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71. 发明授权

EP2121579B1 MALONAMIDES AS OREXIN ANTAGONISTS 有权
标题翻译：马来酸酐
公开(公告)号：EP2121579B1
公开(公告)日：2011-04-20
申请号：EP08717394.4
申请日：2008-03-05
申请人： F. Hoffmann-La Roche AG
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 Ar1 and Ar2 are independently from each other unsubstituted or substituted aryl or heteroaryl; R1/R2 are independently from each other hydrogen, lower alkyl, lower alkyl substituted by halogen, -(CH2)o-O-lower alkyl, -(CH2)o-N-(lower alkyl)2, (CH2)p-cycloalkyl, (CH2)p-heterocycloalkyl, (CH2)p-aryl, (CH2)p-heteroaryl, which rings may be substituted by R, or R1 and R2 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; R3 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：本发明涉及其中Ar1，Ar2，R，R1，R2，R3和n如本文所定义或其药学上合适的酸加成盐，光学纯对映异构体，外消旋体或非对映体混合物的式I化合物。式I化合物是食欲蛋白受体拮抗剂，可用于治疗其中食欲素途径如睡眠障碍的疾病。

72. 发明公开

EP2252587A1 PIPERIDINE SULFONAMIDE DERIVATIVES 有权
标题翻译：哌啶磺酰胺衍生物
公开(公告)号：EP2252587A1
公开(公告)日：2010-11-24
申请号：EP09711149.6
申请日：2009-02-02
申请人： F. Hoffmann-La Roche AG
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 Ar1, Ar2, R1, R2, 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Ar 1，Ar 2，R 1，R 2，m和n如说明书和权利要求书中所定义，或其药学上合适的酸加成盐。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睡眠呼吸暂停，发作性睡病，失眠症，睡眠异常，飞行时差综合征，昼夜节律紊乱或与神经疾病相关的睡眠障碍。

73. 发明公开

EP2234999A1 HETEROARYL DERIVATIVES AS OREXIN RECEPTOR ANTAGONISTS 审中-公开
标题翻译：异位肾上腺皮质激素
公开(公告)号：EP2234999A1
公开(公告)日：2010-10-06
申请号：EP08863484.5
申请日：2008-12-11
申请人： F. Hoffmann-La Roche AG
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 R2; R2 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, SO2-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; R1 is hydrogen or lower alkyl; Het is a heteroaryl group, unsubstituted or substituted by one or more substituents selected from R3; R3 is hydroxy, halogen, =O, lower alkyl, lower alkyl substituted by halogen, lower alkoxy, phenyl, lower alkoxy substituted by halogen, nitro, cyano, SO2-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.

74. 发明公开

EP2200982A1 PIPERIDINE DERIVATIVES AS NK3 RECEPTOR ANTAGONISTS 有权
标题翻译：哌啶，NK-3受体拮抗剂
公开(公告)号：EP2200982A1
公开(公告)日：2010-06-30
申请号：EP08803620.7
申请日：2008-09-04
申请人： F. Hoffmann-La Roche AG
发明人： KNUST, Henner , NETTEKOVEN, Matthias , RATNI, Hasane , VIFIAN, Walter , WU, Xihan
IPC分类号： C07D211/58 , C07D401/04 , A61K31/4468 , A61P25/18
CPC分类号： C07D211/58 , C07D401/04
摘要： The invention relates to a compound of general formula (I) wherein Ar1/Ar2 are independently from each other phenyl or pyridinyl, which are optionally substituted by one or two substituents, selected from the group consisting of halogen, lower alkyl, lower alkoxy, lower alkyl substituted by halogen, lower alkoxy substituted by halogen, lower alkyl substituted by alkoxy, lower alkyl substituted by cyano, lower di-alkyl amino, pyridinyl or cyano; R1 is hydrogen, lower alkyl, -(CH2)2O-lower alkyl, or cycloalkyl: R2 is -S(O)2-lower alkyl or -C(O) -lower alkyl; or R1 and R2 form together with the N-atom to which they are attached a pyrrolidin-2- one or a piperidin-2-one group; R3 is hydrogen, halogen or lower alkyl; R4 is hydrogen or lower alkyl; R5/R5' are independently from each other hydrogen, lower alkyl, lower alkyl substituted by halogen, lower alkyl substituted by hydroxy or cycloalkyl; or R5 and R5' form together with the carbon-atom to which they are attached a cycloalkyl group; or to a pharmaceutically active salt thereof. It has been found that the present compounds are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).

75. 发明公开

EP2155729A1 PROLINAMIDE-TETRAZOLE DERIVATIVES AS NK3 RECEPTOR ANTAGONISTS 有权
标题翻译：作为NK3受体拮抗剂的PROLINAMIDE-TETRAZOLE衍生物
公开(公告)号：EP2155729A1
公开(公告)日：2010-02-24
申请号：EP08760179.5
申请日：2008-05-29
申请人： F. Hoffmann-La Roche AG
发明人： HAN, Bo , KNUST, Henner , NETTEKOVEN, Matthias , RATNI, Hasane , WU, Xihan
IPC分类号： C07D403/12 , A61K31/496 , A61P25/00
CPC分类号： C07D403/12
摘要： The present invention relates to a compound of formula (I) : wherein R1 is cycloalkyl or is phenyl unsubstituted or substituted by one or two halogen atoms; R2 is hydrogen or halogen; R3 is hydrogen, CN, lower alkoxy, lower alkyl or halogen; n is 0, 1 or 2; or to a pharmaceutically suitable acid addition salt thereof. It has been found that the present compounds are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).
摘要翻译：本发明涉及式（I）的化合物：其中R 1为环烷基或为未取代的或被一个或两个卤素原子取代的苯基; R2是氢或卤素; R3是氢，CN，低级烷氧基，低级烷基或卤素; n是0,1或2; 或其药学上合适的酸加成盐。已经发现本发明化合物是用于治疗抑郁症，疼痛，精神病，帕金森病，精神分裂症，焦虑和注意力缺陷多动症（ADHD）的高潜力NK-3受体拮抗剂。

76. 发明公开

EP2155672A1 PROLINAMIDE DERIVATIVES AS NK3 ANTAGONISTS 有权
标题翻译：作为NK3拮抗剂的PROLINAMIDE衍生物
公开(公告)号：EP2155672A1
公开(公告)日：2010-02-24
申请号：EP08760181.1
申请日：2008-05-29
申请人： F. Hoffmann-La Roche AG
发明人： HAN, Bo , KNUST, Henner , NETTEKOVEN, Matthias , RATNI, Hasane , WU, Xihan
IPC分类号： C07D207/16 , C07D401/06 , C07D487/10 , A61P25/16 , A61P25/18 , A61K31/401
CPC分类号： C07D207/16 , C07D401/06 , C07D471/10
摘要： The present invention relates to a compound of formula (I) wherein R1 is hydrogen, halogen, lower alkyl, lower alkyl substituted by halogen, lower alkoxy, or lower alkoxy substituted by halogen; R2 is hydrogen or lower alkyl; R3, R4 form together with the N-atom to which they are attached a non aromatic heterocyclic group, selected from R5 is hydrogen or halogen; R6 is phenyl, unsubstituted or substituted by cyano, halogen, lower alkyl, lower alkoxy, CF3, -(CH2)2O-lower alkyl, C(O)-lower alkyl or C(O)O-lower alkyl, or is pyridinyl, unsubstituted or substituted by CF3, or is -C(O)-phenyl; R7 is hydrogen or lower alkoxy; R8 is phenyl, lower alkyl or -C(O)O-lower alkyl; R9 is hydrogen or S(O)2-lower alkyl; R10 is hydrogen or cycloalkyl; X is -CH2- or -C(O)-; p is 1 or 2; n is 1, 2 or 3; o is 1 or 2; or to a pharmaceutically suitable acid addition salt thereof which are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).
摘要翻译：本发明涉及式（I）的化合物，其中R 1为氢，卤素，低级烷基，被卤素取代的低级烷基，低级烷氧基或被卤素取代的低级烷氧基; R2是氢或低级烷基; R 3，R 4与它们所连接的N原子一起形成选自R 5为氢或卤素的非芳族杂环基团; R 6为未取代的或被氰基，卤素，低级烷基，低级烷氧基，CF 3， - （CH 2）2 O-低级烷基，C（O） - 低级烷基或C（O）O-低级烷基取代的苯基，或为吡啶基，未被取代或被CF 3取代，或者是-C（O） - 苯基; R7是氢或低级烷氧基; R8是苯基，低级烷基或-C（O）O-低级烷基; R9是氢或S（O）2 - 低级烷基; R10是氢或环烷基; X是-CH 2 - 或-C（O） - ; p是1或2; n是1,2或3; o是1或2; 或其药学上合适的酸加成盐，它们是用于治疗抑郁症，疼痛，精神病，帕金森病，精神分裂症，焦虑和注意力缺陷多动障碍（ADHD）的高潜力NK-3受体拮抗剂。

78. 发明公开

EP3551627A1 NEW ISOXAZOLYL ETHER DERIVATIVES AS GABA A ALPHA5 PAM 有权
公开(公告)号：EP3551627A1
公开(公告)日：2019-10-16
申请号：EP17816630.2
申请日：2017-12-07
申请人： F. Hoffmann-La Roche AG
发明人： BUETTELMANN, Bernd , CECERE, Giuseppe , FASCHING, Bernhard , GROEBKE ZBINDEN, Katrin , HERNANDEZ, Maria-Clemencia , KNUST, Henner , KOBLET, Andreas , PINARD, Emmanuel , THOMAS, Andrew
IPC分类号： C07D413/14 , A61K31/4439 , A61K31/501 , A61P25/28

79. 发明授权

EP2364295B1 3-(BENZYLAMINO)-PYRROLIDINE DERIVATIVES AND THEIR USE AS NK-3 RECEPTOR ANTAGONISTS 有权
标题翻译： 3-（苄基氨基）吡咯烷及其作为NK-3受体拮抗剂
公开(公告)号：EP2364295B1
公开(公告)日：2013-02-27
申请号：EP09737458.1
申请日：2009-10-26
申请人： F. Hoffmann-La Roche AG
发明人： BISSANTZ, Caterina , JABLONSKI, Philippe , KNUST, Henner , NETTEKOVEN, Matthias , RATNI, Hasane , RIEMER, Claus
IPC分类号： C07D207/14 , A61K31/401 , A61K31/4025 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/12 , C07D405/12 , C07D409/06 , C07D409/12 , C07D413/06 , C07D413/12 , C07D491/08
CPC分类号： C07D207/14 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/12 , C07D405/12 , C07D409/06 , C07D409/12 , C07D413/06 , C07D413/12 , C07D491/08

80. 发明授权

EP2303871B1 PYRROLIDIN-3-YLMETHYL-AMINE AS OREXIN ANTAGONISTS 有权
标题翻译：吡咯烷-3-基甲基阿明ALS食欲素拮抗剂
公开(公告)号：EP2303871B1
公开(公告)日：2012-05-09
申请号：EP09780805.9
申请日：2009-07-20
申请人： F. Hoffmann-La Roche AG
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.

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