Selected Publications and Patents
2010: Maelicke A, Hoeffle-Maas A, Ludwig J, Maus A, Samochocki
M, Jordis U, Koepke A.
2010: Takata K, Kitamura Y, Saeki MS, Maelicke A, Tomimoto
H, Taniguchi T, Shimohama S.
2010: Ludwig J, Höffle-Maas A, Samochocki
M, Luttmann E, Albuquerque EX, Fels G, Maelicke A
2009: Luttman E, Ludwig J, Höffle-Maas A, Samochocki
M, Maelicke A, Fels G
2007: Maelicke A,
2007: Moser N; Mechawar N; Jones I, De Blasi M; Schroeder
H; Lindstrom J; Maelicke A; Changeux JP; Wevers A.
2006: Maelicke A
2006: Popa RV; Pereira EFR; Lopes C; Maelicke A; Albuquerque
The patent portfolio of GalantosPharma GmbH encompasses multiple inventions thatprovide the basis for international protection for the medical application of galantaminederivatives in the treatment of brain diseases.Memogain® is the key compound of interest developed and protected by Galantos.Memogain® is a pro-drug of galantamine that shows improved brain bioavailability due toconversion of the pro-drug Memogain to galantamine in the brain, enabling cognitiveenhancement and reduced side effects in patients in comparison to non-derivatizedgalantamine.
The Galantos patent portfolio encompassed originally three patent families, thefirst of which was filed prior to founding the company(WO 2007/039138 A1). The European patent EP 1 940 817 B1 was granted in July 2010 and was subsequently validated in 25 European member states.Because '817 was filed prior to Memogain being identified as the most promising candidate compound and hence did not provide sufficiently specific product protection for Memogain, this patent was allowed to lapse in 2012.
The second family of patent applications (WO 2009/127218 A1 and related applications) claims novel pro-drugs of galantaminethat are pharmacologically inactive prior to enzymatic cleavage by endogenous esterases, but leading after cleavage in the brain to release of galantamine at much higher bioavailability than could be achieved by administration of unmodified galantamine. These pro-drugs are suggested to produce higher cognition enhancement and lower (if any) gastrointestinal side effects, and also have diseasemodifying potential. WO ‘218 represents a selection invention with respect to the earlier WO ‘138 and discloses experimental details on the molecular,biochemical and preclinical properties of Memogain®, in addition to examples of the synthetic pathways of the claimed compounds. The mode of action (MoA) of the claimedcompounds is also clearly differentiated from the prior art, thereby imparting “surprisingand unexpected character” to the claimed subject matter.The European patent has recently been granted. Additional national phase applications include the USA, Canada, China, India and Japan.
The third family of patent applications encompasses a European application (EP 12178187) and a provisionalUS filing that claim selected administration methods of the compounds of WO ‘218and highly soluble salts, solutions, emulsions or powder formulations thereof. The claimedsubject matter covers the key products of GalantosPharma and focuses on transmucosaladministration of Memogain® via nasal, buccal and/or sublingual administration and suitablepharmaceutical compositions.