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    HIGH-PURITY TEXAPHYRIN METAL COMPLEXES
    154.
    发明申请
    HIGH-PURITY TEXAPHYRIN METAL COMPLEXES 审中-公开
    高纯度丝印金属复合物

    公开(公告)号：US20130157994A1

    公开(公告)日：2013-06-20

    申请号：US13767583

    申请日：2013-02-14

    Applicant: Pharmacyclics, Inc.

    Inventor： Hugo MADDEN ,  Greg HEMMI ,  Tarak MODY

    IPC: C07F5/00 ,  A61K45/00 ,  A61K31/555

    CPC classification number: C07F5/00 ,  A61K31/555 ,  A61K45/00 ,  C07C41/16 ,  C07C43/2055 ,  C07C205/37 ,  C07D487/22 ,  C07F5/003

    Abstract: Disclosed herein are the methods and compositions for the improved synthesis of texaphyrin metal complexes. The improved synthesis results in high-purity compositions of texaphyrin metal complexes in which more than about 98% of the texaphyrin metal complexes in the composition have the same structure and/or the same molecular weight. Further described herein are pharmaceutical compositions comprising such high-purity compositions, and the use of such high-purity compositions in the treatment of cancer and cardiovascular diseases and disorders.

    Abstract translation: 本文公开了用于改进合成特沙弗林金属络合物的方法和组合物。 改进的合成导致特沙弗林金属络合物的高纯度组合物，其中组合物中超过约98％的特沙弗林金属络合物具有相同的结构和/或相同的分子量。 本文进一步描述的是包含这种高纯度组合物的药物组合物，以及这些高纯度组合物在治疗癌症和心血管疾病和病症中的用途。

    Use of texaphyrins in macrophage-mediated disease
    156.
    发明申请
    Use of texaphyrins in macrophage-mediated disease 审中-公开
    泰克萨菲精在巨噬细胞介导的疾病中的应用

    公开(公告)号：US20020115649A1

    公开(公告)日：2002-08-22

    申请号：US09755795

    申请日：2001-01-05

    Applicant: Pharmacyclics, Inc.

    Inventor： Kathryn W. Woodburn ,  Stuart W. Young

    IPC: A61B005/055 ,  A61K031/555 ,  A61K031/409

    CPC classification number: A61K41/0076 ,  A61K31/407 ,  A61K31/555 ,  A61K41/0038 ,  A61K45/06 ,  A61K2300/00

    Abstract: The present invention provides methods for treating disease of a subject in need thereof by sensitizing the effects of a co-therapeutic agent in macrophages. The method comprises administering a texaphyrin and a co-therapeutic agent to the subject. Texaphyrins are provided for enhancing the cytotoxicity of therapeutic agents in macrophage-mediated disease since texaphyrins have been shown to accumulate in macrophage.

    Abstract translation: 本发明提供了通过增加协同治疗剂在巨噬细胞中的作用来治疗有需要的受试者的疾病的方法。 该方法包括向受试者施用特沙弗林和协同治疗剂。 提供特拉法辛用于增强治疗剂在巨噬细胞介导的疾病中的细胞毒性，因为泰克萨菲精已显示在巨噬细胞中积累。

    Use of texaphyrin in ocular diagnosis and therapy
    157.
    发明申请
    Use of texaphyrin in ocular diagnosis and therapy 审中-公开
    泰克萨菲瑞在眼科诊断和治疗中的应用

    公开(公告)号：US20020025298A1

    公开(公告)日：2002-02-28

    申请号：US09922350

    申请日：2001-08-02

    Applicant: Pharmacyclics, Inc.

    Inventor： Mark S. Blumenkranz ,  Kathryn W. Woodburn ,  Richard A. Miller ,  Stuart W. Young

    IPC: A61K049/00 ,  A61K031/555 ,  A61K031/407

    CPC classification number: A61K41/0076 ,  A61K49/0021 ,  Y10S514/912

    Abstract: The use of texaphyrins for ocular diagnosis and therapy is provided, especially use of photosensitive texaphyrins for photodynamic therapy of conditions of the eye characterized by abnormal vasculature, such as macular degeneration, or pterygium, for example. The photosensitive texaphyrin may be a free-base texaphyrin or may be metallated with a diamagnetic metal. Preferably, the photosensitive texaphyrin is metallated with lutetium. Due to the dual wavelength absorption of texaphyrins, i.e., at 400-500 nm and at 700-800 nm, especially about 732 nm, as compared to porphyrins, texaphyrins are more effective and versatile for use in humans as compared to porphyrins. Texaphyrins serve as effective contrast agents in ocular angiography.

    Abstract translation: 提供了泰克萨菲瑞用于眼部诊断和治疗的用途，特别是使用感光性泰克萨菲瑞用于光动力学治疗眼睛状况的特征是异常脉管系统，例如黄斑变性或翼状ium肉。 感光性泰克萨菲瑞可以是游离碱泰克萨菲瑞，也可以用抗磁性金属进行金属化。 优选地，感光性泰克萨菲瑞用镥金属化。 由于与卟啉相比，泰克萨菲瑞的双波长吸收，即在400-500nm和700-800nm，特别是约732nm，与卟啉相比，泰克萨菲素在人类中更有效和通用。 Texaphyrins作为眼部血管造影术中的有效造影剂。

    Intracellular sensitizers for sonodynamic therapy
    158.
    发明申请
    Intracellular sensitizers for sonodynamic therapy 审中-公开
    细胞内敏感剂用于声动力学治疗

    公开(公告)号：US20010002251A1

    公开(公告)日：2001-05-31

    申请号：US09755824

    申请日：2001-01-05

    Applicant: Pharmacyclics, Inc.

    Inventor： Kathryn W. Woodburn ,  David Kessel

    IPC: A61K009/14 ,  A61K049/00 ,  A61B008/13

    CPC classification number: A61K9/0009 ,  A61B8/481 ,  A61K41/0033 ,  A61N7/00

    Abstract: Texaphyrins are selectively retained in diseased tissue cells. When exposed to low level, non-thermal sonodynamic agent such as ultrasound, the texaphyrin-incorporated cells are selectively destroyed. There is provided a method of sonodynamic therapy by administering an effective amount of an intracellular sensitizer to a mammal in need thereof and providing an effective amount of a sonodynamic agent.

    Abstract translation: 特拉法芬被选择性地保留在患病组织细胞中。 当暴露于低水平，非热声子动力学剂如超声波时，被引入泰克萨菲林的细胞被选择性地破坏。 提供了一种通过向有需要的哺乳动物施用有效量的细胞内增感剂并提供有效量的超声动力学药剂的声力学治疗方法。

    Inhibitors of bruton's tyrosine kinase
    159.
    发明授权
    Inhibitors of bruton's tyrosine kinase 有权
    布鲁特酪氨酸激酶抑制剂

    公开(公告)号：US09206189B2

    公开(公告)日：2015-12-08

    申请号：US14340483

    申请日：2014-07-24

    Applicant: Pharmacyclics, Inc.

    Inventor： Lee Honigberg ,  Erik Verner ,  Zhengying Pan

    IPC: A01N43/90 ,  A61K31/519 ,  C07D487/04 ,  A61K31/00 ,  A61K45/06 ,  A61K9/48

    CPC classification number: A61K31/52 ,  A61K9/4825 ,  A61K31/00 ,  A61K31/519 ,  A61K39/3955 ,  A61K45/06 ,  A61K2300/00 ,  C07D487/04 ,  C07K16/2887 ,  C07K2317/24

    Abstract: Disclosed herein are pyrazolo[3,4-d]pyrimidines that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. Methods for the preparation of the compounds are disclosed. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.

    Abstract translation: 本文公开了与布鲁特酪氨酸激酶（Btk）形成共价键的吡唑并[3,4-d]嘧啶。 还描述了Btk的不可逆抑制剂。 公开了制备化合物的方法。 还公开了包含化合物的药物组合物。 公开了使用Btk抑制剂的方法，单独或与其它治疗剂组合用于治疗自身免疫性疾病或病症，异种免疫疾病或病症，癌症，包括淋巴瘤和炎性疾病或病症。

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