专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明申请

WO2008128891A1 PYRROLIDINE DERIVATIVES AS DUAL NK1/NK3 RECEPTOR ANTAGONISTS 审中-公开
标题翻译：吡咯啉衍生物作为NK1 / NK3受体拮抗剂
公开(公告)号：WO2008128891A1
公开(公告)日：2008-10-30
申请号：PCT/EP2008/054261
申请日：2008-04-09
申请人： F. HOFFMANN-LA ROCHE AG , BISSANTZ, Caterina , HOFFMANN, Torsten , JABLONSKI, Philippe , KNUST, Henner , NETTEKOVEN, Matthias , RATNI, Hasane , WU, Xihan
发明人： BISSANTZ, Caterina , HOFFMANN, Torsten , JABLONSKI, Philippe , KNUST, Henner , NETTEKOVEN, Matthias , RATNI, Hasane , WU, Xihan
IPC分类号： C07D207/14 , C07D401/06 , C07D403/06 , C07D405/06 , C07D471/10 , A61K31/5377 , A61P25/28
CPC分类号： C07D207/14 , C07D401/06 , C07D403/06 , C07D405/06 , C07D471/10
摘要： The invention relates to pyrrolidine derivatives of formula (I) wherein R 1 is hydrogen, halogen or lower alkyl; R 2 is hydrogen, halogen, lower alkoxy or lower alkyl substituted by halogen; R 3 is -(CH 2 ) p -heterocyclyl optionally substituted by lower alkyl, halogen, -S(O) 2 -lower alkyl, -C(O)-lower alkyl, -C(O)O-lower alkyl, hydroxy, lower alkyl substituted by hydroxy, -(CH 2 ) p -O-lower alkyl, -NHCO-lower alkyl, or is C 3-6 -cycloalkyl optionally substituted by =O, -(CH 2 ) p -O-lower alkyl or lower alkinyl, or is unsubstituted or substituted aryl or heteroaryl, wherein the substituents are selected from the group consisting of lower alkyl, CN, -S(O) 2 -lower alkyl, halogen, -C(O) -lower alkyl, hydroxy, lower alkoxy or lower alkoxy substituted by halogen; or is -(CH 2 ) P -NR 4 R 5 ; R 4 /R 5 are independently from each other hydrogen, lower alkyl, -(CRR')p-lower alkyl substituted by hydroxy, -(CRR')p-O-lower alkyl, -(CRR')p-S-lower alkyl, -(CRR') p -O-lower alkyl substituted by hydroxy or C 3-6 -cycloalkyl; R/R' are independently from each other hydrogen, lower alkyl or lower alkyl substituted by hydroxyl; n is 1 or 2; o is 1 or 2; P is 0, 1, 2, 3 or 4; or to pharmaceutically active acid-addition salts thereof.
摘要翻译：本发明涉及式（I）的吡咯烷衍生物，其中R 1是氢，卤素或低级烷基; R 2是氢，卤素，低级烷氧基或被卤素取代的低级烷基; R 3是 - 任选被低级烷基，卤素，-S（O）2取代的 - （CH 2）2 - 杂环基）低级烷基，-C（O） - 低级烷基，-C（O）O-低级烷基，羟基，被羟基取代的低级烷基， - （CH 2）或低级烷基，-NHCO-低级烷基，或为任选被= O， - （CH 2）2取代的C 3-6环烷基，低级烷基或低级炔基，或未取代或取代的芳基或杂芳基，其中取代基选自低级烷基，CN，-S（O）2，低级烷基，卤素，-C（O） - 低级烷基，羟基，低级烷氧基或被卤素取代的低级烷氧基; 或是 - （CH 2）2 - - - - - - - - - - - - - - - R 4和R 5彼此独立地是氢，低级烷基， - 被羟基取代的 - （CRR'）对 - 低级烷基， - （CRR'）pO-低级烷基， - （CRR'）pS-低级烷基， - （CRR'）由羟基或C 3-6 - 环烷基取代的-O-低级烷基; R / R'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; o是1或2; P为0,1,2,3或4; 或其药学活性的酸加成盐。

2. 发明申请

WO2009153179A1 PYRROLIDINE DERIVATIVES AS NK2 RECEPTOR ANTAGONISTS 审中-公开
标题翻译：吡咯啉衍生物作为NK2受体拮抗剂
公开(公告)号：WO2009153179A1
公开(公告)日：2009-12-23
申请号：PCT/EP2009/056987
申请日：2009-06-08
申请人： F. HOFFMANN-LA ROCHE AG , BISSANTZ, Caterina , JABLONSKI, Philippe , KNUST, Henner , KOBLET, Andreas , LIMBERG, Anja , NETTEKOVEN, Matthias , RATNI, Hasane , RIEMER, Claus
发明人： BISSANTZ, Caterina , JABLONSKI, Philippe , KNUST, Henner , KOBLET, Andreas , LIMBERG, Anja , NETTEKOVEN, Matthias , RATNI, Hasane , RIEMER, Claus
IPC分类号： C07D207/14 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/12 , C07D405/06 , C07D405/12 , C07D405/14 , C07D413/10 , A61K31/40 , A61K31/4439 , A61K31/443 , A61P25/24
CPC分类号： C07D207/14 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/12 , C07D405/06 , C07D405/12 , C07D405/14 , C07D413/10
摘要： The present invention relates to a compound of Formula (I) wherein R 1 is hydrogen, halogen, cyano or lower alkyl; n is 1, 2 or 3; R 2 is hydrogen or lower alkyl; R 3 is an aryl- or a heteroaryl ring, wherein the rings are optionally substituted by one or two substituents R'; R' is selected from hydrogen, halogen, lower alkyl, lower alkoxy, lower alkyl substituted by halogen, lower alkoxy substituted by halogen,-S(O) 2 -lower alkyl, CN, -NR 4 R 5 , -C(O)-lower alkyl, heterocyclyl or heteroaryl; R 4 /R 5 are independently from each other hydrogen, -(CO)CF 3 or lower alkyl or is a non aromatic heterocyclic group (II) wherein X is N or CH; Y is -CH(R 7 )-; -N(R 7' )-, or O or can be SO 2 ; R 6 is hydrogen, lower alkyl or hydroxy; R 7 is hydrogen, hydroxy, =0, lower alkyl, lower alkoxy, -S(O) 2 -lower alkyl, -C(O)-lower alkyl, -C(O)CH 2 O-lower alkyl, -CH 2 CN, -C(O)CH 2 CN, -C(O)-cycloalkyl wherein the cycloalkyl group is optionally substituted by cyano, lower alkyl, one or two halogen atoms, =0 or by amino, or is -C(O)O-lower alkyl, -NH-lower alkyl, -NRC(O)O-lower alkyl, -NRC(O)-lower alkyl or -CH 2 O-lower alkyl; and R 7' is hydrogen, lower alkyl, -(CH 2 ) q -S(O) 2 -lower alkyl, -(CH 2 ) q -S(O) 2 -cycloalkyl, -C(O)-lower alkyl, -(CH 2 ) q -cycloalkyl, -C(O)CH 2 -O-lower alkyl, -(CH 2 ) q CN, -C(O)CN, -C(O)CH 2 CN, lower alkyl substituted by halogen, lower alkenyl substituted by halogen, -C(O)-cycloalkyl wherein the cycloalkyl group is optionally substituted by cyano, lower alkyl, one or two halogen atoms, =0 or by amino, or is -C(O)O-lower alkyl or -(CH 2 )qO-lower alkyl and q is O - 3; or R 6 and R 7 may form together with the carbon atoms to which they are attach a five or six- membered non aromatic ring or R 6 and R 7 may form together with the nitrogen and carbon atoms to which they are attach a five or six-membered non aromatic ring; p is 0, 1 or 2; Ar is aryl- or heteroaryl, wherein the rings are optionally substituted by one or two substituents R"; R' ' is selected from hydrogen, halogen, lower alkyl, lower alkyl substituted by halogen, lower alkoxy, lower alkoxy substituted by halogen, -O-CH 2 -cycloalkyl, -NR 4 R 5 , -CN, -CH(CH 3 )CN, -CH 2 O-lower alkyl or pyrrolyl; m is 0, 1 or 2 and o is 0; o is 0, 1 or 2 and m is 1 or pharmaceutically active salts, racemic mixtures, enantiomers, optical isomers or tautomeric forms thereof. The compounds may be used for the treatment of depression, anxiety or schizophrenia.
摘要翻译：本发明涉及式（I）的化合物，其中R 1是氢，卤素，氰基或低级烷基; n为1,2或3; R2是氢或低级烷基; R3是芳基或杂芳基环，其中环任选地被一个或两个取代基R'取代; R'选自氢，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（O）2 - 低级烷基，CN，-NR 4 R 5，-C（O） - 低级烷基，杂环基或杂芳基; R 4 / R 5彼此独立地为氢， - （CO）CF 3或低级烷基或为非芳族杂环基团（II），其中X为N或CH; Y是-CH（R 7） - ; -N（R 7'） - 或O或可以是SO 2; R6是氢，低级烷基或羟基; R 7是氢，羟基，= 0，低级烷基，低级烷氧基，-S（O）2 - 低级烷基，-C（O） - 低级烷基，-C（O）CH 2 O-低级烷基，-CH 2 CN，-C O）CH 2 CN，-C（O） - 环烷基，其中环烷基任选被氰基，低级烷基，一个或两个卤素原子取代，= 0或被氨基取代，或者是-C（O）O-低级烷基，-NH - 低级烷基，-NRC（O）O-低级烷基，-NRC（O） - 低级烷基或-CH 2 O-低级烷基; 并且R 7'是氢，低级烷基， - （CH 2）qS（O）2 - 低级烷基， - （CH 2）qS（O）2-环烷基，-C（O） - 低级烷基， - （CH 2），-C（O）CH 2 -O-低级烷基， - （CH 2）q CN，-C（O）CN，-C（O）CH 2 CN，被卤素取代的低级烷基，被卤素取代的低级链烯基，-C（O） - 环烷基，其中环烷基任选被氰基，低级烷基，一个或两个卤素原子，= O或氨基取代，或者是-C（O）O-低级烷基或 - （CH 2）q O-低级烷基，q是 O - 3; 或者R 6和R 7可以与它们所连接的五元或六元非芳香环的碳原子一起形成，或者R 6和R 7可以与它们所连接的五元或六元非芳环的氮和碳原子一起形成，芳香环 p为0,1或2; Ar是芳基或杂芳基，其中环任选地被一个或两个取代基R“取代; R”选自氢，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， O-CH 2 - 环烷基，-NR 4 R 5，-CN，-CH（CH 3）CN，-CH 2 O-低级烷基或吡咯基; m为0,1或2，o为0; o为0,1或2，m为1 或其药物活性盐，外消旋混合物，对映异构体，旋光异构体或互变异构体形式。化合物可用于治疗抑郁症，焦虑或精神分裂症。

3. 发明申请

WO2010060703A1 3-(BENZYLAMINO)-PYRROLIDINE DERIVATIVES AND THEIR USE AS NK-3 RECEPTOR ANTAGONISTS 审中-公开
标题翻译： 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
公开(公告)号：WO2010060703A1
公开(公告)日：2010-06-03
申请号：PCT/EP2009/064031
申请日：2009-10-26
申请人： F. HOFFMANN-LA ROCHE AG , BISSANTZ, Caterina , JABLONSKI, Philippe , KNUST, Henner , NETTEKOVEN, Matthias , RATNI, Hasane , RIEMER, Claus
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
摘要： 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).
摘要翻译：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）。

4. 发明申请

WO2010040663A1 PYRROLIDINE N-BENZYL DERIVATIVES 审中-公开
标题翻译：吡咯烷N-苄基衍生物
公开(公告)号：WO2010040663A1
公开(公告)日：2010-04-15
申请号：PCT/EP2009/062585
申请日：2009-09-29
申请人： F. HOFFMANN-LA ROCHE AG , BISSANTZ, Caterina , JABLONSKI, Philippe , KNUST, Henner , NETTEKOVEN, Matthias , PATINY-ADAM, Angélique , RATNI, Hasane , RIEMER, Claus
发明人： BISSANTZ, Caterina , JABLONSKI, Philippe , KNUST, Henner , NETTEKOVEN, Matthias , PATINY-ADAM, Angélique , RATNI, Hasane , RIEMER, Claus
IPC分类号： C07D207/10 , C07D401/06 , C07D401/10 , C07D401/14 , C07D403/06 , C07D403/10 , C07D405/06 , C07D413/06 , C07D413/10 , C07D417/10 , C07D471/04 , A61K31/40 , A61K31/4439 , A61K31/42 , A61K31/4025
CPC分类号： C07D207/14 , C07D401/06 , C07D401/10 , C07D401/14 , C07D403/06 , C07D403/10 , C07D405/06 , C07D413/06 , C07D413/10 , C07D417/10 , C07D471/04
摘要： The present invention relates to a compound of formula (I) wherein Ar 1 is aryl or heteroaryl; Ar 2 is aryl or heteroaryl; R 1 is hydrogen, halogen, hydroxy, 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, cyano, amino, mono or di- lower alkyl amino, C(O)-lower alkyl, NHC(O)-lower alkyl, cycloalkyl, heterocyclyl, or is heteroaryl, optionally substituted by lower alkyl; R 2 is hydrogen, halogen, lower alkyl, lower alkoxy, lower alkyl substituted by halogen or cyano; R 3 is hydrogen, halogen, lower alkyl or lower alkyl substituted by halogen; 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; or to a pharmaceutically active salt, to all stereoisomeric forms, including individual diastereoisomers and enantiomers as well as to 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).
摘要翻译：本发明涉及式（I）化合物，其中Ar 1是芳基或杂芳基; Ar2是芳基或杂芳基; R 1是氢，卤素，羟基，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）低级烷基氨基，氰基，氨基，一或二低级烷基氨基，C（O） - 低级烷基，NHC（O） - 低级烷基，环烷基，杂环基，或为任选被低级烷基取代的杂芳基; R2是氢，卤素，低级烷基，低级烷氧基，被卤素或氰基取代的低级烷基; R3是氢，卤素，低级烷基或被卤素取代的低级烷基; 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; 包括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的所有立体异构体形式。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。

5. 发明申请

WO2008084005A1 SPIROPIPERIDINE GLYCINAMIDE DERIVATIVES 审中-公开
标题翻译：螺旋磷酸甘氨酰胺衍生物
公开(公告)号：WO2008084005A1
公开(公告)日：2008-07-17
申请号：PCT/EP2008/050028
申请日：2008-01-03
申请人： F. HOFFMANN-LA ROCHE AG , BISSANTZ, Caterina , GOETSCHI, Erwin , GRUNDSCHOBER, Christophe , MASCIADRI, Raffaello , RATNI, Hasane , ROGERS-EVANS, Mark , SCHNIDER, Patrick
发明人： BISSANTZ, Caterina , GOETSCHI, Erwin , GRUNDSCHOBER, Christophe , MASCIADRI, Raffaello , RATNI, Hasane , ROGERS-EVANS, Mark , SCHNIDER, Patrick
IPC分类号： C07D491/113 , A61K31/438 , A61P25/00 , A61P9/00
CPC分类号： C07D491/113
摘要： The present invention is concerned with novel spiropiperidine glycinamide derivatives as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use as medicaments. The active compounds of the present invention are useful in the prevention and/or treatment of anxiety and depressive disorders and other diseases. In particular, the present invention is concerned with compounds of the general formula (I) wherein X, Y and R 1 to R 10 are as described herein.
摘要翻译：本发明涉及作为V1a受体拮抗剂的新型螺哌啶甘氨酰胺衍生物，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预防和/或治疗焦虑和抑郁症等疾病。特别地，本发明涉及通式（I）的化合物，其中X，Y和R 1至R 10如本文所述。

6. 发明申请

WO2008068184A1 INDOLES WHICH ACT AS VIA RECEPTOR ANTAGONISTS 审中-公开
标题翻译：其作为受体拮抗剂的作用
公开(公告)号：WO2008068184A1
公开(公告)日：2008-06-12
申请号：PCT/EP2007/062984
申请日：2007-11-29
申请人： F. HOFFMANN-LA ROCHE AG , BISSANTZ, Caterina , GRUNDSCHOBER, Christophe , MASCIADRI, Raffaello , RATNI, Hasane , ROGERS-EVANS, Mark , SCHNIDER, Patrick
发明人： BISSANTZ, Caterina , GRUNDSCHOBER, Christophe , MASCIADRI, Raffaello , RATNI, Hasane , ROGERS-EVANS, Mark , SCHNIDER, Patrick
IPC分类号： C07D401/14 , C07D491/04 , A61K31/4427 , A61P25/22 , A61P25/24
CPC分类号： C07D401/14 , C07D491/04
摘要： The present invention is concerned with novel indol-2-yl-carbonyl-piperidin- benzoimidazolon and indol-2-yl-carbonyl-piperidin-benzoxazolon derivatives as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use as medicaments. The active compounds of the present invention are useful in the prevention and/or treatment of anxiety and depressive disorders and other diseases. Present invention comprises compounds of the general formula (I) wherein R 1 to R 11 , X and Y are as defined in the specification.
摘要翻译：本发明涉及新的吲哚-2-基 - 羰基 - 哌啶 - 苯并咪唑酮和吲哚-2-基 - 羰基 - 哌啶 - 苯并恶唑酮衍生物作为V1a受体拮抗剂，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预防和/或治疗焦虑和抑郁症等疾病。本发明包括通式（I）的化合物，其中R 1至R 11，X和Y如说明书中所定义。

7. 发明申请

WO2007006688A1 INDOL-3-CARBONYL-SPIRO-PIPERIDINE DERIVATIVES AS V1A RECEPTOR ANTAGONISTS 审中-公开
标题翻译：作为V1A受体拮抗剂的吲哚-3-羰基 - 丝氨酸 - 哌啶衍生物
公开(公告)号：WO2007006688A1
公开(公告)日：2007-01-18
申请号：PCT/EP2006/063846
申请日：2006-07-04
申请人： F. HOFFMANN-LA ROCHE AG , BISSANTZ, Caterina , GRUNDSCHOBER, Christophe , RATNI, Hasane , ROGERS-EVANS, Mark , SCHNIDER, Patrick
发明人： BISSANTZ, Caterina , GRUNDSCHOBER, Christophe , RATNI, Hasane , ROGERS-EVANS, Mark , SCHNIDER, Patrick
IPC分类号： C07D401/06 , C07D471/10 , C07D491/10 , A61K31/454 , A61P9/00
CPC分类号： C07D471/10 , C07D401/06 , C07D491/10
摘要： This invention relates to indol-3-yl-carbonyl-spiro-piperidine derivatives which act as Via receptor antagonists and which are represented by Formula (I): wherein the spiro-piperidine head group A and the residues R 1 , R 2 and R 3 are as defined herein. The invention further relates to pharmaceutical compositions containing such compounds, their use in medicaments against dysmenorrhea, hypertension, chronic heart failure, inappropriate secretion of vasopressin, liver cirrhosis, nephrotic syndrome, obsessive compulsive disorder, anxious and depressive disorders, and methods of preparation thereof.
摘要翻译：本发明涉及充当Via受体拮抗剂并由式（I）表示的吲哚-3-基 - 羰基 - 螺 - 哌啶衍生物：其中螺哌啶头基A和残基R 1， SUP> R 2和R 3如本文所定义。本发明还涉及含有这些化合物的药物组合物，它们在抗痛经药物，高血压，慢性心力衰竭，不适当的血管加压素分泌，肝硬化，肾病综合征，强迫症，焦虑和抑郁障碍中的用途及其制备方法。

8. 发明申请

WO2010054961A1 SPIRO-5,6-DIHYDRO-4H-2,3,5,10B-TETRAAZA-BENZO[E]AZULENES 审中-公开
标题翻译：螺-5,6-二氢-4H-2,3,5,10b-四氮杂 - 苯并[e]薁
公开(公告)号：WO2010054961A1
公开(公告)日：2010-05-20
申请号：PCT/EP2009/064565
申请日：2009-11-04
申请人： F. HOFFMANN-LA ROCHE AG , BISSANTZ, Caterina , GOETSCHI, Erwin , JAKOB-ROETNE, Roland , MASCIADRI, Raffaello , PINARD, Emmanuel , RATNI, Hasane , ROGERS-EVANS, Mark , SCHNIDER, Patrick
发明人： BISSANTZ, Caterina , GOETSCHI, Erwin , JAKOB-ROETNE, Roland , MASCIADRI, Raffaello , PINARD, Emmanuel , RATNI, Hasane , ROGERS-EVANS, Mark , SCHNIDER, Patrick
IPC分类号： C07D487/10 , C07D495/10 , C07D491/107 , A61K31/4196 , A61K31/435 , A61P9/00
CPC分类号： C07D487/04 , C07D491/107 , C07D495/10
摘要： The present invention is concerned with spiro-dihydrotetraazabenzoazulene derivatives, i.e. spiro-5,6-dihydro-4H-2,3,5,10b-tetraaza-benzo[e]azulene derivatives of formula (I), wherein R 1 , R 2 , R 3 , X, Y, Z, m and n are as described herein. The compounds according to the invention act as Via receptor modulators and are useful as therapeutics acting peripherally and centrally in the conditions of dysmenorrhea, male or female sexual dysfunction, hypertension, chronic heart failure, inappropriate secretion of vasopressin, liver cirrhosis, nephrotic syndrome, anxiety, depressive disorders, obsessive compulsive disorder, autistic spectrum disorders, schizophrenia, and aggressive behavior.
摘要翻译：本发明涉及螺 - 二氢四氮杂苯并薁衍生物，即式（I）的螺-5,6-二氢-4H-2,3,5,10b-四氮杂 - 苯并[e]薁衍生物，其中R1，R2，R3 ，X，Y，Z，m和n如本文所述。根据本发明的化合物作为Via受体调节剂，并且可用作在痛经，男性或女性性功能障碍，高血压，慢性心力衰竭，不适当的血管加压素分泌，肝硬化，肾病综合征，焦虑症的外周和中心作用的治疗剂抑郁障碍，强迫症，孤独症谱系障碍，精神分裂症和侵略行为。

9. 发明申请

WO2008077810A2 SPIRO-PIPERIDINE DERIVATIVES 审中-公开
标题翻译：螺旋哌啶衍生物
公开(公告)号：WO2008077810A2
公开(公告)日：2008-07-03
申请号：PCT/EP2007/063879
申请日：2007-12-13
申请人： F. HOFFMANN-LA ROCHE AG , BISSANTZ, Caterina , GRUNDSCHOBER, Christophe , MASCIADRI, Raffaello , RATNI, Hasane , ROGERS-EVANS, Mark , SCHNIDER, Patrick
发明人： BISSANTZ, Caterina , GRUNDSCHOBER, Christophe , MASCIADRI, Raffaello , RATNI, Hasane , ROGERS-EVANS, Mark , SCHNIDER, Patrick
IPC分类号： C07D211/16 , C07D471/10 , C07D491/10 , A61K31/4355 , A61K31/437 , A61K31/438 , A61P9/00
CPC分类号： C07D491/107 , C07D211/16 , C07D221/20 , C07D401/06 , C07D405/06 , C07D471/10
摘要： The present invention is concerned with novel spiro-piperidine derivatives as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use as medicaments. The active compounds of the present invention are useful in the prevention and/or treatment of anxiety and depressive disorders and other diseases. The compounds of present invention are described with the general formula (I), wherein R 1 to R 5 , R 5' , R 7 to R 9 , R 7' , R 8' , X and Y are as defined in the specification.
摘要翻译：本发明涉及作为V1a受体拮抗剂的新型螺 - 哌啶衍生物，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预防和/或治疗焦虑和抑郁症等疾病。用通式（I）描述本发明的化合物，其中R 1至R 5，R 5'，R“ R 7，R 7，R 8，R 8，X和Y如说明书中所定义。

10. 发明申请

WO2008068185A1 SPIRO-PIPERIDINE DERIVATIVES AS VIA RECEPTOR ANTAGONISTS 审中-公开
标题翻译： SPIRO-哌啶衍生物作为受体拮抗剂
公开(公告)号：WO2008068185A1
公开(公告)日：2008-06-12
申请号：PCT/EP2007/062985
申请日：2007-11-29
申请人： F. HOFFMANN-LA ROCHE AG , BISSANTZ, Caterina , GRUNDSCHOBER, Christophe , MASCIADRI, Raffaello , RATNI, Hasane , ROGERS-EVANS, Mark , SCHNIDER, Patrick
发明人： BISSANTZ, Caterina , GRUNDSCHOBER, Christophe , MASCIADRI, Raffaello , RATNI, Hasane , ROGERS-EVANS, Mark , SCHNIDER, Patrick
IPC分类号： C07D471/10 , C07D491/10 , C07D519/00 , A61P9/00
CPC分类号： C07D471/10 , C07D491/10 , C07D519/00
摘要： The present invention is concerned with novel indol-2-yl-carbonyl-spiro-piperidine derivatives as VIa receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use as medicaments. The active compounds of the present invention are useful in the prevention and/or treatment of anxiety and depressive disorders and other diseases. The compounds of present invention are represented by the general formula (I) wherein R 1 to R 1 , X and Y are as defined in the specification.
摘要翻译：本发明涉及作为VIa受体拮抗剂的新的吲哚-2-基 - 羰基 - 螺 - 哌啶衍生物，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预防和/或治疗焦虑和抑郁症等疾病。本发明的化合物由通式（I）表示，其中R 1至R 1，X和Y如说明书中所定义。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式