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1. (WO2018224063) SOLID FORMS OF ELAGOLIX
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Pub. No.: WO/2018/224063 International Application No.: PCT/CZ2018/050031
Publication Date: 13.12.2018 International Filing Date: 06.06.2018
IPC:
C07D 239/54 (2006.01) ,A61K 31/513 (2006.01) ,A61P 15/00 (2006.01) ,A61P 13/08 (2006.01) ,A61P 35/00 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
239
Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
02
not condensed with other rings
24
having three or more double bonds between ring members or between ring members and non-ring members
28
with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
46
Two or more oxygen, sulfur or nitrogen atoms
52
Two oxygen atoms
54
as doubly bound oxygen atoms or as unsubstituted hydroxy radicals
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
505
Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
513
having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
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
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
08
of the prostate
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35
Antineoplastic agents
Applicants:
ZENTIVA, K.S. [CZ/CZ]; U Kabelovny 130/22 10200 Praha 10 - Dolni Mecholupy, CZ
Inventors:
VLASAKOVA, Ruzena; CZ
CERNA, Igor; CZ
OBADALOVA, Iva; CZ
KREJCIK, Lukas; CZ
DAMMER, Ondrej; CZ
SVOBODOVA, Jaroslava; CZ
SEMBERA, Filip; CZ
Agent:
HARBER IP S.R.O.; Na belidle 64/3 15000 Praha 5, CZ
Priority Data:
PV 2017-33308.06.2017CZ
PV 2017-57622.09.2017CZ
PV 2018-25831.05.2018CZ
Title (EN) SOLID FORMS OF ELAGOLIX
(FR) FORMES À L'ÉTAT SOLIDE D'ÉLAGOLIX
Abstract:
(EN) The invention provides novel solid forms of elagolix and its esters of formula (I), optionally with acids or with polymers, methods of preparation and uses thereof. These solid forms are particularly suitable as intermediates of synthesis of elagolix or as components of pharmaceutical formulations useful in the treatment of e.g. endometriosis, uterine myomas, prostate hyperplasia, prostate, breast and ovarian cancers. (I) R represents an alkaline earth metal, an alkali metal, H, C1-C6 alkyl, C6-C20 aryl or C7-C24 aralkyl.
(FR) L'invention concerne de nouvelles formes solides d'élagolix et de ses esters, éventuellement avec des acides ou des polymères, leur procédé de préparation et leur utilisation. Ces formes solides sont particulièrement appropriées en tant qu'intermédiaires de synthèse d'élagolix ou en tant que composants de formulations pharmaceutiques.
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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: English (EN)
Filing Language: ???LANGUAGE_SYMBOL_CS??? (CS)