國家衛生研究院 NHRI:Item 3990099045/9116

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Please use this identifier to cite or link to this item: http://ir.nhri.org.tw/handle/3990099045/9116

Title:	Indole compounds as inhibitors of tubulin polymerisation for the treatment of angiogenesis related disorders
Authors:	Hsieh, HP;Chang, JY;Liou, JP;Chang, CW
Contributors:	Institute of Biotechnology and Pharmaceutical Research;National Institute of Cancer Research
Abstract:	Indole compounds of the formula: \| \| wherein L \| 1 \| is CO; L \| 2 \| is a bond; R \| 1 \| is aryl or heteroaryl; R \| 2 \| is H, aryl, heteroaryl, halogen, nitro, nitroso, cyano, azide, isothionitro, OR, OC(O)R, OC(O)OR, OC(O)NRR', SO \| 2 \| R, SO \| 3 \| R, SO \| 2 \| NRR', SR, NRR', NRSO \| 2 \| NR'R'', NRSO \| 2 \| R', NRSO \| 3 \| R', NRC(O)R', NRC(O)NR'R'', NRC(C)OR', NRC(N)NR'R'', C(O)OR, C(O)NRR', an amino acid moiety, a polypeptide moiety, a carbohydrate moiety, or a PEG moiety; each of R \| a \| , R \| b \| , R \| c \| , and R \| d \| , independently, is R, halogen, nitro, nitroso, cyano, azide, isothionitro, OR, OC(O)R, OC(O)OR, OC(O)NRR', SO \| 2 \| R, SO \| 3 \| R, SO \| 2 \| NRR', SR, NRR', NRSO \| 2 \| NR'R'', NRSO \| 2 \| R', NRSO \| 3 \| R', NRC(O)R', NRC(O)NR'R'', NRC(O)OR', NRC(N)NR'R'', C(O)R, C(O)OR, C(O)NRR', OP(O)(OR)(OR'), O(CH \| 2 \| ) \| n \| OP(O)(OR)(OR'), or O(CH \| 2 \| ) \| n \| -PEG, or R \| b \| and R \| c \| , R \| a \| and R \| b \| , or R \| c \| and R \| d \| taken together are O(CH \| 2 \| ) \| n \| O; and R \| e \| is H, alkyl, alkenyl, alkynyl, cyclyl, heterocyclyl, halogen, nitro, nitroso, cyano, azide, isothionitro, OR, OC(O)R, OC(O)OR, OC(O)NRR', SO \| 2 \| R, SO \| 3 \| R, SO \| 2 \| NRR', SR, NRR', NRSO \| 2 \| NR'R'', NRSO \| 2 \| R', NRSO \| 3 \| R', NRC(O)R', NRC(O)NR'R'', NRC(O)OR', NRC(N)NR'R'', C(O)R, C(O)OR, or C(O)NRR'; in which each of R, R', and R'', independently, is H, alkyl, alkenyl, alkynyl, aryl, heteroaryl, cyclyl, or heterocyclyl; and n is 1, 2, 3, 4, or 5, as inhibitors of tubulin polymerisation useful in the treatment of angiogenesis-related disorders such as cancer. \| Indole compounds of the formula: <CHEM> wherein L1 is CO; L2 is a bond; R1 is aryl or heteroaryl; R2 is H, aryl, heteroaryl, halogen, nitro, nitroso, cyano, azide, isothionitro, OR, OC(O)R, OC(O)OR, OC(O)NRR', SO2R, SO3R, SO2NRR', SR, NRR', NRSO2NR'R'', NRSO2R', NRSO3R', NRC(O)R', NRC(O)NR'R'', NRC(C)OR', NRC(N)NR'R'', C(O)OR, C(O)NRR', an amino acid moiety, a polypeptide moiety, a carbohydrate moiety, or a PEG moiety; each of Ra, Rb, Rc, and Rd, independently, is R, halogen, nitro, nitroso, cyano, azide, isothionitro, OR, OC(O)R, OC(O)OR, OC(O)NRR', SO2R, SO3R, SO2NRR', SR, NRR', NRSO2NR'R'', NRSO2R', NRSO3R', NRC(O)R', NRC(O)NR'R'', NRC(O)OR', NRC(N)NR'R'', C(O)R, C(O)OR, C(O)NRR', OP(O)(OR)(OR'), O(CH2)nOP(O)(OR)(OR'), or O(CH2)n-PEG, or Rb and Rc, Ra and Rb, or Rc and Rd taken together are O(CH2)nO; and Re is H, alkyl, alkenyl, alkynyl, cyclyl, heterocyclyl, halogen, nitro, nitroso, cyano, azide, isothionitro, OR, OC(O)R, OC(O)OR, OC(O)NRR', SO2R, SO3R, SO2NRR', SR, NRR', NRSO2NR'R'', NRSO2R', NRSO3R', NRC(O)R', NRC(O)NR'R'', NRC(O)OR', NRC(N)NR'R'', C(O)R, C(O)OR, or C(O)NRR'; in which each of R, R', and R'', independently, is H, alkyl, alkenyl, alkynyl, aryl, heteroaryl, cyclyl, or heterocyclyl; and n is 1, 2, 3, 4, or 5, as inhibitors of tubulin polymerisation useful in the treatment of angiogenesis-related disorders such as cancer.
Date:	2011-04-06
Relation:	EP1506960/2011-04-06
Link to:	https://worldwide.espacenet.com/publicationDetails/originalDocument?FT=D&date=20110406&DB=&locale=en_EP&CC=EP&NR=1506960B1&KC=B1&ND=4
Appears in Collections:	[Hsing-Pang Hsieh] Patents [Jang-Yang Chang] Patents

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