BENZOFURAN BASED ANGIOTENSIN-II ANTAGONISTS RELATED TO GR117289 .3. GR138950, A TRIFLAMIDE WITH HIGH ORAL BIOAVAILABILITY

被引：12

作者：

DOWLE, MD

JUDD, DB

MIDDLEMISS, D

SCOPES, DIC

ROSS, BC

PASS, M

TRANQUILLINI, E

JACK, TI

HOBSON, JE

PANCHAL, TA

STUART, PG

DREW, GM

ROBERTSON, MJ

HILDITCH, A

CLARK, KL

TRAVERS, A

HUNT, AAE

MANCHEE, GR

WALKER, DG

EDDERSHAW, PJ

DONNELLY, M

BAYLISS, MK

机构：

[1] Glaxo Group Research, Ware, Herts SG12 0DP, Park Road

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1993年 / 3卷 / 10期

关键词：

D O I：

10.1016/S0960-894X(01)81012-X

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The identification of GR138950, a non-peptide antagonist of angiotensin II with high oral bioavailability, is described. GR138950 is a potent and selective ATI receptor antagonist which causes marked falls in blood pressure in renal hypertensive rats after either systemic or oral administration. It has high bioavailability in both rats and dogs and has been selected as our second candidate for clinical development.

引用

页码：2047 / 2050

页数：4

共 5 条

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[2]

DUDLEY DT, 1993, CURRENT OPINION THER, V3, P581

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HILDITCH, A ;

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[5] BENZOFURAN BASED ANGIOTENSIN-II ANTAGONISTS RELATED TO GR117289 .2. AMINO-ACID AMIDES [J].

MIDDLEMISS, D ;

WATSON, SP ;

ROSS, BC ;

DOWLE, MD ;

SCOPES, DIC ;

MONTANA, JG ;

HIRST, GC ;

PANCHAL, TA ;

PATON, JMS ;

HUBBARD, T ;

STUART, G ;

DREW, GM ;

HILDITCH, A ;

TRAVERS, A ;

ROBERTSON, MJ ;

HUNT, AAE ;

PALMER, E ;

MANCHEE, GR .

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 1993, 3 (10) :2043-2046

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