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1. 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.

2. 发明公开

EP2037926A1 USE OF PKC INHIBITORS IN DIABETIC COMPLICATIONS 审中-公开
标题翻译： PKC抑制剂在糖尿病并发症USE
公开(公告)号：EP2037926A1
公开(公告)日：2009-03-25
申请号：EP07764926.7
申请日：2007-06-28
申请人： NOVARTIS AG
发明人： WAGNER, Jürgen , EVENOU, Jean-Pierre
IPC分类号： A61K31/496 , A61K31/517 , A61P3/10
CPC分类号： A61K31/517 , A61K31/496
摘要： Die vorliegende Erfindung betrifft ein Verfahren zur Herstellung von Pentamethylen- 1,5-diisocyanat, so hergestelltes Pentamethylen-1,5-diisocyanat und dessen Verwendung.

3. 发明公开

EP1767199A3 Methods and compositions for treatment of cancer pain 审中-公开
标题翻译：方法和组合物用于癌症疼痛的治疗
公开(公告)号：EP1767199A3
公开(公告)日：2008-03-26
申请号：EP06126241.6
申请日：2003-04-22
申请人： Novartis AG , Novartis Pharma GmbH
发明人： Fujimoto, Roger Aki , Urban, Laszlo, c/o Novartis Inst. for BioMed Rsrch , Gonzalez, Isabel
IPC分类号： A61K31/196 , C07C229/42 , A61P29/00 , A61P19/00
CPC分类号： A61K31/196
摘要： The invention provides a method of treating cancer pain, e.g. bone cancer pain, in a subject in need of such treatment which comprises administering to the subject an effective amount of a COX-2 inhibitor; advantageously a compound of formula I

wherein R, R 1 , R 2 , R 3 , R 4 , and R 5 are as defined; a pharmaceutically acceptable salts thereof; or a pharmaceutically acceptable prodrug ester thereof.

4. 发明公开

EP1844780A2 Derivatives of aryl-quinazoline/aryl-2-amino-phenyl methanone which promote the release of parathyroid hormone 审中-公开
标题翻译：芳基 - 喹唑啉/芳基-2-氨基 - 苯基 - 甲酮的衍生物，用于促进甲状旁腺激素释放
公开(公告)号：EP1844780A2
公开(公告)日：2007-10-17
申请号：EP07110683.5
申请日：2003-12-22
申请人： Novartis Pharma AG , Novartis Pharma GmbH
发明人： Altmann, Eva , Beerli, René , Gerspacher, Marc , Renaud, Johanne , Weiler, Sven , Widler, Leo
IPC分类号： A61K31/498 , C07D403/06 , C07D239/82 , C07D403/10 , C07D409/06 , C07D405/06 , C07D417/06 , C07D401/06 , C07D413/06 , C07D401/12 , C07D239/78 , C07C49/84 , A61P5/18
CPC分类号： C07C17/12 , C07C45/30 , C07C205/37 , C07C205/44 , C07C205/45 , C07C225/22 , C07C229/18 , C07C255/24 , C07C255/25 , C07C317/18 , C07C317/32 , C07C323/25 , C07C2601/02 , C07D213/64 , C07D239/82 , C07D239/93 , C07D317/58 , C07D401/06 , C07D401/12 , C07D403/06 , C07D403/10 , C07D405/06 , C07D409/06 , C07D413/06 , C07D417/06 , C07C25/18 , C07C47/277
摘要： A compound of formula I

wherein R1, R2, R3 and Y are as defined herein,
or a pharmaceutically-acceptable and -cleavable ester, or acid addition salt thereof,
useful for promoting the release of parathyroid hormone, e.g. for preventing or treating bone conditions which are associated with increased calcium depletion or resorption or in which stimulation of bone formation and calcium fixation in the bone is desirable.

5. 发明公开

EP1767199A2 Methods and compositions for treatment of cancer pain 审中-公开
标题翻译： Methoden und Zusammenstellungen zur Behandlung von Krebsschmerz
公开(公告)号：EP1767199A2
公开(公告)日：2007-03-28
申请号：EP06126241.6
申请日：2003-04-22
申请人： Novartis AG , Novartis Pharma GmbH
发明人： Fujimoto, Roger Aki , Urban, Laszlo, c/o Novartis Inst. for BioMed Rsrch , Gonzalez, Isabel
IPC分类号： A61K31/196 , C07C229/42
CPC分类号： A61K31/196
摘要： The invention provides a method of treating cancer pain, e.g. bone cancer pain, in a subject in need of such treatment which comprises administering to the subject an effective amount of a COX-2 inhibitor; advantageously a compound of formula I

wherein R, R 1 , R 2 , R 3 , R 4 , and R 5 are as defined; a pharmaceutically acceptable salts thereof; or a pharmaceutically acceptable prodrug ester thereof.
摘要翻译：本发明提供了一种治疗癌症疼痛的方法。在需要这种治疗的受试者中的骨癌疼痛包括向受试者施用有效量的COX-2抑制剂; 有利的是其中R，R 1，R 2，R 3，R 4和R 5如所定义的式I化合物; 其药学上可接受的盐; 或其药学上可接受的前药酯。

6. 发明公开

EP1689702A1 ORGANIC COMPOUNDS 有权
标题翻译：有机化合物
公开(公告)号：EP1689702A1
公开(公告)日：2006-08-16
申请号：EP04819222.3
申请日：2004-11-25
申请人： NOVARTIS-PHARMA GMBH , Novartis AG
发明人： NOVARTIS AG , BAESCHLIN, Daniel, Kaspar , MAIBAUM, Jürgen, Klaus , SELLNER, Holger
IPC分类号： C07C237/20 , C07D295/02 , C07C237/24 , C07C271/24 , C07C323/29 , C07C255/50 , C07D319/18 , C07D313/08 , C07D307/79 , C07D207/09 , C07D333/08 , A61P9/12 , A61K31/165 , A61K31/325 , A61K31/44
CPC分类号： C07C237/20 , C07C237/24 , C07C255/60 , C07C271/22 , C07C271/24 , C07C323/41 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2601/18 , C07C2602/08 , C07C2602/42 , C07D207/09 , C07D295/027 , C07D307/79 , C07D313/08 , C07D319/18 , C07D333/08
摘要： Disclosed are δ-amino-Ϝ-hydroxy-ω-aryl-alkanoic acid amide compounds of formula (I) and the salts thereof, having renin-inhibiting properties. Also disclosed are pharmaceutical compositions comprising these compounds and methods of administering them for the treatment of hypertension, atherosclerosis, unstable coronary syndrome, congestive heart failure, cardiac hypertrophy, cardiac fibrosis, cardiomyopathy postinfarction, unstable coronary syndrome, diastolic dysfunction, chronic kidney disease, hepatic fibrosis, complications resulting from diabetes, such as nephropathy, vasculopathy and neuropathy, diseases of the coronary vessels, restenosis following angioplasty, raised intra-ocular pressure, glaucoma, abnormal vascular growth, hyperaldosteronism, cognitive impairment, alzheimers, dementia, anxiety states and cognitive disorders.
摘要翻译：公开了具有肾素抑制性质的式（I）的δ-氨基-β-羟基-ω-芳基 - 链烷酸酰胺化合物及其盐。还公开了包含这些化合物的药物组合物和施用它们以治疗高血压，动脉粥样硬化，不稳定冠状动脉综合征，充血性心力衰竭，心脏肥大，心脏纤维化，心肌梗塞后梗塞，不稳定冠状动脉综合征，舒张功能障碍，慢性肾病，肝纤维化，由糖尿病引起的并发症如肾病，血管病和神经病，冠状血管疾病，血管成形术后再狭窄，眼内压升高，青光眼，血管生长异常，醛固酮增多症，认知障碍，阿尔茨海默病，痴呆，焦虑状态和认知障碍。

7. 发明公开

EP1675965A1 OLIGONUCLEOTIDE MICROARRAY 审中-公开
标题翻译：寡核苷酸微阵列
公开(公告)号：EP1675965A1
公开(公告)日：2006-07-05
申请号：EP04790377.8
申请日：2004-10-13
申请人： Novartis AG , Novartis Forschungsstiftung, Zweigniederlassung Friedrich Miescher Institute for Biomedical Research , NOVARTIS-PHARMA GMBH
发明人： WEILER, Jan , HALL, Jonathan , WANKE, Christoph , LANGE, Jörg, Bernd , FILIPOWICZ, Witold , KOLB, Fabrice
IPC分类号： C12Q1/68
CPC分类号： C12Q1/6883 , C12Q1/6886 , C12Q2600/178
摘要： The present invention relates to oligonucleotide microarrays comprising short chemically modified RNA oligonucleotides and uses of such microarrays in genomics applications. More specifically, the invention provides an oligonucleotide array comprising a surface and a plurality of oligonucleotide, wherein at least one oligonucleotide has at least one modified sugar moiety at the 2'OH position. The microarrays of the invention are more specifically useful to detect small RNAs.

8. 发明公开

EP1675621A2 PHARMACEUTICAL COMPOSITIONS OF LAVENDUSTIN 有权
标题翻译：薰草药物组合物
公开(公告)号：EP1675621A2
公开(公告)日：2006-07-05
申请号：EP04764259.0
申请日：2004-08-18
申请人： Novartis AG , Novartis Pharma GmbH
发明人： KRIWET, Katrin
IPC分类号： A61K47/44 , A61K47/14 , A61K47/10 , A61K47/06 , A61K31/195
CPC分类号： A61K47/06 , A61K9/0014 , A61K31/517 , A61K47/10 , A61K47/14 , A61K47/26 , A61K47/44
摘要： Topical pharmaceutical compositions, e.g. in form of an emulsion, comprising a lavendustin derivative of formula (I): wherein R is methyl, methoxy or ethyl, or a pharmaceutically acceptable salt thereof, and an emollient, and optionally further excipients.

9. 发明公开

EP1673631A2 BIOMARKERS FOR THE PREDICTION OF DRUG-INDUCED DIARRHOEA 审中-公开
标题翻译：生物标志物。药品引起的腹泻的预测
公开(公告)号：EP1673631A2
公开(公告)日：2006-06-28
申请号：EP04765829.9
申请日：2004-10-05
申请人： Novartis AG , Novartis Pharma GmbH
发明人： WOLFGANG, Curt, Douglas
IPC分类号： G01N33/543 , C12Q1/68 , A61K31/427
CPC分类号： C12Q1/6883 , A61K31/427 , C12Q1/6837 , C12Q2600/106 , C12Q2600/156 , C12Q2600/158
摘要： The invention provides biomarkers for the prediction of diarrhoea based upon the gene expression of certain genes by the subject, the expression of the Diego blood type by the subject, or the results of haematological assays.

10. 发明公开

EP1663992A1 2,4-DI (PHENYLAMINO) PYRIMIDINES USEFUL IN THE TREATMENT OF PROLIFERATIVE DISORDERS 审中-公开
标题翻译： 2,4-二（苯基氨基）嘧啶类所产生增殖性疾病的治疗是合适的
公开(公告)号：EP1663992A1
公开(公告)日：2006-06-07
申请号：EP04765358.9
申请日：2004-09-17
申请人： Novartis AG , Novartis Pharma GmbH
发明人： IMBACH, Patricia , ROESEL, Johannes
IPC分类号： C07D239/48 , C07D405/12 , C07D403/12 , C07D401/12 , C07D401/14 , A61K31/506 , A61K35/00
CPC分类号： C07D403/14 , A61K31/505 , A61K31/506 , A61K31/5377 , A61K31/541 , A61K31/55 , C04B35/632 , C07D239/48 , C07D401/12 , C07D403/12
摘要： There is provided a method of preventing or treating proliferative disorders such as a tumor disease, by inhibiting ALK activity with compounds of formula (I) wherein X, R1, R2 , R3 , R4 , R5, R6, R7,R8 and R9 are as indicated in claim 1.

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