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1. (WO2017073065) NOVEL ANTICANCER DRUG
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/2017/073065 International Application No.: PCT/JP2016/004733
Publication Date: 04.05.2017 International Filing Date: 27.10.2016
IPC:
C07D 401/12 (2006.01) ,A61K 31/506 (2006.01) ,A61K 31/5377 (2006.01) ,A61K 31/551 (2006.01) ,A61P 35/00 (2006.01) ,A61P 43/00 (2006.01) ,C07D 401/14 (2006.01) ,C07D 405/14 (2006.01) ,C07D 409/14 (2006.01) ,C07D 417/14 (2006.01) ,C12N 5/10 (2006.01) ,C12N 9/99 (2006.01) ,C12N 15/09 (2006.01) ,G01N 33/15 (2006.01) ,G01N 33/50 (2006.01)
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
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
55
having seven-membered rings, e.g. azelastine, pentylenetetrazole
551
having two nitrogens as ring hetero atoms, e.g. clozapine, dilazep
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
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
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
14
containing three or more hetero rings
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
14
containing three or more hetero rings
C CHEMISTRY; METALLURGY
12
BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
N
MICRO-ORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICRO-ORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
5
Undifferentiated human, animal or plant cells, e.g. cell lines; Tissues; Cultivation or maintenance thereof; Culture media therefor
10
Cells modified by introduction of foreign genetic material, e.g. virus-transformed cells
C CHEMISTRY; METALLURGY
12
BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
N
MICRO-ORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICRO-ORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
9
Enzymes, e.g. ligases (6.); Proenzymes; Compositions thereof; Processes for preparing, activating, inhibiting, separating, or purifying enzymes
99
Enzyme inactivation by chemical treatment
C CHEMISTRY; METALLURGY
12
BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
N
MICRO-ORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICRO-ORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
15
Mutation or genetic engineering; DNA or RNA concerning genetic engineering, vectors, e.g. plasmids, or their isolation, preparation or purification; Use of hosts therefor
09
Recombinant DNA-technology
G PHYSICS
01
MEASURING; TESTING
N
INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
33
Investigating or analysing materials by specific methods not covered by groups G01N1/-G01N31/131
15
Medicinal preparations
G PHYSICS
01
MEASURING; TESTING
N
INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
33
Investigating or analysing materials by specific methods not covered by groups G01N1/-G01N31/131
48
Biological material, e.g. blood, urine; Haemocytometers
50
Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
Applicants:
公益財団法人静岡県産業振興財団 SHIZUOKA INDUSTRIAL FOUNDATION [JP/JP]; 静岡県静岡市葵区追手町44番地の1 44-1, Ohtemachi, Aoi-ku, Shizuoka-shi, Shizuoka 4200853, JP
国立大学法人 岡山大学 NATIONAL UNIVERSITY CORPORATION OKAYAMA UNIVERSITY [JP/JP]; 岡山県岡山市北区津島中一丁目1番1号 1-1, Tsushima-Naka 1-chome Kita-ku, Okayama-shi, Okayama 7008530, JP (JP)
国立大学法人 長崎大学 NAGASAKI UNIVERSITY [JP/JP]; 長崎県長崎市文教町1-14 1-14, Bunkyomachi, Nagasaki-shi, Nagasaki 8528521, JP
学校法人工学院大学 KOGAKUIN UNIVERSITY [JP/JP]; 東京都新宿区西新宿一丁目24番2号 1-24-2,Nishi-shinjyuku,Shinjyuku-ku Tokyo 1638677, JP
学校法人銀杏学園 GINKYO GAKUEN [JP/JP]; 熊本県熊本市北区和泉町亀の甲325番地 325, Kamenokou, Izumi-machi, Kita-ku, Kumamoto-shi, Kumamoto 8615598, JP
東京都 TOKYO METROPOLITAN GOVERNMENT [JP/JP]; 東京都新宿区西新宿二丁目8番1号 8-1, Nishi-Shinjuku 2-chome, Shinjuku-ku, Tokyo 1638001, JP
学校法人幾徳学園 SCHOOL JUDICIAL PERSON IKUTOKUGAKUEN [JP/JP]; 神奈川県厚木市下荻野1030 1030 Shimo-ogino, Atsugi-shi, Kanagawa 2430292, JP
国立大学法人 熊本大学 NATIONAL UNIVERSITY CORPORATION KUMAMOTO UNIVERSITY [JP/JP]; 熊本県熊本市中央区黒髪二丁目39番1号 2-39-1, Kurokami, Chuo-ku, Kumamoto-shi, Kumamoto 8608555, JP (JP)
静岡県公立大学法人 SHIZUOKA PREFECTURAL UNIVERSITY CORPORATION [JP/JP]; 静岡県静岡市駿河区谷田52番1号 52-1 Yada, Suruga-ku, Shizuoka-shi, Shizuoka 4228526, JP
Inventors:
益谷 美都子 MASUTANI, Mitsuko; JP
佐久間 浩彰 SAKUMA, Hiroaki; JP
佐々木 由香 SASAKI, Yuka; JP
小泉 史明 KOIZUMI, Fumiaki; JP
小寺 康夫 KODERA, Yasuo; JP
佐々木 貴之 SASAKI, Takayuki; JP
下山 達 SHIMOYAMA, Tatsu; JP
井上 謙吾 INOUE, Kengo; JP
松野 研司 MATSUNO, Kenji; JP
大川原 正 OKAWARA, Tadashi; JP
イスラム ラフィクル ISLAM, Rafiqul; JP
高村 岳樹 TAKAMURA, Takeji; JP
入江 徹美 IRIE, Tetsumi; JP
石川 吉伸 ISHIKAWA, Yoshinobu; JP
Agent:
廣田 雅紀 HIROTA, Masanori; JP
Priority Data:
2015-21157528.10.2015JP
Title (EN) NOVEL ANTICANCER DRUG
(FR) NOUVEAU MÉDICAMENT ANTICANCÉREUX
(JA) 新規抗がん薬
Abstract:
(EN) Provided is a polyaromatic compound or a pharmacologically acceptable salt thereof, said polyaromatic compound being expressed by formula (I) (therein, A is a biaryl to which a substituted or unsubstituted monocyclic aromatic ring has been bonded, B is a nitrogen-containing monocyclic aromatic ring, C is substituted or unsubstituted benzene, D is substituted or unsubstituted pyrimidine, X is a carbonyl group, Z is NH, and R1 is one substance selected from the group consisting of hydrogen, halogens, substituted or unsubstituted linear or branching C1-6 alkyl groups, substituted or unsubstituted linear or branching C2-6 alkenyl groups, substituted or unsubstituted linear or branching C2-6 alkynyl groups, substituted or unsubstituted C3-6 cycloalkyl groups, organic oxy groups, substituted or unsubstituted aryl groups, substituted or unsubstituted heteroaryl groups, substituted or unsubstituted heterocycloalkyl groups, substituted or unsubstituted aralkyl groups, and substituted or unsubstituted heteroarylalkyl groups). By using the compound of formula (I), the present invention also provides a poly (ADP-ribose) glycohydrolase (PARG) inhibitor, a poly (ADP-ribose) (PAR) accumulation promoter, a cell proliferation inhibitor, a proliferative disease therapeutic agent such as an anticancer agent or similar, an effect enhancer for an anticancer agent, a radiation sensitizing action agent, knockdown cells for use in screening for PARG inhibitors, and a method for determining the efficacy of cancer therapy in a biological sample taken from a subject to whom a PARG inhibitor has been prescribed.
(FR) L'invention concerne un composé polyaromatique ou un sel pharmacologiquement acceptable de celui-ci, ledit composé polyaromatique étant exprimé par la formule (I) (dans laquelle, A représente un biaryle auquel est lié un cycle aromatique monocyclique substitué ou non substitué, B représente un cycle aromatique monocyclique contenant de l'azote, C représente un benzène substitué ou non substitué, D représente une pyrimidine substituée ou non substituée, X représente un groupe carbonyle, Z représente NH, et R1 représente une substance choisie dans le groupe constitué par l'hydrogène, des halogènes, des groupes alkyle en C1-6 ramifiés ou linéaires substitués ou non substitués, des groupes alcényle en C2-6 ramifiés ou linéaires substitués ou non substitués, des groupes alkynyle en C2-6 ramifiés ou linéaires substitués ou non substitués, des groupes cycloalkyle en C3-6 substitués ou non substitués, des groupes oxy organiques, des groupes aryle substitués ou non substitués, des groupes hétéroaryle substitués ou non substitués, des groupes hétérocycloalkyle substitués ou non substitués, des groupes aralkyle substitués ou non substitués et des groupes hétéroarylalkyle substitués ou non substitués. À l'aide du composé de formule (I), l'invention concerne également un inhibiteur de la poly(ADP-ribose) glycohydrolase (PARG), un promoteur d'accumulation de poly(ADP-ribose) (PAR), un inhibiteur de la prolifération cellulaire, un agent thérapeutique contre les maladies prolifératives tel qu'un agent anticancéreux ou similaire, un amplificateur de l'effet d'un agent anticancéreux, un agent à action de sensibilisation au rayonnement, des cellules d'inactivation destinées à être utilisées dans le criblage d'inhibiteurs de la PARG, et une méthode servant à déterminer l'efficacité du traitement du cancer dans un échantillon biologique prélevé sur un sujet auquel un inhibiteur de la PARG a été prescrit.
(JA) 以下の式(I)[式中、Aは、置換又は非置換の単環性芳香族環が連結したビアリールであり、Bは、単環性の含窒素芳香族環であり、Cは、置換若しくは非置換のベンゼンであり、Dは、置換若しくは非置換のピリミジンであり、Xは、カルボニル基であり、Zは、NHであり、Rは、水素、ハロゲン、置換若しくは非置換の直鎖又は分枝の炭素数1~6のアルキル基、置換若しくは非置換の直鎖又は分枝の炭素数2~6のアルケニル基、置換若しくは非置換の直鎖又は分枝の炭素数2~6のアルキニル基、置換又は非置換の炭素数3~6のシクロアルキル基、有機オキシ基、置換又は非置換のアリール基、置換又は非置換のヘテロアリール基、置換又は非置換のヘテロシクロアルキル基、置換又は非置換のアラルキル基、及び、置換又は非置換のヘテロアリールアルキル基から選ばれるいずれか一つである。]で表わされるポリ芳香族化合物若しくはその薬理学的に許容される塩を調製する。 式(I)の化合物を利用することにより、ポリ(ADP-リボース)グリコヒドロラーゼ(PARG)阻害剤、ポリ(ADP-リボース)(PAR)集積促進剤、細胞増殖阻害剤、抗がん剤等の増殖性疾患治療剤、抗がん剤の効果増強剤、放射線増感作用剤、PARG阻害剤のスクリーニングに用いるためのノックダウンした細胞、及びPARG阻害剤を投与した対象から採取された生物学的試料における抗がん治療の有効性の判定方法が提供される。
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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 Organization (AM, AZ, BY, KG, KZ, RU, TJ, TM)
European Patent Office (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)