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
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
收藏
页码:2047 / 2050
页数:4
相关论文
共 5 条
[1]  
CANGIANO JL, 1979, J PHARMACOL EXP THER, V208, P310
[2]  
DUDLEY DT, 1993, CURRENT OPINION THER, V3, P581
[3]   BENZOFURAN BASED ANGIOTENSIN-II ANTAGONISTS RELATED TO GR117289 - ENHANCEMENT OF POTENCY INVITRO AND ORAL ACTIVITY [J].
MIDDLEMISS, D ;
WATSON, SP ;
ROSS, BC ;
DOWLE, MD ;
SCOPES, DIC ;
MONTANA, JG ;
SHAH, P ;
HIRST, GC ;
PANCHAL, TA ;
PATON, JMS ;
PASS, M ;
HUBBARD, T ;
HAMBLETT, J ;
CARDWELL, KS ;
JACK, TI ;
STUART, G ;
COOTE, S ;
BRADSHAW, J ;
DREW, GM ;
HILDITCH, A ;
CLARK, KL ;
ROBERTSON, MJ ;
BAYLISS, MK ;
DONNELLY, M ;
PALMER, E ;
MANCHEE, GRM .
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 1993, 3 (04) :589-594
[4]   BROMOBENZOFURANS - A NEW CLASS OF POTENT, NONPEPTIDE ANTAGONISTS OF ANGIOTENSIN-II [J].
MIDDLEMISS, D ;
DREW, GM ;
ROSS, BC ;
ROBERTSON, MJ ;
SCOPES, DIC ;
DOWLE, MD ;
AKERS, J ;
CARDWELL, K ;
CLARK, KL ;
COOTE, S ;
ELDRED, CD ;
HAMBLETT, J ;
HILDITCH, A ;
HIRST, GC ;
JACK, T ;
MONTANA, J ;
PANCHAL, TA ;
PATON, JMS ;
SHAH, P ;
STUART, G ;
TRAVERS, A .
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 1991, 1 (12) :711-716
[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