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1. 发明申请

WO2008092786A1 6-OXO-6,7-DIHYDRO-5H-DIBENZO[B,D]AZEPIN-7-YL DERIVATIVES 审中-公开
标题翻译： 6-OXO-6,7-二氢-5H-二苯并[B，D] AZEPIN-7-YL衍生物
公开(公告)号：WO2008092786A1
公开(公告)日：2008-08-07
申请号：PCT/EP2008/050768
申请日：2008-01-23
申请人： F. HOFFMANN-LA ROCHE AG , FLOHR, Alexander , JAKOB-ROETNE, Roland , WOSTL, Wolfgang
发明人： FLOHR, Alexander , JAKOB-ROETNE, Roland , WOSTL, Wolfgang
IPC分类号： C07D223/18 , A61K31/55 , A61P35/00 , A61P25/28
CPC分类号： C07D223/18
摘要： The invention relates to 6-oxo-6,7-dihydro-5H-dibenzo[b,d]azepin-7-yl derivatives of Formula (I) wherein R 1 , R 2 and R 3 are as defined herein, as γ-secretase inhibitors useful in the treatment of Alzheimer's disease or common cancer including but not limited to cervical carcinomas and breast carcinomas and malignancies of the hematopoietic system.
摘要翻译：本发明涉及式（I）的6-氧代-6,7-二氢-5H-二苯并[b，d]吖庚因-7-基衍生物，其中R 1，R 2，作为可用于治疗阿尔茨海默病或常见癌症的γ-分泌酶抑制剂，包括但不限于宫颈癌和乳腺癌以及造血系统的恶性肿瘤。

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

WO2011138293A1 2,5,6,7-TETRAHYDRO-[1,4]OXAZEPIN-3-YLAMINE OR 2,3,6,7-TETRAHYDRO-[1,4]OXAZEPIN-5-YLAMINE COMPOUNDS 审中-公开
标题翻译： 2,5,6,7-四氢 - [1,4]氧杂环己烯-3-基胺或2,3,6,7-四氢 - [1,4]氧杂环己烯-5-胺化合物
公开(公告)号：WO2011138293A1
公开(公告)日：2011-11-10
申请号：PCT/EP2011/056990
申请日：2011-05-03
申请人： F. HOFFMANN-LA ROCHE AG , SIENA BIOTECH S.P.A. , BANNER, David , GUBA, Wolfgang , HILPERT, Hans , HUMM, Roland , MAUSER, Harald , MAYWEG, Alexander, V. , NARQUIZIAN, Robert , POWER, Eoin , ROGERS-EVANS, Mark , ROMBACH, Didier , WOLTERING, Thomas , WOSTL, Wolfgang
发明人： BANNER, David , GUBA, Wolfgang , HILPERT, Hans , HUMM, Roland , MAUSER, Harald , MAYWEG, Alexander, V. , NARQUIZIAN, Robert , POWER, Eoin , ROGERS-EVANS, Mark , ROMBACH, Didier , WOLTERING, Thomas , WOSTL, Wolfgang
IPC分类号： C07D267/10 , C07D413/12 , C07D417/12 , A61K31/553 , A61P25/28
CPC分类号： C07D267/10 , C07D413/12 , C07D417/12
摘要： This invention relates to compounds of the formula (I), wherein A, B and R 1 to R 7 are as described below, or to pharmaceutically acceptable salts thereof. These compounds are BACE1 and/or BACE2 inhibitors and can be used as 5 medicaments for the therapeutic and/or prophylactic treatment of diseases such as Alzheimer's disease, diabetes, particularly type 2 diabetes, and other metabolic disorders.
摘要翻译：本发明涉及式（I）化合物，其中A，B和R 1至R 7如下所述，或其药学上可接受的盐。这些化合物是BACE1和/或BACE2抑制剂，可用作5种药物用于治疗和/或预防性治疗诸如阿尔茨海默病，糖尿病，特别是2型糖尿病和其它代谢疾病的疾病。

4. 发明申请

WO2009103626A1 4, 5-DIHYDRO-OXAZOL-2-YL AMINE DERIVATIVES 审中-公开
标题翻译： 4,5-二氢 - 氧杂-2-氨基胺衍生物
公开(公告)号：WO2009103626A1
公开(公告)日：2009-08-27
申请号：PCT/EP2009/051452
申请日：2009-02-09
申请人： F. HOFFMANN-LA ROCHE AG , SIENA BIOTECH S.P.A , ANDREINI, Matteo , GABELLIERI, Emanuele , GUBA, Wolfgang , MARCONI, Guido , NARQUIZIAN, Robert , POWER, Eoin , TRAVAGLI, Massimiliano , WOLTERING, Thomas , WOSTL, Wolfgang
发明人： ANDREINI, Matteo , GABELLIERI, Emanuele , GUBA, Wolfgang , MARCONI, Guido , NARQUIZIAN, Robert , POWER, Eoin , TRAVAGLI, Massimiliano , WOLTERING, Thomas , WOSTL, Wolfgang
IPC分类号： C07D263/28 , C07D413/10 , A61K31/422 , A61P25/28
CPC分类号： C07D263/28 , C07D413/10
摘要： The present invention relates to a compounds of formula I or a pharmaceutically active acid addition salts thereof. It has been found that the present compounds have Asp2 (β-sccretasc, BACE 1 or Mcmapsin-2) inhibitory activity and that the compounds may therefore be used in the treatment of diseases characterised by elevated β-amyloid levels or β-amyloid deposits, particularly Alzheimer's disease.
摘要翻译：本发明涉及式I化合物或其药学活性的酸加成盐。已经发现本发明化合物具有Asp2（β-sccretasc，BACE1或Mcmapsin-2）的抑制活性，因此该化合物可用于治疗以β淀粉样蛋白升高或β-淀粉样蛋白沉积为特征的疾病，特别是阿尔茨海默病。

5. 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。

6. 发明申请

WO2007110335A1 MALONAMIDE DERIVATIVES AS GAMMA SECRETASE INHIBITORS 审中-公开
标题翻译：作为GAMMA秘密酶抑制剂的马来酰胺衍生物
公开(公告)号：WO2007110335A1
公开(公告)日：2007-10-04
申请号：PCT/EP2007/052557
申请日：2007-03-19
申请人： F. HOFFMANN-LA ROCHE AG , FLOHR, Alexander , JAKOB-ROETNE, Roland , WOSTL, Wolfgang
发明人： FLOHR, Alexander , JAKOB-ROETNE, Roland , WOSTL, Wolfgang
IPC分类号： C07D223/18 , A61K31/55 , A61P25/28
CPC分类号： C07D223/18
摘要： The invention relates to malonamide derivatives of Formula (I) wherein A 1 is -CHR- or -C(O)-; A 2 is -C(O)- and R 2 /R 3 are independently from each other hydrogen, lower alkyl, halogen, hydroxy or lower alkoxy; or A 2 is -O-C(O)- and R 2 /R 3 are independently from each other hydrogen or lower alkyl; R is hydrogen or lower alkyl substituted by halogen; R 1 is hydrogen, lower alkyl or -(CH 2 ) n -aryl, optionally substituted by halogen; R 4 is lower alkyl substituted by halogen n is 0, 1 or 2; and to pharmaceutically suitable acid addition salts, optically pure enantiomers, racemates or diastereomeric mixtures thereof for the treatment of Alzheimer's disease.
摘要翻译：本发明涉及式（I）的丙二酰胺衍生物，其中A 1 -Z 1是-CHR-或-C（O） - ; A 2是-C（O） - 且R 2和R 3彼此独立地是氢，低级烷基，卤素，羟基或低级烷氧基或者A 2 -O-C（O） - 和R 2〜R 3彼此独立地为氢或低级烷基; R是氢或被卤素取代的低级烷基; R 1是氢，低级烷基或任选被卤素取代的 - （CH 2 CH 2）n - 芳基; R 4是被卤素取代的低级烷基，n是0,1或2; 以及用于治疗阿尔茨海默氏病的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。

7. 发明申请

WO2007020190A1 FLUORO SUBSTITUTED 2-OXO AZEPAN DERIVATIVES 审中-公开
标题翻译：氟替代2-OXO AZEPAN衍生物
公开(公告)号：WO2007020190A1
公开(公告)日：2007-02-22
申请号：PCT/EP2006/064935
申请日：2006-08-02
申请人： F. HOFFMANN-LA ROCHE AG , FLOHR, Alexander , GALLEY, Guido , JAKOB-ROETNE, Roland , KITAS, Eric Argirios , WOSTL, Wolfgang
发明人： FLOHR, Alexander , GALLEY, Guido , JAKOB-ROETNE, Roland , KITAS, Eric Argirios , WOSTL, Wolfgang
IPC分类号： C07D223/12 , C07D413/12 , C07D401/12 , C07D403/12 , C07D409/14 , A61K31/55 , A61P25/28 , A61P35/00
CPC分类号： C07D409/14 , C07D223/12 , C07D401/12 , C07D403/12 , C07D413/12
摘要： The invention relates to compounds of general formula (I), wherein R 1 is lower alkyl substituted by halogen, or is aryl or heteroaryl, unsubstituted or substituted by halogen; R 2 is heterocycloalkyl, aryl or heteroaryl, which are unsubstituted or substituted by one or more substituents, selected from the group consisting of halogen, lower alkyloxy, lower alkyl substituted by halogen, O-lower alkyl substituted by halogen or are substituted by C(O)-NR" 2 , (CR 2 )m-C(O)-R’ heteroaryl or S(O) 2 -lower alkyl; R 3 /R 3’ , R 4 /R 4’ and R 5 /R5’ are independently from each other hydrogen or fluoro, wherein at least one of R4/R4’ or R 5 /R 5’ is always fluoro; R' is aryl or hydroxy; R" is hydrogen, cycloalkyl or is heterocycloalkyl; R is hydrogen or lower alkyl; m is 0, 1, 2 or 3; and to pharmaceutically suitable acid addition salts, optically pure enantiomers, racemates or diastereomeric mixtures thereof. It has been found that the compounds of general formula (I) are γ-secretase inhibitors and the related compounds may be useful in the treatment of Alzheimer's disease or common cancers including but not limited to cervical carcinomas and breast carcinomas and malignancies of the hematopoietic system.
摘要翻译：本发明涉及通式（I）的化合物，其中R 1为被卤素取代的低级烷基，或未取代或被卤素取代的芳基或杂芳基; R 2是未取代的或被一个或多个选自以下的取代基取代的杂环烷基，芳基或杂芳基：卤素，低级烷氧基，被卤素取代的低级烷基，被卤素或被C（O）-NR“2取代，（CR 2）m C（O）-R'杂芳基或S（O） /低级烷基; R 3，R 3，R 3，R 4，R 4，R 4， R 5 / R 5'或R 5'或R 5'中的至少一个独立地为氢或氟，其中R 4 / R 4'或R 5' 总是氟; R'是芳基或羟基; R“是氢，环烷基或杂环烷基; R是氢或低级烷基; m为0,1,2或3; 以及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。已经发现通式（I）的化合物是γ-分泌酶抑制剂，相关化合物可用于治疗阿尔茨海默病或常见癌症，包括但不限于宫颈癌和乳腺癌以及造血系统的恶性肿瘤。

8. 发明申请

WO2012163790A1 SPIRO-[1,3]-OXAZINES AND SPIRO-[1,4]-OXAZEPINES AS BACE1 AND/OR BACE2 INHIBITORS 审中-公开
标题翻译：作为BACE1和/或BACE2抑制剂的SPIRO- [1,3] - 亚氨基和螺环 - [1,4] - 氧杂环丙烷
公开(公告)号：WO2012163790A1
公开(公告)日：2012-12-06
申请号：PCT/EP2012/059688
申请日：2012-05-24
申请人： F. HOFFMANN-LA ROCHE AG , NARQUIZIAN, Robert , PINARD, Emmanuel , WOSTL, Wolfgang
发明人： NARQUIZIAN, Robert , PINARD, Emmanuel , WOSTL, Wolfgang
IPC分类号： C07D498/10 , A61K31/537 , A61P25/28
CPC分类号： C07D498/10
摘要： The present invention provides spiro-[l,3]-oxazines and spiro-[l,4]-oxazepines of formula (I) having BACE1 and/or BACE2 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease and type 2 diabetes.
摘要翻译：本发明提供了具有BACE1和/或BACE2抑制活性的式（I）的螺 - [1,3] - 恶唑并螺环[1,4] - 氧氮杂，其制备方法，含有它们的药物组合物及其作为治疗活性的用途物质。本发明的活性化合物可用于例如治疗和/或预防性治疗。阿尔茨海默病和2型糖尿病。

9. 发明申请

WO2012156284A1 1,3-OXAZINES AS BACE1 AND/OR BACE2 INHIBITORS 审中-公开
标题翻译：作为BACE1和/或BACE2抑制剂的1,3-氧化物
公开(公告)号：WO2012156284A1
公开(公告)日：2012-11-22
申请号：PCT/EP2012/058707
申请日：2012-05-11
申请人： F. HOFFMANN-LA ROCHE AG , SIENA BIOTECH S.P.A , HILPERT, Hans , NARQUIZIAN, Robert , PINARD, Emmanuel , POLARA, Alessandra , ROGERS-EVANS, Mark , WOLTERING, Thomas , WOSTL, Wolfgang
发明人： HILPERT, Hans , NARQUIZIAN, Robert , PINARD, Emmanuel , POLARA, Alessandra , ROGERS-EVANS, Mark , WOLTERING, Thomas , WOSTL, Wolfgang
IPC分类号： C07D265/08 , C07D413/10 , C07D413/12 , A61K31/5355 , A61K31/535 , A61P25/28
CPC分类号： C07D413/10 , C07D265/08 , C07D413/12
摘要： The present invention provides compounds of formula I having BACE1 and/or BACE2 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease and type 2 diabetes.
摘要翻译：本发明提供具有BACE1和/或BACE2抑制活性的式I化合物，其制备方法，含有它们的药物组合物及其作为治疗活性物质的用途。本发明的活性化合物可用于例如治疗和/或预防性治疗。阿尔茨海默病和2型糖尿病。

10. 发明申请

WO2012126791A1 1,4-OXAZEPINES AS BACE1 AND/OR BACE2 INHIBITORS 审中-公开
标题翻译： 1,4-OXAZEPINES作为BACE1和/或BACE2抑制剂
公开(公告)号：WO2012126791A1
公开(公告)日：2012-09-27
申请号：PCT/EP2012/054510
申请日：2012-03-15
申请人： F. HOFFMANN-LA ROCHE AG , SIENA BIOTECH S.P.A , GABELLIERI, Emanuele , GUBA, Wolfgang , HILPERT, Hans , MAUSER, Harald , MAYWEG, Alexander V. , ROGERS-EVANS, Mark , ROMBACH, Didier , THOMAS, Andrew , WOLTERING, Thomas , WOSTL, Wolfgang
发明人： GABELLIERI, Emanuele , GUBA, Wolfgang , HILPERT, Hans , MAUSER, Harald , MAYWEG, Alexander V. , ROGERS-EVANS, Mark , ROMBACH, Didier , THOMAS, Andrew , WOLTERING, Thomas , WOSTL, Wolfgang
IPC分类号： C07D267/10 , C07D413/12 , A61K31/553 , A61P25/28 , A61P3/10
CPC分类号： C07D267/10 , C07D413/12
摘要： The present invention relates to 1,4-Oxazepines of formula I having BACE1 and/or BACE2 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease and type 2 diabetes.
摘要翻译：本发明涉及具有BACE1和/或BACE2抑制活性的式I的1,4-氧氮杂，其制备方法，含有它们的药物组合物及其作为治疗活性物质的用途。本发明的活性化合物可用于例如治疗和/或预防性治疗。阿尔茨海默病和2型糖尿病。

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