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1. 发明申请

WO2007092846A2 2-AMINO-3,4-DIHYDRO-QUINOLINE DERIVATIVES USEFUL AS INHIBITORS OF ß-SECRETASE (BACE) 审中-公开
标题翻译：作为β-分泌酶（BACE）抑制剂的2-氨基-3,4-二氢喹啉衍生物
公开(公告)号：WO2007092846A2
公开(公告)日：2007-08-16
申请号：PCT/US2007061691
申请日：2007-02-06
申请人： JANSSEN PHARMACEUTICA NV , BAXTER ELLEN , REITZ ALLEN B , CREIGHTON CHRISTOPHER JOHN
发明人： BAXTER ELLEN , REITZ ALLEN B , CREIGHTON CHRISTOPHER JOHN
CPC分类号： C07D413/14 , C07D215/38 , C07D403/12 , C07D405/06 , C07D405/14
摘要： The present invention is directed to 2-amino-3,4-dihydro-quinoline derivatives, pharmaceutical compositions containing them and their use in the treatment of Alzheimer's disease (AD) and related disorders. The compounds of the invention are inhibitors of ß-secretase, also known as b-site cleaving enzyme and BACE, BACE1, Asp2 and memapsin2.
摘要翻译：本发明涉及2-氨基-3,4-二氢喹啉衍生物，含有它们的药物组合物及其在治疗阿尔茨海默病（AD）和相关疾病中的用途。本发明的化合物是β-分泌酶的抑制剂，也称为b位切割酶和BACE，BACE1，Asp2和memapsin2。

2. 发明申请

WO2006017836A3 2-AMINO-QUINAZOLINE DERIVATIVES USEFUL AS INHIBITORS OF BETA-SECRETASE (BACE) 审中-公开
标题翻译：用作β-分泌酶（BACE）抑制剂的2-氨基喹唑啉衍生物
公开(公告)号：WO2006017836A3
公开(公告)日：2006-06-29
申请号：PCT/US2005028191
申请日：2005-08-08
申请人： JANSSEN PHARMACEUTICA NV , BAXTER ELLEN , BISCHOFF FRANCOIS PAUL , BOYD ROBERT , BRAEKEN MIRIELLE , COATS STEVEN , HUANG YIFANG , JORDAN ALFONZO , LUO CHI , MERCKEN MARC HUBERT , REYNOLDS CHARLES H , ROSS TINA MORGAN , TOUNGE BRETT A , SCHULZ MARK , DE WINTER HANS LOUIS JOS , PIETERS SERGE MARIA ALOYSIUS , REITZ ALLEN B
发明人： BAXTER ELLEN , BISCHOFF FRANCOIS PAUL , BOYD ROBERT , BRAEKEN MIRIELLE , COATS STEVEN , HUANG YIFANG , JORDAN ALFONZO , LUO CHI , MERCKEN MARC HUBERT , REYNOLDS CHARLES H , ROSS TINA MORGAN , TOUNGE BRETT A , SCHULZ MARK , DE WINTER HANS LOUIS JOS , PIETERS SERGE MARIA ALOYSIUS , REITZ ALLEN B
IPC分类号： C07D239/84 , A61K31/517 , A61P25/28
CPC分类号： C07D239/84 , C07D401/04 , C07D401/06 , C07D403/06 , C07D405/06 , C07D413/06 , C07H15/26
摘要： The present invention is directed to novel 2-amino-3, 4-dihydroquinazoline derivatives, pharmaceutical compositions containing them and their use in the treatment of Alzheimer's disease (AD) and related disorders. The compounds of the invention are inhibitors of P-secretase, also known as n-site cleaving enzyme and BACE.
摘要翻译：本发明涉及新的2-氨基-3,4-二氢喹唑啉衍生物，含有它们的药物组合物及其在治疗阿尔茨海默病（AD）和相关病症中的用途。本发明的化合物是P-分泌酶的抑制剂，也称为n-位切割酶和BACE。

3. 发明申请

WO2007092839A3 MACROCYCLE DERIVATIVES USEFUL AS INHIBITORS OF BETA-SECRETASE (BACE) 审中-公开
标题翻译：用作β-分泌酶抑制剂（BACE）的大分子衍生物
公开(公告)号：WO2007092839A3
公开(公告)日：2007-10-04
申请号：PCT/US2007061677
申请日：2007-02-06
申请人： JANSSEN PHARMACEUTICA NV , BAXTER ELLEN , REITZ ALLEN B , PARKER MICHAEL H , HUANG YIFANG , HO CHIH Y , STROBEL ERIC D , REYNOLDS CHARLES H
发明人： BAXTER ELLEN , REITZ ALLEN B , PARKER MICHAEL H , HUANG YIFANG , HO CHIH Y , STROBEL ERIC D , REYNOLDS CHARLES H
IPC分类号： C07D487/08 , A61K31/4748 , A61K31/529 , A61P25/28 , C07D498/08 , C07D498/18
CPC分类号： C07D498/08 , C07D487/08
摘要： The present invention is directed to macrocycle derivatives, pharmaceutical compositions containing them and their use in the treatment of Alzheimer's disease (AD) and related disorders. The compounds of the invention are inhibitors ofß-secretase, also known as ß-site cleaving enzyme and BACE, BACE1, Asp2 and memapsin2.
摘要翻译：本发明涉及大环衍生物，含有它们的药物组合物及其在治疗阿尔茨海默病（AD）和相关疾病中的用途。本发明的化合物是β-分泌酶的抑制剂，也称为β位点切割酶和BACE，BACE1，Asp2和memapsin2。

4. 发明申请

WO2007092854A2 2-AMINO-QUINOLINE DERIVATIVES USEFUL AS INHIBITORS OF ß-SECRETASE (BACE) 审中-公开
标题翻译： 2-氨基喹啉衍生物作为β-分泌酶（BACE）的抑制剂有用
公开(公告)号：WO2007092854A2
公开(公告)日：2007-08-16
申请号：PCT/US2007061704
申请日：2007-02-06
申请人： JANSSEN PHARMACEUTICA NV , BAXTER ELLEN , REITZ ALLEN B , HUANG YIFANG , CREIGHTON CHRISTOPHER JOHN , MAHAROOF UMAR SAIBU MOHOMED , REYNOLDS CHARLES H , LUO CHI , TOUNGE BRETT A , ROSS TINA MORGAN , LU TIANBAO
发明人： BAXTER ELLEN , REITZ ALLEN B , HUANG YIFANG , CREIGHTON CHRISTOPHER JOHN , MAHAROOF UMAR SAIBU MOHOMED , REYNOLDS CHARLES H , LUO CHI , TOUNGE BRETT A , ROSS TINA MORGAN , LU TIANBAO
CPC分类号： C07D215/38 , C07D401/12 , C07D405/06 , C07D405/14 , C07D413/14
摘要： The present invention is directed to 2-amino-quinoline derivatives, pharmaceutical compositions containing them and their use in the treatment of Alzheimer's disease (AD) and related disorders. The compounds of the invention are inhibitors of b-secretase, also known as b-site cleaving enzyme and BACE, BACE1, Asp2 and memapsin2.
摘要翻译：本发明涉及2-氨基 - 喹啉衍生物，含有它们的药物组合物及其在治疗阿尔茨海默病（AD）和相关疾病中的用途。本发明的化合物是b分泌酶的抑制剂，也称为b位切割酶和BACE，BACE1，Asp2和memapsin2。

5. 发明专利

BRPI0906625A2 Derivados de tio-2-amino-quinolina-6-substituída úteis como inibidores da beta-secretase (bace) 未知
公开(公告)号：BRPI0906625A2
公开(公告)日：2015-07-14
申请号：BRPI0906625
申请日：2009-01-27
申请人： JANSSEN PHARMACEUTICA NV
发明人： BAXTER ELLEN , CREIGHTON CHRISTOPHER J , LU TIANBAO , REITZ ALLEN B , REYNOLDS CHARLES H , ROSS TINA MORGAN , SIEBER-MCMASTER ELLEN
IPC分类号： C07D215/38 , A61K31/4709 , A61P25/28

6. 发明专利

ES2403185T3 Nuevos derivados de 2-amino-quinazolina útiles como inhibidores de ss-secretasa (BACE) 未知
公开(公告)号：ES2403185T3
公开(公告)日：2013-05-16
申请号：ES05786778
申请日：2005-08-08
申请人： JANSSEN PHARMACEUTICA NV , BAXTER ELLEN , BOYD ROBERT , COATS STEVE , JORDAN ALFONZO , REITZ ALLEN , REYNOLDS CHARLES H , SCOTT MALCOM , SCHULZ MARK , WINTER HANS LOUIS JOS DE
发明人： BAXTER ELLEN , BOYD ROBERT , COATS STEVE , JORDAN ALFONZO , REITZ ALLEN , REYNOLDS CHARLES H , SCOTT MALCOLM , SCHULZ MARK
IPC分类号： C07D239/84 , A61K31/517
摘要： Un compuesto de fórmula (II) **Fórmula** en donde R0 se selecciona del grupo que comprende hidrógeno, metilo y CF3; R1 se selecciona del grupo que comprende hidrógeno, hidroxi, metilo, etilo, trifluorometilo, 2,2,2-trifluoroetilo, metoxi, etoxi y metilcarbonilo; c es un número entero de 0 a 1; A2 se selecciona del grupo que comprende C1-4alqui!o; en donde el C1-4alquilo, opcionalmente, essustituido con uno o más sustituyentes RY; en donde cada RY se selecciona, por separado, del grupo que comprende hidroxi, oxo, C1-4alquilo,C1-4alcoxi, C1-4alquilo sustituido con hidroxi, C1-6alquilo sustituido con amino, cicloalquilo, cicloalquil-C1-4alquil-,bifenilo, arilo, C1-4aralquilo, heteroarilo, heteroaril-C1-4alquil-, heterocicloalquilo, heterocicloalquil-C1-4alquil- yespiro-heterociclilo.

7. 发明专利

CA2714008A1 2-AMINO-QUINOLINE DERIVATIVES USEFUL AS INHIBITORS OF .BETA.-SECRETASE (BACE) 未知
公开(公告)号：CA2714008A1
公开(公告)日：2009-08-06
申请号：CA2714008
申请日：2009-01-29
申请人： JANSSEN PHARMACEUTICA NV
发明人： BAXTER ELLEN , CREIGHTON CHRISTOPHER J , YUNG HO CHIN , YUANG HIFANG , LU TIANBAO , REITZ ALLEN B , REYNOLDS CHARLES H , MORGAN ROSS TINA , SEIBER-MCMASTER ELLEN , LUO CHI
IPC分类号： C07D407/06 , A61K31/4709 , A61P25/28 , C07D407/14 , C07D409/14
摘要： The present invention is directed to novel 2-amino-quinoline derivatives, pharmaceutical compositions containing them and their use in the treatment of Alzheimer's disease (AD), mild cognitive impairment, senility and / or dementia. The compounds of the present invention are inhibitors of ß-secretase, also known as ß-site amyloid cleaving enzyme, BACE, BACE1, Asp2, or memapsin2.

8. 发明专利

ES2397682T3 Derivados de 2-amino-quinolina útiles como inhibidores de la beta-secretasa (BACE) 未知
公开(公告)号：ES2397682T3
公开(公告)日：2013-03-08
申请号：ES09705822
申请日：2009-01-29
申请人： JANSSEN PHARMACEUTICA NV
发明人： BAXTER ELLEN , LU TIANBAO , CREIGHTON CHRISTOPHER J , REITZ ALLEN , REYNOLDS CHARLES , LUO CHI , SIEBER-MCMASTER ELLEN , MORGAN ROSS TINA , HUANG YIFANG , YUNG HO CHIH
IPC分类号： C07D407/06 , A61K31/4709 , A61P25/28 , C07D407/14 , C07D409/14
摘要： Un compuesto de fórmula (I) en la que a es un número entero de 0 a 4; R1 está seleccionado del grupo que consiste en halógeno, alquilo C1-4, alcoxi C1-4, alquilo C1-4 halogenado y alcoxiC1-4 halogenado; - está seleccionado del grupo que consiste en arilo y heteroarilo; R2 está seleccionado del grupo que consiste en hidrógeno y alcoxi C1-4; R3 está seleccionado del grupo que consiste en hidrógeno, alquilo C1-8, alquilo C2-8 sustituido con hidroxi, alquilo C2-8sustituido con NRARB, -alquilo C1-4-O-alquilo C1-4, cicloalquilo, -(alquilo C1-4)-cicloalquilo, heterocicloalquilo y -(alquiloC1-4)-heterocicloalquilo; en la que RA y RB están seleccionados cada uno independientemente del grupo que consisteen hidrógeno y alquilo C1-4; A1 está seleccionado del grupo que consiste en -(CH2)b-; en la que b es un número entero de 2 a 4; L1 está seleccionado del grupo que consiste en -NRC- y -C(O)-NRC-; en la que RC está seleccionado del grupo queconsiste en hidrógeno, alquilo C1-8, alquilo C1-4 sustituido con hidroxi, -alquilo C1-4-O-alquilo C1-4 y cicloalquilo C5-7;R4 está seleccionado del grupo que consiste en alquilo C1-8, alquenilo C2-12, alquilo C1-4-O-alquilo C1-4, -alquilo C1-4-NRDRE, -alquilo C1-4-OH, cicloalquilo, -alquilo C1-4-cicloalquilo, carbociclilo parcialmente insaturado, -alquilo C1-4-(carbociclilo parcialmente insaturado), arilo, aralquilo, heteroarilo, -alquilo C1-4-heteroarilo, heterocicloalquilo y -alquilo C1-4-heterocicloalquilo; en la que RD y RE están seleccionados cada uno independientemente del grupo que consiste en hidrógeno y alquiloC1-4; y en la que el cicloalquilo, carbociclilo parcialmente insaturado, arilo, heteroarilo o heterocicloalquilo, se use solo ocomo parte de un grupo sustituyente, está opcionalmente sustituido con uno o más sustituyentes seleccionadosindependientemente del grupo que consiste en fluoro, alquilo C1-4, -alquilo C1-4-O-alquilo C1-4, carboxi, -C(O)O-alquiloC1-4 y aralquilo; alternativamente, L1 es -NRC- y RC y R4 se toman junto con el átomo de nitrógeno al que están unidos para formaruna estructura de anillo seleccionada del grupo que consiste en 1-pirazolilo, 1-imidazolilo y 1-(1,2,3-triazolilo); en laque el 1-pirazolilo, 1-imidazolilo o 1-(1,2,3-triazolilo) está opcionalmente sustituido con un sustituyente seleccionadodel grupo que consiste en alquilo C1-6; o una sal farmacéuticamente aceptable del mismo.

9. 发明专利

NZ586830A 2-AMINO-QUINOLINE DERIVATIVES USEFUL AS INHIBITORS OF BETA-SECRETASE (BACE) 未知
公开(公告)号：NZ586830A
公开(公告)日：2012-02-24
申请号：NZ58683009
申请日：2009-01-29
申请人： JANSSEN PHARMACEUTICA NV
发明人： BAXTER ELLEN , CREIGHTON CHRISTOPHER J , LU TIANBAO , REITZ ALLEN B , REYNOLDS CHARLES H , MORGAN ROSS TINA , SIEBER-MCMASTER ELLEN , YUNG HO CHIH , HUANG YIFANG , LUO CHI
IPC分类号： C07D407/06 , A61K31/4709 , A61P25/28 , C07D409/14
摘要： Disclosed is a compound of formula (I) wherein a is an integer from 0 to 4; R1 is selected from the group consisting of halogen, C1-4alkyl, C1-4alkoxy, halogenated C1-4alkyl and halogenated C1-4alkoxy; A is selected from the group consisting of aryl and heteroaryl; R2 is selected from the group consisting of hydrogen and C1-4alkoxy; R3 is selected from the group consisting of hydrogen, C1-8alkyl, hydroxyl substituted C2-8alkyl, NRARB substituted C2-8alkyl, -C1-4alkyl-O-C1-4alkyl, cycloalkyl, -(C1-4alkyl)-cycloalkyl, heterocycloalkyl and -(C1-4alkyl)heterocycloalkyl; wherein RA and RB are each independently selected from the group consisting of hydrogen and C1-4alkyl; A1 is selected from the group consisting of -(CH2)b-; wherein b is an integer from 2 to 4; L1 is selected from the group consisting of-NRc- and -C(O)-NRc-; wherein RC is selected from the group consisting of hydrogen, C1-8alkyl, hydroxy substituted C1-4alkyl, -C1-4alkyl-O-C1-4alkyl and C5-7cycloalkyl; R4 is selected from the group consisting of C1-8alkyl, C2-12alkenyl, -C1-4alkyl-O-C1-4alkyl, -C1-4alkyl-NRDRE, -C1-4alkyl-OH, cycloalkyl, -C1-4alkylcycloalkyl, partially unsaturated carbocyclyl, -C1-4alkyl-(partially unsaturated carbocyclyl), aryl, aralkyl, heteroaryl, -C1-4alkyl-heteroaryl, heterocycloalkyl and -C1-4alkyl-heterocycloalkyl; wherein RD and RE are each independently selected from the group consisting of hydrogen and C1-4alkyl; and wherein the cycloalkyl, partially unsaturated carbocyclyl, aryl, heteroaryl or heterocycloalkyl, whether alone or as part of a substituent group, is optionally substituted with one or more substituents independently selected from the group consisting of fluoro, C1-4alkyl, -C1-4alkyl-O-C1-4alkyl, carboxy, -C(O)O-C1-4alkyl and aralkyl; alternatively, L1 is -NRc- and RC and R4 are taken together with the nitrogen atom to which they are attached to form a ring structure selected from the group consisting of 1-pyrazolyl, 1-imidazolyl and 1-(1 ,2,3-triazolyl); wherein the 1-pyrazolyl, 1-imidazolyl or 1-(1,2,3-triazolyl) is optionally substituted with a substituent selected from the group consisting of C1-6alkyl; or a pharmaceutically acceptable salt thereof.

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