HRP20100574T1 - Tricklički spojevi s dušikom kao antibakterijska sredstva - Google Patents

Tricklički spojevi s dušikom kao antibakterijska sredstva Download PDF

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HRP20100574T1
HRP20100574T1 HR20100574T HRP20100574T HRP20100574T1 HR P20100574 T1 HRP20100574 T1 HR P20100574T1 HR 20100574 T HR20100574 T HR 20100574T HR P20100574 T HRP20100574 T HR P20100574T HR P20100574 T1 HRP20100574 T1 HR P20100574T1
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dihydro
methyl
amino
dione
piperidinyl
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HR20100574T
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Evan Davies David
Thomas Davies David
Giordano Ilaria
Joseph Hennessy Alan
David Pearson Neil
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Glaxo Group Limited
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Priority claimed from GB0707705A external-priority patent/GB0707705D0/en
Priority claimed from GB0720569A external-priority patent/GB0720569D0/en
Priority claimed from GB0805311A external-priority patent/GB0805311D0/en
Application filed by Glaxo Group Limited filed Critical Glaxo Group Limited
Publication of HRP20100574T1 publication Critical patent/HRP20100574T1/hr

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—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
    • 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
    • C07D471/16—Peri-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A61P31/06—Antibacterial agents for tuberculosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains three hetero rings
    • C07D487/16—Peri-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Agricultural Chemicals And Associated Chemicals (AREA)
  • Medicines Containing Material From Animals Or Micro-Organisms (AREA)

Abstract

Spoj formule (I) ili njegova farmaceutski prihvatljiva sol i/ili N-oksid: naznačen time što: Z1 i Z2 se neovisno bira između CH i N; R1a i R1b se neovisno bira između vodika; halogena; cijano; (C1-6)alkila; (C1-6)alkiltio; trifluormetila; trifluormetoksi; karboksi; hidroksi, izborno supstituiranog s (C1-6)alkilom ili (C1-6)alkoksi-supstituiranim (C1-6)alkilom; (C1-6)alkoksi-supstituiranog (C1-6)alkila; hidroksi(C1-6)alkila; amino skupine, izborno N-supstituirane s jednom ili dvije (C1-6)alkilne, formilne, (C1-6)alkilkarbonilne ili (C1-6)alkilsulfonilne skupine; i aminokarbonila, gdje amino skupina je izborno supstituirana s (C1-4)alkilom; uz uvjet da R1a je H kada Z2 je N, a R1b je H kada Z1 je N; R2 je vodik ili (C1-4)alkil, ili zajedno s R6 tvori Y, kao što je definirano niže; A je skupina (i): u kojoj: R3 je kao što je definirano za R1a i R1b ili je okso, a n je 1 ili 2: ili A je skupina (ii) gdje: W1, W2 i W3 su CR4R8;ili W2 i W3 su CR4R8, a W1 predstavlja vezu između W3 i N; X je O, CR4R8 ili NR6;jedan R4 je kao što je definirano za R1a i R1b, a ostatak i R8 su vodici ili jedan R4 i R8 su zajedno okso, a ostatak je vodik; R6 je vodik ili (C1-6)alkil; ili zajedno s R2 tvori Y; R7 je vodik; halogen; hidroksi, izborno supstituiran s (C1-6)alkilom; ili (C1-6)alkil; Y je CR4R8CH2; CH2CR4R8; (C=O); CR4R8; CR4R8(C=O); ili (C=O)CR4R8;ili kada X je CR4R8, R8 i R7 zajedno predstavljaju vezu; U se bira između CO i CH2; iR5 je izborno supstituiran biciklički karbociklički ili heterociklički prstenasti sustav (B): koji sadrži do četiri heteroatoma u svakom prstenu, gdje najmanje jedan od prstena (a) i (b) je aromatski; X1 je C ili N kada je dio aromatskog prstena, ili CR14 kada je dio nearomatskog prstena; X2 je N, NR13, O, S(O)x, CO ili CR14 kada je dio aromatskog ili nearomatskog prstena, ili dodatno može biti CR14R15 kada je dio nearomatskog prstena; X3 i X5 su neovisno N ili C; Y1 je 0- do 4-atomska spojnica, čiji svaki atom se neovisno bira između N, NR13, O, S(O)x, CO i CR14 kada je dio aromatskog ili nearomatskog prstena, ili dodatno može biti CR14R15 kada je dio nearomatskog prstena; Y2 je 2- do 6-atomska spojnica, gdje se svaki atom u Y2 neovisno bira između N, NR13, O, S(O)x, CO, CR14 kada je dio aromatskog ili nearomatskog prstena, ili dodatno može biti CR14R15 kada je dio nearomatskog prstena; svakog od R14 i R15 se neovisno bira između: H; (C1-4)alkiltio; halogena; karboksi(C1-4)alkila; (C1-4)alkila; (C1-4)alkoksikarbonila; (C1-4)alkilkarbonila; (C1-4)alkoksi(C1-4)alkila; hidroksi; hidroksi(C1-4)alkila; (C1-4)alkoksi; nitro; cijano; karboksi; amino ili aminokarbonila, izborno mono- ili disupstituiranog s (C1-4)alkilom; iliR14 i R15 zajedno mogu predstavljati okso; svaki R13 je neovisno H; trifluormetil; (C1-4)alkil, izborno supstituiran s hidroksi, (C1-6)alkoksi, (C1-6)alkiltio, halogen ili trifluormetil; (C2-4)alkenil; (C1-4)alkoksikarbonil; (C1-4)alkilkarbonil; (C1-6)alkilsulfonil; aminokarbonil, gdje amino skupina je izborno mono- ili dis

Claims (20)

1. Spoj formule (I) ili njegova farmaceutski prihvatljiva sol i/ili N-oksid: naznačen time što: [image] Z1 i Z2 se neovisno bira između CH i N; R1a i R1b se neovisno bira između vodika; halogena; cijano; (C1-6)alkila; (C1-6)alkiltio; trifluormetila; trifluormetoksi; karboksi; hidroksi, izborno supstituiranog s (C1-6)alkilom ili (C1-6)alkoksi-supstituiranim (C1-6)alkilom; (C1-6)alkoksi-supstituiranog (C1-6)alkila; hidroksi(C1-6)alkila; amino skupine, izborno N-supstituirane s jednom ili dvije (C1-6)alkilne, formilne, (C1-6)alkilkarbonilne ili (C1-6)alkilsulfonilne skupine; i aminokarbonila, gdje amino skupina je izborno supstituirana s (C1-4)alkilom; uz uvjet da R1a je H kada Z2 je N, a R1b je H kada Z1 je N; R2 je vodik ili (C1-4)alkil, ili zajedno s R6 tvori Y, kao što je definirano niže; A je skupina (i): [image] u kojoj: R3 je kao što je definirano za R1a i R1b ili je okso, a n je 1 ili 2: ili A je skupina (ii) [image] gdje: W1, W2 i W3 su CR4R8; ili W2 i W3 su CR4R8, a W1 predstavlja vezu između W3 i N; X je O, CR4R8 ili NR6; jedan R4 je kao što je definirano za R1a i R1b, a ostatak i R8 su vodici ili jedan R4 i R8 su zajedno okso, a ostatak je vodik; R6 je vodik ili (C1-6)alkil; ili zajedno s R2 tvori Y; R7 je vodik; halogen; hidroksi, izborno supstituiran s (C1-6)alkilom; ili (C1-6)alkil; Y je CR4R8CH2; CH2CR4R8; (C=O); CR4R8; CR4R8(C=O); ili (C=O)CR4R8; ili kada X je CR4R8, R8 i R7 zajedno predstavljaju vezu; U se bira između CO i CH2; i R5 je izborno supstituiran biciklički karbociklički ili heterociklički prstenasti sustav (B): [image] koji sadrži do četiri heteroatoma u svakom prstenu, gdje najmanje jedan od prstena (a) i (b) je aromatski; X1 je C ili N kada je dio aromatskog prstena, ili CR14 kada je dio nearomatskog prstena; X2 je N, NR13, O, S(O)x, CO ili CR14 kada je dio aromatskog ili nearomatskog prstena, ili dodatno može biti CR14R15 kada je dio nearomatskog prstena; X3 i X5 su neovisno N ili C; Y1 je 0- do 4-atomska spojnica, čiji svaki atom se neovisno bira između N, NR13, O, S(O)x, CO i CR14 kada je dio aromatskog ili nearomatskog prstena, ili dodatno može biti CR14R15 kada je dio nearomatskog prstena; Y2 je 2- do 6-atomska spojnica, gdje se svaki atom u Y2 neovisno bira između N, NR13, O, S(O)x, CO, CR14 kada je dio aromatskog ili nearomatskog prstena, ili dodatno može biti CR14R15 kada je dio nearomatskog prstena; svakog od R14 i R15 se neovisno bira između: H; (C1-4)alkiltio; halogena; karboksi(C1-4)alkila; (C1-4)alkila; (C1-4)alkoksikarbonila; (C1-4)alkilkarbonila; (C1-4)alkoksi(C1-4)alkila; hidroksi; hidroksi(C1-4)alkila; (C1-4)alkoksi; nitro; cijano; karboksi; amino ili aminokarbonila, izborno mono- ili disupstituiranog s (C1-4)alkilom; ili R14 i R15 zajedno mogu predstavljati okso; svaki R13 je neovisno H; trifluormetil; (C1-4)alkil, izborno supstituiran s hidroksi, (C1-6)alkoksi, (C1-6)alkiltio, halogen ili trifluormetil; (C2-4)alkenil; (C1-4)alkoksikarbonil; (C1-4)alkilkarbonil; (C1-6)alkilsulfonil; aminokarbonil, gdje amino skupina je izborno mono- ili disupstituirana s (C1-4)alkilom; i svaki x je neovisno 0, 1 ili 2.
2. Spoj u skladu s patentnim zahtjevom 1, naznačen time što: (i) Z1 i Z2 su oba CH; (ii) Z1 je N i Z2 je CH; ili (iii) Z1 je CH i Z2 je N.
3. Spoj u skladu s bilo kojim od prethodnih patentnih zahtjeva, naznačen time što R1a je vodik i R1b je vodik.
4. Spoj u skladu s bilo kojim od prethodnih patentnih zahtjeva, naznačen time što A je (ia), n je 1 i R3 je H ili hidroksi na položaju 3, A je (ii), X je CR4R8, gdje R8 je H, a R4 je H ili OH, ili A je (ii), X je O, R7 je H, a svaki od W1, W2 i W3 je CH2.
5. Spoj u skladu s patentnim zahtjevom 4, naznačen time što A je piperidin-4-il ili pirolidin-4-ilmetil.
6. Spoj u skladu s bilo kojim od prethodnih patentnih zahtjeva, naznačen time što U je CH2.
7. Spoj u skladu s bilo kojim od prethodnih patentnih zahtjeva, naznačen time što R5 je aromatski heterociklički prsten (B) s 8-11 atoma u prstenu, uključujući 2-4 heteroatoma, od kojih najmanje jedan je N ili NR13, gdje Y2 sadrži 2-3 heteroatoma, od kojih je jedan S, a 1-2 su N, gdje N je vezan na X3, ili heterociklički prsten (B) sadrži aromatski prsten (a), kojeg se bira između izborno supstituiranih benzo, pirido, piridazino i pirimidino, i prsten nearomatski (b), a Y2 sadrži 3-5 atoma, uključujući najmanje jedan heteroatom, gdje O, S, CH2 ili NR13 je vezan na X5, gdje R13 nije vodik, a NHCO je bilo preko N vezan na X3, ili O, S, CH2 ili NH je vezan na X3.
8. Spoj u skladu s bilo kojim od zahtjeva 1 do 6, naznačen time što R5 se bira između: 3-okso-3,4-dihidro-2H-pirido[3,2-b][1,4]oksazin-6-ila 3-okso-3,4-dihidro-2H-pirido[3,2-b][1,4]tiazin-6-ila 2,3-dihidro-1,4-dioksino[2,3-c]piridin-7-ila 1,3-oksatiolo[5,4-c]piridin-6-ila 6-fluor-2,3-dihidro-1,4-benzodioksin-7-ila 2,3-dihidro-1,4-oksatiino[2,3-c]piridin-7-ila 3,4-dihidro-2H-pirano[2,3-c]piridin-6-ila 5-fluor-2,3-dihidro-1,4-benzodioksin-7-ila 5-karbonitro-2,3-dihidro-1,4-benzodioksin-7-ila 2,3-dihidrobenzo-1,4-dioksin-6-ila.
9. Spoj u skladu s patentnim zahtjevom 1, naznačen time što ga se bira imeđu: 1-({4-[(2,3-Dihidro-1,4-dioksino[2,3-c]piridin-7-ilmetil)amino]-1-piperidinil}metil)-1,2-dihidro-3H,8H-2a,5,8a-triazaacenaftilen-3,8-diona; 1-({4-[(1,3-Oksatiolo[5,4-c]piridin-6-ilmetil)amino]-1-piperidinil}metil)-1,2-dihidro-4H,9H-imidazo[1,2,3-ij]-1,8-naftiridin-4,9-diona; 1-({4-[(2,3-Dihidro-1,4-dioksino[2,3-c]piridin-7-ilmetil)amino]-1-piperidinil}metil)-1,2-dihidro-4H,9H-imidazo[1,2,3-ij]-1,8-naftiridin-4,9-diona; 1-({4-[(7-Bromo-3-okso-3,4-dihidro-2H-pirido[3,2-b][1,4]tiazin-6-ilmetil)amino]-1-piperidinil}metil)-1,2-dihidro-4H,9H-imidazo[1,2,3-ij]-1,8-naftiridin-4,9-diona; (1R)-1-({4-[(1,3-Oksatiolo[5,4-c]piridin-6-ilmetil)amino]-1-piperidinil}metil)-1,2-dihidro-4H,9H-imidazo[1,2,3-ij]-1,8-naftiridin-4,9-diona; (1R)-1-({4-[(2,3-Dihidro-1,4-oksatiino[2,3-c]piridin-7-ilmetil)amino]-1-piperidinil}metil)-1,2-dihidro-4H,9H-imidazo[1,2,3-ij]-1,8-naftiridin-4,9-diona; (1R)-1-({4-[(5,6,7,8-Tetrahidro-3-izokinolinilmetil)amino]-1-piperidinil}metil)-1,2-dihidro-4H,9H-imidazo[1,2,3-ij]-1,8-naftiridin-4,9-diona; (1R)-1-({4-[(6,7-Dihidro-5H-ciklopenta[c]piridin-3-ilmetil)amino]-1-piperidinil}metil)-1,2-dihidro-4H,9H-imidazo[1,2,3-ij]-1,8-naftiridin-4,9-diona; (1R)-1-({4-[(1,3-Dihidrofuro[3,4-c]piridin-6-ilmetil)amino]-1-piperidinil}metil)-1,2-dihidro-4H,9H-imidazo[1,2,3-ij]-1,8-naftiridin-4,9-diona; (1R)-1-({4-[(3,4-Dihidro-2H-pirano[2,3-c]piridin-6-ilmetil)amino]-1-piperidinil}metil)-1,2-dihidro-4H,9H-imidazo[1,2,3-ij]-1,8-naftiridin-4,9-diona; 7-[({1-[(4,9-Diokso-1,2-dihidro-4H,9H-imidazo[1,2,3-ij]-1,8-naftiridin-1-il)metil]-4-piperidinil}amino)metil]-2,3-dihidro-1,4-benzodioksin-5-karbonitrila; 1-[(4-{[(3-Okso-3,4-dihidro-2H-1,4-benzotiazin-6-il)metil]amino}-1-piperidinil)metil]-1,2-dihidro-4H,9H-imidazo[1,2,3-ij]-1,8-naftiridin-4,9-diona; (1R)-1-({4-[(1,3-Oksatiolo[5,4-c]piridin-6-ilmetil)amino]-1-piperidinil}metil)-1,2-dihidro-3H,8H-2a,5,8a-triazaacenaftilen-3,8-diona; (1R)-1-({4-[(2,3-Dihidro-1,4-oksatiino[2,3-c]piridin-7-ilmetil)amino]-1-piperidinil}metil)-1,2-dihidro-3H,8H-2a,5,8a-triazaacenaftilen-3,8-diona; (1R)-1-({4-[(2,3-Dihidro-1,4-dioksino[2,3-c]piridin-7-ilmetil)amino]-1-piperidinil}metil)-1,2-dihidro-3H,8H-2a,5,8a-triazaacenaftilen-3,8-diona; (2R)-2-({4-[(1,3-Oksatiolo[5,4-c]piridin-6-ilmetil)amino]-1-piperidinil}metil)-1,2-dihidro-3H,8H-2a,5,8a-triazaacenaftilen-3,8-diona; (2S)-2-({4-[(1,3-Oksatiolo[5,4-c]piridin-6-ilmetil)amino]-1-piperidinil}metil)-1,2-dihidro-3H,8H-2a,5,8a-triazaacenaftilen-3,8-diona; 2-({4-[(1,3-Oksatiolo[5,4-c]piridin-6-ilmetil)amino]-1-piperidinil}metil)-1,2-dihidro-3H,8H-2a,5,8a-triazaacenaftilen-3,8-diona; (2R)-2-({4-[(2,3-Dihidro-1,4-oksatiino[2,3-c]piridin-7-ilmetil)amino]-1-piperidinil}metil)-1,2-dihidro-3H,8H-2a,5,8a-triazaacenaftilen-3,8-diona; 2-({4-[(2,3-Dihidro-1,4-oksatiino[2,3-c]piridin-7-ilmetil)amino]-1-piperidinil}metil)-1,2-dihidro-3H,8H-2a,5,8a-triazaacenaftilen-3,8-diona; (2S)-2-({4-[(2,3-Dihidro-1,4-oksatiino[2,3-c]piridin-7-ilmetil)amino]-1-piperidinil}metil)-1,2-dihidro-3H,8H-2a,5,8a-triazaacenaftilen-3,8-diona; 2-({4-[(2,3-Dihidro-1,4-dioksino[2,3-c]piridin-7-ilmetil)amino]-1-piperidinil}metil)-1,2-dihidro-3H,8H-2a,5,8a-triazaacenaftilen-3,8-diona; (1R)-1-({4-[(2,3-Dihidro-1,4-oksatiino[2,3-c]piridin-7-ilmetil)amino]-4-metil-1-piperidinil}metil)-1,2-dihidro-4H,9H-imidazo[1,2,3-ij]-1,8-naftiridin-4,9-diona; (1R)-1-({4-Metil-4-[(1,3-Oksatiolo[5,4-c]piridin-6-ilmetil)amino]-1-piperidinil}metil)-1,2-dihidro-4H,9H-imidazo[1,2,3-ij]-1,8-naftiridin-4,9-diona; (2R)-2-({4-[(2,1,3-Benzotiadiazol-5-ilmetil)amino]-1-piperidinil}metil)-1,2-dihidro-3H,8H-2a,5,8a-triazaacenaftilen-3,8-diona; (2R)-2-[(4-{[(7-Fluor-2,3-dihidro-1,4-benzodioksin-6-il)metil]amino}-1-piperidinil)metil]-1,2-dihidro-3H,8H-2a,5,8a-triazaacenaftilen-3,8-diona; (2R)-2-({4-[(3,4-Dihidro-2H-[1,4]oksatiepino[2,3-c]piridin-8-ilmetil)amino]-1-piperidinil}metil)-1,2-dihidro-3H,8H-2a,5,8a-triazaacenaftilen-3,8-diona; (2R)-2-({4-[(1,3-Oksatiolo[4,5-c]piridin-6-ilmetil)amino]-1-piperidinil}metil)-1,2-dihidro-3H,8H-2a,5,8a-triazaacenaftilen-3,8-diona; (2R)-2-[(4-{[(3-Okso-3,4-dihidro-2H-pirido[3,2-b][1,4]tiazin-6-il)metil]amino}-1-piperidinil)metil]-1,2-dihidro-3H,8H-2a,5,8a-triazaacenaftilen-3,8-diona; (1R)-1-({4-[(2,3-Dihidro-1,4-benzodioksin-6-ilmetil)amino]-1-piperidinil}metil)-1,2-dihidro-4H,9H-imidazo[1,2,3-ij]-1,8-naftiridin-4,9-diona; (1R)-1-[(4-{[(8-Fluor-2,3-dihidro-1,4-benzodioksin-6-il)metil]amino}-1-piperidinil)metil]-1,2-dihidro-4H,9H-imidazo[1,2,3-ij]-1,8-naftiridin-4,9-diona; (1R)-1-[(4-{[(7-Klor-3-okso-3,4-dihidro-2H-pirido[3,2-b][1,4]oksazin-6-il)metil]amino}-1-piperidinil)metil]-1,2-dihidro-4H,9H-imidazo[1,2,3-ij]-1,8-naftiridin-4,9-diona; (1R)-1-[(4-{[(4-Klor-7-okso-6,7-dihidro-1H-pirimido[5,4-b][1,4]oksazin-2-il)metil]amino}-1-piperidinil)metil]-1,2-dihidro-4H,9H-imidazo[1,2,3-ij]-1,8-naftiridin-4,9-diona; (1R)-1-[(4-{[(7-Okso-6,7-dihidro-1H-pirimido[5,4-b][1,4]tiazin-2-il)metil]amino}-1-piperidinil)metil]-1,2-dihidro-4H,9H-imidazo[1,2,3-ij]-1,8-naftiridin-4,9-diona; (1R)-1-({4-[(1,2,3-Benzotiadiazol-5-ilmetil)amino]-1-piperidinil}metil)-1,2-dihidro-4H,9H-imidazo[1,2,3-ij]-1,8-naftiridin-4,9-diona; (1R)-1-({4-[(2,3-Dihidro-1-benzofuran-5-ilmetil)amino]-1-piperidinil}metil)-1,2-dihidro-4H,9H imidazo[1,2,3-ij]-1,8-naftiridin-4,9-diona; (1R)-1-({4-[(3,4-Dihidro-2H-pirano[2,3-c]piridin-6-ilmetil)amino]-1-piperidinil}metil)-1,2-dihidro-3H,8H-2a,5,8a-triazaacenaftilen-3,8-diona; (1R)-1-({4-[(2,3-Dihidrofuro[2,3-c]piridin-5-ilmetil)amino]-1-piperidinil}metil)-1,2-dihidro-3H,8H-2a,5,8a-triazaacenaftilen-3,8-diona; (2R)-2-({4-[(2,3-Dihidro-1,4-benzodioksin-6-ilmetil)amino]-1-piperidinil}metil)-1,2-dihidro-3H,8H-2a,5,8a-triazaacenaftilen-3,8-diona; (2R)-2-[(4-{[(8-Fluor-2,3-dihidro-1,4-benzodioksin-6-il)metil]amino}-1-piperidinil)metil]-1,2-dihidro-3H,8H-2a,5,8a-triazaacenaftilen-3,8-diona; 7-{[(1-{[(2R)-3,8-Diokso-1,2-dihidro-3H,8H-2a,5,8a-triazaacenaftilen-2-il]metil}-4-piperidinil)amino]metil}-2,3-dihidro-1,4-benzodioksin-5-karbonitrila; (2R)-2-({4-[(2,3-Dihidrofuro[2,3-c]piridin-5-ilmetil)amino]-1-piperidinil}metil)-1,2-dihidro-3H,8H-2a,5,8a-triazaacenaftilen-3,8-diona; (1R)-1-({4-[(2,3-Dihidro-1,4-benzodioksin-6-ilmetil)amino]-1-piperidinil}metil)-1,2-dihidro-3H,8H-2a,5,8a-triazaacenaftilen-3,8-diona; (1R)-1-({4-[(1,2,5-Tiadiazolo[3,4-b]piridin-6-ilmetil)amino]-1-piperidinil}metil)-1,2-dihidro-4H,9H-imidazo[1,2,3-ij]-1,8-naftiridin-4,9-diona; (1R)-1-[(4-{[(4-Fluor-1H-benzimidazol-2-il)metil]amino}-1-piperidinil)metil]-1,2-dihidro-4H,9H-imidazo[1,2,3-ij]-1,8-naftiridin-4,9-diona; (1R)-1-[((2S)-2-{[(1,3-Oksatiolo[5,4-c]piridin-6-ilmetil)amino]metil}-4-morpholinil)metil]-1,2-dihidro-4H,9H-imidazo[1,2,3-ij]-1,8-naftiridin-4,9-diona; (1R)-1-{[(2S)-2-({[(7-Klor-3-okso-3,4-dihidro-2H-pirido[3,2-b][1,4]oksazin-6-il)metil]amino}metil)-4-morpholinil]metil}-1,2-dihidro-4H,9H-imidazo[1,2,3-ij]-1,8-naftiridin-4,9-diona; (2R)-2-({4-[(1,2,5-Tiadiazolo[3,4-b]piridin-6-ilmetil)amino]-1-piperidinil}metil)-1,2-dihidro-3H,8H-2a,5,8a-triazaacenaftilen-3,8-diona; (1R)-1-({4-[(3,4-Dihidro-2H-kromen-7-ilmetil)amino]-1-piperidinil}metil)-1,2-dihidro-4H,9H-imidazo[1,2,3-ij]-1,8-naftiridin-4,9-diona; (1R)-1-({4-[(2,3-Dihidro-1-benzofuran-6-ilmetil)amino]-1-piperidinil}metil)-1,2-dihidro-4H,9H-imidazo[1,2,3-ij]-1,8-naftiridin-4,9-diona; (1R)-1-({4-[(3,4-Dihidro-2H-kromen-6-ilmetil)amino]-1-piperidinil}metil)-1,2-dihidro-4H,9H-imidazo[1,2,3-ij]-1,8-naftiridin-4,9-diona; (2R)-2-[(4-{[(5-Fluor-2,3-dihidro-1,4-benzodioksin-6-il)metil]amino}-1-piperidinil)metil]-1,2-dihidro-3H,8H-2a,5,8a-triazaacenaftilen-3,8-diona; (1R)-1-{[(2S)-2-({[(7-Fluor-2,3-dihidro-1,4-benzodioksin-6-il)metil]amino}metil)-4-morpholinil]metil}-1,2-dihidro-4H,9H-imidazo[1,2,3-ij]-1,8-naftiridin-4,9-diona; (1R)-1-[((3S)-3-{[(1,3-Oksatiolo[5,4-c]piridin-6-ilmetil)amino]metil}-1-pirolidinil)metil]-1,2-dihidro-4H,9H-imidazo[1,2,3-ij]-1,8-naftiridin-4,9-diona; 7-{[(1-{[(1R)-3,8-Diokso-1,2-dihidro-3H,8H-2a,5,8a-triazaacenaftilen-1-il]metil}-4-piperidinil)amino]metil}-2,3-dihidro-1,4-benzodioksin-5-karbonitrila; (1R)-1-[(4-{[(7-Fluor-2,3-dihidro-1,4-benzodioksin-6-il)metil]amino}-1-piperidinil)metil]-1,2-dihidro-3H,8H-2a,5,8a-triazaacenaftilen-3,8-diona; (1R)-1-[(4-{[(8-Fluor-2,3-dihidro-1,4-benzodioksin-6-il)metil]amino}-1-piperidinil)metil]-1,2-dihidro-3H,8H-2a,5,8a-triazaacenaftilen-3,8-diona; (1R)-1-[(4-{[(2-Okso-2H-kromen-7-il)metil]amino}-1-piperidinil)metil]-1,2-dihidro-4H,9H-imidazo[1,2,3-ij]-1,8-naftiridin-4,9-diona; (1R)-1-[(4-{[(7-Klor-3,4-dihidro-2H-pirido[3,2-b][1,4]oksazin-6-il)metil]amino}-1-piperidinil)metil]-1,2-dihidro-4H,9H-imidazo[1,2,3-ij]-1,8-naftiridin-4,9-diona; (1R)-1-[(4-{(7-Klor-3,4-dihidro-2H-pirido[3,2-b][1,4]tiazin-6-il)metil]amino}-1-piperidinil)metil]-1,2-dihidro-4H,9H-imidazo[1,2,3-ij]-1,8-naftiridin-4,9-diona; (1R)-1-({4-[(3,4-Dihidro-2H-pirido[3,2-b][1,4]tiazin-6-ilmetil)amino]-1-piperidinil}metil)-1,2-dihidro-4H,9H-imidazo[1,2,3-ij]-1,8-naftiridin-4,9-diona; 1-[(4-{[(2,3-Dihidro-1,4-oksatiino[2,3-c]piridin-7-il)metil]amino}-1-piperidinil)metil]-1,2-dihidro-4H,9H-imidazo[1,2,3-ij]-1,8-naftiridin-4,9-diona; 1-({4-[(1,3-Oksatiolo[5,4-c]piridin-6-ilmetil)amino]-1-piperidinil}metil)-1,2-dihidro-4H,9H-imidazo[1,2,3-ij]-1,8-naftiridin-4,9-diona; ili slobodne baze spojeva iz Tablice 1: [image] [image] ili njihovih farmaceutski prihvatljivih soli.
10. Spoj, naznačen time što je (2R)-2-({4-[(3,4-dihidro-2H-pirano[2,3-c]piridin-6-ilmetil)amino]-1-piperidinil}metil)-1,2-dihidro-3H,8H-2a,5,8a-triazaacenaftilen-3,8-dion, ili njegova farmaceutski prihvatljiva sol.
11. Spoj, naznačen time što je (2R)-2-({4-[(3,4-dihidro-2H-pirano[2,3-c]piridin-6-ilmetil)amino]-1-piperidinil}metil)-1,2-dihidro-3H,8H-2a,5,8a-triazaacenaftilen-3,8-dion-hidroklorid.
12. Upotreba spoja u skladu s bilo kojim od zahtjeva 1 do 11, naznačena time što je navedeni spoj namijenjen proizvodnji medikamenta namijenjenog upotrebi u liječenju bakterijskih infekcija kod sisavaca.
13. Upotreba u skladu s patentnim zahtjevom 12, naznačena time što je navedeni spoj namijenjen liječenju infekcija gornjeg i/ili donjog dišnog sustava, infekcija kože i mekih tkiva, infekcije mokraćnog sustava i/ili tuberkuloze.
14. Upotreba spoja u skladu s patentnim zahtjevom 10 ili 11, naznačena time što je navedeni spoj namijenjen proizvodnji medikamenta namijenjenog upotrebi u liječenju bakterijskih infekcija kod sisavaca, gdje bakterijsku infekciju uzrokuje Gram-pozitivni organizam, kojeg se bira između bakterija Staphilococcus aureus, Streptococcus pneumoniae, Streptococcus pyogenes, Enterococcus faecalis i Enterococcus faecium; ili Gram-negativni organizam, kojeg se bira između bakterija Haemophilus influenzae, Moraxella catarrhalis, Escherichia coli, Pseudomonas aeruginosa, Proteus mirabilis, Enterobacter cloacae, Enterobacter aerogenes, Klebsiella pneumoniae i Stenotrophomonas maltophilia; ili Mycobacterium tuberculosis.
15. Spoj u skladu s bilo kojim od zahtjeva 1 do 11, naznačen time što je namijenjen upotrebi u terapiji.
16. Spoj u skladu s bilo kojim od zahtjeva 1 do 11, naznačen time što je namijenjen upotrebi u liječenju bakterijskih infekcija kod sisavaca.
17. Farmaceutski pripravak, naznačen time što sadrži spoj u skladu s bilo kojim od zahtjeva 1 do 9 i farmaceutski prihvatljivu podlogu.
18. Farmaceutski pripravak, naznačen time što sadrži spoj u skladu s patentnim zahtjevom 10 ili 11 i farmaceutski prihvatljivu podlogu.
19. Spoj formule (IIIA): [image] formule (IIIB): [image] ili formule (8) [image] naznačen time što L je -A-N(R20)R2', gdje R20 je vodik, R2' je R2 ili skupina koju se može prevesti u istu, a A, R2, R1a i R1b su kao što je definirano u patentnom zahtjevu 1.
20. Spoj, naznačen time što je (2R)-2-[(4-amino-1-piperidinil)metil]-1,2-dihidro-3H,8H-2a,5,8a-triazaacenaftilen-3,8-dion.
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