公开(公告)号：US07767663B2

公开(公告)日：2010-08-03

申请号：US12369545

申请日：2009-02-11

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.

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。

公开(公告)号：US07767662B2

公开(公告)日：2010-08-03

申请号：US12199356

申请日：2008-08-27

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 ,  A61K35/00 ,  C07D225/06 ,  C07D211/60 ,  C07D498/08

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.

公开(公告)号：US20090208590A1

公开(公告)日：2009-08-20

申请号：US12369549

申请日：2009-02-11

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： A61K33/24 ,  A61K31/33 ,  A61K31/337 ,  A61K31/496 ,  A61K31/7068 ,  A61K31/69 ,  A61K31/505 ,  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.

公开(公告)号：US20090088414A1

公开(公告)日：2009-04-02

申请号：US12199415

申请日：2008-08-27

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： A61K31/33 ,  C07D225/06

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.

公开(公告)号：US20090069280A1

公开(公告)日：2009-03-12

申请号：US12199356

申请日：2008-08-27

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 ,  A61P35/04

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。

公开(公告)号：US20080132678A1

公开(公告)日：2008-06-05

申请号：US12006422

申请日：2008-01-02

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

IPC分类号： C07K5/06 ,  C07F5/02

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。

公开(公告)号：US07348336B2

公开(公告)日：2008-03-25

申请号：US11390287

申请日：2006-03-28

申请人： Olaf Ritzeler ,  Alfredo Castro ,  Louis Grenier ,  Francois Soucy ,  Wayne W. Hancock ,  Hormoz Mazdiyasni ,  Vito Palombella ,  Julian Adams

发明人： Olaf Ritzeler ,  Alfredo Castro ,  Louis Grenier ,  Francois Soucy ,  Wayne W. Hancock ,  Hormoz Mazdiyasni ,  Vito Palombella ,  Julian Adams

IPC分类号： C07D471/02 ,  A61K31/44

CPC分类号： A61K31/437 ,  C07D471/04 ,  Y02A50/411

摘要： The subject matter of the present invention is directed to novel substituted β-carbolines, and specifically compounds of the formula I, which are suitable for the production of pharmaceuticals for the prophylaxis and therapy of disorders in whose course an increased activity of IκB kinase is involved.

摘要翻译： 本发明的主题涉及新的取代的β-咔啉，特别是式I化合物，其适用于生产用于预防和治疗IkappaB激酶活性增加的病症的药物 。

公开(公告)号：US20060019939A1

公开(公告)日：2006-01-26

申请号：US11105203

申请日：2005-04-13

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： A61K31/538 ,  C07D487/02

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.

公开(公告)号：US20050288269A1

公开(公告)日：2005-12-29

申请号：US11107404

申请日：2005-04-14

申请人： Julian Adams ,  Yun Gao ,  Asimina Georges Evangelinos ,  Louis Grenier ,  Roger Pak ,  James Porter ,  James Wright

发明人： Julian Adams ,  Yun Gao ,  Asimina Georges Evangelinos ,  Louis Grenier ,  Roger Pak ,  James Porter ,  James Wright

IPC分类号： C07D211/60 ,  C07D225/06 ,  C07D498/08 ,  C07F5/02 ,  C07F9/6561 ,  A61K31/33 ,  C07D225/04

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.

公开(公告)号：US06617317B1

公开(公告)日：2003-09-09

申请号：US10125997

申请日：2002-04-19

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性化合物接触。 本文还公开了新的硼酸酯和酸化合物，它们的合成和用途。