发明名称 N-acyl-N-heterocyclyl- or naphthyl-alkyl amino acids as angiotensin II antagonists
摘要 <p>The invention relates to N-acyl-N-heterocyclylalkyl-amino acids of the formula <IMAGE> in which R1 is C1-C7-alkyl which is unsubstituted or substituted by halogen or hydroxyl, or C2-C7-alkenyl, C3-C7-cycloalkyl, C3-C7-cycloalkyloxy, C1-C7-alkoxy or C3-C7-cycloalkyl-C1-C7-alkoxy; R2 is 1H-tetrazol-5-yl, carboxyl, C1-C7-alkoxycarbonyl, SO3H, PO2H2, PO3H2 or halogen-C1-C7-alkanesulphonylamino; R3 is 1H-tetrazol-5-yl, hydroxymethyl, C1-C7-alkoxymethyl, formyl, carboxyl, C1-C7-alkoxycarbonyl, C1-C7-alkoxy-C1-C7-alkoxycarbonyl, phenyl-C1-C4-alkoxycarbonyl or carbamoyl whose amino group is unsubstituted or mono- or, independently of one another, disubstituted by C1-C7-alkyl, C3-C7-alkenyl or phenyl-C1-C7-alkyl or is disubstituted by C2-C7-alkylene or C2-C4-alkyleneoxy-C2-C4-alkylene; Alkyl is methylene, ethylene or ethylidene; Het is (i) <IMAGE> in which Y1 is O, S or N(R) and R is hydrogen or C1-C7-alkyl; or (ii) <IMAGE> in which one of the variables Y2 and Y3 is C(R%) and the other is N, or both variables are each C(R%); and R% is hydrogen, halogen, C1-C7-alkyl, C1-C7-alkoxy, C2-C7-alkenyloxy, phenoxy, benzyloxy, trifluoromethyl or S(O)m-R in which m is 0, 1 or 2; and R is hydrogen or C1-C7-alkyl; X1 is -CO- or -S(O)m- and the index m is 0, 1 or 2; one of the variables X2 and X4 is C1-C4-alkylene and the other of the variables X2 and X4 is a bond; or both variables X2 and X4 are each a bond; X3 is C3-C7-cycloalkylidene or the structural element -C(Xa)(Xb)- and Xa is hydrogen or C1-C7-alkyl and Xb is C1-C7-alkyl; and the rings A, B, C and D, apart from the substituents stated in the formula, as well as aromatic substituents, are, independently of one another, unsubstituted or substituted one or more times by substituents selected from the group consisting of halogen, C1-C7-alkyl, C1-C7-alkoxy, C2-C7-alkenyloxy, phenoxy, benzyloxy, trifluoromethyl and S(O)m-R in which m is 0, 1 or 2 and R is hydrogen or C1-C7-alkyl; and their salts; process for the preparation, pharmaceutical products containing a compound of the formula I or a pharmaceutically utilisable salt thereof, and the use.</p>
申请公布号 GR3023708(T3) 申请公布日期 1997.09.30
申请号 GR19970401349T 申请日期 1997.06.09
申请人 NOVARTIS AG 发明人 SCHMIDLIN, TIBUR, DR.;ZBINDEN, PAUL;BUEHLMAYER, PETER, DR.
分类号 A61K31/18;A61K31/19;A61K31/195;A61K31/235;A61K31/40;A61K31/403;A61K31/404;A61K31/41;A61K31/47;A61K31/472;A61K31/665;A61K31/67;A61K31/675;A61P9/00;A61P9/10;A61P9/12;A61P27/02;A61P27/06;C07D209/10;C07D209/14;C07D209/18;C07D209/24;C07D215/12;C07D217/12;C07D217/14;C07D257/04;C07D307/82;C07D333/60;C07D333/62;C07D401/10;C07D401/12;C07D401/14;C07D403/10;C07D403/12;C07D403/14;C07D405/10;C07D405/12;C07D405/14;C07D407/12;C07D409/10;C07D409/12;C07D409/14;(IPC1-7):C07D401/10;C07D407/10;A61K31/33 主分类号 A61K31/18
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