Substituted 2-pyrrolidinone activators of PKC
    61.
    发明授权
    Substituted 2-pyrrolidinone activators of PKC 失效
    PKC的取代的2-吡咯烷酮激活剂

    公开(公告)号:US5962504A

    公开(公告)日:1999-10-05

    申请号:US149609

    申请日:1998-09-08

    CPC分类号: C07D207/26

    摘要: Compounds of formula I: ##STR1## wherein R.sub.1 and R.sub.2 have any of the values defined in the specification, and their pharmaceutically acceptable salts, are PKC activators and are useful for treating diseases, such as, for example, cancer. Also disclosed are pharmaceutical compositions comprising compounds of formula I, processes for preparing compounds of formula I, and intermediates useful for preparing compounds of formula I.

    摘要翻译: 式I化合物:其中R 1和R 2具有说明书中定义的任何值及其药学上可接受的盐,是PKC激活剂,并且可用于治疗疾病,例如癌症。 还公开了包含式I化合物,式I化合物的方法和可用于制备式I化合物的中间体的药物组合物。

    Matriptase, a serine protease and its applications
    65.
    发明授权
    Matriptase, a serine protease and its applications 有权
    Matriptase,丝氨酸蛋白酶及其应用

    公开(公告)号:US07960163B2

    公开(公告)日:2011-06-14

    申请号:US12040467

    申请日:2008-02-29

    摘要: The invention is directed to a method of detecting a malignancy or a pre-malignant lesion in breast or other tissue, or a pathologic condition, by detecting the presence of single-chain or two-chain forms of matriptase in the tissue. The invention is further directed to a method of treating malignancies, which have the phenotype of matriptase production by administering a tumor formation inhibiting effective amount of concentrate of Bowman-Birk inhibitor (BBIC), or other matriptase inhibitor. The invention also is directed to nucleic acids encoding a matriptase protein or fragments thereof, and their use for structure elucidation and modeling to identify other inhibitors of matriptase, as well as to methods of identifying matriptase modulating agents, including activators and inhibitors.

    摘要翻译: 本发明涉及通过检测组织中单链或双链形式的matriptase的存在来检测乳腺或其他组织或病理状况中的恶性肿瘤或恶性前病变的方法。 本发明进一步涉及通过施用抑制有效量的Bowman-Birk抑制剂(BBIC)浓缩物或其它片剂酶抑制剂的肿瘤形成来治疗恶性肿瘤的方法,所述恶性肿瘤具有基质酶产生的表型。 本发明还涉及编码matriptase蛋白质或其片段的核酸,以及其用于结构阐明和建模以鉴定其它抑制剂的用途,以及鉴定片段酶调节剂(包括活化剂和抑制剂)的方法。

    Matriptase, a serine protease and its applications
    67.
    发明授权
    Matriptase, a serine protease and its applications 有权
    Matriptase,丝氨酸蛋白酶及其应用

    公开(公告)号:US07355015B1

    公开(公告)日:2008-04-08

    申请号:US09936333

    申请日:2000-03-10

    IPC分类号: C07K16/00 C07K16/40 A61K38/43

    摘要: The invention is directed to a method of detecting a malignancy or a pre-malignant lesion in breast or other tissue, or a pathologic condition, by detecting the presence of single-chain or two-chain forms of matriptase in the tissue. The invention is further directed to a method of treating malignancies, which have the phenotype of matriptase production by administering a tumor formation inhibiting effective amount of concentrate of Bowman-Birk inhibitor (BBIC), or other matriptase inhibitor. The invention also is directed to nucleic acids encoding a matriptase protein or fragments thereof, and their use for structure elucidation and modeling to identify other inhibitors of matriptase, as well as to methods of identifying matriptase modulating agents, including activators and inhibitors.

    摘要翻译: 本发明涉及通过检测组织中单链或双链形式的matriptase的存在来检测乳腺或其他组织或病理状况中的恶性肿瘤或恶性前病变的方法。 本发明进一步涉及通过施用抑制有效量的Bowman-Birk抑制剂(BBIC)浓缩物或其它片剂酶抑制剂的肿瘤形成来治疗恶性肿瘤的方法,所述恶性肿瘤具有基质酶产生的表型。 本发明还涉及编码matriptase蛋白质或其片段的核酸,以及其用于结构阐明和建模以鉴定其它抑制剂的用途,以及鉴定片段酶调节剂(包括活化剂和抑制剂)的方法。

    Gossypol co-crytals and the use thereof
    68.
    发明申请
    Gossypol co-crytals and the use thereof 有权
    棉酚共同合作伙伴及其用途

    公开(公告)号:US20070293585A1

    公开(公告)日:2007-12-20

    申请号:US11818766

    申请日:2007-06-15

    CPC分类号: A61K31/11

    摘要: This invention relates to compositions comprising co-crystals of (−)-gossypol with a C1-8 carboxylic acid or C1-8 sulfonic acid which are useful as inhibitors of Bcl-2 family proteins. The invention also relates to the use of co-crystals of (−)-gossypol with a C1-8 carboxylic acid or C1-8 sulfonic acid for inducing apoptosis in cells and for sensitizing cells to the induction of apoptotic cell death.

    摘要翻译: 本发明涉及包含( - ) - 棉酚与C 1-8 - 羧酸或C 1-8 - 磺酸的共晶体的组合物,其可用作 Bcl-2家族蛋白。 本发明还涉及( - ) - 棉酚与C 1-8 - 羧酸或C 1-8 - 磺酸的共晶体用于诱导细胞凋亡 细胞和致敏细胞诱导凋亡细胞死亡。

    Gossypol co-crystals and the use thereof
    69.
    发明申请
    Gossypol co-crystals and the use thereof 有权
    棉酚共晶及其用途

    公开(公告)号:US20050234135A1

    公开(公告)日:2005-10-20

    申请号:US11089096

    申请日:2005-03-24

    IPC分类号: A61K31/11

    CPC分类号: A61K31/11

    摘要: This invention relates to compositions comprising co-crystals of (−)-gossypol with a C1-8 carboxylic acid or C1-8 sulfonic acid which are useful as inhibitors of Bcl-2 family proteins. The invention also relates to the use of co-crystals of (−)-gossypol with a C1-8 carboxylic acid or C1-8 sulfonic acid for inducing apoptosis in cells and for sensitizing cells to the induction of apoptotic cell death.

    摘要翻译: 本发明涉及包含( - ) - 棉酚与C 1-8 - 羧酸或C 1-8 - 磺酸的共晶体的组合物,其可用作 Bcl-2家族蛋白。 本发明还涉及( - ) - 棉酚与C 1-8 - 羧酸或C 1-8 - 磺酸的共晶体用于诱导细胞凋亡 细胞和致敏细胞诱导凋亡细胞死亡。

    Substituted 2-pyrrolidinone activators of PKC
    70.
    发明授权
    Substituted 2-pyrrolidinone activators of PKC 有权
    PKC的取代的2-吡咯烷酮激活剂

    公开(公告)号:US06284784B1

    公开(公告)日:2001-09-04

    申请号:US09339072

    申请日:1999-06-23

    IPC分类号: A61K3140

    CPC分类号: C07D207/26

    摘要: Compounds of formula I: wherein R1 and R2 have any of the values defined in the specification, and their pharmaceutically acceptable salts, are PKC activators and are useful for treating diseases, such as, for example, cancer. Also disclosed are pharmaceutical compositions comprising compounds of formula I, processes for preparing compounds of formula I, and intermediates useful for preparing compounds of formula I.

    摘要翻译: 式I化合物:其中R 1和R 2具有说明书中定义的任何值及其药学上可接受的盐,是PKC激活剂,并且可用于治疗疾病,例如癌症。 还公开了包含式I化合物,式I化合物的方法和可用于制备式I化合物的中间体的药物组合物。