HRP20210481T1 - Derivati 3-tetrazolil-benzen-1,2-disulfonamida kao inhibitori metalo-beta-laktamaze - Google Patents

Derivati 3-tetrazolil-benzen-1,2-disulfonamida kao inhibitori metalo-beta-laktamaze Download PDF

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HRP20210481T1
HRP20210481T1 HRP20210481TT HRP20210481T HRP20210481T1 HR P20210481 T1 HRP20210481 T1 HR P20210481T1 HR P20210481T T HRP20210481T T HR P20210481TT HR P20210481 T HRP20210481 T HR P20210481T HR P20210481 T1 HRP20210481 T1 HR P20210481T1
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Croatia
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optionally substituted
ring
independently selected
ora
nrarb
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HRP20210481TT
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Inventor
Frank Bennett
Jinlong Jiang
Alexander Pasternak
Shuzhi DONG
Xin Gu
Jack D. Scott
Haiqun Tang
Zhiqiang Zhao
Yuhua Huang
Dexi YANG
Katherine Young
Li Xiao
Zhibo Zhang
Jianmin Fu
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Merck Sharp & Dohme Corp.
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Publication of HRP20210481T1 publication Critical patent/HRP20210481T1/hr

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    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
    • A61K31/197—Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid
    • A61K31/198—Alpha-amino acids, e.g. alanine or edetic acid [EDTA]
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D257/00—Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms
    • C07D257/02—Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms not condensed with other rings
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    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/407—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with other heterocyclic ring systems, e.g. ketorolac, physostigmine
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    • A61K31/425—Thiazoles
    • A61K31/429—Thiazoles condensed with heterocyclic ring systems
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    • A61K31/431—Compounds containing 4-thia-1-azabicyclo [3.2.0] heptane ring systems, i.e. compounds containing a ring system of the formula, e.g. penicillins, penems containing further heterocyclic rings, e.g. ticarcillin, azlocillin, oxacillin
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Claims (31)

1. Spoj formule I [image] ili njihova farmaceutski prihvatljiva sol, u kojem: X1 je N ili CH; X2 je N ili CH; Z je tetrazolil, gdje Z je vezan preko veze ugljik-ugljik za šestočlanu jezgru prstena koja ima X1 i X2; RA je -(CH2)n-AryA1, -(CH2)n-HetA1, -(CH2)n-C4-C6cikloalkil, ili -(CH2)n-C4-C6cikloalkenil, gdje su navedeni -(CH2)n-C4-C6cikloalkil i -(CH2)n-C4-C6cikloalkenil izborno supstituirani sa 1, 2 ili 3 supstituenta neovisno izabrana od -NH2, -OH, -F i -NRaC(O)C1-C6alkila izborno supstituirana sa 1 ili 2 supstituenta neovisno izabrana od -F, -CF3, -NRaRb i -ORa; R1 je 1) -NH2; 2) -NRa-C1-C6alkil izborno supstituiran sa 1, 2, 3, ili 4 supstituenta neovisno izabrana od sljedećih: -F, -CF3, C1-C6alkil, -CH(NH2)C(O)NH2, - C(O)NRaRb, -C(O)OH, -(CH2)1-2NH2, -NRa(CH2)2-3NH2, -NRaRb, -N+RaRbCH3, -NHCH2CH2OCH3, -ORa i -O(CH2)2-3NH2; 3) -NRaC(O)C1-C6alkil izborno supstituiran sa 1 ili 2 supstituenta neovisno izabrana od sljedećih: -F, -CF3, -C(O)NRaRb, -C(O)OH, -NRaRb, -N+RaRbCH3, - NHCH2CH2OCH3, -ORa i -O(CH2)2-3NH2; 4) -NRa(CH2)n-C3-C6cikloalkil, gdje je C3-C6cikloalkil izborno supstituiran sa -CH2OH ili -NH2; 5) dušikom-vezani 4-6 -člani monocikličan heterocikloalkil sa 0, 1 ili 2 dodatna heteroatoma u prstenu neovisno izabrana od N, O i S, ili dušikom-vezani 6- do 10-člani biciklični heterocikloalkil sa 0, 1, 2 ili 3 dodatna heteroatoma u prstenu izabrana od N, O i S gdje biciklični prsten može biti premošćen, fuzioniran ili spirocikličan, gdje su 4-6 -člani monocikličan heterocikloalkil i 6- do 10-člani biciklični heterocikloalkil izborno supstituirani sa jednim do tri supstituenta, neovisno izabrana od sljedećih: -F, -NRaRb, okso, -(CH2)1-2OH, -CH2NH2, -SO2CH3, i C1-C6 alkil i pri čemu je atom sumpora u prstenu izborno supstituiran sa jednim ili dva okso; 6) -NRa-(C1-C3alkil)n-AryB1, gde je C1-C3alkil izborno supstituiran sa -NH2; i 7) -NRa-(C1-C3alkil)n-HetB1; AryA1 je aromatičan sustav prstena izabran od sljedećih: 1) 5-6 -člani monociklični prsten sa 0, 1, 2, ili 3 heteroatoma u prstenu neovisno izabrana od N, O i S, izborno supstituiran sa 1, 2, ili 3 supstituenta neovisno izabrana od sljedećih: a) halogen, b) -C1-C6alkil, c) -CN, d) -CH2OH, e) -C(O)NRaRb, f) -C(O)NH(CH2)2-4NH2 izborno supstituiran sa jednim ili dva supstituenta neovisno izabrana od -NRaRb i -(CH2)nORa, g) -C(O)ORa, h) -(CH2)pNHRa izborno supstituiran sa jednim ili dva supstituenta neovisno izabrana od -NRaRb ili -ORa, i) -(CH2)pNRaC(=NH)NH2, j) -NRaC(O)C1-C6 alkil izborno supstituiran sa jednim ili dva supstituenta neovisno izabrana od -NRaRb ili -ORa, k) -NRaSO2-C1-C6alkil, l) -NRaSO2-ciklopropil, m) -ORa, n) okso, o) -SC1-C6 alkil izborno supstituiran sa jednim ili dva supstituenta neovisno izabrana od -NRaRb ili -ORa; p) -SO2Ra, q) -SO2NRaRb, r) -SO2NH-ciklopropil, s) -AryA2, t) -(CH2)nNRaAryA2, u) -C(O)NRaHetA2 i v) -HetA2, i 2) 8- do 10-člani biciklični prsten sa 1, 2, 3 ili 4 heteroatoma u prstenu izabrana od N, O i S, gdje S atom izborno ima jedan ili dva okso supstituenta i N atom je izborno u obliku N-oksida i pri čemu je prsten izborno supstituiran sa 1 ili 2 supstituenta neovisno izabrana od sljedećih a) halogen; b) C1-C6alkil izborno supstituiran sa jednim do tri supstituenta neovisno izabrana od -NRaRb, -F i -ORa; c) -(CH2)nCF3; d) -C(=NH)NH2; e) -CN; f) -C(O)CF3; g) -C(O)NRaRb; h) -C(O)NHCH2C(O)ORa; i) -C(O)NH-C2-C4alkil-NH2, j) -C(O)ORa; k) -NRaRb; l) -NHCH2SO3H; m) -(CH2)nNHC(=NH)NH2; n) -NHC(O)C1-C6alkil; o) -NHC(O)NH2; p) -NHC(O)ORa; q) -NHSO2CH3; r) -ORa; s) okso; t) -SO2Ra, u) -CH2-fenil-OCH3; i v) -HetA2; HetA1 je dihidrotiopiranil ili tetrahidropiranil; AryA2 je 5-6-člani aromatični monociklični prsten sa 1, 2 ili 3 heteroatoma u prstenu neovisno izabrana od N, N kao kvaternarne soli i S, ili 4 N atoma prstena, izborno supstituiran sa -CH2OH, -COOH, -CONH2, -C(O)OC1-C6alkil i -(CH2)pNHRa izborno supstituiran sa jednim ili dva supstituenta neovisno izabrana od -NRaRb i -ORa; HetA2 je a 4-6-člani zasićeni monociklični prsten sa 1 ili 2 heteroatoma u prstenu neovisno izabrana od N, O i S, pri čemu je S izborno supstituiran sa dvije okso grupe i pri čemu je prsten izborno supstituiran sa 1 ili 2 supstituenta neovisno izabrana od C1-C6alkil, -CN, -OH i okso; AryB1 je aromatičan prsten izabran od sljedećih: 1) 5-6 -člani monociklični aromatični prsten sa 0, 1, 2, ili 3 N atoma u prstenu, izborno supstituiran sa 1 supstituentom izabranim od -CF3, C1-C6 alkil, -(CH2)nNH2 i -OCH3; ili 2) 9-člani biciklični prsten sa 2 N atoma u prstenu; HetB1 je zasićeni prsten izabran od sljedećih: 1) 4-6 člani zasićeni monociklični prsten sa 1 ili 2 heteroatoma u prstenu neovisno izabrana od N, O i S, gdje je N atom u prstenu izborno u obliku kvaternarnog amina, gdje je S supstituiran sa dvije okso grupe, i gdje je prsten izborno supstituiran sa 1 ili 2 supstituenta neovisno izabrana od sljedećih: -F, C1-C6 alkil, C1-C6 hidroksialkil, -C(O)ORa,-(CH2)kNRaRb, -ORa i okso; ili 2) 6-10-člani biciklični prsten sa 1 ili 2 heteroatoma u prstenu neovisno izabrana od N i O, izborno supstituiran sa -OH ili -NH2, gdje je biciklični prsten premošćen ili fuzioniran; Ra i Rb su neovisno H ili C1-C6 alkil; k je 0, 1, 2, 3, ili 4; svaki n je neovisno 0 ili 1; i svaki p je neovisno 0, 1, 2, ili 3.
2. Spoj prema patentnom zahtjevu 1, ili njegova farmaceutski prihvatljiva sol, naznačen time što X1 i X2 su CH.
3. Spoj prema patentnom zahtjevu 1 ili 2, ili njegova farmaceutski prihvatljiva sol, koji ima formulu IA [image] gdje: RA je AryA1, C4-C6cikloalkil, ili C4-C6cikloalkenil, pri čemu su navedeni C4-C6cikloalkil i C4-C6cikloalkenil izborno supstituirani sa -NH2 ili NHC(O)(CH2)1-3NH2; AryA1 je aromatični sustav prstena izabran od sljedećih: 1) 5-6 -člani monociklični prsten sa 0, 1, ili 2 heteroatoma u prstenu neovisno izabrana od N i S, izborno supstituiran sa 1 ili 2 supstituenta neovisno izabrana od sljedećih: a) F, b) -C1-C6 alkil, c) -CN, d) -CH2OH, e) -C(O)NRaRb, f) -C(O)NH(CH2)2-4NH2, g) -C(O)ORa, h) -(CH2)nNHRa, i) -NHC(=NH)NH2; j) -NHC(O)CH3; k) -NRaSO2-C1-C6alkil, l) -NHSO2-Ciklopropil, m) -ORa, n) -SO2NRaRb, o) -SC1-C6alkil, p) -SO2NH-ciklopropil, q) -AryA2, r) -(CH2)nNRaAryA2, s) -C(O)NRaHetA2 i t) -HetA2, i 2) 8- do 10-člani biciklični prsten sa 1, 2, 3 ili 4 heteroatoma u prstenu izabrana od N, O i S, gdje je S atom izborno supstituiran sa jednim ili dva okso supstituenta i N atom je izborno u obliku N-oksida, i pri čemu je prsten izborno supstituiran sa 1 ili 2 supstituenta neovisno izabrana od sljedećih: F, C1-C6 alkil, -CH2CF3, -CF2CH2NH2, -CF3, -C(=NH)NH2, -CH(NH2)CH3, - CN, -C(O)CF3, -C(O)NRaRb, -C(O)NHCH2C(O)ORa, -C(O)ORa, -(CH2)0-2NRaRb, -NHC(O)CH3, -NHC(O)NH2, -NHC(O)ORa, -NHCH2SO3H, - NHSO2CH3, -ORa, okso, -CH2-fenil-OCH3, i -HetA2; i sve ostale promjenljive su definirane u patentnom zahtjevu 1.
4. Spoj prema bilo kojem od patentnih zahtjeva 1-3, ili njegova farmaceutski prihvatljiva sol, naznačen time što RA je AryAl.
5. Spoj prema patentnom zahtjevu 4, ili njegova farmaceutski prihvatljiva sol, naznačen time što AryA1 je 1) piridil izborno supstituiran sa -NH2, 2) benzoimidazolil supstituiran sa 1 ili 2 supstituenta neovisno izabrana od F, -CH3 i -(CH2)nNH2; ili 3) benzotiazolil supstituiran sa 1 ili 2 supstituenta neovisno izabrana od -CH3 i -(CH2)nNH2.
6. Spoj prema bilo kojem od patentnih zahtjeva 1-5, ili njegova farmaceutski prihvatljiva sol, naznačen time što R1 je: 1) -NH2; 2) -NRa-C1-C6alkil izborno supstituiran sa 1, 2, 3 ili 4 supstituenta neovisno izabrana od sljedećih: -F, -CF3, C1-C6alkil, -CH(NH2)C(O)NH2, -C(O)NRaRb, -C(O)OH, -(CH2)1-2NH2, -NRaRb, -N+RaRbCH3, -NHCH2CH2OCH3, -ORa, -NRa(CH2)2-3NH2, i -O(CH2)2-3NH2; 3) -NRa(CH2)n-C3-C6cikloalkil, gdje je C3-C6cikloalkil izborno supstituiran sa -CH2OH ili -NH2; 4) -NRa-(C1-C3alkil)n-AryB1, gdje je C1-C3alkil izborno supstituiran sa -NH2; i 5) -NRa-(C1-C3alkil)n-HetB1.
7. Spoj prema bilo kojem od patentnih zahtjeva 1-5, ili njegova farmaceutski prihvatljiva sol, naznačen time što R1 je: -NH2, -NH-HetB1 izborno supstituiran sa -NH2, ili -NH-C2-C3alkilNH2, izborno supstituiran sa -CH3, -OH ili -NH2.
8. Spoj prema patentnom zahtjevu 1, ili njegova farmaceutski prihvatljiva sol, koji ima formulu IB: [image] gdje: AryA1 je aromatičan sustav prstena izabran od sljedećih: 1) 5-6 -člani monociklični prsten sa 0 ili 1 N atoma u prstenu supstituiran sa 1 ili 2 supstituenta neovisno izabrana od sljedećih: F, -C1-C6 alkil, -CONH-C2-4alkil-NH2, ili - NHRa; ili 2) 9-člani biciklični prsten sa 2 heteroatoma u prstenu izabrana od N i S, pri čemu je prsten izborno supstituiran sa 1 ili 2 supstituenta neovisno izabrana od sljedećih F, C1-C6 alkil i -(CH2)xNRaRb; R1 je 1) -NH2; 2) -NRa-C1-6alkil izborno supstituiran sa 1 ili 2 F supstituenta i izborno supstituiran sa 1 ili 2 supstituenta neovisno izabrana od sljedećih: -CF3, -CH(NH2)C(O)NH2; -C(O)NRaRb; -C(O)OH; -NRa(CH2)2-3NH2, -NRaRb, - N+RaRbCH3, -NHCH2CH2OCH3, -ORa i -O(CH2)2-3NH2; 3) -NRa(CH2)n-C3-C6cikloalkil, gdje je C3-C6cikloalkil izborno supstituiran sa -CH2OH ili -NH2; 4) -NRa-(C1-C3alkil)n-AryB1; i 5) -NRa-(C1-C3alkil)n-HetB1; Ra i Rb su H ili -CH3; i x je 0, 1 ili 2.
9. Spoj prema patentnom zahtjevu 1 koji ima strukturu [image] [image] [image] [image] [image] [image] [image] [image] [image] ili [image] ili njegova farmaceutski prihvatljiva sol.
10. Cviterion spoja prema patentnom zahtjevu 9, u kojem tetrazol nosi negativni naboj i amin nosi pozitivni naboj.
11. Spoj prema patentnom zahtjevu 1, koji ima strukturu [image] ili njegova farmaceutski prihvatljiva sol.
12. Spoj prema patentnom zahtjevu 1, koji ima strukturu [image] ili njegova farmaceutski prihvatljiva sol.
13. Spoj prema patentnom zahtjevu 1, koji ima strukturu [image] ili njegova farmaceutski prihvatljiva sol.
14. Spoj prema patentnom zahtjevu 1, koji ima strukturu [image] ili njegova farmaceutski prihvatljiva sol.
15. Spoj prema patentnom zahtjevu 1, koji ima strukturu [image] ili njegova farmaceutski prihvatljiva sol.
16. Spoj prema patentnom zahtjevu 1, koji ima strukturu [image] ili njegova farmaceutski prihvatljiva sol.
17. Farmaceutski pripravak koji sadrži spoj prema bilo kojem od patentnih zahtjeva 1 do 16, ili njegovu farmaceutski prihvatljivu sol, i farmaceutski prihvatljiv nosač.
18. Farmaceutski pripravak prema patentnom zahtjevu 17, koji dalje sadrži efikasnu količinu beta-laktamskog antibiotika.
19. Farmaceutski pripravak prema patentnom zahtjevu 17 ili 18, koji dalje sadrži efikasnu količinu jednog ili više spoja inhibitora beta-laktamaze.
20. Farmaceutski pripravak prema patentnom zahtjevu 19, naznačen time što pripravak sadrži spoj inhibitor beta-laktamaze izabran iz grupe koja se sastoji od: relebaktama, avibaktama, vaborbaktama, tazobaktama, sulbaktama i klavulanske kiseline.
21. Farmaceutski pripravak prema patentnom zahtjevu 20, naznačen time što spoj inhibitor beta-laktamaze je tazobaktam i beta-laktamski antibiotik je ceftolozan.
22. Farmaceutski pripravak prema patentnom zahtjevu 20, naznačen time što spoj inhibitor beta-laktamaze je relebaktam.
23. Farmaceutski pripravak prema bilo kojem od patentnih zahtjeva 18 -20, naznačen time što je beta-laktamski antibiotik izabran iz grupe koja se sastoji od imipenema, ertapenema, meropenema, doripenema, biapenema, panipenema, tikarcilina, ampicilina, amoksicilina, karbenicilina, piperacilina, azlocilina, mezlocilina, cefoperazona, cefotaksima, ceftriaksona, cefipima, ceftolozana i ceftazidima.
24. Farmaceutski pripravak prema bilo kojem od patentnih zahtjeva 18-20 i 22-23, naznačen time što beta-laktamski antibiotik je imipenem.
25. Farmaceutski pripravak prema patentnom zahtjevu 24, koji dalje sadrži cilastatin ili njegovu farmaceutski prihvatljivu sol.
26. Spoj prema bilo kojem od patentnih zahtjeva 1-16 ili njegova farmaceutski prihvatljiva sol za uporabu u liječenju ljudskog tijela terapijom.
27. Spoj prema bilo kojem od patentnih zahtjeva 1 do 16, ili njegova farmaceutski prihvatljiva sol, u kombinaciji sa beta-laktamskim antibiotikom ili farmaceutski pripravak prema bilo kojem od patentnih zahtjeva 17 do 25 za uporabu u liječenju bakterijske infekcije.
28. Spoj za uporabu prema patentnom zahtjevu 27, naznačen time što je beta-laktamski antibiotik izabran iz grupe koja se sastoji od imipenema, ertapenema, meropenema, doripenema, biapenema, panipenema, tikarcilina, ampicilina, amoksicilina, karbenicilina, piperacilina, azlocilina, mezlocilina, cefoperazona, cefotaksima, ceftriaksona, cefipima, ceftolozana i ceftazidima.
29. Spoj za uporabu prema patentnom zahtjevu 27, naznačen time što beta-laktamski antibiotik je imipenem.
30. Spoj prema bilo kojem od patentnih zahtjeva 1 do 16, ili njegova farmaceutski prihvatljiva sol, i terapeutski efikasna količina imipenema, cilastatina i relebaktama za uporabu u liječenju bakterijske infekcije.
31. Spoj za uporabu prema patentnom zahtjevu 27-30, naznačen time što je bakterijska infekcija posljedica Pseudomonas spp., Klebsiella spp., Enterobacter spp., Escherichi spp., Morganella spp., Citrobacter spp., Serratia, spp. ili Acintetobacter spp.
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