1443753-08-9

Basic information

• Product Name: 2-(4-iodophenyl)-4-methyl-7-((tetrahydro-2H-pyran-2-yl)oxy)-3-(4-((tetrahydro-2H-pyran-2-yl)oxy)phenyl)chroman-4-ol
• Synonyms: 2-(4-iodophenyl)-4-methyl-7-((tetrahydro-2H-pyran-2-yl)oxy)-3-(4-((tetrahydro-2H-pyran-2-yl)oxy)phenyl)chroman-4-ol
• CAS NO: 1443753-08-9
• Molecular Weight: 642.531
• Mol File: 1443753-08-9.mol

Chemical Properties

• CAS DataBase Reference: 2-(4-iodophenyl)-4-methyl-7-((tetrahydro-2H-pyran-2-yl)oxy)-3-(4-((tetrahydro-2H-pyran-2-yl)oxy)phenyl)chroman-4-ol(CAS DataBase Reference)
• NIST Chemistry Reference: 2-(4-iodophenyl)-4-methyl-7-((tetrahydro-2H-pyran-2-yl)oxy)-3-(4-((tetrahydro-2H-pyran-2-yl)oxy)phenyl)chroman-4-ol(1443753-08-9)
• EPA Substance Registry System: 2-(4-iodophenyl)-4-methyl-7-((tetrahydro-2H-pyran-2-yl)oxy)-3-(4-((tetrahydro-2H-pyran-2-yl)oxy)phenyl)chroman-4-ol(1443753-08-9)

Safety Data

• Hazardous Substances Data: 1443753-08-9(Hazardous Substances Data)

Upstream product

• 67804-60-8 1-(2,4-dimethoxyphenyl)-2-(4-methoxyphenyl)ethanone 
• 829-20-9 2',4'-dimethoxyacetophenone 
• 104-92-7 1-bromo-4-methoxy-benzene 
• 15164-44-0 p-(iodophenyl)carboxaldehyde 
• 130064-21-0 1-(2-hydroxy-4-((tetrahydro-2H-pyran-2-yl)oxy)phenyl)-2-(4-((tetrahydro-2H-pyran-2-yl)oxy)phenyl)ethanone 
• 17720-60-4 2,4,4'-trihydroxy deoxybenzoin 
• 156-38-7 4-hydroxyphenylacetate 
• 108-46-3 recorcinol 

Downstream Products

• 1352307-39-1 3-(4-hydroxyphenyl)-4-methyl-2-(4-((S)-2-((R)-3-methylpyrrolidin-1-yl)propoxy)phenyl)-2H-chromen-7-ol trifluoroacetate 
• 1443752-88-2 C₂₉H₃₃NO₁₀P₂ 
• 1443752-91-7 C₂₉H₃₃NO₁₀P₂ 
• 1443752-92-8 C₃₉H₄₇NO₆ 
• 1443752-93-9 C₃₅H₃₉NO₈ 
• 1443752-90-6 C₂₉H₃₁NO₅ 
• 1443752-79-1 (2S)-3-(4-hydroxyphenyl)-4-methyl-2-(4-{2-[(3R)-3-methylpyrrolidin-1-yl]ethoxy}phenyl)-2H-chromen-7-ol hydrochloride 
• 1443752-76-8 (2S)-3-(4-hydroxyphenyl)-4-methyl-2-(4-{2-[(3R)-3-methylpyrrolidin-1-yl]ethoxy}phenyl)-2H-chromen-7-ol 
• 1443752-77-9 (2R)-3-(4-hydroxyphenyl)-4-methyl-2-(4-{2-[(3R)-3-methylpyrrolidin-1-yl]ethoxy}phenyl)-2H-chromen-7-ol 
• 1443773-75-8 (3R)-3-methyl-1-(2-(4-(4-methyl-7-((tetrahydro-2H-pyran-2-yl)oxy)-3-(4-((tetrahydro-2H-pyran-2-yl)oxy)phenyl)-2H-chromen-2-yl)phenoxy)ethyl)pyrrolidine 
• 1443753-05-6 2-(4-iodophenyl)-4-methyl-7-((tetrahydro-2H-pyran-2-yl)oxy)-3-(4-((tetrahydro-2H-pyran-2-yl)oxy)phenyl)-2H-chromene 
• 1443753-04-5 3-(4-hydroxyphenyl)-2-(4-iodophenyl)-4-methyl-2H-chromen-7-ol 
• 1443752-89-3 C₃₃H₃₅NO₈ 

Relevant articles and documents

Identification of an Orally Bioavailable Chromene-Based Selective Estrogen Receptor Degrader (SERD) That Demonstrates Robust Activity in a Model of Tamoxifen-Resistant Breast Cancer

About 75% of breast cancers are estrogen receptor alpha (ER-α) positive, and women typically initially respond well to antihormonal therapies such as tamoxifen and aromatase inhibitors, but resistance often emerges. Fulvestrant is a steroid-based, selective estrogen receptor degrader (SERD) that both antagonizes and degrades ER-α and shows some activity in patients who have progressed on antihormonal agents. However, fulvestrant must be administered by intramuscular injections that limit its efficacy. We describe the optimization of ER-α degradation efficacy of a chromene series of ER modulators resulting in highly potent and efficacious SERDs such as 14n. When examined in a xenograft model of tamoxifen-resistant breast cancer, 14n (ER-α degradation efficacy = 91%) demonstrated robust activity, while, despite superior oral exposure, 15g (ER-α degradation efficacy = 82%) was essentially inactive. This result suggests that optimizing ER-α degradation efficacy in the MCF-7 cell line leads to compounds with robust effects in models of tamoxifen-resistant breast cancer derived from an MCF-7 background.

ANTI-ESTROGENIC COMPOUNDS

The present disclosure provides a compound of Formula I: or a pharmaceutically acceptable salt wherein X, R1-R8, Y1-Y5, m, n, p, and q are defined herein. The novel 2H-chromene compounds are useful for the modul

COMBINATIONS OF BENZOPYRAN COMPOUNDS, COMPOSITIONS AND USES THEREOF

This invention relates to a method of treating a disorder modulated, mediated or affected by the estrogen receptor in a subject comprising administering to the subject a specific benzopyran (in the form of a mixture of S-C2 and R-C2 diastereomers or its pure S-diastereomer) in combination with an agent selected from the group consisting of an mTOR inhibitor, a CDK 4/6 inhibitor, a PI3 Kinase inhibitor, a taxane, an antimetabolite, and an antitumor antibiotic.

SUBSTITUTED BENZOPYRAN COMPOUNDS, COMPOSITIONS AND USES THEREOF

Benzopyran compounds with anti-estrogenic activity are provided as Formula I, II, III, IV, V, VI, VII, VIII, IX, X, XI, XII, XIII, XIV, XV, XVI, XVII and XVIII. These compounds are useful for the treatment or prevention of a variety of conditions that are modulated through the estrogen receptor in mammals including humans.

NOVEL BENZOPYRAN COMPOUNDS, COMPOSITIONS AND USES THEREOF

Benzopyran compounds with strong anti-estrogenic activity and essentially no estrogenic activity are provided, which are OP- 1038, which is 3-(4-hydroxyphenyl)-4-methyl-2-(4-{2-[(3R)-3-methylpyrrolidin-l-yl]ethoxy}phenyl)-2H-chromen-7-ol, and OP-1074, which is (2S)-3-(4-hydroxyphenyl)-4-methyl-2-(4-{2-[(3R)-3-methylpyrrolidin- 1 -yl]ethoxy}phenyl)-2H-chromen-7-ol. OP-1074 is a pure anti-estrogen when tested in the agonist mode and a complete anti-estrogen when tested in the antagonist mode. These compounds are useful for the treatment or prevention of a variety of conditions that are modulated through the estrogen receptor in mammals including humans.