首页> 外国专利> Derived from beta-starch or beta-sulfonamido carboxylic acids, use of it, pharmaceutical preparation for oral, parenteral and intraperitoneal administration, compound, use of this, and structure fragment

Derived from beta-starch or beta-sulfonamido carboxylic acids, use of it, pharmaceutical preparation for oral, parenteral and intraperitoneal administration, compound, use of this, and structure fragment

机译:衍生自β-淀粉或β-磺酰胺基羧酸,其用途,用于口服,肠胃外和腹膜内给药的药物制剂,化合物,其用途以及结构片段

摘要

"DERIVED FROM BETA-STARCH OR BETA-SULPHONAMIDE CARBOXYLIC ACIDS, USE OF THE SAME, PHARMACEUTICAL PREPARATION FOR ORAL, PARENTAL AND INTRAPERITONEAL ADMINISTRATION, COMPOUND, USE OF THIS, AND, STRUCTURAL FRAGMENT". The invention relates to carboxylic acid derivatives of formula (I): in which the substituents have the following meanings: R¹ is tetrazole or a group (a); W and Z, can be identical or different and are nitrogen or methyl, provided that, if W and Z are methyl, then Q is nitrogen; X is nitrogen or CR ^ 9 ^; Y is nitrogen or CR ^ 10 ^; Q is nitrogen or CR ^ 11 ^, provided that if Q is nitrogen then X is CR ^ 5 ^ and Y is CR ^ 10 ^; R² and R³ are identical or different and are possibly substituted phenyl or naphthyl or phenyl or naphthyl that are linked in an ortho position by a direct bond, a methylene, ethylene or ethylene group, an oxygen or sulfur atom or an SO group ~ 2 ~ -, NH- or N-alkyl or possibly substituted C ~ 5 ~ -C ~ 6 ~ cycloalkyl; R ^ 4 ^ is a remainder of (b) or (c); and R5 is hydrogen, C ~ 1 ~ -C ~ 4 ~ alkyl. The invention further concerns its preparation and its use as endothelin receptor antagonists. The invention also concerns compounds of formula (II) and a structural fragment of formula (d) in which the remains of R¹, R², R³, R ^ 4 ^ and R ^ 5 ^ have the meanings given in claim no. 1 and its use as structural elements in an endothelin receptor antagonist.
机译:“衍生自β-淀粉或β-磺酰胺羧酸,相同的使用,口服,家长和腹膜内给药的药物制剂,化合物,本品的使用和结构性片段”。本发明涉及式(Ⅰ)的羧酸衍生物:其中取代基具有以下含义:R 1是四唑或基团(a); R 1是四唑或基团(a)。 W和Z可以相同或不同,并且可以是氮或甲基,条件是,如果W和Z是甲基,则Q是氮; X是氮或CR ^ 9 ^; Y是氮或CR ^ 10 ^; Q是氮或CR ^ 11 ^,如果Q是氮,则X是CR ^ 5 ^,Y是CR ^ 10 ^; R 2和R 3相同或不同,可能是取代的苯基或萘基或苯基或萘基,它们在邻位通过直接键,亚甲基,亚乙基或亚乙基,一个氧或硫原子或一个SO 2基团相连。 -,NH-或N-烷基或可能取代的C〜5〜-C〜6〜环烷基; R ^ 4 ^是(b)或(c)的余数;并且R5是氢,C〜1〜-C〜4〜烷基。本发明进一步涉及其制备及其作为内皮素受体拮抗剂的用途。本发明还涉及式(Ⅱ)的化合物和式(d)的结构片段,其中R 1,R 2,R 3,R ^ 4 ^和R ^ 5 ^的其余部分具有权利要求1中给出的含义。 1及其在内皮素受体拮抗剂中的结构元素的用途。

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