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1. (WO1992010575) BIFUNCTIONAL INHIBITORS OF THROMBIN AND PLATELET ACTIVATION
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/1992/010575 International Application No.: PCT/US1991/009108
Publication Date: 25.06.1992 International Filing Date: 05.12.1991
Chapter 2 Demand Filed: 07.07.1992
IPC:
A61K 38/00 (2006.01) ,A61K 38/58 (2006.01) ,C07K 14/245 (2006.01) ,C07K 14/46 (2006.01) ,C07K 14/815 (2006.01) ,C12N 15/62 (2006.01)
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
38
Medicinal preparations containing peptides
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
55
Protease inhibitors
57
from animals; from humans
58
from leeches, e.g. hirudin, eglin
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
K
PEPTIDES
14
Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
195
from bacteria
24
from Enterobacteriaceae (F), e.g. Citrobacter, Serratia, Proteus, Providencia, Morganella, Yersinia
245
Escherichia (G)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
K
PEPTIDES
14
Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
435
from animals; from humans
46
from vertebrates
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
K
PEPTIDES
14
Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
81
Protease inhibitors
815
from leeches, e.g. hirudin, eglin
C CHEMISTRY; METALLURGY
12
BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
N
MICRO-ORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICRO-ORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
15
Mutation or genetic engineering; DNA or RNA concerning genetic engineering, vectors, e.g. plasmids, or their isolation, preparation or purification; Use of hosts therefor
09
Recombinant DNA-technology
11
DNA or RNA fragments; Modified forms thereof
62
DNA sequences coding for fusion proteins
Applicants:
BIOGEN, INC. [US/US]; 14 Cambridge Center Cambridge, MA 02142, US
Inventors:
MARAGANORE, John, M.; US
CHAO, Betty, H.; US
STRAUCH, Kathryn, Louise; US
THOMPSON, Jeffrey, Scott; US
Agent:
PIERRI, Margaret, A.; Fish & Neave 875 Third Avenue New York, NY 10022-6250, US
Priority Data:
623,61107.12.1990US
Title (EN) BIFUNCTIONAL INHIBITORS OF THROMBIN AND PLATELET ACTIVATION
(FR) INHIBITEURS BIFONCTIONNELS DE THROMBINE ET D'ACTIVATION PLAQUETTAIRE
Abstract:
(EN) The present invention relates to novel, bifunctional inhibitors of both platelet activation and thrombin. These bifunctional inhibitors are characterized by two domains - a glycoprotein IIb/IIIa inhibitory domain and a thrombin inhibitory domain. The invention also relates to DNA sequences which encode the bifunctional inhibitors of this invention, recombinant DNA molecules which contain these DNA sequences and host transformed with these DNA molecules. The invention further relates to the recombinant expression of the bifunctional inhibitors of this invention by transformed hosts as well as to methods for purifying such recombinant bifunctional inhibitors. This invention also provides compositions and methods employing the novel bifunctional inhibitors alone or together with a fibrinolytic agent. Such compositions may be useful in patients for treating thrombotic disease, increasing reocclusion time, decreasing reperfusion time, simultaneously inhibiting thrombin- and platelet-mediated functions and inhibiting malignant cell growth.
(FR) La présente invention se rapporte à de nouveaux inhibiteurs bifonctionnels d'activation plaquettaire et de thrombine à la fois. Ces inhibiteurs bifonctionnels se caractérisent par deux domaines: un domaine d'inhibition de glycoprotéine IIb/IIIa et un domaine d'inhibition de thrombine. L'inventin on se rapporte aussi à des séquences d'ADN qui codent les inhibiteurs bifonctionnels de l'invention, des molécules d'ADN de recombinaison qui contiennent ces séquences d'ADN et des hôtes transformés à l'aide de ces molécules d'ADN. L'invention se rapporte en outre à l'expression par recombinaison de ces inhibiteurs bifonctionnels par des hôtes transformés ainsi qu'à des procédés de purification de tels inhibiteurs bifonctionnels de recombinaison. L'invention décrit aussi des compositions et des procédés utilisant ces nouveaux inhibiteurs bifonctionnels seuls ou en combinaison avec un agent fibrinolytique. De telles compositions peuvent se révéler utiles en ce qui concerne le traitement de maladies thrombotiques, pour augmenter le temps de réocclusion, diminuer le temps de reperfusion, inhiber simultanément des fonctions à médiation de thrombine et de plaquettes et inhiber la croissance de cellules malignes.
Designated States: AU, CA, JP
European Patent Office (AT, BE, CH, DE, DK, ES, FR, GB, GR, IT, LU, MC, NL, SE)
Publication Language: English (EN)
Filing Language: English (EN)
Also published as:
EP0560913JPH06503474CA2096545AU1991091417