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1. (WO2010128659) DIAMINO HETEROCYCLIC CARBOXAMIDE COMPOUND
Latest bibliographic data on file with the International Bureau   

Pub. No.: WO/2010/128659 International Application No.: PCT/JP2010/057751
Publication Date: 11.11.2010 International Filing Date: 06.05.2010
IPC:
C07D 239/48 (2006.01) ,A61K 31/4965 (2006.01) ,A61K 31/497 (2006.01) ,A61K 31/505 (2006.01) ,A61K 31/506 (2006.01) ,A61K 31/5377 (2006.01) ,A61K 31/541 (2006.01) ,A61K 31/55 (2006.01) ,A61P 35/00 (2006.01) ,A61P 43/00 (2006.01) ,C07D 241/26 (2006.01) ,C07D 401/12 (2006.01) ,C07D 401/14 (2006.01) ,C07D 403/12 (2006.01) ,C07D 405/12 (2006.01) ,C07D 405/14 (2006.01) ,C07D 409/12 (2006.01) ,C07D 413/12 (2006.01) ,C07D 417/12 (2006.01) ,C07D 471/08 (2006.01) ,C07D 491/113 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
239
Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
02
not condensed with other rings
24
having three or more double bonds between ring members or between ring members and non-ring members
28
with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
46
Two or more oxygen, sulfur or nitrogen atoms
48
Two 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
4965
Non-condensed pyrazines
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
4965
Non-condensed pyrazines
497
containing further heterocyclic rings
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
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
506
not condensed and containing further heterocyclic rings
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
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
54
having six-membered rings with at least one nitrogen and at least one sulfur as the ring hetero atoms, e.g. sulthiame
541
Non-condensed thiazines containing further heterocyclic rings
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
55
having seven-membered rings, e.g. azelastine, pentylenetetrazole
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
43
Drugs for specific purposes, not provided for in groups A61P1/-A61P41/108
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
241
Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
02
not condensed with other rings
10
having three double bonds between ring members or between ring members and non-ring members
14
with 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
24
Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
26
with nitrogen atoms directly attached to ring carbon atoms
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
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
14
containing three or more hetero rings
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
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
14
containing three or more hetero rings
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
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
413
Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
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
417
Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/196
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
471
Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/-C07D463/251
02
in which the condensed system contains two hetero rings
08
Bridged systems
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
491
Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/-C07D459/290
02
in which the condensed system contains two hetero rings
10
Spiro-condensed systems
113
with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring
Applicants:
島田 逸郎 SHIMADA, Itsuro [JP/JP]; JP (UsOnly)
黒澤 一雄 KUROSAWA, Kazuo [JP/JP]; JP (UsOnly)
松矢 高広 MATSUYA, Takahiro [JP/JP]; JP (UsOnly)
飯久保 一彦 IIKUBO, Kazuhiko [JP/JP]; JP (UsOnly)
近藤 裕 KONDOH, Yutaka [JP/JP]; JP (UsOnly)
神川 晃雄 KAMIKAWA, Akio [JP/JP]; JP (UsOnly)
冨山 泰 TOMIYAMA, Hiroshi [JP/JP]; JP (UsOnly)
岩井 辰憲 IWAI, Yoshinori [JP/JP]; JP (UsOnly)
アステラス製薬株式会社 ASTELLAS PHARMA INC. [JP/JP]; 東京都中央区日本橋本町二丁目3番11号 3-11, Nihonbashi-Honcho 2-chome, Chuo-ku, Tokyo 1038411, JP (AllExceptUS)
壽製薬株式会社 KOTOBUKI PHARMACEUTICAL CO., LTD. [JP/JP]; 長野県埴科郡坂城町大字坂城6351番地 6351, Oaza-Sakaki, Sakaki-machi, Hanishina-gun, Nagano 3890697, JP (AllExceptUS)
Inventors:
島田 逸郎 SHIMADA, Itsuro; JP
黒澤 一雄 KUROSAWA, Kazuo; JP
松矢 高広 MATSUYA, Takahiro; JP
飯久保 一彦 IIKUBO, Kazuhiko; JP
近藤 裕 KONDOH, Yutaka; JP
神川 晃雄 KAMIKAWA, Akio; JP
冨山 泰 TOMIYAMA, Hiroshi; JP
岩井 辰憲 IWAI, Yoshinori; JP
Agent:
小野 新次郎 ONO, Shinjiro; 東京都千代田区大手町二丁目2番1号 新大手町ビル206区 ユアサハラ法律特許事務所 YUASA AND HARA, Section 206, New Ohtemachi Bldg., 2-1, Ohtemachi 2-chome, Chiyoda-ku, Tokyo 1000004, JP
Priority Data:
2009-11393608.05.2009JP
Title (EN) DIAMINO HETEROCYCLIC CARBOXAMIDE COMPOUND
(FR) COMPOSÉ DE CARBOXAMIDE HÉTÉROCYCLIQUE DIAMINO
(JA) ジアミノへテロ環カルボキサミド化合物
Abstract:
(EN) Disclosed are a compound represented by formula (I) or a salt thereof; a kinase inhibitor for EML4-ALK fusion protein containing the compound; and use of the compound for the treatment of cancers. (In formula (I), -X- represents a group represented by formula (II) or formula (III); A represents –H, a halogen atom, a lower alkyl group, a cycloalkyl group or a lower alkenyl group; R1 represents a substituted phenyl group, a (substituted) heterocyclic group or a (substituted) bicyclic fused ring; R2 represents a (substituted) cycloalkyl group, a (substituted) non-aromatic heterocyclic group, a (substituted) phenyl group, a (substituted) pyridyl group or a (substituted) lower alkyl group; and R3 represents –H or a lower alkyl group; or alternatively R2 and R3 may combine together to form a cyclic amino group.)
(FR) La présente invention a pour objet un composé représenté par la formule (I) ou un sel de celui-ci ; un inhibiteur de kinase pour la protéine de fusion EML4-ALK contenant le composé ; et l'utilisation du composé pour le traitement des cancers. (Dans la formule (I), -X- représente un groupe représenté par la formule (II) ou la formule (III) ; A représente –H, un atome d'halogène, un groupe alkyle inférieur, un groupe cycloalkyle ou un groupe alcényle inférieur ; R1 représente un groupe phényle substitué, un groupe hétérocyclique (substitué) ou un cycle condensé bicyclique (substitué) ; R2 représente un groupe cycloalkyle (substitué), un groupe hétérocyclique non aromatique (substitué), un groupe phényle (substitué), un groupe pyridyle (substitué) ou un groupe alkyle inférieur (substitué) ; et R3 représente –H ou un groupe alkyle inférieur ; ou à titre d'alternative R2 et R3 peuvent se combiner ensemble pour former un groupe amino cyclique).
(JA) 式(I)の化合物又はその塩(式中の記号は以下の意味を表す。 -X-:式(II)又は式(III)の基、A:-H、ハロゲン、低級アルキル、シクロアルキル又は低級アルケニル、R:置換フェニル、(置換)ヘテロ環又は(置換)二環式縮合環、R:(置換)シクロアルキル、(置換)非芳香族ヘテロ環又は(置換)フェニル、(置換)ピリジル又は(置換)低級アルキル、R:-H又は低級アルキル、又は、RとRは一体となって環状アミノ基を形成してもよい。)、該化合物を含有するEML4-ALK 融合タンパクのキナーゼ阻害剤、並びに、該化合物の癌治療への用途。
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African Regional Intellectual Property Organization (ARIPO) (BW, GH, GM, KE, LR, LS, MW, MZ, NA, SD, SL, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Office (AM, AZ, BY, KG, KZ, MD, 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, SE, SI, SK, SM, TR)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, ML, MR, NE, SN, TD, TG)
Publication Language: Japanese (JA)
Filing Language: Japanese (JA)