Exam (elaborations) ) United States (12) Patent Application Publicatio

4) MOLECULES WITH SOLUBILITY TAO AND RELATED METHODS (71) Applicant: Marek Patent Gmbu, Darmstadt (DE) (72) Inventors: Carl Deutsch, I.orsch (Dli): Svcn Kelly, Seeheint-.lugenheim (Dl i): Helena Crassier, Frtutklurt Am Matn (Dli): (:hristoph Korpus, Frankfurter Am Main (DU);,loerg von llagen, Pfungstadt (DE): Ulrike Richter-Sander, Weilheim (DE) (21) Appl. No lg/245,019 (22) PCT Filed Sep. 17, 2021 (86) PCT Noc PCT/EPZ021/075699 5 371 (c)(I) (2) Date Mar. 17, 2023 (30) Foreign Application Priority Data (57) ABSTRACT The present disclosure relates to molecules wtth a solubility tag, whcrcin thc solubtltty tag compnscs a cluto-ohgosaccharidc. mtd to methods Ibr incremut the solubtltty of a molecule Moreover. the present disclosure relates to antibody-dntg cottjugates with solubility tag, methods and contpounds for preparing such mttibody-dntg conjugates. methods for increasin the solubihty of antibody-dru conjugates. antibody-dru con)ugates prepared by such methods, as ss oil tm thc usc ofsuch mtubody-drug conlu ates ut medical treatment. Publication Classiiication (51) Int. CL AGIK 47/54 (2006 01) A 6/K 49///ll (2006 01) rt 61» 47/GK (2006.01) (52) U.S. CI. CP('...467» 47/549 (2017.08): 46/K 49/pllllZ (2013.01): vlG/K 47/6051 (2017.08) Sep 17, 2020 (UP) 201')6705 6 SpeciTication includes a Sequence I.isting. G1, G2, G3 ar)d G4 eys 26 eys 24 '22 2 20 tt5 16 16 100 Time (days post tumor ir)duotiooI Patent Application Publication Feb. 22, 2024 Sheet 1 of 11 US 2024/0058456 A1 61,62, G3and 64 co 26 cn 24 9) 20 a) 18 16 100 Time (days post tumor induction) FIG. IA 61, 65, 66 and 67 cn 26 5 24 '2 3 20 a 18 16 100 Time (days post tumor induction) Patent Application Publication Feb. 22, 2024 Sheet 2 of 11 US 2024/0058456 A1 G1, GB, G9 and G10 ~ 26 ~ 24 '2 3 20 a& 18 16 100 Time (days post tumor induction) FIG. 1C