LV12457B - Acil-piperazinil-pirimidīnu atvasinājumi, to iegūšana un izmantošana par medikamentiem - Google Patents

Acil-piperazinil-pirimidīnu atvasinājumi, to iegūšana un izmantošana par medikamentiem Download PDF

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LV12457B
LV12457B LVP-00-08A LV000008A LV12457B LV 12457 B LV12457 B LV 12457B LV 000008 A LV000008 A LV 000008A LV 12457 B LV12457 B LV 12457B
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piperazinyl
methoxypyrimidine
methoxy
pyrimidine
hydrochloride
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LV12457A (lv
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Jordi Corbera Arjona
David VA�O DOMENECH
Jordi Frigola Constansa
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Laboratorios Del Dr. Esteve, S.A.
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Claims (18)

  1. LV 12457 IZGUDROJUMA FORMULA 1. Acil-piperazinil-pirimidīna atvasinājumi ar vispārīgo formulu (I),
    X 2 (I) kur X ir skābekļa atoms vai sēra atoms; Rļ ir CM alkoksigrupa vai trifluormetilgrupa; R2 ir Cļ.6 alkilgrupa; C3.6 piesātināta cikloalkilgrupa; heterocikloalkilgrupa, kas sastāv no gredzena ar 3 līdz 6 atomiem, kurā heteroatoms ir izvēlēts no atomu rindas: skābeklis, sērs vai slāpeklis, neobligāti N-aizvietota ar C,-C6 alkilgrupu; fenilgrupa, kas neobligāti aizvietota ar 1, 2 vai 3 vienādiem vai dažādiem aizvietotājiem, kas izvēlēti no rindas: fluora atoms, hlora atoms, broma atoms, aminogrupa, acetamīdgrupa, nitrogrupa, metilgrupa, trifluormetilgrupa un metoksigrupa; arilakilgrupa, kas sastāv no cU3 alkilgrupas, kas aizvietota ar fenilgrupu, kura ir neobligāti aizvietota ar 1,2 vai 3 vienādiem vai dažādiem aizvietotājiem, kas izvēlēti no rindas: fluora atoms, hlora atoms, broma atoms, aminogrupa, acetamīdgrupa, nitrogrupa, metilgrupa, trifluormetilgrupa un metoksigrupa; heteroarilgrupa, kas sastāv no neobligāti aizvietota 5-locek|u vai 6-locek|u gredzena ar heteroatomiem, vai no neobligāti aizvietotām sapludinātām 9- līdz 10-locekju heteroaromātiskām sistēmām, kas satur 1 vai 2 heteroatomus, kas izvēlēti no rindas: skābeklis, sērs un slāpeklis, izvēloties augšminētos aizvietotājus no rindas: fluora atoms, hlora atoms, broma atoms, aminogrupa, acetamīdgrupa, nitrogrupa, metilgrupa, trifluormetilgrupa un metoksigrupa; un heteroarilalkilgrupa, kas sastāv no alkilgrupas ar 1 līdz 3 oglekļa atomiem, kas aizvietota ar heteroarilgrupu, kas sastāv no neobligāti aizvietota 5- vai 6-locekļu heteroaromātiska gredzena, vai no sapludinātām 9- līdz 10-locekļu heteroaromātiskām sistēmām, kas ir neobligāti aizvietotas ar 1 vai 2 2 heteroatomiem, kas izvēlēti no rindas: skābeklis, sērs un slāpeklis, izvēloties augšminētos aizvietotājus no rindas: fluora atoms, hlora atoms, broma atoms, aminogrupa, acetamīdgrupa, nitrogrupa, metilgrupa, trifluormetilgrupa un metoksigrupa; 5 un to fizioloģiski saderīgi sāļi.
  2. 2. Savienojums saskaņā ar 1. punktu, kurā R, ir metoksigrupa, etoksigrupa, propoksigrupa, izopropoksigrupa, butoksigrupa, sec-butoksigrupa vai ferc-butoksigrupa. 10
  3. 3. Savienojums saskaņā ar 1. punktu, kurā Rz ir metilgrupa, etilgrupa, propilgrupa, izopropilgrupa, butilgrupa, izobutilgrupa, sec-butilgrupa, terc-butilgrupa, pentilgrupa, izopentilgrupa, neopentilgrupa vai heksilgrupa.
  4. 4. Savienojums saskaņā ar 1. punktu, kurā R2 ir ciklopropilgrupa, ciklobutilgrupa, ciklopentilgrupa vai cikloheksilgrupa.
  5. 5. Savienojums saskaņā ar 1. punktu, kurā Ra ir 2-aziridinilgrupa, 2-tetrahidrofurilgrupa, 3-tetrahidrofurilgrupa, 2-tetrahidrotienilgrupa, 3- 20 tetrahidrotienilgrupa, 2-azetidinilgrupa, 2-pirolidinilgrupa, 3-pirolidinilgrupa, 2- piperidinilgrupa, 3-piperidinilgrupa vai 4-piperidinilgrupa.
  6. 6. Savienojums saskaņā ar 1. punktu, kurā R2 ir 2-fluorfenilgrupa, 3-fluorfenilgrupa, 4-fluorfenilgrupa, 2-hlorfenilgrupa, 3-hlorfenilgrupa, 4- 25 hlorfenilgrupa, 2-bromfenilgrupa, 3-bromfenilgrupa, 4-bromfenilgrupa, 2- aminofenilgrupa, 3-aminofenilgrupa, 4-aminofenilgrupa, 2-nitrofenilgrupa, 3-nitrofenilgrupa, 4-nitrofenilgrupa, 2-acetamīdfenilgrupa, 3-acetamīdfenilgrupa, 4-acetamīdfenilgrupa, 2-metilfenilgrupa, 3-metilfenilgrupa, 4-metiIfenilgrupa, 2-(trifluormetil)fenilgrupa, 3-(trifluormetil)fenilgrupa, 4-{trifluormetil)fenilgrupa, 30 2-metoksifenilgrupa, 3-metoksifenilgrupa, 4-metoksifenilgrupa, 2,3- difluorfenilgrupa, 3,4-difluorfenilgrupa, 2,4-difluorfenilgrupa, 2,3-dibromfenilgrupa, 3,4-dibromfenilgrupa, 2,4-dibromfenilgrupa, 2,3-dimetilfenilgrupa, 3,4-dimetilfenilgrupa, 2,4-dimetilfenilgrupa, 2,3-dimetoksifenilgrupa, 3,4-dimetoksifenilgrupa, 2,4-dimetoksifenilgrupa. 35 3 LV 12457
  7. 7. Savienojums saskaņā ar 1. punktu, kurā R2 ir pie aromātiskā gredzena neobligāti aizvietota fenilmetilgrupa, 1-feniletilgrupa, 2-feniletilgrupa, 3-fenilpropilgrupa.
  8. 8. Savienojums saskaņā ar 1. punktu, kurā R2 ir 2-furilgrupa, 3-furilgrupa, 2- tienilgrupa, 3-tienilgrupa, 3-metil-2-tienilgrupa, 5-metil-2-tienilgrupa, 3-metoksi-2-tienilgrupa, 3-hlor-2-tienilgrupa, 5-hlor-2-tienilgrupa, 2-pirolilgrupa, 3- pirolilgrupa, 2-piridilgrupa, 3-piridilgrupa, 4-piridilgrupa, 2-indolilgrupa, 3-indolilgrupa, 2-benzo[b]tienilgrupa, 3-benzo[b]tienilgrupa, 3-hlor-2-benzo[b]tienilgrupa, pirazolilgrupa, imidazolilgrupa, pirimidinilgrupa, piridazinilgrupa, pirazinilgrupa, benzimidazolilgrupa, hinolilgrupa, oksazolilgrupa vai tiazolilgrupa.
  9. 9. Savienojums saskaņā ar 1. punktu, kurā R2 ir 2-tienilmetilgrupa, 2-benzo[b]tienilmetilgrupa vai 3-(4-hlorpirazolil)propilgrupa.
  10. 10. Savienojums saskaņā ar 1. punktu,kas izvēlēts no sekojošas grupas: 2-[4-(2-furilkarbonil)-1-piperazinil]-4-metoksipirimidīns, 2-[4-(2-furilkarbonil)-1-piperazinil]-4-metoksipirimidīna hidrohlonds, 4-metoksi-2-[4-(2-tienilkarbonil)-1-piperazinil]pirimidins, 4-metoksi-2-[4-(2-tienilkarbonil)-1-piperazinil]pirimicfina hidrohlonds, 2-(4-acetil-1-piperazinil)-4-metoksipirimidīns, 2-{4-[4-(4-hlorpirazolil)butanoil]-1-piperazinil}-4-metoksipirimidīns, 2-{4-[4-(4-hlorpirazolil)butanoil]-1 -piperazinil}-4-metoksipirimidina hidrohlonds, 2-(4-benzoil-1-piperazinil)-4-metoksipirimidins, 2-(4-ciklopropilkarbonil-1-piperazinil)-4-metoksipirimidins, 2-[4-(2-furilkarbonil)-1-piperazinil]-4-(trifluormetil)pirimidīns, 2-[4-(2-tienilkarbonil)-1-piperazinil]-4-(trifluormetil)pirimidīns, 4-metoksi-2-[4-(3-tienilkarbonil)-1-piperazinil]pirimidīns, 4-metoksi-2-[4-(3-tienilkarbonil)-1-piperazinil]pirimidīna hidrohlonds, 2-[4-(5-metil-2-tienilkarbonil)-1-piperazinil]-4-metoksipirimidīns, 2-[4-(5-metil-2-tienilkarbonil)-1-piperazinil]-4-metoksipirimidīna hidrohlonds, 4-metoksi-2-[4-(3-metoksi-2-tienilkarbonil)-1-piperazinil]pirimidins, 4-metoksi-2-[4-(3-metoksi-2-tienilkarbonil)-1-piperazinil]pirimidīna hidrohlonds, 2-[4-(2-benz[b]tienilkarbonil)-1-piperazinil]-4-metoksipirimidīns, 2-[4-(2-benz[b]tienilkarbonil)-1-piperazinil]-4-metoksipirimidīna hidrohlonds, 4 2-[4-(2-indolilkarbonil)-1-piperazinil]-4-metoksipirimidīns) 2-[4-(3-hlor-2-benzo[b]tienilkarbonil)-1-piperazinil]-4-metoksipirimidīns, 2-[4-(3-hlor-2-benzo[b]tienilkarbonil)-1-piperazinil]-4-metoksipirimidīna hidrohiorids, 4-metoksi-2-[4-(2-pirolilkarbonil)-1-piperazinil]pirimidīns, 4-metoksi-2-[4-(2-pirolilkarbonil)-1-piperazinil]pirimidīna hidrohiorids, 4-metoksi-2-[4-(2-tienilacetil)-1-piperazinil]pirimidīns, 4-metoksi-2-[4-(2-tienilacetil)-1-piperazinil]pirimidīna hidrohiorids, 2-[4-(3-metii-2-tienilkarbonil)-1-piperazinil]-4-metoksipirimidins, 2-[4-{3-metil-2-tieniikarbonil)-1-piperazinil]-4-metoksipirimidīna hidrohiorids, 2-[4-(3-hlor-2-tienilkarbonil)-1-piperazinil]-4-metoksipirimidīns, 2-[4-(3-hlor-2-tieniikarbonil)-1-piperazinil]-4-metoksipirimidina hidrohiorids, 2-[4-(3-indolilkarbonil)-1-piperazinil]-4-metoksipirimidins, 2-[4*(3-benzo[b]tienilacetil)-1-piperazinil]-4-metoksipirimidins, 2-[4-(5-hlor-2-tienilkarbonil)-1-piperazinil]-4-metoksipirimidīns, 2-[4-(5-hlor-2-tienilkarbonil)-1-piperazinil]-4-metoksipirimidīna hidrohiorids, 4-metoksi-2-[4-(4-hlorbenzoil)-1-piparazinil]-4-metoksipirimidins, 4-metoksi-2-[4-(4-hlorbenzoil)-1-piperazinil]-4-metoksipirimidina hidrohiorids, 2-[4-(4-fluorbenzoil)-1-piperazinil]-4-metoksipirimidīns, 2-[4-(4-fiuorbenzoil)-1-piperazinil]-4-metoksipirimidina hidrohiorids, 2-[4-(4-hlorbenzoil)-1-piperazinil]-4-metoksipirimidins, 2-[4-(4-hlorbenzoil)-1-piperazinil]-4-metoksipirimidina hidrohiorids, 4-metoksi-2-[4-(3-metoksibenzoil)-1-piperazinil]pirimidīns, 4-metoksi-2-[4-(3-metoksibenzoil)-1-piperazinil]pirimidina hidrohiorids, 2-[4-(3-fluorbenzoil)-1-piperazinil]-4-metoksipirimidins, 2-[4-(3-fluorbenzoil)-1-piperazinil]-4-metoksipirimidīna hidrohiorids, 2-[4-(3-hlorbenzoil)-1-piperazinil]-4-metoksipirimidīns, 2-[4-(3-hlorbenzoil)-1-piperazinil]-4-metoksipirimidīna hidrohiorids, 4-metoksi-2-[4-(2-metoksibenzoil)-1-piperazinil]pirimidīns, 4-metoksi-2-[4-(2-metoksibenzoil)-1-piperazinil]pirimidīna hidrohiorids, 2-[4-(2-fluorbenzoil)-1-piperazinil]-4-metoksipirimidīns, 2-[4-(2-fluorbenzoil)-1-piperazinil]-4-metoksipirimidina hidrohiorids, 2-[4-(2-hlorbenzoil)-1-piperazinil]-4-metoksipirimidins, 2-[4-(2-hlorbenzoil)-1-piperazinil]-4-metoksipirimidina hidrohiorids, 4-metoksi-2-[4-(2-tetrahidrofūrilkarbonil)-1-piperazinil]pirimidins, 4-metoksi-2-(4-tiobenzoiM-piperazinil)pirimidīns, 4-metoksi-2-[4-(2-tetrahidrofuriIkarbonil)-1-piperazinil]pirimidīna hidrohiorids, 5 LV 12457 4-metoksi-2-(4-tiobenzoil-1-piperazinil)pirimidina hidrohlorids, 2-(4-benzoil-1-piperazinil)-4-metoksipirimidīns, 4-metoksi-2-{4-[4-(trifluormetil)benzoil]-1-piperazinil}pirimidīns, 4-metoksi-2-{4-[4-(trifluormetil)benzoil]-1-piperazinil}pirimidina hidrohlorids, 4-metoksi-2-{4-[3-(trifluormetil)benzoil]-1-piperazinil}pirimidins, 4-metoksi-2-{4-[3-(trifluormetil)benzoil]-1-piperazinil}pirimidīna hidrohlorids, 4-metoksi-2-{4-[2-(trifluormetil)benzoil]-1-piperazinil}pirimidīns, 4-metoksi-2-{4-[2-(trifluormetil)benzoil]-1-piperazinil}pirimidīna hidrohlorids, 4-metoksi-2-(4-nikotinoil-1-piperazinil)pirimidīns, 4-metoksi-2-(4-nikotinoil-1-piperazinil)pirimidīna dihidrohlorīds, 2-(4-izonikotinoiM-piperazinil)-4-metoksipirimidīns, 2-(4-izonikotinoil-1-piperazinil)-4-metoksipirimidīna dihidrohlorīds, 2-[4-(1 -imidazolilkarbonil)-1 -piperazinilļ-4-metoksipirimidīns, 2-[4-(1 -imidazolilkarbonil)-1 -piperazinil]-4-metoksipirimidīna hidrohlorids, 2-{4-nikotinoiM-piperazinil)-4-(trifluormetil)pirimidīns, 2-(4-nikotinoil-1-piperazinil)-4-(trifluormetil)pirimidina hidrohlorids, 4-metoksi-2-[4-(2-piridilkarbonil)-1-piperazinil]pirimidins, 4-metoksi-2-[4-(2-piridilkarbonil)-1-piperazinil]pirimidīna dihidrohlorids, 4-etoksi-2-[4-(2-tienilkarbonil)-1-piperazinil]pirimidīns, 4-etoksi-2-[4-(2-tienilkarbonil)-1-piperazinil]pirimidīna hidrohlorids, 2-[4-(3-hlor-2-tienilkarbonil)-1-piperazinil]-4-etoksipirimidins, 2-[4-(3-hlor-2-tienilkarbonil)-1-piperazinil]-4-etoksipirimidina hidrohlorids, 4-etoksi-2-{4-[2'(trifluormetil)benzoil]-1-piperazinil}pirimidīns, 4-etoksi-2-{4-[2-(trifluormetil)benzoil]-1-piperazinil}pirimidīna hidrohlorids, 2-[4-(2-metilbenzoil)-1-piperazinil]-4-metoksipirimidins, 2-[4-(2-metilbenzoil)-1-piperazinil]-4-metoksipirimidīna hidrohlorids, 2-[4-(4-fluorbenzoil)-1-piperazinil]-4-izopropoksipirimidīns, 2-[4-(4-fluorbenzoil)-1-piperazinil]-4-izopropoksipirimidīna hidrohlorids, 4-izopropoksi-2-{4-[2-(trifluormetil)benzoil]-1-piperazinil}pirimidīns, 4-izopropoksi-2-{4-[2-(trifluormetil)benzoil]-1-piperazinil}pirimidīna hidrohlorids, 2-[4-(3-hlor-2-tienilkarbonil)-1-piperazinil]-4-izopropoksipirimidīns, 2-[4-{3-hlor-2-tienilkarbonil)-1-piperazinil]-4-izopropoksipirimidīna hidrohlorids, 2-[4-(cikloheksilkarbonil)-1-piperazinil]-4-metoksipirimidīns, 2-[4-(cikloheksilkarbonil)-1-piperazinil]-4-metoksipirimidīna hidrohlorids, 4-etoksi-2-[4-(4-fluorbenzoil)-1-piperazinil]pirimidīns, 4-etoksi-2-[4-(4-fluorbenzoil)-1-piperazinil]pirimidina hidrohlorids, 2-[4-(2-tiazolilkarbonil)-1-piperazinil]-4-metoksipirimidms, 6 • 2-[4-(2-aminobenzoil)-1 -piperazinil]-4-metoksipirimidins, • 2-[4-(2-aminobenzoil)-1 -piperazinil]-4-metoksipirimidīna hidrohlorids, • 2-[4-(3-fluor-2-tienilkarbonil)-1-piperazinil]-4-metoksipmmidīns, • 2-[4-(3-fluor-2-tienilkarbonii)-1 -piperazinil]-4-metoksipirimidīna hidrohlorids, • 2-[4-(4-metoksi-2-pirimidinil)-1-piperazinilkarbonil]benzoskābe, • 2-[4-(2-acetoksibenzoil)-1-piperazinil]-4-metoksipirimidīns, • 2-[4-(2-hidroksibenzoil)-1 -piperazinil]-4-metoksipirimiclīns, • nātrija 2-[4-(4-metoksi-2-pirimidinil)-1 -piperazinilkarbonilļbenzoāts, • 2-[4-(2-hidroksibenzoil)-1 -piperazinil]-4-metoksipirimidina hidrohlorids, • 4-metoksi-2-[4-(2-metok$ibenzoil)-1 -piperazinil]-4-metoksipirimidīns, un • 4-etoksi-2-[4-(2-piridilkarbonil)-1 -piperaziniljpirimidins.
    N
  11. 11. Metode savienojuma ar vispārīgo formulu (I), kurā X saskaņā ar 1. punktu apzīmē skābekļa atomu, iegūšanai, kas ietver hlorpirimidīna atvasinājuma ar formulu (III), (III) kur R, ir 1. punktā noteiktā nozīme, pakļaušanu reakcijai ar piperizīna atvasinājumu ar vispārīgo formulu (IV),
    (IV) kur R2 ir 1. punktā noteikta nozīme un X apzīmē skābekļa atomu.
  12. 12. Metode savienojuma ar vispārīgo formulu (I), kurā X saskaņā ar 1. punktu apzīmē skābekļa atomu, iegūšanai, kas ietver amīna ar formulu (V), R
    N kur R, ir 1. punktā noteiktā nozīme, 7 LV 12457 pakļaušanu reakcijai ar karboksilskābi ar formulu R2COOH (VI) vai ar minētās skābes sāli, kur R2 ir 1. punktā noteiktā nozīme.
  13. 13. Metode savienojuma ar vispārīgo formulu (I), kurā X saskaņā ar 1. punktu apzīmē skābekļa atomu, iegūšanai, kas ietver amīna ar formulu (V),
    kur R, ir 1. punktā noteiktā nozīme, pakļaušanu reakcijai ar atvasinājuma reaģentu R2COY (VII), kurā R2 ir 1. punktā noteiktā nozīme un Y apzīmē halogēna atomu, azīdgrupu, 1-imidazolilgrupu, grupu 0-C0-R4, kur R4 apzīmē alkilgrupu ar 1 līdz 6 oglekļa atomiem vai ar vienu vai vairākiem halogēna atomiem neobligāti aizvietotu arilgrupu, vai grupu 01¾. kur R5 apzīmē aromātisku grupu ar vienu vai diviem gredzeniem, kas aizvietota ar vienu vai vairākiem halogēna atomiem, vai nitrogrupu, vai N-sukcīnimīdgrupu.
  14. 14. Metode savienojuma ar vispārīgo formulu (I), kurā X saskaņā ar 1. punktu apzīmē sēra atomu, iegūšanai, kas ietver savienojuma ar vispārīgo formulu (I), kurā X apzīmē skābekļa atomu, pakļaušanu reakcijai ar Lavesona (Lavvesson) reaģentu (2,4-bis(4-metoksifenil)-1,3,2,4-ditiadifosfetān-2,4-disulfīdu), vai ar fosfora pentasulfīdu.
  15. 15. Metode savienojumu ar vispārīgo formulu (I) saskaņā ar 1. punktu fizioloģiski saderīgu sāļu iegūšanai, kas ietver savienojuma ar vispārīgo formulu (I) pakļaušanu reakcijai ar neorganisku skābi vai organisku skābi atbilstošā šķīdinātājā.
  16. 16. Farmaceitiska kompozīcija, kas raksturīga ar to, ka tā papildus farmaceitiski pieņemamam nesējam satur vismaz vienu savienojumu ar vispārīgo formulu (I) vai kādu tā fizioloģiski saderīgu sāli saskaņā ar 1.-10. punktiem.
  17. 17. Savienojumu ar vispārīgo formulu (I) vai to farmaceitiski pieņemamu sāļu saskaņā ar jebkuru no 1.-10. punktiem izmantošana medikamenta ar aktivitāti zīdītāju, ieskaitot cilvēku, centrālajā nervu sistēmā ražošanai. 8
  18. 18. Savienojumu ar vispārīgo formulu (I) vai to farmaceitiski pieņemamu sāļu saskaņā ar jebkuru no 1.Ί0. punktiem izmantošana medikamenta ar sedatīvu, pretkrampju, analgezējošu, miotonolītisku, pretklepus, anksiolītisku, antipsihotisku, antidepresīvu, anticerebroišēmisku, pretmigrēnas aktivitāti ražošanai, 5 medikamenta ražošanai miega traucējumu, nelrodeģeneratīvo slimību, izziņas spējas traucējumu un Alcheimera slimības ārstēšanai, iemigšanu veicinošu vai vispārējās anestēzijas līdzekļu ražošanai zīdītājiem, ieskaitot cilvēku.
LVP-00-08A 1997-07-21 2000-01-21 Acil-piperazinil-pirimidīnu atvasinājumi, to iegūšana un izmantošana par medikamentiem LV12457B (lv)

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