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1. (WO2019046612) FIRST-IN-CLASS OF SHMT2 AND MTHFD2 INHIBITORS AS ANTITUMOR AGENTS
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Pub. No.: WO/2019/046612 International Application No.: PCT/US2018/048905
Publication Date: 07.03.2019 International Filing Date: 30.08.2018
IPC:
A61K 31/519 (2006.01) ,C07D 487/04 (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
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
495
having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
505
Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
519
ortho- or peri-condensed with heterocyclic rings
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
487
Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/-C07D477/183
02
in which the condensed system contains two hetero rings
04
Ortho-condensed systems
Applicants:
DUQUESNE UNIVERSITY OF THE HOLY SPIRIT [US/US]; 600 Forbes Avenue Pittsburgh, Pennsylvania 15282, US
WAYNE STATE UNIVERSITY [US/US]; 5057 Woodward Suite 6306 Detroit, Michigan 48202, US
Inventors:
GANGJEE, Aleem; US
MATHERLY, Larry H.; US
Agent:
COCHENOUR, Craig G.; US
Priority Data:
62/552,43231.08.2017US
Title (EN) FIRST-IN-CLASS OF SHMT2 AND MTHFD2 INHIBITORS AS ANTITUMOR AGENTS
(FR) INHIBITEURS DE SHMT2 ET DE MTHFD2 DE PREMIÈRE CATÉGORIE UTILISÉS COMME AGENTS ANTITUMORAUX
Abstract:
(EN) Pyrrolopyrimidine compounds and pharmaceutically acceptable salt thereof are provided. Pharmaceutical compositions having these compounds and acceptable pharmaceutical carriers are disclosed. Pyrrolopyrimidine compounds and pharmaceutically acceptable salts are set forth that are useful to treat a patient having pancreatic, colon, and lung cancers, to target mitochondrial metabolism, and to target serine hydroxymethyltransferase 2 (SHMT2) and 5,10-methylene tetrahydrofolate dehydrogenase 2 (MTHFD2).
(FR) L'invention concerne des composés de pyrrolopyrimidine et un sel pharmaceutiquement acceptable de ceux-ci. L'invention concerne également des compositions pharmaceutiques contenant ces composés et des excipients pharmaceutiques acceptables. L'invention concerne des composés de pyrrolopyrimidine et des sels pharmaceutiquement acceptables qui sont utiles pour traiter un patient présentant les cancers du pancréas, du côlon et du poumon, pour cibler le métabolisme mitochondrial, et pour cibler la sérine hydroxyméthyltransférase 2 (SHMT2) et la 5,10-méthylène tétrahydrofolate déshydrogénase 2 (MTHFD2).
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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, DJ, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IR, IS, JO, JP, KE, KG, KH, KN, KP, KR, KW, KZ, LA, LC, LK, LR, LS, 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, ST, 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)