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    • 7. 发明申请
    • TRIAZA-SPIROPIPERIDINE DERIVATIVES FOR USE AS GLYT-1 INHIBITORS IN THE TREATMENT OF NEUROLOGICAL AND NEUROPSYCHIATRIC DISORDERS
    • 用于治疗神经病学和神经病学疾病的GLYT-1抑制剂的三氮唑嘌呤衍生物
    • WO2005040166A1
    • 2005-05-06
    • PCT/EP2004/011552
    • 2004-10-14
    • F.HOFFMANN-LA ROCHE AGCECCARELLI, Simona, MariaPINARD, EmmanuelSTALDER, Henri
    • CECCARELLI, Simona, MariaPINARD, EmmanuelSTALDER, Henri
    • C07D471/10
    • C07D471/10
    • The invention relates to compounds of the general formula (I), wherein A-A is -CH 2 -CH 2 -, -CH 2 -CH 2 -CH 2 -, -CH 2 -0- or -0-CH 2 -; x is hydrogen or hydroxy; R 1 is aryl or heteroaryl, unsubstituted or substituted by one or more substituents, selected from the group consisting of lower alkyl, lower alkoxy, halogen or trifluoromethyl; R 2 is aryl or heteroaryl, unsubstituted or substituted by one or more substituents, selected from the group consisting of lower alkyl, lower alkoxy, halogen or trifluoromethyl, or is lower alkyl, -(CH 2 ) n -­cycloalkyl, -(CH 2 ) n -CF 3 , -(CH 2 ) p -0-lower alkyl, -(CH 2 ) 1,2 -phenyl, optionally substituted by halogen, lower alkyl, lower alkoxy or trifluoromethyl, or is -(CH 2 ) p -NRR", wherein W and R" form together with the N-atom a heterocyclic ring, selected from the group consisting of piperidine, morpholine, thiomorpholine or 1, I-dioxo thiomorpholine; R 3 , R 4 are independently from each other hydrogen, lower alkyl, phenyl or benzyl; R 5 is hydrogen, lower alkyl or benzyl; R 6 is hydrogen or lower alkyl; n is 0, 1 or 2; and p is 2 or 3; and to pharmaceutically acceptable acid addition salts thereof for the treatment of psychoses, pain, neurodegenerative disfunction in memory and learning, schizophrenia, dementia and other diseases in which cognitive processes are impaired, such as attention deficit disorders or Alzheimer's disease.
    • 本发明涉及通式(I)的化合物,其中A-A为-CH 2 -CH 2 - , - CH 2 -CH 2 -CH 2 - , - CH 2 O-或-O-CH 2 - 。 x是氢或羟基; R 1是未取代的或被一个或多个选自低级烷基,低级烷氧基,卤素或三氟甲基的取代基取代的芳基或杂芳基; R 2是未被取代或被一个或多个选自低级烷基,低级烷氧基,卤素或三氟甲基的取代基取代的芳基或杂芳基,或者是低级烷基, - (CH 2)n - 环烷基, - (CH 2 ) - (CH 2)p -O-低级烷基, - (CH 2)1,2 - 苯基,任选被卤素,低级烷基,低级烷氧基或三氟甲基取代,或是 - (CH 2)p -NRR“ 其中W和R“与N-原子一起形成一个选自哌啶,吗啉,硫代吗啉或1,1-二氧代硫代吗啉的杂环; R 3,R 4彼此独立地为氢,低级烷基,苯基或苄基; R 5是氢,低级烷基或苄基; R 6是氢或低级烷基; n为0,1或2; p为2或3; 以及其药学上可接受的酸加成盐,用于治疗精神病,疼痛,记忆和学习中的神经变性功能障碍,精神分裂症,痴呆和其他认知过程受损的其他疾病,如注意力缺陷障碍或阿尔茨海默病。
    • 9. 发明申请
    • PIPERIDINE-BENZENESULFONAMIDE DERIVATIVES
    • 哌嗪 - 苯甲酰胺衍生物
    • WO2004072034A1
    • 2004-08-26
    • PCT/EP2004/001211
    • 2004-02-10
    • F. HOFFMANN-LA ROCHE AGALBERATI-GIANI, DanielaCECCARELLI, Simona, MariaPINARD, EmmanuelSTALDER, Henri
    • ALBERATI-GIANI, DanielaCECCARELLI, Simona, MariaPINARD, EmmanuelSTALDER, Henri
    • C07D211/58
    • C07D413/12C07D211/58C07D401/08C07D401/12C07D405/04C07D405/12C07D409/12C07D413/14
    • The present invention relates to compounds of the general formula (I) wherein R 1 is lower alkyl, -(CH 2 ) n -aryl, unsubstituted or substituted by one or two substituents, selected from the group consisting of lower alkyl, lower alkoxy, -OCF 3 , halogen, -NR’R” or trifluoromethyl, or heteroaryl; R 2 is lower alkyl, -(CH 2 ) n -aryl, unsubstituted or substituted by one or two substituents, selected from the group consisting of lower alkyl, lower alkoxy, halogen, trifluoromethyl, nitro, cyano, -NR’R”, hydroxy, or by a heteroaryl group, or is heteroaryl, unsubstituted or substituted by one or two substituents, selected from the group consisting of lower alkyl or halogen; R 3 is heteroaryl or is aryl, unsubstituted or substituted by halogen or lower alkyl; R 4 is hydrogen or hydroxy; A is -S(O) 2 -or-C(O)-; X,Y are independently from each other -CH 2 - or -O-, with the proviso that X and Y are not simultaneously -O; R’R” are independently from each other hydrogen, lower alkyl or -C(O)-lower alkyl; n is 0, 1 or 2; and to pharmaceutically acceptable acid addition salts thereof. The compounds may be used for the treatment of psychoses, pain, disfunction in memory and learning, schizophrenia, dementia and other diseases in which cognitive processes are impaired, such as attention deficit disorders or Alzheimer’s disease.
    • 本发明涉及通式(I)的化合物,其中R 1为低级烷基, - (CH 2)n - 芳基,未取代或被一个或两个选自以下的取代基取代:低级烷基,低级烷氧基 ,-OCF 3,卤素,-NR'R“或三氟甲基或杂芳基; R 2是低级烷基, - (CH 2)n - 芳基,未取代或被一个或两个取代基取代,所述取代基选自低级烷基 ,低级烷氧基,卤素,三氟甲基,硝基,氰基,-NR'R“,羟基或杂芳基,或是未被取代或被一个或两个选自低级烷基或卤素的取代基取代的杂芳基; R 3是杂芳基或未被取代或被卤素或低级烷基取代的芳基; R 4是氢或羟基; A是-S(O)2 - 或-C(O) - ; X,Y彼此独立地为-CH 2 - 或-O-,条件是X和Y不同时为-O; R'R“彼此独立地为氢,低级烷基或-C(O) - 低级烷基; n为0,1或2;以及其药学上可接受的酸加成盐。该化合物可用于治疗精神病 记忆障碍,学习障碍,精神分裂症,痴呆等认知过程受损的疾病,如注意力缺陷障碍或阿尔茨海默病。