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公开(公告)号：US20170304383A1
公开(公告)日：2017-10-26
申请号：US15312593
申请日：2015-05-19
发明人： Roger BRIESEWITZ , Dehua PEI , Punit UPADHYAYA
摘要： Disclosed herein are novel compounds that are Ras inhibitors. Also disclosed are compositions comprising the compounds and methods of using the compounds in treating various diseases. In another aspect, provided is an antibody-drug-conjugate comprising an antibody conjugated with a compound described herein. In still another aspect, provided is a pharmaceutical composition comprising a compound or antibody-drug-conjugate described herein. In a further aspect, provided is method of treating a cancer comprising administering a therapeutically effective amount of a compound or antibody-drug-conjugate described herein to a patient in need thereof.
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2.发明授权Small molecule composite surfaces as inhibitors of protein-protein interactions 有权小分子复合物表面作为蛋白质 - 蛋白质相互作用的抑制剂公开(公告)号：US09260484B2
公开(公告)日：2016-02-16
申请号：US14126343
申请日：2012-06-15
申请人： Roger Briesewitz , Dehua Pei , Xianghong Wu
发明人： Roger Briesewitz , Dehua Pei , Xianghong Wu
摘要： A method of inhibiting a binding event between a target protein and a binding protein, comprising administering to a cell in vitro an effective amount of a non-naturally occurring bifunctional inhibitor molecule including (a) protein binding moiety, and (b) an effector region, wherein the protein binding moiety binds to a blocking protein, and wherein the effector region binds to the target protein in order to bind the target protein and the blocking protein and prevent access of the binding protein to the target protein. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
摘要翻译： 一种抑制靶蛋白和结合蛋白之间的结合事件的方法，包括向细胞体外施用有效量的非天然存在的双功能抑制剂分子，包括（a）蛋白质结合部分，和（b）效应子区域 其中所述蛋白质结合部分与阻断蛋白结合，并且其中所述效应区结合所述靶蛋白以便结合所述靶蛋白和所述阻断蛋白并阻止所述结合蛋白进入所述靶蛋白。 该摘要旨在作为用于在特定技术中进行搜索的扫描工具，而不意在限制本发明。
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3.发明申请SMALL MOLECULE COMPOSITE SURFACES AS INHIBITORS OF PROTEIN-PROTEIN INTERACTIONS 有权作为蛋白质 - 蛋白质相互作用的抑制剂的小分子复合表面公开(公告)号：US20140200186A1
公开(公告)日：2014-07-17
申请号：US14126343
申请日：2012-06-15
申请人： Roger Briesewitz , Dehua Pei , Xianghong Wu
发明人： Roger Briesewitz , Dehua Pei , Xianghong Wu
IPC分类号： C07K11/02
摘要： A method of inhibiting a binding event between a target protein and a binding protein, comprising administering to a cell in vitro an effective amount of a non-naturally occurring bifunctional inhibitor molecule including (a) protein binding moiety, and (b) an effector region, wherein the protein binding moiety binds to a blocking protein, and wherein the effector region binds to the target protein in order to bind the target protein and the blocking protein and prevent access of the binding protein to the target protein. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
摘要翻译： 一种抑制靶蛋白和结合蛋白之间的结合事件的方法，包括向细胞体外施用有效量的非天然存在的双功能抑制剂分子，包括（a）蛋白质结合部分，和（b）效应子区域 其中所述蛋白质结合部分与阻断蛋白结合，并且其中所述效应区结合所述靶蛋白以便结合所述靶蛋白和所述阻断蛋白并阻止所述结合蛋白进入所述靶蛋白。 该摘要旨在作为用于在特定技术中进行搜索的扫描工具，而不意在限制本发明。
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4.发明授权Oncokinase fusion polypeptides associated with hyperproliferative and related disorders, nucleic acids encoding the same and methods for detecting and identifying the same 有权与过度增殖和相关病症相关的肿瘤酶融合多肽，编码其的核酸以及用于检测和鉴定相同的方法公开(公告)号：US07585653B2
公开(公告)日：2009-09-08
申请号：US11706519
申请日：2007-02-15
申请人： Roger Briesewitz , John H. Griffin
发明人： Roger Briesewitz , John H. Griffin
CPC分类号： C07K14/71 , C07K2319/00
摘要： Oncokinase fusion polypeptides associated with hyperproliferative disorders and the polynucleotides encoding for such fusion polypeptides are provided. The fusion polypeptides have a C-terminal tyrosine kinase domain fused to an N-terminal domain that is not normally fused to the C-terminal tyrosine kinase domain and they possess constitutively activated tyrosine kinase activity. Also provided are methods for detecting and identifying the fusion polypeptides and polynucleotides and methods of diagnosing disease conditions associated with the fusion polypeptides and polynucleotides. In addition, screening assays for identifying agents useful for treating disease conditions associated with such fusion polypeptides and polynucleotides are provided. Furthermore, methods of treating disease conditions associated with the presence of the fusion polypeptides are provided.
摘要翻译： 提供了与过度增殖性病症相关的肿瘤酶融合多肽和编码这种融合多肽的多核苷酸。 融合多肽具有与N末端结构域融合的C-末端酪氨酸激酶结构域，其通常不与C末端酪氨酸激酶结构域融合，并且它们具有组成型激活的酪氨酸激酶活性。 还提供了用于检测和鉴定融合多肽和多核苷酸的方法以及诊断与融合多肽和多核苷酸相关的疾病状况的方法。 此外，提供了用于鉴定用于治疗与这种融合多肽和多核苷酸相关的疾病病症的试剂的筛选试验。 此外，提供了治疗与融合多肽存在相关的疾病状态的方法。
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5.发明授权Oncokinase fusion polypeptides associated with hyperproliferative and related disorders, nucleic acids encoding the same and methods for detecting and identifying the same 有权与过度增殖和相关病症相关的肿瘤酶融合多肽，编码其的核酸以及用于检测和鉴定相同的方法公开(公告)号：US07195876B2
公开(公告)日：2007-03-27
申请号：US10637356
申请日：2003-08-08
申请人： Roger Briesewitz , John H. Griffin
发明人： Roger Briesewitz , John H. Griffin
CPC分类号： C07K14/71 , C07K2319/00
摘要： Oncokinase fusion polypeptides associated with hyperproliferative disorders and the polynucleotides encoding for such fusion polypeptides are provided. The fusion polypeptides have a C-terminal tyrosine kinase domain fused to an N-terminal domain that is not normally fused to the C-terminal tyrosine kinase domain and they possess constitutively activated tyrosine kinase activity. Also provided are methods for detecting and identifying the fusion polypeptides and polynucleotides and methods of diagnosing disease conditions associated with the fusion polypeptides and polynucleotides. In addition, screening assays for identifying agents useful for treating disease conditions associated with such fusion polypeptides and polynucleotides are provided. Furthermore, methods of treating disease conditions associated with the presence of the fusion polypeptides are provided.
摘要翻译： 提供了与过度增殖性病症相关的肿瘤酶融合多肽和编码这种融合多肽的多核苷酸。 融合多肽具有与N末端结构域融合的C-末端酪氨酸激酶结构域，其通常不与C末端酪氨酸激酶结构域融合，并且它们具有组成型激活的酪氨酸激酶活性。 还提供了用于检测和鉴定融合多肽和多核苷酸的方法以及诊断与融合多肽和多核苷酸相关的疾病状况的方法。 此外，提供了用于鉴定用于治疗与这种融合多肽和多核苷酸相关的疾病病症的试剂的筛选试验。 此外，提供了治疗与融合多肽存在相关的疾病状态的方法。
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公开(公告)号：US10736932B2
公开(公告)日：2020-08-11
申请号：US15312593
申请日：2015-05-19
发明人： Roger Briesewitz , Dehua Pei , Punit Upadhyaya
IPC分类号： A61K47/68 , A61K38/12 , C07K7/64 , A61K38/01 , C07K16/28 , A61K31/01 , A61K39/395 , C07K14/47 , A61K38/00 , A61K39/00
摘要： Disclosed herein are novel compounds that are Ras inhibitors. Also disclosed are compositions comprising the compounds and methods of using the compounds in treating various diseases. In another aspect, provided is an antibody-drug-conjugate comprising an antibody conjugated with a compound described herein. In still another aspect, provided is a pharmaceutical composition comprising a compound or antibody-drug-conjugate described herein. In a further aspect, provided is method of treating a cancer comprising administering a therapeutically effective amount of a compound or antibody-drug-conjugate described herein to a patient in need thereof.
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公开(公告)号：US07060703B2
公开(公告)日：2006-06-13
申请号：US10691094
申请日：2003-10-22
IPC分类号： A61K31/496 , C07D403/10
CPC分类号： C07D403/06 , C07D403/14
摘要： Compounds of formula (I) in which R1, R2, R3 and R4 have the meanings given in the specification, are receptor tyrosine kinase inhibitors useful in the treatment of proliferative disorders, such as cancer.
摘要翻译： 其中R 1，R 2，R 3和R 4的式（I）化合物具有如下含义： 在本说明书中给出的是可用于治疗增殖性疾病如癌症的受体酪氨酸激酶抑制剂。
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8.发明申请Modulating a pharmacokinetic property of a drug by administering a bifunctional molecule containing the drug 有权通过施用含有该药物的双官能分子来调节药物的药代动力学性质公开(公告)号：US20050209265A1
公开(公告)日：2005-09-22
申请号：US11011776
申请日：2004-12-13
IPC分类号： A61K47/48 , A61K31/4745
CPC分类号： A61K47/55 , A61K47/54 , Y10S530/812
摘要： Bifunctional molecules and methods for their use are provided. The subject bifunctional molecules are conjugates of a drug moiety and a pharmacokinetic modulating moiety, where these two moieties are optionally joined by a linking group. The bifunctional molecules are further characterized in that they exhibit at least one modulated pharmacokinetic property upon administration to a host as compared to a free drug control. The subject bifunctional molecules find use in a variety of therapeutic applications.
摘要翻译： 提供了双功能分子及其使用方法。 主题双功能分子是药物部分和药代动力学调节部分的缀合物，其中这两个部分任选地通过连接基团连接。 双官能分子的特征还在于，与游离药物对照相比，它们在施用于宿主时表现出至少一种调节的药代动力学性质。 主题双功能分子可用于各种治疗应用。
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9.发明申请Administering bifunctional molecules containing a drug moiety and presenter protein ligand for therapy 有权管理含有药物部分的双功能分子和用于治疗的展示蛋白配体公开(公告)号：US20050209146A1
公开(公告)日：2005-09-22
申请号：US11011499
申请日：2004-12-13
申请人： Roger Briesewitz , Gerald Crabtree , Thomas Wandless , Gregory Ray , Kurt Vogel
发明人： Roger Briesewitz , Gerald Crabtree , Thomas Wandless , Gregory Ray , Kurt Vogel
CPC分类号： C12N9/90 , A61K38/00 , A61K47/54 , A61K47/552 , C07K5/1027 , C07K7/06 , C07K2319/00 , Y10S530/812
摘要： Bifunctional molecules and methods for their use in the production of binary complexes in a host are provided. The bifunctional molecule is a conjugate of a drug moiety and a presenter protein ligand. In the subject methods, an effective amount of the bifunctional molecule is administered to the host. The bifunctional molecule binds to the presenter protein to produce a binary complex that exhibits at least one of improved affinity, specificity or selectivity as compared to the corresponding free drug. The subject methods and compositions find use in a variety of therapeutic applications.
摘要翻译： 提供了双功能分子及其在宿主生产二元配合物中的应用。 双功能分子是药物部分和呈递蛋白质配体的缀合物。 在本方法中，向宿主施用有效量的双功能分子。 与相应的游离药物相比，双功能分子与展示蛋白结合以产生显示出改善的亲和力，特异性或选择性中的至少一种的二元复合物。 主题方法和组合物可用于各种治疗应用。
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10.发明授权Synthetic bifunctional molecules containing drug moiety and pharmacokinetic modulating moiety 有权含有药物部位和药代动力学调节部分的合成双功能分子公开(公告)号：US08044099B2
公开(公告)日：2011-10-25
申请号：US11011776
申请日：2004-12-13
IPC分类号： A01N37/10 , A61K31/00 , A61K38/43 , A61K38/45 , A61K38/00 , A61K31/19 , C07K1/00 , C07K17/00 , C07D261/04 , C07C62/00
CPC分类号： A61K47/55 , A61K47/54 , Y10S530/812
摘要： Bifunctional molecules and methods for their use are provided. The subject bifunctional molecules are conjugates of a drug moiety and a pharmacokinetic modulating moiety, where these two moieties are optionally joined by a linking group. The bifunctional molecules are further characterized in that they exhibit at least one modulated pharmacokinetic property upon administration to a host as compared to a free drug control. The subject bifunctional molecules find use in a variety of therapeutic applications.
摘要翻译： 提供了双功能分子及其使用方法。 主题双功能分子是药物部分和药代动力学调节部分的缀合物，其中这两个部分任选地通过连接基团连接。 双官能分子的特征还在于，与游离药物对照相比，它们在施用于宿主时表现出至少一种调节的药代动力学性质。 主题双功能分子可用于各种治疗应用。
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