WO2015181728 IMPROVED FORMS OF A PI3K DELTA SELECTIVE INHIBITOR FOR USE IN PHARMACEUTICAL FORMULATIONS

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Publication Number WO/2015/181728

Publication Date 03.12.2015

International Application No. PCT/IB2015/053940

International Filing Date 26.05.2015

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CPC

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Applicants

RHIZEN PHARMACEUTICALS SA [CH]/[CH]

Inventors

VAKKALANKA, Swaroop Kumar Venkata Satya

Priority Data

2596/CHE/2014		27.05.2014		IN
2597/CHE/2014		27.05.2014		IN

Publication Language English (en)

Filing Language English (EN)

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Title

(EN) IMPROVED FORMS OF A PI3K DELTA SELECTIVE INHIBITOR FOR USE IN PHARMACEUTICAL FORMULATIONS

(FR) FORMES AMÉLIORÉES D'UN INHIBITEUR SÉLECTIF DE LA PI3K DELTA UTILISÉES DANS DES PRÉPARATIONS PHARMACEUTIQUES

Abstract

(EN) The present invention relates to solid state forms of a p-toluenesulfonic acid salt (PTSA) of the selective PI3K delta inhibitor (S)-2-(1-(4-amino-3-(3-fluoro-4-isopropoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)ethyl)-3-(3-fluorophenyl)-4H- chromen-4-one (TGR-1202). The present invention also relates to methods of preparing the same, pharmaceutical compositions containing them, and methods of treating a PI3K kinase mediated disease or disorder, such as cancer, by administering the same.

(FR) L'invention concerne des formes à l'état solide d'un sel d'acide p-toluènesulfonique (APTS) sélectif de l'inhibiteur de la PI3K delta (S)-2-(1-(4-amino-3-(3-fluoro-4-isopropoxyphényl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)éthyl)-3-(3-fluorophényl)-4H-chromen-4-one (TGR-1202). L'invention concerne également des procédés de préparation de ces formes, des compositions pharmaceutiques qui les contiennent, et des méthodes de traitement d'une maladie ou d'une affection dans laquelle intervient la PI3K kinase, par exemple le cancer, en administrant ces formes.

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
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

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

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
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

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1. WO2015181728 - IMPROVED FORMS OF A 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