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    3-substituted pyrido[4′,3′:4,5]thieno[2,3-d]pyrimidine derivatives, their preparation and their use
    5.
    发明授权
    3-substituted pyrido[4′,3′:4,5]thieno[2,3-d]pyrimidine derivatives, their preparation and their use 有权
    3-取代的吡啶并[4'，3'：4,5]噻吩并[2,3-d]嘧啶衍生物，其制备及其用途

    公开(公告)号：US06222034B1

    公开(公告)日：2001-04-24

    申请号：US09254449

    申请日：1999-03-10

    Applicant: Gerd Steiner ,  Wilfried Lubisch ,  Alfred Bach ,  Franz Emling ,  Karsten Wicke ,  Hans-Jürgen Teschendorf ,  Berthold Behl ,  Sharon Cheetham ,  Frank Kerrrigan

    Inventor： Gerd Steiner ,  Wilfried Lubisch ,  Alfred Bach ,  Franz Emling ,  Karsten Wicke ,  Hans-Jürgen Teschendorf ,  Berthold Behl ,  Sharon Cheetham ,  Frank Kerrrigan

    IPC: C07D49514

    CPC classification number: C07D495/14

    Abstract: A 3-substituted 3,4,5,6,7,8-hexahydropyrido[4′,3′:4,5]thieno[2,3-d]pyrimidine compound of formula I wherein R1 is hydrogen, C1-C4-alkyl, acetyl or benzoyl, optionally substituted phenyl-C1-C4-alkyl, naphthyl-C1-C3-alkyl, phenyl-C2-C3-alkanone or a phenylcarbamoyl-C2-alkyl, R2 is optionally substituted phenyl, pyridyl, pyrimidyl or pyrazinyl, or an optionally substituted bicyclus wherein one of the two fused rings is a phenyl, a pyridyl, a pyrimidyl or a pyrazinyl ring, A is NH or oxygen, B is hydrogen or methyl, C is hydrogen, methyl or hydroxyl, X is nitrogen, Y is CH2, CH2—C2, CH2—C2—CH2 or CH2—CH, Z is nitrogen, C or CH, and the linkage between Y and Z is a single or a double bond, and n is 2, 3 or 4, or a physiologically tolerated salt thereof, and compositions comprising them and their use as antagonists of 5HT1B and 5HT1A and for the treatment of depression and related disorders.

    Abstract translation: 式I的3-取代的3,4,5,6,7,8-六氢吡啶并[4'，3'：4,5]噻吩并[2,3-d]嘧啶化合物，其中R1为氢，C1-C4-烷基， 乙酰基或苯甲酰基，任选取代的苯基-C 1 -C 4 - 烷基，萘基-C 1 -C 3 - 烷基，苯基-C 2 -C 3 - 烷酮或苯基氨基甲酰基-C 2 - 烷基，R 2是任选取代的苯基，吡啶基，嘧啶基或吡嗪基，或 任选取代的双环，其中两个稠合环之一为苯基，吡啶基，嘧啶基或吡嗪基，A为NH或氧，B为氢或甲基，C为氢，甲基或羟基，X为氮，Y 是CH2，CH2-C2，CH2-C2-CH2或CH2-CH，Z是氮，C或CH，Y和Z之间的键是单键或双键，并且是2,3或4，或 生理上耐受的盐，以及包含它们的组合物及其作为5HT1B和5HT1A的拮抗剂的用途以及用于治疗抑郁症和相关疾病的用途。

    3-substituted pyrido [3',4':4,5] Thieno [2,3-d] pyrimidine derivatives, and production and use of the same
    6.
    发明授权
    3-substituted pyrido [3',4':4,5] Thieno [2,3-d] pyrimidine derivatives, and production and use of the same 有权
    3-取代的吡啶并[3'，4'：4,5]噻吩并[2,3-d]嘧啶衍生物及其制备和使用

    公开(公告)号：US6159981A

    公开(公告)日：2000-12-12

    申请号：US445178

    申请日：1999-12-08

    Applicant: Gerd Steiner ,  Uta Dullweber ,  Dorothea Starck ,  Alfred Bach ,  Karsten Wicke ,  Hans-Jurgen Teschendorf ,  Francisco-Javier Garcia-Ladona ,  Franz Emling

    Inventor： Gerd Steiner ,  Uta Dullweber ,  Dorothea Starck ,  Alfred Bach ,  Karsten Wicke ,  Hans-Jurgen Teschendorf ,  Francisco-Javier Garcia-Ladona ,  Franz Emling

    IPC: A61K31/519 ,  A61P25/00 ,  A61P25/24 ,  A61P43/00 ,  C07D495/14 ,  A61K31/495 ,  A61K31/505

    CPC classification number: C07D495/14

    Abstract: 3-Substituted 3,4,5,6,7,8-hexahydropyrido [3',4':4,5]-thieno[2,3-d]pyrimidine derivatives of the formula I ##STR1## where R.sup.1 is a hydrogen atom, a C.sub.1 -C.sub.4 -alkyl group, an acetyl group, a phenylalkyl C.sub.1 -C.sub.4 radical, the aromatic system being unsubstituted or substituted by halogen, C.sub.1 -C.sub.4 -alkyl, trifluoromethyl, hydroxyl, C.sub.1 -C.sub.4 -alkoxy, amino, cyano or nitro groups, or is a phenylalkanone radical, it being possible for the phenyl group to be substituted by halogen,R.sup.2 is a phenyl, pyridyl, pyrimidinyl or pyrazinyl group which is unsubstituted or mono- or disubstituted by halogen atoms, C.sub.1 -C.sub.4 -alkyl, trifluoromethyl, trifluoromethoxy, hydroxyl, C.sub.1 -C.sub.4 -alkoxy, amino, monomethylamino, dimethylamino, cyano or nitro groups and which may be fused to a benzene nucleus which can be unsubstituted or mono- or disubstituted by halogen atoms, C.sub.1 -C.sub.4 -alkyl, hydroxyl, trifluoromethyl, C.sub.1 -C.sub.4 -alkoxy, amino, cyano or nitro groups and may contain 1 nitrogen atom, or to a 5- or 6-membered ring which may contain 1-2 oxygen atoms,A is NH or an oxygen atom,Y is CH.sub.2, CH.sub.2 --CH.sub.2, CH.sub.2 --CH.sub.2 --CH.sub.2 or CH.sub.2 --CH,Z is a nitrogen atom, carbon atom or CH, it also being possible for the linkage between Y and Z to be a double bond,and n is 2, 3 or 4, and the physiologically tolerated salts thereof.

    Abstract translation: PCT No.PCT / EP98 / 03231 Sec。 371 1999年12月8日第 102（e）日期1999年12月8日PCT提交1998年5月29日PCT公布。 第WO98 / 56793号公报 日期：19983年12月17日 - 取代式I的3,4,5,6,7,8-六氢吡啶并[3'，4'：4,5] - 噻吩并[2,3-d]嘧啶衍生物，其中R1是 一个氢原子，一个C 1 -C 4烷基，一个乙酰基，一个苯基烷基C 1 -C 4基团，该芳族体系是未被取代的或被卤素，C 1 -C 4烷基，三氟甲基，羟基，C 1 -C 4烷氧基，氨基 氰基或硝基，或者是苯基烷酮基，苯基可以被卤素取代，R2是苯基，吡啶基，嘧啶基或吡嗪基，其是未被取代的或被卤原子单取代或被C1- C4-烷基，三氟甲基，三氟甲氧基，羟基，C 1 -C 4 - 烷氧基，氨基，一甲基氨基，二甲基氨基，氰基或硝基，并且它们可以与苯核稠合，苯核可被未被取代或被卤素原子， C 4 - 烷基，羟基，三氟甲基，C 1 -C 4 - 烷氧基，氨基，氰基或硝基，并且可以含有1个氮原子，或可以含有5或6元环， 含有1-2个氧原子，A是NH或氧原子，Y是CH 2，CH 2 -CH 2，CH 2 -CH 2 -CH 2或CH 2 -CH，Z是氮原子，碳原子或CH，也可以是 Y与Z之间的连接为双键，n为2,3或4，以及其生理上耐受的盐。

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