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1. 发明申请

WO2011101304A3 PIPERIDINE DERIVATIVES 审中-公开
标题翻译：哌啶衍生物
公开(公告)号：WO2011101304A3
公开(公告)日：2011-10-20
申请号：PCT/EP2011052101
申请日：2011-02-14
申请人： HOFFMANN LA ROCHE , 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 , A61K31/4523 , A61P25/28 , C07D413/14 , C07D417/14 , C07D471/04 , C07D487/04 , C07D498/04
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; R1 is lower alkyl, lower alkoxy, lower alkyl substituted by halogen, or halogen; R2 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, -(CH2)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; R3 is hydrogen, lower alkyl, cyano or phenyl; R4 is lower alkoxy, lower alkyl or halogen; p is 0 or 1; n is 0, 1 or 2; if n is 2 then R4 may be the same or different; m is 0, 1 or 2; if m is 2 then R1 may be the same or different; o is 0, 1, 2 or 3, if o is 2 or 3 then R2 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 ß-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）化合物。芳基I是含有1至3个选自O，S或N的杂原子的五或六元杂芳基; 杂芳基II是含有1至3个选自O，S或N的杂原子的五或六元杂芳基，或是含有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 R1是低级烷基，低级烷氧基，被卤素取代的低级烷基或卤素; R 2为卤素，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]二氧杂环戊烯取代的低级烷基，或为 - （CHR）对 - 苯基，任选被卤素，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， - （CH2）P-NHC（O）O-低级烷基或被卤素取代的低级烷基，R是氢，卤素，羟基或低级烷氧基，或是任选被羟基或被卤素取代的低级烷基取代的环烯基或环烷基，或是含有1至3个选自O，S或N的杂原子的五或六元杂芳基，其中或任选被卤素取代的O-苯基，或任选被卤素取代的杂环烷基，羟基，被卤素或C（O）O-低级烷基取代的低级烷基， ; R3是氢，低级烷基，氰基或苯基; R4是低级烷氧基，低级烷基或卤素; p为0或1; n为0,1或2; 如果n为2，则R4可以相同或不同; m为0,1或2; 如果m为2，则R1可以相同或不同; o为0,1,2或3，如果o为2或3，则R2可以相同或不同; 或其药物活性的酸加成盐。式（I）化合物是淀粉样蛋白β的调节剂，因此它们可用于治疗或预防与脑中β-淀粉样蛋白沉积相关的疾病，特别是阿尔茨海默病，以及其他疾病如脑淀粉样血管病，淀粉样变性遗传性脑出血，荷兰型（HCHWA-D），多发性梗死性痴呆，痴呆和唐氏综合征。

2. 发明申请

WO2006061136A2 MALONAMIDE DERIVATIVES 审中-公开
标题翻译：马来酰胺衍生物
公开(公告)号：WO2006061136A2
公开(公告)日：2006-06-15
申请号：PCT/EP2005012834
申请日：2005-12-01
申请人： HOFFMANN LA ROCHE , FLOHR ALEXANDER , JAKOB-ROETNE ROLAND , WOSTL WOLFGANG
发明人： FLOHR ALEXANDER , JAKOB-ROETNE ROLAND , WOSTL WOLFGANG
IPC分类号： C07D267/14 , A61K31/553 , A61P25/28
CPC分类号： C07D267/14 , C07D413/12
摘要： The invention relates to compounds of the general Formula (I) wherein R is halogen, lower alkyl or lower alkyl substituted by halogen; R 1 is hydrogen, lower alkyl or lower alkyl substituted by halogen or hydroxy, or is lower alkenyl, -(CH 2 ) n -cycloalkyl, -(CH 2 ) n -COR', or is benzyl, optionally substituted by halogen, or is -(CH 2 ) n -morpholinyl; R' is lower alkoxy, hydroxy or amino; R 2 is hydrogen, lower alkyl or di-lower alkyl, lower alkyl substituted by halogen or hydroxy, or is benzyl or cycloalkyl; R 3 is lower alkyl or lower alkyl substituted by halogen, or is benzyl, optionally substituted by two halogen atoms, or is -(CH 2 ) n -cycloalkyl or -(CH 2 ) n -pyridinyl; X is -CR 4 R 4 - or - CR 4 R 4' -O-; R 4 /R 4 ' is independently from each other hydrogen, halogen, lower alkyl, lower alkoxy, hydroxy or -CH 2 -2-[1,3]dioxalan-; N is 0, 1 or 2; to pharmaceutically suitable acid addition salts thereof and to all forms of optically pure enantiomers, recemates or diastereomers and diastereomeric mixtures thereof for the treatment of Alzheimer's disease.
摘要翻译：本发明涉及通式（I）的化合物，其中R是卤素，被卤素取代的低级烷基或低级烷基; R 1是氢，被卤素或羟基取代的低级烷基或低级烷基，或者是低级烯基， - （CH 2 CH 2）n - ， - （CH 2 CH 2）n -COR'，或是任选被卤素取代的苄基，或是 - （CH 2）2 - >名词 - 吗啉基; R'是低级烷氧基，羟基或氨基; R 2是氢，低级烷基或二低级烷基，被卤素或羟基取代的低级烷基，或是苄基或环烷基; R 3是被卤素取代的低级烷基或低级烷基，或是任选被两个卤素原子取代的苄基，或是 - （CH 2） - （CH 2）n - 亚烷基或 - （CH 2）n - X是-CR 4 S 4 - 或 - CR 4 -OR 4'-O-; R 4和R 4彼此独立地为氢，卤素，低级烷基，低级烷氧基，羟基或-CH 2 - [1,3] dioxalan-; N为0,1或2; 其药学上合适的酸加成盐和所有形式的用于治疗阿尔茨海默氏病的光学纯对映异构体，受体或非对映异构体和非对映体混合物。

3. 发明申请

WO2008034735A3 4-OXO-2,3,4,5-TETRAHYDRO-BENZO[B][1,4]DIAZEPINE DERIVATIVES 审中-公开
标题翻译： 4-氧代-2,3,4,5-四氢苯并[B] [1,4]二氮杂卓衍生物
公开(公告)号：WO2008034735A3
公开(公告)日：2008-05-08
申请号：PCT/EP2007059488
申请日：2007-09-11
申请人： HOFFMANN LA ROCHE , FLOHR ALEXANDER , JAKOB-ROETNE ROLAND , WOSTL WOLFGANG
发明人： FLOHR ALEXANDER , JAKOB-ROETNE ROLAND , WOSTL WOLFGANG
IPC分类号： C07D243/14 , A61K31/5513 , A61P25/28
CPC分类号： C07D243/12
摘要： The invention relates to 4-oxo-2,3,4,5-tetrahydro-benzo[b][1,4]diazepine derivatives of formula (I) wherein R 1 , R 2 , R 3 and R 4 are as defined in the description and claims, which are ?-secretase inhibitors and which may be useful in the treatment of Alzheimer's disease.
摘要翻译：本发明涉及式（I）的4-氧代-2,3,4,5-四氢 - 苯并[b] [1,4]二氮杂衍生物，其中R 1，R 2， R 3和R 4如说明书和权利要求书中所定义，它们是β-分泌酶抑制剂并且可用于治疗阿尔茨海默氏病。

4. 发明申请

WO0197786A3 BENZOTHIAZOLE DERIVATIVES 审中-公开
标题翻译：苯并噻唑衍生物
公开(公告)号：WO0197786A3
公开(公告)日：2002-12-12
申请号：PCT/EP0106506
申请日：2001-06-08
申请人： HOFFMANN LA ROCHE
发明人： ALANINE ALEXANDER , FLOHR ALEXANDER , MILLER AUBRY KERN , NORCROSS ROGER DAVID , RIEMER CLAUS
IPC分类号： A61K31/422 , A61K31/423 , A61K31/427 , A61K31/428 , A61K31/4439 , A61K31/444 , A61K31/4545 , A61K31/455 , A61K31/4725 , A61K31/496 , A61K31/5375 , A61K31/5377 , A61K31/541 , A61K31/551 , A61K31/5513 , A61P11/06 , A61P21/02 , A61P25/04 , A61P25/16 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/26 , A61P25/28 , C07D277/82 , C07D417/04 , C07D417/12 , C07D417/14
CPC分类号： C07D417/04 , A61K31/427 , A61K31/428 , A61K31/4439 , A61K31/444 , A61K31/455 , A61K31/5375 , A61K31/541 , A61K31/5513 , C07D277/82 , C07D417/12 , C07D417/14
摘要： The present invention relates to compounds of the general formula (I) and to their pharmaceutically acceptable salts for the treatment of diseases related to the adenosine A2 receptor, novel compounds of formula I-A per se,their manufacture, medicaments based on a compound in accordance with the invention and their production as well as the use of compounds of compounds of formula I in the control or prevention of illnesses based on the modulation of the adenosine system, such as Alzheimer's disease, Parkinson's disease, neuroprotection, schizophrenia, anxiety, pain, respiration deficits, depression, asthma, allergic responses hypoxia, ischaemia, seizure and substance abuse. Furthermore, compounds of the present invention may be useful as sedatives, muscle relaxants, antipsychotics, antiepileptics, anticonvulsants and cardiaprotective agents.
摘要翻译：本发明涉及通式（I）的化合物及其药学上可接受的盐，用于治疗与腺苷A2受体相关的疾病，式IA本身的新化合物及其制备，基于根据本发明及其生产以及式I化合物的化合物在控制或预防基于腺苷系统如阿尔茨海默氏病，帕金森病，神经保护，精神分裂症，焦虑，疼痛，呼吸的腺苷系统的调节中的用途缺陷，抑郁症，哮喘，过敏反应缺氧，局部缺血，癫痫发作和药物滥用。此外，本发明的化合物可用作镇静剂，肌肉松弛剂，抗精神病药，抗癫痫剂，抗惊厥药和心脏保护剂。

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