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1. WO2014142146 - THERAPEUTIC AGENT FOR MEIBOMIAN DYSFUNCTION

Publication Number WO/2014/142146
Publication Date 18.09.2014
International Application No. PCT/JP2014/056416
International Filing Date 12.03.2014
IPC
A61K 31/453 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
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
453containing a six-membered ring with oxygen as a ring hetero atom
A61K 9/10 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9Medicinal preparations characterised by special physical form
10Dispersions; Emulsions
A61K 9/107 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9Medicinal preparations characterised by special physical form
10Dispersions; Emulsions
107Emulsions
A61P 27/02 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
27Drugs for disorders of the senses
02Ophthalmic agents
CPC
A61K 31/436
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
4353ortho- or peri-condensed with heterocyclic ring systems
436the heterocyclic ring system containing a six-membered ring having oxygen as a ring hetero atom, e.g. rapamycin
A61K 31/453
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
453containing a six-membered ring with oxygen as a ring hetero atom
A61K 31/675
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
66Phosphorus compounds
675having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
A61K 9/0048
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
0048Eye, e.g. artificial tears
A61K 9/10
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9Medicinal preparations characterised by special physical form
10Dispersions; Emulsions
A61K 9/107
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9Medicinal preparations characterised by special physical form
10Dispersions; Emulsions
107Emulsions ; ; Emulsion preconcentrates; Micelles
Applicants
  • 参天製薬株式会社 SANTEN PHARMACEUTICAL CO., LTD. [JP]/[JP]
Inventors
  • 三宅 秀樹 MIYAKE, Hideki
  • 小田 知子 ODA, Tomoko
  • 椎 大介 SHII, Daisuke
Agents
  • 特許業務法人 津国 TSUKUNI & ASSOCIATES
Priority Data
2013-05076613.03.2013JP
Publication Language Japanese (JA)
Filing Language Japanese (JA)
Designated States
Title
(EN) THERAPEUTIC AGENT FOR MEIBOMIAN DYSFUNCTION
(FR) AGENTS THÉRAPEUTIQUES POUR UN DYSFONCTIONNEMENT MEIBOMIEN
(JA) マイボーム機能不全の治療剤
Abstract
(EN)
A compound represented by general formula (1) (in general formula (1): R1 represents a hydroxy group, a dimethylphoshphinoyloxy group, or the like; and R2 and R3 represent methoxy groups or the like) or a pharmaceutically acceptable salt thereof reduces the telangiectasia score around peripheries of meibomian gland orifices, and the obstruction number of the orifices, and thus is useful as a prophylactic and/or therapeutic agent for meibomian dysfunction.
(FR)
La présente invention concerne un composé représenté par la formule générale (1) (dans la formule générale (1) : R1 représente un groupe hydroxy, un groupe diméthylphosphinoyloxy, ou similaire ; et R2 et R3 représentent des groupes méthoxy ou similaires) ou un sel pharmaceutiquement acceptable de celui-ci qui réduit le score de télangiectasie autour des périphéries des orifices des glandes de Meibomius, et le nombre d’obstructions des orifices, et est donc utile en tant qu’agent prophylactique et/ou thérapeutique pour un dysfonctionnement meibomien.
(JA)
 一般式(1):[式中、Rはヒドロキシ基、ジメチルホスフィノイルオキシ基などを示し;RはおよびRはメトキシ基などを示す]で表される化合物またはその薬学的に許容される塩は、マイボーム腺開口部周囲の毛細血管拡張スコアおよび当該開口部の閉塞数を減少させることから、マイボーム機能不全の予防および/または治療剤として有用である。
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