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Claims for Patent: 5,978,698

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Claims for Patent: 5,978,698

Title: Angioplasty procedure using nonionic contrast media
Abstract:A method for treating patients in need of percutaneous transluminal coronary angioplasty which comprises administering nonionic contract media to the patient and treating the patient with a fibrinogen receptor antagonist.
Inventor(s): Sax; Frederic L. (Villanova, PA)
Assignee: Merck & Co., Inc. (Rahway, NJ)
Application Number:08/943,872
Patent Claims: 1. A method for treating a patient having coronary artery blockage which comprises

a) introducing nonionic contrast dye into the coronary artery having blockage to image the blockage,

b) administering a fibrinogen receptor antagonist to the patient, and inserting a balloon catheter into the blockage and inflating the balloon at the location of the blockage to revascularize the artery, and

c) administering fibrinogen receptor antagonist to the patient following balloon inflation wherein the fibrinogen receptor antagonist is administered in a therapeutically effective amount sufficient to provide at least 70% inhibition of fibrinogen binding to GP IIb/IIIa.

2. A method of claim 1 wherein the fibrinogen receptor antagonist is administered to the patient according to step c) for a period of time of at least 24 hours.

3. A method of claim 1 wherein the fibrinogen receptor antagonist is orally administered.

4. A method of claim 3, wherein the fibrinogen receptor antagonist is selected from the group consisting of

2(S)-[(p-Toluenesulfonyl)amino]-3-[[[5,6,7,8-tetrahydro-4-oxo-5-[2-(piperid in-4-yl)ethyl]-4H-pyrazolo-[1,5-a][1,4]diazepin-2-yl]carbonyl]-amino]propio nic acid,

Methyl-N.sup.3 -[2-{3-(4-formamidinophenyl)-isoxazolin-5(R)-yl}-acetyl]-N.sup.2 -(n-butyloxycarbonyl)-2,3-(S)-diaminopropionate acetate salt,

Ethyl 3-[[4-[[4-(aminoiminomethyl)phenyl]amino]-1,4-dioxobutyl]amino]-4-pentynoa te, and,

(R)-methyl-3-[[[3-[4-(aminoiminomethyl)phenyl]-4,5-dihydro-5-isoxazolyl]ace tyl]amino]-N-(butoxycarbonyl)-L-alanine monoacetate.

5. A method of claim 1 wherein the fibrinogen receptor antagonist is intravenously administered.

6. A method of claim 5, wherein the fibrinogen receptor antagonist is selected from the group consisting of

Mpr-(Acetimidyl-Lys)-Gly-Asp-Trp-Phe-Cys-NH.sub.2,

Mpr-(Acetimidyl-Lys)-Gly-Asp-Trp-Phe-Pen-NH.sub.2,

Mpr-(Phenylimidyl-Lys)-Gly-Asp-Trp-Phe-Pen-NH.sub.2,

Mpr-(Phenylimidyl-Lys)-Gly-Asp-Trp-Phe-Cys-NH.sub.2,

N-Methyl-D-phenylalanyl-N-[(1S)-1-formyl-4-guanidinobutyl]-L-prolinamide,

((1-(2-((4-(aminoiminomethyl)benzoyl)amino)-3-(4-hydroxyphenyl)-1-oxopropyl )-4-piperidinyl)oxy)-(S)-acetic acid,

N-(2-(2-(((3-((aminoiminomethyl)amino)propyl)amino)carbonyl)-1-piperidnyl)- 1-(cyclohexylmethyl)-2-oxoethyl)-(R,S)-glycine, and

(2-S-(n-Butylsulfonylamino)-3[4-(piperidin-4-yl)butyloxyphenyl]propionic acid hydrochloride.

7. A method of claim 5 wherein the fibrinogen receptor antagonist is Mpr-(Har)-G-D-W-P-C-NH.sub.2.
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