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1. 发明申请

WO2012143499A3 NOVEL BINDER-DRUG CONJUGATES (ADCS) AND THEIR USE 审中-公开
标题翻译：新建合并偶联物ACTIVE（ADC）和它们的用途
公开(公告)号：WO2012143499A3
公开(公告)日：2012-12-13
申请号：PCT/EP2012057249
申请日：2012-04-20
申请人： BAYER IP GMBH , BAYER PHARMA AG , LERCHEN HANS-GEORG , STELTE-LUDWIG BEATRIX , GOLFIER SVEN , KOPITZ CHARLOTTE CHRISTINE , BEIER RUDOLF , EL SHEIKH SHERIF , HEISLER IRING , HARRENGA AXEL , THIERAUCH KARL-HEINZ , SCHUHMACHER JOACHIM , BRUDER SANDRA , GREVEN SIMONE , LINDEN LARS , WILLUDA JOERG , MAHLERT CHRISTOPH , PETRUL HEIKE , JOERISEN HANNAH , BORKOWSKI SANDRA
发明人： LERCHEN HANS-GEORG , STELTE-LUDWIG BEATRIX , GOLFIER SVEN , KOPITZ CHARLOTTE CHRISTINE , BEIER RUDOLF , EL SHEIKH SHERIF , HEISLER IRING , HARRENGA AXEL , THIERAUCH KARL-HEINZ , SCHUHMACHER JOACHIM , BRUDER SANDRA , GREVEN SIMONE , LINDEN LARS , WILLUDA JOERG , MAHLERT CHRISTOPH , PETRUL HEIKE , JOERISEN HANNAH , BORKOWSKI SANDRA
IPC分类号： A61K47/48 , A61P35/00 , C07K16/30
CPC分类号： A61K47/48715 , A61K31/40 , A61K31/4025 , A61K31/404 , A61K31/422 , A61K31/4245 , A61K31/5355 , A61K31/536 , A61K31/537 , A61K31/5377 , A61K39/3955 , A61K45/06 , A61K47/542 , A61K47/6803 , A61K47/6851 , A61K47/6859 , A61K47/6869 , A61K47/6889 , A61K47/6891 , C07K5/06 , C07K5/06052 , C07K7/02 , C07K7/06 , C07K16/18 , C07K16/2812 , C07K16/2863 , C07K16/30 , C07K2317/565 , C07K2317/76
摘要： The present application relates to novel, anti-mesothelin binder-drug conjugates (ADCs) of N,N-dialkyl auristatins, to effective metabolites of said ADCs, to methods for producing said ADCs, to the use of said ADCs for treating and/or preventing diseases, and to the use of said ADCs for producing pharmaceuticals for treating and/or preventing diseases, in particular hyperproliferative and/or angiogenic diseases, such as cancers. Such treatments can be carried out as monotherapy or in combination with other pharmaceuticals or additional therapeutic measures.
摘要翻译：本申请涉及新的，直接针对的N，N-二Dialkylauristatinen，这些ADC的有效代谢物的靶标间皮素粘结剂 - 药物偶联物（ADC），用于制备这些ADC，对于疾病的治疗和/或预防中使用这些ADC的处理和使用这些ADC的用于制备药物的用于治疗疾病，特别是过度增殖性和/或血管生成性病症如癌症的治疗和/或预防。这样的治疗可以作为单一药剂或与其它药物或其它治疗措施的组合来进行。

2. 发明申请

WO2012143497A3 NOVEL BINDER-DRUG CONJUGATES (ADCS) AND THEIR USE 审中-公开
标题翻译：新建合并偶联物ACTIVE（ADC）和它们的用途
公开(公告)号：WO2012143497A3
公开(公告)日：2013-03-21
申请号：PCT/EP2012057247
申请日：2012-04-20
申请人： BAYER IP GMBH , BAYER PHARMA AG , LERCHEN HANS-GEORG , LINDEN LARS , EL SHEIKH SHERIF , WILLUDA JOERG , KOPITZ CHARLOTTE CHRISTINE , SCHUHMACHER JOACHIM , GREVEN SIMONE , MAHLERT CHRISTOPH , STELTE-LUDWIG BEATRIX , GOLFIER SVEN , BEIER RUDOLF , HEISLER IRING , HARRENGA AXEL , THIERAUCH KARL-HEINZ , BRUDER SANDRA , PETRUL HEIKE , JOERISEN HANNAH , BORKOWSKI SANDRA
发明人： LERCHEN HANS-GEORG , LINDEN LARS , EL SHEIKH SHERIF , WILLUDA JOERG , KOPITZ CHARLOTTE CHRISTINE , SCHUHMACHER JOACHIM , GREVEN SIMONE , MAHLERT CHRISTOPH , STELTE-LUDWIG BEATRIX , GOLFIER SVEN , BEIER RUDOLF , HEISLER IRING , HARRENGA AXEL , THIERAUCH KARL-HEINZ , BRUDER SANDRA , PETRUL HEIKE , JOERISEN HANNAH , BORKOWSKI SANDRA
IPC分类号： A61K47/48 , A61P35/00 , C07K16/30
CPC分类号： A61K47/48715 , A61K31/40 , A61K31/4025 , A61K31/404 , A61K31/422 , A61K31/4245 , A61K31/5355 , A61K31/536 , A61K31/537 , A61K31/5377 , A61K39/3955 , A61K45/06 , A61K47/542 , A61K47/6803 , A61K47/6851 , A61K47/6859 , A61K47/6869 , A61K47/6889 , A61K47/6891 , C07K5/06 , C07K5/06052 , C07K7/02 , C07K7/06 , C07K16/18 , C07K16/2812 , C07K16/2863 , C07K16/30 , C07K2317/565 , C07K2317/76
摘要： The present application relates to novel, anti-C4,4a binder-drug conjugates (ADCs) of N,N-dialkyl auristatins, to effective metabolites of said ADCs, to methods for producing said ADCs, to the use of said ADCs for treating and/or preventing diseases, and to the use of said ADCs for producing pharmaceuticals for treating and/or preventing diseases, in particular hyperproliferative and/or angiogenic diseases, such as cancers. Such treatments can be carried out as monotherapy or in combination with other pharmaceuticals or additional therapeutic measures.
摘要翻译：本申请涉及新的，针对靶的N，N-二Dialkylauristatinen，这些ADC的有效代谢物C4,4a粘合剂 - 药物Konjuagte器（ADC），用于制备这些ADC，用于治疗和/或预防的使用这些ADC的处理疾病以及用于制备药物的用于治疗疾病，特别是过度增殖性和/或血管生成性病症如癌症的治疗和/或预防中使用这些ADC的。这样的治疗可以作为单一药剂或与其它药物或其它治疗措施的组合来进行。

3. 发明申请

WO2012143496A2 NOVEL BINDER-DRUG CONJUGATES (ADCS) AND THEIR USE 审中-公开
标题翻译：新建合并偶联物ACTIVE（ADC）和它们的用途
公开(公告)号：WO2012143496A2
公开(公告)日：2012-10-26
申请号：PCT/EP2012057245
申请日：2012-04-20
申请人： BAYER IP GMBH , BAYER PHARMA AG , LERCHEN HANS-GEORG , EL SHEIKH SHERIF , PETRUL HEIKE , STELTE-LUDWIG BEATRIX , BEIER RUDOLF , SCHUHMACHER JOACHIM , MAHLERT CHRISTOPH , GREVEN SIMONE , LINDEN LARS , WILLUDA JOERG , KOPITZ CHARLOTTE CHRISTINE , GOLFIER SVEN , HEISLER IRING , HARRENGA AXEL , THIERAUCH KARL-HEINZ , BRUDER SANDRA , JOERISEN HANNAH , BORKOWSKI SANDRA
发明人： LERCHEN HANS-GEORG , EL SHEIKH SHERIF , PETRUL HEIKE , STELTE-LUDWIG BEATRIX , BEIER RUDOLF , SCHUHMACHER JOACHIM , MAHLERT CHRISTOPH , GREVEN SIMONE , LINDEN LARS , WILLUDA JOERG , KOPITZ CHARLOTTE CHRISTINE , GOLFIER SVEN , HEISLER IRING , HARRENGA AXEL , THIERAUCH KARL-HEINZ , BRUDER SANDRA , JOERISEN HANNAH , BORKOWSKI SANDRA
IPC分类号： A61K47/48 , A61P35/00 , C07K16/30
CPC分类号： A61K47/48715 , A61K31/40 , A61K31/4025 , A61K31/404 , A61K31/422 , A61K31/4245 , A61K31/5355 , A61K31/536 , A61K31/537 , A61K31/5377 , A61K39/3955 , A61K45/06 , A61K47/542 , A61K47/6803 , A61K47/6851 , A61K47/6859 , A61K47/6869 , A61K47/6889 , A61K47/6891 , C07K5/06 , C07K5/06052 , C07K7/02 , C07K7/06 , C07K16/18 , C07K16/2812 , C07K16/2863 , C07K16/30 , C07K2317/565 , C07K2317/76
摘要： The present application relates to novel, anti-carboanhydrase IX (carboanhydrase IX, CAIX, CA9, G250) binder-drug conjugates (ADCs) of N,N-dialkyl auristatins, to effective metabolites of said ADCs, to methods for producing said ADCs, to the use of said ADCs for treating and/or preventing diseases, and to the use of said ADCs for producing pharmaceuticals for treating and/or preventing diseases, in particular hyperproliferative and/or angiogenic diseases, such as cancers. Such treatments can be carried out as monotherapy or in combination with other pharmaceuticals or additional therapeutic measures.
摘要翻译：本申请涉及到针对靶酸酐酶IX新颖碳（碳酸酐酶IX，CAIX，CA9，G250）定向N个粘合剂 - 药物偶联物（ADC），N-Dialkylauristatinen，这些ADC的有效代谢物，用于制备这些ADC处理使用这些ADC用于治疗和/或预防的疾病，以及用于制备药物的用于治疗疾病，特别是过度增殖性和/或血管生成性病症如癌症的治疗和/或预防中使用这些ADC中的。这样的治疗可以作为单一药剂或与其它药物或其它治疗措施的组合来进行。

4. 发明申请

WO2012143495A3 NOVEL BINDER-DRUG CONJUGATES (ADCS) AND THEIR USE 审中-公开
标题翻译：新建合并偶联物ACTIVE（ADC）和它们的用途
公开(公告)号：WO2012143495A3
公开(公告)日：2012-12-13
申请号：PCT/EP2012057243
申请日：2012-04-20
申请人： BAYER IP GMBH , BAYER PHARMA AG , LERCHEN HANS-GEORG , EL SHEIKH SHERIF , BEIER RUDOLF , BRUDER SANDRA , STELTE-LUDWIG BEATRIX , JOERISEN HANNAH , MAHLERT CHRISTOPH , GREVEN SIMONE , PETRUL HEIKE , SCHUHMACHER JOACHIM , LINDEN LARS , WILLUDA JOERG , KOPITZ CHAROTTE CHRISTINE , GOLFIER SVEN , HEISLER IRING , HARRENGA AXEL , THIERAUCH KARL-HEINZ , BORKOWSKI SANDRA
发明人： LERCHEN HANS-GEORG , EL SHEIKH SHERIF , BEIER RUDOLF , BRUDER SANDRA , STELTE-LUDWIG BEATRIX , JOERISEN HANNAH , MAHLERT CHRISTOPH , GREVEN SIMONE , PETRUL HEIKE , SCHUHMACHER JOACHIM , LINDEN LARS , WILLUDA JOERG , KOPITZ CHAROTTE CHRISTINE , GOLFIER SVEN , HEISLER IRING , HARRENGA AXEL , THIERAUCH KARL-HEINZ , BORKOWSKI SANDRA
IPC分类号： A61K47/48 , A61P35/00 , C07K16/30
CPC分类号： A61K47/48715 , A61K31/40 , A61K31/4025 , A61K31/404 , A61K31/422 , A61K31/4245 , A61K31/5355 , A61K31/536 , A61K31/537 , A61K31/5377 , A61K39/3955 , A61K45/06 , A61K47/542 , A61K47/6803 , A61K47/6851 , A61K47/6859 , A61K47/6869 , A61K47/6889 , A61K47/6891 , C07K5/06 , C07K5/06052 , C07K7/02 , C07K7/06 , C07K16/18 , C07K16/2812 , C07K16/2863 , C07K16/30 , C07K2317/565 , C07K2317/76
摘要： The present application relates to novel, anti-Target Epidermal Growth Factor Receptor (EGFR, GeneID1956) binder-drug conjugates (ADCs) of N,N-dialkyl auristatins, to effective metabolites of said ADCs, to methods for producing said ADCs, to the use of said ADCs for treating and/or preventing diseases, and to the use of said ADCs for producing pharmaceuticals for treating and/or preventing diseases, in particular hyperproliferative and/or angiogenic diseases, such as cancers. Such treatments can be carried out as monotherapy or in combination with other pharmaceuticals or additional therapeutic measures.
摘要翻译：本申请涉及新的抗靶表皮生长因子受体（EGFR，GeneID1956）定向N个粘合剂 - 药物偶联物（ADC），N-Dialkylauristatinen，这些ADC的有效代谢物，用于制备这些ADC，对于使用这些ADC的处理治疗和/或预防的疾病，以及用于制备药物的用于治疗疾病，特别是过度增殖性和/或血管生成性病症如癌症的治疗和/或预防中使用这些ADC的。这样的治疗可以作为单一药剂或与其它药物或其它治疗措施的组合来进行。

5. 发明申请

WO2013087716A3 FGFR ANTIBODY DRUG CONJUGATES (ADCS) AND THE USE THEREOF 审中-公开
标题翻译： FGFR粘结剂-WIRKSTOFF偶联物及其用途
公开(公告)号：WO2013087716A3
公开(公告)日：2013-08-22
申请号：PCT/EP2012075277
申请日：2012-12-12
申请人： BAYER PHARMA AG , BAYER IP GMBH , SEATTLE GENETICS INC
发明人： LERCHEN HANS-GEORG , HAMMER STEFANIE , HARRENGA AXEL , KOPITZ CHARLOTTE CHRISTINE , NISING CARL FRIEDRICH , SOMMER ANETTE , STELTE-LUDWIG BEATRIX , MAHLERT CHRISTOPH , SCHUHMACHER JOACHIM , GOLFIER SVEN , GREVEN SIMONE , BRUDER SANDRA
IPC分类号： A61K47/48
CPC分类号： A61K47/48561 , A61K38/05 , A61K47/6849
摘要： The present application relates to new antibody drug conjugates (ADCs) of N,N dialkylauristatins directed against the target FGFR2, drug metabolites of said ADCs, a method for producing said ADCs, the use of said ADCs for the treatment and/or prevention of illnesses as well as the use of said ADCs for producing pharmaceuticals for the treatment and/or prevention of illnesses, particularly of hyperproliferative and/or angiogenic diseases such as carcinosis. Such treatments can be carried out as monotherapy or in combination with other pharmaceuticals or additional therapeutic measures.
摘要翻译：本申请涉及新的，直接针对的N，N-二Dialkylauristatinen，这些ADC的有效代谢物的目标FGFR2粘合剂 - 药物偶联物（ADC），用于制备这些ADC，对于疾病的治疗和/或预防中使用这些ADC的处理和使用这些ADC的用于制备药物的用于治疗疾病，特别是过度增殖性和/或血管生成性病症如癌症的治疗和/或预防。这样的治疗可以作为单一药剂或与其它药物或其它治疗措施的组合来进行。

6. 发明申请

WO0041469A2 beta -PHENYLALANINE DERIVATIVES AS INTEGRIN ANTAGONISTS 审中-公开
标题翻译： β-内啡肽衍生物作为整合素拮抗剂
公开(公告)号：WO0041469A2
公开(公告)日：2000-07-20
申请号：PCT/EP0000120
申请日：2000-01-11
申请人： BAYER AG , SCHOOP ANDREAS , MUELLER GERHARD , BRUEGGEMEIER ULF , SCHMIDT DELF , STELTE LUDWIG BEATRIX , KELDENICH JOERG , ALBERS MARKUS
发明人： SCHOOP ANDREAS , MUELLER GERHARD , BRUEGGEMEIER ULF , SCHMIDT DELF , STELTE-LUDWIG BEATRIX , KELDENICH JOERG , ALBERS MARKUS
IPC分类号： C07D233/50 , A61K31/198 , A61K31/27 , A61K31/4164 , A61K31/4184 , A61K31/4406 , A61K31/4409 , A61P9/00 , A61P9/10 , A61P19/00 , A61P19/02 , A61P27/02 , A61P29/00 , A61P35/00 , A61P43/00 , C07C311/19 , C07C311/47 , C07D213/40 , C07D213/75 , C07D235/30 , C07C311/00
CPC分类号： C07C311/19 , C07C311/47
摘要： The present invention relates to compounds of general formula (1), wherein R is -SO2R , -COOR , -COR , -CONR 2 or -CSNR 2; R is hydrogen, a substituted or unsubstituted alkyl or cycloalkyl residue, a substituted or unsubstituted aryl residue or a saturated or unsaturated, optionally substituted heterocyclic residue; R is a substituted or unsubstituted alkyl or cycloalkyl residue, a substituted or unsubstituted aryl residue or a saturated or unsaturated, optionally substituted heterocyclic residue; L is a sulphonamide, amide, ether, ester, keto, urea, thioether, sulphoxide or sulphone unit optionally extended by one or two methylene groups; and X is N, O or S; and their physiologically acceptable salts and stereoisomers. The present invention furthermore relates to a process for the preparation of the compounds of formula (1), a pharmaceutical composition containing at least one of these compounds, and the use of compounds of formula (1) for the production of a pharmaceutical composition having integrin-antagonistic action and in particular for the inhibition of angiogenesis and/or for the therapy and prophylaxis of cancer, osteolytic diseases such as osteoporosis, arteriosclerosis, restenosis and ophthalmic disorders.
摘要翻译：本发明涉及通式（1）的化合物，其中R 4是-SO 2 R 4'，-COOR 4，-COR 4'，-CONR 4'2或-CSNR R 4'是氢，取代或未取代的烷基或环烷基残基，取代或未取代的芳基残基或饱和或不饱和的任选取代的杂环残基; R 4'是取代或未取代的杂环残基烷基或环烷基残基，取代或未取代的芳基残基或饱和或不饱和的任选取代的杂环残基; L是任选地被一个或两个亚甲基延伸的磺酰胺，酰胺，醚，酯，酮，脲，硫醚，亚砜或砜单元; X是N，O或S; 及其生理上可接受的盐和立体异构体。本发明还涉及制备式（1）化合物的方法，含有至少一种这些化合物的药物组合物，以及式（1）化合物在制备具有整联蛋白的药物组合物中的用途 - 拮抗作用，特别是用于抑制血管生成和/或用于治疗和预防癌症，溶骨疾病如骨质疏松症，动脉硬化，再狭窄和眼科疾病。

7. 发明申请

WO2017060322A3 PTEFB-INHIBITOR-ADC 审中-公开
标题翻译： PTEFB抑制剂的ADC
公开(公告)号：WO2017060322A3
公开(公告)日：2017-05-18
申请号：PCT/EP2016073825
申请日：2016-10-06
申请人： BAYER PHARMA AG
发明人： WASNAIRE PIERRE , GRIEBENOW NILS , BÖHNKE NIELS , LÜCKING ULRICH , LERCHEN HANS-GEORG , STELTE-LUDWIG BEATRIX , MAHLERT CHRISTOPH , BÖMER ULF , GREVEN SIMONE , DIETZ LISA , TERJUNG CARSTEN , ZHENG KUNZENG , PING GAO , CHEN GANG , XI JIAJUN
IPC分类号： A61K47/68 , A61P35/00 , C07D498/08
CPC分类号： C07D498/18 , A61K47/6803 , A61K47/6849 , A61K47/6851 , A61K47/6857 , A61K47/6863
摘要： It is an object of the present invention to provide substances which, after administration at a relatively low concentration, unfold apoptotic action and may therefore be of benefit for cancer therapy. To achieve this object, the invention provides conjugates of a binder or derivatives thereof with one or more active compound molecules, the active compound molecule being a CDK9 inhibitor attached to the binder via a linker L. The binder is preferably a binder protein or peptide, particularly preferably a human, humanized or chimeric monoclonal antibody or an antigen-binding fragment thereof, in particular an anti-TWEAKR antibody or an antigen-binding fragment thereof or an anti-EGFR antibody or an antigen-binding fragment thereof. Particular preference is given to an anti-TWEAKR antibody which binds specifically to amino acid D in position 47 (D47) of TWEAKR (SEQ ID NO: 169), in particular the anti-TWEAKR antibody TPP-2090, or the anti-EGFR antibodies cetuximab, TPP-4030, TPP-5653, or nimotuzumab. The inventors have found a number of ways to attach the binder to the CDK9 inhibitor in order to achieve the object mentioned above.
摘要翻译：本发明的一个目的是提供在相对低浓度施用后展现凋亡作用并因此可能对癌症治疗有益的物质。为了实现该目的，本发明提供了粘合剂或其衍生物与一种或多种活性化合物分子的缀合物，活性化合物分子是通过连接物L连接至粘合剂的CDK9抑制剂。粘合剂优选为结合蛋白或肽，特别优选人类，人源化或嵌合单克隆抗体或其抗原结合片段，特别是抗TWEAKR抗体或其抗原结合片段或抗EGFR抗体或其抗原结合片段。特别优选抗TWEAKR抗体，其特异性结合TWEAKR（SEQ ID NO：169）的位置47（D47）中的氨基酸D，特别是抗TWEAKR抗体TPP-2090或抗EGFR抗体西妥昔单抗，TPP-4030，TPP-5653或尼妥珠单抗。发明人已经发现了许多将粘合剂附着到CDK9抑制剂上的方法，以达到上述目的。

8. 发明申请

WO2016207090A3 TARGETED CONJUGATES OF KSP INHIBITORS 审中-公开
标题翻译： KSP抑制剂的目标关联
公开(公告)号：WO2016207090A3
公开(公告)日：2017-02-16
申请号：PCT/EP2016064120
申请日：2016-06-20
申请人： BAYER PHARMA AG
发明人： LERCHEN HANS-GEORG , CANCHO GRANDE YOLANDA , STELTE-LUDWIG BEATRIX , SOMMER ANETTE , MAHLERT CHRISTOPH , REBSTOCK ANNE-SOPHIE , GREVEN SIMONE , GRIEBENOW NILS , TEBBE JAN , KENSCH OLIVER
IPC分类号： A61P35/00
CPC分类号： A61K47/6865 , A61K47/6803 , A61K47/6849 , A61K47/6855 , A61K47/6857 , A61K47/6863
摘要： The invention relates to site specific homogeneous binder drug conjugates of kinesin spindle protein inhibitors, to active metabolites of these conjugates, to processes for preparing these conjugates, to the use of these conjugates for the treatment and/or prophylaxis of diseases and to the use of these conjugates for preparing medicaments for treatment and/or prevention of diseases, in particular hyperproliferative and/or angiogenic disorders such as, for example, cancer diseases. Such treatments can be carried out as monotherapy or else in combination with other medicaments or further therapeutic measures.
摘要翻译：本发明涉及驱动蛋白纺锤体蛋白抑制剂的位点特异性均相粘合剂药物缀合物，这些缀合物的活性代谢物，制备这些缀合物的方法，使用这些缀合物用于治疗和/或预防疾病，以及使用这些用于制备用于治疗和/或预防疾病的药物的缀合物，特别是过度增殖和/或血管生成疾病，例如癌症疾病。这样的治疗可以作为单一疗法进行，也可以与其他药物组合进行或进一步的治疗措施。

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