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    USE OF A TEXAPHYRIN IN THE PREPARATION OF A MEDICAMENT FOR USE IN OCULAR DIAGNOSIS AND THERAPY
    94.
    发明申请
    USE OF A TEXAPHYRIN IN THE PREPARATION OF A MEDICAMENT FOR USE IN OCULAR DIAGNOSIS AND THERAPY 审中-公开
    在制备用于眼科诊断和治疗的药物中的曲妥单苷的应用

    公开(公告)号：WO1998025648A2

    公开(公告)日：1998-06-18

    申请号：PCT/US1997022661

    申请日：1997-12-11

    Applicant: PHARMACYCLICS, INC. ,  BLUMENKRANZ, Mark, S. ,  WOODBURN, Kathryn, W. ,  MILLER, Richard, A. ,  YOUNG, Stuart, W.

    Inventor： PHARMACYCLICS, INC.

    IPC: A61K41/00

    CPC classification number: A61K49/0036 ,  A61K41/0076

    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，特别是使用光敏泰克萨菲瑞用于光动力学治疗眼睛状况的特征是例如黄斑变性或翼状by肉的异常脉管系统。 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。

    USE OF A TEXAPHYRIN IN PHOTODYNAMIC THERAPY OF PIGMENT-RELATED LESIONS
    95.
    发明申请
    USE OF A TEXAPHYRIN IN PHOTODYNAMIC THERAPY OF PIGMENT-RELATED LESIONS 审中-公开
    染料在染料相关性淋巴细胞的光化疗中的应用

    公开(公告)号：WO1997035617A1

    公开(公告)日：1997-10-02

    申请号：PCT/US1997005332

    申请日：1997-03-26

    Applicant: PHARMACYCLICS, INC. ,  WOODBURN, Kathryn, W. ,  QUING, Fan ,  YOUNG, Stuart, W.

    Inventor： PHARMACYCLICS, INC.

    IPC: A61K41/00

    CPC classification number: A61K31/407 ,  A61K41/0033 ,  A61K41/0076 ,  Y10S607/901

    Abstract: The present invention involves the use of a photosensitive texaphyrin for the photodynamic treatment of a pigmented lesion, such as a melanodermic lesion, or of a lesion obscured by pigmented tissue, such as melaniferous tissue in a subject. In particular, the invention provides a treatment for the metastatic process of melanoma, and a method for inhibiting growth of established metastases of melanoma. The photosensitive texaphyrin may be a free-base texaphyrin or may be metallated with a diamagnetic metal. Preferably, the texaphyrin is metallated with lutetium. Heretofore, melanoma has been refractory to treatment with photodynamic therapy.

    Abstract translation: 本发明涉及使用感光性泰克萨菲瑞用于色素沉着病变如黑素瘤病变的光动力学治疗，或者受色素组织（如受试者的黑色素组织）遮盖的病变。 特别地，本发明提供了黑素瘤的转移过程的治疗方法，以及抑制已有的黑色素瘤转移的生长的方法。 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。 泰克萨菲瑞优选用镥金属化。 迄今为止，黑素瘤已经用光动力疗法治疗难以治愈。

    PHOSPHOLIPASE C GAMMA 2 AND RESISTANCE ASSOCIATED MUTATIONS
    97.
    发明申请
    PHOSPHOLIPASE C GAMMA 2 AND RESISTANCE ASSOCIATED MUTATIONS 有权
    磷脂酶C游戏2和电阻相关的突变

    公开(公告)号：US20150267261A1

    公开(公告)日：2015-09-24

    申请号：US14664663

    申请日：2015-03-20

    Applicant: Pharmacyclics, Inc.

    Inventor： John C. BYRD ,  Jennifer A. WOYACH

    IPC: C12Q1/68 ,  G01N33/574 ,  A61K31/519

    CPC classification number: C12Q1/6886 ,  A61K31/519 ,  C12Q2600/106 ,  C12Q2600/156 ,  G01N33/57426 ,  G01N2333/916 ,  G01N2800/52

    Abstract: Described herein is a mutation that confers resistance to the treatment with a BTK inhibitor. Described herein is a modified PLCγ2 polypeptide that is modified at amino acid position 742, 845, or 1140 and the modified PLCγ2 polypeptide exhibits decreased inhibition (e.g., resistance) to a covalent and/or irreversible BTK inhibitor. Described herein are diagnostic methods for detecting the modified polypeptide and nucleic acid encoding the modified polypeptide and applications of the methods thereof. Described herein are compositions, combinations, and kits containing the modified polypeptide and methods of using the modified polypeptide. Also described herein are methods of using the modified polypeptide as screening agents for the identification and design of inhibitors of PLCγ2.

    Abstract translation: 本文描述了赋予对用BTK抑制剂治疗的抗性的突变。 本文描述的是在氨基酸位置742,845或1140修饰的修饰的PLCγ2多肽，并且修饰的PLCγ2多肽对共价和/或不可逆的BTK抑制剂表现出降低的抑制（例如抗性）。 本文描述了用于检测修饰的多肽和编码经修饰的多肽的核酸的诊断方法及其方法的应用。 本文描述的是含有修饰多肽的组合物，组合和试剂盒，以及使用修饰多肽的方法。 本文还描述了使用经修饰的多肽作为鉴定和设计PLCγ2抑制剂的筛选剂的方法。

    CRYSTALLINE FORMS OF A BRUTON'S TYROSINE KINASE INHIBITOR
    99.
    发明申请
    CRYSTALLINE FORMS OF A BRUTON'S TYROSINE KINASE INHIBITOR 有权
    BRUTON的酪氨酸激酶抑制剂的晶体形式

    公开(公告)号：US20150158871A1

    公开(公告)日：2015-06-11

    申请号：US14405317

    申请日：2013-06-03

    Applicant: PHARMACYCLICS, INC.

    Inventor： Norbert Purro ,  Mark Smyth ,  Erick Goldman ,  David D. Wirth

    IPC: C07D487/04 ,  A61K45/06 ,  A61K31/519

    CPC classification number: C07D487/04 ,  A61J1/035 ,  A61K9/0053 ,  A61K9/2013 ,  A61K9/2018 ,  A61K9/2054 ,  A61K9/4825 ,  A61K9/4858 ,  A61K9/4866 ,  A61K31/519 ,  A61K45/06 ,  B65D75/36 ,  C07B2200/13 ,  A61K2300/00

    Abstract: Described herein is the Bruton's tyrosine kinase (Btk) inhibitor 1-((R)-3-(4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one, including crystalline forms, solvates and pharmaceutically acceptable salts thereof. Also disclosed are pharmaceutical compositions that include the Btk inhibitor, as well as methods of using the Btk inhibitor, 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: 本文描述了Bruton的酪氨酸激酶（Btk）抑制剂1 - （（R）-3-（4-氨基-3-（4-苯氧基苯基）-1H-吡唑并[3,4-d]嘧啶-1-基）哌啶 -1-基）丙-2-烯-1-酮，包括结晶形式，溶剂化物和药学上可接受的盐。 还公开了包括Btk抑制剂的药物组合物，以及使用Btk抑制剂单独或与其它治疗剂组合用于治疗自身免疫疾病或病症，异种免疫疾病或病症，癌症（包括淋巴瘤）和 炎性疾病或病症。

    METHODS FOR DELAYING OR PREVENTING THE ONSET OF TYPE 1 DIABETES
    100.
    发明申请
    METHODS FOR DELAYING OR PREVENTING THE ONSET OF TYPE 1 DIABETES 审中-公开
    延迟或预防1型糖尿病发作的方法

    公开(公告)号：US20150141438A1

    公开(公告)日：2015-05-21

    申请号：US14542458

    申请日：2014-11-14

    Applicant: Pharmacyclics, Inc.

    Inventor： Peggy L. KENDALL

    IPC: A61K31/519

    CPC classification number: A61K31/519 ,  A61K45/06 ,  A61K2300/00

    Abstract: Described herein are methods for preventing or delaying the onset of Type 1 Diabetes, or inhibiting the maturation of anti-insulin B cells, in an individual in need thereof. The methods include administering to an individual in need thereof ibrutinib, alone or in combination with other Type 1 Diabetes treatments.

    Abstract translation: 本文描述了在有需要的个体中预防或延缓1型糖尿病发作或抑制抗胰岛素B细胞成熟的方法。 所述方法包括单独或与其它1型糖尿病治疗组合使用需要的个体伊布他坦。

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