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Carboxylic acid derivative, use of it, combination, and drug preparation for oral, parenteral and intra-parenteral administration

机译:羧酸衍生物,其用途,组合以及用于口服,肠胃外和胃肠外给药的药物制剂

摘要

"CARBOXYLIC ACID DERIVATIVE, USE OF THE SAME, COMBINATION, AND DRUG PREPARATION FOR ORAL, PARENTAL AND INTRA-PARENTAL ADMINISTRATION" The invention relates to carboxylic acid derivatives of formula (I) in which the substituents have the following meanings ; R¹ = tetrazole or a group (1): R = an OR ^ 7 ^ radical (2), (3): a 5-membered heteroaromatic linked by a nitrogen atom such as pyrrolyl, pyrazolyl, imidazolyl and trizolyl; R², R³ = hydrogen, hydroxy, NH ~ 2 ~, NH (C ~ 1 ~ -C ~ 4 ~ -alkyl), N (C ~ 1 ~ -C ~ 4 ~ -alkyl) ~ 2, ~ halogen, C ~ 1 ~ -C ~ 4 ~ -alkyl, C ~ 2 ~ -C ~ 4 ~ -alkenyl, C ~ 2 ~ -C ~ 4 ~ -alkynyl, C ~ 1 ~ -C ~ 4 ~ -hydroxyalkyl, C ~ 1 ~ -C ~ 4 ~ -alkoxy, C ~ 1 ~ -C ~ 4 ~ -haloalkyl, C ~ 1 ~ -C ~ 4 ~ -alkoxy, C ~ 1 ~ -C ~ 4 ~ -haloalkoxy, or C ~ 1 ~ - C-4-alkylthio; X = halogen, C ~ 1 ~ -C ~ 4 ~ -haloalkyl, hydroxy, R ^ 4 ^ and R ^ 5 ^ = phenyl or naphthyl, C ~ 3 ~ -C ~ 7 ~ -cycloalkyl, phenyl or naphthyl which are bonded in the ortho position by a direct bond, a methylene, ethylene, or ethylene group, an oxygen atom, or sulfur or a SO ~ 2 ~ -NH or N-alkyl group or a 5-membered or 6-membered heteroaromatic; R ^ 6 ^ = hydrogen, phenyl or naphthyl, a five- or six-membered heteroaromatic; C ~ 1 ~ -C ~ 8 ~ alkyl, C ~ 3 ~ -C ~ 6 ~ -alkenyl, C ~ 3 ~ -C ~ 6 ~ -alkynyl or C ~ 3 ~ -C ~ 8 ~ -cycloalkyl, whereby radicals mentioned can be substituted once or many times, with the proviso that R ^ 6 ^ can only mean hydrogen if Z does not represent a single bond; Z = sulfur, oxygen or a simple bond, in addition to physiologically compatible salts and the enanciomeric-pure and diastereomeric-pure forms. The new compounds are suitable for fighting diseases, especially as endothelin antagonists.
机译:本发明涉及式(I)的羧酸衍生物,其中取代基具有以下含义;“羧酸衍生物,其使用的用法,组合和药物的口服,家长和父母内部的给药”。 R 1 =四唑或基团(1):R = OR ^ 7 ^基团(2),(3):由氮原子如吡咯基,吡唑基,咪唑基和三唑基连接的5元杂芳族基; R 2,R 3 =氢,羟基,NH〜2〜,NH(C〜1〜-C〜4〜-烷基),N(C〜1〜-C〜4〜-烷基)〜2,〜卤素,C〜 1〜-C〜4〜-烷基,C〜2〜-C〜4〜-烯基,C〜2〜-C〜4〜-炔基,C〜1〜-C〜4〜-羟烷基,C〜1〜 -C〜4〜-烷氧基,C〜1〜-C〜4〜-卤代烷基,C〜1〜-C〜4〜-烷氧基,C〜1〜-C〜4〜-卤代烷氧基或C〜1〜- C-4-烷硫基; X =卤素,C〜1〜-C〜4〜卤代烷基,羟基,R ^ 4 ^和R ^ 5 ^ =苯基或萘基,C〜3〜-C〜7〜环烷基,苯基或萘基在邻位通过直接键,亚甲基,亚乙基或亚乙基,氧原子或硫或SO〜2〜-NH或N-烷基或5元或6元杂芳族基团; R ^ 6 ^ =氢,苯基或萘基,五元或六元杂芳族; C〜1〜-C〜8〜烷基,C〜3〜-C〜6〜-烯基,C〜3〜-C〜6〜-炔基或C〜3〜-C〜8〜-环烷基可以被取代一次或多次,条件是R ^ 6 ^仅在Z不代表单键的情况下表示氢; Z =除了生理上相容的盐以及对映体纯和非对映体纯形式以外的硫,氧或简单键。新化合物适用于抵抗疾病,特别是作为内皮素拮抗剂。

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