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1. WO2019042641 - CO-CRYSTAL OF AN ORALLY AVAILABLE HIF PROLYL HYDROXYLASE INHIBITOR

Publication Number WO/2019/042641
Publication Date 07.03.2019
International Application No. PCT/EP2018/068754
International Filing Date 11.07.2018
IPC
C07D 217/26 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
217Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
22with 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
26Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
A61K 31/47 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
435having six-membered rings with one nitrogen as the only ring hetero atom
47Quinolines; Isoquinolines
A61P 13/12 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
13Drugs for disorders of the urinary system
12of the kidneys
CPC
A61K 47/02
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
02Inorganic compounds
A61K 9/0053
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9Medicinal preparations characterised by special physical form
0012Galenical forms characterised by the site of application
0053Mouth and digestive tract, i.e. intraoral and peroral administration
A61P 13/12
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
13Drugs for disorders of the urinary system
12of the kidneys
C07B 2200/13
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
2200Indexing scheme relating to specific properties of organic compounds
13Crystalline forms, e.g. polymorphs
C07D 207/16
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
207Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
02with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
04having no double bonds between ring members or between ring members and non-ring members
10with hetero atoms or with carbon atoms having three bonds to hetero atoms, with at the most one to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
16Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
C07D 217/26
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
217Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
22with 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
26Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
Applicants
  • SANDOZ AG [CH]/[CH]
Inventors
  • LENGAUER, Hannes
  • PICHLER, Arthur
  • MARGREITER, Renate
  • GELBRICH, Thomas
Agents
  • KLUSCHANZOFF, Harald
  • ENGLMEIER, Ludwig
Priority Data
17189195.504.09.2017EP
18165661.204.04.2018EP
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) CO-CRYSTAL OF AN ORALLY AVAILABLE HIF PROLYL HYDROXYLASE INHIBITOR
(FR) CO-CRISTAL D'UN INHIBITEUR DE HIF PROLYL HYDROXYLASE DISPONIBLE PAR VOIE ORALE
Abstract
(EN)
The present invention relates to a co-crystal of roxadustat with L-proline and to a process for its preparation. Furthermore, the invention relates to a pharmaceutical composition comprising said roxadustat L-proline co-crystal, at least one pharmaceutically acceptable excipient and optionally at least one photostabilizing agent. The pharmaceutical composition of the present invention can be used as a medicament, in particular for the treatment and/or prevention of anemia in patients with end-stage renal disease (ESRD) and/or chronic kidney disease (CKD).
(FR)
La présente invention concerne un co-cristal de roxadustat avec L-proline et son procédé de préparation. L'invention concerne également une composition pharmaceutique comprenant ledit co-cristal de roxadustat L-proline, au moins un excipient pharmaceutiquement acceptable et éventuellement au moins un agent de photostabilisation. La composition pharmaceutique selon la présente invention peut être utilisée en tant que médicament, en particulier dans le traitement et/ou la prévention de l'anémie chez des patients atteints d'insuffisance rénale terminale (ESRD) et/ou de néphropathie chronique (CKD).
Latest bibliographic data on file with the International Bureau