CA2949932 IMPROVED FORMS OF A PI3K DELTA SELECTIVE INHIBITOR FOR USE IN PHARMACEUTICAL FORMULATIONS

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Application Number 2949932

Application Date 26.05.2015

Publication Number 2949932

Publication Date 03.12.2015

Grant Number

Grant Date 10.08.2021

Publication Kind C

IPC

CPC

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Applicants RHIZEN PHARMACEUTICALS SA

Inventors VAKKALANKA, SWAROOP KUMAR VENKATA SATYA

Priority Data 2596/CHE/2014 27.05.2014 IN
2597/CHE/2014 27.05.2014 IN

Title

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

(FR) FORMES AMELIOREES D'UN INHIBITEUR SELECTIF DE LA PI3K DELTA UTILISEES DANS DES PREPARATIONS PHARMACEUTIQUES

Abstract

(EN) The present invention relates to a crystalline p-toluenesulfonic acid salt of the compound( see above formula)

(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

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

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 C07D451/00 - C07D477/00
02	in which the condensed system contains two hetero rings
04	Ortho-condensed systems

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1. CA2949932 - 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

A	HUMAN NECESSITIES
61	MEDICAL OR VETERINARY SCIENCE; HYGIENE
P	SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
29	Non-central analgesic, antipyretic or anti-inflammatory agents, e.g antirheumatic agents; Non-steroidal anti-inflammatory drugs (NSAIDs)

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