- A selective estrogen receptor modulator for the treatment of hot flushes
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A selective estrogen receptor modulator (SERM) for the potential treatment of hot flushes is described. (R)-(+)-7,9-difluoro-5-[4-(2-piperidin-1-ylethoxy) phenyl]-5H-6-oxachrysen-2-ol, LSN2120310, potently binds ERα and ERβ and is an antagonist in MCF-7 b
- Wallace, Owen B.,Lauwers, Kenneth S.,Dodge, Jeffrey A.,May, Scott A.,Calvin, Joel R.,Hinklin, Ronald,Bryant, Henry U.,Shetler, Pamela K.,Adrian, Mary D.,Geiser, Andrew G.,Sato, Masahiko,Burris, Thomas P.
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p. 843 - 846
(2007/10/03)
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- A selective estrogen receptor modulator designed for the treatment of uterine leiomyoma with unique tissue specificity for uterus and ovaries in rats
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The design of a novel selective estrogen receptor modulator (SERM) for the potential treatment of uterine leiomyoma is described. 16 (LY2066948-HCl) binds with high affinity to estrogen receptors α and β (ERα and ERβ, respectively) and is a potent uterine
- Hummel, Conrad W.,Geiser, Andrew G.,Bryant, Henry U.,Cohen, Ilene R.,Dally, Robert D.,Fong, Kin Chiu,Frank, Scott A.,Hinklin, Ronald,Jones, Scott A.,Lewis, George,McCann, Denis J.,Rudmann, Daniel G.,Shepherd, Timothy A.,Tian, Hongqi,Wallace, Owen B.,Wang, Minmin,Wang, Yong,Dodge, Jeffrey A.
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p. 6772 - 6775
(2007/10/03)
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- SELECTIVE ESTROGEN RECEPTOR MODULATORS
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The present invention relates to a selective estrogen receptor modulators of formula I (I); or a pharmaceutical acid addition salt thereof; and of formula II (II); or a pharmaceutical salt thereof; useful, e.g., for treating endometriosis and/or uterine leiomyoma/leiomyomata.
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Page/Page column 40-42
(2010/02/13)
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- SELECTIVE ESTROGEN RECEPTOR MODULATORS FOR THE TREATMENT OF VASOMOTOR SYMPTOMS
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The present invention relates to a selective estrogen receptor modulator of formula I or Ia: (I) (Ia); or a pharmaceutical acid addition salt thereof; useful for treating vasomotor symptoms, in particular hot flashes, night sweats and other symptoms that affect women around menopause.
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Page/Page column 57-58
(2008/06/13)
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- SELECTIVE ESTROGEN RECEPTOR MODULATORS
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The present invention relates to a selective estrogen receptor modulator of formula I: I; or a pharmaceutical acid addition salt thereof; useful, e.g., for treating endometriosis and uterine leiomyoma. X16065 PCT - -
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Page/Page column 11-12
(2010/02/13)
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- DERIVATIVE OF DIHYDRO-DIBENZO (A) ANTHRACENES AND THEIR USE AS SELECTIVE ESTROGEN RECEPTOR MODULATORS
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The present invention provides a compound of the formula (I) wherein R1 is -H, -OH, -O(C1-C4 alkyl), -OCOC6H5, -OCO(C1-C6 alkyl), or -OSO2(C2-C6
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- DIHYDRO-DIBENZO[B,E]OXEPINE BASED SELECTIVE ESTROGEN RECEPTOR MODULATORS, COMPOSITIONS AND METHODS
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The present invention provides a compound of the formula (I) wherein R1 is -H, -OH, -O(C1-C4 alkyl), -OCOC6H5, -OCO(C1-C6 alkyl), or -OSO2(C2-C6
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- PENTACYCLIC OXEPINES AND DERIVATIVES THEREOF, COMPOSITIONS AND METHODS
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The present invention provides a compound of the formula (I) wherein R1 is -H, -OH, -O(C1-C4 alkyl), -OCOC6H5, -OCO(C1-C6 alkyl), or -OSO2(C2-C6 alkyl); R0, R2 and R3 are each independently -H, -OH, -O(C1-C4 alkyl), -OCOC6H5, -OCO(C1-C6 alkyl), -OSO2(C2-C6 alkyl) or halo; R4 is 1-piperidinyl, 1-pyrrolidinyl, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidinyl, 4-morpholino, dimethylamino, diethylamino, diisopropylamino, or 1-hexamethyleneimino; n is 2 or 3 X is -S- or -HC=CH-; G is -O-, -S-, -SO-, SO2, or -N(R5)-, wherein R5 is -H or C1-C4 alkyl; and Y is -O-, -S-, -NH-, -NMe-, or -CH2-; or a pharmaceutically acceptable salt thereof; pharmaceutical compositions thereof, optionally in combination with estrogen and progestin; methods of inhibiting a disease associated with estrogen deprivation; and methods for inhibiting a disease associated with an aberrant physiological response to endogenous estrogen.
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- SELECTIVE ESTROGEN RECEPTOR MODULATORS CONTAINING A PHENYLSULFONYL GROUP
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The present invention relates to a selective estrogen receptor modulator of formula I or a pharmaceutical acid addition salt thereof; useful, e.g., for treating endometriosis and/or uterine leiomyoma/leiomyomata.
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Page/Page column 68
(2008/06/13)
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