MX9605037A - FACTOR Xa INHIBITORS. - Google Patents

FACTOR Xa INHIBITORS.

Info

Publication number
MX9605037A
MX9605037A MX9605037A MX9605037A MX9605037A MX 9605037 A MX9605037 A MX 9605037A MX 9605037 A MX9605037 A MX 9605037A MX 9605037 A MX9605037 A MX 9605037A MX 9605037 A MX9605037 A MX 9605037A
Authority
MX
Mexico
Prior art keywords
activity
factor
compound
amino acids
provides
Prior art date
Application number
MX9605037A
Other languages
Spanish (es)
Inventor
Fahad Al-Obeidi
Michal Lebl
James A Ostrem
Pavel Safar
Alena Stierandova
Peter Strop
Armin Walser
Original Assignee
Selectide Corp
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Selectide Corp filed Critical Selectide Corp
Priority claimed from PCT/US1995/005268 external-priority patent/WO1995029189A1/en
Publication of MX9605037A publication Critical patent/MX9605037A/en

Links

Classifications

    • YGENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02PCLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00Technologies relating to chemical industry
    • Y02P20/50Improvements relating to the production of bulk chemicals
    • Y02P20/55Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

Abstract

The invention provides compounds which specifically inhibit factor Xa activity. The compounds consist of the structure X1-YIR-X2, wherein X1 is H, acyl, alkyl, acylalkyl, arylalkyl or one or more amino acids, and X2 is a modified C-terminal group, one or more carboxy-protecting groups or one or more amino acids or other substituent, and Y, I and R are tyrosine, isoleucine and arginine, respectively, or peptidomimetic or organic structures that possess the same functional activity as Y, I and R, respectively. In addition, the present invention provides a compound having the structure A1-A2-(A3)m-B, where m is 0 or 1. A compound of the invention can be linear or cyclic and can be about 2 and 43 residues in length. A compound of the invention is characterized, in part, in that it exhibits a specific inhibition of factor Xa activity with a Ki of o 100 'mu'M, preferably o 2 nM, and does not substantially inhibit the activity of other proteases involved in the coagulation cascade. The invention further provides methods of specifically inhibiting the activity of factor Xa and of inhibiting blood clotting in vitro and in an individual and methods of detecting factor Xa levels or activity.
MX9605037A 1995-04-25 1995-04-25 FACTOR Xa INHIBITORS. MX9605037A (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
PCT/US1995/005268 WO1995029189A1 (en) 1994-04-26 1995-04-25 FACTOR Xa INHIBITORS

Publications (1)

Publication Number Publication Date
MX9605037A true MX9605037A (en) 1998-02-28

Family

ID=39165061

Family Applications (1)

Application Number Title Priority Date Filing Date
MX9605037A MX9605037A (en) 1995-04-25 1995-04-25 FACTOR Xa INHIBITORS.

Country Status (1)

Country Link
MX (1) MX9605037A (en)

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Legal Events

Date Code Title Description
FG Grant or registration
MM Annulment or lapse due to non-payment of fees