首页> 外国专利> 1-AMINO TRIAZOLO4,3-AQUINAZOLINE-5- ONES AND/OR -5-THIONES INHIBITING PHOSPHODIESTERASE IV, PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM

1-AMINO TRIAZOLO4,3-AQUINAZOLINE-5- ONES AND/OR -5-THIONES INHIBITING PHOSPHODIESTERASE IV, PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM

机译:抑制磷酸酯酶IV的1-氨基三唑并[4,3-A]喹唑啉-5-酮和/或-5-亚硫基,其制备方法和包含它们的药物组合物

摘要

The present invention relates to triazolo[4,3-a]quinazoline-5-ones and 5-thiones of Formula I and Formula II, whereby I and II are position isomers of group R on nitrogen 3 or 4. Optionally, the invention also relates to the racemic forms, isomers and pharmaceutically acceptable salts thereof. The invention further relates to a method for the production thereof and to compositions containing said derivatives. The compounds act as inhibitors of phosphodiesterase IV (PDE-4) and, as such, have utility in treating asthma, chronic bronchitis, acutte pulmonary attack, atopic dermatitis, pulmonary hypertension, pulmonary insufficiency, cardiac insufficiency, psoriasis, inflammatory conditions of the digestive system such as haemorrhagic rectocolitis and Crohn's disease, acute respiratory distress syndrome, acute pancreatitis, benign hypertrophy of the prostate, rheumatoid arthritis, multiple sclerosis, depression, ischaemia-induced neuronal damage, partial cerebral ischaemia, and cancer such as malignant tumor and chronic lymphoid leukemia.
机译:本发明涉及式I和式II的三唑并[4,3-a]喹唑啉-5-酮和5-硫酮,其中I和II是在氮3或4上的R基团的位置异构体。 “外消旋体”涉及其外消旋形式,异构体及其药学上可接受的盐。本发明进一步涉及其生产方法和含有所述衍生物的组合物。该化合物可作为磷酸二酯酶IV(PDE-4)的抑制剂,因此可用于治疗哮喘,慢性支气管炎,剧烈肺部发作,特应性皮炎,肺动脉高压,肺功能不全,心脏功能不全,牛皮癣,消化道炎性疾病系统,例如出血性直肠结肠炎和克罗恩氏病,急性呼吸窘迫综合征,急性胰腺炎,前列腺良性肥大,类风湿关节炎,多发性硬化症,抑郁症,局部缺血引起的神经元损害,部分脑缺血以及恶性肿瘤和慢性淋巴瘤等癌症白血病。

著录项

  • 公开/公告号HU0202656A3

    专利类型

  • 公开/公告日2004-12-28

    原文格式PDF

  • 申请/专利权人 WARNER-LAMBERT CO. MORRIS PLAINS NEW JERSEY;

    申请/专利号HU20020002656

  • 发明设计人

    申请日2000-04-28

  • 分类号C07D487/04;

  • 国家 HU

  • 入库时间 2022-08-21 22:17:56

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