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AR063211A1 - Derivados de 3-(piridin-3-il)acrilamida y 3-(piridin-3-il)propionamida, un metodo para su preparacion, una composicion farmaceutica que los comprende y su uso en la fabricacion de medicamentos para el tratamiento de enfermedades asociadas con el receptor vaniloide. - Google Patents

Derivados de 3-(piridin-3-il)acrilamida y 3-(piridin-3-il)propionamida, un metodo para su preparacion, una composicion farmaceutica que los comprende y su uso en la fabricacion de medicamentos para el tratamiento de enfermedades asociadas con el receptor vaniloide.

Info

Publication number
AR063211A1
AR063211A1 ARP070103317A ARP070103317A AR063211A1 AR 063211 A1 AR063211 A1 AR 063211A1 AR P070103317 A ARP070103317 A AR P070103317A AR P070103317 A ARP070103317 A AR P070103317A AR 063211 A1 AR063211 A1 AR 063211A1
Authority
AR
Argentina
Prior art keywords
alkyl
alkoxy
unsubstituted
substituted
halogen
Prior art date
Application number
ARP070103317A
Other languages
English (en)
Original Assignee
Amorepacific Corp
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 EP06015724A external-priority patent/EP1882687A1/en
Application filed by Amorepacific Corp filed Critical Amorepacific Corp
Publication of AR063211A1 publication Critical patent/AR063211A1/es

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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
    • C07D213/60—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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    • C07D419/08—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing alicyclic rings
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    • C07C311/01—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms
    • C07C311/02—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
    • C07C311/08—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton having the nitrogen atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
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    • 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
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    • 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
    • C07D213/60—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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    • C07D295/14—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 carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
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  • Physical Education & Sports Medicine (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)

Abstract

Sales farmacéuticamente aceptables, como antagonistas del receptor vaniloide (receptor vaniloide 1; VR1; TRPV1); una composicion farmacéutica que las contiene y su uso en la fabricacion de medicamentos para prevenir o tratar una enfermedad como el dolor, migrana, artralgia, neuralgia, neuropatías, lesion nerviosa, trastorno cutáneo, hipersensibilidad de la vejiga urinaria, síndrome de intestino irritable, incontinencia fecal, trastorno respiratorio, irritacion de la piel, ojos o membrana mucosa, ulcera del estomago y duodeno, enfermedades inflamatorias, enfermedad auditiva, enfermedad cardíaca y otras, Se provee además un método para su preparacion. Reivindicacion 1: Un compuesto de la formula (1), su isomero, o una de sus sales farmacéuticamente aceptables: en donde: X es CR11=CR12, o C:::C; en donde, R11 y R12, si están presentes, son independientemente hidrogeno, halogeno o alquilo C1-5; Z es N; Y es CR6; R1 es hidrogeno, halogeno o alquilo C1-5; R2, R3, R4, y R5 son independientemente hidrogeno, halogeno, nitro, ciano, alquilo C1-5, alcoxi C1-5, haloalquilo C1-5, alquenilo C2-5, alquinilo C2-5, carboxi, alcoxicarbonilo C1-5 o alquiltio C1-5; R6 es hidroxi, halogeno, nitro, carboxi, alquil C1-10, alcoxilo C1-10, alquenilo C2-10, alquinilo C2-10, alquil C1-10tio, alquil C1-10sulfonilo, alquil C1-10carbonilo, alcoxilo C1-10carbonilo, alquenilo C2-10oxi, alcoxi C1-5-alcoxi C1-5, alcoxi C1-5-alcoxi C1-5-alquilo C1-5, piperidilo, piperacinilo, alcoxi C1-5-alquil C1-5amino, alquil C1-10amino, di(alquil C1-10)amino, cicloalquil C3-8 , cicloalquil C3-8 amino, cicloalcoxi C3-8, oxacicloalquiloxi C3-8, N-alcoxi C1-5-alquilC1-5-N-alquilC1-5amino, N-cicloalquil C3-8-N-alquil C1-5amino, N-aril-N-alquil C1-5amino, preferiblemente N-fenil-N-alquil C1-5amino, arilo, preferiblemente fenilo, arilamino, preferiblemente fenilamino, aritio, preferiblemente fenitio, heteroarilo, preferiblemente piridinilo o tienilo, heteroarilamino, ariloxi, preferiblemente fenoxi, heteroariloxi, preferiblemente piridiniloxi, pirrolidinilo o morfoIinilo, R8 y R9 son independientemente hidrogeno, hidroxi, halogeno, nitro, carboxi, alquil C1-10, alcoxilo C1-10, alquenilo C2-10, alquinilo C2-10, alquil C1-10tio, alquil C1- 10sulfonilo, alquil C1-10carbonilo, alcoxilo C1-10carbonilo, alquenilo C2-10oxi, alcoxi C1-5-alcoxi C1-5, alcoxi C1-5-alcoxi C1-5-alquilo C1-5, piperidilo, piperacinilo, alcoxi C1-5-alquil C1-5amino, alquil C1-10amino, di(alquil C1-10)amino, cicloalquil C3-8 , cicloalquil C3-8 amino, cicloalcoxi C3-8, oxacicloalquiloxi C3-8, N-alcoxi C1-5-alquilC1-5-N-alquilC1-5amino, N-cicloalquil C3-8-N-alquil C1-5amino, N-aril-N-alquil C1-5amino, preferiblemente N-fenil-N-alquil C1-5amino, arilo, preferiblemente fenilo, arilamino, preferiblemente fenilamino, aritio, preferiblemente fenitio, heteroarilo, preferiblemente piridinilo o tienilo, heteroarilamino, ariloxi, preferiblemente fenoxi, heteroariloxi, preferiblemente piridiniloxi, pirrolidinilo o morfoIinilo, en donde: cada alquilo, alquenilo y alquinilo, también como parte de un grupo tal como en alcoxi, alquilsulfonilo, alquilcarbonilo, alquilamino o alqueniloxi, puede estar independientemente sustituido o no sustituido con uno o más sustituyentes seleccionados de entre halogeno, hidroxilo, alcoxi C1-5 sustituido o no sustituido con una funcionalidad halo, cicloalquilo C3-8 que puede estar sustituido o no sustituido con uno o dos radicales halogeno y/o grupos metilo, alquilamino C1-5 sustituido o no sustituido con una funcionalidad halo, fenilo que puede estar sustituido o no sustituido con uno o más sustituyentes seleccionados de halogeno, alquil C1-3 no sustituido, o haloalquilo C1-3, o di(C1-5)alquilamino sustituido o no sustituido con funcionalidad halo, cada arilo o heteroarilo, también parte de un grupo tal como en arilamino, ariloxi, heteroarilamino o heteroariloxi, puede estar independientemente sustituido o no sustituido con uno o más sustituyentes seleccionados de halogeno, alquilo C1-5 no sustituido, alcoxi C1-5 no sustituido o haloalquilo C1-5, cada cicloalquilo, también como parte de un grupo tal como en el cicloalcoxi o cicloalquilamino, puede estar sustituido o no sustituido con uno o más grupos alquilo C1-3 sustituidos o no sustituidos con funcionalidad halo, hidroximetilo, hidroxi, metoxi o amino, y cada piperacinilo, piperidilo, morfolinilo y pirrolidinilo puede estar sustituido o no sustituido con uno o más grupos alquilo C1-3 sustituidos o no sustituidos con funcionalidad halo, hidroxialquilo C1-3, alcoxi C1-3, alcoxi C1-3carbonilo, o hidroxilo; R7 es haloalquilo C1-5; y R10 es alquilo C1-5, haloalquilo C1-5, o alquenilo C2-5. Reivindicacion 47: Un proceso para la elaboracion de un compuesto representado por la formula (3) que comprende la reaccion de un compuesto representado por la formula (4); con un compuesto representado por la formula (5); en donde: R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11 y R12 son como los descritos en una cualquiera de las reivindicaciones precedentes. Reivindicacion 49: Un compuesto de la formula (6) en donde W es hidrogeno o fluoro; R1 es hidrogeno o alquilo C1-3, preferiblemente metilo; y R10 es alquilo C1-3, alquenilo C2-3 o haloalquilo C1-3, preferiblemente metilo; con tal que si R1 es hidrogeno y R10 es metilo, entonces W es fluoro.
ARP070103317A 2006-07-27 2007-07-26 Derivados de 3-(piridin-3-il)acrilamida y 3-(piridin-3-il)propionamida, un metodo para su preparacion, una composicion farmaceutica que los comprende y su uso en la fabricacion de medicamentos para el tratamiento de enfermedades asociadas con el receptor vaniloide. AR063211A1 (es)

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US7858621B2 (en) 2010-12-28
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AU2007277519B2 (en) 2011-12-22
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