Title:
LONG-ACTING RASAGILINE PRODRUG, PREPARATION METHOD AND USE THEREOF
Document Type and Number:
WIPO Patent Application WO/2019/037791
Kind Code:
A1
Abstract:
Provided are a long-acting rasagiline prodrug and a preparation method and use thereof. The long-acting rasagiline prodrug has a structure of formula (I), wherein, T is selected from (II) or not present; R1 and R2 are each independently selected from hydrogen, deuterium, and methyl; W is selected from (CH2)n or does not exist, n is selected from an integer from 1 to 15; X is selected from (CH2)m or not present, m is selected from an integer from 1 to 10; Y is selected from -C(=O)NH-, -NHC(=O)- or not present; R3 is selected from substituted or unsubstituted C1-C30 alkyl, substituted or unsubstituted C2-C30 alkenyl, substituted or unsubstituted C2-C30 alkynyl, substituted or unsubstituted C3-C30 cycloalkyl, cholane fatty chain, -R3a-C(＝O)O-R3b, -R3a-OC(＝O)-R3b, -R3a-C(＝O)NH-R3b, -R3a-NHC(＝O)-R3b, or -R3a-S(＝O)1-2O-R3b and -R3a-OS(＝O)1-2-R3b； The rasagiline prodrug provided has a high melting point and low solubility, and can form a drug depot in the body after being prepared into an injection and administered, thereby prolonging the release of the drug in the body and achieving a long-term treatment.
Inventors:
ZHANG JIANCUN (CN)
LI DEYAO (CN)
ZHOU YIQIAN (CN)
WU YIWU (CN)
LI DEYAO (CN)
ZHOU YIQIAN (CN)
WU YIWU (CN)
Application Number:
PCT/CN2018/102494
Publication Date:
February 28, 2019
Filing Date:
August 27, 2018
Export Citation:
Assignee:
GUANGZHOU HENOVCOM BIOSCIENCE CO LTD (CN)
International Classes:
C07C271/16; A61P25/16; A61P25/28; C07C9/00; C07C211/42
Domestic Patent References:
| WO2013088255A1 | 2013-06-20 | |||
| WO2011084846A1 | 2011-07-14 | |||
| WO1996018605A1 | 1996-06-20 | |||
| WO2013088255A1 | 2013-06-20 |
Foreign References:
| CN87101285A | 1988-08-17 | |||
| US20150210712A1 | 2015-07-30 |
Other References:
"McGraw-Hill Dictionary of Chemical Terms", 1984, MCGRAW-HILL BOOK COMPANY
ELIEL, E.WILEN, S.: "Stereochemistry of Organic Compounds", 1994, JOHN WILEY & SONS, INC.
See also references of EP 3674289A4
ELIEL, E.WILEN, S.: "Stereochemistry of Organic Compounds", 1994, JOHN WILEY & SONS, INC.
See also references of EP 3674289A4
Attorney, Agent or Firm:
LEADING INTELLECTUAL PROPERTY FIRM (CN)
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