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1. WO2020007839 - CRYSTALLINE SALTS OF 5-METHYL-(6S)-TETRAHYDROFOLIC ACID AND L-LEUCINE ETHYL ESTER

Publication Number WO/2020/007839
Publication Date 09.01.2020
International Application No. PCT/EP2019/067698
International Filing Date 02.07.2019
IPC
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
7
Drugs for disorders of the blood or the extracellular fluid
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
9
Drugs for disorders of the cardiovascular system
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
19
Drugs for skeletal disorders
08
for bone diseases, e.g. rachitism, Paget's disease
10
for osteoporosis
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
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
28
for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
229
Compounds containing amino and carboxyl groups bound to the same carbon skeleton
02
having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton
04
the carbon skeleton being acyclic and saturated
06
having only one amino and one carboxyl group bound to the carbon skeleton
08
the nitrogen atom of the amino group being further bound to hydrogen atoms
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
475
Heterocyclic compounds containing pteridine ring systems
02
with an oxygen atom directly attached in position 4
04
with a nitrogen atom directly attached in position 2
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, 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
A61P 7/00 (2006.01)
A61P 9/00 (2006.01)
A61P 19/10 (2006.01)
A61P 25/00 (2006.01)
A61P 25/28 (2006.01)
C07C 229/08 (2006.01)
CPC
A61P 19/10
A61P 25/00
A61P 25/28
A61P 7/00
A61P 9/00
C07C 229/08
Applicants
  • MERCK PATENT GMBH [DE/DE]; Frankfurter Strasse 250 64293 DARMSTADT, DE
Inventors
  • MOSER, Rudolf; CH
  • GROEHN, Viola; CH
  • BOEHNI STAMM, Ruth; CH
  • BLATTER, Fritz; CH
  • SZELAGIEWICZ, Martin; CH
Priority Data
18182279.206.07.2018EP
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) CRYSTALLINE SALTS OF 5-METHYL-(6S)-TETRAHYDROFOLIC ACID AND L-LEUCINE ETHYL ESTER
(FR) SELS CRISTALLINS D'ACIDE 5-MÉTHYL-(6S)-TÉTRAHYDROFOLIQUE ET D'ESTER ÉTHYLIQUE DE L-LEUCINE
Abstract
(EN)
The present inventionrefers to a crystalline salt comprising5-methyl-(6S)-tetrahydrofolic acid L-leucine ethyl ester wherein the molar ratio of 5-methyl-(6S)-tetrahydrofolic acid and L-leucine ethyl ester is from 1:0.3 to 1:3.0 (in mol/mol) and/or hydrates and/or solvates thereof as well as to a process of obtaining the same.
(FR)
La présente invention concerne un sel cristallin comprenant de l'acide 5-méthyl-(6S)-tétrahydrofolique et de l'ester éthylique de L-leucine, le rapport molaire de l'acide 5-méthyl-(6S)-tétrahydrofolique à l'ester éthylique de L-leucine étant compris entre 1:0,3 et 1:3,0 (en moles/moles), et/ou des hydrates et/ou des solvates correspondants, ainsi que des procédés d'obtention de ces derniers.
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