Thiadiazine derivatives and use thereof as positive AMPA receptor modulators
    1.
    发明授权
    Thiadiazine derivatives and use thereof as positive AMPA receptor modulators 失效
    噻二嗪衍生物及其作为阳性AMPA受体调节剂的用途

    公开(公告)号:US07476668B2

    公开(公告)日:2009-01-13

    申请号:US10555743

    申请日:2004-05-04

    IPC分类号: C07D513/04 A61K31/542

    CPC分类号: C07D513/04

    摘要: Compounds of formula (I): wherein: A represents thienyl, furyl, pyrrolyl, oxathiol, thiazole, isothiazole, oxazole or imidazole, represents a single bond or a double bond, R1 represents hydrogen, linear or branched (C1-C6)alkyl optionally substituted by one or more groups selected from halogen or (C1-C6)alkoxy-(C1-C6)alkyl, R2 represents hydrogen or linear or branched (C1-C6)alkyl group optionally substituted by one or more halogen, R3 represents hydrogen or a group selected from linear or branched (C1-C6)alkyl, CONHR′ and SO2NHR′ wherein R′ represents linear or branched (C1-C6)alkyl, its enantiomers and diastereoisomers, and addition salts thereof with a pharmaceutically acceptable acid or base. Medicinal products containing the same, which are useful as AMPA inhibitors.

    摘要翻译: 式(I)的化合物:其中:A表示噻吩基,呋喃基,吡咯基,氧硫杂环戊烷,噻唑,异噻唑,恶唑或咪唑,其中:=“3.13mm”wi =“6.35mm” file =“US07476668-20090113-P00001.TIF”alt =“custom character”img-content =“character”img-format =“tif”/>表示单键或双键,R1表示氢,直链或支链( 任选被一个或多个选自卤素或(C 1 -C 6)烷氧基 - (C 1 -C 6)烷基的基团取代的C 1 -C 6烷基,R 2表示氢或任选被一个或多个(C 1 -C 6)烷氧基取代的直链或支链 卤素,R3表示氢或选自直链或支链(C1-C6)烷基,CONHR'和SO2NHR'的基团,其中R'表示直链或支链(C1-C6)烷基,其对映异构体和非对映异构体,以及其加成盐与 药学上可接受的酸或碱。 含有该药物的药物,可用作AMPA抑制剂。

    Fluorinated benzothiadiazine compounds
    2.
    发明授权
    Fluorinated benzothiadiazine compounds 失效
    氟化苯并噻二嗪化合物

    公开(公告)号:US07268129B2

    公开(公告)日:2007-09-11

    申请号:US11041495

    申请日:2005-01-24

    CPC分类号: C07D285/24

    摘要: Compounds of formula (I): wherein: RF represents monofluoro- or polyfluoro-alkyl or monofluoro- or polyfluoro-cycloalkylalkyl, R1 represents hydrogen or a group selected from alkylaminocarbonyl and optionally substituted alkyl, R2 represents hydrogen, halogen or a group selected from cycloalkyl and optionally substituted alkyl, R3 to R6, which may be the same or different, each represent an atom or group selected from hydrogen, halogen, nitro, cyano, alkylsulphonyl, hydroxy, alkoxy, optionally substituted alkyl and optionally substituted amino, its optical isomers when they exist, and also their addition salts with a pharmaceutically acceptable acid or base. Medicinal products containing the same which are useful as AMPA modulators.

    摘要翻译: 式(I)化合物:其中:R F表示单氟或多氟 - 烷基或单氟或多氟环烷基烷基,R 1表示氢或选自烷基氨基羰基 和任选取代的烷基,R 2表示氢,卤素或选自环烷基和任选取代的烷基,R 3至R 6的基团,其中 可以相同或不同,各自表示选自氢,卤素,硝基,氰基,烷基磺酰基,羟基,烷氧基,任选取代的烷基和任选取代的氨基的原子或基团,当它们存在时的光学异构体,以及它们与 药学上可接受的酸或碱。 含有与AMPA调节剂有用的药用产品。

    Thiadiazine derivatives and use thereof as positive ampa receptor modulators
    5.
    发明申请
    Thiadiazine derivatives and use thereof as positive ampa receptor modulators 失效
    噻二嗪衍生物及其作为正安培受体调节剂的用途

    公开(公告)号:US20070004709A1

    公开(公告)日:2007-01-04

    申请号:US10555743

    申请日:2004-05-04

    IPC分类号: A61K31/549 C07D498/02

    CPC分类号: C07D513/04

    摘要: Compounds of formula (I): wherein: A represents thienyl, furyl, pyrrolyl, oxathiol, thiazole, isothiazole, oxazole or imidazole, represents a single bond or a double bond, R1 represents hydrogen, linear or branched (C1-C6)alkyl optionally substituted by one or more groups selected from halogen or (C1-C6)alkoxy-(C1-C6)alkyl, R2 represents hydrogen or linear or branched (C1-C6)alkyl group optionally substituted by one or more halogen, R3 represents hydrogen or a group selected from linear or branched (C1-C6)alkyl, CONHR′ and SO2NHR′ wherein R′ represents linear or branched (C1-C6)alkyl, its enantiomers and diastereoisomers, and addition salts thereof with a pharmaceutically acceptable acid or base. Medicinal products containing the same, which are useful as AMPA inhibitors.

    摘要翻译: 式(I)化合物:其中:A表示噻吩基,呋喃基,吡咯基,氧硫杂环戊烷,噻唑,异噻唑,恶唑或咪唑,表示单键或双键,R <1 表示任选被一个或多个选自卤素或(C 1 -C 6)烷基的基团取代的直链或支链(C 1 -C 6 -C 6)烷基, -C 6 -C 6烷氧基 - (C 1 -C 6 -C 6)烷基,R 2表示氢或直链或 任选被一个或多个卤素取代的支链(C 1 -C 6 -C 6)烷基,R 3 3表示氢或选自直链或 支链(C 1 -C 6 -C 6)烷基,CONHR'和SO 2 NHR',其中R'表示直链或支链(C 1 -C 6) 1 -C 6烷基,其对映体和非对映异构体及其加成盐w 具有药学上可接受的酸或碱。 含有该药物的药物,可用作AMPA抑制剂。

    Benzopyran derivatives, method of production and use thereof

    公开(公告)号:US20070112063A1

    公开(公告)日:2007-05-17

    申请号:US10588265

    申请日:2005-01-21

    IPC分类号: A61K31/353

    摘要: The invention relates to novel benzopyran derivatives of formula I, to their method of production, to composition comprising the derivatives and use thereof. wherein: R1, R2, R3 and R4 are independently hydrogen, halogen, C1-6-alkyl, C3-8-cycloalkyl, hydroxy, C1-6-alkoxy, C1-6-alkoxy-C1-6-alkyl, nitro, amino, cyano, cyanomethyl, perhalomethyl, C1-6-monoalkyl- or dialkylamino, sulfamoyl, C1-6-alkylthio, C1-6-alkylsulfonyl, C1-6-alkylsulfinyl, formyl, C1-6-alkylcarbonylamino, R8arylthio, R8arylsulfinyl, R8arylsulfonyl, C1-6-alkoxycarbonyl, C1-6-alkoxycarbonyl-C1-6-alkyl, carbamoyl, carbamoylmethyl, C1-6-monoalkyl- or dialkylaminocarbonyl, C1-6-monoalkyl- or dialkylaminothiocarbonyl, ureido, C1-6-monoalkyl- or dialkylaminocarbonylamino, thioureido, C1-6-monoalkyl- or dialkylaminothiocarbonylamino, C1-6-monoalkyl- or dialkylaminosulfonyl, carboxy, carboxy-C1-6-alkyl, acyl, R8aryl, R8aryl-C1-6-alkyl, R8aryloxy; R5 and R6 are each independently hydrogen, C1-6-alkyl or, R5 and R6 taken together with the carbon atom to which they are attached form a 3- to 6-membered carbocyclic ring; R7 is 2-, 3- or 4-pyridyl optionally mono- or polysubstituted by R1; R7 is 2- or 3-thienyl optionally mono- or polysubstituted substituted by R1 or R7 is phenyl optionally mono- or polysubstituted by R1 with the exception of or R7 representing C6H5; R8 is hydrogen, halogen, C1-6-alkyl, C3-8-cycloalkyl, hydroxy, C1-6-alkoxy, nitro, amino, cyano, cyanomethyl, perhalomethyl; or a salt thereof with a pharmaceutically acceptable acid or base, or any optical isomer or mixture of optical isomers, including a racemic mixture or any polymorphic and tautomeric form.

    Benzopyran derivatives, method of production and use thereof
    9.
    发明授权
    Benzopyran derivatives, method of production and use thereof 失效
    苯并吡喃衍生物,其制备方法和用途

    公开(公告)号:US07507761B2

    公开(公告)日:2009-03-24

    申请号:US10588265

    申请日:2005-01-21

    摘要: The invention relates to novel benzopyran derivatives of formula I, to their method of production, to composition comprising the derivatives and use thereof. wherein: R1, R2, R3 and R4 are independently hydrogen, halogen, C1-6-alkyl, C3-8-cycloalkyl, hydroxy, C1-6-alkoxy, C1-6-alkoxy-C1-6-alkyl, nitro, amino, cyano, cyanomethyl, perhalomethyl, C1-6-monoalkyl- or dialkylamino, sulfamoyl, C1-6-alkylthio, C1-6-alkylsulfonyl, C1-6-alkylsulfinyl, formyl, C1-6-alkylcarbonylamino, R8arylthio, R8arylsulfinyl, R8arylsulfonyl, C1-6-alkoxycarbonyl, C1-6-alkoxycarbonyl-C1-6-alkyl, carbamoyl, carbamoylmethyl, C1-6-monoalkyl- or dialkylaminocarbonyl, C1-6-monoalkyl- or dialkylaminothiocarbonyl, ureido, C1-6-monoalkyl- or dialkylaminocarbonylamino, thioureido, C1-6-monoalkyl- or dialkylaminothiocarbonylamino, C1-6-monoalkyl- or dialkylaminosulfonyl, carboxy, carboxy-C1-6-alkyl, acyl, R8aryl, R8aryl-C1-6-alkyl, R8aryloxy; R5 and R6 are each independently hydrogen, C1-6-alkyl or, R5 and R6 taken together with the carbon atom to which they are attached form a 3- to 6-membered carbocyclic ring; R7 is 2-, 3- or 4-pyridyl optionally mono- or polysubstituted by R1; R7 is 2- or 3-thienyl optionally mono- or polysubstituted substituted by R1 or R7 is phenyl optionally mono- or polysubstituted by R1 with the exception of or R7 representing C6H5; R8 is hydrogen, halogen, C1-6-alkyl, C3-8-cycloalkyl, hydroxy, C1-6-alkoxy, nitro, amino, cyano, cyanomethyl, perhalomethyl; or a salt thereof with a pharmaceutically acceptable acid or base, or any optical isomer or mixture of optical isomers, including a racemic mixture or any polymorphic and tautomeric form.

    摘要翻译: 本发明涉及式I的新型苯并吡喃衍生物,其制备方法,包含衍生物的组合物及其用途。 其中:R 1,R 2,R 3和R 4独立地是氢,卤素,C 1-6 - 烷基,C 3-8 - 环烷基,羟基,C 1-6 - 烷氧基,C 1-6 - 烷氧基-C 1-6 - 烷基,硝基,氨基 氰基,氰基甲基,全卤代甲基,C 1-6 - 单烷基 - 或二烷基氨基,氨磺酰基,C 1-6 - 烷硫基,C 1-6 - 烷基磺酰基,C 1-6 - 烷基亚磺酰基,甲酰基,C 1-6 - 烷基羰基氨基,R 8芳硫基,R 8芳基亚磺酰基, C 1-6 - 烷氧基羰基-C 1-6 - 烷基,氨基甲酰基,氨基甲酰基甲基,C 1-6 - 单烷基 - 或二烷基氨基羰基,C 1-6 - 单烷基 - 或二烷基氨基硫代羰基,脲基,C 1-6 - 单烷基 - 或二烷基氨基羰基氨基 羧基-C 1-6 - 烷基,酰基,R 8芳基,R 8芳基-C 1-6 - 烷基,R 8芳氧基,C 1-6 - 烷基 - 或二烷基氨基硫代羰基氨基, R 5和R 6各自独立地为氢,C 1-6 - 烷基或者R 5和R 6与它们所连接的碳原子一起形成3-至6-元碳环; R7是任选被R1单取代或多取代的2-,3-或4-吡啶基; R 7是任选被R 1或R 7取代的单或多取代的2-或3-噻吩基,R 3是任选被R1单取代或多取代的苯基,或者R 7代表C 6 H 5; R 8为氢,卤素,C 1-6 - 烷基,C 3-8 - 环烷基,羟基,C 1-6 - 烷氧基,硝基,氨基,氰基,氰基甲基,全卤代甲基。 或其盐与药学上可接受的酸或碱,或任何光学异构体或光学异构体的混合物,包括外消旋混合物或任何多晶型和互变异构形式。