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1. 发明专利

AU2003210865B2 Gamma secretase inhibitors 未知
公开(公告)号：AU2003210865B2
公开(公告)日：2008-01-31
申请号：AU2003210865
申请日：2003-02-05
申请人： PHARMACOPEIA INC , SCHERING CORP
发明人： ASBEROM THEODROS , SMITH ELIZABETH M , PISSARNITSKI DMITRI A , CLADER JOHN W , GUO TAO , JOSIEN HUBERT B , HOBBS DOUGLAS W
IPC分类号： C07D491/113 , A61K31/445 , A61K31/4535 , A61K31/454 , A61K31/4545 , A61K31/4709 , A61K31/4725 , A61K31/496 , A61K31/5377 , A61K31/541 , A61K31/55 , A61K31/551 , A61P25/18 , A61P25/28 , A61P43/00 , C07D211/96 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/14 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/14 , C07D471/10
摘要： This invention discloses novel gamma secretase inhibitors of the formula: wherein: R 1 is a substituted aryl or substituted heteroaryl group; R 2 is an R 1 group, alkyl, -X(CO)Y, or alkylene-X(CO)Y wherein X and Y are as defined herein; each R 3 and each R 3A are independently H, or alkyl; R 11 is aryl, heteroaryl, alkyl, cycloalkyl, arylalkyl, arylcycloalkyl, heteroarylalkyl, heteroarylcycloalkyl, arylheterocycloalkyl, or alkoxyalkyl. Also disclosed is a method of treating Alzheimer's Disease using one or more compounds of the invention.

2. 发明专利

AU2003210865A1 GAMMA SECRETASE INHIBITORS 未知
公开(公告)号：AU2003210865A1
公开(公告)日：2003-09-02
申请号：AU2003210865
申请日：2003-02-05
申请人： SCHERING CORP , PHARMACOPEIA INC
发明人： PISSARNITSKI DMITRI A , JOSIEN HUBERT B , SMITH ELIZABETH M , CLADER JOHN W , ASBEROM THEODROS , GUO TAO , HOBBS DOUGLAS W
IPC分类号： C07D491/113 , A61K31/445 , A61K31/4535 , A61K31/454 , A61K31/4545 , A61K31/4709 , A61K31/4725 , A61K31/496 , A61K31/5377 , A61K31/541 , A61K31/55 , A61K31/551 , A61P25/18 , A61P25/28 , A61P43/00 , C07D211/96 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/14 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/14 , C07D471/10 , A61K31/4427
摘要： This invention discloses novel gamma secretase inhibitors of the formula: wherein: R 1 is a substituted aryl or substituted heteroaryl group; R 2 is an R 1 group, alkyl, -X(CO)Y, or alkylene-X(CO)Y wherein X and Y are as defined herein; each R 3 and each R 3A are independently H, or alkyl; R 11 is aryl, heteroaryl, alkyl, cycloalkyl, arylalkyl, arylcycloalkyl, heteroarylalkyl, heteroarylcycloalkyl, arylheterocycloalkyl, or alkoxyalkyl. Also disclosed is a method of treating Alzheimer's Disease using one or more compounds of the invention.

3. 发明专利

AU2004274449A1 Novel gamma secretase inhibitors 未知
公开(公告)号：AU2004274449A1
公开(公告)日：2005-03-31
申请号：AU2004274449
申请日：2004-09-15
申请人： PHARMACOPEIA INC , SCHERING CORP
发明人： SMITH ELIZABETH M , PISSARNITSKI DMITRI A , GUO TAO , CLADER JOHN W , HOBBS DOUGLAS W , JOSIEN HUBERT B , ASBEROM THEODROS
IPC分类号： C07D211/96 , C07D491/113 , A61K31/44 , A61K31/445 , A61K31/4535 , A61K31/454 , A61K31/4545 , A61K31/4709 , A61K31/4725 , A61K31/496 , A61K31/5377 , A61K31/541 , A61K31/55 , A61K31/551 , A61P25/18 , A61P25/28 , A61P43/00 , C07D207/48 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/14 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/14 , C07D471/10
摘要： This invention discloses novel gamma secretase inhibitors of the formula: wherein: R is a substituted aryl or substituted heteroaryl group; R is an R group, alkyl, -XC(O)Y, alkylene-XC(O)Y, cycloalkylene-X-C(O)-Y, -CH-X-C(O)-NR -Y or -CH-X-C(O)-Y, wherein X and Y are as defined herein; each R and each R are independently H, or alkyl; R is aryl, heteroaryl, alkyl, cycloalkyl, arylalkyl, arylcycloalkyl, heteroarylalkyl, heteroarylcycloalkyl, arylheterocycloalkyl, or alkoxyalkyl. Also disclosed is a method of treating Alzheimer's Disease using one or more compounds of the invention.

4. 发明申请

WO2009008980A2 TETRAHYDROPYRANOCHROMENE GAMMA SECRETASE INHIBITORS 审中-公开
标题翻译：四氢吡喃嗡烯γ-巯基化酶抑制剂
公开(公告)号：WO2009008980A2
公开(公告)日：2009-01-15
申请号：PCT/US2008008192
申请日：2008-07-01
申请人： SCHERING CORP , WU WEN-LIAN , BARA THOMAS A , BURNETT DUANE A , CLADER JOHN W , DOMALSKI MARTIN S , JIN YAN , JOSIEN HUBERT B , LI HONGMEI , LIANG XIAN , PISSARNITSKI DMITRI A , SASIKUMAR THAVALAKULAMGARA K , WONG JESSE K , XU RUO , ZHAO ZHIQIANG , MCNAMARA PAUL
发明人： WU WEN-LIAN , BARA THOMAS A , BURNETT DUANE A , CLADER JOHN W , DOMALSKI MARTIN S , JIN YAN , JOSIEN HUBERT B , LI HONGMEI , LIANG XIAN , PISSARNITSKI DMITRI A , SASIKUMAR THAVALAKULAMGARA K , WONG JESSE K , XU RUO , ZHAO ZHIQIANG , MCNAMARA PAUL
IPC分类号： C07D311/78 , A61K31/35 , A61K31/352 , A61P25/28 , C07D407/12 , C07D493/04
CPC分类号： C07D493/04 , C07D311/78 , C07D407/12
摘要： Disclosed are novel gamma secretase inhibitors of the formula. Also disclosed are methods of inhibiting gamma-secretase, methods of treating neurodegenerative diseases, and methods of treating Alzheimer's Disease. Also disclosed are processes for preparing alkenes in one reaction step using a mixture of an aldehyde (or ketone) and an alkyl substituted with two electron withdrawing groups, and reacting the mixture with: (a) a sulfonyl halide (e.g., a sulfonyl chloride) and a basic tertiary amine, or, (b) a sulfonyl anhydride and a basic amine, or (c) an aryl-C(O)-halide and a basic tertiary amine, or (d) an aryl-C(O)-O-C(O)-aryl and a basic tertiary amine, or (e) an heteroaryl-C(O)-halide and a basic tertiary amine, or (f) a heteroaryl-C(O)-O-C(O)-heteroaryl and a basic tertiary amine.
摘要翻译：公开了下式的新型γ分泌酶抑制剂。还公开了抑制γ-分泌酶的方法，治疗神经退行性疾病的方法以及治疗阿尔茨海默氏病的方法。还公开了使用醛（或酮）和被两个吸电子基团取代的烷基的混合物在一个反应步骤中制备烯烃的方法，并使该混合物与以下物质反应：（a）磺酰卤（例如磺酰氯）（b）磺酰基酸酐和碱性胺，或（c）芳基-C（O） - 卤化物和碱性叔胺，或（d）芳基-C（O） - OC（O） - 芳基和碱性叔胺，或（e）杂芳基-C（O） - 卤化物和碱性叔胺，或（f）杂芳基-C（O）-OC（O） - 杂芳基和一种碱性叔胺。

5. 发明申请

WO2005097768A3 NOVEL GAMMA SECRETASE INHIBITORS 审中-公开
标题翻译：新的GAMMA SECRETASE抑制剂
公开(公告)号：WO2005097768A3
公开(公告)日：2005-12-15
申请号：PCT/US2005011456
申请日：2005-04-04
申请人： SCHERING CORP , ASBEROM THEODROS , CLADER JOHN W , JOSIEN HUBERT B , PISSARNITSKI DMITRI A , ZHAO ZHIQIANG , MCBRIAR MARK D
发明人： ASBEROM THEODROS , CLADER JOHN W , JOSIEN HUBERT B , PISSARNITSKI DMITRI A , ZHAO ZHIQIANG , MCBRIAR MARK D
IPC分类号： A61K31/44 , C07D211/96 , C07D401/06 , C07D401/12 , C07D401/14 , C07D451/04 , C07D471/04 , C07D471/10 , C07D487/04 , C07D487/08 , A61P25/28
CPC分类号： C07D451/04 , C07D211/96 , C07D401/06 , C07D401/12 , C07D413/06 , C07D413/14 , C07D451/06 , C07D471/04 , C07D471/10 , C07D487/04 , C07D487/08
摘要： Gamma-secretase inhibitors of the formula: Chemical formula should be inserted here as it appears on the abstract in paper form. are useful in treating various neurodegenerative diseases, wherein, for example: R1 includes unsubstituted or substituted aryl or heteroaryl groups; R2 includes -C(O)-Y, alkylene-C(O)-Y, alkylene-cycloalkylene-C(O)-Y, cycloalkylene-alkylene-C(O)-Y, alkylene cycloalkylene-alkylene-C(O)-Y, cycloalkylene-C(O)-Y, -S(O)-Y, alkylene-S(O)-Y, alkylene-cycloalkylene-S(O)-Y, cycloalkylene-alkylene-S(O)-Y, alkylene cycloalkylene-alkylene-S(O)-Y, cycloalkylene-S(O)-Y, -S(O2)-Y, alkylene-S(O2)-Y, alkylene cycloalkylene S(O2)-Y, cycloalkylene alkylene S(O2)-Y, alkylene cycloalkylene-alkylene-S(O2)-Y, and cycloalkylene-S(O2)-Y, wherein Y is as defined herein, and each of said alkylene or cycloalkylene may be unsubstituted or substituted as provided herein; each R3 is independently includes H, alkyl, O alkyl, OH, N(R9)2, acyl, and aroyl; or the moiety (R3)2, together with the ring carbon atom to which it is shown attached in formula I, defines a carbonyl group, -C(O)-; each R3A and R3B independently includes H, or alkyl; R11 includes aryl, heteroaryl, alkyl, cycloalkyl, arylalkyl, arylcycloalkyl, heteroarylalkyl, heteroarylcycloalkyl, arylheterocycloalkyl, or alkoxyalkyl. One or more of the compounds of formula I, or pharmaceutically acceptable salts, solvates, and/or esters, or compositions comprised thereof, may be used to treat, e.g., Alzheimer's Disease.
摘要翻译：化学式的γ-分泌酶抑制剂应插入此处，因为它以摘要形式出现在纸上。可用于治疗各种神经变性疾病，其中例如：R 1包括未取代或取代的芳基或杂芳基; R2包括-C（O）-Y，亚烷基-C（O）-Y，亚烷基 - 亚环烷基-C（O）-Y，亚环烷基 - 亚烷基-C（O）-Y，亚烷基亚环烷基 - 亚烷基-C （O）-Y，亚烷基-S（O）-Y，亚烷基 - 亚环烷基-S（O）-Y，亚环烷基 - 亚烷基-S（O）-Y （O）-Y，亚环烷基-S（O）-Y，-S（O 2）-Y，亚烷基-S（O 2）-Y，亚烷基亚环烷基S（O 2）-Y，亚环烷基亚烷基 S（O 2）-Y，亚烷基亚环烷基 - 亚烷基-S（O 2）-Y和亚环烷基-S（O 2）-Y，其中Y如本文所定义，并且所述亚烷基或亚环烷基中的每一个可以未被取代或如所提供的被取代本文; 每个R3独立地包括H，烷基，O烷基，OH，N（R9）2，酰基和芳酰基; 或部分（R 3）2与式I所示的环碳原子一起定义为羰基-C（O） - ; 每个R 3A和R 3B独立地包括H或烷基; R11包括芳基，杂芳基，烷基，环烷基，芳基烷基，芳基环烷基，杂芳基烷基，杂芳基环烷基，芳基杂环烷基或烷氧基烷基。一种或多种式I化合物或其药学上可接受的盐，溶剂化物和/或酯或包含其的组合物可用于治疗例如阿尔茨海默氏病。

6. 发明申请

WO2007084595A3 CARBOCYCLIC AND HETEROCYCLIC ARYLSULFONES AS GAMMA SECRETASE INHIBITORS 审中-公开
标题翻译：作为GAMMA分泌酶抑制剂的CARBOCYCLICYCLIC AND HETEROCYCLIC ARYLSULFONES
公开(公告)号：WO2007084595A3
公开(公告)日：2007-09-07
申请号：PCT/US2007001302
申请日：2007-01-18
申请人： SCHERING CORP , ASBEROM THEODROS , BARA THOMAS , BENNETT CHAD E , BURNETT DUANE A , CAPLEN MARY ANN , CLADER JOHN W , COLE DAVID J , DOMALSKI MARTIN S , JOSIEN HUBERT B , KNUTSON CHAD E , LI HONGMEI , MCBRIAR MARK D , PISSARNITSKI DMITRI A , QIANG LI , RAJAGOPALAN MURALI , SASIKUMAR THAVALAKULAMGAR K , SU JING , TANG HAIQUN , WU WEN-LIAN , XU RUO , ZHAO ZHIQIANG
发明人： ASBEROM THEODROS , BARA THOMAS , BENNETT CHAD E , BURNETT DUANE A , CAPLEN MARY ANN , CLADER JOHN W , COLE DAVID J , DOMALSKI MARTIN S , JOSIEN HUBERT B , KNUTSON CHAD E , LI HONGMEI , MCBRIAR MARK D , PISSARNITSKI DMITRI A , QIANG LI , RAJAGOPALAN MURALI , SASIKUMAR THAVALAKULAMGAR K , SU JING , TANG HAIQUN , WU WEN-LIAN , XU RUO , ZHAO ZHIQIANG
IPC分类号： C07D311/22 , C07D311/80 , C07D311/92 , C07D311/94 , C07D313/08 , C07D335/06
CPC分类号： C07D311/22 , C07C317/14 , C07C317/20 , C07C317/44 , C07C2602/08 , C07C2602/10 , C07C2602/12 , C07D311/80 , C07D311/92 , C07D311/94 , C07D313/08 , C07D335/06 , C07D405/12 , C07D409/12 , C07D491/04 , C07D493/04
摘要： This invention discloses novel gamma secretase inhibitors of the formula: R 2 and R 3 , or R 2 and R 4 , or R 3 and R 4 , together with the atoms to which they are bound, can form a fused cycloalkyl or fused heterocycloalkyl ring. The cycloalkyl ring or the heterocycloalkyl ring can be optionally substituted with one or more substituents. One or more compounds of formula (I), or formulations comprising such compounds, may be useful, e.g. in treating Alzheimer's Disease.
摘要翻译：本发明公开了下式的新型γ分泌酶抑制剂：R 2和R 3，或R 2和R 4 O / >或R 3和R 4以及它们所结合的原子可以形成稠合的环烷基或稠合的杂环烷基环。环烷基环或杂环烷基环可任选被一个或多个取代基取代。一种或多种式（I）化合物或包含这些化合物的制剂可以是有用的，例如，治疗阿尔茨海默病。

7. 发明申请

WO03014075A2 NOVEL GAMMA SECRETASE INHIBITORS 审中-公开
标题翻译：新的GAMMA秘密抑制剂
公开(公告)号：WO03014075A2
公开(公告)日：2003-02-20
申请号：PCT/US0224323
申请日：2002-08-01
申请人： SCHERING CORP
发明人： ASBEROM THEODROS , GUZIK HENRY S , JOSIEN HUBERT B , PISSARNITSKI DMITRI A
IPC分类号： A61K31/437 , A61K31/47 , A61K31/4709 , A61K31/496 , A61K31/5377 , A61P9/10 , A61P25/00 , A61P25/28 , A61P43/00 , C07D215/58 , C07D401/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D471/04 , C07D487/04 , C07D487/08 , C07D521/00 , C07D
CPC分类号： C07D231/12 , C07D215/58 , C07D233/56 , C07D249/08 , C07D401/12 , C07D405/12 , C07D409/12 , C07D471/04 , C07D487/04
摘要： This invention discloses novel gamma secretase inhibitors of the formula:(Chemical formula should be inserted here as it appears on abstract in paper form)wherein: R1 is a substituted aryl or substituted heteroaryl group; R2 is an R1 group, alkyl, -X(CO)Y, -(CR32)1-4X(CO)Y; each R3A is independently H or alkyl; X is -O-, -NH, or -N-alkyl; and Y is -NR6R7, or -N(R3)(CH2)2-6NR6R7. Also disclosed is a method of treating Alzheimer s Disease.
摘要翻译：本发明公开了具有下式的新型γ分泌酶抑制剂：（化学式应该在此插入，如纸上所示），其中：R1是取代的芳基或取代的杂芳基; R2是R1基团，烷基，-X（CO）Y， - （CR32）1-4X（CO）Y; 每个R 3A独立地是H或烷基; X是-O-，-NH或-N-烷基; 并且Y是-NR 6 R 7或-N（R 3）（CH 2）2-6 NR 6 R 7。还公开了治疗阿尔茨海默病的方法。

8. 发明专利

ECSP109845A INHIBIDORES TETRAHIDROPIRANOCROMENO DE GAMMA SECRETASA 未知
公开(公告)号：ECSP109845A
公开(公告)日：2010-02-26
申请号：ECSP109845
申请日：2010-01-05
申请人： SCHERING CORP
发明人： WONG JESSE K , PISSARNITSKI DMITRI A , CLADER JOHN W , LI HONGMEI , JOSIEN HUBERT B , BARA THOMAS , BURNETT DUANE A , DOMALSKI MARTIN S , SASIKUMAR THAVALAKULAMGAR K , WU WEN-LIAN , XU RUO , ZHAO ZHIQIANG , JIN YAN , LIANG XIAN , MCNAMARA PAUL
IPC分类号： A61K31/35 , A61K31/352 , A61P25/28 , C07D311/78
摘要： Se describen nuevos inhibidores de gamma secretasa de la fórmula: .También se describen métodos de inhibir la gamma-secretasa, métodos de tratar enfermedades neurodegenerativas, y métodos de tratar enfermedad de Alzheimer. También se describen procesos para preparar alquenos en un paso de reacción usando una mezcla de un aldehído (o cetona) y un alquilo sustituido con dos grupos atrayentes de electrones y la reacción de la mezcla con: (a) un haluro de sulfonilo (por ej., un cloruro de sulfonilo) y una amina terciaria básica, o, (b) un anhídrido de sulfonilo y una amina básica, o (c) un aril-C(O)-haluro y una amina terciaria básica, o (d) un aril-C(O)-O-C(O)-arilo y una amina terciaria básica, o (e) un heteroaril-C(O)-haluro y una amina terciaria básica, o (f) un heteroaril-C(O)-O-C(O)-heteroarilo y una amina terciaria básica.

9. 发明专利

AU2008275735A2 Tetrahydropyranochromene gamma secretase inhibitors 未知
公开(公告)号：AU2008275735A2
公开(公告)日：2010-02-11
申请号：AU2008275735
申请日：2008-07-01
申请人： SCHERING CORP
发明人： PISSARNITSKI DMITRI A , JOSIEN HUBERT B , WU WEN-LIAN , LI HONGMEI , BARA THOMAS A , CLADER JOHN W , SASIKUMAR THAVALAKULAMGARA K , WONG JESSE K , MCNAMARA PAUL , ZHAO ZHIQIANG , BURNETT DUANE A , LIANG XIAN , XU RUO , DOMALSKI MARTIN S , JIN YAN
IPC分类号： A61K31/35 , A61K31/352 , A61P25/28 , C07D311/78 , C07D407/12 , C07D493/04
摘要： Disclosed are novel gamma secretase inhibitors of the formula. Also disclosed are methods of inhibiting gamma-secretase, methods of treating neurodegenerative diseases, and methods of treating Alzheimer's Disease. Also disclosed are processes for preparing alkenes in one reaction step using a mixture of an aldehyde (or ketone) and an alkyl substituted with two electron withdrawing groups, and reacting the mixture with: (a) a sulfonyl halide (e.g., a sulfonyl chloride) and a basic tertiary amine, or, (b) a sulfonyl anhydride and a basic amine, or (c) an aryl-C(O)-halide and a basic tertiary amine, or (d) an aryl-C(O)-O-C(O)-aryl and a basic tertiary amine, or (e) an heteroaryl-C(O)-halide and a basic tertiary amine, or (f) a heteroaryl-C(O)-O-C(O)-heteroaryl and a basic tertiary amine.

10. 发明专利

AU2008275735A1 Tetrahydropyranochromene gamma secretase inhibitors 未知
公开(公告)号：AU2008275735A1
公开(公告)日：2009-01-15
申请号：AU2008275735
申请日：2008-07-01
申请人： SCHERING CORP
发明人： PISSARNITSKI DMITRI A , JOSIEN HUBERT B , WU WEN-LIAN , LI HONGMEI , BARA THOMAS A , CLADER JOHN W , SASIKUMAR THAVALAKULAMGARA K , WONG JESSE K , MCNAMARA PAUL , ZHAO ZHIQIANG , BURNETT DUANE A , LIANG XIAN , XU RUO , DOMALSKI MARTIN S , JIN YAN
IPC分类号： A61K31/35 , A61K31/352 , A61P25/28 , C07D311/78 , C07D407/12 , C07D493/04
摘要： Disclosed are novel gamma secretase inhibitors of the formula. Also disclosed are methods of inhibiting gamma-secretase, methods of treating neurodegenerative diseases, and methods of treating Alzheimer's Disease. Also disclosed are processes for preparing alkenes in one reaction step using a mixture of an aldehyde (or ketone) and an alkyl substituted with two electron withdrawing groups, and reacting the mixture with: (a) a sulfonyl halide (e.g., a sulfonyl chloride) and a basic tertiary amine, or, (b) a sulfonyl anhydride and a basic amine, or (c) an aryl-C(O)-halide and a basic tertiary amine, or (d) an aryl-C(O)-O-C(O)-aryl and a basic tertiary amine, or (e) an heteroaryl-C(O)-halide and a basic tertiary amine, or (f) a heteroaryl-C(O)-O-C(O)-heteroaryl and a basic tertiary amine.

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