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Title:
LACTULOSE GLYCOSIDE COMPOUND AND PREPARATION METHOD AND USE THEREOF
Document Type and Number:
WIPO Patent Application WO/2018/177381
Kind Code:
A1
Abstract:
The invention relates to the field of pharmaceutical chemistry, and particularly relates to a compound represented by formula (I), a preparation method thereof, and a medical use thereof. In the compound represented by formula (I), a lactulose group is linked to a heteroatom in an aglycone (G) through a glycosidic bond. The aglycone (G) is a group formed by removing a hydrogen atom from heteroatoms of an active drug molecule, and the lactulose group is linked to the heteroatom in the aglycone (G) through an α-glycosidic bond or a β-glycosidic bond. Drug metabolism tests proved that the lactulose glycoside compound according to the invention can pass through a mammalian gastrointestinal tract without being significantly absorbed by the gastrointestinal tract and without being significantly hydrolyzed by the endogenous enzyme of the mammalian host, such that the lactulose glycoside compound can reach a colonic region of the mammal, and the active drug can be released in the colon under the action of the colonic flora. The lactulose glycoside compound has effects of colon targeted drug delivery and can be used in the prevention or treatment of intestinal diseases.

Inventors:
ZHANG SHANCHUN (CN)
PENG JIASHI (CN)
YANG BIN (CN)
WANG YIHUA (CN)
XU MIN (CN)
WANG XIAO (CN)
CHENG KAISHENG (CN)
Application Number:
PCT/CN2018/081138
Publication Date:
October 04, 2018
Filing Date:
March 29, 2018
Export Citation:
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Assignee:
HEFEI COSOURCE PHARMACEUTICALS INC (CN)
NANJING HEQI PHARMACEUTICAL TECH CO LTD (CN)
International Classes:
C07H15/00; A61K31/7016; A61P5/44; A61P31/00; A61P35/00; C07H17/02
Domestic Patent References:
WO2015070256A12015-05-14
WO2010049432A12010-05-06
WO2011027128A12011-03-10
Foreign References:
Other References:
"Study on the oral colon-specific delivery system of 5-fluorouracil with the carrier pectin", DOCTORAL DISSERTATION, 31 December 2007 (2007-12-31), pages 1 - 133, XP009516905
See also references of EP 3604322A4
ACTA PHARMACOLOGICA SINICA, vol. 18, no. 3, 2002, pages 328 - 330
PHARMACEUTICAL JOURNAL OF CHINESE PEOPLE'S LIBERATION ARMY, vol. 17, no. 2, 2001, pages 62 - 64
CARBOHYDRATE POLYMERS, vol. 157, 2017, pages 1442 - 1450
JOURNAL OF PHARMACEUTICAL SCIENCES, vol. 90, no. 12, 2001, pages 2103 - 2112
Attorney, Agent or Firm:
CHINA SCIENCE PATENT & TRADEMARK AGENT LTD. (CN)
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