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公开(公告)号：US20180355056A1
公开(公告)日：2018-12-13
申请号：US15739414
申请日：2016-06-24
申请人： Jorg EDER , Stefan EWERT , Ulrich HASSIEPEN , Yasser KHDER , Lorenz MAYR , Samu MELKKO , Nikolaus SCHIERING
发明人： Jorg EDER , Stefan EWERT , Ulrich HASSIEPEN , Yasser KHDER , Lorenz MAYR , Samu MELKKO , Nikolaus SCHIERING
IPC分类号： C07K16/36 , C07K16/40 , A61K45/06 , A61K39/395 , A61P7/02
CPC分类号： C07K16/36 , A61K39/3955 , A61K45/06 , A61K2039/505 , A61P7/02 , C07K16/40 , C07K2317/21 , C07K2317/33 , C07K2317/34 , C07K2317/55 , C07K2317/56 , C07K2317/565 , C07K2317/76 , C07K2317/92
摘要： The present invention relates to monoclonal antibodies and antigen binding fragments thereof that bind to human Factor XI and activated Factor XI (“Factor XIa”), and pharmaceutical compositions and methods of treatment comprising the same.
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2.发明申请公开(公告)号：US20080214548A1
公开(公告)日：2008-09-04
申请号：US11995994
申请日：2006-07-17
申请人： Stefanie Flohr , Pascal Furet , Patricia Imabach , Ulrich Hommel , Hans-Ulrich litscher , Shirley Gil Parrado , Ulrich Hassiepen , Johann Zimmermann
发明人： Stefanie Flohr , Pascal Furet , Patricia Imabach , Ulrich Hommel , Hans-Ulrich litscher , Shirley Gil Parrado , Ulrich Hassiepen , Johann Zimmermann
IPC分类号： A61K31/53 , C07D251/14 , A61K31/505 , A61P35/04 , C07D239/28
CPC分类号： C07D239/34 , C07D239/42
摘要： The invention relates to compounds of the formula I and salts thereof, to a process for their manufacture, to their use in the treatment of (especially cysteine protease, such as UCH-L3- and/or USP-2 dependent) diseases or for the manufacture of pharmaceutical formulations against these diseases, methods of treatment of warm-blooded animals comprising administering the compounds and/or their salts to said animals and pharmaceutical preparations, especially for the treatment of the diseases, comprising said compounds and/or salts.
摘要翻译： 本发明涉及式I化合物及其盐，其制备方法，用于治疗（特别是半胱氨酸蛋白酶，例如UCH-L3-和/或USP-2依赖性）疾病或用于 制备针对这些疾病的药物制剂，治疗温血动物的方法包括向所述动物和药物制剂施用化合物和/或其盐，特别是用于治疗包含所述化合物和/或盐的疾病。
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公开(公告)号：US20170022292A1
公开(公告)日：2017-01-26
申请号：US15192020
申请日：2016-06-24
申请人： Jorg EDER , Stefan EWERT , Ulrich HASSIEPEN , Yasser KHDER , Lorenz MAYR , Samu MELKKO , Nikolaus SCHIERING
发明人： Jorg EDER , Stefan EWERT , Ulrich HASSIEPEN , Yasser KHDER , Lorenz MAYR , Samu MELKKO , Nikolaus SCHIERING
IPC分类号： C07K16/40
摘要： The present invention relates to monoclonal antibodies and antigen binding fragments thereof that bind to human Factor XI and activated Factor XI (“Factor XIa”), and pharmaceutical compositions and methods of treatment comprising the same.
摘要翻译： 本发明涉及结合人因子XI和活化因子XI（“因子XIa”）的单克隆抗体及其抗原结合片段，以及包含其的药物组合物和治疗方法。
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4.发明授权公开(公告)号：US07700605B2
公开(公告)日：2010-04-20
申请号：US11995994
申请日：2006-07-17
申请人： Stefanie Flohr , Pascal Furet , Patricia Imbach , Ulrich Hommel , Hans-Ulrich Litshcer , Shirley Gil Parrado , Ulrich Hassiepen , Johann Zimmermann
发明人： Stefanie Flohr , Pascal Furet , Patricia Imbach , Ulrich Hommel , Hans-Ulrich Litshcer , Shirley Gil Parrado , Ulrich Hassiepen , Johann Zimmermann
IPC分类号： C07D239/34 , C07D239/42 , C07D239/46 , C07D239/48 , A61K31/505 , A61P35/00 , C07D251/14 , C07D251/42 , C07D251/48 , A61K31/53
CPC分类号： C07D239/34 , C07D239/42
摘要： The invention relates to compounds of the formula I and salts thereof, to a process for their manufacture, to their use in the treatment of (especially cysteine protease, such as UCH-L3- and/or USP-2 dependent) diseases or for the manufacture of pharmaceutical formulations against these diseases, methods of treatment of warm-blooded animals comprising administering the compounds and/or their salts to said animals and pharmaceutical preparations, especially for the treatment of the diseases, comprising said compounds and/or salts.
摘要翻译： 本发明涉及式I化合物及其盐，其制备方法，用于治疗（特别是半胱氨酸蛋白酶，例如UCH-L3-和/或USP-2依赖性）疾病或用于 制备针对这些疾病的药物制剂，治疗温血动物的方法包括向所述动物和药物制剂施用化合物和/或其盐，特别是用于治疗包含所述化合物和/或盐的疾病。
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公开(公告)号：US20120295860A1
公开(公告)日：2012-11-22
申请号：US13560421
申请日：2012-07-27
IPC分类号： A61K31/7056 , A61P3/10 , C07H17/02
CPC分类号： C07H15/26 , B41J2/17593
摘要： The present invention relates to a compound The instant invention relates to a compound of formulae (I A), (I B), (X A), (X B), (Y A) or (Y B),wherein R′ represents and R″ represents hydrogen, hydroxy, C1-C7alkoxy, C1-C8-alkanoyloxy, or R5R4N—CO—O—, where R4 and R5 independently are C1-C7alkyl or phenyl which is unsubstituted or substituted by a substitutent selected from C1-C7alkyl, C1-C7alkoxy, halogen and trifluoromethyl and where R4 additionally is hydrogen; or R4 and R5 together represent C3-C6alkylene, in free form or in form of a pharmaceutically acceptable acid addition salt. Compounds of formulae (I A), (I B), (X A), (X B), (Y A) or (Y B) inhibit DPP-IV (dipeptidyl-peptidase-IV) activity. They are therefore indicated for use as pharmaceuticals in inhibiting DPP-IV and in the treatment of conditions mediated by DPP-IV, such as non-insulin-dependent diabetes mellitus, arthritis, obesity, osteoporosis and further conditions of impaired glucose tolerance.
摘要翻译： 本发明涉及化合物本发明涉及式（IA），（IB），（XA），（XB），（YA）或（YB）的化合物，其中R'表示并且R“表示氢， 羟基，C 1 -C 7烷氧基，C 1 -C 8 - 烷酰氧基或R 5 R 4 N-CO-O-，其中R 4和R 5独立地是C 1 -C 7烷基或未被取代或被选自C 1 -C 7烷基，C 1 -C 7烷氧基，卤素 和三氟甲基，其中R4另外是氢; 或R4和R5一起表示游离形式或药学上可接受的酸加成盐形式的C 3 -C 6亚烷基。 式（I A），（I B），（X A），（X B），（Y A）或（Y B）的化合物抑制DPP-IV（二肽基肽酶-IV）活性。 因此，它们被指示用作抑制DPP-IV的药物和用于治疗由DPP-IV介导的病症，例如非胰岛素依赖性糖尿病，关节炎，肥胖症，骨质疏松症和葡萄糖耐量降低的其它病症。
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公开(公告)号：US08252751B2
公开(公告)日：2012-08-28
申请号：US12744510
申请日：2008-11-25
IPC分类号： C07H15/24 , A61K31/7036 , A61P3/10
CPC分类号： C07H15/26 , B41J2/17593
摘要： The present invention relates to a compound The instant invention relates to a compound of formulae (I A), (I B), (X A), (X B), (Y A) or (Y B), wherein R′ represents and R″ represents hydrogen, hydroxy, C1-C7alkoxy, C1-C8-alkanoyloxy, or R5R4N—CO—O—, where R4 and R5 independently are C1-C7alkyl or phenyl which is unsubstituted or substituted by a substitutent selected from C1-C7alkyl, C1-C7alkoxy, halogen and trifluoromethyl and where R4 additionally is hydrogen; or R4 and R5 together represent C3-C6alkylene; in free form or in form of a pharmaceutically acceptable acid addition salt. Compounds of formulae (I A), (I B), (X A), (X B), (Y A) or (Y B) inhibit DPP-IV (dipeptidyl-peptidase-IV) activity. They are therefore indicated for use as pharmaceuticals in inhibiting DPP-IV and in the treatment of conditions mediated by DPP-IV, such as non-insulin-dependent diabetes mellitus, arthritis, obesity, osteoporosis and further conditions of impaired glucose tolerance.
摘要翻译： 本发明涉及化合物本发明涉及式（IA），（IB），（XA），（XB），（YA）或（YB）的化合物，其中R'表示并且R“表示氢， 羟基，C 1 -C 7烷氧基，C 1 -C 8 - 烷酰氧基或R 5 R 4 N-CO-O-，其中R 4和R 5独立地是C 1 -C 7烷基或未被取代或被选自C 1 -C 7烷基，C 1 -C 7烷氧基，卤素 和三氟甲基，其中R4另外是氢; 或者R 4和R 5一起代表C 3 -C 6亚烷基; 游离形式或药学上可接受的酸加成盐的形式。 式（I A），（I B），（X A），（X B），（Y A）或（Y B）的化合物抑制DPP-IV（二肽基肽酶-IV）活性。 因此，它们被指示用作抑制DPP-IV的药物和用于治疗由DPP-IV介导的病症，例如非胰岛素依赖性糖尿病，关节炎，肥胖症，骨质疏松症和葡萄糖耐量降低的其它病症。
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公开(公告)号：US20100256144A1
公开(公告)日：2010-10-07
申请号：US12665892
申请日：2008-06-26
申请人： Stefanie Flohr , Stefan Andreas Randl , Nils Ostermann , Ulrich Hassiepen , Frederic Berst , Ursula Bodendorf , Bernd Gerhartz , Adreas Marzinzik , Claus Ehrhardt , Josef Gottfried Meingassner
发明人： Stefanie Flohr , Stefan Andreas Randl , Nils Ostermann , Ulrich Hassiepen , Frederic Berst , Ursula Bodendorf , Bernd Gerhartz , Adreas Marzinzik , Claus Ehrhardt , Josef Gottfried Meingassner
IPC分类号： A61K31/4439 , C07D401/12 , C07D207/16 , A61K31/40 , A61K31/454 , C07D403/12 , A61K31/496 , C07D413/12 , A61K31/5377 , A61K31/4545 , C07D217/26 , A61K31/472 , C07D211/60 , A61K31/445 , C07D409/12 , A61K31/4025 , A61P17/10 , A61P17/00 , A61P17/02 , A61P17/06 , A61P17/04 , A61P35/00 , A61P29/00 , C12N9/48 , G01N33/573
CPC分类号： A61K31/401 , A61K31/4025 , A61K31/403 , A61K31/4035 , A61K31/404 , A61K31/4439 , A61K31/4545 , A61K31/496 , C07D207/16 , C07D209/42 , C07D209/52 , C07D211/60 , C07D401/12 , C07D405/12 , C07K2299/00 , C12N9/6445 , C12Y304/21034
摘要： The present invention relates to the crystal structure of the serine protease kallikrein 7 and to the use of this crystal structure in drug discovery. The present invention also relates to compounds binding specifically to this active site of kallikrein 7.
摘要翻译： 本发明涉及丝氨酸蛋白酶激肽释放酶7的晶体结构以及这种晶体结构在药物发现中的应用。 本发明还涉及特异性结合激素释放酶7的该活性位点的化合物。
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公开(公告)号：US08569250B2
公开(公告)日：2013-10-29
申请号：US13560421
申请日：2012-07-27
IPC分类号： A61K31/7036 , A61P3/10
CPC分类号： C07H15/26 , B41J2/17593
摘要： A method of inhibiting dipeptidyl peptidase-IV comprising administering to a mammal in need of such treatment a therapeutically effective amount of a compound of formulae (I A), (I B), (X A), (X B), (Y A) or (Y or B),wherein R′ represents and R″ represents hydrogen, hydroxy, C1-C7alkoxy, C1-C8-alkanoyloxy, or R5R4N—CO—O—, where R4 and R5 independently are C1-C7alkyl or phenyl which is unsubstituted or substituted by a substitutent selected from C1-C7alkyl, C1-C7alkoxy, halogen and trifluoromethyl and where R4 additionally is hydrogen; or R4 and R5 together represent C3-C6alkylene, in free form or in form of a pharmaceutically acceptable acid addition salt.
摘要翻译： 抑制二肽基肽酶-IV的方法包括向需要这种治疗的哺乳动物施用治疗有效量的式（IA），（IB），（XA），（XB），（YA）或（Y或 B），其中R'表示并且R“表示氢，羟基，C 1 -C 7烷氧基，C 1 -C 8 - 烷酰氧基或R 5 R 4 N-CO-O-，其中R 4和R 5独立地是C 1 -C 7烷基或未被取代或取代的苯基 通过选自C 1 -C 7烷基，C 1 -C 7烷氧基，卤素和三氟甲基的取代基，并且其中R 4另外是氢; 或R4和R5一起表示游离形式或药学上可接受的酸加成盐形式的C 3 -C 6亚烷基。
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公开(公告)号：US08309596B2
公开(公告)日：2012-11-13
申请号：US12665892
申请日：2008-06-26
申请人： Stefanie Flohr , Stefan Andreas Randl , Nils Ostermann , Ulrich Hassiepen , Frederic Berst , Ursula Bodendorf , Bernd Gerhartz , Andreas Marzinzik , Claus Ehrhardt , Josef Gottfried Meingassner
发明人： Stefanie Flohr , Stefan Andreas Randl , Nils Ostermann , Ulrich Hassiepen , Frederic Berst , Ursula Bodendorf , Bernd Gerhartz , Andreas Marzinzik , Claus Ehrhardt , Josef Gottfried Meingassner
IPC分类号： A61K31/5377 , A61K31/496 , A61K31/454 , A61K31/437 , A61K31/4375 , A61K31/404 , A61K31/4035 , A61K31/403 , A61K31/4025 , A61K31/40 , C07D413/12 , C07D409/12 , C07D405/12 , C07D401/12 , C07D403/12 , C07D217/26 , C07D211/60 , C07D209/42 , C07D209/44 , C07D209/52 , C07D207/16
CPC分类号： A61K31/401 , A61K31/4025 , A61K31/403 , A61K31/4035 , A61K31/404 , A61K31/4439 , A61K31/4545 , A61K31/496 , C07D207/16 , C07D209/42 , C07D209/52 , C07D211/60 , C07D401/12 , C07D405/12 , C07K2299/00 , C12N9/6445 , C12Y304/21034
摘要： The present invention relates to the crystal structure of the serine protease kallikrein 7 and to the use of this crystal structure in drug discovery. The present invention also relates to compounds binding specifically to this active site of kallikrein 7.
摘要翻译： 本发明涉及丝氨酸蛋白酶激肽释放酶7的晶体结构以及这种晶体结构在药物发现中的应用。 本发明还涉及特异性结合激素释放酶7的该活性位点的化合物。
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公开(公告)号：US20100256080A1
公开(公告)日：2010-10-07
申请号：US12744510
申请日：2008-11-25
CPC分类号： C07H15/26 , B41J2/17593
摘要： The present invention relates to a compound The instant invention relates to a compound of formulae (I A), (I B), (X A), (X B), (Y A) or (Y B), wherein R′ represents and R″ represents hydrogen, hydroxy, C1-C7alkoxy, C1-C8-alkanoyloxy, or R5R4N—CO—O—, where R4 and R5 independently are C1-C7alkyl or phenyl which is unsubstituted or substituted by a substitutent selected from C1-C7alkyl, C1-C7alkoxy, halogen and trifluoromethyl and where R4 additionally is hydrogen; or R4 and R5 together represent C3-C6alkylene; in free form or in form of a pharmaceutically acceptable acid addition salt. Compounds of formulae (I A), (I B), (X A), (X B), (Y A) or (Y B) inhibit DPP-IV (dipeptidyl-peptidase-IV) activity. They are therefore indicated for use as pharmaceuticals in inhibiting DPP-IV and in the treatment of conditions mediated by DPP-IV, such as non-insulin-dependent diabetes mellitus, arthritis, obesity, osteoporosis and further conditions of impaired glucose tolerance.
摘要翻译： 本发明涉及化合物本发明涉及式（IA），（IB），（XA），（XB），（YA）或（YB）的化合物，其中R'表示并且R“表示氢， 羟基，C 1 -C 7烷氧基，C 1 -C 8 - 烷酰氧基或R 5 R 4 N-CO-O-，其中R 4和R 5独立地是C 1 -C 7烷基或未被取代或被选自C 1 -C 7烷基，C 1 -C 7烷氧基，卤素 和三氟甲基，其中R4另外是氢; 或者R 4和R 5一起代表C 3 -C 6亚烷基; 游离形式或药学上可接受的酸加成盐的形式。 式（I A），（I B），（X A），（X B），（Y A）或（Y B）的化合物抑制DPP-IV（二肽基肽酶-IV）活性。 因此，它们被指示用作抑制DPP-IV的药物和用于治疗由DPP-IV介导的病症，例如非胰岛素依赖性糖尿病，关节炎，肥胖症，骨质疏松症和葡萄糖耐量降低的其它病症。
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