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1. (WO2018084321) NOVEL COMPOUND USEFUL FOR BOTH EGFR INHIBITION AND TUMOR THERAPY
Latest bibliographic data on file with the International Bureau    Submit observation

Pub. No.: WO/2018/084321 International Application No.: PCT/JP2017/040340
Publication Date: 11.05.2018 International Filing Date: 01.11.2017
IPC:
C07D 239/94 (2006.01) ,A61K 31/517 (2006.01) ,A61K 31/5377 (2006.01) ,A61P 35/00 (2006.01) ,A61P 35/02 (2006.01) ,A61P 43/00 (2006.01) ,C07D 401/12 (2006.01) ,C07D 403/12 (2006.01) ,C07D 405/12 (2006.01) ,C07D 409/12 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
239
Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
70
condensed with carbocyclic rings or ring systems
72
Quinazolines; Hydrogenated quinazolines
86
with hetero atoms directly attached in position 4
94
Nitrogen atoms
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
495
having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
505
Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
517
ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
535
having six-membered rings with at least one nitrogen and at least one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
5375
1,4-Oxazines, e.g. morpholine
5377
not condensed and containing further heterocyclic rings, e.g. timolol
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35
Antineoplastic agents
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35
Antineoplastic agents
02
specific for leukemia
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
43
Drugs for specific purposes, not provided for in groups A61P1/-A61P41/108
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
401
Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
02
containing two hetero rings
12
linked by a chain containing hetero atoms as chain links
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
403
Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/167
02
containing two hetero rings
12
linked by a chain containing hetero atoms as chain links
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
405
Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
02
containing two hetero rings
12
linked by a chain containing hetero atoms as chain links
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
409
Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
02
containing two hetero rings
12
linked by a chain containing hetero atoms as chain links
Applicants:
国立大学法人九州大学 KYUSHU UNIVERSITY, NATIONAL UNIVERSITY CORPORATION [JP/JP]; 福岡県福岡市東区箱崎六丁目10番1号 6-10-1, Hakozaki, Higashi-ku, Fukuoka-shi, Fukuoka 8128581, JP
Inventors:
王子田 彰夫 OJIDA, Akio; JP
小野 眞弓 ONO, Mayumi; JP
渡 公佑 WATARI, Kosuke; JP
進藤 直哉 SHINDO, Naoya; JP
渕田 大和 FUCHIDA, Hirokazu; JP
Agent:
小林 浩 KOBAYASHI, Hiroshi; 東京都中央区八重洲二丁目8番7号福岡ビル9階 阿部・井窪・片山法律事務所 ABE, IKUBO & KATAYAMA, Fukuoka Bldg. 9th Fl., 8-7, Yaesu 2-chome, Chuo-ku, Tokyo 1040028, JP
Priority Data:
2016-21552002.11.2016JP
Title (EN) NOVEL COMPOUND USEFUL FOR BOTH EGFR INHIBITION AND TUMOR THERAPY
(FR) NOUVEAU COMPOSÉ UTILE À LA FOIS POUR L'INHIBITION DE L'EGFR ET LA THÉRAPIE ANTITUMORALE
(JA) EGFR阻害及び腫瘍治療に有用な新規化合物
Abstract:
(EN) The purpose of the present invention is to develop a safe covalent drug having little fear of side effects by searching for a reactive group having lower reactivity as a substitute for a Michael acceptor and by designing a drug molecule using said reactive group. The present invention relates to, for example, a compound represented by formula (I) or a pharmacologically acceptable salt of the compound.
(FR) Le but de la présente invention est de développer un médicament covalent sûr ayant peu de risque d'effets secondaires par la recherche d'un groupe réactif ayant une basse réactivité en tant que substitut d'un accepteur de Michaël et par la conception d'une molécule de médicament à l'aide dudit groupe réactif. La présente invention concerne, par exemple, un composé représenté par la formule (I) ou un sel pharmacologiquement acceptable du composé.
(JA) 本発明は、マイケルアクセプターに代わる、より穏やかな反応性を有する反応基を探索し、これを用いて薬剤分子をデザインすることで、副作用の懸念の少ない安全なコバレントドラッグを開発することを目的とする。本発明は、例えば、下記式(I):で示される化合物、又はその薬理学的に許容し得る塩等に係るものである。
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Designated States: AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DJ, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IR, IS, JO, JP, KE, KG, KH, KN, KP, KR, KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW
African Regional Intellectual Property Organization (ARIPO) (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Office (AM, AZ, BY, KG, KZ, RU, TJ, TM)
European Patent Office (EPO) (AL, AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, TR)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, KM, ML, MR, NE, SN, TD, TG)
Publication Language: Japanese (JA)
Filing Language: Japanese (JA)