US20170121336 Forms of a PI3K delta selective inhibitor for use in pharmaceutical formulations

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United States of America

Application Number 15313454

Application Date 26.05.2015

Publication Number 20170121336

Publication Date 04.05.2017

Grant Number 09969740

Grant Date 15.05.2018

Publication Kind B2

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Applicants Rhizen Pharmaceuticals SA

Inventors Swaroop K. Vakkalanka

Agents Blank Rome LLP

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

Title

(EN) Forms of a PI3K delta selective inhibitor for use in pharmaceutical formulations

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)-6-fluoro-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.

A	HUMAN NECESSITIES
01	AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
N	PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
43	Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
90	having two or more relevant hetero rings, condensed among themselves or with a common carbocyclic ring system

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
45	Medicinal preparations containing active ingredients not provided for in groups A61K31/-A61K41/132
06	Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca

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

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1. US20170121336 - 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