Method of using cyclooxygenase-2 inhibitors in the treatment and prevention of neoplasia
    2.
    发明授权
    Method of using cyclooxygenase-2 inhibitors in the treatment and prevention of neoplasia 失效
    使用环氧合酶-2抑制剂治疗和预防肿瘤的方法

    公开(公告)号:US06469040B2

    公开(公告)日:2002-10-22

    申请号:US09862128

    申请日:2001-05-21

    IPC分类号: A61K31415

    CPC分类号: A61K31/635 A61K31/415

    摘要: This invention relates to the use of cyclooxygenase-2 inhibitors or derivatives thereof in preventing and treating neoplasia. In particular, the invention describes the method of preventing and treating epithelial cell neoplasia in a subject, said method comprising treating the subject with a therapeutically-effective amount of a compound of Formula I. wherein A, R2 and R3 are as described in the specification.

    摘要翻译: 本发明涉及环氧合酶-2抑制剂或其衍生物在预防和治疗瘤形成中的应用。 特别地,本发明描述了预防和治疗受试者的上皮细胞瘤形成的方法,所述方法包括用治疗有效量的式I化合物治疗受试者。其中A,R2和R3如说明书中所述 。

    Method of using cyclooxygenase-2 inhibitors in the treatment and
prevention of neoplasia
    3.
    发明授权
    Method of using cyclooxygenase-2 inhibitors in the treatment and prevention of neoplasia 失效
    使用环氧合酶-2抑制剂治疗和预防肿瘤的方法

    公开(公告)号:US5972986A

    公开(公告)日:1999-10-26

    申请号:US949922

    申请日:1997-10-14

    CPC分类号: A61K31/635 A61K31/415

    摘要: This invention relates to the use of cyclooxygenase-2 inhibitors or derivatives thereof in preventing and treating neoplasia. In particular, the invention describes the method of preventing and treating epithelial cell neoplasia in a subject, said method comprising treating the subject with a therapeutically-effective amount of a compound of Formula I. ##STR1## wherein A, R.sup.2 and R.sup.3 are as described in the specification.

    摘要翻译: 本发明涉及环氧合酶-2抑制剂或其衍生物在预防和治疗瘤形成中的应用。 特别地,本发明描述了预防和治疗受试者的上皮细胞瘤形成的方法,所述方法包括用治疗有效量的式I化合物治疗受试者。其中A,R2和R3如说明书中所述 。

    Inhibitors of inducible nitric oxide synthase for chemoprevention and treatment of cancers
    4.
    发明授权
    Inhibitors of inducible nitric oxide synthase for chemoprevention and treatment of cancers 失效
    诱导型一氧化氮合酶抑制剂用于化学预防和治疗癌症

    公开(公告)号:US07012098B2

    公开(公告)日:2006-03-14

    申请号:US09961969

    申请日:2001-09-24

    IPC分类号: A61K31/195

    摘要: Agents and methods for chemoprevention and treatment of neoplasia are described, the agents including a selective inhibitor of inducible nitric oxide synthase and a combination of a selective inhibitor of inducible nitric oxide synthase and an inhibitor of cylcooxygenase-2 in a pharmaceutical composition. The agents and methods are used for chemoprevention and treatment of neoplasia including colorectal cancer and other cancers affecting epithelial cells throughout the body. The agents can also be used to treat the fibrosis that occurs with radiation therapy, as well as adenomatous polyps, including those with familial adenomatous polyposis (FAP).

    摘要翻译: 描述了用于化学预防和治疗肿瘤的药剂和方法,所述药物包括诱导型一氧化氮合酶的选择性抑制剂和诱导型一氧化氮合酶的选择性抑制剂和环氧合酶-2的抑制剂在药物组合物中的组合。 药物和方法用于化学预防和治疗包括结肠直肠癌和其他影响整个身体上皮细胞的癌症的瘤形成。 这些药物也可用于治疗放射治疗发生的纤维化,以及腺瘤性息肉,包括家族性腺瘤性息肉病(FAP)的息肉。

    Substituted isoxazoles for the treatment of inflammation
    7.
    发明授权
    Substituted isoxazoles for the treatment of inflammation 失效
    用于治疗炎症的取代的异恶唑

    公开(公告)号:US5633272A

    公开(公告)日:1997-05-27

    申请号:US473884

    申请日:1995-06-07

    摘要: A class of substituted isoxazolyl compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula II ##STR1## wherein R.sup.1 is selected from hydroxyl, lower alkyl, carboxyl, lower carboxyalkyl, lower aminocarbonylalkyl, lower alkoxycarbonylalkyl, lower aralkyl, lower alkoxyalkyl, lower aralkoxyalkyl, lower alkylthioalkyl, lower aralkylthioalkyl, lower alkylaminoalkyl, lower aryloxyalkyl, lower arylthioalkyl, lower haloalkyl, lower hydroxylalkyl, cycloalkyl, cycloalkylalkyl, and aralkyl; wherein R.sup.3 is selected from cycloalkyl, cycloalkenyl, aryl, and heteroaryl; wherein R.sup.3 is optionally substituted at a substitutable position with one or more radicals independently selected from lower alkylsulfinyl, lower alkyl, cyano, carboxyl, lower alkoxycarbonyl, lower haloalkyl, hydroxyl, lower hydroxyalkyl, lower haloalkoxy, amino, lower alkylamino, lower arylamino, lower aminoalkyl, nitro, halo, lower alkoxy, aminosulfonyl, and lower alkylthio; and wherein R.sup.4 is selected from lower alkyl, hydroxyl and amino; or a pharmaceutically-acceptable salt thereof.

    摘要翻译: 描述了一类用于治疗炎症和炎症相关疾病的取代的异恶唑基化合物。 特别感兴趣的化合物由式II其中R1选自羟基,低级烷基,羧基,低级羧基烷基,低级氨基羰基烷基,低级烷氧基羰基烷基,低级芳烷基,低级烷氧基烷基,低级芳烷氧基烷基,低级烷硫基烷基,低级芳烷硫基烷基,低级 低级芳氧基烷基,低级芳基硫代烷基,低级卤代烷基,低级羟基烷基,环烷基,环烷基烷基和芳烷基; 其中R 3选自环烷基,环烯基,芳基和杂芳基; 其中R 3在可取代的位置任选被一个或多个独立地选自低级烷基亚磺酰基,低级烷基,氰基,羧基,低级烷氧基羰基,低级卤代烷基,羟基,低级羟烷基,低级卤代烷氧基,氨基,低级烷基氨基,低级芳基氨基,低级 氨基烷基,硝基,卤素,低级烷氧基,氨基磺酰基和低级烷硫基; 并且其中R 4选自低级烷基,羟基和氨基; 或其药学上可接受的盐。