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1. WO2020115753 - L-DOPA AND/OR DOPA DECARBOXYLSE INHIBITORS CONJUGATED TO SUGAR FOR THE TREATMENT OF DOPAMINE-RESPONSIVE DISORDERS

Publication Number WO/2020/115753
Publication Date 11.06.2020
International Application No. PCT/IL2019/051335
International Filing Date 05.12.2019
IPC
A61K 31/047 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
045Hydroxy compounds, e.g. alcohols; Salts thereof, e.g. alcoholates
047having two or more hydroxy groups, e.g. sorbitol
A61K 31/216 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
21Esters, e.g. nitroglycerine, selenocyanates
215of carboxylic acids
216of acids having aromatic rings, e.g. benactizyne, clofibrate
A61K 31/135 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
13Amines, e.g. amantadine
135having aromatic rings, e.g. methadone
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)
A61K 31/223 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
21Esters, e.g. nitroglycerine, selenocyanates
215of carboxylic acids
22of acyclic acids, e.g. pravastatin
223of alpha-amino acids
A61K 45/06 2006.01
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/-A61K41/132
06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
Applicants
  • B. G. NEGEV TECHNOLOGIES AND APPLICATIONS LTD., AT BEN-GURION UNIVERSITY [IL]/[IL]
  • KUSHNIR, Moshe [IL]/[IL]
Inventors
  • KUSHNIR, Moshe
  • HELDMAN, Eliahu
  • SHAUBI, Eleonora
Agents
  • COHEN, Mark S.
Priority Data
62/775,39605.12.2018US
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) L-DOPA AND/OR DOPA DECARBOXYLSE INHIBITORS CONJUGATED TO SUGAR FOR THE TREATMENT OF DOPAMINE-RESPONSIVE DISORDERS
(FR) INHIBITEURS DE L-DOPA ET/OU DOPA-DÉCARBOXYLASE CONJUGUÉS AU SUCRE POUR LE TRAITEMENT DE TROUBLES SENSIBLES À LA DOPAMINE
Abstract
(EN)
The present invention provides conjugates comprising a sugar such as mannitol and one or more L-DOPA and/or DOPA decarboxylse inhibitors including, inter alia, L- DOPA, carbidopa, benserazide, or a combination thereof, wherein the sugar is conjugated to the carboxyl group of the L-DOPA and/or DOPA decarboxylse inhibitor/ s) via a hydroxyl group of the sugar. The present invention further provides related pharmaceutical compositions and methods of producing the conjugates, as well as methods of use for treating medical disorders responsive to dopamininergic stimulation such as movement disorders including, inter alia, Parkinson's Disease.
(FR)
La présente invention concerne des conjugués comprenant un sucre tel que le mannitol et un ou plusieurs inhibiteurs de la L-DOPA et/ou de la DOPA décarboxylase, notamment, entre autres, la L-DOPA, la carbidopa, le bensérazide ou une combinaison de ceux-ci, le sucre étant conjugué au groupe carboxyle du ou des inhibiteurs de la L-DOPA et/ou de la DOPA décarboxylase par l'intermédiaire d'un groupe hydroxyle du sucre. La présente invention concerne en outre des compositions pharmaceutiques associées et des procédés de production des conjugués, ainsi que des procédés d'utilisation pour traiter des troubles médicaux sensibles à une stimulation dopaminergique tels que des troubles du mouvement comprenant, entre autres, la maladie de Parkinson.
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