AR088596A1 - Compuestos de bencilamina sustituidos - Google Patents

Compuestos de bencilamina sustituidos

Info

Publication number
AR088596A1
AR088596A1 ARP120104076A AR088596A1 AR 088596 A1 AR088596 A1 AR 088596A1 AR P120104076 A ARP120104076 A AR P120104076A AR 088596 A1 AR088596 A1 AR 088596A1
Authority
AR
Argentina
Prior art keywords
group
alkyl
optionally substituted
hydroxy
hydrogen
Prior art date
Application number
Other languages
English (en)
Inventor
Charles Frederick Hamlett Christopher
Ebai Besong Gilbert
James Woodhead Andrew
Chessari Gianni
Douglas Hiscock Steven
Norton David
Maria Saalau-Bethell Susanne
Thomas Thompson Neil
Maria Gerarda Willems Hendrika
Grazia Carr Maria
Millemaggi Alessia
Original Assignee
Astex Therapeutics Ltd
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
Priority claimed from GB201118874A external-priority patent/GB201118874D0/en
Priority claimed from GBGB1118875.2A external-priority patent/GB201118875D0/en
Application filed by Astex Therapeutics Ltd filed Critical Astex Therapeutics Ltd
Publication of AR088596A1 publication Critical patent/AR088596A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C225/00—Compounds containing amino groups and doubly—bound oxygen atoms bound to the same carbon skeleton, at least one of the doubly—bound oxygen atoms not being part of a —CHO group, e.g. amino ketones
    • C07C225/02—Compounds containing amino groups and doubly—bound oxygen atoms bound to the same carbon skeleton, at least one of the doubly—bound oxygen atoms not being part of a —CHO group, e.g. amino ketones having amino groups bound to acyclic carbon atoms of the carbon skeleton
    • C07C225/14—Compounds containing amino groups and doubly—bound oxygen atoms bound to the same carbon skeleton, at least one of the doubly—bound oxygen atoms not being part of a —CHO group, e.g. amino ketones having amino groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being unsaturated
    • C07C225/16—Compounds containing amino groups and doubly—bound oxygen atoms bound to the same carbon skeleton, at least one of the doubly—bound oxygen atoms not being part of a —CHO group, e.g. amino ketones having amino groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being unsaturated and containing six-membered aromatic rings
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/13—Amines
    • A61K31/135—Amines having aromatic rings, e.g. ketamine, nortriptyline
    • A61K31/138—Aryloxyalkylamines, e.g. propranolol, tamoxifen, phenoxybenzamine
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/275—Nitriles; Isonitriles
    • A61K31/277—Nitriles; Isonitriles having a ring, e.g. verapamil
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—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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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • 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
    • A61K31/425—Thiazoles
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4965—Non-condensed pyrazines
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    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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    • A61K31/33—Heterocyclic compounds
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    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
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    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
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    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2013—Organic compounds, e.g. phospholipids, fats
    • A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
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    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841—Filling excipients; Inactive ingredients
    • A61K9/4858—Organic compounds
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
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    • A61P35/00—Antineoplastic agents
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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    • C07C221/00—Preparation of compounds containing amino groups and doubly-bound oxygen atoms bound to the same carbon skeleton
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    • C07C225/00—Compounds containing amino groups and doubly—bound oxygen atoms bound to the same carbon skeleton, at least one of the doubly—bound oxygen atoms not being part of a —CHO group, e.g. amino ketones
    • C07C225/02—Compounds containing amino groups and doubly—bound oxygen atoms bound to the same carbon skeleton, at least one of the doubly—bound oxygen atoms not being part of a —CHO group, e.g. amino ketones having amino groups bound to acyclic carbon atoms of the carbon skeleton
    • C07C225/14—Compounds containing amino groups and doubly—bound oxygen atoms bound to the same carbon skeleton, at least one of the doubly—bound oxygen atoms not being part of a —CHO group, e.g. amino ketones having amino groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being unsaturated
    • C07C225/16—Compounds containing amino groups and doubly—bound oxygen atoms bound to the same carbon skeleton, at least one of the doubly—bound oxygen atoms not being part of a —CHO group, e.g. amino ketones having amino groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being unsaturated and containing six-membered aromatic rings
    • C07C225/18—Compounds containing amino groups and doubly—bound oxygen atoms bound to the same carbon skeleton, at least one of the doubly—bound oxygen atoms not being part of a —CHO group, e.g. amino ketones having amino groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being unsaturated and containing six-membered aromatic rings the carbon skeleton containing also rings other than six-membered aromatic rings
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    • C07C225/22—Compounds containing amino groups and doubly—bound oxygen atoms bound to the same carbon skeleton, at least one of the doubly—bound oxygen atoms not being part of a —CHO group, e.g. amino ketones having amino groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton
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    • C07C229/00—Compounds containing amino and carboxyl groups bound to the same carbon skeleton
    • C07C229/38—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino groups bound to acyclic carbon atoms and carboxyl groups bound to carbon atoms of six-membered aromatic rings of the same carbon skeleton
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    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C237/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
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    • C07C237/04—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being acyclic and saturated
    • C07C237/06—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being acyclic and saturated having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
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    • C07C237/04—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being acyclic and saturated
    • C07C237/10—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being acyclic and saturated having the nitrogen atom of at least one of the carboxamide groups bound to an acyclic carbon atom of a hydrocarbon radical substituted by nitrogen atoms not being part of nitro or nitroso groups
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    • C07C237/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
    • C07C237/24—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a ring other than a six-membered aromatic ring of the carbon skeleton
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    • C07C237/28—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a non-condensed six-membered aromatic ring of the carbon skeleton
    • C07C237/30—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a non-condensed six-membered aromatic ring of the carbon skeleton having the nitrogen atom of the carboxamide group bound to hydrogen atoms or to acyclic carbon atoms
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    • C07C253/00—Preparation of carboxylic acid nitriles
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    • C07C255/49—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C255/58—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing cyano groups and singly-bound nitrogen atoms, not being further bound to other hetero atoms, bound to the carbon skeleton
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    • C07C313/00—Sulfinic acids; Sulfenic acids; Halides, esters or anhydrides thereof; Amides of sulfinic or sulfenic acids, i.e. compounds having singly-bound oxygen atoms of sulfinic or sulfenic groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
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    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/44—Radicals substituted by doubly-bound oxygen, sulfur, or nitrogen atoms, or by two such atoms singly-bound to the same carbon atom
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    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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

La presente provee compuestos que son útiles en el tratamiento de infecciones por virus de hepatitis C (HCV). Reivindicación 1: Un compuesto, caracterizado porque es de la fórmula (1), o una sal, N-óxido, tautómero o estereoisómero del mismo, donde: A es CH o nitrógeno; E es CH o nitrógeno; R¹ se selecciona entre: un grupo hidrocarbonado acíclico C₁₋₈ opcionalmente sustituido con uno o dos sustituyentes R⁶, donde un átomo de carbono del grupo hidrocarbonado acíclico C₁₋₈ puede reemplazarse opcionalmente por un heteroátomo o un grupo seleccionado entre O, S, NRᶜ, S(O) y SO₂, o dos átomos de carbono adyacentes del grupo hidrocarbonado acíclico C₁₋₈ pueden reemplazarse opcionalmente por un grupo seleccionado entre CONRᶜ, NRᶜCO, NRᶜSO₂ y SO₂NRᶜ con la condición de que en cada caso exista al menos un átomo de carbono del grupo hidrocarbonado acíclico C₁₋₈; y un grupo carbocíclico o heterocíclico monocíclico de entre 3 y 7 miembros del anillo, de los cuales 0, 1, 2, 3 ó 4 son heteroátomos como miembros del anillo seleccionados entre O, N y S, donde el grupo carbocíclico o heterocíclico está opcionalmente sustituido con uno o dos sustituyentes R⁷ᵃ; R² se selecciona entre hidrógeno y un grupo X-R⁸; X es un grupo alcandiilo C₁₋₈ donde un átomo de carbono del grupo alcandiilo C₁₋₈ puede estar unido opcionalmente a una unidad -CH₂-CH₂- para formar un grupo ciclopropan-1,1-diilo o dos átomos de carbono adyacentes del grupo alcandiilo C₁₋₈ pueden estar unidos opcionalmente a una unidad -(CH₂)ₙ, donde n es entre 1 y 5, para formar un grupo cicloalcan C₃₋₇-1,2-diilo; R³ es un anillo carbocíclico o heterocíclico monocíclico o bicíclico de entre 3 y 10 miembros que contiene 0, 1, 2 ó 3 heteroátomos como miembros del anillo seleccionados entre N, O y S, y que está opcionalmente sustituido con uno o más sustituyentes R¹³; R⁴ se selecciona entre hidrógeno y un sustituyente R⁴ᵃ; R⁴ᵃ se selecciona entre halógeno; ciano; alquilo C₁₋₄ opcionalmente sustituido con uno o más átomos de flúor; alcoxi C₁₋₄ opcionalmente sustituido con uno o más átomos de flúor; hidroxi-alquilo C₁₋₄; y alcoxi C₁₋₂-alquilo C₁₋₄; R⁵ se selecciona entre hidrógeno y un sustituyente R⁵ᵃ; R⁵ᵃ se selecciona entre alquilo C₁₋₂ opcionalmente sustituido con uno o más átomos de flúor; alcoxi C₁₋₃ opcionalmente sustituido con uno o más átomos de flúor; halógeno; ciclopropilo; y ciano; R⁶ se selecciona entre hidroxi; flúor; carbamoilo; mono- o di-alquil C₁₋₄carbamoilo; nitro; amino; mono- o di-alquil C₁₋₄amino; un grupo carbocíclico o heterocíclico monocíclico de entre 3 y 7 miembros del anillo, de los cuales 0, 1 ó 2 son heteroátomos como miembros del anillo seleccionados entre O, N y S, donde el grupo carbocíclico o heterocíclico está opcionalmente sustituido con uno o dos sustituyentes R⁷ᵇ; R⁷ᵃ y R⁷ᵇ se seleccionan en forma independiente entre sí entre (=O); (=S); amino; halógeno; ciano; hidroxi; alquilo C₁₋₄; hidroxi-alquilo C₁₋₄; amino-alquilo C₁₋₄; mono- y di-alquil C₁₋₄amino-alquilo C₁₋₄; R⁸ se selecciona entre un grupo hidroxi y C(=O)NR¹⁰R¹¹; con la condición de que cuando R⁸ es hidroxi, existen al menos dos átomos de carbono en línea entre el grupo hidroxi y el átomo de nitrógeno al cual X está unido; R¹⁰ se selecciona entre hidrógeno y alquilo C₁₋₄; R¹¹ se selecciona entre hidrógeno; amino-alquilo C₂₋₄ y hidroxi-alquilo C₂₋₄; R¹³ se selecciona entre halógeno; ciano; (=O); (=S); nitro; CH=NOH; y un grupo Rᵃ-Rᵇ; Rᵃ es una unión, O, CO, X¹C(X²), C(X²)X¹, X¹C(X²)X¹, S, SO, SO₂, NRᶜ, o NRᶜSO₂; Rᵇ es hidrógeno; un grupo cíclico Rᵈ; o un grupo hidrocarbonado acíclico C₁₋₈ opcionalmente sustituido con uno o más sustituyentes seleccionados entre hidroxi, oxo, halógeno, ciano, nitro, carboxi, amino, mono- o di-alquil C₁₋₄amino, y un grupo cíclico Rᵈ; donde uno o dos pero no todos los átomos de carbono del grupo hidrocarbonado acíclico C₁₋₈ pueden reemplazarse opcionalmente por O, S, SO, SO₂, NRᶜ, X¹C(X²), C(X²)X¹ o X¹C(X²)X¹; SO₂NRᶜ o NRᶜSO₂; el grupo cíclico Rᵈ es un grupo carbocíclico o heterocíclico monocíclico con entre 3 y 7 miembros del anillo, de los cuales 0, 1, 2 ó 3 son heteroátomos como miembros del anillo seleccionados entre O, N y S y formas oxidadas de los mismos, donde el grupo carbocíclico o heterocíclico está opcionalmente sustituido con uno o más sustituyentes seleccionados entre R¹⁴; R¹⁴ se selecciona entre oxo; halógeno; ciano; y Rᵃ-Rᵉ; Rᵉ es hidrógeno o un grupo hidrocarbonado acíclico C₁₋₈ opcionalmente sustituido con uno o más sustituyentes seleccionados entre fenilo; hidroxi; oxo; halógeno; ciano; carboxi; amino; mono- o di-alquil C₁₋₄amino; donde uno o dos pero no todos los átomos de carbono del grupo hidrocarbonado acíclico C₁₋₈ pueden reemplazarse opcionalmente por O, S, SO, SO₂, NRᶜ, X¹C(X²), C(X²)X¹ o X¹C(X²)X¹; SO₂NRᶜ o NRᶜSO₂; X¹ es O ó NRᶜ; X² es =O ó NRᶜ; y Rᶜ es hidrógeno o alquilo C₁₋₄; pero excluyendo los compuestos 1-(3-benzoilfenil)-etilamina y 1-(3-furan-2-oilcarbonilfenil)-etilamina.
ARP120104076 2011-11-01 2012-10-31 Compuestos de bencilamina sustituidos AR088596A1 (es)

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AU2012331190A1 (en) 2014-04-10
TW201329025A (zh) 2013-07-16
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