公开(公告)号：US20070032506A1

公开(公告)日：2007-02-08

申请号：US11427768

申请日：2006-06-29

Applicant: Peter Giannousis ,  Kathleen Lee ,  Sundeep Dugar

Inventor： Peter Giannousis ,  Kathleen Lee ,  Sundeep Dugar

IPC: A61K31/496 ,  C07D403/02

CPC classification number: C07D209/24

Abstract: The present invention relates to novel crystalline forms of (2R-trans)-6-chloro-5-[[4-[(4-fluorophenyl)methyl]-2,5-dimethyl-1-piperazinyl]carbonyl]-N,N, 1-trimethyl-alpha-oxo-1H-indole-3-acetamide monochloride, methods for their preparation, and pharmaceutical compositions comprising the novel pseudopolymorphs.

Abstract translation: 本发明涉及（2R-反式）-6-氯-5 - [[4 - [（4-氟苯基）甲基] -2,5-二甲基-1-哌嗪基]羰基] -N，N 1-三甲基-α-氧代-1H-吲哚-3-乙酰胺一氯化物，其制备方法和包含新型假多晶型物的药物组合物。

公开(公告)号：US20050220784A1

公开(公告)日：2005-10-06

申请号：US11136242

申请日：2005-05-23

Applicant: Sarvajit Chakravarty ,  Sundeep Dugar ,  John Perumattam ,  George Schreiner ,  David Liu ,  John Lewicki

Inventor： Sarvajit Chakravarty ,  Sundeep Dugar ,  John Perumattam ,  George Schreiner ,  David Liu ,  John Lewicki

IPC: A61K31/517 ,  A61K31/519 ,  A61K31/5355 ,  A61K39/395 ,  A61P1/16 ,  A61P1/18 ,  A61P7/00 ,  A61P9/00 ,  A61P9/04 ,  A61P9/10 ,  A61P11/00 ,  A61P13/12 ,  A61P17/02 ,  A61P19/02 ,  A61P29/00 ,  A61P43/00 ,  C07D239/94 ,  C07D401/04 ,  C07D401/12 ,  C07D403/12 ,  C07D471/04 ,  C07D487/02

CPC classification number: C07D401/12 ,  A61K31/519 ,  C07D239/94 ,  C07D471/04

Abstract: The invention is directed to methods to inhibit TGF-β and/or p38-α kinase using compounds of the formula or the pharmaceutically acceptable salts thereof wherein R3 is a noninterfering substituent; each Z is CR2 or N, wherein no more than two Z positions in ring A are N, and wherein two adjacent Z positions in ring A cannot be N; each R2 is independently a noninterfering substituent; L is a linker; n is 0 or 1; and Ar′ is the residue of a cyclic aliphatic, cyclic heteroaliphatic, aromatic or heteroaromatic moiety optionally substituted with 1-3 noninterfering substituents.

Abstract translation: 本发明涉及使用下式的化合物或其药学上可接受的盐抑制TGF-β和/或p38-α激酶的方法，其中R 3是非干扰性取代基; 每个Z是CR 2或N，其中环A中不超过两个Z位是N，并且其中环A中的两个相邻Z位不能是N; 每个R 2独立地是非干扰取代基; L是连接体; n为0或1; 并且Ar'是任选被1-3个非干扰取代基取代的环脂族，环状杂脂族，芳族或杂芳族部分的残基。

公开(公告)号：US20050171183A1

公开(公告)日：2005-08-04

申请号：US11098905

申请日：2005-04-04

Applicant: Gregory Luedtke ,  Richland Tester ,  Sundeep Dugar ,  Qing Lu ,  John Perumattam ,  Xuefei Tan

Inventor： Gregory Luedtke ,  Richland Tester ,  Sundeep Dugar ,  Qing Lu ,  John Perumattam ,  Xuefei Tan

IPC: A61K31/404 ,  A61K31/407 ,  A61K31/454 ,  A61K31/573 ,  A61K39/395 ,  A61K45/00 ,  A61P1/04 ,  A61P9/10 ,  A61P11/00 ,  A61P11/06 ,  A61P17/06 ,  A61P19/02 ,  A61P19/06 ,  A61P19/08 ,  A61P25/00 ,  A61P25/08 ,  A61P25/28 ,  A61P29/00 ,  A61P31/04 ,  A61P33/06 ,  A61P35/00 ,  A61P37/06 ,  A61P43/00 ,  C07D209/18 ,  C07D401/06 ,  C07D401/12 ,  C07D403/12 ,  C07D487/04 ,  C07D487/10 ,  A61K31/405 ,  C07D487/02 ,  C07D43/02

CPC classification number: C07D401/12 ,  C07D209/18 ,  C07D403/12 ,  C07D487/04 ,  C07D487/10

Abstract: Compounds that inhibit p38-α kinase are those wherein a bicyclic aromatic system is coupled through a saturated ring to an aryl group.

Abstract translation: 抑制p38-α激酶的化合物是其中双环芳族体系通过饱和环与芳基偶联的化合物。

公开(公告)号：US06821966B2

公开(公告)日：2004-11-23

申请号：US09990187

申请日：2001-11-20

Applicant: Sundeep Dugar ,  John Perumattam ,  Gregory Luedtke ,  Xuefei Tan ,  Qing Lu

Inventor： Sundeep Dugar ,  John Perumattam ,  Gregory Luedtke ,  Xuefei Tan ,  Qing Lu

IPC: C07D40306

CPC classification number: C07D401/06 ,  C07D209/42 ,  C07D401/14 ,  C07D403/06 ,  C07D403/12 ,  C07D417/14

Abstract: The invention is directed to methods to inhibit p38-&agr; kinase using compounds of the formula and the pharmaceutically acceptable salts thereof, or a pharmaceutical composition thereof, wherein represents a single or double bond; B is —Wi—COXjY wherein Y is COR2 or an isostere thereof and R2 is hydrogen or a noninterfering substituent, each of W and X is a spacer of 2-6 Å, and each of i and j is independently 0 or 1; each R3 is independently a noninterfering substituent, where n is 0-3; Z3 is NR7 or O; wherein R7 is H or a noninterfering substituent; one Z2 is CA or CR8A and the other is CR1, CR12, NR6 or N wherein each R1, R6 and R8 is independently hydrogen or noninterfering substituent; wherein A is: such that Z1 is CR5 or N wherein R5 is hydrogen or a noninterfering substituent; each of l and k is an integer from 0-2 wherein the sum of l and k is 0-3; Ar is an aryl group substituted with 0-5 noninterfering substituents, wherein two noninterfering substituents can form a fused ring; each R4 is independently a noninterfering substituent where m is 0-4; each of L1 and L2 is a linker; and the distance between the atom of Ar linked to L2 and the center of the &bgr; ring is 4.5-24 Å.

Abstract translation: 本发明涉及使用下式的化合物及其药学上可接受的盐或其药物组合物抑制p38-α激酶的方法，其中表示单键或双键; B是-Wi-COXjY，其中Y是COR 2或其等同体，R 2 是氢或不干扰取代基，W和X各自为2-6的间隔基，i和j各自独立地为0或1;每个R 3独立地为非干扰取代基，其中n为0- 3; Z 3为NR 7或O; 其中R 7是H或不干扰取代基;一个Z 2是CA或CR 8，另一个是CR 1，CR 1，NR 6或N，其中每个R' R 6和R 8独立地是氢或非中间取代基; 其中A是：使得Z 1是CR 5或N，其中R 5是氢或非干扰取代基; l和k各自是0-2的整数，其中l和k的和为0 -3; Ar是被0-5个非直链取代基取代的芳基，其中两个不干扰的取代基可以形成稠环;每个R 4独立地是非干扰取代基，其中m是0-4; L 1和 L 2是连接体; 并且与L 2连接的Ar原子与β环的中心之间的距离为4.5-24埃。

公开(公告)号：US06498168B2

公开(公告)日：2002-12-24

申请号：US09902849

申请日：2001-07-11

Applicant: Derek Lowe ,  Wei Chang ,  Joseph Kozlowski ,  Joel G. Berger ,  Robert McQuade ,  Allen Barnett ,  Margaret Sherlock ,  Wing Tom ,  Sundeep Dugar ,  Lian-Yong Chen ,  John W Clader ,  Samuel Chackalamannil ,  Wang Yuguang ,  Stuart W. McCombie ,  Jayaram R. Tagat ,  Susan F. Vice ,  Wayne Vaccaro ,  Michael J. Green ,  Margaret E. Browne ,  Theodros Asberom

Inventor： Derek Lowe ,  Wei Chang ,  Joseph Kozlowski ,  Joel G. Berger ,  Robert McQuade ,  Allen Barnett ,  Margaret Sherlock ,  Wing Tom ,  Sundeep Dugar ,  Lian-Yong Chen ,  John W Clader ,  Samuel Chackalamannil ,  Wang Yuguang ,  Stuart W. McCombie ,  Jayaram R. Tagat ,  Susan F. Vice ,  Wayne Vaccaro ,  Michael J. Green ,  Margaret E. Browne ,  Theodros Asberom

IPC: C07D40102

CPC classification number: C07D211/20 ,  C07C2601/14 ,  C07D211/22 ,  C07D211/24 ,  C07D211/32 ,  C07D211/58 ,  C07D213/643 ,  C07D213/65 ,  C07D213/68 ,  C07D237/14 ,  C07D239/34 ,  C07D239/38 ,  C07D257/04 ,  C07D277/34 ,  C07D295/03 ,  C07D295/088 ,  C07D295/092 ,  C07D295/096 ,  C07D295/112 ,  C07D295/116 ,  C07D295/125 ,  C07D295/13 ,  C07D295/135 ,  C07D295/145 ,  C07D295/15 ,  C07D295/26 ,  C07D307/33 ,  C07D333/20 ,  C07D335/02 ,  C07D405/12 ,  C07D405/14 ,  C07D409/14

Abstract: Di-N-substituted piperazine or 1,4 di-substituted piperadine compounds in accordance with formula I (including all isomers, salts, esters, and solvates) wherein R, R1, R2, R3, R4, R21, R27, R28, X, Y, and Z are as defined herein are muscarinic antagonists useful for treating cognitive disorders such as Alzheimer's disease. Pharmaceutical compositions and methods of preparation are also disclosed. Also disclosed are synergistic combinations of compounds of the above formula or other compounds capable of enhancing acetylcholine release with acetylcholinesterase inhibitors.

Abstract translation: 根据式I的二-N-取代哌嗪或1,4-二取代哌嗪化合物（包括所有异构体，盐，酯和溶剂合物），其中R，R 1，R 2，R 3，R 4，R 21，R 27，R 28，X Y和Z如本文所定义的是可用于治疗认知障碍如阿尔茨海默氏病的毒蕈碱拮抗剂。 还公开了药物组合物和制备方法。 还公开了上述化合物或能够与乙酰胆碱酯酶抑制剂一起增强乙酰胆碱释放的其它化合物的协同组合。

公开(公告)号：US6011059A

公开(公告)日：2000-01-04

申请号：US198159

申请日：1998-11-23

Applicant: Saleem Ahmad ,  Shung C. Wu ,  Karnail S. Atwal ,  Sundeep Dugar

Inventor： Saleem Ahmad ,  Shung C. Wu ,  Karnail S. Atwal ,  Sundeep Dugar

IPC: A61K31/165 ,  A61K31/34 ,  A61K31/343 ,  A61K31/352 ,  A61K31/353 ,  A61K31/357 ,  A61K31/36 ,  A61K31/38 ,  A61K31/395 ,  A61K31/40 ,  A61K31/4025 ,  A61K31/415 ,  A61K31/42 ,  A61K31/4245 ,  A61K31/435 ,  A61K31/4402 ,  A61K31/4406 ,  A61K31/4409 ,  A61K31/4433 ,  A61K31/445 ,  A61K31/55 ,  A61P3/06 ,  A61P9/04 ,  A61P9/06 ,  A61P9/10 ,  A61P9/12 ,  A61P13/12 ,  C07C279/22 ,  C07C317/44 ,  C07D207/04 ,  C07D207/08 ,  C07D207/09 ,  C07D207/16 ,  C07D207/32 ,  C07D207/327 ,  C07D211/60 ,  C07D213/56 ,  C07D213/61 ,  C07D213/64 ,  C07D231/12 ,  C07D231/38 ,  C07D233/54 ,  C07D233/62 ,  C07D271/12 ,  C07D307/78 ,  C07D307/79 ,  C07D307/81 ,  C07D307/87 ,  C07D307/93 ,  C07D311/58 ,  C07D311/78 ,  C07D317/60 ,  C07D317/62 ,  C07D409/10 ,  C07D413/04 ,  C07D498/00 ,  C07D521/00 ,  A61K31/44 ,  C07C233/62

CPC classification number: C07D207/327 ,  C07C279/22 ,  C07D207/16 ,  C07D213/56 ,  C07D213/61 ,  C07D213/64 ,  C07D231/12 ,  C07D233/56 ,  C07D233/64 ,  C07D249/08 ,  C07D271/12 ,  C07D307/79 ,  C07D307/81 ,  C07D311/58 ,  C07D317/60 ,  C07D317/62 ,  C07D409/10 ,  C07D413/04 ,  C07C2101/02 ,  C07C2102/42

Abstract: Acyl guanidines are provided which are sodium/proton exchange (NHE) inhibitors which have the structure ##STR1## wherein n is 1 to 5; X is N or C--R.sup.5 wherein R.sup.5 is H, halo, alkenyl, alkynyl, alkoxy, alkyl, aryl or heteroaryl; and R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are as defined herein, and where X is N, R.sup.1 is preferably aryl or heteroaryl, and are useful as antianginal and cardioprotective agents. In addition, a method is provided for preventing or treating angina pectoris, cardiac dysfunction, myocardial necrosis, and arrhythmia employing the above acyl guanidines.

Abstract translation: 提供了酰基胍，其是具有其中n为1至5的结构的钠/质子交换（NHE）抑制剂; X是N或C-R5，其中R5是H，卤素，烯基，炔基，烷氧基，烷基，芳基或杂芳基; 并且R 1，R 2，R 3和R 4如本文所定义，并且其中X为N，R 1优选为芳基或杂芳基，并且可用作抗心绞痛和心脏保护剂。 此外，提供了一种用于预防或治疗心绞痛，心脏功能障碍，心肌坏死和使用上述酰基胍的心律失常的方法。

公开(公告)号：US5889006A

公开(公告)日：1999-03-30

申请号：US700628

申请日：1996-08-08

Applicant: Derek B. Lowe ,  Wei K. Chang ,  Joseph A. Kozlowski ,  Joel G. Berger ,  Robert McQuade ,  Allen Barnett ,  Margaret Sherlock ,  Wing Tom ,  Sundeep Dugar ,  Lian-Yong Chen ,  John W. Clader ,  Samuel Chackalamannil ,  Yuguang Wang ,  Stuart W. McCombie ,  Jayaram R. Tagat ,  Susan F. Vice ,  Wayne Vaccaro ,  Michael J. Green ,  Margaret E. Browne ,  Theodros Asberom ,  Craig D. Boyle

Inventor： Derek B. Lowe ,  Wei K. Chang ,  Joseph A. Kozlowski ,  Joel G. Berger ,  Robert McQuade ,  Allen Barnett ,  Margaret Sherlock ,  Wing Tom ,  Sundeep Dugar ,  Lian-Yong Chen ,  John W. Clader ,  Samuel Chackalamannil ,  Yuguang Wang ,  Stuart W. McCombie ,  Jayaram R. Tagat ,  Susan F. Vice ,  Wayne Vaccaro ,  Michael J. Green ,  Margaret E. Browne ,  Theodros Asberom ,  Craig D. Boyle

IPC: C07D211/58 ,  A61K31/00 ,  A61K31/435 ,  A61K31/4427 ,  A61K31/443 ,  A61K31/4433 ,  A61K31/445 ,  A61K31/4465 ,  A61K31/4523 ,  A61K31/4545 ,  A61K31/47 ,  A61K31/4709 ,  A61K31/495 ,  A61K31/496 ,  A61K31/50 ,  A61K31/501 ,  A61K45/00 ,  A61P25/28 ,  C07D211/24 ,  C07D211/32 ,  C07D211/96 ,  C07D239/34 ,  C07D257/04 ,  C07D295/02 ,  C07D295/03 ,  C07D295/084 ,  C07D295/088 ,  C07D295/096 ,  C07D295/112 ,  C07D295/116 ,  C07D295/125 ,  C07D295/13 ,  C07D295/135 ,  C07D295/145 ,  C07D295/15 ,  C07D401/04 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D401/02 ,  C07D403/02 ,  C07D403/14

CPC classification number: C07D405/14 ,  C07D211/24 ,  C07D211/32 ,  C07D239/34 ,  C07D257/04 ,  C07D295/03 ,  C07D295/088 ,  C07D295/092 ,  C07D295/096 ,  C07D295/112 ,  C07D295/116 ,  C07D295/125 ,  C07D295/13 ,  C07D295/135 ,  C07D295/145 ,  C07D295/15 ,  C07D405/12 ,  C07D409/14 ,  C07C2101/14

Abstract: Di-N-substituted piperazine or 1,4 di-substituted piperadine compounds in accordance with formula I (including all isomers, salts, esters, and solvates) ##STR1## wherein R, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.21, R.sup.27, R.sup.28, X, Y, and Z are as defined herein are muscarinic antagonists useful for treating cognitive disorders such as Alzheimer's disease. Pharmaceutical compositions and methods of preparation are also disclosed. Also disclosed are synergistic combinations of compounds of the above formula with acetylcholinesterase inhibitors.

Abstract translation: 根据式I的二-N-取代哌嗪或1,4-二取代哌啶化合物（包括所有异构体，盐，酯和溶剂合物）其中R，R 1，R 2，R 3，R 4，R 21，R 27 R28，X，Y和Z如本文所定义的是可用于治疗认知障碍如阿尔茨海默病的毒蕈碱性拮抗剂。 还公开了药物组合物和制备方法。 还公开了上式化合物与乙酰胆碱酯酶抑制剂的协同组合。

公开(公告)号：US5846966A

公开(公告)日：1998-12-08

申请号：US953825

申请日：1997-10-14

Applicant: Stuart B. Rosenblum ,  Sundeep Dugar ,  Duane A. Burnett ,  John W. Clader ,  Brian A. McKittrick

Inventor： Stuart B. Rosenblum ,  Sundeep Dugar ,  Duane A. Burnett ,  John W. Clader ,  Brian A. McKittrick

IPC: A61K31/21 ,  A61K31/35 ,  A61K31/395 ,  A61K31/397 ,  A61K31/40 ,  A61P3/06 ,  A61P7/00 ,  A61P9/10 ,  C07D205/08

CPC classification number: A61K45/06 ,  A61K31/21 ,  A61K31/35 ,  A61K31/395 ,  A61K31/40 ,  A61K9/2018 ,  A61K9/4858 ,  Y10S514/824

Abstract: Hydroxy-substituted azetidinone hypocholesterolemic agents of the formula ##STR1## or a pharmaceutically acceptable salt thereof, wherein: Ar.sup.1 and Ar.sup.2 are aryl or R.sup.4 -substituted aryl; Ar.sup.3 is aryl or R.sup.5 -substituted aryl; X, Y and Z are --CH.sub.2 --, --CH(lower alkyl)-- or --C(dilower alkyl)--; R and R.sup.2 are --OR.sup.6, --O(CO)R.sup.6, --O(CO)OR.sup.9 or --O(CO)NR.sup.6 R.sup.7 ; R.sup.1 and R.sup.3 are H or lower alkyl; q is 0 or 1; r is 0 or 1; m, n and p are 0-4; provided that at least one of q and r is 1, and the sum of m, n, p, q and r is 1-6; and provided that when p is 0 and r is 1, the sum of m, q and n is 1-5; R.sup.4 is selected from lower alkyl, R.sup.5, --CF.sub.3, --CN, --NO.sub.2 and halogen; R.sup.5 is selected from --OR.sup.6, --O(CO)R.sup.6, --O(CO)OR.sup.9, --O(CH.sub.2).sub.1-5 OR.sup.6, --O(CO)NR.sup.6 R.sup.7, --NR.sup.6 R.sup.7, --NR.sup.6 (CO)R.sup.7, --NR.sup.6 (CO)OR.sup.9, --NR.sup.6 (CO)NR.sup.7 R.sup.8, --NR.sup.6 SO.sub.2 R.sup.9, --COOR.sup.6, --CONR.sup.6 R.sup.7, --COR.sup.6, --SO.sub.2 NR.sup.6 R.sup.7, S(O).sub.0-2 R.sup.9, --O(CH.sub.2).sub.1-10 --COOR.sup.6, --O(CH.sub.2).sub.1-10 CONR.sup.6 R.sup.7, --(lower alkylene)COOR.sup.6 and --CH.dbd.CH--COOR.sup.6 ; R.sup.6, R.sup.7 and R.sup.8 are H, lower alkyl, aryl or aryl-substituted lower alkyl; R.sup.9 is lower alkyl, aryl or aryl-substituted lower alkyl; are disclosed, as well as a method of lowering serum cholesterol by administering said compounds, alone or in combination with a cholesterol biosynthesis inhibitor, pharmaceutical compositions containing them, and a process for preparing them.

Abstract translation: 式（I）的羟基取代的氮杂环丁酮降胆固醇剂或其药学上可接受的盐，其中：Ar 1和Ar 2是芳基或R 4取代的芳基; Ar 3是芳基或者R 5取代的芳基; X，Y和Z是-CH 2 - ， - CH（低级烷基） - 或-C（二卤代烷基） - 。 R和R 2为-OR 6，-O（CO）R 6，-O（CO）OR 9或-O（CO）NR 6 R 7; R1和R3是H或低级烷基; q为0或1; r为0或1; m，n和p为0-4; 条件是q和r中的至少一个是1，m，n，p，q和r的和是1-6; 并且当p为0且r为1时，m，q和n的和为1-5; R4选自低级烷基，R5，-CF3，-CN，-NO2和卤素; R5选自-OR6，-O（CO）R6，-O（CO）OR9，-O（CH2）1-5OR6，-O（CO）NR6R7，-NR6R7，-NR6（CO）R7，-NR6（ CO）OR 9，-NR 6（CO）NR 7 R 8，-NR 6 SO 2 R 9，-COOR 6，-CONR 6 R 7，-COR 6，-SO 2 NR 6 R 7，S（O）0-2R 9，-O（CH 2）1-10 -COOR 6，-O 1-10CONR6R7， - （低级亚烷基）COOR6和-CH = CH-COOR6; R6，R7和R8是H，低级烷基，芳基或芳基取代的低级烷基; R9是低级烷基，芳基或芳基取代的低级烷基; 以及通过单独或与胆固醇生物合成抑制剂组合使用所述化合物，含有它们的药物组合物及其制备方法来降低血清胆固醇的方法。

公开(公告)号：US5744467A

公开(公告)日：1998-04-28

申请号：US813585

申请日：1997-01-08

Applicant: Brian A. McKittrick ,  Sundeep Dugar ,  Duane A. Burnett

Inventor： Brian A. McKittrick ,  Sundeep Dugar ,  Duane A. Burnett

IPC: A61K31/395 ,  A61K31/397 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/4433 ,  A61P3/06 ,  A61P9/10 ,  C07D205/08 ,  C07D401/12 ,  C07D409/12

CPC classification number: C07D401/12 ,  C07D205/08 ,  C07D409/12

Abstract: Sulfur-substituted azetidinone hypocholesterolemic agents of the formula ##STR1## or a pharmaceutically acceptable salt thereof are disclosed, as well as pharmaceutical compositions containing them, and a method of lowering serum cholesterol by administering said compounds, alone or in combination with a cholesterol biosynthesis inhibitor.

Abstract translation: 公开了具有式“IMAGE”I的硫取代的氮杂环丁酮降胆固醇药或其药学上可接受的盐，以及含有它们的药物组合物，以及通过单独或与胆固醇生物合成组合施用所述化合物来降低血清胆固醇的方法 抑制剂。

公开(公告)号：US5624920A

公开(公告)日：1997-04-29

申请号：US342197

申请日：1994-11-18

Applicant: Brian A. McKittrick ,  Sundeep Dugar ,  Duane A. Burnett

Inventor： Brian A. McKittrick ,  Sundeep Dugar ,  Duane A. Burnett

IPC: C07D205/08 ,  C07D401/12 ,  C07D409/12 ,  A61K31/395

CPC classification number: C07D401/12 ,  C07D205/08 ,  C07D409/12

Abstract: Sulfur-substituted azetidinone hypocholesterolemic agents of the formula ##STR1## or a pharmaceutically acceptable salt thereof, wherein: Ar.sup.1 is aryl or R.sup.10 -substituted aryl;Ar.sup.2 is aryl or R.sup.4 -substituted aryl;Ar.sup.3 is aryl or R.sup.5 -substituted aryl;X and Y are --CH.sub.2 --, --CH(lower alkyl)-- or --C(dilower alkyl)--;R is --OR.sup.6, --O(CO)R.sup.6, --O(CO)OR.sup.9 or --O(CO)NR.sup.6 R.sup.7 ; R.sup.1 is hydrogen, lower alkyl or aryl; or R and R.sup.1 together are .dbd.O;q is 0 or 1; r is 0, 1 or 2; m and n are 0-5; provided that the sum of m, n and q is 1-5;R.sup.4 is selected from lower alkyl, --OR.sup.6, --O(CO)R.sup.6, --O(CO)OR.sup.9, --O(CH.sub.2).sub.1-5 OR.sup.6, --O(CO)NR.sup.6 R.sup.7, --NR.sup.6 R.sup.7, --NR.sup.6 (CO)R.sup.7, --NR.sup.6 (CO)OR.sup.9, --NR.sup.6 (CO)NR.sup.7 R.sup.8, --NR.sup.6 SO.sub.2 R.sup.9, --COOR.sup.6, --CONR.sup.6 R.sup.7, --COR.sup.6, --SO.sup.2 NR.sup.6 R.sup.7, S(O).sub.0-2 R.sup.9, --O(CH.sub.2).sub.1-10 --COOR.sup.6, --O(CH.sub.2).sub.1-10 CONR.sup.6 R.sup.7, --(lower alkylene)--COOR.sup.6 and --CH.dbd.CH--COOR.sup.6 ;R.sup.5 is selected from --OR.sup.6, --O(CO)R.sup.6, --O(CO)OR.sup.9, --O(CH.sub.2).sub.1-5 OR.sup.6, --O(CO)NR.sup.6 R.sup.7, --NR.sup.6 R.sup.7, --NR.sup.6 (CO)R.sup.7, --NR.sup.6 (CO)OR.sup.9, --NR.sup.6 (CO)NR.sup.7 R.sup.8, --NR.sup.6 SO.sub.2 R.sup.9, --COOR.sup.6, --CONR.sup.6 R.sup.7, --COR.sup.6, --SO.sub.2 NR.sup.6 R.sup.7, S(O).sub.0-2 R.sup.9, --O(CH.sub.2).sub.1-10 --COOR.sup.6, --O(CH.sub.2).sub.1-10 CONR.sup.6 R.sup.7, --CF.sub.3, --CN, --NO.sub.2, halogen, --(lower alkylene)COOR.sup.6 and --CH.dbd.CH--COOR.sup.6 ;R.sup.6, R.sup.7 and R.sup.8 are H, lower alkyl, aryl or aryl-substituted lower alkyl;R.sup.9 is lower alkyl, aryl or aryl-substituted lower alkyl; andR.sup.10 is selected from lower alkyl, --OR.sup.6, --O(CO)R.sup.6, --O(CO)OR.sup.9, --O(CH.sub.2).sub.1-5 OR.sup.6, --O(CO)NR.sup.6 R.sup.7, --NR.sup.6 R.sup.7, --NR.sup.6 (CO)R.sup.7, --NR.sup.6 (CO)OR.sup.9, --NR.sup.6 (CO)NR.sup.7 R.sup.8, --NR.sup.6 SO.sub.2 R.sup.9, --COOR.sup.6, --CONR.sup.6 R.sup.7, --COR.sup.6, --SO.sub.2 NR.sup.6 R.sup.7, S(O).sub.0-2 R.sup.9, --O(CH.sub.2).sub.1-10 --COOR.sup.6, --O(CH.sub.2).sub.1-10 CONR.sup.6 R.sup.7, --CF.sub.3, --CN, --NO.sub.2 and halogen;are disclosed, as well as pharmaceutical compositions containing them, and a method of lowering serum cholesterol by administering said compounds, alone or in combination with a cholesterol biosynthesis inhibitor.