L-162,389: a potent orally active angiotensin II receptor antagonist with balanced affinity to both AT1 and AT2 receptor subtypes
摘要:
Simple modifications made to our potent angiotensin II AT(1) selective clinical candidate MK-996 provided a compound with balanced binding affinity to both the AT(1) and the AT(2) receptor subtype. This compound. L-162,389, is orally active in rats and dogs.
Substituted triazolinones, triazolinethiones, and triazolinimines as
申请人:Merck & Co., Inc.
公开号:US05411980A1
公开(公告)日:1995-05-02
There are disclosed new substituted triazolinone, triazolinethione, and triazolinimine compounds which are useful as angiotensin II antagonists. These compounds have the general formula: ##STR1## wherein G is R.sup.1 or ##STR2##
Substituted 1,2,4-triazoles bearing acidic functional groups as
申请人:Merck & Co., Inc.
公开号:US05281614A1
公开(公告)日:1994-01-25
Novel substituted triazolinone, triazolinethione, and triazolinimine compounds of the formula I are useful as angiotensin II antagonists. ##STR1##
这些公式I中的新型替代三唑酮,三唑硫酮和三唑亚胺化合物可用作抗血管紧张素II拮抗剂。
Substituted pyrazoles, compositions and use
申请人:Merck & Co., Inc.
公开号:US05262412A1
公开(公告)日:1993-11-16
Substituted pyrazole compounds are angiotensin II antagonists and therefore useful in the treatment of hypertension, and related cardiovascular disorders and ocular hypertension. These compounds have the general formula I: ##STR1##
Substituted triazolinone compounds are angiotensin II antagonists and therefore useful in the treatment of hypertension, and related cardiovascular disorders and ocular hypertension. These compounds have the general formula:
取代的三唑啉酮化合物是血管紧张素 II 拮抗剂,因此可用于治疗高血压、相关心血管疾病和眼压过高。这些化合物的通式如下
ACIDIC ARALKYL TRIAZOLE DERIVATIVES ACTIVE AS ANGIOTENSIN II ANTAGONISTS