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公开(公告)号：US20220267376A1
公开(公告)日：2022-08-25
申请号：US17618751
申请日：2020-06-16
申请人： Tomi K. SAWYER , Pietro ARONICA , Christopher J. BROWN , Fernando J. FERRER , Charles W. JOHANNES , Srinivasaraghavan KANNAN , David P. LANE , Anthony W. PARTRIDGE , Yaw Sing TAN , Chandra S. VERMA , Tsz Ying YUEN , Merck Sharp & Dohme Corp. , Agency for Science, Technology and Research , MSD International GMBH (Singapore Branch)
发明人： Pietro Aronica , Christopher J. Brown , Fernando J. Ferrer , Charles W. Johannes , Srinivasaraghavan Kannan , David P. Lane , Anthony W. Partridge , Tomi K. Sawyer , Yaw Sing Tan , Chandra S. Verma , Tsz Ying Yuen
摘要： Peptidomimetic macrocycles that comprise all-D configuration ?-amino acids and bind mouse double minute 2 (MDM2 aka E3 ubiquitin-protein ligase) and MDMX (aka MDM4) are described. These all-D configuration α-amino acid peptidomimetic macrocycles are protease resistant, cell permeable without inducing membrane disruption, and intracellularly activate p53 by binding MDM2 and MDMX thereby antagonizing MDM2 and MDMX binding to p53. These peptidomimetic macrocycles may be useful in anticancer therapies, particularly in combination with chemotherapy or radiation therapy.
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公开(公告)号：US20230083431A1
公开(公告)日：2023-03-16
申请号：US17783224
申请日：2020-12-15
申请人： Nicolas C. BOYER , Michael B. GARRIGOU , Sookhee Nicole HA , Chunhui HUANG , Anthony W. PARTRIDGE , Tomi K. SAWYER , Pietro ARONICA , Charles W. JOHANNES , Srinivasaraghavan KANNAN , Chandra S. VERMA , Tsz Ying YUEN , Merck Sharp & Dohme LLC , MSD International GMBH (Singapore Branch) , Agency for Science, Technology and Research
发明人： Nicolas C. Boyer , Michael B. Garrigou , Sookhee Nicole Ha , Chunhui Huang , Anthony W. Partridge , Tomi K. Sawyer , Pietro Aronica , Charles W. Johannes , Srinivasaraghavan Kannan , Chandra S. Verma , Tsz Ying Yuen
摘要： The invention provides compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein the variables are as described herein. The compounds or their pharmaceutically acceptable salts can inhibit the G12D mutant of Kirsten rat sarcoma (K-Ras) protein and are expected to have utility as therapeutic agents, for example, for treating cancer. The invention also provides pharmaceutical compositions which comprise compounds of Formula (I) or pharmaceutically acceptable salts thereof. The invention also relates to methods for use of the compounds or their pharmaceutically acceptable salts in the therapy and prophylaxis of cancer and for preparing pharmaceuticals for this purpose.
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公开(公告)号：US20120149648A1
公开(公告)日：2012-06-14
申请号：US13352223
申请日：2012-01-17
申请人： Huw M. Nash , David Allen Annis , Rosana Kapeller-Libermann , Tomi K. Sawyer , Noriyuki Kawahata , Jiawen Han
发明人： Huw M. Nash , David Allen Annis , Rosana Kapeller-Libermann , Tomi K. Sawyer , Noriyuki Kawahata , Jiawen Han
CPC分类号： C07K7/64 , A61K38/12 , A61K38/1761 , A61K45/06
摘要： The present invention provides biologically active peptidomimetic macrocycles for the treatment of cell proliferative disorders such as cancer and immunoproliferative disease.
摘要翻译： 本发明提供用于治疗细胞增殖性疾病如癌症和免疫增殖性疾病的生物活性的拟肽大环化合物。
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公开(公告)号：US20120115793A1
公开(公告)日：2012-05-10
申请号：US13120386
申请日：2009-09-22
CPC分类号： C07K14/47
摘要： The present invention provides novel peptidomimetic macrocycles and methods of using such macrocycles for the treatment of disease.
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公开(公告)号：US20100216688A1
公开(公告)日：2010-08-26
申请号：US12564910
申请日：2009-09-22
CPC分类号： G01N33/5008 , C07K14/00 , C07K14/4705 , C07K14/4747 , C07K14/4748 , G01N2500/10
摘要： The present invention provides biologically active crosslinked polypeptides with improved properties relative to their corresponding precursor polypeptides, having good cell penetration properties and reduced binding to human proteins. The invention additionally provides methods of identifying and making such improved polypeptides.
摘要翻译： 本发明提供了相对于其相应的前体多肽具有改进性质的生物活性交联多肽，其具有良好的细胞穿透性质和降低的与人蛋白质的结合。 本发明另外提供鉴定和制备这种改良多肽的方法。
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公开(公告)号：US06576766B1
公开(公告)日：2003-06-10
申请号：US09554230
申请日：2000-08-17
申请人： Manfred Weigele , Regine Bohacek , Virginia A. Jacobsen , Karina Macek , Michael G. Yang , Noriyuki H. Kawahata , Rajeswari Sundaramoorthi , Yihan Wang , Craig S. Takeuchi , George P. Luke , Chester A. Metcalf, III , William C. Shakespeare , Tomi K. Sawyer
发明人： Manfred Weigele , Regine Bohacek , Virginia A. Jacobsen , Karina Macek , Michael G. Yang , Noriyuki H. Kawahata , Rajeswari Sundaramoorthi , Yihan Wang , Craig S. Takeuchi , George P. Luke , Chester A. Metcalf, III , William C. Shakespeare , Tomi K. Sawyer
IPC分类号： C07D30789
CPC分类号： C07D307/92 , A61K38/00 , C07C237/22 , C07C2601/14 , C07F9/12 , C07F9/3834 , C07F9/3869 , C07F9/3873 , C07F9/3882 , C07F9/65527 , C07K5/06191
摘要： This invention concerns compounds for inhibiting intracellular signal transduction, especially intracellular signal transduction mediate by one or more molecular interactions involving a phosphotyrosine-containing protein. This invention also relates to pharmaceutic compositions containing the compounds and prophylactic and therapeutic methods involving pharmaceutical and veterinary administration of the compounds. The compounds are of formula (1) as defined herein.
摘要翻译： 本发明涉及用于抑制细胞内信号转导的化合物，特别是通过涉及含磷酸酪氨酸的蛋白质的一种或多种分子相互作用介导的细胞内信号转导。 本发明还涉及包含化合物的药物组合物和涉及化合物的药物和兽药施用的预防和治疗方法。 化合物是如本文所定义的式（1）。
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7.发明授权Bicyclic signal transduction inhibitors, compositions containing them & uses thereof 有权双环信号转导抑制剂，含有它们的组合物及其用途公开(公告)号：US06482852B2
公开(公告)日：2002-11-19
申请号：US09854027
申请日：2001-05-11
申请人： William C. Shakespeare , Michael G. Yang , Rajeswari Sundaramoorthi , Regine Bohacek , Charles Joseph Eyermann , Tomi K. Sawyer
发明人： William C. Shakespeare , Michael G. Yang , Rajeswari Sundaramoorthi , Regine Bohacek , Charles Joseph Eyermann , Tomi K. Sawyer
IPC分类号： A61K3121
CPC分类号： C07F9/65527 , C07C237/48 , C07C2601/14 , C07C2602/12 , C07D313/08 , C07F9/12 , C07F9/3834 , C07F9/3873 , C07F9/3882 , C07F9/4021
摘要： This invention concerns compounds for inhibiting intracellular signal transduction, especially intracellular signal transduction mediated by one or more molecular interactions involving a phosphotyrosine-containing protein. This invention also relates to pharmaceutical compositions containing the compounds and prophylactic and therapeutic methods involving pharmaceutical and veterinary administration of the compounds. The compounds are of the formula as defined herein.
摘要翻译： 本发明涉及用于抑制细胞内信号转导的化合物，特别是通过涉及含磷酸酪氨酸的蛋白质的一种或多种分子相互作用介导的细胞内信号转导。 本发明还涉及包含化合物的药物组合物和涉及化合物的药物和兽药施用的预防和治疗方法。 这些化合物是本文定义的式。
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公开(公告)号：US06420384B2
公开(公告)日：2002-07-16
申请号：US09740619
申请日：2000-12-18
IPC分类号： C07D40101
CPC分类号： C07D471/04 , A61K47/54 , A61K47/548 , C07D487/04 , C07F9/4012 , C07F9/405 , C07F9/58 , C07F9/65583 , C07F9/6561 , C07F9/65616
摘要： Compounds and methods of treating or preventing bone disorders including osteoporosis, rheumatoid arthritis, and metastatic bone disease are provided. The inventive compounds comprise a bone targeting moiety and a payload. The payload portion of these inventive compounds inhibit the proton pump of osteoclasts, thereby, reducing bone resorption. Compounds of the present invention include compounds of the following formula:
摘要翻译： 提供了治疗或预防包括骨质疏松症，类风湿性关节炎和转移性骨病在内的骨疾病的化合物和方法。 本发明化合物包括骨靶向部分和有效载荷。 这些本发明化合物的有效载荷部分抑制破骨细胞的质子泵，从而减少骨吸收。 本发明的化合物包括下式的化合物：
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公开(公告)号：US20230285514A1
公开(公告)日：2023-09-14
申请号：US17785279
申请日：2020-12-18
申请人： Elisabetta BIANCHI , Paul E. CARRINGTON , Qiaolin DENG , Songnian LIN , Federica ORVIETO , Anandan PALANI , Antonello PESSI , Tomi K. SAWYER , Merck Sharp & Dohme LLC
发明人： Elisabetta Bianchi , Paul E. Carrington , Qiaolin Deng , Songnian Lin , Federica Orvieto , Anandan Palani , Antonello Pessi , Tomi K. Sawyer
IPC分类号： A61K38/26 , A61K38/28 , C07K14/605
CPC分类号： A61K38/26 , A61K38/28 , C07K14/605
摘要： The stapled peptides of the present invention, and pharmaceutically acceptable salts thereof, are co-agonists of the glucagon and GLP-1 receptors, and may be useful in the treatment, prevention and suppression of diseases mediated by the glucagon receptor and the GLP-1 receptor, including but not limited to, metabolic disorders such as diabetes, non-alcoholic fatty liver disease (NAFLD), non-alcoholic steatohepatitis (NASH), and obesity.
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公开(公告)号：US08808694B2
公开(公告)日：2014-08-19
申请号：US13352223
申请日：2012-01-17
申请人： Huw M. Nash , David Allen Annis , Rosana Kapeller-Libermann , Tomi K. Sawyer , Noriyuki Kawahata , Jiawen Han
发明人： Huw M. Nash , David Allen Annis , Rosana Kapeller-Libermann , Tomi K. Sawyer , Noriyuki Kawahata , Jiawen Han
IPC分类号： A61K39/395 , C12N15/00 , A61K38/12 , A61K38/17
CPC分类号： C07K7/64 , A61K38/12 , A61K38/1761 , A61K45/06
摘要： The present invention provides biologically active peptidomimetic macrocycles for the treatment of cell proliferative disorders such as cancer and immunoproliferative disease.
摘要翻译： 本发明提供用于治疗细胞增殖性疾病如癌症和免疫增殖性疾病的生物活性的拟肽大环化合物。
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