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    Compositions containing quinoline compounds
    3.
    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。

    Process for the manufacture of quinoline derivatives
    4.
    发明授权
    Process for the manufacture of quinoline derivatives 有权
    制备喹啉衍生物的方法

    公开(公告)号：US06875869B2

    公开(公告)日：2005-04-05

    申请号：US10459718

    申请日：2003-06-12

    申请人： Karl Jansson

    发明人： Karl Jansson

    IPC分类号： C07D215/56 ,  C07D491/00 ,  C07D215/16 ,  C07D215/20 ,  C07D498/00 ,  C07D515/00

    CPC分类号： C07D215/56

    摘要： A process for the preparation of the compounds of general formula (I) wherein R is selected from methyl, ethyl, n-propyl, iso-propyl, n-butyl, iso-butyl, sec.-butyl and allyl; R5 is selected from the methyl, ethyl, n-propyl, iso-propyl, methoxy, ethoxy, methylthio, ethylthio, n-propylthio, methylsulphinyl, ethylsulphinyl, fluoro, chloro, bromo, trifluoromethyl, and OCHxFy; wherein x=0-2, y=1-3 with the proviso that x+y=3; R6 is hydrogen; or R5 and R6 taken together are methylenedioxy; R′ is selected from methyl, methoxy, fluoro, chloro, bromo, trifluoromethyl, and OCHxFy, wherein x=0-2, y=1-3 with the proviso that x+y=3; R″ is selected form hydrogen, fluoro and chloro, with the proviso that R″ is selected from fluoro and chloro only when R′ is selected from fluoro and chloro; by reacting a quinoline-3-carboxylic acid ester derivative of formula A with an aniline derivative of formula B in a solvent selected from straight or branched alkanes and cycloalkanes or mixtures thereof with a boiling point between 80 and 200° C.

    摘要翻译： 制备通式（I）的化合物的方法，其中R选自甲基，乙基，正丙基，异丙基，正丁基，异丁基，仲丁基和烯丙基; R5选自甲基，乙基，正丙基，异丙基，甲氧基，乙氧基，甲硫基，乙硫基，正丙硫基，甲基亚磺酰基，乙基亚磺酰基，氟，氯，溴，三氟甲基和OCH x Fy; 其中x = 0-2，y = 1-3，条件是x + y = 3; R6是氢; 或R5和R6一起是亚甲二氧基; R'选自甲基，甲氧基，氟，氯，溴，三氟甲基和OCH x Fy，其中x = 0-2，y = 1-3，条件是x + y = 3; R“选自氢，氟和氯，条件是当R'选自氟和氯时，R”选自氟和氯; 通过使式A的喹啉-3-羧酸酯衍生物与式Bin的苯胺衍生物使选自直链或支链烷烃和环烷烃的溶剂或其混合物的沸点为80-200℃。

    CRYSTALLINE SALTS OF QUINOLINE COMPOUNDS AND METHODS FOR PREPARING THEM
    5.
    发明申请
    CRYSTALLINE SALTS OF QUINOLINE COMPOUNDS AND METHODS FOR PREPARING THEM 有权
    喹啉化合物的晶体沉淀及其制备方法

    公开(公告)号：US20090232889A1

    公开(公告)日：2009-09-17

    申请号：US12405413

    申请日：2009-03-17

    申请人： Karl Jansson ,  Tomas Fristedt ,  Hans Wannman ,  Anders Bjork

    发明人： Karl Jansson ,  Tomas Fristedt ,  Hans Wannman ,  Anders Bjork

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

    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。

    Process for the manufacture of quinoline derivatives
    6.
    发明授权
    Process for the manufacture of quinoline derivatives 有权
    制备喹啉衍生物的方法

    公开(公告)号：US07560557B2

    公开(公告)日：2009-07-14

    申请号：US11084192

    申请日：2005-03-21

    申请人： Karl Jansson

    发明人： Karl Jansson

    IPC分类号： C07D215/00

    CPC分类号： C07D215/56

    摘要： A process for the preparation of the compounds of general formula (I) wherein R is selected from methyl, ethyl, n-propyl, iso-propyl, n-butyl, iso-butyl, sec.-butyl and allyl; R5 is selected from methyl, ethyl, n-propyl, iso-propyl, methoxy, ethoxy, methylthio, ethylthio, n-propylthio, methylsulphinyl, ethylsulphinyl, fluoro, chloro, bromo, trifluoromethyl, and OCHxFy; wherein x=0-2, y=1-3 with the proviso that x+y=3; R6 is hydrogen; or R5 and R6 taken together are methylenedioxy; R′ is selected from hydrogen, methyl, methoxy, fluoro, chloro, bromo, trifluoromethyl, and OCHxFy, wherein x=0-2, y=1−3 with the proviso that x+y=3; R″ is selected from hydrogen, fluoro and chloro, with the proviso that R″ is selected from fluoro and chloro only when R′ is selected from fluoro and chloro; by reacting a quinoline-3-carboxylic acid ester derivative of formula A, where Z is methyl, with an aniline derivative of formula B according to the following reaction diagram, to give the compound of general formula (I), designated “C”, and an alcohol, designated “D”. in a solvent selected from straight or branched alkanes and cycloalkanes or mixtures thereof with a boiling point between 80 and 200° C.

    摘要翻译： 制备通式（I）的化合物的方法，其中R选自甲基，乙基，正丙基，异丙基，正丁基，异丁基，仲丁基和烯丙基; R5选自甲基，乙基，正丙基，异丙基，甲氧基，乙氧基，甲硫基，乙硫基，正丙硫基，甲基亚磺酰基，乙基亚磺酰基，氟，氯，溴，三氟甲基和OCH x Fy; 其中x = 0-2，y = 1-3，条件是x + y = 3; R6是氢; 或R5和R6一起是亚甲二氧基; R'选自氢，甲基，甲氧基，氟，氯，溴，三氟甲基和OCH x Fy，其中x = 0-2，y = 1-3，条件是x + y = 3; R“选自氢，氟和氯，条件是当R'选自氟和氯时，R”选自氟和氯; 通过根据下列反应图使Z为甲基的式A的喹啉-3-羧酸酯衍生物与式B的苯胺衍生物反应，得到标题为“C”的通式（I）的化合物， 和称为“D”的酒精。 在选自直链或支链烷烃和环烷烃或其混合物的溶剂中，沸点在80和200℃之间。

    Novel compounds
    8.
    发明申请
    Novel compounds 有权
    新型化合物

    公开(公告)号：US20060004038A1

    公开(公告)日：2006-01-05

    申请号：US11152777

    申请日：2005-06-15

    申请人： Anders Bjork ,  Karl Jansson

    发明人： Anders Bjork ,  Karl Jansson

    IPC分类号： A61K31/4743 ,  C07D498/02

    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 3，X“，R”是氢，氟或氯，只有当R'是氟或氯时，R“是氟或氯; R 3是氢或C 1 -C 5烷基R 4是氢，CH 2， 其中R 4，R 3，R 3，R 3，R 3，R 3，R 3， C 1 -C 6烷基，苯基，苄基或苯乙基; R 7是甲基或乙基; A和B之一是硫，另一个是C-R 2; 当A为S时，R 2选自氢和甲基，条件是R 3仅在R 3不为氢时为甲基 ; 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。

    Drugs for the treatment of malignant tumors
    9.
    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.

    Stable laquinimod preparations
    10.
    发明授权
    Stable laquinimod preparations 有权
    稳定的laquinimod制剂

    公开(公告)号：US08545885B2

    公开(公告)日：2013-10-01

    申请号：US13471175

    申请日：2012-05-14

    申请人： Muhammad Safadi ,  Daniella Licht ,  Ioana Lovinger ,  Aharon M. Eyal ,  Tomas Fristedt ,  Karl Jansson

    发明人： Muhammad Safadi ,  Daniella Licht ,  Ioana Lovinger ,  Aharon M. Eyal ,  Tomas Fristedt ,  Karl Jansson

    IPC分类号： A61K9/20

    CPC分类号： B65B25/00 ,  A61K9/1623 ,  A61K9/2004 ,  A61K9/2018 ,  A61K31/438 ,  A61K31/4704 ,  C07D209/34 ,  C07D209/42 ,  C07D471/10 ,  Y10T436/145555

    摘要： The subject invention provides a pharmaceutical composition comprising N-ethyl-N-phenyl-1,2,-dihydro-4-hydroxy-5-chloro-1-methyl-2-oxoquinoline-3-carboxamide or the salt thereof; a pharmaceutically acceptable carrier; and not more than 0.5% w/w relative to N-ethyl-N-phenyl-1,2,-dihydro-4-hydroxy-5-chloro-1-methyl-2-oxoquinoline-3-carboxamide of 2-Chloro-6-(1-ethyl-N-methyl-2-oxoindoline-3-carboxamido)benzoic acid, 1H,3H-spiro[5-chloro-1-methylquinoline-2,4-dione-3,3′-[1]ethylindolin-[2]-one], or 5-Chloro-N-ethyl-3-hydroxy-1-methyl-2,4-dioxo-N-phenyl-1,2,3,4-tetrahydro-quinoline-3-carboxamide.

    摘要翻译： 本发明提供了包含N-乙基-N-苯基-1,2-二氢-4-羟基-5-氯-1-甲基-2-氧代喹啉-3-甲酰胺或其盐的药物组合物; 药学上可接受的载体; 并且相对于2-氯 - 苯基-1,2-二氢-4-羟基-5-氯-1-甲基-2-氧代喹啉-3-甲酰胺，相对于N-乙基-N-苯基-1,2-二氢-4-羟基-5-氯-1-甲基-2-氧代喹啉-3-甲酰胺为0.5％w / 6-（1-乙基-N-甲基-2-氧代二氢吲哚-3-甲酰氨基）苯甲酸，1H，3H-螺[5-氯-1-甲基喹啉-2,4-二酮-3,3' - [1] 乙醛基 - [2] - 酮]或5-氯-N-乙基-3-羟基-1-甲基-2,4-二氧代-N-苯基-1,2,3,4-四氢 - 甲酰胺。