ME02100B - Derivati 4-aminopirimidina i njihova primena kao antagonista adenozinskog a2a receptora - Google Patents

Derivati 4-aminopirimidina i njihova primena kao antagonista adenozinskog a2a receptora

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Publication number
ME02100B
ME02100B MEP-2015-55A MEP5515A ME02100B ME 02100 B ME02100 B ME 02100B ME P5515 A MEP5515 A ME P5515A ME 02100 B ME02100 B ME 02100B
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Montenegro
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pyrazol
pyrimidin
bromo
amine
disease
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MEP-2015-55A
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Gómez Juan Alberto Camacho
Laria Julio Cesar Castro-Palomino
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Palobiofarma Sl
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Publication of ME02100B publication Critical patent/ME02100B/me

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Claims (18)

1. Jedinjenje formule (I):gde- R1 predstavlja petočlani heteroaril prsten izabran od pirazol, tiazol, ili triazol prstenova po izboru supstituisanih sa jednim ili dva halogena atoma ili jednom ili dve metil ili trifluorometil grupe- R2 predstavlja vodonikov atom- R3 predstavlja atom broma, atom hlora ili cijano grupu- R4 predstavlja nezavisno:a) petočlanu heteroaril grupu po izboru supstituisanu jednim ili više halogenih atoma ili jednom ili više C1-C8 alkil, cikloalkil, C1-C8 alkoksi, C1-C8 alkiltio, amino, mono- ili di-C1-C8 alkilamino grupab) grupu -N(R5)(R6) u kojoj R5 i R6 predstavljaju nezavisno:- vodonikov atom- alkil ili cikloalkil grupu od 3 do 6 ugljenikovih atoma, linearnu ili razgranatu, po izboru supstituisanu sa jednim ili više halogenih atoma ili jednom ili više cikloalkil, hidroksi, C1-C8 alkoksi, amino, mono- ili di- C1-C8 alkilamino grupa- ili R5 i R6 formiraju zajedno sa azotovim atomom za koji su vezani zasićenu heterocikličnu grupu sa od 4 do 6 članova u koju dalje može biti uveden heteroatom, koji je po izboru supstituisan sa jednim ili više halogenih atoma ili jednom ili više C1-C8 alkil, hidroksi, C1-C8 alkoksi, amino, mono- ili di- C1-C8 alkilamino grupa,ilic) grupu -OR7 ili -SR7, gde R7 predstavlja nezavisno:- C1-C8 alkil ili cikloalkil grupu, linearnu ili razgranatu, po izboru supstituisanu sa jednim ili više halogenih atoma ili sa jednom ili više C1-C8 alkil, C1-C8 alkoksi, amino, mono- ili di- C1-C8 alkilamino grupa- Fenil prsten po izboru supstituisan sa jednim ili više halogenih atoma ili njihovom farmaceutski prihvatljivom soli
2. Jedinjenje prema patentnom zahtevu 1 u kome R4 predstavlja pirazolski prsten vezan na položaju 2 pirimidinskog prstena preko azotovog atoma pirazolskog prstena, gde je ovaj pirazolski prsten po izboru supstituisan sa jednim ili dva halogena atoma ili sa jednom ili dve metil grupe.
3. Jedinjenje prema patentnom zahtevu 1 u kome R4 predstavlja 2-tiazolil prsten, gde je ovaj tiazolski prsten po izboru supstituisan sa jednim ili dva halogena atoma ili sa jednom ili dve metil grupe.
4. Jedinjenje prema patentnom zahtevu 1 u kome R4 predstavlja grupu -N(R5)(R6) kao što je definisano u patentnom zahtevu 1.
5. Jedinjenje prema patentnom zahtevu 4 u kome R5 predstavlja vodonikov atom i R6 predstavlja alkil ili cikloalkil grupu sa 3 do 6 ugljenikovih atoma, linearnu ili razgranatu, po izboru supstituisanu sa halogenim atomima, amino, C1-C8 alkilamino.
6. Jedinjenje prema patentnom zahtevu 1 u kome R3 predstavlja atom broma ili hlora.
7. Jedinjenje prema patentnom zahtevu 6 u kome R1 predstavlja pirazolski ili tiazolski prsten od kojih su oba po izboru supstituisana sa jednim ili dva halogena atoma ili sa jednom ili dve metil ili trifluorometil grupe, i R4 predstavlja pirazolski ili tiazolski prsten od kojih su oba po izboru supstituisana sa jednim ili dva halogena atoma ili sa jednom ili dve metil grupe.
8. Jedinjenje prema patentnom zahtevu 6 u kome R1 predstavlja pirazolski prsten po izboru supstituisan sa jednim ili dva halogena atoma ili sa metil ili trifluorometil grupama, i R4 predstavlja pirazolski prsten po izboru supstituisan sa jednim ili dva halogena atoma ili sa metil grupama.
9. Jedinjenje prema patentnom zahtevu 6 u kome R1 predstavlja pirazol ili tiazol prstenove po izboru supstituisane sa jednim ili dva halogena atoma, metil ili trifluorometil grupama, i R4 predstavlja grupu -N(R5)(R6).
10. Jedinjenje prema patentnom zahtevu 6 u kome R1 predstavlja pirazol ili tiazol prstenove po izboru supstituisane sa jednim ili dva halogena atoma, metil ili trifluorometil grupama, i R4 predstavlja grupu SR7 ili OR7, gde R7 predstavlja linearnu ili razgranatu C1-C8 alkil grupu po izboru supstituisanu sa atomima fluora.
11. Jedinjenje prema patentnom zahtevu 1 koje je jedno od: 5-brom-2,6-di-(1H-pirazol-1-il)pirimidin-4-amina 5-brom-6-(4-metil-1H-pirazol-1-il)-2-(1H-pirazol-1-il)pirimidin-4-amina 5-brom-2-(1H-pirazol-1-il)-6-(pirolidin-1-il)pirimidin-4-amina 5-brom-N4-ciklopentil-2-(1H-pirazol-1-il)pirimidin-4,6-diamina 5-brom-6-(piperidin-1-il)-2-(1H-pirazol-1-il)pirimidin-4-amina 5-brom-6-morfolino-2-(1H-pirazol-1-il)pirimidin-4-amina 5-brom-6-(4-metilpiperazin-1-il)-2-(1H-pirazol-1-il)pirimidin-4-amina 5-brom-N4-ciklopropil-2-(1H-pirazol-1-il)pirimidin-4,6-diamina 6-(azetidin-1-il)-5-brom-2-(1H-pirazol-1-il)pirimidin-4-amina 5-brom-N4-ciklobutil-2-(1H-pirazol-1-il)pirimidin-4,6-diamina 5-brom-6-(2-metilpirolidin-1-il)-2-(1H-pirazol-1-il)pirimidin-4-amina 5-brom-6-((R)-2-metilpirolidin-1-il)-2-(1H-pirazol-1-il)pirimidin-4-amina 1-[6-amino-5-brom-2-(1H-pirazol-1-il)pirimidin-4-il]azetidin-3-ola 1-[6-amino-5-brom-2-(1H-pirazol-1-il)pirimidin-4-il]pirolidin-3-ola 5-brom-6-((S)-3-fluoropirolidin-1-il)-2-(1H-pirazol-1-il)pirimidin-4-amina 5-brom-6-[(S)-3-(dimetilamino)pirolidin-1-il]-2-(1H-pirazol-1-il)pirimidin-4-amina 5-brom-6-(2,5-dimetilpirolidin-1-il)-2-(1H-pirazol-1-il)pirimidin-4-amina 5-brom-6-(3,3-difluoroazetidin-1-il)-2-(1H-pirazol-1-il)pirimidin-4-amina 5-brom-N4-izopropil-2-(1H-pirazol-1-il)pirimidin-4,6-diamina 5-brom-N4-propil-2-(1H-pirazol-1-il)pirimidin-4,6-diamina 5-brom-2-(1H-pirazol-1-il)pirimidin-4,6-diamina 5-hlor-2,6-di-(1H-pirazol-1-il)pirimidin-4-amina 4-amino-2,6-di-(1H-pirazol-1-il)pirimidin-5-karbonitrila 4-amino-6-N-ciklopentilamino-2-(1H-pirazol-1-il)pirimidin-5-karbonitrita N4-terc-butil-5-brom-2-(1H-pirazol-1-il)pirimidin-4,6-diamina 5-brom-2-(4-metil-1H-pirazol-1-il)-6-(1H-pirazol-1-il)pirimidin-4-amina 6-(azetidin-1-il)-5-brom-2-(4-metil-1H-pirazol-1-il)pirimidin-4-amina 5-brom-N4-ciklopentil-2-(4-metil-1H-pirazol-1-il)pirimidin-4,6-diamina 5-brom-N4-ciklopropil-2-(4-metil-1H-pirazol-1-il)pirimidin-4,6-diamina 5-brom-N4-ciklobutil-2-(4-metil-1H-pirazol-1-il)pirimidin-4,6-diamina 5-brom-2-(4-metil-1H-pirazol-1-il)-6-(2-metilpirolidin-1-il)pirimidin-4-amina 5-brom-2-(4-metil-1H-pirazol-1-il)-6-((R)-2-metilpirolidin-1-il)pirimidin-4-amina 5-brom-N-ciklopropil-2-(4-hlor-1H-pirazol-1-il)pirimidin-4,6-diamina 6-(azetidin-1-il)-5-brom-2-(4-hlor-1H-pirazol-1-il)pirimidin-4-amina 5-brom-2,6-di-(4-metil-1H-pirazol-1-il)pirimidin-4-amina 5-brom-2,6-di-(4-hlor-1H-pirazol-1-il)pirimidin-4-amina 5-brom-2,6-di-(3-metil-1H-pirazol-1-il)pirimidin-4-amina 5-brom-6-(3,5-dimetil-1H-pirazol-1-il)-2-(1H-pirazol-1-il)pirimidin-4-amina 5-brom-6-(1H-imidazol-1-il)-2-(1H-pirazol-1-il)pirimidin-4-amina 5-brom-6-(4-hlor-1H-pirazol-1-il)-2(1H-pirazol-1-il)pirimidin-4-amina 5-brom-2-(1H-pirazol-1-il)-6-(2H-1,2,3-triazol-2-il)pirimidin-4-amina 5-brom-2-(1H-pirazol-1-il)-6-(1H-1,2,4-triazol-1-il)pirimidin-4-amina 5-brom-6-izopropoksi-2-(1H-pirazol-1-il)pirimidin-4-amina 5-brom-2-(4-hlor-1H-pirazol-1-il)-6-(1H-pirazol-1-il)pirimidin-4-amina 5-brom-2-(4-hlor-1H-pirazol-1-il)-6-(4-metil-1H-pirazol-1-il)pirimidin-4-amina 5-brom-2-(3,5-dimetil-1H-pirazol-1-il)-6-(1H-pirazol-1-il)pirimidin-4-amina 5-brom-N4-ciklopentil-2-(3,5-dimetil-1H-pirazol-1-il)pirimidin-4,6-diamina 5-brom-2-(3,5-dimetil-1H-pirazol-1-il)-6-(pirolidin-1-il)pirimidin-4-amina 5-brom-N4-izopropil-2-(3,5-dimetil-1H-pirazol-1-il)pirimidin-4,6-diamina 5-brom-2,6-bis(3,5-dimetil-1H-pirazol-1-il)pirimidin-4-amina 5-Brom-2,6-di(tiazol-2-il)pirimidin-4-amina 5-Brom-2-(1H-pirazol-1-il)-6-(tiazol-2-il)pirimidin-4-amina 5-Brom-6-(1H-pirazol-1-il)-2-(tiazol-2-il)pirimidin-4-amina 5-brom-N4-[1-(dimetilamino)propan-2-il]-2-(1H-pirazol-1-il)pirimidin-4,6-diamina 5-brom-N4-(1-metoksipropan-2-il)-2-(1H-pirazol-1-il)pirimidin-4,6-diamina 5-brom-6-(1H-pirazol-1-il)-2-(2H-1,2,3-triazol-2-il)pirimidin-4-amina 5-brom-6-etoksi-2-(1H-pirazol-1-il)pirimidin-4-amina.
12. Jedinjenje prema bilo kojem od patentnih zahteva od 1 do 11 za primenu u lečenju patološkog stanja ili oboljenja koje je podložno ublaženju antagonizmom adenozinskog A2a receptora.
13. Jedinjenje prema patentnom zahtevu od 1 do 11 za primenu u lečenju patološkog stanja ili oboljenja gde je patološko stanje ili oboljenje ishemija, supraventrikularna aritmija, atrijalna fibrilacija, akutna bubrežna insuficijencija, miokardijalna reperfuziona povreda, oboljenja usled zadržavanja tečnosti, alergijske reakcije uključujući ali ne limitirajući se na rinitis, urtikariju, sklerodermu, artritis, druga autoimuna oboljenja, inflamatornu bolest creva, diabetes mellitus, gojaznost, Parkinsonovu bolest, Hantingtonovu bolest, distonije kao što su sindrom nemirnih nogu, diskinezije kao što su one izazvane produženom primenom dopamina ili neuroleptičkih lekova ili poremećajima spavanja, kongestivnom srčanom insuficijencijom, hipertenzijom, intradilatacijskom hipotenzijom, demencijom, anksioznim poremećajima i glaukomom.
14. Jedinjenje prema patentnom zahtevu 13 za primenu u lečenju patološkog stanja ili oboljenja gde su patološka stanja ili oboljenja aritmije, atrijalna fibrilacija, Parkinsonova bolest, Hantingtonova bolest, Alchajmerova bolest, distonije kao što su sindrom nemirnih nogu, diskinezije kao što su one izazvane produženom primenom dopamina ili neuroleptičkih lekova ili poremećajima spavanja, demencijom, anksioznim poremećajima i diabetes mellitus-om.
15. Farmaceutska kompozicija koja sadrži jedinjenje koje je definisano u bilo kom od patentnih zahteva od 1 do 11 pomešana sa farmaceutski prihvatljivim rastvaračem ili nosačem.
16. Kombinovani proizvod koji sadrži jedinjenje prema bilo kom od patentnih zahteva od 1 do 11 i još jedno jedinjenje za lečenje oboljenja kao što su ishemija, supraventrikularna aritmija, atrijalna fibrilacija, akutna bubrežna insuficijencija, miokardijalna reperfuziona povreda, oboljenja usled zadržavanja tečnosti, alergijske reakcije uključujući ali ne limitirajući se na rinitis, urtikariju, sklerodermu, artritis, druga autoimuna oboljenja, inflamatornu bolest creva, diabetes mellitus, gojaznost, Parkinsonovu bolest, Hantingtonovu bolest, Alchajmerovu bolest, distonije kao što su sindrom nemirnih nogu, diskinezije kao što su one izazvane produženom primenom dopamina ili neuroleptičkih lekova ili poremećajima spavanja, kongestivnom srčanom insuficijencijom, hipertenzijom, intradilatacijskom hipotenzijom, demencijom, anksioznim poremećajima i diabetes mellitus-om, za istovremenu, odvojenu ili sekvencijalnu primenu.
17. Kombinovani proizvod koji sadrži jedinjenje prema bilo kom od patentnih zahteva od 1 do 11 sa levodopom, agonistima dopamina, MAO-B inhibitorima, inhibitorima acetilholin esteraze ili bilo kojim lekom koji se koristi za lečenje Parkinsonove bolesti, Hantingtonove bolesti i Alchajmerove bolesti.
18. Kombinovani proizvod koji sadrži jedinjenje prema bilo kom od patentnih zahteva od 1 do 11 sa insulinom, metforminom, GLP-agonistima, sulfonilureama, DPP-IV inhibitorima ili bilo kojim lekom koji se koristi za lečenje dijabetesa.
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