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HRP20120901T1 - Diaminopirimidini kao p2x3 i p2x2/3 - Google Patents

Diaminopirimidini kao p2x3 i p2x2/3 Download PDF

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Publication number
HRP20120901T1
HRP20120901T1 HRP20120901TT HRP20120901T HRP20120901T1 HR P20120901 T1 HRP20120901 T1 HR P20120901T1 HR P20120901T T HRP20120901T T HR P20120901TT HR P20120901 T HRP20120901 T HR P20120901T HR P20120901 T1 HRP20120901 T1 HR P20120901T1
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Croatia
Prior art keywords
isopropyl
methoxy
phenoxy
diamine
pyrimidine
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HRP20120901TT
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English (en)
Inventor
David Scott Carter
Michael Patrick Dillon
Roland Charles Hawley
Clara Jeou Jen Lin
Daniel Warren Parish
Chris Allen Broka
Alam Jahangir
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F. Hoffmann - La Roche Ag
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Publication of HRP20120901T1 publication Critical patent/HRP20120901T1/hr

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    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
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    • 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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Claims (7)

1. Spoj, naznačen time, da ima formulu (I) [image] ili njegova farmaceutski prihvatljiva sol, gdje: X je -O-; Y je vodik; ili -NRdRe, gdje je jedan od Rd i Re vodik, a drugi je vodik; alkil; cikloalkil; cikloalkilalkil; haloalkil; haloalkoksi; hidroksialkil; alkoksialkil; acetil; alkilsulfonil; alkilsulfonilalkil; aminokarboniloksialkil; hidroksikarbonilalkil; hidroksialkiloksikarbonilalkil; aril; aralkil; arilsulfonil; heteroaril; heteroarilalkil; heteroarilsulfonil; heterociklil; ili heterociklilalkil; D je opcijski kisik; R1 je izopropil; R2, R4 i R5 su svaki neovisno vodik; alkil; alkenil; amino; halo; amido; haloalkil; alkoksi; hidroksi; haloalkoksi; nitro; amino; hidroksialkil; alkoksialkil; hidroksialkoksi; alkinilalkoksi; alkilsulfonil; arilsulfonil; cijano; aril; heteroaril; heterociklil; heterociklilalkoksi; ariloksi; heteroariloksi; aralkiloksi; heteroaralkiloksi; opcijski supstituiran fenoksi; -(CH2)m-(Z)n-(CO)-Rf ili -(CH2)m-(Z)n-SO2-(NRg)n-Rf, gdje su m i n svaki neovisno 0 ili 1, Z je O ili NRg, Rf je vodik, alkil, hidroksi, alkoksi, amino, hidroksialkil ili alkoksialkil, i svaki Rg je neovisno vodik ili alkil; R3 je metoksi; R6 je vodik; alkil; halo; haloalkil; amino; ili alkoksi; i jedan od R7 i R8 je vodik, a drugi je vodik; alkil; cikloalkil; cikloalkilalkil; haloalkil; haloalkoksi; hidroksialkil; alkoksialkil; acetil; alkilsulfonil; alkilsulfonilalkil; aminokarboniloksialkil; hidroksikarbonilalkil; hidroksialkiloksikarbonilalkil; aril; aralkil; arilsulfonil; heteroaril; heteroarilalkil; heteroarilsulfonil; heterociklil; ili heterociklilalkil.
2. Spoj prema zahtjevu 1, naznačen time, da ima formulu (II) [image] gdje: X je: -O-; R1 je izopropil; R3 je metoksi; R4 je: vodik; alkil; alkenil; amino; halo; amido; haloalkil; alkoksi; hidroksi; haloalkoksi; nitro; hidroksialkil; alkoksialkil; hidroksialkoksi; alkinilalkoksi; alkilsulfonil; arilsulfonil; cijano; aril; heteroaril; heterociklil; heterociklilalkoksi; ariloksi; heteroariloksi; aralkiloksi; heteroaralkiloksi; opcijski supstituiran fenoksi; (CH2)m-(Z)n-(CO)-Rfili -(CH2)m-(Z)n-SO2-(NRg)n-Rf , gdje su m i n svaki neovisno 0 ili 1, Z je O ili NRg, Rfje vodik, alkil, hidroksi, alkoksi, amino, hidroksialkil ili alkoksialkil, a svaki Rgje neovisno vodik ili alkil; jedan od Rdi Reje vodik, a drugi je: vodik; alkil; cikloalkil; cikloalkilalkil; haloalkil; haloalkoksi; hidroksialkil; alkoksialkil; acetil; alkilsulfonil; alkilsulfonilalkil; aminokarboniloksialkil; hidroksikarbonilalkil; hidroksialkiloksikarbonilalkil; aril; aralkil; arilsulfonil; heteroaril; heteroarilalkil; heteroarilsulfonil; heterociklil; ili heterociklilalkil.
3. Farmaceutski sastav, naznačen time, da obuhvaća farmaceutski prihvatljivo pomoćno sredstvo; te spoj prema zahtjevu 1.
4. Uporaba spoja prema zahtjevu 1, naznačena time, da je za proizvodnju lijeka za liječenje bolesti posredovane antagonistom receptora P2X3ili P2X2/3.
5. Uporaba prema zahtjevu 4, naznačena time, da spomenuta bolest je genitourinarna bolest ili je bolest povezana s bolovima.
6. Uporaba spoja prema zahtjevu 5, naznačena time, da spomenuta genitourinarna bolest je: smanjenje kapaciteta mjehura; učestalo mokrenje; ubrzana inkontinencija; inkontinencija s pritiskom; hiperreaktivnost mjehura; benigna prostatska hipertrofija; prostatitis; hiperrefleksija detruzora; urinarna frekvencija; učestalo noćno mokrenje; urinarna urgencija; prekomjerno aktivni mjehur; hipersenzibilnost karlice; uretritis; sindrom bolne karlice; prostatodinija; cistitis; ili idiopatska hipersenzibilnost mjehura; a bolest koja je povezana s bolovima je: upalna bol, kirurška bol; organska bol; zubobolja; predmenstrualna bol; središnja bol; bol kod opeklina; migrena ili serijske glavobolje; povreda živca; neuritis; neuralgije; otrovanje; ishemijska ozljeda; intersticijalni cistitis; bol kod tumora; viroza, infekcija parazitima ili bakterijama; post-traumatska ozljeda; ili bol povezana sa sindromom osjetljivih crijeva.
7. Spoj formule I prema zahtjevu 1, naznačen time, da je odabran iz skupine koju čine: 5-(2-izopropil-4,5-dimetoksi-fenoksi)-pirimidin-2,4-diamin; 5-(5-bromo-2-izopropil-4-metoksi-fenoksi)-pirimidin-2,4-diamin; 5-(5-kloro-2-izopropil-4-metoksi-fenoksi)-pirimidin-2,4-diamin; 5-(2-izopropil-4-metoksi-5-metil-fenoksi)-pirimidin-2,4-diamin; N2-benzil-5-(5-kloro-2-izopropil-4-metoksi-fenoksi)-pirimidin-2,4-diamin; 5-(5-kloro-2-izopropil-4-metoksi-fenoksi)-N2-(tetrahidro-piran-4-il)-pirimidin-2,4-diamin; 5-(5-kloro-2-izopropil-4-metoksi-fenoksi)-N2-izopropil-pirimidin-2,4-diamin; N2-izopropil-5-(2-izopropil-4,5-dimetoksi-fenoksi)-pirimidin-2,4-diamin; 5-(2-izopropil-4,5-dimetoksi-fenoksi)-N2-fenil-pirimidin-2,4-diamin; N2-benzil-5-(2-izopropil-4,5-dimetoksi-fenoksi)-pirimidin-2,4-diamin; N-[4-amino-5-(2-izopropil-4,5-dimetoksi-fenoksi)-pirimidin-2-il]-acetamid; 5-(2-izopropil-4,5-dimetoksi-fenoksi)-N2-(2,2,2-trifluoro-etil)-pirimidin-2,4-diamin; 5-(2-izopropil-4,5-dimetoksi-fenoksi)-N2-(2-metoksi-etil)-pirimidin-2,4-diamin; 3-[4-amino-5-(5-kloro-2-izopropil-4-metoksi-fenoksi)-pirimidin-2-ilamino]-pentan-1,5-diol; 2-[4-amino-5-(5-kloro-2-izopropil-4-metoksi-fenoksi)-pirimidin-2-ilamino]-butan-1-ol; 1-[5-(2,4-diamino-pirimidin-5-iloksi)-4-izopropil-2-metoksi-fenil]-etanon; 5-[5-(1H-imidazol-2-il)-2-izopropil-4-metoksi-fenoksi]-pirimidin-2,4-diamin; 5-(5-kloro-2-izopropil-4-metoksi-fenoksi)-N2-(3-etansulfonil-1-metil-propil)-pirimidin-2,4-diamin; 5-(2,4-diamino-pirimidin-5-iloksi)-4-izopropil-2-metoksi-benzamid; 5-(2,4-diamino-pirimidin-5-iloksi)-4-izopropil-2-metoksi-benzoična kiselina; 5-[2-izopropil-4-metoksi-5-(1H-tetrazol-5-il)-fenoksi]-pirimidin-2,4-diamin; 5-(2,4-diamino-pirimidin-5-iloksi)-4-izopropil-2-metoksi-benzonitril; 4-[4-amino-5-(5-kloro-2-izopropil-4-metoksi-fenoksi)-pirimidin-2-ilamino]-piperidin-1-karboksilna kiselina-etilester; [5-(2,4-diamino-pirimidin-5-iloksi)-4-izopropil-2-metoksi-fenil]-urea; 5-(5-kloro-2-izopropil-4-metoksi-fenoksi)-N2-(1-ciklopropil-etil)-pirimidin-2,4-diamin; 5-(5-amino-2-izopropil-4-metoksi-fenoksi)-pirimidin-2,4-diamin; N-[5-(2,4-diamino-pirimidin-5-iloksi)-4-izopropil-2-metoksi-fenil]-acetamid; 5-(2-izopropil-4-metoksi-5-tetrazol-1-il-fenoksi)-pirimidin-2,4-diamin; 5-(2-izopropil-4-metoksi-fenoksi)-pirimidin-2,4-diamin; 5-(2-izopropil-5-metansulfonil-4-metoksi-fenoksi)-pirimidin-2,4-diamin; 5-(2-izopropil-4-metoksi-5-metil-fenoksi)-N4-fenil-pirimidin-2,4-diamin; 5-(5-kloro-2-izopropil-4-metoksi-fenoksi)-N2-(1,1-diokso-heksahidro-1λ6-tiopiran-4-il)-pirimidin-2,4-diamin; metil-karbaminska kiselina-2-[4-amino-5-(5-kloro-2-izopropil-4-metoksi-fenoksi)-pirimidin-2-ilamino]-propilester; 5-(2-izopropil-4,5-dimetoksi-fenoksi)-6-metil-pirimidin-2,4-diamin; 1-(4-{2-[4-amino-5-(5-kloro-2-izopropil-4-metoksi-fenoksi)-pirimidin-2-ilamino]-propil}-piperazin-1-il)-etanon; 5-(5-kloro-2-izopropil-4-metoksi-fenoksi)-N2-(1-metansulfonil-piperidin-4-il)-pirimidin-2,4-diamin; 2-[4-amino-5-(5-kloro-2-izopropil-4-metoksi-fenoksi)-pirimidin-2-ilamino]-(R)-propan-1-ol; 5-(2-izopropil-5-metansulfonil-4-metoksi-fenoksi)-N2-(tetrahidro-tiopiran-4-il)-pirimidin-2,4-diamin; 5-(5-kloro-2-izopropil-4-metoksi-fenoksi)-N2-(1,1-diokso-heksahidro-1λ6-tiopiran-4-il)-pirimidin-2,4-diamin; 5-[5-(4,5-dihidro-1H-imidazol-2-il)-2-izopropil-4-metoksi-fenoksi]-pirimidin-2,4-diamin; 5-(5-jodo-2-izopropil-4-metoksi-fenoksi)-pirimidin-2,4-diamin; 5-(2,4-diamino-pirimidin-5-iloksi)-4-izopropil-2-metoksi-benzensulfonamid; 3-[4-amino-5-(5-bromo-2-izopropil-4-metoksi-fenoksi)-pirimidin-2-ilamino]-pentan-1,5-diol; 5-(5-jodo-2-izopropil-4-metoksi-fenoksi)-1-oksi-pirimidin-2,4-diamin; 5-(2-izopropil-4-metoksi-5-vinil-fenoksi)-pirimidin-2,4-diamin; 5-(2-izopropil-4-metoksi-5-pirazol-1-il-fenoksi)-pirimidin-2,4-diamin; 5-[2-izopropil-4-metoksi-5-(3-metil-pirazol-1-il)-fenoksi]-pirimidin-2,4-diamin; 5-(2-izopropil-4-metoksi-5-oksazol-2-il-fenoksi)-pirimidin-2,4-diamin; (S)-2-[4-amino-5-(5-bromo-2-izopropil-4-metoksi-fenoksi)-pirimidin-2-ilamino]-butan-1-ol; 5-(2-izopropil-4-metoksi-5-trifluorometil-fenoksi)-pirimidin-2,4-diamin; 5-(2-izopropil-4-metoksi-5-tiazol-4-il-fenoksi)-pirimidin-2,4-diamin; 5-(2-izopropil-4-metoksi-5-tiofen-3-il-fenoksi)-pirimidin-2,4-diamin; (R)-2-[4-amino-5-(2-izopropil-5-metansulfonil-4-metoksi-fenoksi)-pirimidin-2-ilamino]-butan-1-ol; (S)-2-[4-amino-5-(5-kloro-2-izopropil-4-metoksi-fenoksi)-pirimidin-2-ilamino]-propionska kiselina; 5-[5-(4,5-dihidro-oksazol-2-il)-2-izopropil-4-metoksi-fenoksi]-pirimidin-2,4-diamin; 5-(2-izopropil-5-metansulfonil-4-metoksi-fenoksi)-N2-(2,2,2-trifluoro-etil)-pirimidin-2,4-diamin; (S)-2-[4-amino-5-(5-kloro-2-izopropil-4-metoksi-fenoksi)-pirimidin-2-ilamino]-propionska kiselina-3-hidroksi-2-hidroksimetil-2-metil-propilester; 5-[5-(5-kloro-tiofen-2-il)-2-izopropil-4-metoksi-fenoksi]-pirimidin-2,4-diamin; 5-[2-izopropil-4-metoksi-5-(1-metil-1H-imidazol-2-il)-fenoksi]-pirimidin-2,4-diamin; 5-[2-izopropil-4-metoksi-5-(2H-pirazol-3-il)-fenoksi]-pirimidin-2,4-diamin; 5-(5-imidazol-1-il-2-izopropil-4-metoksi-fenoksi)-pirimidin-2,4-diamin; N2-izopropil-5-(2-izopropil-5-metansulfonil-4-metoksi-fenoksi)-pirimidin-2,4-diamin; 5-(2-izopropil-5-metansulfonil-4-metoksi-fenoksi)-N2-fenil-pirimidin-2,4-diamin; 5-(4-amino-2-etilamino-pirimidin-5-iloksi)-4-izopropil-2-metoksi-benzamid; 2-[4-amino-5-(2-izopropil-5-metansulfonil-4-metoksi-fenoksi)-pirimidin-2-ilamino]-etanol; 5-[2-izopropil-4-metoksi-5-(2-metil-tiazol-4-il)-fenoksi]-pirimidin-2,4-diamin; 5-(2-izopropil-5-metansulfonil-4-metoksi-fenoksi)-N2-(2-metoksi-etil)-pirimidin-2,4-diamin; 5-(2-izopropil-4-metoksi-5-[1,2,3]triazol-1-il-fenoksi)-pirimidin-2,4-diamin; 5-(5-furan-2-il-2-izopropil-4-metoksi-fenoksi)-pirimidin-2,4-diamin; 1-[5-(2,4-diamino-pirimidin-5-iloksi)-4-izopropil-2-metoksi-fenil]-3-etil-urea; N2-ciklopropil-5-(2-izopropil-5-metansulfonil-4-metoksi-fenoksi)-pirimidin-2,4-diamin; 5-[5-(3,5-dimetil-pirazol-1-il)-2-izopropil-4-metoksi-fenoksi]-pirimidin-2,4-diamin; N2-benzil-5-(2-izopropil-5-metansulfonil-4-metoksi-fenoksi)-pirimidin-2,4-diamin; N2-etil-5-(2-izopropil-5-metansulfonil-4-metoksi-fenoksi)-pirimidin-2,4-diamin; 5-(2-izopropil-5-metansulfonil-4-metoksi-fenoksi)-N2-(1-metansulfonil-piperidin-4-il)-pirimidin-2,4-diamin; N2-izobutil-5-(2-izopropil-5-metansulfonil-4-metoksi-fenoksi)-pirimidin-2,4-diamin; 5-(2,4-diamino-pirimidin-5-iloksi)-4-izopropil-2-metoksi-N-metil-benzamid; 5-(2-izopropil-5-izoksazol-5-il-4-metoksi-fenoksi)-pirimidin-2,4-diamin; N2-(4-fluoro-fenil)-5-(2-izopropil-5-metansulfonil-4-metoksi-fenoksi)-pirimidin-2,4-diamin; 5-(2-izopropil-4-metoksi-5-[1,2,4]oksadiazol-3-il-fenoksi)-pirimidin-2,4-diamin; 5-(2-izopropil-5-metansulfonil-4-metoksi-fenoksi)-N2-(tetrahidro-piran-4-il)-pirimidin-2,4-diamin; 1-[5-(2,4-diamino-pirimidin-5-iloksi)-4-izopropil-2-metoksi-fenil]-etanol; 5-(2,5-diizopropil-4-metoksi-fenoksi)-pirimidin-2,4-diamin; 5-(5-benzo[b]tiofen-3-il-2-izopropil-4-metoksi-fenoksi)-pirimidin-2,4-diamin; 5-[2-izopropil-4-metoksi-5-(1-metoksi-etil)-fenoksi]-pirimidin-2,4-diamin; 5-(2-izopropil-4-metoksi-5-oksazol-4-il-fenoksi)-pirimidin-2,4-diamin; 5-(2-izopropil-4-metoksi-5-tiazol-2-il-fenoksi)-pirimidin-2,4-diamin; 5-(5-furan-3-il-2-izopropil-4-metoksi-fenoksi)-pirimidin-2,4-diamin; 5-(2-izopropil-4-metoksi-5-tiofen-2-il-fenoksi)-pirimidin-2,4-diamin; 1-[5-(2,4-diamino-pirimidin-5-iloksi)-4-izopropil-2-metoksi-fenil]-3-fenil-urea; 5-(2,4-diamino-pirimidin-5-iloksi)-4-izopropil-2-metoksi-N-metil-benzensulfonamid; 5-(2-izopropil-5-metansulfonil-4-metoksi-fenoksi)-N2-metil-pirimidin-2,4-diamin; 5-(2-izopropil-4-metoksi-5-pirol-1-il-fenoksi)-pirimidin-2,4-diamin; 5-(2-izopropil-4-metoksi-5-trifluorometoksi-fenoksi)-pirimidin-2,4-diamin; 5’-(2,4-diamino-pirimidin-5-iloksi)-4’-izopropil-2’-metoksi-bifenil-3-karbonitril; 5-[2-izopropil-4-metoksi-5-(4-metil-tiofen-2-il)-fenoksi]-pirimidin-2,4-diamin; 5-(5-kloro-2-izopropil-4-metoksi-fenoksi)-N2-[(S)-1-(4-metil-2,6,7-trioksa-biciklo[2.2.2]okt-1-il)-etil]-pirimidin-2,4-diamin; 5-(2-izopropil-4-metoksi-5-nitro-fenoksi)-pirimidin-2,4-diamin; 5-(4-izopropil-6-metoksi-bifenil-3-iloksi)-pirimidin-2,4-diamin; 5-(2-izopropil-4-metoksi-5-tiazol-5-il-fenoksi)-pirimidin-2,4-diamin; 1-[5-(2,4-diamino-pirimidin-5-iloksi)-4-izopropil-2-metoksi-fenil]-pirolidin-2-on; 5-(2-izopropil-4-metoksi-5-oksazol-5-il-fenoksi)-pirimidin-2,4-diamin; 5-[2-izopropil-4-metoksi-5-(4-metil-tiofen-3-il)-fenoksi]-pirimidin-2,4-diamin; 5-(2-izopropil-4-metoksi-5-nitro-fenoksi)-pirimidin-2,4-diamin; 5-(2-izopropil-4-metoksi-5-[1,2,4]triazol-1-il-fenoksi)-pirimidin-2,4-diamin; 5-(2-izopropil-4,5-dimetoksi-fenoksi)-N2-(2-metoksi-etil)-pirimidin-2,4-diamin; 5-(4’-fluoro-4-izopropil-6-metoksi-bifenil-3-iloksi)-pirimidin-2,4-diamin; 5-(5-kloro-2-izopropil-4-metoksi-fenoksi)-N2-(2,2,2- trifluoro-etil)-pirimidin-2,4-diamin; 5-[2-izopropil-4-metoksi-5-(2-metil-tiazol-5-il)-fenoksi]-pirimidin-2,4-diamin; 5-(2-izopropil-4-metoksi-6-metil-fenoksi)-pirimidin-2,4-diamin; 5-(5-etansulfonil-2-izopropil-4-metoksi-fenoksi)-pirimidin-2,4-diamin; 1-[5-(2,4-diamino-pirimidin-5-iloksi)-4-izopropil-2-metoksi-fenil]-1H-imidazol-2-tiol; 5-[2-izopropil-4-metoksi-5-(1-metil-1H-pirazol-4-il)-fenoksi]-pirimidin-2,4-diamin; 5-(5-fluoro-2-izopropil-4-metoksi-fenoksi)-pirimidin-2,4-diamin; 2-[5-(2,4-diamino-pirimidin-5-iloksi)-4-izopropil-2-metoksi-fenil]-propan-2-ol; 5-(2-izopropil-4-metoksi-5-piridin-4-il-fenoksi)-pirimidin-2,4-diamin; 5-(2,4-diamino-pirimidin-5-iloksi)-N-etil-4-izopropil-2-metoksi-benzensulfonamid; 5-[2-izopropil-5-(4-metansulfonil-piperazin-1-il)-4-metoksi-fenoksi]-pirimidin-2,4-diamin; 5-(2-izopropil-4-metoksi-5-piridin-3-il-fenoksi)-pirimidin-2,4-diamin; 5-(2,4-diamino-pirimidin-5-iloksi)-4-izopropil-2-metoksi-N,N-dimetil-benzamid; 5-[5-(2,5-dimetil-pirol-1-il)-2-izopropil-4-metoksi-fenoksi]-pirimidin-2,4-diamin; N2-(1,1-diokso-heksahidro-1λ6-tiopiran-4-il)-5-(2-izopropil-4,5-dimetoksi-fenoksi)-pirimidin-2,4-diamin; 5-[5-(2,3-dihidro-1H-tetrazol-5-il)-2-izopropil-4-metoksi-fenoksi]-pirimidin-2,4-diamin; i 1-[5-(4-amino-2-metil-pirimidin-5-iloksi)-4-izopropil-2-metoksi-fenil]-pirolidin-2-on.
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