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AR079542A1 - Derivados de benzamida sustituidos, proceso para su preparacion y su uso en el tratamiento de enfermedades mediadas por taars. - Google Patents

Derivados de benzamida sustituidos, proceso para su preparacion y su uso en el tratamiento de enfermedades mediadas por taars.

Info

Publication number
AR079542A1
AR079542A1 ARP100104762A ARP100104762A AR079542A1 AR 079542 A1 AR079542 A1 AR 079542A1 AR P100104762 A ARP100104762 A AR P100104762A AR P100104762 A ARP100104762 A AR P100104762A AR 079542 A1 AR079542 A1 AR 079542A1
Authority
AR
Argentina
Prior art keywords
disorders
lower alkyl
phenyl
optionally substituted
heterocycloalkyl
Prior art date
Application number
ARP100104762A
Other languages
English (en)
Inventor
Roger Norcross
Philippe Pflieger
Zbinden Katrin Groebke
Original Assignee
Hoffmann La Roche
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=43544985&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR079542(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of AR079542A1 publication Critical patent/AR079542A1/es

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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
    • C07D207/06—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 radicals, containing only hydrogen and carbon atoms, attached to ring carbon atoms
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    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
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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
    • A61K31/4025—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 not condensed and containing further heterocyclic rings, e.g. cromakalim
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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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    • C07D207/08—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 hydrocarbon radicals, substituted by hetero atoms, attached to ring carbon atoms
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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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    • 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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    • C07D211/26—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings 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 hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by nitrogen atoms
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    • C07D295/135—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms with the ring nitrogen atoms and the substituent nitrogen atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
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  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)

Abstract

Compuestos de formula (1) en la que: R es hidrogeno o alquilo inferior; R1 es -(CH2)n-(O)o-heterocicloalquilo o -C(O)-heterocicloalquilo, en el que el grupo heterocicloalquilo se sustituye opcionalmente con alquilo inferior, hidroxi, halogeno o con -(CH2)p-arilo; n es 0, 1 o 2; o es 0 o 1; p es 0, 1 o 2; R2 es CF3, cicloalquilo, opcionalmente sustituido con alcoxi inferior o halogeno, o es indan-2-ilo, o es heterocicloalquilo, opcionalmente sustituido con heteroarilo, o es arilo o heteroarilo, en los que los anillos aromáticos se sustituyen opcionalmente con uno o dos sustituyentes, seleccionados de entre alquilo inferior, halogeno, heteroarilo, hidroxi, CF3, OCF3, OCH2CF3, OCH2-cicloalquilo, CH2C(CH2OH)(CH2CI)(CH3), S-alquilo inferior, alcoxi inferior, CH2-alcoxi inferior, alquinilo inferior o ciano, o con -C(O)-fenilo, -O-fenilo, -O-CH2-fenilo, fenilo o -CH2-fenilo, y en los que los anillos fenilo opcionalmente pueden sustituirse halogeno, -C(O)-alquilo inferior, -C(O)-OH o -C(O)-O-alquilo inferior, o los anillos aromáticos se sustituyen opcionalmente con heterocicloalquilo, OCH2-oxetan-3-ilo o O-tetrahidropiran-4-ilo, opcionalmente sustituidos con alquilo inferior; X es un enlace, -NR'-, -CH2NH-, -CHR''-, -(CHR'')q-O-, -O-(CHR'')q o (CH2)2; Y es un enlace o -CH2-; R' es hidrogeno o alquilo inferior; R'' es hidrogeno, alquilo inferior, CF3, alcoxi inferior; q es 0, 1, 2 o 3; o a una sal de adicion de ácido farmacéuticamente aceptable de los mismos. Ahora se ha encontrado que los compuestos de formula (1) presentan una buena afinidad con los receptores asociados a rastros de aminas (TAARs), especialmente con TAAR1. Los compuestos pueden utilizarse para el tratamiento de la depresion, los trastornos de ansiedad, el trastorno bipolar, el trastorno de hiperactividad por déficit de atencion (ADHD), los trastornos relacionados con el estrés, los trastornos psicoticos tales como la esquizofrenia, las enfermedades neurologicas tales como la enfermedad de Parkinson, los trastornos neurodegenerativos tales como la enfermedad de Alzheimer, la epilepsia, la migrana, la hipertension, el abuso de sustancias, y trastornos metabolicos tales como trastornos de la alimentacion, la diabetes, las complicaciones diabéticas, la obesidad, la dislipidemia, los trastornos del consumo y asimilacion de la energía, los trastornos y disfuncion de la homeostasis de la temperatura corporal, los trastornos del sueno y del ritmo circadiano, y los trastornos cardiovasculares.
ARP100104762A 2009-12-22 2010-12-20 Derivados de benzamida sustituidos, proceso para su preparacion y su uso en el tratamiento de enfermedades mediadas por taars. AR079542A1 (es)

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