BICYCLIC NITROGENATED HETEROCYCLIC DERIVATIVE AND PHARMACEUTICAL COMPOSITION CONTAINING SAME

    公开(公告)号:EP3527568A1

    公开(公告)日:2019-08-21

    申请号:EP17863024.0

    申请日:2017-10-16

    摘要: Provided are a novel compound having an antagonistic activity for the P2X 7 receptor, and a pharmaceutical composition having an antagonistic activity for the P2X 7 receptor. A compound represented by Formula (I):

    wherein Z 1 is C(R 4 ) or the like; R 4 is a hydrogen atom or the like; Z 2 is C(R 5a )(R 5a' ) or the like; the dashed line represents the presence or absence of a bond; when the dashed line represents the presence of a bond, then R 5a' is absent; R 5a and R 5a' are each independently a hydrogen atom or the like; Ring Q is a substituted or unsubstituted 5-membered non-aromatic heterocycle or the like; Y 1 is O or the like; R 2a is a group represented by the formula: -(C(R 2a' )(R 2b' )) n -R 1 ; R 2b is a hydrogen atom or the like; R 2a' and R 2b' is each independently a hydrogen atom or the like; R 1 is substituted or unsubstituted aromatic carbocyclyl or the like; X is N(R 7a ) or the like; R 7a is a hydrogen atom or the like; R 3 is substituted or unsubstituted aromatic carbocyclyl or the like; n is an integer from 0 to 4; and m is an integer from 0 to 4, or a pharmaceutically acceptable salt thereof.

    SUSTAINED HIV PROTEASE INHIBITOR
    2.
    发明公开
    SUSTAINED HIV PROTEASE INHIBITOR 审中-公开
    持久的HIV蛋白酶抑制剂

    公开(公告)号:EP3192794A1

    公开(公告)日:2017-07-19

    申请号:EP15839901.4

    申请日:2015-09-10

    摘要: The present invention provides useful compounds for HIV protease inhibitor. A compound represented by formula or its pharmaceutically acceptable salt Formula:

    wherein ring A is

    R 4 is -Y-Z, hydrogen atom, halogen, hydroxy and the like,
    R 5 is hydrogen atom, halogen, hydroxy and the like,
    R 6 is each independently halogen, hydroxy, carboxy and the like,
    ring A may be substituted with said R 6 at any substitutable position(s),
    a is an integer of 0 to 7,
    ring B is substituted or unsubstituted aromatic carbocyclyl, or substituted or unsubstituted aromatic heterocyclyl,
    ring C is substituted or unsubstituted aromatic carbocyclyl, substituted or unsubstituted non-aromatic carbocyclyl, substituted or unsubstituted aromatic heterocyclyl, or substituted or unsubstituted non-aromatic heterocyclyl,
    R 1 is -Y-Z, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl and the like,
    R 2 and R 3 are each independently -Y-Z or hydrogen atom,
    provided that at least one of R 1 , R 2 , R 3 and R 4 is a group represented by formula: -Y-Z,
    Y is a bond, or a spacer of any combination selected from the group consisting of -O-, -S-, -NR 7 -, -C(=O)-, -SO-, -SO 2 -, -NR 7 -C(=O)-, -C(=O)-NR 7 -, -NR 7 -C(=O)-NR 7 -, -NR 7 -C(=O)-O-, -SO 2 -NR 7 -, -NR 7 -SO 2 -, substituted or unsubstituted alkylene, substituted or unsubstituted alkenylene, substituted or unsubstituted alkynylene, substituted or unsubstituted aromatic carbocyclediyl, substituted or unsubstituted non-aromatic carbocyclediyl, substituted or unsubstituted aromatic heterocyclediyl and substituted or unsubstituted non-aromatic heterocyclediyl,
    R 7 are each independently hydrogen atom, hydroxy, carboxy and the like, and
    Z is substituted aromatic carbocyclyl, substituted non-aromatic carbocyclyl, substituted aromatic heterocyclyl or substituted non-aromatic heterocyclyl.

    摘要翻译: 本发明提供了用于HIV蛋白酶抑制剂的有用化合物。 由式或其药学上可接受的盐表示的化合物或其药学上可接受的盐式:其中环A为R 4为-YZ,氢原子,卤素,羟基等,R 5为氢原子,卤素,羟基等,R 6各自独立地为卤素,羟基 ,羧基等,环A可以在任何可取代的位置被所述R6取代,a是0-7的整数,环B是取代或未取代的芳族碳环基或取代或未取代的芳族杂环基,环C是 取代或未取代的芳族碳环基,取代或未取代的非芳族碳环基,取代或未取代的芳族杂环基或取代或未取代的非芳族杂环基,R1是-YZ,取代或未取代的烷基,取代或未取代的烯基, 例如,R2和R3各自独立地是-YZ或氢原子,条件是R1,R2,R3和R4中的至少一个是由式-YZ表示的基团, Y是键,或选自-O - , - S - , - NR 7 - , - C(= O) - , - SO - , - SO 2 - , - NR 7 -C (= O)-NR 7 - , - NR 7 -C(= O)-NR 7 - , - NR 7 -C(= O)-O - , - SO 2 -NR 7 - ,取代或未取代的亚烷基,取代或未取代的亚烯基,取代或未取代的亚炔基,取代或未取代的芳族碳环基,取代或未取代的非芳族碳环基,取代或未取代的芳族杂环二基和取代或未取代的非芳族杂环二基, ,羟基,羧基等,Z是取代的芳族碳环基,取代的非芳族碳环基,取代的芳族杂环基或取代的非芳族杂环基。

    OXADIAZOLE DERIVATIVE HAVING ENDOTHELIAL LIPASE INHIBITORY ACTIVITY
    3.
    发明公开
    OXADIAZOLE DERIVATIVE HAVING ENDOTHELIAL LIPASE INHIBITORY ACTIVITY 有权
    OXADIAZOLDERIVAT MIT ENDOTHELIALLIPASE-HEMMENDER WIRKUNG

    公开(公告)号:EP2514749A1

    公开(公告)日:2012-10-24

    申请号:EP10837586.6

    申请日:2010-12-14

    摘要: Disclosed is a compound which is useful as an endothelial lipase inhibitor.
    A compound represented by the formula:

    its pharmaceutically acceptable salt, or a solvate thereof,
    wherein
    Ring A is aromatic carbocycle or aromatic heterocycle,
    Z is -NR 5 -, -O- or -S-,
    R 5 is hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted aryl or the like,
    R 1 is hydrogen, halogen, hydroxy, cyano, nitro, carboxy, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl or the like,
    R 2 and R 3 are each independently hydrogen, halogen, hydroxy or the like,
    R 4 is a group represented by the formula: -(CR 6 R 7 )n-R 8 ,
    wherein R 6 and R 7 are each independently hydrogen, halogen, hydroxy or the like, n is an integer of 0 to 3, R 8 is carboxy, cyano, substituted or unsubstituted alkyl or the like,
    R x is halogen, hydroxy, cyano, nitro, carboxy, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl or the like,
    m is an integer of 0 to 3.

    摘要翻译: 公开了可用作内皮脂肪酶抑制剂的化合物。 由下式表示的化合物:其药学上可接受的盐或其溶剂合物,其中环A是芳族碳环或芳族杂环,Z是-NR 5 - , - O-或-S-,R 5是氢,取代或未取代的 烷基,取代或未取代的烯基,取代或未取代的炔基,取代或未取代的芳基等,R 1为氢,卤素,羟基,氰基,硝基,羧基,取代或未取代的烷基,取代或未取代的链烯基等 和R 3各自独立地为氢,卤素,羟基等,R 4为下式所示的基团: - (CR 6 R 7)n R 8,其中R 6和R 7各自独立地为氢,卤素,羟基或 n为0〜3的整数,R 8为羧基,氰基,取代或未取代的烷基等,R x为卤素,羟基,氰基,硝基,羧基,取代或未取代的烷基,取代或未取代的链烯基或 m为0〜3的整数。

    ISOXAZOLE DERIVATIVE AND ISOTHIAZOLE DERIVATIVE HAVING INHIBITORY ACTIVITY ON 11 BETA -HYDROXYSTEROID DEHYDROGENASE TYPE I
    6.
    发明公开
    ISOXAZOLE DERIVATIVE AND ISOTHIAZOLE DERIVATIVE HAVING INHIBITORY ACTIVITY ON 11 BETA -HYDROXYSTEROID DEHYDROGENASE TYPE I 审中-公开
    ISOXAZOLDERIVAT UND ISOTHIAZOLDERIVAT MIT HEMMENDER WIRKUNG AUF DIE 11 BETA-HYDROXYSTEROIDDEHYDROGENASE VOM TYP I

    公开(公告)号:EP2006286A2

    公开(公告)日:2008-12-24

    申请号:EP07739976.4

    申请日:2007-03-28

    摘要: Disclosed is a compound useful as an inhibitor of 11β-hydroxysteroid dehydrogenase type 1.
    A compound represented by the formula:

    a pharmaceutically acceptable salt or solvate thereof,
    wherein
    R 1 is a group of the formula: -C(=O)NR 4 R 5 ,
    (wherein R 4 and R 5 are each independently, hydrogen, optionally substituted alkyl or the like) or
    a group of the formula: -NR 6 C(=O)R 7 ,
    (wherein R 6 and R 7 are each independently, hydrogen, optionally substituted alkyl or the like),
    X and Y are each independently -0- or the like,
    Z is a bond or the like,
    R 2 is optionally substituted alkyl, optionally substituted alkenyl or the like,
    R 3 is optionally substituted alkyl, optionally substituted alkenyl or the like.

    摘要翻译: 公开了用作11β-羟基类固醇脱氢酶1型抑制剂的化合物。下式表示的化合物:其药学上可接受的盐或溶剂化物,其中R 1是下式的基团-C(= O)NR 4 R 5,(其中R 4和R 5各自独立地为氢,任选取代的烷基等)或下式-NR 6 C(= O)R 7基团(其中R 6和R 7各自独立地为 ,氢,任选取代的烷基等),X和Y各自独立地为-O-等,Z为键或类似物,R 2为任选取代的烷基,任选取代的烯基等,R 3为任选取代的 取代的烷基,任选取代的烯基等。