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    3-Substituted 3,4-dihydro-thieno[2,3-d]pyrimidin-4-one derivatives, production and use thereof
    1.
    发明申请
    3-Substituted 3,4-dihydro-thieno[2,3-d]pyrimidin-4-one derivatives, production and use thereof 有权
    3-取代的3,4-二氢 - 噻吩并[2,3-d]嘧啶-4-酮衍生物，的制备和用途

    公开(公告)号：US20060142317A1

    公开(公告)日：2006-06-29

    申请号：US10539708

    申请日：2003-12-17

    Applicant: Margaretha Bakker ,  Wilfried Hornberger ,  Andreas Kling ,  Udo Lange ,  Helmut Mack ,  Achim Moeller ,  Reinhold Mueller ,  Kurt Schelhaas ,  Martin Schmidt ,  Gerd Steiner ,  Karsten Wicke

    Inventor： Margaretha Bakker ,  Wilfried Hornberger ,  Andreas Kling ,  Udo Lange ,  Helmut Mack ,  Achim Moeller ,  Reinhold Mueller ,  Kurt Schelhaas ,  Martin Schmidt ,  Gerd Steiner ,  Karsten Wicke

    IPC: A61K31/519 ,  C07D498/14

    CPC classification number: C07D495/14

    Abstract: The invention relates to 3,4-dihydro-thieno[2,3-d]pyrimidin-4-one derivatives which are substituted in position 3 by 5-membered heteroaryl which may be fused to an aryl or heteroaryl radical, where the heteroaryl and, if appropriate, the fused aryl or heteroaryl radical may have 1, 2 or 3 substituents selected independently of one another from C1-5-alkyl, C1-5-alkoxy, C1-5-alkylthio, halogen, CN, halo-C1-5-alkyl, halo-C1-5-alkoxy, hydroxy, —NH2, —N(R6)2, —NH(R6), aryl, aryloxy, aralkyl, aralkyloxy and heteroaryl, where the substituents aryl, aryloxy, aralkyl, aralkyloxy and heteroaryl may have 1, 2 or 3 substituents selected independently of one another from C1-5-alkyl, C1-5-alkoxy, C1-5-alkylthio, halogen, CN, halo-C1-5-alkyl, halo-C1-5-alkoxy, hydroxy, —NH2, —N(R6)2 and —NH(R6). The preparation and use of these derivatives, especially for therapeutic purposes, e.g. for the treatment of depressions, are likewise described.

    Abstract translation: 本发明涉及在3位被5元杂芳基取代的3,4-二氢 - 噻吩并[2,3-d]嘧啶-4-酮衍生物，其可以与芳基或杂芳基稠合，其中杂芳基和 如果合适，稠合的芳基或杂芳基可以具有1,2或3个彼此独立地选自C 1-5 - 烷基，C 1-5 - 烷氧基，C 1-5 - 烷硫基，卤素，CN，卤代-C 1-5 - 烷基，卤代C 1-5 - 烷氧基，羟基，-NH 2，-N（R 6）2，-NH（R 6），芳基，芳氧基，芳烷基，芳烷氧基和杂芳基，其中取代基芳基， 芳氧基，芳烷基，芳烷氧基和杂芳基可以具有1,2或3个选自C 1-5 - 烷基，C 1-5 - 烷氧基，C 卤代C 1 -C 5烷基，卤素，CN，卤代-C 1-5烷基，卤代-C 1-5烷氧基，羟基 ，-NH 2，-N（R 6）2和-NH（R 6）。 这些衍生物的制备和使用，特别是用于治疗目的，例如 为了处理凹陷，同样地描述。

    3-substituted 3,4-dihydro-thieno[2,3-D]pyrimidine derivatives and production and use of the same
    3.
    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。

    Carboxamides and their use as herbicides
    5.
    发明授权
    Carboxamides and their use as herbicides 失效
    羧甲酰胺及其作为除草剂的用途

    公开(公告)号：US5201934A

    公开(公告)日：1993-04-13

    申请号：US592287

    申请日：1990-10-03

    Applicant: Peter Muenster ,  Gerd Steiner ,  Wolfgang Freund ,  Bruno Wuerzer ,  Karl-Otto Westphalen

    Inventor： Peter Muenster ,  Gerd Steiner ,  Wolfgang Freund ,  Bruno Wuerzer ,  Karl-Otto Westphalen

    IPC: A01N43/08 ,  A01N43/10 ,  A01N43/28 ,  A01N43/78 ,  C07D307/68 ,  C07D333/38 ,  C07D405/12 ,  C07D405/14 ,  C07D407/12 ,  C07D409/12 ,  C07D409/14 ,  C07D413/04 ,  C07D417/12 ,  C07D417/14 ,  C07D495/04

    CPC classification number: C07D407/12 ,  A01N43/08 ,  A01N43/10 ,  A01N43/28 ,  C07D307/68 ,  C07D333/38 ,  C07D409/12 ,  C07D417/12

    Abstract: Carboxamides of the formulae Ia to Ic ##STR1## where X is oxygen or sulfur;R.sup.1 is hydrogen or substituted or unsubstituted cycloalkyl or alkyl;R.sup.2 is hydroxy, alkoxy, cyanoalkyl, substituted or unsubstituted alkenyl, alkynyl, phenyl or naphthyl, or one of the groups stated for R.sup.1 ;R.sup.3 and R.sup.4 are nitro, cyano, halogen, substituted or unsubstituted amino, alkoxy, alkylthio, substituted or unsubstituted alkenyl, alkynyl, phenyl, phenoxy or phenylthio, or one of the groups stated for R.sup.1 ;R.sup.5 is formyl, 4,5-dihydrooxazol-2-yl or COYR.sup.6 (Y.dbd.O,S);R.sup.6 is hydrogen, cycloalkyl, substituted or unsubstituted alkyl, alkenyl, alkynyl, cycloalkenyl or phenyl,phthalimido, tetrahydrophthalimido, succinimido, maleimido, benzotriazolyl ora group --N.dbd.CR.sup.7 R.sup.8, whereR.sup.7 and R.sup.8 are hydrogen or alkyl, and R.sup.8 may also be cycloalkyl, phenyl, or R.sup.7 and R.sup.8 together form a 4- to 7-membered alkylene chain;and if R.sup.5 is carboxyl, methoxycarbonyl or ethoxycarbonyl and R.sup.2 is hydrogen, R.sup.3 is not hydrogen and R.sup.4 is not hydrogen or methyl, and if R.sup.5 is carboxyl, methoxycarbonyl or ethoxycarbonyl and R.sup.4 is hydrogen, R.sup.3 is not hydrogen or R.sup.2 is not one of the following groups: hydrogen, C.sub.1 -C.sub.4 -alkyl, phenyl, 2-(3,4-dimethoxyphenyl)ethyl or 2,5-dichlorothien-3-yl;processes for the manufacture of compounds I and herbicidal agents containing them.

    Abstract translation: 式Ia至Ic的酰胺酰胺其中X是氧或硫; R1是氢或取代或未取代的环烷基或烷基; R2是羟基，烷氧基，氰基烷基，取代或未取代的链烯基，炔基，苯基或萘基，或为R1所述的一个基团; R3和R4是硝基，氰基，卤素，取代或未取代的氨基，烷氧基，烷硫基，取代或未取代的烯基，炔基，苯基，苯氧基或苯硫基，或为R1表示的基团之一; R5是甲酰基，4,5-二氢恶唑-2-基或COYR 6（Y = O，S）; R 6是氢，环烷基，取代或未取代的烷基，烯基，炔基，环烯基或苯基，邻苯二甲酰亚氨基，四氢邻苯二甲酰亚胺基，琥珀酰亚胺基，马来酰亚胺基，苯并三唑基或基团-N = CR 7 R 8，其中R 7和R 8是氢或烷基， 环烷基，苯基或R7和R8一起形成4-至7-元亚烷基链; 如果R5是羧基，甲氧基羰基或乙氧基羰基，R2是氢，R3不是氢，R4不是氢或甲基，如果R5是羧基，甲氧基羰基或乙氧基羰基，R4是氢，R3不是氢或R2不是 以下基团：氢，C 1 -C 4 - 烷基，苯基，2-（3,4-二甲氧基苯基）乙基或2,5-二氯噻吩-3-基; 制备化合物I和含有它们的除草剂的方法。

    5,6-Dihydro-11-alkylene-morphanthridin-6-ones
    8.
    发明授权
    5,6-Dihydro-11-alkylene-morphanthridin-6-ones 失效
    5,6-二氢-11-亚烷基 - 异佛尔酮-6-酮

    公开(公告)号：US4336192A

    公开(公告)日：1982-06-22

    申请号：US208974

    申请日：1980-11-20

    Applicant: Gerd Steiner ,  Albrecht Franke

    Inventor： Gerd Steiner ,  Albrecht Franke

    IPC: C07D223/20

    CPC classification number: C07D223/20

    Abstract: 5,6-Dihydro-11-alkylene-morphanthridin-6-ones and processes for their preparation. The compounds are valuable intermediates for chemical syntheses, especially of drugs.

    Abstract translation: 5,6-二氢-11-亚烷基 - 异恶唑-6-酮及其制备方法。 这些化合物是用于化学合成，特别是药物的有价值的中间体。

    Use of 5-ht5-ligands in the treatment of neurodegenerative and neuropsychiatric disturbances
    10.
    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。

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