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1. WO2020115213 - SOLVATE OF A SELECTIVE JAK1 INHIBITOR

Publication Number WO/2020/115213
Publication Date 11.06.2020
International Application No. PCT/EP2019/083831
International Filing Date 05.12.2019
IPC
C07D 487/14 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
12in which the condensed system contains three hetero rings
14Ortho-condensed systems
A61P 19/00 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
19Drugs for skeletal disorders
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
CPC
A61K 31/4985
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 ; or more; nitrogen atoms as the only ring heteroatoms, e.g. piperazine ; or tetrazines
4985Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
A61P 19/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
19Drugs for skeletal disorders
C07D 487/14
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
12in which the condensed system contains three hetero rings
14Ortho-condensed systems
Applicants
  • LEK PHARMACEUTICALS D.D. [SI]/[SI]
Inventors
  • GRIESSER, Ulrich
  • STEFINOVIC, Marijan
  • MÜHLEGGER, Isabella
Agents
  • KLUSCHANZOFF, Harald
  • PFENDER, Sybille
  • SCHUST, Jochen
Priority Data
18210999.107.12.2018EP
19171271.026.04.2019EP
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) SOLVATE OF A SELECTIVE JAK1 INHIBITOR
(FR) SOLVATE D'UN INHIBITEUR SÉLECTIF DE JAK1
Abstract
(EN)
The present invention relates to acetic acid solvates of upadacitinib and processes for their preparation. The invention also relates to a pharmaceutical composition comprising an upadacitinib acetic acid solvate, preferably in a predetermined and/or effective amount and at least one pharmaceutically acceptable excipient. The pharmaceutical composition of the present invention can be used as a medicament, in particular for the treatment and/or prophylaxis of rheumatoid arthritis.
(FR)
La présente invention concerne des solvates d'acide acétique d'upadacitinib et des procédés de préparation associés. L'invention concerne en outre une composition pharmaceutique comprenant le solvate d'acide acétique d'upadacitinib, de préférence dans une quantité prédéterminée et/ou efficace et au moins un excipient pharmaceutiquement acceptable. La composition pharmaceutique selon la présente invention peut être utilisée en tant que médicament, en particulier dans le traitement et/ou la prophylaxie de la polyarthrite rhumatoïde.
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