Tetrahydro-1H-cyclopenta[cd]indene derivatives as hypoxia inducible factor-2(alpha) inhibitors
AssigneeNikang Therapeutics, Inc.
InventorsJiping Fu, Yan Lou, Yigang He
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Abstract
The present disclosure provides certain tetrahydro-1H-cyclopenta[cd]indene compounds that are Hypoxia Inducible Factor 2α (HIF-2α) inhibitors and are therefore useful for the treatment of diseases treatable by inhibition of HIF-2α. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.
Claims19
A method of inhibiting or relieving cancer selected from a renal cancer, glioblastoma, neuroblastoma, paraganglioma, pheochromocytoma, pancreatic neuroendocrine tumors, colorectal cancer, somatostatinomas, hemangioblastomas, gastrointestinal stromal tumors, pituitary tumors, leiomyomas, leiomyosarcomas, polycythaemia, retinal cancers, von Hippel-Lindau disease, astrocytoma, lung cancer, melanoma, breast cancer, cervical cancer, head and neck cancer, ovarian cancer, prostate cancer, uterine leiomyomatosis, multiple myeloma, retinoblastoma, pancreatic endocrine tumors, squamous cell carcinoma, acute myeloid leukemia, myelodysplastic syndrome, and esophageal squamous cell carcinoma in a patient in need thereof which method comprises administering to the patient a therapeutically effective amount of a compound selected from the group consisting of:
- 3-fluoro-5-((1,3,3,4,4-pentafluoro-2a-hydroxy-2,2a,3,4-tetrahydro-1H-cyclopenta[cd]-inden-7-yl)oxy)benzonitrile, according to the following structure:
- 3-fluoro-5-((1,3,3,4,4-pentafluoro-2a-hydroxy-1-methyl-2,2a,3,4-tetrahydro-1H-cyclopenta[cd]inden-7-yl)oxy)benzonitrile, according to the following structure:
- 3-fluoro-5-(((1S,2aR)-1,3,3,4,4-pentafluoro-2a-hydroxy-2,2a,3,4-tetrahydro-1H-cyclopenta[cd]inden-7-yl-1,2,2-d3)oxy)benzonitrile, according to the following structure:
- and
- 3-fluoro-5-(((1S,2aR)-1,3,3,4,4-pentafluoro-2a-hydroxy-2,2a,3,4-tetrahydro-1H-cyclopenta[cd]inden-7-yl-1-d) oxy)benzonitrile-2,4,6-d3, according to the following structure:
- or
- a pharmaceutically acceptable salt thereof.
Dependencies are inferred from the claim text.