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1. 发明申请

WO2007009715A1 2-CYANO-PYRIMIDINES AND -TRIAZINES AS CYSTEINE PROTEASE INHIBITORS 审中-公开
标题翻译：作为CYSTEINE PROTEASE INHIBITORS的2-氰基 - 吡啶并 - 吡啶
公开(公告)号：WO2007009715A1
公开(公告)日：2007-01-25
申请号：PCT/EP2006/006999
申请日：2006-07-17
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , FLOHR, Stefanie , FURET, Pascal , IMBACH, Patricia , HOMMEL, Ulrich , LITSCHER, Hans-Ulrich , GIL PARRADO, Shirley , HASSIEPEN, Ulrich , ZIMMERMANN, Johann
发明人： FLOHR, Stefanie , FURET, Pascal , IMBACH, Patricia , HOMMEL, Ulrich , LITSCHER, Hans-Ulrich , GIL PARRADO, Shirley , HASSIEPEN, Ulrich , ZIMMERMANN, Johann
IPC分类号： C07D239/42 , C07D239/34 , A61K31/505 , A61P19/10
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，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。

2. 发明申请

WO2009000878A1 KALLIKREIN 7 MODULATORS 审中-公开
标题翻译： KALLIKREIN 7调音台
公开(公告)号：WO2009000878A1
公开(公告)日：2008-12-31
申请号：PCT/EP2008/058139
申请日：2008-06-26
申请人： NOVARTIS AG , FLOHR, Stefanie , RANDL, Stefan Andreas , OSTERMANN, Nils , HASSIEPEN, Ulrich , BERST, Frederic , BODENDORF, Ursula , GERHARTZ, Bernd , MARZINZIK, Andreas , EHRHARDT, Claus , MEINGASSNER, Josef Gottfried
发明人： FLOHR, Stefanie , RANDL, Stefan Andreas , OSTERMANN, Nils , HASSIEPEN, Ulrich , BERST, Frederic , BODENDORF, Ursula , GERHARTZ, Bernd , MARZINZIK, Andreas , EHRHARDT, Claus , MEINGASSNER, Josef Gottfried
IPC分类号： C07K14/47 , C07K14/435 , C07D207/16 , C07D209/42 , C07D209/52 , C07D211/60 , C07D401/12 , C07D405/12 , A61K31/401 , A61K31/4025 , A61K31/403 , A61K31/4035 , A61K31/4439 , A61K31/496
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。

3. 发明申请

WO2009068531A2 ORGANIC COMPOUNDS 审中-公开
标题翻译：有机化合物
公开(公告)号：WO2009068531A2
公开(公告)日：2009-06-04
申请号：PCT/EP2008/066159
申请日：2008-11-25
申请人： NOVARTIS AG , HASSIEPEN, Ulrich , KITTELMANN, Matthias
发明人： HASSIEPEN, Ulrich , KITTELMANN, Matthias
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 (formula) and R" represents hydrogen, hydroxy, C 1 -C 7 alkoxy, C 1 -C 8 -alkanoyloxy, or R 5 R 4 N-CO-O-, where R 4 and R 5 independently are C 1 -C 7 alkyl or phenyl which is unsubstituted or substituted by a substitutent selected from C 1 -C 7 alkyl, C 1 -C 7 alkoxy, halogen and trifluoromethyl and where R 4 additionally is hydrogen; or R 4 and R 5 together represent C 3 -C 6 alkylene; 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（式），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 1-4烷氧基，卤素和三氟甲基，R4另外是氢;或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形式，式（IA），（IB），（XA），（XB），（YA）或（YB）抑制DPP-IV（二肽基肽酶-IV）活性，因此它们被用作抑制DPP-IV的药物和用于DPP-IV介导的病症的治疗，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。

4. 发明申请

WO2016207858A1 FACTOR XI ANTIBODIES AND METHODS OF USE 审中-公开
标题翻译：因素XI抗体和使用方法
公开(公告)号：WO2016207858A1
公开(公告)日：2016-12-29
申请号：PCT/IB2016/053790
申请日：2016-06-24
申请人： NOVARTIS AG , EDER, Jorg , EWERT, Stefan , HASSIEPEN, Ulrich , KHDER, Yasser , MAYR, Lorenz M. , MELKKO, Samu , SCHIERING, Nikolaus
发明人： EDER, Jorg , EWERT, Stefan , HASSIEPEN, Ulrich , KHDER, Yasser , MAYR, Lorenz M. , MELKKO, Samu , SCHIERING, Nikolaus
IPC分类号： C07K16/36
CPC分类号： C07K16/40 , A61K2039/505 , C07K16/36 , 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.
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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