HRP20230215T1 - Supstituirani policiklički derivati piridona i njihov predlijek - Google Patents

Supstituirani policiklički derivati piridona i njihov predlijek Download PDF

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Publication number
HRP20230215T1
HRP20230215T1 HRP20230215TT HRP20230215T HRP20230215T1 HR P20230215 T1 HRP20230215 T1 HR P20230215T1 HR P20230215T T HRP20230215T T HR P20230215TT HR P20230215 T HRP20230215 T HR P20230215T HR P20230215 T1 HRP20230215 T1 HR P20230215T1
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Croatia
Prior art keywords
optionally substituted
group
substituent group
substituent
alkyl
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HRP20230215TT
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English (en)
Inventor
Makoto Kawai
Kenji Tomita
Toshiyuki Akiyama
Azusa Okano
Masayoshi Miyagawa
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Shionogi & Co., Ltd.
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Priority claimed from PCT/JP2016/063139 external-priority patent/WO2016175224A1/ja
Publication of HRP20230215T1 publication Critical patent/HRP20230215T1/hr

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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D498/14Ortho-condensed systems
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/53Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
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    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53831,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic ring systems
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    • A61K31/54Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/542Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame ortho- or peri-condensed with heterocyclic ring systems
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    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/553Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
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    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
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    • A61K47/26Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
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    • A61K9/1605Excipients; Inactive ingredients
    • A61K9/1617Organic compounds, e.g. phospholipids, fats
    • A61K9/1623Sugars or sugar alcohols, e.g. lactose; Derivatives thereof; Homeopathic globules
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    • A61K9/2013Organic compounds, e.g. phospholipids, fats
    • A61K9/2018Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
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    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2022Organic macromolecular compounds
    • A61K9/205Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
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    • A61P31/16Antivirals for RNA viruses for influenza or rhinoviruses
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    • C07D471/12Heterocyclic 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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    • C07D471/12Heterocyclic 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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    • C07D513/12Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains three hetero rings
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    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6561Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Claims (8)

1. Spoj, naznačen time, da je predstavljen sljedećim formulama: [image] [image] [image] [image] [image] [image] [image] [image] ili njegova farmaceutski prihvatljiva sol; pri čemu P je vodik ili skupina PR odabrana od sljedećih formula: a) -C(=O)-PR0, b) -CC(=O)-PR1, c) -C(=O)-L-PR1, d) -C(=O)-L-O-PR1, e) -C(=O)-L-O-L-O-PR1, f) -C(=O)-L-O-C(=O)-PR1, g) -C(=O)-O-PR2, h) -C(=O)-N(-K)(PR2), i) -C(=O)-O-L-O-PR2, j) -C(PR3)2-O-PR4, k) -C(PR3)2-O-L-O-PR4, l) -C(PR3)2-O-C(=O)-PR4, m) -C(PR3)2-O-C(=O)-O-PR4, n) -C(PR3)2-O-C(=O)-N(-K)-PR4, o) -C(PR3)2-O-C(=O)-O-L-O-PR4, p) -C(PR3)2-O-C(=O)-O-L-N(PR4)2, q) -C(PR3)2-O-C(=O)-N(-K)-L-O-PR4, r) -C(PR3)2-O-C(=O)-N(-K)-L-N(PR4)2, s) -C(PR3)2-O-C(=O)-O-L-O-L-O-PR4, t) -C(PR3)2-O-C(=O)-O-L-N(-K)-C(=O)-PR4, u) -C(PR3)2-O-P(=O)(-PR5)2, v) -C(PR3)2-PR6, w) -CC=N+(PR7)2)(-N(PR7)2), x) -C(PR3)2-C(PR3)2-C(=O)-O-PR2, y) -C(PR3)2-N(-K)-C(=O)-O-PR2, z) -P(=O)(-PR8)(-PR9), aa) -S(=O)2-O-PR10, bb) PR11, i cc) -C(PR3)2-C(PR3)2-O-PR2, gdje L je ravni ili razgranati alkilen, ili ravni ili razgranati alkenilen; K je vodik, ili alkil opcionalno supstituiran sa supstituentskom skupinom A; PR0 je alkil opcionalno supstituiran sa supstituentskom skupinom A, ili alkenil opcionalno supstituiran sa supstituentskom skupinom A; PR1 je karbociklil skupina opcionalno supstituirana sa supstituentskom skupinom A, heterociklil skupina opcionalno supstituirana sa supstituentskom skupinom A, alkilamino opcionalno supstituiran sa supstituentskom skupinom A, ili alkilsulfanil opcionalno supstituiran sa supstituentskom skupinom A; PR2 je alkil opcionalno supstituiran sa supstituentskom skupinom A, karbociklil skupina opcionalno supstituirana sa supstituentskom skupinom A, heterociklil skupina opcionalno supstituirana sa supstituentskom skupinom A, karbociklilalkil opcionalno supstituiran sa supstituentskom skupinom A, heterociklilalkil opcionalno supstituiran sa supstituentskom skupinom A, ili trialkilsilil; svaki PR3 je neovino vodik ili alkil; svaki PR4 je neovisno alkil opcionalno supstituiran sa supstituentskom skupinom A, karbociklil skupina opcionalno supstituirana sa supstituentskom skupinom A, heterociklil skupina opcionalno supstituirana sa supstituentskom skupinom A, alkilamino opcionalno supstituiran sa supstituentskom skupinom A, karbociklilalkil opcionalno supstituiran sa supstituentskom skupinom A, heterociklilalkil opcionalno supstituiran sa supstituentskom skupinom A, ili trialkilsilil; svaki PR5 je neovisno vodik ili OBn; PR6 je karbociklil skupina opcionalno supstituirana sa supstituentskom skupinom A, ili heterociklil skupina opcionalno supstituirana sa supstituentskom skupinom A; svaki PR7 je neovisno alkil opcionalno supstituiran sa supstituentskom skupinom A; PR8 je alkiloksi opcionalno supstituiran sa supstituentskom skupinom A; PR9 je alkiloksi opcionalno supstituiran sa supstituentskom skupinom A, alkilamino opcionalno supstituiran sa supstituentskom skupinom A, karbocikliloksi opcionalno supstituiran sa supstituentskom skupinom A, heterocikliloksi opcionalno supstituiran sa supstituentskom skupinom A, karbociklilamino opcionalno supstituiran sa supstituentskom skupinom A, ili heterociklilamino opcionalno supstituiran sa supstituentskom skupinom A; PR8 i PR9 se mogu uzeti zajedno sa susjednim atomom fosfora u svrhu tvorbe heterocikla opcionalno supstituiranog sa supstituentskom skupinom A; PR10 je alkil opcionalno supstituiran sa supstituentskom skupinom A, karbociklil skupina opcionalno supstituirana sa supstituentskom skupinom A, heterociklil skupina opcionalno supstituirana sa supstituentskom skupinom A, karbociklilalkil opcionalno supstituiran sa supstituentskom skupinom A, ili heterociklilalkil opcionalno supstituiran sa supstituentskom skupinom A; PR11 je alkil opcionalno supstituiran sa supstituentskom skupinom A, alkenil opcionalno supstituiran sa supstituentskom skupinom A, karbociklil skupina opcionalno supstituirana sa supstituentskom skupinom A, ili heterociklilalkil skupina opcionalno supstituirana sa supstituentskom skupinom A; supstituentska skupina A: okso, alkil, hidroksialkil, amino, alkilamino, karbociklil skupina, heterociklil skupina, karbociklilalkil, alkilkarbonil, halogen, hidroksi, karboksi, alkilkarbonilamino, alkilkarbonilaminoalkil, alkilkarboniloksi, alkiloksikarbonil, alkiloksikarbonilalkil, alkiloksikarboniloksi, alkilaminokarboniloksi, alkilaminoalkil, alkiloksi, cijano, nitro, azido, alkilsulfonil, trialkilsilil, i fosfo.
2. Spoj prema patentnom zahtjevu 1, naznačen time, da je predstavljen jednom od sljedećih formula: [image] [image] gdje P ima isto značenje kao što je opisano u patentnom zahtjevu 1, ili njegova farmaceutski prihvatljiva sol.
3. Spoj prema patentnom zahtjevu 1 ili 2, ili njegova farmaceutski prihvatljiva sol, naznačen time, da PR je skupina odabrana od sljedećih formula: a) -C(=O)-PR0, b) -C(=O)-PR1, g) -C(=O)-O-PR2, h) -C(=O)-N(-K)(PR2), i) -C(=O)-O-L-O-PR2, l) -C(PR3)2-O-C(=O)-PR4, m) -C(PR3)2-O-C(=O)-O-PR4, o) -C(PR3)2-O-C(=O)-O-L-O-PR4, v) -C(PR3)2-PR6, (osim benzil skupine) x) -C(PR3)2-C(PR3)2-C(=O)-O-PR2, y) -C(PR3)2-N(-K)-C(=O)-O-PR2, i z) -P(=O)(-PR8)(-PR9), pri čemu L je ravni ili razgranati niži alkilen; K je vodik, ili alkil opcionalno supstituiran sa supstituentskom skupinom A; PR0 je alkil opcionalno supstituiran sa supstituentskom skupinom A; PR1 je karbociklil skupina opcionalno supstituirana sa supstituentskom skupinom A, ili heterociklil skupina opcionalno supstituirana sa supstituentskom skupinom A; PR2 je alkil opcionalno supstituiran sa supstituentskom skupinom A, karbociklil skupina opcionalno supstituirana sa supstituentskom skupinom A, heterociklil skupina opcionalno supstituirana sa supstituentskom skupinom A, karbociklilalkil opcionalno supstituiran sa supstituentskom skupinom A, ili heterociklilalkil opcionalno supstituiran sa supstituentskom skupinom A; svaki PR3 je neovsino vodik ili alkil; PR4 je alkil opcionalno supstituiran sa supstituentskom skupinom A, karbociklil skupina opcionalno supstituirana sa supstituentskom skupinom A, ili heterociklil skupina opcionalno supstituirana sa supstituentskom skupinom A; PR6 je karbociklil skupina opcionalno supstituirana sa supstituentskom skupinom A, ili heterociklil skupina opcionalno supstituirana sa supstituentskom skupinom A; PR8 je alkiloksi opcionalno supstituiran sa supstituentskom skupinom A; PR9 je alkiloksi opcionalno supstituiran sa supstituentskom skupinom A, alkilamino opcionalno supstituiran sa supstituentskom skupinom A, karbocikliloksi opcionalno supstituiran sa supstituentskom skupinom A, heterocikliloksi opcionalno supstituiran sa supstituentskom skupinom A, karbociklilamino opcionalno supstituiran sa supstituentskom skupinom A, ili heterociklilamino opcionalno supstituiran sa supstituentskom skupinom A; i PR8 i PR9 se mogu uzeti zajedno sa susjednim atomom fosfora u svrhu tvorbe heterocikla opcionalno supstituiranog sa supstituentskom skupinom A; supstituentska skupina A: okso, alkil, alkilamino, karbociklil skupina, heterociklil skupina, alkilkarbonil, halogen, hidroksi, alkilkarbonilamino, alkilkarboniloksi, alkiloksikarbonil, alkiloksikarbonilalkil, alkilaminokarboniloksi, alkiloksi, nitro, azido, alkilsulfonil, i trialkilsilil.
4. Spoj prema patentnom zahtjevu 1, naznačen time, da je predstavljen sa sljedećim formulama: [image] ili njegova farmaceutski prihvatljiva sol.
5. Spoj prema patentnom zahtjevu 4, naznačen time, da je predstavljen sa sljedećom formulom: [image] ili njegova farmaceutski prihvatljiva sol.
6. Farmaceutski pripravak, naznačen time, da sadrži spoj u skladu s jednim od patentnih zahtjeva 1 do 5, ili njegovu farmaceutski prihvatljivu sol.
7. Farmaceutski pripravak prema patentom zahtjevu 6, naznačen time, da je za uporabu u liječenju ili prevenciji infekcije virusnom gripom.
8. Spoj prema bilo kojem od patentnih zahtjeva 1 do 5, ili njegova farmaceutski prihvatljiva sol, naznačen time, da je za uporabu u liječenju ili prevenciji bolesti uzrokovane virusom koji ima endonukleazu ovisnu o kapi.
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