会员体验
专利管家(专利管理)
工作空间(专利管理)
风险监控(情报监控)
数据分析(专利分析)
侵权分析(诉讼无效)
联系我们
交流群
官方交流:
QQ群: 891211   
微信请扫码    >>>
现在联系顾问~
热词
    • 1. 发明授权
    • Pyridin-2-one compounds and their use as modulators of the dopamine D3 receptor
    • 吡啶-2-酮化合物及其作为多巴胺D3受体调节剂的用途
    • US08334289B2
    • 2012-12-18
    • US13103734
    • 2011-05-09
    • Hervé GenesteWilfried BrajeAndreas Haupt
    • Hervé GenesteWilfried BrajeAndreas Haupt
    • A61K31/506
    • C07D401/12
    • The invention relates to novel pyridin-2-one compounds of general formula (I), in which A represents a 4- to 6-membered hydrocarbon chain that can have 1 or 2 methyl groups as substituents, wherein 1 or 2 carbon atoms can be replaced by oxygen, a carbonyl group or sulfur, and the hydrocarbon chain can have a double bond or a triple bond; R1, R2, R3 and R4 have the meanings as cited in the claims and in the description. The invention also relates to the tautomers of compounds I, the physiologically acceptable salts of compounds I, and to the physiologically acceptable salts of the tautomers of compounds I. The invention also relates to the use of compounds of general formula (I) and of the tautomers, and to the use of the physiologically acceptable salts of compounds I and of the tautomers for producing a pharmaceutical agent for treating diseases that respond to the influence of dopamine D3 receptor antagonists or agonists.
    • 本发明涉及通式(I)的新型吡啶-2-酮化合物,其中A表示可具有1或2个甲基作为取代基的4至6元烃链,其中1或2个碳原子可以是 由氧,羰基或硫取代,烃链可以具有双键或三键; R1,R2,R3和R4具有权利要求书和说明书中引用的含义。 本发明还涉及化合物I的互变异构体,化合物I的生理上可接受的盐,以及化合物I的互变异构体的生理上可接受的盐。本发明还涉及通式(I)的化合物和 互变异构体,以及化合物I和互变异构体的生理上可接受的盐的用途,用于制备用于治疗对多巴胺D3受体拮抗剂或激动剂的影响作出反应的疾病的药剂。
    • 2. 发明申请
    • PYRIDIN-2-ONE COMPOUNDS AND THEIR USE AS MODULATORS OF THE DOPAMINE D3 RECEPTOR
    • PYRIDIN-2-ONE化合物及其作为DOPAMINE D3受体的调节剂
    • US20110245266A1
    • 2011-10-06
    • US13103734
    • 2011-05-09
    • Hervé GenesteWilfried BrajeAndreas Haupt
    • Hervé GenesteWilfried BrajeAndreas Haupt
    • A61K31/497C07D403/14A61P25/18A61P25/24
    • C07D401/12
    • The invention relates to novel pyridin-2-one compounds of general formula (I), in which A represents a 4- to 6-membered hydrocarbon chain that can have 1 or 2 methyl groups as substituents, wherein 1 or 2 carbon atoms can be replaced by oxygen, a carbonyl group or sulfur, and the hydrocarbon chain can have a double bond or a triple bond; R1, R2, R3 and R4 have the meanings as cited in the claims and in the description. The invention also relates to the tautomers of compounds I, the physiologically acceptable salts of compounds I, and to the physiologically acceptable salts of the tautomers of compounds I. The invention also relates to the use of compounds of general formula (I) and of the tautomers, and to the use of the physiologically acceptable salts of compounds I and of the tautomers for producing a pharmaceutical agent for treating diseases that respond to the influence of dopamine D3 receptor antagonists or agonists.
    • 本发明涉及通式(I)的新型吡啶-2-酮化合物,其中A表示可具有1或2个甲基作为取代基的4至6元烃链,其中1或2个碳原子可以是 由氧,羰基或硫取代,烃链可以具有双键或三键; R1,R2,R3和R4具有权利要求书和说明书中引用的含义。 本发明还涉及化合物I的互变异构体,化合物I的生理上可接受的盐,以及化合物I的互变异构体的生理上可接受的盐。本发明还涉及通式(I)的化合物和 互变异构体,以及化合物I和互变异构体的生理上可接受的盐的用途,用于制备用于治疗对多巴胺D3受体拮抗剂或激动剂的影响作出反应的疾病的药剂。
    • 4. 发明授权
    • Pyrimidin-2-one compounds and their use as dopamine D3 receptor ligands
    • 嘧啶-2-酮化合物及其作为多巴胺D3受体配体的用途
    • US08008488B2
    • 2011-08-30
    • US10548931
    • 2004-03-12
    • Hervé GenesteAndreas KlingWilfried BrajeAndreas HauptLiliane Unger
    • Hervé GenesteAndreas KlingWilfried BrajeAndreas HauptLiliane Unger
    • C07D403/06C07D403/14C07D401/06C07D401/14A61K31/505A61K31/506A61P25/16A61P25/18A61P25/24A61P25/22A61P25/30
    • C07D239/36C07D239/52C07D239/54C07D239/553C07D239/56C07D401/12C07D403/14C07D405/14C07D409/14
    • The invention relates to pyrimidin 2-one compounds of general formula (I), in addition to the derivatives and tautomers of (I) and the physiologically acceptable salts of said compounds. In said formula, A represents linear or branched C3-C6 alkene, which can have a double bond or triple bond and/or a group Z, which is not adjacent to the nitrogen atom of the pyrimidinone ring and is selected from O, S, C(O), NR3, C(O)NR3, NR3C(O), OC(O) and C(O)O; B represents a group of the formula (II), in which X stands for CH2 or N and Y stands for CH2 or CH2CH2, or X—Y can also jointly represent C═CH, C═CH—CH2 or CH—CH═CH; R1 and R2 are defined as cited in the description and the claims; and Ar represents an optionally substituted aromatic group. The invention also relates to a pharmaceutical agent, containing at least one compound (I) and the tautomers, derivatives and/or acid addition salts of said compound, optionally together with physiologically acceptable carriers and/or auxiliary agents. The invention also relates to the use of compounds of formula (I), and their tautomers, derivatives and pharmacologically acceptable acid addition salts for producing a pharmaceutical agent for treating diseases which respond to the influence of dopamine D3 receptor ligands.
    • 除了(I)的衍生物和互变异构体以及所述化合物的生理学上可接受的盐之外,本发明涉及通式(I)的嘧啶-2-酮化合物。 在所述式中,A表示可以具有双键或三键的直链或支链C 3 -C 6烯基和/或不与嘧啶酮环的氮原子相邻并且选自O,S, C(O),NR 3,C(O)NR 3,NR 3 C(O),OC(O)和C(O)O; B表示式(II)的基团,其中X表示CH2或N,Y表示CH2或CH2CH2,或X-Y也可共同表示C = CH,C = CH-CH 2或CH-CH = CH ; R1和R2定义为在说明书和权利要求书中引用的; 并且Ar表示任选取代的芳族基团。 本发明还涉及含有至少一种化合物(I)和所述化合物的互变异构体,衍生物和/或酸加成盐,任选地与生理上可接受的载体和/或辅助剂一起的药剂。 本发明还涉及式(I)化合物及其互变异构体,衍生物和药理学上可接受的酸加成盐的用途,用于制备用于治疗对多巴胺D3受体配体的影响作出反应的疾病的药剂。
    • 8. 发明授权
    • Small molecule potentiators of metabotropic glutamate receptors
    • US08314120B2
    • 2012-11-20
    • US13073087
    • 2011-03-28
    • Wilfried BrajeKatja JantosHervé GenesteMario MezlerMargaretha Henrica Maria Bakker
    • Wilfried BrajeKatja JantosHervé GenesteMario MezlerMargaretha Henrica Maria Bakker
    • A61K31/4375A61K31/4725A61K31/403C07D471/04C07D217/22C07D487/04C07D209/46
    • C07D401/12C07D401/14C07D403/12C07D413/12C07D413/14
    • The present invention relates to small molecule potentiators of metabotropic receptors, in particular of the mGlu2 receptor. The present invention also relates to the use of these compounds for the prevention or treatment of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The present invention thus provides compounds of formula I wherein X1 is N or C—R1, X2 is N or C—R2, X3 is N or C—R3, X4 is N or C—R4 provided that none or one of X1, X2, X3 or X4 is N; Y1 is N, C or C—R5, Y2 is N, C or C—R6, Y3 is Y1, Y2, N, C or C—R7, Y4 is N, C or C—R8 provided that only the moiety Y1, Y2, Y3 or Y4 to which Z is bound is C and further provided at most one of Y1, Y2, Y3 or Y4 is N; Z is O, S, S(O), S(O)2 or NRZ; Q is CH2 or CH2CH2, where one or two of the hydrogen atoms in CH2 or CH2CH2 may be replaced by halogen, C1-C4-alkyl or C1-C4-haloalkyl; R1 is inter alia hydrogen, halogen, C1-C6-alkyl, C1-C6-haloalkyl, C1-C6-alkoxy, C1-C4-haloalkoxy, C3-C8-cycloalkyl, a radical NR1aR1b, C-bound 3- to 7-membered, saturated heterocyclyl having 1 or 2 nitrogen atoms and 0 or 1 heteroatoms, selected from O and S, as ring members, aryl, aryl-CH2, aryloxy, hetaryl, hetaryloxy or hetaryl-CH2, wherein the heterocyclyl, aryl and hetaryl rings ring in the last six radicals themselves are unsubstituted or carry 1, 2, 3, 4 or 5 identical or different radicals R1c; R2 has one of the meanings given for R1; R3 and R4 are, inter alia, selected from hydrogen, halogen, C1-C4-alkyl, C1-C4-haloalkyl, C3-C6-cycloalkyl, C1-C4-alkoxy, C1-C4-alkoxy-C1-C4-alkyl, phenyl, C1-C4-haloalkoxy, a radical (CH2)nNR′R″; R5, R6, R7, R8 are, independently of each other, selected from hydrogen, halogen, etc.; Ra is C3-C6-cycloalkyl, C1-C6-haloalkyl or C1-C6-alkyl, which is unsubstituted or carries one radical selected from C1-C4-alkoxy, C1-C4-haloalkoxy and a radical NRa1Ra2; and the N-oxides and the pharmaceutically acceptable salts thereof.