130064-26-5Relevant articles and documents
NOVEL BENZOPYRAN COMPOUNDS, COMPOSITIONS AND USES THEREOF
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, (2013/07/05)
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.
Benzopyran-containing compounds and prodrug forms thereof
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Example 1, (2008/06/13)
Certain benzopyran antiestrogens are disclosed for treating estrogen sensitive diseases such as breast cancer. Prodrug forms provide ease of manufacturing, good shelf life, and bioavailibility.
Structure-Activity Relationship of Antiestrogens. Phenolic Analogues of 2,3-Diaryl-2H-1-benzopyrans
Sharma, Arun P.,Saeed, Ashraf,Durani, Susheel,Kapil, Randhir S.
, p. 3222 - 3229 (2007/10/02)
Phenolic analogues of 2--3-phenyl-2H-1-benzopyran (1), a novel antiestrogen, were synthesized and evaluated for their structure-activity relationship.Incorporation of OH at position 7 was found to improve receptor affinity of