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公开(公告)号：US08349814B2
公开(公告)日：2013-01-08
申请号：US13049785
申请日：2011-03-16
申请人： Julian Adams , Mark L. Behnke , Alfredo C. Castro , Catherine A. Evans , Louis Grenier , Michael J. Grogan , Tao Liu , Daniel A. Snyder , Thomas T. Tibbitts
发明人： Julian Adams , Mark L. Behnke , Alfredo C. Castro , Catherine A. Evans , Louis Grenier , Michael J. Grogan , Tao Liu , Daniel A. Snyder , Thomas T. Tibbitts
摘要： The present invention provide compounds, and pharmaceutical compositions thereof, encompassed by the formulae (I), (II) or (III). The present invention also provides methods for treating an FAAH mediated disease, disorder or condition by administering a therapeutically effective amount of a provided compound of the formulae (I), (II) or (III), or a pharmaceutical composition thereof, to a patient in need thereof. Additionally, the present invention provides methods for inhibiting FAAH in a patient by administering a therapeutically effective amount of a compound of the formulae (I), (II) or (III), or a pharmaceutical composition thereof, to a patient in need thereof.
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2.发明申请Analogs of Benzoquinone-Containing Ansamycins and Methods of Use Thereof 有权含有苯并醌的Ansamycins的类似物及其使用方法公开(公告)号：US20120058982A1
公开(公告)日：2012-03-08
申请号：US13191761
申请日：2011-07-27
申请人： Julian Adams , Yun Gao , Asimina T. Georges Evangelinos , Louis Grenier , Roger H. Pak , James R. Porter , James L. Wright
发明人： Julian Adams , Yun Gao , Asimina T. Georges Evangelinos , Louis Grenier , Roger H. Pak , James R. Porter , James L. Wright
IPC分类号： A61K31/395 , A61P35/00
CPC分类号： A61K31/395 , C07D211/60 , C07D225/06 , C07F9/6561
摘要： The present invention provides analogs of benzoquinone-containing ansamycins and uses thereof for treating and modulating disorders associated with hyperproliferation, such as cancer. The present invention provides analogs of benzoquinone-containing ansamycins where the benzoquinone is reduced to a hydroquinone and trapped by reaction with a suitable acid, preferably ones that increase the solubility and air stability of the resulting 17-ammonium hydroquinone ansamycin analog.
摘要翻译： 本发明提供了含苯醌的安莎霉素类似物及其用于治疗和调节与过度增生相关的疾病如癌症的用途。 本发明提供了含有苯醌的安莎霉素的类似物，其中苯醌被还原成氢醌并通过与合适的酸反应而被捕获，优选是增加所得17-氢醌醌霉素类似物的溶解度和空气稳定性的那些。
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公开(公告)号：US07947663B2
公开(公告)日：2011-05-24
申请号：US11870130
申请日：2007-10-10
申请人： Julian Adams , Mark L. Behnke , Alfredo C. Castro , Catherine A. Evans , Louis Grenier , Michael J. Grogan , Tao Liu , Daniel A. Snyder , Thomas T. Tibbitts
发明人： Julian Adams , Mark L. Behnke , Alfredo C. Castro , Catherine A. Evans , Louis Grenier , Michael J. Grogan , Tao Liu , Daniel A. Snyder , Thomas T. Tibbitts
摘要： The present invention provide compounds, and pharmaceutical compositions thereof, encompassed by the formulae (I), (II) or (III). The present invention also provides methods for treating an FAAH mediated disease, disorder or condition by administering a therapeutically effective amount of a provided compound of the formulae (I), (II) or (III), or a pharmaceutical composition thereof, to a patient in need thereof. Additionally, the present invention provides methods for inhibiting FAAH in a patient by administering a therapeutically effective amount of a compound of the formulae (I), (II) or (III), or a pharmaceutical composition thereof, to a patient in need thereof.
摘要翻译： 本发明提供由式（I），（II）或（III）包含的化合物及其药物组合物。 本发明还提供了通过向患者施用治疗有效量的所提供的式（I），（II）或（III）化合物或其药物组合物来治疗FAAH介导的疾病，病症或病症的方法。 需要它。 此外，本发明提供了通过向有需要的患者施用治疗有效量的式（I），（II）或（III）化合物或其药物组合物来抑制患者的FAAH的方法。
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公开(公告)号：US07566706B2
公开(公告)日：2009-07-28
申请号：US11105203
申请日：2005-04-13
申请人： Julian Adams , Yun Gao , Asimina T. Georges Evangelinos , Louis Grenier , Roger H. Pak , James R. Porter , James L. Wright
发明人： Julian Adams , Yun Gao , Asimina T. Georges Evangelinos , Louis Grenier , Roger H. Pak , James R. Porter , James L. Wright
IPC分类号： A61P35/00
CPC分类号： A61K31/395 , C07D211/60 , C07D225/06 , C07F9/6561
摘要： The present invention provides analogs of benzoquinone-containing ansamycins and uses thereof for treating and modulating disorders associated with hyperproliferation, such as cancer. The present invention provides analogs of benzoquinone-containing ansamycins where the benzoquinone is reduced to a hydroquinone and trapped by reaction with a suitable acid, preferably ones that increase the solubility and air stability of the resulting 17-ammonium hydroquinone ansamycin analog.
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公开(公告)号：US07230004B2
公开(公告)日：2007-06-12
申请号：US11213534
申请日：2005-08-26
申请人： Julian Adams , Alfredo C. Castro , Michael A. Foley , Somarajan Nair Janardanan Nair , Marta Nevalainen , James R. Porter , Martin R. Tremblay
发明人： Julian Adams , Alfredo C. Castro , Michael A. Foley , Somarajan Nair Janardanan Nair , Marta Nevalainen , James R. Porter , Martin R. Tremblay
IPC分类号： A61K31/438 , A61K31/4355 , C07D491/10 , C07D491/048
CPC分类号： C07D491/04
摘要： The present invention provides compositions and methods for modulating smoothened-dependent pathway activation. The present invention provides analogs of cyclopamine that 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. The compounds of the present invention are particularly useful in treating cancers.
摘要翻译： 本发明提供用于调节平滑依赖性途径激活的组合物和方法。 本发明提供环巴胺的类似物，其可用于抵消刺猬蛋白途径的不期望的活化的表型效应，例如由刺猬蛋白获得功能，Ptc功能丧失或平滑获得功能突变引起的表型效应。 本发明的化合物特别可用于治疗癌症。
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公开(公告)号：US07119080B2
公开(公告)日：2006-10-10
申请号：US10730231
申请日：2003-12-08
申请人： Julian Adams , Yu-Ting Ma , Ross L. Stein , Matthew Baevsky , Louis Grenier , Louis Plamondon
发明人： Julian Adams , Yu-Ting Ma , Ross L. Stein , Matthew Baevsky , Louis Grenier , Louis Plamondon
CPC分类号： C07K5/0808 , A61K38/00 , C07F5/025 , C07F5/04 , C07K5/06 , C07K5/06043 , C07K5/06139 , C07K5/06191 , C07K5/0827
摘要： Disclosed herein is a method for reducing the rate of degradation of proteins in an animal, comprising contacting cells of the animal with certain boronic ester and acid compounds. Also disclosed herein are novel boronic ester and acid compounds, their synthesis and uses.
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公开(公告)号：US20060074030A1
公开(公告)日：2006-04-06
申请号：US11213534
申请日：2005-08-26
申请人： Julian Adams , Alfredo Castro , Michael Foley , Somarajan Janardanan Nair , Marta Nevalainen , James Porter , Martin Tremblay
发明人： Julian Adams , Alfredo Castro , Michael Foley , Somarajan Janardanan Nair , Marta Nevalainen , James Porter , Martin Tremblay
IPC分类号： A61K31/7052 , A61K31/4747 , C07D491/10
CPC分类号： C07D491/04
摘要： The present invention provides compositions and methods for modulating smoothened-dependent pathway activation. The present invention provides analogs of cyclopamine that 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. The compounds of the present invention are particularly useful in treating cancers.
摘要翻译： 本发明提供用于调节平滑依赖性途径激活的组合物和方法。 本发明提供环巴胺的类似物，其可用于抵消刺猬蛋白途径的不期望的活化的表型效应，例如由刺猬蛋白获得功能，Ptc功能丧失或平滑获得功能突变引起的表型效应。 本发明的化合物特别可用于治疗癌症。
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8.发明申请公开(公告)号：US20050227955A1
公开(公告)日：2005-10-13
申请号：US11022057
申请日：2004-12-23
申请人： Julian Adams , Yun Gao , Asimina Evangelinos , Louis Grenier , Roger Pak , James Porter , James Wright
发明人： Julian Adams , Yun Gao , Asimina Evangelinos , Louis Grenier , Roger Pak , James Porter , James Wright
IPC分类号： C07D211/60 , C07D225/06 , C07D498/08 , C07F5/02 , C07F9/6561 , A61K31/538 , A61K31/424 , C07D487/02 , C07D491/14
CPC分类号： A61K31/395 , C07D211/60 , C07D225/06 , C07F9/6561
摘要： The present invention provides analogs of benzoquinone-containing ansamycins and uses thereof for treating and modulating disorders associated with hyperproliferation, such as cancer. The present invention provides analogs of benzoquinone-containing ansamycins where the benzoquinone is reduced to a hydroquinone and trapped by reaction with a suitable acid, preferably ones that increase the solubility and air stability of the resulting 17-ammonium hydroquinone ansamycin analog.
摘要翻译： 本发明提供了含苯醌的安莎霉素类似物及其用于治疗和调节与过度增生相关的疾病如癌症的用途。 本发明提供了含有苯醌的安莎霉素的类似物，其中苯醌被还原成氢醌并通过与合适的酸反应而被捕获，优选是增加所得17-氢醌醌霉素类似物的溶解度和空气稳定性的那些。
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公开(公告)号：US06699835B2
公开(公告)日：2004-03-02
申请号：US10056563
申请日：2002-01-25
IPC分类号： A61K3800
CPC分类号： C07K5/0827 , A61K38/00 , C07F5/025 , C07F5/04 , C07K5/06191 , C07K7/02
摘要： The invention relates to the formulation of pharmaceutical compounds. More particularly, the invention provides stable, pharmaceutically acceptable compositions prepared from boronic acid compounds and methods for preparing the compositions. The invention also provides novel boronate ester compounds. The invention further provides boronic acid anhydride compounds useful in the methods of the invention.
摘要翻译： 本发明涉及药物化合物的制剂。 更具体地，本发明提供由硼酸化合物制备的稳定的药学上可接受的组合物和制备组合物的方法。 本发明还提供新的硼酸酯化合物。 本发明还提供了可用于本发明方法的硼酸酐化合物。
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公开(公告)号：US06297217B1
公开(公告)日：2001-10-02
申请号：US09490511
申请日：2000-01-25
申请人： Julian Adams , Yu-Ting Ma , Ross Stein , Matthew Baevsky , Louis Grenier , Louis Plamondon
发明人： Julian Adams , Yu-Ting Ma , Ross Stein , Matthew Baevsky , Louis Grenier , Louis Plamondon
IPC分类号： A61K3169
CPC分类号： C07K5/0808 , A61K38/00 , C07F5/025 , C07F5/04 , C07K5/06 , C07K5/06043 , C07K5/06139 , C07K5/06191 , C07K5/0827
摘要： Disclosed herein is a method for reducing the rate of degradation of proteins in an animal comprising contacting cells of the animal with certain boronic ester and acid compounds. Also disclosed herein are novel boronic ester and acid compounds, their synthesis and uses.
摘要翻译： 本文公开了一种用于降低动物中蛋白质降解速率的方法，包括使动物细胞与某些硼酸酯和酸化合物接触。 本文还公开了新的硼酸酯和酸化合物，它们的合成和用途。
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