摘要:
The present invention relates to peptide amino-alcohol derivatives containing a tetra substituted carbon atom. Said peptides inhibit the renin and acid proteases. The invention also relates to the process for their obtention and to pharmaceutical compositions.
摘要:
The invention relates to pharmaceutical compositions containing (2S)-1-{(2R,3S)-5-chloro-3-(2-chlorophenyl)-1-(3,4-dimethoxybenzenesulfonyl)-3-hydroxy-2,3-dihydro-1H-indole-2-carbonyl}pyrrolidine-2-carboxamide, a selective V1a arginine vasopressin receptor antagonist, in combination with the equatorial isomer of 1-{4-(N-tert-butylcarbamoyl)-2-methoxybenzenesulfonyl}-5-ethoxy-3-spiro{4-(2-morpholinoethyloxy)cyclohexane}indol-2-one or one of its salts, a selective V2 arginine vasopressin receptor antagonist. The invention relates to the use of such compositions for the production of medicines designed to treat all diseases for which either arginine vasopressin or the V2 receptors are implicated or to treat all diseases related to a water overlead.
摘要:
The invention relates to 1-Benzenesulfonyl-1,3-dihydroindol-2-one derivatives of the formula ##STR1## and their salts, where appropriate, to their preparation and to pharmaceutical compositions in which they are present. These compounds have an affinity for the vasopressin and/or ocytocin receptors.
摘要:
The invention relates to 1-Benzenesulfonyl-1,3-dihydroindol-2-one derivatives of the formula ##STR1## and their salts, where appropriate, to their preparation and to pharmaceutical compositions in which they are present. These compounds have an affinity for the vasopressin and/or ocytocin receptors.
摘要:
The invention relates to N-sulfonyl derivatives of formulae (I) and (I)' ##STR1## to their preparation, and to pharmaceutical compositions in which they are present. The compounds of formulae (I) and (I)' have an affinity for the vasopressin and ocytocin receptors.
摘要:
The invention relates to N-sulfonyl derivatives of formulae (I) and (I)' ##STR1## to their preparation, and to pharmaceutical compositions in which they are present. The compounds of formulae (I) and (I)' have an affinity for the vasopressin and ocytocin receptors.
摘要:
The invention relates to pepstatin analogs which inhibit renin and acid proteases.These analogs are particularly suitable for the treatment of arterial tension.
摘要:
The invention relates to substituted 1-piperazinylacylpiperidine derivatives of general formula (I) in which: n is 1 or 2; R1 represents a halogen atom; a trifluoromethyl radical; a (C1-C4) alkyl; a (C1-C4)alkoxy; a trifluoromethoxy radical; R2 represents a hydrogen atom or a halogen atom; R3 represents a hydrogen atom; a group —OR5; a group —CH2OR5; a group —NR6R7; a group —NR8COR9; a group —NR8CONR10R11; a group —CH2NR12R13; a group —CH2NR8CONR14R15; a (C1-C4)alkoxycarbonyl; a group —CONR16R17; or else R3 constitutes a double bond between the carbon atom to which it is attached and the adjacent carbon atom of the piperidine ring; R4 represents the aromatic group 1,3-thiazol-2-yl of formula: Preparation process and therapeutic application.
摘要翻译:本发明涉及通式(I)的取代的1-哌嗪基酰基哌啶衍生物,其中n为1或2; R 1表示卤素原子; 三氟甲基; (C 1 -C 4 -C 4)烷基; (C 1 -C 4 -C 4)烷氧基; 三氟甲氧基; R 2表示氢原子或卤素原子; R 3代表氢原子; 一个基团-OR 5; 基团-CH 2或OR 5; 基团-NR 6 R 7; 基团-NR 8 COR 9; 基团-NR 8 CONR 10 R 11; 基团-CH 2 NR 12 R 13; 基团-CH 2 NR 8 CONR 14 R 15 15; (C 1 -C 4 -C 4)烷氧基羰基; 基团-CONR 16 R 17 R 17; 或者R 3 3在其所连接的碳原子和哌啶环的相邻碳原子之间构成双键; R 4代表下式的芳族基团1,3-噻唑-2-基:制备方法和治疗应用。
摘要:
The invention relates to substituted 1-piperazinylacylpiperidine derivatives of general formula (I) in which: n is 1 or 2; p is 1 or 2; R1 represents a halogen atom; a trifluoromethyl radical; a (C1-C4)alkyl; a (C1-C4)alkoxy; a trifluoromethoxy radical; R2 represents a hydrogen atom or a halogen atom; R3 represents a hydrogen atom; a group —OR5; a group —CH2OR5; a group —NR6R7; a group —NR8COR9; a group —NR8CONR10R11; a group —CH2NR12R13; a group —CH2NR8CONR14R15; a (C1-C4)alkoxycarbonyl; a group —CONR16R17; or else R3 constitutes a double bond between the carbon atom to which it is attached and the adjacent carbon atom of the piperidine ring; R4 represents an aromatic group selected from: the said aromatic groups being unsubstituted or being mono- or disubstituted by a substituent selected independently from a halogen atom; a (C1-C4)alkyl; a (C1-C4)alkoxy; a trifluoromethyl radical; Preparation process and therapeutic application.
摘要翻译:本发明涉及通式(I)的取代的1-哌嗪基酰基哌啶衍生物,其中n为1或2; p为1或2; R1表示卤素原子; 三氟甲基; (C1-C4)烷基; (C 1 -C 4)烷氧基; 三氟甲氧基; R2表示氢原子或卤素原子; R3表示氢原子; 一组-OR5; 基团-CH 2 OR 5; 基团-NR 6 R 7; 一个-NR8COR9基团; 一组-NR8CONR10R11; 基团-CH 2 NR 12 R 13; 基团-CH2NR8CONR14R15; (C1-C4)烷氧基羰基; 一组-CONR16R17; 或者R 3构成与其连接的碳原子和哌啶环的相邻碳原子之间的双键; R 4表示选自以下的芳族基团:所述芳族基团是未取代的或被独立地选自卤素原子的取代基单取代或二取代; (C1-C4)烷基; (C 1 -C 4)烷氧基; 三氟甲基; 制备工艺及治疗应用。
摘要:
The invention relates to substituted 1-piperazinylacylpiperidine derivatives of general formula (I) in which: n is 1 or 2; p is 1 or 2; R1 represents a halogen atom; a trifluoromethyl radical; a (C1-C4)alkyl; a (C1-C4)alkoxy; a trifluoromethoxy radical; R2 represents a hydrogen atom or a halogen atom; R3 represents a hydrogen atom; a group —OR5; a group —CH2OR5; a group —NR6R7; a group —NR8COR9; a group —NR8CONR10R11; a group —CH2NR12R13; a group —CH2NR8CONR14R15; a (C1-C4)alkoxycarbonyl; a group —CONR16R17; or else R3 constitutes a double bond between the carbon atom to which it is attached and the adjacent carbon atom of the piperidine ring; R4 represents an aromatic group selected from: the said aromatic groups being unsubstituted or being mono- or disubstituted by a substituent selected independently from a halogen atom; a (C1-C4)alkyl; a (C1-C4)alkoxy; a trifluoromethyl radical; Preparation process and therapeutic application.
摘要翻译:本发明涉及通式(I)的取代的1-哌嗪基酰基哌啶衍生物,其中n为1或2; p为1或2; R 1表示卤素原子; 三氟甲基; (C 1 -C 4 -C 4)烷基; (C 1 -C 4 -C 4)烷氧基; 三氟甲氧基; R 2表示氢原子或卤素原子; R 3表示氢原子; 一个基团-OR 5; 基团-CH 2或OR 5; 基团-NR 6 R 7; 基团-NR 8 COR 9; 基团-NR 8 CONR 10 R 11; 基团-CH 2 NR 12 R 13; 基团-CH 2 NR 8 CONR 14 R 15 15; (C 1 -C 4 -C 4)烷氧基羰基; 基团-CONR 16 R 17 R 17; 或者R 3 3在其所连接的碳原子和哌啶环的相邻碳原子之间构成双键; R 4表示选自以下的芳族基团:所述芳族基团是未取代的或被独立地选自卤素原子的取代基单取代或二取代; (C 1 -C 4 -C 4)烷基; (C 1 -C 4 -C 4)烷氧基; 三氟甲基; 制备工艺及治疗应用。