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公开(公告)号：AU2002324582B9
公开(公告)日：2006-02-16
申请号：AU2002324582
申请日：2002-08-01
Applicant: SCHERING CORP
Inventor： PISSARNITSKI DMITRI A , ASBEROM THEODROS , GUZIK HENRY S , JOSIEN HUBERT B
IPC: C07D487/04 , A61K31/437 , A61K31/47 , A61K31/4709 , A61K31/496 , A61K31/5377 , A61P9/10 , A61P25/00 , A61P25/28 , A61P43/00 , C07D215/58 , C07D401/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D471/04 , C07D487/08 , C07D521/00
Abstract: This invention discloses novel gamma secretase inhibitors of the formula: 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：PL372212A1
公开(公告)日：2005-07-11
申请号：PL37221202
申请日：2002-08-01
Applicant: SCHERING CORP
Inventor： ASBEROM THEODROS , GUZIK HENRY S , JOSIEN HUBERT B , PISSARNITSKI DMITRI A
IPC: A61K31/437 , A61K31/47 , A61K31/4709 , A61K31/496 , A61K31/5377 , A61P9/10 , A61P25/00 , A61P25/28 , A61P43/00 , C07D215/58 , C07D401/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D471/04 , C07D487/04 , C07D487/08 , C07D521/00
Abstract: This invention discloses novel gamma secretase inhibitors of the formula: 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：CA2538590A1
公开(公告)日：2005-03-31
申请号：CA2538590
申请日：2004-09-15
Applicant: SCHERING CORP , PHARMACOPEIA DRUG DISCOVERY
Inventor： ASBEROM THEODROS , CLADER JOHN W , GUO TAO , SMITH ELIZABETH M , HOBBS DOUGLAS W , JOSIEN HUBERT B , PISSARNITSKI DMITRI A
IPC: C07D211/96 , C07D491/113 , A61K31/44 , A61K31/445 , A61K31/4535 , A61K31/454 , A61K31/4545 , A61K31/4709 , A61K31/4725 , A61K31/496 , A61K31/5377 , A61K31/541 , A61K31/55 , A61K31/551 , A61P25/18 , A61P25/28 , A61P43/00 , C07D207/48 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/14 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/14 , C07D471/10
Abstract: This invention discloses novel gamma secretase inhibitors of the formula: wherein: R1 is a substituted aryl or substituted heteroaryl group; R2 is an R1 group, alkyl, -XC(O)Y, alkylene-XC(O)Y, cycloalkylene-X-C(O)-Y, -CH-X-C(O)-N R3- Y or -CH-X-C(O)-Y, wherein X and Y are as defined herein; each R3 and each R 3A are independently H, or alkyl; R11 is aryl, heteroaryl, alkyl, cycloalkyl, arylalkyl, arylcycloalkyl, heteroarylalkyl, heteroarylcycloalkyl, arylheterocycloalkyl, or alkoxyalkyl. Also disclosed is a method of treating Alzheimer's Disease using one or more compounds of the invention.
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公开(公告)号：NO20040933A
公开(公告)日：2004-03-03
申请号：NO20040933
申请日：2004-03-03
Applicant: SCHERING CORP
Inventor： ASBEROM THEODROS , JOSIEN HUBERT B , GUZIK HENRY S , PISSAMITSKI DMITRI A
IPC: A61K31/437 , A61K31/47 , A61K31/4709 , A61K31/496 , A61K31/5377 , A61P9/10 , A61P25/00 , A61P25/28 , A61P43/00 , C07D215/58 , C07D401/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D471/04 , C07D487/04 , C07D487/08 , C07D521/00 , C07D
CPC classification number: C07D231/12 , C07D215/58 , C07D233/56 , C07D249/08 , C07D401/12 , C07D405/12 , C07D409/12 , C07D471/04 , C07D487/04
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公开(公告)号：AT233260T
公开(公告)日：2003-03-15
申请号：AT97936296
申请日：1997-08-06
Applicant: SCHERING CORP
Inventor： LOWE DEREK B , CHANG WEI K , KOZLOWSKI JOSEPH A , BERGER JOEL G , MCQUADE ROBERT , BARNETT ALLEN , SHERLOCK MARGARET , TOM WING , DUGAR SUNDEEP , CHEN LIAN-YONG , CLADER JOHN W , CHACKALAMANNIL SAMUEL , WANG YUGUANG , MCCOMBIE STUART W , TAGAT JAYARAM R , VICE SUSAN F , VACCARO WAYNE D , GREEN MICHAEL J , BROWNE MARGARET E , BOYLE CRAIG D , JOSIEN HUBERT B , ASBEROM THEODROS
IPC: C07D211/58 , A61K31/00 , A61K31/435 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/445 , A61K31/4465 , A61K31/4523 , A61K31/4545 , A61K31/47 , A61K31/4709 , A61K31/495 , A61K31/496 , A61K31/50 , A61K31/501 , A61K45/00 , A61P25/28 , C07D211/24 , C07D211/32 , C07D211/96 , C07D239/34 , C07D257/04 , C07D295/02 , C07D295/03 , C07D295/084 , C07D295/088 , C07D295/096 , C07D295/112 , C07D295/116 , C07D295/125 , C07D295/13 , C07D295/135 , C07D295/145 , C07D295/15 , C07D401/04 , C07D401/10 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D409/14 , C07D413/14 , C07D405/00
Abstract: Di-N-substituted piperazine or 1,4 di-substituted piperadine compounds in accordance with formula I (including all isomers, salts, esters, and solvates) wherein R, R1, R2, R3, R4, R21, R27, R28, X, Y, and Z are as defined herein are muscarinic antagonists useful for treating cognitive disorders such as Alzheimer's disease. Pharmaceutical compositions and methods of preparation are also disclosed. Also disclosed are synergistic combinations of compounds of the above formula with acetylcholinesterase inhibitors.
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Patent Agency Ranking
公开(公告)号：BR9812793A
公开(公告)日：2000-10-17
申请号：BR9812793
申请日：1998-11-23
Applicant: SCHERING CORP
Inventor： CHACKALAMANNIL SAMUEL , ASBEROM THEODROS , XIA YAN , DOLLER DARIO , CLASBY MARTIN C , CZARNIECKI MICHAEL F
IPC: C07D491/056 , A61K31/4184 , A61K31/423 , A61K31/427 , A61K31/44 , A61K31/443 , A61K31/4433 , A61K31/4545 , A61K31/47 , A61K31/4709 , A61K31/4738 , A61K31/496 , A61K31/497 , A61K31/498 , A61K31/501 , A61K31/506 , A61K31/5377 , A61K31/55 , A61P7/02 , A61P9/00 , A61P9/04 , A61P9/06 , A61P9/10 , A61P9/12 , A61P35/00 , A61P43/00 , C07D401/06 , C07D405/04 , C07D405/06 , C07D405/12 , C07D405/14 , C07D409/14 , C07D413/06 , C07D417/06 , C07D417/14 , C07D471/04 , C07D491/04 , C07D493/04 , C07D493/10
Abstract: 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-NR -, -C(O)NR -. -NR C(O)-, (a), optionally substituted alkenyl or optionally substituted alkynyl; X is -O- or -NR - when the double dotted line represents a single bond, or X is -OH or -NHR when the bond is absent; Y is =O, =S, (H, H), (H, OH) or (H, C1-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 is absent when the double dotted line represents a single bond and is H, -NR R , or -OR when the bond is absent; or Y is (A) or (B) and R is H or C1-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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公开(公告)号：CZ20001856A3
公开(公告)日：2000-10-11
申请号：CZ20001856
申请日：1998-11-23
Applicant: SCHERING CORP
Inventor： CHACKALAMANNIL SAMUEL , ASBEROM THEODROS , YIA YAN , DOLLER DARIO , CLASBY MARTIN C , CZARNIECKI MICHAEL F
IPC: C07D491/056 , A61K31/4184 , A61K31/423 , A61K31/427 , A61K31/44 , A61K31/443 , A61K31/4433 , A61K31/4545 , A61K31/47 , A61K31/4709 , A61K31/4738 , A61K31/496 , A61K31/497 , A61K31/498 , A61K31/501 , A61K31/506 , A61K31/5377 , A61K31/55 , A61P7/02 , A61P9/00 , A61P9/04 , A61P9/06 , A61P9/10 , A61P9/12 , A61P35/00 , A61P43/00 , C07D401/06 , C07D405/04 , C07D405/06 , C07D405/12 , C07D405/14 , C07D409/14 , C07D413/06 , C07D417/06 , C07D417/14 , C07D471/04 , C07D491/04 , C07D493/04 , C07D493/10
Abstract: 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-NR -, -C(O)NR -. -NR C(O)-, (a), optionally substituted alkenyl or optionally substituted alkynyl; X is -O- or -NR - when the double dotted line represents a single bond, or X is -OH or -NHR when the bond is absent; Y is =O, =S, (H, H), (H, OH) or (H, C1-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 is absent when the double dotted line represents a single bond and is H, -NR R , or -OR when the bond is absent; or Y is (A) or (B) and R is H or C1-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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公开(公告)号：AU724001B2
公开(公告)日：2000-09-07
申请号：AU3899997
申请日：1997-08-06
Applicant: SCHERING CORP
Inventor： LOWE DEREK B , CHANG WEI K , KOZLOWSKI JOSEPH A , BERGER JOEL G , MCQUADE ROBERT , BARNETT ALLEN , SHERLOCK MARGARET , TOM WING , DUGAR SUNDEEP , CHEN LIAN-YONG , CLADER JOHN W , CHACKALAMANNIL SAMUEL , WANG YUGUANG , MCCOMBIE STUART W , TAGAT JAYARAM R , VICE SUSAN F , VACCARO WAYNE D , GREEN MICHAEL J , BROWNE MARGARET E , ASBEROM THEODROS , BOYLE CRAIG D , JOSIEN HUBERT B
IPC: C07D211/58 , A61K31/00 , A61K31/435 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/445 , A61K31/4465 , A61K31/4523 , A61K31/4545 , A61K31/47 , A61K31/4709 , A61K31/495 , A61K31/496 , A61K31/50 , A61K31/501 , A61K45/00 , A61P25/28 , C07D211/24 , C07D211/32 , C07D211/96 , C07D239/34 , C07D257/04 , C07D295/02 , C07D295/03 , C07D295/084 , C07D295/088 , C07D295/096 , C07D295/112 , C07D295/116 , C07D295/125 , C07D295/13 , C07D295/135 , C07D295/145 , C07D295/15 , C07D401/04 , C07D401/10 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D409/14 , C07D413/14
Abstract: Di-N-substituted piperazine or 1,4 di-substituted piperadine compounds in accordance with formula I (including all isomers, salts, esters, and solvates) wherein R, R1, R2, R3, R4, R21, R27, R28, X, Y, and Z are as defined herein are muscarinic antagonists useful for treating cognitive disorders such as Alzheimer's disease. Pharmaceutical compositions and methods of preparation are also disclosed. Also disclosed are synergistic combinations of compounds of the above formula with acetylcholinesterase inhibitors.
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公开(公告)号：NZ333513A
公开(公告)日：2000-04-28
申请号：NZ33351397
申请日：1997-07-08
Applicant: SCHERING CORP
Inventor： ASBEROM THEODROS , LOWE DEREK B , GREEN MICHAEL J
IPC: A61K31/00 , A61K31/443 , A61K31/4433 , A61K31/445 , A61K31/4465 , A61K31/4468 , A61K31/4545 , A61K45/06 , A61P25/28 , C07D211/58 , C07D405/12 , C07D405/14 , C07D409/14
Abstract: A 1,4-di-substituted piperidine muscarinic antagonist of formula (I) or a pharmaceutically acceptable salt, ester, or solvate thereof is claimed wherein: X is a bond, -O-, -S-, -SO-, -SO2-, -CO-, -C(OR7)2-, -CH2-O-, -O-CH2-, -CH=CH-, -CH2-, -CH- alkyl-, -C-(alkyl)2-, -CONR17-, -NR17CO-, -SO2NR17- or -NR17SO2-; R is cycloalkyl or a group of formula (a), (b), (c), (d) or (e) or an optionally substituted phenyl or pyridyl; R1 is H, -CN, -CF3, alkyl, cycloalkyl, cycloalkenyl, alkenyl, -COR15, -CO2-(alkyl), -CO2-aryl, -CO2-heteroaryl, -CO2-(alkyl)aryl or -CO2-alkylheteroaryl, alkylaryl, alkylheteroaryl or -CON(R13)2; R2 is cycloalkyl, cycloalkenyl, t-butoxycarbonyl or optionally substituted 4-piperidinyl; R3 and R4 are independently H, halo, -CF3, alkyl, alkoxy or -OH; R5 and R6 are independently H, alkyl, -CF3, alkoxy, -OH, alkylcarbonyl, alkoxycarbonyl, R13CONH-, R14OCONH-, R13NHCONH- or NH2CONR13-; R7 is H or alkyl, or the two R7 groups may form -(CH2)2-4; R13, R15 and R17 are as defined in the specification. A pharmaceutical composition containing a compound of formula I useful for treating cognitive disorders such as Alzheimer's disease is claimed.
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公开(公告)号：SK15599A3
公开(公告)日：2000-03-13
申请号：SK15599
申请日：1997-08-06
Applicant: SCHERING CORP
Inventor： LOWE DEREK B , CHANG WEI K , KOZLOWSKI JOSEPH A , BERGER JOEL G , MCQUADE ROBERT , BARNETT ALLEN , SCHERLOCK MARGARET , TOM WING , DUGAR SUNDEEP , CHEN LIAN-YONG , CLADER JOHN W , CHACKALAMANNIL SAMUEL , WANG YUGUANG , MCCOMBIE STUART W , TAGAT JAYARAM R , VICE SUSAN F , VACCARO WAYNE D , GREEN MICHAEL J , BROWNE MARGARET E , ASBEROM THEODROS , BOYLE CRAIG D , JOSIEN HUBERT B
IPC: A61K31/00 , A61K31/435 , A61K31/4427 , A61K31/443 , A61K31/4433 , C07D211/58 , A61K31/445 , A61K31/4465 , A61K31/4523 , A61K31/4545 , A61K31/47 , A61K31/4709 , A61K31/495 , A61K31/496 , A61K31/50 , A61K31/501 , A61K45/00 , A61P25/28 , C07D211/24 , C07D211/32 , C07D211/96 , C07D239/34 , C07D257/04 , C07D295/02 , C07D295/03 , C07D295/084 , C07D295/088 , C07D295/096 , C07D295/112 , C07D295/116 , C07D295/125 , C07D295/13 , C07D295/135 , C07D295/145 , C07D295/15 , C07D401/04 , C07D401/10 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D409/14 , C07D413/14
Abstract: Di-N-substituted piperazine or 1,4 di-substituted piperadine compounds in accordance with formula I (including all isomers, salts, esters, and solvates) wherein R, R1, R2, R3, R4, R21, R27, R28, X, Y, and Z are as defined herein are muscarinic antagonists useful for treating cognitive disorders such as Alzheimer's disease. Pharmaceutical compositions and methods of preparation are also disclosed. Also disclosed are synergistic combinations of compounds of the above formula with acetylcholinesterase inhibitors.
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