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    2,3-dioxo-1,2,3,4-tetrahydro-quinoxalinyl derivatives
    1.
    发明授权
    2,3-dioxo-1,2,3,4-tetrahydro-quinoxalinyl derivatives 失效

    公开(公告)号：US6080743A

    公开(公告)日：2000-06-27

    申请号：US29525

    申请日：1998-02-27

    申请人： Pierre Acklin ,  Hans Allgeier ,  Yves Auberson ,  Michel Biollaz ,  Robert Moretti ,  Silvio Ofner ,  Siem Jacob Veenstra

    发明人： Pierre Acklin ,  Hans Allgeier ,  Yves Auberson ,  Michel Biollaz ,  Robert Moretti ,  Silvio Ofner ,  Siem Jacob Veenstra

    IPC分类号： A61K31/00 ,  A61K31/495 ,  A61K31/498 ,  A61K31/502 ,  A61K31/505 ,  A61K31/506 ,  A61K31/535 ,  A61K31/5355 ,  A61K31/5375 ,  A61K31/5377 ,  A61K31/55 ,  A61K31/662 ,  A61P25/28 ,  A61P43/00 ,  C07D241/44 ,  C07D401/06 ,  C07D401/12 ,  C07D403/06 ,  C07D403/12 ,  C07D405/12 ,  C07D409/06 ,  C07D413/06 ,  C07D417/06 ,  C07D417/12 ,  C07D491/113 ,  C07F9/6509

    CPC分类号： C07D401/06 ,  C07D241/44 ,  C07D401/12 ,  C07D417/12 ,  C07F9/650994

    摘要： 2,3-Dioxo-1,2,3,4-tetrahydro-quinoxalinyl derivatives of formula (I), ##STR1## wherein one of the radicals R.sub.1, and R.sub.2 is a group R.sub.5 and the other is a group of formula --CH(R.sub.6)--alk--R.sub.7 (Ia), --alk--CH(R.sub.6 -R.sub.7 (Ib), --alk--N(R.sub.8)--X--R.sub.7 (Ic), --alk--N.sup.+ (R.sub.8)(R.sup.9)--X--R.sub.7 A.sup.- (Id), --alk--O--X--R.sub.7 (Ie) or --alk--S--X--R.sub.7 (If), R.sub.3, R.sub.4 and R.sub.5 are each independently of the others hydrogen, lower alkyl, halogen, trifluoromethyl, cyano or nitro, R.sub.6 is unsubstituted or lower alkylated and/or lower alkanoylated amino, R.sub.7 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, R.sub.8 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 R.sub.7 and R.sub.8, together with X and the nitrogen atom bonding R.sub.8 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, R.sub.9 is an aliphatic or araliphatic radical, or R.sub.7, R.sub.8 and R.sub.9 together with X and the nitrogen atom bonding R.sub.8, R.sub.9 and X, form an unsubstituted or substituted quaternary heteroaryl radical bonded via the quaternary nitrogen atom, with A.sup.- being the anion of a protonic acid, alk is lower alkylene, and X (unless, together with R.sub.7 and R.sub.8 and the nitrogen atom bonding R.sub.8 and X or together with the nitrogen atom bonding R.sub.8, R.sub.9 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.

    Substituted aminoalkane phosphonic acids
    2.
    发明授权
    Substituted aminoalkane phosphonic acids 有权
    取代的氨基烷烃膦酸

    公开(公告)号：US06117873A

    公开(公告)日：2000-09-12

    申请号：US297010

    申请日：1999-04-23

    申请人： Pierre Acklin ,  Hans Allgeier ,  Yves Auberson ,  Silvio Ofner ,  Siem Jacob Veenstra

    发明人： Pierre Acklin ,  Hans Allgeier ,  Yves Auberson ,  Silvio Ofner ,  Siem Jacob Veenstra

    IPC分类号： A61K31/675 ,  A61P9/00 ,  A61P25/00 ,  A61P25/08 ,  A61P43/00 ,  C07F9/6509 ,  A61K31/495 ,  C07F9/02

    CPC分类号： C07F9/650994

    摘要： Compounds of the formula I ##STR1## in which R.sub.1 is hydroxyl or an aliphatic, araliphatic or aromatic radical,X is a divalent aliphatic, cycloaliphatic, cycloaliphatic-aliphatic, araliphatic, heteroarylaliphatic or aromatic radical,R.sub.2 is hydrogen or an aliphatic or araliphatic radical, alk is lower alkylidene andR.sub.3, R.sub.4 and R.sub.5 independently of one another are hydrogen, lower alkyl, halogen, trifluoromethyl, cyano or nitro,and their salts can be used for the treatment of pathological conditions which respond to blockage of excitatory amino acid receptors, and for the production of pharmaceutical preparations.

    摘要翻译： PCT No.PCT / EP97 / 05843 Sec。 371日期1999年4月23日第 102（e）1999年4月23日PCT PCT 1997年10月22日PCT公布。 第WO98 / 17672号PCT公告 日期：1998年4月30日，其中R 1为羟基或脂族，芳脂族或芳族基团的式I化合物，X为二价脂族，脂环族，脂环族 - 脂族，芳脂族，杂芳基脂族或芳族基团，R2为氢或脂族或芳族 芳脂肪族基团，烷基是亚烷基，R3，R4和R5彼此独立地是氢，低级烷基，卤素，三氟甲基，氰基或硝基，并且它们的盐可用于治疗响应兴奋性氨基酸阻断的病理状况 酸受体和用于制备药物制剂。