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1. (WO2018041946) CRYSTALLINE HYDRATE OF THE COMPOUND (2S,3R)-ISOPROPYL 2-(((2-(1,5-DIMETHYL-6-OXO-1,6-DIHYDROPYRIDIN-3-YL)-1-((TETRAHYDRO-2H-PYRAN-4-YL)METHYL)-1H-BENZO[D]IMIDAZOL-5-YL)METHYL)AMINO)-3-HYDROXYBUTANOATE EDISYLATE
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Pub. No.: WO/2018/041946 International Application No.: PCT/EP2017/071867
Publication Date: 08.03.2018 International Filing Date: 31.08.2017
IPC:
C07D 405/14 (2006.01) ,A61P 19/02 (2006.01) ,A61K 31/4427 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
405
Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
14
containing three or more hetero rings
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
19
Drugs for skeletal disorders
02
for joint disorders, e.g. arthritis, arthrosis
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
4427
containing further heterocyclic ring systems
Applicants:
GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED [GB/GB]; 980 Great West Road Brentford Middlesex TW8 9GS, GB
Inventors:
HENLEY, Nicholas Paul; GB
Agent:
FOWLER, Gavin James; GB
Priority Data:
1614939.502.09.2016GB
Title (EN) CRYSTALLINE HYDRATE OF THE COMPOUND (2S,3R)-ISOPROPYL 2-(((2-(1,5-DIMETHYL-6-OXO-1,6-DIHYDROPYRIDIN-3-YL)-1-((TETRAHYDRO-2H-PYRAN-4-YL)METHYL)-1H-BENZO[D]IMIDAZOL-5-YL)METHYL)AMINO)-3-HYDROXYBUTANOATE EDISYLATE
(FR) HYDRATE CRISTALLIN DU COMPOSÉ (2S,3R)-ISOPROPYL 2-(((2-(1,5-DIMÉTHYL-6-OXO-1,6-DIHYDROPYRIDIN-3-YL)-1-((TÉTRAHYDRO-2H-PYRAN-4-YL)MÉTHYL)-1H-BENZO[D]IMIDAZOL-5-YL)MÉTHYL)AMINO)-3-HYDROXYBUTANOATE ÉDISYLATE
Abstract:
(EN) The present invention relates to a crystalline hydrate of the compound (2S,3R)-isopropyl 2-(((2-(l,5-dimethyl-6-oxo-l,6-dihydropyridin-3-yl)-l-((tetrahydro-2H-pyran-4-yl)methyl)-1H-benzo[d]imidazol-5-yl)methyl)amino)-3-hydroxybutanoate edisylate and to its use in the treatment of various disorders for which a BET inhibitor is indicated, in particular inflammatory and autoimmune diseases, and cancers. Processes for the manufacture of this crystalline form and pharmaceutical compositions comprising the crystalline form are also disclosed and form part of the present invention.
(FR) La présente invention concerne un hydrate cristallin du composé (2S,3R)-isopropyl 2-(((2-(l,5-diméthyl-6-oxo-l,6-dihydropyridin-3-yl)-l-((tétrahydro-2H-pyran-4-yl)méthyl)-1H-benzo[d]imidazol-5-yl)méthyl)amino)-3-hydroxybutanoate édisylate et son utilisation dans le traitement de divers troubles pour lesquels un inhibiteur de BET est indiqué, en particulier des maladies inflammatoires et auto-immunes, et des cancers. Des procédés de fabrication de cette forme cristalline et des compositions pharmaceutiques comprenant la forme cristalline sont également décrits et font partie de la présente invention.
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)