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1. 发明申请

WO2008122513A1 HETEROCYCLES AS OREXIN ANTAGONISTS 审中-公开
标题翻译：杂交体作为OREXIN拮抗剂
公开(公告)号：WO2008122513A1
公开(公告)日：2008-10-16
申请号：PCT/EP2008/053545
申请日：2008-03-26
申请人： F. HOFFMANN-LA ROCHE AG , GOBBI, Luca , KNUST, Henner , MALHERBE, Parichehr , NETTEKOVEN, Matthias , PINARD, Emmanuel , ROCHE, Olivier , ROGERS-EVANS, Mark
发明人： GOBBI, Luca , KNUST, Henner , MALHERBE, Parichehr , NETTEKOVEN, Matthias , PINARD, Emmanuel , ROCHE, Olivier , ROGERS-EVANS, Mark
IPC分类号： C07D471/04 , C07D495/04 , A61K31/4365 , A61K31/437 , A61K31/4375 , A61P25/00 , A61P43/00
CPC分类号： C07D471/04 , C07D495/04
摘要： The present invention relates to compounds of formula (I) wherein R 1 /R 2 are independently from each other hydrogen or lower alkyl; R 3 is independently from the number of substituents hydrogen, halogen, lower alkyl, lower alkyl substituted by halogen, lower alkoxy or lower alkoxy substituted by halogen; R 4 is halogen, lower alkyl, lower alkyl substituted by halogen, lower alkoxy or lower alkoxy substituted by halogen; hetaryl is a one or two membered heteroaromatic ring, connected to the carbon atoms of the piperidine group selected from the group consisting of (II), (II), (IV) or (V) or to pharmaceutically suitable acid addition salts, optically pure enantiomers, racemates or diastereomeric mixtures thereof. It has been found that the compounds of formula I are orexin receptor antagonists and the related compounds may be useful in the treatment of disorders, in which orexin pathways are involved like sleep disorders.
摘要翻译：本发明涉及式（I）化合物，其中R 1和R 2彼此独立地为氢或低级烷基; R 3独立于取代基的数目，氢，卤素，低级烷基，被卤素取代的低级烷基，被卤素取代的低级烷氧基或低级烷氧基; R 4是卤素，低级烷基，被卤素取代的低级烷基，被卤素取代的低级烷氧基或低级烷氧基; 杂芳基是与选自（II），（II），（IV）或（V）的哌啶基团的碳原子连接的一个或两个元杂芳环，或者与药学上合适的酸加成盐，光学上纯的对映异构体，外消旋体或非对映体混合物。已经发现，式I化合物是食欲素受体拮抗剂，并且相关化合物可用于治疗其中食欲素途径如睡眠障碍的疾病。

2. 发明申请

WO2008110488A1 MALONAMIDES AS OREXIN ANTAGONISTS 审中-公开
标题翻译：马洛康作为OREXIN ANTAGONISTS
公开(公告)号：WO2008110488A1
公开(公告)日：2008-09-18
申请号：PCT/EP2008/052639
申请日：2008-03-05
申请人： F. HOFFMANN-LA ROCHE AG , GOBBI, Luca , KNUST, Henner , MALHERBE, Parichehr , NETTEKOVEN, Matthias , PINARD, Emmanuel , ROCHE, Olivier , ROGERS-EVANS, Mark
发明人： GOBBI, Luca , KNUST, Henner , MALHERBE, Parichehr , NETTEKOVEN, Matthias , PINARD, Emmanuel , ROCHE, Olivier , ROGERS-EVANS, Mark
IPC分类号： C07C233/08 , C07C233/15 , C07C233/22 , A61K31/167
CPC分类号： C07C233/29 , C07C233/15 , C07C233/32 , C07C233/88 , C07C2601/02 , C07C2601/08 , C07D211/16 , C07D211/46 , C07D213/40 , C07D213/75 , C07D295/185 , C07D309/14
摘要： The present invention relates to compounds of formula wherein Ar 1 and Ar 2 are independently from each other unsubstituted or substituted aryl or heteroaryl; R 1 /R 2 are independently from each other hydrogen, lower alkyl, lower alkyl substituted by halogen, -(CH 2 ) o -O-lower alkyl, -(CH 2 ) o -N-(lower alkyl) 2 , (CH 2 )p -cycloalkyl, (CH 2 ) p -heterocycloalkyl, (CH 2 ) p -aryl, (CH 2 ) p -heteroaryl, which rings may be substituted by R, or R 1 and R 2 may form together with the N-atom to which they are attached a heterocyclic ring, optionally with further ring-heteroatoms selected from N, O or S, which ring may be substituted by R; R is halogen, lower alkyl, lower alkyl substituted by halogen, lower alkoxy or lower alkoxy substituted by halogen; R 3 is hydrogen or lower alkyl; n is O, 1, 2, 3 or 4; o is 1, 2 or 3; P is 0, 1 or 2; or to pharmaceutically suitable acid addition salts, optically pure enantiomers, racemates or diastereomeric mixtures thereof. It has been found that the compounds of formula I are orexin receptor antagonists and the related compounds may be useful in the treatment of disorders, in which orexin pathways are involved like sleep disorders.
摘要翻译：本发明涉及下式的化合物，其中Ar 1和Ar 2 2彼此独立地为未取代或取代的芳基或杂芳基; R 1和R 2彼此独立地为氢，低级烷基，被卤素取代的低级烷基， - （CH 2 CH 2） -O-低级烷基， - （CH 2）2 - （低级烷基）2 - ， - （CH 3） SUB> 2

3. 发明申请

WO2008107335A1 AMINOAMIDES AS OREXIN ANTAGONISTS 审中-公开
标题翻译： AMINOAMIDES作为OREXIN ANTAGONISTS
公开(公告)号：WO2008107335A1
公开(公告)日：2008-09-12
申请号：PCT/EP2008/052245
申请日：2008-02-25
申请人： F. HOFFMANN-LA ROCHE AG , GOBBI, Luca , KNUST, Henner , MALHERBE, Parichehr , NETTEKOVEN, Matthias , PINARD, Emmanuel , ROCHE, Olivier , ROGERS-EVANS, Mark
发明人： GOBBI, Luca , KNUST, Henner , MALHERBE, Parichehr , NETTEKOVEN, Matthias , PINARD, Emmanuel , ROCHE, Olivier , ROGERS-EVANS, Mark
IPC分类号： C07C237/06 , C07D213/36 , A61K31/16
CPC分类号： C07D213/36 , A61K9/2018 , A61K9/4858 , C07C237/20 , C07C2601/02 , C07C2601/04
摘要： The present invention relates to compounds of formula (I) wherein Ar 1 , Ar 2 and Ar 3 are independently from each other unsubstituted or substituted aryl or heteroaryl; R 1 , R 2 and R 3 are independently from each other hydroxy, halogen, lower alkyl, lower alkyl substituted by halogen, lower alkoxy, lower alkoxy substituted by halogen, cyano, 3-hydroxy-oxetan-3-yl, SO 2 -lower alkyl or di-lower alkyl amino; R 4 /R 5 are independently from each other hydrogen, lower alkyl, lower alkyl substituted by halogen, lower alkyl substituted by hydroxy, -(CH 2 ) o -O-lower alkyl, -(CH 2 ) o -N-(lower alkyl) 2 , (CH 2 ) p -cycloalkyl, (CH 2 ) p -aryl, which aryl ring may be substituted by halogen, or R 4 and R 5 may form together with the N-atom to which they are attached a heterocyclic ring, optionally with further ring-heteroatoms selected from N, O or S; R 6 is hydrogen or lower alkyl; R 7 is hydrogen or lower alkyl; R 8 is hydrogen or cyano; n is 0, 1, 2 or 3; o is 1, 2 or 3; p is 0, 1 or 2; or to pharmaceutically suitable acid addition salts, optically pure enantiomers, racemates or diastereomeric mixtures thereof. It has been found that the compounds of formula (I) are orexin receptor antagonists and the related compounds may be useful in the treatment of disorders, in which orexin pathways are involved like sleep disorders.
摘要翻译：本发明涉及式（I）化合物，其中Ar 1，Ar 2和Ar 3彼此独立地为未取代或取代的芳基或杂芳基; R 1，R 2和R 3彼此独立地为羟基，卤素，低级烷基，被卤素取代的低级烷基，低级烷氧基，由卤素取代的低级烷氧基，氰基，3-羟基 - 氧杂环丁烷-3-基，SO 2 - 低级烷基或二 - 低级烷基氨基; R 4和R 5彼此独立地为氢，低级烷基，被卤素取代的低级烷基，被羟基取代的低级烷基， - （CH 2） -O - 低级烷基， - （CH 2）2 - （低级烷基）2 - （CH 2）2 - 环烷基，（CH 2）n - 芳基，该芳基环（CH 2）可以被卤素取代，或者R 4和R 5可以与它们所连接的N-原子一起形成杂环，任选地与另外的选择的杂环杂原子一起形成来自N，O或S; R 6是氢或低级烷基; R 7是氢或低级烷基; R 8是氢或氰基; n为0,1,2或3; o是1,2或3; p为0,1或2; 或其药学上合适的酸加成盐，旋光纯对映异构体，外消旋体或非对映体混合物。已经发现式（I）化合物是食欲素受体拮抗剂，并且相关化合物可用于治疗其中食欲素途径参与睡眠障碍的病症。

4. 发明申请

WO2009100994A1 PIPERIDINE SULFONAMIDE DERIVATIVES 审中-公开
标题翻译：哌啶磺酰胺衍生物
公开(公告)号：WO2009100994A1
公开(公告)日：2009-08-20
申请号：PCT/EP2009/051135
申请日：2009-02-02
申请人： F. HOFFMANN-LA ROCHE AG , KNUST, Henner , NETTEKOVEN, Matthias , PINARD, Emmanuel , ROCHE, Olivier , ROGERS-EVANS, Mark
发明人： KNUST, Henner , NETTEKOVEN, Matthias , PINARD, Emmanuel , ROCHE, Olivier , ROGERS-EVANS, Mark
IPC分类号： C07D211/96 , C07D401/06 , A61K31/54 , A61K31/4545 , A61P25/00
CPC分类号： C07D401/06 , C07D211/96
摘要： The present invention relates to piperidine sulphonamide derivatives of formula (I) wherein Ar 1 , Ar 2 , R 1 , R 2 , m and n are as defined in the description and claims, or pharmaceutically suitable acid addition salts thereof. The compounds of formula I are orexin receptor antagonists and the related compounds may be useful in the treatment of sleep apnea, narcolepsy, insomnia, parasomnia, jet lag syndrome, circadian rhythms disorder or sleep disorders associated with neurological diseases.
摘要翻译：本发明涉及式（I）的哌啶磺酰胺衍生物，其中Ar1，Ar2，R1，R2，m和n如说明书和权利要求中所定义，或其药学上合适的酸加成盐。式I化合物是食欲蛋白受体拮抗剂，相关化合物可用于治疗睡眠呼吸暂停，发作性睡病，失眠，睡眠不足，时差综合症，昼夜节律障碍或与神经疾病相关的睡眠障碍。

5. 发明申请

WO2009092642A1 SULFONAMIDES AS OREXIN ANTAGONISTS 审中-公开
标题翻译： SULFONAMIDES作为OREXIN拮抗剂
公开(公告)号：WO2009092642A1
公开(公告)日：2009-07-30
申请号：PCT/EP2009/050272
申请日：2009-01-12
申请人： F. HOFFMANN-LA ROCHE AG , KNUST, Henner , NETTEKOVEN, Matthias , PINARD, Emmanuel , ROCHE, Olivier , ROGERS-EVANS, Mark
发明人： KNUST, Henner , NETTEKOVEN, Matthias , PINARD, Emmanuel , ROCHE, Olivier , ROGERS-EVANS, Mark
IPC分类号： C07D207/06 , C07D207/08 , C07D211/16 , A61P25/00 , A61K31/4015
CPC分类号： C07D207/06 , C07D207/08 , C07D211/16
摘要： The present invention is concerned with novel sulfonamides of formula wherein R 1 , R 2 , R 3 and n are as described in the description and claims. The compounds are orexin receptor antagonists may be useful in the treatment of disorders, in which orexin pathways are involved.
摘要翻译：本发明涉及新型的具有下式的磺酰胺，其中R1，R2，R3和n如说明书和权利要求中所述。化合物是食欲素受体拮抗剂可用于治疗其中涉及食欲素途径的病症。

6. 发明申请

WO2009080533A1 HETEROARYL DERIVATIVES AS OREXIN RECEPTOR ANTAGONISTS 审中-公开
标题翻译：异丙肾上腺素衍生物作为OREXIN受体拮抗剂
公开(公告)号：WO2009080533A1
公开(公告)日：2009-07-02
申请号：PCT/EP2008/067273
申请日：2008-12-11
申请人： F. HOFFMANN-LA ROCHE AG , KNUST, Henner , NETTEKOVEN, Matthias , PINARD, Emmanuel , ROCHE, Olivier , ROGERS-EVANS, Mark
发明人： KNUST, Henner , NETTEKOVEN, Matthias , PINARD, Emmanuel , ROCHE, Olivier , ROGERS-EVANS, Mark
IPC分类号： C07D401/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D498/04 , A61K31/4025 , A61P25/00
CPC分类号： C07D413/12 , C07D401/12 , C07D409/14 , C07D413/14 , C07D417/12 , C07D417/14 , C07D498/04
摘要： The present invention relates to compounds of Formula (I), wherein Ar is an unsubstituted or substituted aryl or heteroaryl group, wherein the aryl and the heteroaryl group may be substituted by one or more substituents R 2 ; R 2 is hydroxy, halogen, lower alkyl, lower alkyl substituted by halogen, lower alkoxy, lower alkoxy substituted by halogen, C(O)-lower alkyl, nitro, NR , R ,, , cyano, S-lower alkyl, SO 2 -lower alkyl, cycloalkyl, heterocycloalkyl, phenyloxy, benzyloxy, phenyl, NH-phenyl or heteroaryl, wherein the phenyl and heteroaryl group is unsubstituted or substituted by one or more substituents selected from lower alkyl or halogen; R , /R ,, are independently from each other hydrogen or lower alkyl; R 1 is hydrogen or lower alkyl; Het is a heteroaryl group, unsubstituted or substituted by one or more substituents selected from R 3 ; R 3 is hydroxy, halogen, =O, lower alkyl, lower alkyl substituted by halogen, lower alkoxy, phenyl, lower alkoxy substituted by halogen, nitro, cyano, SO 2 -lower alkyl, cycloalkyl or heterocycloalkyl; n is 1 or 2; or to pharmaceutically suitable acid addition salts, optically pure enantiomers, racemates or diastereomeric mixtures thereof. It has been found that the compounds of formula (I) are orexin receptor antagonists and the related compounds may be useful in the treatment of sleep apnea, narcolepsy, insomnia, parasomnia, jet lag syndrome, circadian rhythms disorder or sleep disorders associated with neurological diseases.
摘要翻译：本发明涉及式（I）化合物，其中Ar为未取代或取代的芳基或杂芳基，其中芳基和杂芳基可被一个或多个取代基R2取代; R 2是羟基，卤素，低级烷基，被卤素取代的低级烷基，低级烷氧基，被卤素取代的低级烷氧基，C（O） - 低级烷基，硝基，NR，R'，氰基，S-低级烷基，SO 2 - 烷基，环烷基，杂环烷基，苯氧基，苄氧基，苯基，NH-苯基或杂芳基，其中苯基和杂芳基是未取代的或被一个或多个选自低级烷基或卤素的取代基取代; R 1 / R 3彼此独立地为氢或低级烷基; R1是氢或低级烷基; Het是未取代或被一个或多个选自R 3的取代基取代的杂芳基; R 3是羟基，卤素，= O，低级烷基，被卤素取代的低级烷基，低级烷氧基，苯基，被卤素，硝基，氰基，SO 2 - 低级烷基，环烷基或杂环烷基取代的低级烷氧基; n为1或2; 或其药学上合适的酸加成盐，旋光纯对映异构体，外消旋体或非对映体混合物。已经发现，式（I）化合物是食欲肽受体拮抗剂，相关化合物可用于治疗睡眠呼吸暂停，发作性睡病，失眠，睡眠，时差综合征，昼夜节律障碍或与神经系统疾病相关的睡眠障碍。

7. 发明申请

WO2010012620A1 PYRROLIDIN-3-YLMETHYL-AMINE AS OREXIN ANTAGONISTS 审中-公开
标题翻译：吡咯烷-3-基甲基胺作为OREXIN拮抗剂
公开(公告)号：WO2010012620A1
公开(公告)日：2010-02-04
申请号：PCT/EP2009/059271
申请日：2009-07-20
申请人： F. HOFFMANN-LA ROCHE AG , KNUST, Henner , NETTEKOVEN, Matthias , PINARD, Emmanuel , ROCHE, Olivier , ROGERS-EVANS, Mark
发明人： KNUST, Henner , NETTEKOVEN, Matthias , PINARD, Emmanuel , ROCHE, Olivier , ROGERS-EVANS, Mark
IPC分类号： C07D403/12 , C07D413/12 , C07D413/14 , C07D417/12 , A61K31/423 , A61P25/00
CPC分类号： C07D413/12 , C07D403/12 , C07D413/14 , C07D417/12
摘要： The present invention is concerned with compounds of formula (I) wherein R 1 , R 2 , Ar, Hetaryl, m and n are as described in the description and claims. The compounds are orexin receptor antagonists may be useful in the treatment of disorders, in which orexin pathways are involved.
摘要翻译：本发明涉及式（I）的化合物，其中R 1，R 2，Ar，杂芳基，m和n如说明书和权利要求中所述。化合物是食欲素受体拮抗剂可用于治疗其中涉及食欲素途径的病症。

8. 发明申请

WO2009153180A1 HETEROAROMATIC MONOAMIDES AS OREXININ RECEPTOR ANTAGONISTS 审中-公开
标题翻译：作为OREXININ受体拮抗剂的异种单体
公开(公告)号：WO2009153180A1
公开(公告)日：2009-12-23
申请号：PCT/EP2009/056992
申请日：2009-06-08
申请人： F. HOFFMANN-LA ROCHE AG , KNUST, Henner , NETTEKOVEN, Matthias , PINARD, Emmanuel , ROCHE, Olivier , ROGERS-EVANS, Mark
发明人： KNUST, Henner , NETTEKOVEN, Matthias , PINARD, Emmanuel , ROCHE, Olivier , ROGERS-EVANS, Mark
IPC分类号： C07D213/40 , C07D213/56 , C07D213/75 , C07D215/38 , C07D231/40 , C07D261/08 , C07D277/46 , C07D333/20 , C07D401/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07K5/02 , A61K31/44 , A61K31/4406
CPC分类号： C07D213/40 , C07D213/56 , C07D213/75 , C07D215/38 , C07D231/40 , C07D261/08 , C07D277/46 , C07D333/20 , C07D401/12 , C07D405/12 , C07D409/12 , C07D413/12
摘要： The present invention is concerned with novel sulfonamides of formula I wherein R 1 , R 2 , R 3 , R 4 , R 5 , Ar, Ar 1 , Ar 2 , n, o and p are as described in the description and claims. The compounds are orexin receptor antagonists may be useful in the treatment of disorders, in which orexin pathways are involved.
摘要翻译：本发明涉及式I的新型磺酰胺，其中R 1，R 2，R 3，R 4，R 5，Ar，Ar 1，Ar 2，n，o和p如说明书和权利要求中所述。化合物是食欲素受体拮抗剂可用于治疗涉及食欲素途径的病症。

9. 发明申请

WO2009016087A1 MONOAMIDE DERIVATIVES AS OREXIN RECEPTOR ANTAGONISTS 审中-公开
标题翻译：单酰胺衍生物作为OREXIN受体拮抗剂
公开(公告)号：WO2009016087A1
公开(公告)日：2009-02-05
申请号：PCT/EP2008/059697
申请日：2008-07-24
申请人： F. HOFFMANN-LA ROCHE AG , KNUST, Henner , NETTEKOVEN, Matthias , PINARD, Emmanuel , ROCHE, Olivier , ROGERS-EVANS, Mark
发明人： KNUST, Henner , NETTEKOVEN, Matthias , PINARD, Emmanuel , ROCHE, Olivier , ROGERS-EVANS, Mark
IPC分类号： C07C233/88 , C07C235/68 , C07C235/78 , C07D277/62 , C07D317/48 , A61K31/167 , A61K31/357 , A61K31/428 , A61P25/20
CPC分类号： C07D405/12 , C07C233/29 , C07C235/38 , C07C235/80 , C07C237/20 , C07C237/22 , C07C251/48 , C07C255/58 , C07C255/60 , C07C271/22 , C07D205/04 , C07D207/12 , C07D209/44 , C07D211/46 , C07D213/56 , C07D231/56 , C07D235/06 , C07D235/08 , C07D235/10 , C07D235/16 , C07D235/26 , C07D277/62 , C07D305/02 , C07D305/08 , C07D307/14 , C07D307/52 , C07D307/79 , C07D317/28 , C07D317/46 , C07D317/66 , C07D319/20 , C07D333/24 , C07D471/04 , C07D487/04 , C07D491/107
摘要： The present invention relates to compounds of formula (I), wherein Ar is aryl or heteroaryl; R 1 is hydrogen, halogen, lower alkyl, lower alkyl substituted by halogen, lower alkoxy, lower alkoxy substituted by halogen, cyano, SO 2 -lower alkyl or hydroxy; R 2 is hydrogen, halogen, lower alkyl, lower alkyl substituted by halogen, lower alkoxy, lower alkoxy substituted by halogen, cyano, S-lower alkyl, SO 2 -lower alkyl, NO 2 or hydroxy; R 3 is hydrogen, halogen, lower alkyl, lower alkyl substituted by halogen, lower alkoxy, -(CH 2 ) m -O-lower alkyl, lower alkoxy substituted by halogen, 3-hydroxy-oxetan-3-yl, cyano or SO 2 -lower alkyl; or if o is 2, R 3 may form in 3 and 4 position together with the carbon atoms to which they are attached an addional ring with the groups -O-CH 2 -O-, -O-CF 2 -CF 2 -O-, -N=CH-S-, -O-CF 2 -O-, -(CH 2 ) 4 -, -NH-C(O)-NH-, -O-(CH 2 ) 2 - or _(CH 2 ) 2 -O-; R 4 /R 5 are independently from each other hydrogen, -(CR" 2 ) m OH, lower alkyl, lower alkoxy, -NRR', or is -(CH 2 ) 0,1 -heterocycloalkyl, optionally substituted by hydroxy, or R 4 and R 5 are together =O or =N-OH,; R/R' are independently from each other hydrogen, lower alkyl, C(O)H, -(CR" 2 )m-OH, -(CR" 2 )m-NR" 2 , -(CR" 2 ) m -NR"-C(O)-lower alkyl, -(CR" 2 ) m -O-lower alkyl, -(CR" 2 ) m -O-lower alkenyl, -C(O)O-lower alkyl, -C(O)-CR" 2 -NH-C(O)O-lower alkyl, -C(O)-CR" 2 -NR" 2 , or is -(CH 2 ) 0,1 -heterocycloalkyl or -(CH 2 ) 0,1 -furan-2-yl; R" are independently from each other hydrogen, lower alkoxy, phenyl or lower alkyl; n is 1, 2, 3 or 4; o is 1, 2 or 3; p is 1, 2 or 3; m is 1, 2 or 3; or to pharmaceutically suitable acid addition salts, optically pure enantiomers, racemates or diastereomeric mixtures thereof. The compounds of formula (I) may be used for example for the treatment of the sleep disorders, which are sleep apnea, narcolepsy, insomnia, parasomnia, jet lag syndrome, circadian rhythms disorder or sleep disorders associated with neurological diseases.
摘要翻译：本发明涉及式（I）化合物，其中Ar为芳基或杂芳基; R 1为氢，卤素，低级烷基，被卤素取代的低级烷基，低级烷氧基，被卤素取代的低级烷氧基，氰基，SO 2 - 低级烷基或羟基; R 2是氢，卤素，低级烷基，被卤素取代的低级烷基，低级烷氧基，被卤素取代的低级烷氧基，氰基，S-低级烷基，SO 2 - 低级烷基，NO 2或羟基; R 3是氢，卤素，低级烷基，被卤素取代的低级烷基，低级烷氧基， - （CH 2）m -O-低级烷基，被卤素取代的低级烷氧基，3-羟基 - 氧杂环丁烷-3-基，氰基或SO 2 - 低级烷基; 或者如果o是2，则R3可以与它们所连接的碳原子一起形成3和4位与-O-CH 2 -O-，-O-CF 2 -CF 2 -O-，-N = CH-S-，-O-CF2-O-， - （CH2）4-，-NH-C（O）-NH-，-O-（CH2）2-或_（CH2） R 4 / R 5彼此独立地为氢， - （CR“2）mOH，低级烷基，低级烷氧基，-NRR'或为任选被羟基取代的 - （CH 2）0,1 - 杂环烷基，或R 4和R 5为一起= O或= N-OH; R / R'彼此独立地为氢，低级烷基，C（O）H， - （CR“2）m -OH， - （CR”2）m -NR“ 2， - （CR“2）m-NR”-C（O） - 低级烷基， - （CR“2）mO-低级烷基， - （CR”2）mO-低级烯基，-C（O）低级烷基，-C（O）-CR“2-NH-C（O）O-低级烷基，-C（O）-CR”2 -NR“2或为 - （CH 2） - （CH 2）0,1 - 呋喃-2-基; R“彼此独立地为氢，低级烷氧基，苯基或低级烷基; n为1,2,3或4; o是1,2或3; p为1,2或3; m为1,2或3; 或其药学上合适的酸加成盐，旋光纯对映异构体，外消旋体或非对映体混合物。式（I）的化合物可用于例如睡眠呼吸暂停，发作性睡眠，失眠，睡眠睡眠，时差综合征，昼夜节律障碍或与神经疾病相关的睡眠障碍的睡眠障碍。

10. 发明申请

WO2008052899A1 ETHER DERIVATIVES DUAL MODULATORS OF THE 5-HT2A AND D3 RECEPTORS 审中-公开
标题翻译： 5-HT2A和D3受体的二级衍生物双重调节剂
公开(公告)号：WO2008052899A1
公开(公告)日：2008-05-08
申请号：PCT/EP2007/061253
申请日：2007-10-22
申请人： F. HOFFMANN-LA ROCHE AG , GOBBI, Luca Claudio , JAESCHKE, Georg , ROCHE, Olivier , RODRIGUEZ SARMIENTO, Rosa Maria , STEWARD, Lucinda
发明人： GOBBI, Luca Claudio , JAESCHKE, Georg , ROCHE, Olivier , RODRIGUEZ SARMIENTO, Rosa Maria , STEWARD, Lucinda
IPC分类号： C07D211/46 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/12 , C07D413/12 , A61P25/00 , A61K31/445 , A61K31/4525 , A61K31/453 , A61K31/4535 , A61K31/454 , A61K31/4709
CPC分类号： C07D401/12 , C07D211/46 , C07D401/14 , C07D405/12 , C07D409/12 , C07D413/12
摘要： The present invention relates to dual modulators of the serotonin 5-HT 2a and dopamine D 3 receptors which are represented by the general formula (I) wherein R 1 , R 2 and A are as defined in the specification, to a process for the manufacture thereof, as well as to pharmaceutically acceptable salts thereof for the manufacture of a medicament for the treatment or prevention of cognitive disorders, drug addiction, depression, anxiety, drug dependence, dementias, memory impairment, psychotic disorders comprising schizophrenia, schizoaffective disorders, bipolar disease, mania, psychotic depression, and psychoses comprising paranoia and delusions.
摘要翻译：本发明涉及由通式（I）表示的5-羟色胺5-HT 2a和多巴胺D 3 N 3受体的双重调节剂，其中R 1， / SUP>，R 2和A如说明书中所定义，其制备方法及其药学上可接受的盐用于制备用于治疗或预防认知障碍，药物成瘾，抑郁，焦虑，药物依赖，痴呆，记忆障碍，包括精神分裂症，分裂情感障碍，双相性精神障碍，躁狂症，精神病性抑郁症和包括偏执狂和妄想的精神病的精神障碍。

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