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    Use of 5-ht5-ligands in the treatment of neurodegenerative and neuropsychiatric disturbances
    2.
    发明授权
    Use of 5-ht5-ligands in the treatment of neurodegenerative and neuropsychiatric disturbances 失效
    5-ht5配体在治疗神经变性和神经精神障碍中的应用

    公开(公告)号：US06750221B1

    公开(公告)日：2004-06-15

    申请号：US09889157

    申请日：2001-07-11

    Applicant: Francisco Javier Garcia-Ladona ,  Laszlo Szabo ,  Gerd Steiner ,  Hans-Peter Hofmann

    Inventor： Francisco Javier Garcia-Ladona ,  Laszlo Szabo ,  Gerd Steiner ,  Hans-Peter Hofmann

    IPC: A61K31505

    CPC classification number: G01N33/566 ,  A61K31/519 ,  G01N2500/02 ,  G01N2500/04

    Abstract: The invention relates to the use of binding partners for 5-HT5-receptors in the treatment of neuropathological and in particular neurodegenerative and/or neuropsychiatric disturbances which can occur notably in cases of cerebral ishcemia, cerebral stroke, epilepsy and attacks in general, chronic schizophrenia, other psychotic illnesses, dementia, notably Alzheimer's disease, demyelination diseases, notably multiple sclerosis and brain tumors. The invention also relates to methods, especially screening methods, for identifying and characterizing such binding partners.

    Abstract translation: 本发明涉及5-HT5受体的结合配偶体在治疗神经病理学，特别是神经变性和/或神经精神障碍中的用途，其可以在脑血症，脑卒中，癫痫和一般发作的慢性精神分裂症 ，其他精神病，痴呆，特别是阿尔茨海默病，脱髓鞘疾病，特别是多发性硬化和脑肿瘤。 本发明还涉及用于鉴定和表征这些结合配偶体的方法，特别是筛选方法。

    3-substituted 3,4-dihydro-thieno[2,3-D]pyrimidine derivatives and production and use of the same
    5.
    发明授权
    3-substituted 3,4-dihydro-thieno[2,3-D]pyrimidine derivatives and production and use of the same 有权
    3-取代的3,4-二氢 - 噻吩并[2,3-D]嘧啶衍生物及其制备和应用

    公开(公告)号：US06159962A

    公开(公告)日：2000-12-12

    申请号：US445222

    申请日：1999-12-06

    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 ,  C07D495/04 ,  C07D417/06 ,  A61K31/551 ,  A61K31/559 ,  C07D417/14

    CPC classification number: C07D495/04

    Abstract: 3-Substituted 3,4-dihydrothieno[2,3-d]pyrimidine derivatives of the formula I ##STR1## where R.sup.1 and R.sup.2 are a hydrogen atom or a C.sub.1 -C.sub.4 -alkyl group,R.sup.3 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 may 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 being possible for the linkage between Y and Z also to be a double bond,and n is 2, 3 or 4, and the physiologically tolerated salts thereof.

    Abstract translation: PCT No.PCT / EP98 / 03230 Sec。 371 1999年12月6日第 102（e）日期1999年12月6日PCT提交1998年5月29日PCT公布。 第WO98 / 56792号公报 日期：19983年12月17日 - 取代的式I的3,4-二氢噻吩并[2,3-d]嘧啶衍生物，其中R 1和R 2是氢原子或C 1 -C 4 - 烷基，R 3是苯基，吡啶基， C 1 -C 4 - 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，氰基或硝基被单取代或被二取代的嘧啶基或吡嗪基， C 1 -C 4烷基，羟基，三氟甲基，C 1 -C 4 - 烷氧基，氨基，氰基或硝基可被未被取代或单取代或被二取代的苯核，并且可以含有1个氮原子或5个 - 或6-元环，其可以含有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，Y和Z之间的连接也可以是双键，n是2,3或4，以及其生理上耐受的盐。

    3-substituted pyrido [3',4':4,5] Thieno [2,3-d] pyrimidine derivatives, and production and use of the same
    7.
    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。

    USE OF BINDING PARTNERS FOR 5-HT5 RECEPTORS FOR THE TREATMENT OF NEURODEGENERATIVE AND NEUROPSYCHIATRIC DISORDERS
    9.
    发明申请
    USE OF BINDING PARTNERS FOR 5-HT5 RECEPTORS FOR THE TREATMENT OF NEURODEGENERATIVE AND NEUROPSYCHIATRIC DISORDERS 审中-公开
    使用5-HT5受体拮抗剂治疗神经损伤和神经缺血性疾病

    公开(公告)号：US20120196301A1

    公开(公告)日：2012-08-02

    申请号：US13296433

    申请日：2011-11-15

    Applicant: Francisco Javier Garcia-Ladona ,  Laszlo Szabo ,  Gerd Steiner ,  Hans-Peter Hofmann

    Inventor： Francisco Javier Garcia-Ladona ,  Laszlo Szabo ,  Gerd Steiner ,  Hans-Peter Hofmann

    IPC: G01N33/566 ,  C07D495/14

    CPC classification number: G01N33/566 ,  A61K31/519 ,  G01N2500/02 ,  G01N2500/04

    Abstract: The present invention relates to the use of binding partners for 5-HT5 receptors for the treatment of neuropathological, in particular neurodegenerative and/or neuropsychiatric, disorders, which can occur, in particular, in cerebral ischemia, stroke, epilepsy and seizures in general, chronic schizophrenia, other psychotic disorders, dementia, in particular Alzheimer's dementia, demyelinizing disorders, in particular multiple sclerosis, and brain tumors. The invention also relates to processes for the identification and characterization of such binding partners, in particular in the form of screening processes.

    Abstract translation: 本发明涉及5-HT5受体的结合配偶体用于治疗神经病理特别是神经变性和/或神经精神障碍的用途，其可以发生，特别是脑缺血，中风，癫痫和癫痫发作， 慢性精神分裂症，其他精神病，痴呆，特别是阿尔茨海默氏痴呆，脱髓鞘疾病，特别是多发性硬化和脑肿瘤。 本发明还涉及用于鉴定和表征这些结合配偶体的方法，特别是以筛选方法的形式。

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