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21. 发明公开

EP1723145A4 SUBSTITUTED 5,12-DIAZA-BENZOANTHRACENE ANALOGUES 审中-公开
标题翻译：取代的5,12-二氮杂苯并噻喃桂醛
公开(公告)号：EP1723145A4
公开(公告)日：2009-12-02
申请号：EP05729389
申请日：2005-03-11
申请人： NEUROGEN CORP
发明人： CALDWELL TIMOTHY M , HODGETTS KEVIN J , HUTCHISON ALAN
IPC分类号： C07D471/14 , A61K31/44
CPC分类号： C07D498/14 , C07D471/12 , C07D471/14 , C07D491/22 , C07D498/04

22. 发明公开

EP1745024A4 1-ARYL-4-SUBSTITUTED ISOQUINOLINES 有权
标题翻译：异喹啉1-芳基-4-取代
公开(公告)号：EP1745024A4
公开(公告)日：2008-01-09
申请号：EP05747952
申请日：2005-05-06
申请人： NEUROGEN CORP
发明人： LEE KYUNGAE , YUAN JUN , MAYNARD GEORGE D , HUTCHISON ALAN , MITCHELL SCOTT
IPC分类号： A61K31/47 , A61P29/00 , C07D217/02 , C07D217/14 , C07D217/16 , C07D217/22 , C07D401/04 , C07D401/14 , C07D405/12 , C07D413/14
CPC分类号： C07D405/12 , A61K31/47 , C07D217/14 , C07D217/16 , C07D217/22 , C07D401/04 , C07D401/06 , C07D401/14 , C07D413/14

23. 发明公开

EP1487796A4 SUBSTITUTED BIARYL AMIDES AS C5A RECEPTOR MODULATORS 审中-公开
标题翻译：取代联芳AS C5A受体的调节剂
公开(公告)号：EP1487796A4
公开(公告)日：2005-11-16
申请号：EP03745585
申请日：2003-03-25
申请人： NEUROGEN CORP
发明人： GAO YANG , HUTCHISON ALAN , PETERSON JOHN , PRINGLE WALLACE , THURKAUF ANDREW , YOON TAEYOUNG , ZHAO HE
IPC分类号： C07C233/65 , C07C235/62 , C07D207/32 , C07D207/327 , C07D209/08 , C07D231/56 , C07D235/06 , C07D317/58 , C07D333/24 , C07D521/00 , C07D215/00 , A61K31/38 , A61K31/40 , A61K31/415 , C07D233/02 , C07D235/02 , C07D317/44 , C07D405/00 , C07D409/00
CPC分类号： C07D249/08 , C07C233/65 , C07C235/62 , C07C2602/08 , C07D207/327 , C07D209/08 , C07D231/12 , C07D231/56 , C07D233/56 , C07D235/06 , C07D317/58 , C07D333/24
摘要： Substituted biaryl amides of Formula I are provided. Such compounds are ligands that may be used to modulate C5a receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological C5a receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using them to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.

24. 发明专利

ES2384619T3 Isoquinolinas 1-aril-4-sustituidas 未知
公开(公告)号：ES2384619T3
公开(公告)日：2012-07-09
申请号：ES05747952
申请日：2005-05-06
申请人： NEUROGEN CORP , NOVARTIS INT PHARM LTD
发明人： LEE KYUNGAE , YUAN JUN , MAYNARD GEORGE D , HUTCHISON ALAN , MITCHELL SCOTT
IPC分类号： A61K31/47 , A61P29/00 , C07D217/02 , C07D217/14 , C07D217/16 , C07D217/22 , C07D401/04 , C07D401/14 , C07D405/12 , C07D413/14
摘要： Un compuesto según la fórmula I**Fórmula**o una sal farmacéuticamente aceptable de los mismos, en la que:R1 se selecciona de hidrógeno, alquilo de C1-C6, alquenilo de C2-C6, alquinilo de C2-C6, alcoxi de C1-C6, haloalquilode C1-C6, haloalcoxi de C1-C6, (cicloalquil C3-C7)-alquilo de C0-C4;R2 es -(CRARB)OR4;R3 representa entre 0 y 4 sustituyentes, cada uno de los cuales se selecciona independientemente de halógeno,hidroxi, amino, ciano, alquilo opcionalmente sustituido, haloalquilo opcionalmente sustituido, alqueniloopcionalmente sustituido, alquinilo opcionalmente sustituido, cicloalquilo opcionalmente sustituido, alcoxiopcionalmente sustituido, haloalcoxi opcionalmente sustituido, hidroxialquilo opcionalmente sustituido,alcoxialquilo opcionalmente sustituido, mono- y di-alquilamino opcionalmente sustituido, aminoalquiloopcionalmente sustituido, -E-(CRCRD)m-Z, y -E-(CRCRD)m-XRA;R4 es:(i) alquilo de C2-C8, alquenilo de C2-C8, alquinilo de C2-C8, (cicloalquil C3-C7)-alquilo de C0-C4, mono- o di-(alquilC1-C4-amino)-alquilo de C2-C4, (heterocicloalquilo de 3 a 7 miembros)-alquilo de C0-C4, aril-alquilo de C0-C4, o(heteroaril)-alquilo de C0-4, cada uno de los cuales está sustituido con 0 a 4 sustituyentes seleccionadosindependientemente de Rx, alcanoilo de C2-C4, mono- y di-(alquil C1-C4)amino(alquilo de C1-C4), mono- y dialquilC1-C4-amino(alcoxi de C1-C4), (heterocicloalquilo de 3 a 7 miembros)alquilo de C0-C4 y XRy; o(ii) se une a R5 para formar, con el nitrógeno al que están unidos R4 y R5, un heterociclo que tiene de 1 a 3 anillos,5 a 7 miembros anulares en cada anillo, en el que el heterociclo está sustituido con 0 a 4 sustituyentesseleccionados independientemente de Rx, oxo y W-Z;R5 es:(i) hidrógeno;(ii) alquilo de C1-C6, alquenilo de C2-C6, alquinilo de C2-C6, (carbociclo C3-C7)-alquilo de C0-C4, cada uno de loscuales está sustituido con 0 a 3 sustituyentes seleccionados independientemente de halógeno, hidroxi, amino,ciano, alquilo de C1-C4, alcoxi de C1-C4, metilamino, dimetilamino, trifluorometilo y trifluorometoxi; o(iii) está unido a R4 para formar, con el nitrógeno al que están unidos R5 y R4, un heterociclo que tiene de 1 a 3anillos, 5 a 7 miembros anulares en cada anillo, en el que el heterociclo está sustituido con 0 a 4 sustituyentesseleccionados independientemente de Rx, oxo y W-Z;Ar es fenilo mono-, di- o tri-sustituido, naftilo opcionalmente sustituido, o heteroarilo opcionalmente sustituido, en elque Ar es heteroarilo opcionalmente sustituido cuando R2 es -NR4R5;RA, RA' y RB, que pueden ser iguales o diferentes, se seleccionan independientemente en cada caso de: (i) hidrógenoe hidroxi, y (ii) grupos alquilo, grupos cicloalquilo, y grupos (cicloalquil)alquilo, cada uno de los cuales estáopcionalmente sustituido con uno o más sustituyente(s) seleccionado(s) independientemente de oxo, hidroxi,halógeno, ciano, amino, alcoxi de C1-6, -NH(alquilo de C1-6), -N(alquilo de C1-6)(alquilo de C1-6), -NHC(>=O)(alquilode C1-6), -N(alquilo de C1-6)C(>=O)(alquilo de C1-6), -NHS(O)n(alquilo de C1-6), -S(O)n(alquilo de C1-6),-S(O)nNH(alquilo de C1-6), -S(O)nN(alquilo de C1-6)(alquilo de C1-6), y Z;Rx se escoge independientemente, en cada caso, de halógeno, hidroxi, amino, ciano, nitro, -COOH, -C(>=O)NH2,alcoxi C1-C6-carbonilo, mono- y di-(alquil C1-6)aminocarbonilo, alquilo de C1-C6, alquenilo de C2-C6, alquinilo deC2-C6, mono- y di-(alquil C1-C6)amino, alcoxi de C1-C6, hidroxialquilo de C1-C2, haloalquilo de C1-C2, haloalcoxide C1-C2, (cicloalquil C3-C7)-alquilo de C0-C4, y -S(On)alquilo de C1-C6;

25. 发明专利

AU2002232768B2 Benzimidazole and pyridylimidazole derivatives as ligands for GABA receptors 未知
公开(公告)号：AU2002232768B2
公开(公告)日：2007-09-06
申请号：AU2002232768
申请日：2001-12-21
申请人： NEUROGEN CORP , PFIZER
发明人： CAI GUOLIN , YUAN JUN , ALLEN MARTIN PATRICK , LIU NIAN , HONG XIE LING , MITCHELL SCOTT , GUSTAVSON LINDA M , PETERSON JOHN M , SINGH VINOD , ALBAUGH PAMELA , LUKE GEORGE P , GHOSH MANUKA , HUTCHISON ALAN , LI GUIYING , CURRIE KEVIN S , LEE KYUNGAE , MAYNARD GEORGE D , LIRAS SPIROS
IPC分类号： C07D401/14 , A61K31/415 , A61K31/4184 , A61K31/4196 , A61K31/422 , A61K31/4245 , A61K31/435 , A61K31/437 , A61K31/438 , A61K31/4439 , A61K31/454 , A61K31/506 , A61K31/5377 , A61K31/541 , A61K31/55 , A61P25/00 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , C07D233/20 , C07D233/54 , C07D401/04 , C07D403/04 , C07D403/06 , C07D403/14 , C07D405/04 , C07D405/14 , C07D409/14 , C07D413/06 , C07D413/14 , C07D417/04 , C07D417/06 , C07D417/14 , C07D471/04 , C07D473/00 , C07D491/08 , C07D491/10 , C07D491/113
摘要： This invention relates to benzimidazoles, pyridylimidazoles and related bicyclic heteroaryl compounds, all of which may be described by of Formula I The invention is particularly related to such compounds that bind with high selectivity and high affinity to the benzodiazepine site of GABAA receptors. This invention also relates to pharmaceutical compositions comprising such compounds and to the use of such compounds in treatment of certain central nervous system (CNS) diseases. Novel processes for preparing compounds of Formula I are disclosed. This invention also relates to the use of benzimidazoles, pyridylimidazoles and related bicyclic heteroaryl compounds of Formula I in combination with one or more other CNS agents to potentiate the effects of the other CNS agents. Additionally this invention relates to the use such compounds as probes for the localization of GABAA receptors in tissue sections.

26. 发明专利

DE60113302T2 未知
公开(公告)号：DE60113302T2
公开(公告)日：2006-06-29
申请号：DE60113302
申请日：2001-12-21
申请人： NEUROGEN CORP , PFIZER
发明人： LI GUIYING , PETERSON M , ALBAUGH PAMELA , CURRIE S , CAI GUOLIN , GUSTAVSON M , LEE KYUNGAE , HUTCHISON ALAN , SINGH VINOD , MAYNARD D , YUAN JUN , LING HONG XIE , GHOSH MANUKA , LIU NIAN , LUKE P , MITCHELL SCOTT , ALLEN PATRICK , LIRAS SPIROS
IPC分类号： C07D401/14 , A61K31/415 , A61K31/4184 , A61K31/4196 , A61K31/422 , A61K31/4245 , A61K31/435 , A61K31/437 , A61K31/438 , A61K31/4439 , A61K31/454 , A61K31/506 , A61K31/5377 , A61K31/541 , A61K31/55 , A61P25/00 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , C07D233/20 , C07D233/54 , C07D401/04 , C07D403/04 , C07D403/06 , C07D403/14 , C07D405/04 , C07D405/14 , C07D409/14 , C07D413/06 , C07D413/14 , C07D417/04 , C07D417/06 , C07D417/14 , C07D471/04 , C07D473/00 , C07D491/08 , C07D491/10 , C07D491/113
摘要： This invention relates to benzimidazoles, pyridylimidazoles and related bicyclic heteroaryl compounds, all of which may be described by of Formula I The invention is particularly related to such compounds that bind with high selectivity and high affinity to the benzodiazepine site of GABAA receptors. This invention also relates to pharmaceutical compositions comprising such compounds and to the use of such compounds in treatment of certain central nervous system (CNS) diseases. Novel processes for preparing compounds of Formula I are disclosed. This invention also relates to the use of benzimidazoles, pyridylimidazoles and related bicyclic heteroaryl compounds of Formula I in combination with one or more other CNS agents to potentiate the effects of the other CNS agents. Additionally this invention relates to the use such compounds as probes for the localization of GABAA receptors in tissue sections.

27. 发明专利

DE60014339T8 未知
公开(公告)号：DE60014339T8
公开(公告)日：2006-04-27
申请号：DE60014339
申请日：2000-03-31
申请人： NEUROGEN CORP
发明人： DESIMONE W , HUTCHISON ALAN , SHAW KENNETH , ROSEWATER L
IPC分类号： C07D235/16 , C07D471/04 , A61K31/4184 , A61K31/427 , A61K31/437 , A61K31/454 , A61K31/4725 , A61K31/5377 , A61P25/00 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , A61P43/00 , C07D235/10 , C07D235/14 , C07D401/04 , C07D401/06 , C07D401/12 , C07D405/06 , C07D405/12 , C07D409/12 , C07D409/14 , C07D417/12
摘要： Disclosed are compounds of the formula: or the pharmaceutically acceptable non-toxic salts thereof wherein the A, B, C, D, X, R 1 , R 2 , R 3 , R 4 , R 5 , and R 6 , are variables defined herein, which compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAa brain receptors, and are therefore useful in the diagnosis and treatment of anxiety, Down Syndrome, sleep, cognitive and seizure disorders, depression, overdose with benzodiazepine drugs, and enhancement of memory and alertness.

28. 发明专利

ES2249384T3 ESPIRO(ISOBENZOFURAN-1,4'-PIPERADIN)-3-ONAS Y 3H-ESPIROBENZOFURAN-1,4-PIPERIDINAS. 未知
公开(公告)号：ES2249384T3
公开(公告)日：2006-04-01
申请号：ES01270536
申请日：2001-12-11
申请人： NEUROGEN CORP , PFIZER
发明人： BAKTHAVATCHALAM RAJAGOPAL , BLUM CHARLES A , BRIELMANN HARRY L , DARROW JAMES WILLIAM , DE LOMBAERT STEPHANE , HUTCHISON ALAN
IPC分类号： C07D491/107 , A61K31/438 , A61K31/444 , A61K31/4545 , A61K31/496 , A61K31/497 , A61K31/4985 , A61K31/506 , A61K31/517 , A61K31/519 , A61K51/00 , A61P3/04 , A61P3/10 , A61P9/00 , A61P25/00 , A61P25/18 , A61P25/24 , A61P43/00 , C07D487/04 , C07D487/10 , C07D491/10 , C07D519/00
摘要： Un compuesto de **fórmula** o una sal o profármaco farmacéuticamente aceptable del mismo, en la que: X es oxígeno o H2; cada uno de A, D, V, W, Y y Z es independientemente CR1; B es N o CR2; E es N o CR3; R1 se selecciona independientemente cada vez que está presente entre: (i) hidrógeno, halógeno, hidroxi, amino, nitro, ciano, -C(=O)NH2 y -COOH; y (ii) L-RA-Q-G, en la que L es un enlace, -O-, -C(=O)-, -OC(=O)-, -C(=O)O-, -O- C(=O)O-, -S(O)n-;-NRB-, -C(=O)NHRB-, -NHRBC(=O)-, -NRBS(O)n- o -S(O)nNRB-; n se elige independientemente cada vez que está presente entre 0, 1 ó 2; RA es alquilo (C1-C8), alquenilo (C2-C8), alquinilo (C2-C8), cicloalquilo (C3-C8), cicloalquenilo (C3-C8), cicloalquinilo (C3-C8) o heterocicloalquilo (C3-C8), cada uno opcionalmente sustituido con 1 a 5 sustituyentes seleccionados independientemente entre hidroxi, halógeno, amino, ciano, nitro, alquilo (C1-C6) y halo-alquilo (C1- C6).

29. 发明专利

AP1503A Benzimidazole and pyridylimidazole derivatives as ligands for GABA receptors 未知
公开(公告)号：AP1503A
公开(公告)日：2005-12-24
申请号：AP2003002818
申请日：2001-12-21
申请人： NEUROGEN CORP , PFIZER
发明人： LI GUIYING , PETERSON JOHN M , ALBAUGH PAMELA , CURRIE KEVIN S , CAL GUOLIN , GUSTAVSON LINDA M , LEE KYUNGAE , HUTCHISON ALAN , SINGH VINOD , MAYNARD GEORGE D , YUAN JUN , LING HONG XIE , GHOSH MANUKA , LIU NIAN , LUKE GEORGE P , MITCHELL SCOTT , LIRAS SPIROS , ALLEN MARTIN PATRICK
IPC分类号： C07D401/14 , A61K31/00 , A61K31/415 , A61K31/4184 , A61K31/4196 , A61K31/422 , A61K31/4245 , A61K31/435 , A61K31/437 , A61K31/438 , A61K31/4439 , A61K31/454 , A61K31/506 , A61K31/5377 , A61K31/541 , A61K31/55 , A61P25/00 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , C07D233/20 , C07D233/54 , C07D401/04 , C07D403/04 , C07D403/06 , C07D403/14 , C07D405/04 , C07D405/14 , C07D409/14 , C07D413/06 , C07D413/14 , C07D417/04 , C07D417/06 , C07D417/14 , C07D471/04 , C07D473/00 , C07D491/08 , C07D491/10 , C07D491/113
摘要： This invention relates to benzimidazoles, pyridylimidazoles and related bicyclic heteroaryl compounds, all of which may be described by of formula (1), the invention is particularly related to such compounds that bind with high selectivity and high affinity to the benzodiazepine site of GABA receptors. This invention also relates to pharmaceutical compositions comprising such compounds and to the use of such compounds in treatment of certain central nervous system (cns) diseases, Novel processes for preparing compounds of formula I are disclosed. This invention also relates to the use of benzimidazoles, pyridylimidazoles and related bicyclic heteroaryl compounds of formula 1 in combination with one or more other CNS agents to potentiate the effects of the other CNS agents. Additionally this invention relates to the use such compounds as probes for the localization of GABA receptors in tissue sections.

30. 发明专利

CA2557545A1 SUBSTITUTED 5,12-DIAZA-BENZOANTHRACENE ANALOGUES 未知
公开(公告)号：CA2557545A1
公开(公告)日：2005-09-22
申请号：CA2557545
申请日：2005-03-11
申请人： NEUROGEN CORP
发明人： CALDWELL TIMOTHY M , HODGETTS KEVIN J , HUTCHISON ALAN
IPC分类号： C07D471/14 , A61K31/44
摘要： Substituted 5,12-diaza-benzoanthracene analogues are provided, of the Formul a (I) wherein variables are as described herein. Such compounds are ligands th at may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals a nd livestock animals. Pharmaceutical compositions and methods for using such compounds to treat such disorders are provided, as are methods for using suc h ligands for receptor localization studies.

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