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1. (WO2019042485) SOLID FORMS OF ROXADUSTAT
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Pub. No.: WO/2019/042485 International Application No.: PCT/CZ2018/000039
Publication Date: 07.03.2019 International Filing Date: 30.08.2018
IPC:
C07D 217/26 (2006.01) ,A61P 7/06 (2006.01) ,A61K 31/472 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
217
Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
22
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 carbon atoms of the nitrogen-containing ring
26
Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
7
Drugs for disorders of the blood or the extracellular fluid
06
Antianaemics
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
47
Quinolines; Isoquinolines
472
Non-condensed isoquinolines, e.g. papaverine
Applicants:
ZENTIVA, K.S. [CZ/CZ]; U Kabelovny 130 102 37 Praha 10, CZ
Inventors:
CERNA, Igor; CZ
SEMBERA, Filip; CZ
KREJCIK, Lukas; CZ
DAMMER, Ondrej; CZ
ZAPADLO, Michal; CZ
GIAFFREDA, Stefano, Lucas; IT
MODENA, Enrico; IT
IANNI, Cristina; IT
Agent:
JIROTKOVA, Ivana; Rott, Ruzicka & Guttman Vinohradska 37 120 00 Praha 2, CZ
Priority Data:
PV 2017-50330.08.2017CZ
PV 2018-27708.06.2018CZ
Title (EN) SOLID FORMS OF ROXADUSTAT
(FR) FORMES À L'ÉTAT SOLIDE DE ROXADUSTAT
Abstract:
(EN) The solution relates to solid forms of roxadustat with the systematic name of (4-hydroxy-1-methyl-7-phenoxyisoquinoline-3-carbonyl)glycine of formula (I), methods of their preparation and use in a drug form. These solid forms of roxadustat of formula (I) are prepared by a reaction of roxadustat free acid with suitable coformers (inorganic or organic acids, bases, neutral molecules, or salts or ion pairs) in a suitable solvent or mixtures of solvents, the coformer is selected from the group consisting of meglumine, Ν,Ν'-dibenzylethylenediamine, tert-butylamine, diethylamine, dicyclohexylamine, ammonia, lithium, potassium hydroxide, calcium salt, magnesium salt, iron (III) salt, iron (II) salt, 2-naphtalenesulfonic acid, benzenesulfonic acid, p-toluenesulfonic acid, 3-ethyl-1 -methyl- 1H-imidazol-3-ium acetate and caffeine.
(FR) La présente invention concerne des formes à l'état solide de roxadustat sous le nom systématique de (4-hydroxy-1-méthyl-7-phénoxyisoquinoline-3-carbonyl)glycine de formule (I), leurs procédés de préparation et d'utilisation sous forme de médicament. Les formes à l'état solide de roxadustat de formule (I), selon l'invention sont préparées par une réaction de l'acide libre de roxadustat avec des co-formateurs appropriés (acides inorganiques ou organiques, bases, molécules neutres, ou sels ou paires d'ions) dans un solvant approprié ou des mélanges de solvants, le co-formateur est choisi dans le groupe constitué de méglumine, N,Ν'-dibenzylethylènediamine, tert-butylamine, diéthylamine, dicyclohexylamine, ammoniac, lithium, hydroxyde de potassium, sel de calcium, sel de magnésium, sel de fer (III), sel de fer (II), acide 2-naphtalènesulfonique, acide benzènesulfonique, acide p-toluènesulfonique, acétate de 3-éthyl-1-méthyl-1H-imidazol-3-ium et la caféine.
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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: English (EN)