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1. (WO2019065954) OPTICALLY ACTIVE PYRROLIDINE COMPOUND AND METHOD FOR PRODUCING SAME
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Pub. No.: WO/2019/065954 International Application No.: PCT/JP2018/036225
Publication Date: 04.04.2019 International Filing Date: 28.09.2018
IPC:
C07D 401/14 (2006.01) ,A61K 31/454 (2006.01) ,A61P 43/00 (2006.01) ,C07D 207/16 (2006.01) ,C07D 263/26 (2006.01) ,C07D 413/06 (2006.01) ,C07B 61/00 (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
435
having six-membered rings with one nitrogen as the only ring hetero atom
44
Non-condensed pyridines; Hydrogenated derivatives thereof
445
Non-condensed piperidines, e.g. piperocaine
4523
containing further heterocyclic ring systems
454
containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
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
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
04
having no double bonds between ring members or between ring members and non-ring members
10
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
16
Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
263
Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
02
not condensed with other rings
08
having one double bond between ring members or between a ring member and a non-ring member
16
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
18
Oxygen atoms
20
attached in position 2
26
with hetero atoms or acyl radicals directly attached to the ring nitrogen atom
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
413
Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
02
containing two hetero rings
06
linked by a carbon chain containing only aliphatic carbon atoms
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
B
GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
61
Other general methods
Applicants:
田辺三菱製薬株式会社 MITSUBISHI TANABE PHARMA CORPORATION [JP/JP]; 大阪府大阪市中央区道修町三丁目2番10号 3-2-10, Dosho-machi, Chuo-ku, Osaka-shi, Osaka 5418505, JP
Inventors:
鶴本 穣治 TSURUMOTO, Joji; JP
諸熊 賢治 MOROKUMA, Kenji; JP
Agent:
山尾 憲人 YAMAO, Norihito; JP
森本 靖 MORIMOTO, Yasushi; JP
Priority Data:
2017-19033129.09.2017JP
Title (EN) OPTICALLY ACTIVE PYRROLIDINE COMPOUND AND METHOD FOR PRODUCING SAME
(FR) COMPOSÉ DE PYRROLIDINE OPTIQUEMENT ACTIF ET PROCÉDÉ DE PRODUCTION DE CELUI-CI
(JA) 光学活性ピロリジン化合物及びその製造方法
Abstract:
(EN) The present invention provides: a methyl 1-{2-[(3S, 4R)-1-[(3R, 4R)-1-cyclopentyl-3-fluoro-4-(4-methoxyphenyl)pyrrolidin-3-carbonyl]-4-(methoxymethyl)pyrrolidin-3-yl]-5-(trifluoromethyl)phenyl}piperidine-4-carboxylate 1/2 ethane-1,2-disulfonic acid which is represented by formula (1) and is excellent in crystallinity; a method for producing the same; a production intermediate thereof; and a production method using this compound.
(FR) La présente invention concerne : un acide méthyle 1-{2-[(3S, 4R)-1-[(3R, 4R)-1-cyclopentyl-3-fluoro-4-(4-méthoxyphényl)pyrrolidin-3-carbonyl]-4-(méthoxyméthyl)pyrrolidin-3-yl]-5-(trifluorométhyl)phényl}pipéridine-4-carboxylate 1/2 éthane-1,2-disulfonique représenté par la formule (1) et qui présente une excellente cristallinité; un procédé de production de celui-ci; un intermédiaire de production de celui-ci; et un procédé de production l'utilisant.
(JA) 本発明は、結晶性に優れた、式(1):で表される、メチル 1-{2-[(3S,4R)-1-[(3R,4R)-1-シクロペンチル-3-フルオロ-4-(4-メトキシフェニル)ピロリジン-3-カルボニル]-4-(メトキシメチル)ピロリジン-3-イル]-5-(トリフルオロメチル)フェニル}ピペリジン-4-カルボキシラート 1/2 エタン-1,2-ジスルホン酸、並びにその製造方法およびその製造中間体、並びにこの化合物を用いた製造方法を提供する。
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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, 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)