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1. (WO2010121570) METHYL CANTHARIMIDE COMPOUNDS, TREATMENT METHOD USING THEM AND THEIR PREPARATION METHOD
Latest bibliographic data on file with the International Bureau   

Pub. No.: WO/2010/121570 International Application No.: PCT/CN2010/072152
Publication Date: 28.10.2010 International Filing Date: 23.04.2010
IPC:
C07D 491/18 (2006.01) ,A61K 31/428 (2006.01) ,A61K 31/429 (2006.01) ,A61P 35/00 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
491
Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/-C07D459/290
12
in which the condensed system contains three hetero rings
18
Bridged systems
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
425
Thiazoles
428
condensed with carbocyclic 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
41
having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
425
Thiazoles
429
condensed with heterocyclic ring systems
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35
Antineoplastic agents
Applicants:
陈新滋 CHAN, Albert, Sun-chi [CN/CN]; CN (UsOnly)
邓焯安 TANG, Johnny, Cheuk-on [CN/CN]; CN (UsOnly)
林剑虹 LAM, Kim-hung [CN/CN]; CN (UsOnly)
徐宗宪 CHUI, Chung-hin [CN/CN]; CN (UsOnly)
郭汉龙 KOK, Stanton Hon Lung [CN/CN]; CN (UsOnly)
袁进华 YUEN, Marcus Chun Wah [CN/CN]; CN (UsOnly)
陈秀馨 CHAN, Sau Hing [CN/CN]; CN (UsOnly)
郑楚卿 CHENG, Chor Hing [CN/CN]; CN (UsOnly)
张斐怡 CHEUNG, Filly [CN/CN]; CN (UsOnly)
香港理工大学 THE HONG KONG POLYTECHNIC UNIVERSITY [CN/CN]; 中国香港特别行政区 九龙红磡 Hunghom, Kowloon Hong Kong, CN (AllExceptUS)
Inventors:
陈新滋 CHAN, Albert, Sun-chi; CN
邓焯安 TANG, Johnny, Cheuk-on; CN
林剑虹 LAM, Kim-hung; CN
徐宗宪 CHUI, Chung-hin; CN
郭汉龙 KOK, Stanton Hon Lung; CN
袁进华 YUEN, Marcus Chun Wah; CN
陈秀馨 CHAN, Sau Hing; CN
郑楚卿 CHENG, Chor Hing; CN
张斐怡 CHEUNG, Filly; CN
Agent:
深圳市顺天达专利商标代理有限公司 SHENZHEN STANDARD PATENT & TRADEMARK AGENT LTD.; 中国广东省深圳市 深南大道1056号银座国际大厦810-815室 Room 810-815 Yinzuo International Building No.1056 Shennan Boulevard, Futian Shenzhen, Guangdong 518040, CN
Priority Data:
12/428,48823.04.2009US
Title (EN) METHYL CANTHARIMIDE COMPOUNDS, TREATMENT METHOD USING THEM AND THEIR PREPARATION METHOD
(FR) COMPOSÉS DE CANTHARIMIDE DE MÉTHYLE, MÉTHODE DE TRAITEMENT UTILISANT CEUX-CI ET PROCÉDÉ DE PRÉPARATION DE CES COMPOSÉS
(ZH) 甲基斑蝥胺化合物及使用其的治疗方法、其制备方法
Abstract:
(EN) Methyl cantharimide compounds, the treatment method using them and their preparation method are disclosed. The methyl cantharimide compounds contain the main chain as shown by the following formula (I): wherein R1, R2, R3 and R4 are respectively selected from H, C(O)OR5, C(O)R6, C(O)NR7R8, NR9C(O) R10, N-R11R12, O-R13, S-R14, P(O) (OR15) (OR16), As(O) (OR17) (OR18), SO2R19, SO3R20 and B(OR21); X1-X4 are respectively selected from nitrogen or carbon; R1-R4 are not all hydrogen; Y1, Y2 and R5-R21 are respectively selected from hydrogen, C1-12 alkyl, aryl, heterocyclic group and a bioactive polymer. The methyl cantharimide compounds of the invention have lower cytotoxicity to normal cells and have higher cytotoxicity to cancer cells.
(FR) L'invention concerne des composés de cantharimide de méthyle, une méthode de traitement utilisant ceux-ci et un procédé de préparation de ces composés. Les composés de cantharimide de méthyle contiennent la chaîne principale représentée par la formule suivante: dans laquelle R1, R2, R3 et R4 sont sélectionnés respectivement dans le groupe comprenant H, C(O)OR5, C(O)R6, C(O)NR7R8, NR9C(O) R10, N-R11R12, O-R13, S-R14, P(O) (OR15) (OR16), As(O) (OR17) (OR18), SO2R19, SO3R20 et B(OR21); X1-X4 sont sélectionnés respectivement entre un azote et un carbone; R1-R4 ne représentent pas tous un hydrogène; Y1, Y2 et R5-R21 sont sélectionnés respectivement dans le groupe comprenant un hydrogène, un alkyle en C1-12, un aryle, un groupe hétérocyclique et un polymère bioactif. Les composés de cantharimide de méthyle de l'invention présentent une cytotoxicité réduite à l'égard des cellules normales et une cytotoxicité accrue à l'égard des cellules cancéreuses.
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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, 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, SD, SL, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Office (AM, AZ, BY, KG, KZ, MD, RU, TJ, TM)
European Patent Office (EPO) (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: Chinese (ZH)
Filing Language: Chinese (ZH)