发明名称 Pharmaceutical formulation comprising pyrazolo[4,3-d] pyrimidines and endothelin receptor antagonists or thienopyrimidines and endothelin receptor antagonists.
摘要 A pharmaceutical composition (A) contains (i) at least one pyrazolo[4,3-d]pyrimidine derivative (I), its salt and/or solvate, and (ii) at least one endothelin receptor antagonist (II). A pharmaceutical composition (A) contains (i) at least one pyrazolo[4,3-d]pyrimidine derivative of formula (I), its salt and/or solvate, and (ii) at least one endothelin receptor antagonist (II). [Image] R1>, R2>H, A, OH, OA or Hal, or together comprise 3-5C alkylene, OCH2CH2, CH2OCH2, OCH2O or OCH2CH2O; R3>, R4>H or A; X : R5>, R6> or R7> substituted once by R8>; R5>1-10C alkylene, with one or two methylene replaced by CH=CH, O, S or SO; R6>5-12C cycloalkyl(alkylene); R7>phenyl(methyl); R8>COOH, COOA, aminocarbonyl (optionally substituted by 1 or 2 A) or CN; A : 1-6C alkyl; and Hal : F, Cl, Br or I. An independent claim is also included for a kit comprising: (a) [7-(3-chloro-4-methoxy-benzylamino)-1-methyl-3-propyl-1H-pyrazolo[4,3-d] pyrimidin-5-ylmethoxy]acetic acid (Ia), it's salt and/or solvate; and (b) an endothelin receptor antagonist. ACTIVITY : Antianginal; Hypotensive; Antiarteriosclerotic; Cardiant; Cerebroprotective; Antiinflammatory; Antiallergic; Antiasthmatic; Ophthalmological; Nephrotropic; Hepatotropic; Vasotropic. No details of tests are given. MECHANISM OF ACTION : Phosphodiesterase V inhibitor.
申请公布号 ZA200306819(B) 申请公布日期 2004.12.01
申请号 ZA20030006819 申请日期 2003.09.01
申请人 MERCK PATENT GMBH. 发明人 HANS-MICHAEL EGGENWEILER;VOLKER EIERMANN;PIERRE SCHELLING
分类号 A61K31/519;A61K45/06 主分类号 A61K31/519
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