US 12,331,016 B2
Multi-arm single molecular weight polyethylene glycol active derivative and application thereof
Zhen Wei, Tianjin (CN); Meina Lin, Tianjin (CN); and Xuan Zhao, Tianjin (CN)
Assigned to JenKem Technology Co., Ltd. (Tianjin), Tianjin (CN)
Filed by JENKEM TECHNOLOGY CO., LTD. (TIANJIN), Tianjin (CN)
Filed on Oct. 18, 2022, as Appl. No. 18/047,454.
Application 18/047,454 is a continuation of application No. 16/729,653, filed on Dec. 30, 2019, granted, now 11,518,728.
Application 16/729,653 is a continuation of application No. PCT/CN2018/093523, filed on Jun. 29, 2018.
Claims priority of application No. 201710523405.7 (CN), filed on Jun. 30, 2017; and application No. 201810651779.1 (CN), filed on Jun. 22, 2018.
Prior Publication US 2023/0098089 A1, Mar. 30, 2023
This patent is subject to a terminal disclaimer.
Int. Cl. C07C 59/305 (2006.01); A61K 47/54 (2017.01); A61K 47/60 (2017.01); C07C 31/20 (2006.01); C07C 31/22 (2006.01); C07C 31/24 (2006.01); C07C 59/31 (2006.01); C07C 235/08 (2006.01); C07D 303/12 (2006.01)
CPC C07C 59/305 (2013.01) [A61K 47/60 (2017.08); C07C 31/202 (2013.01); C07D 303/12 (2013.01)] 18 Claims
 
1. A multi-arm single molecular weight polyethylene glycol active derivative having the following structure:

OG Complex Work Unit Chemistry
wherein A is a core structure, and is a polyol group selected from the group consisting of pentaerythritol, oligo-pentaerythritol, glycerol and oligoglycerol, or a glyceryl ether group thereof,
X1 is a linking group selected from any one or a combination of two or more of the group consisting of —(CH2)i—, —(CH2)iO—, —(CH2)iNHCO—, —(CH2)iCONH—, —(CH2)iOCO—, and —(CH2)iCOO—, and i is an integer from 1 to 10,
R is a linking group selected from any one or a combination of two or more of the group consisting of —NHCO—, —CONH—, —OCO—, —COO—, and —O—,
X2 is a linking group selected from any one or a combination of two or more of the group consisting of —(CH2)j—, —(CH2)jO—, —(CH2)jCO—, —(CH2)jNH—, —(CH2)jNHCO—, —(CH2)jCONH—, —(CH2)jOCO— and —(CH2)jCOO—, and j is an integer from 0 to 10,
PEG has the following structure: —(CH2CH2O)m—, m is an integer from 8 to 200, and
F is the same or different —X3—Z type structure,
X3 is a linking group selected from any one or a combination of two or more of the group consisting of —(CH2)k—, —(CH2)kO—, —(CH2)kCO—, —(CH2)kNH—, —(CH2)kNHCO—, —(CH2)kCONH—, —(CH2)kNHCONH—, —(CH2)kOCO—, —(CH2)kCOO—, —(CH2)kOCOO— and —(CH2)kOCONH—, and k is an integer from 0 to 10,
Z is an active terminal group selected from any one of the group consisting of —H and

OG Complex Work Unit Chemistry
 and
n is an integer from 3 to 24.