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公开(公告)号:PE20091095A1
公开(公告)日:2009-07-25
申请号:PE2008002022
申请日:2008-12-05
Applicant: SCHERING CORP
Inventor: BARA THOMAS , BURNETT DUANE , CLADER JHON , JOSIEN HUBERT , PISSARNITSKI DMITRI , ZHAO ZHIQIANG , HUANG XIANHAI , PALANI ANANDAN , QIN JUN , ASLANIAN ROBERT G , ZHU ZHAONING , GREENLEE WILLIAM J , ZHU XIAOHONG , MANDAL MIHIRBARAN , DHONDI PAWAN , MCCRACKEN TROY , ZHOU WEI , BENNETT CHAD E
IPC: A61K31/4738 , A61P25/28 , C07D403/10 , C07D471/04 , C07D487/04
Abstract: REFERIDA A UN COMPUESTO DERIVADO DE FORMULA (I) DONDE R1 ES ALQUILO, CICLOALQUILO, ARILO, ENTRE OTROS; R2 ES INDOLINA, PIRROLO[3,2-c]PIRIDINA, PIRROLO[2,3-b]PIRIDINA, ENTRE OTROS; R3 ES -ARIL, -HETEROARIL, CICLOALQUILO, ENTRE OTROS; R4 ES -ARILALCOXI, -ARILALQUILAMINO, ARILO, ENTRE OTROS; L ES ENLACE DIRECTO, -O-, -N(R5)-, ENTRE OTROS; R5 ES H, ALQUILO, ALQUENILO, ENTRE OTROS. SON COMPUESTOS SELECCIONADOS: 1-(4-FLUOROBENCIL)-4-(4-(4-METIL-1H-IMIDAZOL-1-IL)FENIL)INDOLINA, 1-(4-FLUOROBENCIL)-4-(4-(4-METIL-1H-IMIDAZOL-1-IL)FENIL)-1H-PIRROLO[3,2c]PIRIDINA, 1-(4-FLUOROBENCIL)-4-(4-(4-METIL-1H-IMIDAZOL-1-IL)FENIL)-1H-PIRROLO[2,3b]PIRIDINA, ENTRE OTROS. SE REFIERE TAMBIEN A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON MODULADORES DE GAMMA SECRETASA, SIENDO UTILES PARA EL TRATAMIENTO DE ENFERMEDAD DE ALZHEIMER, SINDROME DE DOWN, DEFICIENCIA COGNITIVA SUAVE, ENTRE OTROS
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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
Inventor: BURNETT DUANE , CLADER JOHN , THIRUVENGADAM TIRUVETTIPURAM , TANN CHOU-HONG , LEE JUNNING , MC ALLISTER TIMOTHY , COLON CESAR , BARTON DEREK , BRESLOW RONALD , DUGAR SUNDEEP , VACCARO WAYNE
IPC: 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
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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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
Inventor: WU WEN-LIAN , BARA THOMAS , BURNETT DUANE , CLADER JOHN W , DOMALSKI MARTIN S , JIN YAN , JOSIEN HUBERT B , LI HONGMEI , LIANG XIAN , PISSARNITSKI DMITRI A , SASIKUMAR THAVALAKULAMGAR , WONG JESSE K
IPC: A61K31/35 , A61K31/352 , A61P25/28 , C07D311/78 , C07D407/12 , C07D493/04
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; ...
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公开(公告)号:AU2008333865A2
公开(公告)日:2010-07-29
申请号:AU2008333865
申请日:2008-12-04
Applicant: SCHERING CORP
Inventor: PALANI ANANDAN , DHONDI PAWAN , MANDAL MIHIRBARAN , PISSARNITSKI DMITRI , GREENLEE WILLIAM J , ZHAO ZHIQIANG , CLADER JOHN , ASLANIAN ROBERT G , BENNETT CHAD E , MCCRACKEN TROY , HUANG XIANHAI , BURNETT DUANE , ZHU ZHAONING , ZHU XIAOHONG , BARA THOMAS , QIN JUN , ZHOU WEI , JOSIEN HUBERT
IPC: C07D403/10 , A61K31/4738 , A61P25/28 , C07D471/04 , C07D487/04 , C07D498/04 , C07D513/04
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公开(公告)号:AT432702T
公开(公告)日:2009-06-15
申请号:AT04789487
申请日:2004-09-30
Applicant: SCHERING CORP
Inventor: SASIKUMAR THAVALAKULAMGARA , BURNETT DUANE
IPC: A61K31/4184 , A61P3/04 , C07D235/30 , C07D401/12 , C07D403/12
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公开(公告)号:AT396996T
公开(公告)日:2008-06-15
申请号:AT03791865
申请日:2003-08-27
Applicant: SCHERING CORP
Inventor: WU WEN-LIAN , BURNETT DUANE , GREENLEE WILLIAM , SASIKUMAR THAVALAKULAM
IPC: C07D487/04 , A61K31/55 , A61P25/00 , C07D513/04
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公开(公告)号:AT393766T
公开(公告)日:2008-05-15
申请号:AT04715072
申请日:2004-02-26
Applicant: SCHERING CORP
Inventor: SASIKUMAR THAVALAKULAMGARA , WU WEN-LIAN , BURNETT DUANE , QIANG LI
IPC: C07D401/04 , A61K31/165 , A61K45/06 , C07D401/14 , C07D405/14 , C07D409/14 , C07D417/14
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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
Inventor: BURNETT DUANE , CLADER JOHN , THIRUVENGADAM TIRUVETTIPURAM K , TANN CHOU-HONG , LEE JUNNING , MC ALLISTER TIMOTHY , COLON CESAR , BARTON DEREK H R , BRESLOW RONALD , DUGAR SUNDEEP , VACCARO WAYNE
IPC: A61K31/397 , A61K31/40 , A61K31/415 , A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/395 , 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
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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公开(公告)号:AU2008333865A1
公开(公告)日:2009-06-11
申请号:AU2008333865
申请日:2008-12-04
Applicant: SCHERING CORP
Inventor: PALANI ANANDAN , DHONDI PAWAN , MANDAL MIHIRBARAN , PISSARNITSKI DMITRI , GREENLEE WILLIAM J , ZHAO ZHIQIANG , CLADER JOHN , ASLANIAN ROBERT G , BENNETT CHAD E , MCCRACKEN TROY , HUANG XIANHAI , BURNETT DUANE , ZHU ZHAONING , ZHU XIAOHONG , BARA THOMAS , QIN JUN , ZHOU WEI , JOSIEN HUBERT
IPC: C07D403/10 , A61K31/4738 , A61P25/28 , C07D471/04 , C07D487/04 , C07D498/04 , C07D513/04
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公开(公告)号:CL2008002084A1
公开(公告)日:2009-01-23
申请号:CL2008002084
申请日:2008-07-15
Applicant: SCHERING CORP
Inventor: XU RUO , WU WEN-LIAN , LI HONGMEI , SASIKUMAR THAVALAKULAMGARA K , BURNETT DUANE , ASBEROM THEODROS , JOSIEN HUBERT B
IPC: A61K31/352 , A61K31/519 , A61K31/542 , A61P25/28 , C07D211/00 , C07D279/00 , C07D307/00 , C07D309/00 , C07D491/052 , C07D493/04 , C07D513/04 , C07D513/14
Abstract: Compuestos derivados de bencensulfonil cromano, tiocromano, tetrahidronaftaleno, inhibidores de la gamma secretasa; composición farmacéutica; y su uso para tratar enfermedades neurodegenerativas.
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