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1. 发明申请

WO02055496A8 ARYL PIPERIDINE AND PIPERAZINE DERIVATIVES AS INDUCERS OF LDL-RECEPTOR EXPRESSION 审中-公开
标题翻译：作为低密度脂蛋白受体表达的诱导剂的ARYL PIPERIDINE AND PIPERAZINE DERIVATIVES
公开(公告)号：WO02055496A8
公开(公告)日：2003-07-17
申请号：PCT/GB0100158
申请日：2001-01-15
申请人： GLAXO GROUP LTD , BOUILLOT ANNE MARIE JEANNE , BOMBRUN AGNES , DUMAITRE BERNARD ANDRE , GOSMINI ROMAIN LUC MARIE , RAMSDEN NIGEL GRAHAME , CONGREVE MILES STUART
发明人： BOUILLOT ANNE MARIE JEANNE , BOMBRUN AGNES , DUMAITRE BERNARD ANDRE , GOSMINI ROMAIN LUC MARIE , RAMSDEN NIGEL GRAHAME , CONGREVE MILES STUART
IPC分类号： C07D295/12 , A61K31/445 , A61K31/4468 , A61K31/451 , A61K31/4525 , A61K31/4535 , A61K31/454 , A61K31/4545 , A61K31/495 , A61K31/551 , A61P1/18 , A61P3/04 , A61P3/06 , A61P3/10 , A61P9/10 , A61P43/00 , C07D211/14 , C07D211/20 , C07D211/22 , C07D211/46 , C07D211/58 , C07D295/13 , C07D401/04 , C07D401/12 , C07D405/04 , C07D405/12 , C07D405/14 , C07D409/04 , C07D409/12 , C07D417/12
CPC分类号： C07D295/13 , A61K31/451 , A61K31/495 , C07D211/14 , C07D211/22 , C07D211/46 , C07D211/58 , C07D401/04 , C07D401/12 , C07D405/04 , C07D405/12 , C07D409/04 , C07D409/12
摘要： The invention concerns Use of a compound of formula (I) or a physiologically acceptable salt, solvate or derivative thereof, in the manufacture of a medicament for the treatment of diseases ameliorated by LDL-r upregulation, to novel compounds and pharmaceutical compositions within the scope of formula (I).
摘要翻译：本发明涉及式（I）化合物或其生理上可接受的盐，溶剂合物或衍生物在制备用于治疗LDL-r上调改善的疾病的药物中的用途，涉及范围内的新化合物和药物组合物的式（I）化合物。

2. 发明申请

WO1998016526A1 TETRAHYDRO-6H-PYRAZINO[1,2-B]ISOQUINOLINE 1,4-DIONES AS APOPROTEIN B-100 INHIBITORS 审中-公开
标题翻译：四氢呋喃-6H-吡咯并[1,2-B]异喹啉1,4-二酮作为APOPROTEIN B-100抑制剂
公开(公告)号：WO1998016526A1
公开(公告)日：1998-04-23
申请号：PCT/EP1997005636
申请日：1997-10-15
申请人： GLAXO GROUP LIMITED , LABAUDINIERE, Richard, Frederic , MARTRES, Paul , DODIC, Nerina , DUMAITRE, Bernard, Andre
发明人： GLAXO GROUP LIMITED
IPC分类号： C07D471/04
CPC分类号： C07D471/04
摘要： The prevent invention relates to compounds of formula (I) wherein R represents C3-8 cycloalkyl, optionally substituted by C1-4 alkyl; R represents hydrogen, halogen, NO2, CN, CHO, NHSO2R , NR R , NR COR , a 5-membered heteroaromatic ring optionally substituted by C1-4 alkyl, or a group X-Z; R represents hydrogen or a prop-2-enyl group; Y represents methylene or difluoromethylene; X represents a C1-6 alkylene, C2-6 alkenylene, C3-6 alkynylene or an N-linked imine group; Z represents hydrogen, C1-4alkoxy, CO2R , or an optionally substituted 5- or 6-membered heteroaromatic or phenyl group, where optional substitution is selected from a group consisting of CO2R , NR R , and NO2; Ar represents a phenyl or 5- or 6-membered heteroaromatic group optionally substituted by one or more groups selected from halogen, cyano, C1-4 alkyl, C1-4 alkoxy, CF3, S(O)nR , NHSO2R , NO2, NR R , NR COR , CO2R , CONR R , OCF3, and a 5-membered heterocyclic group optionally substituted by C1-4 alkyl; R represents C1-4 alkyl or trifluoromethyl; R and R independently represent hydrogen or C1-4 alkyl, or together R and R form a 3- to 6-membered cycloalkylamine ring; R and R independently represent hydrogen or C1-4 alkyl; R represents C1-4 alkyl or (CH2)mE, where m is 0 or 1 and E is a 5- or 6-membered heteroaromatic group; n is an integer from 0-3; and pharmaceutically acceptable derivatives thereof, to processes for their preparation; and their use in the treatment of conditions mediated by ApoB-100 regulation.
摘要翻译：本发明涉及式（I）化合物，其中R 0表示任选被C 1-4烷基取代的C 3-8环烷基; R 1表示氢，卤素，NO 2，CN，CHO，NHSO 2 R 3，NR 4 R 5，NR 6 COR 7，任选被C 1-4取代的5元杂芳环烷基或基团XZ; R 2表示氢或丙-2-烯基; Y表示亚甲基或二氟亚甲基; X表示C 1-6亚烷基，C 2-6亚烯基，C 3-6亚炔基或N-连接的亚胺基; Z表示氢，C 1-4烷氧基，CO 2 R 6或任选取代的5或6元杂芳族或苯基，其中任选的取代选自CO 2 R 6，NR 4 R 5 >和NO2; Ar表示任选被一个或多个选自卤素，氰基，C 1-4烷基，C 1-4烷氧基，CF 3，S（O）n R 5，NHSO 2 R 5的基团取代的苯基或5-或6-元杂芳基 >，NO 2，NR 4 R 5，NR 6 COR 8，CO 2 R 6，CONR 4 R 5，OCF 3和任选被C 1 -C 6取代的5元杂环基， 4烷基; R 3表示C 1-4烷基或三氟甲基; R 4和R 5独立地表示氢或C 1-4烷基，或者R 4和R 5一起形成3-至6-元环烷基胺环; R 6和R 8独立地表示氢或C 1-4烷基; R 7表示C 1-4烷基或（CH 2）mE，其中m为0或1，E为5或6元杂芳基; n是0-3的整数; 及其药学上可接受的衍生物，用于其制备方法; 及其用于治疗由ApoB-100调节介导的病症。

3. 发明申请

WO2004007493A1 ARYL PIPERIDINE DERIVATIVES AS INDUCERS OF LDL-RECEPTOR EXPRESSION FOR THE TREATMENT OF HYPERCHOLESTEROLEMIA 审中-公开
标题翻译：作为低密度脂蛋白受体表达诱导剂治疗高脂血症的ARYL哌啶衍生物
公开(公告)号：WO2004007493A1
公开(公告)日：2004-01-22
申请号：PCT/EP2003/007617
申请日：2003-07-11
申请人： GLAXO GROUP LIMITED , BOUILLOT, Anne, Marie, Jeanne , DUMAITRE, Bernard, Andre
发明人： BOUILLOT, Anne, Marie, Jeanne , DUMAITRE, Bernard, Andre
IPC分类号： C07D417/12
CPC分类号： C07D417/12 , C07D211/22 , C07D417/14
摘要： This invention relates to novel compounds which up-regulate LDL receptor (LDL-r) expression and to processes for their preparation, pharmaceutical compositions containing them and their medical use. More particularly, this invention relates to novel aromatic piperidines of formula (I) and their use in therapy. wherein Ar 1 is substituted by at least one R' group selected from: -O(CR a R b ) n C(O)NR x R y ,. -O(CH 2 ) n CN, -O(CH 2 )nO(CH2) m OR 2 , -O(CH 2 )nCO 2 R 2 , -OSO 2 NR X R y , -OSO 2 (CH 2 ) p CH 3 , -(CR a R b ) n C(O)NR X R y , -(CH 2 ) n CN, -(CH 2 )nO(CH 2 ) m OR 2 , -(CH 2 ) n CO 2 R 2 , -(CH 2 )nC(O)R 2 , - SO 2 NR X R y , -SO 2 (CH 2 ) p CH 3 , -CH=CHC(O)NR x R y , -CH=CHCN, -CH=CHCO 2 R 2 , -CO 2 R 2 , - C(O)R 2 , -C(O)NR X R y and C 2-5 alkenyl; and Ar 2 is substituted by 1-4 groups independently selected from the group consisting of: (CH 2 ) n OH and -C0 2 (CH 2 ) p CH 3 .
摘要翻译：本发明涉及上调LDL受体（LDL-r）表达的新化合物及其制备方法，含有它们的药物组合物及其医疗用途。更具体地说，本发明涉及式（I）的新型芳族哌啶及其在治疗中的用途。其中Ar 1被至少一个选自以下的R 1基团取代：-O（CR a R b）n C（O）NR x R y。 -O（CH2）nCN，-O（CH2）nO（CH2）mOR2，-O（CH2）nCO2R2，-OSO2NRXRy，-OSO2（CH2）pCH3， - （CRαR）nC（O）NRXRy， - （CH2）nCN， - （CH2）nO（CH2）mOR2， - （CH2）nCO2R2， - （CH2）nC（O） SO 2 NR X R y，-SO 2（CH 2）p CH 3，-CH = CHC（O）NR x R y，-CH = CHCN，-CH = CHCO 2 R 2，-CO 2 R 2，-C（O）R 2，-C O）NR X R y和C 2-5烯基; 并且Ar 2被独立地选自：（CH 2）n OH和-CO 2（CH 2）p CH 3的1-4个基团取代。

4. 发明申请

WO2004000785A2 CHEMICAL COMPOUNDS 审中-公开
标题翻译：化学化合物
公开(公告)号：WO2004000785A2
公开(公告)日：2003-12-31
申请号：PCT/EP2003/006417
申请日：2003-06-18
申请人： SMITHKLINE BEECHAM CORPORATION , DODIC, Nerina , DUMAITRE, Bernard, Andre , GELLIBERT, Francoise, Jeanne , SIERRA, Michael, Lawrence
发明人： DODIC, Nerina , DUMAITRE, Bernard, Andre , GELLIBERT, Francoise, Jeanne , SIERRA, Michael, Lawrence
IPC分类号： C07C229/00
CPC分类号： C07D231/12 , C07D231/38 , C07D271/06 , C07D277/28 , C07D277/42 , C07D409/12 , C07D417/12
摘要： A compound of formula (I) or a pharmaceutically acceptable salt, solvate, or hydrolysable ester thereof, wherein:
摘要翻译：式（I）化合物或其药学上可接受的盐，溶剂合物或可水解的酯，其中：

5. 发明申请

WO2002096894A1 THIAZOLE OR OXAZOLE DERIVATIVES WHICH ARE USEFUL IN THE TREATMENT OF CARDIOVASCULAR AND RELATED DISEASES 审中-公开
标题翻译：可用于治疗心血管和相关疾病的噻唑或氧唑衍生物
公开(公告)号：WO2002096894A1
公开(公告)日：2002-12-05
申请号：PCT/EP2002/005885
申请日：2002-05-29
申请人： GLAXO GROUP LIMITED , DUMAITRE, Bernard, Andre , GOSMINI, Romain, Luc, Marie
发明人： DUMAITRE, Bernard, Andre , GOSMINI, Romain, Luc, Marie
IPC分类号： C07D277/56
CPC分类号： C07D417/06 , C07D277/56
摘要： A compound of formula (1) and pharmaceutically acceptable salts, solvates and hydrolysable esters thereof: wherein R 1 and R 2 are independently H or C 1-3 alkyl or R 1 and R 2 which are bonded to the same carbon atom may together with the carbon atom to which they are bonded form a 3-5 membered cycloalkyl ring; X 1 represents O or S; Each R 3 , R 4 , R 8 and R 9 independently represents H, halogen, -CH 3 and OCH 3 ; R 5 represents H or C 1-6 alkyl or R 4 and R 5 together form a 3-6 membered cycloalkyl ring. X 2 represents NH, NCH 3 or O; One of Y and Z is N, and the other is O or S; R 6 represents phenyl or pyridyl (wherein the N is in position 2 or 3) and is optionally substituted by one more halogen, CF 3 , C 1-6 straight or branched alkyl (optionally substituted by halogen), with the provision that when R 6 is pyridyl, the N is unsubstituted. R 7 represents C 1-6 alkyl, (optionally substituted by one or halogens), -C 0-6 alkyl-5 membered heteroaryl C 0-6 alkyl (O) n - phenyl, wherein n is 0 or 1, with the proviso that when R 1 and R 2 are methyl, R 8 and R 9 are H, R 5 is H, then R 7 cannot be CH 3 or CF 3 .
摘要翻译：式（1）的化合物及其药学上可接受的盐，溶剂合物和可水解的酯：其中R 1和R 2独立地是H或C 1-3烷基或R 1和R 2，它们与相同的碳原子可以与它们所键合的碳原子一起形成3-5元环烷基环; X1表示O或S; 每个R 3，R 4，R 8和R 9独立地表示H，卤素，-CH 3和OCH 3; R 5表示H或C 1-6烷基或R 4和R 5一起形成3-6元环烷基环。 X2表示NH，NCH 3或O; Y和Z之一是N，另一个是O或S; R 6表示苯基或吡啶基（其中N在2或3位），并且任选地被另外一个卤素，CF 3，C 1-6直链或支链烷基（任选被卤素取代）取代，其条件是当R 6是吡啶基，N是未取代的。 R 7表示C 1-6烷基（任选被一个或多个卤素取代），-C 0-6烷基-5-元杂芳基C 0-6烷基（O）n - 苯基，其中n为0或1，条件是当R 1和R 2为甲基时，R 8和R 9为H，R 5为H，则R 7不能为CH 3或CF 3。

6. 发明申请

WO2004000785A3 PHENYLOXYALKANONIC ACID DERIVATIVES AS HPPAR ACTIVATORS 审中-公开
标题翻译：苯丙酮酸衍生物作为HPPAR激活剂
公开(公告)号：WO2004000785A3
公开(公告)日：2004-10-14
申请号：PCT/EP0306417
申请日：2003-06-18
申请人： SMITHKLINE BEECHAM CORP , DODIC NERINA , DUMAITRE BERNARD ANDRE , GELLIBERT FRANCOISE JEANNE , SIERRA MICHAEL LAWRENCE
发明人： DODIC NERINA , DUMAITRE BERNARD ANDRE , GELLIBERT FRANCOISE JEANNE , SIERRA MICHAEL LAWRENCE
IPC分类号： A61K31/415 , A61K31/4155 , A61K31/4245 , A61K31/426 , A61K31/427 , A61P1/14 , A61P3/04 , A61P3/06 , A61P3/10 , A61P5/50 , A61P9/04 , A61P9/10 , A61P25/00 , A61P43/00 , C07D231/12 , C07D231/38 , C07D271/06 , C07D277/20 , C07D277/28 , C07D277/42 , C07D409/12 , C07D417/12 , C07C271/06 , A61K31/425 , C07C231/12 , C07C409/12 , C07C231/38 , C07C277/28 , C07C277/42 , C07C417/12
CPC分类号： C07D231/12 , C07D231/38 , C07D271/06 , C07D277/28 , C07D277/42 , C07D409/12 , C07D417/12
摘要： A compound of formula (I) or a pharmaceutically acceptable salt, solvate, or hydrolysable ester thereof, wherein:
摘要翻译：式（I）化合物或其药学上可接受的盐，溶剂合物或可水解的酯，其中：

7. 发明申请

WO2004006922A1 ARYL PIPERIDINE DERIVATIVES AS INDUCERS OF LDL-RECEPTOR EXPRESSION FOR THE TREATMENT OF HYPERCHOLESTEROLEMIA 审中-公开
标题翻译：作为低密度脂蛋白受体表达诱导剂治疗高脂血症的ARYL哌啶衍生物
公开(公告)号：WO2004006922A1
公开(公告)日：2004-01-22
申请号：PCT/EP2003/007612
申请日：2003-07-11
申请人： GLAXO GROUP LIMITED , BOUILLOT, Anne, Marie, Jeanne , DUMAITRE, Bernard, Andre
发明人： BOUILLOT, Anne, Marie, Jeanne , DUMAITRE, Bernard, Andre
IPC分类号： A61K31/445
CPC分类号： C07D401/04 , C07D211/14 , C07D401/12 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/12 , C07D417/12 , C07D417/14
摘要： This invention relates to novel compounds which up-regulate LDL receptor (LDL-r) expression and to processes for their preparation, pharmaceutical compositions containing them and their medical use. More particularly, this invention relates to novel aromatic piperidines of formula (I) and their use in therapy.
摘要翻译：本发明涉及上调LDL受体（LDL-r）表达的新化合物及其制备方法，含有它们的药物组合物及其医疗用途。更具体地，本发明涉及式（I）的新型芳族哌啶及其在治疗中的用途。

8. 发明申请

WO2004006924A1 ARYL PIPERIDINE DERIVATIVES AND USE THEREOF TO REDUCE ELEVATED LEVELS OF LDL-CHOLESTEROL 审中-公开
标题翻译： ARYL PIPERIDINE衍生物及其用途，以降低LDL-胆固醇的高度水平
公开(公告)号：WO2004006924A1
公开(公告)日：2004-01-22
申请号：PCT/EP2003/007615
申请日：2003-07-11
申请人： GLAXO GROUP LIMITED , BOUILLOT, Anne, Marie, Jeanne , DUMAITRE, Bernard, Andre
发明人： BOUILLOT, Anne, Marie, Jeanne , DUMAITRE, Bernard, Andre
IPC分类号： A61K31/445
CPC分类号： C07D413/12 , C07D211/22 , C07D417/12
摘要： This invention relates to novel compounds which up-regulate LDL receptor (LDL-r) expression and to processes for their preparation, pharmaceutical compositions containing them and their medical use. More particularly, this invention relates to novel aromatic piperidines and their use in therapy.
摘要翻译：本发明涉及上调LDL受体（LDL-r）表达的新化合物及其制备方法，含有它们的药物组合物及其医疗用途。更具体地说，本发明涉及新型芳香族哌啶及其在治疗中的应用。

9. 发明申请

WO2004006923A1 ARYL PIPERIDINE DERIVATIVES AS INDUCERS OF LDL-RECEPTOR EXPRESSION FOR THE TREATMENT OF HYPERCHOLESTEROLEMIA 审中-公开
标题翻译：作为低密度脂蛋白受体表达诱导剂治疗高脂血症的ARYL哌啶衍生物
公开(公告)号：WO2004006923A1
公开(公告)日：2004-01-22
申请号：PCT/EP2003/007613
申请日：2003-07-11
申请人： GLAXO GROUP LIMITED , BOUILLOT, Anne, Marie, Jeanne , DUMAITRE, Bernard, Andre
发明人： BOUILLOT, Anne, Marie, Jeanne , DUMAITRE, Bernard, Andre
IPC分类号： A61K31/445
CPC分类号： C07D401/04 , C07D207/16 , C07D211/22 , C07D401/12 , C07D409/12 , C07D413/12 , C07D417/12
摘要： This invention relates to novel compounds which up-regulate LDL receptor (LDL-r) expression. and to processes for their preparation, pharmaceutical compositions containing them and their medical use. More particularly, this invention relates to novel aromatic piperidines of formula (I) and their use in therapy. wherein Ar 1 is substituted, by at least one R 1 group selected from: -O(CR a R b ) n C(O)NR X R y , -O(CH 2 ) n CN, -O(CH 2 )nO(CH 2 ) m OR 2 , -O(CH 2 )nCO 2 R 2 , -OS0 2 NR x R y , -OSO 2 (CH 2 ) p CH 3 , -(CR a R b ) n C(O)NR X R y , -(CH 2 ) n CN, -(CH 2 ) n O(CH 2 )mOR 2 , -(CH 2 ) n CO 2 R 2 , -(CH 2 ) n C(O)R 2 , - SO 2 NR x R y , -SO 2 (CH 2 ) p CH 3 , -CH=CHC(O)NR x R y , -CH=CHCN, -CH=CHCO 2 R 2 , -CO 2 R 2 , - C(O)R 2 , -C(O)NR x R y and C 2-5 alkenyl.
摘要翻译：本发明涉及上调LDL受体（LDL-r）表达的新化合物。及其制备方法，含有它们的药物组合物及其医疗用途。更具体地，本发明涉及式（I）的新型芳族哌啶及其在治疗中的用途。其中Ar 1被至少一个选自以下的R 1取代：-O（CR a R b）n C（O）NR X R y，-O（CH 2）n CN，-O（CH 2）n O ）mOR 2，-O（CH 2）n CO 2 R 2，-OSO 2 NR x R y，-OSO 2（CH 2）p CH 3， - （CR a R b）n C（O）NR X R y， - （CH 2）nCN， - （CH 2）（CH2）mOR2， - （CH2）nCO2R2， - （CH2）nC（O）R 2，-SO2NRxRy，-SO2（CH2）pCH3，-CH = CHC（O）NRxRy， -CH = CHCN，-CH = CHCO 2 R 2，-CO 2 R 2，-C（O）R 2，-C（O）NR x R y和C 2-5烯基。

10. 发明申请

WO02055495A8 ARYL PIPERIDINE DERIVATIVES AS INDUCERS OF LDL-RECEPTOR EXPRESSION 审中-公开
标题翻译：作为低密度脂蛋白受体表达诱导剂的ARYL PIPERIDINE衍生物
公开(公告)号：WO02055495A8
公开(公告)日：2003-07-17
申请号：PCT/GB0100155
申请日：2001-01-15
申请人： GLAXO GROUP LTD , BOUILLOT ANNE MARIE JEANNE , BOMBRUN AGNES , DUMAITRE BERNARD ANDRE , GOSMINI ROMAIN LUC MARIE , RAMSDEN NIGEL GRAHAME , CONGREVE MILES STUART
发明人： BOUILLOT ANNE MARIE JEANNE , BOMBRUN AGNES , DUMAITRE BERNARD ANDRE , GOSMINI ROMAIN LUC MARIE , RAMSDEN NIGEL GRAHAME , CONGREVE MILES STUART
IPC分类号： C07D211/14 , A61K31/445 , A61P1/18 , A61P3/06 , A61P3/10 , A61P9/00 , A61P9/10 , A61P43/00 , C07D211/22 , C07D211/34 , C07D401/06 , C07F9/59 , C07D211/26 , C07F9/12
CPC分类号： A61K31/445 , C07D211/22 , C07D211/34 , C07D401/06 , C07F9/592
摘要： The invention concerns a compound of formula (I), wherein Ar1 represents phenyl, naphthyl or phenyl fused by a C3-8cycloalkyl, where each group is substituted by a group -O-Z and optionally one to three further groups independently represented by R ; Ar2 represents phenyl or 5-6 membered heteroaromatic group, where each group is optionally substituted by one to four groups independently selected from halogen, C1-4 alkyl and C1-4 alkoxy; Ar3 represents a phenyl or a 5-6 membered heteroaromatic group, where each group is optionally substituted by one to four groups independently selected from hydroxy, alkyl, C1-4 alkoxy, C2-4 alkenyl, C2-4 alkenyloxy, C1-4 perfluoroalkoxy, C1-4 acylamino or an electron withdrawing group; A represents -C(H)-; E represents -C1-6 alkylene-; X represents -CON(H or C1-4alkyl)- or -N(H or C1-4alkyl)CO-;Y represents a direct link, -N(H or C1-4alkyl)CO- or -CON(H or C1-4alkyl)-; Z represents a metabolically labile group; R represents halogen, -S(C1-4alkyl)-, -O-(C0-4 alkylene)-R or -(C0-4alkylene)-R , where each alkylene group may additionally incorporate an oxygen in the chain, with the proviso that there are at least two carbon atoms between any chain heteroatoms; R represents: i) hydrogen, C1-4 perfluoroalkyl, C2-3alkenyl, ii) phenyl, naphthyl, a 5- or 6-membered heteroaromatic group or 1,2,3,4-tetrahydronaphthyl, optionally substituted by one or two halogen, hydroxy, C1-4 alkyl, C1-4 alkoxy groups, iii) C3-8cycloalkyl, a 3-7 membered heterocycloalkyl, iv) amino, C1-4 alkylamino or di-C1-4alkylamino, with the proviso that there are at least two carbon atoms between any chain heteroatoms;and physiologically acceptable salts, solvates and pharmaceutical compositions thereof and their use in treating disorders associated with elevated circulating levels of LDL-cholesterol.
摘要翻译：本发明涉及式（I）化合物，其中Ar 1表示苯基，萘基或被C 3-8环烷基稠合的苯基，其中每个基团被基团-OZ和任选地一个至三个另外由R 1独立地表示的基团取代。 ; Ar2表示苯基或5-6元杂芳基，其中每个基团任选被一至四个独立地选自卤素，C 1-4烷基和C 1-4烷氧基的基团取代; Ar 3表示苯基或5-6元杂芳基，其中各基团任选被一至四个独立地选自羟基，烷基，C 1-4烷氧基，C 2-4烯基，C 2-4链烯氧基，C 1-4全氟烷氧基，C 1-4酰基氨基或吸电子基团; A表示-C（H） - ; E表示-C 1-6亚烷基; X代表-CON（H或C 1-4烷基） - 或-N（H或C 1-4烷基）CO-; Y代表直链，-N（H或C 1-4烷基）CO-或-CON（H或C1- 1-4） - ; Z代表不稳定组; R 1表示卤素，-S（C 1-4烷基） - ， - O-（C 0-4亚烷基）-R 2或 - （C 0-4亚烷基）-R 2，其中每个亚烷基可另外包含链中的氧，条件是在任何链杂原子之间存在至少两个碳原子; R 2表示：i）氢，C 1-4全氟烷基，C 2-3烯基，ii）苯基，萘基，5或6元杂芳基或1,2,3,4-四氢萘基，任选地被一个或两个卤素，羟基，C 1-4烷基，C 1-4烷氧基，iii）C 3-8环烷基，3-7元杂环烷基，iv）氨基，C 1-4烷基氨基或二-C 1-4烷基氨基，条件是存在任何链状杂原子之间的至少两个碳原子;以及其生理上可接受的盐，溶剂化物和药物组合物，以及它们在治疗与升高的LDL-胆固醇循环水平相关的疾病中的用途。

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