公开(公告)号：ZA9810685B

公开(公告)日：1999-12-23

申请号：ZA9810685

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 ,  C07D ,  A61K

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.

公开(公告)号：BR9711119A

公开(公告)日：1999-11-23

申请号：BR9711119

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-YOUNG ,  CLADER JOHN W ,  CHACKALAMANNIL SAMUEL ,  WANG YUGUANG ,  MCCOMBIE STUART W ,  MCCOMBIE JAYARAM W ,  VICE SUSAN F ,  VACCARO WAINE D ,  GREEN MICHAEL J ,  BROWNE MARGARET ,  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.

公开(公告)号：NO990551L

公开(公告)日：1999-04-07

申请号：NO990551

申请日：1999-02-05

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: A61K31/00 ,  A61K31/435 ,  A61K31/4427 ,  A61K31/443 ,  C07D211/58 ,  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.

公开(公告)号：NO990551A

公开(公告)日：1999-04-07

申请号：NO990551

申请日：1999-02-05

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

CPC classification number: C07D405/14 ,  C07C2601/14 ,  C07D211/24 ,  C07D211/32 ,  C07D239/34 ,  C07D257/04 ,  C07D295/03 ,  C07D295/088 ,  C07D295/092 ,  C07D295/096 ,  C07D295/112 ,  C07D295/116 ,  C07D295/125 ,  C07D295/13 ,  C07D295/135 ,  C07D295/145 ,  C07D295/15 ,  C07D405/12 ,  C07D409/14

公开(公告)号：CA2261725A1

公开(公告)日：1998-02-12

申请号：CA2261725

申请日：1997-08-06

Applicant: SCHERING CORP

Inventor： BERGER JOEL G ,  MCQUADE ROBERT ,  SHERLOCK MARGARET ,  LOWE DEREK B ,  GREEN MICHAEL J ,  BARNETT ALLEN ,  CHEN LIAN-YONG ,  MCCOMBIE STUART W ,  TAGAT JAYARAM R ,  VACCARO WAYNE D ,  KOZLOWSKI JOSEPH A ,  CHACKALAMANNIL SAMUEL ,  CHANG WEI K ,  TOM WING ,  BROWNE MARGARET E ,  JOSIEN HUBERT B ,  ASBEROM THEODROS ,  BOYLE CRAIG D ,  DUGAR SUNDEEP ,  VICE SUSAN F ,  WANG YUGUANG ,  CLADER JOHN W

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 ,  C07D417/14 ,  A61K31/53

Abstract: Di-N-substituted piperazine or 1,4 di-substituted piperidine 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 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.

公开(公告)号：ZA9707011B

公开(公告)日：1998-02-06

申请号：ZA9707011

申请日：1997-08-06

Applicant: SCHERING CORP

Inventor： LOWE DEREK B ,  BERGER JOEL G ,  SHERLOCK MARGARET ,  CHEN LIAN-YONG ,  WANG YUGUANG ,  VICE SUSAN F ,  BROWNE MARGARET E ,  JOSIEN HUBERT B ,  CHANG WEI K ,  MCQUADE ROBERT ,  TOM WING ,  CLADER JOHN W ,  MCCOMBIE STUART W ,  VACCARO WAYNE D ,  ASBEROM THEODROS ,  KOZLOWSKI JOSEPH A ,  BARNETT ALLEN ,  DUGAR SUNDEEP ,  CHACKALAMANNIL SAMUEL ,  TAGAT JAYARAM R ,  GREEN MICHAEL J ,  BOYLE CRAIG D

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 ,  C07D ,  A61J ,  A61K

CPC classification number: C07D405/14 ,  C07C2601/14 ,  C07D211/24 ,  C07D211/32 ,  C07D239/34 ,  C07D257/04 ,  C07D295/03 ,  C07D295/088 ,  C07D295/092 ,  C07D295/096 ,  C07D295/112 ,  C07D295/116 ,  C07D295/125 ,  C07D295/13 ,  C07D295/135 ,  C07D295/145 ,  C07D295/15 ,  C07D405/12 ,  C07D409/14

公开(公告)号：ZA9601293B

公开(公告)日：1996-08-19

申请号：ZA9601293

申请日：1996-02-19

Applicant: SCHERING CORP

Inventor： LOWE DEREK ,  KOZLOWSKI JOSEPH ,  MCQUADE ROBERT ,  SHERLOCK MARGARET ,  DUGAR SUNDEEP ,  CLADER JOHN W ,  WANG YUGUANG ,  TAGAT JAYARAM R ,  VACCARO WAYNE ,  BROWNE MARGARET E ,  CHANG WEI ,  BERGER JOEL G ,  BARNETT ALLEN ,  TOM WING ,  CHEN LIAN-YONG ,  CHACKALAMANNIL SAMUEL ,  MCCOMBIE STUART W ,  VICE SUSAN F ,  GREEN MICHAEL J ,  ASBEROM THEODROS

IPC: A61K20060101 ,  C07D20060101 ,  C07K20060101 ,  A61K ,  C07D ,  C07K

公开(公告)号：OA9662A

公开(公告)日：1993-05-15

申请号：OA60254

申请日：1992-07-31

Applicant: SCHERING CORP

Inventor： ASBEROM THEODROS ,  O'CONNOR EDWARD ,  BERGER JOEL GILBERT ,  CLADER JOHN WELCH

IPC: A61K31/55 ,  A61P25/04 ,  A61P25/18 ,  A61P25/24 ,  A61P25/26 ,  A61P25/30 ,  C07D223/18 ,  C07D223/32

CPC classification number: C07D223/18 ,  C07D223/32

公开(公告)号：NO923042D0

公开(公告)日：1992-07-31

申请号：NO923042

申请日：1992-07-31

Applicant: SCHERING CORP

Inventor： ASBEROM THEODROS ,  O'CONNOR EDWARD ,  BERGER JOEL GILBERT ,  CLADER JOHN WELCH

IPC: C07D223/00 ,  C07D223/18 ,  C07D223/32

公开(公告)号：AT515495T

公开(公告)日：2011-07-15

申请号：AT02759233

申请日：2002-08-01

Applicant: SCHERING CORP

Inventor： ASBEROM THEODROS ,  GUZIK HENRY ,  JOSIEN HUBERT ,  PISSARNITSKI DMITRI

IPC: C07D201/00 ,  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.