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81. 发明专利

ES2168396T3 未知
公开(公告)号：ES2168396T3
公开(公告)日：2002-06-16
申请号：ES95943048
申请日：1995-12-18
申请人： SCHERING CORP
发明人： VACCARO WAYNE D , BURNETT DUANE A , CLADER JOHN W
IPC分类号： A61K31/397 , A61K31/41 , A61K31/4427 , A61K31/445 , A61K31/495 , A61K31/535 , A61K31/54 , A61P3/06 , A61P9/10 , C07D205/08 , C07D205/12 , C07D401/10 , C07D403/12 , C07D413/10 , C07D491/08 , C07D491/10 , C07D491/113 , C07D521/00 , C07D403/10 , A61K31/395
摘要： 4-[(Heterocycloalkyl or heteroaromatic)-substituted phenyl]-2-azetidinone hypocholesterolemic agents of the formula I or a pharmaceutically acceptable salt thereof, wherein: A is optionally substituted heterocycloalkyl, heteroaryl, benzofused heterocycloalkyl, or benzofused heteroaryl; Ar1 and Ar2 are optionally substituted aryl; Q is a bond or, with the 3-position ring carbon of the azetidinone, forms a spiro group; and R1 is alkylene; alkylene wherein a carbon in the chain is replaced by -O-, -C(O)-, phenylene, -NR8-, -S(O)0-2- or cycloalkylene; or alkenylene; or, when Q is a bond, R1 can be alkylene substituted by one or two hydroxy groups or hydroxy derivatives, wherein the alkylene chain can optionally be joined to Ar1 through -O- or -S(O)0-2- or joined to the azetidinone ring through a -S(O)0-2- group; a method of lowering serum cholesterol by administering said compounds, pharmaceutical compositions containing them, and the combination of a substituted azetidinone and a cholesterol biosynthesis inhibitor for the treatment and prevention of atherosclerosis.

82. 发明专利

PL182617B1 HYDROXYL DERIVATIVES OF COMPOUNDS OF AZETIDINONE TYPE USEFUL AS HYPOCHOLESTEROLAEMIC AGENTS 未知
公开(公告)号：PL182617B1
公开(公告)日：2002-02-28
申请号：PL31358994
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： 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.

83. 发明专利

CZ289033B6 Sulfur derivatives of azetidinone compounds, pharmaceutical preparation in which they are comprised and process of its preparation as well as a kit thereof 未知
公开(公告)号：CZ289033B6
公开(公告)日：2001-10-17
申请号：CZ148697
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： Disclosed are azetidinone compound sulfur derivatives of the general formula I that are useful when treating or preventing aterosclerosis, because they reduce content of cholesterol in blood plasma. In pharmaceutical preparations, they are used either as such or in a mixture with inhibitors of cholesterol biosynthesis.

84. 发明专利

UA41948C2 ЗАМІЩЕНІ ГІДРОКСИЛОМ АЗЕТИДИНОНИ, ПРИДАТНІ ЯК ГІПОХОЛЕСТЕРИНЕМІЧНИЙ ЗАСІБ, ФАРМАЦЕВТИЧНА КОМПОЗИЦІЯ НА ЇХ ОСНОВІ ТА СПОСІБ ЛІКУВАННЯ АБО ПРОФІЛАКТИКИ 未知
公开(公告)号：UA41948C2
公开(公告)日：2001-10-15
申请号：UA96031081
申请日：1994-09-14
申请人： SCHERING CORP
发明人： ROSENBLUM STUART B , DUGAR SUNDEEP , BURNETT DUANE A , KLADER JOHN V , MACHITRICK 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： Винахідналежитьдозаміщенихгідроксиломазетидинонам, придатнимякгіпохолестеринемічнийзасібв галузілікуванняі профілактикиатеросклерозу. Новігіпохолестеринемичнісполукиданоговинаходумаютьформулу (I) (I) абоє фармацевтичноприйнятноюсіллюсполукиформули (I) деАr1 іАr2 незалежноодинвідодноговибраніз групи, щовключаєарилі заміщенийзалишком R4 арилАr3, - арилабозаміщенийзалишком R5 арил, X, Y і Z незалежноодинвідодноговибраніз групи, щовключає -СН2-, -СН(нижчийалкіл) -, -С(ді-нижчийалкіл)-,R і R2 незалежноодинвідодноговибраніз групи, щовключає --OR6, -O(CO)R6, -O(CO)OR9 і -O(CO)NR6R7,R1 і R3 незалежноодинвідодноговибраніз групи, щовключаєводень, нижчийалкілі арил, q, - 0 або 1,r - 0 або 1, m,n і p незалежноодинвідодногоозначаютьчисло 0 ¸ 4, прицьомущонайменшеодинз індексів q і r означаєчисло 1, ісумаіндексів m, n, p, q і r дорівнює 1, 2,3,4,5 або 6, іякщо p - 0, і r - 1, тосума m, q і n дорівнює 1,2,3,4 або 5

85. 发明专利

GR3030312T3 HYDROXY-SUBSTITUTED AZETIDINONE COMPOUNDS USEFUL AS HYPOCHOLESTEROLEMIC AGENTS 未知
公开(公告)号：GR3030312T3
公开(公告)日：1999-09-30
申请号：GR990401399
申请日：1999-05-27
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.

86. 发明专利

ES2132432T3 未知
公开(公告)号：ES2132432T3
公开(公告)日：1999-08-16
申请号：ES94928563
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： 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.

87. 发明专利

CZ9701486A3 SULFUR DERIVATIVES OF AZETIDINONE COMPOUNDS USEFUL AS HYPOCHOLESTEROLEMIC AGENTS 未知
公开(公告)号：CZ9701486A3
公开(公告)日：1997-11-12
申请号：CZ148697
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
CPC分类号： C07D401/12 , C07D205/08 , C07D409/12

88. 发明专利

MX9704482A 4-(FENILO SUSTITUIDO CON (HETEROCICLOALQUILO O HETEROAROMATICO))-2-AZETIDINONAS COMO AGENTES HIPOLIPIDEMICOS. 未知
公开(公告)号：MX9704482A
公开(公告)日：1997-10-31
申请号：MX9704482
申请日：1995-12-18
申请人： SCHERING CORP
发明人： VACCARO WAYNE D , BURNETT DUANE A , CLADER JOHN A
IPC分类号： A61K31/397 , A61K31/41 , A61K31/4427 , A61K31/445 , A61K31/495 , A61K31/535 , A61K31/54 , A61P3/06 , A61P9/10 , C07D205/08 , C07D205/12 , C07D401/10 , C07D403/12 , C07D413/10 , C07D491/08 , C07D491/10 , C07D491/113 , C07D521/00 , C07D403/10 , A61K31/395
摘要： ??La presente invencion se refiere a los agentes hipocolesterolémicos 4-[fenilo sustituido con (heterocicloalquilo o heteroaromático)]-2-azetidinonas de la formula (I) o una sal farmacéuticamente aceptable de estos, en donde: A es heterocicloalquilo opcionalmente sustituido, heteroarilo opcionalmente sustituido, heterocicloalquilo benzofusionado opcionalmente sustituido o heteroarilo benzofusionado opcionalmente sustituido; Ar1 es arilo opcionalmente sustituido; Ar2 es arilo opcionalmente sustituido; Q es un enlace, o con el carbono del anillo de azetidinona en la posicion 3 forma el grupo espiro (a); y R1 se selecciona del grupo que consiste en -(CH)q-, en donde que es 2-6, siempre y cuando Q sea un anillo espiro, q también puede ser 0 o 1; -(CH2)e-G(CH2)r-, en donde G es -O-, -C(O)-, fenilo, -NR8- o -S(O)o-2-, e es 0-5 y r es 0-5, siempre que la suma e y r sea 1-6; alquenileno, y -(CH2)f- V-(CH2)g-, en donde V es cicloalquileno, f es 1-5 g es 02, siempre y cuando la suma de f y g sea 1-6; R5 es (b), (c), (d), (e), (f), (g) o (h), R6 y r7 y R7 son -CH2-, -CH (alquilo)= CH-; o R5 junto con R6 adyacente, o R5 junto con R7 adyacente, forman un grupo -CH=CH- o -C (alquilo); a y b son independientemente 0-3, siempre y cuando no sean 0; y cuando Q es enlace, R1 también puede ser (i), (j) o (k); M es -O-; -S-, -S(O)2-; X, Y y Z -CH2-, -CH(alquilo)- o C(dialquilo); R10 y R12 -OR14, -O(CO) R14, -O(CO)OR16 o O(CO)NR14R15; R11 y R13 son H, alquilo o arilo, o R10 y R11 juntos son =O, o R12 y R13 juntos son =O; d es 1-3; es 0-4; s es 0 o 1; t es 0 o 1; m, n y p son independientemente 0-4; siempre y cuando por lo menos uno de los dos, s y t sea 1, y la suma de m, n, p, s y t sea 1-6, siempre y cuando p sea O y t sea 1, la suma de m,s y n es 1-5; y siempre que p sea 0 y s sea 1, la suma de m t y n es 1-5; v es 0 o 1; j y k son independientemente 1-5, siempre que la suma de j, k y v sea 1-5, R8 es H, alquilo, arilalquilo, -C(O)R14 o -COOR14, R9 es H, alquilo, alcoxi, -COOH, NO2, -NR14R15, OH o halogeno; R14 y R15 son H, alquilo, arilo y arilalquilo; R16 es alquilo o arilo opcionalmente sustituido; y R19 es H, OH o alcoxi, así como un método para reducir el colesterol en suero administrando estos compuestos, las composiciones farmacéuticas que los contiene, y la combinacion de una azetidinona sustituida y un inhibidor de la biosíntesis del colesterol para el tratamiento y prevencion de la aterosclerosis.

89. 发明专利

AU681445B2 Hydroxy-substituted azetidinone compounds useful as hypocholesterolemic agents 未知
公开(公告)号：AU681445B2
公开(公告)日：1997-08-28
申请号：AU7795294
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： 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.

90. 发明专利

FI972099A0 未知
公开(公告)号：FI972099A0
公开(公告)日：1997-05-16
申请号：FI972099
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 , C07D
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.

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