The present disclosure relates to HIF-2 inhibitors and methods of making and using them for treating cancer. Certain compounds were potent in HIF-2 scintillation proximity assay, luciferase assay, and VEGF ELISA assay, and led to tumor size reduction and regression in 786-O xenograft bearing mice in vivo.

The present disclosure relates to HIF-2 inhibitors and methods of making and using them for treating cancer. Certain compounds were potent in HIF-2 scintillation proximity assay, luciferase assay, and VEGF ELISA assay, and led to tumor size reduction and regression in 786-O xenograft bearing mice in vivo.

Compounds of formula (I), wherein R.sub.1 is as defined in the claims, exhibit COMT enzyme inhibiting activity and are thus useful as COMT inhibitors. Methods of treatment and pharmaceutical dosage forms are also disclosed.

Compounds of formula (I), wherein R.sub.1 is as defined in the claims, exhibit COMT enzyme inhibiting activity and are thus useful as COMT inhibitors. Methods of treatment and pharmaceutical dosage forms are also disclosed.

This invention relates to a synthetic method for the preparation of Compound 1 and precursors thereof. Compound 1 is prepared via reaction of isoxazole 2 with phenylether (R)-3-ONa.

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This invention relates to a synthetic method for the preparation of Compound 1 and precursors thereof. Compound 1 is prepared via reaction of isoxazole 2 with phenylether (R)-3-ONa.

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The present disclosure relates to HIF-2? inhibitors and methods of making and using them for treating cancer. Certain compounds were potent in HIF-2? scintillation proximity assay, luciferase assay, and VEGF ELISA assay, and led to tumor size reduction and regression in 786-O xenograft bearing mice in vivo.

The present disclosure relates to HIF-2? inhibitors and methods of making and using them for treating cancer. Certain compounds were potent in HIF-2? scintillation proximity assay, luciferase assay, and VEGF ELISA assay, and led to tumor size reduction and regression in 786-O xenograft bearing mice in vivo.

The present invention provides a compound having a superior Toll-like receptor 4 (TLR4) signaling inhibitory action, which may be useful as a prophylactic or therapeutic drug for diseases such as autoimmune diseases and/or inflammatory diseases, or chemotherapy-induced peripheral neuropathy (CIPN), chemotherapy-induced neuropathic pain (CINP), liver failure, and ischemia reperfusion injury (IRI).

The present invention relates to ethyl 6-((2-chloro-4-fluorobenzyl)sulfonyl)-3-hydroxycyclohex-1-ene-1-carboxylate or an optical isomer thereof.

The present invention provides a compound having a superior Toll-like receptor 4 (TLR4) signaling inhibitory action, which may be useful as a prophylactic or therapeutic drug for diseases such as autoimmune diseases and/or inflammatory diseases, or chemotherapy-induced peripheral neuropathy (CIPN), chemotherapy-induced neuropathic pain (CINP), liver failure, and ischemia reperfusion injury (IRI).

The present invention relates to ethyl 6-((2-chloro-4-fluorobenzyl)sulfonyl)-3-hydroxycyclohex-1-ene-1-carboxylate or an optical isomer thereof.