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1. (WO2018049836) NEW CRYSTALLINE FORM OF PIMAVANSERIN TARTRATE, PREPARATION METHOD THEREFOR, AND USE
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Pub. No.: WO/2018/049836 International Application No.: PCT/CN2017/084983
Publication Date: 22.03.2018 International Filing Date: 19.05.2017
IPC:
C07D 211/58 (2006.01) ,C07C 51/43 (2006.01) ,C07C 59/255 (2006.01) ,A61K 31/4468 (2006.01) ,A61P 25/16 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
211
Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
04
with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
06
having no double bonds between ring members or between ring members and non-ring members
36
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
56
Nitrogen atoms
58
attached in position 4
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
51
Preparation of carboxylic acids or their salts, halides, or anhydrides
42
Separation; Purification; Stabilisation; Use of additives
43
by change of the physical state, e.g. crystallisation
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
59
Compounds having carboxyl groups bound to acyclic carbon atoms and containing any of the groups OH, O-metal, -CHO, keto, ether, groups, groups, or groups
235
Saturated compounds having more than one carboxyl group
245
containing hydroxy or O-metal groups
255
Tartaric acid
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
4468
having a nitrogen atom directly attached in position 4, e.g. clebopride, fentanyl
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
14
for treating abnormal movements, e.g. chorea, dyskinesia
16
Anti-Parkinson drugs
Applicants:
上海诚妙医药科技有限公司 SHANGHAI BEGREAT PHARMATECH [CN/CN]; 中国上海市 浦东新区南汇新城镇环湖西二路888号孟晓明 MENG Xiaoming, Nanhui New Town 888, Zhenhuanxier Road, Pudong New Area Shanghai 200120, CN
Inventors:
孟晓明 MENG, Xiaoming; CN
Priority Data:
201610347779.319.05.2016CN
Title (EN) NEW CRYSTALLINE FORM OF PIMAVANSERIN TARTRATE, PREPARATION METHOD THEREFOR, AND USE
(FR) NOUVELLE FORME CRISTALLINE DE TARTRATE DE PIMAVANSÉRINE, SON PROCÉDÉ DE PRÉPARATION ET SON UTILISATION
(ZH) 匹莫范色林酒石酸盐的新晶型及其制备方法和用途
Abstract:
(EN) A polymorph III of N-(4-fluorobenzyl)-N-(1-methylpiperidin-4-yl)-N'-[4-(2-methylpropoxy)phenylmethyl]urea tartrate, a preparation method therefor, and a medicinal use. Compared to the existing crystalline forms, the new crystalline form has clear advantages with respect to solubility, stability and the preparation process.
(FR) L'invention concerne un polymorphe III de tartrate de N-(4-fluorobenzyl)-N-(1-méthylpipéridin-4-yl)-N'-[4-(2-méthylpropoxy)phénylméthyl]urée, son procédé de préparation et une utilisation médicinale. Par rapport aux formes cristallines existantes, la nouvelle forme cristalline présente des avantages évidents par rapport à la solubilité, à la stabilité et au processus de préparation.
(ZH) N-(4-氟苄基)-N-(1-甲基哌啶-4-基)-N'-[4-(2-甲基丙氧基)苯基甲基]脲酒石酸盐的多晶型III及其制备方法和药用用途。与现有晶型相比,新晶型在溶解度、稳定性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 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: Chinese (ZH)
Filing Language: Chinese (ZH)