AR037655A1 - Derivados de bencensulfonilo, una composicion farmaceutica que los comprende, el uso de dichos derivados para la fabricacion de un medicamento para el tratamiento asociado al receptor retinoide x, un metodo para la preparacion de un agente alquilante - Google Patents

Derivados de bencensulfonilo, una composicion farmaceutica que los comprende, el uso de dichos derivados para la fabricacion de un medicamento para el tratamiento asociado al receptor retinoide x, un metodo para la preparacion de un agente alquilante

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AR037655A1
AR037655A1 ARP020104451A ARP020104451A AR037655A1 AR 037655 A1 AR037655 A1 AR 037655A1 AR P020104451 A ARP020104451 A AR P020104451A AR P020104451 A ARP020104451 A AR P020104451A AR 037655 A1 AR037655 A1 AR 037655A1
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Argentina
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hydrogen
attached
carbon atoms
understanding
optionally substituted
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ARP020104451A
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English (en)
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Novartis Ag
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404—Indoles, e.g. pindolol
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    • A61K31/41—Heterocyclic 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
    • A61K31/42—Oxazoles
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    • C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/10—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members 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
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Abstract

Derivados bencensulfonilos que comprenden un compuesto de la fórmula (1), en donde: L es el radical de la fórmula (2), en donde: R1 es hidrógeno, opcionalmente alquilo sustituido, arilo, heteroarilo, aralquilo, o cicloalquilo; R2 es hidrógeno, hidroxilo, alquilo opcionalmente sustituido, arilo, aralquilo, alcoxilo, ariloxilo, aralcoxilo, tioalquilo, tioarilo, o tioaralquilo; R3 es hidrógeno o arilo; o R2 y R3 son combinados alquileno, que junto con los átomos de carbono con los que están unidos, forman un anillo de 5 a 7 miembros; n es 0 ó un entero de 1 a 2; Y es hidrógeno; ó Y y R2, tomados junto con los átomos de carbono con los que están unidos, forman un enlace, en el entendido de que n es 1; R4 es hidrógeno; ó R4 e Y, tomados junto con los átomos de carbono con los que están unidos, forman un enlace, en el entendido de que n es 1, y R2 y R3, tomados junto con los átomos de carbono con los que están unidos, forman un enlace; o L es un radical de la fórmula (3), en donde R1 es hidrógeno, alquilo opcionalmente sustituido, arilo, heteroarilo, aralquilo, o cicloalquilo; R" es hidrógeno, alquilo opcionalmente sustituido, alcoxilo, o halógeno; m es un entero de 1 a 2; Y es hidrógeno; R4 es hidrógeno; ó R4 e Y, tomados junto con los átomos de carbono con los que están unidos, forman un enlace, en el entendido de que m es 1; R y R' son independientemente hidrógeno, halógeno, alquilo opcionalmente sustituido, alcoxilo, aralquilo, o heteroaralquilo; ó R y R' combinados juntos, forman un grupo metilendioxilo, en el entendido de que R y R' están unidos a los átomos de carbono adyacentes uno al otro; o R y R' combinados junto con los átomos de carbono con los que están unidos, forman un anillo aromático o heteroaromático de 5 a 6 miembros opcionalmente sustituidos, en el entendido de que R y R' están unidos a los átomos de carbono adyacentes uno al otro; ó R-C y R'-C pueden ser independientemente reemplazados por nitrógeno; X es -Z-(CH2)p-Q-W, en donde Z es un enlace, O, S, -C(O)-, ó -C(O)NR5-, en donde R5 es hidrógeno, alquilo, o aralquilo; p es un entero de 1 a 8; Q es un enlace, en el entendido de que Z no es un enlace cuando p es 1; ó Q es -O(CH2)r- ó -S(CH2)r-, en donde r es cero ó un entero de 1 a 8; ó Q es -C(CH2)1-8O-, -S(CH2)1-8O-, -S(CH2)1-8S-, -C(O)- ó -C(O)NR6-, en donde R6 es hidrógeno, alquilo opcionalmente sustituido, cicloalquilo, arilo, heteroarilo, aralquilo, o heteroaralquilo; ó Q es -NR6-, -NR5C(O)-, -NR5C(O)NH-, ó -NR5C(O)O-, en el entendido de que p no es 1; W es cicloalquilo, arilo, heterociclilo, aralquilo, o heteroaralquilo; ó W y R6, tomados junto con el átomo de carbono con el que están unidos, forman un anillo bicíclico de 8 a 12 miembros, que opcionalmente pueden estar sustituido o puede contener otro heteroátomo seleccionado a partir de oxígeno, nitrógeno, y azufre; o una sal farmacéuticamente aceptable del mismo; o un isómero óptico del mismo; o una mezcla de isómeros ópticos del mismo, composiciones farmacéuticas, el uso de dichos derivados para la fabricación de medicamentos que son potentes agonistas de los Receptores Activados por el Proliferador de Peroxisoma (PPARs). De acuerdo con lo anterior, los compuestos son útiles para el tratamiento de condiciones mediadas por la actividad del receptor PPAR en mamíferos. Estas condiciones incluyen dislipidemia, hiperlipidemia, hipercolesteremia, aterosclerosis, hipertrigliceridemia, insuficiencia cardíaca, infarto del miocardio, enfermedades vasculares, enfermedades cardiovasculares, hipertensión, obesidad, inflamación, artritis, cáncer, enfermedad de Alzheimer, desordenes de la piel, enfermedades respiratorias, desórdenes oftálmicos, enfermedades inflamatorias del intestino, colitis ulcerativa, y enfermedad de Crohn. Los compuestos son particularmente útiles en mamíferos como agentes hipoglicémicos para el tratamiento y la prevención de condiciones en donde estén implicadas una tolerancia deteriorada a la glucosa, hiperglicemia, y resistencia a la insulina, tales como diabetes tipo 1 y tipo 2, y síndrome X. Se prefieren que son agonistas dobles de los receptores PPARa y PPARg. También se describe un método para la preparación de un agente alquilante.
ARP020104451A 2001-11-21 2002-11-20 Derivados de bencensulfonilo, una composicion farmaceutica que los comprende, el uso de dichos derivados para la fabricacion de un medicamento para el tratamiento asociado al receptor retinoide x, un metodo para la preparacion de un agente alquilante AR037655A1 (es)

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US33198601P 2001-11-21 2001-11-21
US39690602P 2002-07-18 2002-07-18

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JP (2) JP4171700B2 (es)
KR (1) KR100607019B1 (es)
CN (2) CN100429201C (es)
AR (1) AR037655A1 (es)
AT (1) ATE370931T1 (es)
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Families Citing this family (83)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20030139434A1 (en) † 2000-01-21 2003-07-24 Bork Balkan Combinations comprising dipeptidylpeptidase-iv inhibitor
ES2311117T3 (es) * 2002-12-10 2009-02-01 Novartis Ag Combinacion de un inhibidor de dpp-iv y un compuesto ppar-alfa.
DE10300099A1 (de) * 2003-01-07 2004-07-15 Bayer Healthcare Ag Indol-Phenylsulfonamid-Derivate
DE10308351A1 (de) 2003-02-27 2004-11-25 Aventis Pharma Deutschland Gmbh 1,3-substituierte Cycloalkylderivate mit sauren, meist heterocyclischen Gruppen, Verfahren zu ihrer Herstellung und ihre Verwendung als Arzneimittel
PT1638963E (pt) * 2003-05-20 2009-11-18 Novartis Ag Heterociclos de azoto n-acilado como ligandos de receptores activados pelo proliferador peroxissomal
BRPI0412380A (pt) * 2003-07-08 2006-09-19 Novartis Ag compostos de benzenossulfonilamino e composições farmacêuticas que contêm esses compostos
DE10335449A1 (de) * 2003-08-02 2005-02-17 Bayer Healthcare Ag Bicyclische Indolinsulfonamid-Derivate
US20080125403A1 (en) 2004-04-02 2008-05-29 Merck & Co., Inc. Method of Treating Men with Metabolic and Anthropometric Disorders
FR2869904B1 (fr) * 2004-05-07 2006-07-28 Fournier S A Sa Lab Modulateurs des recepteurs lxr
AR050631A1 (es) * 2004-09-09 2006-11-08 Novartis Ag Combinacion de compuestos organicos
CA2593483A1 (en) * 2005-01-18 2006-07-27 Novartis Ag Methods of use of dual ppar agonist compounds and drug delivery devices containing such compounds
US7429667B2 (en) 2005-01-20 2008-09-30 Ardea Biosciences, Inc. Phenylamino isothiazole carboxamidines as MEK inhibitors
FR2886293B1 (fr) 2005-05-30 2007-08-24 Fournier S A Sa Lab Nouveaux composes de l'indoline
JP2008542355A (ja) 2005-05-31 2008-11-27 ファイザー株式会社 Ｖｒ１アンタゴニストとしての置換アリールオキシ−ｎ−ビシクロメチルアセトアミド化合物
WO2007008541A2 (en) * 2005-07-08 2007-01-18 Kalypsys, Inc. Cellular cholesterol absorption modifiers
GT200600302A (es) * 2005-07-13 2007-03-19 Agonistas de ppara/y y procesos de preparación
PE20070427A1 (es) 2005-08-30 2007-04-21 Novartis Ag Compuestos derivados de benzimidazoles sustituidos como inhibidores de tirosina quinasas
JP2009514974A (ja) * 2005-11-07 2009-04-09 アイアールエム・リミテッド・ライアビリティ・カンパニー Ｐｐａｒモジュレーターとしての化合物および組成物
GB0526257D0 (en) * 2005-12-22 2006-02-01 Novartis Ag Organic compounds
EP2402319B1 (en) 2006-03-31 2017-08-30 Novartis AG DGAT Inhibitors
WO2007121269A2 (en) 2006-04-11 2007-10-25 Ardea Biosciences, Inc. N-aryl-n'alkyl sulfamides as mek inhibitors
PE20080184A1 (es) 2006-04-11 2008-03-28 Novartis Ag Derivados de aza-biciclo[3.2.1]octan en el tratamiento de diabetes
EP2012786B1 (en) 2006-04-18 2010-10-06 Ardea Biosciences, Inc. Pyridone sulfonamides and pyridone sulfamides as mek inhibitors
AR063311A1 (es) 2006-10-18 2009-01-21 Novartis Ag Compuestos organicos
EP2527360B1 (en) 2007-06-04 2015-10-28 Synergy Pharmaceuticals Inc. Agonists of guanylate cyclase useful for the treatment of gastrointestinal disorders, inflammation, cancer and other disorders
US8034782B2 (en) 2008-07-16 2011-10-11 Synergy Pharmaceuticals, Inc. Agonists of guanylate cyclase useful for the treatment of gastrointestinal disorders, inflammation, cancer and other disorders
US8969514B2 (en) 2007-06-04 2015-03-03 Synergy Pharmaceuticals, Inc. Agonists of guanylate cyclase useful for the treatment of hypercholesterolemia, atherosclerosis, coronary heart disease, gallstone, obesity and other cardiovascular diseases
US20100120694A1 (en) 2008-06-04 2010-05-13 Synergy Pharmaceuticals, Inc. Agonists of Guanylate Cyclase Useful for the Treatment of Gastrointestinal Disorders, Inflammation, Cancer and Other Disorders
UA99731C2 (ru) 2007-07-30 2012-09-25 Ардеа Биосайенсис, Инк Кристаллические полиморфные формы n-(ариламино)сульфонамидов как ингибиторы мэк, композиция (варианты) и применение
ES2499018T3 (es) 2007-09-20 2014-09-26 Irm Llc Compuestos y composiciones como moduladores de la actividad de GPR119
US9305735B2 (en) 2007-09-28 2016-04-05 Brigham Young University Reinforced polymer x-ray window
US20100285271A1 (en) 2007-09-28 2010-11-11 Davis Robert C Carbon nanotube assembly
US8498381B2 (en) 2010-10-07 2013-07-30 Moxtek, Inc. Polymer layer on X-ray window
EP2380631A1 (en) 2008-07-15 2011-10-26 Novartis AG Heteroaryl derivatives as DGAT1 inhibitors
US8247971B1 (en) 2009-03-19 2012-08-21 Moxtek, Inc. Resistively heated small planar filament
EP2411366B8 (en) 2009-03-27 2015-07-15 Ardea Biosciences, Inc. Dihydropyridin sulfonamides and dihydropyridin sulfamides as mek inhibitors
WO2010114636A1 (en) * 2009-04-03 2010-10-07 Mount Sinai School Of Medicine Of New York University Compositions for treatment of alzheimer's disease
WO2011014520A2 (en) 2009-07-29 2011-02-03 Irm Llc Compounds and compositions as modulators of gpr119 activity
EP2486033A1 (en) 2009-10-09 2012-08-15 Irm Llc Compounds and compositions as modulators of gpr119 activity
EP2947073B1 (en) * 2009-10-22 2019-04-03 Fibrotech Therapeutics Pty Ltd Fused ring analogues of anti-fibrotic agents
US8394858B2 (en) 2009-12-03 2013-03-12 Novartis Ag Cyclohexane derivatives and uses thereof
US7983394B2 (en) 2009-12-17 2011-07-19 Moxtek, Inc. Multiple wavelength X-ray source
US8697739B2 (en) 2010-07-29 2014-04-15 Novartis Ag Bicyclic acetyl-CoA carboxylase inhibitors and uses thereof
US20130156720A1 (en) 2010-08-27 2013-06-20 Ironwood Pharmaceuticals, Inc. Compositions and methods for treating or preventing metabolic syndrome and related diseases and disorders
US9616097B2 (en) 2010-09-15 2017-04-11 Synergy Pharmaceuticals, Inc. Formulations of guanylate cyclase C agonists and methods of use
US8526574B2 (en) 2010-09-24 2013-09-03 Moxtek, Inc. Capacitor AC power coupling across high DC voltage differential
ES2618411T3 (es) 2010-10-07 2017-06-21 Novartis Ag Nuevas formas cristalinas de la sal sódica de ácido (4-{4-[5-(6-trifluorometil-piridin-3-ilamino)-piridin-2-il]-fenil}-ciclohexil)-acético
AP3807A (en) 2011-01-13 2016-09-30 Novartis Ag Novel heterocyclic derivatives and their use in the treatment of neurological disorders
MX2013008192A (es) 2011-01-13 2013-12-16 Novartis Ag Inhibidores de bace-2 para tratamiento de transtornos metabolicos.
US8804910B1 (en) 2011-01-24 2014-08-12 Moxtek, Inc. Reduced power consumption X-ray source
US8750458B1 (en) 2011-02-17 2014-06-10 Moxtek, Inc. Cold electron number amplifier
US8929515B2 (en) 2011-02-23 2015-01-06 Moxtek, Inc. Multiple-size support for X-ray window
US8792619B2 (en) 2011-03-30 2014-07-29 Moxtek, Inc. X-ray tube with semiconductor coating
CN103619862A (zh) 2011-04-14 2014-03-05 诺瓦提斯公司 糖苷衍生物及其用途
US8614195B2 (en) 2011-04-14 2013-12-24 Novartis Ag Glycoside derivatives and uses thereof
US9076628B2 (en) 2011-05-16 2015-07-07 Brigham Young University Variable radius taper x-ray window support structure
US9174412B2 (en) 2011-05-16 2015-11-03 Brigham Young University High strength carbon fiber composite wafers for microfabrication
US8989354B2 (en) 2011-05-16 2015-03-24 Brigham Young University Carbon composite support structure
EA201490228A1 (ru) 2011-07-08 2014-08-29 Новартис Аг Новые производные трифторметилоксадиазола и их применение для лечения заболевания
UY34278A (es) 2011-08-25 2013-04-05 Novartis Ag Derivados novedosos de oxazina y su uso en el tratamiento de enfermedades
WO2013043744A2 (en) 2011-09-21 2013-03-28 Inception 1, Inc. Tricyclic compounds useful as neurogenic and neuroprotective agents
BR112014008686A2 (pt) 2011-10-13 2017-04-25 Novartis Ag derivados de oxazina e uso dos mesmos no tratamento de doença
EA201491060A1 (ru) 2011-11-28 2014-09-30 Новартис Аг Новые производные трифторметилоксадиазола и их применение для лечения заболевания
US20150004144A1 (en) 2011-12-02 2015-01-01 The General Hospital Corporation Differentiation into brown adipocytes
US8761344B2 (en) 2011-12-29 2014-06-24 Moxtek, Inc. Small x-ray tube with electron beam control optics
WO2013160873A1 (en) 2012-04-27 2013-10-31 Novartis Ag Cyclic bridgehead ether dgat1 inhibitors
EP2841432A1 (en) 2012-04-27 2015-03-04 Novartis AG Tetrahydropyran dgat1 inhibitors
WO2014052619A1 (en) 2012-09-27 2014-04-03 Irm Llc Piperidine derivatives and compositions as modulators of gpr119 activity
AU2014205276B2 (en) 2013-01-11 2016-10-20 Novartis Ag Meglumine salt forms of 2-((1 R,4R)-4-(4-(5-(benzoxazol-2-ylamino)pyridin-2-yl)phenyl)cyclohexyl) acetic acid and their use as DGAT1 inhibitors
US9173623B2 (en) 2013-04-19 2015-11-03 Samuel Soonho Lee X-ray tube and receiver inside mouth
EA201592263A1 (ru) 2013-06-05 2016-05-31 Синерджи Фармасьютикалз, Инк. Ультрачистые агонисты гуанилатциклазы c, способ их получения и использования
EP3157947A1 (en) 2014-06-23 2017-04-26 Novartis AG Hsa-gdf-15 fusion polypeptide and use thereof
US10588980B2 (en) 2014-06-23 2020-03-17 Novartis Ag Fatty acids and their use in conjugation to biomolecules
JP6946304B2 (ja) 2015-12-22 2021-10-06 ノバルティス アーゲー 増殖分化因子１５（ｇｄｆ−１５）を使用して代謝障害を処置するまたは軽快させる方法
EP3437651A1 (en) 2017-08-03 2019-02-06 Université de Strasbourg Peptides for treatment and prevention of nonalcoholic fatty liver disease
CN111432829B (zh) 2017-12-14 2023-07-14 斯特拉斯堡大学 用于治疗和预防非酒精性脂肪肝病和纤维化的肽
WO2020110008A1 (en) 2018-11-27 2020-06-04 Novartis Ag Cyclic pentamer compounds as proprotein convertase subtilisin/kexin type 9 (pcsk9) inhibitors for the treatment of metabolic disorder
UY38485A (es) 2018-11-27 2020-06-30 Novartis Ag Compuestos tetrámeros cíclicos como inhibidores de proproteína convertasa subtilisina/kexina tipo 9 (pcsk9), método de tratamiento, uso y su preparación
EP3887388A1 (en) 2018-11-27 2021-10-06 Novartis AG Cyclic peptides as proprotein convertase subtilisin/kexin type 9 (pcsk9) inhibitors for the treatment of metabolic disorders
RS64265B1 (sr) 2018-12-21 2023-07-31 Univ Strasbourg Peptidi za lečenje i prevenciju dijabetesa i povezanih poremećaja
WO2022219495A1 (en) 2021-04-12 2022-10-20 Novartis Ag 2-((4-((s)-2-(4-chloro-2-fluorophenyl)-2-methylbenzo[d][1,3]dioxol-4-yl)piperidin-1-yl)methyl)-1-(((s)-oxetan-2-yl)methyl)-1h-imidazole derivatives as activators of the glp1 receptor for the treatment of obesity
WO2023084449A1 (en) 2021-11-12 2023-05-19 Novartis Ag Diaminocyclopentylpyridine derivatives for the treatment of a disease or disorder
WO2023152698A1 (en) 2022-02-10 2023-08-17 Novartis Ag 2-((4-((s)-2-(4-chloro-2-fluorophenyl)-2-methylbenzo[d][1,3]dioxol-4-yl)piperidin-1-yl)methyl)-1-(((s)-oxetan-2-yl)methyl)-1h-imidazole derivatives as activators of the glp1 receptor for the treatment of obesity

Family Cites Families (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB8525578D0 (en) * 1985-10-17 1985-11-20 Hoffmann La Roche Heterocyclic compounds
JP2606735B2 (ja) * 1988-02-19 1997-05-07 石原産業株式会社 ２―アミノ―４，６―ジクロロピリミジンの製造方法
US5036153A (en) * 1989-05-11 1991-07-30 Braish Tamim F Preparation of 2,5-diazabicyclo[2.2.1]heptanes and intermediates
PT98673B (pt) * 1990-08-15 1999-01-29 British Bio Technology Processo para a preparacao de compostos que sao antagonistas do factor de activacao de plaquetas por exemplo derivados de benzimidazole e de seus intermediarios
DE4206045A1 (de) 1992-02-27 1993-09-02 Bayer Ag Sulfonylbenzyl substituierte pyridone
US5795890A (en) * 1995-09-27 1998-08-18 Ono Pharmaceutical Co., Ltd. Sulfonamide derivatives
FR2765222B1 (fr) * 1997-06-27 1999-12-31 Fournier Ind & Sante Nouveaux composes de n-benzenesulfonyl-l-proline, procede de preparation et utilisation en therapeutique
CO5011105A1 (es) 1997-12-22 2001-02-28 Novartis Ag Compuestos organicos para tratar la obesidad y desordenes relacionados, composiciones farmaceuticas que los comprenden y procesos para su preparacion
UY25842A1 (es) * 1998-12-16 2001-04-30 Smithkline Beecham Corp Antagonistas de receptores de il-8
FR2790260B1 (fr) * 1999-02-26 2001-05-04 Fournier Ind & Sante Nouveaux composes de n-(benzenesulfonamide), procede de preparation et utilisation en therapeutique
YU72201A (sh) 1999-04-28 2005-07-19 Aventis Pharma Deutschland Gmbh. Derivati di-aril kiseline kao ppar receptorski ligandi
DK1206457T3 (da) * 1999-08-27 2004-02-16 Lilly Co Eli Biaryl-oxa(thia)zolderivater og deres anvendelse som modulatorer PPAP'ER

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