Nonpeptide glycoprotein IIb/IIIa inhibitors .13. Design and synthesis of an orally active pyrazolopiperazinone nonpeptide fibrinogen receptor antagonist.

被引：26

作者：

Askew, BC ^{[1
]}

McIntyre, CJ ^{[1
]}

Hunt, CA ^{[1
]}

Claremon, DA ^{[1
]}

Baldwin, JJ ^{[1
]}

Anderson, PS ^{[1
]}

Gould, RJ ^{[1
]}

Lynch, RJ ^{[1
]}

Chang, CCT ^{[1
]}

Cook, JJ ^{[1
]}

Lynch, JJ ^{[1
]}

Holahan, MA ^{[1
]}

Sitko, GR ^{[1
]}

Stranieri, MT ^{[1
]}

机构：

[1] MERCK RES LABS,DEPT PHARMACOL,W POINT,PA 19486

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1997年 / 7卷 / 12期

关键词：

D O I：

10.1016/S0960-894X(97)00256-4

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The synthesis and antiplatelet activity of a series of pyrazolopiperazinone nonpeptide fibrinogen receptor antagonists is reported. The sulfonamide analog 6 (L-734,115), significantly inhibited ex vivo platelet aggregation 24 h after oral administration at doses of 1.0 and 2.0 mg/kg to dogs and rhesus monkeys, respectively. (C) 1997 Elsevier Science Ltd.

引用

页码：1531 / 1536

页数：6

共 16 条

[1] IDENTIFICATION AND CHARACTERIZATION OF CELL-SUBSTRATUM ADHESION RECEPTORS ON CULTURED HUMAN-ENDOTHELIAL CELLS
ALBELDA, SM
DAISE, M
LEVINE, EM
BUCK, CA
[J]. JOURNAL OF CLINICAL INVESTIGATION, 1989, 83 (06) : 1992 - 2002
[2] NONPEPTIDE GLYCOPROTEIN IIB/IIIA INHIBITORS .6. DESIGN AND SYNTHESIS OF RIGID, CENTRALLY CONSTRAINED NONPEPTIDE FIBRINOGEN RECEPTOR ANTAGONISTS
ASKEW, BC
MCINTYRE, CJ
HUNT, CA
CLAREMON, DA
GOULD, RJ
LYNCH, RJ
ARMSTRONG, DJ
[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 1995, 5 (05) : 475 - 480
[3] CADROY Y, 1990, CARDIOVASCULAR PHARM, P515
[4] PLATELETS AND THROMBOLYTIC THERAPY
COLLER, BS
[J]. NEW ENGLAND JOURNAL OF MEDICINE, 1990, 322 (01) : 33 - 42
[5] Cook Nigel S., 1994, Drugs of the Future, V19, P135
[6] NONPEPTIDE FIBRINOGEN RECEPTOR ANTAGONISTS .7. DESIGN AND SYNTHESIS OF A POTENT, ORALLY-ACTIVE FIBRINOGEN RECEPTOR ANTAGONIST
DUGGAN, ME
NAYLOROLSEN, AM
PERKINS, JJ
ANDERSON, PS
CHANG, CTC
COOK, JJ
GOULD, RJ
IHLE, NC
HARTMAN, GD
LYNCH, JJ
LYNCH, RJ
MANNO, PD
SCHAFFER, LW
SMITH, RL
[J]. JOURNAL OF MEDICINAL CHEMISTRY, 1995, 38 (17) : 3332 - 3341
[7] NONPEPTIDE FIBRINOGEN RECEPTOR ANTAGONISTS .3. DESIGN AND DISCOVERY OF A CENTRALLY CONSTRAINED INHIBITOR
EGBERTSON, MS
NAYLOR, AM
HARTMAN, GD
COOK, JJ
GOULD, RJ
HOLAHAN, MA
LYNCH, JJ
LYNCH, RJ
STRANIERI, MT
VASSALLO, LM
[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 1994, 4 (15) : 1835 - 1840
[8] EGBERTSON MS, IN PRESS BIOORG MED
[9] UNSTABLE ANGINA WITH FATAL OUTCOME - DYNAMIC CORONARY THROMBOSIS LEADING TO INFARCTION AND OR SUDDEN-DEATH - AUTOPSY EVIDENCE OF RECURRENT MURAL THROMBOSIS WITH PERIPHERAL EMBOLIZATION CULMINATING IN TOTAL VASCULAR OCCLUSION
FALK, E
[J]. CIRCULATION, 1985, 71 (04) : 699 - 708
[10] JAKABOWSKI JA, 1992, ANN REPT MED CHEM, V27, P99

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