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1. 发明申请

WO0209684A8 ERBB-2 SELECTIVE SMALL MOLECULE KINASE INHIBITORS 审中-公开
标题翻译： ERBB-2选择性小分子激酶抑制剂
公开(公告)号：WO0209684A8
公开(公告)日：2002-07-04
申请号：PCT/US0123869
申请日：2001-07-30
申请人： UNIV GEORGETOWN , SHAOMENG WANG , DAJUN YANG , ISTVAN ENYEDY
发明人： SHAOMENG WANG , DAJUN YANG , ISTVAN ENYEDY
IPC分类号： A61K31/00 , A61K31/192 , A61K31/216 , A61K39/395 , A61K41/00 , A61P35/00
CPC分类号： A61K31/216 , A61K31/00 , A61K31/192
摘要： A novel method for erbB-2 kinase inhibition by compounds identifies through computational modeling and data processing and/or rational and de novo drug design is provided the compounds bind erbB-2 kinase molecules and which can be used as erbB-2 kinase agonists or antagonists. These compounds are useful especially in the treatment of cancer, particularly breast cancer, and can be used alone or in combination with other chemotherapeutic agents, particularly with hercetin, a humanized anti-HER-2 antibody, or with radiation therapy. A specific compound which is examplified is "compound B17" =methyl-(posa-notrophenyl)-2-propynoate.
摘要翻译：化合物抑制erbB-2激酶的新方法通过计算模型和数据处理来识别，和/或合理的从头药物设计提供了化合物结合erbB-2激酶分子并且可以用作erbB-2激酶激动剂或拮抗剂。这些化合物特别用于治疗癌症，特别是乳腺癌，并且可以单独使用或与其他化学治疗剂组合使用，特别是与Hercetin，人源化抗HER-2抗体或放射疗法组合使用。示例的具体化合物是“化合物B17”=甲基 - （正 - 苯基）-2-丙炔酸酯。

2. 发明申请

WO0209684A3 ERBB-2 selective small molecule kinase inhibitors 审中-公开
标题翻译： ERBB-2选择性小分子激酶抑制剂
公开(公告)号：WO0209684A3
公开(公告)日：2002-04-25
申请号：PCT/US0123869
申请日：2001-07-30
申请人： UNIV GEORGETOWN , SHAOMENG WANG , DAJUN YANG , ISTVAN ENYEDY
发明人： SHAOMENG WANG , DAJUN YANG , ISTVAN ENYEDY
IPC分类号： A61K31/00 , A61K31/192 , A61K31/216 , A61K39/395 , A61K41/00 , A61P35/00
CPC分类号： A61K31/216 , A61K31/00 , A61K31/192
摘要： A novel method for erbB-2 kinase inhibition by compounds identifies through computational modeling and data processing and/or rational and de novo drug design is provided the compounds bind erbB-2 kinase molecules and which can be used as erbB-2 kinase agonists or antagonists. These compounds are useful especially in the treatment of cancer, particularly breast cancer, and can be used alone or in combination with other chemotherapeutic agents, particularly with hercetin, a humanized anti-HER-2 antibody, or with radiation therapy. A specific compound which is examplified is 'compound B17' =methyl-(posa-notrophenyl)-2-propynoate.
摘要翻译：化合物的erbB-2激酶抑制的新方法通过计算建模和数据处理鉴定，和/或合理和从头药物设计提供了化合物结合erbB-2激酶分子，并且其可以用作erbB-2激酶激动剂或拮抗剂。这些化合物特别用于治疗癌症，特别是乳腺癌，并且可以单独使用或与其它化学治疗剂，特别是与黑塞生，人源化抗HER-2抗体或放射治疗组合使用。例示的具体化合物是“化合物B17”=甲基 - （对硝基苯基）-2-丙炔酸酯。

3. 发明申请

US20080248566A1 MATRIPTASE, A SERINE PROTEASE AND ITS APPLICATIONS 有权
标题翻译： MATRIPTASE，丝氨酸蛋白酶及其应用
公开(公告)号：US20080248566A1
公开(公告)日：2008-10-09
申请号：US12040467
申请日：2008-02-29
申请人： Robert B. Dickson , Chen-Yong Lin , Michael Johnson , Shaomeng Wang , Istvan Enyedy
发明人： Robert B. Dickson , Chen-Yong Lin , Michael Johnson , Shaomeng Wang , Istvan Enyedy
IPC分类号： C12N5/06 , C12N15/11 , C12N15/00
CPC分类号： A61K49/0039 , A61K38/00 , A61K49/0056 , A61K49/0058 , A61K51/10 , C12Q1/37 , G01N33/573 , G01N2333/96433 , G01N2500/20
摘要： The invention is directed to a method of detecting a malignancy or a pre-malignant lesion in breast or other tissue, or a pathologic condition, by detecting the presence of single-chain or two-chain forms of matriptase in the tissue. The invention is further directed to a method of treating malignancies, which have the phenotype of matriptase production by administering a tumor formation inhibiting effective amount of concentrate of Bowman-Birk inhibitor (BBIC), or other matriptase inhibitor. The invention also is directed to nucleic acids encoding a matriptase protein or fragments thereof, and their use for structure elucidation and modeling to identify other inhibitors of matriptase, as well as to methods of identifying matriptase modulating agents, including activators and inhibitors.
摘要翻译：本发明涉及通过检测组织中单链或双链形式的matriptase的存在来检测乳腺或其他组织或病理状况中的恶性肿瘤或恶性前病变的方法。本发明进一步涉及通过施用抑制有效量的Bowman-Birk抑制剂（BBIC）浓缩物或其它片剂酶抑制剂的肿瘤形成来治疗恶性肿瘤的方法，所述恶性肿瘤具有基质酶产生的表型。本发明还涉及编码matriptase蛋白质或其片段的核酸，以及其用于结构阐明和建模以鉴定其它抑制剂的用途，以及鉴定片段酶调节剂（包括活化剂和抑制剂）的方法。

4. 发明申请

US20080058322A1 Small molecule inhibitors targeted at Bcl-2 审中-公开
公开(公告)号：US20080058322A1
公开(公告)日：2008-03-06
申请号：US11811019
申请日：2007-06-08
申请人： Shaomeng Wang , Dajun Yang , Istvan Enyedy
发明人： Shaomeng Wang , Dajun Yang , Istvan Enyedy
IPC分类号： A61K31/12 , A61K31/33 , A61K31/40 , A61K31/44 , A61K31/535 , A61P43/00
CPC分类号： A61K45/06 , A61K31/00 , A61K31/122 , A61K31/395 , A61K31/404 , A61K31/4184 , A61K31/444 , A61K31/452 , A61K31/473 , A61K31/4745 , A61K31/519 , A61K31/655 , A61K2300/00
摘要： The present invention relates to small molecule antagonists of Bcl-2 family proteins such as Bcl-2 and/or Bcl-XL. In particular, the present invention provides non-peptide cell permeable small molecules (e.g., tricyclo-dibenzo-diazocine-dioxides) that bind to a pocket in Bcl-2/Bcl-XL that block the anti-apoptotic function of these proteins in cancer cells and tumor tissues exhibiting Bcl-2 protein overexpression. In preferred embodiments, the small molecules of the present invention are active at the BH3 binding pocket of Bcl-2 family proteins (e.g., Bcl-2, Bcl-XL, and Mcl-1). The compositions and methods of the present invention are useful therapeutics for cancerous diseases either alone or in combination with chemotherapeutic or other drugs.

5. 发明授权

US06677377B2 Structure based discovery of inhibitors of matriptase for the treatment of cancer and other conditions 失效
标题翻译：基于结构发现的matriptase抑制剂用于治疗癌症和其他病症
公开(公告)号：US06677377B2
公开(公告)日：2004-01-13
申请号：US09885295
申请日：2001-06-21
申请人： Chen-Yong Lin , Robert B. Dickson , Shaomeng Wang , Istvan Enyedy , Sheau-Ling Lee
发明人： Chen-Yong Lin , Robert B. Dickson , Shaomeng Wang , Istvan Enyedy , Sheau-Ling Lee
IPC分类号： A61K31155
CPC分类号： A61K31/655 , A61K31/155 , A61K31/341 , A61K31/404 , A61K31/505 , A61K49/0002 , G01N33/574 , G01N2333/96486
摘要： The present invention relates to a method of inhibiting carcinoma progression wherein matriptase plays a role in a subject in need of such inhibition including administering to a subject an effective amount of a compound comprising two positively charged groups, which are the same or different. The groups are linked by a chemical group having a length of between 5 and 30 A, and preferably between 15 and 24 A. Diagnostic methods based on matriptase action and therapeutic methods involving inhibition of matriptase activity are provided.
摘要翻译：本发明涉及一种抑制癌症进展的方法，其中底物酶在需要这种抑制的受试者中起作用，包括向受试者施用有效量的包含相同或不同的两个带正电基团的化合物。这些基团通过长度为5至30A，优选15至24A的化学基团连接。提供了基于片段酶作用的诊断方法和涉及抑制matriptase活性的治疗方法。

6. 发明授权

US07960163B2 Matriptase, a serine protease and its applications 有权
标题翻译： Matriptase，丝氨酸蛋白酶及其应用
公开(公告)号：US07960163B2
公开(公告)日：2011-06-14
申请号：US12040467
申请日：2008-02-29
申请人： Robert B. Dickson , Chen-Yong Lin , Michael Johnson , Shaomeng Wang , Istvan Enyedy
发明人： Robert B. Dickson , Chen-Yong Lin , Michael Johnson , Shaomeng Wang , Istvan Enyedy
IPC分类号： C12N9/00 , C12N9/50 , C12N1/20 , C12N15/00 , C07H21/04
CPC分类号： A61K49/0039 , A61K38/00 , A61K49/0056 , A61K49/0058 , A61K51/10 , C12Q1/37 , G01N33/573 , G01N2333/96433 , G01N2500/20
摘要： The invention is directed to a method of detecting a malignancy or a pre-malignant lesion in breast or other tissue, or a pathologic condition, by detecting the presence of single-chain or two-chain forms of matriptase in the tissue. The invention is further directed to a method of treating malignancies, which have the phenotype of matriptase production by administering a tumor formation inhibiting effective amount of concentrate of Bowman-Birk inhibitor (BBIC), or other matriptase inhibitor. The invention also is directed to nucleic acids encoding a matriptase protein or fragments thereof, and their use for structure elucidation and modeling to identify other inhibitors of matriptase, as well as to methods of identifying matriptase modulating agents, including activators and inhibitors.
摘要翻译：本发明涉及通过检测组织中单链或双链形式的matriptase的存在来检测乳腺或其他组织或病理状况中的恶性肿瘤或恶性前病变的方法。本发明进一步涉及通过施用抑制有效量的Bowman-Birk抑制剂（BBIC）浓缩物或其它片剂酶抑制剂的肿瘤形成来治疗恶性肿瘤的方法，所述恶性肿瘤具有基质酶产生的表型。本发明还涉及编码matriptase蛋白质或其片段的核酸，以及其用于结构阐明和建模以鉴定其它抑制剂的用途，以及鉴定片段酶调节剂（包括活化剂和抑制剂）的方法。

7. 发明授权

US07355015B1 Matriptase, a serine protease and its applications 有权
标题翻译： Matriptase，丝氨酸蛋白酶及其应用
公开(公告)号：US07355015B1
公开(公告)日：2008-04-08
申请号：US09936333
申请日：2000-03-10
申请人： Robert B. Dickson , Chen-Yong Lin , Michael Johnson , Shaomeng Wang , Istvan Enyedy
发明人： Robert B. Dickson , Chen-Yong Lin , Michael Johnson , Shaomeng Wang , Istvan Enyedy
IPC分类号： C07K16/00 , C07K16/40 , A61K38/43
CPC分类号： A61K49/0039 , A61K38/00 , A61K49/0056 , A61K49/0058 , A61K51/10 , C12Q1/37 , G01N33/573 , G01N2333/96433 , G01N2500/20
摘要： The invention is directed to a method of detecting a malignancy or a pre-malignant lesion in breast or other tissue, or a pathologic condition, by detecting the presence of single-chain or two-chain forms of matriptase in the tissue. The invention is further directed to a method of treating malignancies, which have the phenotype of matriptase production by administering a tumor formation inhibiting effective amount of concentrate of Bowman-Birk inhibitor (BBIC), or other matriptase inhibitor. The invention also is directed to nucleic acids encoding a matriptase protein or fragments thereof, and their use for structure elucidation and modeling to identify other inhibitors of matriptase, as well as to methods of identifying matriptase modulating agents, including activators and inhibitors.
摘要翻译：本发明涉及通过检测组织中单链或双链形式的matriptase的存在来检测乳腺或其他组织或病理状况中的恶性肿瘤或恶性前病变的方法。本发明进一步涉及通过施用抑制有效量的Bowman-Birk抑制剂（BBIC）浓缩物或其它片剂酶抑制剂的肿瘤形成来治疗恶性肿瘤的方法，所述恶性肿瘤具有基质酶产生的表型。本发明还涉及编码matriptase蛋白质或其片段的核酸，以及其用于结构阐明和建模以鉴定其它抑制剂的用途，以及鉴定片段酶调节剂（包括活化剂和抑制剂）的方法。

8. 发明授权

US07427689B2 ErbB-2 selective small molecule kinase inhibitors 失效
标题翻译： ErbB-2选择性小分子激酶抑制剂
公开(公告)号：US07427689B2
公开(公告)日：2008-09-23
申请号：US10343267
申请日：2001-07-30
申请人： Shaomeng Wang , Dajun Yang , Istvan Enyedy
发明人： Shaomeng Wang , Dajun Yang , Istvan Enyedy
IPC分类号： C07C205/00
CPC分类号： A61K31/216 , A61K31/00 , A61K31/192
摘要： A novel method for erbB-2 kinase inhibition by compounds identifies through computational modeling and data processing and/or rational and de novo drug design is provided the compounds bind erbB-2 kinase molecules and which can be used as erbB-2 kinase agonists or antagonists. These compounds are useful especially in the treatment of cancer, particularly breast cancer, and can be used alone or in combination with other chemotherapeutic agents, particularly with hercetin, a humanized anti-HER-2 antibody, or with radiation therapy. A specific compound which is exemplified is “compound B17”=methyl-(p-nitrophenyl)-2-propynoate.
摘要翻译：化合物的erbB-2激酶抑制的新方法通过计算建模和数据处理鉴定，和/或合理和从头药物设计提供了化合物结合erbB-2激酶分子，并且其可以用作erbB-2激酶激动剂或拮抗剂。这些化合物特别用于治疗癌症，特别是乳腺癌，并且可以单独使用或与其它化学治疗剂，特别是与赫氏原，人源化抗HER-2抗体或放射治疗组合使用。例示的具体化合物是“化合物B17”=甲基 - （对硝基苯基）-2-丙炔酸酯。

9. 发明申请

US20080293696A1 2-Aminoarylcarboxamides Useful as Cancer Chemotherapeutic Agents 审中-公开
标题翻译：用作癌症化学治疗剂的2-氨基芳基羧酰胺
公开(公告)号：US20080293696A1
公开(公告)日：2008-11-27
申请号：US11630850
申请日：2005-06-23
申请人： Catherine Brennan , Julie A. Dixon , William J. Scott , Aniko Redman , Benjamin D. Jones , Barton Phillips , Philip Wickens , Istvan Enyedy , Ellalahewage Kumarasinghe , Charles Kreiman , Jacques Dumas , Uday Khire , Chih-Yuan Chuang , Harold C.E. Kluender , Zhenqiu Hong , Lei Wang , Donald Bierer
发明人： Catherine Brennan , Julie A. Dixon , William J. Scott , Aniko Redman , Benjamin D. Jones , Barton Phillips , Philip Wickens , Istvan Enyedy , Ellalahewage Kumarasinghe , Charles Kreiman , Jacques Dumas , Uday Khire , Chih-Yuan Chuang , Harold C.E. Kluender , Zhenqiu Hong , Lei Wang , Donald Bierer
IPC分类号： A61K31/55 , C07D405/12 , A61K31/4433 , A61K31/444 , A61P35/00 , C07D405/14 , A61K31/506
CPC分类号： C07D319/08
摘要： A compound having the formula (1) in which the ring containing E is a phenyl, a pyridine, or a pyrimidine. In formula (1) the symbol A represents wherein the group R4 represents halogen, CF3, or H, provided that the maximum number of CF3 groups on any A is 2, and the maximum number of hydrogens on A is 2 for the A groups which together with the carbon atoms to which they are attached form 6-membered rings, and the maximum number of hydrogens on A is 1 for the A group which together with the carbon atoms to which it is attached forms a 5-membered ring. Z represents N or CH when E forms a phenyl ring, and represents CH when E forms a pyridine or pyrimidine. The groups R1, R2 and R3 and the subscripts a, b, and d are as defined in the text and claims. Pharmaceutical compositions containing a compound of formula (1) and methods of treating cancer using compounds of formula (1) are also disclosed and claimed.
摘要翻译：具有式（1）的化合物，其中含有E的环是苯基，吡啶或嘧啶。在式（1）中，符号A表示其中基团R 4表示卤素，CF 3或H，条件是任何A上的CF 3基团的最大数目为2，并且A组中的最大氢数为2，与它们连接的碳原子一起形成6元环，并且对于与连接的碳原子一起形成5元环的A基团，A上的最大氢数为1。当E形成苯环时，Z表示N或CH，当E形成吡啶或嘧啶时，Z表示CH。基团R1，R2和R3以及下标a，b和d如本文和权利要求中所定义。还公开并要求保护含有式（1）化合物的药物组合物和使用式（1）化合物治疗癌症的方法。

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