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1. WO2021060949 - CO-CRYSTALLINE EFINACONAZOLE, AND METHOD FOR PRODUCING SAME

Publication Number WO/2021/060949
Publication Date 01.04.2021
International Application No. PCT/KR2020/013163
International Filing Date 25.09.2020
IPC
A61K 9/14 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9Medicinal preparations characterised by special physical form
14Particulate form, e.g. powders
A61K 31/454 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
44Non-condensed pyridines; Hydrogenated derivatives thereof
445Non-condensed piperidines, e.g. piperocaine
4523containing further heterocyclic ring systems
454containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
A61P 17/00 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
17Drugs for dermatological disorders
A61P 31/10 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
31Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
10Antimycotics
C07D 401/06 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
401Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
02containing two hetero rings
06linked by a carbon chain containing only aliphatic carbon atoms
Applicants
  • 대봉엘에스 주식회사 DAEBONG LS, LTD [KR]/[KR]
Inventors
  • 박은주 PARK, Eun Ju
  • 지현 JI, Hyun
  • 김은미 KIM, Eun Mi
  • 박진오 PARK, Jin Oh
Agents
  • 고봉진 KOH, Bong Jin
Priority Data
10-2019-011864626.09.2019KR
Publication Language Korean (KO)
Filing Language Korean (KO)
Designated States
Title
(EN) CO-CRYSTALLINE EFINACONAZOLE, AND METHOD FOR PRODUCING SAME
(FR) ÉFINACONAZOLE CO-CRISTALLIN, ET SON PROCÉDÉ DE PRODUCTION
(KO) 공결정형 에피나코나졸, 및 이의 제조방법
Abstract
(EN)
The present invention relates to a co-crystalline efinaconazole, and a method for producing same, wherein an efinaconazole and a pharmaceutically acceptable co-former are formed as a co-crystal. An efinaconazole co-crystallized product according to the present invention satisfies all of the requirements of an active ingredient of a pharmaceutical composition, while exhibiting high stability against heat and other components, and thus can be effectively used when formulating pharmaceuticals. In addition, the manufacturing process is simple and easy, thus making commercial mass production possible.
(FR)
La présente invention concerne un éfinaconazole co-cristallin et son procédé de production, un éfinaconazole et un co-agent de formation pharmaceutiquement acceptable étant formés sous forme de co-cristal. Un produit co-cristallisé d'éfinaconazole selon la présente invention satisfait toutes les exigences d'un principe actif d'une composition pharmaceutique, tout en présentant une stabilité élevée contre la chaleur et d'autres constituants, et peut donc être efficacement utilisé lors de la formulation de produits pharmaceutiques. De plus, le processus de fabrication est simple et facile, ce qui rend donc possible la production commerciale de masse.
(KO)
본 발명은 공결정형 에피나코나졸, 및 이의 제조방법에 관한 것으로서, 에피나코나졸 및 약제학적으로 허용 가능한 공형성체가 공결정상으로 이루어진 것을 특징으로 한다. 본 발명의 에피나코나졸 공결정화물은, 약제조성물의 활성성분으로서 요구되는 사항을 모두 만족하면서도, 열과 다른 조성 성분에 높은 안정성을 나타내어, 의약품 제제 시에 유용하게 사용될 수 있다. 또한, 제조공정이 간편하고 쉬워서 상업적인 대량생산이 가능하다.
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