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31. 发明申请

WO0132211A2 CONJUGATE COMPOUNDS FOR TREATING ATHEROMA, TUMORS AND OTHER NEOPLASTIC TISSUE 审中-公开
标题翻译：治疗ATHEROMA，肿瘤和其他神经组织的联合化合物
公开(公告)号：WO0132211A2
公开(公告)日：2001-05-10
申请号：PCT/US0029524
申请日：2000-10-27
申请人： PHARMACYCLICS INC , UNIV TEXAS , SESSLER JONATHAN L , MADGA DARREN
发明人： SESSLER JONATHAN L , MADGA DARREN
IPC分类号： A61K41/00
CPC分类号： A61K41/0038 , A61K41/0057 , A61K41/0071 , A61K41/0076
摘要： Disclosed are compounds which are conjugates of (a) a moiety capable of localizing in the cells of a tumor or atheroma and (b) a moiety capable of catalyzing the production of reactive oxygen species from a cellular metabolite. The disclosed compounds which are useful for treating atheroma, tumors and other neoplastic tissue.
摘要翻译：公开了以下化合物：（a）能够在肿瘤或动脉粥样化细胞中定位的部分和（b）能够催化细胞代谢产物产生活性氧的部分的结合物。所公开的可用于治疗动脉粥样硬化，肿瘤和其它肿瘤组织的化合物。

32. 发明申请

WO1998007733A1 NUCLEIC ACIDS INTERNALLY-DERIVATIZED WITH A TEXAPHYRIN METAL COMPLEX AND USES THEREOF 审中-公开
标题翻译：用维生素金属复合物内部衍生的核酸及其用途
公开(公告)号：WO1998007733A1
公开(公告)日：1998-02-26
申请号：PCT/US1997014682
申请日：1997-08-20
申请人： PHARMACYCLICS, INC. , MAGDA, Darren , CROFTS, Shaun, P. , WRIGHT, Meredith
发明人： PHARMACYCLICS, INC.
IPC分类号： C07H21/00
CPC分类号： C12N15/113 , C07H21/00 , C12N2310/321 , C12N2310/3511 , C12Q1/6816 , C12N2310/3527
摘要： Texaphyrin metal complex-oligonucleotide and -oligonucleotide analog conjugates are provided where the texaphyrin is bound to an internal linkage of the oligonucleotide or oligonucleotide analog, the conjugates having catalytic activity for the hydrolysis of ribonucleic acid. Further, conjugates demonstrating catalytic turnover are described, the conjugates being especially effective under conditions where the concentration of RNA target exceeds that of available conjugate.
摘要翻译：提供了Texaphyrin金属络合物 - 寡核苷酸和寡核苷酸类似物缀合物，其中泰克萨菲瑞与寡核苷酸或寡核苷酸类似物的内部连接键合，该缀合物具有核糖核酸水解的催化活性。此外，描述了显示催化周转的结合物，缀合物在RNA靶标的浓度超过可用缀合物浓度的条件下特别有效。

33. 发明申请

WO1997026915A1 USE OF A THEXAPHYRIN IN THE PREPARATION OF A MEDICAMENT FOR USE WITH A CHEMOTHERAPEUTIC AGENT IN CANCER CHEMOSENSITIZATION 审中-公开
标题翻译：用于治疗癌症化学治疗药物的药物的制备中的用途
公开(公告)号：WO1997026915A1
公开(公告)日：1997-07-31
申请号：PCT/US1997000907
申请日：1997-01-23
申请人： PHARMACYCLICS, INC. , MILLER, Richard, A. , YOUNG, Stuart, W.
发明人： PHARMACYCLICS, INC.
IPC分类号： A61K41/00
CPC分类号： A61K31/555 , A61K31/675 , A61K31/70 , A61K33/24 , A61K38/14 , A61K41/0076 , A61K31/335 , A61K2300/00
摘要： Methods for cancer chemosensitization are provided. Texaphyrins are new chemosensitizers for enhancing the cytotoxicity of chemotherapeutic agents. The enhancement appears to be P-glycoprotein-independent since texaphyrins are effective in both a P-glycoprotein-expressing and a P-glycoprotein-nonexpressing cell line. Methods are provided for the treatment of cancers such as leukemia, lymphoma, carcinoma, and sarcoma using a texaphyrin as a chemosensitizer.
摘要翻译：提供了癌症化学敏化方法。 Texaphyrins是增加化学治疗剂细胞毒性的新型化学增敏剂。增强似乎是P-糖蛋白不依赖性，因为泰克萨菲精对p-糖蛋白表达和P-糖蛋白无影响的细胞系都有效。提供了使用泰克萨菲瑞作为化学敏化剂治疗癌症如白血病，淋巴瘤，癌和肉瘤的方法。

34. 发明申请

WO1996038461A1 CLEAVAGE OF RNA USING METAL COMPLEXES 审中-公开
标题翻译：使用金属复合物清除RNA
公开(公告)号：WO1996038461A1
公开(公告)日：1996-12-05
申请号：PCT/US1996008262
申请日：1996-05-31
申请人： PHARMACYCLICS, INC. , BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEM , MAGDA, Darren , SESSLER, Jonathan, L.
发明人： PHARMACYCLICS, INC. , BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEM
IPC分类号： C07H21/00
CPC分类号： C12N15/113 , A61K41/0038 , A61K41/0042 , A61K41/0076 , A61K47/546 , A61K49/0021 , B01J31/1815 , B01J2531/025 , B01J2531/36 , C07D487/22 , C07H21/00 , C12N2310/15 , C12N2310/321 , C12N2310/3511 , C12N2310/3527 , C12N2310/3521
摘要： A particular class of metal complexes, specifically certain texaphyrin metal complexes, which both hydrolyze and photocleave ribonucleic acid, and which also both hydrolyze ribonucleic acid and photocleave deoxyribonucleic acid, is provided. The texaphyrin metal complex for each set of reactions has catalytic activity for phosphate ester hydrolysis and is photosensitive. A complex having the advantage of multiple activities can result in lower treatment dosages and lower treatment costs.
摘要翻译：提供了特殊类别的金属络合物，特别是水解和光切核糖核酸的某些特沙弗林金属络合物，并且还水解核糖核酸和光切割脱氧核糖核酸。用于每组反应的泰克萨菲金属络合物对磷酸酯水解具有催化活性并且是光敏的。具有多种活性优点的复合物可以降低治疗剂量并降低治疗成本。

35. 发明申请

WO1996009315A1 DNA PHOTOCLEAVAGE USING TEXAPHYRINS 审中-公开
标题翻译：使用丝印蛋白的DNA光合作用
公开(公告)号：WO1996009315A1
公开(公告)日：1996-03-28
申请号：PCT/US1995012312
申请日：1995-09-21
申请人： BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEM , PHARMACYCLICS, INC.
发明人： BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEM , PHARMACYCLICS, INC. , MAGDA, Darren , SESSLER, Jonathan, L. , IVERSON, Brent, L. , SANSOM, Petra, I. , WRIGHT, Meredith , MODY, Tarak, D. , HEMMI, Gregory, W.
IPC分类号： C07H21/00
CPC分类号： C12N15/113 , A61K41/0038 , A61K41/0042 , A61K41/0076 , A61K47/54 , A61K47/546 , A61K49/0021 , A61K49/0052 , A61K49/0054 , A61K49/06 , A61K49/085 , A61K49/10 , A61K51/0485 , A61L2/0011 , B01J31/061 , B01J31/1658 , B01J31/1815 , B01J2531/025 , B01J2531/38 , C07D487/22 , C07H21/00 , C12N2310/15 , C12N2310/321 , C12N2310/3511 , Y10T436/147777 , C12N2310/3521
摘要： Methods of cleavage of a polymer of deoxyribonucleic acid using photosensitive texaphyrins are disclosed. A preferred method of use is the site-specific cleavage of a polymer of deoxyribonucleic acid, and a preferred texaphyrin is a derivatized texaphyrin having binding specificity, in particular, a texaphyrin covalently coupled to a site-directing molecule, preferably an oligonucleotide.
摘要翻译：公开了使用光敏泰克萨菲蛋白分解脱氧核糖核酸聚合物的方法。优选的使用方法是脱氧核糖核酸的聚合物的位点特异性切割，并且优选的泰克萨菲瑞是具有结合特异性的衍生化泰克萨菲林，特别是共价偶联到位点定向分子，优选寡核苷酸的泰克萨菲林。

36. 发明申请

WO9429316A3 TEXAPHYRIN METAL COMPLEX MEDIATED ESTER HYDROLYSIS 审中-公开
标题翻译：纺丝金属复合介质酯酶水解
公开(公告)号：WO9429316A3
公开(公告)日：1995-02-02
申请号：PCT/US9406284
申请日：1994-06-09
申请人： UNIV TEXAS , PHARMACYCLICS INC , SESSLER JONATHAN L , ROSS KEVIN L , WRIGHT MEREDITH , HEMMI GREGORY W , DOW WILLIAM C , SMITH DANIEL A , KRAL VLADIMIR A , IVERSON BRENT , MODY TARAK , MILLER RICHARD A , MAGDA DARREN
发明人： SESSLER JONATHAN L , ROSS KEVIN L , WRIGHT MEREDITH , HEMMI GREGORY W , DOW WILLIAM C , SMITH DANIEL A , KRAL VLADIMIR A , IVERSON BRENT , MODY TARAK , MILLER RICHARD A , MAGDA DARREN
IPC分类号： A61K41/00 , A61K47/48 , A61K49/00 , A61K49/06 , A61K49/08 , A61K51/04 , A61L2/00 , B01J31/06 , B01J31/16 , B01J31/18 , C07B61/00 , C07D487/22 , C07F9/06 , C07F9/6558 , C07F9/6561 , C07H21/00 , C12N15/10 , C12Q1/68
CPC分类号： C07D487/22 , A61K41/0038 , A61K41/0076 , A61K47/546 , A61K49/0021 , A61K49/0036 , A61K49/085 , A61K49/106 , A61K49/126 , A61K51/0485 , A61L2/0011 , B01J31/061 , B01J31/1658 , B01J31/1815 , B01J2531/025 , B01J2531/23 , B01J2531/26 , B01J2531/27 , B01J2531/28 , B01J2531/38 , B01J2531/72 , B01J2531/842 , B01J2531/845 , B01J2531/847 , B01J2531/96 , C07H21/00
摘要： A method of phosphate ester hydrolysis including incubating a solution of an aqueous phosphate ester with a texaphyrin metal complex. The metal is a metal cation having catalytic activity for ester bond hydrolysis in aqueous solution, in particular, a lanthanide metal cation, preferably Eu(III) or Dy(III). A preferred substrate is RNA and a preferred texaphyrin is a derivatized texaphyrin having binding specificity, in particular, a texaphyrin covalently coupled to a site-directed molecule, preferably an oligonucleotide.

37. 发明申请

WO1994029316A2 TEXAPHYRIN METAL COMPLEX MEDIATED ESTER HYDROLYSIS 审中-公开
标题翻译：纺丝金属复合介质酯酶水解
公开(公告)号：WO1994029316A2
公开(公告)日：1994-12-22
申请号：PCT/US1994006284
申请日：1994-06-09
申请人： BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEM , PHARMACYCLICS, INC. , SESSLER, Jonathan, L. , ROSS, Kevin, L. , WRIGHT, Meredith , HEMMI, Gregory, W. , DOW, William, C. , SMITH, Daniel, A. , KRAL, Vladimir, A. , IVERSON, Brent , MODY, Tarak , MILLER, Richard, A. , MAGDA, Darren
发明人： BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEM , PHARMACYCLICS, INC.
IPC分类号： C07D487/22
CPC分类号： C07D487/22 , A61K41/0038 , A61K41/0076 , A61K47/546 , A61K49/0021 , A61K49/0036 , A61K49/085 , A61K49/106 , A61K49/126 , A61K51/0485 , A61L2/0011 , B01J31/061 , B01J31/1658 , B01J31/1815 , B01J2531/025 , B01J2531/23 , B01J2531/26 , B01J2531/27 , B01J2531/28 , B01J2531/38 , B01J2531/72 , B01J2531/842 , B01J2531/845 , B01J2531/847 , B01J2531/96 , C07H21/00
摘要： A method of phosphate ester hydrolysis including incubating a solution of an aqueous phosphate ester with a texaphyrin metal complex. The metal is a metal cation having catalytic activity for ester bond hydrolysis in aqueous solution, in particular, a lanthanide metal cation, preferably Eu(III) or Dy(III). A preferred substrate is RNA and a preferred texaphyrin is a derivatized texaphyrin having binding specificity, in particular, a texaphyrin covalently coupled to a site-directed molecule, preferably an oligonucleotide.
摘要翻译：磷酸酯水解方法，包括将磷酸酯水溶液与泰克萨菲金属络合物的溶液孵育。金属是具有催化活性的金属阳离子，用于水溶液中的酯键水解，特别是镧系元素金属阳离子，优选Eu（III）或Dy（III）。优选的底物是RNA，优选的泰克萨菲瑞是具有结合特异性的衍生的泰克萨菲林，特别是共价偶联到定点分子，优选寡核苷酸的泰克萨菲林。

38. 发明申请

WO2015143400A1 PHOSPHOLIPASE C GAMMA 2 AND RESISTANCE ASSOCIATED MUTATIONS 审中-公开
标题翻译：磷脂酶GAMMA 2和电阻相关突变
公开(公告)号：WO2015143400A1
公开(公告)日：2015-09-24
申请号：PCT/US2015/021871
申请日：2015-03-20
申请人： PHARMACYCLICS, INC.
发明人： BYRD, John, C. , WOYACH, Jennifer, A.
IPC分类号： C12Q1/68
CPC分类号： C12Q1/6886 , A61K31/519 , C12Q2600/106 , C12Q2600/156 , G01N33/57426 , G01N2333/916 , G01N2800/52
摘要： Described herein is a mutation that confers resistance to the treatment with a BTK inhibitor. Described herein is a modified PLCy2 polypeptide that is modified at amino acid position 742, 845, or 1140 and the modified PLCy2 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 PLCy2.
摘要翻译：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PLCy2多肽，并且修饰的PLCy2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。本文还描述了使用修饰的多肽作为用于鉴定和设计PLCy2的抑制剂的筛选剂的方法。

39. 发明申请

WO2015023703A1 METHODS FOR THE TREATMENT OF HER2 AMPLIFIED CANCER 审中-公开
标题翻译：治疗HER2放大癌的方法
公开(公告)号：WO2015023703A1
公开(公告)日：2015-02-19
申请号：PCT/US2014/050783
申请日：2014-08-12
申请人： PHARMACYCLICS, INC. , CHEN, Jun , BUGGY, Joseph, J. , ELIAS, Laurence
发明人： CHEN, Jun , BUGGY, Joseph, J. , ELIAS, Laurence
IPC分类号： A61K31/4162 , A61K31/4155 , A61K31/519 , A61K31/506 , A61P35/00
CPC分类号： A61K31/519 , A61K31/454 , A61K45/06
摘要： Described herein are methods and compositions for treating HER2-amplified cancer. The methods include administering to an individual in need thereof ibrutinib.
摘要翻译：本文描述了用于治疗HER2扩增的癌症的方法和组合物。所述方法包括向有需要的个体施用伊布他尼。

40. 发明申请

WO2014168975A1 IBRUTINIB COMBINATION THERAPY 审中-公开
标题翻译： IBRUTINIB组合治疗
公开(公告)号：WO2014168975A1
公开(公告)日：2014-10-16
申请号：PCT/US2014/033378
申请日：2014-04-08
申请人： PHARMACYCLICS, INC. , JANSSEN PHARMACEUTICA NV , CHANG, Betty , BALASUBRAMANIAN, Sriram , CROWLEY, Richard , KUO, Hsu-Ping
发明人： CHANG, Betty , BALASUBRAMANIAN, Sriram , CROWLEY, Richard , KUO, Hsu-Ping , HALL, Brett , SASSER, A. Kate , SCHAFFER, Michael , DAVIS, Cuc , CASNEUF, Tineke , VERSELE, Matthias , LIGTENBERG, Willem
IPC分类号： A61K31/519 , A61K31/573 , A61K31/56 , A61P35/00
CPC分类号： A61K31/519 , A61K31/282 , A61K31/395 , A61K31/4439 , A61K31/454 , A61K31/4745 , A61K31/496 , A61K31/5377 , A61K31/5383 , A61K31/573 , A61K31/664 , A61K31/704 , A61K31/7048 , A61K31/7068 , A61K39/3955 , A61K45/06 , A61K2039/505 , A61K2300/00
摘要： Combinations of Bruton's tyrosine kinase (Btk) inhibitors, e.g., 1-((R)-3-(4-amino-phenoxyphenyl)- 1 H-pyrazolo [3,4-d]pyrimidin- 1 -yl)piperidin- 1 -yl)prop-2-en- 1 -one, with a second anticancer agent are provided. Also provided are methods of treating cancers, and autoimmune disorders by administering combinations of Bruton's tyrosine kinase (Btk) inhibitors, e.g., 1-((R)-3-(4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1- yl)piperidin-1-yl)prop-2-en-1-one, and second anticancer agents.
摘要翻译： Bruton酪氨酸激酶（Btk）抑制剂的组合，例如1 - （（R）-3-（4-氨基 - 苯氧基苯基）-1H-吡唑并[3,4-d]嘧啶-1-基）哌啶-1-基] 哌嗪-1-基）丙-2-烯-1-酮与第二抗癌剂。还提供了通过施用布鲁顿酪氨酸激酶（Btk）抑制剂的组合来治疗癌症和自身免疫性疾病的方法，例如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-酮和第二抗癌剂。

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