Tritylation of tetrazole and its 5-substituted derivatives with triphenylmethyl chloride under conditions of phase-transfer catalysis regioselectively yields the corresponding 5-substituted 2-trityltetrazoles which can be used to protect N-H bonds in nitrogen-containing heterocycles and O-H bonds in primary alcohols. Thermolysis of 2-trityltetrazoles in benzonitrile leads to 3,6-disubstituted 1,2,4,5-tetrazines. Thermal transformation of the same compounds in dodecane follows a radically different mechanism, resulting in formation of difficultly accessible 8,8-diphenylheptafulvenes. The structure of the latter was proved by X-ray analysis.
[EN] NEW PYRAZOLE DERIVATIVES AS ANGIOTENSIN II ANTAGONIST<br/>[FR] NOUVEAUX DERIVES DE PYRAZOLE UTILISES COMME ANTAGONISTES DE L'ANGIOTENSINE II
申请人:J. URIACH & CIA, S.A.
公开号:WO1996004273A1
公开(公告)日:1996-02-15
(EN) Compounds of general formula (I) and their salts and solvates are angiotensin II receptor antagonists and as such are useful in the treatment of hypertension, congestive heat failure and elevated intraocular pressure. Pharmaceutical compositions including these compounds and processes for their preparation are also provided.(FR) Les composés de formule générale (I) (ainsi que leurs sels et solvates) sont des antagonistes du récepteur de l'angiotensine II et à ce titre sont utiles dans le traitement de l'hypertension, de l'insuffisance cardiaque congestive et de l'hypertension intra-oculaire. Des compositions pharmaceutiques renfermant ces composés et des procédés pour leur préparation sont également décrits.
(中文) 通式 (I) 及其盐和溶剂化合物是血管紧张素 II 受体拮抗剂,因此在治疗高血压、充血性心力衰竭和眼内压升高方面非常有用。还提供了包括这些化合物的药物组合物和其制备方法。
Tetrazolyl compounds and their pharmaceutical use
申请人:Lilly Industries Limited
公开号:EP0186426A2
公开(公告)日:1986-07-02
There are described pharmaceutical compounds of the formula
in which R' is C7-20 alkyl or C7-20 alkenyl containing 1 to 3 double bonds, R2 and R3 are each hydrogen or a protecting group, and X is C1-6 alkylene; and salts thereof.
Anti-hypertensive benzofuran derivatives substituted by N-imidazolyl-methyl groups which are condensed with optionally nitrogen containing, six-membered rings
申请人:GLAXO GROUP LIMITED
公开号:EP0514197A1
公开(公告)日:1992-11-19
The invention provides compounds of the general formula (I):
or a physiologically acceptable salt, solvate or metabolically labile ester thereof
wherein
R¹ and Ar are as defined in the claims and
het represents the group
A represents a variety of 4-membered optionally substitued linkages;
R⁶ represents a hydrogen atom or a group selected from C1-6alkyl, C2-6alkenyl, C1-6alkylthio, C1-6alkoxy, C3-7cycloalkyl, or C3-7cycloalkylC1-4alkyl.
The compounds may be used in the treatment or prophylaxis of hypertension and diseases associated with cognitive disorders.