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1. EP3601287 - 2,6-DISUBSTITUTED-9-CYCLOPENTYL-9H-PURINES, USE THEREOF AS MEDICAMENTS, AND PHARMACEUTICAL COMPOSITIONS

Office
European Patent Office
Application Number 18720082
Application Date 19.03.2018
Publication Number 3601287
Publication Date 05.02.2020
Publication Kind B1
IPC
C07D 473/34
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
473Heterocyclic compounds containing purine ring systems
26with an oxygen, sulfur, or nitrogen atom directly attached in position 2 or 6, but not in both
32Nitrogen atom
34attached in position 6, e.g. adenine
A61K 31/52
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
495having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
519ortho- or peri-condensed with heterocyclic rings
52Purines, e.g. adenine
A61P 35/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
CPC
C07D 473/16
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
473Heterocyclic compounds containing purine ring systems
02with oxygen, sulfur or nitrogen atoms directly attached in positions 2 and 6
16two nitrogen atoms
A61K 31/52
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
495having six-membered rings with two ; or more; nitrogen atoms as the only ring heteroatoms, e.g. piperazine ; or tetrazines
505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
519ortho- or peri-condensed with heterocyclic rings
52Purines, e.g. adenine
A61P 35/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
A61P 35/02
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
02specific for leukemia
C07D 473/34
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
473Heterocyclic compounds containing purine ring systems
26with an oxygen, sulfur or nitrogen atom directly attached in position 2 or 6, but not in both
32Nitrogen atom
34attached in position 6, e.g. adenine
A61K 31/5377
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
535having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
53751,4-Oxazines, e.g. morpholine
5377not condensed and containing further heterocyclic rings, e.g. timolol
Applicants UNIV PALACKEHO
Inventors GUCKY TOMAS
REZNICKOVA EVA
JORDA RADEK
KRYSTOF VLADIMIR
STRNAD MIROSLAV
RADOSOVA MUCHOVA TEREZA
DIVOKY VLADIMIR
Designated States
Priority Data 2017-157 20.03.2017 CZ
Title
(DE) 2,6-DISUBSTITUIERTE-9-CYCLOPENTYL-9H-PURINE, VERWENDUNG DAVON ALS ARZNEIMITTEL UND PHARMAZEUTISCHE ZUSAMMENSETZUNGEN
(EN) 2,6-DISUBSTITUTED-9-CYCLOPENTYL-9H-PURINES, USE THEREOF AS MEDICAMENTS, AND PHARMACEUTICAL COMPOSITIONS
(FR) 9-CYCLOPENTYL-9H-PURINES À DISUBSTITUTION EN POSITION 2 ET 6, LEUR UTILISATION EN TANT QUE MÉDICAMENTS, ET COMPOSITIONS PHARMACEUTIQUES
Abstract
(EN) The present invention relates to novel 2,6-disubstituted-9-cyclopentyl-9H-purines of general formula I, capable of inhibiting the activity of kinases such as FLT3, CDKs and PDGFRs in cancer and other related proliferative diseases. The invention further includes pharmaceutical compositions containing the 2,6-disubstituted-9-cyclopentyl-9H-purines. Compounds of the present invention can be used as active ingredients of a pharmaceutical compositions for treating acute myeloid leukemia (AML).
(FR) La présente invention concerne de nouvelles 9-cyclopentyl-9H-purines à disubstitution en position 2 et 6, de formule générale I, capables d'inhiber l'activité de kinases telles que FLT3, CDK et PDGFR dans le cancer et d'autres maladies prolifératives apparentées. L'invention concerne en outre des compositions pharmaceutiques contenant les 9-cyclopentyl-9H-purines à disubstitution en position 2 et 6. Les composés de la présente invention peuvent être utilisés en tant que principes actifs d'une compositions pharmaceutique pour le traitement de la leucémie myéloïde aiguë (AML).
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