ME01421B - 5-supstituisani derivati kinazolinona kao protivtumorska sredstva - Google Patents

5-supstituisani derivati kinazolinona kao protivtumorska sredstva

Info

Publication number
ME01421B
ME01421B MEP-2012-60A MEP6012A ME01421B ME 01421 B ME01421 B ME 01421B ME P6012 A MEP6012 A ME P6012A ME 01421 B ME01421 B ME 01421B
Authority
ME
Montenegro
Prior art keywords
optionally substituted
alkyl
halogens
stereoisomer
solvate
Prior art date
Application number
MEP-2012-60A
Other languages
English (en)
Inventor
George W Muller
Hon-Wah Man
Original Assignee
Celgene Corp
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 Celgene Corp filed Critical Celgene Corp
Publication of ME01421B publication Critical patent/ME01421B/me

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    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
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Abstract

Spoj formule (II) ili njegova farmaceutski prihvatljiva sol, solvat ili stereoizomer, naznačen time što: R4 je:halogen; -(CH2)nOH; (C1-C6)alkil, izborno supstituisan s jednim ili više halogena; ili (C1-C6)alkoksi, izborno supstituisan s jednim ili više halogena;R5 je: vodonik: -(CH2)nOH; fenil; -O-( C1-C6)alkil; ili (C1-C6)alkil, izborno supstituisan s jednimili više halogena; R6je: vodonik; ili (C1-C6)alkil, izborno supstituisan s jednim ili višehalogena; i n je 0, 1 ili 2.Patent sadrži još 13 patentnih zahtjeva.

Claims (14)

1. Spoj formule (II): ili njegova farmaceutski prihvatljiva sol, solvat ili stereoizomer, naznačen time što: R4 je: halogen; -(CH2)nOH; (C1-C6)alkil, izborno supstituiran s jednim ili više halogena; ili (C1-C6)alkoksi, izborno supstituiran s jednim ili više halogena; R5 je: vodik; -(CH2)nOH; fenil; -0-(C1-C6)alkil; ili (C1-C6)alkil, izborno supstituiran s jednim ili više halogena; R6 je: vodik; ili (C1-C6)alkil, izborno supstituiran s jednim ili više halogena; i nje 0, 1 ili 2.
2.    Spoj u skladu s patentnim zahtjevom 1, ili njegova farmaceutski prihvatljiva sol, solvat ili stereoizomer, naznačen time što R4 je metil ili metoksi; ili što R4 je F ili Cl; ili što R4 je -CF3.
3.    Spoj u skladu s patentnim zahtjevom 1, naznačen time što je: ili njegova farmaceutski prihvatljiva sol, solvat ili stereoizomer.
4. Spoj formule (III): ili njegova farmaceutski prihvatljiva sol, solvat ili stereoizomer, naznačen time što: Rd je: vodik; (C1-C6)alkil, izborno supstituiran s jednim ili više halogena; -C(0)-(C1-C6)alkil, gdje je alkil izborno supstituiran s jednim ili više halogena; -C(OMCH2)n-(C3-C10-cikloalkil); -C(0)-(CH2)n-NReRf, gdje su Re i Rf međusobno neovisno: vodik; (C1-C6)alkil, izborno supstituiran s jednim ili više halogena; ili (C1-C6)alkoksi, izborno supstituiran s jednim ili više halogena; ili -C(0)-(CH2)n-0-(C1-C6)alkil; R7 je: vodik; -(CH2)nOH; fenil; -0-(C1-C6)alkil; ili (C1-C6)alkil, izborno supstituiran s jednim ili više halogena; R8 je: vodik; ili (C1-C6)alkil, izborno supstituiran s jednim ili više halogena; i nje 0, 1 ili 2.
5. Spoj u skladu s patentnim zahtjevom 4, ili njegova farmaceutski prihvatljiva sol, solvat ili stereoizomer, naznačen time što R7 je metil.
6. Spoj u skladu s patentnim zahtjevom 4, ili njegova farmaceutski prihvatljiva sol, solvat ili stereoizomer, naznačen time što Rd je -C(0)-(C1-C6)alkil; ili što Rd je -C(0)-CH2-0-(C1-C6)alkil.
7. Spoj u skladu s patentnim zahtjevom 4, naznačen time što je: ili njegova farmaceutski prihvatljiva sol, solvat ili stereoizomer.
8. Spoj formule (IV): ili njegova farmaceutski prihvatljiva sol, solvat ili stereoizomer, naznačen time što: R8 je: -(CH2)n-(6- do 10-eročlani aril); -C(0)-(CH2)n-(6- do 10-eročlani aril) ili -C(0)-(CH2)n-(6- do 10-eročlani heteroaril), gdje je aril ili heteroaril izborno supstituiran s jednim ili više: halogena; -SCF3; (C1-C6)alkila, koji je i sam izborno supstituiran s jednim ili više halogena; ili (C1-C6)alkoksi, koji je i sam izborno supstituiran s jednim ili više halogena; -C(0)-(CH2)n-NHRh, gdje Rh je: 6- do 10-eročlani aril, izborno supstituiran s jednim ili više: halogena; (C1-C6)alkil, koji je i sam izborno supstituiran s jednim ili više halogena; ili (C1-C6)alkoksi, koji je i sam izborno supstituiran s jednim ili više halogena; ili -C(0)-(CH2)n-0-(CH2)n-(6- do 10-eročlani aril); R9 je: vodik; -(CH2)nOH; fenil; -0-(C1-C6)alkil; ili (C1-C6)alkil, izborno supstituiran s jednim ili više halogena; R10 je: vodik; ili (C1-C6)alkil, izborno supstituiran s jednim ili više halogena; i n je 0, 1 ili 2.
9. Spoj u skladu s patentnim zahtjevom 8, naznačen time što R9 je metil.
10. Spoj u skladu s patentnim zahtjevom 8, naznačen time što RB je -C(0)-fenil, -C(0)-CH2-fenil, ili -C(0)-NH-fenil; gdje fenil može biti izborno supstituiran s jednim ili više metila, -CF3 ili halogena.
11. Spoj u skladu s patentnim zahtjevom 8, naznačen time što je: ili njegova farmaceutski prihvatljiva sol, solvat ili stereoizomer.
12. Farmaceutski pripravak, naznačen time što sadrži spoj u skladu s bilo kojim od patentnih zahtjeva I do II, ili njegovu farmaceutski prihvatljivu sol, solvat ili stereoizomer.
13. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 11, ili njegova farmaceutski prihvatljiva sol, solvat ili stereoizomer, naznačen time što je namijenjen upotrebi u liječenju, managing ili sprječavanje bolesti ili poremećaja, gdje je bolest ili poremećaj rak, poremećaj povezan s angiogenezom, bol, makularna degeneracija ili srodan sindrom, kožna bolest, plućni poremećaj, poremećaj povezan s azbestom, parazitarna bolest, poremećaj imunodeficijencije, poremećaj CNS-a, ozljeda CNS-a, ateroskleroza ili srodan poremećaj, disfunkcionalan san ili srodan poremećaj, hemoglobinopatija ili srodan poremećaj, ili poremećaj povezan s TNFα.
14. Spoj u skladu s patentnim zahtjevom 13, naznačen time što ga se pripravlja za primjenu uz drugo aktivno sredstvo.
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