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公开(公告)号：US08101186B2
公开(公告)日：2012-01-24
申请号：US11676148
申请日：2007-02-16
CPC分类号： C07K14/70539 , A61K38/00 , C07K7/06 , C07K7/08 , C07K14/00 , C07K14/70535 , G01N2333/70535
摘要： The invention relates to peptides which bind to human FcRn and inhibit binding of the Fc portion of an IgG to an FcRn, thereby modulating serum IgG levels. The disclosed compositions and methods may be used for example, in treating autoimmune diseases and inflammatory disorders. The invention also relates to methods of using and methods of making the peptides of the invention.
摘要翻译： 本发明涉及结合人FcRn并抑制IgG的Fc部分与FcRn的结合的肽，从而调节血清IgG水平。 所公开的组合物和方法可用于例如治疗自身免疫性疾病和炎症性疾病。 本发明还涉及制备本发明的肽的方法和制备方法。
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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 。
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3.发明申请Compounds and methods for inhibiting the interaction of BCL proteins with binding partners 有权抑制BCL蛋白与结合配偶体相互作用的化合物和方法公开(公告)号：US20070155705A1
公开(公告)日：2007-07-05
申请号：US11640480
申请日：2006-12-15
申请人： Alfredo Castro , Michael Grogan , Edward Holson , Brian Hopkins , Nii Koney , Stephane Peluso , Daniel Snyder
发明人： Alfredo Castro , Michael Grogan , Edward Holson , Brian Hopkins , Nii Koney , Stephane Peluso , Daniel Snyder
IPC分类号： A61K31/66 , A61K31/421 , A61K31/426 , C07F9/02
CPC分类号： C07D207/16 , C07D207/08 , C07D207/12 , C07D207/14 , C07D211/60 , C07D233/32 , C07D265/30 , C07D277/04 , C07D277/06 , C07D295/04
摘要： The present invention relates to heterocyclic compounds that bind to Bcl proteins and inhibit Bcl function, compositions comprising such compounds, and methods for treating and modulating disorders associated with hyperproliferation, such as cancer.
摘要翻译： 本发明涉及结合Bcl蛋白并抑制Bcl功能的杂环化合物，包含这些化合物的组合物，以及用于治疗和调节与过度增殖相关的疾病如癌症的方法。
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4.发明申请公开(公告)号：US20060025460A1
公开(公告)日：2006-02-02
申请号：US11156364
申请日：2005-06-17
申请人： Alfredo Castro , Wei Deng , Kristopher Depew , Michael Foley , Christian Fritz , Asimina Georges Evangelinos , Michael Grogan , Nafeeza Hafeez , Edward Holson , Brian Hopkins , Nii Koney , Tao Liu , David Mann , Lisa Marcaurelle , Daniel Snyder , Dennis Underwood , Andrew Wylie , Lin-Chen Yu , Linping Zhang
发明人： Alfredo Castro , Wei Deng , Kristopher Depew , Michael Foley , Christian Fritz , Asimina Georges Evangelinos , Michael Grogan , Nafeeza Hafeez , Edward Holson , Brian Hopkins , Nii Koney , Tao Liu , David Mann , Lisa Marcaurelle , Daniel Snyder , Dennis Underwood , Andrew Wylie , Lin-Chen Yu , Linping Zhang
IPC分类号： C07D261/02 , A61K31/42
CPC分类号： C07D261/02 , C07D261/18 , C07D413/10 , C07D413/12 , C07D417/12 , C07D498/04
摘要： One aspect of the present invention relates to heterocyclic compounds that bind to bcl proteins and inhibit Bcl function. Another aspect of the present invention relates to compositions comprising a heterocyclic compound of the invention. The present invention provides methods for treating and modulating disorders associated with hyperproliferation, such as cancer.
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公开(公告)号：US08431566B2
公开(公告)日：2013-04-30
申请号：US13250080
申请日：2011-09-30
IPC分类号： A61K31/55 , C07D491/20
CPC分类号： C07D491/20 , C07D215/06
摘要： The present invention relates to steroidal alkaloids useful in the treatment of hedgehog pathway related disorders, particularly cancer.
摘要翻译： 本发明涉及可用于治疗刺猬蛋白通路相关疾病，特别是癌症的类固醇生物碱。
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公开(公告)号：US20070254831A1
公开(公告)日：2007-11-01
申请号：US11676148
申请日：2007-02-16
申请人： Adam Mezo , Kevin McDonnell , Cristina Hehir , Alfredo Castro
发明人： Adam Mezo , Kevin McDonnell , Cristina Hehir , Alfredo Castro
CPC分类号： C07K14/70539 , A61K38/00 , C07K7/06 , C07K7/08 , C07K14/00 , C07K14/70535 , G01N2333/70535
摘要： The invention relates to peptides which bind to human FcRn and inhibit binding of the Fc portion of an IgG to an FcRn, thereby modulating serum IgG levels. The disclosed compositions and methods may be used for example, in treating autoimmune diseases and inflammatory disorders. The invention also relates to methods of using and methods of making the peptides of the invention.
摘要翻译： 本发明涉及结合人FcRn并抑制IgG的Fc部分与FcRn的结合的肽，从而调节血清IgG水平。 所公开的组合物和方法可用于例如治疗自身免疫性疾病和炎症性疾病。 本发明还涉及制备本发明的肽的方法和制备方法。
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公开(公告)号：US07026331B2
公开(公告)日：2006-04-11
申请号：US10627978
申请日：2003-07-28
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 beta-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 。
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公开(公告)号：US06552216B1
公开(公告)日：2003-04-22
申请号：US09236784
申请日：1999-01-25
申请人： Juswinder Singh , Zhongli Zheng , Peter Sprague , Herman Van Vlijmen , Alfredo Castro , Steven P. Adams
发明人： Juswinder Singh , Zhongli Zheng , Peter Sprague , Herman Van Vlijmen , Alfredo Castro , Steven P. Adams
IPC分类号： C07C20500
CPC分类号： C07C275/40 , A61K31/185 , A61K31/197 , A61K31/27 , A61K31/341 , A61K31/36 , A61K31/381 , A61K31/40 , A61K31/4015 , A61K31/4035 , A61K31/405 , A61K31/416 , A61K31/4184 , A61K31/421 , A61K31/426 , A61K31/443 , A61K31/4433 , A61K31/445 , A61K31/4525 , A61K31/4535 , A61K31/454 , A61K31/496 , A61K31/501 , A61K31/505 , A61K31/54 , A61K31/55 , A61K31/5513 , C07C275/42 , C07C311/06 , C07C311/60 , C07C323/41 , C07D207/09 , C07D207/16 , C07D207/26 , C07D207/27 , C07D209/08 , C07D209/42 , C07D211/26 , C07D211/34 , C07D211/60 , C07D211/70 , C07D213/75 , C07D217/26 , C07D233/68 , C07D233/88 , C07D237/04 , C07D243/12 , C07D243/14 , C07D243/24 , C07D253/06 , C07D271/107 , C07D271/113 , C07D273/00 , C07D277/06 , C07D277/46 , C07D277/56 , C07D295/135 , C07D295/15 , C07D307/68 , C07D317/58 , C07D317/60 , C07D335/10 , C07D401/04 , C07D401/06 , C07D401/14 , C07D403/12 , C07D405/06 , C07D405/12 , C07D471/04 , C07K5/0202 , C07K5/021 , C07K5/06026 , C07K5/0808 , C07K5/0823 , G01N33/68 , G01N2500/00
摘要： Pharmacophore models of VLA-4 inhibitors, methods of identifying novel inhibitors and novel inhibitors identified by these methods.
摘要翻译： VLA-4抑制剂的药效学模型，鉴定新型抑制剂的方法和通过这些方法鉴定的新型抑制剂。
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公开(公告)号：US20100093713A1
公开(公告)日：2010-04-15
申请号：US12640335
申请日：2009-12-17
申请人： Michael E. Hepperle , Julie Fields Liu , Francois Soucy , Yingchun Ye , Robert S. Murray , Raman Prakash , Jeremy D. Little , Alfredo Castro , Hormoz Mazdiyasni , Paul E. Fleming , Dominic Reynolds
发明人： Michael E. Hepperle , Julie Fields Liu , Francois Soucy , Yingchun Ye , Robert S. Murray , Raman Prakash , Jeremy D. Little , Alfredo Castro , Hormoz Mazdiyasni , Paul E. Fleming , Dominic Reynolds
IPC分类号： A61K31/541 , C07D471/04 , A61P35/04 , A61P37/00 , A61K31/5377 , A61P29/00 , A61K31/501 , A61K31/437 , C07D295/10
CPC分类号： C07D265/30 , C07D471/04
摘要： This invention provides beta-carboline compounds of formula wherein Ring A is a substituted pyridinyl, pyrimidinyl, morpholinyl, piperidinyl, piperazinyl, pyrrolidinyl, pyranyl, tetrahydrofuranyl, cyclohexyl, cyclopentyl or thiomorpholinyl ring and R1, R2 and R3 are as described in the specification. The compounds are IKK-2 inhibitors that are useful for treating IKK-2-mediated diseases such as inflammatory diseases and cancer.
摘要翻译： 本发明提供下式的β-咔啉化合物，其中环A是取代的吡啶基，嘧啶基，吗啉基，哌啶基，哌嗪基，吡咯烷基，吡喃基，四氢呋喃基，环己基，环戊基或硫代吗啉基，R1，R2和R3如说明书中所述。 这些化合物是可用于治疗IKK-2介导的疾病如炎性疾病和癌症的IKK-2抑制剂。
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10.发明申请Compounds and methods for inhibiting the interaction of BCL proteins with binding partners 有权抑制BCL蛋白与结合配偶体相互作用的化合物和方法公开(公告)号：US20080306127A9
公开(公告)日：2008-12-11
申请号：US11600332
申请日：2006-11-15
申请人： Alfredo Castro , Edward Holson , Brian Hopkins , Nii Koney , Daniel Snyder , Thomas Tibbitts
发明人： Alfredo Castro , Edward Holson , Brian Hopkins , Nii Koney , Daniel Snyder , Thomas Tibbitts
IPC分类号： A61K31/42 , C07D413/02 , C07D261/02
CPC分类号： C07D261/02 , C07D261/18 , C07D413/10 , C07D413/12 , C07D417/12 , C07D498/04
摘要： One aspect of the present invention relates to heterocyclic compounds that bind to bcl proteins and inhibit Bcl function. Another aspect of the present invention relates to compositions comprising a heterocyclic compound of the invention. The present invention provides methods for treating and modulating disorders associated with hyperproliferation, such as cancer.
摘要翻译： 本发明的一个方面涉及结合bcl蛋白并抑制Bcl功能的杂环化合物。 本发明的另一方面涉及包含本发明的杂环化合物的组合物。 本发明提供了治疗和调节与过度增生相关的疾病如癌症的方法。
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