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31. 发明专利

CZ288891B6 Pharmaceutical preparation exhibiting hypocholesterolaemic activity 未知
公开(公告)号：CZ288891B6
公开(公告)日：2001-09-12
申请号：CZ20001415
申请日：2000-04-19
申请人： SCHERING CORP
发明人： ROSENBLUM STUART B , DUGAR SUNDEEP , BURNETT DUANE A , CLADER JOHN W , MCKITTRICK BRIAN A
IPC分类号： A61K31/21 , A61K31/35 , A61K31/395 , A61K31/397 , A61K31/40 , A61P3/06 , A61P7/00 , A61P9/10 , C07D205/08
摘要： Hydroxy-substd. azetidinone derivs. of formula (I) and their salts are new. Ar1,Ar2 = aryl (opt. substd. by 1-5 gps. R4); Ar3 = aryl (opt. substd. by 1-5 gps. R5); X, Y, Z = CH2, CH(1-6C alkyl) or C(di(1-6C alkyl); R, R2 = OR6, OCOR6, OCOOR9 or OCONR6R7; R1, R3 = H, 1-6C alkyl or aryl; q, r = 0 or 1; m, n, p = 0-4, provided that i) at least one of q and r is 1, and the sum of m, n q and r is 1-6, and ii) when p is 0 and r is 1, the sum of m, q and n is 1-5; R4 = 1-6C alkyl, OR6, OCOR6, OCOR9, O(CH2)sOR6, OCONR6R7, NR6R7, NR6COR7, NR6COOR9, NR9, NR6CONR7R8, NR6CONR7R8, NR6SO2R9, COOR6, CONR6R7, COR6, SO2NR6R7, S(O)tR9, O(CH2)uCOOR6, O(CH2)uCONR6R7, lower alkylCOOR6, CH=CH-COOR6, CF3, CN, NO2 or halogen; R5 = OR6, OCOR6, O(CO)R9, O(CH2)vOR6, -O(CO)NR6R7, NR6R7, NR6COR7, NR6COOR9, NR6COOR9, NR6CONR7R8, NR6SO2R9, COOR6, CONR6R7, COR6, SO2NR6R7, S(O)tR9, -O(CH2)uCOOR6, O(CH2)uCONR6R7, lower alkylCOOR6 or -CH=CH-COOR6; s = 1-5; t = 0-2; u = 1-10; v = 1-5; R6, R7, R8 = H, 1-6C alkyl (opt.substd. with aryl) or aryl; and R9 = 1-6C alkyl (opt. substd. with aryl) or aryl.

32. 发明专利

CZ288861B6 Hydroxy substituted azetidinones, process of their preparation, pharmaceutical preparation in which they are comprised and their use 未知
公开(公告)号：CZ288861B6
公开(公告)日：2001-09-12
申请号：CZ83996
申请日：1994-09-14
申请人： SCHERING CORP
发明人： ROSENBLUM STUART B , DUGAR SUNDEEP , BURNETT DUANE A , CLADER JOHN W , MCKITTRICK BRIAN A
IPC分类号： A61K31/21 , A61K31/35 , A61K31/395 , A61K31/397 , A61K31/40 , A61P3/06 , A61P7/00 , A61P9/10 , C07D205/08
摘要： In the present invention there are disclosed hydroxy substituted azetidinones of the general formula I, in which the substituents have specific meanings and pharmaceutically acceptable salts thereof. Preparation process of their subgroup of the general formula IA is characterized by a) treating of lactone of the general formula II with a strong base b) bringing the reaction product obtained in the stage a) into reaction with imine of the general formula III, c) adding an acid to the reaction mixture d) removing protecting groups, if present and e) optionally functionalizing hydroxy substituents on R and on carbon to which the substituent Re3 is attached, and hydroxy group or amino group on any of Are1, Are2 and Are3, and optionally converting the obtained hydroxy substituted azetidinones to salts thereof. The pharmaceutical preparation, forming also a part of the invention and intended for treating or prevention of aterosclerosis or reduction of cholesterol level in plasma contains as

33. 发明专利

ES2155849T3 未知
公开(公告)号：ES2155849T3
公开(公告)日：2001-06-01
申请号：ES94907200
申请日：1994-01-19
申请人： SCHERING CORP
发明人： DUGAR SUNDEEP , CLADER JOHN W , BURNETT DUANE A , BROWNE MARGARET E , DAVIS HARRY R
IPC分类号： A61K31/395 , A61K31/397 , A61K31/435 , A61K31/695 , A61P3/06 , A61P9/10 , C07D205/12 , C07D471/10 , C07F7/18
摘要： Novel compounds of the formula or a pharmaceutically acceptable salt thereof, wherein: R1 is R2 and R3 are independently selected from -CH2-, -CH(lower alkyl)-, -C(di-lower alkyl)-, -CH=CH- and -C(lower alkyl)=CH-; or R1 with R2, or R1 with R3, form -CH=CH- or -CH=C(lower alkyl)-; u and v are independently 0-3, provided both are not zero; R4 is B-(CH2)mC(O)-; m is 0-5; B-(CH2)q-; q is 0-6; B-(CH2)e-Z-(CH2)r; Z is -O-, -C(O)-, phenylene, -N(R8)- or -S(O)0-2-, e and r is 0-5; the sum of e and r is 0-6; B-(C2-C6 alkenylene)-; B'-(C4-C6 alkadienylene)-; B-(CH2)t-Z-(C2-C6 alkenylene)-; t is 0-3; the sum of t and the number of carbon atoms in the alkenylene chain is 2-6; B-(CH2)f-V-(CH2)g-; V is cycloalkylene, f is 1-5, g is 0-5; the sum of f and g is 1-6; B-(CH2)t-V-(C2-C6 alkenylene)- or B'-(C2-C6 alkenylene)-V-(CH2)t-; the sum of t and the number of carbon atoms in the alkenylene chain is 2-6, B-(CH2)a-Z-(CH2)b-V-(CH2)d-; a, b and d are 0-6; the sum of a, b and d is 0-6; T-(CH2)s-; T is cycloalkyl, s is 0-6; or R1 and R4 together form B is optionally-substituted phenyl, indanyl, indenyl, naphthyl, tetrahydronaphthyl or optionally substituted-heteroaryl; and R20 and R21 are independently optionally-substituted phenyl, optionally-substituted naphthyl, indanyl, indenyl, tetrahydronaphthyl, benzodioxolyl, optionally-substituted heteroaryl, optionally-substituted benzofused heteroaryl or cyclopropyl, pharmaceutical compositions, the use as hypocholesterolemic agents, processes for preparing, and the use in combination with cholesterol biosynthesis inhibitors to treat or prevent athersclerosis.

34. 发明专利

NO305902B1 未知
公开(公告)号：NO305902B1
公开(公告)日：1999-08-16
申请号：NO961133
申请日：1996-03-20
申请人： SCHERING CORP
发明人： MCKITTRICK BRIAN A , BURNETT DUANE A , CLADER JOHN W , DUGAR SUNDEEP , ROSENBLUM STUART B
IPC分类号： A61K31/21 , A61K31/35 , C07D205/08 , A61K31/395 , A61K31/397 , A61K31/40 , A61P3/06 , A61P7/00 , A61P9/10
摘要： Hydroxy-substd. azetidinone derivs. of formula (I) and their salts are new. Ar1,Ar2 = aryl (opt. substd. by 1-5 gps. R4); Ar3 = aryl (opt. substd. by 1-5 gps. R5); X, Y, Z = CH2, CH(1-6C alkyl) or C(di(1-6C alkyl); R, R2 = OR6, OCOR6, OCOOR9 or OCONR6R7; R1, R3 = H, 1-6C alkyl or aryl; q, r = 0 or 1; m, n, p = 0-4, provided that i) at least one of q and r is 1, and the sum of m, n q and r is 1-6, and ii) when p is 0 and r is 1, the sum of m, q and n is 1-5; R4 = 1-6C alkyl, OR6, OCOR6, OCOR9, O(CH2)sOR6, OCONR6R7, NR6R7, NR6COR7, NR6COOR9, NR9, NR6CONR7R8, NR6CONR7R8, NR6SO2R9, COOR6, CONR6R7, COR6, SO2NR6R7, S(O)tR9, O(CH2)uCOOR6, O(CH2)uCONR6R7, lower alkylCOOR6, CH=CH-COOR6, CF3, CN, NO2 or halogen; R5 = OR6, OCOR6, O(CO)R9, O(CH2)vOR6, -O(CO)NR6R7, NR6R7, NR6COR7, NR6COOR9, NR6COOR9, NR6CONR7R8, NR6SO2R9, COOR6, CONR6R7, COR6, SO2NR6R7, S(O)tR9, -O(CH2)uCOOR6, O(CH2)uCONR6R7, lower alkylCOOR6 or -CH=CH-COOR6; s = 1-5; t = 0-2; u = 1-10; v = 1-5; R6, R7, R8 = H, 1-6C alkyl (opt.substd. with aryl) or aryl; and R9 = 1-6C alkyl (opt. substd. with aryl) or aryl.

35. 发明专利

AU698750B2 Sulfur-substituted azetidinone compounds useful as hypocholesterolemic agents 未知
公开(公告)号：AU698750B2
公开(公告)日：1998-11-05
申请号：AU4140196
申请日：1995-11-15
申请人： SCHERING CORP
发明人： MCKITTRICK BRIAN A , DUGAR SUNDEEP , BURNETT DUANE A
IPC分类号： A61K31/395 , A61K31/397 , A61K31/44 , A61K31/4427 , A61K31/4433 , A61P3/06 , A61P9/10 , C07D205/08 , C07D401/12 , C07D409/12
摘要： Sulfur-substituted azetidinone hypocholesterolemic agents of the formula I or a pharmaceutically acceptable salt thereof, wherein: Ar1 is aryl, R10-substituted aryl or heteroaryl; Ar2 is aryl or R4-substituted aryl; Ar3 is aryl or R5-substituted aryl; X and Y are -CH2-, -CH(lower alkyl)- or -C(dilower alkyl)-; R is -OR6, -O(CO)R6, -O(CO)OR9 or -O(CO)NR6R7; R1 is hydrogen, lower alkyl or aryl; or R and R1 together are =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; R4 is selected from lower alkyl, -OR6, -O(CO)R6, -O(CO)OR9, -O(CH2)1-5OR6, -O(CO)NR6R7, -NR6R7, -NR6(CO)R7, -NR6(CO)OR9, -NR6(CO)NR7R8, -NR6SO2R9, -COOR6, -CONR6R7, -COR6, -SO2NR6R7, S(O)0-2R9, -O(CH2)1-10-COOR6, -O(CH2)1-10CONR6R7, -(lower alkylene)-COOR6 and -CH=CH-COOR6; R5 is selected from -OR6, -O(CO)R6, -O(CO)OR9, -O(CH2)1-5OR6, -O(CO)NR6R7, -NR6R7, -NR6(CO)R7, -NR6(CO)OR9, -NR6(CO)NR7R8, -NR6SO2R9, -COOR6, -CONR6R7, -COR6, -SO2NR6R7, S(O)0-2R9, -O(CH2)1-10-COOR6, -O(CH2)1-10CONR6R7, -CF3, -CN, -NO2, halogen, -(lower alkylene)COOR6 and -CH=CH-COOR6; R6, R7 and R8 are H, lower alkyl, aryl or aryl-substituted lower alkyl; R9 is lower alkyl, aryl or aryl-substituted lower alkyl; and R10 is selected from lower alkyl, -OR6, -O(CO)R6, -O(CO)OR9, -O(CH2)1-5OR6, -O(CO)NR6R7, -NR6R7, -NR6(CO)R7, -NR6(CO)OR9, -NR6(CO)NR7R8, -NR6SO2R9, -COOR6, -CONR6R7, -COR6, -SO2NR6R7, S(O)0-2R9, -O(CH2)1-10-COOR6, -O(CH2)1-10CONR6R7, -CF3, -CN, -NO2 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.

36. 发明专利

SG46208A1 Hydroxy-substituted azetidinone compounds useful as hypocholesterolemic agents 未知
公开(公告)号：SG46208A1
公开(公告)日：1998-02-20
申请号：SG1996000732
申请日：1994-09-14
申请人： SCHERING CORP
发明人： ROSENBLUM STUART B , DUGAR SUNDEEP , BURNETT DUANE A , CLADER JOHN W , MCKITTRICK BRIAN A
IPC分类号： A61K31/21 , A61K31/35 , A61K31/395 , A61K31/397 , A61K31/40 , A61P3/06 , A61P7/00 , A61P9/10 , C07D205/08 , C07D , A61K
摘要： Hydroxy-substd. azetidinone derivs. of formula (I) and their salts are new. Ar1,Ar2 = aryl (opt. substd. by 1-5 gps. R4); Ar3 = aryl (opt. substd. by 1-5 gps. R5); X, Y, Z = CH2, CH(1-6C alkyl) or C(di(1-6C alkyl); R, R2 = OR6, OCOR6, OCOOR9 or OCONR6R7; R1, R3 = H, 1-6C alkyl or aryl; q, r = 0 or 1; m, n, p = 0-4, provided that i) at least one of q and r is 1, and the sum of m, n q and r is 1-6, and ii) when p is 0 and r is 1, the sum of m, q and n is 1-5; R4 = 1-6C alkyl, OR6, OCOR6, OCOR9, O(CH2)sOR6, OCONR6R7, NR6R7, NR6COR7, NR6COOR9, NR9, NR6CONR7R8, NR6CONR7R8, NR6SO2R9, COOR6, CONR6R7, COR6, SO2NR6R7, S(O)tR9, O(CH2)uCOOR6, O(CH2)uCONR6R7, lower alkylCOOR6, CH=CH-COOR6, CF3, CN, NO2 or halogen; R5 = OR6, OCOR6, O(CO)R9, O(CH2)vOR6, -O(CO)NR6R7, NR6R7, NR6COR7, NR6COOR9, NR6COOR9, NR6CONR7R8, NR6SO2R9, COOR6, CONR6R7, COR6, SO2NR6R7, S(O)tR9, -O(CH2)uCOOR6, O(CH2)uCONR6R7, lower alkylCOOR6 or -CH=CH-COOR6; s = 1-5; t = 0-2; u = 1-10; v = 1-5; R6, R7, R8 = H, 1-6C alkyl (opt.substd. with aryl) or aryl; and R9 = 1-6C alkyl (opt. substd. with aryl) or aryl.

37. 发明专利

ES2107548T3 未知
公开(公告)号：ES2107548T3
公开(公告)日：1997-12-01
申请号：ES92916790
申请日：1992-07-21
申请人： SCHERING CORP
发明人： BURNETT DUANE A , CLADER JOHN W , THIRUVENGADAM TIRUVETTIPURAM K , TANN CHOU-HONG , LEE JUNNING , MC ALLISTER TIMOTHY
IPC分类号： A61K31/397 , A61K31/40 , A61K31/415 , A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/47 , A61K31/395 , A61K31/495 , A61K31/535 , A61K31/695 , A61P3/06 , A61P9/10 , C07D205/08 , C07D205/085 , C07D401/04 , C07D403/04 , C07D405/04 , C07D405/10 , C07D409/04 , C07D413/10 , C07F7/08 , C07F7/10 , C07F7/18
摘要： Novel compounds of the formula wherein A is -CH=CH-B; -C IDENTICAL C-B; -(CH2)p-X-B, wherein p is 0-2 and X is a bond, -NH- or-S(O)0-2; optionally substituted heteroaryl or benzofused heteroaryl; -C(O)-B; or wherein k is 1-2; D is B'-(CH2)mC(O)-, wherein m is 1-5; B'-(CH2)q-, wherein q is 2-6; B'-(CH2)e-Z-(CH2)r-, wherein Z is -O-, -C(O)-, phenylene, -NR8- or -S(O)0-2-, e is 0-5 and r is 1-5, provided that the sum of e and r is 1-6; B'-(alkenylene)-; B'-(alkadienylene)-; B'-(CH2)t-Z-(alkenylene), wherein t is 0-3, provided that the sum of t and the number of carbon atoms in the alkenylene chain is 2-6; B'-(CH2)f-V-(CH2)g-, wherein V is cycloalkylene, f is 1-5 and g is 0-5, provided that the sum of f and g is 1-6; B'-(CH2)t-V-(alkenylene) or B'-(alkenylene)-V-(CH2)t-, provided that the sum of t and the number of carbon atoms in the alkenylene chain is 2-6; B'-(CH2)a-Z-(CH2)b-V-(CH2)d-, wherein a, b and d are 0-6, provided that the sum of a, b and d is 0-6; T(CH2)s-, wherein T is cycloalkyl and s is 1-6; naphthylmethyl or optionally substituted heteroarylmethyl; B is optionally substituted phenyl; B' is naphthyl, optionally substituted heteroaryl or optionally substituted phenyl; R is hydrogen, fluoro, alkyl, alkenyl, alkynyl, or B-(CH2)h-, wherein h is 0-3; R4 is optionally substituted phenyl, indanyl, benzofuranyl, tetrahydronaphthyl, pyridyl, pyrazinyl, pyrimidinyl or quinolyl; are disclosed, as well as their use as hypocholesterolemic agents; the method of using compounds of the formula II wherein R20 is optionally substituted phenyl, optionally substituted naphthyl, optionally substituted heteroaryl, or optionally substituted benzofused heteroaryl, R21, R22 and R23 are independently selected from H or R20; E, F and G are independently a bond; cycloalkylene; alkylene; alkenylene; alkynylene; a substituted alkylene, alkenylene or alkynylene chain ; an interrupted alkylene, alkenylene or alkynylene chain ; or an interrupted alkylene, alkenylene or alkynylene chain substituted by one or more substituents; or one of R21-E and R22-F is selected from the group consisting of halogeno, OH, alkoxy, -OC(O)R5, -NR10R11, -SH or -S(alkyl); R5 is alkyl, phenyl, R14-phenyl, benzyl or R14-benzyl; R10 and R11 are independently selected from H and lower alkyl, or a pharmaceutically acceptable salt thereof, in a pharmaceutically aceptable carrier as hypocholesterolemic agents is also disclosed.

38. 发明专利

NO972272L 未知
公开(公告)号：NO972272L
公开(公告)日：1997-05-16
申请号：NO972272
申请日：1997-05-16
申请人： SCHERING CORP
发明人： MCKITTRICK BRIAN A , DUGAR SUNDEEP , BURNETT DUANE A
IPC分类号： A61K31/395 , A61K31/397 , A61K31/44 , A61K31/4427 , A61K31/4433 , A61P3/06 , A61P9/10 , C07D205/08 , C07D401/12 , C07D409/12
摘要： Sulfur-substituted azetidinone hypocholesterolemic agents of the formula I or a pharmaceutically acceptable salt thereof, wherein: Ar1 is aryl, R10-substituted aryl or heteroaryl; Ar2 is aryl or R4-substituted aryl; Ar3 is aryl or R5-substituted aryl; X and Y are -CH2-, -CH(lower alkyl)- or -C(dilower alkyl)-; R is -OR6, -O(CO)R6, -O(CO)OR9 or -O(CO)NR6R7; R1 is hydrogen, lower alkyl or aryl; or R and R1 together are =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; R4 is selected from lower alkyl, -OR6, -O(CO)R6, -O(CO)OR9, -O(CH2)1-5OR6, -O(CO)NR6R7, -NR6R7, -NR6(CO)R7, -NR6(CO)OR9, -NR6(CO)NR7R8, -NR6SO2R9, -COOR6, -CONR6R7, -COR6, -SO2NR6R7, S(O)0-2R9, -O(CH2)1-10-COOR6, -O(CH2)1-10CONR6R7, -(lower alkylene)-COOR6 and -CH=CH-COOR6; R5 is selected from -OR6, -O(CO)R6, -O(CO)OR9, -O(CH2)1-5OR6, -O(CO)NR6R7, -NR6R7, -NR6(CO)R7, -NR6(CO)OR9, -NR6(CO)NR7R8, -NR6SO2R9, -COOR6, -CONR6R7, -COR6, -SO2NR6R7, S(O)0-2R9, -O(CH2)1-10-COOR6, -O(CH2)1-10CONR6R7, -CF3, -CN, -NO2, halogen, -(lower alkylene)COOR6 and -CH=CH-COOR6; R6, R7 and R8 are H, lower alkyl, aryl or aryl-substituted lower alkyl; R9 is lower alkyl, aryl or aryl-substituted lower alkyl; and R10 is selected from lower alkyl, -OR6, -O(CO)R6, -O(CO)OR9, -O(CH2)1-5OR6, -O(CO)NR6R7, -NR6R7, -NR6(CO)R7, -NR6(CO)OR9, -NR6(CO)NR7R8, -NR6SO2R9, -COOR6, -CONR6R7, -COR6, -SO2NR6R7, S(O)0-2R9, -O(CH2)1-10-COOR6, -O(CH2)1-10CONR6R7, -CF3, -CN, -NO2 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.

39. 发明专利

NO972272A 未知
公开(公告)号：NO972272A
公开(公告)日：1997-05-16
申请号：NO972272
申请日：1997-05-16
申请人： SCHERING CORP
发明人： MCKITTRICK BRIAN A , DUGAR SUNDEEP , BURNETT DUANE A
IPC分类号： A61K31/395 , A61K31/397 , A61K31/44 , A61K31/4427 , A61K31/4433 , A61P3/06 , A61P9/10 , C07D205/08 , C07D401/12 , C07D409/12
CPC分类号： C07D401/12 , C07D205/08 , C07D409/12

40. 发明专利

BG61118B2 SUBSTITUTED BETA-LACTAM COMPOUNDS USEFUL AS HYPOCHOLESTEROLEMIC AGENTS AND PROCESSES FOR THE PREPARATION THEREOF 未知
公开(公告)号：BG61118B2
公开(公告)日：1996-11-29
申请号：BG9856594
申请日：1994-02-24
申请人： SCHERING CORP
发明人： BURNETT DUANE A , CLADER JOHN W , THIRUVENGADAM TIRUVETTIPURAM K , TANN CHOU-HONG , LEE JUNNING , MCALLISTER TIMOTHY , COLON CESAR , BARTON DEREK H , BRESLOW RONALD , DUGAR SUNDEEP , VACCARO WAYNE
IPC分类号： A61K31/395 , A61K31/397 , A61K31/40 , A61K31/415 , A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/47 , A61K31/495 , A61K31/535 , A61K31/695 , A61P3/06 , A61P9/10 , C07D205/08 , C07D205/085 , C07D401/04 , C07D403/04 , C07D405/04 , C07D405/10 , C07D409/04 , C07D413/10 , C07F7/08 , C07F7/10 , C07F7/18
摘要： Novel compounds of the formula wherein A is -CH=CH-B; -C IDENTICAL C-B; -(CH2)p-X-B, wherein p is 0-2 and X is a bond, -NH- or-S(O)0-2; optionally substituted heteroaryl or benzofused heteroaryl; -C(O)-B; or wherein k is 1-2; D is B'-(CH2)mC(O)-, wherein m is 1-5; B'-(CH2)q-, wherein q is 2-6; B'-(CH2)e-Z-(CH2)r-, wherein Z is -O-, -C(O)-, phenylene, -NR8- or -S(O)0-2-, e is 0-5 and r is 1-5, provided that the sum of e and r is 1-6; B'-(alkenylene)-; B'-(alkadienylene)-; B'-(CH2)t-Z-(alkenylene), wherein t is 0-3, provided that the sum of t and the number of carbon atoms in the alkenylene chain is 2-6; B'-(CH2)f-V-(CH2)g-, wherein V is cycloalkylene, f is 1-5 and g is 0-5, provided that the sum of f and g is 1-6; B'-(CH2)t-V-(alkenylene) or B'-(alkenylene)-V-(CH2)t-, provided that the sum of t and the number of carbon atoms in the alkenylene chain is 2-6; B'-(CH2)a-Z-(CH2)b-V-(CH2)d-, wherein a, b and d are 0-6, provided that the sum of a, b and d is 0-6; T(CH2)s-, wherein T is cycloalkyl and s is 1-6; naphthylmethyl or optionally substituted heteroarylmethyl; B is optionally substituted phenyl; B' is naphthyl, optionally substituted heteroaryl or optionally substituted phenyl; R is hydrogen, fluoro, alkyl, alkenyl, alkynyl, or B-(CH2)h-, wherein h is 0-3; R4 is optionally substituted phenyl, indanyl, benzofuranyl, tetrahydronaphthyl, pyridyl, pyrazinyl, pyrimidinyl or quinolyl; are disclosed, as well as their use as hypocholesterolemic agents; the method of using compounds of the formula II wherein R20 is optionally substituted phenyl, optionally substituted naphthyl, optionally substituted heteroaryl, or optionally substituted benzofused heteroaryl, R21, R22 and R23 are independently selected from H or R20; E, F and G are independently a bond; cycloalkylene; alkylene; alkenylene; alkynylene; a substituted alkylene, alkenylene or alkynylene chain ; an interrupted alkylene, alkenylene or alkynylene chain ; or an interrupted alkylene, alkenylene or alkynylene chain substituted by one or more substituents; or one of R21-E and R22-F is selected from the group consisting of halogeno, OH, alkoxy, -OC(O)R5, -NR10R11, -SH or -S(alkyl); R5 is alkyl, phenyl, R14-phenyl, benzyl or R14-benzyl; R10 and R11 are independently selected from H and lower alkyl, or a pharmaceutically acceptable salt thereof, in a pharmaceutically aceptable carrier as hypocholesterolemic agents is also disclosed.

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