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1. WO2018171819 - 2,6-DISUBSTITUTED-9-CYCLOPENTYL-9H-PURINES, USE THEREOF AS MEDICAMENTS, AND PHARMACEUTICAL COMPOSITIONS

Publication Number WO/2018/171819
Publication Date 27.09.2018
International Application No. PCT/CZ2018/050010
International Filing Date 19.03.2018
IPC
C07D 473/34 2006.1
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
A61P 35/00 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
A61K 31/52 2006.1
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
CPC
A61K 31/337
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
335having oxygen as the only ring hetero atom, e.g. fungichromin
337having four-membered rings, e.g. taxol
A61K 31/4745
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
435having six-membered rings with one nitrogen as the only ring hetero atom
47Quinolines; Isoquinolines
4738ortho- or peri-condensed with heterocyclic ring systems
4745condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines
A61K 31/519
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
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
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
A61K 31/704
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
70Carbohydrates; Sugars; Derivatives thereof
7028Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages
7034attached to a carbocyclic compound, e.g. phloridzin
704attached to a condensed carbocyclic ring system, e.g. sennosides, thiocolchicosides, escin, daunorubicin
Applicants
  • UNIVERZITA PALACKEHO V OLOMOUCI [CZ]/[CZ]
Inventors
  • GUCKY, Tomas
  • REZNICKOVA, Eva
  • JORDA, Radek
  • KRYSTOF, Vladimir
  • STRNAD, Miroslav
  • RADOSOVA MUCHOVA, Tereza
  • DIVOKY, Vladimir
Agents
  • HARTVICHOVA, Katerina
Priority Data
PV 2017-15720.03.2017CZ
Publication Language English (en)
Filing Language English (EN)
Designated States
Title
(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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