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1. WO2019194211 - OXAZOLE COMPOUND CRYSTAL

Publication Number WO/2019/194211
Publication Date 10.10.2019
International Application No. PCT/JP2019/014730
International Filing Date 03.04.2019
IPC
C07D 263/32 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
263Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
02not condensed with other rings
30having two or three double bonds between ring members or between ring members and non-ring members
32with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
A61K 31/421 2006.1
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
41having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
42Oxazoles
4211,3-Oxazoles, e.g. pemoline, trimethadione
A61P 17/00 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
17Drugs for dermatological disorders
CPC
A61K 31/421
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
41having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
42Oxazoles
4211,3-Oxazoles, e.g. pemoline, trimethadione
A61K 9/06
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9Medicinal preparations characterised by special physical form
06Ointments; Bases therefor; ; Other semi-solid forms, e.g. creams, sticks, gels
A61P 17/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
17Drugs for dermatological disorders
A61P 17/02
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
17Drugs for dermatological disorders
02for treating wounds, ulcers, burns, scars, keloids, or the like
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 263/32
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
263Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
02not condensed with other rings
30having two or three double bonds between ring members or between ring members and non-ring members
32with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
Applicants
  • OTSUKA PHARMACEUTICAL CO., LTD. [JP]/[JP]
Inventors
  • KANAI, Naohiko
  • YASUTOMI, Takayuki
  • HIROTA, Ryosuke
Agents
  • SAEGUSA & PARTNERS
Priority Data
2018-07271704.04.2018JP
Publication Language English (en)
Filing Language English (EN)
Designated States
Title
(EN) OXAZOLE COMPOUND CRYSTAL
(FR) CRISTAL D'UN COMPOSÉ D'OXAZOLE
Abstract
(EN) Provided is a crystal of a specific oxazole compound that has specific inhibitory activity against PDE4, and that shows excellent stability. Specifically, provided is a crystal of an oxazole compound represented by formula (5) wherein the crystal has peaks at diffraction angles 2θ(°) of 9.6±0.2, 19.1±0.2, and 21.2±0.2 in an X-ray powder diffraction pattern measured using CuKα characteristic X-rays.
(FR) L'invention concerne un cristal d'un composé d'oxazole spécifique ayant une activité inhibitrice spécifique dirigée contre PDE4, et présentant une excellente stabilité. Plus particulièrement, l'invention concerne un cristal d'un composé d'oxazole représenté par la formule (5), le cristal ayant des pics à des angles de diffraction 2θ (°) de 9,6 ± 0,2, 19,1 ± 0,2, et 21,2 ± 0,2 dans un motif de diffraction de rayon X sur poudre mesuré à l'aide de rayons X caractéristiques CuKα.
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