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    [[2-(Amino-3,4-dioxo-1-cyclobuten-1-yl)amino]alkyl]-acid derivatives for the treatment of pain
    2.
    发明申请
    [[2-(Amino-3,4-dioxo-1-cyclobuten-1-yl)amino]alkyl]-acid derivatives for the treatment of pain 失效
    [[2-（氨基-3,4-二氧代-1-环丁烯-1-基）氨基]烷基] - 酸衍生物，用于治疗疼痛

    公开(公告)号：US20060205696A1

    公开(公告)日：2006-09-14

    申请号：US11433737

    申请日：2006-05-12

    申请人： Michael Brandt ,  Margaret Zaleska ,  John Moyer

    发明人： Michael Brandt ,  Margaret Zaleska ,  John Moyer

    IPC分类号： A61K31/663 ,  A61K31/4245 ,  A61K31/41 ,  A61K31/195 ,  A61K31/215

    CPC分类号： C07D243/10 ,  A61K31/122 ,  A61K31/198 ,  A61K31/4245 ,  A61K31/551 ,  A61K31/662 ,  A61K45/06

    摘要： This invention provides a method of treating pain in a mammal that includes administering to a mammal in need of such treatment a pain treating effective amount of a compound of the formula (I): where R1 is H, alkyl or phenylalkyl; R2 is H, alkyl, alkenyl or phenylalkyl; or R1 and R2 taken together as Z are —CH2C—H2—, —CH2C(R6)(R7)CH2— or —CH2C(R8)(R9)—C(R10)(R11)CH2—, where R6, R8 and R10 are, independently, H, alkyl or hydroxyl and R7, R9 and R11 are, independently, H or alkyl; A is alkylene or alkenylene; X is CO2R3, P(O)(OR4)(OR5), 3,5-dioxo-1,2,4-oxadiazolidin-2-yl or 5-tetrazolyl in which R3, R4 and R5 are, independently, H or alkyl, or a pharmaceutically acceptable salt thereof. The present invention also provides pharmaceutical compositions for treating pain containing a pain treating effective amount of the compound of formula (I).

    摘要翻译： 本发明提供一种治疗哺乳动物疼痛的方法，包括向需要这种治疗的哺乳动物施用疼痛治疗有效量的式（I）化合物：其中R 1是H， 烷基或苯基烷基; R 2是H，烷基，烯基或苯基烷基; 或R 1和R 2一起作为Z是-CH 2 CH 2 - ， - CH＆lt; SUB （R 6）（R 7）CH 2 - 或-CH 2 CH 2 C（R 8）（R 9） - （R 10） - （R 11） 其中R 6，R 8和R 10独立地为H，烷基或羟基，R 1，R 2， R 9，R 9和R 11独立地是H或烷基; A是亚烷基或亚烯基; X是CO 2 R 3，P（O）（OR 4）（OR 5），3， 5-二氧代-1,2,4-恶二唑烷-2-基或其中R 3，R 4和R 5的5-四唑基， 独立地是H或烷基，或其药学上可接受的盐。 本发明还提供用于治疗疼痛的药物组合物，其含有疼痛治疗有效量的式（I）化合物。

    4-[(2,4-Dichloro-5-methoxyphenyl)amino]-6-alkoxy-7-ethynyl-3-quinolinecarbonitriles for the treatment of ischemic injury
    3.
    发明申请
    4-[(2,4-Dichloro-5-methoxyphenyl)amino]-6-alkoxy-7-ethynyl-3-quinolinecarbonitriles for the treatment of ischemic injury 审中-公开
    4 - [（2,4-二氯-5-甲氧基苯基）氨基] -6-烷氧基-7-乙炔基-3-喹啉碳腈治疗缺血性损伤

    公开(公告)号：US20060116375A1

    公开(公告)日：2006-06-01

    申请号：US11255556

    申请日：2005-10-21

    申请人： Diane Boschelli ,  Ana Sosa ,  Margaret Zaleska

    发明人： Diane Boschelli ,  Ana Sosa ,  Margaret Zaleska

    IPC分类号： A61K31/5377 ,  A61K31/496 ,  A61K31/4706

    CPC分类号： A61K31/4706 ,  A61K31/496 ,  A61K31/5377 ,  C07D215/54

    摘要： Compounds of the formula: wherein: R is methyl or ethyl; R′ and R″ are independently alkyl of 1 to 3 carbon atoms, or R′ and R″, taken together with the nitrogen to which they are attached, can form a 5 or 6 membered saturated ring which may optionally contain an additional heteroatom selected from NR′″, O or S(O)n; n is 0-2; and R′″ is hydrogen or alkyl of 1 to 3 carbon atoms, and pharmaceutically acceptable salts thereof, and their use for inhibiting vascular permeability caused by disease, injury or other trauma.

    摘要翻译： 下式化合物：其中：R是甲基或乙基; R'和R“独立地为1至3个碳原子的烷基，或者R'和R”与它们所连接的氮一起可以形成5或6元饱和环，其可以任选地含有另外的 选自NR“'，O或S（O）n的杂原子; n为0-2; R“是氢或1〜3个碳原子的烷基及其药学上可接受的盐，以及它们用于抑制由疾病，损伤或其他创伤引起的血管通透性的用途。