Title:
NOVEL POMALIDOMIDE DERIVATIVE, PREPARATION METHOD THEREFOR, AND USE THEREOF
Document Type and Number:
WIPO Patent Application WO/2023/163538
Kind Code:
A1
Abstract:
The present invention relates to: a novel pomalidomide derivative exhibiting effects better than those of pomalidomide; a preparation method therefor; and use thereof. The novel pomalidomide derivative according to the present invention has excellent binding force to cereblon, has low cytotoxicity, has a low potential for causing teratogenic side effects, can regulate the expression of TNF-α and proinflammatory cytokines, and has excellent in vivo pharmacokinetic stability even while inhibiting oxidative stress, and thus is expected to exhibit effects better than those of commercial thalidomide-based drugs.
Inventors:
KIM DONG SEOK (KR)
HWANG INHO (KR)
KIM SUN (KR)
HWANG INHO (KR)
KIM SUN (KR)
Application Number:
PCT/KR2023/002638
Publication Date:
August 31, 2023
Filing Date:
February 24, 2023
Export Citation:
Assignee:
AEVIS BIO INC (KR)
International Classes:
C07D401/04; A61K31/454; A61P1/00; A61P17/06; A61P19/02; A61P25/00; A61P29/00; A61P35/00; A61P43/00
Foreign References:
| US9623020B2 | 2017-04-18 | |||
| US20110245210A1 | 2011-10-06 |
Other References:
TWEEDIE DAVID, FRANKOLA KATHRYN A., LUO WEIMING, LI YAZHOU, GREIG NIGEL H: "Thalidomide Analogues Suppress Lipopolysaccharide-Induced Synthesis of TNF-α and Nitrite, an Intermediate of Nitric Oxide, in a Cellular Model of Inflammation", THE OPEN BIOCHEMISTRY JOURNAL, vol. 5, 19 July 2011 (2011-07-19), pages 37 - 44, XP093087007, ISSN: 1874-091X, DOI: 10.2174/1874091X01105010037
SCERBA MICHAEL T., SIEGLER MAXIME A., GREIG NIGEL H.: "Thionation of Aminophthalimide Hindered Carbonyl Groups and Application to the Synthesis of 3,6′-Dithionated Pomalidomides", SYNLETT, GEORG THIEME VERLAG, DE, vol. 31, no. 09, 1 June 2021 (2021-06-01), DE , pages 917 - 922, XP093087011, ISSN: 0936-5214, DOI: 10.1055/s-0040-1720460
RUCHELMAN ALEXANDER L.; MAN HON-WAH; ZHANG WEIHONG; CHEN ROGER; CAPONE LORI; KANG JIAN; PARTON ANASTASIA; CORRAL LAURA; SCHAFER PE: "Isosteric analogs of lenalidomide and pomalidomide: Synthesis and biological activity", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, ELSEVIER, AMSTERDAM NL, vol. 23, no. 1, 1 January 2013 (2013-01-01), Amsterdam NL , pages 360 - 365, XP028961553, ISSN: 0960-894X, DOI: 10.1016/j.bmcl.2012.10.071
SCERBA MICHAEL T., SIEGLER MAXIME A., GREIG NIGEL H.: "Thionation of Aminophthalimide Hindered Carbonyl Groups and Application to the Synthesis of 3,6′-Dithionated Pomalidomides", SYNLETT, GEORG THIEME VERLAG, DE, vol. 31, no. 09, 1 June 2021 (2021-06-01), DE , pages 917 - 922, XP093087011, ISSN: 0936-5214, DOI: 10.1055/s-0040-1720460
RUCHELMAN ALEXANDER L.; MAN HON-WAH; ZHANG WEIHONG; CHEN ROGER; CAPONE LORI; KANG JIAN; PARTON ANASTASIA; CORRAL LAURA; SCHAFER PE: "Isosteric analogs of lenalidomide and pomalidomide: Synthesis and biological activity", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, ELSEVIER, AMSTERDAM NL, vol. 23, no. 1, 1 January 2013 (2013-01-01), Amsterdam NL , pages 360 - 365, XP028961553, ISSN: 0960-894X, DOI: 10.1016/j.bmcl.2012.10.071
Attorney, Agent or Firm:
ERUUM & LEEON INTELLECTUAL PROPERTY LAW FIRM (KR)
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