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1. 发明申请

WO2005014517A2 NOVEL DIBENZO[B,F]OXEPINE-10-CARBOXAMIDES AND PHARMACEUTICAL USES THEREOF 审中-公开
标题翻译：新二苯并[B，F] OXEPINE-10-羧酰胺及其药物用途
公开(公告)号：WO2005014517A2
公开(公告)日：2005-02-17
申请号：PCT/EP2004/008283
申请日：2004-07-23
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , AUBERSON, Yves , BETSCHART, Claudia , FLOHR, Stefanie , GLATTHAR, Ralf , SIMIC, Oliver , TINTELNOT-BLOMLEY, Marina , TROXLER, Thomas, J. , VANGREVELINGHE, Eric , VEENSTRA, Siem, Jacob
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： C07C61/00
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(C 1-4 )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, R 1 is hydrogen or (C 1-4 )alkyl, R 2 is optionally substituted (C 1-8 )alkyl, (C 3-7 )cycloalkyl, (C 3-7 )cycloalkyl(C 1-4 )alkyl, aryl or heteroaryl, R 3 is CH(R e )CONR a R b or (CH 2 ) n NR c ,R d , n is 0, 1 or 2, R a , R b , R c and R d , independently, are hydrogen or optionally substituted (C 1-8 )alkyl, (C 3-7 )cycloalkyl, (C 3-7 )cycloalkyl(C 1-4 )alkyl, (C 7-9 )bicycloalkyl, 1-aza-(C 7-9 )bicycloalkyl, aryl, aryl(C 1-4 )alkyl, heteroaryl, heteroaryl(C 1-4 )alkyl or heterocyclyl, or R a , R b , R c and R d , together with the nitrogen to which they are attached, form an optionally substituted pyrrolidinyl, piperidino, morpholino or piperazinyl group, R e is (C 1-8 )alkyl, (C 1-4 )alkoxy(C 1-4 )alkyl, (C 3-7 )cycloalkyl or (C 3-7 )cycloalkyl(C 1-4 )alkyl, and R 4 , R 5 , R 6 , R 7 , R 8 and R 9 , independently, are hydrogen, (C 1-4 )alkyl, (C 1-4 )alkoxy, (C 1-4 )alkyl-SO 2 , 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：本发明涉及式（I）化合物，其中X是O，NH，N（C 1-4）烷基，CO或CHOH，Y是CH或N，A和B各自是氢或一起形成第二键碳原子，R 1是氢或（C 1-4）烷基，R 2是任选取代的（C 1-8）烷基，（C 3-7）环烷基，（C 3-7）环烷基（C 1-4）烷基，芳基或杂芳基，R3是CH（Re）CONRaRb或（CH2）nNRc，Rd，n是0,1或2，Ra，Rb，Rc和Rd独立地是氢或任选取代的（C 1-8）烷基，（ C3-7）环烷基，（C3-7）环烷基（C1-4）烷基，（C7-9）双环烷基，1-氮杂 - （C7-9）双环烷基，芳基，芳基（C1-4）烷基，杂芳基，杂芳基（C 1-4）烷基或杂环基，或R a，R b，R c和R d与它们所连接的氮一起形成任选取代的吡咯烷基，哌啶子基，吗啉代或哌嗪基，Re是（C 1-8）烷基，（C 1-4）烷氧基（C 1-4）烷基，（C 3-7）环烷基或（C 3-7）环烷基（C 1-4）烷基，R 4，R 5，R 6，R 7，R 8和R 9独立地为氢，（C1-4 ）烷基，（C 1-4）烷氧基，（C 1-4）烷基-SO 2，氰基，硝基或卤素; 制备这种式（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-淀粉样蛋白生成和/或聚集相关的神经和血管疾病，以及包含这些化合物的药物组合物和组合的式（I）化合物。

2. 发明申请

WO2005049585A1 MACROCYCLIC LACTAMS AND PHARMACEUTICAL USE THEREOF 审中-公开
标题翻译：大肠杆菌及其药物用途
公开(公告)号：WO2005049585A1
公开(公告)日：2005-06-02
申请号：PCT/EP2004/012497
申请日：2004-11-04
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , AUBERSON, Yves , BETSCHART, Claudia , GLATTHAR, Ralf , LAUMEN, Kurt , MACHAUER, Rainer , TINTELNOT-BLOMLEY, Marina , TROXLER, Thomas, J. , VEENSTRA, Siem, Jacob
发明人： AUBERSON, Yves , BETSCHART, Claudia , GLATTHAR, Ralf , LAUMEN, Kurt , MACHAUER, Rainer , TINTELNOT-BLOMLEY, Marina , TROXLER, Thomas, J. , VEENSTRA, Siem, Jacob
IPC分类号： C07D245/02
CPC分类号： C07D245/02 , C07D255/00 , C07D273/00 , C07D281/00 , C07D471/08 , C07D513/08
摘要： The present invention relates to novel macrocyclic compounds of the formula (I) wherein R 1 , R 2 , R 3 , U, V, W, X, Y, Z and n are as defined in the specification, the number of ring atoms included in the macrocyclic ring being 14, 15, 16 or 17, in free base form or in acid addition salt form, to their preparation, to their use as pharmaceuticals and to pharmaceutical compositions comprising them.
摘要翻译：本发明涉及式（I）的新的大环化合物，其中R 1，R 2，R 3，U，V，W，X，Y，Z和n如说明书中所定义，大环中包括的环原子数环为14,15,16或17，以游离碱形式或以酸加成盐形式，其制备用作药物和包含它们的药物组合物。

3. 发明申请

WO2005035535A1 CERTAIN SUBSTITUTED SPIROCYCLIC LACTAMS AND USE THEREOF AS PHARMACEUTICALS 审中-公开
标题翻译：某些替代的螺旋藻和其作为药物的用途
公开(公告)号：WO2005035535A1
公开(公告)日：2005-04-21
申请号：PCT/EP2004/011054
申请日：2004-10-04
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , AUBERSON, Yves , GLATTHAR, Ralf , SALTER, RHYS , SIMIC, Oliver , TINTELNOT-BLOMLEY, Marina
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 R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , m and p are as defined in the specification, to their preparation, to their use as pharmaceuticals and to pharmaceutical compositions containing them.
摘要翻译：本发明涉及下式的新的2-（6-氧代-1,7-二氮杂 - 螺[4-4]壬-7-基） - 丙酰胺其中R1，R2，R3，R4，R5，R6， m和p如说明书中所定义，它们的制备，用作药物和含有它们的药物组合物。

4. 发明申请

WO2014013469A1 CARBAMATE/UREA DERIVATIVES 审中-公开
标题翻译：碳酸盐/尿素衍生物
公开(公告)号：WO2014013469A1
公开(公告)日：2014-01-23
申请号：PCT/IB2013/055916
申请日：2013-07-18
申请人： NOVARTIS AG , AUBERSON, Yves , BOCK, Mark Gary , BRAGA, Dario , CURZI, Marco , DODD, Stephanie Kay , GIAFFREDA, Stefano Luca , JIANG, Haiyang , KARPINSKI, Piotr , TROXLER, Thomas J. , WANG, Tielin , WANG, Xiaoyang , ZHANG, Xuechun
发明人： AUBERSON, Yves , BOCK, Mark Gary , BRAGA, Dario , CURZI, Marco , DODD, Stephanie Kay , GIAFFREDA, Stefano Luca , JIANG, Haiyang , KARPINSKI, Piotr , TROXLER, Thomas J. , WANG, Tielin , WANG, Xiaoyang , ZHANG, Xuechun
IPC分类号： C07D401/14 , C07D401/04 , A61K31/4545 , A61P25/00
CPC分类号： C07D401/04 , A61K31/496 , A61K31/501 , C07B2200/13 , C07C57/15 , C07C59/265 , C07D403/04
摘要： The invention relates to compound of the formula (I) or a salt thereof, wherein the substituents are as defined in the specification; to its preparation, to its use as medicament and to medicaments comprising it.
摘要翻译：本发明涉及式（I）化合物或其盐，其中取代基如说明书中所定义; 作为其制备，用作药物和包含它的药物。

5. 发明申请

WO2007096194A1 RADIO-LABELED ISOXAZOLE DERIVATIVES USEFUL FOR THE LABELING AND DIAGNOSTIC OF HSP90 FUNCTIONALITY 审中-公开
标题翻译：用于标记和诊断HSP90功能的无机标记的异丙唑衍生物
公开(公告)号：WO2007096194A1
公开(公告)日：2007-08-30
申请号：PCT/EP2007/001627
申请日：2007-02-26
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , AUBERSON, Yves , BERGSTROEM, Mats , CHENE, Patrick , MARTARELLO, Laurent , SCHOEPFER, Joseph , BRIARD, Emmanuelle
发明人： AUBERSON, Yves , BERGSTROEM, Mats , CHENE, Patrick , MARTARELLO, Laurent , SCHOEPFER, Joseph , BRIARD, Emmanuelle
IPC分类号： C07B59/00 , A61K51/04
CPC分类号： C07B59/002
摘要： A radio-labeled isoxazole derivative of formula I, wherein R 1 represents H, N-{ 11 C]alkyl-piperazinyl, N-[ 11 C]alkyl-piperazinyl-alkyl, N-[ 3 H]alkyl- piperazinyl, N-methyl-piperazinyl or N-[ 3 H]alkyl-piperazinyl-alkyl. R 2 represents H, alkoxy, [ 11 C]alkoxy, N-[ 11 C]alkyl-piperazinyl, N-[ 11 C]alkyl-piperazinyl-alkyl, [ 3 H]aIkoxy1 N-pHJalkyl-piperazinyl, N-pHJalkyl-piperazinyl-alkyl, N-alkyl-piperazinyl-alkyl, methylsulfonyl-ethylaminomethyl, halo, [ 18 F]fluoro, O-{ 18 F]fluoroalkyl, CH 2 NH[ 18 F]fluoroalkyl, or CH 2 N-alkyt-[ 18 F]fluoroalkyl, R 3 represents alkyl, N-alkyl amidoyl, N-[ 18 F]fluoroalkyl amidoyl, N-haloalkyl amidoyl, and R 4 represents H, alkyl or halo, under the proviso that at least one of the radicals R 1 . R 2 and R 3 bears a radio-labeled carbon or fluoro atom, or a salt thereof.
摘要翻译：式I的放射性标记的异恶唑衍生物，其中R 1表示H，N - （C 1 -C 6）烷基 - 哌嗪基，N - [ C 1 -C 4烷基 - 哌嗪基 - 烷基，N - [ - H]烷基 - 哌嗪基，N-甲基 - 哌嗪基或N - [叔丁氧基]烷基 - 哌嗪基 - 。 R 2表示H，烷氧基，[ - 11 C]烷氧基，N - [（C 1 -C 6）烷基 - 哌嗪基，N - 11 C]烷基 - 哌嗪基 - 烷基，[叔丁氧基]烷氧基，N-pHJ烷基 - 哌嗪基，N-pHJ烷基 - 哌嗪基 - 烷基，N-烷基 - 哌嗪基 - 烷基，甲基磺酰基 - 乙基氨基甲基，卤素，[F 18 F]氟，O - { - 18 F]氟代烷基，CH 2 NH [18] F]氟烷基或CH 2 N-烷基 - [ - 18 F]氟代烷基，R 3表示烷基，N-烷基酰氨基，N- F卤代烷基酰胺基，N-卤代烷基酰胺基和R 4代表H，烷基或卤素，条件是至少一个基团R 1， 1 。 R 2和R 3都带有放射性标记的碳或氟原子或其盐。

6. 发明申请

WO2005030723A1 PYRIDYLACETYLENES FOR USE AS RADIOTRACERS AND IMAGING AGENTS 审中-公开
标题翻译：用作放射剂和成像剂的吡咯烷酮
公开(公告)号：WO2005030723A1
公开(公告)日：2005-04-07
申请号：PCT/EP2004/010743
申请日：2004-09-24
申请人： NOVARTIS AG , NOVARTIS PHARMA GmbH , GASPARINI, Fabrizio , AUBERSON, Yves , KESSLER, Lea , AMETAMEY, Simon, Mensah
发明人： GASPARINI, Fabrizio , AUBERSON, Yves , KESSLER, Lea , AMETAMEY, Simon, Mensah
IPC分类号： C07D213/53
CPC分类号： C07D213/53
摘要： The present invention relates to novel pyridylacetylene derivatives of formula I, their Preparation, their use as radiotracers/markers and compositions containing them.
摘要翻译：本发明涉及式I的新型吡啶基乙炔衍生物，其制备方法，它们作为放射性示踪剂/标记物的用途和含有它们的组合物。

7. 发明申请

WO2003047581A1 ACETYLENE DERIVATIVES HAVING MGLUR 5 ANTAGONISTIC ACTIVITY 审中-公开
标题翻译：具有MGLUR 5拮抗活性的乙酰衍生物
公开(公告)号：WO2003047581A1
公开(公告)日：2003-06-12
申请号：PCT/EP2002/013670
申请日：2002-12-03
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , GASPARINI, Fabrizio , AUBERSON, Yves , OFNER, Silvio
发明人： GASPARINI, Fabrizio , AUBERSON, Yves , OFNER, Silvio
IPC分类号： A61K31/4709
CPC分类号： C07C271/16 , C07D209/08 , C07D209/44 , C07D215/08 , C07D215/20 , C07D401/04 , C07D401/06 , C07D405/06 , C07D405/12
摘要： The invention provides compounds of formula (I) wherein m, n, A, R, R', R", R o , X and Y are as defined in the description, and their preparation. The compounds of formula (I) are useful as pharmaceuticals in the treatment of e.g. nervous system disorders.
摘要翻译：本发明提供式（I）化合物，其中m，n，A，R，R'，R“，Ro，X和Y如说明书中所定义，及其制备。药物治疗例如神经系统疾病。

8. 发明申请

WO2005039549A1 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：用于治疗与β-淀粉样蛋白生成和/或聚集相关的神经病和血管疾病的吲哚基吡咯烷酮衍生物
公开(公告)号：WO2005039549A1
公开(公告)日：2005-05-06
申请号：PCT/EP2004/012082
申请日：2004-10-26
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , AUBERSON, Yves , BILBE, Graeme , KUHN, Rainer, R. , VON MATT, Peter , RUEEGER, Heinrich , STAUFENBIEL, Matthias , WAGNER, Jürgen , ZIMMERMANN, Kaspar
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
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.
摘要翻译：本发明涉及对蛋白激酶PKCα，PKCβ，PKCγ，PKCε，PKCθ，CDK-1，KDR，PKA等具有活性的式（I）抑制剂或其药学上可接受的盐的用途， Flt-1，Flt-2，Flt-3或Flt-4，或上述酶的组合，用于治疗和/或预防与β-淀粉样蛋白产生和/或聚集相关的神经和血管障碍，例如神经变性疾病如唐氏综合征，记忆和认知障碍，痴呆，淀粉样蛋白神经病，脑炎症，神经和脑外伤，血管淀粉样变性或淀粉样变性脑出血。

9. 发明申请

WO2005016934A1 3H-PHENOXAZINE DERIVATIVES SUITABLE AS NEAR-INFRARED IMAGING AGENTS, PREPARATION AN USE THEREOF 审中-公开
标题翻译：适用于近红外成像剂的3H-苯并恶嗪衍生物，其制备方法
公开(公告)号：WO2005016934A1
公开(公告)日：2005-02-24
申请号：PCT/EP2004/009225
申请日：2004-08-17
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , AUBERSON, Yves , GREMLICH, Hans-Ulrich , HINTERSTEINER, Martin , KINZY, Willy , KNEUER, Rainer
发明人： AUBERSON, Yves , GREMLICH, Hans-Ulrich , HINTERSTEINER, Martin , KINZY, Willy , KNEUER, Rainer
IPC分类号： C07D498/22
CPC分类号： C07D513/14
摘要： The present invention provides compounds of formula (I) wherein X and Y represent CH, CH 2 or a divalent or trivalent heteroatom under the proviso that X and Y are not simultaneously CH or CH 2 ; 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 CH 2 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 CH 2 or a divalent heteroatom; A represents (CH 3 CR 4 ) p and Q represents (CR 9 R 10 ) n ; n and p represent independently of each other 0 or 1; R 6 , R 7 , R 13 and R 14 denote independently of each other hydrogen, halogen, (C 1-4 )alkyl, (C 1-4 )alkylSO 2 , SO 3 H, carboxy, (C 1-4 )alkoxy carbonyl, (C 1-4 )alkoxy, OH or NR 15 R 16 ; R 1 , R 2 , R 3 , R 4 , R 9 , R 10 , R 11 and R 12 denote independently of each other hydrogen, (C 1-4 )alkyl, carboxy, (C 1-4 )alkoxy carbonyl or (C 1-4 )alkoxy, or, when X is CH or CH 2 then R 1 and R 2 can also be OH or NR 15 R 16 , or when Y is CH or CH 2 then R 11 , R 12 can also be OH or NR 15 R 16 ; R 5 , R 8 , R 15 and R 16 are independently of each other hydrogen, (C 1-4 )alkyl, (C 1-4 )alkoxy, R 17 O-C(O)-(C 1-4 )alkyl or (reactive group)-(C 1-4 )alkyl; and R 17 represents hydrogen or (C 1-4 )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.
摘要翻译：本发明提供式（I）化合物，其中X和Y表示CH，CH 2或二价或三价杂原子，条件是X和Y不同时为CH或CH 2; m和o彼此独立地表示0或1，条件是如果m是0，则Y和相邻C原子之间的虚线表示键，Y是CH或三价杂原子，如果m是1，则虚线 Y与相邻C原子之间的直线不存在且Y为CH 2或二价杂原子，如果o为0，则X与相邻C原子之间的虚线表示键，X为CH或三价杂原子，如果o为1 则X与相邻C原子之间的虚线不存在，X为CH 2或二价杂原子; A表示（CH 3 CR 4）p且Q表示（CR 9 R 10）n; n和p彼此独立地表示0或1; R6，R7，R13和R14彼此独立地表示氢，卤素，（C1-4）烷基，（C1-4）烷基SO2，SO3H，羧基，（C1-4）烷氧基羰基，（C1-4）烷氧基，OH 或NR15R16; R1，R2，R3，R4，R9，R10，R11和R12彼此独立地表示氢，（C1-4）烷基，羧基，（C1-4）烷氧基羰基或（C1-4）烷氧基，或当X 那么R1和R2也可以是OH或NR15R16，或当Y是CH或CH2时R11，R12也可以是OH或NR15R16; R5，R8，R15和R16彼此独立地为氢，（C1-4）烷基，（C1-4）烷氧基，R17O-C（O） - （C1-4）烷基或（反应性基团） - （C1- 4）烷基; R 17表示氢或（C 1-4）烷基; 包含这种化合物的组合物，制备式（I）化合物的方法，在脑中标记靶结构，特别是淀粉样蛋白斑的方法，用于鉴定阿尔茨海默氏病的方法，式I化合物作为近红外显影剂和包含通过反应性基团与生物分子共价连接的式（I）化合物的共轭物。

10. 发明申请

WO2003092701A2 NEW USES OF SUBSTITUTED AMINOALKANEPHOSPHONIC ACIDS 审中-公开
标题翻译：取代的氨基嘌呤磷酸的新用途
公开(公告)号：WO2003092701A2
公开(公告)日：2003-11-13
申请号：PCT/EP2003/004466
申请日：2003-04-29
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , LINGENHÖHL, Kurt , AUBERSON, Yves , FOX, Alyson , NEIJT, Hans, Ch. , KALKMAN, Hans, O.
发明人： LINGENHÖHL, Kurt , AUBERSON, Yves , FOX, Alyson , NEIJT, Hans, Ch. , KALKMAN, Hans, O.
IPC分类号： A61K31/675
CPC分类号： A61K31/675
摘要： The present invention relates the use of substituted aminoalkanephosphonic acids in treating neuropathic pain, affective and attention disorders, schizophrenia, tinnitus, myopia and other ocular disorders.
摘要翻译：本发明涉及取代的氨基烷基膦酸在治疗神经性疼痛，情感和注意障碍，精神分裂症，耳鸣，近视和其他眼部疾病中的用途。

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