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1. WO2016144654 - INHIBITORS OF GROWTH FACTOR ACTIVATION ENZYMES

Publication Number WO/2016/144654
Publication Date 15.09.2016
International Application No. PCT/US2016/020516
International Filing Date 02.03.2016
IPC
A61K 38/04 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
38Medicinal preparations containing peptides
04Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
A61K 38/06 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
38Medicinal preparations containing peptides
04Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
06Tripeptides
C07K 5/09 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
5Peptides having up to four amino acids in a fully defined sequence; Derivatives thereof
04containing only normal peptide links
08Tripeptides
09the side chain of the first amino acid containing more amino groups than carboxyl groups, or derivatives thereof, e.g. Lys, Arg
C07K 5/083 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
5Peptides having up to four amino acids in a fully defined sequence; Derivatives thereof
04containing only normal peptide links
08Tripeptides
083the side chain of the first amino acid being acyclic, e.g. Gly, Ala
CPC
A61K 38/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
38Medicinal preparations containing peptides
A61K 47/64
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
50the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
51the non-active ingredient being a modifying agent
62the modifying agent being a protein, peptide or polyamino acid
64Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent
A61K 49/0052
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
49Preparations for testing in vivo
001Preparation for luminescence or biological staining
0013Luminescence
0017Fluorescence in vivo
005characterised by the carrier molecule carrying the fluorescent agent
0052Small organic molecules
A61K 49/0056
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
49Preparations for testing in vivo
001Preparation for luminescence or biological staining
0013Luminescence
0017Fluorescence in vivo
005characterised by the carrier molecule carrying the fluorescent agent
0056Peptides, proteins, polyamino acids
A61K 51/0453
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
51Preparations containing radioactive substances for use in therapy or testing in vivo
02characterised by the carrier ; , i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
04Organic compounds
041Heterocyclic compounds
044having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
0453having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
A61K 51/08
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
51Preparations containing radioactive substances for use in therapy or testing in vivo
02characterised by the carrier ; , i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
04Organic compounds
08Peptides, e.g. proteins ; , carriers being peptides, polyamino acids, proteins
Applicants
  • WASHINGTON UNIVERSITY [US]/[US]
Inventors
  • JANETKA, James,, W.
  • HAN, Zhenfu
  • HARRIS, Peter
  • KARMAKAR, Partha
Agents
  • TIETZ, Paul, D.
Priority Data
62/130,11709.03.2015US
62/220,99819.09.2015US
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) INHIBITORS OF GROWTH FACTOR ACTIVATION ENZYMES
(FR) INHIBITEURS D'ENZYMES D'ACTIVATION DE FACTEUR DE CROISSANCE
Abstract
(EN)
The present invention generally relates to compounds that are useful for inhibiting one or more of hepatocyte growth factor activator, matriptase, hepsin, Factor Xa, or thrombin. The present invention also relates to various methods of using the inhibitor compounds including treating a malignancy, a pre-malignant condition, or cancer by administering an effective amount of the inhibitor to a subject in need thereof.
(FR)
La présente invention concerne d'une manière générale des composés qui sont utiles pour inhiber un ou plusieurs éléments parmi l'activateur du facteur de croissance des hépatocytes, la matriptase, l'hepsine, le facteur Xa ou la thrombine. La présente invention concerne également divers procédés d'utilisation des composés inhibiteurs comprenant le traitement d'une tumeur maligne, un état pré-malin, ou un cancer par l'administration d'une quantité efficace de l'inhibiteur à un sujet en ayant besoin.
Also published as
Latest bibliographic data on file with the International Bureau