AR060537A1 - 1,2,4-triazoles trisustituidos - Google Patents

1,2,4-triazoles trisustituidos

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Publication number
AR060537A1
AR060537A1 ARP070101670A ARP070101670A AR060537A1 AR 060537 A1 AR060537 A1 AR 060537A1 AR P070101670 A ARP070101670 A AR P070101670A AR P070101670 A ARP070101670 A AR P070101670A AR 060537 A1 AR060537 A1 AR 060537A1
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Argentina
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alkyl
group
cyano
substituents
polyhaloalkyl
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ARP070101670A
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Janssen Pharmaceutica Nv
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    • C07D249/00Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/081,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/41961,2,4-Triazoles
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    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/26Psychostimulants, e.g. nicotine, cocaine
    • AHUMAN NECESSITIES
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    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D249/00Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/081,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
    • C07D249/101,2,4-Triazoles; Hydrogenated 1,2,4-triazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D249/14Nitrogen atoms
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    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/04Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
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    • C07D491/02Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
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    • C07D491/02Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
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    • C07D491/02Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04Ortho-condensed systems
    • C07D491/044Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/048Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered

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Abstract

La presente hace referencia a 3-anilina-5-aril derivados de triazol y análogos o sales aceptables para uso farmacéutico de los mismos, a procesos para prepararlos, a composiciones farmacéuticas que los contienen y a su uso en terapia. La presente particularmente hace referencia a moduladores alostéricos positivos de receptores nicotínicos de acetilcolina, teniendo tal modulador alostérico positivo la capacidad de aumentar la eficacia de los agonistas de los receptores nicotínicos. Reivindicacion 1: Un compuesto de acuerdo con la formula (1) que incluye todas las formas estereoquímicamente isoméricas del mismo, donde Z es alquilo C1-6 o alquilo C1-6 sustituido con uno o más sustituyentes seleccionados en forma independiente del grupo que consiste en hidroxi, ciano, alquil C1-6-O-, R1R2N-C(=O)-, R7-O-C(=O)-NR8-, R10-O-C(=O)-, R3-C(=O)-NR4-, HO-N-C(=NH)-, halo, oxo, polihaloalquilo C1-6 y Het; Q es fenilo, piridinilo, indolinilo, benzodioxolilo, 1,4-benzodioxanilo, benzofuranilo, 2,3-dihidrobenzofuranilo, isoxazolilo, oxazolilo, tiazolilo, isotiazolilo, pirimidinilo, o piridazinilo, donde cada radical se sustituye en forma opcional con uno, dos o tres sustituyentes seleccionados cada uno en forma independiente del grupo que consiste en halo, hidroxilo, ciano, alquilo C1-6, alquil C1-6-O-, alquiltio C1-6, alquil C1-6-O-C(=O)-, HO-C(=O)- alquil C1-6-, Het, polihaloalquilo C1-6, HO-alquil C1-6-, polihaloalquil C1-6-O-, amino, aminoalquil C1-6-, alquil C1-6- S(=O)2-, mono o di(alquil C1-6)amino, formilamino, alquil C1-6-C(=O)-NR11- y R12R13N-C(=O)-; L es alquilo C1-6 sustituido en forma opcional con uno o donde es posible dos o más sustituyentes seleccionados cada uno en forma independiente del grupo que consiste en halo, alquil C1-6-O-, alquiltio C1-6, alquil C1-6-O-C(=O)-, polihaloalquilo C1-6 y polihaloalquil C1-6-O-; o es cicloalquilo C3-6, fenilo, pirimidinilo, piridinilo, pirimidazolilo, piridazinilo, tetrahidropiranilo, imidazotiazolilo, benzodioxolilo, indolinilo, isoindolinilo, benzofuranilo, quinolinilo, isoquinolinilo, benzoxazolilo, 5,6,7,8,-tetrahidroquinolinilo, 5,6,7,8,-tetrahidroisoquinolinilo, 2,3-dihidropirrolopiridinilo, furopiridinilo, 2,3-dihidrobenzofuranilo, benzodioxanilo, dihidrofuropiridinilo, 7-azaindolinilo y 3,4-dihidro-2H-1,4-benzoxazinilo; donde cada uno de los radicales mencionados con anterioridad se sustituye en forma opcional con uno o dos o más sustituyentes, seleccionándose cada sustituyente en forma independiente del grupo que consiste en halo, hidroxilo, ciano, alquilo C1-6, alquil C1-6-O-, alquiltio C1-6, alquil C1-6-O-C(=O)-, HO-C(=O)-alquil C1-6 -, Het1, polihaloalquilo C1-6, HO-alquil C1-6-, polihaloalquil C1-6-O-, amino, aminoalquil C1-6-, alquil C1-6-S(=O)2-, mono o di(alquil C1-6)amino, formilamino, alquil C1-6-C(=O)-NR14-, R15R16N-C(=O)-, morfolinilo, CH3O-alquil C1-6NH-, HO-alquil C1-6-NH-, benciloxi, cicloalquilo C3-6, cicloalquil C3-6-NH-, cicloalquil C3-6-alquil C1-6-NH-, polihaloalquil C1-6-C(=O)-NR14-, alquil C1-6 C(=O)-, y alquil C1-6-O-alquil C1-6-; R1 y R2 representan cada uno en forma independiente hidrogeno, alquilo C1-6, cicloalquilo C3-6, alquil C1-4-O-alquilo C1-6, Het2, HO-alquilo C1- 6, polihaloalquilo C1-6, cicloalquilo C3-6 sustituido con alquilo C1-4, cicloalquil C3-6-alquilo C1-6, dimetilamino-alquilo C1-4 o 2-hidroxiciclopentan-1-ilo; o R1 y R2 tomados en conjunto con el átomo de nitrogeno al cual están unidos forman un radical heterocíclico seleccionado del grupo que consiste en pirrolidinilo, piperidinilo, piperazinilo, morfolinilo, tiomorfolinilo y pirazolidinilo; donde dicho radical heterocíclico se sustituye en forma opcional con 1, 2 o 3 sustituyentes seleccionados cada uno en forma independiente del grupo que consiste en halo, hidroxi, amino, ciano y alquilo C1-6; R3 representa hidrogeno, alquilo C1-6, cicloalquilo C3-6, Het3 o alquilo C1-6 sustituido con uno o más sustituyentes seleccionados del grupo que consiste en hidroxi, ciano, alquil C1-4-O- y Het4; R4 y R8 representan cada uno en forma independiente hidrogeno, alquilo C1-6 o cicloalquilo C3-6; donde cada uno de estos radicales alquilo puede sustituirse con uno o más sustituyentes seleccionados del grupo que consiste en hidroxi, ciano y alquil C1-4-O-; R6 representa hidrogeno, alquilo C1-6, o cuando Q representa fenilo, R6 puede también ser un alcandiilo C2-6 unido a dicho anillo fenilo para formar junto con el nitrogeno al cual está unido y dicho anillo fenilo un sistema anular bicíclico fusionado que contiene 9 a 10 átomos anulares tal como indolinilo o tetrahidroquinolinilo, cada uno sustituido en forma opcional con trifluorometilo; R7 y R10 representan cada uno en forma independiente hidrogeno, alquilo C1-6 o cicloalquilo C3-6; donde cada uno de estos radicales alquilo puede sustituirse con uno o más sustituyentes seleccionados del grupo que consiste en hidroxi, ciano, alquil C1-4-O-, Het4 y NH2-C(CH3)=N-; R11 y R14 representan cada uno en forma independiente hidrogeno, alquilo C1-6 o cicloalquilo C3-6; donde cada uno de estos radicales alquilo puede sustituirse con uno o más sustituyentes seleccionados del grupo que consiste en hidroxi, ciano y alquil C14-O-; R12 y R13 representan cada uno en forma independiente hidrogeno, alquilo C1-6 o cicloalquilo C3-6; donde cada uno de estos radicales alquilo puede sustituirse con uno o más sustituyentes seleccionados del grupo que consiste en hidroxi, ciano o alquil C1-4-O-; o R12 y R13 tomados en conjunto con el átomo de nitrogeno al cual están unidos pueden formar un radical heterocíclico seleccionado del grupo que consiste en pirrolidinilo, piperidinilo, piperazinilo, morfolinilo, tiomorfolinilo y pirazolidinilo; donde dicho radical heterocíclico se sustituye en forma opcional con 1, 2 o 3 sustituyentes seleccionados cada uno en forma independiente del grupo que consiste en halo, hidroxi, amino, ciano, alquilo C1-6 o polihaloalquilo C1-6; R15 y R16 representan cada uno en forma independiente hidrogeno, alquilo C1-6 o cicloalquilo C3-6; donde cada uno de estos radicales alquilo puede sustituirse con uno o más sustituyentes seleccionados del grupo que consiste en hidroxi, ciano y alquil C1-4-O-; o R15 y R16 tomados en conjunto con el átomo de nitrogeno al cual están unidos pueden formar un radical heterocíclico seleccionado del grupo que consiste en pirrolidinilo, piperidinilo, piperazinilo, morfolinilo, tiomorfolinilo y pirazolidinilo; donde dicho radical heterocíclico se sustituye en forma opcional con 1, 2 o 3 sustituyentes seleccionados cada uno en forma independiente del grupo que consiste en halo, hidroxi, amino, ciano, alquilo C1-6 y polihaloalquilo C1-6; Het y Het1 representan cada uno en forma independiente piperidinilo, piperazinilo, pirrolidinilo, morfolinilo, imidazolilo, oxazolilo, oxadiazolilo, tiazolilo, isoxazolilo, isotiazolilo, tiomorfolinilo o pirazolilo; donde cada radical se sustituye en forma independiente con 1, 2 o 3 sustituyentes, seleccionándose cada sustituyente en forma independiente del grupo que consiste en halo, hidroxi, amino, ciano, alquilo C1-6 y polihaloalquilo C1-6; Het2 representa piperidinilo, piperazinilo, pirrolidinilo, morfolinilo, imidazolilo, oxazolilo, oxadiazolilo, tiazolilo, isoxazolilo, isotiazolilo, tiomorfolinilo, pirazolilo o tetrahidrofuranilo; donde cada radical se sustituye en forma independiente con 1, 2 o 3 sustituyentes, seleccionándose cada sustituyente en forma independiente del grupo que consiste en halo, hidroxi, amino, ciano, alquilo C1-6 y polihaloalquilo C1-6; Het3 representa piperidinilo, piperazinilo, pirrolidinilo, morfolinilo, imidazolilo, oxazolilo, oxadiazolilo, tiazolilo, isoxazolilo, isotiazolilo, tiomorfolinilo o pirazolilo; donde cada radical se sustituye en forma opcional con 1, 2 o 3 sustituyentes, seleccionándose cada sustituyente en forma independiente del grupo que consiste en halo, hidroxi, amino, ciano, alquilo C1-6 y polihaloalquilo C1-6; Het4 representa piperidinilo, piperazinilo, pirrolidinilo, morfolinilo, imidazolilo, oxazolilo, oxadiazolilo, tiazolilo, isoxazolilo, isotiazolilo, tiomorfolinilo o pirazolilo; donde cada radical se sustituye en forma opcional con 1, 2 o 3 sustituyentes, seleccionándose cada sustituyente en forma independiente del grupo que consiste en halo, hidroxi, amino, ciano o alquilo C1-6; un N-oxido, una sal de adicion aceptable para uso farmacéutico, un solvato o una amina cuaternaria del mismo.
ARP070101670A 2006-04-19 2007-04-18 1,2,4-triazoles trisustituidos AR060537A1 (es)

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EP (1) EP2010516B1 (es)
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KR (1) KR101465413B1 (es)
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AR (1) AR060537A1 (es)
AU (1) AU2007239498B2 (es)
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CA (1) CA2648157C (es)
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HK (1) HK1135375A1 (es)
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Publication number Priority date Publication date Assignee Title
JO3019B1 (ar) 2006-04-19 2016-09-05 Janssen Pharmaceutica Nv ثلاثي مستبدل 4،2،1-ثلاثي زولات
EP2083921A2 (en) * 2006-09-04 2009-08-05 Neurosearch A/S Pharmaceutical combinations of a nicotine receptor modulator and a cognitive enhancer
MX2010004177A (es) * 2007-10-18 2010-05-03 Janssen Pharmaceutica Nv 1,2,4-triazoles trisustituidos.
JO2784B1 (en) 2007-10-18 2014-03-15 شركة جانسين فارماسوتيكا ان. في 5,3,1 - Triazole substitute derivative
AR070936A1 (es) * 2008-03-19 2010-05-12 Janssen Pharmaceutica Nv 1,2,4 -triazoles trisustituidos
AR071763A1 (es) * 2008-05-09 2010-07-14 Janssen Pharmaceutica Nv Pirazoles trisustituidos, composiciones farmaceuticas que los contienen, y usos de los mismos en el tratamiento de trastornos neurologicos y psiquiatricos
BR112012005960A2 (pt) * 2009-09-17 2016-03-15 Janssen Pharmaceutica Nv n-fenil-1-(4-piridinil)-1h-pirazol-3-aminas substituídas
JO3078B1 (ar) * 2009-11-27 2017-03-15 Janssen Pharmaceutica Nv مورفولينوثيازولات بصفتها منظمات الوستيرية نوع الفا 7 موجبة
AU2012213086B2 (en) 2011-02-03 2016-05-05 Lupin Limited Pyrrole derivatives used as modulators of alpha7 nAChR
EA024170B1 (ru) 2011-02-23 2016-08-31 Люпин Лимитед ГЕТЕРОАРИЛЬНЫЕ ПРОИЗВОДНЫЕ В КАЧЕСТВЕ МОДУЛЯТОРОВ nAChR АЛЬФА7
CA2824350C (en) 2011-02-25 2019-07-02 Janssen Pharmaceutica Nv (pyridin-4-yl)benzylamides as allosteric modulators of alpha 7 nachr
US9187420B2 (en) 2011-03-31 2015-11-17 Lupin Limited Pyrrole derivatives as nicotinic acetylcholine receptor modulators for use in the treatment of neurodegenerative disorders such as alzheimer's and parkinson's disease
WO2013005153A1 (en) 2011-07-05 2013-01-10 Lupin Limited Biaryl derivatives as nachr modulators
IN2014MN01756A (es) 2012-03-06 2015-07-03 Lupin Ltd
EP2945936A1 (en) 2012-11-12 2015-11-25 Lupin Limited Thiazole derivatives as alpha 7 nachr modulators
EP2945941B1 (en) 2013-01-16 2016-12-07 Lupin Limited Pyrrole derivatives as alpha 7 nachr modulators
WO2014141091A1 (en) 2013-03-13 2014-09-18 Lupin Limited Pyrrole derivatives as alpha 7 nachr modulators
TW201446243A (zh) 2013-06-03 2014-12-16 Lupin Ltd 4-(5-(4-氯苯基)-2-(2-環丙基乙醯基)-1,4-二甲基-1氫-吡咯-3-基)苯磺醯胺作為α7尼古丁乙醯膽鹼受體調節劑
CA2913987A1 (en) 2013-06-17 2014-12-24 Lupin Limited Pyrrole derivatives as alpha 7 nachr modulators
ES2796276T3 (es) * 2015-02-05 2020-11-26 Ab Science Compuestos con actividad antitumoral
CN110835336B (zh) * 2018-08-16 2022-10-04 中国药科大学 含氧杂环取代唑类化合物及其用途

Family Cites Families (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE3773746D1 (en) 1986-05-07 1991-11-21 Fisons Plc Pyrazole.
FR2792314B1 (fr) 1999-04-15 2001-06-01 Adir Nouveaux composes aminotriazoles, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
PT1070708E (pt) * 1999-07-21 2004-05-31 Hoffmann La Roche Derivados de triazol
FR2802530B1 (fr) 1999-12-17 2002-02-22 Sanofi Synthelabo Nouveaux derives amino substitues ramifies du 3-amino-1-phenyl-1h[1,2,4]triazole, procedes pour leur preparation et compositions pharmaceutiques les contenant
DK1506200T3 (da) 2002-05-07 2007-04-10 Neurosearch As Diazabicykliske biarylderivater
CN1326857C (zh) * 2002-09-30 2007-07-18 神经研究公司 新的1,4-二氮杂双环烷烃衍生物、其制备和应用
WO2005004818A2 (en) * 2003-07-09 2005-01-20 Imclone Systems Incorporated Heterocyclic compounds and their use as anticancer agents
WO2005012263A1 (en) 2003-07-24 2005-02-10 Pharmagene Laboratories Limited 5-ht2b receptor antagonists
FR2862647B1 (fr) 2003-11-25 2008-07-04 Aventis Pharma Sa Derives de pyrazolyle, procede de preparation et intermediaires de ce procede a titre de medicaments et de compositions pharmaceutiques les renfermant
WO2006064375A2 (en) 2004-12-16 2006-06-22 Ab Science Aminoaryl substituted five-membered ring heterocyclic compounds for the treatment of diseases
EP1926719B1 (en) 2005-09-13 2017-05-31 Janssen Pharmaceutica NV 2-aniline-4-aryl substituted thiazole derivatives
JO3019B1 (ar) 2006-04-19 2016-09-05 Janssen Pharmaceutica Nv ثلاثي مستبدل 4،2،1-ثلاثي زولات

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