AR021455A1 - PHARMACEUTICAL COMPOSITION OF 2-PHENYL-1- [4- (AMINO-1-IL-ALC-1-INIL) -BENCIL] -1H-INDOL-5-OL AND STROGEN AND ITS USE FOR THE MANUFACTURE OF A MEDICINAL PRODUCT - Google Patents

PHARMACEUTICAL COMPOSITION OF 2-PHENYL-1- [4- (AMINO-1-IL-ALC-1-INIL) -BENCIL] -1H-INDOL-5-OL AND STROGEN AND ITS USE FOR THE MANUFACTURE OF A MEDICINAL PRODUCT

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Publication number
AR021455A1
AR021455A1 ARP990102311A AR021455A1 AR 021455 A1 AR021455 A1 AR 021455A1 AR P990102311 A ARP990102311 A AR P990102311A AR 021455 A1 AR021455 A1 AR 021455A1
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Argentina
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alkyl
phenyl
group
optionally substituted
independently selected
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Spanish (es)
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American Home Prod
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Application filed by American Home Prod filed Critical American Home Prod
Publication of AR021455A1 publication Critical patent/AR021455A1/en

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

Abstract

Composicion farmacéutica que contiene uno o más estrogenos y compuestos de 2-fenil-1-[4-(amino-1-il-alc-inil)-bencil]-1H-indol-5-ol que son utilescomo agentes estrogénicos, los compuestos tienen la estructura general (1), donde: R1 se selecciona de H, OH, o ésteres de C1-4 o sus alquil éteres,o halogeno; R2, R3, R4, R5 y R6 se seleccionan independientemente de H, OH o ésteres de C1-4 o sus alquil éteres, halogeno, ciano, alquilo C1-6, otrifluorometilo, con la condicion de que cuando R1 es H, R2no es OH; X se selecciona de H, alquilo C1-6, ciano, nitro, trifluormetilo, halogeno; n es 2 o 3;Y se selecciona de: a) la porcion (2), donde R7 y R8 se seleccionan independientemente del grupo formado por H, alquilo C1-6 o fenilo; b) un heterociclode cinco miembros saturado, no saturado o parcialmente no saturado que contiene hasta dos heteroátomos seleccionados del grupo formado por -O-, -NH-, -N(alquilo C1-4)-, -N=, y -S(O)m-; donde m es un entero entre 0-2, opcionalmente sustituido por 1-3 sustituyentes independientemente seleccionados delgrupo formado por hidrogeno, hidroxilo, halo, alquilo C1-4, trihalometilo, alcoxi C1-4, trihalometoxi, aciloxi C1-4, alquiltio C1-4, alquilsulfinilo C1-4,alquisulfonilo C1-4, hidroxi alquilo C1-4, -CO2H-, -CN-, -CONHR1-, -NH2-, alquilamino C1-4, dialquilamino C1-4, -NHSO2R1, -NHCOR1-, -NO2, y feniloopcionalmente sustituido con 1-3 alquilo C1-4; c) un heterociclo de seis miembros saturados, no saturados o parcialmente no saturados que contienehastados heteroátomos seleccionados del grupo formado por -O-, -NH, -N(alquilo C1-4)-, -N= y -S(O)m-, donde m es un entero entre 0-2, opcionalmentesustituido con 1-3 sustituyentes independientemente seleccionados del grupo formado por hidrogeno, 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-, alquilaminoC1-4, dialquilamino C1-4, -NHSO2R1-, -NHCOR1-, -NO2- y fenilo opcionalmente sustituido con 1-3 alquilo C1-4; d) un heterociclo de siete miembros saturado,Pharmaceutical composition containing one or more estrogens and compounds of 2-phenyl-1- [4- (amino-1-yl-alc-inyl) -benzyl] -1H-indole-5-ol which are useful as estrogenic agents, the compounds they have the general structure (1), where: R1 is selected from H, OH, or C1-4 esters or their alkyl ethers, or halogen; R2, R3, R4, R5 and R6 are independently selected from H, OH or C1-4 esters or their alkyl ethers, halogen, cyano, C1-6 alkyl, otrifluoromethyl, with the proviso that when R1 is H, R2 is not OH; X is selected from H, C1-6 alkyl, cyano, nitro, trifluoromethyl, halogen; n is 2 or 3; Y is selected from: a) the portion (2), 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 five-membered 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 between 0-2, optionally substituted by 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- alkylthio 4, 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 C 1-4 alkyl; c) a six-membered saturated, unsaturated or partially unsaturated heterocycle containing many 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 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, alkylthio C1-4, 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 seven-member heterocycle,

ARP990102311 1998-05-15 1999-05-14 PHARMACEUTICAL COMPOSITION OF 2-PHENYL-1- [4- (AMINO-1-IL-ALC-1-INIL) -BENCIL] -1H-INDOL-5-OL AND STROGEN AND ITS USE FOR THE MANUFACTURE OF A MEDICINAL PRODUCT AR021455A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US7960498A 1998-05-15 1998-05-15

Publications (1)

Publication Number Publication Date
AR021455A1 true AR021455A1 (en) 2002-07-24

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Application Number Title Priority Date Filing Date
ARP990102311 AR021455A1 (en) 1998-05-15 1999-05-14 PHARMACEUTICAL COMPOSITION OF 2-PHENYL-1- [4- (AMINO-1-IL-ALC-1-INIL) -BENCIL] -1H-INDOL-5-OL AND STROGEN AND ITS USE FOR THE MANUFACTURE OF A MEDICINAL PRODUCT

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AR (1) AR021455A1 (en)

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