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1. 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。

2. 发明申请

WO2011092272A1 GAMMA SECRETASE MODULATERS 审中-公开
标题翻译： GAMMA秘密调制解调器
公开(公告)号：WO2011092272A1
公开(公告)日：2011-08-04
申请号：PCT/EP2011/051184
申请日：2011-01-28
申请人： F. HOFFMANN-LA ROCHE AG , BAUMANN, Karlheinz , GOETSCHI, Erwin , GREEN, Luke , JOLIDON, Synese , KNUST, Henner , LIMBERG, Anja , LUEBBERS, Thomas , THOMAS, Andrew
发明人： BAUMANN, Karlheinz , GOETSCHI, Erwin , GREEN, Luke , JOLIDON, Synese , KNUST, Henner , LIMBERG, Anja , LUEBBERS, Thomas , THOMAS, Andrew
IPC分类号： C07D471/04 , C07D487/04 , C07D498/04 , A61K31/4196 , A61P25/00
CPC分类号： C07D471/04 , C07D487/04 , C07D498/04
摘要： The invention relates to compounds of formula ( I ) wherein R 1 /R 1' are independently from each other hydrogen, halogen, lower alkoxy or cyano; R 2 is lower alkyl, halogen, lower alkoxy, lower alkyl substituted by halogen, lower alkoxy substituted by halogen, lower alkyl substituted by OR, =0, -C(O)O-lower alkyl, -C(O)NH-lower alkyl, cyano, CH 2 -O-lower alkyl, cycloalkyl, NRR'or is -O-(CH 2 ) o -phenyl optionally substituted by halogen, or is -(CH 2 ) o -phenyl optionally substituted by one, two or three substituents, selected from halogen, -(CH 2 ) o -cyano, lower alkyl, lower alkyl substituted by halogen, lower alkyl substituted by hydroxy, C(O)H, -CH 2 -NH 2 -, -CH 2 -NH-C(O)O-lower alkyl, -CH 2 -NH-C(O)-lower alkyl, -CH 2 -NH-lower alkyl, -CH 2 -NH-S(O) 2 -lower alkyl, lower alkoxy or by lower alkoxy substituted by halogen, or is -(CH 2 ) o -cycloalkyl, or is -(CH 2 ) o -heterocycloalkyl which is optionally substituted by halogen, CF 3 , lower alkyl, -CH 2 CN, -C(O)-lower alkyl, -C(O)O-lower alkyl or S(O) 2 -lower alkyl, or is heteroaryl selected from the group consisting of furanyl, pyrazinyl, pyridinyl, benzooxazolyl or benzoimidazolyl which are optionally substituted by lower alkyl, or is 4-methyl-3,4-dihydro-2H-benzo[l,4]oxazine R and R' are independently from each other hydrogen or lower alkyl, and o is 0 or 1; R 3 may occur once or twice and is lower alkyl; A is Formula a), b), c), d), e), f), h), i), j) and Formula k); R 2' is hydrogen, lower alkyl, lower alkyl substituted by halogen, C(O)-lower alkyl, S(O) 2 -lower alkyl or phenyl optionally substituted by halogen; hetaryl is a 5 or 6 membered N, S or O-containing heteroaryl group; n is O, 1, 2 or 3; if n is 2 or 3, R 2 may be the same or not; or to pharmaceutically active acid addition salts thereof. The present 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：本发明涉及其中R 1 / R 1'彼此独立地为氢，卤素，低级烷氧基或氰基的式（I）化合物; R2是低级烷基，卤素，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，被OR取代的低级烷基，= 0，-C（O）O-低级烷基，-C（O），氰基，CH 2 -O-低级烷基，环烷基，NRR'或是任选被卤素取代的-O-（CH 2）o - 苯基，或是被选定的被一个，两个或三个取代基任选取代的 - （CH 2）卤代低级烷基，被卤素取代的低级烷基，被羟基取代的低级烷基，C（O）H，-CH 2 -NH 2 - ， - CH 2 -NH-C（O）O-低级烷基，-CH 2 -NH-C（O） - 低级烷基，-CH 2 -NH-低级烷基，-CH 2 -NH-S（O）2 - 低级烷基，低级烷氧基或被卤素取代的低级烷氧基，（CH 2）o - 环烷基，或者是 - （CH 2）o - 杂环烷基，其任选被卤素，CF 3，低级烷基，-CH 2 CN，-C（O） - 低级烷基，-C（O）O-低级烷基或 S（O）2-低级烷基，或者是选自呋喃基，吡嗪基，吡啶基，苯并恶唑基或苯并咪唑基的杂芳基。或是4-甲基-3,4-二氢-2H-苯并[1,4]恶嗪R和R'彼此独立地为氢或低级烷基，o为0或1; R3可以发生一次或两次，并且是低级烷基; A是公式a），b），c），d），e），f），h），i），j）和公式k）; R 2'是氢，低级烷基，被卤素取代的低级烷基，C（O） - 低级烷基，任选被卤素取代的S（O）2 - 低级烷基或苯基）杂芳基是5或6元N，S或O的杂芳基; n是0,1,2或3; 如果n为2或3，则R2可以相同或不相同; 或其药物活性的酸加成盐。本发明的式（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，例如脑淀粉样血管病，遗传性脑出血伴淀粉样变性，荷兰型（HCHWA-D），多发梗死性痴呆，痴呆和唐氏综合征。

3. 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。

4. 发明申请

WO2012116965A1 BRIDGED PIPERIDINE DERIVATIVES 审中-公开
标题翻译：桥连哌啶衍生物
公开(公告)号：WO2012116965A1
公开(公告)日：2012-09-07
申请号：PCT/EP2012/053301
申请日：2012-02-28
申请人： F. HOFFMANN-LA ROCHE AG , BAUMANN, Karlheinz , GREEN, Luke , LIMBERG, Anja , LUEBBERS, Thomas , THOMAS, Andrew
发明人： BAUMANN, Karlheinz , GREEN, Luke , LIMBERG, Anja , LUEBBERS, Thomas , THOMAS, Andrew
IPC分类号： C07D471/04 , C07D519/00 , A61K31/4196 , A61P25/00
CPC分类号： C07D451/04
摘要： The present invention relates to compounds of formula (l); hetaryl I is a five or six membered heteroaryl group, containing 1 to 3 heteroatoms, selected from S or N; hetaryl II is a six membered heteroaryl group, containing 1 to 3 heteroatoms, selected from S or N, or is a two membered ring system containing 1 to 4 heteroatoms selected from S, 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 lower alkyl, lower alkyl substituted by halogen, halogen, lower alkoxy, cycloalkyl substituted by lower alkyl or lower alkyl substituted by halogen, or is lower alkyl substituted by hydroxy, or is furyl, or is O-benzyl, (CH2)p-phenyl, optionally substituted by halogen, lower alkoxy, lower alkyl substituted by halogen, lower alkyl or by cyano; R 3 is hydrogen or lower alkyl; Y is (CH 2 )n-, -CH 2 OCH 2 -, -CH 2 O-, CH 2 S-, -CH 2 SCH 2 - and is bonded to two of the ring carbon atoms, bonding being to either the ring carbon atoms a and b or the ring carbon atoms c and d; p is 0 or 1; m is 0, 1 or 2; if m is 2 then R 1 may be the same or different; -75- n is 2 or 3; o is 0, 1 or 2, if o is 2, then R 2 may be the same or different; or to pharmaceutically active acid addition salts thereof. The present 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 Alzheimers 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; 杂芳基I是含有1至3个选自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S或N的杂原子或是含有1至4个选自S或N的杂原子的二元环体系的六元杂芳基，其中至少一个环在本质上是芳族的; R1是低级烷基，低级烷氧基，被卤素或卤素取代的低级烷基; R2是低级烷基，被卤素取代的低级烷基，卤素，低级烷氧基，被低级烷基取代的环烷基或被卤素取代的低级烷基，或被羟基取代的低级烷基，或是呋喃基，或是O-苄基，（CH2）p 苯基，任选被卤素，低级烷氧基，被卤素，低级烷基或氰基取代的低级烷基取代; R3是氢或低级烷基; Y是（CH 2）n - ， - CH 2 OCH 2 - ， - CH 2 O - ，CH 2 S - ， - CH 2 SCH 2 - 并键合到两个环碳原子上，键合为环碳原子a和b或环碳原子c 和d p为0或1; m为0,1或2; 如果m为2，则R1可以相同或不同; -75- n为2或3; o为0,1或2，如果o为2，则R2可以相同或不同; 或其药物活性的酸加成盐。本发明式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和其它疾病如脑淀粉样蛋白血管病，遗传性脑出血伴淀粉样变性，荷兰型（HCHWA-D），多发性梗死性痴呆，痴呆和唐氏综合征。

5. 发明申请

WO2009087127A1 MODULATORS FOR AMYLOID BETA 审中-公开
标题翻译： AMYLOID BETA的调节剂
公开(公告)号：WO2009087127A1
公开(公告)日：2009-07-16
申请号：PCT/EP2009/050036
申请日：2009-01-05
申请人： F. HOFFMANN-LA ROCHE AG , BAUMANN, Karlheinz , FLOHR, Alexander , GOETSCHI, Erwin , JACOBSEN, Helmut , JOLIDON, Synese , LUEBBERS, Thomas
发明人： BAUMANN, Karlheinz , FLOHR, Alexander , GOETSCHI, Erwin , JACOBSEN, Helmut , JOLIDON, Synese , LUEBBERS, Thomas
IPC分类号： C07D277/60 , C07D401/14 , C07D403/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07D491/052 , C07D513/04 , C07D491/113 , A61P25/28 , A61K31/428 , A61K31/517 , A61K31/519 , A61K31/527
CPC分类号： C07D417/12 , C07D277/82 , C07D401/14 , C07D403/12 , C07D413/14 , C07D417/14 , C07D471/04 , C07D491/052 , C07D491/113 , C07D513/04 , C07F7/1856
摘要： The invention relates to compounds of formula (I) R 1 is -C(O)O-lower alkyl, cyano or is hetaryl; hetaryl is a five-or six membered heteraryl group, optionally substituted by R'; R' is halogen, lower alkyl, lower alkyl substituted by halogen, lower alkoxy or lower alkoxy substituted by halogen; R 2 is hydrogen, lower alkoxy, lower alkyl, halogen or cyano; R 3 is -(CH 2 ) n -C(O)O-lower alkyl, lower alkyl, lower alkoxy, hydroxy, -O-Si(CH 3 ) 2 -lower alkyl, -C(O)-N(lower alkyl) 2 , -O-S(O) 2 -lower alkyl, C 3-7 -cycloalkyl, S(O) 2 -aryl, heterocyclyl, -C(O)-heterocyclyl, or is aryl or hetaryl, which aryl or hetaryl rings are optionally substituted by one or more R'; R 4 is hydrogen, lower alkyl, hydroxy or CH 2 CN; X is S or -N=C(R 5 )-; R 5 is hydrogen, lower alkyl or hydroxy, is a bond, -O-, -CH 2 -, -CH 2 -CH 2 -, formula (II) or or -N(R)-; R is hydrogen, lower alkyl, C(O)O-lower alkyl, C(O)-lower alkyl, S(O) 2 -lower alkyl, or benzyl; n is 0 or 1 or to pharmaceutically active acid addition salts. 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为-C（O）O-低级烷基，氰基或杂芳基; 杂芳基是任选被R'取代的五元或六元杂芳基; R'是卤素，低级烷基，被卤素取代的低级烷基，低级烷氧基或被卤素取代的低级烷氧基; R2是氢，低级烷氧基，低级烷基，卤素或氰基; R3是 - （CH2）nC（O）O-低级烷基，低级烷基，低级烷氧基，羟基，-O-Si（CH3）2-低级烷基，-C（O）-N（低级烷基）（O）2-低级烷基，C 3-7 - 环烷基，S（O）2-芳基，杂环基，-C（O） - 杂环基，或芳基或杂芳基，该芳基或杂芳基环任选被一个或多个 R'; R4是氢，低级烷基，羟基或CH2CN; X是S或-N = C（R5） - ; R 5是氢，低级烷基或羟基，是键，-O-，-CH 2 - ， - CH 2 -CH 2 - ，式（II）或-N（R） - ; R是氢，低级烷基，C（O）O-低级烷基，C（O） - 低级烷基，S（O）2 - 低级烷基或苄基; n为0或1或与药学活性的酸加成盐。这些化合物可用于治疗阿尔茨海默病，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，痴呆症或唐氏综合症。

6. 发明申请

WO2009103652A1 MODULATORS FOR AMYLOID BETA 审中-公开
标题翻译： AMYLOID BETA的调节剂
公开(公告)号：WO2009103652A1
公开(公告)日：2009-08-27
申请号：PCT/EP2009/051613
申请日：2009-02-12
申请人： F. HOFFMANN-LA ROCHE AG , BAUMANN, Karlheinz , FLOHR, Alexander , GOETSCHI, Erwin , JACOBSEN, Helmut , JOLIDON, Synese , LUEBBERS, Thomas
发明人： BAUMANN, Karlheinz , FLOHR, Alexander , GOETSCHI, Erwin , JACOBSEN, Helmut , JOLIDON, Synese , LUEBBERS, Thomas
IPC分类号： C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , A61P25/28 , A61K31/4439 , A61K31/506 , A61K31/4196
CPC分类号： C07D403/12 , C07D401/12 , C07D401/14 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14
摘要： The invention relates to compounds of formula (I) wherein the substituents are as described in claim 1. It has been found that the present 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）化合物，其中取代基如权利要求1所述。已经发现，本发明式（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，遗传性脑出血伴淀粉样变性，荷兰型（HCHWA-D），多发性梗塞性痴呆，痴呆 pugilistica和唐氏综合症。

7. 发明申请

WO2008138753A1 HETARYLANILINES AS MODULATORS FOR AMYLOID BETA 审中-公开
标题翻译：作为AMYLOID BETA的调节剂的海参
公开(公告)号：WO2008138753A1
公开(公告)日：2008-11-20
申请号：PCT/EP2008/055290
申请日：2008-04-30
申请人： F. HOFFMANN-LA ROCHE AG , BAUMANN, Karlheinz , FLOHR, Alexander , JACOBSEN, Helmut , JOLIDON, Synese , LUEBBERS, Thomas
发明人： BAUMANN, Karlheinz , FLOHR, Alexander , JACOBSEN, Helmut , JOLIDON, Synese , LUEBBERS, Thomas
IPC分类号： C07D417/12 , C07D513/04 , A61K31/427 , A61K31/428 , A61K31/429 , A61P25/28
CPC分类号： C07D513/04 , C07D417/12
摘要： The invention relates to compounds of formula (I) : wherein hetaryl I is formula (II); hetaryl II is formula (III); or to pharmaceutically active acid addition salts. It has been found that the present 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.
摘要翻译：本发明涉及式（I）的化合物：其中杂芳基I是式（II）; 芳基II是式（III）; 或药用活性酸加成盐。已经发现，本发明式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，特别是阿尔茨海默氏病。

8. 发明申请

WO2017042114A1 BRIDGED PIPERIDINE DERIVATIVES 审中-公开
标题翻译：桥连哌啶衍生物
公开(公告)号：WO2017042114A1
公开(公告)日：2017-03-16
申请号：PCT/EP2016/070800
申请日：2016-09-05
申请人： F. HOFFMANN-LA ROCHE AG , HOFFMANN-LA ROCHE INC.
发明人： BAUMANN, Karlheinz , GALLEY, Guido , JAKOB-ROETNE, Roland , LIMBERG, Anja , NEIDHART, Werner , RODRIGUEZ SARMIENTO, Rosa Maria , BARTELS, Bjoern , RATNI, Hasane
IPC分类号： C07D519/00 , A61K31/4375 , A61P25/28
CPC分类号： C07D519/00
摘要： The present invention relates to compounds of formula (I); hetaryl is a five membered heteroaryl group, containing 1 to 3 heteroatoms, selected from O, S or N; R 1 is hydrogen, halogen, lower alkyl, lower alkoxy, lower alkyl substituted by halogen, S-lower alkyl substituted by halogen or lower alkoxy substituted by halogen, or two neighboring carbon atoms may form on phenyl an additional ring containing -O-CH 2 -O-; n is 1 to 5; R 2 is hydrogen or lower alkyl substituted by halogen; R 3 is hydrogen or lower alkyl substituted by halogen; or to pharmaceutically active acid addition salts thereof, to racemic mixtures or to its corresponding enantiomers or optical isomers or stereoisomers 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; 杂芳基是含有1至3个选自O，S或N的杂原子的五元杂芳基; 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S-低级烷基或被卤素取代的低级烷氧基或两个相邻的碳原子，可在苯基上形成另外的含有-O-CH 2 - O-; n为1至5; R2是氢或被卤素取代的低级烷基; R3是氢或被卤素取代的低级烷基; 或其药学活性的酸加成盐，外消旋混合物或其相应的对映异构体或其旋光异构体或立体异构体。这些化合物可用于治疗阿尔茨海默病，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，痴呆症或唐氏综合症。

9. 发明申请

WO2014060386A1 INDOL-AMIDE COMPOUNDS AS BETA-AMYLOID INHBITORS 审中-公开
标题翻译：内酰胺化合物作为β-淀粉样物质
公开(公告)号：WO2014060386A1
公开(公告)日：2014-04-24
申请号：PCT/EP2013/071478
申请日：2013-10-15
申请人： F. HOFFMANN-LA ROCHE AG , HOFFMANN-LA ROCHE INC.
发明人： BAUMANN, Karlheinz , FLOHR, Alexander , JOLIDON, Synese , KNUST, Henner , LUEBBERS, Thomas , NETTEKOVEN, Matthias
IPC分类号： C07D401/14 , C07D405/14 , C07D401/04 , C07D401/06 , C07D403/06 , C07D405/04 , A61K31/404 , A61K31/454 , C07D403/04 , A61K31/497 , A61P25/00
CPC分类号： C07D209/42 , C07D401/04 , C07D401/06 , C07D401/14 , C07D403/04 , C07D403/06 , C07D405/04 , C07D405/14
摘要： The present invention provides compounds of formula (I), wherein Z, R 1 , R 2 , and R 3 are as described herein, as well as pharmaceutically acceptable salts and esters thereof. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions comprising them and their use as medicaments for the treatment of Alzheimer's disease.
摘要翻译：本发明提供式（I）化合物，其中Z，R 1，R 2和R 3如本文所述，以及其药学上可接受的盐和酯。此外，本发明涉及制备式（I）化合物，包含它们的药物组合物及其作为用于治疗阿尔茨海默氏病的药物的用途。

10. 发明申请

WO2023006645A1 HALOACETHYDRAZIDES USEFUL AS AEP INHIBITORS 审中-公开
公开(公告)号：WO2023006645A1
公开(公告)日：2023-02-02
申请号：PCT/EP2022/070752
申请日：2022-07-25
申请人： F. HOFFMANN-LA ROCHE AG , HOFFMANN-LA ROCHE INC.
发明人： BARTELS, Bjoern , BAUMANN, Karlheinz , GRUENINGER, Fiona , HOCHSTRASSER, Remo , KUHN, Bernd , MORANDI, Federica , PINARD, Emmanuel
IPC分类号： C07D207/16 , A61P25/28 , A61K31/40
摘要： The invention relates to novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5, R6, R7, W, m and n are as described herein, composition including the compounds and methods of using the compounds.

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