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

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Application Number 2020088147

Application Date 20.05.2020

Publication Number 2020122022

Publication Date 13.08.2020

Publication Kind A

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CPC

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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

(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

C	CHEMISTRY; METALLURGY
07	ORGANIC CHEMISTRY
D	HETEROCYCLIC COMPOUNDS
487	Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/-C07D477/183
02	in which the condensed system contains two hetero rings
04	Ortho-condensed systems

A	HUMAN NECESSITIES
61	MEDICAL OR VETERINARY SCIENCE; HYGIENE
P	SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35	Antineoplastic agents

A	HUMAN NECESSITIES
61	MEDICAL OR VETERINARY SCIENCE; HYGIENE
K	PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31	Medicinal preparations containing organic active ingredients
33	Heterocyclic compounds
395	having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
495	having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
505	Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
519	ortho- or peri-condensed with heterocyclic rings

C	CHEMISTRY; METALLURGY
07	ORGANIC CHEMISTRY
D	HETEROCYCLIC COMPOUNDS
487	Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/-C07D477/183
02	in which the condensed system contains two hetero rings
04	Ortho-condensed systems

A	HUMAN NECESSITIES
61	MEDICAL OR VETERINARY SCIENCE; HYGIENE
P	SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35	Antineoplastic agents

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

C	CHEMISTRY; METALLURGY
07	ORGANIC CHEMISTRY
B	GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
2200	Indexing scheme relating to specific properties of organic compounds
13	Crystalline forms, e.g. polymorphs

C	CHEMISTRY; METALLURGY
07	ORGANIC CHEMISTRY
C	ACYCLIC OR CARBOCYCLIC COMPOUNDS
309	Sulfonic acids; Halides, esters, or anhydrides thereof
01	Sulfonic acids
28	having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
29	of non-condensed six-membered aromatic rings
30	of six-membered aromatic rings substituted by alkyl groups

Y	SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
02	TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
A	TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
50	in human health protection, e.g. against extreme weather
30	Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change