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1. WO2014168103 - DIPYRROMETHENE CRYSTAL AND METHOD FOR MANUFACTURING SAME

Publication Number WO/2014/168103
Publication Date 16.10.2014
International Application No. PCT/JP2014/060055
International Filing Date 07.04.2014
IPC
C07D 207/34 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
207Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
02with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
30having two double bonds between ring members or between ring members and non-ring members
34with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
A61K 31/40 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
40having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
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 31/40
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
40having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
A61K 9/0095
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9Medicinal preparations characterised by special physical form
0087Galenical forms not covered by A61K9/02 - A61K9/7023
0095Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches
A61K 9/2018
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9Medicinal preparations characterised by special physical form
20Pills, tablets, ; discs, rods
2004Excipients; Inactive ingredients
2013Organic compounds, e.g. phospholipids, fats
2018Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
A61K 9/4858
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9Medicinal preparations characterised by special physical form
48Preparations in capsules, e.g. of gelatin, of chocolate
4841Filling excipients; Inactive ingredients
4858Organic compounds
A61P 13/12
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
13Drugs for disorders of the urinary system
12of the kidneys
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
Applicants
  • 第一三共株式会社 DAIICHI SANKYO COMPANY,LIMITED [JP]/[JP]
Inventors
  • 渡邉 仁 WATANABE, Masashi
  • 岡地 隆弘 OKACHI, Takahiro
  • 川原 倫明 KAWAHARA, Michiaki
  • 長澤 大史 NAGASAWA, Hiroshi
  • 佐藤 仙忠 SATO, Noritada
  • 瀧田 崇 TAKITA, Takashi
  • 長谷川 玄 HASEGAWA, Gen
Agents
  • 石橋 公樹 ISHIBASHI Koki
Priority Data
2013-08187910.04.2013JP
Publication Language Japanese (JA)
Filing Language Japanese (JA)
Designated States
Title
(EN) DIPYRROMETHENE CRYSTAL AND METHOD FOR MANUFACTURING SAME
(FR) CRISTAL DE DIPYRROMÉTHÈNE ET SON PROCÉDÉ DE FABRICATION
(JA) ピロール誘導体の結晶及びその製造方法
Abstract
(EN)
Provided are an intermediate in the manufacture of an atropisomer of a dipyrromethene that has excellent mineralocorticoid receptor antagonism, a method for manufacturing the same and crystals thereof. A method for manufacturing an atropisomer of a dipyrromethene that includes the step of dividing the atropisomer of general formula (I) [In the formula, R1 is a methyl group or a trifluoromethyl group, R2 is a hydrogen atom or a C1-C3 alkoxy group, and n is an integer selected from 1 to 3.] characterized by using an optically active amine that has a cinchonan skeleton, and crystals of (S)-1-(2- hydroxyethyl)-4-methyl-N-[4-(methylsulfonyl)phenyl]-5-[2-( trifluoromethyl)phenyl]-1H-pyrrole-3-carboxamide.
(FR)
L'invention porte sur un produit intermédiaire dans la fabrication d'un atropisomère d'un dipyrrométhène qui présente un excellent effet antagoniste sur les récepteurs des minéralocorticoïdes, un procédé pour sa fabrication ainsi que des cristaux de celui-ci. L'invention concerne également un procédé de fabrication d'un atropisomère d'un dipyrrométhène qui comprend l'étape de division de l'atropisomère de formule générale (I) [Dans la formule, R1 est un groupe méthyle ou un groupe trifluorométhyle, R2 est un atome d'hydrogène ou un groupe alcoxy en C1-C3, et n est un nombre entier sélectionné parmi 1 à 3.] caractérisé par l'utilisation d'une amine optiquement active qui possède un squelette cinchonane, et de cristaux de (S)-1-(2-hydroxyéthyl)-4-méthyl-N-[4-(méthylsulfonyl)phényl]-5-[2-(trifluorométhyl)phényl]-1H-pyrrole-3-carboxamide.
(JA)
 本発明は、優れたミネラルコルチコイド受容体拮抗作用を有するピロール誘導体のアトロプ異性体の製造中間体、製造方法及びその結晶を提供する。 シンコナン骨格を有する光学活性アミンを用いることを特徴とする、下記一般式(I) [式中、R1はメチル基又はトリフルオロメチル基を示し、R2は水素原子又はC1-C3アルコキシ基を示し、nは1~3から選択される整数を示す。] のアトロプ異性体を分割する工程を含む、ピロール誘導体のアトロプ異性体の製造方法及び(S)-1-(2-ヒドロキシエチル)-4-メチル-N-[4-(メチルスルホニル)フェニル]-5-[2-(トリフルオロメチル)フェニル]-1H-ピロール-3-カルボキサミドの結晶。
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