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1. 发明申请

WO2008033764A2 QUINAZOLINONE AND ISOQUINOLINONE ACETAMIDE DERIVATIVES 审中-公开
标题翻译：喹唑啉酮和异喹啉酮酰胺衍生物
公开(公告)号：WO2008033764A2
公开(公告)日：2008-03-20
申请号：PCT/US2007078022
申请日：2007-09-10
申请人： ORGANON NV , LETOURNEAU JEFFREY , JOKIEL PATRICK , NAPIER ELIZABETH , HO KOC-KAN , OHLMEYER MICHAEL , MCARTHUR DUNCAN ROBERT , FIONA JEREMIAH , RATCLIFFE PAUL DAVID , SCHULZ JUERGEN
发明人： LETOURNEAU JEFFREY , JOKIEL PATRICK , NAPIER ELIZABETH , HO KOC-KAN , OHLMEYER MICHAEL , MCARTHUR DUNCAN ROBERT , FIONA JEREMIAH , RATCLIFFE PAUL DAVID , JURGEN SCHULZ
IPC分类号： A61K31/517 , A61K31/5377 , A61K31/551 , A61P25/00 , C07D401/02 , C07D403/02 , C07D413/14
CPC分类号： C07D403/04 , C07D217/24 , C07D239/91 , C07D401/04 , C07D405/12 , C07D409/04 , C07D409/12 , C07D471/08 , C07D487/04
摘要： The present invention relates to a quinazolinone or isoquinolinone derivative of formula I, wherein R 1 is C 1-6 alkyl, C 3-6 cycloalkyl, C 3-6 cycloalkylC 1-3 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, said C 1-6 alkyl, C 3-6 cycloalkyl and C 3-6 cycloalkylC 1-3 alkyl being optionally substituted with hydroxy, C 1-6 alkyloxy, cyano or one or more halogens; R 2 is C 6-10 aryl optionally substituted with one to three substituents selected from halogen, hydroxy, cyano, C 1-6 alkyl, C 3-6 cycloalkyl, C 1-6 alkyloxy and C 3-6 cycloalkyloxy, said C 1-6 alkyl, C 3-6 cycloalkyl, C 1-6 alkyloxy and C 3-6 Cycloalkyloxy being optionally substituted with one or more halogens; or R 2 is a 5-10 membered heteroaryl ring system comprising a heteroatom selected from N, O and S and optionally substituted with a substituent selected from methyl, C 1-6 alkyloxy and halogen; or R 2 is C 4-7 cycloalkyl; R 3 is an optional substituent selected from C 1-6 alkyl, C 1-6 alkyloxy and halogen, said C 1-6 alkyl and C 1-6 alkyloxy being optionally substituted with one or more halogens; R 4 is a group located at the 6- or 7- position of the quinazolinone or isoquinolinone ring having the formula Il, wherein R 5 together with one of R 6 forms a 4-8 membered saturated or unsaturated heterocyclic ring optionally comprising a further heteroatomic moiety selected from O, S and NR 9 , said heterocyclic ring being optionally substituted with one or two substituents selected from methyl, halogen, hydroxy and oxo or R 5 together with one of R 7 and R 8 forms a 6-8 membered heterocyclic ring optionally substituted with one or two substituents selected from methyl, halogen, hydroxy and oxo; Each R 6 is independently H, halogen or C 1-4 alkyl optionally substituted with halogen or SO 2 CH 3 or one of R 6 together with R 5 forms a 4-8 membered saturated or unsaturated heterocyclic ring optionally comprising a further heteroatomic moiety selected from O, S and NR 9 , said heterocyclic ring being optionally substituted with one or two substituents selected from methyl, halogen, hydroxy and oxo; R 7 and R 8 are independently H, C 1-6 alkyl, C 3-6 cycloalkyl, C 3-6 cycloalkylc 1-3 alkyl, cyanoC 1-3 alkyl, C 6-10 aryl, C 6-10 arylC 1-3 alkyl, C 1-3 alkyloxyC 1-3 alkyl or C 1-6 acyl said C 1-6 alkyl, C 3-6 cycloalkyl and C 3-6 cycloalkylC 1-3 alkyl being optionally substituted with hydroxy, 1 or more halogens or diC 1-2 alkylamino; or R 7 and R 8 together with the nitrogen to which they are bonded form a 4-8 membered saturated or unsaturated heterocyclic ring optionally comprising a further heteroatomic moiety selected from O, S and NR 10 , said heterocyclic ring being optionally substituted with one or two substituents selected from C 1-6 alkyl, halogen, hydroxy,
摘要翻译：本发明涉及式I的喹唑啉酮或异喹啉酮衍生物，其中R 1是C 1-6烷基，C 3-6环烷基，C 3-6环烷基C 1-3烷基，C 2-6链烯基，C 2-6亚炔基所述C 1-6烷基，C 3-6环烷基和C 3-6环烷基C 1-3烷基，烷基任选被羟基，C 1-6烷氧基，氰基或一个或多个卤素取代; R 2是任选被一至三个选自卤素，羟基，氰基，C 1-6烷基的取代基取代的C 6-10芳基， C 3-6环烷基，C 1-6烷氧基和C 3-6环烷氧基，所述C 1-6 - 亚烷基烷基，C 3-6环烷基，C 1-6烷氧基和C 3-6环烷氧基任选被一个或多个卤素取代; 或R 2是包含选自N，O和S的杂原子并任选被选自甲基，C 1-6烷基的取代基取代的5-10元杂芳基环系统。烷氧基和卤素; 或R 2是C 4-7环烷基; R 3是选自C 1-6烷基，C 1-6烷氧基和卤素的任意取代基，所述C 1〜 C 1-6烷基和任选被一个或多个卤素取代的C 1-6烷氧基; R 4是位于具有式II的喹唑啉酮或异喹啉酮环的6-或7-位的基团，其中R 5与R“ 6〜6元饱和或不饱和杂环任选地包含选自O，S和NR 9的另外的杂原子部分，所述杂环任选被一个或两个选自下列的取代基取代：从甲基，卤素，羟基和氧代或R 5与R 7和R 8和R 8之一一起形成6-8元杂环，任选地被一个或两个选自甲基，卤素，羟基和氧代的取代基取代; 每个R 6独立地是H，卤素或任选被卤素或SO 2 CH 3取代的C 1-4烷基 >或R 6中的一个与R 5一起形成4-8元饱和或不饱和杂环，任选地包含另外的选自O，S和NRO的杂原子部分所述杂环任选被一个或两个选自甲基，卤素，羟基和氧代的取代基取代; R 7和R 8独立地为H，C 1-6烷基，C 3-6环烷基，C 3-6个环烷基C 1-3烷基，氰基C 1-3烷基，C 6-10芳基，C C 6-10芳基C 1-3烷基，C 1-3烷氧基C 1-3烷基或C _{1-6个酰基，所述C 1-6烷基，C 3-6环烷基和C 3-6环烷基C SUB 任选被羟基，一个或多个卤素或二-C 1-2烷基氨基取代的烷基，或R 7和R 8与它们所键合的氮一起形成4-8元饱和或不饱和杂环，任选地包含另外的选自O， S和NR 10，所述杂环任选被一个或两个选自C 1-6烷基，卤素，羟基，}

2. 发明公开

EP2069315A4 QUINAZOLINONE AND ISOQUINOLINONE ACETAMIDE DERIVATIVES 无效转让
标题翻译： CHINAZOLINON-和ISOCHINOLINON-的乙酰胺衍生物
公开(公告)号：EP2069315A4
公开(公告)日：2010-11-03
申请号：EP07842157
申请日：2007-09-10
申请人： ORGANON NV , PHARMACOPEIA LLC
发明人： LETOURNEAU JEFFREY , JOKIEL PATRICK , NAPIER SUSAN ELIZABETH , HO KOC-KAN , OHLMEYER MICHAEL , MCARTHUR DUNCAN ROBERT , FIONA JEREMIAH , RATCLIFFE PAUL DAVID , JURGEN SCHULZ
IPC分类号： C07D239/70 , A61K31/472 , A61K31/4725 , A61K31/496 , A61K31/519 , A61K31/5513 , A61P25/24 , C07D217/24 , C07D243/08
CPC分类号： C07D403/04 , C07D217/24 , C07D239/91 , C07D401/04 , C07D405/12 , C07D409/04 , C07D409/12 , C07D471/08 , C07D487/04

3. 发明专利

CO6160322A2 DERIVADOS DE QUINAZOLINONA E ISOQUINOLINONA ACETAMIDA 未知
公开(公告)号：CO6160322A2
公开(公告)日：2010-05-20
申请号：CO09036257
申请日：2009-04-08
申请人： ORGANON NV , PHARMACOPEIA LLC
发明人： LETOURNEAU JEFFREY , JOKIEL PATRICK , JURGEN SCHULZ , RATCLIFFE PAUL DAVID , FIONA JEREMIAH , MCARTHUR DUNCAN ROBERT , OHLMEYER MICHAEL , HO KOC-KAN , NAPIER SUSAN ELIZABETH
IPC分类号： C07D239/70
摘要： 1.- Un derivado de quinazolinona o isoquinolinona CARACTERIZADO porque tiene la fórmula I:dondeR1 es C1-6alquilo, C3-6cicloalquilo, C3-6cicloalquil-C1-3alquilo, C2-6alquenilo, C2-6alquinilo, estando dichos C1-6alquilo, C3-6cicloalquilo y C3-6cicloalquilo1-3alquilo opcionalmente sustituidos con hidroxi, C1-6alquiloxi, ciano o uno o más halógenos; R2 es C6-10arilo opcionalmente sustituido con uno a tres sustituyentes seleccionados entre halógeno, hidroxi, ciano, C1-6alquilo, C3-6cicloalquilo, C1-6alquiloxi y C3-6cicloalquiloxi, estando dichos C1-6alquilo, C3-6cicloalquilo, C1-6-alquiloxi y C3-6cicloalquiloxi opcionalmente sustituidos con uno o más halógenos; o R2 es un sistema de anillo heteroarilo de 5-10 miembros que comprende un heteroátomo seleccionado entre N, O y S, y está opcionalmente sustituido con un sustituyente seleccionado entre metilo, C1-6alquiloxi y halógeno; o R2 es C4-7cicloalquilo;R3 es un sustituyente opcional seleccionado entre C1-6alquilo, C1-6alquiloxi y halógeno, estando dichos C1- 6alquilo y C1-6alquiloxi opcionalmente sustituidos con uno o más halógenos; R4 es un grupo ubicado en la posición 6 ó 7 del anillo quinazolinona o isoquinolinona y tiene la fórmula II:dondeR5 junto con uno de R6 forman un anillo heterocíclico saturado o no saturado de 4-8 miembros que opcionalmente comprende una especie heteroatómica adicional seleccionada entre O, S y NR9, estando dicho anillo heterocíclico opcionalmente sustituido con uno o dos sustituyentes seleccionados entre metilo, halógeno, hidroxi y oxo, o R5 junto con uno de R7 y R8 forman un anillo heterocíclico de 6-8 miembros opcionalmente sustituido con uno o dos sustituyentes seleccionados entre metilo, halógeno, hidroxi y oxo; ...

4. 发明专利

AT523500T 未知
公开(公告)号：AT523500T
公开(公告)日：2011-09-15
申请号：AT07842157
申请日：2007-09-10
申请人： ORGANON NV , PHARMACOPEIA LLC
发明人： LETOURNEAU JEFFREY , JOKIEL PATRICK , NAPIER SUSAN , HO KOC-KAN , OHLMEYER MICHAEL , MCARTHUR DUNCAN , FIONA JEREMIAH , RATCLIFFE PAUL , JURGEN SCHULZ
IPC分类号： C07D239/70 , A61K31/472 , A61K31/4725 , A61K31/496 , A61K31/519 , A61K31/5513 , C07D217/24 , C07D243/08
摘要： Disclosed herein are quinazolinone or isoquinolinone derivatives of formula I, or pharmaceutically acceptable salts or solvates thereof, wherein each of the substituents is given the definition as set forth in the specification and claims. Also disclosed are pharmaceutical compositions comprising quinazolinone or isoquinolinone according to the present invention and its use in therapy.

5. 发明专利

AU2007296634A1 Quinazolinone and isoquinolinone acetamide derivatives 未知
公开(公告)号：AU2007296634A1
公开(公告)日：2008-03-20
申请号：AU2007296634
申请日：2007-09-10
申请人： ORGANON NV
发明人： NAPIER SUSAN ELIZABETH , JOKIEL PATRICK , MCARTHUR DUNCAN ROBERT , RATCLIFFE PAUL DAVID , FIONA JEREMIAH , JURGEN SCHULZ , HO KOC-KAN , OHLMEYER MICHAEL , LETOURNEAU JEFFREY
IPC分类号： C07D239/70 , A61K31/472 , A61K31/4725 , A61K31/496 , A61K31/519 , A61K31/5513 , A61P25/24 , C07D217/24 , C07D243/08
摘要： Disclosed herein are quinazolinone or isoquinolinone derivatives of formula I, or pharmaceutically acceptable salts or solvates thereof, wherein each of the substituents is given the definition as set forth in the specification and claims. Also disclosed are pharmaceutical compositions comprising quinazolinone or isoquinolinone according to the present invention and its use in therapy.

6. 发明专利

MX2009002686A DERIVADOS DE ACETAMIDA DE QUINAZOLINONA E ISOQUINOLINONA. 未知
公开(公告)号：MX2009002686A
公开(公告)日：2009-10-13
申请号：MX2009002686
申请日：2007-09-10
申请人： ORGANON NV
发明人： MCARTHUR DUNCAN ROBERT , LETOURNEAU JEFFREY , HO KOC-KAN , OHLMEYER MICHAEL , JOKIEL PATRICK , RATCLIFFE PAUL DAVID , NAPIER ELIZABETH , FIONA JEREMIAH , JURGEN SCHULZ
IPC分类号： A61K31/517 , A61K31/5377 , A61K31/551 , A61P25/00 , C07D401/02 , C07D403/02 , C07D413/14
摘要： La presente invención se refiere a un derivado de quinazolinona o isoquinolinona de la fórmula I, en donde R1 es C1-6alquilo, C3-6clicloalquilo, C3-6cicloalquilC1-3alquilo, C2-6alquenilo, C2-6alquinilo, siendo los C1-6alquilo, C3-6cicloalquilo y C3-6cicloalquilC1-3alquilo opcionalmente sustituidos con hidroxi, C1-6alquiloxi, ciano o uno o más halógenos; R2 es C6-10arilo opcionalmente substituido con de uno a tres sustituyentes seleccionados de halógeno, hidroxi, ciano, C1-6alquilo, C3-6cicloalquilo, C1-6alquiloxi, y C3-6cicloalquiloxi, siendo los C1-6alquilo, C3-6cicloalquilo, C1-6alquiloxi y C3-6Cicloalquiloxi, opcionalmente substituidos con uno o más halógenos; o R2 es un sistema de anillo de heteroarilo de 5 a 10 miembros que comprende un heteroátomo seleccionado de N,O y S, y opcionalmente substituido con un sustituyente seleccionado de metilo, C1-6alquiloxi y halógeno; o R2 es C4-7cicloalquilo; R3 es un sustituyente opcional seleccionado de C1-6alquilo, C1-6alquiloxi y halógeno, siendo el C1-6alquilo y C1-6alquiloxi opcionalmente sustituido con uno o más halógenos; R4 es un grupo localizado en la posición 6- ó 7- del anillo de quinazolinona o isoquinolinona que tiene la fórmula II, en donde R5 junto con uno de R6 forma un anillo heterocíclico saturado o insaturado de 4 a 8 miembros que comprende opcionalmente una porción heteroaromática adicional seleccionada de O, S y NR9, siendo sustituido el anillo heterocíclico con uno o dos sustituyentes seleccionados de metilo, halógeno, hidroxi y oxo o R5 junto con uno de R7 y R8 forma un anillo heterocíclico de 6 a 8 miembros opcionalmente sustituido de uno a dos sustituyentes seleccionados de metilo, halógeno, hidroxi y oxo; cada R6 es independientemente H, halógeno o C1-4alquilo opcionalmente sustituido con halógeno o SO2CH3 o uno de R6 junto con R5 forma un anillo heterocíclico saturado o insaturado de 4 a 8 miembros que comprende opcionalmente una porción heteroaromática adicional seleccionada de O, S y NR9, siendo el anillo heterocíclico opcionalmente sustituido con uno o dos sustituyentes seleccionados de metilo, halógeno, hidroxi y oxo; R7 y R8 son independientemente H, C1-6alquilo, C3-6cilcoalquilo, C3-6cicloalquilC1-3alquilo, cianoC1-3alquilo, C6-10arilo, C6-10arilC1-3alquilo, C1-3alquiloxiC1-3alquilo ó C1-6acilo siendo el C1-6alquilo, C1-3cicloalquilo y C3-6cicloalquilC1-3alquilo opcionalmente sustituido con hidroxi, 1 o más halógenos o diC1-2alquilamino; o R7 y R8 junto con el nitrógeno al cual se enlazan forman un anillo heterocíclico saturado o insaturado de 4 a 8 miembros que comprende opcionalmente una porción heteroatómica adicional seleccionada de O, S y NR10, siendo el anillo heterocíclico opcionalmente substituido con uno o dos sustituyentes seleccionados de C1-6alquilo, halógeno, hidorxi.

7. 发明专利

ECSP099177A DERIVADOS DE QUINAZOLINONA E ISOQUINOLINONA 未知
公开(公告)号：ECSP099177A
公开(公告)日：2009-06-30
申请号：ECSP099177
申请日：2009-03-11
申请人： ORGANON NV , PHARMACOPEIA LLC
发明人： MCARTHUR DUNCAN ROBERT , LETOURNEAU JEFFREY , HO KOC-KAN , OHLMEYER MICHAEL , JOKIEL PATRICK , NAPIER SUSAN ELIZABETH , RATCLIFFE PAUL DAVID , FIONA JEREMIAH , JURGEN SCHULZ
IPC分类号： A61K31/472 , A61P25/24 , C07D239/70
摘要： La presente invención se refiere a un derivado de quinazolinona o isoquinolinona de fórmula I: o una sal o solvato farmacéuticamente aceptable del mismo, donde R1, R2, R3, R4 y X son como se definió en la reivindicación 1. La presente invención se refiere además a una composición farmacéutica que comprende una quinazolinona o isoquinolinona de acuerdo con la presente invención, y a su uso en terapia.

8. 发明专利

CA2663161A1 QUINAZOLINONE AND ISOQUINOLINONE ACETAMIDE DERIVATIVES 未知
公开(公告)号：CA2663161A1
公开(公告)日：2008-03-20
申请号：CA2663161
申请日：2007-09-10
申请人： ORGANON NV , PHARMACOPEIA L L C
发明人： LETOURNEAU JEFFREY , JOKIEL PATRICK , FIONA JEREMIAH , HO KOC-KAN , JURGEN SCHULZ , NAPIER SUSAN ELIZABETH , MCARTHUR DUNCAN ROBERT , OHLMEYER MICHAEL , RATCLIFFE PAUL DAVID
IPC分类号： C07D239/70 , A61K31/472 , A61K31/4725 , A61K31/496 , A61K31/519 , A61K31/5513 , A61P25/24 , C07D217/24 , C07D243/08
摘要： The present invention relates to a quinazolinone or isoquinolinone deriva tive of formula I, wherein R1 is C1-6alkyl, C3-6cycloalkyl, C3-6cycloalkylC1 -3alkyl, C2-6alkenyl, C2-6alkynyl, said C1-6alkyl, C3-6cycloalkyl and C3-6cy cloalkylC1-3alkyl being optionally substituted with hydroxy, C1-6alkyloxy, c yano or one or more halogens; R2 is C6-10aryl optionally substituted with on e to three substituents selected from halogen, hydroxy, cyano, C1-6alkyl, C3 -6cycloalkyl, C1-6alkyloxy and C3-6cycloalkyloxy, said C1-6alkyl, C3-6 cyclo alkyl, C1-6 alkyloxy and C3-6Cycloalkyloxy being optionally substituted with one or more halogens; or R2 is a 5-10 membered heteroaryl ring system compr ising a heteroatom selected from N, O and S and optionally substituted with a substituent selected from methyl, C1-6alkyloxy and halogen; or R2 is C4-7c ycloalkyl; R3 is an optional substituent selected from C1-6alkyl, C1-6alkylo xy and halogen, said C1-6alkyl and C1-6alkyloxy being optionally substituted with one or more halogens; R4 is a group located at the 6- or 7- position o f the quinazolinone or isoquinolinone ring having the formula Il, wherein R5 together with one of R6 forms a 4-8 membered saturated or unsaturated heter ocyclic ring optionally comprising a further heteroatomic moiety selected fr om O, S and NR9, said heterocyclic ring being optionally substituted with on e or two substituents selected from methyl, halogen, hydroxy and oxo or R5 t ogether with one of R7 and R8 forms a 6-8 membered heterocyclic ring optiona lly substituted with one or two substituents selected from methyl, halogen, hydroxy and oxo; Each R6 is independently H, halogen or C1-4alkyl optionally substituted with halogen or SO2CH3 or one of R6 together with R5 forms a 4- 8 membered saturated or unsaturated heterocyclic ring optionally comprising a further heteroatomic moiety selected from O, S and NR9, said heterocyclic ring being optionally substituted with one or two substituents selected from methyl, halogen, hydroxy and oxo; R7 and R8 are independently H, C1-6alkyl, C3-6cycloalkyl, C3-6cycloalkylc1-3alkyl, cyanoC1-3alkyl, C6-10aryl, C6-10ar ylC1-3alkyl, C1-3alkyloxyC1-3alkyl or C1-6acyl said C1-6alkyl, C3-6cycloalky l and C3-6cycloalkylC1-3alkyl being optionally substituted with hydroxy, 1 o r more halogens or diC1-2alkylamino; or R7 and R8 together with the nitrogen to which they are bonded form a 4-8 membered saturated or unsaturated heter ocyclic ring optionally comprising a further heteroatomic moiety selected fr om O, S and NR10, said heterocyclic ring being optionally substituted with o ne or two substituents selected from C1-6alkyl, halogen, hydroxy,

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