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1. 发明申请

WO2018035391A1 SECO-CYCLOPROPAPYRROLOINDOLE COMPOUNDS, ANTIBODY-DRUG CONJUGATES THEREOF, AND METHODS OF MAKING AND USE 审中-公开
标题翻译：二环丙基吡咯并吲哚化合物，其抗体 - 药物偶联物及其制备和使用方法
公开(公告)号：WO2018035391A1
公开(公告)日：2018-02-22
申请号：PCT/US2017/047465
申请日：2017-08-18
申请人： BRISTOL-MYERS SQUIBB COMPANY , THE SCRIPPS RESEARCH INSTITUTE
发明人： YANG, Fukang , ZHANG, Qian , SNYDER, Lawrence B. , GANGWAR, Sanjeev , BOGER, Dale L.
IPC分类号： C07D487/04 , C07D519/00 , A61K47/68 , A61K31/407 , A61K31/437 , A61P35/00
摘要： seco-Cyclopropapyrroloindole compounds of formula (I) where Hal, R 1 , R 2 , and R 3 are as defined in the application, are potent anti-cancer agents that can be used in antibody-drug conjugates.
摘要翻译：其中Hal，R 1，R 2和R 3分别代表氢原子的式（I）的开环 - 环丙基吡咯并吲哚化合物，其中R 1，R 2，R 3，如申请中所定义，是可用于抗体 - 药物缀合物中的有效的抗癌剂。

2. 发明公开

EP4132934A1 MEAYAMYCIN ANALOGUES AND METHODS OF USE 无效转让
公开(公告)号：EP4132934A1
公开(公告)日：2023-02-15
申请号：EP21722684.4
申请日：2021-04-08
申请人： Bristol-Myers Squibb Company , The Scripps Research Institute
发明人： BOGER, Dale L. , CHOWDARI, Naidu S. , GANGWAR, Sanjeev
IPC分类号： C07D493/10 , A61P35/00 , A61K31/35 , C07D405/14 , C07D407/06 , C07D417/14

3. 发明公开

EP3500574A1 SECO-CYCLOPROPAPYRROLOINDOLE COMPOUNDS, ANTIBODY-DRUG CONJUGATES THEREOF, AND METHODS OF MAKING AND USE 有权
公开(公告)号：EP3500574A1
公开(公告)日：2019-06-26
申请号：EP17758392.9
申请日：2017-08-18
申请人： Bristol-Myers Squibb Company , The Scripps Research Institute
发明人： YANG, Fukang , ZHANG, Qian , SNYDER, Lawrence B. , GANGWAR, Sanjeev , BOGER, Dale L.
IPC分类号： C07D487/04 , C07D519/00 , A61K47/68 , A61K31/407 , A61K31/437 , A61P35/00

4. 发明申请

WO2013148631A1 CYCLIC PRODRUGS OF DUOCARMYCIN ANALOGS 审中-公开
标题翻译：环孢霉素类似物的循环作用
公开(公告)号：WO2013148631A1
公开(公告)日：2013-10-03
申请号：PCT/US2013/033809
申请日：2013-03-26
申请人： THE SCRIPPS RESEARCH INSTITUTE
发明人： BOGER, Dale L.
IPC分类号： A61K31/27
CPC分类号： C07D498/06 , A61K45/06 , C07D209/62
摘要： The invention provides prodrugs of DNA-reactive analogs of duocarmycin and CC-1065 anticancer agents, wherein a cyclic prodrug form, such as carbamate, thionocarbamate, or carbamimidate, can be hydrolyzed by the patient in vivo to yield a respective bioactive agent comprising a DNA-alkylating moiety and a binding/targeting moiety. The DNA-reactive moiety is a γ-spirocyclohexenone fused to a heterocyclyl group which can be produced by endogenous hydrolysis of a cyclic carbamate prodrug of the invention. The cyclic carbamate prodrug produces no residual byproduct during activation in vivo . Methods of synthesis and biological methods and data are also provided.
摘要翻译：本发明提供了杜卡霉素和CC-1065抗癌剂的DNA反应性类似物的前药，其中环状前体药物形式如氨基甲酸酯，硫代氨基甲酸酯或氨基甲酰亚胺酯可以在体内由患者水解，得到包含DNA的相应生物活性剂 - 烷基化部分和结合/靶向部分。 DNA反应性部分是与可以通过本发明的环状氨基甲酸酯前药的内源性水解产生的杂环基团融合的γ-螺环烯酮酮。环状氨基甲酸酯前体体在体内活化期间不产生残留副产物。还提供了合成方法和生物学方法和数据。

5. 发明申请

WO2013022763A1 GLYCOPEPTIDE ANTIBIOTIC ANALOGS EFFECTIVE AGAINST VANCOMYCIN-RESISTANT BACTERIAL STRAINS 审中-公开
标题翻译：抗乙型脑炎抗生素类抗生素类抗生素
公开(公告)号：WO2013022763A1
公开(公告)日：2013-02-14
申请号：PCT/US2012/049548
申请日：2012-08-03
申请人： THE SCRIPPS RESEARCH INSTITUTE , BOGER, Dale L.
发明人： BOGER, Dale L.
IPC分类号： A61K31/70 , A01N43/04 , A61K38/14
CPC分类号： C07K9/008 , A61K38/00 , A61K38/14 , C07K7/06
摘要： The invention is directed to glycopeptide antibiotics and their aglycones that are engineered to overcome bacterial resistance by replacement of a single, specific peptide carboxamide group in the core peptide of the glycopeptide antibiotic with an amidine group. The amidine pseudopeptide analog of the glycopeptide is effective in killing vancomycin-resistant bacteria at therapeutically achievable concentrations in a patient. For example, a [ψ[C(=NH)NH]Tpg 4 ]-vancomycin aglycon designed to exhibit the dual binding to D-Ala-D-Ala and D-Ala-D-Lac needed to reinstate activity against vancomycin-resistant bacteria has been shown to overcome a common mode of bacterial resistance to the "last resort" antibiotics of the glycopeptide class. The pseudopeptide amidine analogs can be prepared from corresponding pseudopeptide thioamide analogs, which can be prepared synthetically, semi-synthetically, or biosynthetically.
摘要翻译：本发明涉及通过用脒基取代糖肽抗生素的核心肽中的单个特异性肽羧酰胺基而被工程化以克服细菌耐药性的糖肽抗生素及其糖苷配基。糖肽的脒假肽类似物在患者中以治疗可达到的浓度杀死万古霉素抗性细菌是有效的。例如，设计用于显示与D-Ala-D-Ala和D-Ala-D-Lac的双重结合的[α[C（= NH）NH] Tpg4] - 万古霉素糖苷配基需要恢复对万古霉素抗性细菌的活性已被证明能够克服对糖肽类的“最后手段”抗生素的细菌耐药性的共同模式。假肽脒类似物可以由相应的假肽硫代酰胺类似物制备，其可以合成，半合成或生物合成制备。

6. 发明授权

EP2830614B1 CYCLIC PRODRUGS OF DUOCARMYCIN ANALOGS 失效
标题翻译：多卡拉霉素类似物的循环前药
公开(公告)号：EP2830614B1
公开(公告)日：2017-04-26
申请号：EP13769317.2
申请日：2013-03-26
申请人： The Scripps Research Institute
发明人： BOGER, Dale L.
IPC分类号： A61K31/27 , A61P35/00
CPC分类号： C07D498/06 , A61K45/06 , C07D209/62

7. 发明公开

EP2830614A1 CYCLIC PRODRUGS OF DUOCARMYCIN ANALOGS 失效
标题翻译：循环前体药物OFF卡霉素类似物
公开(公告)号：EP2830614A1
公开(公告)日：2015-02-04
申请号：EP13769317.2
申请日：2013-03-26
申请人： The Scripps Research Institute
发明人： BOGER, Dale L.
IPC分类号： A61K31/27
CPC分类号： C07D498/06 , A61K45/06 , C07D209/62
摘要： The invention provides prodrugs of DNA-reactive analogs of duocarmycin and CC-1065 anticancer agents, wherein a cyclic prodrug form, such as carbamate, thionocarbamate, or carbamimidate, can be hydrolyzed by the patient
in vivo to yield a respective bioactive agent comprising a DNA-alkylating moiety and a binding/targeting moiety. The DNA-reactive moiety is a γ-spirocyclohexenone fused to a heterocyclyl group which can be produced by endogenous hydrolysis of a cyclic carbamate prodrug of the invention. The cyclic carbamate prodrug produces no residual byproduct during activation
in vivo . Methods of synthesis and biological methods and data are also provided.

8. 发明公开

EP2739289A1 GLYCOPEPTIDE ANTIBIOTIC ANALOGS EFFECTIVE AGAINST VANCOMYCIN-RESISTANT BACTERIAL STRAINS 有权
标题翻译：糖肽抗生素类似物效能AGAINST万古霉素抗性细菌菌株
公开(公告)号：EP2739289A1
公开(公告)日：2014-06-11
申请号：EP12821494.7
申请日：2012-08-03
申请人： The Scripps Research Institute
发明人： BOGER, Dale L.
IPC分类号： A61K31/70 , A01N43/04 , A61K38/14
CPC分类号： C07K9/008 , A61K38/00 , A61K38/14 , C07K7/06
摘要： The invention is directed to glycopeptide antibiotics and their aglycones that are engineered to overcome bacterial resistance by replacement of a single, specific peptide carboxamide group in the core peptide of the glycopeptide antibiotic with an amidine group. The amidine pseudopeptide analog of the glycopeptide is effective in killing vancomycin-resistant bacteria at therapeutically achievable concentrations in a patient. For example, a [Ψ[C(═NH)NH]Tpg4]-vancomycin aglycon designed to exhibit the dual binding to D-Ala-D-Ala and D-Ala-D-Lac needed to reinstate activity against vancomycin-resistant bacteria has been shown to overcome a common mode of bacterial resistance to the “last resort” antibiotics of the glycopeptide class. The pseudopeptide amidine analogs can be prepared from corresponding pseudopeptide thioamide analogs, which can be prepared synthetically, semi-synthetically, or biosynthetically.

9. 发明授权

EP2739289B1 GLYCOPEPTIDE ANTIBIOTIC ANALOGS EFFECTIVE AGAINST VANCOMYCIN-RESISTANT BACTERIAL STRAINS 有权
公开(公告)号：EP2739289B1
公开(公告)日：2020-05-06
申请号：EP12821494.7
申请日：2012-08-03
申请人： The Scripps Research Institute
发明人： BOGER, Dale L.
IPC分类号： A61K31/70 , A01N43/04 , A61K38/14 , A61P31/04

10. 发明公开

EP3177601A2 TLR-INDEPENDENT SMALL MOLECULE ADJUVANTS 有权
标题翻译：独立于TLR的小分子佐剂
公开(公告)号：EP3177601A2
公开(公告)日：2017-06-14
申请号：EP15830729.8
申请日：2015-08-05
申请人： The Scripps Research Institute , Board of Regents of the University of Texas System
发明人： BOGER, Dale L. , BEUTLER, Bruce
IPC分类号： C07D307/78 , C07D209/04 , C07D209/12 , A61K31/343 , A61K31/404
CPC分类号： A61K31/343 , A61K31/167 , A61K31/381 , A61K31/404 , A61K31/4439 , A61K31/498 , A61K31/506 , A61K39/39 , C07C237/44 , C07C2601/14 , C07D209/18 , C07D209/42 , C07D307/85 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12
摘要： which X, Y, Z, n, R1, R2, R3, R4 and W are defined within. Also disclosed are a method of its preparation and use, as well as a pharmaceutical composition containing the same.
摘要翻译：公开了在结构上对应于下式I或其药学上可接受的盐的TLR非依赖性佐剂化合物，其中X，Y，Z，n，R 1，R 2，R 3，R 4和W定义于其中。还公开了其制备和使用方法，以及含有其的药物组合物。

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