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1. (WO2019065793) CRYSTALS
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Pub. No.: WO/2019/065793 International Application No.: PCT/JP2018/035830
Publication Date: 04.04.2019 International Filing Date: 27.09.2018
IPC:
C07D 401/14 (2006.01) ,A61K 31/497 (2006.01) ,A61P 7/00 (2006.01) ,A61P 35/02 (2006.01) ,A61P 43/00 (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
14
containing three or more hetero 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
4965
Non-condensed pyrazines
497
containing further heterocyclic rings
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
7
Drugs for disorders of the blood or the extracellular fluid
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
Applicants:
日本新薬株式会社 NIPPON SHINYAKU CO., LTD. [JP/JP]; 京都府京都市南区吉祥院西ノ庄門口町14番地 14, Kisshoin Nishinosho Monguchicho, Minami-ku, Kyoto-shi, Kyoto 6018550, JP
Inventors:
冨士原 聡夫 FUJIWARA Toshio; US
ジョアンナ ビス Joanna Bis; US
センシル クマー クサラクマリー スクマー Senthil Kumar Kusalakumari Sukumar; US
Agent:
中村 文胤 NAKAMURA Ayatsugu; JP
Priority Data:
2017-18729728.09.2017JP
Title (EN) CRYSTALS
(FR) CRISTAUX
(JA) 結晶
Abstract:
(EN) The main purpose of the present invention is to provide novel crystals of (S)-N2-[1-(4-fluorophenyl)ethyl]-4-(1-methyl-1H-pyrazol-4-yl)-N6-(pyrazin-2-yl)pyridine-2,6-diamine maleate (hereinafter "compound A"). A type I crystal of compound A, exhibiting diffraction peaks at diffraction angles (2θ) of 6.9 degrees, 9.4 degrees, 12.5 degrees, 15.1 degrees, 16.4 degrees, 18.3 degrees, 19.0 degrees, 24.9 degrees, 25.4 degrees, 27.3 degrees, and 27.7 degrees in the powder x-ray diffraction spectrum obtained using CuKα radiation (λ = 1.54 Å). A type II crystal of compound A, exhibiting diffraction peaks at diffraction angles (2θ) of 6.9 degrees, 9.2 degrees, 12.4 degrees, 14.8 degrees, 16.5 degrees, 18.1 degrees, 18.5 degrees, 19.8 degrees, 23.6 degrees, 24.9 degrees, and 27.7 degrees in the powder x-ray diffraction spectrum obtained using CuKα radiation (λ = 1.54 Å).
(FR) L'invention a pour objet de fournir de nouveaux cristaux de sel d'acide(S)-N-[1-(4-fluorophényl)éthyl-4-(1-méthyl-1H-pyrazol-4-yl)-N-(pyrazin-2-yl)pyridine-2,6-diamine maléique (ci-après, "composé (A)"). Plus précisément, l'invention concerne des cristaux de type I du composé (A) tels que des angles de diffraction (2θ) présentent des pics de diffraction aux angles de 6,9 degrés, 9,4 degrés, 12,5 degrés, 15,1 degrés, 16,4 degrés, 18,3 degrés, 19,0 degrés, 24,9 degrés, 25,4 degrés, 27,3 degrés et 27,7 degrés, dans un spectre de diffraction des rayons X sur poudre obtenu au moyen d'un rayonnement radioactif Cu Kα(λ=1,54Å). Plus précisément, l'invention concerne des cristaux de type II du composé (A) tels que des angles de diffraction (2θ) présentent des pics de diffraction aux angles de 6,9 degrés, 9,2 degrés, 12,4 degrés, 14,8 degrés, 16,5 degrés, 18,1 degrés, 18,5 degrés, 19,8 degrés, 23,6 degrés, 24,9 degrés et 27,7 degrés, dans un spectre de diffraction des rayons X sur poudre obtenu au moyen d'un rayonnement radioactif Cu Kα(λ=1,54Å).
(JA) 本発明の主目的は、(S)-N-[1-(4-フルオロフェニル)エチル]-4-(1-メチル-1H-ピラゾール-4-イル)-N-(ピラジン-2-イル)ピリジン-2,6-ジアミン マレイン酸塩(以下、「化合物A」という。)の新規な結晶を提供することにある。 Cu Kα放射線(λ=1.54Å)を用いて得られる粉末X線回折スペクトルにおいて、回折角(2θ)が6.9度、9.4度、12.5度、15.1度、16.4度、18.3度、19.0度、24.9度、25.4度、27.3度および27.7度に回折ピークを示す、化合物AのI型結晶。 Cu Kα放射線(λ=1.54Å)を用いて得られる粉末X線回折スペクトルにおいて、回折角(2θ)が6.9度、9.2度、12.4度、14.8度、16.5度、18.1度、18.5度、19.8度、23.6度、24.9度および27.7度に回折ピークを示す、化合物AのII型結晶。
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)