AR041629A1 - USE OF NOREPINEFRINE RECAPTATION MODULATORS TO PREVENT AND TREAT VASOMOTOR SYMPTOMS - Google Patents

USE OF NOREPINEFRINE RECAPTATION MODULATORS TO PREVENT AND TREAT VASOMOTOR SYMPTOMS

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Publication number
AR041629A1
AR041629A1 ARP030103756A AR041629A1 AR 041629 A1 AR041629 A1 AR 041629A1 AR P030103756 A ARP030103756 A AR P030103756A AR 041629 A1 AR041629 A1 AR 041629A1
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Argentina
Prior art keywords
ethyl
cyclohexanol
piperazinyl
hydrochloric
methyl
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Spanish (es)
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Wyeth Corp
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=35578057&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR041629(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Wyeth Corp filed Critical Wyeth Corp
Publication of AR041629A1 publication Critical patent/AR041629A1/en

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  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

Uso de compuestos y composición de compuestos que regulan los niveles de norepinefrina para la prevención y el tratamiento de los síntomas vasomotores, tales como, los sofocos, causados por, entre otros, las disfunciones de la termorregulación, donde dichos compuestos duales NRI/SRI son venlafaxina o una sal farmacéuticamente aceptable del mismo. Reivindicación 31: Una composición farmacéutica que comprende: a. Por lo menos un inhibidor de la recaptación de norepinefrina o una sal farmacéuticamente aceptable del mismo; y b. Por lo menos un inhibidor de la recaptación de serotonina o una sal farmacéuticamente aceptable del mismo; y c por lo menos un vehículo excipiente farmacéuticamente aceptado. Reivindicación 33: Una composición farmacéutica de acuerdo a lo establecido en el número 31, donde dicho inhibidor de la recaptación de norepinefrina sea seleccionado de un grupo que consiste en maprotilina; reboxetina; norpramina/desipramina; nisoxetina; atomoxetina; amoxapina; doxepina; lofepramina; amitriptilina; 1-[1-(3-fluorofenil)-2-(4-metil-piperacinil)etil]ciclohexanol; 1-[1-(3-clorofenil)-2-(4-metil-1-piperacinil)etil]ciclohexanol; 1-[2-(4-metil-1-piperacinil)-1-[3-(trifluorometil)fenil]-etil]ciclohexanol; 1-[1-(4-metoxifenil)-2-[4-metil-1-piperacinil)etil]ciclohexanol; 1-[1-(3-clorofenil)-2-(4-(3-clorofenil)-1-piperacinil]etil]ciclohexanol; 1-[1-(3-metoxifenil)-2-[4-fenilmetil-1-piperacinil]etil]ciclohexanol; 1-[2-(3-clorofenil)-1-piperacinil]1-(3-metoxifenil)etil]ciclohexanol; 1-[2-[4-(6-cloro-2-piracinil)-1-piperacinil]-1-[3-metoxi-fenil)etil]ciclohexanol; 1-[2-[4-(fenilmetil)-1-piperacinil]-1-[3-(trifluorometil)fenil]etil]-ciclohexanol; 1-[1-(3-metoxifenil)-2-[4-[3-(trifluorometil)fenil]-1-piperacinil]etil]-ciclohexanol; 1-[1-(4-fluorofenil)-2-...[4-fenilmetil)-1-piperacinil]etil]ciclohexanol; 1-[1-(3-metoxifenil)2-[4-[3-(trifluorometil)fenil]-1-piperacinil]etil]ciclopentanol; 1-[1-(4-fluorofenil)-2-[4-(fenilmetil)-1-piperacinil]etil]ciclohexanol; 1-[2-(dimetilamino)-1-(3-trifluorometilfenil)etil]ciclohexanol; 1-[1-(3-fluorofenil)-2-(4-metil-1-piperacinil)etil]-ciclohexanol; 1-[1-(3-clorofenil)-2-(dimetilamino)etil]ciclohexanol; 1-[1-(3-clorofenil)-2-(dimetilamino)etil]ciclohexanol; 1-[1-(3-clorofenil)-2-piperacin-1-il-etil]-ciclohexanol; y combinaciones y sales farmacéuticamente aceptables de los mismos. Reivindicación 34: Una composición farmacéutica de acuerdo a lo establecido en el número 31, donde dicho inhibidor de la recaptación de norepinefrina es desipramina. Reivindicación 35: Una composición farmacéutica de acuerdo a lo establecido en el número 31, donde dicho inhibidor de la recaptación de norepinefrina es 1-[1-(3-clorofenil)-2-(4-metil-1-piperacinil)etil]ciclohexanol. Reivindicación 37: Una composición farmacéutica de acuerdo a lo establecido en el número 31, donde dicho inhibidor de la recaptación de serotonina es seleccionado de un grupo que consiste en: fluoxetina, paroxetina, sertralina, fluvoxamina, y combinaciones, y sales farmacéuticamente aceptables de los mismos. Reivindicación 38: Una composición farmacéutica que comprende: a) por lo menos un inhibidor de la recaptación de norepinefrina o una sal farmacéuticamente aceptable del mismo; y b) por lo menos un agonista de los receptores adrenérgicos alfa2 o una sal farmacéuticamente aceptable del mismo;: y c) por lo menos un vehículo excipiente farmacéuticamente aceptado. Reivindicación 44: Una composición farmacéutica de acuerdo a lo establecido en el número 38, donde dicho antagonista de los receptores adrenérgicos alfa2 es un compuesto seleccionado del grupo que comprende; atipamezol; 2-[2-(4-(2-metoxifenil)-piperacin-1-il)etil]-4,4-dimetil-1,3-(2H,4H)-isoquinolindiona diclorhídrica (ARC 239 diclorhídrico); 2-[(4,5-dihidro-1H-imidazol-2-il)metil]-2,3-dihidro-1-metil-1H-isoindol maleato (BRL44408 maleato); BRL48962; BRL41992; SKF 104856; SKF 104078; MK912; 2-(2-etil-2,3-dihidro-2-benzofuranil)-4,5-dihidro-1H-imidazol clorhídrico (efaroxan clorhídrico); 2-(1,4-benzodioxano-2-il)-2-imidazolin clorhídrico (idazoxan clorhídrico); 2-(1-etil-2-indazoil)metil]-1,4-benzodioxano clorhídrico (imiloxan clorhídrico);17alfa-hidroxi-20alfa-yohimbano-16beta-ácido carboxílico, metil éster clorhídrico (rauwolscina clorhídrica); (8alfaR, 12alfaS, 13alfaS)-5,8,8,8alfa,9,10,11,1212alfa,13,13alfa-dihidro-3-metoxi-12(etilsulfonil)-6H-isoquino(2,1-il)[1,6]naftiridina clorhídrica (RS 79948 clorhídrico) 2-(2,3-dihidro-2-metoxi-1,4-benzodioxina-2-il)-4,5-dihidro-1H-imidazol clorhídrico (RX 821002 clorhídrico); 8-[(2,3-dihidro-1,4-benzodioxina-2-il)metil]-1-fenil-1,3,8-triazaspiro[4,5]decan-4-uno (espiroxatrina); 17alfa-hidroxiyohimbano-16alfa-ácido carboxílico metil éster clorhídrico (yohimbina clorhídrica); y combinaciones y sales farmacéuticamente aceptables de los mismos.Use of compounds and composition of compounds that regulate norepinephrine levels for the prevention and treatment of vasomotor symptoms, such as hot flashes, caused by, among others, thermoregulation dysfunctions, where said dual NRI / SRI compounds are venlafaxine or a pharmaceutically acceptable salt thereof. Claim 31: A pharmaceutical composition comprising: a. At least one norepinephrine reuptake inhibitor or a pharmaceutically acceptable salt thereof; and b. At least one serotonin reuptake inhibitor or a pharmaceutically acceptable salt thereof; and c at least one pharmaceutically accepted excipient vehicle. Claim 33: A pharmaceutical composition as set forth in No. 31, wherein said norepinephrine reuptake inhibitor is selected from a group consisting of maprotiline; reboxetine; norpramine / desipramine; nisoxetine; atomoxetine; amoxapine; doxepine; lofepramine; amitriptyline; 1- [1- (3-fluorophenyl) -2- (4-methyl-piperazinyl) ethyl] cyclohexanol; 1- [1- (3-Chlorophenyl) -2- (4-methyl-1-piperazinyl) ethyl] cyclohexanol; 1- [2- (4-methyl-1-piperazinyl) -1- [3- (trifluoromethyl) phenyl] -ethyl] cyclohexanol; 1- [1- (4-Methoxyphenyl) -2- [4-methyl-1-piperazinyl) ethyl] cyclohexanol; 1- [1- (3-chlorophenyl) -2- (4- (3-chlorophenyl) -1-piperazinyl] ethyl] cyclohexanol; 1- [1- (3-methoxyphenyl) -2- [4-phenylmethyl-1- piperacinyl] ethyl] cyclohexanol; 1- [2- (3-chlorophenyl) -1-piperazinyl] 1- (3-methoxyphenyl) ethyl] cyclohexanol; 1- [2- [4- (6-chloro-2-pyrazinyl) - 1-piperazinyl] -1- [3-methoxy-phenyl) ethyl] cyclohexanol; 1- [2- [4- (phenylmethyl) -1-piperazinyl] -1- [3- (trifluoromethyl) phenyl] ethyl] -cyclohexanol; 1- [1- (3-Methoxyphenyl) -2- [4- [3- (trifluoromethyl) phenyl] -1-piperazinyl] ethyl] -cyclohexanol; 1- [1- (4-fluorophenyl) -2 -... [4-phenylmethyl) -1-piperazinyl] ethyl] cyclohexanol; 1- [1- (3-Methoxyphenyl) 2- [4- [3- (trifluoromethyl) phenyl] -1-piperazinyl] ethyl] cyclopentanol; 1- [1- (4-fluorophenyl) -2- [4- (phenylmethyl) -1-piperazinyl] ethyl] cyclohexanol; 1- [2- (dimethylamino) -1- (3-trifluoromethylphenyl) ethyl] cyclohexanol; 1- [1- (3-fluorophenyl) -2- (4-methyl-1-piperazinyl) ethyl] -cyclohexanol; 1- [1- (3-Chlorophenyl) -2- (dimethylamino) ethyl] cyclohexanol; 1- [1- (3-Chlorophenyl) -2- (dimethylamino) ethyl] cyclohexanol; 1- [1- (3-Chlorophenyl) -2-piperazin-1-yl-ethyl] -cyclohexanol; and combinations and pharmaceutically acceptable salts thereof. Claim 34: A pharmaceutical composition as set forth in No. 31, wherein said norepinephrine reuptake inhibitor is desipramine. Claim 35: A pharmaceutical composition as set forth in No. 31, wherein said norepinephrine reuptake inhibitor is 1- [1- (3-chlorophenyl) -2- (4-methyl-1-piperazinyl) ethyl] cyclohexanol . Claim 37: A pharmaceutical composition according to the provisions of No. 31, wherein said serotonin reuptake inhibitor is selected from a group consisting of: fluoxetine, paroxetine, sertraline, fluvoxamine, and combinations, and pharmaceutically acceptable salts thereof. same. Claim 38: A pharmaceutical composition comprising: a) at least one norepinephrine reuptake inhibitor or a pharmaceutically acceptable salt thereof; and b) at least one alpha2 adrenergic receptor agonist or a pharmaceutically acceptable salt thereof: and c) at least one pharmaceutically accepted carrier vehicle. Claim 44: A pharmaceutical composition as set forth in No. 38, wherein said alpha2 adrenergic receptor antagonist is a compound selected from the group comprising; atipamezole; 2- [2- (4- (2-Methoxyphenyl) -piperacin-1-yl) ethyl] -4,4-dimethyl-1,3- (2H, 4H) -isoquinolindione dichlorhydric (ARC 239 dichlorohydric); 2 - [(4,5-dihydro-1H-imidazol-2-yl) methyl] -2,3-dihydro-1-methyl-1H-isoindole maleate (BRL44408 maleate); BRL48962; BRL41992; SKF 104856; SKF 104078; MK912; 2- (2-Ethyl-2,3-dihydro-2-benzofuranyl) -4,5-dihydro-1H-imidazole hydrochloric acid (efaroxan hydrochloric); 2- (1,4-benzodioxane-2-yl) -2-imidazolin hydrochloric (idazoxan hydrochloric); 2- (1-Ethyl-2-indazoyl) methyl] -1,4-benzodioxane hydrochloric (imiloxan hydrochloric); 17alpha-hydroxy-20alpha-yohimbano-16beta-carboxylic acid, hydrochloric methyl ester (rauwolscin hydrochloric); (8alphaR, 12alfaS, 13alfaS) -5,8,8,8alfa, 9,10,11,1212alfa, 13,13alpha-dihydro-3-methoxy-12 (ethylsulfonyl) -6H-isoquin (2,1-yl) [2,1 1,6] hydrochloric naphthyridine (RS 79948 hydrochloric) 2- (2,3-dihydro-2-methoxy-1,4-benzodioxine-2-yl) -4,5-dihydro-1H-imidazole hydrochloric (RX 821002 hydrochloric) ; 8 - [(2,3-dihydro-1,4-benzodioxin-2-yl) methyl] -1-phenyl-1,3,8-triazaspiro [4,5] decan-4-one (spiroxatrine); 17alpha-hydroxyyohimbano-16alpha-carboxylic acid methyl hydrochloric ester (yohimbine hydrochloric); and combinations and pharmaceutically acceptable salts thereof.

ARP030103756 2002-10-15 2003-10-15 USE OF NOREPINEFRINE RECAPTATION MODULATORS TO PREVENT AND TREAT VASOMOTOR SYMPTOMS AR041629A1 (en)

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ARP030103756 AR041629A1 (en) 2002-10-15 2003-10-15 USE OF NOREPINEFRINE RECAPTATION MODULATORS TO PREVENT AND TREAT VASOMOTOR SYMPTOMS

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CL (1) CL2003002077A1 (en)

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CN112220767B (en) * 2020-09-25 2022-10-25 安徽省公众检验研究院有限公司 Preparation method of altimezole hydrochloride sustained-release tablet

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CN1705484A (en) 2005-12-07
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AR041628A1 (en) 2005-05-26

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