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    Morfolina-Spiro piperidina amida cíclica como moduladores del canal iónico
    25.
    发明专利
    Morfolina-Spiro piperidina amida cíclica como moduladores del canal iónico 未知

    公开(公告)号：ES2618929T3

    公开(公告)日：2017-06-22

    申请号：ES12710841

    申请日：2012-03-13

    Applicant: VERTEX PHARMA

    Inventor： HADIDA-RUAH SARA ,  BINCH HAYLEY ,  DENINNO MICHAEL ,  FANNING LEV ,  FRIEMAN BRYAN ,  GROOTENHUIS PETER ,  HILGRAF NICOLE ,  JOSHI PRAMOD ,  KALLEL EDWARD ,  PONTILLO JOSEPH ,  SILINA ALINA ,  SHETH URVI ,  HURLEY DENNIS ,  ARUMUGAM VIJAYALAKSMI ,  MILLER MARK

    IPC: C07D498/10 ,  A61K31/424 ,  A61P29/00

    Abstract: Un compuesto de fórmula I:**Fórmula** o una sal farmacéuticamente aceptable del mismo, en la que, independientemente para cada caso: R1 es alquilo C1-C6, fluoroalquilo C1-C6, cicloalquilo C3-C8, halo, NR8SO2R8, SO2R8, SR8, SOR8, NR8COR8, NR8CO2R8, CN, CON(R8)2, SO2N(R8)2, CF3, heterocicloalquilo, fenilo, heteroarilo, o una cadena lineal, ramificada o cíclica (C1-C8)-R9 en donde hasta dos unidades CH2 pueden reemplazarse con O, CO, S, SO, SO2, N, CF2, o NR8; R2 es alquilo C1-C6, alquilo C1-C6, fluoroalquilo, cicloalquilo, arilo, heteroarilo, o heterocicloalquilo, COR8, CO2R8, CON(R8)2, CF3, CHF2, o una cadena lineal, ramificada, o cíclica (C1-C8)-R9 en la que hasta dos unidades CH2 pueden reemplazarse por O, CO, S, SO, SO2, N, CF2, o NR8; R3 es alquilo C1-C6 o halo; R8es H, alquilo C1-C6, o cicloalquilo C3-C8, de cadena lineal, ramificada o cíclica (C1-C8)-R9 en la que hasta dos unidades CH2 pueden reemplazarse por O, CO, S, SO, SO2, N, CF2, o NR, O2R8 tomados junto con los átomos a los que están unidos forman un anillo; R9 es H, CF3, CHF2, CH2F, CO2R, OH, arilo, heteroarilo, cicloalquilo Cicloalquilo C3-C8, heterocicloalquilo, N(R)2, NRCOR, CON(R)2, CN,O SO2R; R es H, alquilo C1-C6, arilo, heteroarilo, cicloalquilo C3-C8, o heterocicloalquilo; A es un arilo, heteroarilo o heterocíclico; n es un número entero de 1 a 4 inclusive; y o es un número entero de 0 a 4 inclusive; donde cada alquilo, fluoroalquilo, cicloalquilo, heterocicloalquilo, fenilo, heteroarilo, cicloalquilo C3-C8, o arilo de R1 a R8 se sustituye ontionalmente con uno o más sustituyentes seleccionados de halo, ciano, oxoalcoxi, hidroxi, amino, nitro, arilo, haloalquilo, y alquilo.

    ARYL AMIDES USEFUL AS INHIBITORS OF VOLTAGE-GATED SODIUM CHANNELS
    28.
    发明专利
    ARYL AMIDES USEFUL AS INHIBITORS OF VOLTAGE-GATED SODIUM CHANNELS 未知

    公开(公告)号：NZ584519A

    公开(公告)日：2012-07-27

    申请号：NZ58451908

    申请日：2008-10-10

    Applicant: VERTEX PHARMA

    Inventor： CHEN WEICHUAN CAROLINE ,  KRENITSKY PAUL ,  TERMIN ANDREAS ,  WILSON DEAN ,  JOSHI PRAMOD

    IPC: C07D213/65 ,  A61K31/33 ,  A61P19/02 ,  C07C233/64 ,  C07D213/643

    Abstract: The disclosure relates to aryl amide compounds of formula (I) which are useful as inhibitors of voltage-gated sodium channels, wherein the variables shown in formula (I) are as defined in the specification. The disclosure also relates to pharmaceutically acceptable compositions comprising these compounds and their use for treating or lessening the severity in a subject of one or more of acute, chronic, neuropathic, or inflammatory pain, arthritis, migraine, cluster headaches, trigeminal neuralgia, herpetic neuralgia, general neuralgias, epilepsy or epilepsy conditions, neurodegenerative disorders, psychiatric disorders such as anxiety and depression, dipolar disorder, myotonia, arrhythmia, movement disorders, neuroendocrine disorders, ataxia, multiple sclerosis, irritable bowel syndrome, incontinence, visceral pain, osteoarthritis pain, postherpetic neuralgia, diabetic neuropathy, radicular pain, sciatica, back pain, head or neck pain, severe or intractable pain, nociceptive pain, breakthrough pain, postsurgical pain, cancer pain, stroke, cerebral ischemia, traumatic brain injury, amyotrophic lateral sclerosis, stress- or exercise induced angina, palpitations, hypertension, migraine, or abnormal gastro-intestinal motility.

    29.
    发明专利
    未知

    公开(公告)号：AT540033T

    公开(公告)日：2012-01-15

    申请号：AT06837387

    申请日：2006-11-13

    Applicant: VERTEX PHARMA

    Inventor： WILSON DEAN ,  FANNING LEV T D ,  KRENITSKY PAUL ,  TERMIN ANDREAS ,  JOSHI PRAMOD ,  SHETH URVI

    IPC: C07D403/04

    Abstract: The present invention relates to compounds useful as inhibitors of voltage-gated sodium channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.

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