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1. WO2016027754 - ACID-ADDITION SALT OF Trk-INHIBITING COMPOUND

Publication Number WO/2016/027754
Publication Date 25.02.2016
International Application No. PCT/JP2015/072990
International Filing Date 17.08.2015
IPC
C07D 401/12 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
12linked by a chain containing hetero atoms as chain links
A61K 31/506 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
505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
506not condensed and containing further heterocyclic rings
A61K 45/00 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
45Medicinal preparations containing active ingredients not provided for in groups A61K31/-A61K41/132
A61P 1/04 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
1Drugs for disorders of the alimentary tract or the digestive system
04for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
A61P 11/02 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
11Drugs for disorders of the respiratory system
02Nasal agents, e.g. decongestants
A61P 13/02 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
02of urine or of the urinary tract, e.g. urine acidifiers
CPC
A61K 31/506
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
505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
506not condensed and containing further heterocyclic rings
A61K 45/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
45Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
A61K 45/06
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
45Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
A61P 1/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
1Drugs for disorders of the alimentary tract or the digestive system
A61P 1/04
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
1Drugs for disorders of the alimentary tract or the digestive system
04for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
A61P 11/02
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
11Drugs for disorders of the respiratory system
02Nasal agents, e.g. decongestants
Applicants
  • 小野薬品工業株式会社 ONO PHARMACEUTICAL CO., LTD. [JP]/[JP]
Inventors
  • 竹内 淳 TAKEUCHI, Jun
  • 板谷 敏 ITADANI, Satoshi
  • 井倉 誠泰 IKURA, Masahiro
  • 東野 勝人 HIGASHINO, Masato
  • 木嶋 秀臣 KIJIMA, Hideomi
  • 小野 静香 ONO, Shizuka
  • 康廣 徹也 YASUHIRO, Tetsuya
  • 長浦 健 NAGAURA, Takeshi
Agents
  • 特許業務法人三枝国際特許事務所 SAEGUSA & PARTNERS
Priority Data
2014-16562218.08.2014JP
Publication Language Japanese (JA)
Filing Language Japanese (JA)
Designated States
Title
(EN) ACID-ADDITION SALT OF Trk-INHIBITING COMPOUND
(FR) SEL D'ADDITION ACIDE DE COMPOSÉ INHIBITEUR DE Trk
(JA) Trk阻害化合物の酸付加塩
Abstract
(EN)
In order to provide an agent for the prevention and/or treatment of Trk-related diseases, the present invention provides a compound that has selective inhibitory activity on Trk, persistently suppresses NGF vascular hyperpermeability, has no drug interactions, and also has exceptional absorbability and solubility in free bases. The compound of the present invention has selective inhibitory activity on Trk, persistently suppresses NGF vascular hyperpermeability, has no drug interactions, and has exceptional absorbability and solubility in free bases, and is therefore useful as a drug for the prevention and/or treatment of Trk-related diseases.
(FR)
L'invention vise à fournir un agent pour la prévention et/ou le traitement de maladies associées à Trk. La solution proposée par la présente invention consiste en un composé qui possède une activité inhibitrice sélective envers Trk, inhibe de manière persistante l'hyperperméabilité vasculaire du NGF, ne présente pas d'interactions médicamenteuses, et présente en outre d'exceptionnelles caractéristiques de solubilité et absorbabilité dans les bases libres. Le composé de la présente invention présente une activité inhibitrice sélective envers Trk, inhibe de manière persistante l'hyperperméabilité vasculaire du NGF, ne présente pas d'interactions médicamenteuses et présente d'exceptionnelles caractéristiques de solubilité et absorbabilité dans les bases libres. Il est par conséquent utile en tant que médicament pour la prévention et/ou le traitement de maladies associées à Trk.
(JA)
Trk関連疾患の予防および/または治療剤を提供するため、Trk選択的な阻害活性を有し、NGF血管透過性亢進を持続的に抑制し、薬物相互作用を有さないことに加え、さらに遊離塩基に対して溶解性、吸収性に優れた化合物を提供すること。 本発明化合物が、Trk選択的な阻害活性を有し、NGF血管透過性亢進を持続的に抑制し、薬物相互作用を有さず、遊離塩基に対して溶解性、吸収性に優れた化合物であることから、Trk関連疾患の予防および/または治療薬として有用である。
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