首页> 外国专利> DERIVATIVES OF 4 (4-ALKOXI-3-HIDROXIFENIL) -2-PIRROLIDONE AS PDE-4 INHIBITORS FOR THE TREATMENT OF NEUROLOGICAL SYNDROMES.

DERIVATIVES OF 4 (4-ALKOXI-3-HIDROXIFENIL) -2-PIRROLIDONE AS PDE-4 INHIBITORS FOR THE TREATMENT OF NEUROLOGICAL SYNDROMES.

机译:4(4-ALKOXI-3-HIDROXIFENIL)-2-吡咯烷酮作为PDE-4抑制剂的衍生物,用于治疗神经系统综合征。

摘要

Compound of formula I: ** (See formula) ** in which R1 is 3 (R) -tetrahydrofuranyl; R2 is alkyl with 1 to 4 carbon atoms, which is unsubstituted or substituted one or more times by halogen; R3 is H, arylalkyl with 7 to 16 carbon atoms, which is unsubstituted or substituted one or more times by halogen, alkyl, hydroxy, alkoxy, nitro, methylenedioxy, ethylenedioxy, amino, alkylamino, dialkylamino, hydroxyalkyl, hydroxyalkoxy, carboxy, cyano , acyl, alkoxycarbonyl, alkylthio, alkylsulfinyl, alkylsulfonyl, phenoxy and acyloxy, or combinations thereof, heterocyclic alkyl group, which is saturated, partially saturated or completely unsaturated, having 5 to 10 ring atoms where at least 1 ring atom it is an N, O or S atom, which is unsubstituted or substituted one or more times in the heterocyclic portion by halogen, aryl, alkyl, alkoxy, cyano, trifluoromethyl, nitro, oxo, amino, alkylamino, dialkylamino, carboxy or combinations thereof. same and / or substituted in the alkyl portion by halogen, oxo, cyano, or combinations thereof. alkoxyalkyl with 3 to 8 carbon atoms, -C (O) R4, or -CH2CONHR5; R4 is aryl with 6 to 14 carbon atoms, i.e. unsubstituted or substituted one or more times by halogen, CF3, OCF3, alkyl, hydroxy, alkoxy, nitro, methylenedioxy, ethylenedioxy, amino, alkylamino, dialkylamino, hydroxyalkyl, hydroxyalquoxy, carboxy , cyano, acyl, alkoxycarbonyl, alkylthio, alkylsulfinyl, alkylsulfonyl, phenoxy, acylamido and acyloxy, or combinations thereof, or a heterocyclic group, which is saturated, partially saturated or completely unsaturated, with 5 to 10 ring atoms in which at least 1 ring atom is an N, O or S atom, which is unsubstituted or substituted one or more times by halogen, aryl, alkyl, alkoxy, cyano, trifluoromethyl, nitro, oxo, amino, alkylamino, dialkylamino, or combinations of the same; and R5 is aryl with 6 to 14 carbon atoms, which is unsubstituted or substituted one or more times by halogen, CF3, OCF3, alkyl, hydroxy, alkoxy, nitro, methylenedioxy, ethylenedioxy, amino, alkylamino, dialkylamino, hydroxyalkyl, hydroxyalquoxy, carboxy, cyano, acyl, alkoxycarbonyl, alkylthio, alkylsulfinyl, alkylsulfonyl, phenoxy, acylamido and acyloxy, or combinations thereof, or a heterocyclic group, which is saturated, partially saturated or completely unsaturated, with 5 to 10 ring atoms where minus 1 ring atom is an N, O or S atom, which is unsubstituted or substituted one or more times by halogen, aryl, alkyl, alkoxy, alkoxycarbonyl, cyano, trifluoromethyl, nitro, oxo, amino, alkylamino, dialkylamino, or combinations thereof, with the proviso that: (a) when R2 is CH3, R3 is not H.
机译:式I化合物:**(参见式)**其中R 1为3(R)-四氢呋喃基; R 2为碳数为1至4的烷基,其未被取代或被卤素取代一次或多次。 R 3是H,具有7至16个碳原子的芳烷基,其未被取代或被卤素,烷基,羟基,烷氧基,硝基,亚甲基二氧基,乙二氧基,氨基,烷基氨基,二烷基氨基,羟基烷基,羟基烷氧基,羧基,氰基,酰基,烷氧基羰基,烷硫基,烷基亚磺酰基,烷基磺酰基,苯氧基和酰氧基,或它们的组合,为饱和,部分饱和或完全不饱和的具有5至10个环原子的杂环烷基,其中至少1个环原子为N,O或S原子,其未被取代或在杂环部分中被卤素,芳基,烷基,烷氧基,氰基,三氟甲基,硝基,氧代,氨基,烷基氨基,二烷基氨基,羧基或其组合取代一次或多次。在烷基部分中相同和/或被卤素,氧代,氰基或其组合取代。具有3至8个碳原子的烷氧基烷基,-C(O)R 4或-CH 2 CONHR 5; R 4是具有6至14个碳原子的芳基,即未被取代或被卤素,CF 3,OCF 3,烷基,羟基,烷氧基,硝基,亚甲基二氧基,乙二氧基,氨基,烷基氨基,二烷基氨基,羟烷基,羟基烷氧基,羧基,氰基取代或取代一次或多次。 ,酰基,烷氧基羰基,烷硫基,烷基亚磺酰基,烷基磺酰基,苯氧基,酰基酰胺基和酰氧基,或其组合,或具有5至10个环原子的饱和,部分饱和或完全不饱和的杂环基,其中至少1个环原子为N,O或S原子,其未被取代或被卤素,芳基,烷基,烷氧基,氰基,三氟甲基,硝基,氧代,氨基,烷基氨基,二烷基氨基或它们的组合取代一次或多次; R5是具有6至14个碳原子的芳基,其未被取代或被卤素,CF3,OCF3,烷基,羟基,烷氧基,硝基,亚甲基二氧基,亚乙基二氧基,氨基,烷基氨基,二烷基氨基,羟基烷基,羟基烷氧基,羧基取代或被取代一次或多次。 ,氰基,酰基,烷氧基羰基,烷硫基,烷基亚磺酰基,烷基磺酰基,苯氧基,酰基酰胺基和酰氧基,或它们的组合,或具有5至10个环原子的饱和,部分饱和或完全不饱和的杂环基,其中-1个环原子为负N,O或S原子,未被取代或被卤素,芳基,烷基,烷氧基,烷氧羰基,氰基,三氟甲基,硝基,氧代,氨基,烷基氨基,二烷基氨基或其组合取代或多次取代,但条件是:(a)当R2为CH3时,R3不为H。

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