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公开(公告)号：US20120172448A1
公开(公告)日：2012-07-05
申请号：US13312320
申请日：2011-12-06
Applicant: Thomas LAMPE , Michael G. HAHN , Johannes-Peter STASCH , Karl-Heinz SCHLEMMER , Frank WUNDER , Sherif EL SHEIKH , Volkhart Min-Jian LI , Eva-Maria BECKER , Friederike STOLL , Andreas KNORR , Peter KOLKHOF , Elisabeth WOLTERING
Inventor： Thomas LAMPE , Michael G. HAHN , Johannes-Peter STASCH , Karl-Heinz SCHLEMMER , Frank WUNDER , Sherif EL SHEIKH , Volkhart Min-Jian LI , Eva-Maria BECKER , Friederike STOLL , Andreas KNORR , Peter KOLKHOF , Elisabeth WOLTERING
IPC: A61K31/196 , C07C231/14 , A61P9/04 , A61P13/12 , A61P9/12 , A61P9/00 , A61P7/02 , C07C233/55 , A61P9/10
CPC classification number: C07C231/02 , A61K31/196 , C07C233/24 , C07C233/55
Abstract: The present application relates to novel substituted 1-benzylcycloalkylcarboxylic acid derivatives, to processes for their preparation, to their use for the treatment and/or prevention of diseases, and to their use for producing medicaments for the treatment and/or prevention of diseases, especially for the treatment and/or prevention of cardiovascular disorders.
Abstract translation: 本申请涉及新的取代的1-苄基环烷基羧酸衍生物，其制备方法，其用于治疗和/或预防疾病的用途及其用于制备用于治疗和/或预防疾病的药物的用途，特别是 用于治疗和/或预防心血管疾病。
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公开(公告)号：US20140127240A1
公开(公告)日：2014-05-08
申请号：US14113070
申请日：2012-04-20
Applicant: Hans-Georg Lerchen , Lars Linden , Sherif El Sheikh , Jörg Willuda , Charlotte C. Kopitz , Joachim Schuhmacher , Simone Greven , Christoph Mahlert , Beatrix Stelte-Ludwig , Sven Golfier , Rudolf Beier , Iring Heisler , Axel Harrenga , Karl-Heinz Thierauch , Sandra Bruder , Heike Petrul , Hannah Jörißen , Sandra Brokowski
Inventor： Hans-Georg Lerchen , Lars Linden , Sherif El Sheikh , Jörg Willuda , Charlotte C. Kopitz , Joachim Schuhmacher , Simone Greven , Christoph Mahlert , Beatrix Stelte-Ludwig , Sven Golfier , Rudolf Beier , Iring Heisler , Axel Harrenga , Karl-Heinz Thierauch , Sandra Bruder , Heike Petrul , Hannah Jörißen , Sandra Brokowski
CPC classification number: 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 , C07K5/0205 , C07K5/0207 , C07K5/06 , C07K5/06034 , C07K5/06052 , C07K5/0606 , C07K7/02 , C07K7/06 , C07K16/18 , C07K16/28 , C07K16/2812 , C07K16/2863 , C07K16/30 , C07K2317/21 , C07K2317/24 , C07K2317/565 , C07K2317/76
Abstract: The present patent application relates to novel binder-drug conjugates (ADCs) of N,N-dialkylauristatins directed against the target epidermal growth factor receptor (EGFR, gene ID 1956), effective metabolites of these ADCs, methods for producing these ADCs, use of these ADCs for treatment and or prevention of diseases as well as the use of these ADCs to produce pharmaceutical drugs for treatment and/or prevention of diseases, in particular hyperproliferative and/or angiogenic diseases such as cancer, for example. Such treatments may be administered as monotherapy or in combination with other pharmaceutical drugs or other therapeutic measures.
Abstract translation: 本专利申请涉及针对靶表皮生长因子受体（EGFR，基因ID 1956）的N，N-二烷基硫酸锡的新型粘合剂 - 药物共轭物（ADC），这些ADC的有效代谢物，制备这些ADC的方法， 这些ADC用于治疗和/或预防疾病，以及使用这些ADC来制备用于治疗和/或预防疾病，特别是过度增生和/或血管发生疾病例如癌症的药物。 这样的治疗可以作为单一疗法或与其它药物或其他治疗措施组合施用。
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公开(公告)号：US20140080763A1
公开(公告)日：2014-03-20
申请号：US14004699
申请日：2012-03-12
Applicant: Hans-Georg Lerchen , Sherif El Sheikh , Beatrix Stelte-Ludwig , Joachim Schuhmacher , Mark Gnoth
Inventor： Hans-Georg Lerchen , Sherif El Sheikh , Beatrix Stelte-Ludwig , Joachim Schuhmacher , Mark Gnoth
CPC classification number: A61K38/07 , A61K38/00 , A61K45/06 , A61K47/6415 , C07K5/0205
Abstract: The present application relates to new derivatives, substituted on the N terminus by a carboxyalkyl group, of monomethylauristatin E and monomethylauristatin F, to processes for preparing these derivatives, to the use of these derivatives for treating and/or preventing diseases, and to the use of these derivatives for producing medicaments for treating and/or preventing diseases, more particularly hyperproliferative and/or angiogenic disorders such as cancer disorders, for example. Such treatments may be applied as a monotherapy or else in combination with other medicaments or further therapeutic measures.
Abstract translation: 本申请涉及在N末端被羧基烷基取代的单甲基海洛定蛋白E和单甲基海洛定蛋白F的新衍生物，用于制备这些衍生物的方法，这些衍生物用于治疗和/或预防疾病的用途和用途 的这些衍生物用于制备用于治疗和/或预防疾病的药物，更具体地是过度增殖和/或血管生成障碍，例如癌症病症。 这样的治疗可以作为单一疗法应用，也可以与其它药物组合使用或其它治疗措施。
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公开(公告)号：US20130261064A1
公开(公告)日：2013-10-03
申请号：US13876777
申请日：2011-09-26
Applicant: Hans-Georg Lerchen , Sherif El Sheikh , Beatrix Srelte Ludwig , Sven Golfier , Joachim Schumacher , Joan Mark Gnoth , Ursula Krenz
Inventor： Hans-Georg Lerchen , Sherif El Sheikh , Beatrix Srelte Ludwig , Sven Golfier , Joachim Schumacher , Joan Mark Gnoth , Ursula Krenz
CPC classification number: C07K5/1021 , A61K38/00 , A61K38/07 , A61K38/08 , A61K45/06 , C07K1/1077 , C07K5/0205 , C07K7/02
Abstract: The present application relates to new derivatives of monomethylauristatin F, substituted on the N terminus by a carboxyalkyl group, processes for preparing these derivatives, their use for the treatment and/or prevention of diseases and to produce medication for the treatment and/or prevention of diseases, particularly hyperproliferative and/or angiogenic disorders such as cancer disorders, for example. Such treatments can occur as monotherapies or in combination with other medication or further therapeutic measures.
Abstract translation: 本申请涉及通过羧基烷基在N末端被取代的单甲基海洛定蛋白F的新衍生物，用于制备这些衍生物的方法，其用于治疗和/或预防疾病以及产生用于治疗和/或预防 疾病，特别是过度增生和/或血管发生疾病，例如癌症。 这种治疗可以作为单一疗法发生，或与其他药物或其他治疗措施组合发生。
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公开(公告)号：US20130066055A1
公开(公告)日：2013-03-14
申请号：US13451950
申请日：2012-04-20
Applicant: Hans-Georg Lerchen , Lars Linden , Sherif El Sheikh , Jörg Willuda , Charlotte Christine Kopitz , Joachim Schuhmacher , Simone Greven , Christoph Mahlert , Beatrix Stelte-Ludwig , Sven Golfier , Rudolf Beier , Iring Heisler , Axel Harrenga , Karl-Heinz Thierauch , Sandra Bruder , Heike Petrul , Hannah Jörissen , Sandra Borkowski
Inventor： Hans-Georg Lerchen , Lars Linden , Sherif El Sheikh , Jörg Willuda , Charlotte Christine Kopitz , Joachim Schuhmacher , Simone Greven , Christoph Mahlert , Beatrix Stelte-Ludwig , Sven Golfier , Rudolf Beier , Iring Heisler , Axel Harrenga , Karl-Heinz Thierauch , Sandra Bruder , Heike Petrul , Hannah Jörissen , Sandra Borkowski
IPC: C07K17/02
CPC classification number: 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 , C07K5/0205 , C07K5/0207 , C07K5/06 , C07K5/06034 , C07K5/06052 , C07K5/0606 , C07K7/02 , C07K7/06 , C07K16/18 , C07K16/28 , C07K16/2812 , C07K16/2863 , C07K16/30 , C07K2317/21 , C07K2317/24 , C07K2317/565 , C07K2317/76
Abstract: The present application relates to new binder-drug conjugates (ADCs) of N,N-dialkylauristatins that are directed against the target C4.4a, to active metabolites of these ADCs, to processes for preparing these ADCs, to the use of these ADCs for treating and/or preventing illnesses, and also to the use of these ADCs for producing medicaments for treating and/or preventing illnesses, more particularly hyperproliferative and/or angiogenic diseases such as, for example, cancer diseases. Such treatments may be practised as a monotherapy or else in combination with other medicaments or further therapeutic measures.
Abstract translation: 本申请涉及针对目标C4.4a的N，N-二烷基硫酸钠的新粘合剂 - 药物共轭物（ADC），这些ADC的活性代谢物，制备这些ADC的方法，使用这些ADC 治疗和/或预防疾病，以及使用这些ADC用于制备用于治疗和/或预防疾病的药物，更特别是过度增殖和/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来实施，或者与其它药物组合或进一步的治疗措施。
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Patent Agency Ranking
公开(公告)号：US09018258B2
公开(公告)日：2015-04-28
申请号：US13312320
申请日：2011-12-06
Applicant: Thomas Lampe , Michael G. Hahn , Johannes-Peter Stasch , Karl-Heinz Schlemmer , Frank Wunder , Sherif El Sheikh , Volkhart Min-Jian Li , Eva-Maria Becker , Friederike Stoll , Andŕeas Knorr , Peter Kolkhof , Elisabeth Woltering
Inventor： Thomas Lampe , Michael G. Hahn , Johannes-Peter Stasch , Karl-Heinz Schlemmer , Frank Wunder , Sherif El Sheikh , Volkhart Min-Jian Li , Eva-Maria Becker , Friederike Stoll , Andŕeas Knorr , Peter Kolkhof , Elisabeth Woltering
IPC: A61K31/196 , C07C233/55 , C07C231/02 , C07C233/24
CPC classification number: C07C231/02 , A61K31/196 , C07C233/24 , C07C233/55
Abstract: The present application relates to novel substituted 1-benzylcycloalkylcarboxylic acid derivatives, to processes for their preparation, to their use for the treatment and/or prevention of diseases, and to their use for producing medicaments for the treatment and/or prevention of diseases, especially for the treatment and/or prevention of cardiovascular disorders.
Abstract translation: 本申请涉及新的取代的1-苄基环烷基羧酸衍生物，其制备方法，其用于治疗和/或预防疾病的用途及其用于制备用于治疗和/或预防疾病的药物的用途，特别是 用于治疗和/或预防心血管疾病。
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公开(公告)号：US08987209B2
公开(公告)日：2015-03-24
申请号：US13876777
申请日：2011-09-26
Applicant: Hans-Georg Lerchen , Sherif El Sheikh , Beatrix Stelte-Ludwig , Sven Golfier , Joachim Schuhmacher , Jean Mark Gnoth , Ursula Krenz
Inventor： Hans-Georg Lerchen , Sherif El Sheikh , Beatrix Stelte-Ludwig , Sven Golfier , Joachim Schuhmacher , Jean Mark Gnoth , Ursula Krenz
CPC classification number: C07K5/1021 , A61K38/00 , A61K38/07 , A61K38/08 , A61K45/06 , C07K1/1077 , C07K5/0205 , C07K7/02
Abstract: The present application relates to new derivatives of monomethylauristatin F, substituted on the N terminus by a carboxyalkyl group, processes for preparing these derivatives, their use for the treatment and/or prevention of diseases and to produce medication for the treatment and/or prevention of diseases, particularly hyperproliferative and/or angiogenic disorders such as cancer disorders, for example. Such treatments can occur as monotherapies or in combination with other medication or further therapeutic measures.
Abstract translation: 本申请涉及通过羧基烷基在N末端被取代的单甲基海洛定蛋白F的新衍生物，用于制备这些衍生物的方法，其用于治疗和/或预防疾病以及产生用于治疗和/或预防 疾病，特别是过度增生和/或血管发生疾病，例如癌症。 这种治疗可以作为单一疗法发生，或与其他药物或其他治疗措施组合发生。
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公开(公告)号：US20130122024A1
公开(公告)日：2013-05-16
申请号：US13451916
申请日：2012-04-20
Applicant: Hans-Georg LERCHEN , Beatrix STELTE-LUDWIG , Sven GOLFIER , Charlotte Christine KOPITZ , Rudolf BEIER , Sherif EL SHEIKH , Iring HEISLER , Axel HARRENGA , Karl-Heinz THIERAUCH , Joachim SCHUHMACHER , Sandra BRUDER , Simone GREVEN , Lars LINDEN , Jörg WILLUDA , Christoph MAHLERT , Heike PETRUL , Hannah JÖRIßEN , Sandra Borkowski
Inventor： Hans-Georg LERCHEN , Beatrix STELTE-LUDWIG , Sven GOLFIER , Charlotte Christine KOPITZ , Rudolf BEIER , Sherif EL SHEIKH , Iring HEISLER , Axel HARRENGA , Karl-Heinz THIERAUCH , Joachim SCHUHMACHER , Sandra BRUDER , Simone GREVEN , Lars LINDEN , Jörg WILLUDA , Christoph MAHLERT , Heike PETRUL , Hannah JÖRIßEN , Sandra Borkowski
IPC: C07K16/18 , A61K39/395 , A61K45/06 , C07K7/06
CPC classification number: 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 , C07K5/0205 , C07K5/0207 , C07K5/06 , C07K5/06034 , C07K5/06052 , C07K5/0606 , C07K7/02 , C07K7/06 , C07K16/18 , C07K16/28 , C07K16/2812 , C07K16/2863 , C07K16/30 , C07K2317/21 , C07K2317/24 , C07K2317/565 , C07K2317/76
Abstract: The present application relates to new binder-drug conjugates (ADCs) of N,N-dialkylauristatins that are directed against the target mesothelin, to active metabolites of these ADCs, to processes for preparing these ADCs, to the use of these ADCs for treating and/or preventing illnesses, and also to the use of these ADCs for producing medicaments for treating and/or preventing illnesses, more particularly hyperproliferative and/or angiogenic diseases such as, for example, cancer diseases. Such treatments may be practised as a monotherapy or else in combination with other medicaments or further therapeutic measures.
Abstract translation: 本申请涉及针对靶间皮素的N，N-二烷基海马素的新粘合剂 - 药物偶联物（ADC），这些ADC的活性代谢物，制备这些ADC的方法，以及使用这些ADC用于治疗和 /或预防疾病，以及使用这些ADC用于制备用于治疗和/或预防疾病的药物，更特别是过度增殖和/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来实施，或者与其它药物组合或进一步的治疗措施。
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公开(公告)号：US09029406B2
公开(公告)日：2015-05-12
申请号：US14004699
申请日：2012-03-12
Applicant: Hans-Georg Lerchen , Sherif El Sheikh , Beatrix Stelte-Ludwig , Joachim Schuhmacher , Mark Gnoth
Inventor： Hans-Georg Lerchen , Sherif El Sheikh , Beatrix Stelte-Ludwig , Joachim Schuhmacher , Mark Gnoth
IPC: C07D207/333 , C07D413/12 , C07D403/12 , A61K31/4025 , A61K31/4245 , A61K38/07 , C07K5/02 , A61K45/06 , C07K5/103 , A61K38/00 , A61K47/48
CPC classification number: A61K38/07 , A61K38/00 , A61K45/06 , A61K47/6415 , C07K5/0205
Abstract: The present application relates to new derivatives, substituted on the N terminus by a carboxyalkyl group, of monomethylauristatin E and monomethylauristatin F, to processes for preparing these derivatives, to the use of these derivatives for treating and/or preventing diseases, and to the use of these derivatives for producing medicaments for treating and/or preventing diseases, more particularly hyperproliferative and/or angiogenic disorders such as cancer disorders, for example. Such treatments may be applied as a monotherapy or else in combination with other medicaments or further therapeutic measures.
Abstract translation: 本申请涉及在N末端被羧基烷基取代的单甲基海洛定蛋白E和单甲基海洛定蛋白F的新衍生物，用于制备这些衍生物的方法，这些衍生物用于治疗和/或预防疾病的用途和用途 的这些衍生物用于制备用于治疗和/或预防疾病的药物，更具体地是过度增殖和/或血管生成障碍，例如癌症病症。 这样的治疗可以作为单一疗法应用，也可以与其它药物组合使用或其它治疗措施。
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10.发明授权公开(公告)号：US08987256B2
公开(公告)日：2015-03-24
申请号：US12937995
申请日：2009-04-06
Applicant: Michael Hahn , Eva-Maria Becker , Andreas Knorr , Dirk Schneider , Johannes-Peter Stasch , Karl-Heinz Schlemmer , Frank Wunder , Friederike Stoll , Stefan Heitmeier , Klaus Münter , Nils Griebenow , Thomas Lampe , Sherif El Sheikh , Volkhart Min-Jian Li
Inventor： Michael Hahn , Eva-Maria Becker , Andreas Knorr , Dirk Schneider , Johannes-Peter Stasch , Karl-Heinz Schlemmer , Frank Wunder , Friederike Stoll , Stefan Heitmeier , Klaus Münter , Nils Griebenow , Thomas Lampe , Sherif El Sheikh , Volkhart Min-Jian Li
IPC: A61K31/5395 , A61K31/502 , A61K31/4245 , A61K31/53 , C07D237/32 , C07D273/04 , C07D271/113 , C07D253/075 , C07D209/46 , C07D209/48 , C07D213/64 , C07D215/227 , C07D231/56 , C07D233/32 , C07D237/14 , C07D239/88 , C07D253/08 , C07D261/20 , C07D263/20 , C07D275/06 , C07D417/12 , A61K31/421 , A61K31/451 , A61K31/426 , C07D263/22 , C07D211/76 , C07D401/12 , C07D405/12 , C07D277/34 , A61P7/02 , A61P9/12 , A61P3/00 , A61P9/04 , A61P9/10
CPC classification number: C07D237/32 , C07D209/46 , C07D209/48 , C07D211/76 , C07D213/64 , C07D215/227 , C07D231/56 , C07D233/32 , C07D237/14 , C07D239/88 , C07D253/075 , C07D253/08 , C07D261/20 , C07D263/20 , C07D271/113 , C07D273/04 , C07D275/06 , C07D277/34 , C07D417/12
Abstract: The present application relates to novel carboxylic acid derivatives having an oxo-substituted azaheterocyclic partial structure, processes for their preparation, their use for the treatment and/or prophylaxis of diseases, and their use for producing medicaments for the treatment and/or prophylaxis of diseases, especially for the treatment and/or prevention of cardiovascular disorders.
Abstract translation: 本申请涉及具有氧代取代的氮杂环状部分结构的新型羧酸衍生物，其制备方法，其用于治疗和/或预防疾病的用途及其用于治疗和/或预防疾病的药物的用途 ，特别是用于治疗和/或预防心血管疾病。
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