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1. (WO2018076537) D-3-PHOSPHOGLYCERATE DEHYDROGENASE ALLOSTERIC INHIBITOR AND USE THEREOF
Latest bibliographic data on file with the International Bureau    Submit observation

Pub. No.: WO/2018/076537 International Application No.: PCT/CN2016/113476
Publication Date: 03.05.2018 International Filing Date: 30.12.2016
IPC:
A61K 31/166 (2006.01) ,A61K 31/341 (2006.01) ,A61K 35/00 (2006.01) ,C07D 307/52 (2006.01) ,A61P 35/00 (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
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
33
Heterocyclic compounds
335
having oxygen as the only ring hetero atom, e.g. fungichromin
34
having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
341
not condensed with another ring, e.g. ranitidine, furosemide, bufetolol, muscarine
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
35
Medicinal preparations containing material or reaction products thereof with undetermined constitution
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
307
Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
02
not condensed with other rings
34
having two or three double bonds between ring members or between ring members and non-ring members
38
with substituted hydrocarbon radicals attached to ring carbon atoms
52
Radicals substituted by nitrogen atoms not forming part of a nitro radical
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35
Antineoplastic agents
Applicants: PEKING UNIVERSITY[CN/CN]; No. 5 Yiheyuan Road, Haidian District Beijing 100871, CN
Inventors: LAI, Luhua; CN
LIU, Ying; CN
WANG, Qian; CN
LIU, Pei; CN
Agent: BEIJING WANXIANGXINYUE INTELLECTUAL PROPERTY OFFICE; Room 1625, 6th Floor, Beijing Resource Yanyuan Hotel No. 1 Yiheyuan Road, Haidian District Beijing 100080, CN
Priority Data:
201610926351.431.10.2016CN
201610941898.131.10.2016CN
Title (EN) D-3-PHOSPHOGLYCERATE DEHYDROGENASE ALLOSTERIC INHIBITOR AND USE THEREOF
(FR) INHIBITEUR ALLOSTÉRIQUE DE LA D-3-PHOSPHOGLYCÉRATE DÉSHYDROGÉNASE ET SON UTILISATION
(ZH) D-3-磷酸甘油酸脱氢酶别构抑制剂及其应用
Abstract:
(EN) Disclosed are a D-3-phosphoglycerate dehydrogenase allosteric inhibitor and the use thereof, wherein one class is the benzoyl hydrazine compound for the allosteric site MDL-1 of the enzyme, and the other class is the furan compound for the allosteric site MDL-2 of the enzyme. In vitro enzymatic activity tests, cell viability tests and mouse xenograft model experiments confirm that the two classes of allosteric inhibitors can specifically inhibit the activity of D-3-phosphoglycerate dehydrogenase and delay the growth of cancer cells by reducing the overexpression of the enzyme in cancer cells. Same are used alone or in combination, or in combination with other anti-cancer drugs and can treat, prevent or inhibit tumour diseases such as breast cancer, colon cancer, melanoma and non-small cell lung cancer.
(FR) L'invention concerne un inhibiteur allostérique de la D-3-phosphoglycérate déshydrogénase et son utilisation, une classe étant le composé benzoyle hydrazine pour le site allostérique MDL-1 de l'enzyme, et l'autre classe est le composé furannique pour le site allostérique MDL-2 de l'enzyme. Des tests d'activité enzymatique in vitro, des tests de viabilité cellulaire et des expériences de modèle de xénogreffe de souris confirment que les deux classes d’inhibiteurs allostériques peuvent inhiber spécifiquement l'activité de la D-3-phosphoglycérate déshydrogénase et retarder la croissance de cellules cancéreuses en réduisant la surexpression de l'enzyme dans les cellules cancéreuses. Ceux-ci sont utilisés seuls ou en combinaison, ou en combinaison avec d'autres médicaments anticancéreux et peuvent traiter, prévenir ou inhiber des maladies tumorales telles que le cancer du sein, le cancer du côlon, le mélanome et le cancer du poumon non à petites cellules.
(ZH) 本发明公布了D-3-磷酸甘油酸脱氢酶别构抑制剂及其应用,一类是针对酶的别构位点MDL-1的苯甲酰肼类化合物,另一类是针对酶的别构位点MDL-2的呋喃类化合物。体外酶活性测试、细胞活性测试及小鼠异种移植模型实验证实,这两类别构抑制剂可特异性抑制D-3-磷酸甘油酸脱氢酶的活性,并通过降低该酶在癌细胞中的过表达延缓癌细胞的生长。它们单独或联用使用,或与其他抗癌药物组合应用,可治疗、预防或抑制乳腺癌、结肠癌、黑色素瘤及非小细胞肺癌等肿瘤疾病。
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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: Chinese (ZH)
Filing Language: Chinese (ZH)