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    • 21. 发明申请
      WO2009019163A1 PYRROLIDINE ARYL-ETHER AS NK3 RECEPTOR ANTAGONISTS 审中-公开
    • PYRROLIDINE ARYL-ETHER AS NK3 RECEPTOR ANTAGONISTS
    • 吡咯烷酮ARYL-ETHER作为NK3受体拮抗剂
    • WO2009019163A1
    • 2009-02-12
    • PCT/EP2008/059908
    • 2008-07-29
    • F. HOFFMANN-LA ROCHE AG , JABLONSKI, Philippe , KAWASAKI, Kenichi , KNUST, Henner , LIMBERG, Anja , NETTEKOVEN, Matthias , RATNI, Hasane , RIEMER, Claus , WU, Xihan
    • JABLONSKI, Philippe , KAWASAKI, Kenichi , KNUST, Henner , LIMBERG, Anja , NETTEKOVEN, Matthias , RATNI, Hasane , RIEMER, Claus , WU, Xihan
    • C07D401/08 , C07D401/06
    • C07D401/06 , C07D401/08
    • The invention relates to a compound of general formula (I) wherein Ar 1 is aryl or a five or six membered heteroaryl; Ar 2 is aryl or a five or six membered heteroaryl; R 1 is hydrogen, halogen, lower alkyl, lower alkoxy, lower alkyl substituted by halogen, lower alkoxy substituted by halogen, S-lower alkyl, -S(O) 2 -lower alkyl, -S(O) 2 -di-lower alkyl amino, -(CH 2 ) q R, cyano, amino, mono or di-lower alkyl amino, NHC(O)-lower alkyl, cycloalkyl or is or a five membered heteroaryl, optionally substituted by lower alkyl; wherein R is cyano, di-lower alkyl amino or pyrrolidin-1-yl; R 2 is hydrogen, halogen, lower alkyl, lower alkyl substituted by halogen or cyano; R 3 is hydrogen or lower alkyl or CH 2 OH; R 4 is hydrogen, halogen, lower alkyl, lower alkyl substituted by halogen or cyano; n is 1, 2 or 3; in case n is 2 or 3, R 1 may be the same or different; o is 1, 2 or 3; in case o is 2 or 3, R 2 may be the same or different; p is 1, 2 or 3; in case p is 2 or 3, R 4 may be the same or different; q is 1 or 2; or to a pharmaceutically active salt thereof, including all stereoisomeric forms, individual diastereoisomers and enantiomers of the compound of formula (I) as well as racemic and non-racemic mixtures 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).
    • 本发明涉及通式（I）的化合物，其中Ar 1是芳基或五或六元杂芳基; Ar 2是芳基或五或六元杂芳基; R 1是氢，卤素，低级烷基，低级烷氧基，被卤素取代的低级烷基，被卤素取代的低级烷氧基，S-低级烷基，-S（O）2 - 低级烷基，-S（O） 氨基， - （CH 2）q R，氰基，氨基，一或二低级烷基氨基，NHC（O） - 低级烷基，环烷基或任选被低级烷基取代的五元杂芳基; 其中R是氰基，二低级烷基氨基或吡咯烷-1-基; R2是氢，卤素，低级烷基，被卤素或氰基取代的低级烷基; R3是氢或低级烷基或CH2OH; R4是氢，卤素，低级烷基，被卤素或氰基取代的低级烷基; n为1,2或3; 在n为2或3的情况下，R 1可以相同或不同; o是1,2或3; 在o为2或3的情况下，R 2可以相同或不同; p为1,2或3; 在p为2或3的情况下，R 4可以相同或不同; q为1或2; 或其药物活性盐，包括式（I）化合物的所有立体异构形式，单独的非对映异构体和对映异构体以及其外消旋和非外消旋混合物。 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。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
    • 22. 发明申请
      WO2012093109A1 PYRROLIDINE DERIVATIVES AS NK3 ANTAGONISTS 审中-公开
    • PYRROLIDINE DERIVATIVES AS NK3 ANTAGONISTS
    • 吡咯啉衍生物作为NK3拮抗剂
    • WO2012093109A1
    • 2012-07-12
    • PCT/EP2012/050034
    • 2012-01-03
    • F. HOFFMANN-LA ROCHE AG , KNUST, Henner , NETTEKOVEN, Matthias , RATNI, Hasane , VIFIAN, Walter
    • KNUST, Henner , NETTEKOVEN, Matthias , RATNI, Hasane , VIFIAN, Walter
    • C07D401/06 , C07D401/14 , C07D403/06 , C07D413/10 , A61K31/4025 , A61P25/00
    • C07D401/06 , C07D401/14 , C07D403/06 , C07D407/06 , C07D413/10
    • The invention relates to compounds of formula (I) wherein R 1 is (A), or is phenyl, pyridinyl or pyridazinyl, wherein phenyl, pyridinyl and pyridazinyl may optionally be substituted by cyano, lower alkyl, halogen-substituted phenyl, lower alkyl-substituted [1,2,4]oxadiazol-3-yl or by 2-oxo-piperidin-1-yl; X is NR or O; R is C(O)-lower alkyl, -C(O)-cycloalkyl substituted by lower alkyl, cycloalkyl or is phenyl, pyridinyl or pyridazinyl, wherein phenyl, pyridinyl and pyridazinyl may optionally be substituted by lower alkyl, lower alkoxy, cyano, -C(O)-lower alkyl, halogen or lower alkyl substituted by halogen; R 2 is hydrogen or lower alkyl; R 3 is hydrogen, halogen, cyano, lower alkyl or lower alkyl substituted by halogen; R 4 is hydrogen or lower alkyl; wherein R 2 and R 4 are not simultaneously hydrogen or lower alkyl; R 5 is lower alkyl; R 6 halogen, hydroxy, lower alkyl, lower alkoxy, lower alkyl substituted by halogen, S(O) 2 -lower alkyl or cyano; 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).
    • 本发明涉及式（I）化合物，其中R 1为（A），或为苯基，吡啶基或哒嗪基，其中苯基，吡啶基和哒嗪基可任选被氰基，低级烷基，卤素取代的苯基，低级烷基取代 [1,2,4]恶二唑-3-基或2-氧代 - 哌啶-1-基; X是NR或O; R是C（O） - 低级烷基，被低级烷基，环烷基或苯基，吡啶基或哒嗪基取代的-C（O） - 环烷基，其中苯基，吡啶基和哒嗪基可以任选地被低级烷基，低级烷氧基，氰基， -C（O） - 低级烷基，卤素或被卤素取代的低级烷基; R2是氢或低级烷基; R3是氢，卤素，氰基，被卤素取代的低级烷基或低级烷基; R4是氢或低级烷基; 其中R2和R4不同时为氢或低级烷基; R5是低级烷基; R 6卤素，羟基，低级烷基，低级烷氧基，被卤素取代的低级烷基，S（O）2 - 低级烷基或氰基; 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，焦虑和注意缺陷多动障碍（ADHD）的高潜力NK-3受体拮抗剂。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
    • 23. 发明申请
      WO2010086259A1 PIPERIDINE DERIVATIVES AS NK3 RECEPTOR ANTAGONISTS 审中-公开
    • PIPERIDINE DERIVATIVES AS NK3 RECEPTOR ANTAGONISTS
    • 作为NK3受体拮抗剂的哌啶衍生物
    • WO2010086259A1
    • 2010-08-05
    • PCT/EP2010/050591
    • 2010-01-19
    • F. HOFFMANN-LA ROCHE AG , KNUST, Henner , NETTEKOVEN, Matthias , RATNI, Hasane , RIEMER, Claus , VIFIAN, Walter
    • KNUST, Henner , NETTEKOVEN, Matthias , RATNI, Hasane , RIEMER, Claus , VIFIAN, Walter
    • C07D401/12 , C07D401/14 , C07D413/14 , A61K31/454 , A61K31/4545 , A61P25/24 , A61P25/04 , A61P25/18 , A61P25/16 , A61P25/22
    • C07D413/14 , C07D401/12 , C07D401/14
    • The present invention relates to a compounds of formula (I) wherein Ar 1 is aryl or a six membered heteroaryl; Ar 2 is aryl or a six membered heteroaryl; R 1 is hydrogen, halogen, lower alkyl, lower alkoxy or lower alkyl substituted by halogen; R 2 is hydrogen, halogen, lower alkyl, lower alkyl substituted by halogen or cyano; R 3 is hydrogen or lower alkyl; R 4 is hydrogen, lower alkyl, phenyl, optionally substituted by halogen, or is a five membered heteroaryl, optionally substituted by lower alkyl, or is aryl optionally substituted by halogen; is a six membered heterocyclic group, wherein X is -N(SO 2 CH 3 ); R 6 is hydrogen; Y is -N(R 7' )- R 7' is a 6-membered heteroaryl group, optionally substituted by cyano or C(O)-cycloalkyl, wherein the cycloalkyl group is optionally substituted by lower alkyl, n is 1; m is 1; o is1; p is 1; s is 0; t is 1; u is 1; or to a pharmaceutically active salt, a racemic mixture, an enantiomer, an optical isomer or a tautomeric form thereof. It has been found that the present compounds are high potential NK-3 receptor antagonist for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia anxiety and attention deficit hyperactivity disorder (ADHD).
    • 本发明涉及式（I）的化合物，其中Ar 1是芳基或6元杂芳基; Ar 2是芳基或六元杂芳基; R1是氢，卤素，低级烷基，低级烷氧基或被卤素取代的低级烷基; R2是氢，卤素，低级烷基，被卤素或氰基取代的低级烷基; R3是氢或低级烷基; R4是氢，低级烷基，任选被卤素取代的苯基，或是任选被低级烷基取代的五元杂芳基，或者是被卤素任意取代的芳基; 是六元杂环基，其中X是-N（SO 2 CH 3）; R6是氢; Y是-N（R 7'）-R 7'是任选被氰基或C（O） - 环烷基取代的6元杂芳基，其中环烷基任选被低级烷基取代，n是1; m为1; o is1; p为1; s是0; t为1; 你是1 或其药物活性盐，外消旋混合物，对映体，旋光异构体或其互变异构形式。 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。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
    • 25. 发明申请
      WO2009080533A1 HETEROARYL DERIVATIVES AS OREXIN RECEPTOR ANTAGONISTS 审中-公开
    • HETEROARYL DERIVATIVES AS OREXIN RECEPTOR ANTAGONISTS
    • 异丙肾上腺素衍生物作为OREXIN受体拮抗剂
    • WO2009080533A1
    • 2009-07-02
    • PCT/EP2008/067273
    • 2008-12-11
    • F. HOFFMANN-LA ROCHE AG , KNUST, Henner , NETTEKOVEN, Matthias , PINARD, Emmanuel , ROCHE, Olivier , ROGERS-EVANS, Mark
    • KNUST, Henner , NETTEKOVEN, Matthias , PINARD, Emmanuel , ROCHE, Olivier , ROGERS-EVANS, Mark
    • C07D401/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D498/04 , A61K31/4025 , A61P25/00
    • C07D413/12 , C07D401/12 , C07D409/14 , C07D413/14 , C07D417/12 , C07D417/14 , C07D498/04
    • 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.
    • 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 。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
    • 27. 发明申请
      WO2008107335A1 AMINOAMIDES AS OREXIN ANTAGONISTS 审中-公开
    • AMINOAMIDES AS OREXIN ANTAGONISTS
    • AMINOAMIDES作为OREXIN ANTAGONISTS
    • WO2008107335A1
    • 2008-09-12
    • PCT/EP2008/052245
    • 2008-02-25
    • F. HOFFMANN-LA ROCHE AG , GOBBI, Luca , KNUST, Henner , MALHERBE, Parichehr , NETTEKOVEN, Matthias , PINARD, Emmanuel , ROCHE, Olivier , ROGERS-EVANS, Mark
    • GOBBI, Luca , KNUST, Henner , MALHERBE, Parichehr , NETTEKOVEN, Matthias , PINARD, Emmanuel , ROCHE, Olivier , ROGERS-EVANS, Mark
    • C07C237/06 , C07D213/36 , A61K31/16
    • C07D213/36 , A61K9/2018 , A61K9/4858 , C07C237/20 , C07C2601/02 , C07C2601/04
    • 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.
    • 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。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
    • 29. 发明申请
      WO2010060703A1 3-(BENZYLAMINO)-PYRROLIDINE DERIVATIVES AND THEIR USE AS NK-3 RECEPTOR ANTAGONISTS 审中-公开
    • 3-(BENZYLAMINO)-PYRROLIDINE DERIVATIVES AND THEIR USE AS NK-3 RECEPTOR ANTAGONISTS
    • 3-（苯甲酰胺） - 吡咯烷衍生物及其作为NK-3受体拮抗剂的用途
    • WO2010060703A1
    • 2010-06-03
    • PCT/EP2009/064031
    • 2009-10-26
    • F. HOFFMANN-LA ROCHE AG , BISSANTZ, Caterina , JABLONSKI, Philippe , KNUST, Henner , NETTEKOVEN, Matthias , RATNI, Hasane , RIEMER, Claus
    • BISSANTZ, Caterina , JABLONSKI, Philippe , KNUST, Henner , NETTEKOVEN, Matthias , RATNI, Hasane , RIEMER, Claus
    • 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
    • C07D207/14 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/12 , C07D405/12 , C07D409/06 , C07D409/12 , C07D413/06 , C07D413/12 , C07D491/08
    • The present invention relates to a compounds of formula I wherein Ar is aryl; R 1 is hydrogen, halogen, lower alkyl, lower alkoxy, lower alkyl substituted by halogen, lower alkoxy substituted by halogen, cyano, amino, mono or di-lower alkyl amino, C(O)-lower alkyl, or is aryl or heteroaryl; R 2 is hydrogen or halogen; R 3 is -(CH 2 ) p -heterocyclyl, optionally substituted by one or two substituents R 4 ; or is lower alkyl, lower alkoxy, -(CH 2 ) p -O-lo wer alkyl, -(CH 2 ) P -CN, -O-(CH 2 ) p -CN, -(CH 2 ) p -heteroaryl, -(CH 2 ) p -C(O)-heteroaryl, -O-(CH 2 ) p -heterocyclyl, -(CH 2 ) p -aryl, optionally substituted by lower alkoxy or halogen, -(CH 2 ) p -O-aryl, optionally substituted by lower alkyl, -(CH 2 ) p -NR'-heterocyclyl, optionally substituted by lower alkyl, -CH 2 ) p -NR'R", -CH 2 ) p -NR'-CH 2 ) p' -NR'R", -CH 2 ) p -NR'-CH 2 ) p' -CN, -CH 2 ) p -C(O)-NR'R" or is -O-(CH 2 ) p -NR'R"; R 4 is hydroxy, lower alkyl, -(CH 2 ) P -OH, -(CH 2 ) P -NR'R", -NR'-C(O)-lower alkyl, -(CH 2 ) p -CN, -S(O) 2 -lower alkyl, -NR'-S(O) 2 -lower alkyl, -S(O)2-NR'R", -C(O)-lower alkyl, -C(O)-lower cycloalkyl, wherein the cycloalkyl may be substituted by lower alkyl, or is -C(O)-NR'R", heterocyclyl, optionally substituted by =0, or is heteroaryl, optionally substituted by alkoxy or cyano, or is aryl optionally substituted by alkoxy, cyano or is 2-oxa-5-aza-bicyclo[2.2.1]hept-5-yl; R' and R' ' are independently from each other hydrogen, lower alkyl or -(CH 2 ) P -OH; n is 1 or 2; in case n is 1 or 2, R 1 may be the same or different; o is 1 or 2; in case o is 1 or 2, R 2 may be the same or different; p,p' are the same or different and are O, 1, 2 3 or 4; or to a pharmaceutically active salt, a racemic mixture, an enantiomer, an optical isomer or a tautomeric form 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).
    • 本发明涉及式Ⅰ化合物，其中Ar为芳基; R 1为氢，卤素，低级烷基，低级烷氧基，被卤素取代的低级烷基，被卤素取代的低级烷氧基，氰基，氨基，一或二低级烷基氨基，C（O） - 低级烷基，或为芳基或杂芳基; R2是氢或卤素; R3是 - （CH2）对 - 杂环基，任选被一个或两个取代基R 4取代; 或（CH 2）p-CN，-O-（CH 2）p -CN， - （CH 2）p - 杂芳基， - （CH 2）p C（ - （CH 2）p - 芳基，任选被低级烷氧基或卤素取代的 - （CH 2）p - 芳基， - （CH 2） -CH 2）p-NR'R“，-CH 2）p-NR'-CH 2）p'-NR'R”，-CH 2）p -NR'-CH 2） p'-CN，-CH2）pC（O）-NR'R“或是-O-（CH2）p-NR'R”; R4是羟基，低级烷基， - （CH2）P-OH， - （CH2）P-NR'R“，-NR'-C（O） - 低级烷基， - （CH2）p-CN，-S ）低级烷基，-NR'-S（O）2 - 低级烷基，-S（O）2 -NR'R“，-C（O） - 低级烷基，-C（O） - 低级环烷基，其中 可以被低级烷基取代，或者是-C（O）-NR'R“，任选地被0取代的杂环基，或被任选被烷氧基或氰基取代的杂芳基，或者是被烷氧基任意取代的芳基，氰基 或是2-氧杂-5-氮杂 - 双环[2.2.1]庚-5-基; R'和R“彼此独立地为氢，低级烷基或 - （CH 2）P-OH; n为1或 2;在n为1或2的情况下，R 1可以相同或不同; o为1或2;在o为1或2的情况下，R 2可以相同或不同; p，p'相同或不同， O，1,2,3或4;或其药学活性盐，外消旋混合物，对映异构体，旋光异构体或互变异构体形式。已经发现本发明化合物是高潜在的NK-3受体拮抗剂 治疗抑郁症，疼痛，精神病，P 阿金森氏病，精神分裂症，焦虑和注意缺陷多动障碍（ADHD）。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
    • 30. 发明申请
      WO2010054968A1 QUINAZOLINE DERIVATIVES AS NK3 RECEPTOR ANTAGONISTS 审中-公开
    • QUINAZOLINE DERIVATIVES AS NK3 RECEPTOR ANTAGONISTS
    • 喹唑啉衍生物作为NK3受体拮抗剂
    • WO2010054968A1
    • 2010-05-20
    • PCT/EP2009/064604
    • 2009-11-04
    • F. HOFFMANN-LA ROCHE AG , KNUST, Henner , LIMBERG, Anja , NETTEKOVEN, Matthias , RATNI, Hasane , RIEMER, Claus , VIFIAN, Walter
    • KNUST, Henner , LIMBERG, Anja , NETTEKOVEN, Matthias , RATNI, Hasane , RIEMER, Claus , VIFIAN, Walter
    • C07D401/04 , C07D401/14 , C07D405/14 , C07D409/14 , A61K31/517 , A61P25/16 , A61P25/18
    • C07D401/04 , C07D401/14 , C07D405/14 , C07D409/14
    • The present invention relates to a compounds of formula I wherein R 1 is hydroxy or NR'R"; R' and R" are independently from each other hydrogen, lower alkyl, cycloalkyl, or may form together with the N-atom to which they are attached a heteroalkyl ring; R 2 is hydrogen, lower alkyl, lower alkoxy, halogen, lower alkyl substituted by halogen, lower alkoxy substituted by halogen, cyano or S(O) 2 -Iower alkyl; R 3 is lower alkyl, -(CH 2 ) m -aryl, optionally substituted by halogen, or is -(CH 2 ) m -cycloalkyl; R 4 and R 5 are independently from each other hydrogen or lower alkyl substituted by halogen, or are -(CR 2 ) m -aryl or -(CR 2 ) m -heteroaryl, wherein the rings may be substituted by one or more substituents, selected from halogen, lower alkyl, lower alkyl substituted by halogen, cyano, hydroxy, NR'R" or by lower alkoxy substituted by halogen, or are -(CR 2 ) m -cycloalkyl, optionally substituted by hydroxy or by aryl, or are a heteroalkyl ring, optionally substituted by =O or -(CR 2 ) m -aryl, or R 4 and R 5 are together with the N-atom to which they are attached a heterocyclic ring system, optionally substituted by lower alkyl, aryl or halogen-substituted aryl, and R may be independently from each other hydrogen, lower alkyl or lower alkyl substituted by hydroxyl; n is 1 or 2; m is 0, 1 or 2; or to a pharmaceutically active salt, a racemic mixture, an enantiomer, an optical isomer or a tautomeric form 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).
    • 本发明涉及式Ⅰ化合物，其中R1是羟基或NR'R“; R'和R”彼此独立地是氢，低级烷基，环烷基，或者可以与它们所在的N-原子一起形成 连接杂烷基环; R 2是氢，低级烷基，低级烷氧基，卤素，被卤素取代的低级烷基，被卤素取代的低级烷氧基，氰基或S（O）2 - 低级烷基） R 3是低级烷基， - （CH 2）m - 芳基，任选被卤素取代，或是 - （CH 2）m - 环烷基; R 4和R 5彼此独立地为氢或被卤素取代的低级烷基，或是 - （CR 2）m - 芳基或 - （CR 2）m - 杂芳基，其中所述环可以被一个或多个选自卤素， 低级烷基，被卤素，氰基，羟基，NR'R“取代的低级烷基或被卤素取代的低级烷氧基取代，或者是任选被羟基或芳基取代的 - （CR 2）m - 环烷基，或者是杂烷基环， 被取代为= O或 - （CR 2）m - 芳基，或者R 4和R 5与它们所连接的N-原子一起是杂环体系，任选地被低级烷基，芳基或卤素取代的芳基取代，R可以 彼此独立地为氢，被羟基取代的低级烷基或低级烷基; n为1或2; m为0,1或2;或者为药物活性盐，外消旋混合物，对映体，旋光异构体或互变异构体 已经发现本发明化合物是高潜在的NK-3受体拮抗剂 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）。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
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