IP Library Granted Patent US 12686686
Granted Patent B2
US 12686686 · App. 18/157,529 · Granted Jul 21, 2026

Daphnane diterpenoid resistant to prostate cancer and preparation method thereof

Inventors: Sheng Yin (Guangdong, CN); Xuelong Yan (Guangdong, CN); Junjian Wang (Guangdong, CN); Jialuo Huang (Guangdong, CN); Guihua Tang (Guangdong, CN)
Assignee: SUN YAT-SEN UNIVERSITY
C07D491/22A61K45/06A61P35/00C07D303/32C07D491/18
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Quick Facts
Patent No.
US 12686686
App. No.
18/157,529
Granted
Jul 21, 2026
Kind
B2
Abstract

The invention relates to a daphnane diterpenoid resistant to a prostate cancer and a preparation method thereof. A daphnane diterpenoid compound as represented by formula (I) or formula (II) significantly inhibits the proliferation of various prostate cancer cells; the activities of some such compounds at a cellular level and an animal level are higher than that of the existing clinical targeting drug enzalutamide; and the daphnane diterpenoid compounds have strong synergistic effects when used in combination with the enzalutamide and are expected to become candidate drugs for treatment or adjuvant treatment of a castration-resistant prostate cancer.

Claims (85)

1 . A method for treatment or adjuvant treatment of a castration-resistant prostate cancer in a patient, comprising:

determining whether the patient suffers from the castration-resistant prostate cancer, and

administering to the patient a therapeutic amount of a daphnane diterpenoid compound of formula I or a pharmaceutically acceptable salt thereof;

wherein:

in the formula I, a bond between C-1 and C-2 is a double bond, a bond between C-6 and C-7 is a single bond, and a bond between C-15 and C-16 is a double bond;

R 1 is absent;

R 2 is carbonyl;

R 3 is hydroxyl;

R 4 is hydroxyl;

R 5 is fluorine, chlorine, bromine, or iodine;

R 6 is fluorine, chlorine, bromine, or iodine;

R 7 is phenyl;

R 8 is absent; and

R 9 is hydrogen, hydroxyl, acetyl, benzoyl, isobutyryl, butyryl, or propionyl.

2 . The method according to claim 1 , further comprising administering to the patient at least one compound having a therapeutic effect on the castration-resistant prostate cancer.

3 . The method according to claim 2 , wherein the compound having the therapeutic effect on the castration-resistant prostate cancer is selected from the group consisting of enzalutamide, abiraterone, cyclophosphamide, adriamycin, docetaxel, mitoxantrone, and combinations thereof.

4 . A method for treatment or adjuvant treatment of a castration-resistant prostate cancer in a patient, comprising

determining whether the patient suffers from the castration-resistant prostate cancer, and

administering to the patient a therapeutic amount of a daphnane diterpenoid compound of formula IV or a pharmaceutically acceptable salt thereof;

wherein the compound of formula IV is selected from the group consisting of.

Compound

R 3

R 4

R 5

R 6

R 7

R 9

YH-45

OH

OBz

βCl

αOH

Ph

OAc

YH-46

OH

OBz

αOH

βCl

Ph

OAc

YH-47

OH

OH

βCl

αOH

Ph

OAc

YH-48

OH

OH

αOH

βCl

Ph

OAc

YH-49

OH

OH

βCl

αOH

Ph

OBz

YH-50

OH

OH

αOH

βCl

Ph

OBz

YH-52

OH

OH

βBr

αOH

Ph

OBz

YH-53

OH

OH

αOH

βBr

Ph

OBz

5 . The method according to claim 4 , further comprising administering to the patient at least one compound having a therapeutic effect on the castration-resistant prostate cancer.

6 . The method according to claim 4 , wherein the compound having the therapeutic effect on the castration-resistant prostate cancer is selected from the group consisting of enzalutamide, abiraterone, cyclophosphamide, adriamycin, docetaxel, mitoxantrone, and combinations thereof.