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1. 发明申请

US20160331751A1 PHARMACEUTICAL COMPOSITIONS 审中-公开
标题翻译：药物组合物
公开(公告)号：US20160331751A1
公开(公告)日：2016-11-17
申请号：US15106886
申请日：2014-12-19
申请人： Stephane Ferretti , Sebastien Jeay , Ensar Halilovic , Fang Li , Hui-Qin Wang
发明人： Stephane Ferretti , Sebastien Jeay , Ensar Halilovic , Fang Li , Hui-Qin Wang
IPC分类号： A61K31/519 , A61K31/506 , A61K31/496
CPC分类号： A61K31/519 , A61K31/4188 , A61K31/496 , A61K31/505 , A61K31/506 , A61K2300/00
摘要： The disclosure relates to a pharmaceutical combination of a mdm2/4 inhibitor, namely (S)-1-(4-Chloro-phenyl)-7-isopropoxy-6-methoxy-2-(4-{methyl-[4-(4-methyl-3-oxo-piperazin-1-yl)-trans-cyclohexylmethyl]-amino}-phenyl)-1,4-dihydro-2H-isoquinolin-3-one or (S)-5-(5-Chloro-1-methyl-2-oxo-1,2-dihydro-pyridin-3-yl)-6-(4-chloro-phenyl)-2-(2,4-dimethoxy-pyrimidin-5-yl)-1-isopropyl-5,6-dihydro-1H-pyrrolo[3,4-d]imidazol-4-one, and a cyclin dependent kinase 4/6 (CDK4/6) inhibitor 7-Cyclopentyl-2-(5-piperazin-1-yl-pyridin-2-ylamino)-7H-pyrrolo[2,3-d]pyrimidine-6-carboxylic acid dimethylamide. In addition, the disclosure relates to a pharmaceutical combination product. The disclosure also relates to corresponding pharmaceutical formulations, uses and treatment methods comprising said mdm2/4 inhibitor or a cyclin dependent kinase 4/6 (CDK4/6) inhibitor.
摘要翻译：本公开涉及mdm2 / 4抑制剂的药物组合，即（S）-1-（4-氯 - 苯基）-7-异丙氧基-6-甲氧基-2-（4- {甲基 - [4-（4 - 甲基-3-氧代 - 哌嗪-1-基） - 反式 - 环己基甲基] - 氨基} - 苯基）-1,4-二氢-2H-异喹啉-3-酮或（S）-5-（5-氯 - -1-甲基-2-氧代-1,2-二氢 - 吡啶-3-基）-6-（4-氯 - 苯基）-2-（2,4-二甲氧基 - 嘧啶-5-基）-1-异丙基 -5,6-二氢-1H-吡咯并[3,4-d]咪唑-4-酮和细胞周期蛋白依赖性激酶4/6（CDK4 / 6）抑制剂7-环戊基-2-（5-哌嗪-1-基）吡啶-2-基氨基）-7H-吡咯并[2,3-d]嘧啶-6-甲酸二甲基酰胺。此外，本公开涉及药物组合产品。本公开还涉及包含所述mdm2 / 4抑制剂或细胞周期蛋白依赖性激酶4/6（CDK4 / 6）抑制剂的相应药物制剂，用途和治疗方法。

2. 发明申请

US20150159222A1 MARKERS ASSOCIATED WITH HUMAN DOUBLE MINUTE 2 INHIBITORS 审中-公开
标题翻译：与人类双重2分子抑制剂相关的标记
公开(公告)号：US20150159222A1
公开(公告)日：2015-06-11
申请号：US14413510
申请日：2013-07-25
申请人： Swann Gaulis , Sebastien Jeay
发明人： Swann Gaulis , Sebastien Jeay
IPC分类号： C12Q1/68 , G01N33/50 , G01N33/574 , A61K31/496
CPC分类号： C12Q1/6886 , A61K31/496 , C07D401/12 , C12Q1/6883 , C12Q2600/106 , C12Q2600/136 , C12Q2600/156 , C12Q2600/158 , C12Y603/02019 , G01N33/5011 , G01N33/574 , G01N33/5748 , G01N33/57496 , G01N33/6875 , G01N2333/4704 , G01N2333/4748 , G01N2333/9015 , G01N2800/52
摘要： The invention provides methods of monitoring differential gene expression of biomarkers to determine patient sensitivity to Human Double Minute inhibitors (MDM2i), methods of determining the sensitivity of a cell to an MDM2i by measuring biomarkers and methods of screening for candidate MDM2i.
摘要翻译：本发明提供监测生物标志物差异基因表达以确定患者对人双分钟抑制剂（MDM2i）的敏感性的方法，通过测量生物标志物和筛选候选MDM2i的方法来确定细胞对MDM2i的敏感性的方法。

3. 发明申请

US20160289770A1 MARKERS ASSOCIATED WITH HUMAN DOUBLE MINUTE 2 INHIBITORS 审中-公开
公开(公告)号：US20160289770A1
公开(公告)日：2016-10-06
申请号：US15157686
申请日：2016-05-18
申请人： Swann Gaulis , Sebastien Jeay
发明人： Swann Gaulis , Sebastien Jeay
IPC分类号： C12Q1/68 , G01N33/574
CPC分类号： C12Q1/6886 , A61K31/496 , C07D401/12 , C12Q1/6883 , C12Q2600/106 , C12Q2600/136 , C12Q2600/156 , C12Q2600/158 , C12Y603/02019 , G01N33/5011 , G01N33/574 , G01N33/5748 , G01N33/57496 , G01N33/6875 , G01N2333/4704 , G01N2333/4748 , G01N2333/9015 , G01N2800/52
摘要： The invention provides methods of monitoring differential gene expression of biomarkers to determine patient sensitivity to Human Double Minute inhibitors (MDM2i), methods of determining the sensitivity of a cell to an MDM2i by measuring biomarkers and methods of screening for candidate MDM2i.

4. 发明申请

US20080261870A1 Use of the Pro-Peptide Domain of Lysyl Oxidase as a Therapeutic Agent 审中-公开
标题翻译：使用赖氨酰氧化酶的前肽结构域作为治疗剂
公开(公告)号：US20080261870A1
公开(公告)日：2008-10-23
申请号：US10585651
申请日：2005-01-06
申请人： Philip C. Trackman , Amitha H. Palamakumbura , Gail E. Sonenshein , Sebastien Jeay
发明人： Philip C. Trackman , Amitha H. Palamakumbura , Gail E. Sonenshein , Sebastien Jeay
IPC分类号： A61K38/17 , C12Q1/02 , A61P35/04
CPC分类号： A61K38/44 , C12Q1/26 , C12Y104/03013 , G01N33/5011 , G01N2333/906 , G01N2500/10
摘要： A therapeutic composition that includes an active portion of the lysyl oxidase pro-peptide in a pharmaceutically acceptable carrier substance and methods of using such a therapeutic composition are disclosed. The active agent does not have lysyl oxidase enzymatic activity. Preferably, the active polypeptide is active in inhibiting cell growth in soft agar and active in inhibiting tumor formation. In addition, the active polypeptide preferably comprises an active portion of the amino acid sequence given in SEQ ID NO.: 1 or SEQ ID NO.: 2, or conservative substitions thereof. Alternatively, the active polypeptide comprises a polypeptide comprising an active portion of an amino acid sequence selected from the group consisting of SEQ ID NOs.: 3-8, or conservative substitions thereof.
摘要翻译：公开了包含可药用载体物质中赖氨酰氧化酶原肽的活性部分的治疗组合物和使用这种治疗组合物的方法。活性剂不具有赖氨酰氧化酶酶活性。优选地，活性多肽在软琼脂中抑制细胞生长具有活性并且在抑制肿瘤形成中具有活性。此外，活性多肽优选包含SEQ ID NO：1或SEQ ID NO：2中给出的氨基酸序列的活性部分或其保守性变体。或者，活性多肽包含包含选自SEQ ID NO：3-8或其保守性变体的氨基酸序列的活性部分的多肽。

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