[4-(6-HALO-7-SUBSTITUTED-2,4-DIOXO-1,4-DIHYDRO-2H-QUINAZOLIN-3-YL)-PHENYL]-5-CHLORO-THIOPHEN-2-YL-SULFONYLUREAS AND FORMS AND METHODS RELATED THERETO
    1.
    发明申请
    [4-(6-HALO-7-SUBSTITUTED-2,4-DIOXO-1,4-DIHYDRO-2H-QUINAZOLIN-3-YL)-PHENYL]-5-CHLORO-THIOPHEN-2-YL-SULFONYLUREAS AND FORMS AND METHODS RELATED THERETO 审中-公开
    [4-(6-卤代-7-取代的-2,4-二氧-1,4-二氢-2H-喹唑啉-3-基) - 苯基] -5-氯 - 噻吩-2-基 - 磺酰基脲 相关的方法

    公开(公告)号:WO2007056219A3

    公开(公告)日:2007-12-27

    申请号:PCT/US2006043093

    申请日:2006-11-03

    CPC classification number: C07D409/12

    Abstract: The present invention provides novel sulfonylurea compounds of formula (I) and pharmaceutically acceptable derivatives and polymorph and amorphous forms thereof. The compounds in their various forms are effective platelet ADP receptor inhibitors and may be used in various pharmaceutical compositions, and are particularly effective for the prevention and/or treatment of cardiovascular diseases, particularly those diseases related to thrombosis. The invention also provides a method for preparing such compounds and forms and for preventing or treating thrombosis and thrombosis related conditions in a mammal comprising the step of administering a therapeutically effective amount of a compound of formula (I) or a pharmaceutically acceptable salt or forms thereof.

    Abstract translation: 本发明提供了式(I)的新型磺酰脲化合物及其药学上可接受的衍生物和多晶型物及其无定形形式。 各种形式的化合物是有效的血小板ADP受体抑制剂,并且可以用于各种药物组合物中,并且特别有效用于预防和/或治疗心血管疾病,特别是与血栓形成相关的疾病。 本发明还提供了用于制备这些化合物和形式以及用于预防或治疗哺乳动物的血栓形成和血栓形成相关病症的方法,其包括施用治疗有效量的式(I)化合物或其药学上可接受的盐或其形式 。

    SUBSTITUTED-(QUINAZOLINYL)PHENYL THIOPHENYL-SULFONYLUREAS, METHODS FOR MAKING AND INTERMEDIATES THEREOF
    4.
    发明申请
    SUBSTITUTED-(QUINAZOLINYL)PHENYL THIOPHENYL-SULFONYLUREAS, METHODS FOR MAKING AND INTERMEDIATES THEREOF 审中-公开
    取代的(喹唑啉基)苯基噻吩基 - 磺酰基脲,其制备方法和中间体

    公开(公告)号:WO2007056167A2

    公开(公告)日:2007-05-18

    申请号:PCT/US2006042998

    申请日:2006-11-03

    CPC classification number: C07D409/12

    Abstract: The present invention provides sulfonylurea compounds of formula (VIII) and pharmaceutically acceptable derivatives thereof and a process for making thereof. The compounds in their various forms are effective platelet ADP receptor inhibitors and may be used in various pharmaceutical compositions, and are particularly effective for the prevention and/or treatment of cardiovascular diseases, particularly those diseases related to thrombosis. The invention also provides intermediate compounds useful in the process, as well as final products produced by the process, and salts or prodrugs thereof. The invention also provides a method for inhibition platelet ADP receptor and preventing or treating thrombosis and thrombosis related conditions in a mammal comprising the step of administering a therapeutically effective amount of a compound of formula (VIII) or a pharmaceutically acceptable salt or forms thereof.

    Abstract translation: 本发明提供了式(VIII)的磺酰脲化合物及其药学上可接受的衍生物及其制备方法。 各种形式的化合物是有效的血小板ADP受体抑制剂,并且可以用于各种药物组合物中,并且特别有效用于预防和/或治疗心血管疾病,特别是与血栓形成相关的疾病。 本发明还提供了用于该方法的中间体化合物,以及由该方法产生的最终产物,及其盐或前体药物。 本发明还提供了抑制血小板ADP受体并预防或治疗哺乳动物血栓形成和血栓形成相关病症的方法,其包括施用治疗有效量的式(VIII)化合物或其药学上可接受的盐或其形式的步骤。

    2,6-Diamino-pirimidin-5-il-carboxamidas como inhibidores de syk o JAK quinasas

    公开(公告)号:ES2546502T3

    公开(公告)日:2015-09-24

    申请号:ES09742982

    申请日:2009-04-16

    Abstract: Un compuesto que tiene la fórmula (I):**Fórmula** o uno de sus tautómeros o sales farmacéuticamente aceptables, en donde: D1 es fenilo sustituido con heteroarilo; cada E1 está seleccionado de modo independiente del grupo que consiste en alquilo C1-8, alquenilo C2-8, alquinilo C2-8, alcoxi C1-8, alquil C1-8-tio, aminocarbonilo, alcoxi C1-8-carbonil-alquileno C1-8, alcoxi C1-8-carbonil C1-8alcoxi C1-8, alcoxi C1-8-carbonilamino, oxo, halo, ciano, haloalquilo C1-8, haloalcoxi C1-8, aminosulfonilo, heteroarilsulfinilo; amino, hidroxilo, arilalquileno C1-8, fenilo, aminoalquilo C1-8, aminocicloalquilo C3-8, heterociclilo, heteroarilo, acilo C1-8, alquil C1-8 sulfonilo, acilamino y heterociclilalquileno C1-8; el subíndice n es 0, 1, 2, 3 ó 4; el resto:**Fórmula** es bien: (a)**Fórmula** y donde X e Y están seleccionados independientemente del grupo que consiste en: CH2, NH, NCOOH3 y S; (b) seleccionado del grupo que consiste en:**Fórmula** y donde cada R8a y R8b es independientemente H, hidroxilo, halo o si están en carbonos adyacentes, pueden combinarse con los átomos a los que están unidos para formar un anillo de benceno fusionado; y cada R9a y R9b es independientemente H, hidroxilo, halo o si están en carbonos adyacentes, pueden combinarse con los átomos a los que están unidos para formar un anillo de benceno fusionado; y la línea ondulada indica el punto de unión al resto de la molécula; o**Fórmula** (c) donde cada R8a y R8b es independientemente H o pueden combinarse con los átomos a los que están unidos para formar un anillo de benceno fusionado; y la línea ondulada indica el punto de unión al resto de la molécula; y "cicloalquilo" se refiere a un grupo hidrocarbonado mono o policíclico alifático, que puede formar un anillo con puente o un anillo espiro, y que puede tener uno o más enlaces dobles o triples.

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