Patent application EP20460023A (EP), filed 2020-05-13
Publication number: EP3744331A1
Title: COMBINATION OF BETULIN AND CYCLODEXTRIN FOR USE IN THE TREATMENT OF ALZHEIMER'S DISEASE
Abstract: The present invention relates to a combination of neuroprotective pentacyclic triterpenes that are used to prevent the development and treatment of Alzheimer's disease and a pharmaceutical composition containing such a compound or compounds.The invention relates to a combination of a pentacyclic triterpene compound represented by the formulawherein the R<sup>1</sup> substituent is a -OH (betulin) group with cyclodextrin, for use in the prevention of Alzheimer's disease, wherein the manufactured pharmaceutical preparation contains an effective amount of the compound.
IPC codes: A61K  31/    56            A I
A61K  47/    40            A I
A61K  47/    54            A I
A61P  25/    28            A I
Claims: number: 1
text: A compound of the pentacyclic triterpenes compound represented by the formula
number: 2
text: A compound of the pentacyclic triterpenes compound represented by the formula
number: 3
text: A pharmaceutical composition characterized in that it comprises combinations of a pentacyclic triterpene compound of the formula
Office action: search_report, dated 2020-12-02
Rejection reasons: novelty_epc_54
Prior art cited: ref_id: CN106265793A
ref_type: patent
severity: background
ref_id: WO2018133563A1
ref_type: patent
severity: background
ref_id: WO2018096039A1
ref_type: patent
severity: background
ref_id: EP2712619A1
ref_type: patent
severity: background
ref_id: KR20140101119A
ref_type: patent
severity: background
ref_id: US2011288169A1
ref_type: patent
severity: background
ref_id: - SOICA ET AL: "Betulin complex in gamma-cyclodextrin derivatives: properties and antineoplasic activities in in vitro and in vivo tumor models", INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES, vol. 13, 1 January 2012 (2012-01-01), pages 14992 - 15011, XP055712886
ref_type: npl
severity: background
ref_id: - HAI MING WANG ET AL: "A Comparison Investigation on the Solubilization of Betulin and Betulinic Acid in Cyclodextrin Derivatives", NATURAL PRODUCT COMMUNICATIONS, vol. 7, no. 3, 1 March 2012 (2012-03-01), US, XP055738170, ISSN: 1934-578X, DOI: 10.1177/1934578X1200700304
ref_type: npl
severity: background
ref_id: - FEFLEA S ET AL: "Abst P610: Betulin in formulation with ramified gamma type cyclodextrin targeting tumour cells and angiogenesis", PLANTA MEDICA, THIEME VERLAG, DE, vol. 76, no. 12, 29 August 2010 (2010-08-29), pages 1349, XP009523378, ISSN: 0032-0943, DOI: 10.1055/S-00000058
ref_type: npl
severity: background
ref_id: - VIKTORIA V. SURSYAKOVA ET AL: "Thermodynamic parameters for the complexation of water-insoluble betulin derivatives with (2-hydroxypropyl)-[gamma]-cyclodextrin determined by phase-solubility technique combined with capillary zone electrophoresis", ELECTROPHORESIS, vol. 40, no. 12-13, 8 April 2019 (2019-04-08), pages 1656 - 1661, XP055738069, ISSN: 0173-0835, DOI: 10.1002/elps.201800516
ref_type: npl
severity: background
ref_id: - MUMTAZ ALI ET AL: "Neurologically Potent Molecules from Crataegus oxyacantha; Isolation, Anticholinesterase Inhibition, and Molecular Docking", FRONTIERS IN PHARMACOLOGY, vol. 8, 7 June 2017 (2017-06-07), pages 1 - 11, XP055712877, DOI: 10.3389/fphar.2017.00327
ref_type: npl
severity: background
ref_id: - LINH MY THI LAM ET AL: "Anti-cholinesterases and memory improving effects of Vietnamese Xylia xylocarpa", CHEMISTRY CENTRAL JOURNAL, vol. 10, no. 1, 3 August 2016 (2016-08-03), pages 1 - 10, XP055712874, DOI: 10.1186/s13065-016-0197-5
ref_type: npl
severity: background
ref_id: US2011288169
ref_type: patent
severity: novelty_destroying
ref_id: KR20140101119
ref_type: patent
severity: novelty_destroying
ref_id: - SOICA ET AL, "Betulin complex in gamma-cyclodextrin derivatives: properties and antineoplasic activities in in vitro and in vivo tumor models", INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES, (20120101), vol. 13, pages 14992 - 15011, XP055712886 [X] 3 * the whole document *
ref_type: npl
severity: novelty_destroying
ref_id: - HAI MING WANG ET AL, "A Comparison Investigation on the Solubilization of Betulin and Betulinic Acid in Cyclodextrin Derivatives", NATURAL PRODUCT COMMUNICATIONS, US, (20120301), vol. 7, no. 3, doi:10.1177/1934578X1200700304, ISSN 1934-578X, XP055738170 [X] 3 * the whole document *
ref_type: npl
severity: novelty_destroying
ref_id: - FEFLEA S ET AL, "Abst P610: Betulin in formulation with ramified gamma type cyclodextrin targeting tumour cells and angiogenesis", PLANTA MEDICA, THIEME VERLAG, DE, (20100829), vol. 76, no. 12, doi:10.1055/S-00000058, ISSN 0032-0943, page 1349, XP009523378 [X] 3 * abstract *
ref_type: npl
severity: novelty_destroying
ref_id: - VIKTORIA V. SURSYAKOVA ET AL, "Thermodynamic parameters for the complexation of water-insoluble betulin derivatives with (2-hydroxypropyl)-[gamma]-cyclodextrin determined by phase-solubility technique combined with capillary zone electrophoresis", ELECTROPHORESIS, (20190408), vol. 40, no. 12-13, doi:10.1002/elps.201800516, ISSN 0173-0835, pages 1656 - 1661, XP055738069 [X] 3 * Introduction *
ref_type: npl
severity: novelty_destroying
Final disposition: pending (2020-12-02)