14165-90-3Relevant academic research and scientific papers
1,2,4,5-Tetrahydro-3H-benzazepine compounds, a process for their preparation and pharmaceutical compositions containing them
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Page/Page column 12, (2009/04/24)
Compounds of formula (I): wherein: R1 represents a hydrogen atom or a group selected from cycloalkyl, benzyl and optionally substituted alkyl,R2, R3, R4 and R5 each represent a hydrogen atom or a hydroxy, methyl, —OSO2R10, —OCOR10 or optionally substituted alkoxy group, or R2 and R3, or R3 and R4, or R4 and R5 together form a group —O—(CH2)q—O—, —O—CH═CH—O— or —O—CH═CH—,R6, R7, R8 and R9 each represent a hydrogen atom or an alkoxy group, or R6 and R7, or R7 and R8, or R8 and R9 together form a group —O—(CH2)q—O—-,R10 represents a group selected from linear or branched C1-C6alkoxy, NR11R′11 and optionally substituted alkyl,R11 and R′11 each represent a hydrogen atom or an alkyl group, or R11 and R′1 together with the nitrogen atom carrying them form an optionally substituted, monocyclic or bicyclic, nitrogen-containing heterocycle,X represents O, NH or CH2,m and p each represent 0 or 1,n and q each represent 1 or 2, in racemic form or in the form of optical isomers,and also addition salts thereof with a pharmaceutically acceptable acid. Medicinal products containing the same which are useful in treating various pathologies.
SAR studies of capsazepinoid bronchodilators. Part 1: The importance of the catechol moiety and aspects of the B-ring structure
Dalence-Guzman, Maria F.,Berglund, Magnus,Skogvall, Staffan,Sterner, Olov
, p. 2499 - 2512 (2008/09/21)
Capsazepine as well as its derivatives and analogues are general inhibitors of constriction of human small airways. From a systematic variation of the capsazepine structure, divided into four regions, SARs were established. This part concerns the catechol moiety of the A-ring as well as the 2,3,4,5-tetrahydro-1H-2-azepine moiety (the B-ring) of capsazepine. It is revealed that a conformational constrain (as a fused ring) is important and that compounds with a six-membered B-ring (as a 1,2,3,4-tetrahydroisoquinoline) in general are more potent than the corresponding isoindoline, 2,3,4,5-tetrahydro-1H-2-benzazepine and 2,3,4,5-tetrahydro-1H-3-benzazepine derivatives.
