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Pharmaceutical composition containing aminoadamantane compounds useful for the treatment of agranulomatosis, Wegener's granulomatosis and immune deficiency diseases

机译:含有氨基金刚烷化合物的药物组合物,可用于治疗粒状肉瘤病,韦格纳肉芽肿病和免疫缺陷疾病

摘要

In the present invention, there is disclosed the use of an aminoadamantane compound of the general formula (I), in which Ri1, Ri2, Ri3 and Ri4 are selected independently on each other from -NRi5Ri6, -NRi5Ri6Ri7e+, hydrogen, aryl or heteroaryl with up to 7 ring members, alkyl containing 1 to 20 carbon atoms, alkenyl containing 1 to 20 carbon atoms and alkynyl containing 1 to 20 carbon atoms, wherein the alkyl, alkenyl and alkynyl residues can be branched, unbranched or cyclized and optionally substituted with halogen, aryl or heteroaryl with up to 7 ring members with the proviso that at least one of the residues Ri1, Ri2, Ri3 and Ri4 is represented by -NRi5Ri6 or -NRi5Ri6Ri7e+; and Ri5, Ri6 and Ri7 are selected independently on each other from hydrogen, aryl or heteroaryl with up to 7 ring members, alkyl containing 1 to 20 carbon atoms, alkenyl containing 1 to 20 carbon atoms and alkynyl containing 1 to 20 carbon atoms, wherein the alkyl, alkenyl and alkynyl residues can be branched, unbranched or cyclized and optionally substituted with halogen, aryl or heteroaryl with up to 7 ring members, or Ri5 and Ri6, together with the nitrogen atom, form a heterocyclic group with up to 7 ring members; for the preparation of a medicament useful for the treatment of agranulomatosis, Wegener's granulomatosis and/or immune deficiency diseases particularly AIDS, wherein the medicament increases the activity of neutrophils in a patient possessing already activated neutrophils through a concentration of the aminoadamantane compound of the general formula (I) of from 10e-6 to 10e-5 M in blood plasma.
机译:在本发明中,公开了通式(I)的氨基金刚烷化合物的用途,其中Ri1,Ri2,Ri3和Ri4彼此独立地选自-NRi5Ri6,-NRi5Ri6Ri7e +,氢,芳基或杂芳基最多7个环成员,含1至20个碳原子的烷基,含1至20个碳原子的烯基和含1至20个碳原子的炔基,其中烷基,烯基和炔基残基可以是支链,直链或环化的,并可选地被卤素取代;具有最多7个环成员的芳基或杂芳基,条件是残基Ri1,Ri2,Ri3和Ri4中至少一个由-NRi5Ri6或-NRi5Ri6Ri7e +表示;和Ri5,Ri6和Ri7彼此独立地选自氢,具有至多7个环成员的芳基或杂芳基,含1至20个碳原子的烷基,含1至20个碳原子的烯基和含1至20个碳原子的炔基,其中烷基,烯基和炔基残基可以是支链的,直链的或环化的,并可选地被卤素,芳基或杂芳基取代,具有最多7个环成员,或Ri5和Ri6与氮原子一起形成最多7个环的杂环成员;用于制备可用于治疗粒状肉瘤病,韦格纳肉芽肿病和/或免疫缺陷性疾病特别是AIDS的药物,其中该药物通过浓缩以下通式的氨基金刚烷类化合物来提高已具有中性粒细胞活性的患者的中性粒细胞活性(I)血浆中的10e-6至10e-5M。

著录项

  • 公开/公告号CZ299356B6

    专利类型

  • 公开/公告日2008-07-02

    原文格式PDF

  • 申请/专利权人 MERZ PHARMA GMBH & CO. KGAA;

    申请/专利号CZ19980000524

  • 发明设计人 ELSTNER ERICH F.;

    申请日1996-08-21

  • 分类号A61K31/13;G01N33/49;A61K31;A61K31/132;A61K31/135;A61K31/14;A61K31/42;A61K38/06;A61P7;A61P29;A61P31;A61P31/18;A61P33;A61P33/02;A61P35;A61P37;A61P37/04;C07C211/03;

  • 国家 CZ

  • 入库时间 2022-08-21 20:08:27

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