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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

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.

7. 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。

8. 发明授权

EP0934326B1 SUBSTITUIERTE AMINOALKANPHOSPHONSÄUREN 失效
标题翻译：取代aminoalkanephosphonic酸
公开(公告)号：EP0934326B1
公开(公告)日：2006-05-03
申请号：EP97946755.2
申请日：1997-10-22
申请人： Novartis AG , Novartis Pharma GmbH
发明人： ACKLIN, Pierre , ALLGEIER, Hans , AUBERSON, Yves , OFNER, Silvio , VEENSTRA, Siem, Jacob
IPC分类号： C07F9/6509 , A61K31/675
CPC分类号： C07F9/650994
摘要： Compounds have the formula (I), in which R1 stands for hydroxy or an aliphatic, araliphatic or aromatic radical; X stands for a bivalent aliphatic, cycloaliphatic, cycloaliphatic-aliphatic, araliphatic, heteroarylaliphatic or aromatic radical; R2 stands for hydrogen or an aliphatic or araliphatic radical; alk stands for lower alkylidene; and R3, R4 and R5 independently represent hydrogen, lower alkyl, halogen, trifluoromethyl, cyano or nitro. These compounds and their salts may be used for treating pathological conditions which respond to the blocking of exciter amino acid receptors, and for producing pharmaceutical compositions.

9. 发明公开

EP1613610A1 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：EP1613610A1
公开(公告)日：2006-01-11
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.

10. 发明公开

EP1483262A1 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：EP1483262A1
公开(公告)日：2004-12-08
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.

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