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1. 发明申请

WO2010070047A1 SOLUBLE POLYPEPTIDES FOR USE IN TREATING AUTOIMMUNE AND INFLAMMATORY DISORDERS 审中-公开
标题翻译：用于治疗自身免疫和炎症性疾病的可溶性多聚体
公开(公告)号：WO2010070047A1
公开(公告)日：2010-06-24
申请号：PCT/EP2009/067411
申请日：2009-12-17
申请人： NOVARTIS AG , RAYMOND, Marianne , SARFATI, Marie , WELZENBACH, Karl , WOISETSCHLAEGER, Maximilian
发明人： RAYMOND, Marianne , SARFATI, Marie , WELZENBACH, Karl , WOISETSCHLAEGER, Maximilian
IPC分类号： C07K14/435 , A61K38/17 , C07K14/705 , C12N1/15 , C12N1/21 , C12N5/10 , C12N15/68
CPC分类号： C07K14/4703 , A61K38/00
摘要： The present invention relates to soluble CD47 binding polypeptides, for use as a medicament, in particular for the prevention or treatment of autoimmune and inflammatory disorders, for example allergic asthma and inflammatory bowel diseases. The Invention more specifically relates to a soluble CD47 binding polypeptide for use as a medicament, comprising an extracellular domain of SIRPα (CD172a) or functional derivatives which bind to human CD47.
摘要翻译：本发明涉及用作药物，特别是用于预防或治疗自身免疫性和炎症性疾病，例如过敏性哮喘和炎症性肠病的可溶性CD47结合多肽。本发明更具体地涉及用作药物的可溶性CD47结合多肽，其包含SIRPA（CD172a）的细胞外结构域或与人CD47结合的功能性衍生物。

2. 发明申请

WO2011076781A1 TETRAVALENT CD47-ANTIBODY CONSTANT REGION FUSION PROTEIN FOR USE IN THERAPY 审中-公开
标题翻译：四分之一CD47-抗体恒定区融合蛋白用于治疗
公开(公告)号：WO2011076781A1
公开(公告)日：2011-06-30
申请号：PCT/EP2010/070355
申请日：2010-12-21
申请人： NOVARTIS AG , HUBER, Thomas , KOLBINGER, Frank , SARFATI, Marie , WELZENBACH, Karl
发明人： HUBER, Thomas , KOLBINGER, Frank , SARFATI, Marie , WELZENBACH, Karl
IPC分类号： C07K14/705 , C07K19/00 , C07K16/00 , A61K39/00 , A61P11/06 , A61P29/00 , A61K38/00
CPC分类号： C07K14/70503 , A61K38/00 , C07K14/70596 , C07K2319/30
摘要： The present invention relates to soluble SIRPα binding proteins, for use as a medicament, in particular for the prevention or treatment of autoimmune and inflammatory disorders, for example allergic asthma and inflammatory bowel diseases. The invention more specifically relates to a soluble SIRPα binding protein comprising a complex of two heterodimers, wherein each heterodimer essentially consists of: (i) a first monovalent single chain polypeptide comprising a first SIRPα binding domain fused at the N-terminal part of a heavy chain constant region of an antibody; and, (ii) a second monovalent single chain polypeptide comprising a second SIRPα binding domain fused at the N-terminal part of a CL light chain constant region of an antibody. The invention further relates to soluble SIRPα-binding antibody-like protein as shown in Figure 1.
摘要翻译：本发明涉及用作药物，特别是用于预防或治疗自身免疫性和炎症性疾病，例如过敏性哮喘和炎症性肠病的可溶性SIRPA结合蛋白。本发明更具体地涉及包含两个异二聚体复合物的可溶性SIRPA结合蛋白，其中每个异源二聚体基本上由以下组成：（i）第一单价单链多肽，其包含在沉重的N末端部分融合的第一个SIRPA结合结构域抗体的链恒定区; 和（ii）第二单价单链多肽，其包含在抗体的CL轻链恒定区的N末端部分融合的第二SIRPA结合结构域。本发明还涉及如图1所示的可溶性SIRPA结合抗体样蛋白。

3. 发明申请

WO2012172521A1 SOLUBLE PROTEINS FOR USE AS THERAPEUTICS 审中-公开
标题翻译：可溶性蛋白用作治疗药物
公开(公告)号：WO2012172521A1
公开(公告)日：2012-12-20
申请号：PCT/IB2012/053040
申请日：2012-06-15
申请人： NOVARTIS AG , HUBER, Thomas , KOLBINGER, Frank , WELZENBACH, Karl
发明人： HUBER, Thomas , KOLBINGER, Frank , WELZENBACH, Karl
IPC分类号： C07K19/00 , A61K38/17 , C07K16/24 , C07K16/44 , C07K14/705
CPC分类号： C07K16/2896 , C07K14/70596 , C07K16/241 , C07K16/2803 , C07K16/44 , C07K2317/35 , C07K2317/51 , C07K2317/515 , C07K2317/92 , C07K2319/32
摘要： The present invention relates to improved binding proteins, for use as a medicament, in particular for the prevention or treatment of autoimmune and inflammatory disorders, for example allergic asthma and inflammatory bowel diseases. The invention more specifically relates to a soluble protein, comprising a complex of two heterodimers, wherein each heterodimer essentially consists of: (i) a first single chain polypeptide comprising: (a) an antibody heavy chain sequence having VH, CH1, CH2, and CH3 regions; and (b) a monovalent region of a mammalian binding molecule fused to the VH region; and (ii) a second single chain polypeptide comprising: (c) an antibody light chain sequence having a VL and CL region; and (d) a monovalent region of a mammalian binding molecule fused to the VL region; characterised in that each pair of VH and VL CDR sequences has specificity for an antigen, such that the total valency of said soluble protein is six. The invention further relates to soluble SIRPa-binding antibody-like proteins as shown in Figure 1.
摘要翻译：本发明涉及改进的结合蛋白，用作药物，特别是用于预防或治疗自身免疫性和炎症性疾病，例如过敏性哮喘和炎症性肠病。本发明更具体地涉及包含两个异二聚体复合物的可溶性蛋白质，其中每个异二聚体基本上由以下组成：（i）第一单链多肽，其包含：（a）具有VH，CH1，CH2和 CH3区; 和（b）与VH区融合的哺乳动物结合分子的单价区域; 和（ii）第二单链多肽，其包含：（c）具有VL和CL区的抗体轻链序列; 和（d）与VL区融合的哺乳动物结合分子的单价区域; 其特征在于每对VH和VL CDR序列对抗原具有特异性，使得所述可溶性蛋白的总价为6。本发明还涉及如图1所示的可溶性SIRPA结合抗体样蛋白。

4. 发明申请

WO0228842A3 DIAZACYCLOALKANEDIONE DERIVATIVES WHICH ARE USEFUL AS LFA-1 ANTAGONIST 审中-公开
标题翻译：可用作LFA-1拮抗剂的二氮杂环丁酮衍生物
公开(公告)号：WO0228842A3
公开(公告)日：2002-06-13
申请号：PCT/EP0111342
申请日：2001-10-01
申请人： NOVARTIS AG , NOVARTIS ERFIND VERWALT GMBH , ALBERT RAINER , DAWSON KING JANET , EHRHARDT CLAUS , WATTANASIN SOMPONG , WEITZ SCHMIDT GABRIELE , WELZENBACH KARL
发明人： ALBERT RAINER , DAWSON KING JANET , EHRHARDT CLAUS , WATTANASIN SOMPONG , WEITZ SCHMIDT GABRIELE , WELZENBACH KARL
IPC分类号： A61K31/495 , A61K31/496 , A61K31/4965 , A61K31/551 , A61P17/00 , A61P17/04 , A61P17/06 , A61P19/02 , A61P29/00 , A61P37/02 , A61P37/08 , A61P43/00 , C07D241/08 , C07D243/08 , C07D401/06 , C07D401/10 , C07D401/12
CPC分类号： C07D401/06 , A61K31/4965 , A61K31/551 , C07D241/08 , C07D243/08 , C07D401/12
摘要： Compounds of formula (I) wherein R is carboxy, esterified carboxy or amidated carboxy; R1 and R3 are independently lower alkyl, (hydroxy, lower alkoxy, amino, acylamino, mono- or di- lower alkylamino or mercapto)-lower alkyl, lower alkyl-(thio, sulfinyl or sulfonyl)-lower alkyl, cycloalkyl, aryl, biaryl, (cycloalkyl, aryl or biaryl)-lower alkyl, or (carboxy, esterified carboxy or amidated carboxy)-lower alkyl; R2 is hydrogen, lower alkyl, cycloalkyl, aryl, biaryl, arylaminocarbonyl, or aryl-(oxy, thio or amino); n is 1 or 2; Y is lower-alkylene or lower alkenylene; and pharmaceutically acceptable salts thereof; which are useful as LFA-1 antagonists.
摘要翻译：式（I）的化合物，其中R是羧基，酯化的羧基或酰胺化的羧基; R 1和R 3独立地为低级烷基，（羟基，低级烷氧基，氨基，酰氨基，一或二低级烷基氨基或巯基） - 低级烷基，低级烷基 - （硫代，亚磺酰基或磺酰基） - 低级烷基，环烷基，芳基，（环烷基，芳基或联芳基） - 低级烷基，或（羧基，酯化羧基或酰胺基羧基） - 低级烷基; R2是氢，低级烷基，环烷基，芳基，联芳基，芳基氨基羰基或芳基 - （氧基，硫代或氨基）。 n为1或2; Y是低级亚烷基或低级亚烯基; 及其药学上可接受的盐; 其作为LFA-1拮抗剂是有用的。

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