首页> 外国专利> Compound, process for preparing a compound, composition, use of a compound, and methods for treating or preventing a disease in a mammal where a phosphodiesterase isoenzyme inhibitor and / or a bronchodilator should be expected to be beneficial for the treatment or prevention of asthma in a mammal and for the treatment or prevention of chronic obstructive pulmonary disease (copd) in a mammal

Compound, process for preparing a compound, composition, use of a compound, and methods for treating or preventing a disease in a mammal where a phosphodiesterase isoenzyme inhibitor and / or a bronchodilator should be expected to be beneficial for the treatment or prevention of asthma in a mammal and for the treatment or prevention of chronic obstructive pulmonary disease (copd) in a mammal

机译:化合物,制备化合物的方法,组合物,化合物的使用以及在哺乳动物中治疗或预防疾病的方法,其中预期磷酸二酯酶同工酶抑制剂和/或支气管扩张剂对治疗或预防哮喘有益。哺乳动物,用于治疗或预防哺乳动物的慢性阻塞性肺疾病(copd)

摘要

"COMPOUND, PROCESS TO PREPARE A COMPOUND, COMPOSITION, USE OF A COMPOUND, AND METHODS FOR THE TREATMENT OR PREVENTION OF A DISEASE IN A MAMMALIAN WHERE TO EXPOSE AN INHIBITOR OF PHOSPHODIESTERASE AND / OR A BRONCODYLOSIS, OR BRONZODYCHEMISTRY FOR THE TREATMENT OR PREVENTION OF ASTHMA IN A MAMMALIAN AND FOR THE TREATMENT OR PREVENTION OF CHRONIC OBSTRUCTIVE PULMONARY DISEASE (COPD) IN A MAMMALIAN ". The compounds of the general formula (I) in which each of R ^ 1 ^ ^ and R ^ 2 ^ ^ independently represents a C ~ 1-6 ~ alkyl or C ~ 2-7 ~ acyl group; X represents OCH ~ 2 ~ or a CR ^ 3 ^ R ^ 4 ^ group, each of R ^ 3 ^ or R ^ 4 ^ independently representing a hydrogen atom or a C ~ 1-3 ~ alkyl group; R5 represents a hydrogen atom or a C ~ 1-3 ~ alkyl, C ~ 2-3 ~ alkenyl or C ~ 2-3 ~ alkynyl group; R ^ 3 ^ represents a hydrogen atom or a C ~ 1-6 ~ alkyl, C ~ 2-6 ~ alkenyl, C ~ 2-6 ~ alkynyl, amino, C ~ 1-6 ~ amino, dialkyl (C ~ 1-6 ~) amino or C ~ 2-7 ~ acylamino; each of R ^ 7 ^ and R ^ 8 ^ independently represents a hydrogen or halogen atom or a hydroxy, trifluoromethyl, C ~ 1-6 ~ alkyl, C ~ 2-6 ~ alkenyl, C ~ 2-6 ~ alkynyl, C ~ 2-7 ~ acyl, C ~ 1-6 ~ alkylthio, C ~ 1-6 ~ alkoxy, C ~ 3-6 ~ cycloalkyl; R ^ 9 ^ represents a hydrogen or halogen atom or a hydroxy, trifluoromethyl, C ~ 1-6 ~ alkyl, C ~ 2-6 ~ alkenyl, C ~ 2-6 ~ alkynyl, C ~ 2-7 ~ acyl group, C ~ 1-6 ~ alkylthio, C ~ 1-6 ~ alkoxy or C ~ 3-6 ~ cycloalkyl, or salts thereof are useful for the treatment of respiratory disorders such as asthma. The compounds of the invention have a longer duration of action than the known compound trequininsin (9,10-dimethoxy-3-methyl-2-mesitylimino-2,3,6,7-tetrahydro-4H-pyrimido [6, 1 -a] isoquinolin-4-one) and threquinsin does not taste very bitter.
机译:“化合物,制备化合物的过程,化合物的使用,化合物的治疗或预防哺乳动物的疾病的方法,该疾病可引起磷酸二酯酶和/或铜锈病或铜环过氧化物酶的抑制剂哺乳动物的哮喘,以及哺乳动物的慢性阻塞性肺疾病(COPD)的治疗或预防”。通式(I)的化合物,其中R ^ 1 ^ ^和R ^ 2 ^ ^各自独立地表示C〜1-6〜烷基或C〜2-7〜酰基; X代表OCH〜2〜或CR ^ 3 ^ R ^ 4 ^基团,R ^ 3 ^或R ^ 4 ^各自独立地代表氢原子或C〜1-3〜烷基。 R5代表氢原子或C〜1-3〜烷基,C〜2-3〜烯基或C〜2-3〜炔基; R ^ 3 ^代表氢原子或C〜1-6〜烷基,C〜2-6〜烯基,C〜2-6〜炔基,氨基,C〜1-6〜氨基,二烷基(C〜1- 6〜)氨基或C〜2-7〜酰氨基; R ^ 7 ^和R ^ 8 ^各自独立地表示氢或卤素原子或羟基,三氟甲基,C〜1-6〜烷基,C〜2-6〜烯基,C〜2-6〜炔基,C〜 2-7〜酰基,C〜1-6〜烷硫基,C〜1-6〜烷氧基,C〜3-6〜环烷基; R ^ 9 ^代表氢或卤素原子或羟基,三氟甲基,C〜1-6〜烷基,C〜2-6〜烯基,C〜2-6〜炔基,C〜2-7〜酰基,C 〜1-6〜烷硫基,C〜1-6〜烷氧基或C〜3-6〜环烷基或其盐可用于治疗呼吸系统疾病,例如哮喘。本发明的化合物具有比已知化合物trequininsin(9,10-二甲氧基-3-甲基-2-mesitylimino-2,3,6,7-四氢-4H-嘧啶[6,1-a ] isoquinolin-4-one)和threquinsin不会很苦。

著录项

  • 公开/公告号BR0009449A

    专利类型

  • 公开/公告日2002-01-08

    原文格式PDF

  • 申请/专利权人 VERNALIS LIMITED;

    申请/专利号BR20000009449

  • 发明设计人 ALEXANDER WILLIAM OXFORD;DAVID JACK;

    申请日2000-03-29

  • 分类号C07D471/04;A61K31/519;C07D498/04;A61K31/553;A61P11/00;

  • 国家 BR

  • 入库时间 2022-08-22 00:46:17

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