SI2751083T1 - Kinolonska spojina - Google Patents

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SI2751083T1
SI2751083T1 SI201231233T SI201231233T SI2751083T1 SI 2751083 T1 SI2751083 T1 SI 2751083T1 SI 201231233 T SI201231233 T SI 201231233T SI 201231233 T SI201231233 T SI 201231233T SI 2751083 T1 SI2751083 T1 SI 2751083T1
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salt
optionally substituted
alkyl
compound
formula
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SI201231233T
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Mamuti Abudusaimi
Fangguo Ye
Jiangqin Sun
Hisashi Miyamoto
Jay-Fei Cheng
Daisuke Oka
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Otsuka Pharmaceutical Co., Ltd.
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Publication of SI2751083T1 publication Critical patent/SI2751083T1/sl

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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
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    • A61K31/47—Quinolines; Isoquinolines
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    • A61K31/4965—Non-condensed pyrazines
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    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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    • A61K31/5375—1,4-Oxazines, e.g. morpholine
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    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms 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
    • C07D215/48—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • C07D215/54—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 3
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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
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  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Quinoline Compounds (AREA)
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Claims (12)

  1. Kinolonska spojina Patentni zahtevki
    1. Spojina, predstavljena s formulo (I) kjer
    X je atom fluora; Rje atom vodika ali alkil; R1 je (1) ciklopropil, po izbiri substituiran z 1 do 3 atomi halogenov ali (2) fenil, po izbiri substituiran z 1 do 3 atomi halogenov; R je atom vodika; alkil, po izbiri substituiran z 1 ali 2 substituentoma, izbranima iz skupine, ki jo sestavljajo atom halogena in hidroksil; alkoksi; haloalkoksi; atom halogena; ciano; ciklopropil; nitro; amino; formil; alkenil ali alkinil; ali R1 in R2 sta vezana, da tvorita 5- ali 6-členski obroč, po izbiri substituiran z alkilom; R3 je (1) spojena heterociklična skupina s formulo
    kjer - predstavlja enojno vez ali dvojno vez, X1 je C(R5) ali N, R4 je atom vodika ali alkil, in Rsje (a) atom vodika, (b) atom halogena, (c) ciano, (d) nitro, (e) hidroksi, (f) alkil, po izbiri substituiran z 1 do 3 atomi halogenov, (g) alkenil ali alkinil, (h) aril, ali (i) alkoksi, po izbiri substituiran z 1 do 3 atomi halogenov, kadar je X1 C(R5), sta R4 in R5 po izbiri vezana, da tvorita 5- ali 6-členski obroč, po izbiri substituiran z okso, pri čemer je navedena spojena heterociklična skupina po izbiri substituirana z 1 ali 2 substituentoma, izbranima iz skupine, ki jo sestavljajo atom halogena, ciano, nitro, hidroksi in alkil, (2) skupina s formulo kjer
    X5 je C(RU) ali N, X6 je CH2, C(=0), O, S, S02 ali N(R12), X7 je CH(R13), C(=0) ali N(R14), X8 je CH(R15) ali C(=0), R10, R12 in R14 so vsak neodvisno (a) atom vodika ali (b) alkil, in R11, R13 in R15 so vsak neodvisno (a) atom vodika, (b) atom halogena, (c) ciano, (d) nitro, (e) amino, (f) alkilamino, (g) dialkilamino, (h) alkil, po izbiri substituiran s hidroksi, ali (i) alkenil, kadar je X5 C(Rn), sta R10 in R11 po izbiri vezana, da tvorita 5- ali 6-členski obroč, po izbiri substituiran z alkilom ali okso, in kadar je X6 N(R12) in je X7 CH(R13), sta R12 in R13 po izbiri vezana, da tvorita 5- ali 6-členski obroč, ali (3) izokromenil, ali njena sol.
  2. 2. Spojina po zahtevku 1, kjer je R3 spojena heterociklična skupina s formulo
    kjer so ------- , X1 in R4 kot so definirani v zahtevku 1 in je navedena spojena heterociklična skupina po izbiri substituirana z 1 ali 2 substituentoma, izbranima iz skupine, ki jo sestavljajo atom halogena, ciano, nitro, hidroksi in alkil, ali njena sol.
  3. 3. Spoj ina po zahtevku 1, kjer je R3 skupina s formulo
    kjer so X5, X6, X7, X8 in R10 kot so definirani v zahtevku 1, ali njena sol.
  4. 4. Spojina po zahtevku 1, kjer je R3 izokromenil, ali njena sol.
  5. 5. Spojina po zahtevku 1, kjer je R atom vodika, ali njena sol.
  6. 6. Spojina po zahtevku 1, kjer je R1 ciklopropil, 2-fluorociklopropil ali 2,4-difluorofenil, ali njena sol. *
  7. 7. Spojina po zahtevku 1, kjer je R metil, metoksi ali atom klora, ali njena sol.
  8. 8. Spojina po zahtevku 1, ki je spojina, predstavljena s formulo
    ali njena sol.
  9. 9. Spojina po zahtevku 1, ki je spojina, predstavljena s formulo
    ali njena sol.
  10. 10. Farmacevtski sestavek, ki obsega spojino po katerem koli od zahtevkov od 1 do 9 ali njeno sol in farmacevtsko sprejemljiv nosilec.
  11. 11. Spojina po katerem koli od zahtevkov od 1 do 9 ali njena sol za uporabo kot zdravilo za uporabo kot protimikrobno sredstvo ali za uporabo v preprečevanju ali zdravljenju bakterijske infekcije.
  12. 12. Uporaba spojine po katerem koli od zahtevkov od 1 do 9 ali njene soli za izdelavo zdravila za preprečevanje ali zdravljenje bakterijske infekcije.
SI201231233T 2011-08-31 2012-08-30 Kinolonska spojina SI2751083T1 (sl)

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