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1. 发明申请

WO2007014921A1 MACROCYCLIC INHIBITORS OF HEPATITIS C VIRUS 审中-公开
标题翻译：丙型肝炎病毒大肠杆菌抑制剂
公开(公告)号：WO2007014921A1
公开(公告)日：2007-02-08
申请号：PCT/EP2006/064815
申请日：2006-07-28
申请人： TIBOTEC PHARMACEUTICALS LTD. , MEDIVIR AB , RABOISSON, Pierre Jean-Marie Bernard , DE KOCK, Herman Augustinus , DORANGE, Ismet , VENDEVILLE, Sandrine Marie Helene , SURLERAUX, Dominique Louis Nestor Ghislain , TAHRI, Abdellah , SIMONNET, Yvan , VAN DE VREKEN, Wim , HU, Lili , SIMMEN, Kenneth Alan , NILSSON, Karl Magnus , SAMUELSSON, Bengt Bertil , ROSENQUIST, Åsa Annica Kristina , WALLBERG, Hans Kristian
发明人： RABOISSON, Pierre Jean-Marie Bernard , DE KOCK, Herman Augustinus , DORANGE, Ismet , VENDEVILLE, Sandrine Marie Helene , SURLERAUX, Dominique Louis Nestor Ghislain , TAHRI, Abdellah , SIMONNET, Yvan , VAN DE VREKEN, Wim , HU, Lili , SIMMEN, Kenneth Alan , NILSSON, Karl Magnus , SAMUELSSON, Bengt Bertil , ROSENQUIST, Åsa Annica Kristina , WALLBERG, Hans Kristian
IPC分类号： C07D401/14 , C07K5/078 , A61K31/4725 , A61P31/14
CPC分类号： C07D401/14 , C07D401/12 , C07D417/14 , C07D487/04 , C07K5/06191
摘要： Inhibitors of HCV replication of formula (I) and the N -oxides, salts, and stereoisomers thereof, wherein X is N, CH and where X bears a double bond it is C; R 1 is -OR 5 , -NH-SO 2 R 6 ; R 2 is hydrogen, and where X is C or CH, R 2 may also be C 1-6 alkyl; R 3 is hydrogen, C 1-6 alkyl, C 1-6 alkoxyC 1-6 alkyl, or C 3-7 cycloalkyl; R 4 is isoquinolinyl optionally substituted with one, two or three substituents each independently selected from C 1-6 alkyl, C 1-6 alkoxy, hydroxy, halo, polyhalo- C 1-6 alkyl, polyhaloC 1-6 alkoxy, amino, mono- or diC 1-6 alkylamino, mono- or DiC 1-6 alkylaminocarbonyl, C 1-6 alkylcarbonyl-amino, aryl, and Het; n is 3, 4, 5, or 6; each dashed line (represented by ) represents an optional double bond; R 5 is hydrogen; aryl; Het; C 3-7 cycloalkyl optionally substituted with C 1-6 alkyl; or C 1-6 alkyl optionally substituted with C 3-7 cycloalkyl, aryl or with Het; R 6 is aryl; Het; C 3-7 cycloalkyl optionally substituted with C 1-6 alkyl; or C 1-6 alkyl optionally substituted with C 3-7 cycloalkyl, aryl or with Het; each aryl is phenyl optionally substituted with one, two or three substituents; and each Het is a 5 or 6 membered saturated, partially unsaturated or completely unsaturated heterocyclic ring containing 1 to 4 heteroatoms each independently selected from nitrogen, oxygen and sulfur, and being optionally substituted with one, two or three substituents; pharmaceutical compositions containing compounds (I) and processes for preparing compounds (I). Bioavailable combinations of the inhibitors of HCV of formula (I) with ritonavir are also provided.
摘要翻译：式（I）的HCV复制抑制剂及其N-氧化物，盐和立体异构体，其中X为N，CH，X为双键时为C; R 1是-OR 5，-NH-SO 2 R 6; R 2是氢，并且其中X是C或CH，R 2也可以是C 1-6烷基; R 3是氢，C 1-6烷基，C 1-6烷氧基C 1-6烷基，或 ç_{3-7 环烷基; R 4是任选地被一个，两个或三个独立地选自C 1-6烷基，C 1-6 - 烷氧基，羟基，卤素，多卤代-C 1-6烷基，多卤C 1-6烷氧基，氨基，单或二C 1-6烷基氨基，单或二C 1-6烷基氨基羰基，C 1-6烷基羰基 - 氨基，芳基和Het; n为3,4,5或6; 每个虚线（代表）表示任选的双键; R 5是氢; 芳基; HET; 任选被C 1-6烷基取代的C 3-7环烷基; 或任选被C 3-7环烷基，芳基或与Het取代的C 1-6烷基; R 6是芳基; HET; 任选被C 1-6烷基取代的C 3-7环烷基; 或任选被C 3-7环烷基，芳基或与Het取代的C 1-6烷基; 每个芳基是任选被一个，两个或三个取代基取代的苯基; 并且每个Het是含有1至4个各自独立地选自氮，氧和硫的杂原子的5或6元饱和，部分不饱和或完全不饱和的杂环，并且任选地被一个，两个或三个取代基取代; 含有化合物（I）的药物组合物和制备化合物（I）的方法。还提供了式（I）的HCV抑制剂与利托那韦的生物可利用组合。}

2. 发明公开

EP1919904A1 MACROCYCLIC INHIBITORS OF HEPATITIS C VIRUS 有权
标题翻译： MAKROZYKLISCHE缝边DES肝炎C-VIRUS
公开(公告)号：EP1919904A1
公开(公告)日：2008-05-14
申请号：EP06778068.4
申请日：2006-07-28
申请人： Tibotec Pharmaceuticals Ltd. , MEDIVIR AB
发明人： RABOISSON, Pierre Jean-Marie Bernard , DE KOCK, Herman Augustinus , DORANGE, Ismet , VENDEVILLE, Sandrine Marie Helene , SURLERAUX, Dominique Louis Nestor Ghislain , TAHRI, Abdellah , SIMONNET, Yvan , VAN DE VREKEN, Wim , HU, Lili , SIMMEN, Kenneth Alan , NILSSON, Karl Magnus , SAMUELSSON, Bengt Bertil , ROSENQUIST, Åsa Annica Kristina , WALLBERG, Hans Kristian
IPC分类号： C07D401/14 , C07K5/078 , A61K31/4725 , A61P31/14
CPC分类号： C07D401/14 , C07D401/12 , C07D417/14 , C07D487/04 , C07K5/06191
摘要： Inhibitors of HCV replication of formula (I) and the N-oxides, salts, and stereoisomers thereof, wherein X is N, CH and where X bears a double bond it is C; R1 is -OR5, -NH-SO2R6; R2 is hydrogen, and where X is C or CH, R2 may also be C1-6alkyl; R3 is hydrogen, C1-6alkyl, C1-6alkoxyC1-6alkyl, or C3-7cycloalkyl; R4 is isoquinolinyl optionally substituted with one, two or three substituents each independently selected from C1-6alkyl, C1-6alkoxy, hydroxy, halo, polyhalo- C1-6alkyl, polyhaloC1-6alkoxy, amino, mono- or diC1-6alkylamino, mono- or DiC1-6alkylaminocarbonyl, C1-6alkylcarbonyl-amino, aryl, and Het; n is 3, 4, 5, or 6; each dashed line (represented by ) represents an optional double bond; R5 is hydrogen; aryl; Het; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl, aryl or with Het; R6 is aryl; Het; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl, aryl or with Het; each aryl is phenyl optionally substituted with one, two or three substituents; and each Het is a 5 or 6 membered saturated, partially unsaturated or completely unsaturated heterocyclic ring containing 1 to 4 heteroatoms each independently selected from nitrogen, oxygen and sulfur, and being optionally substituted with one, two or three substituents; pharmaceutical compositions containing compounds (I) and processes for preparing compounds (I). Bioavailable combinations of the inhibitors of HCV of formula (I) with ritonavir are also provided.

3. 发明申请

WO2006097534A1 1,3-DIHYDRO-BENZIMIDAZOL-2-YLIDENE AMINES AS INHIBITORS OF RESPIRATORY SYNCYTIAL VIRUS REPLICATION 审中-公开
标题翻译：作为呼吸道同种病毒复制的抑制剂的1,3-二氢苯并咪唑-2-基锂胺
公开(公告)号：WO2006097534A1
公开(公告)日：2006-09-21
申请号：PCT/EP2006/060852
申请日：2006-03-17
申请人： TIBOTEC PHARMACEUTICALS LTD , BONFANTI, Jean-François , FORTIN, Jérôme, Michel, Claude , DORANGE, Ismet
发明人： BONFANTI, Jean-François , FORTIN, Jérôme, Michel, Claude , DORANGE, Ismet
IPC分类号： C07D401/06 , C07D401/14 , A61K31/4184 , A61P11/00
CPC分类号： C07D401/06 , C07D235/30 , C07D401/14
摘要： Novel 1,3-dihydro-benzimidazo l-2-ylidene amine derivatives of formula (I) the addition salts and stereochemically iso meric forms wherein each Alk is C 1-6 alkanediyl; Q is hydrogen; C 1-6 alkyl subst ituted with one or two Ar 2 radicals; C 1-6 6alkyl subst ituted with quinolinyl, oxazolidinyl, thiazolidinyl, morpholinyl, thiomorpholinyl, or with pyrrolidinonyl; -CO-Ar 2 ; or Q is a radical of formula wherein t is 1, 2 or 3; R 4 is amino, mono-or di(C 1-6 alkyl)amino ; R 1 is Ar 2 , -CO-Ar 2 or a monocyclic or bicyclic heterocycle which may optionally be subst ituted; R 2 is as R 1 and additionally can be hydrogen; where Q is other than hydrogen, R 3 is hydrogen; and where Q is other than hydrogen, R 3 is a radical: (b) wherein R 6 is hydrogen, C 1-6 alkyl, substituted C 1-6 alkyl; R 7 , R 8 , R 9 are halo, cyano, C 1-6 alkyl, substituted C 1-6 alkyl, C 2-6 alkenyl, cyanoC 2-6 alkenyl, C 2-6 alkynyl, cyanoC 2 6 alkynyl, Ar1 1 , R 10a -O-, R 10a -S-, -N(R 5a R 5b ), R 10a -O-C(=O)-, N(R 5a R 5b )-C(=O)-, R 10a -C(=O)-NR 5b -, R 10b -C(=O)-O-; and R 8 and/or R 9 may also be hydrogen; which are RSV inhibitors. Compositions containing these compounds and processes for preparing these compounds and compositions.
摘要翻译：式（I）的新型1,3-二氢 - 苯并咪唑-1-基-2-亚基胺衍生物，其加成盐和立体化学异构体，其中每个Alk是C 1-6烷二基; Q是氢; 被一个或两个Ar 2基团取代的C 1-6烷基; 喹啉基，恶唑烷基，噻唑烷基，吗啉基，硫代吗啉基或与吡咯烷酮基反应的C 1-6-6烷基; -CO-的Ar ^{2 ; 或Q是式的基团，其中t是1,2或3; R 4是氨基，单 - 或二（C 1-6 - 烷基）氨基; R 1是Ar 2，-CO-Ar 2或可以任选被取代的单环或双环杂环; R 2是R 1，另外可以是氢; 其中Q不是氢，R 3是氢; 并且其中Q不是氢，R 3是自由基：（b）其中R 6是氢，C 1-6烷基，取代的C 1-6烷基; R 9，R 8，R 9是卤素，氰基，C 1-6烷基，取代的C 1 -C 6烷基， C 1-6亚烷基，C 2-6链烯基，氰基C 2-6烯基，C 2-6炔基，氰基C 2-6炔基，Ar 1，R 10a，-O-，R 10a，-S-， - N （R 5a，R 5b），R 10a -OC（= O） - ，N（R 5a）R 5 -C（= O） - ，R 10a -C（= O）-NR 5b， - R 10b， / SUP> C（= O）-O-; R 8和/或R 9也可以是氢; 其为RSV抑制剂。含有这些化合物的组合物和制备这些化合物和组合物的方法。}

4. 发明申请

WO2008119773A1 AMIDE DERIVATIVES AS INHIBITORS OF ASPARTYL PROTEASES 审中-公开
标题翻译：作为ASPARTYL蛋白抑制剂的酰胺衍生物
公开(公告)号：WO2008119773A1
公开(公告)日：2008-10-09
申请号：PCT/EP2008/053767
申请日：2008-03-28
申请人： MEDIVIR AB , KVARNSTRÖM, Ingemar , BÄCK, Marcus , SANDGREN, Veronica , OSCARSON, Stefan , BJÖRKLUND, Catarina , ROSENQUIST, Åsa , SAMUELSSON, Bertil , JOHANSSON, Per-Ola , DORANGE, Ismet
发明人： KVARNSTRÖM, Ingemar , BÄCK, Marcus , SANDGREN, Veronica , OSCARSON, Stefan , BJÖRKLUND, Catarina , ROSENQUIST, Åsa , SAMUELSSON, Bertil , JOHANSSON, Per-Ola , DORANGE, Ismet
IPC分类号： C07C311/07 , C07C311/08 , C07C237/22 , C07D207/26 , C07D213/56 , A61K31/18 , A61K31/16 , A61P25/28
CPC分类号： C07C311/08 , C07C237/22 , C07C311/07 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07D207/26 , C07D213/56
摘要： The invention provides compounds of the formula (I). N-oxides, addition salts, quaternary amines, metal complexes, stereochemically isomeric forms and metabolites thereof, wherein W is H,C 1-C 6 alkyl, C 3-C 6 cycloalkyl, aryl or heterocyclyl; Q is aryl or heterocyclyl; A is a five or six membered saturated, partially unsaturated or aromatic ring; D is (II) or (III) the other variables are as defined in the specification. The compounds of the invention are inhibitors of BACE and are among other things useful for the treatment and/or prevention of conditions associated with BACE activity such as Alzheimer's disease.
摘要翻译：本发明提供式（I）化合物。 N-氧化物，加成盐，季胺，金属络合物，立体化学异构形式及其代谢物，其中W是H，C 1 -C 6烷基，C 3 -C 6环烷基，芳基或杂环基; Q是芳基或杂环基; A是五或六元饱和，部分不饱和或芳环; D是（II）或（III）其他变量如说明书中所定义。本发明的化合物是BACE的抑制剂，并且可用于治疗和/或预防与BACE活性相关的病症如阿尔茨海默氏病。

5. 发明申请

WO2010107384A1 ASPARTYL PROTEASE INHIBITORS 审中-公开
标题翻译： ASPARTYL PROTEASE抑制剂
公开(公告)号：WO2010107384A1
公开(公告)日：2010-09-23
申请号：PCT/SE2010/050307
申请日：2010-03-19
申请人： MEDIVIR AB , AYESA, Susana , BELDA, Oscar , DORANGE, Ismet , ERSMARK, Karolina , JOHANSSON, Per-Ola , LUNDGREN, Stina , ROSENQUIST, Åsa , SAMUELSSON, Bertil , WIKTELIUS, Daniel , WÄHLING, Horst
发明人： AYESA, Susana , BELDA, Oscar , DORANGE, Ismet , ERSMARK, Karolina , JOHANSSON, Per-Ola , LUNDGREN, Stina , ROSENQUIST, Åsa , SAMUELSSON, Bertil , WIKTELIUS, Daniel , WÄHLING, Horst
IPC分类号： C07D213/81 , A61K31/166 , A61K31/18 , A61K31/402 , A61K31/426 , A61K31/44 , A61K31/4439 , A61K31/444 , A61P25/28 , C07C237/34 , C07C311/08 , C07D207/08 , C07D277/28 , C07D401/06 , C07D417/12
CPC分类号： C07C311/08 , C07C237/34 , C07C2601/02 , C07C2601/04 , C07D207/08 , C07D213/81 , C07D277/28 , C07D401/06 , C07D417/12
摘要： A compound of formula (I) N-oxides, addition salts, quaternary amines metal complexes stereochemically isomeric forms and metabolites thereof, wherein A is CR 1 Or N; formula (A) or formula (B) D is H, C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, G is NR 10 or O Q is C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, C 3 -C 6 Cycloalkyl, aryl or heterocyclyl; W is H, C 1 -C 6 alkyl, C 3 -C 6 Cycloalkyl, CH 2 F, CHF 2 or CF 3 ; one of X' and X" is H or CH 3 , the other is C 1 -C 3 alkyl, F, OH, NRaRb, CF 3 or N 3 ; or X' and X" are both F; Y is NRd or O; Z is O, NRa, CHRd, CF 2 or S(=0)r or a bond; the other variables are as defined in the specification. The compounds of the invention are inhibitors of BACE and are among other things useful for the treatment and/or prevention of conditions associated with BACE activity such as Alzheimer's disease.
摘要翻译：式（I）的化合物N-氧化物，加成盐，季胺金属络合物立体化学异构形式及其代谢物，其中A是CR 1或N; 式（A）或式（B）D是H，C1-C6烷基，C2-C6链烯基，C2-C6炔基，G是NR10或OQ是C1-C6烷基，C2-C6链烯基，C2-C6炔基，C3-C6环烷基，芳基或杂环基 ; W是H，C 1 -C 6烷基，C 3 -C 6环烷基，CH 2 F，CHF 2或CF 3; X'和X“之一是H或CH3，另一个是C 1 -C 3烷基，F，OH，NR a R b，CF 3或N 3;或X'和X”均为F; Y为NRd或O; Z是O，NR a，CHR d，CF 2或S（= O）r或键; 其他变量如规范中所定义。本发明的化合物是BACE的抑制剂，并且可用于治疗和/或预防与BACE活性相关的病症如阿尔茨海默氏病。

6. 发明公开

EP1951704A1 1,3-DIHYDRO-BENZIMIDAZOL-2-YLIDENE AMINES AS INHIBITORS OF RESPIRATORY SYNCYTIAL VIRUS REPLICATION 有权转让
标题翻译：用于治疗或预防病毒感染SUITABLE 1,3-二氢-2- YLIDENAMINE
公开(公告)号：EP1951704A1
公开(公告)日：2008-08-06
申请号：EP06708798.1
申请日：2006-03-17
申请人： Tibotec Pharmaceuticals Ltd.
发明人： BONFANTI, Jean-François , FORTIN, Jérôme, Michel, Claude , DORANGE, Ismet
IPC分类号： C07D401/06 , C07D401/14 , A61K31/4184 , A61P11/00
CPC分类号： C07D401/06 , C07D235/30 , C07D401/14
摘要： Novel 1,3-dihydro-benzimidazo l-2-ylidene amine derivatives of formula (I) the addition salts and stereochemically iso meric forms wherein each Alk is C1-6alkanediyl; Q is hydrogen; C1-6alkyl subst ituted with one or two Ar2 radicals; C1-66alkyl subst ituted with quinolinyl, oxazolidinyl, thiazolidinyl, morpholinyl, thiomorpholinyl, or with pyrrolidinonyl; -CO-Ar2; or Q is a radical of formula wherein t is 1, 2 or 3; R4 is amino, mono-or di(C1-6alkyl)amino ; R1 is Ar2, -CO-Ar2 or a monocyclic or bicyclic heterocycle which may optionally be subst ituted; R2 is as R1 and additionally can be hydrogen; where Q is other than hydrogen, R3 is hydrogen; and where Q is other than hydrogen, R3 is a radical: (b) wherein R6 is hydrogen, C1-6alkyl, substituted C1-6alkyl; R7, R8, R9 are halo, cyano, C1-6alkyl, substituted C1-6alkyl, C2-6alkenyl, cyanoC2-6alkenyl, C2-6alkynyl, cyanoC2 6alkynyl, Ar11, R10a-O-, R10a-S-, -N(R5aR5b), R10a-O-C(=O)-, N(R5aR5b)-C(=O)-, R10a-C(=O)-NR5b-, R10b-C(=O)-O-; and R8 and/or R9 may also be hydrogen; which are RSV inhibitors. Compositions containing these compounds and processes for preparing these compounds and compositions.

7. 发明申请

WO2010042030A1 ASPARTYL PROTEASE INHIBITORS 审中-公开
标题翻译： ASPARTYL PROTEASE抑制剂
公开(公告)号：WO2010042030A1
公开(公告)日：2010-04-15
申请号：PCT/SE2009/051105
申请日：2009-10-05
申请人： MEDIVIR AB , LUNDBERG, Stina , AYESA, Susana , BELDA, Oscar , DORANGE, Ismet , ERSMARK, Karolina , HAMMER, Kristin , JOHANSSON, Per-Ola , LINDSTRÖM, Stefan , ROSENQUIST, Åsa , SAMUELSSON, Bertil , BÄCK, Marcus , KVARNSTRÖM, Ingemar , WÅNGSELL, Fredrik , BJÖRKLUND, Katarina
发明人： LUNDBERG, Stina , AYESA, Susana , BELDA, Oscar , DORANGE, Ismet , ERSMARK, Karolina , HAMMER, Kristin , JOHANSSON, Per-Ola , LINDSTRÖM, Stefan , ROSENQUIST, Åsa , SAMUELSSON, Bertil , BÄCK, Marcus , KVARNSTRÖM, Ingemar , WÅNGSELL, Fredrik , BJÖRKLUND, Katarina
IPC分类号： C07D213/75 , A61K31/195 , A61K31/455 , A61P25/28 , C07C229/38 , C07D207/26 , C07D263/20 , C07D279/02 , C07D285/06
CPC分类号： C07D213/81 , C07C233/78 , C07C237/34 , C07C309/66 , C07C311/08 , C07C311/16 , C07D207/27 , C07D263/22 , C07D277/28 , C07D279/02 , C07D285/10 , C07D295/26 , C07D401/12 , C07D417/12
摘要： A compound of formula (I): N-oxides, addition salts, quaternary amines metal complexes stereochemically isomeric forms and metabolites thereof, wherein A is CR 1 or N; D is H, C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl or Q is C 2 -C 6 alkenyl, C 2 -Cealkynyl, aryl or heterocyclyl; W is H, Ci-Cealkyl, C 2 -C 6 alkenyl, haloC 1 -C 3 alkyl, hydroxyC 1 -C 3 alkyl, C 3 -C 6 Cy cloalkyl, aryl or heterocyclyl; one of X' and X" is H or CH 3 , the other is C 1 -C 3 alkyl, F, OH, NRaRb, CF 3 or N 3 ; or X' and X" are both F; Y is a bond, CH 2 , NRa, O, CH 2 CH 2 , CH 2 NRa, CH 2 O or S(=O) r ; Z is O, S(=O) r or NRa; the other variables are as defined in the specification. The compounds of the invention are inhibitors of BACE and are among other things useful for the treatment and/or prevention of conditions associated with BACE activity such as Alzheimer's disease.
摘要翻译：式（I）的化合物：N-氧化物，加成盐，季胺金属络合物立体化学异构形式及其代谢物，其中A是CR 1或N; D是H，C 1 -C 6烷基，C 2 -C 6烯基，C 2 -C 6炔基或Q是C 2 -C 6烯基，C 2 -C 6炔基，芳基或杂环基; W是H，C 1 -C 6烷基，C 2 -C 6烯基，卤代C 1 -C 3烷基，羟基C 1 -C 3烷基，C 3 -C 6环烷基，芳基或杂环基; X'和X“之一是H或CH3，另一个是C 1 -C 3烷基，F，OH，NR a R b，CF 3或N 3;或X'和X”均为F; Y是键，CH2，NRa，O，CH2CH2，CH2NRa，CH2O或S（= O）r; Z是O，S（= O）r或NR a; 其他变量如规范中所定义。本发明的化合物是BACE的抑制剂，并且可用于治疗和/或预防与BACE活性相关的病症如阿尔茨海默氏病。

8. 发明申请

WO2008135488A1 ASPARTYL PROTEASE INHIBITORS 审中-公开
标题翻译： ASPARTYL PROTEASE抑制剂
公开(公告)号：WO2008135488A1
公开(公告)日：2008-11-13
申请号：PCT/EP2008/055326
申请日：2008-04-30
申请人： MEDIVIR AB , BJÖRKLUND, Catarina , KVARNSTRÖM, Ingemar , AYESA, Susana , JOHANSSON, Per-Ola , DORANGE, Ismet , ERSMARK, Karolina , SAMUELSSON, Bertil , ROSENQUIST, Åsa
发明人： BJÖRKLUND, Catarina , KVARNSTRÖM, Ingemar , AYESA, Susana , JOHANSSON, Per-Ola , DORANGE, Ismet , ERSMARK, Karolina , SAMUELSSON, Bertil , ROSENQUIST, Åsa
IPC分类号： C07D267/00 , C07D313/00 , A61P25/28 , A61K31/365
CPC分类号： C07D313/00 , C07D267/00
摘要： The invention provides compounds of the formula (I) N-oxides, addition salts, quaternary amines, metal complexes, stereochemically isomeric forms and metabolites thereof, wherein G is-O-, -S(=O) r -, -CRdRd or -NRa-; W is H, C 1 -C 6 alkyl, C 3 -C 6 cycloalkyl, aryl or heterocyclyl; L 1 is a bond, methyleneor ethylene; L 2 is CHR 1 ;or L 1 and L 2 together form CH=CH; L 3 is a bond, C(=O) or CH 2 ; V 1 and V 2 are independently a bond, NRa, CRdRd or O; R 1 is H, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, C 1 -C 4 alkoxyC 1 -C 4 alkyl, C 1 -C 4 alkoxyC 1 -C 4 alkoxyC 1 -C 4 alkyl, C 0 -C 3 alkandiylcarbocyclyl or C 0 -C 3 alkandiylheterocyclyl; R 2b are both H, or the two R 2b together form=O; ring A is a five or six membered saturated, partially unsaturated or aromatic ring; and the other variables are as defined in the specification. The compounds of the invention are inhibitors of BACE and are among other things useful for the treatment and/or prevention of conditions associated with BACE activity such as Alzheimer´s disease.
摘要翻译：本发明提供式（I）的化合物N-氧化物，加成盐，季胺，金属配合物，立体化学异构形式及其代谢物，其中G是-O-，-S（= O） > - ，-CRdRd或-NRa-; W是H，C 1 -C 6烷基，C 3 -C 6 -C 6环烷基，芳基或杂环基; L 1是键，亚甲基或亚乙基; L 2是CHR 1或L 1和L 2一起形成CH = CH; L 3是一个键，C（= O）或CH 2; V 1和V 2独立地是键，NR a，CR d R d或O; R 1是H，C 1 -C 6烷基，C 1 -C 6烷基，C 1 -C 6烷基，C 1 -C 6烷基，烷氧基，C 1 -C 4烷氧基C 1 -C 4烷基，C 1 -C 4烷基，C 1 -C 4烷基， / SUB> -C _{4 烷氧基C _{1 -C _{4 烷氧基C _{1 -C ₄}}}}

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