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    INTRAVITREAL MITOCHONDRIAL-TARGETED PEPTIDE PRODRUGS AND METHODS OF USE
    1.
    发明申请
    INTRAVITREAL MITOCHONDRIAL-TARGETED PEPTIDE PRODRUGS AND METHODS OF USE 审中-公开

    公开(公告)号：WO2022256377A2

    公开(公告)日：2022-12-08

    申请号：PCT/US2022/031728

    申请日：2022-06-01

    申请人： EYEDEA BIO, LLC

    发明人： GARCIA, Andres ,  LIU, Xunpei

    IPC分类号： C07K5/09 ,  A61K38/07 ,  A61K45/06 ,  A61P27/02 ,  A61K47/542 ,  C07K14/47

    摘要： Described herein are therapeutic compositions for the treatment of mitochondrial disorders, and in particular mitochondrial disorders of the eye, including age-related macular degeneration (AMD). In particular, described herein are prodrugs of mitochondrial targeted tetrapeptides that have a cleavable covalent bond (e.g., an ester bond) to a conjugation moiety, wherein the conjugation moiety of the prodrug noncovalently complexes with one or more complexation agents to form drug-complex particulates with a defined avidity, and one or more drug-complex particulates are added to and dispersed within a dispersal medium forming a multiphasic colloidal suspension that serves as an extended release drug delivery system for ocular drug delivery. This extended release drug delivery system may be injected or inserted into the eye (e.g., vitreous) to reverse and prevent mitochondrial dysfunction in the eye for one or more months without requiring retreatment.

    COSMETIC OR DERMATOLOGICAL PEPTIDE-BASED TREATMENT OF THE SKIN AND ITS INTEGUMENTS
    5.
    发明申请
    COSMETIC OR DERMATOLOGICAL PEPTIDE-BASED TREATMENT OF THE SKIN AND ITS INTEGUMENTS 审中-公开

    公开(公告)号：WO2022023406A1

    公开(公告)日：2022-02-03

    申请号：PCT/EP2021/071120

    申请日：2021-07-28

    申请人： SEDERMA

    发明人： MONDON, Philippe ,  RINGENBACH, Caroline ,  GRACIOSO, Olga

    IPC分类号： A61K8/39 ,  A61K8/64 ,  A61Q19/00 ,  A61Q1/12 ,  A61Q19/08 ,  C07K5/09 ,  C07K7/06 ,  A61K47/542

    摘要： The treatment according to the invention provides for the use of at least one peptide of general Formula X-(Xaa)nK* TSK* X'aa- (Xaa)mZ for a non-therapeutic cosmetic treatment of keratin materials of the skin and of its integuments, including treatment of the epidermis, scalp, hair, and nails. In the formula, K* is chosen from lysine, hydroxylysine, ornithine, diaminobutyric acid or diaminopropionic acid or their formyl, acetyl, trifluoroacetyl, methanesulfonyl or succinyl derivatives, the two K* possibly being identical or different; (Xaa)n and (Xaa)'m correspond independently of each other to a sequence of n or m amino acids Xaa chosen independently of each other from among G, A, P, V, L, I and F, n and m being integers which may be equal or different between 0 and 5; X'aa corresponds to S or T, at the N-terminus X chosen from H, -CO-R1, -SO2-R1 or a biotinoyl group; at the C -terminal Z end chosen from OH, OR1, N2, NHR1 or NR1R2: and R1 and R2 being, independently of one another, chosen from an alkyl, aryl, aralkyl, alkylaryl, alkoxy, saccharide and aryloxy group, which may be linear, branched, cyclic, polycyclic, unsaturated, hydroxyl, carbonyl, phosphoryl and/or sulfurised, said group having from 1 to 24 carbon atoms and possibly having in its backbone an O, S and / or N heteroatom. A preferred peptide is the Pal- KTSKS.

    LIGAND DRUG CONJUGATES AND MODIFIED BET INHIBITORS
    7.
    发明申请
    LIGAND DRUG CONJUGATES AND MODIFIED BET INHIBITORS 审中-公开

    公开(公告)号：WO2021140343A1

    公开(公告)日：2021-07-15

    申请号：PCT/GB2021/050058

    申请日：2021-01-11

    申请人： HOVIONE SCIENTIA LIMITED ,  TURNER, Craig

    发明人： TRAQUETE, Rui Miguel Petrucci Albuquerque ,  BERNARDES, Gonçalo José Lopes

    IPC分类号： A61K47/54 ,  A61P35/00 ,  A61K47/542

    摘要： A ligand drug conjugate comprising a) a targeting ligand; b) a cleavable bridge; and a bromodomain and extraterminal (BET) inhibitor is provided. The targeting ligand may comprise a cancer targeting ligand. The BET inhibitor may comprise I-BET762, (+)-JQ1, MS417, OXT015, (2), RVX-208, (3), OXFBD02, OXFBD03, I-BET151, (4), PFI-1, I-BET726, MS436, XD14 or a modified BET inhibitor. Modified BET inhibitors are also provided, including RT48 ((S) -2- (6-(4-chlorophenyl)-8-methoxy-1-methyl-4H-benzo[f] [1,2,4] triazolo [4,3-a] [1,4] diazepin-4-yl)-1-(4-(dimethylamino) piperidin-1-yl) ethan-1-one) and RT53 ((S) -2- (6- (4-chlorophenyl) -8-methoxy-1-methyl-4H-benzo[f] [1,2,4] triazolo [4,3-a] [1,4] diazepin-4-yl) -N-(4- (4- (dimethylamino) piperidin-1-yl) phenyl) acetamide). A pro-drug of a BET inhibitor is also provided. A method of preparing a ligand drug conjugate according to the invention is also provided. The method comprises i) functionalising a BET inhibitor with a tertiary amine to form a modified BET inhibitor according to the invention; ii) bonding the modified BET inhibitor formed in step i) to a cleavable bridge; and iii) bonding the cleavable bridge bound to the modified BET inhibitor formed in step ii) to a targeting ligand. A ligand drug conjugate according to the invention for use as a medicament is also provided.