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    2,4-dioxo-3-quinazolinylaryl sulfonylureas
    1.
    发明授权
    2,4-dioxo-3-quinazolinylaryl sulfonylureas 失效
    2,4-二氧代-3-喹唑啉基芳基磺酰脲

    公开(公告)号：US07109332B2

    公开(公告)日：2006-09-19

    申请号：US10956004

    申请日：2004-09-29

    申请人： Robert M. Scarborough ,  Wolin Huang ,  Anjali Pandey ,  Shawn M. Bauer ,  Xiaoming Zhang ,  Zhaozhong J. Jia

    发明人： Robert M. Scarborough ,  Wolin Huang ,  Anjali Pandey ,  Shawn M. Bauer ,  Xiaoming Zhang ,  Zhaozhong J. Jia

    IPC分类号： C07D409/12 ,  C07D409/14 ,  A61K31/517 ,  A61P7/02

    CPC分类号： C07D409/12 ,  C07D409/14

    摘要： 2,4-Dioxo-3-quinazolinylaryl sulfonylurea compounds having the formula: wherein R is a member selected from the group consisting of H and C1-6 alkyl; R1 is a member selected from the group consisting of H, C1-6 alkyl, C1-6 haloalkyl, C3-5 cycloalkyl and C3-5 cycloalkyl-alkyl; R2 is a member selected from the group consisting of H, halogen, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C1-6 alkoxy, cyano and —C(O)R2a, wherein R2a is a member selected from the group consisting of C1-6 alkoxy and (C1-6 alkyl)0-2 amino; L is a 1 to 3 carbon linking group selected from the group consisting of —CH2—, —CH(CH3)—, —CH2CH2—, —CH2CH(CH3)— and —CH2CH2CH2—; L1 is a linking group selected from the group consisting of a bond and —CH2—; L2 is a linking group selected from the group consisting of a bond, —NH— and —CH2—; and Ar1 is an aromatic ring selected from the group consisting of benzene, pyridine and pyrimidine; are provided. The compounds are useful for the inhibition of ADP-platelet aggregation, particularly in the treatment of thrombosis and thrombosis related conditions or disorders.

    摘要翻译： 2,4-二氧代-3-喹唑啉基芳基磺酰脲类化合物，其具有下式：其中R是选自H和C 1-6烷基的成员; R 1是选自H，C 1-6烷基，C 1-6卤代烷基，C 1 -C 6烷基，C 1 -C 6烷基， 3-5个环烷基和C 3-5环烷基 - 烷基; R 2是选自H，卤素，C 1-6 - 烷基，C 2-6 - 烯基，C 1 -C 6烷基， C 1-6烷基，C 1-6烷氧基，氰基和-C（O）R 2a， 其中R 2a是选自C 1-6烷氧基和（C 1-6烷基）烷基的成员， 0-2氨基; L是选自-CH 2 - ， - CH（CH 3 CH 3） - ， - CH 2 - ， - CH 2 CH 2（CH 3 CH 3） - 和-CH 2 CH 2 CH 2 - ; L 1是选自键和-CH 2 - 的连接基团。 L 2是从由-NH-和-CH 2 - 的键组成的组中的连接基团。 和Ar 1是选自苯，吡啶和嘧啶的芳环; 被提供。 该化合物可用于抑制ADP-血小板聚集，特别是在治疗血栓形成和血栓相关病症或病症中。

    [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
    7.
    发明授权
    [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 有权
    [4-（6-卤代-7-取代-2,4-二氧代-1,4-二氢-2H-喹唑啉-3-基） - 苯基] -5-氯 - 噻吩-2-基 - 磺酰脲，形成和 与之相关的方法

    公开(公告)号：US08058284B2

    公开(公告)日：2011-11-15

    申请号：US11556490

    申请日：2006-11-03

    申请人： Robert Scarborough ,  Carroll Anna Scarborough, legal representative ,  Wolin Huang ,  Mukund Mehrotra ,  Xiaoming Zhang ,  Hilary Cannon ,  Craig M. Grant

    发明人： Robert Scarborough ,  Wolin Huang ,  Mukund Mehrotra ,  Xiaoming Zhang ,  Hilary Cannon ,  Craig M. Grant

    IPC分类号： A61K31/517 ,  C07D409/12

    CPC分类号： C07D409/12

    摘要： 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.

    摘要翻译： 本发明提供式（I）的新型磺酰脲化合物及其药学上可接受的衍生物及其多晶型物和无定形形式。 各种形式的化合物是有效的血小板ADP受体抑制剂，可用于各种药物组合物中，并且特别有效预防和/或治疗心血管疾病，特别是与血栓形成有关的疾病。 本发明还提供了一种制备此类化合物和形式并用于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，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的步骤 。

    [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
    8.
    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 有权
    [4-（6-羟基-7-取代-2,4-二氧代-1,4-二氢-2H-喹唑啉-3-基） - 苯基] -5-氯代 - 噻吩-2-基] - 磺酰基和形式 方法相关

    公开(公告)号：US20070123547A1

    公开(公告)日：2007-05-31

    申请号：US11556490

    申请日：2006-11-03

    申请人： Robert Scarborough ,  Wolin Huang ,  Mukund Mehrotra ,  Xiaoming Zhang ,  Hilary Cannon ,  Craig Grant ,  Carroll Scarborough

    发明人： Robert Scarborough ,  Wolin Huang ,  Mukund Mehrotra ,  Xiaoming Zhang ,  Hilary Cannon ,  Craig Grant ,  Carroll Scarborough

    IPC分类号： A61K31/517 ,  C07D409/02

    CPC分类号： C07D409/12

    摘要： 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.

    摘要翻译： 本发明提供式（I）的新型磺酰脲化合物及其药学上可接受的衍生物及其多晶型物和无定形形式。 各种形式的化合物是有效的血小板ADP受体抑制剂，可用于各种药物组合物中，并且特别有效预防和/或治疗心血管疾病，特别是与血栓形成有关的疾病。 本发明还提供了一种制备此类化合物和形式并用于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，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的步骤 。

    Representations for graphical user interfaces of operators, data types, and data values in a plurality of natural languages
    10.
    发明授权
    Representations for graphical user interfaces of operators, data types, and data values in a plurality of natural languages 有权
    多种自然语言中运算符，数据类型和数据值的图形用户界面的表示

    公开(公告)号：US08548798B2

    公开(公告)日：2013-10-01

    申请号：US12981687

    申请日：2010-12-30

    申请人： Laura J. Cowen ,  Doina L. Klinger ,  James S. Taylor ,  Xiaoming Zhang

    发明人： Laura J. Cowen ,  Doina L. Klinger ,  James S. Taylor ,  Xiaoming Zhang

    IPC分类号： G06F17/28

    CPC分类号： G06F8/34 ,  G06F9/454

    摘要： A natural language-independent computer program is constructed. A data element is defined by a graphical representation in a user interface. A data element has a data type and a value. An operator is defined on multiple data elements by association of the graphical representations in the user interface. A natural language-independent graph data structure is defined by the association of data elements representing the logic of a computer program. The data types and operators have referenced descriptions in one or more natural languages, enabling a logical expression such as a computer program to be defined and understood in one or more natural languages.

    摘要翻译： 构建了与自然语言无关的计算机程序。 数据元素由用户界面中的图形表示来定义。 数据元素具有数据类型和值。 通过用户界面中的图形表示的关联在多个数据元素上定义运算符。 自然语言无关图形数据结构由表示计算机程序逻辑的数据元素的关联定义。 数据类型和操作符已经以一种或多种自然语言引用描述，使得能够以一种或多种自然语言来定义和理解诸如计算机程序之类的逻辑表达式。