HRP20110441T1 - Derivati 2-benzilpiridazinona kao inhibitori met kinaze - Google Patents
Derivati 2-benzilpiridazinona kao inhibitori met kinaze Download PDFInfo
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- HRP20110441T1 HRP20110441T1 HR20110441T HRP20110441T HRP20110441T1 HR P20110441 T1 HRP20110441 T1 HR P20110441T1 HR 20110441 T HR20110441 T HR 20110441T HR P20110441 T HRP20110441 T HR P20110441T HR P20110441 T1 HRP20110441 T1 HR P20110441T1
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- FPYJSJDOHRDAMT-KQWNVCNZSA-N 1h-indole-5-sulfonamide, n-(3-chlorophenyl)-3-[[3,5-dimethyl-4-[(4-methyl-1-piperazinyl)carbonyl]-1h-pyrrol-2-yl]methylene]-2,3-dihydro-n-methyl-2-oxo-, (3z)- Chemical compound C=1C=C2NC(=O)\C(=C/C3=C(C(C(=O)N4CCN(C)CC4)=C(C)N3)C)C2=CC=1S(=O)(=O)N(C)C1=CC=CC(Cl)=C1 FPYJSJDOHRDAMT-KQWNVCNZSA-N 0.000 title 1
- FSXKVYGFNNIDBZ-UHFFFAOYSA-N 2-benzylpyridazin-3-one Chemical class O=C1C=CC=NN1CC1=CC=CC=C1 FSXKVYGFNNIDBZ-UHFFFAOYSA-N 0.000 title 1
- 229940043355 kinase inhibitor Drugs 0.000 title 1
- 239000003757 phosphotransferase inhibitor Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims abstract 18
- 150000003839 salts Chemical class 0.000 claims abstract 18
- 239000000203 mixture Substances 0.000 claims abstract 16
- 125000004433 nitrogen atom Chemical group N* 0.000 claims abstract 12
- 125000004430 oxygen atom Chemical group O* 0.000 claims abstract 12
- CURLTUGMZLYLDI-UHFFFAOYSA-N Carbon dioxide Chemical compound O=C=O CURLTUGMZLYLDI-UHFFFAOYSA-N 0.000 claims abstract 10
- 125000004432 carbon atom Chemical group C* 0.000 claims abstract 10
- MZAGXDHQGXUDDX-JSRXJHBZSA-N (e,2z)-4-ethyl-2-hydroxyimino-5-nitrohex-3-enamide Chemical compound [O-][N+](=O)C(C)C(/CC)=C/C(=N/O)/C(N)=O MZAGXDHQGXUDDX-JSRXJHBZSA-N 0.000 claims abstract 8
- 229920006395 saturated elastomer Polymers 0.000 claims abstract 6
- 125000004434 sulfur atom Chemical group 0.000 claims abstract 6
- 125000000217 alkyl group Chemical group 0.000 claims abstract 5
- 125000000623 heterocyclic group Chemical group 0.000 claims abstract 5
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims abstract 5
- 125000003118 aryl group Chemical group 0.000 claims abstract 4
- ZUOUZKKEUPVFJK-UHFFFAOYSA-N diphenyl Chemical compound C1=CC=CC=C1C1=CC=CC=C1 ZUOUZKKEUPVFJK-UHFFFAOYSA-N 0.000 claims abstract 4
- 235000010290 biphenyl Nutrition 0.000 claims abstract 2
- 239000004305 biphenyl Substances 0.000 claims abstract 2
- 125000001624 naphthyl group Chemical group 0.000 claims abstract 2
- 229910052760 oxygen Inorganic materials 0.000 claims abstract 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims abstract 2
- RWRDLPDLKQPQOW-UHFFFAOYSA-N Pyrrolidine Chemical compound C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 claims 6
- YNAVUWVOSKDBBP-UHFFFAOYSA-N Morpholine Chemical compound C1COCCN1 YNAVUWVOSKDBBP-UHFFFAOYSA-N 0.000 claims 4
- GLUUGHFHXGJENI-UHFFFAOYSA-N Piperazine Chemical compound C1CNCCN1 GLUUGHFHXGJENI-UHFFFAOYSA-N 0.000 claims 4
- NQRYJNQNLNOLGT-UHFFFAOYSA-N Piperidine Chemical compound C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 claims 4
- 125000002541 furyl group Chemical group 0.000 claims 4
- 125000002883 imidazolyl group Chemical group 0.000 claims 4
- 125000001786 isothiazolyl group Chemical group 0.000 claims 4
- 125000000842 isoxazolyl group Chemical group 0.000 claims 4
- 125000001715 oxadiazolyl group Chemical group 0.000 claims 4
- 125000002971 oxazolyl group Chemical group 0.000 claims 4
- 125000003226 pyrazolyl group Chemical group 0.000 claims 4
- 125000004076 pyridyl group Chemical group 0.000 claims 4
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 4
- 125000000168 pyrrolyl group Chemical group 0.000 claims 4
- 125000003831 tetrazolyl group Chemical group 0.000 claims 4
- 125000001113 thiadiazolyl group Chemical group 0.000 claims 4
- 125000000335 thiazolyl group Chemical group 0.000 claims 4
- 125000001544 thienyl group Chemical group 0.000 claims 4
- 125000001425 triazolyl group Chemical group 0.000 claims 4
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 3
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 3
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 3
- 206010028980 Neoplasm Diseases 0.000 claims 2
- 239000003795 chemical substances by application Substances 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 2
- 125000002950 monocyclic group Chemical group 0.000 claims 2
- 125000002757 morpholinyl group Chemical group 0.000 claims 2
- 125000004193 piperazinyl group Chemical group 0.000 claims 2
- 125000003386 piperidinyl group Chemical group 0.000 claims 2
- 125000003373 pyrazinyl group Chemical group 0.000 claims 2
- 125000002098 pyridazinyl group Chemical group 0.000 claims 2
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 2
- 239000000126 substance Substances 0.000 claims 2
- 239000002253 acid Substances 0.000 claims 1
- 230000010933 acylation Effects 0.000 claims 1
- 238000005917 acylation reaction Methods 0.000 claims 1
- 239000000654 additive Substances 0.000 claims 1
- 230000029936 alkylation Effects 0.000 claims 1
- 238000005804 alkylation reaction Methods 0.000 claims 1
- 125000003277 amino group Chemical group 0.000 claims 1
- 238000006254 arylation reaction Methods 0.000 claims 1
- 210000004369 blood Anatomy 0.000 claims 1
- 239000008280 blood Substances 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 230000032050 esterification Effects 0.000 claims 1
- 238000005886 esterification reaction Methods 0.000 claims 1
- 238000007327 hydrogenolysis reaction Methods 0.000 claims 1
- 210000000987 immune system Anatomy 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 238000003797 solvolysis reaction Methods 0.000 claims 1
- LMBFAGIMSUYTBN-MPZNNTNKSA-N teixobactin Chemical compound C([C@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H](CCC(N)=O)C(=O)N[C@H]([C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H]1C(N[C@@H](C)C(=O)N[C@@H](C[C@@H]2NC(=N)NC2)C(=O)N[C@H](C(=O)O[C@H]1C)[C@@H](C)CC)=O)NC)C1=CC=CC=C1 LMBFAGIMSUYTBN-MPZNNTNKSA-N 0.000 claims 1
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- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing aromatic rings
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Abstract
Spojevi prema formuli I naznačeni time daR1 označava H ili A, R2 označava nezasićeni, zasićeni ili aromatski 5- ili 6-člani heterocikal koji ima 1 do 4 N, O i/ili S atoma, koji mogu biti nesupstituirani ili mono-, di- ili tri-supstituirani sa Hal, A, [C(R3)2]nOR3, N=CR3N(R3)2, SR3, NO2, CN, COOR3, CON(R3)2, NR3COA, NR3SO2A, SO2N(R3)2, S(O)mA, [C(R3)2]nN(R3)2, [C(R3)2]nHet, O[C(R3)2]nN(R3)2, O[C(R3)2]nHet, S[C(R3)2]nN(R3)2, S[C(R3)2]nHet, NR3[C(R3)2]nN(R3)2, NR3[C(R3)2]nHet, NHCON(R3)2, NHCONH[C(R3)2]nN(R3)2, NHCONH[C(R3)2]nHet, [C(R3)2]nNHCO[C(R3)2]nN(R3)2, [C(R3)2]nNHCO[C(R3)2]nHet, CON(R3)2, CONR3[C(R3)2]nN(R3)2, CONR3[C(R3)2]nNR3COOA, CONR3[C(R3)2]nOR3, CONR3[C(R3)2]nHet, COHet, COA i/ili =O (karbonil kisik), R3 označava H ili A, R4,R4' svaki, nezavisno jedan od drugoga, označava H, Hal, A, OR3, CN, COOR3, CON(R3)2, NR3COA, NR3SO2A, SO2N(R3)2 ili S(O)mA, Ar označava fenil, naftil ili bifenil, svaki od kojih je nesupstituiran ili mono-, di- ili tri-supstituiran sa Hal, A, [C(R3)2]nOR3, [C(R3)2]nN(R3)2, SR3, NO2, CN, COOR3, CON(R3)2, NR3COA, NR3SO2A, SO2N(R3)2, S(O)mA, CO-Het, Het, O[C(R3)2]nN(R3)2, O[C(R3)2]nHet, NHCOOA, NHCON(R3)2, NHCOO[C(R3)2]nN(R3)2, NHCOO[C(R3)2]nHet, NHCONH[C(R3)2]nN(R3)2, NHCONH[C(R3)2]nHet, OCONH[C(R3)2]nN(R3)2, OCONH[C(R3)2]nHet, CONR3[C(R3)2]nN(R3)2, CONR3[C(R3)2]nHet i/ili COA, Het označava a mono-, bi- ili triciklički zasićeni, nezasićeni ili aromatski heterocikal koji ima 1 do 4 N, O i/ili S atoma, koji mogu biti nesupstituirani ili mono-, di- ili tri- supstituirani sa Hal, A, [C(R3)2]nOR3, [C(R3)2]nN(R3)2, SR3, NO2, CN, COOR3, CON(R3)2, NR3COA, NR3SO2A, SO2N(R3)2, S(O)mA, CO-Het1, [C(R3)2]nHet1, O[C(R3)2]n- N(R3)2, O[C(R3)2]nHet1, NHCOOA, NHCON(R3)2, NHCOO[C(R3)2]nN(R3)2, NHCOO[C(R3)2]nHet1 NHCONH[C(R3)2]nN(R3)2, NHCONH[C(R3)2]nHet1, OCONH[C(R3)2]nN(R3)2, OCONH[C(R3)2]nHet1, CO-Het1, CHO, COA, =S, =NH, =NA i/ili =O (karbonil oksi- gen), Het1 označava monociklički zasićeni heterocikal koji ima 1 do 2 N i/ili O atoma, koji mogu biti mono- ili di-supstituirani sa A, OA, OH, Hal i/ili =O (karbonil kisik), A označava nerazgranati ili razgranati alkil koji ima 1-10 C atoma, gdje 1-7 H atoma mogu biti zamijenjeni sa F i/ili gdje jedna ili dvije ne-susjedne CH2 skupine mogu biti zamijenjene sa O NH, S, SO, SO2 i/ili sa CH=CH skupinama, ili cikličkim alkilom koji ima 3-7 C atoma, Hal označava F, Cl, Br ili I, m označava 0, 1 ili 2, n označava 0, 1, 2, 3 ili 4, i njihove farmaceutski korisne soli, tautomeri i stereoizomeri, uključujući njihove mješavine u svim omjerima. Patent sadrži još 15 patentnih zahtjeva.
Claims (16)
1. Spojevi prema formuli I
[image]
naznačeni time da
R1 označava H ili A,
R2 označava nezasićeni, zasićeni ili aromatski 5- ili 6-člani heterocikal koji ima 1 do 4 N, O i/ili S atoma, koji mogu biti nesupstituirani ili mono-, di- ili tri-supstituirani sa Hal, A, [C(R3)2]nOR3, N=CR3N(R3)2, SR3, NO2, CN, COOR3, CON(R3)2, NR3COA, NR3SO2A, SO2N(R3)2, S(O)mA, [C(R3)2]nN(R3)2, [C(R3)2]nHet, O[C(R3)2]nN(R3)2, O[C(R3)2]nHet, S[C(R3)2]nN(R3)2, S[C(R3)2]nHet, NR3[C(R3)2]nN(R3)2, NR3[C(R3)2]nHet, NHCON(R3)2, NHCONH[C(R3)2]nN(R3)2, NHCONH[C(R3)2]nHet, [C(R3)2]nNHCO[C(R3)2]nN(R3)2, [C(R3)2]nNHCO[C(R3)2]nHet, CON(R3)2, CONR3[C(R3)2]nN(R3)2, CONR3[C(R3)2]nNR3COOA, CONR3[C(R3)2]nOR3, CONR3[C(R3)2]nHet, COHet, COA i/ili =O (karbonil kisik),
R3 označava H ili A,
R4,R4' svaki, nezavisno jedan od drugoga, označava H, Hal, A, OR3, CN, COOR3, CON(R3)2, NR3COA, NR3SO2A, SO2N(R3)2 ili S(O)mA,
Ar označava fenil, naftil ili bifenil, svaki od kojih je nesupstituiran ili mono-, di- ili tri-supstituiran sa Hal, A, [C(R3)2]nOR3, [C(R3)2]nN(R3)2, SR3, NO2, CN, COOR3, CON(R3)2, NR3COA, NR3SO2A, SO2N(R3)2, S(O)mA, CO-Het, Het, O[C(R3)2]nN(R3)2, O[C(R3)2]nHet, NHCOOA, NHCON(R3)2, NHCOO[C(R3)2]nN(R3)2, NHCOO[C(R3)2]nHet, NHCONH[C(R3)2]nN(R3)2, NHCONH[C(R3)2]nHet, OCONH[C(R3)2]nN(R3)2, OCONH[C(R3)2]nHet, CONR3[C(R3)2]nN(R3)2, CONR3[C(R3)2]nHet i/ili COA,
Het označava a mono-, bi- ili triciklički zasićeni, nezasićeni ili aromatski heterocikal koji ima 1 do 4 N, O i/ili S atoma, koji mogu biti nesupstituirani ili mono-, di- ili tri- supstituirani sa Hal, A, [C(R3)2]nOR3, [C(R3)2]nN(R3)2, SR3, NO2, CN, COOR3, CON(R3)2, NR3COA, NR3SO2A, SO2N(R3)2, S(O)mA, CO-Het1, [C(R3)2]nHet1, O[C(R3)2]n- N(R3)2, O[C(R3)2]nHet1, NHCOOA, NHCON(R3)2, NHCOO[C(R3)2]nN(R3)2, NHCOO[C(R3)2]nHet1 NHCONH[C(R3)2]nN(R3)2, NHCONH[C(R3)2]nHet1, OCONH[C(R3)2]nN(R3)2, OCONH[C(R3)2]nHet1, CO-Het1, CHO, COA, =S, =NH, =NA i/ili =O (karbonil oksi- gen),
Het1 označava monociklički zasićeni heterocikal koji ima 1 do 2 N i/ili O atoma, koji mogu biti mono- ili di-supstituirani sa A, OA, OH, Hal i/ili =O (karbonil kisik),
A označava nerazgranati ili razgranati alkil koji ima 1-10 C atoma, gdje 1-7 H atoma mogu biti zamijenjeni sa F i/ili gdje jedna ili dvije ne-susjedne CH2 skupine mogu biti zamijenjene sa O NH, S, SO, SO2 i/ili sa CH=CH skupinama, ili cikličkim alkilom koji ima 3-7 C atoma,
Hal označava F, Cl, Br ili I,
m označava 0, 1 ili 2,
n označava 0, 1, 2, 3 ili 4,
i njihove farmaceutski korisne soli, tautomeri i stereoizomeri, uključujući njihove mješavine u svim omjerima.
2. Spojevi prema zahtjevu 1 naznačeni time da
R2 označava nezasićeni ili aromatski 5- ili 6-člani heterocikal koji ima 1 do 4 N i/ili O atoma, koji mogu biti nesupstituirani ili mono-, di- ili trisupstituirani sa Hal, A, [C(R3)2]nN(R3)2, [C(R3)2]nHet, O[C(R3)2]nN(R3)2 i/ili O[C(R3)2]nHet,
i njihove farmaceutski korisne soli, tautomeri i stereoizomeri, uključujući njihove mješavine u svim omjerima.
3. Spojevi prema zahtjevu 1 ili 2 naznačeni time da
R4, R4' označava H,
i njihove farmaceutski korisne soli, tautomeri i stereoizomeri, uključujući njihove mješavine u svim omjerima.
4. Spojevi prema jednom ili više od zahtjeva 1-3 naznačeni time da
Het označava monociklički zasićeni, nezasićeni ili aromatski heterocikal koji ima 1 do 4 N, O i/ili S atoma, koji mogu biti nesupstituirani ili mono-, di- ili tri-supstituirani sa A i/ili [C(R3)2]nHet1,
i njihove farmaceutski korisne soli, tautomeri i stereoizomeri, uključujući njihove mješavine u svim omjerima.
5. Spojevi prema jednom ili više od zahtjeva 1-4 naznačeni time da
A označava nerazgranati ili razgranati alkil koji ima 1-8 C atoma, gdje 1-7 H atoma mogu biti zamijenjeni sa F i/ili Cl,
ili
ciklički alkil koji ima 3-7 C atoma,
i njihove farmaceutski korisne soli, tautomeri i stereoizomeri, uključujući njihove mješavine u svim omjerima.
6. Spojevi prema jednom ili više od zahtjeva 1-5 naznačeni time da
R3 označava H, metil, etil ili propil,
i njihove farmaceutski korisne soli, tautomeri i stereoizomeri, uključujući njihove mješavine u svim omjerima.
7. Spojevi prema jednom ili više od zahtjeva 1-6 naznačeni time da
Het1 označava monociklički zasićeni heterocikal koji ima 1 do 2 N i/ili O atoma, koji mogu biti mono- ili di-supstituirani sa A i/ili =O (karbonil kisik),
i njihove farmaceutski korisne soli, tautomeri i stereoizomeri, uključujući njihove mješavine u svim omjerima.
8. Spojevi prema jednom ili više od zahtjeva 1-7 naznačeni time da
R2 označava furil, tienil, pirolil, imidazolil, pirazolil, oksazolil, izoksazolil, tiazolil, izotiazolil, piridil, pirimidinil, triazolil, tetrazolil, oksadiazolil ili tiadiazolil, svaki od kojih je monosupstituiran sa Hal, A, [C(R3)2]nN(R3)2, [C(R3)2]nHet, O[C(R3)2]nN(R3)2 ili O[C(R3)2]nHet,
i njihove farmaceutski korisne soli, tautomeri i stereoizomeri, uključujući njihove mješavine u svim omjerima.
9. Spojevi prema jednom ili više od zahtjeva 1-8 naznačeni time da
Het označava piperidinil, piperazinil, pirolidinil, morfolinil, furil, tienil, pirolil, imidazolil, pirazolil, oksazolil, izoksazolil, tiazolil, izotiazolil, piridil, pirimidinil, triazolil, tetrazolil, oksadiazolil, tiadiazolil, piridazinil ili pirazinil, svaki od kojih je monosupstituiran sa A ili [C(R3)2]nHet1,
i njihove farmaceutski korisne soli, tautomeri i stereoizomeri, uključujući njihove mješavine u svim omjerima.
10. Spojevi prema jednom ili više od zahtjeva 1-9 naznačeni time da
Het1 označava pirolidin, piperidin, piperazin ili morfolin, svaki od kojih je nesupstituiran ili mono- ili di-supstituiran sa A i/ili =O (karbonil kisik),
i njihove farmaceutski korisne soli, tautomeri i stereoizomeri, uključujući njihove mješavine u svim omjerima.
11. Spojevi prema jednom ili više od zahtjeva 1-10 naznačeni time da
R1 označava H ili A,
R2 označava nezasićeni ili aromatski 5- ili 6-člani heterocikal koji ima 1 do 4 N i/ili O atoma, koji mogu biti nesupstituirani ili mono-, di- ili trisupstituirani sa Hal, A, [C(R3)2]nN(R3)2, [C(R3)2]nHet, O[C(R3)2]nN(R3)2 i/ili O[C(R3)2]nHet,
R3 označava H, metil, etil ili propil,
R4 R4' označava H,
Het označava monociklički zasićeni, nezasićeni ili aromatski heterocikal koji ima 1 do 4 N, O i/ili S atoma, koji mogu biti nesupstituirani ili mono-, di- ili tri-supstituirani sa A i/ili [C(R3)2]nHet1,
Het1 označava monociklički zasićeni heterocikal koji ima 1 do 2 N i/ili O atoma, koji mogu biti mono- ili di-supstituirani sa A i/ili =O (karbonil kisik),
A označava nerazgranati ili razgranati alkil koji ima 1-8 C atoma, gdje 1-7 H atoma može biti zamijenjeno sa F i/ili Cl,
ili
ciklički alkil koji ima 3-7 C atoma,
Hal označava F, Cl, Br ili 1,
n označava 0, 1, 2, 3 ili 4,
i njihove farmaceutski korisne soli, tautomeri i stereoizomeri, uključujući njihove mješavine u svim omjerima.
12. Spojevi prema jednom ili više od zahtjeva 1-11 naznačeni time da
R1 označava H ili A,
R2 označava furil, tienil, pirolil, imidazolil, pirazolil, oksazolil, izoksazolil, tiazolil, izotiazolil, piridil, pirimidinil, triazolil, tetrazolil, oksadiazolil ili tiadiazolil, svaki od kojih je monosupstituiran sa Hal, A, [C(R3)2]nN(R3)2, [C(R3)2]nHet, O[C(R3)2]nN(R3)2 ili O[C(R3)2]nHet,
R3 označava H, metil, etil ili propil,
R4, R4' označavaju H,
Het označava piperidinil, piperazinil, pirolidinil, morfolinil, furil, tienil, pirolil, imidazolil, pirazolil, oksazolil, izoksazolil, tiazolil, izotiazolil, piridil, pirimidinil, triazolil, tetrazolil, oksadiazolil, tiadiazolil, piridazinil ili pirazinil, svaki od kojih je monosupstituiran sa A ili [C(R3)2]nHet1,
Het1označava pirolidin, piperidin, piperazin ili morfolin, svaki od kojih je nesupstituiran ili mono- ili di-supstituiran sa A i/ili =O (karbonil kisik),
A označava nerazgranati ili razgranati alkil koji ima 1-8 C atoma, gdje 1-7 H atoma može biti zamijenjeno sa F i/ili Cl,
ili
ciklički alkil koji ima 3-7 C atoma,
Hal označava F, Cl, Br ili I,
n označava 0, 1, 2, 3 ili 4,
i njihove farmaceutski korisne soli, tautomeri i stereoizomeri, uključujući njihove mješavine u svim omjerima.
13. Spojevi prema zahtjevu 1, naznačeni time da su odabrani iz skupine :
[image]
i farmaceutski korisne soli, tautomeri i stereoizomeri, uključujući njihove mješavine u svim omjerima.
14. Postupak za pripremu spojeva prema formuli I prema zahtjevima 1-13 i njihovih farmaceutski korisnih soli, tautomera i stereoizomera, naznačen time da
a) spoj formule II
[image]
gdje R1 ima značenje navedeno u zahtjevu 1,
reagira sa spojem formule III
[image]
gdje R2, R3, R4 i R4'imaju značenja navedena u zahtjevu 1
i
L označava Cl, Br, I ili slobodnu ili reaktivno funkcionalnu izmijenjenu OH skupinu,
ili
b) radikal R2 je pretvoren u drugi radikal R2 sa
i) arilacijom heterocikla,
ii) acilacijom ili alkilacijom amino skupine,
iii) esterifikacijom hidroksilne skupine,
ili
c) oslobađanja od jednog od svojih funkcionalnih derivata tretiranjem sa sredstvom za solvolizu ili sredstvom za hidrogenolizu,
i/ili
baza ili kiselina prema formuli I je pretvorena u jednu od njenih soli.
15. Lijekovi naznačeni time da sadrže barem jedan spoj prema formuli I u skladu sa zahtjevima 1-13 i/ili njihove farmaceutski korisne soli, tautomeri i stereoizomeri, uključujući njihove mješavine u svim omjerima, te proizvoljno pomoćne tvari i/ili kemijske dodatke.
16. Spojevi prema zahtjevima 1-13 i njihove farmaceutski korisne soli, tautomeri i stereoizomeri, uključujući njihove mješavine u svim omjerima, naznačeni time da su za upotrebu za liječenje bolesti, gdje je bolest koja se liječi solidni tumor ili tumor krvi i imunog sustava.
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| PCT/EP2008/009970 WO2009083076A1 (de) | 2007-12-21 | 2008-11-25 | 2-benzylpyridazinonderivate als met-kinasehemmer |
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2007
- 2007-12-21 DE DE102007061963A patent/DE102007061963A1/de not_active Withdrawn
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- 2008-11-25 AT AT08865961T patent/ATE506358T1/de active
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