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    Novel compounds
    12.
    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

    Applicant: Anders Bjork ,  Karl Jansson

    Inventor： Anders Bjork ,  Karl Jansson

    IPC: A61K31/4743 ,  C07D498/02

    CPC classification number: C07D495/04

    Abstract: 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.

    Abstract translation: 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
    13.
    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

    Applicant: Gunnar Hedlund ,  Karl Jansson ,  Stig Jönsson ,  Anders Björk

    Inventor： Gunnar Hedlund ,  Karl Jansson ,  Stig Jönsson ,  Anders Björk

    IPC: A61K3147

    CPC classification number: A61K31/47 ,  C07D215/54 ,  C07D215/56

    Abstract: 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.

    Compensation for parasitic capacitance of a capacitive sensor
    14.
    发明授权
    Compensation for parasitic capacitance of a capacitive sensor 有权
    补偿电容传感器的寄生电容

    公开(公告)号：US08446158B1

    公开(公告)日：2013-05-21

    申请号：US12267487

    申请日：2008-11-07

    Applicant: Håkan Karl Jansson

    Inventor： Håkan Karl Jansson

    IPC: G01R27/08 ,  G01R35/00

    CPC classification number: H03K17/9622 ,  G06F3/0418 ,  G06F3/044 ,  H03K2217/94031 ,  H03K2217/960715 ,  H03K2217/960725

    Abstract: An apparatus for converting a capacitance measured on a capacitive sensor to a digital code may include a modulation capacitor to receive charge transferred from the sensor and compensation circuitry to divert charge from the modulation capacitor. A method for operating the apparatus may include generating a digital bitstream based on the capacitance of the sensor and compensating for a parasitic capacitance of the capacitive sensor.

    Abstract translation: 用于将在电容传感器上测量的电容转换为数字代码的装置可以包括用于接收从传感器传送的电荷的调制电容器和用于从调制电容器转移电荷的补偿电路。 用于操作该装置的方法可以包括基于传感器的电容产生数字比特流并补偿电容式传感器的寄生电容。

    Crystalline salts of quinoline compounds and methods for preparing them
    15.
    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

    Applicant: Karl Jansson ,  Tomas Fristedt ,  Hans Wännman ,  Anders Björk

    Inventor： Karl Jansson ,  Tomas Fristedt ,  Hans Wännman ,  Anders Björk

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

    CPC classification number: A61K31/4704 ,  A61K31/4706 ,  C07D215/56

    Abstract: 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.

    Abstract translation: 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。

    Stable laquinimod preparations
    17.
    发明授权
    Stable laquinimod preparations 有权
    稳定的laquinimod制剂

    公开(公告)号：US08178127B2

    公开(公告)日：2012-05-15

    申请号：US12317104

    申请日：2008-12-19

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

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

    IPC: A61K9/20

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

    Abstract: 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.

    Abstract translation: 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。

    Compounds
    18.
    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

    Applicant: Anders Björk ,  Karl Jansson

    Inventor： Anders Björk ,  Karl Jansson

    IPC: A61K31/4365 ,  C07D495/06

    CPC classification number: C07D495/04

    Abstract: 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.

    Abstract translation: 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
    19.
    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

    Applicant: Karl Jansson ,  Tomas Fristedt ,  Hans Wännman ,  Anders Björk

    Inventor： Karl Jansson ,  Tomas Fristedt ,  Hans Wännman ,  Anders Björk

    IPC: C07D215/38

    Abstract: 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.

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