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1. WO2016003919 - ANALOGS OF PRIDOPIDINE, THEIR PREPARATION AND USE

Publication Number WO/2016/003919
Publication Date 07.01.2016
International Application No. PCT/US2015/038349
International Filing Date 29.06.2015
IPC
A61K 31/451 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
435having six-membered rings with one nitrogen as the only ring hetero atom
44Non-condensed pyridines; Hydrogenated derivatives thereof
445Non-condensed piperidines, e.g. piperocaine
451having a carbocyclic ring directly attached to the heterocyclic ring, e.g. glutethimide, meperidine, loperamide, phencyclidine, piminodine
CPC
A61K 31/451
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
435having six-membered rings with one nitrogen as the only ring hetero atom
44Non condensed pyridines; Hydrogenated derivatives thereof
445Non condensed piperidines, e.g. piperocaine
451having a carbocyclic group directly attached to the heterocyclic ring, e.g. glutethimide, meperidine, loperamide, phencyclidine, piminodine
A61P 25/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25Drugs for disorders of the nervous system
A61P 25/14
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25Drugs for disorders of the nervous system
14for treating abnormal movements, e.g. chorea, dyskinesia
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
C07D 211/24
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
211Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
04with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
06having no double bonds between ring members or between ring members and non-ring members
08with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
18with substituted hydrocarbon radicals attached to ring carbon atoms
20with hydrocarbon radicals, substituted by singly bound oxygen or sulfur atoms
24by sulfur atoms to which a second hetero atom is attached
C07D 211/42
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
211Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
04with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
06having no double bonds between ring members or between ring members and non-ring members
36with 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
40Oxygen atoms
42attached in position 3 or 5
Applicants
  • TEVA PHARMACEUTICAL INDUSTRIES LTD. [IL]/[IL] (AE, AG, AL, AM, AO, AT, AU, AZ, BA, BE, BF, BG, BH, BJ, BN, BR, BW, BY, BZ, CA, CF, CG, CH, CI, CL, CM, CN, CO, CR, CU, CY, CZ, DE, DK, DM, DO, DZ, EC, EE, EG, ES, FI, FR, GA, GB, GD, GE, GH, GM, GN, GQ, GR, GT, GW, HN, HR, HU, ID, IE, IL, IN, IR, IS, IT, JP, KE, KG, KM, KN, KP, KR, KZ, LA, LC, LK, LR, LS, LT, LU, LV, LY, MA, MC, MD, ME, MG, MK, ML, MN, MR, MT, MW, MX, MY, MZ, NA, NE, NG, NI, NL, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, SC, SD, SE, SG, SI, SK, SL, SM, SN, ST, SV, SY, SZ, TD, TG, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, UZ, VC, VN, ZA, ZM, ZW)
  • TEVA PHARMACEUTICALS USA, INC. [US]/[US] (BB)
  • SCHMIDT, Malle [EE]/[EE] (US)
  • PÄRI, Malle [EE]/[EE] (US)
  • LAOS, Marit [EE]/[EE] (US)
  • MAASALU, Ants [EE]/[EE] (US)
  • KALJUSTE, Kalle [EE]/[EE] (US)
Inventors
  • SCHMIDT, Malle
  • PÄRI, Malle
  • LAOS, Marit
  • MAASALU, Ants
  • KALJUSTE, Kalle
Agents
  • WHITE, John, P.
Priority Data
62/019,33730.06.2014US
62/076,43606.11.2014US
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) ANALOGS OF PRIDOPIDINE, THEIR PREPARATION AND USE
(FR) ANALOGUES DE PRIDOPIDINE, LEUR PRÉPARATION ET UTILISATION
Abstract
(EN)
This invention provides an isolated compound having the structure: The invention also provides for a process for preparing 4-(3-(methylsulfonyl)phenyl)-1-propylpiperidin-4-ol, 1-(3,3-bis(3-(methylsulfonyl)phenyl)propyl)-4-(3-(methylsulfonyl) phenyl)piperidone, 1,4-bis((3-(1 -propylpiperidin-4-yl)phenyl)sulfonyl)butane, (3R,4S)-4-(3-(methylsulfonyl)phenyl)-1-propylpiperidin-3-ol, 4-(3-(methylsulfonyl)phenyl)-l-propylpiperidine 1- oxide, 1-(2-methylpentyl)-4-(3-(methylsulfonyl)phenyl)piperidine, 4-(3-(methylsulfinyl)phenyl)-1-propyl-1,2,3,6-tetrahydropyridine, and 4-(3-(methylsulfonyl)phenyl)-1-propyl-1,2,3,6-tetrahydropyridine. This invention also provides an impurity or a salt thereof for use, as a reference standard to detect trace amounts of the impurity in a pharmaceutical composition comprising pridopidine or a pharmaceutically acceptable salt thereof. This invention further provides a process for producing a pridopidine drug product comprising obtaining a pridopidine drug substance and mixing the pridopidine drug substance with suitable excipients so as to produce the pridopidine drug product. This invention also provides a process for producing a pridopidine drug product. This invention also provides a process of distributing a pridopidine drug product.
(FR)
L'invention concerne un composé isolé ayant la structure: . L'invention concerne également un procédé de préparation de 4-(3-(méthylsulfonyl)phényl)-1-propylpipéridin-4-ol, de 1-(3,3-bis(3-(méthylsulfonyl)phényl)propyl)-4-(3-(méthylsulfonyl)phényl)pipéridone, de 1,4-bis((3-(1-propylpipéridin-4-yl)phényl)sulfonyl)butane, de (3R,4S)-4-(3-(méthylsulfonyl)phényl)-1-propylpipéridin-3-ol, de 4-(3-(méthylsulfonyl)phényl)-l-propylpipéridine 1-oxyde, de 1-(2-méthylpentyl)-4-(3-(méthylsulfonyl)phényl)pipéridine, de 4-(3-(méthylsulfinyl)phényl)-1-propyl-1,2,3,6-tétrahydropyridine et de 4-(3-(méthylsulfonyl)phényl)-1-propyl-1,2,3,6-tétrahydropyridine. L'invention concerne également une impureté ou un sel de celle-ci pour une utilisation comme standard de référence pour détecter des quantités à l'état de traces de l'impureté dans une composition pharmaceutique comprenant de la pridopidine ou un sel pharmaceutiquement acceptable de celle-ci. L'invention concerne également un procédé de production d'un produit médicamenteux de pridopidine comprenant l'obtention d'une substance médicamenteuse de pridopidine et le mélange de la substance médicamenteuse de pridopidine avec des excipients appropriés de manière à produire le produit médicamenteux de pridopidine. L'invention concerne également un procédé de production d'un produit médicamenteux de pridopidine. L'invention concerne également un procédé de distribution d'un produit médicamenteux de pridopidine.
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