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AR018608A1 - PHARMACEUTICAL COMPOSITION OF 3- [4- (2-PHENYL-INDOL-1-ILMETILE) -PENYL] -ACRYLAMIDE AND STROGEN AND ITS USE FOR THE MANUFACTURE OF A MEDICINAL PRODUCT - Google Patents

PHARMACEUTICAL COMPOSITION OF 3- [4- (2-PHENYL-INDOL-1-ILMETILE) -PENYL] -ACRYLAMIDE AND STROGEN AND ITS USE FOR THE MANUFACTURE OF A MEDICINAL PRODUCT

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Publication number
AR018608A1
AR018608A1 ARP990102309A AR018608A1 AR 018608 A1 AR018608 A1 AR 018608A1 AR P990102309 A ARP990102309 A AR P990102309A AR 018608 A1 AR018608 A1 AR 018608A1
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AR
Argentina
Prior art keywords
alkyl
phenyl
group
unsaturated
independently selected
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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 AR018608A1 publication Critical patent/AR018608A1/en

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  • Indole Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Composicion farmacéutica que contiene uno o más estrogenos y compuestos de 3-[4-(2-fenil-indol-1-ilmetil)-fenil]-acrilamida que son utiles como agentesestrogénicos, los compuestos tienen la siguiente estructura general,de formulas (I) donde R1 se selecciona de H, OH o ésteres de C1-4 o sus alquil ésteres, ohalogeno;R2,R3,R4,R5 y R6 se seleccionan independientemente de H,OH o ésteres C1-C4 o sus alquil éteres, halogeno, ciano, alquilo C1-6, trifluorometilo, conla condicion de que cuando R1 es H,R2 no es OH; X se selecciona de H, alquilo C1-6, ciano, nitro, trifluormetilo, halogeno; Y se selecciona de a) la porcion(II),donde R7 y R8 se seleccionan independientemente del grupo formado por H, alquilo C1-6, o fenilo, b) un heterociclo de 5 miembros saturado, no saturado oparcialmente no saturado que contiene hasta 2 heteroátomos seleccionados del grupo formado por -O-, -NH-, -N(alquilo C1-4), -N=, y -S(O)m-,donde m es un enteroentre 0-2, opcionalmente sustituido por 1-3 sustituyentes independientemente seleccionados del grupo formado por H, hidroxilo, halo, alquilo de C1-4,trihalometilo, alcoxi C1-4,trihalometoxi,aciloxi C1-4, alquiltio C1-4,alquilsulfinilo C1-4,alquilsulfonilo C1-4,hidroxi alquilo C1-4, -CO2H, -CN-, -CONHR1-,-NH2-,alquilamino C1-4, dialquilamino C1-4,-NHSO2R1-, NHCOR1-,-NO2 y fenilo sustituido con 1-3 alquilo C1-4; a)un heterociclo de 6 miembros saturados,no saturadoso parcialmente no saturados que contiene hasta 2 heteroátomos seleccionados del grupo formado por -O-, NH-, -N(alquilo C1-4)-, -N=, y- S(O)m-, donde m es unentero entre 0-2, opcionalmente sustituido con 1-3 sustituyentes independientemente seleccionados del grupo formado por H, hidroxilo, halo, alquilo C1-4,trihalometilo,alcoxi C1-4,trihalometoxi,aciloxi C1-4,alquiltio C1-4, alquilsulfinilo C1-4, alquilsulfonilo C1-4,hidroxi alquilo C1-4, -CO2H-, -CN-, -CONHR1-,-NH2-, alquilamino C1-4, dialquilamino C1-4, -NHSO2R1-, -NHCOR1-,-NO2- y fenilo opcionalmente sustituido con 1-3 alquilo (C1-4); d) un heterociclo de 7miembros saturado, no saturado o parcialmente no saturado que contiene hasta 2 heteroátomos seleccionados del grupo formado por -O-, -NH-, -N(alquilo C1-4)-, -Pharmaceutical composition containing one or more estrogens and compounds of 3- [4- (2-phenyl-indole-1-ylmethyl) -phenyl] -acrylamide which are useful as estrogenic agents, the compounds have the following general structure, of formulas (I ) where R1 is selected from H, OH or C1-4 esters or their alkyl esters, ohalogen; R2, R3, R4, R5 and R6 are independently selected from H, OH or C1-C4 esters or their alkyl ethers, halogen, cyano, C1-6 alkyl, trifluoromethyl, with the proviso that when R1 is H, R2 is not OH; X is selected from H, C1-6 alkyl, cyano, nitro, trifluoromethyl, halogen; Y is selected from a) the portion (II), where R7 and R8 are independently selected from the group consisting of H, C1-6 alkyl, or phenyl, b) a saturated, unsaturated or partially unsaturated 5-membered heterocycle containing up to 2 heteroatoms selected from the group consisting of -O-, -NH-, -N (C1-4 alkyl), -N =, and -S (O) m-, where m is an integer between 0-2, optionally substituted by 1 -3 substituents independently selected from the group consisting of H, hydroxyl, halo, C 1-4 alkyl, trihalomethyl, C 1-4 alkoxy, trihalomethoxy, C 1-4 acyloxy, C 1-4 alkylthio, C 1-4 alkylsulfinyl, C 1-4 alkylsulfonyl, hydroxy C1-4 alkyl, -CO2H, -CN-, -CONHR1 -, - NH2-, C1-4 alkylamino, C1-4 dialkylamino, -NHSO2R1-, NHCOR1 -, - NO2 and phenyl substituted with 1-3 C1 alkyl 4; a) a 6-membered saturated, unsaturated, partially unsaturated heterocycle containing up to 2 heteroatoms selected from the group consisting of -O-, NH-, -N (C1-4 alkyl) -, -N =, and- S (O ) m-, where m is a binder between 0-2, optionally substituted with 1-3 substituents independently selected from the group consisting of H, 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, -CO2H-, -CN-, -CONHR1 -, - NH2-, C1-4 alkylamino, C1-4 dialkylamino, -NHSO2R1 -, -NHCOR1 -, - NO2- and phenyl optionally substituted with 1-3 (C1-4) alkyl; d) a saturated, unsaturated or partially unsaturated 7-member heterocycle containing up to 2 heteroatoms selected from the group consisting of -O-, -NH-, -N (C1-4 alkyl) -, -

ARP990102309 1998-05-15 1999-05-14 PHARMACEUTICAL COMPOSITION OF 3- [4- (2-PHENYL-INDOL-1-ILMETILE) -PENYL] -ACRYLAMIDE AND STROGEN AND ITS USE FOR THE MANUFACTURE OF A MEDICINAL PRODUCT AR018608A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US7964498A 1998-05-15 1998-05-15

Publications (1)

Publication Number Publication Date
AR018608A1 true AR018608A1 (en) 2001-11-28

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Family Applications (1)

Application Number Title Priority Date Filing Date
ARP990102309 AR018608A1 (en) 1998-05-15 1999-05-14 PHARMACEUTICAL COMPOSITION OF 3- [4- (2-PHENYL-INDOL-1-ILMETILE) -PENYL] -ACRYLAMIDE AND STROGEN AND ITS USE FOR THE MANUFACTURE OF A MEDICINAL PRODUCT

Country Status (1)

Country Link
AR (1) AR018608A1 (en)

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