2.
    发明专利
    未知

    公开(公告)号:DE69222532D1

    公开(公告)日:1997-11-06

    申请号:DE69222532

    申请日:1992-07-21

    Applicant: SCHERING CORP

    Abstract: 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.

    INHIBIDORES TETRAHIDROPIRANOCROMENO DE GAMMA SECRETASA

    公开(公告)号:CO6270309A2

    公开(公告)日:2011-04-20

    申请号:CO09149364

    申请日:2009-12-30

    Applicant: SCHERING CORP

    Abstract: 1.- Un compuesto de la formula:o una de sus sales, solvatos o ésteres aceptables para uso farmacéutico, en donde: X se selecciona del grupo que consiste en N y CH2; R1 se selecciona del grupo que consiste en: (1) -alquilen-S(O)2-alquilo(C1-C6), (2) -alquilen-S(O)2-haloalquilo(C1-C6); (3) -alquilen-S(O)2-R6, (4) -alquilen-S(O)2-R8, (5) -alquilen-S(O)2-alquilo(C1-C6) sustituido, (6) -alquilen-(1,1-dioxido de tetrahidrotiofeno), (7) -alquenil-S(O)2-alquilo(C1-C6), y (8) -cicloalquil-S(O)2-alquilo(C1-C6); en donde dicho grupo R1 -alquilen-S(O)2-alquilo(C1-C6) sustituido esta sustituido con uno o mas sustituyentes seleccionados de modo independiente del grupo que consiste en: -OH, halo, -CN, -CF3, -O-alquilo(C1-C6), y -O- (haloalquilo(C1-C6)); R2 se selecciona del grupo que consiste en: H y alquilo; R6 se selecciona del grupo que consiste e. (1) arilo (C6-C14) no sustituido, (2) arilo (C6-C14) sustituido con uno o mas grupos L1A, (3) heteroarilo (C5-C14) no sustituido, (4) heteroarilo (C5-C14) sustituido con uno o mas grupos L1A, (5) heteroarilalquilo(C5-C14) no sustituido, y (5) heteroarilalquilo (C5-C14) sustituido con uno o mas grupos L1A;R8 se selecciona del grupo que consiste en cicloalquilo no sustituido y cicloalquilo sustituido con uno o mas grupos L3 (en donde los ejemplos de dichos grupos cicloalquilo (no sustituido o sustituido) incluyen anillos cicloalquilo C3-C10);cada L3 se selecciona de modo independiente del grupo que consiste en: (1) -CN, (2) =O, (3) -CH2OH, (4) amino, (5) halo, (6) -CH2NH2, (7) -CH2NHalquiIo, (8) -C(O)OH, (9) -alquilen-C(O)NH alquilo (C1 a C6), (10) -alquilen-C(O)N(alquilo (C1 a C6))2 en donde cada alquilo se selecciona de modo independiente, (11) -alquilen-C(O)NH haloalquilo (C1 a C6), y (12) -alquilen-C(O)N(haloalquilo (C1 a C6))2 en donde cada alquilo se selecciona de modo independiente); Ar se selecciona del grupo que consiste en: (1) arilo no sustituido, (2) arilo sustituido con uno o mas grupos L1A, (3) heteroarilo no sustituido, y (4) heteroarilo sustituido con uno o mas grupos L1A; ...

    SUBSTITUTED BETA-LACTAM COMPOUNDS USEFUL AS HYPOCHOLESTEROLEMIC AGENTS AND PROCESSES OF THEIR PREPARATION

    公开(公告)号:SK7994A3

    公开(公告)日:1994-07-06

    申请号:SK7994

    申请日:1992-07-21

    Applicant: SCHERING CORP

    Abstract: 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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