- Compound for targeted ubiquitination degradation of ERalpha protein and application thereof
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The invention provides a compound with estrogen receptor alpha (ERalpha) activity, and particularly provides a 1,3,5-triazine compound with a general formula (I) or a general formula (II) or a pharmaceutically acceptable salt thereof. The definitions of the groups are as described in the specification. The compound disclosed by the invention has ERalpha degradation activity and can be used for preparing medicines for treating human breast cancer and endometrial cancer.
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- 17ALPHA-SUBSTITUTED STEROIDS AS SYSTEMIC ANTIANDROGENS AND SELECTIVE ANDROGEN RECEPTOR MODULATORS
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Compounds having the structure, their salts or N-oxide derivatives: are used to treat or reduce le likelihood of acquiring androgen-dependent diseases, such as prostate cancer, benign prostatic hyperplasia, polycystic ovarian syndrome, acne, hirsutism, seborrhea, androgenic alopecia and male baldness. They can be formulated together with pharmaceutically acceptable diluent or carrier or otherwise made into any pharmaceutical dosage form. Combinations with other active pharmaceutical agents are also disclosed.
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Page/Page column 70; 72
(2008/12/08)
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- Synthesis and evaluation of B-, C-, and D-ring-substituted estradiol carboxylic acid esters as locally active estrogens
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We have synthesized derivatives of estradiol that are structurally modified to serve as "soft" estrogens and act within a geographically limited area of the body; estrogens without systemic action. We have previously shown with 16α-substituted analogues o
- Labaree, David C.,Zhang, Jing-Xin,Harris, Heather A.,O'Connor, Craig,Reynolds, Toni Y.,Hochberg, Richard B.
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p. 1886 - 1904
(2007/10/03)
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- Compounds with hydroxycarbonyl-halogenoalkyl side chain
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The present invention provides a compound consisting of a moiety and a group chemically bonded to said moiety, wherein said moiety contains a compound having low activity following oral administration or its parent scaffold and said group has the followin
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- An Anomalous Oxidation of 11α-Hydroxyoestratrienes with Pyridinium Dichromate.
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The oxidation of 3,17β-dibenzyloxy-11α-hydroxyoestra-1,3,5(10)-triene with pyridinium dichromate has been shown to yield the corresponding 9α-hydroxy-11-ketone as well as the anticipated 11-ketone.The 9β-methyl ether was obtained as a result of a methanolic work-up and is shown to arise by an acid-catalysed methanolysis of the 9α-alcohol.The stereochemistry of the 9β-methyl ether was confirmed by X-ray crystallographic analysis.
- Hanson, James R.,Hitchcock, Peter B.,Yang-zhi, Ling,Jia-yi, Tan
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p. 651 - 670
(2007/10/02)
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