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1. 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。

2. 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。

3. 发明申请

WO2006004880A3 SUBSTITUTED N-ARYLSULFONYLHETEROCYCLIC AMINES AS GAMMA-SECRETASE INHIBITORS 审中-公开
标题翻译：作为GAMMA-分泌酶抑制剂的取代的N-芳基磺酰氧基化胺
公开(公告)号：WO2006004880A3
公开(公告)日：2007-03-08
申请号：PCT/US2005023187
申请日：2005-06-28
申请人： SCHERING CORP , JOSIEN HUBERT B , CLADER JOHN W , BARA THOMAS A , XU RUO , LI HONGMEI , PISSARNITSKI DMITRI , ZHAO ZHIQIANG
发明人： JOSIEN HUBERT B , CLADER JOHN W , BARA THOMAS A , XU RUO , LI HONGMEI , PISSARNITSKI DMITRI , ZHAO ZHIQIANG
IPC分类号： C07D265/30 , A61K31/5377 , A61P25/28 , C07D413/12 , C07D451/02 , C07D487/08
CPC分类号： C07D265/30 , C07D413/12 , C07D451/02 , C07D487/08
摘要： This invention discloses novel gamma secretase inhibitors of the formula I: wherein: L is -O- , -N(R 6 )-, -S-, -S(O)-, or -S(O 2 )-; R 1 is selected from the group consisting of aryl and heteroaryl; R 2 is selected from the group consisting of alkyl, -C(O)-Y, -X-C(O)-Y, -alkylene-X-C(O)-Y, -alkylene-C(O)-Y, -alkylene-cycloalkylene-X-C(O)-Y, -alkylene-cycloalkylene-C(O)-Y, -cycloalkylene-alkylene-X-C(O)-Y, -cycloalkylene-alkylene-C(O)-Y, -cycloalkylene-X-C(O)-Y, -cycloalkylene-C(O)-Y, -alkylene-cycloalkylene-alkylene-X-C(O)-Y, -alkylene-cycloalkylene-alkylene-C(O)-Y, aryl, and heteroaryl; R 3 is selected from the group consisting of aryl, heteroaryl, alkyl, cycloalkyl, arylalkyl, arylcycloalkyl, heteroarylalkyl, heteroarylcycloalkyl, arylheterocycloalkyl, and alkoxyalkyl; each R 4 and R 5 is independently selected from the group consisting of H and alkyl; and Y is selected from the group consisting of -NR 8 R 9 , -N(R 6 )-(CH 2 ) b -NR 8 R 9 , aryl, heteroaryl, alkyl, cycloalkyl, arylalkyl, arylcycloalkyl, heteroarylalkyl, heteroarylcycloalkyl, and arylheterocycloalkyl; or Y is selected from the group consisting of Formula II and Formula III: 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：本发明公开了式I的新型γ分泌酶抑制剂：其中：L是-O-，-N（R 6） - ， - S - ， - S（O） - 或-S（ 0 _{2 ） - ; R 1选自芳基和杂芳基; R 2选自烷基，-C（O）-Y，-XC（O）-Y， - 亚烷基-XC（O）-Y， - 亚烷基-C（O ）-Y-亚烷基 - 亚环烷基-OC（O）-Y-亚烷基 - 亚环烷基-C（O）-Y-亚烷基 - 亚烷基-OC（O）-Y-亚烷基 - 亚烷基-C（O） Y（ - ）亚环烷基-C（O）-Y-亚烷基-C（O）-Y-亚烷基 - 亚环烷基亚烷基-XC（O）-Y-亚烷基 - 亚环烷基 - 亚烷基-C（O）-Y，芳基和杂芳基; R 3选自芳基，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，芳基杂环烷基和烷氧基烷基; 每个R 4和R 5独立地选自H和烷基; 并且Y选自-NR 8 R 9，-N（R 6） - （CH 2）芳基，杂芳基，烷基，环烷基，芳基烷基，芳基环烷基，杂芳基烷基，杂芳基环烷基和芳基杂环烷基 ; 或Y选自式II和式III的化合物：一种或多种式I化合物或包含该化合物的制剂可用于，例如，治疗阿尔茨海默病。}

4. 发明申请

WO2008153792A3 GAMMA SECRETASE MODULATORS 审中-公开
标题翻译： GAMMA秘密调节器
公开(公告)号：WO2008153792A3
公开(公告)日：2009-05-07
申请号：PCT/US2008006733
申请日：2008-05-28
申请人： SCHERING CORP , ZHU ZHAONING , GREENLEE WILLIAM J , SUN ZHONG-YUE , GALLO GIOCONDA , XU RUO , HUANG XIANHAI , ZHU XIAOHONG
发明人： ZHU ZHAONING , GREENLEE WILLIAM J , SUN ZHONG-YUE , GALLO GIOCONDA , XU RUO , HUANG XIANHAI , ZHU XIAOHONG
IPC分类号： C07D413/10 , A61K31/421 , A61K31/4355 , A61K31/5365 , A61P25/28 , C07D498/04
CPC分类号： C07D498/04 , C07D413/10
摘要： In its many embodiments, the present invention provides a novel class of heterocyclic compounds as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the central nervous system using such compounds or pharmaceutical compositions.
摘要翻译：在其许多实施方案中，本发明提供了一类新颖的杂环化合物作为γ-分泌酶的调节剂，制备这些化合物的方法，含有一种或多种这样的化合物的药物组合物，制备包含一种或多种这类化合物的药物制剂的方法和方法使用这些化合物或药物组合物治疗，预防，抑制或改善与中枢神经系统相关的一种或多种疾病。

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