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1. (WO2014168103) DIPYRROMETHENE CRYSTAL AND METHOD FOR MANUFACTURING SAME
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/2014/168103 International Application No.: PCT/JP2014/060055
Publication Date: 16.10.2014 International Filing Date: 07.04.2014
IPC:
C07D 207/34 (2006.01) ,A61K 31/40 (2006.01) ,A61P 43/00 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
207
Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
02
with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
30
having two double bonds between ring members or between ring members and non-ring members
34
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
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
40
having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
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:
第一三共株式会社 DAIICHI SANKYO COMPANY,LIMITED [JP/JP]; 東京都中央区日本橋本町三丁目5番1号 3-5-1,Nihonbashi Honcho,Chuo-ku, Tokyo 1038426, JP
Inventors:
渡邉 仁 WATANABE, Masashi; JP
岡地 隆弘 OKACHI, Takahiro; JP
川原 倫明 KAWAHARA, Michiaki; JP
長澤 大史 NAGASAWA, Hiroshi; JP
佐藤 仙忠 SATO, Noritada; JP
瀧田 崇 TAKITA, Takashi; JP
長谷川 玄 HASEGAWA, Gen; JP
Agent:
石橋 公樹 ISHIBASHI Koki; 東京都品川区広町一丁目2番58号 第一三共株式会社内 c/o DAIICHI SANKYO COMPANY, LIMITED, 1-2-58, Hiromachi,Shinagawa-ku Tokyo 1400005, JP
Priority Data:
2013-08187910.04.2013JP
Title (EN) DIPYRROMETHENE CRYSTAL AND METHOD FOR MANUFACTURING SAME
(FR) CRISTAL DE DIPYRROMÉTHÈNE ET SON PROCÉDÉ DE FABRICATION
(JA) ピロール誘導体の結晶及びその製造方法
Abstract:
(EN) Provided are an intermediate in the manufacture of an atropisomer of a dipyrromethene that has excellent mineralocorticoid receptor antagonism, a method for manufacturing the same and crystals thereof. A method for manufacturing an atropisomer of a dipyrromethene that includes the step of dividing the atropisomer of general formula (I) [In the formula, R1 is a methyl group or a trifluoromethyl group, R2 is a hydrogen atom or a C1-C3 alkoxy group, and n is an integer selected from 1 to 3.] characterized by using an optically active amine that has a cinchonan skeleton, and crystals of (S)-1-(2- hydroxyethyl)-4-methyl-N-[4-(methylsulfonyl)phenyl]-5-[2-( trifluoromethyl)phenyl]-1H-pyrrole-3-carboxamide.
(FR) L'invention porte sur un produit intermédiaire dans la fabrication d'un atropisomère d'un dipyrrométhène qui présente un excellent effet antagoniste sur les récepteurs des minéralocorticoïdes, un procédé pour sa fabrication ainsi que des cristaux de celui-ci. L'invention concerne également un procédé de fabrication d'un atropisomère d'un dipyrrométhène qui comprend l'étape de division de l'atropisomère de formule générale (I) [Dans la formule, R1 est un groupe méthyle ou un groupe trifluorométhyle, R2 est un atome d'hydrogène ou un groupe alcoxy en C1-C3, et n est un nombre entier sélectionné parmi 1 à 3.] caractérisé par l'utilisation d'une amine optiquement active qui possède un squelette cinchonane, et de cristaux de (S)-1-(2-hydroxyéthyl)-4-méthyl-N-[4-(méthylsulfonyl)phényl]-5-[2-(trifluorométhyl)phényl]-1H-pyrrole-3-carboxamide.
(JA)  本発明は、優れたミネラルコルチコイド受容体拮抗作用を有するピロール誘導体のアトロプ異性体の製造中間体、製造方法及びその結晶を提供する。 シンコナン骨格を有する光学活性アミンを用いることを特徴とする、下記一般式(I) [式中、R1はメチル基又はトリフルオロメチル基を示し、R2は水素原子又はC1-C3アルコキシ基を示し、nは1~3から選択される整数を示す。] のアトロプ異性体を分割する工程を含む、ピロール誘導体のアトロプ異性体の製造方法及び(S)-1-(2-ヒドロキシエチル)-4-メチル-N-[4-(メチルスルホニル)フェニル]-5-[2-(トリフルオロメチル)フェニル]-1H-ピロール-3-カルボキサミドの結晶。
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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, LT, 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, 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:
CA2908879CN105164105KR1020150139854EP2985277US20160096803IL241892
US20170057915JPWO2014168103CA2958625EP3190102CN106916092US20170233341
JP2017141274BR112015025729IN2372/MUMNP/2015ES2661125IL260782