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1. (WO2010075561) SMALL MOLECULE INHIBITORS OF NECROPTOSIS
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/2010/075561 International Application No.: PCT/US2009/069483
Publication Date: 01.07.2010 International Filing Date: 23.12.2009
IPC:
A01N 43/40 (2006.01) ,A61K 31/44 (2006.01)
A HUMAN NECESSITIES
01
AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
N
PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
43
Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
34
having rings with one nitrogen atom as the only ring hetero atom
40
six-membered rings
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
435
having six-membered rings with one nitrogen as the only ring hetero atom
44
Non-condensed pyridines; Hydrogenated derivatives thereof
Applicants:
PRESIDENT AND FELLOWS OF HARVARD COLLEGE [US/US]; 17 Quincy Street Cambridge, MA 02138, US (AllExceptUS)
YUAN, Junying [US/US]; US (UsOnly)
HSU, Emily, S. [US/DE]; DE (UsOnly)
Inventors:
YUAN, Junying; US
HSU, Emily, S.; DE
Agent:
BIEKER-BRADY, Kristina; Clark & Elbing LLP 101 Federal Street Boston, MA 02110, US
Priority Data:
61/140,61523.12.2008US
Title (EN) SMALL MOLECULE INHIBITORS OF NECROPTOSIS
(FR) INHIBITEURS DE LA NÉCROPTOSE DE PETITE TAILLE MOLÉCULAIRE
Abstract:
(EN) The invention features a series of heterocyclic derivatives that inhibit tumor necrosis factor alpha (TNF-α) induced necroptosis. The heterocyclic compounds of the invention are described by Formulas (I)-(VIII) and by Compounds (I)-(I), (13)-(26), (27)-(33), (48)-(57), and (58)-(70). These necrostatins are shown to inhibit TNF-α induced necroptosis in FADD- deficient variant of human Jurkat T cells. The invention further features pharmaceutical compositions featuring necrostatins. The compounds and compositions of the invention may also be used to treat disorders where necroptosis is likely to play a substantial role.
(FR) L'invention concerne une série de dérivés hétérocycliques qui inhibent la nécroptose induite par le facteur alpha de nécrose tumorale (TNF-α). Les composés hétérocycliques de l'invention sont décrits par les formules (I) à (VIII) et par les composés (I)-(I), (13) à (26), (27) à (33), (48) à (57) et (58) à (70). L'invention montre que ces nécrostatines inhibent la nécroptose induite par le TNF-α dans des variantes FADD-déficientes de cellules Jurkat T humaines. L'invention concerne également des compositions pharmaceutiques contenant des nécrostatines. Les composés et les compositions de l'invention peuvent aussi être utilisés pour traiter des troubles dans lesquels la nécroptose est susceptible de jouer un rôle important.
Designated States: AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, 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, IS, JP, KE, KG, KM, 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, PE, PG, PH, PL, PT, RO, RS, RU, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, 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, LS, MW, MZ, NA, SD, SL, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Organization (AM, AZ, BY, KG, KZ, MD, RU, TJ, TM)
European Patent Office (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, SE, SI, SK, SM, TR)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, ML, MR, NE, SN, TD, TG)
Publication Language: English (EN)
Filing Language: English (EN)
Also published as:
EP2381775JP2012513481US20120122889CN102316735CA2772760JP2015061853
EP3000468AU2009329879AU2016202262IN5352/CHENP/2011