TREATMENT OR PREVENTION OF LEUKAEMIA
    4.
    发明公开

    公开(公告)号:US20240299349A1

    公开(公告)日:2024-09-12

    申请号:US17768631

    申请日:2020-10-14

    CPC classification number: A61K31/403 A61K31/09 A61K31/136

    Abstract: The present invention provides compounds for use in the treatment or prevention of leukaemia which are based on a 2-amino-[1,1′]-biphenyl or corresponding carbazole scaffold, in particular, it provides the following compounds of formula (I), their stereoisomers, and their pharmaceutically acceptable salts for use in such treatment: (I) (I) wherein: Y is selected from C=0 and —CR9 (in which R9 is H, —OH or —O-alkyl, (e.g., —O—C1-6 alkyl)); Z is selected from C=0 and —CR10 (in which R10 is H, —OH, —O-alkyl, (e.g., —O—C1-4 alkyl) or —O—C(O)RA wherein RA is H or alkyl (e.g. C1-4 alkyl)); R1 is —NO2 or —NR11R12 (wherein R11 and R12 are both H, or R11 is H and R12 is a group of the formula —C(O)RA in which RA is H or alkyl (e.g. C1-6 alkyl)); each of R2, R4, and R6 to R8 are independently selected from H, alkyl (e.g. C1-6 alkyl), —O-alkyl (e.g. —O—C1-6 alkyl), and halogen; R3 and R5 are independently selected from H, —O-alkyl (e.g. —O—C1-6 alkyl), and halogen; or R1 and R8 together form a group NR13 (in which R13 is H, alkyl (e.g. C1-6 alkyl), or a group of the formula —C(O)RA in which RA is H or alkyl (e.g. G1-6 alkyl)); and represents an optional bond between two adjacent carbon atoms in the ring; with the proviso that when Y and Z are both C═O, and R1 and R8 together form a group NR13, at least one of R2 and R3 is other than H or —CH3. Such compounds find particular use in the treatment or prevention of chronic myeloid leukaemia (GML), acute myeloid leukaemia (AML), acute lymphocytic leukaemia (ALL) or t-ALL (T-cell acute lymphoblastic leukaemia).

    THERAPEUTICS FOR KELOIDS AND OTHER FIBROTIC DISORDERS

    公开(公告)号:US20240216372A1

    公开(公告)日:2024-07-04

    申请号:US18398315

    申请日:2023-12-28

    Abstract: This disclosure relates to pharmaceutical compositions comprising one or more therapeutic agents selected from a SERPINE1 serine protease inhibitor, a histone acetyltransferase inhibitor, a histone deacetylase inhibitor, an insulin-like growth factor inhibitor, an anti-hypertensive agent, a topoisomerase II inhibitor, a tyrosine kinase inhibitor, an agent that downregulates growth factors or any combination thereof, and methods of treating fibrotic disorders, including keloid, pulmonary fibrosis, hepatic fibrosis, cardiac fibrosis, renal fibrosis, mediastinal fibrosis, retroperitoneal cavity fibrosis, bone marrow fibrosis, and/or scleroderma using the same. The disclosed methods can be accompanied by application of radiation and/or surgical resection. For treating keloids, the compositions can be formulated topically and do not cause systemic side effects. For treating fibrotic diseases of internal organs, the compositions can be administered systemically or delivered to the affected organs. The compositions can include two or more therapeutic agents that work synergistically, allowing lower doses of each therapeutic agent.

Patent Agency Ranking