ME02879B - Jedinjenja biciklične uree, tiouree, guanidina i cijanoguanidina korisna za lečenje bola - Google Patents

Jedinjenja biciklične uree, tiouree, guanidina i cijanoguanidina korisna za lečenje bola

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Publication number
ME02879B
ME02879B MEP-2017-14A MEP201714A ME02879B ME 02879 B ME02879 B ME 02879B ME P201714 A MEP201714 A ME P201714A ME 02879 B ME02879 B ME 02879B
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Montenegro
Prior art keywords
alkyl
alkoxy
continued
optionally substituted
compound
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MEP-2017-14A
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German (de)
English (en)
French (fr)
Inventor
Shelley Allen
Steven Wade Andrews
James F Blake
Barbara J Brandhuber
Julia Haas
Yutong Jiang
Timothy Kercher
Gabrielle R Kolakowski
Allen A Thomas
Shannon L Winski
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Array Biopharma Inc
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Publication of ME02879B publication Critical patent/ME02879B/me

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Claims (33)

1. Jedinjenje koje ima formulu I:ili njegovi stereoizomeri, tautomeri ili farmaceutski prihvatljive soli ili solvati, u kojima:X je O, S, NH ili N-CN;Prsten A je formula A-1 ili A-2Y je H, halogen, (1-3C alkoksi)(1-6C)alkil, (1-6C)alkil [izborno supstituisan sa 1-5 fluoro], cijano(1-6C)alkil, hidroksi(1-6C)alkil, dihidroksi(2-6C)alkil, aminokarbonil(1-6C)alkil, (1-6C)alkoksi [izborno supstituisan sa 1-5 fluoro], CN, aminokarbonil ili (1-4C alkoksi)karbonil;Ra, Rb i Rc su nezavisno izabrani od H, halogena, (1-3C)alkil, (1-3C)alkoksi i CN;B je NR1, O, veza, CRdRe, S ili SO2;D je NR1, O, veza, CRfRg, S ili SO2;E je NR1, O, veza ili CRhRi, S ili SO2;F je CRjRk;uz uslov da je prsten formiran pomoću B, D, E i F zajedno sa atomima za koje su vezani sadrži najmanje pet atoma i nula ili jedan od B, D ili E je NR1 ili O;G je CRmRn;K je NR1;R1 je (1-6C)alkil [izborno supstituisan sa jednim do pet fluoro], (1-6C)cikloalkil [izborno supstituisan sa jednim do pet fluoro], (1-3C alkoksi)(2-6C)alkil [izborno supstituisan sa jedan do pet fluoro], (1-6C)alkilC(=O)- ili (1-6C alkoksi)C=O-;Rd, Re, Rf, Rg, Rh, Ri, Rj i Rk su nezavisno H, OH, (1-6C)alkil [izborno supstituisan sa jednim do pet fluoro], (3-6C)cikloalkil [izborno supstituisan sa jednim do pet fluoro], (1-3C alkoksi)(2-6C)alkil [izborno supstituisan sa jednim do pet fluoro], hidroksi(2-6C)alkil [izborno supstituisan sa jednim do pet fluoro], (2-6C)cijanoalkil, (1-6C)alkoksi [izborno supstituisan sa jednim do pet fluoro] ili (1-3C alkoksi)(2-6C)alkoksi [izborno supstituisan sa jednim do pet fluoro] ili jedan od para Rd i Re, ili Rf i Rg ili Rh i Ri, ili Rj i Rk, zajedno sa atomom ugljenika za koji su vezani formiraju (3-6C)cikloalkil, oksetanil ili azetidinil prsten, ili jedan od para od Rd i Re, ili Rf i Rg, ili Rh i Ri, ili Rj i Rk formiraju okso grupu, i pri čemu samo jedan od Rd i Re može biti OH i nijedan nije OH ako je B vezan za heteroatom, i samo jedan od Rf i Rg može biti OH i nijedan nije OH ako je D vezan za heteroatom, i samo jedan od Rh i Ri može biti OH i nijedan nije OH ako je E vezan za heteroatom, i samo jedan od Rj i Rk može biti OH i nijedan nije OH ako je F vezan za heteroatom; Rm je H, (1-3C)alkil [izborno supstituisan sa 1-5 fluoro], ciklopropil ili ciklobutil, iRn je H ili (1-3C)alkil [izborno supstituisan sa 1-5 fluoro] ili Rm i Rn zajedno formiraju okso grupu;Rp je H, (1-6C)alkil [izborno supstituisan sa jednim do pet fluoro], (3-6C)cikloalkil [izborno supstituisan sa jednim do pet fluoro], (1-3C alkoksi)(2-6C)alkil [izborno supstituisan sa jednim do pet fluoro], hidroksi(2-6C)alkil [izborno supstituisan sa jednim do pet fluoro] ili (2-6C)cijanoalkil;Prsten C je formula C-1R3 je (1-6C)alkil, hidroksi(1-6C)alkil, Ar2, hetCyc1, (3-7C)cikloalkil ili hetAr2;Ar2 je fenil izborno supstituisan sa jednom ili više grupa nezavisno izabranih od halogena i (1-6C)alkil;hetCyc1 je 5-6-člani zasićeni ili delimično nezasićeni heterociklični prsten koji ima 1-2 heteroatoma u prstenu nezavisno izabrana od N i O;hetAr2 je 5-6 člani heteroaril prsten koji ima 1-3 heteroatoma u prstenu nezavisno izabrana od N, O i S and izborno supstituisan sa jednom ili više grupa nezavisno izabranih od (1-6C)alkil i halogena;R4 je OH, (1-6C)alkil, monofluoro(1-6C)alkil, difluoro(1-6C)alkil, trifluoro(1-6C)alkil, tetrafluro(2-6C)alkil, pentafluro(2-6C)alkil, cijano(1-6C)alkil, hidroksi(1-6C)alkil, dihidroksi(2-6C)alkil, (1-3C alkoksi)(1-6C)alkil, amino(1-6C)alkil, aminokarbonil(1-6C)alkil, (1-3C)alkilsulfonamido(1-6C)alkil, sulfamido(1-6C)alkil, hidroksikarbonil(1-6C)alkil, hetAr3(1-6C)alkil, Ar3(1-6C)alkil, (1-6C)alkoksi, monofluoro(1-6C)alkoksi, difluoro(1-6C)alkoksi, trifluoro(1-6C)alkoksi, tetrafluoro(2-6C)alkoksi, pentafluoro(2-6C)alkoksi, cijano(1-6C)alkoksi, hidroksi(1-6C)alkoksi, dihidroksi(2-6C)alkoksi, amino(2-6C)alkoksi, hidroksil-karbonil(1-6C)alkoksi, hetCyc2(1-6C)alkoksi, hetAr3(1-6C)alkoksi, Ar3(1-6C)alkoksi, (1-4C alkoksi)(1-6C)alkoksi, (1-3C alkilsulfonil)(1-6C)alkoksi, (3-6C)cikloalkil [izborno supstituisan sa F, OH, (1-6C alkil), (1-6C) alkoksi ili (1-3Calkoksi)(1-6C)alkil], hetAr4, hetAr4-O-, Ar4, hetCyc2(O)CH2-, (1-4C alkoksikarbonil)(1-6C)alkoksi, hidroksikarbonil(1-6C)alkoksi, aminokarbonil(1-6C)alkoksi, hetCyc2C(=O)(1-6C)alkoksi, hidroksi(1-3C alkoksi)(1-6C)alkoksi, hidroksitrifluoro(1-6C)alkoksi, (1-3C)alkilsulfonamido(1-6C)alkoksi, (1-3C)alkilamido(1-6C)alkoksi, di(1-3Calkil)amino-karboksi, hetCyc2C(=O)O-, hidroksidifluoro(1-6C)alkil, (1-4C alkilkarboksi)(1-6C)alkil, (1-6C)alkoksikarbonil, hidroksilkarbonil, aminokarbonil, (1-3C alkoksi)aminokarbonil, hetCyc3, halogen, CN, trifluorometilsulfonil, N-(1-3C alkil)oksadiazolonil, hetAr5 ili hetCyc4-O-;hetCyc2 je 4-6 –člani heterociklični prsten koji ima 1-2 heteroatoma u prstenu nezavisno izabrana od N i O i izborno supstituisana sa 1-2 grupe nezavisno izabrane od (1-6C)alkil, (1-4C alkilkarboksi)(1-6C)alkil i (1-6C)acil;hetCyc3 je 4-7 –člani heterociklus koji ima 1-2 heteroatoma u prstenu nezavisno izabrana od N i O i izborno supstituisan sa jednim ili više supstituenata nezavisno izabranih od F, CN, (1-6C)alkil, trifluoro(1-6C)alkil, hidroksi(1-6C)alkil, (1-3C alkoksi)(1-6C)alkil, (1-6C)acil-, (1-6C)alkilsulfonil, trifluorometilsulfonil i (1-4C alkoksi)karbonil;hetAr3 je 5-člani heteroaril prsten koji ima 1-3 atoma u prstenu nezavisno izabrana od N, O i S i izborno supstituisan sa (1-6C)alkil;Ar3 je fenil izborno supstituisan sa (1-4C)alkoksi;hetAr4 je 5-6 –člani heteroaril prsten koji ima 1-3 heteroatoma u prstenu nezavisno izabrana od N, S i O i izborno supstituisan sa jednim ili više supstituenata nezavisno izabranih od (1-6C)alkil, halogena, CN, hidroksi(1-6C)alkil, trifluoro(1-6C)alkil, difluoro(1-6C)alkil, fluoro(1-6C)alkil, (3-6C)cikloalkil, (3-6C cikloalkil)CH2- (3-6C cikloalkil)C(=O)-, (1-3C alkoksi)(1-6C)alkil, (1-6C)alkoksi, (1-6C)alkilsulfonil, NH2, (1-6Calkil)amino, di(1-6C alkil)amino, (1-3C trifluoroalkoksi), fluoro(1-6C alkil)amino, difluoro(1-6C alkil)amino, trifluoro(1-6C alkil)amino i (3-4C cikloalkil)amino;hetAr5 je grupa izabrana od struktura:gde je Rz jednak (3-4C)cikloalkil ili (1-3C)alkil (izborno supstituisan sa 1-3 fluoro), gde je svaka od navedenih hetAr5 grupa izborno dalje supstituisana sa jednom ili više grupa nezavisno izabranih od F i (1-3C)alkila izborno supstituisanog sa 1-3 fluoro;hetCyc4 je 7-8 člani premošćeni heterociklus koji ima atom azota u prstenu i izborno supstituisan sa jednim ili više grupa nezavisno izabranih od (1-6C)alkila i halogena;Ar4 je fenil izborno supstituisan sa jednom ili više grupa nezavisno izabranih od (1-6C)alkila, halogena, CN, CF3, CF3O-, (1-6C)alkoksi, (1-6Calkil)OC(=O)-, aminokarbonila, (1-6C)alkiltio, hidroksi(1-6C)alkil, (1-6Calkil)SO2-, HOC(=O)- i (1-3C alkoksi)(1-3C alkil)OC(=O)-; iR5 je (1-6C)alkil, monofluoro(1-6C)alkil, difluoro(1-6C)alkil, trifluoro(1-6C)alkil, tetrafluoro(2-6C)alkil, pentafluoro(2-6C)alkil, halogen, CN, (1-4C)alkoksi, hidroksi(1-4C)alkil, (1-3C alkoksi)(1-4C)alkil, (1-4Calkil)OC(=O)-, (1-6C)alkiltio, (3-4C)cikloalkil, amino, aminokarbonil, trifluoro(1-3C alkil)amido ili fenil (izborno supstituisan sa jednom ili više grupa nezavisno izabranih od halogena, (1-6C)alkila i (1-6C)alkoksi); ili R4 i R5 zajedno sa atomima za koje su vezani formiraju 5-6 –člani zasićeni, delimično nezasićeni ili nezasićeni heterociklični prsten koji ima heteroatom u prstenu izabran od N, O ili S, gde je navedeni heterociklični prsten izborno supstituisan sa jednim ili dva supstituenta nezavisno izabrana od (1-6C alkil)C(=O)O-, (1-6C)acil, (1-6C)alkil i okso, i navedeni atom sumpora u prstenu je izborno oksidovan do S(=O) ili SO2.
2. Jedinjenje prema patentnom zahtevu 1, naznačeno time što X je O.
3. Jedinjenje prema bilo kom od patentnih zahteva 1-2, naznačeno time što su nula do četiri Rd, Re, Rf, Rg, Rh, Ri, Rj i Rk nezavisno H, OH, (1-6C)alkil [izborno supstituisan sa jednim do pet fluoro], (3-6C)cikloalkil [izborno supstituisan sa jednim do pet fluoro], (1-3C alkoksi)(2-6C)alkil [izborno supstituisan sa jednim do pet fluoro], hidroksi(2-6C)alkil [izborno supstituisan sa jednim do pet fluoro], (2-6C)cijanoalkil, (1-6C)alkoksi [izborno supstituisan sa jednim do pet fluoro] ili (1-3C alkoksi)(2-6C)alkoksi [izborno supstituisan sa jednim do pet fluoro] ili jedan par Rd i Re, ili Rf i Rg, ili Rh i Ri, ili Rj i Rk, zajedno sa atomom ugljenika za koji su vezani formiraju (3-6C)cikloalkil, oksetanil ili azetidinil prsten, ili jedan par Rd i Re, ili Rf i Rg, ili Rh i Ri, ili Rj i Rk formiraju okso grupu, i preostali su vodonik, pri čemu samo jedan od Rd i Re može biti OH i nijedan nije OH ako je B povezan za heteroatom, i samo jedan od Rf i Rg može biti OH i nijedan nije OH ako je D povezan za heteroatom, i samo jedan od Rh i Ri mogu biti OH i nijedan nije OH ako je E povezan za heteroatom, i samo jedan od Rj i Rk može biti OH i nijedan nije OH ako je F povezan za heteroatom.
4. Jedinjenje prema patentnom zahtevu 3, naznačeno time što su nula do dva od Rd, Re, Rf, Rg, Rh, Ri, Rj i Rk nezavisno OH, metil, metoksi, CH3OCH2CH2O- ili ciklopropil, ili jedan od para Rd i Re, ili Rf i Rg, ili Rh i Ri, ili Rj i Rk, zajedno sa atomom ugljenika za koji su vezani formiraju (3-6C)cikloalkil, oksetanil ili azetidinil prsten, ili jedan od para Rd i Re, ili Rf i Rg, ili Rh i Ri, ili Rj i Rk formiraju okso grupu, i preostali su vodonik, pri čemu samo jedan od od Rd i Re može biti OH i nijedan nije OH ako je B povezan za heteroatom, i samo jedan od Rf i Rg može biti OH i nijedan nije OH ako je D povezan za heteroatom, i samo jedan od Rh i Ri može biti OH i nijedan nije OH ako je E vezan za heteroatom, i samo jedan od Rj i Rk može biti OH i nijedan nije OH ako je F vezan za heteroatom.
5. Jedinjenje prema bilo kom od patentnih zahteva 1-4, naznačenao time što prsten A je A-1.
6. Jedinjenje prema patentnom zahtevu 5, naznačeno time što B je veza ili CRdRe, D je veza ili CRfRg, E je veza ili CRhRi, i F je CRjRk, uz uslov da prsten formiran pomoću B, D, E, i F zajedno sa atomima za koje su vezani sadrži najmanje pet atoma.
7. Jedinjenje prema bilo kom od patentnih zahteva 1-6, naznačeno time što Y je H, halogen ili (1-3C alkoksi)(1-6C)alkil.
8. Jedinjenje prema bilo kom od patentnih zahteva 1-7, naznačeno time što Ra, Rb i Rc su nezavisno izabrani od halogena, (1-3C)alkil, (1-3C)alkoksi i CN.
9. Jedinjenje prema bilo kom od patentnih zahteva 1-8, naznačeno time što: R4 je OH, (1-6C)alkil, monofluoro(1-6C)alkil, difluoro(1-6C)alkil, trifluoro(1-6C)alkil, tetrafluro(2-6C)alkil, pentafluro(2-6C)alkil, cijano(1-6C)alkil, hidroksi(1-6C)alkil, dihidroksi(2-6C)alkil, (1-3C alkoksi)(1-6C)alkil, amino(1-6C)alkil, aminokarbonil(1-6C)alkil, (1-3C)alkilsulfonamido(1-6C)alkil, sulfamido(1-6C)alkil, hidroksikarbonil(1-6C)alkil, hetAr3(1-6C)alkil, Ar3(1-6C)alkil, (1-6C)alkoksi, monofluoro(1-6C)alkoksi, difluoro(1-6C)alkoksi, trifluoro(1-6C)alkoksi, tetrafluoro(2-6C)alkoksi, pentafluoro(2-6C)alkoksi cijano(1-6C)alkoksi, hidroksi(1-6C)alkoksi, dihidroksi(2-6C)alkoksi, amino(2-6C)alkoksi, hidroksil-karbonil(1-6C)alkoksi, hetCyc2(1-6C)alkoksi, hetAr3(1-6C)alkoksi, Ar3(1-6C)alkoksi, (1-4C alkoksi)(1-6C)alkoksi, (1-3C alkilsulfonil)(1-6C)alkoksi, (3-6C)cikloalkil [izborno supstituisan sa F, OH, (1-6C alkil), (1-6C) alkoksi ili (1-3Calkoksi)(1-6C)alkil], hetAr4, hetAr4-O-, Ar4, hetCyc2(O)CH2-, (1-4C alkoksikarbonil)(1-6C)alkoksi, hidroksikarbonil(1-6C)alkoksi, aminokarbonil(1-6C)alkoksi, hetCyc2C(=O)(1-6C)alkoksi, hidroksi(1-3Calkoksi)(1-6C)alkoksi, hidroksitrifluoro(1-6C)alkoksi, (1-3C)alkilsulfonamido(1-6C)alkoksi, (1-3C)alkilamido(1-6C)alkoksi, di(1-3Calkil)amino-karboksi, hetCyc2C(=O)O-, hidroksidifluoro(1-6C)alkil, (1-4C alkilkarboksi)(1-6C)alkil, (1-6C)alkoksikarbonil, hidroksilkarbonil, aminokarbonil, (1-3C alkoksi)aminokarbonil, hetCyc3, halogen, CN, trifluorometilsulfonil, N-(1-3C alkil)oksadiazolonil ili hetAr5; i R5 je (1-6C)alkil, monofluoro(1-6C)alkil, difluoro(1-6C)alkil, trifluoro(1-6C)alkil, tetrafluoro(2-6C)alkil, pentafluoro(2-6C)alkil, halogen, CN, (1-4C)alkoksi, hidroksi(1-4C)alkil, (1-3C alkoksi)(1-4C)alkil, (1-4Calkil)OC(=O)-, (1-6C)alkiltio, (3-4C)cikloalkil, amino, aminokarbonil, trifluoro(1-3C alkil)amido ili fenil (izborno supstituisan sa jednom ili više grupa nezavisno izabrana od halogena, (1-6C)alkil i (1-6C)alkoksi).
10. Jedinjenje prema patentnom zahtevu 9, naznačeno time što R4 je izabran od (1-6C)alkoksi, hetAr4 i hetAr5.
11. Jedinjenje prema patentnom zahtevu 10, naznačeno time što R4 je hetAr4 ili hetAr5.
12. Jedinjenje prema bilo kom od patentnih zahteva 1-11, naznačeno time što R5 je izabran od halogena, CN, (1-6C)alkil, (1-4C)alkoksi, hidroksi(1-4C)alkil, (1-6C)alkiltio ili fenila izborno supstituisanog sa jednom ili više grupa nezavisno izabranih od halogena, (1-6C)alkil i (1-6C)alkoksi.
13. Jedinjenje prema patentnom zahtevu 12, naznačeno time što R5 je (1-6C)alkil.
14. Jedinjenje prema bilo kom od patentnih zahteva 1-13, naznačeno time što R3 je izabran od Ar2 i (1-6C)alkil.
15. Jedinjenje prema patentnom zahtevu 14, naznačeno time što R3 je Ar2.
16. Jedinjenje prema patentnom zahtevu 9, naznačeno time što R4 je izabran od H, (1-6C)alkil, trifluoro(1-6C)alkil, hidroksi(1-6C)alkil, cijano(1-6C)alkil, (1-3C alkoksi)(1-6C)alkil, (1-6C)alkoksi, monofluoro(1-6C)alkoksi, cijano(1-6C)alkoksi, hidroksi(1-6C)alkoksi, dihidroksi(2-6C)alkoksi, hetCyc2(1-6C)alkoksi, Ar3(1-6C)alkoksi, (1-4C alkoksi)(1-6C)alkoksi, (1-3C alkilsulfonil)(1-6C)alkoksi, (3-6C)cikloalkil, hetAr4, hetAr4-O-, Ar4 i hetAr5.
17. Jedinjenje prema patentnom zahtevu 16, naznačeno time što R4 je hetCyc2(1-6C)alkoksi.
18. Jedinjenje prema patentnom zahtevu 17, naznačeno time što R5 je (1-6C)alkil.
19. Jedinjenje prema patentnom zahtevu 18, naznačeno time što R3 je Ar2.
20. Jedinjenje prema patentnom zahtevu 19, naznačeno time što Y je H.
21. Jedinjenje prema patentnom zahtevu 1, izabrano od Pr. # Struktura 1 2 4 5 6 7 (nastavak) Pr. # Struktura 8 9 10 11 12 13 (nastavak) Pr.# Struktura 14 15 16 17 18 (nastavak) Pr.# Struktura 19 20 21 25 (nastavak) Pr.# Struktura 26 27 29 30 (nastavak) Pr.# Struktura 31 32 33 34 (nastavak) Pr.# Struktura 35A 35B 36 37 (nastavak) Pr.# Struktura 38 39 40 41 (nastavak) Pr.# Struktura 42 43 44 45 (nastavak) Pr.# Struktura 46 49 51 52 (nastavak) Pr.# Struktura 53 54 55 56 (nastavak) Pr.# Struktura 57 58 59 60 (nastavak) Pr.# Struktura 61 62 63 64 (nastavak) Pr.# Struktura 65 66 67 68 (nastavak) Pr.# Struktura 69 70 71 72 (nastavak) Pr.# Struktura 73 74 75 76 (nastavak) Pr.# Struktura 77 78 79 80 (nastavak) Pr.# Struktura 81 82 83 84 (nastavak) Pr.# Struktura 85 86 87 88 (nastavak) Pr.# Struktura 89 90 91 92 (nastavak) Pr.# Struktura 93 94 95 96 97 (nastavak) Pr.# Struktura 98 99 100 101 102 103 (nastavak) Pr.# Struktura 104 105 106 107 108 109 (nastavak) Pr.# Struktura 110 111 112 113 114 115 (nastavak) Pr.# Struktura 116 117 118 119 120 121 (nastavak) Pr.# Struktura 122 123 124 125 126 127 (nastavak) Pr.# Struktura 128 129 130 131 132 (nastavak) Pr.# Struktura 133 134 135 136 (nastavak) Pr.# Struktura 137 138 139 140 (nastavak) Pr.# Struktura 141 142 143 144 (nastavak) Pr.# Struktura 146 147 148 149 (nastavak) Pr.# Struktura 150 151 152 153 (nastavak) Pr.# Struktura 154 155 156 157 (nastavak) Pr.# Struktura 158 159 160 ili njegova farmaceutski prihvatljiva so.
22. Jedinjenje prema patentnom zahtevu 21, izabrano od Pr.# Struktura 37 (nastavak) Pr.# Struktura 55 56 57 (nastavak) Pr.# Struktura 58 59 60 61 (nastavak) Pr.# Struktura 62 63 64 65 (nastavak) Pr.# Struktura 66 67 68 69 (nastavak) Pr.# Struktura 70 71 72 73 (nastavak) Pr.# Struktura 74 75 76 77 (nastavak) Pr.# Struktura 78 101 118 121 123 127 (nastavak) Pr.# Struktura 128 137 138 139 (nastavak) Pr.# Struktura 140 141 142 154 (nastavak) Pr.# Struktura 155
23. Jedinjenje prema patentnom zahtevu 21, izabrano od: Pr.# Struktura 74 80 (nastavak) Pr.# Struktura 82 84 86 87 (nastavak) Pr.# Struktura 117 122 129 144 (nastavak) Pr.# Struktura 146 147 151 153 (nastavak) Pr.# Struktura 155
24. Farmaceutska kompozicija, koja sadrži jedinjenje formule I kao što je definisano u bilo kom od patentnih zahteva 1 do 23 ili njegovu farmaceutski prihvatljivu so, i farmaceutski prihvatljiv razblaživač ili nosač.
25. Jedinjenje formule I prema bilo kom od patentnih zahteva 1 do 23, ili njegova farmaceutski prihvatljiva so, ili farmaceutska kompozicija prema patentnom zahtevu 24, za upotrebu u lečenju.
26. Jedinjenje formule I prema bilo kom od patentnih zahteva 1 do 23, ili njegova farmaceutski prihvatljiva so, ili farmaceutska kompozicija prema patentnom zahtevu 24, za upotrebu u lečenju bola, kancera, inflamacije/inflamatornih bolesti, neurodegenerativnih bolesti, određenih infektivnih bolesti, Sjogrenovog sindroma, endometrioze, dijabetičke periferne neuropatije, prostatitisa i sindroma pelvičnog bola.
27. Jedinjenje ili farmaceutska kompozicija prema patentnom zahtevu 26, za upotrebu u lečenju bola.
28. Jedinjenje ili farmaceutska kompozicija za upotrebu prema patentnom zahtevu 27, naznačeno time što bol je hronični bol.
29. Jedinjenje ili farmaceutska kompozicija za upotrebu prema patentnom zahtevu 27, naznačeno time što bol je akutni bol.
30. Jedinjenje ili farmaceutska kompozicija za upotrebu prema patentnom zahtevu 27, naznačeno time što bol je inflamatorni bol, neuropatski bol, bol povezan sa kancerom, bol povezan sa operacijom ili bol povezan sa frakturom kosti.
31. Jedinjenje ili farmaceutska kompozicija za upotrebu prema patentnom zahtevu 26, naznačeno time što, navedeni kancer je kancer koji ima disregulaciju TrkA.
32. Jedinjenje formule I prema bilo kom od patentnih zahteva 1 do 23, ili njegova farmaceutski prihvatljiva so, za upotrebu u pripremi leka za lečenje bola, kancera, inflamacije/inflamatornih bolesti, neurodegenerativnih bolesti, određenih infektivnih bolesti, Sjogrenovog sindroma, endometrioze, dijabetičke periferne neuropatije, prostatitisa i sindroma pelvičnog bola.
33. Postupak za pripremu jedinjenja prema patentnom zahtevu 1, koji sadrži: (a) za jedinjenje formule I gde X je O, spajanje odgovarajućeg jedinjenja koje ima formulu II sa odgovarajućim jedinjenjem koje ima formulu III u prisustvu karbonildiimidazola ili trifozgena i baze; ili (b) za jedinjenje formule I gde X je S, spajanje odgovarajućeg jedinjenja koje ima formulu II sa odgovarajućim jedinjenjem koje ima formulu III u prisustvu di(1H-imidazol-2-il)metantiona i baze; ili (c) za jedinjenje formule I gde X je O, spajanje odgovarajućeg jedinjenja koje ima formulu II sa odgovarajućim jedinjenjem koje ima formulu IV gde L1 je odlazeća grupa, u prisustvu baze; ili (d) za jedinjenje formule I gde X je O, spajanje odgovarajućeg jedinjenja koje ima formulu V gde L2 je odlazeća grupa, sa odgovarajućim jedinjenjem koje ima formulu III u prisustvu baze; ili (e) za jedinjenje formule I gde X je O, aktiviranje odgovarajućeg jedinjenja koje ima formulu VI sa difenilfosforil azidom, a zatim spajanje aktivnog intermedijera sa odgovarajućim jedinjenjem koje ima formulu III u prisustvu baze; ili (f) za jedinjenje formule I gde X je O, spajanje odgovarajućeg jedinjenja koje ima formulu II sa odgovarajućim jedinjenjem koje ima formulu VII u prisustvu baze; ili (g) za jedinjenje formule I gde X je O, spajanje odgovarajućeg jedinjenja koje ima formulu VIII sa odgovarajućim jedinjenjem koje ima formulu III u prisustvu baze; i izborno uklanjanje zaštitnih grupa i izborno pripremu njegove farmaceutski prihvatljive soli.
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