首页> 外国专利> Spirazabicyclical heterocyclic compound, pharmaceutical composition, use of a compound, and, treatment processes or prophylaxis of human diseases or conditions in which the activation of the nicotinic alpha7 receptor is beneficial, of psychotic disorders or disorders of intellectual weakening and imbalance of the normal circadian rhythm due to subsonic or supersonic travel, smoking cessation, nicotine addiction, pain and ulcerative colitis and preparation of a compound

Spirazabicyclical heterocyclic compound, pharmaceutical composition, use of a compound, and, treatment processes or prophylaxis of human diseases or conditions in which the activation of the nicotinic alpha7 receptor is beneficial, of psychotic disorders or disorders of intellectual weakening and imbalance of the normal circadian rhythm due to subsonic or supersonic travel, smoking cessation, nicotine addiction, pain and ulcerative colitis and preparation of a compound

机译:螺双环杂环化合物,药物组合物,该化合物的用途以及对烟碱性精神病或正常昼夜节律的智力减弱和失衡的疾病或烟碱α7受体活化有益的人类疾病或病症的治疗过程或预防由于亚音速或超音速旅行,戒烟,尼古丁成瘾,疼痛和溃疡性结肠炎以及化合物的制备

摘要

"SPIROAZABICYCLIC HETEROCYCLIC COMPOUND, PHARMACEUTICAL COMPOSITION, USE OF A COMPOUND, AND, TREATMENT PROCESSES OR PROPHYLAXIS OF HUMAN DISEASES OR CONDITIONS IN WHICH THE ALPHETIC DETECTOR OF THE HYDROPHIC NICHETRIC DETECTOR IS DEFECTIVE, DEFICIENTAL HISTORICAL DETECTIONS. NORMAL DUE TO SUBSYNIC OR SUPERSONIC TRAVEL, SMOKING CESSATION, NICOTIN VICE, PAIN AND ULCERATIVE COLITIS AND PREPARATION OF A COMPOUND ". A compound of formula (I) where n is 0 or 1; m is 0 or 1; p is 0 or 1; X is oxygen or sulfur; Y is CH, N or NO; W is oxygen, H ~ 2 ~ or F ~ 2 ~; A is N or C (R²); G is N or C (R³); D is N or C (R ^ 4 ^); with the proviso that no more than one of A, G and D is nitrogen, but at least one of Y, A, G and D is nitrogen or NO; R. is hydrogen or C ~ 1 ~ to C ~ 4 ~ alkyl; R², R³ and R ^ 4 ^ are independently hydrogen, halogen, C ~ 1 ~ -C ~ 4 ~ alkyl, C ~ 2 ~ -C ~ 4 ~ alkenyl, C ~ 2 ~ -C ~ 4 ~ alkyl, aryl, heteroaryl , OH, OC ~ 1 ~ -C ~ 4 ~ alkyl, CO ~ 2 ~ R ~ 1 ~, -CN, -NO ~ 2 ~, -NR ^ 5 ^ R ^ 6 ^, -CF ~ 3 ~, -OSO ~ 2 ~ CF ~ 3 ~ or R² and R³, or R³ and R ^ 4 ^, respectively, can together form another six-membered aromatic or heteroaromatic ring A and G, or G and D, respectively, containing between zero and two nitrogen atoms, and replaced by one to two of the following substituents; independently hydrogen, halogen, C ~ 1 ~ -C ~ 4 ~ alkyl, C ~ 2 ~ -C ~ 4 ~ alkaline, C ~ 2 ~ -C ~ 4 ~ alkynyl, aryl, heteroaryl, OH, OC ~ 1 ~ - alkyl C ~ 4 ~, CO ~ 2 ~ R ~ 1 ~, -CN, -NO ~ 2 ~, -NR ^ 5 ^ R ^ 6 ^, -CF ~ 3 ~, -OSO ~ 2 ~ CF ~ 3 ~; R ^ 5 ^ and R ^ 6 ^ are independently hydrogen, C ~ 1 ~ -C ~ 4 ~ alkyl, C (O) R ^ 7 ^, C (O) NHR ^ 8 ^, C (O) OR ^ 9 ^ , SO ~ 2 ~ R ^ 10 ^, or together can be (CH ~ 2 ~) ~ j ~ Q (CH ~ 2 ~) ~ k ~, where Q is O, S, NR ^ 11 ^ or a bond ; j is 2 to 7, k is 0 to 2; R ^ 7 ^, R ^ 8 ^, R ^ 9 ^, R ^ 10 ^ and R ^ 11 ^ are independently C ~ 1 ~ -C ~ 4 ~ alkyl, aryl or heteroaryl, or an enantiomer thereof, and their salts pharmaceutically acceptable, processes for preparing them, composition containing them, and their use in therapy, especially in the treatment or prophylaxis of psychotic disorders and intellectual impairment disorders.
机译:“螺旋形的杂多波检测器在正常情况下是决定性的,在一定程度上,螺旋形的杂环化合物,药物组合物,化合物的使用以及人类疾病或状况的治疗过程或前兆是决定性的,在很大程度上取决于正常的细菌。停止,尼古丁副产物,疼痛和溃疡性结肠炎以及化合物的制备”。式(I)的化合物,其中n为0或1; m为0或1; p为0或1; X是氧或硫; Y为CH,N或NO; W是氧,H〜2〜或F〜2〜; A为N或C(R 2); G为N或C(R 3); D为N或C(R ^ 4 ^);条件是A,G和D中不超过一个是氮,但Y,A,G和D中至少一个是氮或NO; R.是氢或C〜1〜至C〜4〜烷基; R 2,R 3和R ^ 4 ^独立地为氢,卤素,C〜1〜-C〜4〜烷基,C〜2〜-C〜4〜烯基,C〜2〜-C〜4〜烷基,芳基,杂芳基,OH,OC〜1〜-C〜4〜烷基,CO〜2〜R〜1〜,-CN,-NO〜2〜,-NR ^ 5 ^ R ^ 6 ^,-CF〜3〜,-OSO 〜2〜CF〜3〜或R²和R³,或R³和R ^ 4 ^可以一起形成另一个六元芳族或杂芳族环A和G,或G和D,分别包含零个至两个氮原子原子,并被以下一到两个取代基取代;独立地为氢,卤素,C〜1〜-C〜4〜烷基,C〜2〜-C〜4〜碱​​性,C〜2〜-C〜4〜炔基,芳基,杂芳基,OH,OC〜1〜-烷基C〜4〜,CO〜2〜R〜1〜,-CN,-NO〜2〜,-NR ^ 5 ^ R ^ 6 ^,-CF〜3〜,-OSO〜2〜CF〜3〜; R ^ 5 ^和R ^ 6 ^独立地是氢,C〜1〜-C〜4〜烷基,C(O)R ^ 7 ^,C(O)NHR ^ 8 ^,C(O)OR ^ 9 ^ ,SO〜2〜R ^ 10 ^,或一起可以是(CH〜2〜)〜j〜Q(CH〜2〜)〜k〜,其中Q为O,S,NR ^ 11 ^或键; j为2至7,k为0至2; R ^ 7 ^,R ^ 8 ^,R ^ 9 ^,R ^ 10 ^和R ^ 11 ^独立地为C〜1〜-C〜4〜烷基,芳基或杂芳基或其对映异构体及其盐可接受的制备方法,包含它们的组合物及其在治疗中的用途,尤其是在治疗或预防精神病和智力障碍方面。

著录项

  • 公开/公告号BR9810924A

    专利类型

  • 公开/公告日2000-08-15

    原文格式PDF

  • 申请/专利权人 ASTRA AKTIEBOLAGET;

    申请/专利号BR19989810924

  • 申请日1998-07-10

  • 分类号C07D491/22;A61K31/435;A61K31/44;

  • 国家 BR

  • 入库时间 2022-08-22 01:57:08

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