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Last Updated: April 23, 2024

Claims for Patent: 4,741,903

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Summary for Patent: 4,741,903

Title:	Novel enzyne derivatives
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.
Inventor(s):	Smith; Richard A. G. (Reigate, GB2)
Assignee:	Beecham Group p.l.c. (GB2)
Application Number:	07/039,114
Patent Claims:	1. A derivative of 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 derived from the linking agent selected from the group consisting of 4-[N-2-(3-[2-pyridyl]dithiopropionyl)hydrazino]benzoic acid-4'-amidinophenyl ester; N-(6-[3-(2-pyridyl)dithiopropionyl]aminohexyl)anthranilic acid-4'-amidinophenyl ester; 4-amidinophenyl N-4-(N-2-[3-(2-pyridyldithio)propionyl]aminoethyl)aminobenzoate; and 2-chloro-4-amidinophenyl N-4-(N-2-[3-(2-pyridyldithio)propionyl]aminoethyl)aminobenzoate. 2. A derivative according to claim 1 selected from the group consisting of 4-[N-2-(3-[4'-butyrimino(N'-.epsilon.-lys human high molecular weight urokinase)]dithiopropionyl)hydrazino]benzoyl-O-(ser-740) human plasmin; N-[N'-6-(3-[4'-butyrimino(N"-.epsilon.-lys human high molecular weight urokinase)]dithiopropionyl)aminohexyl]anthraniloyl-O-(ser-740) human plasmin; 4-N-[N'-2-(3-[4'-butyrimino(N"-.epsilon.-lys human high molecular weight urokinase)]dithiopropionyl)aminoethyl]aminobenzoyl-O-(ser-740) human plasmin; and 4-[N-2-(3-[4'-butyrimino(N'-.epsilon.-lys human immunoglobulin G)]dithiopropionyl)hydrazino]benzoyl-O-(ser-478) human tissue-type plasminogen activator. 3. A pharmaceutical composition useful for treating thrombotic diseases in humans which comprises a therapeutically effective amount of 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 derived from the linking agent selected from the group consisting of 4-[N-2-(3-[2-pyridyl]dithiopropionyl)hydrazino]benzoic acid-4'-amidinophenyl ester; N-(6-[3-(2-pyridyl)dithiopropionyl]aminohexyl)anthranilic acid-4'-amidinophenyl ester; 4-amidinophenyl N-4-(N-2-[3-(2-pyridyldithio)propionyl]aminoethyl)aminobenzoate; and 2-chloro-4-amidinophenyl N-4-(N-2-[3-(2-pyridyldithio)propionyl]aminoethyl)aminobenzoate, in combination with a pharmaceutically acceptable carrier. 4. A composition according to claim 3 wherein the derivative is selected from the group consisting of 4-[N-2-(3-[4'-butyrimino(N'-.epsilon.-lys human high molecular weight urokinase)]dithiopropionyl)hydrazino]benzoyl-O-(ser-740) human plasmin; N-[N'-6-(3-[4'-butyrimino(N"-.epsilon.-lys human high molecular weight urokinase)]dithiopropionyl)aminohexyl]anthraniloyl-O-(ser-740) human plasmin; 4-N-[N'-2-(3-[4'-butyrimino(N"-.epsilon.-lys human high molecular weight urokinase)]dithiopropionyl)aminoethyl]aminobenzoyl-O-(ser-740) human plasmin; and 4-[N-2-(3-[4'-butyrimino(N'-.epsilon.-lys human immunoglobulin G)]dithiopropionyl)hydrazino]benzoyl-O-(ser-478) human tissue-type plasminogen activator. 5. A method of treating thrombotic diseases in humans which comprises administering to a human in need thereof a therapeutically effective amount of 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 derived from the linking agent selected from the group consisting of 4-[N-2-(3-[2-pyridyl]dithiopropionyl)hydrazino]benzoic acid-4'-amidinophenyl ester; N-(6-[3-(2-pyridyl)dithiopropionyl]aminohexyl)anthranilic acid-4'-amidinophenyl ester; 4-amidinophenyl N-4-(N-2-[3-(2-pyridyldithio)propionyl]aminoethyl)aminobenzoate; and 2-chloro-4-amidinophenyl N-4-(N-2-[3-(2-pyridyldithio)propionyl]aminoethyl)aminobenzoate, in combination with a pharmaceutically acceptable carrier. 6. A method according to claim 5 wherein the derivative is selected from the group consisting of 4-[N-2-(3-[4'-butyrimino(N'-.epsilon.-lys human high molecular weight urokinase)]dithiopropionyl)hydrazino]benzoyl-O-(ser-740) human plasmin; N-[N'-6-(3-[4'-butyrimino(N"-.epsilon.-lys human high molecular weight urokinase)]dithiopropionyl)aminohexyl]anthraniloyl-O-(ser-740) human plasmin; 4-N-[N'-2-(3-[4'-butyrimino(N"-.epsilon.-lys human high molecular weight urokinase)]dithiopropionyl)aminoethyl]aminobenzoyl-O-(ser-740) human plasmin; and 4-[N-2-(3-[4'-butyrimino(N'-.epsilon.-lys human immunoglobulin G)]dithiopropionyl)hydrazino]benzoyl-O-(ser-478) human tissue-type plasminogen activator.

Details for Patent 4,741,903

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Applicant	Tradename	Biologic Ingredient	Dosage Form	BLA	Approval Date	Patent No.	Expiredate
Microbix Biosystems Inc.	KINLYTIC	urokinase	For Injection	021846	01/16/1978	⤷ Try a Trial	2003-12-24
Csl Behring Ag	CARIMUNE, CARIMUNE NF, PANGLOBULIN, SANDOGLOBULIN	immune globulin intravenous (human)	For Injection	102367	07/27/2000	⤷ Try a Trial	2003-12-24
Csl Behring Ag	PRIVIGEN	immune globulin intravenous (human), 10% liquid	Injection	125201	07/26/2007	⤷ Try a Trial	2003-12-24
Csl Behring Ag	PRIVIGEN	immune globulin intravenous (human), 10% liquid	Injection	125201	10/02/2009	⤷ Try a Trial	2003-12-24
Csl Behring Ag	PRIVIGEN	immune globulin intravenous (human), 10% liquid	Injection	125201	02/07/2013	⤷ Try a Trial	2003-12-24
>Applicant	>Tradename	>Biologic Ingredient	>Dosage Form	>BLA	>Approval Date	>Patent No.	>Expiredate

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