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51. 发明专利

CA2114007A1 SUBSTITUTED BETA-LACTAM COMPOUNDS USEFUL AS HYPOCHOLESTEROLEMIC AGENTS AND PROCESSES FOR THE PREPARATION THEREOF 未知
公开(公告)号：CA2114007A1
公开(公告)日：1993-02-04
申请号：CA2114007
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 , MCALLISTER TIMOTHY , COLON CESAR , BARTON DEREK H R , BRESLOW RONALD , DUGAR SUNDEEP , VACCARO WAYNE
IPC分类号： A61K31/397 , A61K31/4427 , A61K31/496 , A61K31/5377 , A61P3/06 , C07D205/08 , C07D401/04 , C07D403/04 , C07D405/10 , C07D409/04 , C07D413/10 , C07D417/04 , C07F7/10
摘要： 2114007 9302048 PCTABS00019 Novel compounds of formula (I) wherein A is -CH=CH-B; -C=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 (Ia), 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 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 acceptable carrier as hypocholesterolemic agents is also disclosed.

52. 发明专利

ZA201000191B BENZENESULFONYL-CHROMANE,THIOCHROMANE,TETRAHYDRONAPHTHALENE AND RELATED GAMMA SECRETASE INHIBITORS 未知
公开(公告)号：ZA201000191B
公开(公告)日：2011-06-29
申请号：ZA201000191
申请日：2010-01-11
申请人： SCHERING CORP
发明人： SASIKUMAR THAVALAKULAMGARA K , XU RUO , BURNETT DUANE A , WU WEN-LIAN , ASBEROM THEODROS , LI HONGMEI , JOSIEN HUBERT B
摘要： Disclosed are novel gamma secretase inhibitors of the formula (I): or a pharmaceutically acceptable salt, solvate, or ester thereof, wherein L1, n, X, Ar, Y, Z, Q, and Q1 are as defined herein. Also disclosed are methods for inhibiting gamma secretase, methods for treating Alzheimer's disease, methods of treating one or more neurodegenerative diseases, and methods of inhibiting the deposition of amyloid protein (e.g., amyloid beta protein) in, on or around neurological tissue (e.g., the brain) using the compounds of formula 1.0.

53. 发明专利

DE602005022191D1 TRICYCLISCHE VERBINDUNGEN UND DEREN VERWENDUNG ALS MGLUR1-ANTAGONISTEN 未知
公开(公告)号：DE602005022191D1
公开(公告)日：2010-08-19
申请号：DE602005022191
申请日：2005-06-14
申请人： SCHERING CORP
发明人： MATASI JULIUS J , TULSHIAN DEEN , BURNETT DUANE A , WU WEN-LIAN , KORAKAS PETER , SILVERMAN LISA S , SASIKUMAR THAVALAKULAMGARA K , QIANG LI , DOMALSKI MARTIN S
IPC分类号： C07D495/14 , A61K31/519 , A61P25/00 , C07D471/14 , C07D491/14 , C07D495/04

54. 发明专利

MX2010001506A MODULADORES DE GAMMA SECRETASA. 未知
公开(公告)号：MX2010001506A
公开(公告)日：2010-03-10
申请号：MX2010001506
申请日：2008-08-04
申请人： SCHERING CORP
发明人： GREENLEE WILLIAM J , BURNETT DUANE A , MCKITTRICK BRIAN , ZHU ZHAONING , MAZZOLA ROBERT D , BENNETT CHAD E , CALDWELL JOHN P , HAUNG XIANHAI , JOSIEN HUBERT B
IPC分类号： C07D487/04 , C07D217/24 , C07D498/04
摘要： En sus muchas modalidades, la presente invención provee una nueva clase de compuestos heterocíclicos como moduladores de gamma secretasa, métodos para preparar dichos compuestos, composiciones farmacéuticas que contienen uno o más de dichos compuestos, métodos para preparar formulaciones farmacéuticas que comprenden uno o más de dichos compuestos, y métodos de tratamiento, prevención, inhibición o mejora de una o más enfermedades asociadas con el sistema nervioso central utilizando dichos compuestos o composiciones farmacéuticas.

55. 发明专利

PE20090712A1 MODULADORES DE LA GAMMA SECRETASA 未知
公开(公告)号：PE20090712A1
公开(公告)日：2009-06-20
申请号：PE2008001683
申请日：2008-09-26
申请人： SCHERING CORP
发明人： ZHU ZHAONING , MCKITTRICK BRIAN A , GREENLEE WILLIAM J , MAZZOLA ROBERT D JR , CALDWELL JOHN P , BENNETT CHAD E , BURNETT DUANE A
IPC分类号： A61K31/4178 , A61P25/28 , C07D233/76 , C07D233/86 , C07D233/88 , C07D403/04
摘要： REFERIDA A UN COMPUESTO DE FORMULA (I), DONDE B ES H, ALCOXI, ALQUILO, =O, =S, ENTRE OTROS; W ES -C(O)-, -S(O)2-; X DE PREDERENCIA N; R1, R8, R9 Y R10 SON CADA UNO H, ALQUILO, ARILALQUIL-, CICLOALQUILALQUIL-, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: (R)-3-(1-(4-FLOROFENIL)ETIL)-5-(3-METOXI-4-(4-METIL-1H-IMIDAZOL-1-IL)BENZILIDINA)-2-TIOXOIMIDAZOLIDIN-4-ONA; (R)-3-(1-(4-FLUOROFENIL)ETIL)-3-IMINO-5-(3-METOXI-4-(4-METIL-1H-IMIDAZOL-1-IL)BENZILIDINA)-2-IMIDAZOLIDIN-4-ONA; ENTRE OTROS. SE REFIERE TAMBIEN UN PROCEDIMIENTO DE PREPARACION, A UNA COMPOSICION FARMACEUTICA Y A UN METODO DE TRATAMIENTO. DICHOS COMPUESTOS SON MODULADORES DE GAMMA SECRETASA, UTILES EN EL TRATAMIENTO DE ENFERMEDAD DE ALZHEIMER, DETERIORO COGNITIVO LEVE, SINDROME DE DOWN, ENTRE OTROS

56. 发明专利

PE04352009A1 INHIBIDORES DE TETRAHIDROPIRANOCROMENO DE GAMMA SECRETASA 未知
公开(公告)号：PE04352009A1
公开(公告)日：2009-04-18
申请号：PE0011212008
申请日：2008-07-02
申请人： SCHERING CORP
发明人： BARA THOMAS A , BURNETT DUANE A , CLADER JOHN W , DOMALSKI MARTIN S , JIN YAN , JOSIEN HUBERT B , LI HONGMEI , LIANG XIAN , PISSARNITSKI DMITRI , SASIKUMAR TRAVALAKULAMGARA K , WONG JESSE K , XU RUO , ZHAO ZHIQIANG , MCNAMARA PAUL E , WU WEN-LIAN
IPC分类号： A61K31/35 , A61K31/352 , A61P25/28 , C07D311/78 , C07D407/12 , C07D493/04
CPC分类号： C07D493/04 , C07D311/78 , C07D407/12
摘要： REFERIDA A UN COMPUESTO DE FORMULA (I), DONDE X ES N, CH2; R1 ES -ALQUILEN-SO2-ALQUILO(C1-C6), -ALQUILEN-SO2-HALOALQUILO(C1-C6), ALQUILEN-(1,1-DIOXIDO DE TETRAHIDROTIOFENO), ENTRE OTROS; R2 ES H, ALQUILO; Ar ES ARILO, HETEROARILO, ARILO SUSTITUIDO CON UNO O MAS L1A, ENTRE OTROS; L1A ES HALOGENO, ALQUILO, -CN, CF3, -O-(HALOALQUILO(C1-C6)), ENTRE OTROS; L1 ES HALOGENO, -CN, -CF3, -O-ALQUILO(C1-C6), -C(O)-O-ALQUILO(C1-C6), ALQUILEN-OH, ENTRE OTROS; n ES 0-3. SON COMPUESTOS PREFERIDOS: (a), (b), ENTRES OTROS. SE REFIERE TAMBIEN UN PROCEDIMIENTO DE PREPARACION Y A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INHIBIDRORES DE GAMMA-SECRETASA, UTILES EN EL TRATAMIENTO DE ENFERMEDADES NEURODEGENERATIVAS, ENFERMEDAD DE ALZHEIMER E INHIBIENDO EL DEPOSITO DE PROTEINA AMIELOIDE EN, SOBRE O ALREDEDOR DEL TEJIDO NEUROLOGICO

57. 发明专利

MX2008004024A ANTAGONISTAS DE RECEPTOR DE GLUTAMATO METABOTROPICO-1 TETRACICLICOS FUSIONADOS COMO AGENTES TERAPEUTICOS. 未知
公开(公告)号：MX2008004024A
公开(公告)日：2009-02-27
申请号：MX2008004024
申请日：2006-09-21
申请人： SCHERING CORP
发明人： BURNETT DUANE A , WU WEN-LIAN
IPC分类号： A61K31/538 , C07D491/02 , C07D498/02
摘要： En sus muchas modalidades, la presente invención provee compuestos tetracíclicos de la fórmula I o la fórmula II (ver fórmula (I) y fórmula (II)) (en donde las diversas porciones son como se define aquí) útiles como antagonistas de receptor de glutamato metabotrópico (mGluR), particularmente como antagonistas de receptor de glutamato metabotrópico 1 selectivos, composiciones farmacéuticas que contienen los compuestos, y métodos de tratamiento que usan los compuestos y composiciones para tratar enfermedades asociadas con receptor de glutamato metabotrópico (v.gr., mGluR1) tales como, por ejemplo, dolor, migraña, ansiedad, incontinencia urinaria y enfermedades neurodegenerativas tales como enfermedad de Alzheimer.

58. 发明专利

DE602004018617D1 未知
公开(公告)号：DE602004018617D1
公开(公告)日：2009-02-05
申请号：DE602004018617
申请日：2004-03-03
申请人： SCHERING CORP
发明人： BURNETT DUANE A , CLADER JOHN W
IPC分类号： C07D405/12 , A61K31/397 , A61P3/06 , C07D405/14
摘要： The present invention provides compounds represented by the structural formula (I): or pharmaceutically acceptable isomers, salts, solvates or esters of the compound of Formula (I), wherein each of the substituents is as specified herein, formulations including the above compounds, processes for preparing the same and methods for treating atherosclerosis, hypercholesterolemia, or sitosterolemia, and for lowering plasma levels of sterols and/or stanols.

59. 发明专利

CA2693216A1 BENZENESULFONYL-CHROMANE, THIOCHROMANE, TETRAHYDRONAPHTHALENE AND RELATED GAMMA SECRETASE INHIBITORS 未知
公开(公告)号：CA2693216A1
公开(公告)日：2009-01-22
申请号：CA2693216
申请日：2008-07-15
申请人： SCHERING CORP
发明人： SASIKUMAR THAVALAKULAMGARA K , BURNETT DUANE A , ASBEROM THEODROS , WU WEN-LIAN , LI HONGMEI , XU RUO , JOSIEN HUBERT B
IPC分类号： C07D491/04 , A61K31/35 , A61K31/519 , A61K31/54 , A61K31/542 , C07D493/04 , C07D513/04 , C07D513/14
摘要： Disclosed are novel gamma secretase inhibitors of the formula (I): or a pharmaceutically acceptable salt, solvate, or ester thereof, wherein L1' n, X, Ar, Y, Z, Q, and Q1 are as defined herein. Also disclosed are methods for inhibiting gamma secretase, methods for treating Azheimer's disease, methods of treating one or more neurodegenerative diseases, and methods of inhibiting the deposition of amyloid protein (e.g., amyloid beta protein) in, on or around neurological tissue (e.g., the brain) using the compounds of formula 1Ø

60. 发明专利

AU2008276492A1 Benzenesulfonyl-chromane, thiochromane, tetrahydronaphthalene and related gamma secretase inhibitors 未知
公开(公告)号：AU2008276492A1
公开(公告)日：2009-01-22
申请号：AU2008276492
申请日：2008-07-15
申请人： SCHERING CORP
发明人： XU RUO , ASBEROM THEODROS , LI HONGMEI , WU WEN-LIAN , JOSIEN HUBERT B , BURNETT DUANE A , SASIKUMAR THAVALAKULAMGARA K
IPC分类号： C07D491/04 , A61K31/35 , A61K31/519 , A61K31/54 , A61K31/542 , C07D493/04 , C07D513/04 , C07D513/14
摘要： Disclosed are novel gamma secretase inhibitors of the formula (I): or a pharmaceutically acceptable salt, solvate, or ester thereof, wherein L1, n, X, Ar, Y, Z, Q, and Q1 are as defined herein. Also disclosed are methods for inhibiting gamma secretase, methods for treating Alzheimer's disease, methods of treating one or more neurodegenerative diseases, and methods of inhibiting the deposition of amyloid protein (e.g., amyloid beta protein) in, on or around neurological tissue (e.g., the brain) using the compounds of formula 1.0.

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