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公开(公告)号：US09072660B2
公开(公告)日：2015-07-07
申请号：US13607489
申请日：2012-09-07
CPC分类号： A61K9/0014 , A61K31/496 , A61K47/10 , A61K47/14 , A61K47/26 , A61K47/32 , A61K47/40
摘要： Methods of transdermally delivering a therapeutic amount of a triazole-triazolone compound are provided, e.g. for the prevention or treatment of basal cell carcinoma (BCC) in a subject. A therapeutic level of a triazole-triazolone compound such as itraconazole is delivered transdermally to a subject. Also provided are topical triazole-triazolone compositions that find use in practicing the subject methods.
摘要翻译： 提供治疗量的三唑 - 三唑酮化合物的经皮递送方法。 用于预防或治疗受试者的基底细胞癌（BCC）。 治疗水平的三唑 - 三唑酮化合物如伊曲康唑经皮递送给受试者。 还提供了用于实践本发明方法的局部三唑 - 三唑酮组合物。
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公开(公告)号：US20130109700A1
公开(公告)日：2013-05-02
申请号：US13607489
申请日：2012-09-07
IPC分类号： A61K9/00
CPC分类号： A61K9/0014 , A61K31/496 , A61K47/10 , A61K47/14 , A61K47/26 , A61K47/32 , A61K47/40
摘要： Methods of transdermally delivering a therapeutic amount of a triazole-triazolone compound are provided, e.g. for the prevention or treatment of basal cell carcinoma (BCC) in a subject. A therapeutic level of a triazole-triazolone compound such as itraconazole is delivered transdermally to a subject. Also provided are topical triazole-triazolone compositions that find use in practicing the subject methods.
摘要翻译： 提供治疗量的三唑 - 三唑酮化合物的经皮递送方法。 用于预防或治疗受试者的基底细胞癌（BCC）。 治疗水平的三唑 - 三唑酮化合物如伊曲康唑经皮递送给受试者。 还提供了用于实践本发明方法的局部三唑 - 三唑酮组合物。
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3.发明申请INHIBITORS OF HEDGEHOG SIGNALING PATHWAYS, COMPOSITIONS AND USES RELATED THERETO 审中-公开HEDGEHOG信号通道，组合物和相关用途的抑制剂公开(公告)号：US20100273818A1
公开(公告)日：2010-10-28
申请号：US12652134
申请日：2010-01-05
IPC分类号： A61K31/438 , A61P35/00 , C12N5/02 , A61P15/16
CPC分类号： A61K31/4355 , A61K31/00 , A61K31/435 , A61K31/438 , A61K31/58
摘要： The present invention makes availables assays and reagents inhibiting paracrine and/or autocrine signals produced by a hedgehog protein or aberrant activation of a hedgehog signal transduction pathway, e.g., which involve the use of a steroidal alkaloid or other small molecule.
摘要翻译： 本发明使得可用性测定和试剂抑制由刺猬蛋白质产生的旁分泌和/或自分泌信号或异常激活刺猬蛋白信号转导途径，例如涉及使用甾族生物碱或其它小分子。
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4.发明授权Modulators of hedgehog signaling pathways, compositions and uses related thereto 失效刺猬蛋白信号通路的调节剂，组合物和与之相关的用途公开(公告)号：US07655674B2
公开(公告)日：2010-02-02
申请号：US10512804
申请日：2003-04-22
IPC分类号： A61K31/47 , A61K31/445
CPC分类号： A61K31/454 , A61K31/135 , A61K31/4184 , A61K31/44 , A61K31/4418 , A61K31/4422 , A61K31/443 , A61K31/444 , A61K31/496 , A61K31/675 , A61K31/695
摘要： The present invention makes available methods and reagents for inhibiting aberrant growth states resulting from hedgehog gain-of-function, ptc loss-of-function or smoothened gain-of-function comprising contacting the cell with a hedgehog antagonist, such as a small molecule, in a sufficient amount to aberrant growth state, e.g., to agonize a normal ptc pathway or antagonize smoothened or hedgehog activity. Such methods and reagents may also inhibit the hedgehog pathway in normal cells, e.g., where normal levels of hedgehog signalling are unwanted.
摘要翻译： 本发明提供用于抑制由刺猬获得功能，功能丧失功能或平滑增益功能引起的异常生长状态的可用方法和试剂，包括使细胞与刺猬蛋白拮抗剂如小分子接触， 足够量的异常生长状态，例如，激发正常的ptc途径或拮抗平滑或刺猬活性。 这些方法和试剂也可以抑制正常细胞中的刺猬蛋白通路，例如其中正常水平的刺猬蛋白信号传导是不需要的。
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公开(公告)号：US20090203713A1
公开(公告)日：2009-08-13
申请号：US11990729
申请日：2006-08-22
申请人： Philip A. Beachy , Jun O. Liu
发明人： Philip A. Beachy , Jun O. Liu
IPC分类号： A61K31/496 , A61P35/00
CPC分类号： A61K31/415 , A61K31/365 , A61K31/44 , A61K31/496 , A61K31/497
摘要： Compounds, compositions, kits and methods for modulating hedgehog pathway activity, and treating conditions related to abnormal or aberrant hedgehog pathway activity, are disclosed.
摘要翻译： 公开了用于调节刺猬蛋白通路活性的化合物，组合物，试剂盒和方法以及治疗与异常或异常的刺猬蛋白通路活性相关的病症。
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公开(公告)号：US20090088339A1
公开(公告)日：2009-04-02
申请号：US12330439
申请日：2008-12-08
申请人： Philip A. Beachy , Jussi Taipale
发明人： Philip A. Beachy , Jussi Taipale
IPC分类号： C40B30/06 , C12Q1/02 , A01K67/027 , G06Q50/00
CPC分类号： C12N15/1058 , A01K2217/05 , C07K14/705 , C12N15/1034 , G06Q50/22 , Y02A90/22
摘要： The present invention related to methods and reagents for generating and using activating mutations of receptors and ion channels.
摘要翻译： 本发明涉及用于产生和使用受体和离子通道的活化突变的方法和试剂。
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7.发明授权公开(公告)号：US06214794B1
公开(公告)日：2001-04-10
申请号：US08729743
申请日：1996-10-07
IPC分类号： C07K14475
CPC分类号： G01N33/92 , A61K38/00 , C07K14/43581 , C07K2319/00 , C07K2319/21 , C07K2319/23 , C07K2319/50 , C12N15/62 , G01N2500/10
摘要： The present invention provides two novel polypeptides, referred to as the “N” and “C” fragments of hedgehog, or N-terminal and C-terminal fragments, respectively, which are derived after specific cleavage at a Gly↓Cys Phe site recognized by the autoproteolytic domain in the native protein. Methods of identifying compositions which affect hedgehog activity based on inhibition of cholesterol modification of hedgehog protein are described. Also provided are methods of use of the N and C fragments.
摘要翻译： 本发明提供两种新的多肽，分别被称为刺猬蛋白的“N”和“C”片段，或分别在由Gly↓Cys Phe位点识别的Gly↓Cys Phe位点上特异性切割后产生的N-末端和C-末端片段 天然蛋白中的自体蛋白水解结构域。 描述了基于对刺猬蛋白胆固醇修饰的抑制影响刺猬蛋白活性的组合物的方法。 还提供了使用N和C片段的方法。
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公开(公告)号：US20230391861A1
公开(公告)日：2023-12-07
申请号：US18026546
申请日：2021-09-27
申请人： Philip A. BEACHY , Yunxiao ZHANG , Aashish MANGLIK , Wan-Jin LU , Shuo HAN , The Board of Trustees of the Leland Stanford Junior University
发明人： Philip A. Beachy , Yunxiao Zhang , Aashish Manglik , Wan-Jin Lu , Shuo Han
CPC分类号： C07K16/22 , C07K14/39 , C12N15/70 , C07K2317/569 , C07K2319/02 , C07K2319/03 , C07K2317/24 , A61K38/00
摘要： Provided is a conformation-specific antigen binding domain (ABD) specific for the Hedgehog receptor Patched1, which may be provided in the form of a nanobody. This nanobody potently activates the Hedgehog pathway in vitro and in vivo by stabilizing an alternative conformation of a Patched1 “switch helix”. This ABD or nanobody is water soluble, i.e. does not require lipid modifications for its activity, facilitating mechanistic studies of Hedgehog pathway activation and therapeutic use.
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公开(公告)号：US09440988B2
公开(公告)日：2016-09-13
申请号：US13363934
申请日：2012-02-01
IPC分类号： C07D491/048 , A61K31/4355 , A61K31/58 , C07D491/10 , C07D519/00 , C07J69/00
CPC分类号： C07D491/10 , A61K31/4355 , A61K31/58 , C07D491/048 , C07D519/00 , C07J69/00
摘要： The present invention makes available, inter alia, methods and reagents for modulating smoothened-dependent pathway activation. In certain embodiments, the subject methods can be used to counteract the phenotypic effects of unwanted activation of a hedgehog pathway, such as resulting from hedgehog gain-of-function, ptc loss-of-function or smoothened gain-of-function mutations.
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公开(公告)号：US09427431B2
公开(公告)日：2016-08-30
申请号：US13364121
申请日：2012-02-01
IPC分类号： A61K31/4355 , A61K31/00 , A61K31/435 , A61K31/438 , A61K31/58
CPC分类号： A61K31/4355 , A61K31/00 , A61K31/435 , A61K31/438 , A61K31/58
摘要： The present invention makes availables assays and reagents inhibiting paracrine and/or autocrine signals produced by a hedgehog protein or aberrant activation of a hedgehog signal transduction pathway, e.g., which involve the use of a steroidal alkaloid or other small molecule.
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