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    Combinations comprising ampa receptor antagonists for the treatment of schizophrenia
    1.
    发明申请
    Combinations comprising ampa receptor antagonists for the treatment of schizophrenia 审中-公开
    包含用于治疗精神分裂症的安瓿受体拮抗剂的组合

    公开(公告)号：US20070082873A1

    公开(公告)日：2007-04-12

    申请号：US10577196

    申请日：2004-10-27

    申请人： Kurt Lingenhöhl ,  Ference Martenyi ,  Silvio Ofner ,  Mary Karolchyk ,  Hans Kalkman

    发明人： Kurt Lingenhöhl ,  Ference Martenyi ,  Silvio Ofner ,  Mary Karolchyk ,  Hans Kalkman

    IPC分类号： A61K31/675

    CPC分类号： A61K45/06 ,  A61K31/675 ,  A61K2300/00

    摘要： The present invention relates to combinations suitable for the treatment of psychiatric/neurological disorders, in particular schizophrenia. The combinations comprise at least one AMPA receptor antagonist and at least one compound selected from the group consisting of (a) anti-epileptic drugs selected from barbiturates and derivatives thereof, benzodiazepines, carboxamides, hydantoins, succinimides, valproic acid and other fatty acid derivates and other anti-epileptic drugs, (b) conventional antipsychotics and (c) atypical antipsychotics.

    摘要翻译： 本发明涉及适用于治疗精神病/神经障碍，特别是精神分裂症的组合。 所述组合包含至少一种AMPA受体拮抗剂和至少一种选自（a）选自巴比妥类及其衍生物，苯并二氮杂，甲酰胺，乙内酰脲，琥珀酰亚胺，丙戊酸和其它脂肪酸衍生物的抗癫痫药物的化合物和 其他抗癫痫药，（b）常规抗精神病药和（c）非典型抗精神病药。

    1-acylpiperidine compounds
    4.
    发明授权
    1-acylpiperidine compounds 失效
    1-酰基哌啶化合物

    公开(公告)号：US5310743A

    公开(公告)日：1994-05-10

    申请号：US929186

    申请日：1992-08-11

    申请人： Walter Schilling ,  Silvio Ofner ,  Siem J. Veenstra

    发明人： Walter Schilling ,  Silvio Ofner ,  Siem J. Veenstra

    IPC分类号： C07D211/26 ,  A61K31/4427 ,  A61K31/443 ,  A61K31/4433 ,  A61K31/445 ,  A61K31/451 ,  A61K31/452 ,  A61K31/4523 ,  A61K31/4525 ,  A61K31/4535 ,  A61K31/454 ,  A61K31/47 ,  A61K31/4709 ,  A61P1/00 ,  A61P11/08 ,  A61P25/00 ,  A61P25/04 ,  A61P25/18 ,  A61P25/20 ,  A61P25/24 ,  A61P25/26 ,  A61P27/02 ,  A61P29/00 ,  A61P43/00 ,  C07D20060101 ,  C07D211/58 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D409/12 ,  C07D471/04 ,  C07D215/12 ,  A01N43/42 ,  C07D215/16

    CPC分类号： C07D401/12 ,  C07D211/58 ,  C07D401/14 ,  C07D405/12 ,  C07D409/12 ,  C07D471/04

    摘要： 1-Acylpiperidine compound of the formula I ##STR1## in which R.sub.1 is an optionally substituted aralkyl, aryloxyalkyl, heteroaralkyl, aroyl, heteroaroyl, cycloalkylcarbonyl, aralkanoyl, heteroarylalkanoyl, aralkoxycarbonyl or arylcarbamoyl radical or the acyl radical of an .alpha.-amino acid which is optionally N-substituted by lower alkanoyl or carbamoyl-lower-alkanoyl, R.sub.2 is cycloalkyl or an optionally substituted aryl or heteroaryl radical, R.sub.3 is hydrogen, alkyl, carbamoyl or an alkanoyl or alkenoyl radical which is optionally substituted by carboxyl or esterified or amidated carboxyl, R.sub.4 is an optionally substituted aryl or optionally partially hydrogenated heteroaryl radical, X.sub.1 is methylene, ethylene, a direct linkage, an optionally ketalised carbonyl group or an optionally etherified hydroxymethylene group, X.sub.2 is alkylene, carbonyl or a direct linkage, and X.sub.3 is carbonyl, oxo-lower-alkylene, oxo(aza)-lower-alkylene or an alkylene radical which is optionally substituted by phenyl, hydroxymethyl, optionally esterified or amidated carboxyl or, in higher than the .alpha. position, by hydroxyl, and its salts have substance-P-antagonistic properties and can be used as pharmaceutically active substances in pharmaceuticals for the treatment of disorders in whose development substance P plays an essential part.

    摘要翻译： 式I的1-酰基哌啶化合物其中R 1是任选取代的芳烷基，芳氧基烷基，杂芳烷基，芳酰基，杂芳酰基，环烷基羰基，芳烷酰基，杂芳基烷酰基，芳烷氧基羰基或芳基氨基甲酰基或α-氨基的酰基 酸，其任选被低级烷酰基或氨基甲酰基 - 低级 - 烷酰基N-取代，R 2是环烷基或任选取代的芳基或杂芳基，R 3是氢，烷基，氨基甲酰基或任选被羧基或酯化的烷酰基或烯酰基 或酰胺化的羧基，R 4是任选取代的芳基或任选部分氢化的杂芳基，X 1是亚甲基，亚乙基，直链，任选的缩酮化羰基或任选醚化的羟基亚甲基，X 2是亚烷基，羰基或直链， X 3是羰基，氧代 - 低级 - 亚烷基，氧代（氮杂） - 低级 - 亚烷基或任选被苯基取代的亚烷基， 羟甲基，任选酯化或酰胺化的羧基，或高于α位置的羟基，其盐具有物质P-拮抗性质，可用作药物中的药物活性物质，用于治疗其发育物质P所起的障碍 一个重要的部分。

    2,3-dioxo-1,2,3,4-tetrahydro-quinoxalinyl derivatives
    6.
    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.

    1-acylpiperidine compounds
    9.
    发明授权
    1-acylpiperidine compounds 失效
    1-酰基哌啶化合物

    公开(公告)号：US5541195A

    公开(公告)日：1996-07-30

    申请号：US196360

    申请日：1994-04-04

    申请人： Walter Schilling ,  Silvio Ofner ,  Siem J. Veenstra

    发明人： Walter Schilling ,  Silvio Ofner ,  Siem J. Veenstra

    IPC分类号： C07D211/26 ,  A61K31/4427 ,  A61K31/443 ,  A61K31/4433 ,  A61K31/445 ,  A61K31/451 ,  A61K31/452 ,  A61K31/4523 ,  A61K31/4525 ,  A61K31/4535 ,  A61K31/454 ,  A61K31/47 ,  A61K31/4709 ,  A61P1/00 ,  A61P11/08 ,  A61P25/00 ,  A61P25/04 ,  A61P25/18 ,  A61P25/20 ,  A61P25/24 ,  A61P25/26 ,  A61P27/02 ,  A61P29/00 ,  A61P43/00 ,  C07D20060101 ,  C07D211/58 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D409/12 ,  C07D471/04 ,  C07D215/12 ,  C07D409/00

    CPC分类号： C07D401/12 ,  C07D211/58 ,  C07D401/14 ,  C07D405/12 ,  C07D409/12 ,  C07D471/04

    摘要： 1-Acylpiperidine compound of the formula I ##STR1## in which R.sub.1 is an optionally substituted aralkyl, aryloxyalkyl, heteroaralkyl, aroyl, heteroaroyl, cycloalkylcarbonyl, aralkanoyl, heteroarylalkanoyl, aralkoxycarbonyl or arylcarbamoyl radical or the acyl radical of an .alpha.-amino acid which is optionally N-substituted by lower alkanoyl or carbamoyl-lower-alkanoyl, R.sub.2 is cycloalkyl or an optionally substituted aryl or heteroaryl radical, R.sub.3 is hydrogen, alkyl, carbamoyl or an alkanoyl or alkenoyl radical which is optionally substituted by carboxyl or esterified or amidated carboxyl, R.sub.4 is an optionally substituted aryl or optionally partially hydrogenated heteroaryl radical, X.sub.1 is methylene, ethylene, a direct linkage, an optionally ketalised carbonyl group or an optionally etherified hydroxymethylene group, X.sub.2 is alkylene, carbonyl or a direct linkage, and X.sub.3 is carbonyl, oxo-lower-alkylene, oxo(aza)-lower-alkylene or an alkylene radical which is optionally substituted by phenyl, hydroxymethyl, optionally esterified or amidated carboxyl or, in higher than the .alpha. position, by hydroxyl, and its salts have substance-P-antagonistic properties and can be used as pharmaceutically active substances in pharmaceuticals for the treatment of disorders in whose development substance P plays an essential part.

    摘要翻译： 式I的1-酰基哌啶化合物其中R 1是任选取代的芳烷基，芳氧基烷基，杂芳烷基，芳酰基，杂芳酰基，环烷基羰基，芳烷酰基，杂芳基烷酰基，芳烷氧基羰基或芳基氨基甲酰基或α-氨基的酰基 酸，其任选被低级烷酰基或氨基甲酰基 - 低级 - 烷酰基N-取代，R 2是环烷基或任选取代的芳基或杂芳基，R 3是氢，烷基，氨基甲酰基或任选被羧基或酯化的烷酰基或烯酰基 或酰胺化的羧基，R 4是任选取代的芳基或任选部分氢化的杂芳基，X 1是亚甲基，亚乙基，直链，任选的缩酮化羰基或任选醚化的羟基亚甲基，X 2是亚烷基，羰基或直链， X 3是羰基，氧代 - 低级 - 亚烷基，氧代（氮杂） - 低级 - 亚烷基或任选被苯基取代的亚烷基， 羟甲基，任选酯化或酰胺化的羧基，或高于α位置的羟基，其盐具有物质P-拮抗性质，可用作药物中的药物活性物质，用于治疗其发育物质P所起的障碍 一个重要的部分。