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1. (WO2017128932) NOVEL POLYMORPH OF FLIBANSERIN AND PREPARATION METHOD THEREOF AND USE OF SAME
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/2017/128932 International Application No.: PCT/CN2017/000143
Publication Date: 03.08.2017 International Filing Date: 03.02.2017
IPC:
C07D 235/26 (2006.01) ,A61K 31/496 (2006.01) ,A61P 15/00 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
235
Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
02
condensed with carbocyclic rings or ring systems
04
Benzimidazoles; Hydrogenated benzimidazoles
24
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 in position 2
26
Oxygen 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
496
Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
15
Drugs for genital or sexual disorders; Contraceptives
Applicants:
孟晓明 MENG, Xiaoming [CN/CN]; CN
Inventors:
孟晓明 MENG, Xiaoming; CN
Priority Data:
201610072487.331.01.2016CN
Title (EN) NOVEL POLYMORPH OF FLIBANSERIN AND PREPARATION METHOD THEREOF AND USE OF SAME
(FR) NOUVEAU POLYMORPHE DE FLIBANSÉRINE, SON PROCÉDÉ DE PRÉPARATION ET LEUR UTILISATION
(ZH) 氟班色林的新晶型及其制备方法及其用途
Abstract:
(EN) The present invention discloses novel polymorphs I, II, and V of a [2-(4-(3-trifluoromethyl-benzyl)piperazin-1-yl)ethyl]-2,3-dihydro-1H-benzimidazol-2-one and a preparation method and pharmaceutical application thereof. The polymorph I is a trihydrate crystal, the polymorph II is an anhydrous crystal, and the polymorph V is an anhydrous crystal. When compared with an existing crystal form, the novel polymorphs provide significant advantages in terms of solubility and preparation techniques.
(FR) La présente invention concerne de nouveaux polymorphes I, II et V d'un [2-(4-(3-trifluorométhyl-benzyl)pipérazin-1-yl)éthyl]-2,3-dihydro-1H-benzimidazol-2-one et son procédé de préparation ainsi que son application pharmaceutique. Le polymorphe I est un cristal trihydraté, le polymorphe II est un cristal anhydre, et le polymorphe V est un cristal anhydre. En comparaison avec une forme cristalline existante, les nouveaux polymorphes présentent des avantages significatifs en termes de solubilité et de techniques de préparation.
(ZH) 本发明公开了[2-(4-(3-三氟甲基-苯基)哌嗪-1-基)乙基]-2,3-二氢-1H-苯并咪唑-2-酮的新多晶型I,II,V,及其制备方法和药用用途。晶型I为三水合物晶型,晶型II为无水晶型,晶型V为无水晶型,与现有晶型相比,新晶型在溶解度和制备工艺方面具有明显优势。
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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, 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 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: Chinese (ZH)
Filing Language: Chinese (ZH)
Also published as:
CN108699007