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1. WO2004080462 - c-Kit KINASE INHIBITOR

Publication Number WO/2004/080462
Publication Date 23.09.2004
International Application No. PCT/JP2004/003087
International Filing Date 10.03.2004
IPC
C07D 215/48 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
215Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
02having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
16with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
48Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
CPC
A61K 31/47
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
A61P 11/06
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
11Drugs for disorders of the respiratory system
06Antiasthmatics
A61P 3/04
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
3Drugs for disorders of the metabolism
04Anorexiants; Antiobesity agents
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
A61P 37/08
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
37Drugs for immunological or allergic disorders
08Antiallergic agents
Applicants
  • エーザイ株式会社 EISAI CO., LTD. [JP]/[JP] (AllExceptUS)
  • 山本 裕之 YAMAMOTO, Yuji [JP]/[JP] (UsOnly)
  • 渡辺 達夫 WATANABE, Tatsuo [JP]/[JP] (UsOnly)
  • 岡田 雅之 OKADA, Masayuki [JP]/[JP] (UsOnly)
  • 鶴岡 明彦 TSURUOKA, Akihiko [JP]/[JP] (UsOnly)
Inventors
  • 山本 裕之 YAMAMOTO, Yuji
  • 渡辺 達夫 WATANABE, Tatsuo
  • 岡田 雅之 OKADA, Masayuki
  • 鶴岡 明彦 TSURUOKA, Akihiko
Agents
  • 長谷川 芳樹 HASEGAWA, Yoshiki
Priority Data
2003-06282310.03.2003JP
2003-30280327.08.2003JP
Publication Language Japanese (JA)
Filing Language Japanese (JA)
Designated States
Title
(EN) c-Kit KINASE INHIBITOR
(FR) INHIBITEUR DE KINASE C-KIT
(JA) c-Kitキナーゼ阻害剤
Abstract
(EN)
It is found out that a compound represented by the following general formula I shows a potent c-Kit kinase inhibitory activity and suppresses the proliferation of cancer cells activated by c-Kit kinase both in vitro and in vivo. Thus, a novel anticancer agent showing a c-Kit kinase inhibitory activity is found out. General formula I: (I) wherein R1 represents methyl, etc.; R2 represents cyano, etc.; R3 represents hydrogen, etc.; and R4 represents hydrogen, etc.
(FR)
Selon l'invention, on a découvert qu'un composé représenté par la formule générale (I) présente une puissante activité inhibitrice de kinase c-Kit et supprime la prolifération de cellules cancéreuses activées par la kinase c-Kit à la fois in vivo et in vitro. Ainsi, on a découvert un nouvel agent anticancéreux présentant une activité inhibitrice de kinase c-Kit. Dans la formule (I), R1 représente méthyle, etc., R2 représente cyano, etc., R3 représente hydrogène, etc., et R4 représente hydrogène, etc.
(JA)
not available
Also published as
Latest bibliographic data on file with the International Bureau