专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明授权

EP1613610B8 BENZO 1,2,5 OXADIAZOLES AND BENZO 1,2,5 THIADIAZOLES USEFUL AS HISTOPATHOLOGICAL STAINING AGENTS, IMAGING AGENTS AND BIOMARKERS 有权
标题翻译： BENZO¬1,2,5恶二唑和噻二唑BENZO¬1,2,5ALS病理ANFÄRBUNGSMITTEL，图片资源和生物标志物
公开(公告)号：EP1613610B8
公开(公告)日：2009-12-16
申请号：EP04725341.4
申请日：2004-04-02
申请人： Novartis AG , Novartis Pharma GmbH
发明人： AUBERSON, Yves , HINTERMANN, Samuel , ZIMMERMANN, Kaspar
IPC分类号： C07D271/12 , C07D285/14 , A61K51/04
CPC分类号： C07D271/12 , A61K47/6813 , C07D285/14
摘要： The present invention relates to novel benzo[1,2,5]oxadiazoles and benzo[1,2,5]thiadiazoles of formula (I) wherein X is O or S, R1 is 5-(2-fluoro-ethylamino)-thiazol-2-yl, 5-(2-18F-ethylamino)- thiazol-2-yl or a group of formula (a) wherein Y is CH or N, R2 is NHCH3, NH11CH3, N(CH3)11CH3, N(CH3)2, N(11CH3)2, NH(CH2)nF, NH(CH2)n18F, N(CH3)(CH2)nF, N(CH3)-(CH2)n 18F, O-(CH2)nF, O-(CH2)n 18F, CONH(CH2)nF or CONH(CH2)n18F (n being in each case 2 to 4) and R3 is hydroxy, (C1-4)alkoxy, hydrogen or nitro, in free base or acid addition salt form; their preparation, their use as markers in diagnosis and compositions containing them.

2. 发明授权

EP1651592B1 NOVEL DIBENZO[B,F]OXEPINE-10-CARBOXAMIDES AND PHARMACEUTICAL USES THEREOF 有权
标题翻译： NEW二苯并[b，f]恶-10-羧酸酰胺和它们的药物应用
公开(公告)号：EP1651592B1
公开(公告)日：2009-04-29
申请号：EP04763454.8
申请日：2004-07-23
申请人： NOVARTIS AG , Novartis Pharma GmbH
发明人： AUBERSON, Yves , BETSCHART, Claudia , FLOHR, Stefanie , GLATTHAR, Ralf , SIMIC, Oliver , TINTELNOT-BLOMLEY, Marina , TROXLER, Thomas, J. , VANGREVELINGHE, Eric , VEENSTRA, Siem, Jacob
IPC分类号： C07C235/40 , C07D313/14 , C07D267/20 , A61K31/335 , A61K31/395 , A61K31/165 , A61P25/28
CPC分类号： C07D405/12 , C07C235/82 , C07C2603/32 , C07D313/14 , C07D407/12 , C07D413/12 , C07D453/02 , C07D491/04
摘要： The present invention pertains to compounds of formula (I) wherein X is O, NH, N(C1-4)alkyl, CO or CHOH, Y is CH or N, A and B are each hydrogen or together form a second bond between the carbon atoms to which they are attached, R1 is hydrogen or (C1-4)alkyl, R2 is optionally substituted (C1-8)alkyl, (C3-7)cycloalkyl, (C3-7)cycloalkyl(C1-4)alkyl, aryl or heteroaryl, R3 is CH(Re)CONRaRb or (CH2)nNRc,Rd, n is 0, 1 or 2, Ra, Rb, Rc and Rd, independently, are hydrogen or optionally substituted (C1-8)alkyl, (C3-7)cycloalkyl, (C3-7)cycloalkyl(C1-4)alkyl, (C7-9)bicycloalkyl, 1-aza-(C7-9)bicycloalkyl, aryl, aryl(C1-4)alkyl, heteroaryl, heteroaryl(C1-4)alkyl or heterocyclyl, or Ra, Rb, Rc and Rd, together with the nitrogen to which they are attached, form an optionally substituted pyrrolidinyl, piperidino, morpholino or piperazinyl group, Re is (C1-8)alkyl, (C1-4)alkoxy(C1-4)alkyl, (C3-7)cycloalkyl or (C3-7)cycloalkyl(C1-4)alkyl, and R4, R5, R6, R7, R8 and R9, independently, are hydrogen, (C1-4)alkyl, (C1-4)alkoxy, (C1-4)alkyl-SO2, cyano, nitro or halogen; to a process for the preparation of such compounds of formula (I), their use as a pharmaceuticals, especially in the treatment of neurological and vascular disorders related to beta-amyloid generation and/or aggregation, and to pharmaceutical compositions and combinations comprising such compounds of formula (I).

3. 发明授权

EP1670803B1 CERTAIN SUBSTITUTED SPIROCYCLIC LACTAMS AND USE THEREOF AS PHARMACEUTICALS 有权
标题翻译：某些取代螺环内酰胺及其用作药物
公开(公告)号：EP1670803B1
公开(公告)日：2008-03-12
申请号：EP04765790.3
申请日：2004-10-04
申请人： Novartis AG , Novartis Pharma GmbH
发明人： AUBERSON, Yves , GLATTHAR, Ralf , SALTER, RHYS , SIMIC, Oliver , TINTELNOT-BLOMLEY, Marina
IPC分类号： C07D487/10
CPC分类号： C07D487/10
摘要： The present invention relates to novel 2-(6-oxo-1,7-diaza-spiro[4-4]non-7-yl)-propionam ides of the formula wherein R1, R2, R3, R4, R5, R6, m and p are as defined in the specification, to their preparation, to their use as pharmaceuticals and to pharmaceutical compositions containing them.

4. 发明授权

EP1483262B1 COUMARINES USEFUL AS BIOMARKERS 有权
标题翻译：作为生物标志物SUITABLE香豆素
公开(公告)号：EP1483262B1
公开(公告)日：2007-11-14
申请号：EP03743381.0
申请日：2003-03-05
申请人： Novartis AG , Novartis Pharma GmbH
发明人： AUBERSON, Yves
IPC分类号： C07D417/04 , C07D471/04 , C07D413/14 , C07D413/04 , C07D405/04 , G01N33/53
CPC分类号： C07D405/04 , C07D413/04 , C07D413/14 , C07D417/04 , C07D471/04
摘要： The invention provides compounds of formula (I), wherein R, R1, R2, R3 and R4 are as defined in the description, and their preparation. The compounds of formula I are useful as biomarkers.

5. 发明公开

EP1658294A1 3H-PHENOXAZINE DERIVATIVES SUITABLE AS NEAR-INFRARED IMAGING AGENTS, PREPARATION AN USE THEREOF 有权
标题翻译： AS合适的近红外3H-嗪，生产和使用的手段
公开(公告)号：EP1658294A1
公开(公告)日：2006-05-24
申请号：EP04764213.7
申请日：2004-08-17
申请人： Novartis AG , Novartis Pharma GmbH
发明人： AUBERSON, Yves , GREMLICH, Hans-Ulrich , HINTERSTEINER, Martin , KINZY, Willy , KNEUER, Rainer
IPC分类号： C07D498/22 , C07D513/22 , A61K49/00
CPC分类号： C07D513/14
摘要： The present invention provides compounds of formula (I) wherein X and Y represent CH, CH2 or a divalent or trivalent heteroatom under the proviso that X and Y are not simultaneously CH or CH2; m and o represent independently of each other 0 or 1, with the proviso that if m is 0 then the dotted line between Y and the neighboring C atom represents a bond and Y is CH or a trivalent heteroatom, if m is 1 then the dotted line between Y and the neighboring C atom is absent and Y is CH2 or a divalent heteroatom, if o is 0 then the dotted line between X and the neighboring C atom represents a bond and X is CH or a trivalent heteroatom, if o is 1 then the dotted line between X and the neighboring C atom is absent and X is CH2 or a divalent heteroatom; A represents (CH3CR4)p and Q represents (CR9R10)n; n and p represent independently of each other 0 or 1; R6, R7, R13 and R14 denote independently of each other hydrogen, halogen, (C1-4)alkyl, (C1-4)alkylSO2, SO3H, carboxy, (C1-4)alkoxy carbonyl, (C1-4)alkoxy, OH or NR15R16; R1, R2, R3, R4, R9, R10, R11 and R12 denote independently of each other hydrogen, (C1-4)alkyl, carboxy, (C1-4)alkoxy carbonyl or (C1-4)alkoxy, or, when X is CH or CH2 then R1 and R2 can also be OH or NR15R16, or when Y is CH or CH2 then R11, R12 can also be OH or NR15R16; R5, R8, R15 and R16 are independently of each other hydrogen, (C1-4)alkyl, (C1-4)alkoxy, R17O-C(O)-(C1-4)alkyl or (reactive group)-(C1-4)alkyl; and R17 represents hydrogen or (C1-4)alkyl; compositions comprising such compounds, a process for the production of such compounds of formula (I), a method of labeling target structures, especially amyloid plaques, in the brain, a method for identifying Alzheimer's disease, use of a compound of formula I as a near-infrared imaging agent and a conjugate comprising a compound of formula (I) covalently linked to a biomolecule through a reactive group.

6. 发明授权

EP1670762B1 PYRIDYLACETYLENES FOR USE AS RADIOTRACERS AND IMAGING AGENTS 有权
标题翻译： PYRIDYLACETYLENE FOR USE AS放射性标记物中和手段IMAGING
公开(公告)号：EP1670762B1
公开(公告)日：2012-12-05
申请号：EP04765586.5
申请日：2004-09-24
申请人： Novartis AG , Novartis Pharma GmbH
发明人： GASPARINI, Fabrizio , AUBERSON, Yves , KESSLER, Lea , AMETAMEY, Simon, Mensah
IPC分类号： C07D213/53 , A61K31/44 , A61P43/00
CPC分类号： C07D213/53

7. 发明公开

EP1682103A1 INDOLYL-PYRROLEDIONE DERIVATIVES FOR THE TREATMENT OF NEUROLOGICAL AND VASCULAR DISORDERS RELATED TO BETA-AMYLOID GENERATION AND/OR AGGREGATION 审中-公开
标题翻译：吲哚PYRROLDION衍生物对神经和血管问题的处理相关的β淀粉样蛋白的产生和/或聚集
公开(公告)号：EP1682103A1
公开(公告)日：2006-07-26
申请号：EP04790865.2
申请日：2004-10-26
申请人： Novartis AG , Novartis Pharma GmbH
发明人： AUBERSON, Yves , BILBE, Graeme , KUHN, Rainer, R. , VON MATT, Peter , RUEEGER, Heinrich , STAUFENBIEL, Matthias , WAGNER, Jürgen , ZIMMERMANN, Kaspar
IPC分类号： A61K31/00 , A61K31/496 , A61K31/517 , A61P25/00 , A61P25/28
CPC分类号： A61K31/00 , A61K31/496 , A61K31/517
摘要： The invention relates to the use of an inhibitor of formula (I), or a pharmaceutically acceptable salt thereof having an activity on protein kinases PKC alpha, PKC beta, PKC gamma, PKC epsilon, PKC theta, CDK-1, KDR, PKA, Flt-1, Flt-2, Flt-3 or Flt-4, or on a combination of the above enzymes, for the treatment and/or prevention of neurological and vascular disorders related to beta-amyloid generation and/or aggregation such as neurodegenerative diseases like Down's Syndrome, memory and cognitive impairment, dementia, amyloid neuropathies, brain inflammation, nerve and brain trauma, vascular amyloidosis, or cerebral hemorrhage with amyloidosis.

8. 发明授权

EP1453512B8 ACETYLENE DERIVATIVES HAVING MGLUR 5 ANTAGONISTIC ACTIVITY 有权转让
标题翻译：具有MGLUR 5拮抗活性的乙炔衍生物
公开(公告)号：EP1453512B8
公开(公告)日：2006-07-19
申请号：EP02792867.0
申请日：2002-12-03
申请人： Novartis AG , Novartis Pharma GmbH
发明人： GASPARINI, Fabrizio , AUBERSON, Yves , OFNER, Silvio , Hart, Terance W. , Zimmermann, Kaspar
IPC分类号： A61K31/4709 , A61K31/404 , A61P25/00 , C07D209/32 , C07D405/06 , C07D405/12 , C07D209/08 , C07D209/44 , C07C271/16 , C07C233/23 , C07C271/24 , C07D215/20
CPC分类号： C07C271/16 , C07D209/08 , C07D209/44 , C07D215/08 , C07D215/20 , C07D401/04 , C07D401/06 , C07D405/06 , C07D405/12

9. 发明授权

EP1658294B1 3H-PHENOXAZINE DERIVATIVES SUITABLE AS NEAR-INFRARED IMAGING AGENTS, PREPARATION AN USE THEREOF 有权
标题翻译： AS合适的近红外3H-嗪，生产和使用的手段
公开(公告)号：EP1658294B1
公开(公告)日：2007-01-10
申请号：EP04764213.7
申请日：2004-08-17
申请人： Novartis AG , Novartis Pharma GmbH
发明人： AUBERSON, Yves , GREMLICH, Hans-Ulrich , HINTERSTEINER, Martin , KINZY, Willy , KNEUER, Rainer
IPC分类号： C07D498/22 , C07D513/22 , A61K49/00
CPC分类号： C07D513/14
摘要： The present invention provides compounds of formula (I) wherein X and Y represent CH, CH2 or a divalent or trivalent heteroatom under the proviso that X and Y are not simultaneously CH or CH2; m and o represent independently of each other 0 or 1, with the proviso that if m is 0 then the dotted line between Y and the neighboring C atom represents a bond and Y is CH or a trivalent heteroatom, if m is 1 then the dotted line between Y and the neighboring C atom is absent and Y is CH2 or a divalent heteroatom, if o is 0 then the dotted line between X and the neighboring C atom represents a bond and X is CH or a trivalent heteroatom, if o is 1 then the dotted line between X and the neighboring C atom is absent and X is CH2 or a divalent heteroatom; A represents (CH3CR4)p and Q represents (CR9R10)n; n and p represent independently of each other 0 or 1; R6, R7, R13 and R14 denote independently of each other hydrogen, halogen, (C1-4)alkyl, (C1-4)alkylSO2, SO3H, carboxy, (C1-4)alkoxy carbonyl, (C1-4)alkoxy, OH or NR15R16; R1, R2, R3, R4, R9, R10, R11 and R12 denote independently of each other hydrogen, (C1-4)alkyl, carboxy, (C1-4)alkoxy carbonyl or (C1-4)alkoxy, or, when X is CH or CH2 then R1 and R2 can also be OH or NR15R16, or when Y is CH or CH2 then R11, R12 can also be OH or NR15R16; R5, R8, R15 and R16 are independently of each other hydrogen, (C1-4)alkyl, (C1-4)alkoxy, R17O-C(O)-(C1-4)alkyl or (reactive group)-(C1-4)alkyl; and R17 represents hydrogen or (C1-4)alkyl; compositions comprising such compounds, a process for the production of such compounds of formula (I), a method of labeling target structures, especially amyloid plaques, in the brain, a method for identifying Alzheimer's disease, use of a compound of formula I as a near-infrared imaging agent and a conjugate comprising a compound of formula (I) covalently linked to a biomolecule through a reactive group.

10. 发明公开

EP1651592A2 NOVEL DIBENZO[B,F]OXEPINE-10-CARBOXAMIDES AND PHARMACEUTICAL USES THEREOF 有权
标题翻译： NEER DIBENZO [B，F] OXEPIN-10-CARBONSÄUREAMIDEUND DEREN PHARMAZEUTISCHE ANWENDUNGEN
公开(公告)号：EP1651592A2
公开(公告)日：2006-05-03
申请号：EP04763454.8
申请日：2004-07-23
申请人： Novartis AG , Novartis Pharma GmbH
发明人： AUBERSON, Yves , BETSCHART, Claudia , FLOHR, Stefanie , GLATTHAR, Ralf , SIMIC, Oliver , TINTELNOT-BLOMLEY, Marina , TROXLER, Thomas, J. , VANGREVELINGHE, Eric , VEENSTRA, Siem, Jacob
IPC分类号： C07C235/40 , C07D313/14 , C07D267/20 , A61K31/335 , A61K31/395 , A61K31/165 , A61P25/28
CPC分类号： C07D405/12 , C07C235/82 , C07C2603/32 , C07D313/14 , C07D407/12 , C07D413/12 , C07D453/02 , C07D491/04
摘要： The present invention pertains to compounds of formula (I) wherein X is O, NH, N(C1-4)alkyl, CO or CHOH, Y is CH or N, A and B are each hydrogen or together form a second bond between the carbon atoms to which they are attached, R1 is hydrogen or (C1-4)alkyl, R2 is optionally substituted (C1-8)alkyl, (C3-7)cycloalkyl, (C3-7)cycloalkyl(C1-4)alkyl, aryl or heteroaryl, R3 is CH(Re)CONRaRb or (CH2)nNRc,Rd, n is 0, 1 or 2, Ra, Rb, Rc and Rd, independently, are hydrogen or optionally substituted (C1-8)alkyl, (C3-7)cycloalkyl, (C3-7)cycloalkyl(C1-4)alkyl, (C7-9)bicycloalkyl, 1-aza-(C7-9)bicycloalkyl, aryl, aryl(C1-4)alkyl, heteroaryl, heteroaryl(C1-4)alkyl or heterocyclyl, or Ra, Rb, Rc and Rd, together with the nitrogen to which they are attached, form an optionally substituted pyrrolidinyl, piperidino, morpholino or piperazinyl group, Re is (C1-8)alkyl, (C1-4)alkoxy(C1-4)alkyl, (C3-7)cycloalkyl or (C3-7)cycloalkyl(C1-4)alkyl, and R4, R5, R6, R7, R8 and R9, independently, are hydrogen, (C1-4)alkyl, (C1-4)alkoxy, (C1-4)alkyl-SO2, cyano, nitro or halogen; to a process for the preparation of such compounds of formula (I), their use as a pharmaceuticals, especially in the treatment of neurological and vascular disorders related to beta-amyloid generation and/or aggregation, and to pharmaceutical compositions and combinations comprising such compounds of formula (I).
摘要翻译：本发明涉及新型的二苯并[b，f]氧杂七环素-10-甲酰胺化合物，其用于制备式I化合物的方法，它们作为药物的用途，特别是用于治疗与β受体相关的神经和血管疾病，淀粉样蛋白生成和/或聚集，以及包含式I化合物的药物组合物和组合。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式