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1. 发明申请

WO2011048150A1 USE OF 1H-QUINAZOLINE-2,4-DIONES 审中-公开
标题翻译：使用1H-喹唑啉-2,4-二酮
公开(公告)号：WO2011048150A1
公开(公告)日：2011-04-28
申请号：PCT/EP2010/065805
申请日：2010-10-20
申请人： NOVARTIS AG , ALLGEIER, Hans , AUBERSON, Yves , AVRAMEAS, Alexandre , BLAETTLER, Thomas , CARCACHE, David , FLOERSHEIM, Philipp , FROESTL, Wolfgang , GUIBOURDENCHE, Christel , KALKMAN, Hans, O. , KALLEN, Joerg , KOLLER, Manuel , LINGENHÖHL, Kurt , MA, Shenglin , MATTES, Henri , NOZULAK, Joachim , ORAIN, David , RENAUD, Johanne , STROHMAIER, Christine
发明人： ALLGEIER, Hans , AUBERSON, Yves , AVRAMEAS, Alexandre , BLAETTLER, Thomas , CARCACHE, David , FLOERSHEIM, Philipp , FROESTL, Wolfgang , GUIBOURDENCHE, Christel , KALKMAN, Hans, O. , KALLEN, Joerg , KOLLER, Manuel , LINGENHÖHL, Kurt , MA, Shenglin , MATTES, Henri , NOZULAK, Joachim , ORAIN, David , RENAUD, Johanne , STROHMAIER, Christine
IPC分类号： A61K31/517 , A61P25/08
CPC分类号： A61K31/517 , A61K31/34
摘要： The invention concerns the use of competitive AMPA receptor antagonists for the treatment, prevention or delay of progression of Rasmussen's encephalitis and/or certain forms of epilepsy.
摘要翻译：本发明涉及竞争性AMPA受体拮抗剂用于治疗，预防或延缓拉斯穆森脑炎和/或某些形式的癫痫发展的用途。

2. 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。

3. 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。

4. 发明申请

WO9902497A3 PYRIDINE DERIVATIVES 审中-公开
标题翻译：吡啶衍生物
公开(公告)号：WO9902497A3
公开(公告)日：1999-04-01
申请号：PCT/EP9804266
申请日：1998-07-09
申请人： NOVARTIS AG , NOVARTIS ERFIND VERWALT GMBH , SIBIA NEUROSCIENCES INC , ALLGEIER HANS , AUBERSON YVES , BIOLLAZ MICHEL , COSFORD NICHOLAS DAVID , GASPARINI FABRIZIO , HECKENDORN ROLAND , JOHNSON EDWIN CARL , KUHN RAINER , VARNEY MARK ANDREW , VELICELEBI GOENUEL
发明人： ALLGEIER HANS , AUBERSON YVES , BIOLLAZ MICHEL , COSFORD NICHOLAS DAVID , GASPARINI FABRIZIO , HECKENDORN ROLAND , JOHNSON EDWIN CARL , KUHN RAINER , VARNEY MARK ANDREW , VELICELEBI GOENUEL
IPC分类号： A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4418 , A61K31/4427 , A61K31/443 , A61K31/4439 , A61K31/444 , A61K31/4545 , A61K31/4709 , A61K31/496 , A61K31/497 , A61K31/506 , A61P9/10 , A61P21/02 , A61P21/04 , A61P25/00 , A61P25/04 , A61P25/08 , A61P25/14 , A61P25/16 , A61P25/22 , A61P25/24 , A61P25/28 , A61P43/00 , C07D213/16 , C07D213/26 , C07D213/30 , C07D213/50 , C07D213/52 , C07D213/53 , C07D213/55 , C07D213/56 , C07D213/57 , C07D213/65 , C07D213/74 , C07D213/79 , C07D213/80 , C07D213/81 , C07D213/82 , C07D213/84 , C07D213/89 , C07D215/12 , C07D401/06 , C07D401/10 , C07D401/12 , C07D401/14 , C07D405/06 , C07D409/06 , C07D413/06 , C07F7/08
CPC分类号： C07D213/06 , C07D213/16 , C07D213/26 , C07D213/30 , C07D213/50 , C07D213/52 , C07D213/53 , C07D213/55 , C07D213/56 , C07D213/57 , C07D213/65 , C07D213/74 , C07D213/79 , C07D213/80 , C07D213/81 , C07D213/82 , C07D213/84 , C07D213/89 , C07D215/12 , C07D401/06 , C07D401/10 , C07D405/06 , C07D409/06 , C07F7/0812
摘要： Compounds of the formula (I), wherein X and R1 to R5 are as defined in the description, are useful for treating disorders mediated full or in part by mGluR5.
摘要翻译：式（I）化合物，其中X和R 1至R 5如说明书中所定义，可用于治疗全部或部分由mGluR5介导的病症。

5. 发明申请

WO2005014517A3 NOVEL DIBENZO[B,F]OXEPINE-10-CARBOXAMIDES AND PHARMACEUTICAL USES THEREOF 审中-公开
标题翻译：新的DIBENZO [B，F] OXEPINE-10-CARBOXAMIDES及其药物用途
公开(公告)号：WO2005014517A3
公开(公告)日：2005-04-28
申请号：PCT/EP2004008283
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： C07C235/82 , C07D313/14 , C07D405/12 , C07D407/12 , C07D413/12 , C07D453/02 , C07D491/04 , C07C235/40 , A61K31/165 , A61K31/335 , A61K31/395 , A61P25/28 , C07D267/20
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：本发明涉及式（I）的化合物，其中X是O，NH，N（C 1-4）烷基，CO或CHOH，Y是CH或N，A和B各自是氢或一起在（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，R 3为CH（R e）CONR a R b或（CH 2）n NR c，R d，n为0,1或2，R a，R b，R c和R d独立地为氢或任选取代的（C 1-8）（C 1-7）环烷基，（C 3-7）环烷基（C 1-4）烷基，（C 7-9）双环烷基，1-氮杂 - （C 7-9）双环烷基，芳基，（C 1-4）烷基或杂环基，或者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，R e是（C 1-8）烷基，（C 1-4）烷基，（C 3-7）环烷基或（C 3-7）环烷基（C 1-4）烷基，且R 4，，（C1-4 ）烷基，（C 1-4）烷氧基，（C 1-4）烷基-SO 2，氰基，硝基或卤素; 涉及制备式（I）化合物的方法，其作为药物的用途，特别是用于治疗与β-淀粉状蛋白产生和/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（I）的结构。

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

WO1998017672A1 SUBSTITUTED AMINOALKANE PHOSPHONIC ACIDS 审中-公开
标题翻译：取代aminoalkanephosphonic酸
公开(公告)号：WO1998017672A1
公开(公告)日：1998-04-30
申请号：PCT/EP1997005843
申请日：1997-10-22
申请人： NOVARTIS AG , ACKLIN, Pierre , ALLGEIER, Hans , AUBERSON, Yves , OFNER, Silvio , VEENSTRA, Siem, Jacob
发明人： NOVARTIS AG
IPC分类号： C07F09/6509
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.
摘要翻译：式（I）其中R1是羟基或脂族，芳脂族或芳族基团的化合物; X为二价脂族，脂环族，脂环族 - 脂族，芳脂族，heteroarylaliphatic或芳族基团; R 2表示氢或脂族或芳脂族基团，alk是低级亚烷基; 和R 3，R 4和R 5独立地是氢，低级烷基，卤素，三氟甲基，氰基或硝基; 和它们的盐可被用于其中兴奋性氨基酸受体的阻断响应的病理状况的治疗，以及用于生产药物制剂。

9. 发明申请

WO1997008155A1 NOVEL 2,3-DIOXO-1,2,3,4-TETRAHYDRO-QUINOYXALINYL DERIVATIVES 审中-公开
标题翻译：新的2,3-二氧代-1,2,3,4-四氢喹啉衍生物
公开(公告)号：WO1997008155A1
公开(公告)日：1997-03-06
申请号：PCT/EP1996003644
申请日：1996-08-19
申请人： NOVARTIS AG , ACKLIN, Pierre , ALLGEIER, Hans , AUBERSON, Yves , BIOLLAZ, Michel , MORETTI, Robert , OFNER, Silvio , VEENSTRA, Siem, Jacob
发明人： NOVARTIS AG
IPC分类号： C07D241/44
CPC分类号： C07D401/06 , C07D241/44 , C07D401/12 , C07D417/12 , C07F9/650994
摘要： 2,3-Dioxo-1,2,3,4-tetrahydro-quinoxalinyl derivatives of formula (I), wherein one of the radicals R1, and R2 is a group R5 and the other is a group of formula -CH(R6)-alk-R7 (Ia), -alk-CH(R6-R7 (Ib), -alk-N(R8)-X-R7 (Ic), -alk-N (R8)(R9)-X-R7A (Id), -alk-O-X-R7 (Ie) or -alk-S-X-R7 (If), R3, R4 and R5 are each independently of the others hydrogen, lower alkyl, halogen, trifluoromethyl, cyano or nitro, R6 is unsubstituted or lower alkylated and/or lower alkanoylated amino, R7 is hydrogen; an aliphatic, cycloaliphatic or heterocycloaliphatic radical; cyano; acyl derived from carbonic acid or from a semiester or semiamide of carbonic acid, from sulfuric acid or from an aliphatic or aromatic sulfonic acid or from phosphoric acid or from a phosphonic acid ester; amino that is unsubtituted or aliphatically or araliphatically substituted and/or substituted by aliphatic, araliphatic or aromatic acyl; or an aromatic or heteroaromatic radical, R8 is hydrogen; an aliphatic or araliphatic radical; or acyl derived from an aliphatic or araliphatic carboxylic acid or from an aliphatic or araliphatic semiester of carbonic acid, or R7 and R8, together with X and the nitrogen atom bonding R8 and X, form an unsubstitued or substituted mono- or di-azaxycloalkyl, azoxacycloalkyl, azathiacycloalkyl or optionally oxidised thiacycloalkyl radical bonded via a nitrogen atom, or an unsubstituted or substituted, optionally partially hxdrogenated aryl or heteroaryl radical, R9 is an aliphatic or araliphatic radical, or R7, R8 and R9 together with X and the nitrogen atom bonding R8, R9 and X, form an unsubstituted or substituted quaternary heteroaryl radical bonded via the quaternary nitrogen atom, with A being the anion of a protonic acid, alk is lower alkylene, and X (unless, together with R7 and R8 and the nitrogen atom bonding R8 and X or together with the nitrogen atom bonding R8, R9 and X, it forms part of one of the mentioned ring systems) is a divalent aliphatic, cycloaliphatic or araliphatic radical or a direct bond, and the pharmaceutically acceptable salts thereof can be used in the preparation of a medicament for the treatment of pathological conditions that are responsive to blocking of AMPA, kainate and/or glycine binding sites of the NMDA receptor.
摘要翻译：式（I）的2,3-二氧代-1,2,3,4-四氢 - 喹喔啉基衍生物，其中基团R 1和R 2之一是基团R 5，另一个是式-CH（R 6） -alk-R7（Ia），-alk-CH（R6-R7（Ib））-alk-N（R8）-X-R7（Ic），-alk-N +（R8）（R9）-X -R7A - （Id），-alk-OX-R7（Ie）或-alk-SX-R7（If），R3，R4和R5各自独立地为氢，低级烷基，卤素，三氟甲基，氰基或硝基，R 6是未取代的或低级烷基化的和/或低级烷酰基化的氨基，R 7是氢;脂族，脂环族或杂环脂族基团;氰基;衍生自碳酸的酰基或来自碳酸的半酯或半酰胺，脂族或芳族磺酸或磷酸或膦酸酯;未取代或脂族或芳烃取代和/或被脂族或芳族酰基取代的氨基;或芳族或杂芳族基团，R 8为氢; 脂肪族或芳脂族辐射 CAL; 或衍生自脂族或芳脂族羧酸的酰基或来自碳酸或R 7和R 8的脂族或芳脂肪族半酯与X以及键合R 8和X的氮原子形成未取代或取代的单 - 或二 - 氮杂环烷基的酰基，氮杂环烷基，氮杂环烷基或任意氧化的经氮原子键合的硫代环烷基，或未取代或取代的，任选部分羟基化的芳基或杂芳基，R 9为脂族或芳脂族基，或者R 7，R 8和R 9与X和氮原子键合 R8，R9和X形成通过季氮原子键合的未取代或取代的季杂芳基，A 1是质子酸的阴离子，alk是低级亚烷基和X（除非与R 7和R 8一起键合R8和X的氮原子或与R8，R9和X键合的氮原子一起形成所述环系中一个的一部分）是二价脂族，脂环族或芳族脂肪族基团或直接键合，并且其药学上可接受的盐可用于制备用于治疗对阻断NMDA受体的AMPA，红藻氨酸和/或甘氨酸结合位点有反应的病理状况的药物。

10. 发明申请

WO1996026183A1 1-ARYL-2-ACYLAMINO-ETHANE COMPOUNDS AND THEIR USE AS NEUROKININ ESPECIALLY NEUROKININ 1 ANTAGONISTS 审中-公开
标题翻译： 1-ARYL-2-ACYLAMINO-ETHANE化合物及其作为神经元素特异性神经营养因子1拮抗剂
公开(公告)号：WO1996026183A1
公开(公告)日：1996-08-29
申请号：PCT/EP1996000555
申请日：1996-02-09
申请人： CIBA-GEIGY AG , GERSPACHER, Marc , VON SPRECHER, Andreas , ROGGO, Silvio , MAH, Robert , OFNER, Silvio , VEENSTRA, Siem, Jacob , BETSCHART, Claudia , AUBERSON, Yves , SCHILLING, Walter
发明人： CIBA-GEIGY AG
IPC分类号： C07C237/22
CPC分类号： C07D213/40 , C07C237/22 , C07C255/29 , C07C311/51 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2601/18 , C07D209/08 , C07D209/12 , C07D209/20 , C07D211/22 , C07D211/44 , C07D211/48 , C07D211/58 , C07D213/70 , C07D215/46 , C07D223/12 , C07D231/12 , C07D231/38 , C07D233/56 , C07D235/16 , C07D235/28 , C07D239/42 , C07D241/20 , C07D249/08 , C07D295/13 , C07D295/135 , C07D295/185 , C07D401/12 , C07D403/12 , C07D417/12 , C07D471/10
摘要： 1-Aryl-2-acylamino-ethane compounds of formula (I), wherein R1 is aryl or heteroaryl; R2 is hydrogen, lower alkyl or aryl-lower alkyl; R3 is hydrogen, lower alkyl, aryl or heteroaryl; R4 is aryl or heteroaryl; X is C1-C7alkylene, C2-C7 alkenyline or C4-C7 alkanedienylene, and Am is an unsubstituted or mono- or di-substituted amino group, a disubstituted amino group being understood as including also an amino group in which the amino nitrogen is bonded into a ring, or a salt thereof, have valuable pharmaceutical properties and are especially effective as NK1 antagonists. They are prepared in a manner known per se.
摘要翻译：式（I）的1-芳基-2-酰基氨基 - 乙烷化合物，其中R 1是芳基或杂芳基; R2是氢，低级烷基或芳基 - 低级烷基; R3是氢，低级烷基，芳基或杂芳基; R4是芳基或杂芳基; X是C 1 -C 7亚烷基，C 2 -C 7链烯基或C 4 -C 7链烷二烯基，并且Am是未取代或单取代或二取代的氨基，二取代的氨基也被理解为也包括其中氨基氮键合的氨基成环或其盐具有有价值的药物性质，并且作为NK1拮抗剂是特别有效的。它们是以本身已知的方式准备的。

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