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1. WO2020115715 - DEUTERATED ANALOGS OF ACETYL-LEUCINE

Publication Number WO/2020/115715
Publication Date 11.06.2020
International Application No. PCT/IB2019/060525
International Filing Date 06.12.2019
IPC
A61P 25/06 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25Drugs for disorders of the nervous system
06Antimigraine agents
A61K 31/198 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
185Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
19Carboxylic acids, e.g. valproic acid
195having an amino group
197the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid (GABA), beta-alanine, epsilon-aminocaproic acid, pantothenic acid
198Alpha-amino acids, e.g. alanine, edetic acid (EDTA)
A61P 25/28 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25Drugs for disorders of the nervous system
28for 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
C07B 59/00 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
59Introduction of isotopes of elements into organic compounds
C07C 233/47 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
233Carboxylic acid amides
01having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
45having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups
46with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom
47having the carbon atom of the carboxamide group bound to a hydrogen atom or to a carbon atom of an acyclic saturated carbon skeleton
CPC
A61K 31/198
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
185Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic, hydroximic acids
19Carboxylic acids, e.g. valproic acid
195having an amino group
197the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid, pantothenic acid
198Alpha-aminoacids, e.g. alanine, edetic acids [EDTA],
A61K 45/06
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
45Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
A61P 25/06
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25Drugs for disorders of the nervous system
06Antimigraine agents
A61P 25/28
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25Drugs for disorders of the nervous system
28for 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
C07B 59/001
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
59Introduction of isotopes of elements into organic compounds ; ; Labelled organic compounds per se
001Acyclic or carbocyclic compounds
C07C 233/47
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
233Carboxylic acid amides
01having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
45having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups
46with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom
47having the carbon atom of the carboxamide group bound to a hydrogen atom or to a carbon atom of an acyclic saturated carbon skeleton
Applicants
  • INTRABIO LTD. [GB]/[GB]
Inventors
  • MANN, Michiko
Priority Data
62/776,29706.12.2018US
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) DEUTERATED ANALOGS OF ACETYL-LEUCINE
(FR) ANALOGUES DEUTÉRÉS D'ACÉTYL-LEUCINE
Abstract
(EN)
The present disclosure provides compounds represented by Formula I: I, and the pharmaceutically acceptable salts and solvates thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, and R13 are as defined as set forth in the specification, and the deuterium enrichment of any one or more of R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, and R13 is about 15% or more. The present disclosure also provides compounds having Formula I for use to treat or delay the progression of a lysosomal storage disorder or a neurodegenerative disease in a subject, provide neuroprotection in a subject having a lysosomal disorder, treat or prevent a migraine, and the symptoms associated therewith, in a subject, or improve mobility and/or cognitive function in a subject.
(FR)
La présente invention concerne des composés représentés par la formule I : I, et leurs sels et solvates pharmaceutiquement acceptables, où R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12 et R13 sont tels que définis dans la description, et l'enrichissement en deutérium de l'un quelconque ou de plusieurs de R3, R4, R5, R6, R7, R8, R9, R10, R11, R12 et R13 est d'environ 15 % ou plus. La présente invention concerne également des composés de Formule I destinés à être utilisés pour traiter ou retarder la progression d'un trouble de stockage lysosomal ou d'une maladie neurodégénérative chez un sujet, fournir une neuroprotection chez un sujet ayant un trouble lysosomal, traiter ou prévenir une migraine, et les symptômes associés à celle-ci, chez un sujet, ou améliorer la mobilité et/ou la fonction cognitive chez un sujet.
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