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21. 发明申请

WO2011085886A1 PYRROLIDINE DERIVATIVES 审中-公开
标题翻译：吡咯烷衍生物
公开(公告)号：WO2011085886A1
公开(公告)日：2011-07-21
申请号：PCT/EP2010/069434
申请日：2010-12-13
申请人： F. HOFFMANN-LA ROCHE AG , KNUST, Henner , KOBLET, Andreas , NETTEKOVEN, Matthias , RATNI, Hasane , RIEMER, Claus , VIFIAN, Walter
发明人： KNUST, Henner , KOBLET, Andreas , NETTEKOVEN, Matthias , RATNI, Hasane , RIEMER, Claus , VIFIAN, Walter
IPC分类号： C07D207/14 , C07D401/06 , C07D403/06 , C07D405/06 , C07D407/04 , C07D413/06 , C07D417/14 , A61K31/5377 , A61P25/18
CPC分类号： A61K31/40 , A61K31/4025 , A61K31/454 , A61K31/4545 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/5377 , C07D207/14 , C07D401/06 , C07D403/06 , C07D405/06 , C07D407/04 , C07D413/06 , C07D417/14
摘要： The present invention relates to compounds of formula (I) 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).
摘要翻译：本发明涉及式（I）化合物或其药物活性盐。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，焦虑和注意缺陷多动障碍（ADHD）的高潜力NK-3受体拮抗剂。

22. 发明申请

WO2011067166A1 AZACYCLIC SPIRO DERIVATIVES 审中-公开
标题翻译： AZACYCLIC SPIRO衍生物
公开(公告)号：WO2011067166A1
公开(公告)日：2011-06-09
申请号：PCT/EP2010/068265
申请日：2010-11-26
申请人： F. HOFFMANN-LA ROCHE AG , ACKERMANN, Jean , CONTE, Aurelia , HUNZIKER, Daniel , NEIDHART, Werner , NETTEKOVEN, Matthias , SCHULZ-GASCH, Tanja , WERTHEIMER, Stanley
发明人： ACKERMANN, Jean , CONTE, Aurelia , HUNZIKER, Daniel , NEIDHART, Werner , NETTEKOVEN, Matthias , SCHULZ-GASCH, Tanja , WERTHEIMER, Stanley
IPC分类号： C07D471/10 , A61K31/438 , A61P3/00 , A61P3/10
CPC分类号： C07D471/10
摘要： Compounds of Formula (I) as well as pharmaceutically acceptable salts thereof can be used in the form of pharmaceutical compositions, wherein R 1 , R 2 , R 3 and n have the significance given in claim 1.
摘要翻译：式（I）化合物及其药学上可接受的盐可以以药物组合物的形式使用，其中R 1，R 2，R 3和n具有权利要求1中给出的含义。

23. 发明申请

WO2011045292A1 SPIRO-CONDENSED CYCLOHEXANE DERIVATIVES AS HSL INHIBITORS USEFUL FOR THE TREATMENT OF DIABETES 审中-公开
标题翻译：作为HSL抑制剂用于治疗糖尿病的螺旋状冷凝环孢菌素衍生物
公开(公告)号：WO2011045292A1
公开(公告)日：2011-04-21
申请号：PCT/EP2010/065232
申请日：2010-10-12
申请人： F. HOFFMANN-LA ROCHE AG , ACKERMANN, Jean , BRUGGER, Stephan , CONTE, Aurelia , HUNZIKER, Daniel , NEIDHART, Werner , NETTEKOVEN, Matthias , SCHULZ-GASCH, Tanja , WERTHEIMER, Stanley
发明人： ACKERMANN, Jean , BRUGGER, Stephan , CONTE, Aurelia , HUNZIKER, Daniel , NEIDHART, Werner , NETTEKOVEN, Matthias , SCHULZ-GASCH, Tanja , WERTHEIMER, Stanley
IPC分类号： C07D209/54 , C07D401/06 , C07D401/12 , C07D403/12 , C07D405/04 , C07D405/12 , C07D409/12 , C07D413/12 , A61K31/403 , A61P3/00
CPC分类号： C07D209/54 , C07D401/06 , C07D401/12 , C07D403/12 , C07D405/04 , C07D405/12 , C07D409/12 , C07D413/12
摘要： Compounds of formula (I) as well as pharmaceutically acceptable salts thereof can be used in the form of pharmaceutical compositions as HSL inhibitors for the treatment of diabetes, wherein R 1 ,R 2 , R 3 , C a and C b have the significance given in claim 1.
摘要翻译：式（I）化合物及其药学上可接受的盐可以药物组合物的形式用作治疗糖尿病的HSL抑制剂，其中R1，R2，R3，Ca和Cb具有权利要求1中给出的含义。

24. 发明申请

WO2010094667A1 PYRROLIDINE DERIVATIVES AS NK3 RECEPTOR ANTAGONISTS 审中-公开
标题翻译：吡咯啉衍生物作为NK3受体拮抗剂
公开(公告)号：WO2010094667A1
公开(公告)日：2010-08-26
申请号：PCT/EP2010/051887
申请日：2010-02-16
申请人： F. HOFFMANN-LA ROCHE AG , KNUST, Henner , LIMBERG, Anja , NETTEKOVEN, Matthias , RATNI, Hasane , RIEMER, Claus
发明人： KNUST, Henner , LIMBERG, Anja , NETTEKOVEN, Matthias , RATNI, Hasane , RIEMER, Claus
IPC分类号： C07D207/08 , C07D401/12 , C07D401/14 , C07D403/14 , A61P25/00 , A61K31/496 , A61K31/506 , A61K31/4439 , A61K31/4545 , A61K31/501
CPC分类号： C07D207/08 , C07D207/09 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14
摘要： The present invention relates to a compounds of formula I wherein A is -NR'-, -S-, -S(O)- or -S(O) 2 -; R' is hydrogen or lower alkyl; Ar is aryl or is a five or six membered heteroaryl group, containing one or two N-atoms; R is a five or six membered heterocyclic group X 1 is N or CH; and X 2 is -N(R 1 )-, -CH 2 -, -O-, -S-, -S(O)-, or -S(O) 2 -, R 1 is hydrogen, lower alkyl, S(O) 2 -lower alkyl, C(O)-lower alkyl, C(O)-cycloalkyl optionally substituted by lower alkyl; with the proviso that at least one of X 1 or X 2 contains a heteroatom, or is a five or six membered heteroaryl group, containing one or two N-atoms, which groups are unsubstituted or may be substituted by one or two R 1 ; wherein R 1 is lower alkyl or cyano; R 2 is lower alkyl substituted by halogen, halogen, cyano or nitro; R 3 is halogen; R 4 is hydrogen or lower alkyl; o is 1 or 2; in case o is 2, R 2 may be the same or different; p is 1 or 2; in case p is 2, R 3 may be the same or different; 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, bipolar disorders, anxiety and attention deficit hyperactivity disorder (ADHD).
摘要翻译：本发明涉及式I化合物，其中A为-NR' - ， - S - ， - S（O） - 或-S（O）2 - ; R'是氢或低级烷基; Ar是芳基或是含有一个或两个N-原子的五或六元杂芳基; R是五或六元杂环基，X 1是N或CH; 并且X 2为-N（R 1） - ， - CH 2 - ， - O - ， - S - ， - S（O） - 或-S（O）2 - ，R 1为氢，低级烷基，S（O）低级烷基，C（O） - 低级烷基，任选被低级烷基取代的C（O） - 环烷基; 条件是X 1或X 2中的至少一个含有杂原子，或是含有一个或两个N原子的五或六元杂芳基，该基团是未取代的或可被一个或两个R 1取代; 其中R1是低级烷基或氰基; R2是被卤素，卤素，氰基或硝基取代的低级烷基; R3是卤素; R4是氢或低级烷基; o是1或2; 在o为2的情况下，R 2可以相同或不同; p为1或2; 在p为2的情况下，R 3可以相同或不同; 或其药物活性盐。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，双相情感障碍，焦虑和注意缺陷多动障碍（ADHD）的高潜力NK-3受体拮抗剂。

25. 发明申请

WO2009150110A1 PYRROLIDINE ETHER DERIVATIVES AS NK3 RECEPTOR ANTAGONISTS 审中-公开
标题翻译：吡咯烷酮衍生物作为NK3受体拮抗剂
公开(公告)号：WO2009150110A1
公开(公告)日：2009-12-17
申请号：PCT/EP2009/056989
申请日：2009-06-08
申请人： F. HOFFMANN-LA ROCHE AG , JABLONSKI, Philippe , KAWASAKI, Kenichi , KNUST, Henner , LIMBERG, Anja , NETTEKOVEN, Matthias , RATNI, Hasane , RIEMER, Claus
发明人： JABLONSKI, Philippe , KAWASAKI, Kenichi , KNUST, Henner , LIMBERG, Anja , NETTEKOVEN, Matthias , RATNI, Hasane , RIEMER, Claus
IPC分类号： C07D401/12 , C07D401/14 , A61K31/445 , A61P25/00
CPC分类号： C07D401/14 , C07D401/12
摘要： The present invention relates to a compounds of formula I wherein R 1 , R 2 , R 3 , R', Ar, o, n and m are as defined in the specification. 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化合物，其中R 1，R 2，R 3，R'，Ar，O，n和m如说明书中所定义。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，焦虑和注意缺陷多动障碍（ADHD）的高潜力NK-3受体拮抗剂。

26. 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。

27. 发明申请

WO2008068174A9 4,5,6,7-TETRAHYDRO-THIENO [2,3-C] PYRIDINES AS H3 MODULATORS 审中-公开
公开(公告)号：WO2008068174A9
公开(公告)日：2008-06-12
申请号：PCT/EP2007/062930
申请日：2007-11-28
申请人： F. HOFFMANN-LA ROCHE AG , CHEN, Li , LAI, Wayne Wen , NETTEKOVEN, Matthias , ROCHE, Olivier , ZHENG, Deye
发明人： CHEN, Li , LAI, Wayne Wen , NETTEKOVEN, Matthias , ROCHE, Olivier , ZHENG, Deye
IPC分类号： C07D495/04 , A61K31/4365 , A61P3/04 , A61P3/10
摘要： The present invention relates to compounds of formula (I), wherein R 1 and R 2 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prevention of diseases which are associated with the modulation of H3 receptors.

28. 发明申请

WO2008068173A9 4, 5, 6, 7-TETRAHYDRO-THIENO [3, 2-C] PYRIDINE DERIVATIVES AS H3 MODULATORS 审中-公开
公开(公告)号：WO2008068173A9
公开(公告)日：2008-06-12
申请号：PCT/EP2007/062927
申请日：2007-11-28
申请人： F. HOFFMANN-LA ROCHE AG , CHEN, Li , LAI, Wayne Wen , NETTEKOVEN, Matthias , ROCHE, Olivier , ZHENG, Deye
发明人： CHEN, Li , LAI, Wayne Wen , NETTEKOVEN, Matthias , ROCHE, Olivier , ZHENG, Deye
IPC分类号： C07D495/04 , A61K31/4365 , A61P3/04 , A61P3/10
摘要： The present invention relates to compounds of formula (I) wherein R 1 and R 2 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prevention of diseases which are associated with the modulation of H3 receptors.

29. 发明申请

WO2008015125A1 1H-INDOL-6-YL-PIPERAZIN-1-YL-METHANONE-DERIVATIVES FOR USE AS H3 RECEPTOR MODULATORS 审中-公开
标题翻译：用作H3受体调节剂的1H-INDOL-6-YL-PIPERAZIN-1-YL-METHANONE-DORIVIVE
公开(公告)号：WO2008015125A1
公开(公告)日：2008-02-07
申请号：PCT/EP2007/057599
申请日：2007-07-24
申请人： F. HOFFMANN-LA ROCHE AG , NETTEKOVEN, Matthias , ROCHE, Olivier
发明人： NETTEKOVEN, Matthias , ROCHE, Olivier
IPC分类号： C07D403/02 , A61K31/496 , A61P3/04
CPC分类号： C07D403/06 , C07D401/14 , C07D413/14
摘要： The present invention relates to compounds of formula I wherein R 1 to R 4 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prevention of diseases such as obesity and other disorders which are associated with the modulation of H3 receptors.
摘要翻译：本发明涉及式I化合物，其中R 1至R 4如在说明书和权利要求书中所定义，及其药学上可接受的盐。该化合物可用于治疗和/或预防与H3受体的调节相关的疾病如肥胖症和其它病症。

30. 发明申请

WO2007068641A1 PYRROLO [2 , 3-B] PYRIDINE DERIVATIVES AS H3 RECEPTOR MODULATORS 审中-公开
标题翻译：吡咯并[2,3-B]吡啶衍生物作为H3受体调节剂
公开(公告)号：WO2007068641A1
公开(公告)日：2007-06-21
申请号：PCT/EP2006/069390
申请日：2006-12-06
申请人： F. HOFFMANN-LA ROCHE AG , NETTEKOVEN, Matthias , ROCHE, Olivier
发明人： NETTEKOVEN, Matthias , ROCHE, Olivier
IPC分类号： C07D471/04 , A61K31/4353 , A61P3/06 , A61P3/10
CPC分类号： C07D471/04
摘要： The present invention relates to compounds of formula (I) wherein R 1 to R 4 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prevention of diseases which are associated with the modulation of H3 receptors.
摘要翻译：本发明涉及式（I）化合物，其中R 1至R 4如在说明书和权利要求书中所定义，及其药学上可接受的盐。该化合物可用于治疗和/或预防与H3受体的调节相关的疾病。

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