WO2019143829 FASORACETAM CRYSTALLINE FORMS

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Publication Number WO/2019/143829

Publication Date 25.07.2019

International Application No. PCT/US2019/014027

International Filing Date 17.01.2019

IPC

CPC

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Applicants

THE CHILDREN'S HOSPITAL OF PHILADELPHIA [US]/[US]

Inventors

LEYSSENS, Tom
HARMSEN, Bram

Agents

RIGAUT, Kathleen, D.

Priority Data

62/619,031	18.01.2018	US
62/668,108	07.05.2018	US
62/683,419	11.06.2018	US

Publication Language English (en)

Filing Language English (EN)

Designated States

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Title

(EN) FASORACETAM CRYSTALLINE FORMS

(FR) FORMES CRISTALLINES DU FASORACÉTAM

Abstract

(EN) The disclosure is directed to crystalline forms and mixtures thereof of R-fasoracetam. Such crystalline forms include Form II monohydrate R-fasoracetam and the anhydrate form of R-fasoracetam. The disclosure further includes mixtures of the anhydrate form of R-fasoracetam together with one or more of Form I monohydrate R-fasoracetam and Form II monohydrate R-fasoracetam.

(FR) L'invention concerne des formes cristallines et des mélanges associés du R-fasoracétam. De telles formes cristallines comprennent la forme II du monohydrate de R-fasoracétam et la forme anhydre du R-fasoracétam. L'invention concerne en outre des mélanges de la forme anhydre du R-fasoracétam conjointement avec la forme I du monohydrate de R-Fasoracétam et/ou la forme II du monohydrate de R-fasoracétam.

C	CHEMISTRY; METALLURGY
12	BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
Q	MEASURING OR TESTING PROCESSES INVOLVING ENZYMES, NUCLEIC ACIDS OR MICROORGANISMS; COMPOSITIONS OR TEST PAPERS THEREFOR; PROCESSES OF PREPARING SUCH COMPOSITIONS; CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL OR ENZYMOLOGICAL PROCESSES
1	Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions
68	involving nucleic acids

G	PHYSICS
01	MEASURING; TESTING
N	INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
33	Investigating or analysing materials by specific methods not covered by groups G01N1/-G01N31/131
48	Biological material, e.g. blood, urine; Haemocytometers
50	Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
68	involving proteins, peptides or amino acids

C	CHEMISTRY; METALLURGY
12	BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
Q	MEASURING OR TESTING PROCESSES INVOLVING ENZYMES, NUCLEIC ACIDS OR MICROORGANISMS; COMPOSITIONS OR TEST PAPERS THEREFOR; PROCESSES OF PREPARING SUCH COMPOSITIONS; CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL OR ENZYMOLOGICAL PROCESSES
1	Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions
68	involving nucleic acids

G	PHYSICS
01	MEASURING; TESTING
N	INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
33	Investigating or analysing materials by specific methods not covered by groups G01N1/-G01N31/131
48	Biological material, e.g. blood, urine; Haemocytometers
50	Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
68	involving proteins, peptides or amino acids

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
435	having six-membered rings with one nitrogen as the only ring hetero atom
44	Non condensed pyridines; Hydrogenated derivatives thereof
445	Non condensed piperidines, e.g. piperocaine
4523	containing further heterocyclic ring systems
454	containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone

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1. WO2019143829 - FASORACETAM CRYSTALLINE FORMS

A	HUMAN NECESSITIES
61	MEDICAL OR VETERINARY SCIENCE; HYGIENE
P	SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25	Drugs for disorders of the nervous system

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
D	HETEROCYCLIC COMPOUNDS
207	Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
02	with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
18	having one double bond between ring members or between a ring member and a non-ring member
22	with hetero atoms or with carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
24	Oxygen or sulfur atoms
26	2-Pyrrolidones
273	with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to other ring carbon atoms
277	Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals

C	CHEMISTRY; METALLURGY
07	ORGANIC CHEMISTRY
D	HETEROCYCLIC COMPOUNDS
207	Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
02	with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
18	having one double bond between ring members or between a ring member and a non-ring member
22	with hetero atoms or with carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
24	Oxygen or sulfur atoms
26	2-Pyrrolidones
273	with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to other ring carbon atoms
277	Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
28	2-Pyrrolidone-5- carboxylic acids; Functional derivatives thereof, e.g. esters, nitriles

C	CHEMISTRY; METALLURGY
07	ORGANIC CHEMISTRY
D	HETEROCYCLIC COMPOUNDS
207	Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
02	with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
18	having one double bond between ring members or between a ring member and a non-ring member
22	with hetero atoms or with carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
24	Oxygen or sulfur atoms
26	2-Pyrrolidones
273	with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to other ring carbon atoms
277	Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals

C	CHEMISTRY; METALLURGY
07	ORGANIC CHEMISTRY
D	HETEROCYCLIC COMPOUNDS
207	Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
02	with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
18	having one double bond between ring members or between a ring member and a non-ring member
22	with hetero atoms or with carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
24	Oxygen or sulfur atoms
26	2-Pyrrolidones
273	with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to other ring carbon atoms
277	Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
28	2-Pyrrolidone-5- carboxylic acids; Functional derivatives thereof, e.g. esters, nitriles