RS51861B2 - Heterociklični inhibitori mek-a - Google Patents

Heterociklični inhibitori mek-a

Info

Publication number
RS51861B2
RS51861B2 RS20110131A RSP20110131A RS51861B2 RS 51861 B2 RS51861 B2 RS 51861B2 RS 20110131 A RS20110131 A RS 20110131A RS P20110131 A RSP20110131 A RS P20110131A RS 51861 B2 RS51861 B2 RS 51861B2
Authority
RS
Serbia
Prior art keywords
alkyl
halogen
heteroaryl
aryl
cycloalkyl
Prior art date
Application number
RS20110131A
Other languages
English (en)
Inventor
Allison L Marlow
Eli Wallace
Jeongbeob Seo
Joseph P Lyssikatos
Hong Woon Yang
Jim Blake
Original Assignee
Array Biopharma Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Array Biopharma Inc filed Critical Array Biopharma Inc
Publication of RS51861B2 publication Critical patent/RS51861B2/sr

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    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/44—Iso-indoles; Hydrogenated iso-indoles
    • C07D209/46—Iso-indoles; Hydrogenated iso-indoles with an oxygen atom in position 1
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    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
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    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
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    • C07D471/02—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 two hetero rings
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Claims (29)

  1. Patentni Zahtevi 1. Jedinjenje, uključujući njegove razdvojene enantiomere, diastereomere i farmaceutski prihvatljive soli, koje ima formulu:
    gde X j e N i l i CR<10>; R<1>, R<2>, R<8>, R<9>i R<10>su nezavisno vodonik, halogen, cijano, nitro, trifluorometil, difluorometil, fluorometil, fluorometoksi, difluorometoksi, triftuorometoksi, azido, -SR", - OR<3>, -C(O)R<3>, -C(O)OR<3>, -NR<4>C(O)OR<6>, -OC(O)R<3>,-NR<4>SO2R<8>, -SO2NR<3>R<4>, -NR<4>C(O)R<3>, -C(O)NR<3>R<4>, -NR<5>C(O)NR<3>R<4>,-NR<5>C(NCN)NR3<R>4, -NR<3>R<4>, C1-C10 alkil C2-C10 alkenil, C2-C10 alkinil, C3-cikloalkil, C3- C10 cikloalkilalkil, -S(O)j(C1C6 alkil), -S(O)j(CR<4>R<5>)m-aril, aril, arilalkil, heteroaril, heteroarilalkil, heterociklil, heterociklilalkil, -O(CR<4>R<5>)m-aril, -Nr<4>(CR<4>R<5>)m-aril, - O(CR<4>R<5>)m-heteroariI, -NR<4>(CR<4>R<5>)m-heteroaril, -O(CR<4>R<5>)m-heterociklil ili - NR<4>(CR<4>R<5>)m-heterocikIiI, pri čemu bilo koji od navedenih alkil, alkenil, alkinil, cikloalkil, aril, arilalkil, heteroaril, heteroarilalkil, heterociklil i heterociklilalkil delova je po izboru supstituisan sa jednom ili više grupa nezavisno izabranih od okso (uz uslov da on nije supstituisan na arilu ili heteroarilu), halogena, cijano, nitro, trifluorometil, difluorometoksi, trifluorometoksi, azido, -NR<4>SO2R<6>, - SO2NR<3>R<4>; -C(O)R<3>, -C(O)OR<3>, -OC(O)R<3>, - NR<4>C(O)OR<6>, NR<4>C(O)R<3>, - C(O)NR<3>R<4>, -NR<3>R<4>, -NR<5>C(O)NR<3>R<4>, -NR<5>C(NCN)NR<3>R<4>, - OR<3>, aril, heteroaril, arilalkil, heteroarilalkil, heterociklil, i heterociklilalkil, i pri čemu navedeni aril, heteroaril, arilalkil, heteroarilalkil, heterociklil ili heterociklilalkil prstenovi mogu dodatno biti supstituisani sa jednom ili više grupa izabranih od halogena, hidroksil, cijano, nitro, azido, fluorometil, difluorometil, trifluorometil, C1-C4 alkil, C2-C4 alkenil, C2-C4 alkinil, C3-C6 cikloalkil, C3-C6 heterocikloalkil, NR<3>R<4>i OR<3>; R<7>je vodonik, trifluorometil, C1-C10 alkil, C2-C10 alkenil, C2-C10 alkinil, C3- C10 cikloalkil, C3-C10 cikloalkilalkil, aril, arilalkil, heteroaril, heteroarilalkil, heterociklil, ili heterociklilalkil, pri čemu bilo koji od navedenih alkil, alkenil, alkinil, cikloalkil, aril, arilalkil, heteroaril, heteroarilalkil, heterociklil i heterociklilalkil delova je po izboru supstituisan sa jednom ili više grupa nezavisno izabranih od okso (uz uslov da on nije supstituisan na arilu ili heteroarilu), halogena, cijano, nitro, trifluorometil, difluorometil, fluorometil, difluorometoksi, trifluorometoksi, azido, -NR<11>SO2R<14>, -SO2NR<11>R<12>, -C(O)R<11>, C(O)OR<11>, -OC(O)R<11>, -NR<11>C(O)OR<14>, -NR<11>C(O)R<12>, -C(O)NR<11>R<12>, -SR<11>, -S(O)R<14>, -SO2R<14>, -NR<11>R<12>, -NR<11>C(O)NR<12>R<13>,-NR<11>C(NCN)NR<12>R<13>, -OR<11>, C1-C10 alkil, C2-C10 alkenil, C2-C10 alkinil, C3-C10 cikloalkil, aril, heteroaril, arilalkil, heteroarilalkil, heterociklil, i heterociklilalkil, i pri čemu navedeni aril, heteroaril, arilalkil, heteroarilalkil, heterociklil ili heterociklilalkil prstenovi mogu dodatno biti supstituisani sa jednom ili više grupa izabranih od halogena, hidroksil, cijano, nitro, azido, fluorometil, difluorometil, trifluorometil, C1-C4 alkil, C2-C4 alkenil, C2-C4 alkinil, C3-C6 cikloalkil, C3-C6heterocikloalkil, NR<3>R<4>i OR<3>; R<3>je vodonik, trifluorometil, C1-C10 alkil, C2-C10 alkenil, C2-C10 alkinil, C3- C10 cikloalkil, C3-C10 cikloalkilalkil, aril, arilalkil, heteroaril, heteroarilalkil, heterociklil, heterociklilalkil, fosfata ili ostatka aminokiseline, pri čemu bilo koji od navedenih alkil, alkenil, alkinil, cikloalkil, aril, arilalkil, heteroaril, heteroarilalkil, heterociklil i heterociklilalkil delova je po izboru supstituisan sa jednom ili više grupa nezavisno izabranih od okso (uz uslov da on nije supstituisan na arilu ili heteroarilu), halogena, cijano, nitro, trifluorometil, difluorometoksi, trifluorometoksi, azido, -NR<11>SO2R<14>, -SO2NR<11>R<12>, -C(O)R<11>, C(O)OR<11>, - OC(O)R<11>, -NR<11>C(O)OR<14>, - NR<11>C(O)R<12>, -C(O)NR<11>R<12>, -SR<11>, -S(O)R<14>, - SO2R<14>, -NR<11>R<12>, -NR<11>C(O)NR<12>R<13>, - NR<11>C(NCN)NR<12>R<13>, -OR<11>, aril, heteroaril, arilalkil, heteroarilalkil, heterociklil, i heterociklilalkil, ili R<3>i R<4>zajedno sa atomom za koji su vezani grade 4 do 10 člani karbociklični, heteroaril ili heterociklični prsten, pri čemu bilo koji od navedenih karbocikličnih, heteroaril ili heterocikličnih prstenova je po izboru supstituisan sa jednom ili više grupa nezavisno izabranih od halogena, cijano, nitro, trifluorometil, difluorometoksi, trifluorometoksi, azido, -NR<11>SO2R<14>, -SO2NR<11>R<12>, -C(O)R<11>, C(O)OR<11>, -OC(O)R<11>,-NR<11>C(O)OR<14>, -NR<11>C(O)R<12>, -C(O)NR<11>R<12>, -SR", -S(O)R<14>, -SO2R<14>, -NR<11>R<12>, -NR<11>C(O)NR<12>R<13>, -NR<11>C(NCN)NR<12>R<13>, -OR<11,>aril, heteroaril, arilalkil, heteroarilalkil, heterociklil, i heterociklilalkil; R<4>i R<5>nezavisno su vodonik ili C1-C6 alkil, ili R<4>i R<5>tzajedno sa atomom za koji su vezani grade 4 do 10 člani karbociklični, heteroaril ili heterociklični prsten, pri čemu bilo koji od navedenih karbocikličnih, heteroaril i heterocikličnih prstenova je po izboru supstituisan sa jednom ili više grupa nezavisno izabranih od halogena, cijano, nitro, trifluorometil, difluorometoksi, trifluorometoksi, azido, -NR<11>SO2R<14>, -SO2NR<11>R<12>, -C(O)R<11>, C(O)OR<11>, -OC(O)R<11>, - NR<11>C(O)OR<14>, -NR<11>C(O)R<12>, -C(O)NR<11>R<12>, -SR", - S(O)R<14>, -SO2R<14>, -NR<11>R<12>, - NR<1 1>C(O)NR<12>R<13>, -NR<11>C(NCN)NR<12>R<13>, -OR<11>, aril, heteroaril, arilalkil, heteroarilalkil, heterociklil, i heterociklilalkil; R<6>je trifluorometil, C1-C10 alkil, C3-C10 cikloalkil, aril, arilalkil, heteroaril, heteroarilalkil, heterociklil ili heterociklilalkil, pri čemu bilo koji od navedenih alkil, cikloalkil, aril, arilalkil, heteroaril, heteroarilalkil, heterociklil i heterociklilalkil delova je po izboru supstituisan sa jednom ili više grupa nezavisno izabranih od okso (uz uslov da on nije supstituisan na arilu ili heteroarilu), halogena, cijano, nitro, trifluorometil, difluorometoksi, trifluorometoksi, azido, -NR<11>SO2R<14>, - SO2NR<11>R<12>, -C(O)R<11>, C(O)OR<11>, -OC(O)R<11>, -NR<11>C(O)OR<14>, - NR<11>C(O)R<12>, - C(O)NR<11>R<12>, -SR<11>, -S(O)R<14>, -SO2R<14>, -NR<11>R<12>, -NR<11>C(O)NR<12>R<13>, - NR<11>C(NCN)NR<12>R<13>, -OR<11>, aril, heteroaril, arilalkil, heteroarilalkil, heterociklil, i heterociklilalkil; R<11>, R<12>i R<13>nezavisno su vodonik, C1-C10 alkil, C2-C10 alkenil, aril i arilalkil, i R<14>is C1-C10 alkil, C1-C10 alkenil, aril i arilalkil; ili bilo koja dva od R<11>, R<12>, R<13>ili R<14>zajedno sa atomom za koji su vezani grade 4 do 10 člani karbociklični, heteroaril ili heterociklični ring, pri čemu bilo koji od navedennih alkil, alkenil, aril, arilalkil karbocikličnih prstenova, heteroaril prstenova ili heterocikličnh prstenova je po izboru supstituisan sa jednom ili više grupa nezavisno izabranih od halogena, cijano, nitro, trifluorometil, difluorometoksi, trifluorometoksi, azido, aril, heteroaril, arilalkil, heteroarilalkil, heterociklil, i heterociklilalkil; W je heterociklil, -C(O)OR<3>, -C(O)NR<4>OR<3>, -C(O)NR<4>SO2R<3>, -C(O)(C3-C10 cikloalkil), -C(O)(C1-C10 alkil), -C(0)(aril), -C(0)(heteroaril), -C(O)(heterociklil) ili CR<3>OR<3>, pri čemu bilo koji od navedenih heterociklil, -C(O)OR<3>, -C(O)N<4>R<4>OR<3>, -C(O)NR<4>SO2R<3>, -C(O)(C3-C10 cikloalkil), -C(O)(C1-C10 alkil), - C(O)(aril), -C(O)(heteroaril), -C(O)(heterociklil) i CR<3>OR<3>je po izboru supstituisan sa jednom ili više grupa nezavisno izabranih od halogena, cijano, nitro, azido, - NR<3>R<4>, -OR<3>, C1-C10 alkil, C2-C10 alkenil, C2-C10 alkinil, cikloalkil i heterocikloalkil, pri čemu bilo koji od navedenih C1-C10 alkil, C2-C10 alkenil, C2-C10 alkinil, cikloalkil i heterocikloalkila je po izboru supstituisan sa 1 ili biše grupa nezavisno izabranih od -NR<3>R<4>i -OR<3>; uz uslov da kad X je CH, W ne može biti C(O)aril ili C(O)heteroaril, i dodatno uz uslov da kad X je CH, W je C(O)OR<3>i R<9>je F, R<7>ne može biti H; m je 0, 1,2,3,4 ili 5; i j je 0, 1 ili 2.
  2. 2. Jedinjenje prema zahtevu 1, naznačeno time, što X je OR<10>, i R<10>je vodonik, halogen, metil, fluorometil, difluorometil, fluormetil ili etil.
  3. 3. Jedinjenje prema zahtevu 2, naznačeno time, što R<9>je vodonik, halogen, metil, fluorometil, difluorometil, trifluorometil ili etil.
  4. 4. Jedinjenje prema zahtevu 3, naznačeno time, što W je izabran od C(O)OR<3>, C(O)NR<4>OR<3>i C(O)NR<4>S(O)2R<3>, pri čemu bilo koji od navedenih C(O)OR<3>, C(O)NR<4>OR<3>ili C (O) NR<4>S(O)2R<3>je po izboru supstituisan sa jednom ili više grupa izabranih od halogena, hidroksil, cijano, nitro, azido, fluorometil, difluorometil, trifluorometil, metoksi, fluorometoksi, difluorometoksi, trifluorometoksi, amino, aminometil, dimetilamino, aminoetil, dietilamino, etoksi, C1-C4 alkil, C2-C4 alkenil, C2-C4alkinil, C3-C6 cikloalkil i C3- C6 heterocikloalkil, pri čemu bilo koji od navedenih C1-C4 alkil, C2-C4 alkenil, C2-C4alkinil, cikloalkil ili heterocikloalkil može dodatno biti po izboru supstituisan sa jednom ili više grupa izabranih od NR<3>R<4>i OR<3>.
  5. 5. Jedinjenje prema zahtevu 3, pri čemu W je izabran od C(O)OR<3>; i C(O)NHOR<3>, pri čemu bilo koji od navedenih C(O)OR<3>, C(O)NHR<3>, i C(O)NHOR<3>je po izboru supstituisan sa jednom ili više grupa izabranih od halogena, hidroksil, cijano, nitro, azido, fluorometil, difluorometil, trifluorometil, metoksi, fluorometoksi, difluorometoksi, trifluorometoksi, amino, aminometil, dimetilamino, aminoetil, dietilamino, etoksi, C1-C4 alkil, C2-C4 alkenil, C2-C4 alkinil, C3-C6 cikloalkil i C3-C6 heterocikloalkil, pri čemu bilo koji od navedenih C1-C4 alkil, C2-C4 alkenil, C2-C4 alkinil, cikloalkil ili heterocikloalkila može dodatno biti po izboru supstituisan sa jednom ili više grupa izabranih od NR<3>R<4>i OR<3>; i R<3>je izabran od vodonika, C1-C4 alkil, C2-C4 alkenil, C2-C4 alkinil, C3-C6 cikloalkil i C3-C6heterocikloalkil, pri čemu bilo koji od navedenih C1-C4 alkil, C2-C4 alkenil, C2-C4 alkinil, cikloalkil ili heterocikloalkia je po izboru supstituisan sa jednom ili više grupa izabranih od NR<11>R<12>i OR<11>.
  6. 6. Jedinjenje prema zahtevu 4 , pri čemu R<7>je C1-C4 alkil, C2-C4 alkenil ili C2-C4 alkinil, pri čemu navedeni C1-C4alkil, C2-C4alkenil i C2-C4 alkinil mogu biti po izboru supstituisani sa jednom ili više grupa izabranih od halogena, hidroksil, cijano, nitro, azido, fluorometil, difluorometil, trifluorometil, metoksi, fluorometoksi, difluorometoksi, amino, aminometil, dimetilamino, aminoetil, dietilamino, etoksi, cikloalkil, heterocikioalkil, aril ili heteroaril, pri čemu navedeni cikloalkil, heterocikioalkil, aril ili heteroaril prstenovi mogi biti po izboru supstituisani sa jednom ili više grupa izabranih od halogena, hidroksil, cijano, nitro, azido, fluorometil, difluorometil, trifluorometil, C1-C4 alkil, C2-C4 alkenil, C2- C4 alkinil, C3-C6 cikloalkil, C3-C6 heterocikioalkil, NR<3>R<4>i OR<3>.
  7. 7. Jedinjenje prema zahtevu 5, naznačeno time, što R<7>je C1-C4 alkil, C2-C4 alkenil ili C2-C4 alkinil, pri čemu navedeni C1-C<4>alkil, C2-C4 alkenil i C1-C4 alkinil mogu biti po izboru supstituisani sa jednom ili više grupa izabranih od halogena, hidroksil, cijano, nitro, azido, fluorometil, difluorometil, trifluorometil, metoksi, fluorometoksi, difluorometoksi, amino, aminometil, dimetilamino, aminoetil, dietilamino, etoksi, cikloalkil, heterocikioalkil, aril ili heteroaril, pri čemu navedeni cikloalkil, heterocikioalkil, aril ili heteroaril prstenovi mogi biti po izboru supstituisani sa jednom ili vuše grupa izabranih od halogena, hidroksil, cijano, nitro, azido, fluorometil, difluorometil, trifluorometil, C1-C4 alkil, C2-C4 alkenil, C2-C4 alkinil, C3-C6 cikloalkil, C3-C6 heterocikioalkil, NR<3>R<4>i OR<3>.
  8. 8. Jedinjenje prema zahtevu 6 ili zahtevu 7, naznačeno time, što R<8>je halogen, hidroksil, cijano, nitro, azido, metil, fluorometil, difluorometil, trifluorometil, metoksi, fluorometoksi, difluorometoksi, trifluorometoksi, amino, aminometil, dimetilamino, aminoetil, dietilamino, etil, etoksi ili SR<11>.
  9. 9. Jedinjenje prema zahtevu 8, naznačeno time, što R<1>i R<2>su nezavisno vodonik, halogen, metil, fluorometil, difluorometil, trifluorometil ili etil.
  10. 10. Jedinjenje prema zahtevu 6, naznačeno time, što R<1>je halogen ili metil, R<2>je vodonik i R<8>je vodonik, halogen, metil, fluorometil, difluorometil, trifluorometil ili SR<11>.
  11. 11. Jedinjenje prema zahtevu 7, naznačeno time, što R<1>je halogen ili metil, R<2>je vodonik i R<8>je vodonik, halogen, metil, fluorometil, difluorometil, trifluorometil ili SR<11>.
  12. 12. Jedinjenje prema zahtevu 10, naznačeno time, što R<1>je halogen, R<3>je halogen, R<9>je alkil ili halogen, i R<2>se nalazi na položaju susednom -NH- grupi, i pri čemu R<2>je vodonik.
  13. 13. Jedinjenje prema zahtevu 11, naznačeno time, što R<1>je halogen, R<8>je halogen, R<9>je alkil ili halogen, i R<2>se nalazi na položaju susednom -NH- grupi, i pri čemu R<2>je vodonik.
  14. 14. Jedinjenje prema zahtevu 1, naznačeno time, što X je N.
  15. 15. Jedinjenje prema zahtevu 14, naznačeno time, što R<9>je vodonik, halogen, metil, fluorometil, difluorometil, trifluorometil ili etil.
  16. 16. Jedinjenje prema zahtevu 15, naznačeno time, što W je izabran od C(O)OR<3>i C(O)NHOR<3>, pri čemu bilo koji od navedenih C(O)OR<3>, i C(O)NHOR<3>je po izboru supstituisan sa jednom ili više grupa izabranih od halogena, hidroksil, cijano, nitro, azido, fluorometil, difluorometil, trifluorometil, metoksi, fluorometoksi, difluorometoksi, trifluorometoksi, amino, aminometil, dimetilamino, aminoetil, dietilamino, etoksi, C1-C4 alkil, C2-C4 alkenil, C2-C4 alkinil, C3-C6 cikloalkil i C3-C6 heterocikloalkil, pri čemu bilo koji od navedenih C1-C4 alkil, C2-C4 alkenil, C2-C4 alkinil, cikloalkil ili heterocikloalkil može dodatno biti po izboru supstituisan sa jednom ili više grupa izabranih od NR<3>R<4>i OR<3>; i R<3>je izabran od vodonika, C1-C4 alkil, C2-C4 alkenil, C2-C4 alkinil, C3-C6 cikloalkil i C3-C6heterocikloalkil, pri čemu bilo koji od navedenih C1-C4 alkil, C2-C4 alkenil, C2-C4 alkinil, cikloalkil ili heterocikloalkil je po izboru supstituisan sa jednom ili više grupa izabranih od NR<11>R<12>i OR<11>.
  17. 17. Jedinjenje prema zahtevu 16, naznačeno time, što R<7>je C1-C4 alkil, C2-C4 alkenil ili C2-C4 alkinil, pri čemu navedni C1C4alkil, C2-C4 alkenil i C2-C4 alkinil mogu biti po izboru supstituisani sa jednom ili više grupa izabranih od halogena, hidroksil, cijano, nitro, azido, fluorometil, difluorometil, trifluorometil, metoksi, fluorometoksi, difluorometoksi, amino, aminometil, dimetilamino, aminoetil, dietilamino, etoksi, cikloalkil, heterocikloalkil, aril ili heteroaril, pri čemu navedeni cikloalkil, heterocikloalkil, aril ili heteroaril prstenovi mogu biti po izboru supstituisani sa jednom ili više grupa izabranih od halogena, hidroksil, cijano, nitro, azido, fluorometil, difluorometil, trifluorometil, C1-C4 alkil, C2-C4 alkenil, C2-C4 alkinil, C3-C6 cikloalkil, C3-C6 heterocikloalkil, NR<3>R<4>i OR<3>.
  18. 18. Jedinjenje prema zahtevu 17, naznačeno time, što R<8>je halogen, hidroksil, cijano, nitro, azido, metil, fluorometil, difluorometil, trifluorometil, metoksi, fluorometoksi, difluorometoksi, trifluorometoksi, amino, aminometil, dimetilamino, aminoetil, dietilamino, etil, etoksi ili SR<11>.
  19. 19. Jedinjenje prema zahtevu 18, naznačeno time, što R<1>i R<2>su nezavisno vodonik, halogen, metil, fluorometil, difluorometil, trifluorometil ili etil.
  20. 20. Jedinjenje prema zahtevu 19, naznačeno time, što R<1>je halogen ili metil, R<2>je vodonik i R<8>je vodonik, halogen, metil, fluorometil, difluorometil, trifluorometil ili SR<11>.
  21. 21. Jedinjenje prema zahtevu 20, naznačeno time, što R<1>je halogen, R<8>je halogen, R<9>je alkil ili halogen, i R<2>se nalazi na položaju susednom -NH grupi, i pri čemu R<2>je vodonik.
  22. 22. Kompozicija, naznačena time što sadrži jedinjenje prema bilo kome od zahteva 1, 5, 7, 13 i 17, i farmaceutski prihvatljiv nosač.
  23. 23. Jedinjenje prema bilo kome od zahteva 1, 5, 7, 13 i 17, za upotrebu kao lek.
  24. 24. Jedinjenje prema bilo kome od zahteva 1, 5, 7, 13 i 17, za upoptrebu kao lek za lečenje hiperproliferativnog poremećaja ili inflamatornog stanja.
  25. 25. Upotreba jedinjenja prema bilo kome od zahteva 1 , 5 , 7, 13 i 17, u proizvodnji leka za lečenje hiperproliferativnog poremećaja ili inflamatornog stanja.
  26. 26. Metoda za dobijanje jedinjenja formule 56
    pri čemu R<1>, R<2>i R<9>su nezavisno vodonik, halogen, metil, fluorometil, difluorometil, trifluorometil ili etil; R<4>je vodonik ili C1-C6 alkil; R<3>je alkil, alkenil, alkinil, cikloalkil, heterocikloalkil, aril ili heteroaril, pri čemu navedeni alkil, alkenil, alkinil, cikloalkil, heterocikloalkil, aril ili heteroaril mogu biti po izboru supstituisani sa jednom ili više grupa izabranih od halogena, hidroksil, cijano, nitro, amino, azido, fluorometil, difluorometil, trifluorometil, metoksi, fluorometoksi, difluorometoksi, amino, aminometil, dimetilamino, aminoetil, dietilamino, etoksi, cikloalkil, heterocikloalkil, aril ili heteroaril; R<7>je alkil; i R<8>je halogen, hidroksil, cijano, nitro, azido, metil, fluorometil, difluorometil, trifluorometil, metoksi, fluorometoksi, difluorometoksi, trifluorometoksi, amino, aminometil, dimetilamino, aminoetil, dietilamino, SR<1>, etil ili etoksi, pri čemu navedena metoda sadrži: (a) reagovanje jedinjenja formule 53 ili 58
    sa alkil halidom i bazom, što je praćeno reagovanjem sa derivatom anilina da bi se dobilo jedinjenje formule 54
    i (b) (i) reagovanje jedinjenja formule 54 sa hidroksilaminom da bi se dobilo jedinjenje formule 56
    ili (ii) reagovanje jedinjenja formule 54 sa vodenim rastvorom baze da bi se dobilo jedinjenje formule 55
    pa zatim reagovanje jedinjenja formule 55 sa hidroksilaminom u prisustvu sredstva za kuplovanje da bi se dobilo jedinjenje formule 56.
  27. 27. Metoda za dobijanje jedinjenja formule 57
    pri čemu R<1>, R<2>i R<9>su nezavisno vodonik, halogen, metil, fluorometil, difluorometil, trifluorometil ili etil; R<4>je vodonik ili C1-C6 alkil; R<3>je alkil, alkenil, alkinil, cikloalkil, heterocikloalkil, aril ili heteroaril, pri čemu navedeni alkil, alkenil, alkinil, cikloalkil, heterocikloalkil, aril ili heteroaril mogu biti po izboru supstituisani sa jednim ili više grupa izabranih halogena, hidroksil, cijano, nitro, amino, azido, fluorometil, difluorometil, trifluorometil, metoksi, fluorometoksi, difluorometoksi, amino, aminometil, dimetilamino, aminoetil, dietilamino, etoksi, cikloalkil, heterocikloalkil, aril ili heteroaril; R<7>je alkil; i R<8>je halogen, hidroksil, cijano, nitro, azido, metil, fluorometil, difluorometil, trifluorometil, metoksi, fluorometoksi, difluorometoksi, trifluorometoksi, amino, aminometil, dimetilamino, aminoetil, dietilamino, SR<1>, etil ili etoksi; pri čemu navedena metoda sadrži: (a) reagovanje jedinjenja formule 53 ili 58
    sa alkil halidom i bazom, pa zatim reagovanje sa derivatom anilina da bi se dobilo jedinjenje formule 54
    (b) reagovanje jedinjenja formule 54 sa vodenimrastvorom baze da bi se dobilo jedinjenje formule 55
    i (c) reagovanje jedinjenja formule 55 sa aminom u prisustvu sredstva za kuplovanje da bi se dobilo jedinjenje formule 57.
  28. 28. Metoda za dobijanje jedinjenja formule 87
    pri čemu X je CH ili N; R<1>, R<2>i R<9>su nezavisno vodonik, halogen, metil, fluorometil, difluorometil, trifluorometil ili etil; R<7>je alkil; i R<8>je halogen, hidroksil, cijano, nitro, azido, metil, fluorometil, difluorometil, trifluorometil, metoksi, fluorometoksi, difluorometoksi, trifluorometoksi, amino, aminometil, dimetilamino, aminoetil, dietilamino, SR<1>, etil ili etoksi; pri čemu navedena metoda sadrži: (a) reagovanje jedinjenja formule 55 ili 62
    sa hidrazinom u prisustvu sredstva za kuplovanje da bi se dobilo jedinjenje formule 86<i>
    i (b) reagovanje jedinjenja formule 86 sa cijanogen bromidom da bi se dobilo jedinjenje formule 87.
  29. 29. Jedinjenje izabrano od sledećih Ciklopropilmetoksi-amid 2-(4-bromo-2-fluoro-fenilamino)-1-metil-6-okso-1,6-dihidro- piridin-3-karboksilne kiseline, (2-Hidroksi-etoksi)-amid 2-(4-bromo-2-fluoro-fenilamino)-1-metiI-6-okso-1,6-dihidro- piridin-3-karboksilne kiseline, (2-Hidroksi-etoksi)-amid 2-(4-bromo-2-fluoro-fenilamino)-5-fluoro-1 -metil-okso-1,6- dihidro-piridin-3-karboksilne kiseline, (2-Hidroksi-etoksi)-amid 2-(4-bromo-2-fluoro-fenilamino)-1 -etil-6-okso-1,6-dihidro-piridin- 3-karboksilne kiseline (2-Hidroksi-etoksi)-amid 2-(2-fluoro-4-metil-fenilamino)-1 -metil-6-okso-1,6-dihidro-piridin- 3-karboksilne kiseline, Metoksi-amid 2-(2-fluoro-4-iodo-fenilamino)-1 -metil-6-okso-1,6-dihidro-piridin-3-karboksilne kiseline.
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