首页> 外国专利> N-ACIL-N-HETEROCICLIL-ONAFTALENIL-ALQUIL-AMINOACIDOS AS ANTAGONISTS OF ANGIOTENSIN II.

N-ACIL-N-HETEROCICLIL-ONAFTALENIL-ALQUIL-AMINOACIDOS AS ANTAGONISTS OF ANGIOTENSIN II.

机译:N-酰基-N-杂环基-对苯二甲酰基-烷基-氨基酸作为血管紧张素II的拮抗剂。

摘要

THE INVENTION REFERS TO N-ACILO-NHETEROCICLILOALKYL AMINO ACIDS OF THE FORMULA IN WHICH R1 MEANS C1-C7 ALKYL, WHICH IS INSTITUTED OR REPLACED BY HALOGENO OR HYDROXIDE, C3-C7-C7, C7, ALCOXILOC1-C7 OR CICLOALQUILOC3-C7-ALCOXILOC1-C7; R2 IS 1H-TETRAZOLE-5-YL, CARBOXYL, ALCOXYL-CARBONYL-C1-C7, SO3H, PO2H2, PO3H2 OR HALOGEN-C1-C7-ALCANOSULFONYLAMINE; R3 MEANS 1H-TETRAZOLE-5-YL, HYDROXYMETHYL, ALCOXY-METHYL-C1-C7, FORMYL, CARBOXYL, ALCOXY-CARBONYL-C1-C7, C1-C7 ALCOXYLOCARBONYL-C1-C7-C1-C7-C1-C7 -CARBONYL, PHENYL-C1-C4ALCOXYL-CARBONYL OR CARBAMOYLO, WHOSE GROUP AMINO IS UNSUBSTITUTED OR DISSTITUTED BY C1-C7 ALKYL, C1-C7-ALKYNYL, MONO-OR INDEPENDENT ALIENYLE, DISPOSED BY AENILE C2-C7 OR C2-C4-ALKYLENOXYL-C2-C4; ALK METHYLEL, IS ETILEL OR ETILIDEL HET, MEANS (I) IN WHICH Y1 IS INSTEAD OF O, S O N (R) AND R MEANS ALKYLOC1-C7; O MEANS (II) IN WHICH ONE OF THE VARIABLES Y2 AND Y3 IS INSTEAD OF C (R '') AND THE OTHER INSTEAD OF N, OR THE TWO VARIABLES INSTEAD OF C (R ''); Y R '' MEANS HYDROGEN, HALOGEN, ALKYL-C1-C7, ALCOXYL-C1-C7, ALKYNYLOXYL-C2-C7, FELOXYL, BENCILOXYL, TRIFLUOROMETILE O S (O) M, ES, 0, 0 AND R IS HYDROGEN OR ALQUILOU THE INDEX M IS INSTEAD OF 0, 1 OR 2; ONE OF THE X2 AND X4 VARIABLES IS INSTEAD OF RENTS-C1-C4 AND THE OTHER X2 AND X4 VARIABLES ARE INSTEAD OF A LINK; OR THE TWO VARIABLES X2 AND X4 ARE EVERY TIME INSTEAD OF A LINK; X3 MEANS C3-C7-CYCLLOALKYLLIDS OR STRUCTURE ELEMENT C (XA) (XB) IDROGEN OR ALKYL-C1-C7 AND XB IS C1-C7 ALKYL; AND THE RINGS A, B, CYD, UP TO THE SUBSTITUTES INDICATED IN THE FORMULA, AS WELL AS THE AROMATIC SUBSTITUTES, ARE SUBSTITUTED INDEPENDENT BETWEEN OR SUBSTITUTED ONE OR SEVERAL SOME-SELECTED BY A VERY MUCH-COMPUTER GROUP -C1-C7, C2-C7-ALKYNYLOXYL, PHENOXYL, BENZYLOXYL, TRIFLUOROMEYLL AND S (O) MR, WHERE M, IS 0, 1 OR 2; Y R IS HYDROGEN OR ALKYL-C1-C7; AND ITS SALTS; MANUFACTURING METHOD, PHARMACEUTICAL PREPARATIONS CONTAINING A COMBINATION OF FORMULA I OR A SALT OF IT FOR PHARMACEUTICAL EMPLOYMENT, AS WELL AS EMPLOYMENT.
机译:本发明涉及R 1代表C 1 -C 7烷基的式的N-苯环-杂环烷基氨基酸,其被卤素或羟基,C 3 -C 7 -C 7,C 7,烷氧基C 1 -C 7或环戊基1-取代或取代。 -C7; R2为1H-四唑-5-基,羧基,醇羰基-C1-C7,SO3H,PO2H2,PO3H2或卤素-C1-C7-烷磺酰胺基; R3表示1H-四唑-5-基,羟甲基,羟甲基-C1-C7,甲酰基,羧基,羟羰基-C1-C7,C1-C7羟羰基-C1-C7-C1-C7-C1-C7-羰基,苯基-C1-C4羟羰基或碳酰氨基,其基团氨基未被C1-C7烷基,C1-C7炔基,单或独立的烯丙基取代或取代,由烯丙基C2-C7或C2-C4炔基氧基取代-C4; (1)在Y1代入O,S O N(R)和R的情况下,烷基甲磺酸乙酯或乙腈代表(I)烷烃OC1-C7;其中,变量Y2和Y3中的一个代替C(R”),另一个变量N替代两个C的变量(R”)中的O均值(II); YR''表示氢,卤代烷,烷基C1-C7,羟乙基-C1-C7,炔氧基-C2-C7,苯甲酰,苯甲酰,三聚体OS(O)M,ES,0、0和R为氢或铝的指数M代表0、1或2; X2和X4变量之一代替了租金C1-C4,而其他X2和X4变量则代替了链接。或两个变量X2和X4每次都代表链接; X3是指C3-C7-环烷基或结构元素C(XA)(XB)-IDROGEN或烷基-C1-C7,并且XB是C1-C7烷基;直到公式中指示的取代基以及芳香族取代基之间的A,B,CYD环由非常多的计算机主机群-C1-C7中的一个或多个取代或独立取代-C7-炔基氧基,苯氧基,苄基氧基,三氟甲苯和S(O)MR,其中M为0、1或2; Y R为氢或烷基-C1-C7;及其盐制造方法,包括配方I或其盐的组合的药物制剂,用于制药业以及从业人员。

著录项

  • 公开/公告号ES2101824T3

    专利类型

  • 公开/公告日1997-07-16

    原文格式PDF

  • 申请/专利权人 NOVARTIS AG;

    申请/专利号ES19920810603T

  • 申请日1992-08-06

  • 分类号C07D401/10;A61K31/33;C07D409/10;C07D407/10;C07D333/60;C07D257/04;

  • 国家 ES

  • 入库时间 2022-08-22 03:23:59

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