Title:
USE OF NOVEL POMALIDOMIDE DERIVATIVE FOR TREATING BRAIN DISEASES
Document Type and Number:
WIPO Patent Application WO/2023/163539
Kind Code:
A1
Abstract:
The present invention relates to a use of a novel pomalidomide derivative which is for treating brain diseases, and exhibits improved pharmacological effects as compared to pomalidomide. The novel pomalidomide derivative according to the present invention exhibits excellent binding to cereblon, has almost no cytotoxicity, is unlikely to cause teratogenic adverse effects, can control TNF-α expression, exibits excellent in vivo pharmacokinetic stability while suppressing oxidative stress, ameliorates a decrease in motor function which is a symptom of Parkinson's disease, and increases tyrosine hydroxylase expression which is reduced by Parkinson's disease, and thus can be used for preventing or treating brain diseases such as Parkinson's disease.
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Inventors:
KIM DONG SEOK (KR)
HWANG INHO (KR)
KIM SUN (KR)
HWANG INHO (KR)
KIM SUN (KR)
Application Number:
PCT/KR2023/002639
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. 32, 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 1900 (1900-01-01), 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. 32, 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 1900 (1900-01-01), 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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