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1. (WO2014197775) THIOUREA COMPOUNDS AND THEIR USE AS INHIBITORS OF SIRT2 OR SIRT5
Latest bibliographic data on file with the International Bureau   

Pub. No.: WO/2014/197775 International Application No.: PCT/US2014/041251
Publication Date: 11.12.2014 International Filing Date: 06.06.2014
IPC:
A61K 31/167 (2006.01) ,A61K 31/166 (2006.01) ,A61K 31/16 (2006.01) ,A61P 25/28 (2006.01) ,A61P 25/16 (2006.01)
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
16
Amides, e.g. hydroxamic acids
165
having aromatic rings, e.g. colchicine, atenolol, progabide
167
having the nitrogen atom of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
16
Amides, e.g. hydroxamic acids
165
having aromatic rings, e.g. colchicine, atenolol, progabide
166
having the carbon atom of a carboxamide group directly attached to the aromatic ring, e.g. procainamide, procarbazine, metoclopramide, labetalol
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
16
Amides, e.g. hydroxamic acids
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
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
14
for treating abnormal movements, e.g. chorea, dyskinesia
16
Anti-Parkinson drugs
Applicants:
CORNELL UNIVERSITY [US/US]; Cornell Center for Technology, Enterprise & Commercialization 395 Pine Tree Road Suite 310 Ithaca, New York 14850, US
Inventors:
LIN, Hening; US
Agent:
GROLZ, Edward W.; US
Priority Data:
61/831,73806.06.2013US
Title (EN) THIOUREA COMPOUNDS AND THEIR USE AS INHIBITORS OF SIRT2 OR SIRT5
(FR) COMPOSÉS À BASE DE THIOURÉE ET LEUR UTILISATION EN TANT QU'INHIBITEURS DE SIRT2 OU SIRT5
Abstract:
(EN) A compound useful as a Sirt2 or Sirt5 inhibitor having the formula (1) wherein: R1 is a hydrocarbon group having at least two carbon atoms connected by carbon-carbon bonds, wherein said hydrocarbon group is optionally endcapped by a neutral or anionic oxygen-containing group; R2a, R2b, and R2c are independently selected from hydrogen atom and hydrocarbon groups; X0, X1, X2, and X3 are independently selected from -(CH2)n-, -NR5-, -O-, -S-, and a bond, wherein n represents 1, 2, or 3, provided that at least one of X0-X3 is -(CH2)n-; and R3 and R4 are independently selected from the group consisting of hydrogen atom, hydrocarbon groups, biological groups, and protecting groups. Also described are pharmaceutical compositions of the inhibiting compounds, and methods of treatment by administration of the inhibiting compounds.
(FR) La présente invention concerne un composé pouvant être utilisé en tant qu'inhibiteur de Sirt2 ou Sirt5 et représenté par la formule (1) dans laquelle : R1 représente un groupe hydrocarboné comportant au moins deux atomes de carbone reliés par des liaisons carbone-carbone, ledit groupe hydrocarboné étant éventuellement coiffé à une extrémité par un groupe contenant un atome d'oxygène neutre ou anionique ; R2a, R2b et R2csont choisis indépendamment parmi un atome d'hydrogène et des groupes hydrocarbonés ; X0, X1, X2 et X3 sont choisis indépendamment parmi -(CH2)n-, -NR5-, -O-, -S- et une liaison, n étant égal à 1, 2 ou 3, sous réserve qu'au moins un des X 0 et X3 représente -(CH2)n ; et R3 et R4 sont choisis indépendamment dans le groupe constitué d'un atome d'hydrogène, de groupes hydrocarbonés, de groupes biologiques et de groupes protecteurs. L'invention concerne également des compositions pharmaceutiques contenant lesdits composés inhibiteurs et des méthodes de traitement consistant à administrer lesdits composés inhibiteurs.
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Designated States: AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IR, IS, JP, KE, KG, KN, KP, KR, KZ, LA, LC, LK, LR, LS, LT, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW
African Regional Intellectual Property Organization (ARIPO) (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Office (AM, AZ, BY, KG, KZ, RU, TJ, TM)
European Patent Office (EPO) (AL, AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, TR)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, KM, ML, MR, NE, SN, TD, TG)
Publication Language: English (EN)
Filing Language: English (EN)