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1. WO2019054451 - CRYSTALS OF TETRAHYDRONAPHTHYL UREA DERIVATIVE

Publication Number WO/2019/054451
Publication Date 21.03.2019
International Application No. PCT/JP2018/034021
International Filing Date 13.09.2018
IPC
C07D 401/04 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
04directly linked by a ring-member-to-ring- member bond
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
A61P 43/00 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
43Drugs for specific purposes, not provided for in groups A61P1/-A61P41/108
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
A61P 43/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
43Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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 401/04
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
04directly linked by a ring-member-to-ring-member bond
Applicants
  • 持田製薬株式会社 MOCHIDA PHARMACEUTICAL CO., LTD. [JP]/[JP]
Inventors
  • 河田 裕治 KAWADA Yuji
  • 斉藤 文彦 SAITOH Fumihiko
  • 永末 央 NAGASUE Hiroshi
  • 佐藤 勉 SATOH Tsutomu
Agents
  • 田中 伸一郎 TANAKA Shinichiro
  • 弟子丸 健 DESHIMARU Takeshi
  • ▲吉▼田 和彦 YOSHIDA Kazuhiko
  • 箱田 篤 HAKODA Atsushi
  • 山崎 一夫 YAMASAKI Kazuo
  • 服部 博信 HATTORI Hironobu
Priority Data
2017-17803015.09.2017JP
Publication Language Japanese (JA)
Filing Language Japanese (JA)
Designated States
Title
(EN) CRYSTALS OF TETRAHYDRONAPHTHYL UREA DERIVATIVE
(FR) CRISTAUX DE DÉRIVÉ DE TÉTRAHYDRONAPHTYLE URÉE
(JA) テトラヒドロナフチルウレア誘導体の結晶
Abstract
(EN)
Provided are type-I, type-III, type-V and type-VI crystals of 1-((1R,2R)-2-hydroxy-4,4-dimethyl-1,2,3,4-tetrahydronaphthalen-1-yl)-3-(5-methyl-6-(2-methylpyrimidin-5-yl)-2-phenylpyridin-3-yl) urea which are useful as bulk pharmaceutical crystals. Also provided are type-I, type-III, type-V and type-VI crystals of 1-((1R,2R)-2-hydroxy-4,4-dimethyl-1,2,3,4-tetrahydronaphthalen-1-yl)-3-(5-methyl-6-(2-methylpyrimidin-5-yl)-2-phenylpyridin-3-yl) urea having excellent TrkA inhibitory effect, medicines and medicinal compositions containing these crystals, and a method for producing these crystals.
(FR)
L'invention concerne des cristaux de type I, de type III, de type V et de type VI de 1-((1R,2R)-2-hydroxy-4,4-diméthyl-1,2,3,4-tétrahydronaphthalèn-1-yl)-3-(5-méthyl-6-(2-méthylpyrimidin-5-yl)-2-phénylpyridin-3-yl) urée qui sont utiles en tant que cristaux pharmaceutiques en vrac. L'invention concerne également des cristaux de type I, de type III, de type V et de type VI de 1-((1R,2R)-2-hydroxy-4,4-diméthyl-1,2,3,4-tétrahydronaphthalèn-1-yl)-3-(5-méthyl-6-(2-méthylpyrimidin-5-yl)-2-phénylpyridin-3-yl) urée ayant un excellent effet inhibiteur de TrkA, des médicaments et des compositions médicinales contenant ces cristaux, et un procédé de production desdits cristaux.
(JA)
本発明は、医薬品原薬の結晶として有用な1-((1R,2R)-2-ヒドロキシ-4,4-ジメチル-1,2,3,4-テトラヒドロナフタレン-1-イル)-3-(5-メチル-6-(2-メチルピリミジン-5-イル)-2-フェニルピリジン-3-イル)ウレアのI型結晶、III結晶、V型結晶及びVI型結晶を提供する。本発明は、また、優れたTrkA阻害作用を有する1-((1R,2R)-2-ヒドロキシ-4,4-ジメチル-1,2,3,4-テトラヒドロナフタレン-1-イル)-3-(5-メチル-6-(2-メチルピリミジン-5-イル)-2-フェニルピリジン-3-イル)ウレアのI型結晶、III結晶、V型結晶及びVI型結晶、当該結晶を含む医薬及び医薬組成物、並びに当該結晶の製造方法を提供する。
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