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15 条记录 (耗时 0.041 秒)

    Halogen substituted tetracyclic tetrahydrofuran derivatives
    11.
    发明授权
    Halogen substituted tetracyclic tetrahydrofuran derivatives 失效
    卤素取代四环四氢呋喃衍生物

    公开(公告)号：US06699858B2

    公开(公告)日：2004-03-02

    申请号：US10292270

    申请日：2002-11-12

    申请人： José Ignacio Andrés-Gil ,  Francisco Javier Fernández-Gadea ,  Pilar Gil-Lopetegui

    发明人： José Ignacio Andrés-Gil ,  Francisco Javier Fernández-Gadea ,  Pilar Gil-Lopetegui

    IPC分类号： A61K31501

    CPC分类号： C07D405/06 ,  C07D307/93 ,  C07D493/04

    摘要： This invention concerns the compounds of formula (I), the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein n is zero, 1, 2, 3, 4, 5 or 6; X is CH2 or O; R1 and R2 each independently are hydrogen, C1-6alkyl, C1-6alkylcarbonyl, halomethylcarbonyl or C1-6alkyl substituted with hydroxy, C1-6alkyloxy, carboxyl, C1-6alkylcarbonyloxy, C1-6alkyloxycarbonyl or aryl; or R1 and R2 taken together with the nitrogen atom to which they are attached may form a morpholinyl ring or an optionally substituted heterocycle; R3 and R4 are both halogen; or R3 is halogen and R4 is hydrogen; or R3 is hydrogen and R4 is halogen; and aryl is phenyl or phenyl substituted with 1, 2 or 3 substituents selected from halo, hydroxy, C1-6alkyl and halomethyl. The compounds of formula (I) may be used as therapeutic agents.

    摘要翻译： 本发明涉及式（I）化合物，N-氧化物形式，其药学上可接受的加成盐和立体化学异构形式，其中n为0,1,2,3,4,5或6; X是CH 2或O; R 1和R 2各自独立地为氢，C 1-6烷基，C 1-6烷基羰基，卤代甲基羰基或被羟基，C 1-6烷氧基，羧基，C 1-6烷基羰基氧基，C 1-6烷氧基羰基或芳基取代的C 1-6烷基。 或R 1和R 2与它们所连接的氮原子一起可以形成吗啉基环或任选取代的杂环; R 3和R 4都是卤素; 或R 3是卤素，R 4是氢; 或R 3为氢，R 4为卤素; 并且芳基是苯基或被1,2或3个选自卤素，羟基，C 1-6烷基和卤代甲基的取代基取代的苯基。 式（I）化合物可用作治疗剂。

    Halogen substituted tetracyclic tetrahydrofuran derivatives
    12.
    发明授权
    Halogen substituted tetracyclic tetrahydrofuran derivatives 失效
    卤素取代四环四氢呋喃衍生物

    公开(公告)号：US06511976B1

    公开(公告)日：2003-01-28

    申请号：US09529252

    申请日：2000-04-06

    申请人： José Ignacio Andrés-Gil ,  Francisco Javier Fernández-Gadea ,  Pilar Gil-Lopetegui ,  Adolfo Díaz-Martinez

    发明人： José Ignacio Andrés-Gil ,  Francisco Javier Fernández-Gadea ,  Pilar Gil-Lopetegui ,  Adolfo Díaz-Martinez

    IPC分类号： A61K31497

    CPC分类号： C07D405/06 ,  C07D307/93 ,  C07D493/04

    摘要： This invention concerns the compounds of formula (I), the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein n is zero, 1, 2, 3, 4, 5 or 6; X is CH2 or O; R1 and R2 each independently are hydrogen, C1-6alkyl, C1-6alkylcarbonyl, halomethylcarbonyl or C1-6alkyl substituted with hydroxy, C1-6alkyloxy, carboxyl, C1-6alkylcarbonyloxy, C1-6alkyloxycarbonyl or aryl; or R1 and R2 taken together with the nitrogen atom to which they are attached may form a morpholinyl ring or an optionally substituted heterocycle; R3 and R4 are both halogen; or R3 is halogen and R4 is hydrogen; or R3 is hydrogen and R4 is halogen; and aryl is phenyl or phenyl substituted with 1, 2 or 3 substituents selected from halo, hydroxy, C1-6alkyl and halomethyl. The compounds of formula (I) may be used as therapeutic agents.

    摘要翻译： 本发明涉及式（I）化合物，N-氧化物形式，其药学上可接受的加成盐和立体化学异构形式，其中n为0,1,2,3,4,5或6; X是CH 2或O; R 1和R 2各自独立地为氢，C 1-6烷基，C 1-6烷基羰基，卤代甲基羰基或被羟基，C 1-6烷氧基，羧基，C 1-6烷基羰基氧基，C 1-6烷氧基羰基或芳基取代的C 1-6烷基。 或者R 1和R 2与它们所连接的氮原子一起可以形成吗啉基环或任选取代的杂环; R3和R4都是卤素; 或R3是卤素，R4是氢; 或R3是氢，R4是卤素; 并且芳基是苯基或被1,2或3个选自卤素，羟基，C 1-6烷基和卤代甲基的取代基取代的苯基。 式（I）化合物可用作治疗剂。

    Substituted tetracyclic tetrahydrofuran derivatives
    15.
    发明授权
    Substituted tetracyclic tetrahydrofuran derivatives 失效
    取代的四环四氢呋喃衍生物

    公开(公告)号：US06288058B1

    公开(公告)日：2001-09-11

    申请号：US09745517

    申请日：2000-12-21

    申请人： Pilar Gil-Lopetegui ,  Francisco Javier Fernández-Gadea ,  Theo Frans Meert

    发明人： Pilar Gil-Lopetegui ,  Francisco Javier Fernández-Gadea ,  Theo Frans Meert

    IPC分类号： A61K63155

    CPC分类号： C07D493/04 ,  C07D307/93

    摘要： This invention concerns the compounds of formula (I), the N-oxide forms, the pharmaceutically acceptable addition salts and the stereoisomeric forms thereof, wherein n is zero to 6; p and q are zero to 4; r is zero to 5; R1 and R2 each independently are hydrogen; optionally substituted C1-6alkyl; C1-6alkylcarbonyl; halomethylcarbonyl; or R1 and R2 taken together with the nitrogen atom to which they are attached may form a morpholinyl ring or an optionally substituted heterocycle; each R3 and R4 independently are halo, cyano, hydroxy, halomethyl, halomethoxy, carboxyl, nitro, amino, mono- or di(C1-6alkyl)amino, C1-6alkylcarbonylamino, aminosulfonyl, mono- or di(C1-6alkyl)aminosulfonyl, C1-6alkyl, C1-6alkyloxy, C1-6alkylcarbonyl, C1-6alkyloxycarbonyl; each R5 independently is C1-6alkyl, cyano or halomethyl; X is CR6R7, NR8, O, S, S(═O) or S(═O)2; aryl is optionally substituted phenyl; provided that the compound is other than (±)-3,3a,8,12b-tetrahydro-N-methyl-2H-dibenzo[3,4:6,7]-cyclohepta[1,2-b]-furan-2-methanamine oxalic acid. The compounds of formula (I) may be used as therapeutic agents in the treatment or the prevention of CNS disorders, cardiovascular disorders or gastrointestinal disorders.

    摘要翻译： 本发明涉及式（I）化合物，N-氧化物形式，其药学上可接受的加成盐和立体异构形式，其中n为0-6; p和q为零至4; r为0〜5; R1和R2各自独立地为氢; 任选取代的C 1-6烷基; C 1-6烷基羰基; 卤代甲基羰基; 或者R 1和R 2与它们所连接的氮原子一起可以形成吗啉基环或任选取代的杂环; 每个R 3和R 4独立地是卤素，氰基，羟基，卤代甲基，卤代甲氧基，羧基，硝基，氨基，单或二（C 1-6烷基）氨基，C 1-6烷基羰基氨基，氨基磺酰基，一或二（C 1-6烷基）氨基磺酰基， C 1-6烷基，C 1-6烷氧基，C 1-6烷基羰基，C 1-6烷氧基羰基; 每个R 5独立地是C 1-6烷基，氰基或卤代甲基; X是CR 6 R 7，NR 8，O，S，S（= O）或S（= O）2; 芳基是任选取代的苯基; 条件是该化合物不是（±）-3,3a，8,12b-四氢-N-甲基-2H-二苯并[3,4：6,7] - 环庚并[1,2-b] - 呋喃-2-基 - 草胺草酸。 式（I）化合物可用作治疗或预防CNS障碍，心血管疾病或胃肠道疾病的治疗剂。