PE20030411A1 - 8ß-SUBSTITUTED DERIVATIVES OF 11ß-FENYL AND 11ß-HEXIL-ESTRA-1,3,5 (10) -TRIENE THAT HAVE AFFINITY FOR ESTROGEN RECEPTORS - Google Patents

8ß-SUBSTITUTED DERIVATIVES OF 11ß-FENYL AND 11ß-HEXIL-ESTRA-1,3,5 (10) -TRIENE THAT HAVE AFFINITY FOR ESTROGEN RECEPTORS

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Publication number
PE20030411A1
PE20030411A1 PE2001001011A PE2001001011A PE20030411A1 PE 20030411 A1 PE20030411 A1 PE 20030411A1 PE 2001001011 A PE2001001011 A PE 2001001011A PE 2001001011 A PE2001001011 A PE 2001001011A PE 20030411 A1 PE20030411 A1 PE 20030411A1
Authority
PE
Peru
Prior art keywords
estra
r19so2o
ocor22
halogen
alkyl
Prior art date
Application number
PE2001001011A
Other languages
Spanish (es)
Inventor
Olaf Peters
Nico Brauer
Alexander Hillisch
Christa Hegele-Hartung
Karl-Heinrich Fritzemeier
Original Assignee
Schering Ag
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Schering Ag filed Critical Schering Ag
Priority to PE2001001011A priority Critical patent/PE20030411A1/en
Publication of PE20030411A1 publication Critical patent/PE20030411A1/en

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Abstract

SE REFIERE A DERIVADOS 8ß-SUSTITUIDOS DE 11ß-FENIL Y 11ß-HEXIL-ESTRA-1,3,5(10)-TRIENO DE FORMULA I DONDE R2 ES H, HALOGENO, R18, OR18; R18 ES H, ALQUILO, ACILO, TRIFLUOROMETILO, R19SO2O, R19 ES R20R21N; R20 Y R21 SON H, ALQUILO C1-C5, COR22; R22 ES CICLOALQUILO C3-C7, ARILO, HETEROARILO, ARALQUILO, POLIMETILENIMINO, MORFOLINO; R3 ES R18O, R19SO2, OCOR22; R6 Y R6' SON H O UNO FORMA CON R7 UN ENLACE; R7 Y R7' SON H; R8 ES ALQUILO, ALQUENILO, ETINILO C1-C5, PROP-1-INILO; R14 ES H, FORMA UN ENLACE CON R15; R15 ES H, FORMA UN ENLACE CON R14 O R16; R15' Y R16' SON H, HALOGENO, R18O, R19SO2O, OCOR22; R17' Y R17 SON H, H Y HALO, H Y BENCILOXI, H Y R19SO2O, R18-O, OCOR22, JUNTOS SON =CR23R24; R23 Y R24 SON H, HALOGENO, O. SON COMPUESTOS PREFERIDOS 8ß-METIL-11ß-PENTIL-1,3,5(10)-TRIEN-3,17ß-DIOL, 11ß-PENTIL-8ß-VINIL-ESTRA-1,3,5(10)-TRIEN-3,17ß-DIOL, ENTRE OTROS. TAMBIEN SE REFIERE A UNA COMPOSICION QUE COMPRENDE ADEMAS ANTAGONISTAS DE GnRH, ANTAGONISTAS DE RECEPTORES DE PROGESTERONA, MESOPROGESTINAS, GESTAGENOS, GESTAGENOS SELECTIVOS DE TEJIDOS. LOS COMPUESTOS TIENEN AFINIDAD POR RECEPTORES DE ESTROGENO, INHIBEN LA GENERACION DEL FOLICULO, OVULACION PUDIENDO SER UTILES COMO ANTICONCEPTIVOS, O PARA CONTRACEPTIVOS EN EL HOMBRE, Y PARA EL TRATAMIENTO DE ENFERMEDADES OVARICAS PROLIFERATIVAS, BENIGNAS, MALIGNAS, CARCINOMAS OVARICOS, TUMORES CELULARES DE GRANULOSAREFERS TO 8ß-SUBSTITUTED DERIVATIVES OF 11ß-FENYL AND 11ß-HEXIL-ESTRA-1,3,5 (10) -TRIENE OF FORMULA I WHERE R2 IS H, HALOGEN, R18, OR18; R18 IS H, ALKYL, ACILO, TRIFLUOROMETHYL, R19SO2O, R19 IS R20R21N; R20 AND R21 ARE H, C1-C5 ALKYL, COR22; R22 IS C3-C7 CYCLOALKYL, ARYL, HETEROARYL, ARALKYL, POLYMETHYLENIMINE, MORPHOLINE; R3 IS R18O, R19SO2, OCOR22; R6 AND R6 'ARE H O ONE FORM WITH R7 A LINK; R7 AND R7 'ARE H; R8 IS ALKYL, ALKENYL, C1-C5 ETHINYL, PROP-1-INYL; R14 IS H, FORMS A LINK WITH R15; R15 IS H, FORMS A LINK WITH R14 OR R16; R15 'AND R16' ARE H, HALOGEN, R18O, R19SO2O, OCOR22; R17 'AND R17 ARE H, H AND HALO, H AND BENZYLOXY, H AND R19SO2O, R18-O, OCOR22, TOGETHER ARE = CR23R24; R23 AND R24 ARE H, HALOGEN, O. THE PREFERRED COMPOUNDS 8ß-METHYL-11ß-PENTIL-1,3,5 (10) -TRIEN-3,17ß-DIOL, 11ß-PENTIL-8ß-VINYL-ESTRA-1, 3,5 (10) -TRIEN-3,17ß-DIOL, AMONG OTHERS. IT ALSO REFERS TO A COMPOSITION THAT ALSO INCLUDES GnRH ANTAGONISTS, PROGESTERONE RECEPTOR ANTAGONISTS, MESOPROGESTINES, GESTAGENS, TISSUE SELECTIVE GESTAGENS. THE COMPOUNDS HAVE AFFINITY FOR ESTROGEN RECEPTORS, INHIBIT THE GENERATION OF THE FOLLICLE, OVULATION, MAY BE USEFUL AS CONTRACEPTIVES, OR FOR CONTRACEPTIVES IN MAN, AND FOR THE TREATMENT OF OVARIC, PROLIFERATIVE, CARUMINARY, OR OVARICAL, CULIFERATIVE, OVARIC, TUBALOMAR, OR MALIFERATIVE DISEASES.

PE2001001011A 2001-10-12 2001-10-12 8ß-SUBSTITUTED DERIVATIVES OF 11ß-FENYL AND 11ß-HEXIL-ESTRA-1,3,5 (10) -TRIENE THAT HAVE AFFINITY FOR ESTROGEN RECEPTORS PE20030411A1 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
PE2001001011A PE20030411A1 (en) 2001-10-12 2001-10-12 8ß-SUBSTITUTED DERIVATIVES OF 11ß-FENYL AND 11ß-HEXIL-ESTRA-1,3,5 (10) -TRIENE THAT HAVE AFFINITY FOR ESTROGEN RECEPTORS

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
PE2001001011A PE20030411A1 (en) 2001-10-12 2001-10-12 8ß-SUBSTITUTED DERIVATIVES OF 11ß-FENYL AND 11ß-HEXIL-ESTRA-1,3,5 (10) -TRIENE THAT HAVE AFFINITY FOR ESTROGEN RECEPTORS

Publications (1)

Publication Number Publication Date
PE20030411A1 true PE20030411A1 (en) 2003-05-21

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Family Applications (1)

Application Number Title Priority Date Filing Date
PE2001001011A PE20030411A1 (en) 2001-10-12 2001-10-12 8ß-SUBSTITUTED DERIVATIVES OF 11ß-FENYL AND 11ß-HEXIL-ESTRA-1,3,5 (10) -TRIENE THAT HAVE AFFINITY FOR ESTROGEN RECEPTORS

Country Status (1)

Country Link
PE (1) PE20030411A1 (en)

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