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RS54785B1 - Pirolopirazin-spirociklični piperidin amidi kao modulatori jonskih kanala - Google Patents

Pirolopirazin-spirociklični piperidin amidi kao modulatori jonskih kanala

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Publication number
RS54785B1
RS54785B1 RS20160229A RSP20160229A RS54785B1 RS 54785 B1 RS54785 B1 RS 54785B1 RS 20160229 A RS20160229 A RS 20160229A RS P20160229 A RSP20160229 A RS P20160229A RS 54785 B1 RS54785 B1 RS 54785B1
Authority
RS
Serbia
Prior art keywords
cycloalkyl
alkyl
replaced
units
halo
Prior art date
Application number
RS20160229A
Other languages
English (en)
Inventor
Ruah Sara S Hadida
Edward Adam Kallel
Mark Thomas Miller
Vijayalaksmi Arumugam
Jason Mccartney
Corey Anderson
Peter Diederik Jan Grootenhuis
Licong Jiang
Original Assignee
Vertex Pharma
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
Application filed by Vertex Pharma filed Critical Vertex Pharma
Publication of RS54785B1 publication Critical patent/RS54785B1/sr

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    • 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
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
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    • C07D471/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains three hetero rings
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    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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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.
RS20160229A 2011-02-02 2012-02-02 Pirolopirazin-spirociklični piperidin amidi kao modulatori jonskih kanala RS54785B1 (sr)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201161438685P 2011-02-02 2011-02-02
US201161440987P 2011-02-09 2011-02-09
US201161495538P 2011-06-10 2011-06-10
EP12704985.6A EP2670752B1 (en) 2011-02-02 2012-02-02 Pyrrolopyrazine-spirocyclic piperidine amides as modulators of ion channels
PCT/US2012/023593 WO2012106499A1 (en) 2011-02-02 2012-02-02 Pyrrolopyrazine-spirocyclic piperidine amides as modulators of ion channels

Publications (1)

Publication Number Publication Date
RS54785B1 true RS54785B1 (sr) 2016-10-31

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RS20160229A RS54785B1 (sr) 2011-02-02 2012-02-02 Pirolopirazin-spirociklični piperidin amidi kao modulatori jonskih kanala

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EP (2) EP2670752B1 (sr)
JP (2) JP6021824B2 (sr)
KR (1) KR101923367B1 (sr)
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Families Citing this family (63)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NZ583420A (en) 2007-08-24 2012-06-29 Vertex Pharma Isothiazolopyridinones useful for the treatment of (inter alia) cystic fibrosis
CA2812526A1 (en) 2010-05-06 2011-11-10 Vertex Pharmaceuticals Incorporated Heterocyclic chromene-spirocyclic piperidine amides as modulators of ion channels
JP6021824B2 (ja) * 2011-02-02 2016-11-09 バーテックス ファーマシューティカルズ インコーポレイテッドＶｅｒｔｅｘ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ Ｉｎｃｏｒｐｏｒａｔｅｄ イオンチャネルのモジュレーターとしてのピロロピラジン−スピロ環式ピペリジンアミド
CA2827311A1 (en) 2011-02-18 2012-08-23 Vertex Pharmaceuticals Incorporated Chroman-spirocyclic piperidine amides as modulators of ion channels
ES2618929T3 (es) 2011-03-14 2017-06-22 Vertex Pharmaceuticals Incorporated Morfolina-Spiro piperidina amida cíclica como moduladores del canal iónico
WO2013064984A1 (en) 2011-10-31 2013-05-10 Xenon Pharmaceuticals Inc. Biaryl ether sulfonamides and their use as therapeutic agents
CA2853439A1 (en) 2011-10-31 2013-05-10 Xenon Pharmaceuticals Inc. Benzenesulfonamide compounds and their use as therapeutic agents
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