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Serving 500+ biopharmaceutical companies globally:

Mallinckrodt
Argus Health
Federal Trade Commission
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US Army
Healthtrust
Fuji
US Department of Justice
Covington
Boehringer Ingelheim

Generated: September 20, 2017

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Title: Platelet aggregation inhibitors
Abstract:An assay for screening snake venom for the presence or absence of platelet aggregation inhibitors (PAIs) based on specific receptor binding is described. Using this assay, the identification and characterization of PAIs in a wide range of snake venom samples was accomplished. The isolated and purified PAI from several of these active snake venoms is described and characterized. In addition, PAIs lacking the Arg-Gly-Asp (RGD) adhesion sequence but containing K*-(G/Sar)-D wherein K* is a modified lysyl residue of the formula wherein each R.sup.1 is independently H, alkyl(1-6C) or at most one R.sup.1 is R.sup.2 --C.dbd.NR.sup.3 wherein R.sup.2 is H, alkyl(1-6C), phenyl or benzyl, or is NR.sup.4.sub.2 in which each R.sup.4 is independently H or alkyl(1-6C) and R.sup.3 is H, alkyl(1-6C), phenyl or benzyl, or R.sup.2 --C.dbd.NR.sup.3 is a radical selected from the group consisting of: ##STR1## where m is an integer of 2-3, and each R.sup.5 is independently H or alkyl(1-6C); and wherein one or two (CH.sub.2) may be replaced by O or S provided said O or S is not adjacent to another heteroatom are prepared and shown to specifically inhibit the binding of fibrinogen or von Willebrand Factor to GP IIb-IIIa.
Inventor(s): Scarborough; Robert M. (Belmont, CA), Wolf; David Lawrence (Palo Alto, CA), Charo; Israel F. (Lafayette, CA)
Assignee: COR Therapeutics, Inc. (South San Francisco, CA)
Application Number:08/463,765
Patent Claims: 1. A compound of the formula: ##STR12## wherein Y.sub.1 -X.sub.1 is Mpr, n1 is 0, K.sup.* is Har, G or Sar is G, AA.sub.2 is W, n2 is 1, AA.sub.3 is a proline residue, n3 is 1, n4 is 0, X.sub.2 is C, Y.sub.2 is NH.sub.2, and ##STR13## represents a disulfide bond, or a physiologically acceptable basic or acid addition salt thereof.

2. A compound according to claim 1 having the formula: ##STR14##

3. A compound comprising a physiologically acceptable acid addition salt of the compound of claim 2.

4. A compound comprising a platelet aggregation inhibitor of the formula: ##STR15## wherein Y.sub.1 -X.sub.1 is Mpr, n1 is 0, K.sup.* is Har, G or Sar is G, AA.sub.2 is W, n2 is 1, AA.sub.3 is a proline residue, n3 is 1, n4 is 0, X.sub.2 is C, Y.sub.2 is NH.sub.2, and ##STR16## represents a disulfide bond, or a physiologically acceptable basic or acid addition salt thereof.

5. A compound according to claim 4, the platelet aggregation inhibitor having the formula: ##STR17##

6. A compound comprising a physiologically acceptable acid addition salt of the compound of claim 5.

7. A compound consisting essentially of a platelet aggregation inhibitor that inhibits (a) binding of Fg or vWF to GP IIb-IIIa more than (b) binding of vitronectin to vitronectin receptor or fibronectin to fibronectin receptor, which platelet aggregation inhibitor has the formula: ##STR18## wherein Y.sub.1 -X.sub.1 is Mpr, n1 is 0, K.sup.* is Har, G or Sar is G, AA.sub.2 is W, n2 is 1, AA.sub.3 is a proline residue, n3 is 1, n4 is 0, X.sub.2 is C, Y.sub.2 is NH.sub.2, and ##STR19## represents a disulfide bond, or a physiologically acceptable basic or acid addition salt thereof.

8. A compound according to claim 7, having the formula: ##STR20##

9. A compound comprising a physiologically acceptable acid addition salt of the compound of claim 8.

10. A pharmaceutical composition which comprises a compound as in any one of claims 1-9 in admixture with a pharmaceutically acceptable excipient.

11. The compound of claim 10, wherein said compound is present in an amount effective to inhibit platelet aggregation.
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Serving 500+ biopharmaceutical companies globally:

Covington
Deloitte
Express Scripts
Merck
Fish and Richardson
US Department of Justice
Novartis
Healthtrust
Julphar
Baxter

Drugs may be covered by multiple patents or regulatory protections. All trademarks and applicant names are the property of their respective owners or licensors. Although great care is taken in the proper and correct provision of this service, thinkBiotech LLC does not accept any responsibility for possible consequences of errors or omissions in the provided data. The data presented herein is for information purposes only. There is no warranty that the data contained herein is error free. thinkBiotech performs no independent verifification of facts as provided by public sources nor are attempts made to provide legal or investing advice. Any reliance on data provided herein is done solely at the discretion of the user. Users of this service are advised to seek professional advice and independent confirmation before considering acting on any of the provided information. thinkBiotech LLC reserves the right to amend, extend or withdraw any part or all of the offered service without notice.

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