公开(公告)号：CA2747750A1

公开(公告)日：2010-07-01

申请号：CA2747750

申请日：2009-12-18

Applicant: SCHERING CORP

Inventor： ASBEROM THEODROS ,  ZHU ZHAONING ,  CLADER JOHN W ,  SUN ZHONG-YUE ,  MANDAL MIHIRBARAN ,  GALLO GIOCONDA ,  LIU XIAOXIANG

IPC: C07D513/14 ,  A61K31/4245 ,  A61K31/5365 ,  A61K31/542 ,  A61P25/00 ,  C07D498/14

Abstract: This invention provides novel compounds that are modulators of gamma secretase. The compounds have the formula (Chemical formula should be inserted here as it appears on abstract in paper form). Also disclosed are methods of modulating gamma secretase activity and methods of treating Alzheimer's Disease using the compounds of formula (I).

公开(公告)号：CA2747744A1

公开(公告)日：2010-07-01

申请号：CA2747744

申请日：2009-12-18

Applicant: SCHERING CORP

Inventor： ASBEROM THEODROS ,  HUANG XIANHAI ,  ZHU ZHAONING ,  CLADER JOHN W ,  PISSARNITSKI DMITRI A ,  JOSIEN HUBERT B ,  LI HONGMEI

IPC: C07D498/04 ,  A61K31/4245 ,  A61P25/00 ,  A61P25/28

Abstract: This invention provides novel compounds that are modulators of gamma secretase. The compounds have the formula (Chemical formula should be inserted here as it appears on abstract in paper form). Also disclosed are methods of modulating gamma secretase activity and methods of treating Alzheimer's Disease using the compounds of formula (I).

公开(公告)号：CA2742317A1

公开(公告)日：2010-05-14

申请号：CA2742317

申请日：2009-11-05

Applicant: SCHERING CORP

Inventor： ZHU ZHAONING ,  GREENLEE WILLIAM J ,  COLE DAVID JAMES ,  PISSARNITSKI DMITRI A ,  GALLO GIOCONDA V ,  LI HONGMEI ,  JOSIEN HUBERT B ,  QIN JUN ,  KNUTSON CHAD E ,  MANDAL MIHIRBARAN ,  VICAREL MONICA L ,  RAJAGOPALAN MURALI ,  DHONDI PAWAN KUMAR ,  XU RUO ,  SUN ZHONG-YUE ,  BARA THOMAS A ,  HUANG XIANHAI ,  ZHU XIAOHONG ,  ZHAO ZHIQIANG ,  CLADER JOHN W ,  PALANI ANANDAN ,  ASBEROM THEODROS ,  MCCRACKEN TROY ,  BENNETT CHAD E

IPC: C07D413/10 ,  A61K31/4162 ,  A61K31/4245 ,  A61P25/28 ,  C07D471/04 ,  C07D498/04 ,  C07D498/20

Abstract: In its many embodiments, the present invention provides novel heterocyclic compounds as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the central nervous system using such compounds or pharmaceutical compositions.

公开(公告)号：PE20090447A1

公开(公告)日：2009-04-18

申请号：PE2008001184

申请日：2008-07-15

Applicant: SCHERING CORP

Inventor： SASIKUMAR THAVALAKULAMGARA K ,  BURNETT DUANE A ,  ASBEROM THEODROS ,  WU WEN-LIAN ,  XU RUO ,  LI HONGMEI ,  JOSIEN HUBERT B

IPC: A61K31/35 ,  A61K31/519 ,  A61K31/54 ,  A61K31/542 ,  C07D491/04

Abstract: SE REFIERE A UN COMPUESTO DE FORMULA 1, DONDE X ES -O-, -S-, -S(O2)-, ENTRE OTROS; ----ES ENLACE OPCIONAL; Y, Z SON CADA UNO N, C; Q ES ANILLO DE 5-8 MIEMBROS FUSIONADOS CON A1 Y Q1; Q1 ES ANILLO DE 5-7 MIEMBROS CON UN HETEROATOMO SLEECIONADO DE N, O, S(O) Y S(O2) FUSIONADO CON Q; L1 ES HALOGENO, ALQUILO, -CN, -CF3, -O-(ALQUILO C1-C6), ENTRE OTROS; Ar ES ARILO SUSTITUIDO O NO, HETEROARILO SUSTITUIDO O NO. UN COMPUESTO PREFERIDO ES (5aR,13aS)-11bR-[(4-CLOROFENIL)SULFONIL]-8,11-DIFLUORO-2,3,5a,6,11b,12,13,13a-OCTAHIDRO[1]BENZOPIRANO[4',3':5,6]PIRIDO[1,2-c]PIRIMIDIN-4(1H)-ONA. DICHOS COMPUESTOS SON INHIBIDORES DE GAMMA SECRETASA UTILES EN EL TRATAMIENTO DE ALZHEIMER

公开(公告)号：CA2686589A1

公开(公告)日：2008-11-13

申请号：CA2686589

申请日：2008-05-05

Applicant: SCHERING CORP

Inventor： GREENLEE WILLIAM J ,  CLADER JOHN ,  PALANI ANANDAN ,  HUANG XIANHAI ,  ZHU XIAOHONG ,  XU RUO ,  JOSIEN HUBERT ,  ZHU ZHAONING ,  VOIGT JOHANNES H ,  ZHAO ZHIQIANG ,  GALLO GIOCONDA ,  MAZZOLA ROBERT D JR ,  QIN JUN ,  PISSARNITSKI DMITRI A ,  ASBEROM THEODROS ,  MCBRIAR MARK D ,  LI HONGMEI ,  SUN ZHONG-YUE

IPC: C07D413/10 ,  A61K31/4245 ,  A61P25/00 ,  A61P25/28 ,  C07D413/14 ,  C07D498/04 ,  C07D498/10 ,  C07D498/20

Abstract: In its many embodiments, the present invention provides a novel class of heterocyclic compounds as modulators of gamma secretase, methods of preparin g such compounds, pharmaceutical compositions containing one or more such co mpounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or am elioration of one or more diseases associated with the central nervous syste m using such compounds or pharmaceutical compositions.

公开(公告)号：AU2008248129A1

公开(公告)日：2008-11-13

申请号：AU2008248129

申请日：2008-05-05

Applicant: SCHERING CORP

Inventor： ZHU XIAOHONG ,  ZHAO ZHIQIANG ,  CLADER JOHN ,  SUN ZHONG-YUE ,  GREENLEE WILLIAM J ,  PISSARNITSKI DMITRI A ,  LI HONGMEI ,  XU RUO ,  GALLO GIOCONDA ,  PALANI ANANDAN ,  MAZZOLA ROBERT D JR ,  MCBRIAR MARK D ,  QIN JUN ,  ZHU ZHAONING ,  HUANG XIANHAI ,  JOSIEN HUBERT ,  ASBEROM THEODROS

IPC: C07D413/10 ,  A61K31/4245 ,  A61P25/00 ,  A61P25/28 ,  C07D413/14 ,  C07D498/04 ,  C07D498/10 ,  C07D498/20

Abstract: The present invention provides a novel class of heterocyclic compounds of Formula (I) as modulators of gamma secretase, wherein the definitions of the variables of Formula (I) are defined herein, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the central nervous system using such compounds or pharmaceutical compositions.

公开(公告)号：NO20083598A

公开(公告)日：2008-10-20

申请号：NO20083598

申请日：2008-08-19

Applicant: SCHERING CORP

Inventor： ASBEROM THEODROS ,  LI HONGMEI ,  SU JING ,  TANG HAIQUN ,  BARA THOMAS A ,  BENNETT CHAD E ,  BURNETT DUANE A ,  CAPLEN MARY ANN ,  CLADER JOHN W ,  COLE DAVID J ,  DOMALSKI MARTIN S ,  JOSIEN HUBERT B ,  KNUTSON CHAD E ,  MCBRIAR MARK D ,  PISSARNITSKI DMITRI A ,  QIANG LI ,  RAJAGOPALAN MURALI ,  SASIKUMAR THAVALAKULAMGAR K ,  WU WEN-LIAN ,  XU RUO

IPC: C07D311/22 ,  C07C317/14

CPC classification number: C07D311/22 ,  C07C317/14 ,  C07C317/20 ,  C07C317/44 ,  C07C2602/08 ,  C07C2602/10 ,  C07C2602/12 ,  C07D311/80 ,  C07D311/92 ,  C07D311/94 ,  C07D313/08 ,  C07D335/06 ,  C07D405/12 ,  C07D409/12 ,  C07D491/04 ,  C07D493/04

公开(公告)号：MX2008009414A

公开(公告)日：2008-10-01

申请号：MX2008009414

申请日：2007-01-18

Applicant: SCHERING CORP

Inventor： ASBEROM THEODROS ,  ASBEROM THEODROS ,  XU RUO ,  QIANG LI ,  BURNETT DUANE A ,  CLADER JOHN W ,  SU JING ,  CAPLEN MARY ANN ,  PISSARNITSKI DMITRI A ,  JOSIEN HUBERT B ,  ZHAO ZHIQIANG ,  MCBRIAR MARK D ,  LI HONGMEI ,  TANG HAIQUN ,  KNUTSON CHAD E ,  WU WEN-LIAN ,  BARA THOMAS ,  BENNETT CHAD E ,  COLE DAVID J ,  DOMALSKI MARTIN S ,  RAJAGOPALAN MURALI ,  SASIKUMAR THAVALAKULAMGAR K

IPC: C07D311/22 ,  C07D311/80 ,  C07D311/92 ,  C07D311/94 ,  C07D313/08 ,  C07D335/06

Abstract: Esta invención describe novedosos inhibidores de gamma secretasa de la fórmula R2 y R3, o R2 y R4, o R3 y R4, que junto con los átomos a los cuales están unidos, pueden formar un anillo cicloalquilo fusionado o heterocicloalquilo fusionado; el anillo cicloalquilo o el anillo heterocicloalquilo pueden estar opcionalmente sustituidos con uno o más sustituyentes; uno o más compuestos de fórmula (I), o formulaciones que comprenden dichos compuestos, pueden ser útiles, por ejemplo en el tratamiento de la Enfermedad de Alzheimer. (ver fórmula (I)).

公开(公告)号：CA2637897A1

公开(公告)日：2007-07-26

申请号：CA2637897

申请日：2007-01-18

Applicant: SCHERING CORP

Inventor： XU RUO ,  JOSIEN HUBERT B ,  CLADER JOHN W ,  DOMALSKI MARTIN S ,  ASBEROM THEODROS ,  PISSARNITSKI DMITRI A ,  BARA THOMAS ,  KNUTSON CHAD E ,  WU WEN-LIAN ,  QIANG LI ,  CAPLEN MARY ANN ,  SASIKUMAR THAVALAKULAMGAR K ,  RAJAGOPALAN MURALI ,  ZHAO ZHIQIANG ,  BURNETT DUANE A ,  SU JING ,  TANG HAIQUN ,  BENNETT CHAD E ,  LI HONGMEI ,  COLE DAVID J ,  MCBRIAR MARK D

IPC: C07D311/22 ,  C07D311/80 ,  C07D311/92 ,  C07D311/94 ,  C07D313/08 ,  C07D335/06

Abstract: This invention discloses novel gamma secretase inhibitors of the formula: R2 and R3, or R2 and R4, or R3 and R4, together with the atoms to which they are bound, can form a fused cycloalkyl or fused heterocycloalkyl ring. The cycloalkyl ring or the heterocycloalkyl ring can be optionally substituted with one or more substituents. One or more compounds of formula (I), or formulations comprising such compounds, may be useful, e.g. in treating Alzheimer's Disease.

公开(公告)号：CA2212895C

公开(公告)日：2007-04-10

申请号：CA2212895

申请日：1996-02-16

Applicant: SCHERING CORP

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

IPC: C07D295/08 ,  C07D295/096 ,  A61K31/335 ,  A61K31/357 ,  A61K31/36 ,  A61K31/365 ,  A61K31/4427 ,  A61K31/443 ,  A61K31/445 ,  A61K31/4468 ,  A61K31/451 ,  A61K31/495 ,  A61K31/496 ,  A61K31/505 ,  A61K31/535 ,  A61K31/5375 ,  A61K31/5377 ,  A61K31/695 ,  A61P25/28 ,  C07D211/14 ,  C07D211/22 ,  C07D211/24 ,  C07D211/26 ,  C07D211/32 ,  C07D211/58 ,  C07D211/62 ,  C07D213/63 ,  C07D213/70 ,  C07D233/84 ,  C07D237/14 ,  C07D239/32 ,  C07D239/34 ,  C07D241/18 ,  C07D257/04 ,  C07D263/58 ,  C07D271/06 ,  C07D277/34 ,  C07D295/02 ,  C07D295/03 ,  C07D295/084 ,  C07D295/088 ,  C07D295/108 ,  C07D295/112 ,  C07D295/116 ,  C07D295/12 ,  C07D295/125 ,  C07D295/13 ,  C07D295/135 ,  C07D295/14 ,  C07D295/145 ,  C07D295/15 ,  C07D307/33 ,  C07D309/12 ,  C07D317/28 ,  C07D317/62 ,  C07D333/20 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07F7/10

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 or other compounds capable of enhan cing acetylcholine release with acetylcholinesterase inhibitors.