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    PIROLOPIRAZIN-SPIROCIKLIČNI PIPERIDIN AMIDI KAO MODULATORI JONSKIH KANALA
    11.
    发明专利
    PIROLOPIRAZIN-SPIROCIKLIČNI PIPERIDIN AMIDI KAO MODULATORI JONSKIH KANALA 未知

    公开(公告)号：RS54785B1

    公开(公告)日：2016-10-31

    申请号：RSP20160229

    申请日：2012-02-02

    Applicant: VERTEX PHARMA

    Inventor： HADIDA RUAH SARA S ,  KALLEL EDWARD ADAM ,  MILLER MARK THOMAS ,  ARUMUGAM VIJAYALAKSMI ,  MCCARTNEY JASON ,  ANDERSON COREY ,  GROOTENHUIS PETER DIEDERIK JAN ,  JIANG LICONG

    IPC: C07D471/20 ,  A61K31/4985 ,  A61P25/00

    Abstract: Jedinjenje formule I:ili njegova farmaceutski prihvatljiva so, u kome, nezavisno od svakog slučaja:R1 je H, C1-C8 alkil, C3-C8 cikloalkil, halo, CN, NR8SO2R8, SO2R8, SR8, SOR8, NR8COR8, NR8CO2R8, CON(R8)2, SO2N(R8)2, CF3, heterocikloalkil ili linearni, razgranati ili ciklični (C1-C8)-R9 gde do dve CH2 jedinice mogu biti zamenjene sa O, CO, S, SO, SO2 ili NR8, ili dva R1 uzeta zajedno formiraju okso grupu, ili 3 do 7-člani fuzionisani cikloalkil prsten, ili 3 do 7-člani spirocikličan prsten;R2 je H, C1-C8 alkil, halo, C1-C8 haloalkil, CN, OH, SO2R8, SR8, SOR8, COR8, CO2R8, CON(R8)2, SO2N(R8)2, CF3, CHF2 ili linearni, razgranati ili ciklični (C1-C8)-R9 gde do dve CH2 jedinice mogu biti zamenjene sa O, CO, S, SO, SO2, CF2 ili NR ;R3 je H, C1-C8 alkil, C3-C8 cikloalkil, CO2R8, COR8, COH, CON(R8)2, CF3, CH2CF3, CH2CHF2 ili linearni, razgranati ili ciklični (C1-C8)-R9 gde do dve CHF2 jedinice mogu biti zamenjene sa O, CO, S, SO, SO2 ili NR8;R4 je H, C1-C8 alkil, halo, C3-C8 cikloalkil, gde do dve CH2 jedinice mogu biti zamenjene sa O, CO, S, SO, SO2 ili NR8, ili 2 R4 uzeti zajedno formiraju fuzionisani 3 do 7-člani cikloalkil prsten;R je H, C1-C8 alkil, CF3, C3-C8 cikloalkil, fluoroalkil, aril, heteroaril ili linearni, razgranati ili ciklični (C1-C8)-R9 gde do dve CH2 jedinice mogu biti zamenjene sa O, CO, S, SO, SO2 ili NR, ili 2 R uzeta zajedno sa atomima za koje su vezani formiraju prsten; R9 je H, CF3, CO2R, OH, aril, heteroaril, C3-C8 cikloalkil, heterocikloalkil, N(R)2, NRCOR, CON(R)2, CN, halo ili SO2R;R je H, C1-C8 alkil, aril, heteroaril, C3-C8 cikloalkil ili heterocikloalkil;A je izborno supstituisan aril, heteroaril ili heterociklik;m je ceo broj od 0 do 4 uključujući 0 i 4;n je ceo broj od 0 do 3 uključujući 0 i 3; io je ceo broj od 0 do 4 uključujući 0 i 4.Prijava sadrži još 24 patentna zahteva.

    Chroman-spirocyclic piperidine amides as modulators of ion channels
    12.
    发明专利
    Chroman-spirocyclic piperidine amides as modulators of ion channels 未知

    公开(公告)号：NZ613709A

    公开(公告)日：2016-08-26

    申请号：NZ61370912

    申请日：2012-02-16

    Applicant: VERTEX PHARMA

    Inventor： HADIDA-RUAH SARA SABINA ,  KALLEL EDWARD ADAM ,  ARUMUGAM VIJAYALAKSMI ,  MILLER MARK THOMAS ,  BEAR BRIAN RICHARD ,  DENINNO MICHAEL PAUL ,  ZHOU JINGLAN ,  UY JOHNNY ,  FRIEMAN BRYAN A

    IPC: A61P29/00 ,  A61K31/438 ,  C07D491/107 ,  C07D491/20 ,  C07D495/10

    Abstract: Disclosed are (aryl)(spiro[chroman-2,4’-piperidine]-1’-yl)methanone derivatives and analogues as represented by the general formula (I), or a pharmaceutically acceptable salt thereof, wherein: W is N or CR1, or one W is a bond and the remaining W are N, NR1, or CR1, wherein up to two W are N or NR1; a dashed circle denotes aromaticity or heteroaromaticity; R1 is H, a fully saturated alkyl, haloalkyl, halo, CN, SO2R7, SR7, SOR7, NR7COR7, NR7CO2R7, CON(R7)2, SO2N(R7)2, CF3, OCF3, OCHF2, aryl, heteroaryl, cycloalkyl, heterocycloalkyl, a fully saturated straight chain or branched (C1-C8)-R8, or a cyclic (C3-C8)-R8, wherein the aryl, heteroaryl, cycloalkyl or heterocycloalkyl are optionally substituted with one or more substituents selected from halo, cyano, oxoalkoxy, hydroxy, amino, nitro, aryl, haloalkyl, and alkyl, and wherein up to two CH2 units of the straight chain, branched or cyclic group may be replaced with O, S, SO, or CF2; R2 is alkyl, alkoxy, halo, CN, OR7a, N(R7)2, NR7SO2R7, SO2R7, SR7, SOR7, CO2R7, NR7COR7, NR7CO2R7, CON(R7)2, SO2N(R7)2, CF3, OCF3, OCHF2, CH2OCHF2, CH2OCH2CHF2, aryl, heteroaryl, cycloalkyl, heterocycloalkyl, a straight chain or branched (C1-C8)-R8, or a cyclic (C3-C8)-R8, wherein the aryl, heteroaryl, cycloalkyl, or heterocycloalkyl are optionally substituted with one or more substituents of halo, cyano, oxoalkoxy, hydroxy, amino, nitro, aryl, haloalkyl, and alkyl, and wherein up to two CH2 units of the straight chain, branched or cyclic group may be replaced with O, CO, S, SO, SO2 or NR7, with the proviso that R2 is not OH; R3 is alkyl or cycloalkyl, wherein up to two CH2 units may be replaced by O, NR8, S, SO, SO2, or 2 occurrences of R3 taken together form a cycloalkyl group; R7 is H, alkyl, fluoroalkyl, or cycloalkyl; R7a is alkyl, fluoroalkyl, or cycloalkyl; R8 is H, CF3, CO2R7, OH, aryl, heteroaryl, cycloalkyl, heterocycloalkyl, N(R7)2, NR7COR7, CON(R7)2, CN, or SO2R7, wherein the aryl, heteroaryl, cycloalkyl, or heterocycloalkyl are optionally substituted with one or more substituents of halo, cyano, oxoalkoxy, hydroxy, amino, nitro, aryl, haloalkyl, and alkyl; A is aryl or heteroaryl wherein the aryl or heteroaryl is optionally substituted with one or more substituents of halo, cyano, oxoalkoxy, hydroxy, amino, nitro, aryl, haloalkyl, and alkyl; X is O, S, or SO; n is an integer from 1 to 4 inclusive; and o is an integer from 0 to 4 inclusive; wherein, unless specified otherwise, the alkyl, haloalkyl, cycloalkyl, heterocycloalkyl and alkoxy groups include a completely saturated carbon chain or an aliphatic carbon chain containing one or more units of unsaturation. Representative compounds include (4-isopropoxy-3-methoxyphenyl)(4-isopropoxyspiro[chroman-2,4’-piperidine]-1’-yl)methanone, (4-isopropylsulfonyl-2-methylphenyl)(6-fluoro-4-ethoxy-spiro[chroman-2,4’-piperidine]-1’-yl)methanone, (3,4-dimethoxyphenyl)(4-phenyl-spiro[chroman-2,4’-piperidine]-1’-yl)methanone, (4-(2-hydroxypropan-2-yl)-3-methylphenyl)(6-cyano-4-isopropoxy-spiro[chroman-2,4’-piperidine]-1’-yl)methanone, (4-isopropoxy-3-methylphenyl)(spiro[chroman-2,4’-piperidine]-1’-yl)methanone, (4-isopropoxy-3-methoxyphenyl)(4-(methylthiomethyl)spiro[chroman-2,4’-piperidine]-1’-yl)methanone, etc. etc.. Also disclosed is a pharmaceutical composition comprising a compound as defined above and a pharmaceutically acceptable carrier, for the treating or lessening the severity of the pain in a subject afflicted with acute, chronic, neuropathic, or inflammatory pain, arthritis, migraine, cluster headaches, trigeminal neuralgia, herpatic neuralgia, general neuralgias, epilepsy or epilepsy conditions, neurodegenerative disorders, psychiatric disorders, anxiety, 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 abormal gastro-intestinal motility.

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