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1. (WO1991008765) STABILIZATION OF K2P PRO
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/1991/008765 International Application No.: PCT/EP1990/002250
Publication Date: 27.06.1991 International Filing Date: 19.12.1990
IPC:
A61K 38/49 (2006.01) ,A61K 47/12 (2006.01) ,A61K 47/18 (2006.01) ,A61K 47/22 (2006.01) ,A61K 47/26 (2006.01)
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
38
Medicinal preparations containing peptides
16
Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
43
Enzymes; Proenzymes; Derivatives thereof
46
Hydrolases (3)
48
acting on peptide bonds (3.4)
49
Urokinase; Tissue plasminogen activator
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47
Medicinal preparations characterised by the non-active ingredients used, e.g. carriers, inert additives
06
Organic compounds
08
containing oxygen
12
Carboxylic acids; Salts or anhydrides thereof
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47
Medicinal preparations characterised by the non-active ingredients used, e.g. carriers, inert additives
06
Organic compounds
16
containing nitrogen
18
Amines; Quaternary ammonium compounds
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47
Medicinal preparations characterised by the non-active ingredients used, e.g. carriers, inert additives
06
Organic compounds
22
Heterocyclic compounds
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47
Medicinal preparations characterised by the non-active ingredients used, e.g. carriers, inert additives
06
Organic compounds
26
Carbohydrates
Applicants:
BOEHRINGER MANNHEIM GMBH [DE/DE]; Sandhofer Straße 112-132 D-6800 Mannheim-Waldhof, DE (AllExceptUS)
KOHNERT, Ulrich [DE/DE]; DE (UsOnly)
RUDOLPH, Rainer [DE/DE]; DE (UsOnly)
Inventors:
KOHNERT, Ulrich; DE
RUDOLPH, Rainer; DE
Agent:
WEICKMANN, H. ; Möhlstraße 22 D-8000 München 80, DE
Priority Data:
P 39 42 141.420.12.1989DE
Title (DE) K2P PRO-STABILISIERUNG
(EN) STABILIZATION OF K2P PRO
(FR) STABILISATION DE K2P PRO
Abstract:
(DE) Pharmazeutisches Präparat eines nicht glykosylierten t-PA-Derivats K2P pro mit einer enzymatischen Aktivität von mindestens 1,4 MU/ml und einem pH-Wert von 4,5 bis 6,5, das Citrat und mindestens eine Verbindung aus der aus a) Ascorbinsäure, b) EDTA, c) Aminoverbindungen der Formel R1R2N - R - X, wobei X = SO3H, CH(NH2)-CO2H, CO2H, H, NH2 oder OH ist, R = C1-C9-Alkylen, vorzugsweise C4-C7-Alkylen, C3-C6-Cycloalkylen oder Benzyliden ist und R1 und R2 voneinander unabhängig H oder C1-C3-Alkyl sind, d) Guanidin-analoge Verbindungen der Formel (I) wobei Y = H2N+ oder 0 ist, Z = H oder (CH2)m V, (CH2)mCH(NH2)-CO2H, CH(CO2H)-(CH2)mCO2H ist, V = NH2 oder CO2H und m = 1 bis 4 ist, e) mit einer oder mehreren Hydroxy-, Keto- oder/und weiteren Carboxylgruppen substituierten Carbonsäuren, f) Dimethylbiguanid, g) Pyrimidinnukleosiden und Pyrimidinnukleotiden, h) Trehalose, Glucosamin bestehenden Gruppe enthält sowie Arzneimittel auf Basis des t-PA-Derivats K2P pro als Wirkstoff und Verfahren zu seiner Herstellung.
(EN) The invention relates to a pharmaceutical preparation of a non-glycosylized t-PA derivative, K2P pro, with an enzymatic activity of at least 1.4 MU/ml and a pH of 4.5 to 6.5, containing citrate and at least one compound from the following group: a) ascorbic acid, b) EDTA, c) amino compounds of formula R1R2N - R - X, where X = SO3H, CH(NH2)-CO2H, CO2H, H, NH2 or OH, R = C1-C9 alkylene, preferably C4-C7 alkylene, C3-C6 cycloalkylene or benzylidene and R1 and R2, independently of each other, are H or C1-C3 alkyl, d) guianidine analogs of formula (II), where Y = H2N+ or 0, Z = H or (CH2)m V, (CH2)mCH(NH2)-CO2H, CH(CO2H)-(CH2)mCO2H, V = NH2 or CO2H and m = 1 to 4, e) carboxylic acids substituted with one or more hydroxyl, keto and/or further carboxyl groups, f) dimethylbiguanide, g) pyrimidine nucleosides and pyrimidine nucleotides, h) trehalose, glucosamine. The invention also relates to a drug based on the t-PA derivative K2P pro as the active ingredient and a process for producing it.
(FR) Une composition pharmaceutique d'un dérivé K2P pro de t-PA non glycosylé, ayant une activité enzymatique d'au moins 1,4 MU/ml et une valeur de pH comprise entre 4,5 et 6,5, contient du citrate et au moins un composé du groupe formé par: a) l'acide ascorbique; b) l'EDTA; c) des composés amine ayant la formule R1R2N - R - X, dans laquelle X = SO3H, CH(NH2)-CO2H, CO2H, H, NH2 ou OH, R =C1-C9-alkylène, de préférence C4-C7-alkylène, C3-C6-cycloalkylène ou benzylidène et R1 et R2 représentent indépendamment l'un de l'autre H ou C1-C3-alkyle; d) des composés analogues de la guanidine ayant la formule (II), dans laquelle Y = H2N+ ou 0; Z = H ou (CH2)m V, (CH2)mCH(NH2)-CO2H, CH(CO2H)-(CH2)mCO2H; V = NH2 ou CO2H et m = 1 à 4; e) des acides carboxyliques substitués par un ou plusieurs groupes hydroxyles, cétoniques et/ou des groupes carboxyles additionnels; f) la diméthylbiguanide; g) des nucléosides et des nucléotides de pyrimidine; h) le tréhalose et la glucosamine. L'invention concerne également un médicament à base du dérivé K2P pro de t-PA comme principe actif et son procédé de production.
Designated States: AU, CA, FI, HU, JP, KR, NO, SU, US
European Patent Office (AT, BE, CH, DE, DK, ES, FR, GB, GR, IT, LU, NL, SE)
Publication Language: German (DE)
Filing Language: German (DE)
Also published as:
FI913908NO19913238ES2060357EP0458950US5352452JPH04503683
CA2046861KR1019920700681AU1991070443DK0458950