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1. 发明授权

EP1487805B1 PYRIMIDINE DERIVATIVES 有权转让
标题翻译：嘧啶衍生物
公开(公告)号：EP1487805B1
公开(公告)日：2012-07-04
申请号：EP03744366.0
申请日：2003-03-14
申请人： Novartis AG , Novartis Pharma GmbH
发明人： BAENTELI, Rolf , ZENKE, Gerhard , COOKE, Nigel, Graham , DUTHALER, Rudolf , THOMA, Gebhard , VON MATT, Anette , HONDA, Toshiyuki , MATSUURA, Naoko , NONOMURA, Kazuhiko , OHMORI, Osamu , UMEMURA, Ichiro , HINTERDING, Klaus , PAPAGEORGIOU, Christos
IPC分类号： C07D239/48 , A61K31/505 , A61P35/04
CPC分类号： C07D239/48 , A61K31/505 , A61K31/506 , A61K31/5377 , A61K31/55 , A61K45/06 , C07D231/12 , C07D233/56 , C07D249/08 , C07D401/12 , C07D401/14 , C07D403/12 , C07D417/12
摘要： There are provided compounds of formula (I), wherein X, R1, R2, R3, R4, R5, R6, R7, R8 and R9 are as indicated in claim 1, useful in disorders where ZAP-70 and/or Syk inhibition plays a role or caused by a malfunction of signal cascades connected with FAK.

2. 发明公开

EP1546315A1 ATOMIC STRUCTURE OF THE CATALYTIC DOMAIN FOR USE IN DESIGNING AND IDENTIFYING INHIBITORS OF ZAP-70 KINASE 审中-公开
标题翻译：设计与鉴定ZAP-70激酶抑制剂的催化结构域原子结构
公开(公告)号：EP1546315A1
公开(公告)日：2005-06-29
申请号：EP03750632.6
申请日：2003-09-25
申请人： Novartis AG , Novartis Pharma GmbH
发明人： GEISER, Martin , GEISSE, Sabine , OSTERMEIER, Christian , RAMAGE, Paul , RAULF, Friedrich , ZENKE, Gerhard
IPC分类号： C12N9/12 , G01N23/20 , G01N33/573
CPC分类号： C12N9/12 , A61K38/00 , C07K2299/00 , C12N9/1205
摘要： The present invention relates to the three dimensional structure of ZAP-70 protein tyrosine kinase and describes methods of making a crystal of ZAP-70 and purification of the catalytic domain of ZAP-70 for use in crystallisation. The invention also relates to the use of the three dimensional structure of the catalytic domain of ZAP-70 for identifying and designing ligands which inhibit the biological function of ZAP-70.

3. 发明公开

EP1337527A1 INDOLYLMALEIMIDE DERIVATIVES AS PROTEIN KINASE C INHIBITORS 有权
标题翻译： INDOLYLMALEIMIDDERIVATIVE AS蛋白激酶C抑制剂
公开(公告)号：EP1337527A1
公开(公告)日：2003-08-27
申请号：EP01993604.6
申请日：2001-11-05
申请人： Novartis AG , Novartis Pharma GmbH
发明人： ALBERT, Rainer , COOKE, Nigel, Graham , COTTENS, Sylvain , EHRHARDT, Claus , EVENOU, Jean-Pierre , SEDRANI, Richard , VON MATT, Peter , WAGNER, Jürgen , ZENKE, Gerhard
IPC分类号： C07D403/04 , C07D403/14 , A61K31/404 , A61P29/00 , A61P37/06
CPC分类号： C07D403/14 , A61K45/06 , C07D231/12 , C07D233/56 , C07D249/08 , C07D401/14 , C07D403/04 , C07D471/10
摘要： Indolylmaleimide derivatives comprising either a substituted phenyl, naphthyl, tetrahydronaphthyl, quinazolinyl, quinolyl, isoquinolyl or pyrimidinyl residue have interesting pharmaceutical properties, e.g. in the treatment and/or prevention of T-cell mediated acute or chronic inflammatory diseases or disorders, autoimmune diseases, graft rejection or cancer.

4. 发明授权

EP1490355B1 INDOLYLMALEIMIDE DERIVATIVES 有权转让
标题翻译： INDOLYLMALEIMID衍生物
公开(公告)号：EP1490355B1
公开(公告)日：2011-07-27
申请号：EP03720413.8
申请日：2003-04-02
申请人： Novartis AG , Novartis Pharma GmbH
发明人： EVENOU, Jean-Pierre , VON MATT, Peter , WAGNER, Jürgen , ZENKE, Gerhard
IPC分类号： C07D403/04 , C07D403/14 , C07D401/14 , A61K31/404 , A61K31/4709 , A61K31/4725 , A61P29/00 , A61P37/00
CPC分类号： A61K31/496 , C07D401/14 , C07D403/04 , C07D403/14
摘要： Provided are compounds of Formula (I), which are useful in the treatment and/or prevention of diseases or disorders mediated by T lymphocytes and/or PKC, e.g. acute or chronic rejection of organ or tissue allo- or xenografts, graft versus host diseases, atherosclerosis, vascular occlusion due to vascular injury such as angioplasty, restenosis, obesity, syndrome X, impaired glucose tolerance, polycystic ovary syndrome, hypertension, heart failure, chronic obstructive pulmonary disease, CNS diseases such as Alzheimer disease or amyotrophic lateral sclerosis, cancer, infectious diseases such as AIDS, septic shock or adult respiratory distress syndrome, ischemia/reperfusion injury e.g. myocardial infraction, stroke, gut ischemia, renal failure or hemorrhage shock, or traumatic shock, e.g. traumatic brain injury. The compounds of (I) are also useful in the treatment and/or prevention of T-cell mediated acute or chronic inflammatory diseases or disorders or autoimmune diseases e.g. rheumatoid arthritis, osteoarthritis, systemic lupus erythematosus, Hashimoto’s thyroidis, multiple sclerosis, myasthenia gravis, diabetes type I or II and the disorders associated therewith, e.g. angiopathy, diabetic proliferative retinopathy, diabetic macular edema, nephropathy, neuropathy and dawn phenomenon, respiratory diseases such as asthma or inflammatory lung injury, inflammatory liver injury, inflammatory glomerular injury, cutaneous manifestations of immunologically-mediated disorders or illnesses, inflammatory and hyperproliferative skin diseases (such as psoriasis, atopic dermatitis, allergic contact dermatitis, irritant contact dermatitis and further eczematous dermatitises, seborrhoeic dermatitis), inflammatory eye diseases, e.g. Sjoegren’s syndrome, keratoconjunctivitis or uveitis, inflammatory bowel disease, Crohn’s disease or ulcerative colitis.

5. 发明授权

EP1664035B1 2,4 DI(HETERO)-ARYLAMINO-PYRIMIDINE DERIVATIVES AS ZAP-70 AND/OR SYK INHIBITORS 有权
标题翻译：作为ZAP-70和/或SYK抑制剂的2,4-二（HETERO） - 芳基氨基 - 嘧啶衍生物
公开(公告)号：EP1664035B1
公开(公告)日：2011-02-16
申请号：EP04786952.4
申请日：2004-09-15
申请人： Novartis AG , Novartis Pharma GmbH
发明人： BAENTELI, Rolf , BERNHARD, Marie, Claude , BUEHLMAYER, Peter , COOKE, Nigel, Graham , DUTHALER, Rudolf , HINTERDING, Klaus , THOMA, Gebhard , VAN EIS, Maurice , VON MATT, Anette , WALLISER, Louis , ZENKE, Gerhard
IPC分类号： C07D405/12 , C07D239/48 , C07D405/14 , C07D413/14 , C07D417/14 , C07D403/12 , A61K31/506
CPC分类号： C07D239/48 , C07D403/12 , C07D405/12 , C07D405/14 , C07D413/14 , C07D417/14 , Y02P20/582
摘要： Disclosed are pyrimidine derivatives of formula (I); wherein R0, R1, R3 to R9, and Z have a signification as indicated in claim 1, which have ZAP-70 and/or Syk inhibitory activities.
摘要翻译：公开了式（I）的嘧啶衍生物; 其中R0，R1，R3至R9和Z具有如权利要求1所述的含义，其具有ZAP-70和/或Syk抑制活性。

6. 发明授权

EP1337527B1 INDOLYLMALEIMIDE DERIVATIVES AS PROTEIN KINASE C INHIBITORS 有权
标题翻译：作为蛋白激酶C抑制剂的吲哚基马来酰亚胺衍生物
公开(公告)号：EP1337527B1
公开(公告)日：2009-10-14
申请号：EP01993604.6
申请日：2001-11-05
申请人： Novartis AG , Novartis Pharma GmbH
发明人： ALBERT, Rainer , COOKE, Nigel, Graham , COTTENS, Sylvain , EHRHARDT, Claus , EVENOU, Jean-Pierre , SEDRANI, Richard , VON MATT, Peter , WAGNER, Jürgen , ZENKE, Gerhard
IPC分类号： C07D403/04 , C07D403/14 , A61K31/404 , A61P29/00 , A61P37/06
CPC分类号： C07D403/14 , A61K45/06 , C07D231/12 , C07D233/56 , C07D249/08 , C07D401/14 , C07D403/04 , C07D471/10
摘要： Indolylmaleimide derivatives comprising either a substituted phenyl, naphthyl, tetrahydronaphthyl, quinazolinyl, quinolyl, isoquinolyl or pyrimidinyl residue have interesting pharmaceutical properties, e.g. in the treatment and/or prevention of T-cell mediated acute or chronic inflammatory diseases or disorders, autoimmune diseases, graft rejection or cancer.
摘要翻译：包含取代的苯基，萘基，四氢萘基，喹唑啉基，喹啉基，异喹啉基或嘧啶基残基的吲哚基马来酰亚胺衍生物具有令人感兴趣的药学性质，用于治疗和/或预防T细胞介导的急性或慢性炎性疾病或病症，自身免疫性疾病，移植排斥或癌症。

7. 发明公开

EP1664035A1 2,4 DI (HETERO) -ARYLAMINO-PYRIMIDINE DERIVATIVES AS ZAP-70 AND/OR SYK INHIBITORS 有权
标题翻译：作为ZAP-70和/或SYK抑制剂的2,4-二（HETERO） - 芳基氨基 - 嘧啶衍生物
公开(公告)号：EP1664035A1
公开(公告)日：2006-06-07
申请号：EP04786952.4
申请日：2004-09-15
申请人： Novartis AG , Novartis Pharma GmbH
发明人： BAENTELI, Rolf , BERNHARD, Marie, Claude , BUEHLMAYER, Peter , COOKE, Nigel, Graham , DUTHALER, Rudolf , HINTERDING, Klaus , THOMA, Gebhard , VAN EIS, Maurice , VON MATT, Anette , WALLISER, Louis , ZENKE, Gerhard
IPC分类号： C07D405/12 , C07D239/48 , C07D405/14 , C07D413/14 , C07D417/14 , C07D403/12 , A61K31/506
CPC分类号： C07D239/48 , C07D403/12 , C07D405/12 , C07D405/14 , C07D413/14 , C07D417/14 , Y02P20/582
摘要： Disclosed are pyrimidine derivatives of formula (I); wherein R0, R1, R3 to R9, and Z have a signification as indicated in claim 1, which have ZAP-70 and/or Syk inhibitory activities.
摘要翻译：公开了式（I）的嘧啶衍生物; 其中R0，R1，R3至R9和Z具有如权利要求1所述的含义，其具有ZAP-70和/或Syk抑制活性。

8. 发明公开

EP1490355A1 INDOLYLMALEIMIDE DERIVATIVES 有权转让
标题翻译：吲哚基马来酰亚胺衍生物
公开(公告)号：EP1490355A1
公开(公告)日：2004-12-29
申请号：EP03720413.8
申请日：2003-04-02
申请人： Novartis AG , Novartis Pharma GmbH
发明人： EVENOU, Jean-Pierre , VON MATT, Peter , WAGNER, Jürgen , ZENKE, Gerhard
IPC分类号： C07D403/04 , C07D403/14 , C07D401/14 , A61K31/404 , A61K31/4709 , A61K31/4725 , A61P29/00 , A61P37/00
CPC分类号： A61K31/496 , C07D401/14 , C07D403/04 , C07D403/14
摘要： Provided are compounds of Formula (I), which are useful in the treatment and/or prevention of diseases or disorders mediated by T lymphocytes and/or PKC, e.g. acute or chronic rejection of organ or tissue allo- or xenografts, graft versus host diseases, atherosclerosis, vascular occlusion due to vascular injury such as angioplasty, restenosis, obesity, syndrome X, impaired glucose tolerance, polycystic ovary syndrome, hypertension, heart failure, chronic obstructive pulmonary disease, CNS diseases such as Alzheimer disease or amyotrophic lateral sclerosis, cancer, infectious diseases such as AIDS, septic shock or adult respiratory distress syndrome, ischemia/reperfusion injury e.g. myocardial infraction, stroke, gut ischemia, renal failure or hemorrhage shock, or traumatic shock, e.g. traumatic brain injury. The compounds of (I) are also useful in the treatment and/or prevention of T-cell mediated acute or chronic inflammatory diseases or disorders or autoimmune diseases e.g. rheumatoid arthritis, osteoarthritis, systemic lupus erythematosus, Hashimoto’s thyroidis, multiple sclerosis, myasthenia gravis, diabetes type I or II and the disorders associated therewith, e.g. angiopathy, diabetic proliferative retinopathy, diabetic macular edema, nephropathy, neuropathy and dawn phenomenon, respiratory diseases such as asthma or inflammatory lung injury, inflammatory liver injury, inflammatory glomerular injury, cutaneous manifestations of immunologically-mediated disorders or illnesses, inflammatory and hyperproliferative skin diseases (such as psoriasis, atopic dermatitis, allergic contact dermatitis, irritant contact dermatitis and further eczematous dermatitises, seborrhoeic dermatitis), inflammatory eye diseases, e.g. Sjoegren’s syndrome, keratoconjunctivitis or uveitis, inflammatory bowel disease, Crohn’s disease or ulcerative colitis.
摘要翻译：提供了可用于治疗和/或预防由T淋巴细胞和/或PKC介导的疾病或病症的式（I）化合物，器官或组织异体或异种移植物的急性或慢性排斥，移植物抗宿主疾病，动脉粥样硬化，血管损伤引起的血管闭塞如血管成形术，再狭窄，肥胖症，X综合征，葡萄糖耐量降低，多囊卵巢综合征，高血压，心力衰竭，慢性阻塞性肺病，CNS疾病如阿尔茨海默病或肌萎缩侧索硬化，癌症，感染性疾病如AIDS，脓毒性休克或成人呼吸窘迫综合征，缺血/再灌注损伤例如心肌梗塞，中风，肠缺血，肾衰或出血性休克或创伤性休克，创伤性脑损伤。（I）的化合物还可用于治疗和/或预防T细胞介导的急性或慢性炎性疾病或病症或自身免疫性疾病，例如类风湿性关节炎，骨关节炎，系统性红斑狼疮，桥本氏甲状腺炎，多发性硬化症，重症肌无力，I型或II型糖尿病和与其相关的病症，血管病，糖尿病增殖性视网膜病，糖尿病黄斑水肿，肾病，神经病和黎明现象，呼吸疾病如哮喘或炎症性肺损伤，炎性肝损伤，炎性肾小球损伤，免疫介导的病症或疾病的皮肤表现，炎性和过度增殖性皮肤病（如牛皮癣，特应性皮炎，过敏性接触性皮炎，刺激性接触性皮炎和进一步的湿疹性皮炎，脂溢性皮炎），炎症性眼病如舍霍格综合征，角膜结膜炎或葡萄膜炎，炎性肠病，克罗恩病或溃疡性结肠炎。

9. 发明公开

EP1487805A1 PYRIMIDINE DERIVATIVES 有权转让
标题翻译：嘧啶衍生物
公开(公告)号：EP1487805A1
公开(公告)日：2004-12-22
申请号：EP03744366.0
申请日：2003-03-14
申请人： Novartis AG
发明人： BAENTELI, Rolf , ZENKE, Gerhard , COOKE, Nigel, Graham , DUTHALER, Rudolf , THOMA, Gebhard , VON MATT, Anette , HONDA, Toshiyuki , MATSUURA, Naoko , NONOMURA, Kazuhiko , OHMORI, Osamu , UMEMURA, Ichiro , HINTERDING, Klaus , PAPAGEORGIOU, Christos
IPC分类号： C07D239/48 , A61K31/505 , A61P35/04
CPC分类号： C07D239/48 , A61K31/505 , A61K31/506 , A61K31/5377 , A61K31/55 , A61K45/06 , C07D231/12 , C07D233/56 , C07D249/08 , C07D401/12 , C07D401/14 , C07D403/12 , C07D417/12
摘要： There are provided compounds of formula (I), wherein X, R1, R2, R3, R4, R5, R6, R7, R8 and R9 are as indicated in claim 1, useful in disorders where ZAP-70 and/or Syk inhibition plays a role or caused by a malfunction of signal cascades connected with FAK.
摘要翻译：提供式（I）化合物，其中X，R 1，R 2，R 3，R 4，R 5，R 6，R 7，R 8和R 9如权利要求1中所示，可用于ZAP-70和/ 一个角色或由FAK连接的信号级联发生故障引起。

10. 发明公开

EP1309622A2 LAT PEPTIDES AND THEIR USE IN ASSAYS FOR IDENTIFYING IMMUNOSUPPRESSANTS 审中-公开
标题翻译： LAT肽和它们在用于鉴定免疫抑制剂
公开(公告)号：EP1309622A2
公开(公告)日：2003-05-14
申请号：EP01971889.9
申请日：2001-08-07
申请人： Novartis AG , Novartis-Erfindungen Verwaltungsgesellschaft m.b.H.
发明人： CARDINAUX, François , ZENKE, Gerhard
IPC分类号： C07K14/47 , C07K4/00
CPC分类号： C07K7/06 , A61K38/00 , C07K7/08 , C07K14/4705
摘要： The invention relates to novel peptides and their use in assays for identifying novel immunosuppressants. More particularly the present invention provides methods and compositions for identifying compounds that will modulate the interaction of protein tyrosine kinase substrates with their intracellular ligands, as well as between their intracellular ligands and other members of the signaling pathway.

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