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1. (WO2019065792) CRYSTAL
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Pub. No.: WO/2019/065792 International Application No.: PCT/JP2018/035828
Publication Date: 04.04.2019 International Filing Date: 27.09.2018
IPC:
C07D 241/20 (2006.01) ,A61K 31/4965 (2006.01) ,A61P 1/04 (2006.01) ,A61P 7/02 (2006.01) ,A61P 9/00 (2006.01) ,A61P 9/08 (2006.01) ,A61P 9/10 (2006.01) ,A61P 9/12 (2006.01) ,A61P 11/00 (2006.01) ,A61P 11/06 (2006.01) ,A61P 11/14 (2006.01) ,A61P 13/12 (2006.01) ,A61P 17/02 (2006.01) ,A61P 25/00 (2006.01) ,A61P 43/00 (2006.01)
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
20
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
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
1
Drugs for disorders of the alimentary tract or the digestive system
04
for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
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
02
Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
9
Drugs for disorders of the cardiovascular system
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
9
Drugs for disorders of the cardiovascular system
08
Vasodilators for multiple indications
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
9
Drugs for disorders of the cardiovascular system
10
for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
9
Drugs for disorders of the cardiovascular system
12
Antihypertensives
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
11
Drugs for disorders of the respiratory system
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
11
Drugs for disorders of the respiratory system
06
Antiasthmatics
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
11
Drugs for disorders of the respiratory system
14
Antitussive agents
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
13
Drugs for disorders of the urinary system
12
of the kidneys
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
17
Drugs for dermatological disorders
02
for treating wounds, ulcers, burns, scars, keloids, or the like
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25
Drugs for disorders of the nervous system
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
Agent:
中村 文胤 NAKAMURA Ayatsugu; JP
Priority Data:
2017-18729628.09.2017JP
Title (EN) CRYSTAL
(FR) CRISTAUX
(JA) 結晶
Abstract:
(EN) The main purpose of the present invention is to provide a novel crystal of 2-{4-[N-(5,6-diphenylpyrazine-2-yl)-N-isopropylamino]butyloxy} acetic acid (hereinafter "compound B"). A type I crystal of compound B with which, in a powder X-ray diffraction spectrum obtained by using CuKα radiation (λ=1.54 Å), the diffraction angle (2θ) shows peaks at the diffraction angles 6.4°, 8.1°, 9.5°, 10.9°, 13.2°, 15.7°, 17.0°, 19.5°, 20.3°, 21.0°, and 22.8°. A type II crystal of compound B with which, in a powder X-ray diffraction spectrum obtained by using CuKα radiation (λ=1.54 Å), the diffraction angle (2θ) shows peaks at the diffraction angles 9.6°, 11.4°, 11.7°, 16.3°, 17.5°, 18.5°, 18.7°, 19.9°, 20.1°, 21.0°, and 24.6°.
(FR) L'invention a pour objet de fournir de nouveaux cristaux d'acide 2-{4-[N-(5,6-diphénylpyrazin-2-yl)-N- isopropyl‐amino]butyloxy} acétique (ci-après, "composé (B)"). Plus précisément, l'invention concerne des cristaux de type I du composé (B) tels que des angles de diffraction (2θ) présentent des pics aux angles de diffraction de 6,4 degrés, 8,1 degrés, 9,5 degrés, 10,9 degrés, 13,2 degrés, 15,7 degrés, 17,0 degrés, 19.5 degrés, 20,3 degrés, 21,0 degrés et 22,8 degrés, dans un spectre de diffraction des rayons X sur poudre obtenu au moyen d'un rayonnement radioactif Cu Kα(λ=1,54Å). En outre, l'invention concerne des cristaux de type II du composé (B) tels que des angles de diffraction (2θ) présentent des pics aux angles de diffraction 9,6 degrés, 11,4 degrés, 11,7 degrés, 16,3 degrés, 17,5 degrés, 18,5 degrés, 18,7 degrés, 19,9 degrés, 20,1 degrés, 21,0 degrés et 24,6 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、2-{4-[N-(5,6-ジフェニルピラジン-2-イル)-N-イソプロピルアミノ]ブチルオキシ}酢酸(以下、「化合物B」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6.4度、8.1度、9.5度、10.9度、13.2度、15.7度、17.0度、19.5度、20.3度、21.0度および22.8度の回折角にピークを示す、化合物B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9.6度、11.4度、11.7度、16.3度、17.5度、18.5度、18.7度、19.9度、20.1度、21.0度および24.6度の回折角にピークを示す、化合物B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)