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HRP20220577T1 - Derivat benzazepina, metoda pripreme, farmaceutski sastav i njegova upotreba - Google Patents

Derivat benzazepina, metoda pripreme, farmaceutski sastav i njegova upotreba Download PDF

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HRP20220577T1
HRP20220577T1 HRP20220577TT HRP20220577T HRP20220577T1 HR P20220577 T1 HRP20220577 T1 HR P20220577T1 HR P20220577T T HRP20220577T T HR P20220577TT HR P20220577 T HRP20220577 T HR P20220577T HR P20220577 T1 HRP20220577 T1 HR P20220577T1
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Daxin Gao
Yuxun Wang
Shoujun Chen
Heping Yang
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Shanghai De Novo Pharmatech Co., Ltd.
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Claims (13)

1. Spoj formule (I), stereoizomer, stabilni izotopski derivat ili njegova farmaceutski prihvatljiva sol; [image] pri čemu, L je -C(O)-, -C(S)- ili -S(O)2-; L1 je veza; R je izabran iz skupine koja se sastoji od R-1 do R-19: [image] [image] [image] [image] [image] svaki R7 i R7aje nezavisno izabran od vodika, halogena, alkila, hidroalkila, alkenila, alkinila, Cy1, -L2-Cy1, -SRd, -ORd, -C(O)ORd, -C(O)Rd, -C(O)NRdRe, -C(O)NRdS(O)2Re, -C(=NH)Re, -C(=NH)NRdRe, -S(O)2Re i - S(O)2NRdRe; pri čemu je alkil, alkenil ili alkinil nesupstituiran ili supstituiran u bilo kojem položaju s jednim ili više od jednog supstituenta izabranog iz skupine koja se sastoji od -CN, -NO2, -SRd, -ORd, -OC(O)Rd, -OC(O)ORd, -OC(O)NRdRe, -C(O)ORd, -C(O)Rd, - C(O)NRdRe, -C(O)NRdS(O)2Re, -NRdRe, -NRdC(O)Re, -N(Rd)C(O)ORe, - N(Rd)C(O)NRdRe, -NRdC(=NH)Re, -NRdC(=NH)NRdRe, -NRdS(O)2Re, - NRdS(O)2NRdRe, -N(Rd)C(O)N(Rd)S(O)2Re, -S(O)1-2Re, -S(O)2NRdRe, - S(O)(=NCN)Re, -S(O)(=NRd)Re, -S(O)(=NSO2Rd)Re, -S(O)2N(Rd)C(O)Re, - S(O)2N(Rd)C(O)NRdRe, -P(O)(ORd)2, -OP(O)(ORd)2 or -B(ORd)2; ili je R7 [image] ili [image] ; svaki R8 je nezavisno vodik, halogen, alkil, haloalkil, haloalkoksi, alkenil, alkinil, Cy1, -L2-Cy1, -CN, -NO2, -SRd, -ORd, -OC(O)Rd, -OC(O)ORd, - OC(O)NRdRe, -C(O)ORd, -C(O)Rd, -C(O)NRdRe, -C(O)NRdS(O)2Re, -C(=NH)Re, -C(=NH)NRdRe, -NRdRe, -NRdC(O)Re, -N(Rd)C(O)ORe, -N(Rd)C(O)NRdRe, - NRdS(O)2Re, -NRdC(=NH)Re, -NRdC(=NH)NRdRe, -S(O)1-2Re, -S(O)2NRdRe i - NRdS(O)2NRdRe; pri čemu je alkil, alkenil ili alkinil nesupstituiran ili supstituiran u bilo kojem položaju s jednim ili više od jednog supstituenta izabranog iz skupine koja se sastoji od -CN, -NO2, -SRd, -ORd, -OC(O)Rd, -OC(O)ORd, -OC(O)NRdRe, -C(O)ORd, -C(O)Rd, -C(O)NRdRe, -C(O)NRdS(O)2Re, -NRdRe, -NRdC(O)Re, -N(Rd)C(O)ORe, - N(Rd)C(O)NRdRe, -NRdC(=NH)Re, -NRdC(=NH)NRdRe, -NRdS(O)2Re, - NRdS(O)2NRdRe, -N(Rd)C(O)N(Rd)S(O)2Re, -S(O)1-2Re, -S(O)2NRdRe, - S(O)2N(Rd)C(O)Re or -S(O)2N(Rd)C(O)NRdRe; svaki n je nezavisno 1, 2 ili 3; L2 je veza, C2-6 alkenilen, C2-6 alkinilen, ili -(CRa1Rb1)m-; svaki Cy1 je nezavisno cikloalkil, heterocikloalkil, aril ili heteroaril; Cy1 je nesupstituiran ili selektivno supstituiran na bilo kojem položaju s jednim ili više od jednog supstituenta izabranog iz skupine koja se sastoji od halogena, alkila, haloalkila, haloalkoksija, hidroksialkila, aminoalkila, alkenila, alkinila, -CN, -NO2, -SRd2, -ORd2, -OC(O)Rd2, - OC(O)ORd2, -OC(O)NRd2Re2, -C(O)ORd2, -C(O)Rd2, -C(O)NRd2Re2, -NRd2Re2, -NRd2C(O)Re2, -N(Rd2)C(O)ORe2, -N(Rd2)C(O)NRd2Re2, -NRd2S(O)2Re2, - NRd2C(=NH)Re2, -NRd2C(=NH)NRd2Re2, -S(O)1-2Re2, -S(O)2NRd2Re2 i - NRd2S(O)2NRd2Re2; R1, R2 i R3 su nezavisno izabrani od vodika, deuterija ili alkila; ili, R2 i R3 zajedno s atomom C na koji su vezani, oblikuju C3-8 cikloalkil ili 3-8-člani heterocikloalkil; R4, R5 i R6 su nezavisno izabrani od vodika, deuterija, halogena, amina, cijana, nitra, C1-6 alkila, C1-6 haloalkila, C1-6 haloalkoksija, C1-6 alkoksija, C2-6 alkenila, C2-6 alkinila, C1-6 hidroksialkila, C3-8 cikloalkila, 3-8-članog heterocikloalkila, fenila ili 5-6-članog heteroarila; RA je izabran od -ORd1 ili -NRd1Re1; RB je -NRd1Re1; svaki Ra1 i Rb1 je nezavisno izabran od vodika, deuterija, halogena, C1-6 alkila, C1-6 alkoksija, C2-6 alkenila, C2-6 alkinila, C3-8 cikloalkila, 3-8-članog heterocikloalkila, C6-10 arila, 5-6-članog heteroarila, C3-8 cikloalkil C1-6 alkila, 3-8-članog heterocikloalkil C1-6 alkila, fenil C1-6 alkila ili 5-6-članog heteroaril C1-6 alkila; C1-6 alkila, C1-6 alkoksija, C2-6 alkenila, C2-6 alkinila, C3-8 cikloalkila, 3-8-članog heterocikloalkila, C6-10 arila ili 5-6-članog heteroarila nesupstituiranog ili supstituiranog na bilo kojem položaju s 1 do 3 supstituenta izabranih iz skupine koja se sastoji od halogena, hidroksila, amina, karboksila, C2-6 alkenila, C2-6 alkinila, C1-6 alkila, C1-6 haloalkila, C1-6 alkoksija i C1-6 haloalkoksija; ili Ra1 i Rb1 zajedno s atomom C na koji su vezani, oblikuju C3-8 cikloalkil ili 3-8-člani heterocikloalkil; svaki od Rd, Re, Rd1 i Re1 je samostalno izabran od vodika, C1-6 alkila, C2-6 alkenila, C2-6 alkinila, C3-8 cikloalkila, 3-8-članog heterocikloalkila, C6-10 arila, 5-6-članog heteroarila, C3-8 cikloalkil C1-6 alkila, 3-8-članog heterocikloalkil C1-6 alkila, fenil C1-6 alkila ili 5-6-članog heteroaril C1-6 alkila; Rd, Re, Rd1 ili Re1 je nesupstituiran ili supstituiran na bilo kojem položaju s 1 do 3 supstituenta izabranih iz skupine koja se sastoji od halogena, hidroksila, amina, karboksila, C1-6 alkila, C1-6 alkoksija, C1-6 alkilamina, C1-6 haloalkila, C1-6 haloalkoksija, C2-6 alkenila i C2-6 alkinila; ili, Rd i Re, ili Rd1 i Re1 zajedno s atomom N na koji su vezani, oblikuju 3-8-člani heterocikloalkil; heterocikloalkil može dalje obuhvaćati 1 do 3 heteroatoma izabranih iz skupine koja se sastoji od N, O i S; heterocikloalil je nesupstituiran ili supstituiran na bilo kojem položaju s 1 do 3 supstituenta izabranih iz skupine koja se sastoji od halogena, amina, hidroksila, karboksila, cijana, C1-6 alkila, C1-6 haloalkila, C2-6 alkenila, C2-6 alkinila, C1-3 alkila, amino C1-3 alkila, -ORd2, -OC(O)Rd2, - OC(O)ORd2, -OC(O)NPd2Re2, -C(O)ORd2, -C(O)Rd2, -C(O)NRd2Re2, -NRd2Re2, - NRd2C(O)Re2, -N(Rd2)C(O)ORe2, -N(Rd2)C(O)NRd2Re2, -NRd2S(O)2Re2, - NRd2C(=NH)Re2, -NRd2C(=NH)NRd2Re2, -NRd2S(O)2NRd2Re2, -S(O)1-2Rd2 i - S(O)2NRd2Re2; svaki od Rd2 i Re2 je nezavisno izabran od vodika, C1-6 alkila, C2-6 alkenila, C2-6 alkinila, C3-8 cikloalkila, 3-8-članog heterocikloalkila, C6-10 arila, 5-6-članog heteroarila, C3-8 cikloalkil C1-6 alkila, 3-8-članog heterocikloalkil C1-6 alkila, fenil C1-6 alkila ili 5-6-članog heteroaril C1-6 alkila; Rd2 ili Re2 je nesupstituiran ili supstiruiran na bilo kojem položaju s 1 do 3 supstituenta izabranih iz skupine koja se sastoji od halogena, hidroksila, amina, karboksila, C1-6alkila, C1-6 alkoksija, C1-6 alkilamina, C1-6 haloalkila, C1-6 haloalkoksija, C2-6 alkenila i C2-6 alkinila; ili, Rd2 i Re2 zajedno s atomom N na koji su vezani, oblikuju 3-8-člani heterocikloalkil; svaki m je 1, 2, 3, 4, 5, ili 6.
2. Spoj formule (I), stereoizomer, stabilni izotopski derivat ili njegova farmaceutski prihvatljiva sol prema patentnom zahtjevu 1, pri čemu svaki R1, R2 i R3 je H; svaki R4, R5 i R6 je nezavisno izabran od H, D, F, Cl, Br, -CN, -NH2, -CH3, -OCH3, -OCF3, -CH2F, -CHF2 or -CF3.
3. Spoj formule (I), stereoizomer, stabilni izotopski derivat ili njegova farmaceutski prihvatljiva sol prema patentnom zahtjevu 1, pri čemu je svaki Rd1 i Re1 nezavisno izabran od vodika, C1-6alkila, C1-6haloalkila, C3-8 cikloalkila ili 3-8-članog heterocikloalkila; Rd1 ili Re1 je nesupstituiran ili opcionalno supstituiran na bilo kojem položaju s jednim hidroksilom; ili, Rd1 i Re1 zajedno s atomom N na koji su vezani, oblikuju C3-8 heterocikloalkil; heterocikloalkil može dalje sadržavati 1-3 hetero atoma izabranih od N, O i S; heterocikloalkil je nesupstituiran ili supstituiran na bilo kojem položaju s jednim supstituentom izabranim iz skupine koja se sastoji od C1-4 alkila, C1-3 haloalkila, i C1-3 aminoalkila.
4. Spoj formule (I), stereoizomer, stabilni izotopski derivat ili njegova farmaceutski prihvatljiva sol prema patentnom zahtjevu 1, pri čemu je RB –NH2-.
5. Spoj formule (I), stereoizomer, stabilni izotopski derivat ili njegova farmaceutski prihvatljiva sol prema patentnom zahtjevu 1, pri čemu, svaki od R7 je nezavisno vodik, C1-6alkil, C1-6haloalkil, C2-6 alkenil, C2-6 alkinil, Cy1, -L2-Cy1, -SRd, -ORd, -C(O)ORd, -C(O)Rd, -C(O)NRdRe, -C(=NH)Re, - C(=NH)NRdRe, -S(O)2Re ili -S(O)2NRaRe; pri čemu C1-6 alkil, C2-6 alkenil or C2-6 alkinil je nesupstituiran ili supstituiran na bilo kojem položaju s 1 do 3 supstituenta izabranih iz skupine koja se sastoji od -CN, -NO2, -CN, -SRd, -ORd, -OC(O)Rd, -OC(O)ORd, - OC(O)NRdRe, -C(O)ORd, -C(O)Rd, -C(O)NRdRe, -NRdRe, -NRdC(O)Re, - N(Rd)C(O)ORe, -N(Rd)C(O)NRdRe, -NRdS(O)2Re, -NRdC(=NH)Re, -NRdC(=NH)NRdRe, -S(O)1-2Re, -S(O)2NRdRe, -S(O)(=NCN)Re, -S(O)(=NRd)Re, -S(O)(=NSO2Rd)Re, -NRdS(O)2NRdRe, -P(O)(ORd)2, -OP(O)(ORd)2, -B(ORd)2, [image] ili [image] ; i/ili, svaki R7a je nezavisno vodik ili C1-6 alkil; i/ili, svaki R8 je nezavisno vodik, metil, etil, n-propil, tert-butil, izopropil, izobutil, n-butil, -CN, -NO2, -NH2, -CF3, -OCF3, -CH3, -OCH3, F, Cl ili Br; i/ili, L2 je veza, -CH2-, -CH2CH2-, -CH2CH2CH2-, -CH2CH2C(CH3)2-, -CH2CH2CH2CH2- ili -CH2CH(CH3)CH2-; i/ili, svaki od Cy1 je nezavisno C3-10 cikloalkil, 3-10-člani heterocikloalkil, C6-10 aril ili 5-10-člani heteroaril; Cy1 je nesupstituiran ili supstiruiran na bilo kojem položaju s 1 do 3 supstituenta izabranih iz skupine koja se sastoji od F, Cl, Br, C1-4 alkila, C1-3 haloalkila, C1-3 haloalkoksija, C1-3 hidroksialkila, C1-3aminoalkila, C2-6 alkenila, C2-6 alkinila, -CN, -NO2, -SRd2, -ORd2, -OC(O)Rd2, -OC(O)ORd2, -OC(O)NRd2Re2, -C(O)ORd2, -C(O)Rd2, -C(O)NRd2Re2, -NRd2Re2, -NRd2C(O)Re2, - N(Rd2)C(O)ORe2, -N(Rd2)C(O)NRd2Re2, -NRd2S(O)2Re2, -NRd2C(=NH)Re2, - NRd2C(=NH)NRd2Re2, -S(O)1-2Re2, -S(O)2NRd2Re2 i -NRd2S(O)2NRd2Re2; i/ili, svaki od Rd, Re, Rd2 i Re2 je nezavisno izabran od vodika, C1-6 alkila, C1-6 haloalkila, C2-6 alkenila, C2-6 alkinila, C3-8 cikloalkila, 3-8-članog heterocikloalkila, C6-10 arila, 5-6-članog heteroarila, C3-8 cikloalkil C1-6 alkila, 3-8-članog heterocikloalkil C1-6 alkila, fenil C1-6 alkila ili 5-6-članog heteroaril C1-6 alkila; Rd, Re, Rd2 ili Re2 je nesupstituiran ili supstituiran na bilo kojem položaju s 1 do 3 supstituenta izabranih iz skupine koja se sastoji od halogena, hidroksila, amina, karboksila, C1-4 alkila, C1-3 haloalkila, C1-3 haloalkoksija, C1-3 alkoksija, C1-3 alkilamina, C2-6 alkenila i C2-6 alkinila; ili, Rd i Re zajedno s atomom N na koji su vezani, oblikuju 3-8-člani heterocikloalkil; heterocikloalkil može dalje sadržavati 1 do 3 hetero atoma izabranih od N, O, i S; ili, Rd2 i Re2 zajedno s atomom N na koji su vezani, oblikuju 3-8-člani heterocikloalkil.
6. Spoj formule (I), stereoizomer, stabilni izotopski derivat ili njegova farmaceutski prihvatljiva sol prema patentnim zahtjevima 1 do 5, pri čemu je svaki R7 nezavisno vodik, metil, etil, n-propil, tert-butil, izopropil. izobutil, n-butil, neofentil, tert-amil, ciklopropil, ciklobutil, ciklofenil, cikloheksil, fenil, piridil, pirimidinil, benzil, [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] ili [image] .
7. Spoj formule (I), stereoizomer, stabilni izotopski derivat ili njegova farmaceutski prihvatljiva sol prema barem jednom od patentnih zahtjeva 1 do 6, koji je prikazan kao spoj formule (IA), (IB), (IC), (ID), (IE), (IF), (IG), (IH), (II), (IJ), (IK) ili (IL), stereoizomer, stabilni izotopski derivat ili njegova farmaceutski prihvatljiva sol; spoj formule (IA), stereoizomer, stabilni izotopski derivat ili njegova farmaceutski prihvatljiva sol: [image] pri čemu, [image] je jednostruka ili dvostruka veza; Y je O ili S; U je N, C(R8) ili C(O), V je N, C(R8) ili N(R7a); i, [image] , U i V su bilo koja kombinacija od sljedećih: 1) [image] je dvostruka veza, U je N, V je C(Rs); 2) [image] je dvostruka veza, U je C(Rs), V je N; 3) [image] je dvostruka veza, U je C(Rs), V je C(Rs); 4) [image] je jednostruka veza, U je C(Rs), V je C(Rs); 5) [image] je jednostruka veza, U je C(O), V je N(R7a); n je 1; L1, Rd1, Re1, R4, R5, i R6 su definirani kao u bilo kojem patentnom zahtjevu 1-6; R7, R8 i R7a su definirani kao u bilo kojem patentnom zahtjevu 1, 5 ili 6; spoj formule (IB) ili (IC), stereoizomer, stabilni izotopski derivat ili njegova farmaceutski prihvatljiva sol: [image] pri čemu, [image] je jednostruka veza ili dvostruka veza; Y je O ili S; Rd1, Re1, R4, R5, i R6 su definirani kao u bilo kojem patentnom zahtjevu 1-6; R7 i R8 su definirani kao u bilo kojem patentnom zahtjevu 1, 5 i 6; spoj formule (ID) ili (IE), stereoizomer, stabilni izotopski derivat ili njegova farmaceutski prihvatljiva sol: [image] pri čemu, Y je O ili S; Rd1, Re1, R4, R5, i R6 su definirani kao u bilo kojem patentnom zahtjevu 1-6; R7 i R8 su definirani kao u bilo kojem patentnom zahtjevu 1, 5 i 6; spoj formule (IF) ili (IG), stereoizomer, stabilni izotopski derivat ili njegova farmaceutski prihvatljiva sol: [image] pri čemu, Y je O ili S; Rd1, Re1, R4, R5, i R6 su definirani kao u bilo kojem patentnom zahtjevu 1-6; R7 i R8 su definirani kao u bilo kojem patentnom zahtjevu 1, 5 i 6; spoj formule (IH) ili (II), stereoizomer, stabilni izotopski derivat ili njegova farmaceutski prihvatljiva sol: [image] pri čemu, Rd1, Re1, R4, R5, i R6 su definirani kao u bilo kojem patentnom zahtjevu 1-6; R7 i R7a su definirani kao u bilo kojem patentnom zahtjevu 1, 5 i 6; spoj formule (IJ), stereoizomer, stabilni izotopski derivat ili njegova farmaceutski prihvatljiva sol: [image] pri čemu, [image] je jednostruka veza ili dvostruka veza; Z je N(R7a) ili S; n je 1 ili 2; L1, Rd1, Re1, R4, R5 i R6 su definirani kao u bilo kojem patentnom zahtjevu 1-6; R7, R7a i R8 su definirani kao u bilo kojem patentnom zahtjevu 1, 5 i 6; spoj formule (IK) ili (IL), stereoizomer, stabilni izotopski derivat ili njegova farmaceutski prihvatljiva sol: [image] pri čemu, Z je NH, N(CH3) ili S; Rd1, Re1, R4, R5 i R6 su definirani kao u bilo kojem patentnom zahtjevu 1-6; R7 i R8 su definirani kao u bilo kojem patentnom zahtjevu 1, 5 i 6.
8. Spoj formule (I), stereoizomer, stabilni izotopski derivat ili njegova farmaceutski prihvatljiva sol prema patentnom zahtjevu 1, pri čemu je spoj formule (I) izabran od skupine koja se sastoji od [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] i [image]
9. Metoda pripreme spoja formule (I), stereoizomera, stabilnog izotopskog derivata ili njegove farmaceutski prihvatljive soli prema barem jednom od patentnih zahtjeva 1-8, koja je bilo koja od sljedećih metoda: metoda 1 obuhvaća provođenje Suzukijeve reakcije spajanja sa spojem formule I-a i [image] za dobivanje spoja formule (I); [image] metoda 2 obuhvaća provođenje Suzukijeve reakcije spajanja sa spojem formule I-b i R-M za dobivanje spoja spormula (I); [image] pri čemu, M je brom, klor, jod, ili -OS(O)2CF3; R1, R2, R3, R4, R5, R6, RA, RB, R i L su definirani kao u bilo kojem patentnom zahtjevu 1-8.
10. Farmaceutski sastav, koji obuhvaća terapeutski učinkovitu količinu spoja formule (I), stereoizomer, stabilni izotopski derivat ili njegovu farmaceutski prihvatljivu sol prema barem jednom od patentnih zahtjeva 1-8, i farmaceutski prihvatljivu pomoćnu(e) tvar(i).
11. Spoj formule (I), stereoizomer, stabilni izotopski derivat ili njegova farmaceutski prihvatljiva sol prema barem jednom od patentnih zahtjeva 1-8 za upotrebu u liječenju, ublažavanju i/ili prevenciji srodnih bolesti posredovanih putem TLRa (Toll-like receptora), pri čemu su bolesti posredovane putem TLRa izabrane iz skupine koja se sastoji od raka, virusnih infekcija, upala i autoimunih bolesti.
12. Spoj formule (I), stereoizomer, stabilni izotopski derivat ili njegova farmaceutski prihvatljiva sol za upotrebu prema patentnom zahtjevu 11, pri čemu je lijek dalje korišten u kombinaciji s jednom ili više od jedne vrste terapeutskih agensa i/ili terapeutske metode za liječenje, poboljšanje i/ili prevenciju srodnih bolesti posredovanih putem TLRa, pri čemu su bolesti posredovane putem TLRa izabrane iz skupine koja se sastoji od raka, virusnih infekcija, upala i autoimunih bolesti.
13. Spoj formule (I), stereoizomer, stabilni izotopski derivat ili njegova farmaceutski prihvatljiva sol za upotrebu prema barem jednom od patentnih zahtjeva 11-12, pri čemu je TLR TLR7 i/ili TLR8.
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