申请人： Anders Björk ,  Stig Jönsson ,  Tomas Fex ,  Gunnar Hedlund

    发明人： Anders Björk ,  Stig Jönsson ,  Tomas Fex ,  Gunnar Hedlund

    IPC分类号： A61K314704

    CPC分类号： C07D215/56

    摘要： 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.

    摘要翻译： 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。

    Compositions containing quinoline compounds
    4.
    发明授权
    Compositions containing quinoline compounds 有权
    含有喹啉化合物的组合物

    公开(公告)号：US07589208B2

    公开(公告)日：2009-09-15

    申请号：US11050441

    申请日：2005-02-04

    申请人： Karl Jansson ,  Tomas Fristedt ,  Hans Wännman ,  Anders Björk

    发明人： Karl Jansson ,  Tomas Fristedt ,  Hans Wännman ,  Anders Björk

    IPC分类号： C07D215/38

    CPC分类号： A61K31/47 ,  A61K9/1617 ,  A61K9/2009 ,  A61K9/2013 ,  A61K9/2054 ,  A61K9/2059 ,  A61K31/4706

    摘要： A stable solid pharmaceutical composition consisting essentially of an effective amount of a salt of formula (II) together with an alkaline-reacting component maintaining the pH preferably above 8, or a salt with a divalent metal cation; and at least one pharmaceutical excipient; said salt of formula (II) being essentially stable during storage at room temperature for a period of at least 3 years. A process for stabilizing the salt of formula (II). A crystalline salt of formula (II) and a process for preparing said salt.

    摘要翻译： 一种稳定的固体药物组合物，其基本上由有效量的式（II）的盐与保持pH优选高于8的碱反应组分或与二价金属阳离子的盐组成; 和至少一种药物赋形剂; 所述式（II）的盐在室温下储存至少3年的时间基本上是稳定的。 稳定式（II）的盐的方法。 式（II）的结晶盐和制备所述盐的方法。

    Crystalline salts of quinoline compounds and methods for preparing them
    5.
    发明授权
    Crystalline salts of quinoline compounds and methods for preparing them 有权
    喹啉化合物的结晶盐及其制备方法

    公开(公告)号：US08314124B2

    公开(公告)日：2012-11-20

    申请号：US12405413

    申请日：2009-03-17

    申请人： Karl Jansson ,  Tomas Fristedt ,  Hans Wännman ,  Anders Björk

    发明人： Karl Jansson ,  Tomas Fristedt ,  Hans Wännman ,  Anders Björk

    IPC分类号： A61K9/28 ,  A61K31/4704 ,  C07D215/22

    CPC分类号： A61K31/4704 ,  A61K31/4706 ,  C07D215/56

    摘要： A stable solid pharmaceutical composition consisting essentially of an effective amount of a crystalline salt of formula (II) together with an alkaline-reacting component maintaining the pH preferably above 8, or a salt with a divalent metal cation; and at least one pharmaceutical excipient; said salt of formula (II) being essentially stable during storage at room temperature for a period of at least 3 years. A process for stabilizing the salt of formula (II). A crystalline salt of formula (II) and a process for preparing said salt.

    摘要翻译： 一种稳定的固体药物组合物，其基本上由有效量的式（II）的结晶盐与保持pH优选高于8的碱反应组分或与二价金属阳离子形成的盐组成; 和至少一种药物赋形剂; 所述式（II）的盐在室温下储存至少3年的时间基本上是稳定的。 稳定式（II）的盐的方法。 式（II）的结晶盐和制备所述盐的方法。

    Compounds
    6.
    发明授权
    Compounds 有权
    化合物

    公开(公告)号：US07553849B2

    公开(公告)日：2009-06-30

    申请号：US11152777

    申请日：2005-06-15

    申请人： Anders Björk ,  Karl Jansson

    发明人： Anders Björk ,  Karl Jansson

    IPC分类号： A61K31/4365 ,  C07D495/06

    CPC分类号： C07D495/04

    摘要： A compound of formula (I) wherein R is methyl, ethyl, n-propyl, iso-propyl, n-butyl or allyl; R′ is hydrogen, C1-C4 alkyl, C1-C3 alkoxy; halogen, trifluoromethyl or OCHxFy, R″ is hydrogen, fluoro or chloro, that R″ being fluoro or chloro only when R′ is fluoro or chloro; R3 is hydrogen or C1-C5 alkyl R4 is hydrogen, CH2OCOC(CH3)3, pharmaceutically acceptable inorganic or organic cations, or COR4′ wherein R4′ is C1-C5 alkyl, phenyl, benzyl or phenethyl; R7 is methyl or ethyl; one of A and B is sulphur and the other is C-R2; when A is S, R2 is selected from hydrogen and methyl, with the proviso that R2 is methyl only when R3 is not hydrogen; and when B is S, R2 is hydrogen; and any tautomer thereof. A pharmaceutical composition comprising a compound of formula (I), a method of treating malignant tumours or diseases resulting from autoimmunity or pathologic inflammation.

    摘要翻译： 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'是氢，C 1 -C 4烷基，C 1 -C 3烷氧基; 卤素，三氟甲基或OCH x F y，R“是氢，氟或氯，只有当R'是氟或氯时，R”是氟或氯; R3是氢或C1-C5烷基R4是氢，CH2OCOC（CH3）3，药学上可接受的无机或有机阳离子，或COR4'，其中R4'是C1-C5烷基，苯基，苄基或苯乙基; R7是甲基或乙基; A和B之一是硫，另一个是C-R2; 当A为S时，R2选自氢和甲基，条件是仅当R3不为氢时R2为甲基; 当B为S时，R 2为氢; 及其互变异构体。 一种药物组合物，其包含式（I）化合物，治疗恶性肿瘤的方法或由自身免疫或病理性炎症引起的疾病。

    Compositions containing quinoline compounds
    7.
    发明授权
    Compositions containing quinoline compounds 有权

    公开(公告)号：US07511143B2

    公开(公告)日：2009-03-31

    申请号：US11050441

    申请日：2005-02-04

    申请人： Karl Jansson ,  Tomas Fristedt ,  Hans Wännman ,  Anders Björk

    发明人： Karl Jansson ,  Tomas Fristedt ,  Hans Wännman ,  Anders Björk

    IPC分类号： C07D215/38

    摘要： A stable solid pharmaceutical composition consisting essentially of an effective amount of a salt of formula (II) together with an alkaline-reacting component maintaining the pH preferably above 8, or a salt with a divalent metal cation; and at least one pharmaceutical excipient; said salt of formula (II) being essentially stable during storage at room temperature for a period of at least 3 years. A process for stabilizing the salt of formula (II). A crystalline salt of formula (II) and a process for preparing said salt.

    Method and system for controlled cooling of small milk quantities
    8.
    发明授权
    Method and system for controlled cooling of small milk quantities 失效
    少量奶粉控制冷却方法和系统

    公开(公告)号：US06769261B2

    公开(公告)日：2004-08-03

    申请号：US10363911

    申请日：2003-09-29

    申请人： Mats Gustavsson ,  Anders Björk ,  Magnus Lidman

    发明人： Mats Gustavsson ,  Anders Björk ,  Magnus Lidman

    IPC分类号： F25D2312

    CPC分类号： A01J9/04

    摘要： A system for controlling the cooling of small milk quantities in a cooling tank (4). An agitation pipe (2) extended through a regular milk outlet (26) in a first end wall (6) of the tank is provided, having a nozzle end (32) for introducing incoming/re-circulated milk onto a milk cooling surface (14) at a predetermined position (dp). The position (dp) being situated (1) between a first end wall (6) and a central part of the tank (4) and laterally displaced (b) relative to the perpendicular central axis of the tank. The nozzle end (32) is directed towards a second end wall (8) of the tank (4). Agitation is performed by the agitation pipe (2) upon demand or when the milk quantity is insufficient for a regular agitator element (27) to work properly.

    摘要翻译： 一种用于控制冷却罐（4）中的小奶量冷却的系统。 提供了延伸穿过罐的第一端壁（6）中的正常牛奶出口（26）的搅拌管（2），其具有用于将进入/再循环的牛奶引入到牛奶冷却表面上的喷嘴端（32） 14）在预定位置（dp）。 位置（dp）位于第一端壁（6）和罐（4）的中心部分之间并且相对于罐的垂直中心轴线横向移位（b）（1）。 喷嘴端（32）指向罐（4）的第二端壁（8）。 根据需要通过搅拌管（2）进行搅拌，或当奶量不足以使常规搅拌器元件（27）正常工作时。

    Method, Computer Program Product and Milking Station for Initiating an Action to be Performed with Respect to a Milking Animal
    9.
    发明申请
    Method, Computer Program Product and Milking Station for Initiating an Action to be Performed with Respect to a Milking Animal 审中-公开
    方法，计算机程序产品和挤奶站，启动与挤奶动物相关的行动

    公开(公告)号：US20080109266A1

    公开(公告)日：2008-05-08

    申请号：US10556347

    申请日：2004-05-12

    申请人： Anders Björk ,  Susanne Granz

    发明人： Anders Björk ,  Susanne Granz

    IPC分类号： G06Q10/00 ,  A01J5/017

    CPC分类号： A01J5/007 ,  G06Q10/063

    摘要： A method includes the steps of recording milk yields (MY?1#191, MY?2#191, MY?N#191) from milkings of an udder quarter or udder of a milking animal; recording the times (t1, t2, . . . , tN) of the milkings; calculating milk secretion rates (MSR1, MSR2, . . . , MSRN) for said udder quarter or udder based on the milk yields and times; fitting a time dependent function (F(t)) to the calculated secretion rates, said time dependent function comprising one portion, which increases with time, and one portion, which decreases with time; estimating an expected milk secretion rate (EMSRt1+N) for said udder quarter or udder at a time (tN+1) following the last milking based on said function (F(t)); determining an expected milk yield (EMYtN+1) for said udder quarter or udder at said time based on the expected secretion rate and, at said time, the time period lapsed since last milking; and initiating an action to be performed with respect to said animal depending on said expected milk yield.

    摘要翻译： 一种方法包括从哺乳动物的乳房四分之一或乳房的乳汁中记录乳产量（MY≥1＃191，MY≥2＃191，MY≤N＃191）的步骤; 记录乳汁的时间（t 1> 1，t 2 2，...，t N N N）; 基于牛奶产量计算所述乳房季度或乳房的乳汁分泌率（MSR <1>，MSR 2>，...，MSR N N） 和时代 将时间依赖函数（F（t））拟合到所计算的分泌速率，所述时间依赖函数包括随时间增加的一部分和随时间减少的一部分; 基于所述功能估计在最后一次挤奶之后的时间（t N N + 1），所述乳房四分之一或乳房的预期乳分泌率（EMSR ） F（t））; 基于预期的分泌速率确定所述乳房季度或乳房在所述乳房季度或乳房的预期乳产量（EMYTN + 1N），并且在所述时间，自上次挤奶后经过的时间段; 并根据所述预期的产奶量开始相对于所述动物进行的动作。