Pyrrolidine compounds having thromboxane A.sub.2 receptor antago

Details Pyrrolidine compounds having thromboxane A.sub.2 receptor antago Pyrrolidine compounds having thromboxane A.sub.2 receptor antago

1992-12-18

1994-03-22

Ivy, C. Warren

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

514333, 514423, 514424, 514426, 514428, 546256, 546281, 548530, 548531, 548538, 548539, 548542, 548557, 548572, A61K 3144, C07D40106, C07D20748

Patent

active

052964949

ABSTRACT:
Compounds of formula (I): ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, m, n, and R are as defined in the Specification.
Medicinal products containing the same are useful in the treatment or prevention of thrombotic afflictions due to their thromboxane A.sub.2 receptor antagonistic activity and their thromboxane A.sub.2 synthase inhibitory activity.

REFERENCES:
patent: 4916152 (1990-04-01), Setoi
patent: 5168101 (1992-12-01), Arai
Gallagher et al "Electrophile-mediated cyclization" J. Chem. Soc. Perk. Trans 1(4) 433-440 (1992).
Setoi et al "Preparation of 1-alkyl-2-(carboxyalkenyl)-3-acylamino pyrrolidine as TBXA.sub.2 antagonist" CA 114:42564q (1991).
Zeffren et al "The Study of Enzyme Mechanisms" John Wiley and Sons, p. 87 (1974).
Inhibition of Collagen-induced Human Platelet Activation in Citrated Whole Blood by ICI D1542, A Thromboxane A.sub.2 Synthase Inhibitor and Cyclic Endoperoxide . . . V. C. Menys, Platelets 3, 331-335 (1992).
Thromboxane Receptor Antagonism Combined with Thromboxane Synthase Inhibition 5. Synthesis and evaluation of Enantiomers of 8-[[(4-Cholorophenyl)sulfonyl]amino . . . S. S. Bhagwat et al., J. Med. Chem. 36, 205-210 (1993).
Ridogrel Inhibits Systemic and Renal Formation of Thromboxane A.sub.2 /Prostaglandin Endoperoxide Receptors upon Chronic Administration to Man, C. Weber et al., Thrombosis and Haemostasis 68(2), 214-220 (1992).
Bay u 3405, Thromboxane Endoperoxide Receptor Antagonist, Drugs of the Future 16(8): 701-705 (1991).
Antiplatelet Activity of the Long-Acting Thromboxane Receptor Antagonist BMS 180,291 in Monkeys, W. A. Schumacher et al., Prostaglandins 44, 389-397 (1992).

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