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公开(公告)号：EP0912515A1
公开(公告)日：1999-05-06
申请号：EP97932321.0
申请日：1997-07-08
申请人： SCHERING CORPORATION
CPC分类号： C07D405/12 , A61K45/06 , C07D211/58
摘要： 1,4-Di-substituted piperidine muscarinic antagonists of formula (I) or a pharmaceutically acceptable salt, ester, or solvate thereof, wherein X is a bond, -O-, -S-, -SO-, -SO2-, -CO-, -C(OR7)2-, -CH2-O-, -O-CH2-, -CH=CH-, -CH2-, -CH(C1-C6 alkyl)-, -C(C1-C6 alkyl)2-, -CONR?17-, -NR17¿CO-, -SO¿2NR?17- or -NR17SO2-; R is C3-C6 cycloalkyl, (a), (b), (c), (d), (e), optionally substituted phenyl or optionally substituted pyridyl; R1 is H, -CN, -CF¿3?, alkyl, cycloalkyl, cycloalkenyl, alkenyl, -COR?15¿, -COO(alkyl, aryl, heteroaryl, alkylaryl or alkylheteroaryl), alkylaryl, alkylheteroaryl or -CON(R13)2; R2 is cycloalkyl, cycloalkenyl, t-butoxycarbonyl or optionally substituted 4-piperidinyl; R?3 and R4¿ are H, halo, -CF¿3?, alkyl, alkoxy or -OH; R?5 and R6¿ are H, alkyl, -CF¿3?, alkoxy, -OH, alkylcarbonyl, alkoxycarbonyl, R?13¿CONH-, R14OCONH-, R13NHCONH- or NH¿2?CONR?13-; R7¿ is H or alkyl, or the two R7 groups may form -(CH¿2?)2-4; R?13¿ is H, alkyl, cycloalkyl, -(alkyl)COOR15, aryl, heteroaryl, alkylaryl, alkylheteroaryl and adamantyl; R14 is H or alkyl; R15 is H, C¿1?-C20 alkyl, C1-C6 cycloalkyl, aryl or heteroaryl; and R?17¿ is H, C¿1?-C6 alkyl, aryl or heteroaryl; useful for treating cognitive disorders such as Alzheimer's disease are disclosed, as well as pharmaceutical compositions and methods of preparation. Also disclosed are combinations of compounds of formula (I) capable of enhancing ACh release with ACh'ase inhibitors.
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公开(公告)号：EP1492765B1
公开(公告)日：2011-07-06
申请号：EP02759233.6
申请日：2002-08-01
申请人： Schering Corporation
IPC分类号： C07D201/00
CPC分类号： C07D231/12 , C07D215/58 , C07D233/56 , C07D249/08 , C07D401/12 , C07D405/12 , C07D409/12 , C07D471/04 , C07D487/04
摘要： This invention discloses novel gamma secretase inhibitors of the formula:(Chemical formula should be inserted here as it appears on abstract in paper form)wherein: R1 is a substituted aryl or substituted heteroaryl group; R2 is an R1 group, alkyl, -X(CO)Y, -(CR32)1-4X(CO)Y; each R3A is independently H or alkyl; X is -O-, -NH, or -N-alkyl; and Y is -NR6R7, or -N(R3)(CH2)2-6NR6R7. Also disclosed is a method of treating Alzheimer s Disease.
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公开(公告)号：EP2217604A1
公开(公告)日：2010-08-18
申请号：EP08848226.0
申请日：2008-11-03
申请人： Schering Corporation
IPC分类号： C07D487/10 , C07D487/20 , C07D493/20 , C07D495/20 , C07D498/10 , C07D498/20 , C07D498/22 , C07F7/08 , C07F9/6571
CPC分类号： C07D498/10 , C07D487/10 , C07D487/20 , C07D493/20 , C07D495/20 , C07D498/20 , C07D498/22 , C07F7/0812 , C07F9/657181
摘要： This invention provides novel compounds that are modulators of gamma secretase. The compounds have the formula (I). Also disclosed are methods of modulating gamma secretase activity and methods of treating Alzheimer's Disease using the compounds of formula (I).
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公开(公告)号：EP1442042A1
公开(公告)日：2004-08-04
申请号：EP02786685.4
申请日：2002-11-07
申请人： SCHERING CORPORATION
发明人： ASBEROM, Theodros , CLADER, John, W. , HU, Yueqing , PISSARNITSKI, Dmitri, A. , STAMFORD, Andrew, W. , XU, Ruo
IPC分类号： C07D487/14 , C07D487/20 , A61K31/527 , A61K31/551 , A61P9/00 , A61P13/00 , A61P15/00
CPC分类号： C07D487/14
摘要： A compound having the formula (Ia) or (b), salt or solvate thereof, with the variables as defined herein, which can inhibit selectively phosphodiesterase V and can be useful for treating sexual dysfunction and other physiological disorders, symptoms and diseases
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公开(公告)号：EP1421084A1
公开(公告)日：2004-05-26
申请号：EP02761506.1
申请日：2002-08-26
申请人： Schering Corporation
发明人： ASBEROM, Theodros , HU, Yueqing,5F Tower D,Hong Kong Univ. of , PISSARNITSKI, Dmitri, A. , XU, Ruo , WANG, Yuguang , CHACKALAMANNIL, Samuel , CLADER, John, W. , STAMFORD, Andrew, W.
IPC分类号： C07D487/14 , A61K31/519 , A61P15/10
CPC分类号： C07D487/14
摘要： A polycyclic guanine phosphodiesterase V inhibitor having the formula (I.1) or (II.1), with the variables defined herein, which is useful for treating sexual dysfunction and other physiological disorders (I), (II), A representative example is: (III)
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公开(公告)号：EP1036072A1
公开(公告)日：2000-09-20
申请号：EP98958039.4
申请日：1998-11-23
申请人： SCHERING CORPORATION
发明人： CHACKALAMANNIL, Samuel , ASBEROM, Theodros , XIA, Yan , DOLLER, Dario , CLASBY, Martin, C. , CZARNIECKI, Michael, F.
IPC分类号： C07D405/06 , C07D405/14 , C07D409/14 , C07D405/12 , C07D417/06 , C07D401/06 , C07D491/04 , C07D471/04 , C07D493/10 , A61K31/44 , A61K31/47
CPC分类号： C07D401/06 , C07D405/06 , C07D405/12 , C07D405/14 , C07D409/14 , C07D417/06 , C07D471/04 , C07D491/04 , C07D493/10
摘要： Heterocyclic-substituted tricyclics of formula (I) or a pharmaceutically acceptable salt thereof, wherein: the single dotted line represents an optional double bond; the double dotted line represents an optional single bond; n is 0-2; Q is optionally substituted cycloalkyl, heterocycloalkyl, aryl or heteroaryl; Het is an optionally substituted mono-, bi- or tricyclic heteroaromatic group; B is -(CH2)n3-, wherein n3 is 0-5, -CH2-O-, -CH2S-, -CH2-NR6-, -C(O)NR?6-. -NR6¿C(O)-, (a), optionally substituted alkenyl or optionally substituted alkynyl; X is -O- or -NR6- when the double dotted line represents a single bond, or X is -OH or -NHR20 when the bond is absent; Y is =O, =S, (H, H), (H, OH) or (H, C¿1?-C6 alkoxy) when the double dotted line represents a single bond, or when the bond is absent, Y is =O, (H, H), (H, OH), (H, SH) or (H, C1-C6 alkoxy); R?15¿ is absent when the double dotted line represents a single bond and is H, -NR18R19, or -OR17 when the bond is absent; or Y is (A) or (B) and R15 is H or C¿1?-C6 alkyl; are disclosed, as well as pharmaceutical compositions containing them and a method of treating diseases associated with thrombosis, atherosclerosis, restenosis, hypertension, angina pectoris, arrhythmia, heart failure, and cancer by administering said compounds.
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