NOVEL S1P1 RECEPTOR AGONIST, CRYSTALLINE SALTS, PROCESSES FOR PREPARING, AND USES RELATED THERETO

    公开(公告)号:US20250034090A1

    公开(公告)日:2025-01-30

    申请号:US18841455

    申请日:2023-03-07

    Abstract: The present invention relates to crystalline salts of (R)-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclo-penta[b]indol-3-yl)acetic acid, and pharmaceutical compositions comprising them that are useful as SiP1 receptor modulator. The compound (R)-2-(9-chloro-7-(4-isopropoxy-3-(trifluoromethyl)benzyloxy)-2,3-dihydro-1H-pyrrolo[1,2-a]indol-1-yl)acetic acid identified as an SiP1 receptor modulator is useful in the treatment of SiP1 receptor-associated disorders, for example, diseases and disorders mediated by lymphocytes, transplant rejection, autoimmune diseases and disorders, inflammatory diseases and disorders (e.g., acute and chronic inflammatory conditions), cancer, and conditions characterized by an underlying defect in vascular integrity or that are associated with angiogenesis such as may be pathologic (e.g., as may occur in inflammation, tumor development, and atherosclerosis).

    METHODS OF TREAMENT
    4.
    发明公开
    METHODS OF TREAMENT 审中-公开

    公开(公告)号:US20240216392A1

    公开(公告)日:2024-07-04

    申请号:US18524124

    申请日:2023-11-30

    CPC classification number: A61K31/5517 A61P25/08

    Abstract: Provided herein are treatment methods including administering a 5-hydroxytryptamine (HT)2C receptor agonist to a patient in need thereof. An exemplary method includes treating or preventing a 5-hydroxytryptamine (HT)2C receptor-associated disorder in a patient in need thereof, wherein the method comprises administering to the patient (R)—N-(2,2-difluoroethyl)-7-methyl-1,2,3,4,6,7-hexahydro-[1,4]diazepino[6,7,1-hi]indole-8-carboxamide (Compound 1), or a pharmaceutically acceptable salt thereof, wherein Compound 1, or a pharmaceutically acceptable salt thereof, is administered twice daily.

    Compounds useful in the treatment of autoimmune and inflammatory disorders

    公开(公告)号:US11555015B2

    公开(公告)日:2023-01-17

    申请号:US17273681

    申请日:2019-09-05

    Abstract: The present invention relates to certain compounds of Formula (Ia) and pharmaceutically acceptable salts thereof, which exhibit useful pharmacological properties, for example, as agonists of the S1P1 receptor: Also provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the treatment of S1P1 receptor-associated disorders, for example, a disease or disorder mediated by lymphocytes, an autoimmune disease or disorder, an inflammatory disease or disorder, an inflammatory skin disease or disorder, cancer, psoriasis, atopic dermatitis, rheumatoid arthritis, Crohn's disease, transplant rejection, multiple sclerosis, systemic lupus erythematosus, ulcerative colitis, type I diabetes, and acne, microbial infections or diseases and viral infections or diseases.

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