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1. WO2013184119 - DIHYDRONAPHTHYRIDINES AND RELATED COMPOUNDS USEFUL AS KINASE INHIBITORS FOR THE TREATMENT OF PROLIFERATIVE DISEASES

Publication Number WO/2013/184119
Publication Date 12.12.2013
International Application No. PCT/US2012/041378
International Filing Date 07.06.2012
IPC
A61K 31/4375 2006.01
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
4353ortho- or peri-condensed with heterocyclic ring systems
4375the heterocyclic ring system containing a six-membered ring having nitrogen as a ring hetero atom, e.g. quinolizines, naphthyridines, berberine, vincamine
CPC
A61K 31/4375
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
4353ortho- or peri-condensed with heterocyclic ring systems
4375the heterocyclic ring system containing a six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
A61P 1/04
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
1Drugs for disorders of the alimentary tract or the digestive system
04for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
A61P 15/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
15Drugs for genital or sexual disorders
A61P 17/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
17Drugs for dermatological disorders
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
Applicants
  • FLYNN, Daniel L. [US]/[US]
  • KAUFMAN, Michael D. [US]/[US]
  • PETILLO, Peter, A. [US]/[US]
Inventors
  • FLYNN, Daniel L.
  • KAUFMAN, Michael D.
  • PETILLO, Peter, A.
Agents
  • TUSCAN, Michael S.
Priority Data
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) DIHYDRONAPHTHYRIDINES AND RELATED COMPOUNDS USEFUL AS KINASE INHIBITORS FOR THE TREATMENT OF PROLIFERATIVE DISEASES
(FR) DIHYDRONAPHTYRIDINES ET COMPOSÉS APPARENTÉS UTILES COMME INHIBITEURS DE KINASES POUR LE TRAITEMENT DE MALADIES PROLIFÉRATIVES
Abstract
(EN)
The invention relates to dihydronaphthyridines and related compounds; compositions comprising an effective amount of a dihydronaphthyridine or a related compound; and methods for treating or preventing proliferative diseases comprising the administration of an effective amount of a dihydronaphthyridine or a related compound. The present invention discloses the unexpected utility of compounds that inhibit cKIT kinase across a broad range of c-KIT mutations, including complex occurrences of primary mutations (KIT exon 9 or 11) and secondary KIT mutations (exons 13, 14, 17 and 18) that may arise in individual, refractory GIST patients. Also unexpected is the utility of compounds of the present invention to inhibit the problematic exon 17 D816V c-KIT mutation, for which there is currently no effective therapy.
(FR)
L'invention concerne des dihydronaphtyridines et des composés apparentés; des compositions comprenant une quantité efficace d'une dihydronaphtyridine ou d'un composé apparenté; et des procédés de traitement et de prévention de maladies prolifératives comprenant l'administration d'une quantité efficace d'une dihydronaphthyridine ou d'un composé apparenté. La présente invention décrit l'utilité inattendue de composés qui inhibent la kinase cKIT sur une large gamme de mutations de c-KIT, notamment des occurrences complexes de mutations primaires (exon 9 ou 11 de KIT) et des mutations secondaires de KIT (exons 13, 14, 17 et 18) susceptibles d'apparaître chez des patients atteints de GIST réfractaires individuels. L'utilité des composés de la présente invention pour inhiber la mutation problématique exon 17 D816V de c-KIT, pour laquelle il n'existe actuellement aucune thérapie efficace, est également inattendue.
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