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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

WO2010063610A1 PYRIDAZINONE DERIVATIVES 审中-公开
标题翻译：吡咯烷酮衍生物
公开(公告)号：WO2010063610A1
公开(公告)日：2010-06-10
申请号：PCT/EP2009/065692
申请日：2009-11-24
申请人： F. HOFFMANN-LA ROCHE AG , ALBERATI, Daniela , GOBBI, Luca , KOERNER, Matthias , KUHN, Bernd , PETERS, Jens-Uwe , RODRIGUEZ SARMIENTO, Rosa Maria , ROGERS-EVANS, Mark , RUDOLPH, Markus
发明人： ALBERATI, Daniela , GOBBI, Luca , KOERNER, Matthias , KUHN, Bernd , PETERS, Jens-Uwe , RODRIGUEZ SARMIENTO, Rosa Maria , ROGERS-EVANS, Mark , RUDOLPH, Markus
IPC分类号： C07D403/04 , C07D403/14 , C07D405/14 , A61P25/00 , A61K31/501
CPC分类号： C07D403/04 , C07D403/14 , C07D405/14
摘要： The present invention is concerned with novel pyridazinone derivatives of formula (I) wherein R 1 , R 2 , R 3 and R 4 are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit PDE10A and can be used as medicaments.
摘要翻译：本发明涉及式（I）的新的哒嗪酮衍生物，其中R 1，R 2，R 3和R 4如说明书和权利要求书中所定义，以及其生理上可接受的盐和酯。这些化合物抑制PDE10A，可用作药物。

5. 发明申请

WO2007093540A1 BENZOYL-PIPERIDINE DERIVATIVES AS 5HT2/D3 MODULATORS 审中-公开
标题翻译：作为5HT2 / D3调节剂的苯甲酰哌啶衍生物
公开(公告)号：WO2007093540A1
公开(公告)日：2007-08-23
申请号：PCT/EP2007/051160
申请日：2007-02-07
申请人： F. HOFFMANN-LA ROCHE AG , GOBBI, Luca , JAESCHKE, Georg , LUEBBERS, Thomas , ROCHE, Olivier , RODRIGUEZ SARMIENTO, Rosa Maria , STEWARD, Lucinda
发明人： GOBBI, Luca , JAESCHKE, Georg , LUEBBERS, Thomas , ROCHE, Olivier , RODRIGUEZ SARMIENTO, Rosa Maria , STEWARD, Lucinda
IPC分类号： C07D401/06 , C07D413/06 , C07D417/06 , C07C211/32 , A61K31/505 , A61P25/18
CPC分类号： C07D401/06 , C07D413/06 , C07D417/06
摘要： The present invention relates to compounds of the general formula (I) as dual modulators of the 5-HT 2a and D 3 receptors useful against CNS disorders, wherein A, R 1 , R 2 , n, p, q and r are as defined in the specification.
摘要翻译：本发明涉及作为可用于中枢神经系统疾病的5-HT 2a和D 3 N受体的双重调节剂的通式（I）的化合物，其中A， SUP> 1，R 2，n，p，q和r如说明书中所定义。

6. 发明申请

WO2009013212A2 DUAL MODULATORS OF 5-HT2A AND D3 RECEPTORS 审中-公开
标题翻译： 5-HT2A和D3受体的双重调节剂
公开(公告)号：WO2009013212A2
公开(公告)日：2009-01-29
申请号：PCT/EP2008/059356
申请日：2008-07-17
申请人： F. HOFFMANN-LA ROCHE AG , GOBBI, Luca , JAESCHKE, Georg , ROCHE, Olivier , RODRIGUEZ SARMIENTO, Rosa, Maria , STEWARD, Lucinda
发明人： GOBBI, Luca , JAESCHKE, Georg , ROCHE, Olivier , RODRIGUEZ SARMIENTO, Rosa, Maria , STEWARD, Lucinda
CPC分类号： C07D413/04 , C07D413/14
摘要： The present invention relates to compounds of the general formula (I), wherein R 1 , R 2 , X and n are as defined in the specification as dual modulators of the serotonin 5-HT 2a and dopamine D 3 receptors, their manufacture, pharmaceutical compositions containing them and their use as medicaments. Compounds of general formula (I) have high affinity for the dopamine D3 and serotonin (5-Hydroxytryptamine; 5-HT) 5-HT 2A receptors and are effective in the treatment of psychotic disorders, as well as other diseases such as depression and anxiety, drug dependence, dementias and memory impairment.
摘要翻译：本发明涉及通式（I）的化合物，其中R1，R2，X和n如说明书中所定义，作为5-羟色胺5-HT2a和多巴胺D3受体的双重调节剂，其制备方法，含有它们的药物组合物和用作药物。通式（I）的化合物对多巴胺D3和5-羟色胺（5-羟色胺，5-HT）5-HT 2A受体具有高亲和力，并且有效治疗精神病，以及其它疾病如抑郁和焦虑，药物依赖，痴呆和记忆障碍。

7. 发明申请

WO2012076430A1 TRIAZOLOPYRIDINE COMPOUNDS 审中-公开
标题翻译：三唑啉化合物
公开(公告)号：WO2012076430A1
公开(公告)日：2012-06-14
申请号：PCT/EP2011/071685
申请日：2011-12-05
申请人： F. HOFFMANN-LA ROCHE AG , FLOHR, Alexander , GOBBI, Luca , GROEBKE ZBINDEN, Katrin , KOERNER, Matthias , PETERS, Jens-Uwe
发明人： FLOHR, Alexander , GOBBI, Luca , GROEBKE ZBINDEN, Katrin , KOERNER, Matthias , PETERS, Jens-Uwe
IPC分类号： C07D471/04 , C07D519/00 , A61K31/437 , A61P25/00 , A61P35/00 , A61P3/10
CPC分类号： C07D471/04 , C07D519/00
摘要： The invention is concerned with triazolopyridine compounds of formula (I), wherein R 1 , R 2 , R 3 and R 4 are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit PDEIOA and can be used as medicaments.
摘要翻译：本发明涉及式（I）的三唑并吡啶化合物，其中R 1，R 2，R 3和R 4如说明书和权利要求书中所定义，以及其生理上可接受的盐。这些化合物抑制PDEIOA并可用作药物。

8. 发明申请

WO2011117264A1 N-(IMIDAZOPYRIMIDIN-7-YL)-HETEROARYLAMIDE DERIVATIVES AND THEIR USE AS PDE10A INHIBITORS 审中-公开
标题翻译： N-（咪唑并吡啶-7-YL）-HETEROARYLAMIDE衍生物及其作为PDE10A抑制剂的用途
公开(公告)号：WO2011117264A1
公开(公告)日：2011-09-29
申请号：PCT/EP2011/054385
申请日：2011-03-23
申请人： F. HOFFMANN-LA ROCHE AG , ALVAREZ SÁNCHEZ, Rubén , BLEICHER, Konrad , FLOHR, Alexander , GOBBI, Luca , GROEBKE ZBINDEN, Katrin , KOERNER, Matthias , KUHN, Bernd , PETERS, Jens-Uwe , RUDOLPH, Markus
发明人： ALVAREZ SÁNCHEZ, Rubén , BLEICHER, Konrad , FLOHR, Alexander , GOBBI, Luca , GROEBKE ZBINDEN, Katrin , KOERNER, Matthias , KUHN, Bernd , PETERS, Jens-Uwe , RUDOLPH, Markus
IPC分类号： C07D487/04 , C07D519/00 , A61K31/519 , A61P25/00 , A61P25/18
CPC分类号： C07D487/04 , C07D519/00
摘要： The invention is concerned with novel imidazopyrimidine derivatives of formula (I) wherein R 1 , R 2 and R 8 are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit PDEIOA and used as medicaments.
摘要翻译：本发明涉及式（I）的新型咪唑并嘧啶衍生物，其中R 1，R 2和R 8如说明书和权利要求书中所定义，以及其生理上可接受的盐和酯。这些化合物抑制PDEIOA并用作药物。

9. 发明申请

WO2012004206A1 ANELLATED PYRIDINE COMPOUNDS 审中-公开
标题翻译：陈化吡啶化合物
公开(公告)号：WO2012004206A1
公开(公告)日：2012-01-12
申请号：PCT/EP2011/061167
申请日：2011-07-04
申请人： F. HOFFMANN-LA ROCHE AG , GOBBI, Luca , RODRIGUEZ SARMIENTO, Rosa Maria , WICHMANN, Juergen
发明人： GOBBI, Luca , RODRIGUEZ SARMIENTO, Rosa Maria , WICHMANN, Juergen
IPC分类号： C07D491/048 , C07D495/04 , A61K31/496 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30
CPC分类号： C07D495/04 , C07D491/048
摘要： The present invention is concerned with novel dual modulators of the 5-HT2A and D3 receptors of formula (I) wherein X, Y, A, R 1, R 2 , and R 3 are as described herein, as well as pharmaceutically acceptable salts and esters thereof. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions comprising them and their use as medicaments.
摘要翻译：本发明涉及式（I）的5-HT2A和D3受体的新型双重调节剂，其中X，Y，A，R 1，R 2和R 3如本文所述，以及其药学上可接受的盐和酯。此外，本发明涉及制备式（I）化合物，包含它们的药物组合物及其作为药物的用途。

10. 发明申请

WO2010034646A1 BENZO[D]ISOXAZOL-3-YL-PIPERAZIN DERIVATIVES USEFUL AS MODULATORS OF DOPAMINE D3 RECEPTORS 审中-公开
标题翻译：苯并[D] ISOXAZOL-3-YL-PIPERAZIN衍生物作为DOPAMINE D3受体的调节剂有用
公开(公告)号：WO2010034646A1
公开(公告)日：2010-04-01
申请号：PCT/EP2009/061906
申请日：2009-09-15
申请人： F. HOFFMANN-LA ROCHE AG , GOBBI, Luca , JAESCHKE, Georg , RODRIGUEZ SARMIENTO, Rosa Maria , STEWARD, Lucinda
发明人： GOBBI, Luca , JAESCHKE, Georg , RODRIGUEZ SARMIENTO, Rosa Maria , STEWARD, Lucinda
IPC分类号： C07D413/04 , A61K31/496 , A61P25/00
CPC分类号： C07D413/04
摘要： The present invention relates to compounds of the general formula (I), having affinity and selectivity for the dopamine D3 receptors, their manufacture, pharmaceutical compositions containing them and their use as medicaments. The active compounds of the present invention are useful for the therapeutic and/or prophylactic treatment of cognitive disorders.
摘要翻译：本发明涉及对多巴胺D3受体具有亲和性和选择性的通式（I）化合物，其制备方法，含有它们的药物组合物及其作为药物的用途。本发明的活性化合物可用于认知障碍的治疗和/或预防性治疗。

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