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1. (WO2017151762) USE OF TRANS-[TETRACHLOROBIS(1H-INDAZOLE)RUTHENATE (III)] FOR THE TREATMENT OF CANCER
Latest bibliographic data on file with the International Bureau    Submit observation

Pub. No.: WO/2017/151762 International Application No.: PCT/US2017/020190
Publication Date: 08.09.2017 International Filing Date: 01.03.2017
IPC:
A01N 55/02 (2006.01) ,A61K 31/28 (2006.01) ,A61K 31/555 (2006.01) ,A61K 31/416 (2006.01) ,A61K 33/24 (2006.01) ,A61K 38/16 (2006.01) ,A61P 35/00 (2006.01) ,C07K 16/18 (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
55
Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing elements other than carbon, hydrogen, halogen, oxygen, nitrogen and sulfur
02
containing metal atoms
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
28
Compounds containing heavy metals
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
555
containing heavy metals, e.g. hemin, hematin, melarsoprol
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
41
having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
415
1,2-Diazoles
416
condensed with carbocyclic ring systems, e.g. indazole
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
33
Medicinal preparations containing inorganic active ingredients
24
Heavy metals; Compounds thereof
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
38
Medicinal preparations containing peptides
16
Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35
Antineoplastic agents
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
K
PEPTIDES
16
Immunoglobulins, e.g. monoclonal or polyclonal antibodies
18
against material from animals or humans
Applicants:
INTEZYNE TECHNOLOGIES [US/US]; 3720 Spectrum Blvd. Suite 1074 Tampa, Florida 33612, US
Inventors:
BAKEWELL, Suzanne; US
SETHURAMAN, Jyothi; US
KEPPLER, Bernhard K.; DE
Agent:
REID, Andrea L.C.; US
ARICO, Joseph W.; US
FLEMING, Paul R.; US
SCALTRITO, Donald V.; US
DECHERT LLP; One International Place, 40th Floor 100 Oliver Street Boston, Massachusetts 02110-2605, US
Priority Data:
62/301,78601.03.2016US
Title (EN) USE OF TRANS-[TETRACHLOROBIS(1H-INDAZOLE)RUTHENATE (III)] FOR THE TREATMENT OF CANCER
(FR) UTILISATION DE TRANS-[TÉTRACHLOROBIS(1H-INDAZOLE)RUTHÉNATE (III)] POUR LE TRAITEMENT DU CANCER
Abstract:
(EN) IT-139, sodium trans-[tetrachlorobis(1H-indazole)ruthenate (III)], is an intravenously administered small molecule compound. In preclinical anti-tumor and mechanism of action studies, IT-139 showed activity against a broad range of tumor types, including those which are resistant to standard anti-cancer agents (e.g., platinums, vinca alkaloids, taxanes, anthracyclines). This activity is believed to arise from IT-139's novel mechanism of action that targets the GRP78 pathway. It was found that up-regulation of GRP78 is a key cancer cell survival pathway. Downregulation of GRP78 using IT-139 removes this resistance pathway allowing for chemotherapy and immuno-oncology agents to be more effective in treating cancer.
(FR) Selon la présente invention, IT-139, trans-[tétrachlorobis(1H-indazole)ruthénate (III) de sodium], est un composé à petite molécule administré par voie intraveineuse. Dans des études précliniques anticancéreuses et de mécanisme d’action, IT-139 à présenter une activité contre une large gamme de type de tumeur, y compris celles qui sont résistantes aux agents anticancéreux standards (par exemple, platines, alcaloïdes de pervenche, taxanes, anthracyclines). Il est estimé que cette activité est liée au nouveau mécanisme d’action d’IT-139 qui cible la voie GRP78. Il a été découvert que la régulation positive de GRP78 est une voie clé de survie des cellules cancéreuses. La régulation négative de GRP78 au moyen d’IT-139 élimine cette voie de résistance, de façon à permettre que des agents chimiothérapeutiques et d’immuno-oncologie soient plus efficaces dans le traitement du cancer.
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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, 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)