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US 4,730,050 AGranted
Novel enzyme derivatives
AssigneeBeecham Group Limited
InventorRichard A. G. Smith
Life of this patent
Estimating the term…
Abstract
A derivative of a fibrinolytic enzyme in which the catalytic site on the enzyme which is responsible for fibrinolytic activity is blocked by a human protein attached thereto by way of a reversible linking group.
Claims9
A compound of the formula (II):
- ##STR4## wherein B is a hydrophilic linking group;
- A is a bridging group comprising one or two heteroatoms independently selected from the group consisting of oxygen, sulphur and nitrogen, in which the nitrogen is unsubstituted or substituted by alkyl of 1 to 6 carbon atoms;
- X is an optionally substituted benzoyl group further substituted at the 2- or 4-position by the moiety A, and optionally substituted acryloyl group joined to A at the 2- or 3-position or a naphthoyl group;
- and W is a group capable of reacting directly with the amino acid side chain of a protein or with a protein attachment group to produce a covalent bond between B and said side chain or attachment group;
- Z is a counter anion;
- and R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are ach hydrogen or an electron withdrawing moiety which increases the reactivity of an amidinophenyl ester.
3 more elements
Dependencies are inferred from the claim text.