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Title:
PYRROLOBENZODIAZEPINE DERIVATIVE AND LIGAND-LINKER CONJUGATE THEREOF
Document Type and Number:
WIPO Patent Application WO/2021/137646
Kind Code:
A1
Abstract:
The present invention relates to a pyrrolobenzodiazepine derivative compound, a conjugate thereof with a ligand, and a use thereof, wherein the pyrrolobenzodiazepine derivative compound is more stable in plasma and is also stable in circulation, and exhibits excellent efficacy. In particular, the conjugate with a ligand adopts linker technology, which can maximize the medicinal effect of a drug by allowing the drug to be easily released in cancer cells, thus allowing the conjugate to more reliably reach target cells and effectively exhibit a medicinal effect, while significantly reducing toxicity. Thus, the invention has the great advantage of enabling the targeting of proliferative diseases such as cancer, disease-specific treatments, maximization of medicinal effects, and minimization of side effects.

Inventors:
SONG HO YOUNG (KR)
PARK YUN-HEE (KR)
LEE KUN JUNG (KR)
OH JI HYE (KR)
KIM SUNG MIN (KR)
PARK KYUNG EUN (KR)
PARK YONG GYU (KR)
RYU HYUN MIN (KR)
HAN NA RA (KR)
CHUNG CHUL WOONG (KR)
CHAE JEI WOOK (KR)
KIM YONG ZU (KR)
Application Number:
PCT/KR2020/019466
Publication Date:
July 08, 2021
Filing Date:
December 30, 2020
Export Citation:
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Assignee:
LEGOCHEM BIOSCIENCES INC (KR)
International Classes:
C07H15/26; A61K31/7056; A61P35/00
Domestic Patent References:
WO2007039752A12007-04-12
Foreign References:
US20170333442A12017-11-23
KR20180110645A2018-10-10
Other References:
G. BARALDI ET AL.: "Synthesis, in Vitro Antiproliferative Activity, and DNA-Binding Properties of Hybrid Molecules Containing Pyrrolo(2,1-c)(1,4)benzodiazepine and Minor-Groove-Binding Oligopyrrole Carriers", JOURNAL OF MEDICINAL CHEMISTRY, AMERICAN CHEMICAL SOCIETY, vol. 42, no. 25, 1 January 1999 (1999-01-01), pages 5131 - 5141, XP002272006, ISSN: 0022-2623, DOI: 10.1021/jm991033w
ROHTASH KUMAR, REDDY B.S.NARAYAN, LOWN J.WILLIAM: "Design and Synthesis of Novel Pyrrolo[2,1-c][1,4]benzodiazepine - Imidazole Containing Polyamide Conjugates", HETEROCYCLIC COMMUNICATIONS., DE GRUYTER, DE, vol. 8, no. 1, 1 January 2002 (2002-01-01), DE, pages 19 - 26, XP055409277, ISSN: 0793-0283, DOI: 10.1515/HC.2002.8.1.19
GEORGE VARVOUNIS: "An Update on the Synthesis of Pyrrolo[1,4]benzodiazepines", MOLECULES, vol. 21, no. 2, pages 154, XP055558979, DOI: 10.3390/molecules21020154
YALAMATI DAMAYANTHI, B. S. PRAVEEN REDDY, J. WILLIAM LOWN: "Design and Synthesis of Novel Pyrrolo[2,1- c ][1,4]benzodiazepine‚ąíLexitropsin Conjugates", THE JOURNAL OF ORGANIC CHEMISTRY, AMERICAN CHEMICAL SOCIETY, vol. 64, no. 1, 1 January 1999 (1999-01-01), pages 290 - 292, XP055409275, ISSN: 0022-3263, DOI: 10.1021/jo9812072
Attorney, Agent or Firm:
HANSUNG INTELLECTUAL PROPERTY (KR)
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