AR018349A1 - PHARMACEUTICAL COMPOSITION THAT INCLUDES STROGENS AND ANTIESTROGENS AND ITS USE FOR THE MANUFACTURE OF A MEDICINAL PRODUCT - Google Patents

PHARMACEUTICAL COMPOSITION THAT INCLUDES STROGENS AND ANTIESTROGENS AND ITS USE FOR THE MANUFACTURE OF A MEDICINAL PRODUCT

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Publication number
AR018349A1
AR018349A1 ARP990102226A AR018349A1 AR 018349 A1 AR018349 A1 AR 018349A1 AR P990102226 A ARP990102226 A AR P990102226A AR 018349 A1 AR018349 A1 AR 018349A1
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AR
Argentina
Prior art keywords
alkyl
group
unsaturated
optionally substituted
independently selected
Prior art date
Application number
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Spanish (es)
Original Assignee
American Home Prod
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 American Home Prod filed Critical American Home Prod
Publication of AR018349A1 publication Critical patent/AR018349A1/en

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  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

Composicion farmacéutica que comprende uno o más estrogenos y un compuesto que es util como agente estrogénico selectivo de tejidos, que tiene laestructura general de formulas I y II en donde R1 se selecciona entre H, OH o los alquil éteres o ésteresC1-4 de los mismos, o halogenos; R2,R3, R4 R5 y R6 son independientemente seleccionados entre H, OH o los alquil éteres o ésteres C1-4 de los mismos, halogeno, ciano, alquilo C1-6, otrifluorometilo, con la condicion que, cuando R1 es H, R2 no es OH;X es (CH2)n, n es 1 o 2, n es 2-4; Y se selecciona entre: a) la porcion, de la formulaIII en donde R7 y R8 son independientemente seleccionados entre el grupo de H, alquilo C1-6, fenilo; b) un heterociclo de cinco miembros, saturado, insaturadoo parcialmente insaturado, que contiene hasta dos heteroátomos seleccionados entre el grupo que consiste de -O-, -NH-, -N(alquilo C1-4)-, -N=, y -S(O)m-, endonde m es un entero de desde 0 - 2, opcionalmente sustituido con 1 - 3 sustituyentes independientemente seleccionados entre el grupo que consiste de hidrogeno,hidroxilo, halo, alquilo C1-4, trihalometilo, alcoxi C1-4, trihalometoxi, aciloxi C1-4, alquiltio C1-4, alquilsulfinilo C1-4, alquilsulfonilo C1-4, hidroxialquilo (C1-4), fenilo opcionalmente sustituido con 1 -3 alquilo(C1-4), -CO2H-, CN-, CONHR1-, -NH2-, alquilamino C1-4, dialquilamino C1-4, -NHSO2R1-, -NHCOR1-,-NO2-; c) un heterociclo de seis miembros, saturado, insaturado o parcialmente insaturado, que contiene hasta dos heteroátomos seleccionados entre el grupo queconsiste de -O-, -NH-, -N(alquilo C1-4)-, -N=, y -S(O)m-, en donde m es un entero de desde 0 - 2, opcionalmente sustituido con 1 -3 sustituyentesindependientemente seleccionados entre el grupo que consiste en hidrogeno, hidroxilo, halo, alquilo C1-4, trihalometilo, alcoxi C1-4, trihalometoxi, aciloxiC1-4, alquiltio C1-4, alquilsulfinilo C1-4, alquilsulfonilo C1-4, hidroxi alquilo(C1-4), fenilo opcionalmente sustituido con 1 - 3 alquilo (C1-4), -CO2H-, -CN--CONHR1-, -NH2, alquilamino C1-4 dialquilamino C1-4, -NHSO2R1-, NHCOR1-, -NO2-, d) un heterociclo de siete miembros, saturado, insaturado, o parcialmentePharmaceutical composition comprising one or more estrogens and a compound that is useful as a selective estrogenic agent of tissues, having the general structure of formulas I and II wherein R 1 is selected from H, OH or the alkyl ethers or C 1-4 esters thereof , or halogens; R2, R3, R4 R5 and R6 are independently selected from H, OH or C1-4 alkyl ethers or esters thereof, halogen, cyano, C1-6 alkyl, otrifluoromethyl, with the proviso that, when R1 is H, R2 it is not OH; X is (CH2) n, n is 1 or 2, n is 2-4; And it is selected from: a) the portion, of the formula III where R7 and R8 are independently selected from the group of H, C1-6 alkyl, phenyl; b) a five-membered, saturated, unsaturated or partially unsaturated heterocycle, containing up to two heteroatoms selected from the group consisting of -O-, -NH-, -N (C1-4 alkyl) -, -N =, and - S (O) m-, where m is an integer from 0-2, optionally substituted with 1-3 substituents independently selected from the group consisting of hydrogen, hydroxyl, halo, C1-4 alkyl, trihalomethyl, C1-4 alkoxy , trihalomethoxy, C1-4 acyloxy, C1-4 alkylthio, C1-4 alkylsulfinyl, C1-4 alkylsulfonyl, hydroxy (C1-4) alkyl, phenyl optionally substituted with 1-3 alkyl (C1-4), -CO2H-, CN- , CONHR1-, -NH2-, C1-4 alkylamino, C1-4 dialkylamino, -NHSO2R1-, -NHCOR1 -, - NO2-; c) a six-membered heterocycle, saturated, unsaturated or partially unsaturated, containing up to two heteroatoms selected from the group consisting of -O-, -NH-, -N (C1-4 alkyl) -, -N =, and - S (O) m-, wherein m is an integer from 0-2, optionally substituted with 1-3 substituents independently selected from the group consisting of hydrogen, hydroxyl, halo, C1-4 alkyl, trihalomethyl, C1-4 alkoxy , trihalomethoxy, C1-4 acyloxy, C1-4 alkylthio, C1-4 alkylsulfinyl, C1-4 alkylsulfonyl, hydroxy (C1-4) alkyl, phenyl optionally substituted with 1-3 (C1-4) alkyl, -CO2H-, -CN --CONHR1-, -NH2, C1-4 alkylamino C1-4 dialkylamino, -NHSO2R1-, NHCOR1-, -NO2-, d) a seven-membered heterocycle, saturated, unsaturated, or partially

ARP990102226 1998-05-12 1999-05-11 PHARMACEUTICAL COMPOSITION THAT INCLUDES STROGENS AND ANTIESTROGENS AND ITS USE FOR THE MANUFACTURE OF A MEDICINAL PRODUCT AR018349A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US7671198A 1998-05-12 1998-05-12

Publications (1)

Publication Number Publication Date
AR018349A1 true AR018349A1 (en) 2001-11-14

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Application Number Title Priority Date Filing Date
ARP990102226 AR018349A1 (en) 1998-05-12 1999-05-11 PHARMACEUTICAL COMPOSITION THAT INCLUDES STROGENS AND ANTIESTROGENS AND ITS USE FOR THE MANUFACTURE OF A MEDICINAL PRODUCT

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AR (1) AR018349A1 (en)

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