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21. 发明申请

WO2010052199A1 HETEROCYCLIC GAMMA SECRETASE MODULATORS 审中-公开
标题翻译：杂环游戏分泌物调节剂
公开(公告)号：WO2010052199A1
公开(公告)日：2010-05-14
申请号：PCT/EP2009/064497
申请日：2009-11-03
申请人： F. HOFFMANN-LA ROCHE AG , BAUMANN, Karlheinz , GOETSCHI, Erwin , JOLIDON, Synese , LIMBERG, Anja , LUEBBERS, Thomas
发明人： BAUMANN, Karlheinz , GOETSCHI, Erwin , JOLIDON, Synese , LIMBERG, Anja , LUEBBERS, Thomas
IPC分类号： A61K31/4178 , C07D401/12 , C07D413/12 , C07D417/12
CPC分类号： C07D417/12 , C07D401/12 , C07D403/12 , C07D413/12
摘要： The invention relates to the use of compounds of formula wherein R 1 is a five or six membered heteroaryl group, optionally substituted by one or two R'; R' is lower alkyl; R 2 is hydrogen, lower alkyl, lower alkoxy, hydroxy, halogen or cyano; Z is N, C, O or S; V is N, C(R''), O or S; W is N, C(R''), O, or S; Y is N or C; with the proviso that only one of Z, V or W may be O or S; R'' is hydrogen, lower alkyl, lower alkyl substituted by halogen or hydroxy, or is C(O)O-R 4 ; L is a bond, -(CR 4 2 ) n -, -C(O)NR 4 -, -C(O)NR 4 CH 2 -, or -C(O)-; R 4 may be the same or different and is hydrogen or lower alkyl; R 3 is lower alkyl, phenyl, optionally substituted by one or more R''' or is cycloalkyl; R''' is halogen, cyano, lower alkyl, lower alkyl substituted by halogen or hydroxy, or is lower alkoxy or is C(O)O-R 4 ; n is 1, 2 or 3; or to pharmaceutically active acid addition salts for the manufacture of medicaments for the treatment of Alzheimer's disease, cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica or Down syndrome.
摘要翻译：本发明涉及下式化合物的用途，其中R 1是任选被一个或两个R'取代的五或六元杂芳基; R'是低级烷基; R2是氢，低级烷基，低级烷氧基，羟基，卤素或氰基; Z是N，C，O或S; V是N，C（R“），O或S; W是N，C（R“），O或S; Y为N或C; 条件是Z，V或W中只有一个可以是O或S; R“是氢，低级烷基，被卤素或羟基取代的低级烷基，或是C（O）O-R 4; L是键， - （CR 4 2）n - ， - C（O）NR 4 - ， - C（O）NR 4 CH 2 - 或-C（O） - ; R 4可以相同或不同，为氢或低级烷基; R3是低级烷基，任选被一个或多个R“取代的苯基，或是环烷基; R“是卤素，氰基，低级烷基，被卤素或羟基取代的低级烷基，或是低级烷氧基，或是C（O）O-R4; n为1,2或3; 或用于制备用于治疗阿尔茨海默氏病，脑淀粉样血管病，淀粉样变性遗传性脑出血，荷兰型（HCHWA-D），多发性梗死性痴呆，痴呆症或唐氏综合征的药物的药学活性的酸加成盐。

22. 发明申请

WO2009024502A1 PYRROLIDINE ARYL-ETHER AS NK3 RECEPTOR ANTAGONISTS 审中-公开
标题翻译：吡咯烷酮ARYL-ETHER作为NK3受体拮抗剂
公开(公告)号：WO2009024502A1
公开(公告)日：2009-02-26
申请号：PCT/EP2008/060566
申请日：2008-08-12
申请人： F. HOFFMANN-LA ROCHE AG , JABLONSKI, Philippe , KAWASAKI, Kenichi , KNUST, Henner , LIMBERG, Anja , NETTEKOVEN, Matthias , RATNI, Hasane , RIEMER, Claus , WU, Xihan
发明人： JABLONSKI, Philippe , KAWASAKI, Kenichi , KNUST, Henner , LIMBERG, Anja , NETTEKOVEN, Matthias , RATNI, Hasane , RIEMER, Claus , WU, Xihan
IPC分类号： C07D207/08 , C07D401/06 , C07D401/14 , C07D403/06 , C07D403/14 , C07D487/04 , C07D491/04 , C07D491/10 , A61K31/4468 , A61K31/496 , A61K31/506 , A61K31/5377 , A61P23/00 , A61P25/00 , A61P25/16
CPC分类号： C07D401/14 , C07D207/08 , C07D401/06 , C07D403/06 , C07D403/14 , C07D487/04 , C07D491/04 , C07D491/10
摘要： The invention relates to a compound of general formula (I) wherein is aryl or a five or six membered heteroaryl; is a six to nine membered mono or bi-heterocyclic group, wherein X may be a carbon atom, SO 2 or a further hetero atom, selected from the group consisting of N or O; if X is a carbon atom, O, SO 2 or unsubstituted N, then R 1 is hydrogen, hydroxy, cyano, -(CH 2 ) q -OH, -(CH 2 ) q -NRR', -(CH 2 ) q -CN, lower alkyl, -S(O) 2 -lower alkyl, -NR-S(O) 2 -lower alkyl, -C(O)-lower alkyl, -NR-C(O)-lower alkyl, phenyl, or is a heterocyclic group selected from piperidinyl- 2 -one; if X is a N-atom, substituted by R 1 , then R 1 is hydrogen, -(CH 2 ) q -OH, -(CH 2 ) q -NRR', -(CH 2 ) q -CN, lower alkyl, -S(O) 2 - lower alkyl, aryl or a five or six membered heteroaryl or -C(O)-lower alkyl, provided that q is 2 or 3. R/R' are independently from each other hydrogen or lower alkyl; R 2 is hydrogen, halogen, lower alkyl, cyano, lower alkoxy substituted by halogen, lower alkyl substituted by halogen or is a five or six membered heteroaryl; R 3 is hydrogen or halogen; R 4 is hydrogen or lower alkyl; n is 1 or 2; in case n is 2, R 1 may be the same or different; 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; q is 1, 2 or 3; s is 0, 1, 2, 3 or 4; 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).
摘要翻译：本发明涉及通式（I）的化合物，其中芳基或五或六元杂芳基; 是6至9元单或双杂环基团，其中X可以是选自N或O的碳原子，SO 2或另外的杂原子; 如果X是碳原子，O，SO2或未取代的N，那么R 1是氢，羟基，氰基， - （CH 2）q -OH， - （CH 2）q -NRR'， - （CH 2）q-CN ，低级烷基，-S（O）2 - 低级烷基，-NR-S（O）2 - 低级烷基，-C（O） - 低级烷基，-NR-C（O） - 低级烷基，苯基或选自哌啶-2-酮的杂环基; 如果X是被R 1取代的N-原子，则R 1是氢， - （CH 2）q -OH， - （CH 2）q -NRR'， - （CH 2）q-CN，低级烷基， -S（O）2 - 低级烷基，芳基或五或六元杂芳基或-C（O） - 低级烷基，条件是q为2或3.R / R'彼此独立地为氢或低级烷基; R 2是氢，卤素，低级烷基，氰基，被卤素取代的低级烷氧基，被卤素取代的低级烷基或是五或六元杂芳基; R 3是氢或卤素; R 4是氢或低级烷基; n为1或2; 在n为2的情况下，R 1可以相同或不同; 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; q为1,2或3; s为0，1，2，3或4; 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。

23. 发明申请

WO2011101304A2 PIPERIDINE DERIVATIVES 审中-公开
标题翻译：哌啶衍生物
公开(公告)号：WO2011101304A2
公开(公告)日：2011-08-25
申请号：PCT/EP2011/052101
申请日：2011-02-14
申请人： F. HOFFMANN-LA ROCHE AG , BAUMANN, Karlheinz , FLOHR, Alexander , GOETSCHI, Erwin , GREEN, Luke , JOLIDON, Synese , KNUST, Henner , LIMBERG, Anja , LUEBBERS, Thomas , THOMAS, Andrew
发明人： BAUMANN, Karlheinz , FLOHR, Alexander , GOETSCHI, Erwin , GREEN, Luke , JOLIDON, Synese , KNUST, Henner , LIMBERG, Anja , LUEBBERS, Thomas , THOMAS, Andrew
IPC分类号： C07D401/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D487/04 , C07D498/04 , A61K31/4523 , A61P25/28
CPC分类号： C07D471/04 , C07D401/14 , C07D413/14 , C07D417/14 , C07D487/04 , C07D498/04
摘要： The invention relates to compounds of formula (I). Hetaryl I is a five or six membered heteroaryl group, containing 1 to 3 heteroatoms, selected from O, S or N; hetaryl II is a five or six membered heteroaryl group, containing 1 to 3 heteroatoms, selected from O, S or N, or is a two membered ring system containing 1 to 4 heteroatoms selected from S, O or N, wherein at least one ring is aromatic in nature; R 1 is lower alkyl, lower alkoxy, lower alkyl substituted by halogen, or halogen; R 2 is halogen, lower alkyl, lower alkoxy, hydroxy, lower alkyl substituted by halogen, lower alkyl substituted by hydroxy or benzo[1,3]dioxolyl, or is -(CHR) p -phenyl, optionally substituted by halogen, lower alkyl, lower alkoxy, S(O) 2 -lower alkyl, cyano, nitro, lower alkoxy substituted by halogen, dimethylamino, -(CH 2 )P-NHC(O)O-Iower alkyl, or lower alkyl substituted by halogen, and R is hydrogen, halogen, hydroxy or lower alkoxy, or is cycloalkenyl or cycloalkyl, optionally substituted by hydroxy or lower alkyl substituted by halogen, or is a five or six membered heteroaryl group, containing 1 to 3 heteroatoms, selected from O, S or N, which is optionally substituted by halogen, lower alkyl, lower alkoxy or dimethylamino, or is O-phenyl, optionally substituted by halogen, or is heterocycloalkyl, optionally substituted by halogen, hydroxy, lower alkyl substituted by halogen or C(O)O-lower alkyl; R 3 is hydrogen, lower alkyl, cyano or phenyl; R 4 is lower alkoxy, lower alkyl or halogen; p is 0 or 1; n is 0, 1 or 2; if n is 2 then R 4 may be the same or different; m is 0, 1 or 2; if m is 2 then R 1 may be the same or different; o is 0, 1, 2 or 3, if o is 2 or 3 then R 2 may be the same or different; or to pharmaceutically active acid addition salts thereof. The compounds of formula (I) are modulators for amyloid beta and thus, they may be useful for the treatment or prevention of a disease associated with the deposition of β-amyloid in the brain, in particular Alzheimer's disease, and other diseases such as cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica and Down syndrome.
摘要翻译：本发明涉及式（I）的化合物。 Hetary11是含有1至3个选自O，S或N的杂原子的五元或六元杂芳基; 杂芳基II是含有1至3个选自O，S或N的杂原子的五元或六元杂芳基，或者是含有1至4个选自S，O或N的杂原子的二元环体系，其中至少一个环本质上是芳香的; R 1为低级烷基，低级烷氧基，被卤素取代的低级烷基或卤素; R 2是卤素，低级烷基，低级烷氧基，羟基，被卤素取代的低级烷基，被羟基或苯并[1,3]二氧杂环戊烯基取代的低级烷基，或者是 - （CHR）p 低级烷基，低级烷氧基，S（O）2 - 低级烷基，氰基，硝基，被卤素取代的低级烷氧基，二甲基氨基， - （CH 2）（O）O-低级烷基或被卤素取代的低级烷基，且R为氢，卤素，羟基或低级烷氧基，或者为环烯基或环烷基，任选被羟基或低级被卤素取代的烷基，或者是含有1至3个选自O，S或N的杂原子的五元或六元杂芳基，其任选被卤素，低级烷基，低级烷氧基或二甲基氨基取代，或者是O-苯基，任选被卤素取代，或者为任选被卤素，羟基，被卤素取代的低级烷基或C（O）O-低级烷基取代的杂环烷基; R 3是氢，低级烷基，氰基或苯基; R 4是低级烷氧基，低级烷基或卤素; p是0或1; n是0,1或2; 如果n是2，则R 4可以相同或不同; m是0,1或2; 如果m是2，则R 1可以相同或不同; o是0,1,2或3，如果o是2或3，则R 2可以相同或不同; 或其药学活性酸加成盐。式（I）化合物是β-淀粉样蛋白的调节剂，因此它们可用于治疗或预防与β-淀粉状蛋白在脑中沉积相关的疾病，特别是阿尔茨海默氏病和其他疾病，如脑具有淀粉样变性的遗传性脑出血，荷兰型（HCHWA-D），多发性梗塞型痴呆，拳击员痴呆和唐氏综合症。

24. 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。

25. 发明申请

WO2004069133A2 NOVEL N-MONOACYLATED O-PHENYLENEDIAMINES, THEIR CONDENSED HETEROCYCLIC DERIVATIVES AND THEIR USE AS PHARMACEUTICAL AGENTS 审中-公开
标题翻译：新型N-单取代邻苯二甲酸，它们的稠合杂环衍生物及其作为药物代谢物的用途
公开(公告)号：WO2004069133A2
公开(公告)日：2004-08-19
申请号：PCT/EP2004/001045
申请日：2004-02-05
申请人： F. HOFFMANN-LA ROCHE AG
发明人： FERTIG, Georg , HERTING, Frank , KUBBIES, Manfred , LIMBERG, Anja , REIFF, Ulrike , WEIDNER, Michael
IPC分类号： A61K
CPC分类号： C07D333/70 , C07D209/42 , C07D307/85
摘要： Objects of the present invention are new mono-acylated o-phenylendiamines derivatives of formula (I), wherein X represents N, S or O; R represents CH 3 -(O-CH 2 CH 2 )n- or C 1 -C 6 -alkyl, which alkyl group is monosubstituted with -CO 2 H, -OH, R 1 R 2 N-, pyridin-2-yl, pyrrolidin-1-yl, piperidino or morpholino; R 1 , R 2 independently from each other denote C 1 -C 6 alkyl; n is 1, 2, 3 or 4; and pharmaceutically acceptable salts thereof. The present invention also encompasses pharmaceutically acceptable salts or prodrugs of the compounds of formula I as well as the use of these compounds to produce medicaments.
摘要翻译：本发明的目的是式（I）的新的单酰化邻苯基亚胺衍生物，其中X表示N，S或O; R表示CH 3 - （O-CH 2 CH 2）n - 或C 1 -C 6烷基，该烷基被-CO 2 H，-OH，R 1 R 2，吡啶-2-基，吡咯烷-1-基哌啶子基或吗啉代; R 1，R 2彼此独立地表示C 1 -C 6烷基; n为1,2,3或4; 及其药学上可接受的盐。本发明还包括式I化合物的药学上可接受的盐或前药以及这些化合物用于制备药物的用途。

26. 发明申请

WO2018065340A1 BICYCLIC HETEROARYL DERIVATIVES 审中-公开
标题翻译：双环杂芳基衍生物
公开(公告)号：WO2018065340A1
公开(公告)日：2018-04-12
申请号：PCT/EP2017/074927
申请日：2017-10-02
申请人： F. HOFFMANN-LA ROCHE AG , HOFFMANN-LA ROCHE INC.
发明人： BARTELS, Bjoern , JAKOB-ROETNE, Roland , LIMBERG, Anja , NEIDHART, Werner , RATNI, Hasane , REUTLINGER, Michael , VASTAKAITE, Greta
IPC分类号： C07D487/04 , A61K31/4196 , A61K31/437 , A61K31/551
摘要： The present invention relates to a compound of formula (I), wherein R 1 is hydrogen, lower alkyl, lower alkyl substituted by halogen, halogen, lower alkoxy or lower alkoxy substituted by halogen; and R 1 may be different if n is 2 or 3; R 2 is hydrogen, lower alkyl, lower alkyl substituted by halogen, halogen, CN, lower alkoxy or lower alkoxy substituted by halogen; X is CH or N; m is 1, 2 or 3; -( ) m is –(CH 2 ) m -; n is 1, 2 or 3; Ar is a five membered heteroaryl group, selected from formula (A), (B), (C), (D), (E) or (F), wherein R 3 is hydrogen, methyl or chloro; R 4 is hydrogen or methyl; R 5 is F, Cl, CHF 2 or CF 3 ; or to pharmaceutically active acid addition salts thereof. The compounds may be used for the treatment of Alzheimer's disease, cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica or Down syndrome.
摘要翻译：本发明涉及式（I）化合物，其中R 1是氢，低级烷基，被卤素，卤素，低级烷氧基或低级烷氧基取代的低级烷基被卤素取代; 如果n是2或3，R 1和R 1可以不同; R 2是氢，低级烷基，被卤素，卤素，CN，低级烷氧基或被卤素取代的低级烷氧基取代的低级烷基; X是CH或N; m是1,2或3; - （）_{m 是 - （CH _{2 ）_{m - ; n是1,2或3; Ar是选自式（A），（B），（C），（D），（E）或（F）的五元杂芳基，其中R 3是氢，甲基或氯; R 4是氢或甲基; R 5是F，Cl，CHF 2或CF 3; 或其药学活性酸加成盐。这些化合物可用于治疗阿尔茨海默氏病，脑淀粉样血管病，具有淀粉样变性的遗传性脑出血，荷兰型（HCHWA-D），多发梗塞性痴呆，拳击员痴呆或唐氏综合症。}}}

27. 发明申请

WO2004054999A1 ENANTIOMERS OF THIOPHENE HYDROXAMIC ACID DERIVATIVES AND THEIR USE AS HDAC INHIBITORS 审中-公开
标题翻译：硫代羟基酸衍生物的合成及其作为HDAC抑制剂的用途
公开(公告)号：WO2004054999A1
公开(公告)日：2004-07-01
申请号：PCT/EP2003/014235
申请日：2003-12-15
申请人： F. HOFFMANN-LA ROCHE AG
发明人： GROSSMANN, Adelbert , HERTING, Frank , KOERNER, Matthias , KUENKELE, Klaus-Peter , LIMBERG, Anja , MUNDIGL, Olaf , TIBES, Ulrich
IPC分类号： C07D333/38
CPC分类号： C07D409/12 , C07D333/38 , C07D413/12
摘要： Compounds of Formula (I) wherein Ar, R1 and R2 have the meanings defined in the specification, process of manufacturing these compounds and medicaments with HDAC inhibitor activity containing such a compound.
摘要翻译：式（I）的化合物，其中Ar，R 1和R 2具有本说明书中定义的含义，制备这些化合物的方法和含有这种化合物的HDAC抑制剂活性的药物。

28. 发明申请

WO2004052838A1 ARYLENE-CARBOXYLIC ACID (2-AMINO-PHENYL)-AMIDE DERIVATIVES AS PHARMACEUTICAL AGENTS 审中-公开
标题翻译：作为药物代谢物的亚甲基 - 羧酸（2-氨基苯基）酰胺衍生物
公开(公告)号：WO2004052838A1
公开(公告)日：2004-06-24
申请号：PCT/EP2003/013941
申请日：2003-12-09
申请人： F. HOFFMANN-LA ROCHE AG
发明人： FERTIG, Georg , HERTING, Frank , KOERNER, Matthias , KUBBIES, Manfred , LIMBERG, Anja , REIFF, Ulrike , WEIDNER, Michael
IPC分类号： C07C233/77
CPC分类号： C07D213/82 , C07C237/42 , C07C275/24 , C07C2601/02 , C07C2601/08 , C07C2601/10 , C07C2601/14 , C07D333/38
摘要： The present invention describes compounds of general formula (I), a process for their manufacture, medicaments containing them and their manufacture as well as the use of these compounds as pharmaceutical agents. The compounds according to this invention show antiproliferative and differentiation- inducing activity, which results in inhibition of tumor cell proliferation, induction of apoptosis and inhibition of invasion.
摘要翻译：本发明描述了通式（I）的化合物，其制备方法，含有它们的药物及其制备以及这些化合物作为药剂的用途。根据本发明的化合物显示抗增殖和分化诱导活性，其导致抑制肿瘤细胞增殖，诱导凋亡和抑制侵袭。

29. 发明申请

WO2018060300A1 BRIDGED PIPERIDINE DERIVATIVES 审中-公开
标题翻译：桥联的哌啶衍生物
公开(公告)号：WO2018060300A1
公开(公告)日：2018-04-05
申请号：PCT/EP2017/074575
申请日：2017-09-28
申请人： F. HOFFMANN-LA ROCHE AG , HOFFMANN-LA ROCHE INC.
发明人： BARTELS, Bjoern , JAKOB-ROETNE, Roland , LIMBERG, Anja , NEIDHART, Werner , RATNI, Hasane , REUTLINGER, Michael , SARIE, Jérôme Charles , VASTAKAITE, Greta
IPC分类号： C07D519/00 , A61K31/4196 , A61P25/28
摘要： The present invention relates to a compound of formula (I), wherein R 1 is hydrogen, lower alkyl, lower alkyl substituted by halogen, halogen, lower alkoxy or lower alkoxy substituted by halogen; R may be the same or different, if n = 2 or 3; n is 1, 2 or 3; m is 1, 2 or 3; Ar is a five or six membered heteroaryl group, selected from (II), (III), (IV) or (V) wherein R 2 is hydrogen, lower alkyl, lower alkyl substituted by halogen, halogen or lower alkoxy; R 3 is hydrogen or halogen; -() m - is –(CH 2 ) m - or to pharmaceutically active acid addition salts thereof. The compounds may be used for the treatment of Alzheimer's disease, cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica or Down syndrome.
摘要翻译：本发明涉及式（I）化合物，其中R 1是氢，低级烷基，被卤素，卤素，低级烷氧基或低级烷氧基取代的低级烷基被卤素取代; 如果n = 2或3，则R可以相同或不同; n是1,2或3; m是1,2或3; Ar是选自（II），（III），（IV）或（V）的五元或六元杂芳基，其中R 2是氢，低级烷基，被卤素取代的低级烷基，卤素或低级烷氧基; R 3是氢或卤素; - （ - ）m - 是 - （CH 2）m-或其药学活性酸加成盐。这些化合物可用于治疗阿尔茨海默氏病，脑淀粉样血管病，具有淀粉样变性的遗传性脑出血，荷兰型（HCHWA-D），多发梗塞性痴呆，拳击员痴呆或唐氏综合症。

30. 发明申请

WO2014040969A1 2-OXO-2,3-DIHYDRO-INDOLES FOR THE TREATMENT OF CNS DISORDERS 审中-公开
标题翻译：用于治疗CNS病症的2-氧代-2,3-二氢吲哚
公开(公告)号：WO2014040969A1
公开(公告)日：2014-03-20
申请号：PCT/EP2013/068668
申请日：2013-09-10
申请人： F. HOFFMANN-LA ROCHE AG , HOFFMANN-LA ROCHE INC.
发明人： BRUNNER, Daniela , MALBERG, Jessica , SHANKAR, Bavani G. , KOLCZEWSKI, Sabine , LIMBERG, Anja , PRINSSEN, Eric , RIEMER, Claus , STOLL, Theodor
IPC分类号： C07D403/12 , C07D401/14 , C07D401/12 , C07D471/04 , C07D209/34 , A61K31/44 , A61K31/506 , A61K31/4178 , A61K31/404 , A61K31/437 , A61P25/00
CPC分类号： C07D471/04 , A61K31/4439 , A61K31/444 , A61K31/506 , A61K45/06 , C07D209/34 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/14
摘要： The present invention is concerned with 2-oxo-2,3-dihydro-indoles of general formula (I) wherein (N 1 ) is phenyl or a heteroaryl group, selected from pyridinyl, pyrimidinyl, imidazolyl, isoxazolyl or pyrazolyl; (N 2 ) is phenyl or pyridinyl, wherein the N atom in the pyridinyl group may be on all free positions; R 1 is hydrogen, lower alkyl, lower alkyl substituted by halogen, lower alkoxy or halogen; n is 1 or 2; if n is 2, R 1 may be the same or not; R 2 /R 2' are independently from each other lower alkyl, or form together with the carbon atom to which they are attached a C 3-6 -cycloalkyl ring; R 3 is lower alkyl, C 3-6 -cycloalkyl, CH 2 -C 3-6 -cycloalkyl, C 3-6 -cycloalkyl wherein one ring-carbon atom is replaced by -O-, (CH 2 ) 3 -O-C 3-6 -cycloalkyl, lower alkyl substituted by hydroxy, lower alkyl substituted by halogen, (CH 2 ) 3 -S(O) 2 -C 3-6 -cycloalkyl or (CH 2 ) 2 -S(O) 2 -lower alkyl; R 4 is hydrogen, halogen or lower alkyl; m is 1 or 2; if m is 2, R 4 may be the same or not; as well as with a pharmaceutically acceptable salts thereof, with a racemic mixture, or with its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof.
摘要翻译：本发明涉及通式（I）的2-氧代-2,3-二氢 - 吲哚，其中（N1）是苯基或杂芳基，选自吡啶基，嘧啶基，咪唑基，异恶唑基或吡唑基; （N 2）是苯基或吡啶基，其中吡啶基中的N原子可以在所有的自由位上; R1是氢，低级烷基，被卤素取代的低级烷基，低级烷氧基或卤素; n为1或2; 如果n为2，则R1可以相同或不相同; R2 / R2'彼此独立地为低级烷基，或与它们所连接的碳原子一起形成C 3-6 - 环烷基环; R3是低级烷基，C3-6-环烷基，CH2-C3-6环烷基，C3-6-环烷基，其中一个环 - 碳原子被-O - ，（CH2）3-O-C3-6-环烷基取代，被羟基取代的低级烷基，被卤素取代的低级烷基，（CH 2）3 -S（O）2 -C 3-6 - 环烷基或（CH 2）2 -S（O） R4是氢，卤素或低级烷基; m为1或2; 如果m为2，则R4可以相同或不相同; 以及其药学上可接受的盐，与外消旋混合物或其相应的对映异构体和/或其光学异构体和/或立体异构体。

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