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1. JP2020122022 - IMPROVED FORMS OF PI3K DELTA SELECTIVE INHIBITOR FOR USE IN PHARMACEUTICAL FORMULATIONS

Office
Japan
Application Number 2020088147
Application Date 20.05.2020
Publication Number 2020122022
Publication Date 13.08.2020
Publication Kind A
IPC
C07D 487/04
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
487Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/-C07D477/183
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
A61P 35/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
A61K 31/519
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
519ortho- or peri-condensed with heterocyclic rings
CPC
C07D 487/04
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
487Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by C07D451/00 - C07D477/00
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
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
A61P 29/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
29Non-central analgesic, antipyretic or anti-inflammatory agents, e.g antirheumatic agents; Non-steroidal anti-inflammatory drugs (NSAIDs)
A61P 35/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
A61K 31/519
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
519ortho- or peri-condensed with heterocyclic rings
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
Applicants RHIZEN PHARMACEUTICALS SA
ライゼン・ファーマシューティカルズ・エスアー
Inventors SWAROOP KUMAR VENKATA SATYA VAKKALANKA
スワループ・クマール・ヴェンカタ・サティア・ヴァッカランカ
Agents 村山 靖彦
実広 信哉
阿部 達彦
Priority Data 2596/CHE/2014 27.05.2014 IN
2597/CHE/2014 27.05.2014 IN
Title
(EN) IMPROVED FORMS OF PI3K DELTA SELECTIVE INHIBITOR FOR USE IN PHARMACEUTICAL FORMULATIONS
(JA) 医薬製剤用PI3Kデルタ選択的抑制剤の改良形態
Abstract
(EN)

PROBLEM TO BE SOLVED: To provide a p-toluenesulfonic acid salt (PTSA) of a selective PI3K delta inhibitor (S)-2-(1-(4-amino-3-(3-fluoro-4-isopropoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)ethyl)-6-fluoro-3-(3-fluorophenyl)-4H- chromen-4-one (TGR-1202) that exhibits enhanced solubility and pharmacokinetics upon oral administration.

SOLUTION: The present invention relates to a PTSA salt of TGR-1202 having a d(0.9) of from about 5 to about 50 μm, such as from about 5 to about 25 μm or from about 5 to about 15 μm.

SELECTED DRAWING: None

COPYRIGHT: (C)2020,JPO&INPIT


(JA)

【課題】本発明が解決しようとする課題は、経口投与において高められた溶解性及び薬物動態を示す、選択的PI3Kデルタ抑制剤(S)−2−(1−(4−アミノ−3−(3−フルオロ−4−イソプロポキシフェニル)−1H−ピラゾロ[3,4−d]ピリミジン−1−イル)エチル)−6−フルオロ−3−(3−フルオロフェニル)−4H−クロメン−4−オン(TGR−1202)のp−トルエンスルホン酸塩(PTSA)を提供することである。
【解決手段】本発明は、約5〜約50μm、例えば、約5〜約25μmまたは約5〜約15μmのd(0.9)を有する、TGR−1202のPTSA塩に関する。
【選択図】なし