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1. WO2020193459 - SOLID FORMS OF A COMPOUND OF HBV CORE PROTEIN ALLOSTERIC MODIFIER

Publication Number WO/2020/193459
Publication Date 01.10.2020
International Application No. PCT/EP2020/057937
International Filing Date 23.03.2020
IPC
C07D 487/04 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
487Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/-C07D477/183
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
A61K 31/4985 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
495having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
4985Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
A61P 31/12 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
31Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
12Antivirals
CPC
C07D 487/04
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
487Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by C07D451/00 - C07D477/00
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
Applicants
  • F. HOFFMANN-LA ROCHE AG [CH]/[CH] (AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BE, BF, BG, BH, BJ, BN, BR, BW, BY, BZ, CA, CF, CG, CH, CI, CL, CM, CN, CO, CR, CU, CY, CZ, DE, DJ, DK, DM, DO, DZ, EC, EE, EG, ES, FI, FR, GA, GB, GD, GE, GH, GM, GN, GQ, GR, GT, GW, HN, HR, HU, ID, IE, IL, IN, IR, IS, IT, JO, JP, KE, KG, KH, KM, KN, KP, KR, KW, KZ, LA, LC, LK, LR, LS, LT, LU, LV, LY, MA, MC, MD, ME, MG, MK, ML, MN, MR, MT, MW, MX, MY, MZ, NA, NE, NG, NI, NL, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, SC, SD, SE, SG, SI, SK, SL, SM, SN, ST, SV, SY, SZ, TD, TG, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, UZ, VC, VN, WS, ZA, ZM, ZW)
  • HOFFMANN-LA ROCHE INC. [US]/[US] (US)
Inventors
  • WANG, Xuemei
  • XIONG, Jing
Agents
  • HALBIG, Dirk
Priority Data
PCT/CN2019/07954325.03.2019CN
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) SOLID FORMS OF A COMPOUND OF HBV CORE PROTEIN ALLOSTERIC MODIFIER
(FR) FORMES SOLIDES D'UN COMPOSÉ DU MODIFICATEUR ALLOSTÉRIQUE DE LA PROTÉINE CAPSIDIQUE DU VHB
Abstract
(EN)
The present invention relates to novel solid forms of compound (I), 3-[(8aS)-7-[[(4S)-5-ethoxycarbonyl-4-(3-fluoro-2-methyl-phenyl)-2-thiazol-2-yl-l,4- dihydropyrimidin-6-yl]methyl]-3-oxo-5,6,8,8a-tetrahydro-lH-imidazo[l,5-a]pyrazin-2-yl]-2,2- dimethyl-propanoic acid and pharmaceutical compositions comprising solid forms thereof disclosed herein, which can be used as a HBV capsid inhibitor (or HBV Core Protein Allosteric Modifier), or for the treatment or prophylaxis of a viral disease in a patient relating to HBV infection or a disease caused by HBV infection.
(FR)
La présente invention concerne de nouvelles formes solides du composé (I), acide 3-[(8aS)-7-[[(4S)-5-éthoxycarbonyl-4-(3-fluoro-2-méthyl-phényl)-2-thiazol-2-yl-l,4- dihydropyrimidin-6-yl]méthyl]-3-oxo-5,6,8,8a-tétrahydro-lH-imidazo[l,5-a]pyrazin-2-yl]-2,2- diméthyl et des compositions pharmaceutiques comprenant des formes solides de ce composé, qui peuvent être utilisées en tant qu'inhibiteur de capside du VHB (ou modificateur allostérique de la protéine de capside du VHB), ou pour le traitement ou la prophylaxie d'une maladie virale chez un patient associée à une infection par le VHB ou une maladie provoquée par l'infection par le VHB.
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