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1. (WO2017090275) 5'-POSITION DIBENZYL PHOSPHORIC ACID ESTER OF 5-AZACYTIDINE OR 2'-DEOXY BODY THEREOF
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/2017/090275 International Application No.: PCT/JP2016/072009
Publication Date: 01.06.2017 International Filing Date: 27.07.2016
IPC:
C07H 19/12 (2006.01) ,A61K 31/706 (2006.01) ,A61P 31/04 (2006.01) ,A61P 35/00 (2006.01) ,A61P 43/00 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
H
SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
19
Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro derivatives thereof
02
sharing nitrogen
04
Heterocyclic radicals containing only nitrogen as ring hetero atom
12
Triazine radicals
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
70
Carbohydrates; Sugars; Derivatives thereof
7042
Compounds having saccharide radicals and heterocyclic rings
7052
having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
706
containing six-membered rings with nitrogen as a ring hetero atom
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
31
Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
04
Antibacterial agents
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
Applicants:
大原薬品工業株式会社 OHARA PHARMACEUTICAL CO., LTD. [JP/JP]; 滋賀県甲賀市甲賀町鳥居野121番地15 121-15 Toriino, Koka-cho, Koka-shi Shiga 5203403, JP
Inventors:
酒向 孫市 SAKO Magoichi; JP
羅 雄 LUO Xiong; JP
Agent:
謝 卓峰 SHA Takuho; JP
Priority Data:
2015-23139027.11.2015JP
2016-08514421.04.2016JP
PCT/JP2016/06565927.05.2016JP
Title (EN) 5'-POSITION DIBENZYL PHOSPHORIC ACID ESTER OF 5-AZACYTIDINE OR 2'-DEOXY BODY THEREOF
(FR) ESTER D'ACIDE DIBENZYLPHOSPHORIQUE EN POSITION 5' DE LA 5-AZACYTIDINE OU 2'-DÉSOXY-5-AZACYTIDINE
(JA) 5-アザシチジン又は其の2'-デオキシ体の5'位ジベンジル燐酸エステル
Abstract:
(EN) [Problem] To provide a drug that substitutes for injections (5-azacytidine or 2'-deoxy-5-azacytidine) that are clinically used as bone marrow tumor therapeutic drugs, said drug having high stability with respect to metabolic enzyme cytidine deaminase, being absorbed in the body even by means of oral administration, and having an effect of being integrated into an RNA and DNA biosynthesis pathway and inhibiting protein synthesis. [Solution] The abovementioned problem is solved by a novel compound represented by formula (1): (in the formula, R is a hydroxyl group or a hydrogen atom, and R1 and R2 are benzyl groups that may have a substituent group).
(FR) Le problème abordé par la présente invention est de pourvoir à un médicament qui se substitue aux injections (5-azacytidine ou 2'-désoxy-5-azacytidine) qui sont cliniquement utilisées à titre de médicaments thérapeutiques contre les tumeurs de moelle osseuse, ledit médicament étant caractérisé en ce qu'il a une stabilité élevée vis-à-vis de l'enzyme métabolique cytidine désaminase, est absorbé dans le corps même par une administration par voie orale, et en ce qu'il a pour effet de s'intégrer à une voie de biosynthèse de l'ARN et de l'ADN et d'inhiber la synthèse des protéines. La solution selon l'invention porte sur un nouveau composé représenté par la formule (1) : (dans la formule : R est un groupe hydroxyle ou un atome d'hydrogène, et R1 et R2 sont des groupes benzyle qui peuvent porter un groupe de substitution).
(JA) 【課題】骨髄腫瘍治療薬として臨床使用されている注射剤(5-アザシチジンや2'-デオキシ-5-アザシチジン)に代わり、代謝酵素シチジンデアミナーゼに対して高い安定性を有し、且つ、経口投与でも体内に吸収され、RNA及びDNAの生合成経路に組み込まれて蛋白合成を阻害する作用を有する薬剤を提供すること。 【解決手段】 式(1):(式中、Rは水酸基又は水素原子であり、R、Rはそれぞれ置換基を有していてもよいベンジル基)で表される新規化合物が上記課題を解決した。
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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, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IR, IS, JP, KE, KG, KN, KP, KR, 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 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)
Also published as:
EP3192799MYPI 2018701906CN108290920KR1020180088664ID2018/10518