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1. 发明申请

WO2005069771A3 SMALL MOLECULE ANTAGONISTS OF BCL-2 FAMILY PROTEINS 审中-公开
标题翻译： BCL-2家族蛋白的小分子拮抗剂
公开(公告)号：WO2005069771A3
公开(公告)日：2006-02-23
申请号：PCT/US2004040553
申请日：2004-12-06
申请人： UNIV MICHIGAN , UNIV GEORGETOWN MED CENTER , WANG SHAOMENG , YANG DAJUN
发明人： WANG SHAOMENG , YANG DAJUN
IPC分类号： C12Q1/02 , A61K31/11 , A61K31/12 , A61K31/122 , A61K31/135 , A61K31/19 , A61K31/225 , A61K31/335 , A61K45/00 , A61K45/06 , A61P9/00 , A61P31/04 , A61P31/10 , A61P31/12 , A61P31/18 , A61P35/00 , A61P35/02 , A61P43/00
CPC分类号： A61K31/11 , A61K45/06 , A61K2300/00
摘要： The present invention relates to naturally occurring and chemically synthesized small molecule antagonists of Bcl-2 family proteins. In particular, the present invention provides gossypol compounds (
摘要翻译：本发明涉及Bcl-2家族蛋白质的天然存在和化学合成的小分子拮抗剂。特别地，本发明提供棉酚化合物（<

2. 发明申请

WO0073326A3 REDOX-STABLE, NON-PHOSPHORYLATED CYCLIC PEPTIDE INHIBITORS OF SH2 DOMAIN BINDING TO TARGET PROTEIN, CONJUGATES THEREOF, COMPOSITIONS AND METHODS OF SYNTHESIS AND USE 审中-公开
标题翻译： SH2结合到目标蛋白上的REDOX-STABLE，非磷酸化循环肽抑制剂，其结合物，组合物和合成和使用方法
公开(公告)号：WO0073326A3
公开(公告)日：2001-05-25
申请号：PCT/US0015201
申请日：2000-06-02
申请人： US GOV HEALTH & HUMAN SERV , ROLLER PETER P , LONG YA QUI , LUNG FENG DI T , KING C RICHTER , YANG DAJUN
发明人： ROLLER PETER P , LONG YA-QUI , LUNG FENG-DI T , KING C RICHTER , YANG DAJUN
IPC分类号： A61K38/00 , C07K7/06 , C07K7/56 , C07K14/47
CPC分类号： C07K7/56 , A61K38/00 , A61K47/64 , C07K7/06
摘要： The present invention provides a compound of formula (I) in which L is sulfur, sulfoxide, oxygen or methylene, and in which, optionally, one or more of Tyr , Glu , Val , Met and Tyr is modified. Also provided is a compound of formula (II) in which (i)aa is Adi and aa is Glu or (ii) each of aa and is Adi, L is sulfur, sulfoxide, oxygen or methylene, and in which, optionally, one or more of Tyr , Val , Met and Tyr is modified. The above compounds (and their conjugates) bind to an SH2 domain in a protein comprising an SH2 domain, are non-phosphorylated, are redox-stable in vivo , and are characterized by an IC50 in vivo of less than about 4.0 mu M with respect to the SH2 domain in Grb2. Upon binding to the SH2 domain of Grb2, a compound as described above has a turn conformation. Optionally, there is a conservative or neutral amino acid substitution at either one or both of Leu and Gly . Also provided by the present invention is a conjugate comprising a compound as described above and a carrier agent, a composition comprising (i) a compound or a conjugate as described above and (ii) a carrier, a method of inhibiting binding of an SH2 domain in a protein comprising an SH2 domain to a target protein in an animal, wherein the SH2 domain is contacted with a target protein-binding inhibiting effective amount of a compound or a conjugate as described above, and a method of synthesizing such conjugates.
摘要翻译：本发明提供式（I）化合物，其中L是硫，亚砜，氧或亚甲基，并且其中任选地，一个或多个Tyr 3，Glu 4，Val 6， 8>和Tyr <9>被修饰。还提供了式（II）化合物，其中（i）aa 1是Adi，aa 4是Glu或（ii）a a 1各自为Ad 1，L为硫，亚砜，氧或亚甲基，并且其中任选地，Tyr 3，Val 6，Met 8和Tyr 9中的一个或多个被修饰。上述化合物（及其缀合物）与包含SH2结构域的蛋白质中的SH2结构域结合，未被磷酸化，在体内是氧化还原稳定的，其特征在于IC 50 相对于Grb2中的SH2结构域，体积小于约4.0μM。当结合到Grb2的SH2结构域时，如上所述的化合物具有转向构象。任选地，在Leu 2和Gly 7中的任一个或两个上存在保守或中性氨基酸取代。本发明还提供了包含上述化合物和载体剂的组合物，包含（i）如上所述的化合物或缀合物和（ii）载体的组合物，抑制SH2结构域结合的方法在包含SH2结构域的蛋白质中与动物中的靶蛋白质相结合，其中SH2结构域与靶蛋白结合抑制有效量的上述化合物或结合物接触，以及合成这种缀合物的方法。

3. 发明申请

WO2010056932A1 PULSATILE DOSING OF GOSSYPOL FOR TREATMENT OF DISEASE 审中-公开
标题翻译：用于治疗疾病的药物治疗药物
公开(公告)号：WO2010056932A1
公开(公告)日：2010-05-20
申请号：PCT/US2009/064295
申请日：2009-11-13
申请人： ASCENTA THERAPEUTICS, INC. , HOLMLUND, Jon, T. , SORENSEN, Mel , LEOPOLD, Lance , YANG, Dajun
发明人： HOLMLUND, Jon, T. , SORENSEN, Mel , LEOPOLD, Lance , YANG, Dajun
IPC分类号： A61K45/00
CPC分类号： A61K31/12 , A61K31/282 , A61K31/337 , A61K31/437 , A61K31/454 , A61K31/517 , A61K45/06 , A61K2300/00
摘要： This invention relates to pulsatile dose administration of gossypol or pharmaceutical compositions thereof for treating diseases, disorders and conditions responsive to gossypol, inhibiting the activity of anti-apoptotic Bcl-2 family proteins, inducing apoptosis in cells and increasing the sensitivity of cells to inducers of apoptosis.
摘要翻译：本发明涉及棉酚的脉动剂量给药或其药物组合物，用于治疗对棉酚有反应的疾病，病症和病症，抑制抗凋亡Bcl-2家族蛋白的活性，诱导细胞凋亡，并增加细胞对诱导剂的敏感性细胞凋亡。

4. 发明申请

WO2002097053A2 SMALL MOLECULE ANTAGONISTS OF BCL2 FAMILY PROTEINS 审中-公开
标题翻译： BCL2家族蛋白的小分子拮抗剂
公开(公告)号：WO2002097053A2
公开(公告)日：2002-12-05
申请号：PCT/US2002/017206
申请日：2002-05-30
申请人： THE REGENTS OF THE UNIVERSITY OF MICHIGAN , WANG, Shaomeng , YANG, Dajun
发明人： WANG, Shaomeng , YANG, Dajun
IPC分类号： C12N
CPC分类号： A61K31/11 , A61K45/06 , A61K2300/00
摘要： The present invention relates to naturally occurring and chemically synthesized small molecules antagonists of Bcl-2 family proteins. In particular, the present invention provides gossypol derivatives and methods of using gossypol derivatives as antagonists of the anti-apoptotic effects of Bcl-2 and Bcl-X L proteins especially in cancer cells that overexpress Bcl-2 family proteins (e.g., Bcl-2 and/or Bcl-X L ).
摘要翻译：本发明涉及Bcl-2家族蛋白质的天然存在和化学合成的小分子拮抗剂。特别地，本发明提供棉酚衍生物和使用棉酚衍生物作为Bcl-2和Bcl-XL蛋白的抗凋亡作用的拮抗剂的方法，特别是在过表达Bcl-2家族蛋白（例如Bcl-2和 /或Bcl-XL）。

5. 发明申请

WO0213833A2 SMALL MOLECULE INHIBITORS TARGETED AT Bcl-2 审中-公开
标题翻译：小分子抑制剂定位于Bcl-2
公开(公告)号：WO0213833A2
公开(公告)日：2002-02-21
申请号：PCT/US0125575
申请日：2001-08-16
申请人： UNIV GEORGETOWN MED CENTER , WANG SHAOMENG , YANG DAJUN , ENYEDY ISTVAN J
发明人： WANG SHAOMENG , YANG DAJUN , ENYEDY ISTVAN J
IPC分类号： A61K31/33 , A61K31/655 , A61K31/675 , A61K31/70 , A61K33/24 , A61K45/06 , A61P35/00 , A61P35/04
CPC分类号： A61K31/655 , A61K31/675 , A61K31/70 , A61K33/24 , A61K45/06 , A61K2300/00
摘要： A method for promotion of cell death in tumor cells using tricylo-dibenzo-diazocine-dioxides that bind to a pocket of Bcl-2 and block the Bcl-2 anti-apoptotic function. A method of use of compound of the general structural Formula (I) for use in treatment of cancer: wherein X and Y, and R and R1', and R2, R3, R4 and R5 and A and A1, have any of the values defined in the specification.
摘要翻译：使用结合Bcl-2的口袋并阻断Bcl-2抗凋亡功能的三羟甲基 - 二苯并二氮杂环己烷二氧化物促进肿瘤细胞中细胞死亡的方法。一般结构式（I）的化合物用于治疗癌症的方法：其中X和Y，以及R和R 1'以及R 2，R 3，R 4和R 5以及A和A 1具有任何值在规范中定义。

6. 发明申请

WO2005069771A2 SMALL MOLECULE ANTAGONISTS OF BCL-2 FAMILY PROTEINS 审中-公开
标题翻译： BCL-2家族蛋白的小分子拮抗剂
公开(公告)号：WO2005069771A2
公开(公告)日：2005-08-04
申请号：PCT/US2004/040553
申请日：2004-12-06
申请人： THE REGENTS OF THE UNIVERSITY OF MICHIGAN , GEORGETOWN UNIVERSITY MEDICAL CENTER , WANG, Shaomeng , YANG, Dajun
发明人： WANG, Shaomeng , YANG, Dajun
IPC分类号： C12Q1/02 , A61K31/11 , A61K31/12 , A61K31/122 , A61K31/135 , A61K31/19 , A61K31/225 , A61K31/335 , A61K45/00 , A61K45/06 , A61P9/00 , A61P31/04 , A61P31/10 , A61P31/12 , A61P31/18 , A61P35/00 , A61P35/02 , A61P43/00
CPC分类号： A61K31/11 , A61K45/06 , A61K2300/00
摘要： The present invention relates to naturally occurring and chemically synthesized small molecule antagonists of Bcl-2 family proteins. In particular, the present invention provides gossypol compounds ( e.g ., isomers, enantiomers, racemic compounds, metabolites, derivatives, pharmaceutically acceptable salts, in combination with acids or bases, and the like) and methods of using these compounds as antagonists of the nati-apoptotic effects of Bcl-2 family member proteins ( e.g ., Bcl-2 Bcl-X L , and the like). The present invention also provides compositions comprising gossypol compounds and optionally one or more additional therapeutic agents ( e.g ., anticancer/chemotherapeutic agents). The present invention also provides methods for treating diseases and pathologies ( e.g ., neoplastic diseases) comprising administering a composition comprising gossypol compounds and optionally one or more additional therapeutic agents ( e.g ., anticancer/chemotheratpeutic agents) and/or techniques ( e.g ., radiation therapies, surgical interventions, and the like) to a subject or in vitro cells, tissues, and organs.
摘要翻译：本发明涉及Bcl-2家族蛋白质的天然存在和化学合成的小分子拮抗剂。特别地，本发明提供了棉酚化合物（例如异构体，对映异构体，外消旋化合物，代谢物，衍生物，药学上可接受的盐，与酸或碱的组合等）和使用这些化合物作为天然药物的拮抗剂的方法， Bcl-2家族蛋白（例如Bcl-2 Bcl-XL等）的凋亡作用。本发明还提供包含棉酚化合物和任选的一种或多种另外的治疗剂（例如抗癌/化学治疗剂）的组合物。本发明还提供了治疗疾病和病症（例如，肿瘤性疾病）的方法，包括施用包含棉酚化合物和任选的一种或多种另外的治疗剂（例如抗癌/化学治疗剂）和/或技术（例如，放射疗法，外科手术等）到受试者或体外细胞，组织和器官。

7. 发明申请

WO0241828A3 HOUTTUYNINUM COMPOSITIONS AND METHODS FOR INHIBITING THE ACTIVITY OF ERBB-2 BASED THEREON 审中-公开
标题翻译：抑制ERBB-2活性的鱼腥草组合物和方法
公开(公告)号：WO0241828A3
公开(公告)日：2002-08-01
申请号：PCT/US0143123
申请日：2001-11-19
申请人： YANG DAJUN , ZHU XIAO F , WANG JINGSON , ZENG YIXING
发明人： YANG DAJUN , ZHU XIAO F , WANG JINGSON , ZENG YIXING
IPC分类号： A61K20060101 , A61K31/10 , A61K31/12 , A61K36/185 , A61K35/78
CPC分类号： A61K36/185
摘要： The present invention relates to methods and compositions for inhibiting the activity of erbB-2. The described methods and compositions are particularly useful for inhibiting cellular proliferative disorders, such as cancer, characterized by over-activity and/or inappropriate activity of erbB-2. More particularly, method for the treatment of a cellular proliferative disorder characterized by over-activity or inappropriate activity of erbB-2 is provided including the step of administering to a patient in need of such treatment a therapeutically effective amount of soluble extract of houttuynum, or a compound selected from the group consisting of houttuyninum, Houttuymia cordata, neo-houttuyninum (decanoyl acetaldehyde), analogs thereof, pharmaceutically acceptable salts thereof, and/or prodrugs thereof.
摘要翻译：本发明涉及用于抑制erbB-2活性的方法和组合物。所描述的方法和组合物特别用于抑制以erbB-2的过度活性和/或不适当的活性为特征的细胞增殖性病症，例如癌症。更具体地说，提供了治疗以erbB-2的过度活性或不适当活性为特征的细胞增殖性病症的方法，包括给需要这种治疗的患者施用治疗有效量的鱼腥草的可溶性提取物或选自鱼腥草，鱼腥草，鱼腥草（壬酰基茴香醛），其类似物，其药学上可接受的盐，和/或其前药的化合物。

8. 发明申请

WO2002013833A3 SMALL MOLECULE INHIBITORS TARGETED AT Bcl-2 审中-公开
公开(公告)号：WO2002013833A3
公开(公告)日：2002-02-21
申请号：PCT/US2001/025575
申请日：2001-08-16
申请人： GEORGETOWN UNIVERSITY MEDICAL CENTER , WANG, Shaomeng , YANG, Dajun , ENYEDY, Istvan, J.
发明人： WANG, Shaomeng , YANG, Dajun , ENYEDY, Istvan, J.
IPC分类号： A61K31/655
摘要： A method for promotion of cell death in tumor cells using tricylo-dibenzo-diazocine-dioxides that bind to a pocket of Bcl-2 and block the Bcl-2 anti-apoptotic function. A method of use of compound of the general structural Formula (I) for use in treatment of cancer: wherein X and Y, and R and R¿1?, and R¿2?, R¿3?, R¿4? and R¿5? and A and A¿1?, have any of the values defined in the specification.

9. 发明申请

WO2008150506A1 PULSATILE DOSING OF GOSSYPOL FOR TREATMENT OF DISEASE 审中-公开
标题翻译：用于治疗疾病的药物治疗药物
公开(公告)号：WO2008150506A1
公开(公告)日：2008-12-11
申请号：PCT/US2008/006936
申请日：2008-06-02
申请人： ASCENTA THERAPEUTICS, INC. , HOLMLUND, Jon, T. , SORENSEN, Mel , LEOPOLD, Lance , YANG, Dajun
发明人： HOLMLUND, Jon, T. , SORENSEN, Mel , LEOPOLD, Lance , YANG, Dajun
IPC分类号： A01N43/16
CPC分类号： A61K31/11 , A61K31/337 , A61K45/06 , Y02A50/411 , A61K2300/00
摘要： This invention relates to pulsatile dose administration of gossypol or pharmaceutical compositions thereof for treating diseases, disorders and conditions responsive to gossypol, inhibiting the activity of anti-apoptotic Bcl-2 family proteins, inducing apoptosis in cells and increasing the sensitivity of cells to inducers of apoptosis.
摘要翻译：本发明涉及棉酚的脉动剂量给药或其药物组合物，其用于治疗对棉酚有反应的疾病，病症和病症，抑制抗凋亡Bcl-2家族蛋白的活性，诱导细胞凋亡，并增加细胞对诱导剂的敏感性细胞凋亡。

10. 发明申请

WO2002097053A3 SMALL MOLECULE ANTAGONISTS OF BCL2 FAMILY PROTEINS 审中-公开
公开(公告)号：WO2002097053A3
公开(公告)日：2002-12-05
申请号：PCT/US2002/017206
申请日：2002-05-30
申请人： THE REGENTS OF THE UNIVERSITY OF MICHIGAN , GEORGETOWN UNIVERSITY MEDICAL CENTER , WANG, Shaomeng , YANG, Dajun
发明人： WANG, Shaomeng , YANG, Dajun
IPC分类号： A61K31/11
摘要： The present invention relates to naturally occurring and chemically synthesized small molecules antagonists of Bcl-2 family proteins. In particular, the present invention provides gossypol derivatives and methods of using gossypol derivatives as antagonists of the anti-apoptotic effects of Bcl-2 and Bcl-X L proteins especially in cancer cells that overexpress Bcl-2 family proteins (e.g., Bcl-2 and/or Bcl-X L ).

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