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1. 发明申请

WO2010015518A2 4-DIMETHYLAMINO-PHENYL-SUBSTITUTED NAPHTHYRIDINES, AND USE THEREOF AS MEDICAMENTS 审中-公开
标题翻译： 4二甲氨基 - 取代萘啶及其作为药物
公开(公告)号：WO2010015518A2
公开(公告)日：2010-02-11
申请号：PCT/EP2009059493
申请日：2009-07-23
申请人： BOEHRINGER INGELHEIM INT , FIEGEN DENNIS , HANDSCHUH SANDRA , HOBBIE SILKE , HOFFMANN MATTHIAS , KONO TAKESHI , SATO YAYOI , SCHNAPP ANDREAS , SCHULER-METZ ANNETTE
发明人： FIEGEN DENNIS , HANDSCHUH SANDRA , HOBBIE SILKE , HOFFMANN MATTHIAS , KONO TAKESHI , SATO YAYOI , SCHNAPP ANDREAS , SCHULER-METZ ANNETTE
IPC分类号： C07D471/04 , A61K31/4375 , A61P11/06 , C07D519/00
CPC分类号： C07D471/04 , C07D519/00
摘要： The invention relates to novel substituted naphthyridines of formula 1 as well as pharmacologically acceptable salts, diastereomers, enantiomers, racemates, hydrates, or solvates thereof. In formula 1, R1 can represent a group A selected from among the group comprising -O-R3, -NR3 R4, -CR3 R4 R5,-(ethyne)-R3, -S-R3, -SO-R3, and SO2 -R3, or R1 represents a group B selected from among the group comprising: - C6-10-aryl; - a five-membered to ten-membered, monocyclic or bicyclic heteroaryl containing 1 to 3 heteroatoms independently selected from among the group comprising N, O, and S, wherein said heteroaryl is linked to the structure according to formula 1 via a C atom or an N atom; - a three-membered to ten-membered, monocyclic or bicyclic, saturated or partially saturated heterocycle containing 1 to 3 heteroatoms independently selected from among the group comprising N, O, and S, wherein said heterocycle is linked to the structure according to formula 1 via a C atom or an N atom; and - a 5-membered to 11-membered spiro group which can optionally contain 1, 2, or 3 heteroatoms independently selected from among the group comprising N, O, and S, wherein said spiro group is linked to the structure according to formula 1 via a C atom or an N atom, wherein said group B can be optionally substituted as described in claim 1, and R3,R4,R5, R6, and m can have the meanings indicated in claim 1. The invention also relates to pharmaceutical compositions containing said compounds.
摘要翻译：本发明涉及式1的新的取代的萘啶，以及其药理学上可接受的盐，非对映体，对映体，外消旋体，水合物或溶剂合物，其中R 1是选自-O-R 3，-NR 3 R 4，-CR 3 R 4 R组成的组中选择的基团A 5 ， - （乙炔）-R 3，-S-R 3，-SO-R 3，和SO 2 -R 3或R 1是基团B选自的组中选择 - C6-10芳基， - 五到十元单环或双环杂芳基具有选自N，O和S的组中独立选择的1-3个杂原子; 其中所述杂芳基或者通过一个C原子或通过N原子连接的，具有以下结构的根据式1， - 三至具有从所述组独立地选自1-3个杂原子至十元单环或双环，饱和或部分饱和的杂环选自N，O和S，其中所述杂环或者通过一个C原子或通过N原子连接的，具有以下结构的根据式1，以及 - 5-至11-元螺环基团，任选地含有1,2或 3可以是选自N，O和S的组中独立选择的杂原子，所述螺环基团则通过一个C原子或通过N原子连接的，具有以下结构的根据式1，其中所述残基B是任选地作为可以如权利要求1，其中R3，R4，R5，R6和m可以具有权利要求1中所述的含义，以及含有这些化合物的药物组合物中所述被取代。

2. 发明专利

CA2732087A1 SUBSTITUTED NAPHTHYRIDINES AND THEIR USE AS MEDICAMENTS 未知
公开(公告)号：CA2732087A1
公开(公告)日：2010-02-11
申请号：CA2732087
申请日：2009-07-23
申请人： BOEHRINGER INGELHEIM INT
发明人： BOUYSSOU THIERRY , DAHMANN GEORG , ENGELHARDT HARALD , FIEGEN DENNIS , HANDSCHUH SANDRA , HOBBIE SILKE , HOFFMANN MATTHIAS , KONO TAKESHI , REISER ULRICH , SATO YAYOI , SCHNAPP ANDREAS , SCHULER-METZ ANNETTE
IPC分类号： C07D471/04 , A61K31/4375 , A61P11/00 , A61P11/06 , A61P17/00 , A61P19/00 , A61P19/10 , C07D487/04 , C07D487/10 , C07D513/04
摘要： The invention relates to novel substituted naphthyridines of the formula (1) and to pharmacologically compatible salts, diastereomers, enantiomers, racemates, hydrates or solvates thereof, where R2 and where R1 can be a radical A or R1 can be a radical B as described in claim 1 and where R3, R4, R5, R6, R6', R7, R8, R9, R10, V, n and m can have the meanings indicated in claim 1, and pharmaceutical compositions containing these compounds.

3. 发明专利

AR072913A1 NAFTIRIDINAS SUSTITUIDAS Y SU UTILIZACION COMO MEDICAMENTO 未知
公开(公告)号：AR072913A1
公开(公告)日：2010-09-29
申请号：ARP090102993
申请日：2009-08-04
申请人： BOEHRINGER INGELHEIM INT
发明人： SATO YAYOI , HOBBIE SILKE , HOFFMANN MATTHIAS , REISER ULRICH , SCHNAPP ANDREAS , SCHULER-METZ ANNETTE , BOUYSSOU THIERRY , ENGELHARDT HARALD , HANDSCHUH SANDRA , FIEGEN DENNIS , DAHMANN GEORG , KONO TAKESHI
IPC分类号： C07D471/04 , A61K31/4375 , A61P11/00
摘要： Las composiciones farmacéuticas que contienen estos compuestos. Reivindicacion 1: Compuestos caracterizados porque tienen la formula (1) en donde significa R1 un radical A seleccionado del grupo constituido por -O-R3, -NR3R4, -CR3R4R5. -(etino)-R3, S-R3, -SO-R3 y SO2-R3 o R1 un radical B seleccionado del grupo constituido por -arilo C6-10, un heteroarilo mono o bicíclico, con cinco a diez miembros, con 1-3 heteroátomos seleccionados independientemente entre sí del grupo constituido por N, O y S; en donde este heteroarilo está enlazado bien sea a través de un átomo de C o a través de un átomo de N con la estructura segun la formula (1), un heterociclo mono o bicíclico, con tres a diez miembros, saturado o parcialmente saturado, con 1-3 heteroátomos seleccionados independientemente entre sí del grupo constituido por N, O y S, en donde este heterociclo está enlazado bien sea a través de un átomo de C o a través de un átomo de N con la estructura segun la formula (1), y un grupo espiro con 5 a 11 miembros, el cual puede contener eventualmente 1, 2 o 3 heteroátomos seleccionados independientemente entre sí del grupo constituido por N, O y S, en donde este grupo espiro está enlazado bien sea a través de un átomo de C o a través de un átomo de N con la estructura segun la formula (1), pudiendo estar sustituido este radical B eventualmente con uno o varios radicales seleccionados independientemente entre sí del grupo constituido por H, halogeno alquilo C1-3, -NH(alquilo C1-4), -N(alquilo C1-4)2, -NH2, alquilo C1-3-OH, -OH, Oxo, -CO-NH2, alquilen C1-3-CO-NH2 -CO-NH-alquilo C1-3, alquileno C1-3-CO-NH(alquilo C1-3), -CO-NH(cicloalquilo C3-5), alquilen C1-3-CO-NH(cicloalquilo C3-5), -NH-CO-NH2, -NH-CO-NH(alquilo C1-3), -NH-CO-N(alquilo C1-3)2, O-alquilo C1-3, -alquileno C1-3-NH2, -fenilo y -CO-alquilo C1-5 en donde R2 significa el compuesto de formula (2) en donde significa V: CH2, O, NH, S, SO, SO2, N-alquilo C1-3, N-aIquileno C1-3-cicloalquilo C3-7, N-cicloalquilo C3-7, N-CO-alquilo C1-6, N-CO-cicloalquilo C3-7, N-alquileno C1-3-fenilo; n = 0-2; R6 y R6' se seleccionan independientemente entre sí del grupo constituido por H, halogeno, metilo, -O-metilo, etilo, -O-etilo, propilo, -O-propilo, OH, =O, -CO-NH2, -CO-NH-alquilo C1-3, -COOH, -COO-alquilo C1-3; R7, R8, R9 y R10 H, alquilo C1-3, -O-alquilo C1-3, F, =O u OH, R3 H o un radical que se selecciona del grupo constituido por alquilo C1-6, fluoroalquilo C1-6, -alquil C1-5-OH, arilo C6-10, alquilen C1-4-arilo C6-10, -etenilo, alquilen C1-4-(eteno), -etinilo, -alquilen C1-4-(etino), -alquilen C1-4-(etino)-NH2, alquilen C1-4-(etino)-alquilen C1-4-NH2, -CHOH-alquilen C1-4-NH2, -alquilen C1-4-CHOH-alquilen C1-4-NH2, -CHOH-NH2, -alquilen C1-4-CHOH-NH2, -NH(alquilen C1-3), -(alquilen C1-4-NH(alquilo C1-3, cicloalquilo C3-10, mono- o bicíclico, saturado o parcialmente saturado, -alquilen C1-4-cicloalquilo C3-10 mono- o bicíclico, saturado o parcialmente saturado, -Het, -alquilen C1-4-Het, -Hetarilo, y alquilen C1-4-heteroarilo pudiendo estar sustituido este radical eventualmente con uno o varios radicales seleccionados independientemente entre sí del grupo constituido por H, -OH. -Oxo, COOH, -halogeno, -alquilo C1-3, -haloalquilo C1-3, -alquil C1-3-OH, -cicloalquilo C3-7, O-alquilo C1-4, -NH(alquilo C1-4, -alquenilo C1-4-NH(alquilo C1-4), -N(alquilo C1-4)2, -alquilen C1-4-N(alquilo C1-4)2, -NH-CO-NH2, -alquileno C1-4-NH-CO-NH2, -CO-NH2, -alquileno C1-4-CO-NH2, -CO-NH(alquilo C1-3), -alquileno C1-4-CO-NH(alquilo C1-3), -CO-N(alquilo C1-3)2, -alquilen C1-4-CO-N(alquilo C1-3)2, -NH-(CO)m-NH2, -NH-alquilen C1-4-(CO)m-NH2, -NH-(CO)m-NH(alquilo C1-3), -NH-(alquilen C1-4)-(CO)m-NH(alquilo C1-3), -NH-(CO)m-N(alquilo C1-3)2, -NH-alquileno C1-4-(CO)m-N(alquilo C1-3), -O-alquilen C2-4-NH2, -O-alquilen C2-4-NH(alquilo C1-3), -O-alquilen C2-4-N(alquilo C1-3)2, -NH-CO-alquilo C1-3, -alquilen C1-4-NH-CO-alquilo C1-3, -cicloalquilo C3-5, -NH-SO2-alquilo C1-4, -SO2-alquilo C1-4, -SO2-cicloalquilo C3-5, -SO2-NH2, -SO2-NH-alquilo C1-3, -SO2-N(alquilo)3 , -SO2-Het, -O-Het, -O-alquilen C1-4-Het, -NH-Het, -NH-alquilen C1-4-Het, -NH-hetarilo, -NH-alquilen C1-4-Hetarilo, -Het, -alquilen C1-4-Het, representando Het un heterociclo con tres a diez miembros, saturado o parcialmente saturado, mono- o bicíclico, sustituido eventualmente con 1-3 radicales seleccionados de alquilo C1-3, halogeno, CH2-NH2, NH2, OH; CO-NH2 y oxo el cual contiene 1-3 heteroátomos seleccionados independientemente entre sí del grupo constituido por N, O y S, y representando Hetaril un heteroarilo con cinco a diez miembros, mono- o bicíclico, sustituido eventualmente con 1-3 radicales seleccionados de alquilo C1-3, halogeno, CH2-NH2, NH2, OH, CO-NH2 y oxo, el cual contiene 1-3 heteroátomos seleccionados independientemente entre sí del grupo constituido por N, O y S, m = 0 o 1, R4 y R5 significan H, metilo o etilo, y sales farmacologicamente tolerables de los mismos.

4. 发明专利

CA2731926A1 4-DIMETHYLAMINO-PHENYL-SUBSTITUTED NAPHTHYRIDINES, AND USE THEREOF AS MEDICAMENTS 未知
公开(公告)号：CA2731926A1
公开(公告)日：2010-02-11
申请号：CA2731926
申请日：2009-07-23
申请人： BOEHRINGER INGELHEIM INT
发明人： FIEGEN DENNIS , HANDSCHUH SANDRA , HOBBIE SILKE , HOFFMANN MATTHIAS , KONO TAKESHI , SATO YAYOI , SCHNAPP ANDREAS , SCHULER-METZ ANNETTE
IPC分类号： C07D471/04 , A61K31/4375 , A61P11/06 , C07D519/00
摘要： The invention relates to novel substituted naphthyridines of formula 1 as well as pharmacologically acceptable salts, diastereomers, enantiomers, racemates, hydrates, or solvates thereof. In formula 1, R1 can represent a group A selected from among the group comprising -O-R3, -NR3 R4, -CR3 R4 R5,-(ethyne)-R3, -S-R3, -SO-R3, and SO2 -R3, or R1 represents a group B selected from among the group comprising: - C6-10-aryl; - a five-membered to ten-membered, monocyclic or bicyclic heteroaryl containing 1 to 3 heteroatoms independently selected from among the group comprising N, O, and S, wherein said heteroaryl is linked to the structure according to formula 1 via a C atom or an N atom; - a three-membered to ten-membered, monocyclic or bicyclic, saturated or partially saturated heterocycle containing 1 to 3 heteroatoms independently selected from among the group comprising N, O, and S, wherein said heterocycle is linked to the structure according to formula 1 via a C atom or an N atom; and - a 5-membered to 11-membered spiro group which can optionally contain 1, 2, or 3 heteroatoms independently selected from among the group comprising N, O, and S, wherein said spiro group is linked to the structure according to formula 1 via a C atom or an N atom, wherein said group B can be optionally substituted as described in claim 1, and R3,R4,R5, R6, and m can have the meanings indicated in claim 1. The invention also relates to pharmaceutical compositions containing said compounds.

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