US 12,448,410 B2
Derivative of sarsasapogenin, pharmaceutical composition and use thereof
Shawn Mu, Shenzhen (CN); and Na Wang, Shenzhen (CN)
Assigned to Phytovent Biopharma, Shenzhen (CN)
Appl. No. 17/279,732
Filed by Phytovent Biopharma, Shenzhen (CN)
PCT Filed May 13, 2019, PCT No. PCT/CN2019/086530
§ 371(c)(1), (2) Date Mar. 25, 2021,
PCT Pub. No. WO2020/062883, PCT Pub. Date Apr. 2, 2020.
Claims priority of application No. 201811145429.4 (CN), filed on Sep. 29, 2018.
Prior Publication US 2022/0033436 A1, Feb. 3, 2022
Int. Cl. C07J 71/00 (2006.01); A61K 31/58 (2006.01); A61K 45/06 (2006.01); A61P 35/00 (2006.01)
CPC C07J 71/0005 (2013.01) [A61K 31/58 (2013.01); A61K 45/06 (2013.01); A61P 35/00 (2018.01)] 21 Claims
 
1. A derivative of sarsasapogenin having a structure of formula I,

OG Complex Work Unit Chemistry
wherein, Z is selected from a monoheterocyclyl, a diheterocyclyl, and NR1R2, where the monoheterocyclyl or diheterocyclyl contain one or two heteroatoms selected from sulfur, oxygen, and NRa;
R1 and R2 are each independently selected from hydrogen and substituted or unsubstituted C1-C10 alkyl, or both R1 and R2 together the nitrogen of NR1R2 form a 3-8 membered ring substituted by one or more substituents selected from C1-C10 alkyl, C3-C10 cycloalkyl, C6-C20 aryl, C3-C14 heteroaryl, halogen, hydroxyl, amino, nitro, cyano, formyl, carboxyl, alkoxy, —CF3, —SF5 and 3-8 membered heterocyclyl containing one or more heteroatoms selected from sulfur, oxygen, and NRa;
Ra is independently selected from H, C1-C10 alkyl, C3-C10 cycloalkyl, C6-C20 aryl and C3-C14 heteroaryl optionally substituted with at least one substituent selected from halogen, hydroxyl, amino, nitro, cyano, formyl, carboxyl, alkoxy, —CF3, and —SF5;
X is selected from C(O) and S(O)2;
Y is selected from C(Rd)(Re), C(O), and S(O)2, wherein Rd and Re are independently selected from H, C1-C10 alkyl, C3-C10 cycloalkyl, C6-C20 aryl and C3-C14 heteroaryl, optionally substituted with at least one substituent selected from halogen, hydroxyl, amino, nitro, cyano, formyl, carboxyl, alkoxy, —CF3, and —SF5; or Rd and Re together with the carbon atom they are attached to, form a 3-8 membered ring; and
n is an integer selected from 0 to 10, and m is an integer selected from 0 and 1, with the proviso that m and n cannot both be 0;
or an enantiomer, diastereomer, tautomer, or a pharmaceutically acceptable thereof.