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
    • 5. 发明申请
    • NOVEL 2,3-DIOXO-1,2,3,4-TETRAHYDRO-QUINOYXALINYL DERIVATIVES
    • 新的2,3-二氧代-1,2,3,4-四氢喹啉衍生物
    • WO1997008155A1
    • 1997-03-06
    • PCT/EP1996003644
    • 1996-08-19
    • NOVARTIS AGACKLIN, PierreALLGEIER, HansAUBERSON, YvesBIOLLAZ, MichelMORETTI, RobertOFNER, SilvioVEENSTRA, Siem, Jacob
    • NOVARTIS AG
    • C07D241/44
    • C07D401/06C07D241/44C07D401/12C07D417/12C07F9/650994
    • 2,3-Dioxo-1,2,3,4-tetrahydro-quinoxalinyl derivatives of formula (I), wherein one of the radicals R1, and R2 is a group R5 and the other is a group of formula -CH(R6)-alk-R7 (Ia), -alk-CH(R6-R7 (Ib), -alk-N(R8)-X-R7 (Ic), -alk-N (R8)(R9)-X-R7A (Id), -alk-O-X-R7 (Ie) or -alk-S-X-R7 (If), R3, R4 and R5 are each independently of the others hydrogen, lower alkyl, halogen, trifluoromethyl, cyano or nitro, R6 is unsubstituted or lower alkylated and/or lower alkanoylated amino, R7 is hydrogen; an aliphatic, cycloaliphatic or heterocycloaliphatic radical; cyano; acyl derived from carbonic acid or from a semiester or semiamide of carbonic acid, from sulfuric acid or from an aliphatic or aromatic sulfonic acid or from phosphoric acid or from a phosphonic acid ester; amino that is unsubtituted or aliphatically or araliphatically substituted and/or substituted by aliphatic, araliphatic or aromatic acyl; or an aromatic or heteroaromatic radical, R8 is hydrogen; an aliphatic or araliphatic radical; or acyl derived from an aliphatic or araliphatic carboxylic acid or from an aliphatic or araliphatic semiester of carbonic acid, or R7 and R8, together with X and the nitrogen atom bonding R8 and X, form an unsubstitued or substituted mono- or di-azaxycloalkyl, azoxacycloalkyl, azathiacycloalkyl or optionally oxidised thiacycloalkyl radical bonded via a nitrogen atom, or an unsubstituted or substituted, optionally partially hxdrogenated aryl or heteroaryl radical, R9 is an aliphatic or araliphatic radical, or R7, R8 and R9 together with X and the nitrogen atom bonding R8, R9 and X, form an unsubstituted or substituted quaternary heteroaryl radical bonded via the quaternary nitrogen atom, with A being the anion of a protonic acid, alk is lower alkylene, and X (unless, together with R7 and R8 and the nitrogen atom bonding R8 and X or together with the nitrogen atom bonding R8, R9 and X, it forms part of one of the mentioned ring systems) is a divalent aliphatic, cycloaliphatic or araliphatic radical or a direct bond, and the pharmaceutically acceptable salts thereof can be used in the preparation of a medicament for the treatment of pathological conditions that are responsive to blocking of AMPA, kainate and/or glycine binding sites of the NMDA receptor.
    • 式(I)的2,3-二氧代-1,2,3,4-四氢 - 喹喔啉基衍生物,其中基团R 1和R 2之一是基团R 5,另一个是式-CH(R 6) -alk-R7(Ia),-alk-CH(R6-R7(Ib))-alk-N(R8)-X-R7(Ic),-alk-N +(R8)(R9)-X -R7A - (Id),-alk-OX-R7(Ie)或-alk-SX-R7(If),R3,R4和R5各自独立地为氢,低级烷基,卤素,三氟甲基,氰基 或硝基,R 6是未取代的或低级烷基化的和/或低级烷酰基化的氨基,R 7是氢;脂族,脂环族或杂环脂族基团;氰基;衍生自碳酸的酰基或来自碳酸的半酯或半酰胺, 脂族或芳族磺酸或磷酸或膦酸酯;未取代或脂族或芳烃取代和/或被脂族或芳族酰基取代的氨基;或芳族或杂芳族基团,R 8为氢; 脂肪族或芳脂族辐射 CAL; 或衍生自脂族或芳脂族羧酸的酰基或来自碳酸或R 7和R 8的脂族或芳脂肪族半酯与X以及键合R 8和X的氮原子形成未取代或取代的单 - 或二 - 氮杂环烷基的酰基, 氮杂环烷基,氮杂环烷基或任意氧化的经氮原子键合的硫代环烷基,或未取代或取代的,任选部分羟基化的芳基或杂芳基,R 9为脂族或芳脂族基,或者R 7,R 8和R 9与X和氮原子键合 R8,R9和X形成通过季氮原子键合的未取代或取代的季杂芳基,A 1是质子酸的阴离子,alk是低级亚烷基和X(除非与R 7和R 8一起 键合R8和X的氮原子或与R8,R9和X键合的氮原子一起形成所述环系中一个的一部分)是二价脂族,脂环族或芳族 脂肪族基团或直接键合,并且其药学上可接受的盐可用于制备用于治疗对阻断NMDA受体的AMPA,红藻氨酸和/或甘氨酸结合位点有反应的病理状况的药物。