Novel compounds
    2.
    发明公开
    Novel compounds 失效
    新化合物

    公开(公告)号:EP0363085A3

    公开(公告)日:1991-03-27

    申请号:EP89309920.0

    申请日:1989-09-28

    申请人: BEECHAM GROUP PLC

    摘要: A compound of formula (I) or a pharmaceutically acceptable salt thereof:
    in which one of X and Y represents hydrogen and the other represents -CH₂-Z where Z is a group
    in which Q represents a 3-membered divalent residue completing a 5-membered aromatic ring and comprises one or two heteroatoms selected from oxygen, nitrogen and sulphur, or three nitrogen atoms, any amino nitrogen being optionally substituted by a C₁₋₂ alkyl, cyclopropyl or propargyl group, and any ring carbon atom being optionally substituted by a group R₁; or a group
    in which A₁, A₂ and A₃ complete a 5-membered aromatic ring and A₁ is oxygen or sulphur, one of A₂ and A₃ is CR₂ and the other is nitrogen or CR₃, or A₂ is oxygen or sulphur, one of A₁ and A₃ is CR₂ and the other is CR₃; and R₁, R₂ and R₃ independently selected from hydrogen, halogen, CN, OR₄, SR₄ N(R₄)₂, NHCOR₄, NHCOOCH₃, NHCOOC₂H₅, NHOR₄, NHNH₂, NO₂, COR₄, COR₅, C₂₋₄alkenyl, C₂₋₄ alkynyl, cyclopropyl or C₁₋₂ alkyl optionally substituted with OR₄, N(R₄)₂, SR₄, CO₂R₄, CON(R₄)₂ or one, two or three halogen atoms, in which each R₄ is independently hydrogen or C₁₋₂ alkyl and R₅ is OR₄, NH₂ or NHR₄; r represents an integer of 2 or 3, s represents an integer of 1 or 2 and t represents 0 or 1, with the proviso that when Y is hydrogen s is 1.

    摘要翻译: 式(Ⅰ)化合物或其药学上可接受的盐:其中X和Y中的一个代表氢而另一个代表-CH 2 -Z,其中Z是其中Q代表完成5-元杂环的3元二价残基的基团, 其包含一个或两个选自氧,氮和硫或三个氮原子的杂原子,任意氨基氮任选被C 1-2烷基,环丙基或炔丙基取代,并且任何环碳原子任选被 基团R 1; 或其中A 1,A 2和A 3完成5元芳族环并且A 1是氧或硫的基团,A 2和A 3中的一个是CR 2,另一个是氮或CR 3,或A 2是氧或硫,A 1和 A 3是CR 2,另一个是CR 3; (R 4)2,NHCOR 4,NHCOOCH 3,NHCOOC 2 H 5,NHOR 4,NHNH 2,NO 2,COR 4,COR 5,C 2-4链烯基,C 2-4炔基,环丙基, 或任意被OR 4,N(R 4)2,SR 4,CO 2 R 4,CON(R 4)2或1,2或3个卤素原子取代的C 1-2烷基,其中每个R 4独立地是氢或C 1-2烷基,R 5是OR 4 ,NH 2或NHR 4; r表示2或3的整数,s表示1或2的整数,并且t表示0或1,条件是当Y是氢时,s是1。

    Novel compounds
    3.
    发明公开
    Novel compounds 失效
    Chemische Verbindungen。

    公开(公告)号:EP0363085A2

    公开(公告)日:1990-04-11

    申请号:EP89309920.0

    申请日:1989-09-28

    申请人: BEECHAM GROUP PLC

    摘要: A compound of formula (I) or a pharmaceutically acceptable salt thereof:
    in which one of X and Y represents hydrogen and the other represents -CH₂-Z where Z is a group
    in which Q represents a 3-membered divalent residue completing a 5-membered aromatic ring and comprises one or two heteroatoms selected from oxygen, nitrogen and sulphur, or three nitrogen atoms, any amino nitrogen being optionally substituted by a C₁₋₂ alkyl, cyclopropyl or propargyl group, and any ring carbon atom being optionally substituted by a group R₁; or a group
    in which A₁, A₂ and A₃ complete a 5-membered aromatic ring and A₁ is oxygen or sulphur, one of A₂ and A₃ is CR₂ and the other is nitrogen or CR₃, or A₂ is oxygen or sulphur, one of A₁ and A₃ is CR₂ and the other is CR₃; and R₁, R₂ and R₃ independently selected from hydrogen, halogen, CN, OR₄, SR₄ N(R₄)₂, NHCOR₄, NHCOOCH₃, NHCOOC₂H₅, NHOR₄, NHNH₂, NO₂, COR₄, COR₅, C₂₋₄alkenyl, C₂₋₄ alkynyl, cyclopropyl or C₁₋₂ alkyl optionally substituted with OR₄, N(R₄)₂, SR₄, CO₂R₄, CON(R₄)₂ or one, two or three halogen atoms, in which each R₄ is independently hydrogen or C₁₋₂ alkyl and R₅ is OR₄, NH₂ or NHR₄; r represents an integer of 2 or 3, s represents an integer of 1 or 2 and t represents 0 or 1, with the proviso that when Y is hydrogen s is 1.

    摘要翻译: 式(I)化合物或其药学上可接受的盐:其中X和Y中的一个代表氢,另一个表示-CH 2 -Z,其中Z是基团其中Q表示3元 二价残基完成5元芳环,并且包含一个或两个选自氧,氮和硫的杂原子,或三个氮原子,任选被C 1-2烷基,环丙基或炔丙基取代的任何氨基氮,以及任何环碳 任选被基团R 1取代的原子; 或其中A1,A2和A3完成5元芳环并且A1为氧或硫的基团,A2和A3之一为CR2,另一个为氮或CR 3,或A2为氧或硫,一 A1和A3是CR2,另一个是CR3; 和R 1,R 2和R 3独立地选自氢,卤素,CN,OR 4,SR 4 N(R 4)2,NHCOR 4,NHCOOCH 3,NHCOOC 2 H 5,NHOR 4,NHNH 2,NO 2,COR 4,COR 5,C 2-4链烯基,C 2-4炔基, 或任选被OR 4,N(R 4)2,SR 4,CO 2 R 4,CON(R 4)2或一个,两个或三个卤素原子取代的C 1-2烷基,其中每个R 4独立地是氢或C 1-2烷基,R 5是OR 4 ,NH2或NHR4; r表示2或3的整数,s表示1或2的整数,t表示0或1,条件是当Y为氢时,s为1。

    Azabicyclic compounds, process for their preparation and pharmaceutical compositions containing them
    6.
    发明公开
    Azabicyclic compounds, process for their preparation and pharmaceutical compositions containing them 失效
    氮杂双环化合物,其制备方法和含有它们的药物组合物。

    公开(公告)号:EP0322182A2

    公开(公告)日:1989-06-28

    申请号:EP88312038.8

    申请日:1988-12-19

    申请人: BEECHAM GROUP PLC

    CPC分类号: C07D487/08 C07D453/02

    摘要: Novel compounds of formula (I), processes for their preparation, and their use as pharmaceutical agents are described:
    in which p represents an integer of 2 to 4; r represents an integer of 1 or 2; s represents 0 or 1; and X represents a group
    in which A₁ is oxygen or sulphur, one of A₂ and A₃ is CR₁ and the other is nitrogen or CR₂, or A₂ is oxygen or sulphur, A₁ is CH and A₃ is CR₁, where R₁ and R₂ are independently selected from hydrogen and C₁₋₂ alkyl, with the proviso that when r is 2, R₁ and R₂ are hydrogen or methyl.

    摘要翻译: 式(I)的新的化合物,它们的制备方法以及它们作为药物的用途进行了说明:其中p darstellt为2至4的整数; řdarstellt上的1或2整数; 小号darstellt 0或1; 和X darstellt一组中A 1是氧或硫,A2中的一个和A3是CR1且另一个是氮或CR 2,或A 2是氧或硫,A 1为CH和A 3是CR 1,其中R1和R2 独立地选自氢和C 1-2烷基,其条件没有当r是2,R1和R2是氢或甲基。

    Heterocyclic compounds, process for their preparation and pharmaceutical compositions containing them
    8.
    发明公开
    Heterocyclic compounds, process for their preparation and pharmaceutical compositions containing them 失效
    杂环化合物,它们的制备方法和含有它们的药物组合物。

    公开(公告)号:EP0339834A2

    公开(公告)日:1989-11-02

    申请号:EP89303653.3

    申请日:1989-04-13

    申请人: BEECHAM GROUP PLC

    CPC分类号: C07D471/08 C07D487/08

    摘要: Novel compounds of formula (I), processes for their preparation, and their use as pharmaceutical agents are described:
    in which X represents a group
    wherein one of Y and Z represents nitrogen and the other represents CR where R is selected from halogen, CN, OR¹, SR¹, N(R¹)₂, NHR¹, NHCOR¹, NHCOOCH₃, NHCOOC₂H₅, NHOR¹, NHNH₂, COR¹, COR², C₂₋₄ alkenyl, C₂₋₄ alkynyl or C₁₋₂ alkyl substituted with OR¹, N(R¹)₂, SR¹, CO₂R¹, CON(R¹)₂ or one or two halogen atoms, in which R¹ is hydrogen or C₁₋₂ alkyl and R² is OR¹, NH₂ or NHR¹; and each of p and q independently represents an integer of 2 to 4.

    摘要翻译: 式(I)的新的化合物,它们的制备方法以及它们作为药物的用途进行了说明:其中x darstellt的基团 worin的Y一个和Z darstellt氮,其它的darstellt CR,其中R为 选自卤素,CN,OR <1>,SR <1>,N(R <1>)2,NHR <1>,NHCOR <1>,NHCOOCH3,NHCOOC2H5,NHOR <1>,NHNH 2,COR <1>中选择 ,COR <2>,C2-4链烯基,C 2-4炔基或具有或取代的C 1-2烷基<1>,N(R <1>)2,SR <1>,CO 2 <1>,CON(R < 1>)2或一个或两个卤素原子,其中R <1>是氢或C 1-2烷基且R <2>是或<1>,NH 2或NHR <1>; 且每个p和qunabhängigdarstellt至第四的2个整数的

    Bridgehead substituted azabicyclic derivatives
    9.
    发明公开
    Bridgehead substituted azabicyclic derivatives 失效
    桥头取代的氮杂双环衍生物

    公开(公告)号:EP0287356A2

    公开(公告)日:1988-10-19

    申请号:EP88303334.2

    申请日:1988-04-13

    申请人: BEECHAM GROUP PLC

    CPC分类号: C07D471/08 C07D487/08

    摘要: A compound of formula (I) or a pharmaceutically acceptable salt thereof:
    in which X represents R₁OOC- in which R₁ is C₁₋₄ alkyl, C₂₋₄ alkenyl or C₂₋₄ alkynyl; R₂O- in which R₂ is C₁₋₂ alkyl, C₁₋₂ alkylcarbonyl or aminocarbonyl optionally substituted by one or two methyl groups;

    a group
    in which Y represents a 3-membered divalent residue completing a 5-membered aromatic ring and comprises one or two heteroatoms selected from oxygen, nitrogen and sulphur, any amino nitrogen optionally substituted by a C₁₋₂ alkyl group, Y being optionally C-substituted by a methyl group; or a group
    in which A₁ is oxygen or sulphur, one of A₂ and A₃ is CR₃ and the other is nitrogen or CR₄ where R₃ and R₄ are independently selected from hydrogen and methyl; and each of p and q independently represents an integer of 2 to 4.

    摘要翻译: 式(Ⅰ)化合物或其药学上可接受的盐:其中X代表R10OC-,其中R 1是C 1-4烷基,C 2-4链烯基或C 2-4炔基; R 2 O-(其中R 2是C 1-2烷基,C 1-2烷基羰基或氨基羰基,其任选地被一个或两个甲基取代) 其中Y代表完成5元芳族环并包含1或2个选自氧,氮和硫的杂原子的3元二价残基,任选被C 1-2烷基取代的氨基氮,Y任选为C 被甲基取代; 或其中A 1是氧或硫的基团,A 2和A 3之一是CR 3,另一个是氮或CR 4,其中R 3和R 4独立地选自氢和甲基; 并且p和q中的每一个独立地表示2至4的整数。