ME01311B - N-oksidi kao proljekovi 4-fenil-piridinskih derivata koji su antagonisti nki receptora - Google Patents

N-oksidi kao proljekovi 4-fenil-piridinskih derivata koji su antagonisti nki receptora

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Publication number
ME01311B
ME01311B MEP-2008-770A MEP77008A ME01311B ME 01311 B ME01311 B ME 01311B ME P77008 A MEP77008 A ME P77008A ME 01311 B ME01311 B ME 01311B
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Montenegro
Prior art keywords
lower alkyl
hydrogen
phenyl
halogen
lower alkoxy
Prior art date
Application number
MEP-2008-770A
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English (en)
French (fr)
Inventor
Torsten Hoffmann
Sonia Maria Poli
Patrick Schnider
Andrew Sleight
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.)
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Publication date
Application filed by Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of ME01311B publication Critical patent/ME01311B/me

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    • C07D213/02Heterocyclic 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
    • C07D213/04Heterocyclic 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
    • C07D213/60Heterocyclic 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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Abstract

Ovaj pronalazak se odnosi na jedinjenja opšte formule  I  je R vodonik, niži   alkil, niži akoksi, halogen ili trifluormetil; R 1   je vodonik ili halogen; ili R i R 1   mogu biti zajedno sa ugljenikovim atomima prstena za koji su prikačeni - CH=CH-CH=CH-;R 2  i R 2 ' su nezavno jedan od drugog vodonik, halogen,   trifluormetil, niži akoksi ili cijano; ili   R 2  i R 2  mogu biti zajedno -CH=CH-CH=CH-, proizvoljno supstituisan sa jedn im ili dva supstituenta izabrana od nižeg alkil   ili nižeg akoksi;R 3 , R 3  su nezavisno jedan od drugog vodonik, niži alkil ili   cikloalkil; R 4 , R 4  su nezavisno jedan od drugog -(CH 2 ) m OR 6  ili niži alkil; ili R 4  i   R 4  čine zajedno sa N-atomom za koji su prikačen i ciklični tercijarni amin   grupe II R 5   je vodonik, hidroksi, niži alkil, -niži akoksi, -(CH 2 )OH, -COOR 3 , -CON(R 3 ) 2 , -N(R 3 )CO-niži alkil ili-C(O)R 3 ; R 6   je vodonik, niži alkil ili fenil;X je -(O)N(R 6 )- , -N(R 6 )C(O)-, -(CH 2 ) m O- ili -O(CH 2 ) m -; n je 0, 1, 2, 3  ili 4; i m je 1, 2   ili 3; i na njihove farmaceutski prihvatljive kisele adicione soli. Nađeno je da ova jedinjenja mogu da se koriste kao prolekovi za   tretiranje ili prevenciju bolesti, povezanih sa NK1 receptorom .      
MEP-2008-770A 2000-07-14 2001-07-09 N-oksidi kao proljekovi 4-fenil-piridinskih derivata koji su antagonisti nki receptora ME01311B (me)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP00115287 2000-07-14
PCT/EP2001/007850 WO2002006236A1 (en) 2000-07-14 2001-07-09 N-oxides as nk1 receptor antagonist prodrugs of 4-phenyl-pyridine derivatives

Publications (1)

Publication Number Publication Date
ME01311B true ME01311B (me) 2013-12-20

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US (4) US6593472B2 (me)
EP (1) EP1303490B1 (me)
JP (1) JP3950044B2 (me)
KR (1) KR100501608B1 (me)
CN (1) CN1178917C (me)
AR (1) AR029717A1 (me)
AT (1) ATE400556T1 (me)
AU (1) AU7061901A (me)
BR (1) BRPI0112475B8 (me)
CA (1) CA2415890C (me)
CY (1) CY1108557T1 (me)
CZ (1) CZ303639B6 (me)
DE (1) DE60134749D1 (me)
DK (1) DK1303490T3 (me)
EC (1) ECSP034431A (me)
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HK (1) HK1058198A1 (me)
HR (1) HRP20030003B1 (me)
HU (1) HU230316B1 (me)
IL (2) IL153834A0 (me)
JO (1) JO2372B1 (me)
MA (1) MA26929A1 (me)
ME (1) ME01311B (me)
MX (1) MXPA03000366A (me)
MY (1) MY154976A (me)
NO (1) NO324700B1 (me)
NZ (1) NZ523273A (me)
PA (1) PA8522001A1 (me)
PE (1) PE20020272A1 (me)
PL (1) PL205207B1 (me)
PT (1) PT1303490E (me)
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RU (1) RU2266284C2 (me)
SI (1) SI1303490T1 (me)
UY (1) UY26839A1 (me)
WO (1) WO2002006236A1 (me)
ZA (1) ZA200210207B (me)

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US20030083345A1 (en) * 2001-07-10 2003-05-01 Torsten Hoffmann Method of treatment and/or prevention of brain, spinal or nerve injury

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