摘要:
A series of novel spiro-substituted glutaramide derivatives have been prepared, including the pharmaceutically acceptable salts thereof and bioprecursors therefor, wherein the spiro-substituent completes a 5- or 6- membered carbocyclic ring and is located at the carbon atom adjacent to the carbamoyl group. These particular compounds are inhibitors of the neutral endopeptidase E.C.3,4.24.11 enzyme and are therefore useful in therapy as diuretic agents for the treatment of hypertension, heart failure, renal insufficiency and other disorders. Methods for preparing these compounds from known starting materials are provided.
摘要:
A series of novel spiro-substituted glutaramide derivatives have been prepared, including the pharmaceutically acceptable salts thereof and bioprecursors therefor, wherein the spiro-substituent completes a 5- or 6-membered carbocycyclic ring and is located at the carbon atom adjacent to the carbamoyl group. These particular compounds are inhibitors of the neutral endopeptidase E.C.3.4.24.11 enzyme and are therefore useful in therapy as diuretic agents for the treatment of hypertension, heart failure, renal insufficiency and other disorders. Methods for preparing these compounds from known starting materials are provided.
摘要:
The invention provides the substantially optically pure 2(S)-stereoisomeric form of compounds of the formulae: ##STR1## and the salts thereof, together with processes for their preparation. The compounds are intermediates for the preparation of antihypertensive agents.
摘要:
Compounds of formula (I) are diuretic agents for treating various cardiovascular diseases including hypertension, heart failure and renal insufficiency.
摘要:
The invention provides the substantially optically pure 2(S)-steroisomeric form of compounds of the formulae: ##STR1## and the salts thereof, together with processes for their preparation. The compounds are intermediates for the preparation of antihypertensive agents.
摘要:
The invention provides the substantially optically pure 2(S)-stereoisomeric form of compounds of the formulae: ##STR1## and the salts thereof, together with processes for their preparation. The compounds are intermediates for the preparation of antihypertensive agents.
摘要:
2-Acylaminoalkyl-3-[1-(carboxycycloalkylcarbamoyl)cycloalkyl]propanoic acid derivatives (which may also be viewed as glutaramide derivatives) are useful in the treatment of hypertension, heart failure and renal insufficiency, based upon their inhibition of zinc-dependant, neutral endopiptidase.
摘要:
Compounds of the formula ##STR1## wherein A is a carbocyclic, saturated or unsaturated ring; R.sup.1 is hydrogen or alkyl; R and R.sup.4 are each alkyl, cycloalkyl, benzyl or a readily hydrolyzable ester group; Y is a bond or a straight or branch alkylene; R.sup.2 is hydrogen, aryl, heterocyclic, R.sup.6 CONR.sup.5, R.sup.7 NR.sup.5 CO, R.sup.7 NR.sup.5 SO.sub.2 --or R.sup.8 SO.sub.2 NR.sup.5 --where R.sup.5 is hydrogen, alkyl or aralkyl; R.sup.6 is alkyl, aryl, aralkyl, heterocyclic, heterocyclyalkyl or a group of the formula ##STR2## where R.sup.9 is hydrogen, hydroxy, alkoxy, alkyl, hydroxyalkyl, aralkyl, alkylene, heterocyclic, heterocyclylalkyl, R.sup.12 CONH--, R.sup.12 SO.sub.2 NH-- or (R.sup.13).sub.2 N--; R.sup.10 and R.sup.11 are each hydrogen or alkyl; or R.sup.10 is hydrogen and R.sup.11 is aminoalkyl, imidazolylmethyl, aryl, aralkyl, aralkoxyalkoxy, hydroxyalkyl or methylthioalkyl; or R.sup.10 and R.sup.11 together with the carbon to which they are attached form a carbocyclic or heterocyclic ring optionally substituted by amino, alkanoyl or aroyl; R.sup.12 is alkyl, cycloalkyl, aryl, aralkyl, heterocyclic or heterocyclylalkyl; each R.sup.13 is hydrogen, alkyl, aralkyl or both R.sup.13 together with the nitrogen to which they are attached form a heterocyclic ring; R.sup.7 is alkyl, aryl, aralkyl, heterocyclic, heterocyclyalkyl or a group ##STR3## where R.sup.10 and R.sup.11 are as defined and R.sup.14 is (R.sup.13).sub.2 NCO, R.sup.12 OCH.sub.2 -- or R.sup.15 OCO, where R.sup.12 and R.sup.13 are as defined and R.sup.15 is alkyl, cycloalkyl or aralkyl; and R.sup.8 is alkyl, aryl, aralkyl, heterocyclic or heterocyclylalkyl; R.sup.3 is a group ##STR4## where R.sup.16 is hydrogen, halo, hydroxy, alkoxy, cycloalkoxy, alkenyloxy, alkoxycarbonyloxy, cycloalkoxycarbonylalkoxy or alkyl SO.sub.2 NH--; and R.sup.20 is hydrogen, alkyl, alkoxy, alkanoyl or halo; or R.sup.3 is 3-indolylmethyl or 3-indazolylmethyl, each optionally substituted in the benzenoid ring by alkyl, alkoxy, hydroxy or trifluoromethyl as antihypertensive agents.
摘要翻译:其中A是碳环,饱和或不饱和环的式IMA的化合物; R1是氢或烷基; R和R4各自为烷基,环烷基,苄基或易水解的酯基; Y是一个键或直链或支链亚烷基; R2是氢,芳基,杂环,R6CONR5,R7NR5CO,R7NR5SO2或R8SO2NR5,其中R5是氢,烷基或芳烷基; 其中R 9是氢,羟基,烷氧基,烷基,羟基烷基,芳烷基,亚烷基,杂环基,杂环基烷基,R 12 CONH-,R 12 SO 2 NH-或(R 13) 2N-; R 10和R 11各自为氢或烷基; 或R 10为氢,R 11为氨基烷基,咪唑基甲基,芳基,芳烷基,芳烷氧基烷氧基,羟基烷基或甲硫基烷基; 或R 10和R 11与它们所连接的碳一起形成任选被氨基,烷酰基或芳酰基取代的碳环或杂环; R 12是烷基,环烷基,芳基,芳烷基,杂环或杂环基烷基; 每个R 13是氢,烷基,芳烷基或两者R 13与它们所连接的氮一起形成杂环; R 7是烷基,芳基,芳烷基,杂环基,杂环烷基或基团,其中R 10和R 11如上所定义,R 14是(R 13)2 COCO,R 12 OCH 2或R 15 OCO,其中R 12和R 13如上定义,R 15是烷基,环烷基 或芳烷基; R8是烷基,芳基,芳烷基,杂环或杂环基烷基; R3是一个基团,其中R16是氢,卤素,羟基,烷氧基,环烷氧基,烯氧基,烷氧基羰氧基,环烷氧基羰基烷氧基或烷基SO2NH-; 和R 20是氢,烷基,烷氧基,烷酰基或卤素; 或R3是3-吲哚基甲基或3-吲唑基甲基,其各自任选在苯环中被烷基,烷氧基,羟基或三氟甲基取代作为抗高血压剂。
摘要:
2-Acylaminoalkyl-3-[1-(carboxycycloalkylcarbamoyl)cycloalkyl]propanoic acid derivatives (which may also be viewed as glutaramide derivatives) are useful in the treatment of hypertension, heart failure and renal insufficiency, based upon their inhibition of zinc-dependent, neutral endopiptidase.
摘要:
Organic material, particularly organic material floating on a water surface, can be encapsulated by reacting, in the presence of the organic material, (A) a functionalized liquid polymer containing anhydride functional groups which groups are derived from an alpha, beta-ethylenically unsaturated dicarboxylic acid anhydride and (B) an alkoxylated fatty monoamine or polyamine having from 1.5 to 15 moles of alkoxylate per mole of fatty amine. The functionalized polymer (A) may be, for example, maleinized polybutadiene and the alkoxylated fatty amine may be, for example, N,N.sup.1, N.sup.1 -tris (2-hydroxypropyl)-N-oleyl-1,3-diaminopropane. Preferably, the alkoxylated fatty amine is derived from a fatty amine having an iodine value of at least 65. The method may also be used to encapsulate a solid contaminated with organic material e.g. oil drilling cuttings.