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Machine translation
1. (WO2012051105) SELECTIVE PROTON COUPLED FOLATE TRANSPORTER AND FOLATE RECEPTOR, AND GARFTASE AND/OR OTHER FOLATE METABOLIZING ENZYMES INHIBITOR COMPOUNDS AND METHODS OF USING THE SAME
Latest bibliographic data on file with the International Bureau   

Pub. No.:    WO/2012/051105    International Application No.:    PCT/US2011/055584
Publication Date: 19.04.2012 International Filing Date: 10.10.2011
IPC:
A01N 43/54 (2006.01), A01N 43/90 (2006.01), A61K 31/517 (2006.01)
Applicants: DUQUESNE UNIVERSITY OF THE HOLY SPIRIT [US/US]; 600 Forbes Avenue Pittsburgh, PA 15282 (US) (For All Designated States Except US).
WAYNE STATE UNIVERSITY [US/US]; 5057 Woodward, Suite 6306 Detroit, MI 48202 (US) (For All Designated States Except US).
GANGJEE, Aleem [US/US]; (US) (For US Only).
MATHERLY, Larry H. [US/US]; (US) (For US Only)
Inventors: GANGJEE, Aleem; (US).
MATHERLY, Larry H.; (US)
Agent: COCHENOUR, Craig, G.; Buchanan Ingersoll & Rooney PC One Oxford Centre 301 Grant Street, 20th Floor Pittsburgh, PA 15219 (US)
Priority Data:
12/902,310 12.10.2010 US
Title (EN) SELECTIVE PROTON COUPLED FOLATE TRANSPORTER AND FOLATE RECEPTOR, AND GARFTASE AND/OR OTHER FOLATE METABOLIZING ENZYMES INHIBITOR COMPOUNDS AND METHODS OF USING THE SAME
(FR) TRANSPORTEUR SÉLECTIF DE FOLATES COUPLÉS AUX PROTONS ET RÉCEPTEUR DES FOLATES, ET GARFTASE ET/OU AUTRES COMPOSÉS INHIBITEURS D'ENZYMES MÉTABOLISANT LES FOLATES ET PROCÉDÉS D'UTILISATION DE CEUX-CI
Abstract: front page image
(EN)The present invention provides selective proton coupled folate transporter and folate receptor, and glycinamide ribonucleotide formyltransferase enzyme and/or other folate metabolizing enzyme inhibitors having a fused cyclic pyrimidine compound, including tautomers thereof, and pharmaceutically acceptable salts, prodrugs, solvates and hydrates thereof. These compounds are useful in methods for treating cancer, selectively targeting cancerous cells via the proton coupled folate transporter, folate receptor alpha, and/or folate receptor beta pathways, inhibiting GARFTase and/or other folate metabolizing enzymes in cancerous cells, and selectively targeting activated macrophages in a patient having an autoimmune disease, such as rheumatoid arthritis.
(FR)La présente invention concerne un transporteur sélectif de folates couplés aux protons et un récepteur des folates, et l'enzyme glycinamide ribonucléotide formyltransférase et/ou d'autres inhibiteurs d'enzymes métabolisant les folates ayant un composé de pyrimidine cyclique fusionné, incluant les tautomères de celui-ci, et les sels, promédicaments, solvates et hydrates de ceux-ci pharmaceutiquement acceptables. Ces composés sont utiles dans des procédés de traitement du cancer, ciblant sélectivement les cellules cancéreuses via les voies du transporteur de folates couplés aux protons, du récepteur alpha du folate, et/ou du récepteur bêta du folate, en inhibant la GARFTase et/ou d'autres enzymes métabolisant les folates dans les cellules cancéreuses, et ciblant sélectivement les macrophages activés chez un patient ayant une maladie autoimmune, comme l'arthrite rhumatoïde.
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, QA, RO, RS, RU, RW, 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 (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Organization (AM, AZ, BY, KG, KZ, MD, RU, TJ, TM)
European Patent Office (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, ML, MR, NE, SN, TD, TG).
Publication Language: English (EN)
Filing Language: English (EN)