HRP20161032T1 - Ciklički amidi kao inhibitori metap-2 - Google Patents

Ciklički amidi kao inhibitori metap-2 Download PDF

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Publication number
HRP20161032T1
HRP20161032T1 HRP20161032TT HRP20161032T HRP20161032T1 HR P20161032 T1 HRP20161032 T1 HR P20161032T1 HR P20161032T T HRP20161032T T HR P20161032TT HR P20161032 T HRP20161032 T HR P20161032T HR P20161032 T1 HRP20161032 T1 HR P20161032T1
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Croatia
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HRP20161032TT
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Timo Heinrich
Frank Zenke
Mireille Krier
Manja FRIESE-HAMIM
Jeyaprakashnarayanan SEENISAMY
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Merck Patent Gmbh
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Publication of HRP20161032T1 publication Critical patent/HRP20161032T1/hr

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    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/18—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
    • C07D207/22—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D207/24—Oxygen or sulfur atoms
    • C07D207/26—2-Pyrrolidones
    • C07D207/273—2-Pyrrolidones with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to other ring carbon atoms
    • C07D207/277—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
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Claims (11)

1. Spojevi s formulom I [image] naznačeni time da R označava NR2R4, Alk, C(=CH2)[C(R4)2]nAr2, Het2, O[C(R4)2]nAr2 ili OA, X označava CO ili CH2, Y označava CO ili CH2, R1 označava H, [C(R4)2]nAr1, (CH2)nHet, (CH2)nCyc, [C(R4)2]nCOOH, [C(R4)2]nCONHAr1, [C(R4)2]nCONH2, [C(R4)2]nNHA, [C(R4)2]nNA2, O[C(R4)2]nAr1, [C(R4)2]nOR7, [C(R4)2]nCOO(CH2)nAr1, [C(R4)2]nCOOA, [C(R4)2]nCONH[C(R4)2]pCON(R4)2 ili [C(R4)n]nCONHCR4-[(CH2)nN(R4)2]CON(R4)2, R2 označava H, [C(R4)2]nAr2, (CH2)nCOHet1, (CH2)nCOAr2, (CH2)mNA2 ili (CH2)nHet, R3 označava OH ili OCOA, R4 označava H ili alkil koji ima 1, 2, 3 ili 4 C atoma, R2 i R4 zajedno također označavaju alkilen koji ima 2, 3, 4 ili 5 C atoma, gdje CH2 skupina može također biti zamijenjena s N(CH2)mOH ili SO2 R5, R6 svaki, međusobno neovisno, označavaju H, F ili A, R5 i R6 zajedno također označavaju alkilen koji ima 2, 3, 4 ili 5 C atoma, gdje CH2 skupina može također biti zamijenjena s NCOA ili O, R7 označava H ili A, Ar1 označava fenil koji je nesupstituiran ili jednostruko-, dvostruko-, trostruko-, četverostruko- ili peterostruko supstituiran s Hal, OH, OA, CONH2, CONHA, CONA2, NHSO2A, CONHCyc, NHSO2Cyc, CONHAr2, COHet1 i/ili NASO2A, Ar2 označava fenil koji je nesupstituiran ili jednostruko-, dvostruko-, trostruko-, četverostruko- ili peterostruko supstituiran s Hal, A, CONH2 i/ili OAr3, Ar3 označava fenil koji je nesupstituiran ili jednostruko supstituiran s NH2, Het označava mono- ili biciklički zasićeni, nezasićeni ili aromatski heterocikl koji ima 1 do 4 N i/ili O i/ili S atoma koji je nesupstituiran ili je jednostruko-, dvostruko- ili trostruko- supstituiran s Hal, A, OA, CN, NH2, NHA, NA2, NO2, CN, COOH, COOA, (CH2)nCONH2, (CH2)nCONHA, (CH2)nCONA2, NHCOA, COA, CHO, Het1, SO2A, SO2NH2, SO2NHA, SO2NA2, CONHNH2, CONHAr3, =O i/ili Ar3, Het1 označava monociklički zasićeni heterocikl koji ima 1 do 4 N i/ili O i/ili S atoma koji je nesupstituiran ili je jednostruko-, dvostruko- ili trostruko- supstituiran s =O i/ili COOA, Het2 označava izoindolil, A označava nerazgranati ili razgranati alkil koji ima 1-10 C atoma, u kojem 1-7 H atoma mogu biti zamijenjeni s F, Cl, Br, OH, CHO, COA, COOA, CN, CONA2, CONHA i/ili CONH2, i/ili u kojem jedna ili dvije ne-susjedne CH i/ili CH2 skupine mogu biti zamijenjene s O, ili Cyc, Alk označava alkenil koji ima 2, 3, 4, 5 ili 6 C atoma, Cyc označava ciklički alkil koji ima 3-7 C atoma koji je nesupstituiran ili je jednostruko-, dvostruko- ili trostruko- supstituiran s NHCOA, NHSO2 OH, OA, A, NH2, NHA, NA2, COOA, COOH i/ili CONHA, Hal označava F, Cl, Br ili I, m označava 1, 2, 3 ili 4, n označava 0, 1, 2, 3 ili 4, p označava 1, 2 ili 3, i njihove farmaceutski korisne soli, tautomeri i stereoizomeri, uključujući njihove smjese u svim omjerima, gdje su isključeni sljedeći spojevi: metil 3-hidroksipiperidin-3-karboksilat, 1-tert-butil 3-metil 3-hidroksipiperidin-1,3-dikarboksilat, tert-butil 3-allil-3-hidroksipirolidin-1-karboksilat, tert-butil 3-allil-3-hidroksipiperidin-1-karboksilat.
2. Spojevi prema zahtjevu 1 naznačeni time da Het označava pirazinil, pirazolil, benzimidazolil, piridil, indolil, dihidroindolil, benzofuranil, tetrahidropiranil, dihidrokinolinil, dihidroizokinolinil, tetrahidrokinolinil, tetrahidroizokinolinil, indazolil, imidazolil, pirolil, oksazolil, oksadiazolil, izoksazolil, benzotiazolil, piperidin-1-il, pirolidin-1-il, 3,4-dihidro-2H-pirido[3,2-b]-1,4-oksazinil, 3,4-dihidro-2H-benzo-1,4-oksazinil, benzofuranil, azetidinil, 3-azabiciklo[3.2.0]heksil, pirol[2,3-b]piridinil, tetrahidrofuranil, tetrahidro-1,8-naftiridinil, 2,3-dihidrobenzoizotiazolil, 1,2,3,4-tetrahidrobenzotiazinil ili heksahidrobenzo-1,3-dioksolil, svaki od kojih je nesupstituiran ili je jednostruko-, dvostruko- ili trostruko- supstituiran s Hal, A, OA, CN, NH2, NHA, NA2, NO2, CN, COOH, COOA, (CH2)nCONH2, (CH2)n-CONHA, (CH2)nCONA2, NHCOA, COA, CHO, Het1, SO2A, SO2NH2, SO2NHA, SO2NA2, CONHNH2, CONHAr3, =O i/ili Ar3, i njihove farmaceutski korisne soli, tautomeri i stereoizomeri, uključujući njihove smjese u svim omjerima.
3. Spojevi prema zahtjevu 1 ili 2 naznačeni time da Het1 označava piridazinil, pirazolil, piridil, piperazinil, morfolinil, pirimidinil, furil, tienil, imidazolil, pirolil, oksazolil, oksadiazolil, izoksazolil, tiazolil, triazolil, tetrazolil, tiadiazol, piperidin-1-il, pirolidin-1-il, tetrahidropiranil, 1,2-oksazinan-2-il, 1,2,5-oksadiazinan-2-il, 1,3-oksazinan-3-il ili heksahidropirimidinil, svaki od kojih je nesupstituiran ili je jednostruko-, dvostruko- ili trostruko- supstituiran s A i/ili OA, i njihove farmaceutski korisne soli, tautomeri i stereoizomeri, uključujući njihove smjese u svim omjerima.
4. Spojevi prema zahtjevu 1 naznačeni time da R označava NR2R4, Alk, C(=CH2)[C(R4)2]nAr2, Het2, O[C(R4)2]n-Ar2 ili OA, X označava CO ili CH2, Y označava CO ili CH2, R1 označava H, [C(R4)2]nAr1, (CH2)nHet, (CH2)nCyc, [C(R4)2]n-COOH, [C(R4)2]nCONHAr1, [C(R4)2]nCONH2, [C(R4)2]nNHA, [C(R4)2]nNA2, O[C(R4)2]nAr1, [C(R4)2]nOR7, [C(R4)2]nCOO-(CH2)nAr1 [C(R4)2]nCOOA, [C(R4)2]nCONH[C(R4)2]p-CON(R4)2 ili [C(R4)2]nCONHCR4[(CH2)nN(R4)2]CON(R4)2, R2 označava H, [C(R4)2]nAr2, (CH2)nCOHet1, (CH2)nCOAr2, (CH2)mNA2 ili (CH2)nHet, R3 označava OH ili OCOA, R4 označava H ili alkil koji ima 1, 2, 3 ili 4 C atoma, R2 i R4 zajedno također označavaju alkilen koji ima 2, 3, 4 ili 5 C atoma, gdje CH2 skupina može također biti zamijenjena s N(CH2)mOH ili SO2, R5, R6 svaki, međusobno neovisno, označavaju H, F ili A, R5 i R6 zajedno također označavaju alkilen koji ima 2, 3, 4 ili 5 C atoma, gdje CH2 skupina može također biti zamijenjena s NCOA ili O, R7 označava H ili A, Ar1 označava fenil koji je nesupstituiran ili jednostruko-, dvostruko-, trostruko-, četverostruko- ili peterostruko supstituiran s Hal, OH, OA, CONH2, CONHA, CONA2, NHSO2A, CONHCyc, NHSO2Cyc, CONHAr2, COHet1 i/ili NASO2A, Ar2 označava fenil koji je nesupstituiran ili jednostruko-, dvostruko-, trostruko-, četverostruko- ili peterostruko supstituiran s Hal, A, CONH2 i/ili OAr3, Ar3 označava fenil koji je nesupstituiran ili jednostruko supstituiran s NH2, Het označava pirazinil, pirazolil, benzimidazolil, piridil, indolil, dihidroindolil, benzofuranil, tetrahidropiranil, , dihidroizokinolinil, tetrahidrokinolinil, tetrahidroizokinolinil, indazolil, imidazolil, pirolil, oksazolil, oksadiazolil, izoksazolil, benzotiazolil, piperidin-1-il, pirolidin-1-il, 3,4-dihidro-2H-pirido[3,2-b]-1,4-oksazinil, 3,4-dihidro-2H-benzo-1,4-oksazinil, benzofuranil, azetidinil, 3-azabiciklo[3.2.0]heksil, pirol[2,3-b]piridinil, tetrahidrofuranil, tetrahidro-1,8-naftiridinil, 2,3-dihidro-benzoizotiazolil, 1,2,3,4-tetrahidrobenzotiazinil ili heksahidrobenzo-1,3-dioksolil, svaki od kojih je nesupstituiran ili je jednostruko-, dvostruko- ili trostruko- supstituiran s Hal, A, OA, CN, NH2, NHA, NA2, NO2, CN, COOH, COOA, (CH2)nCONH2, (CH2)n-CONHA, (CH2)nCONA2, NHCOA, COA, CHO, Het1, SO2A, SO2NH2, SO2NHA, SO2NA2, CONHNH2, CONHAr3, =O i/ili Ar3, Het1 označava piridazinil, pirazolil, piridil, piperazinil, morfolinil, pirimidinil, furil, tienil, imidazolil, pirolil, oksazolil, oksadiazolil, izoksazolil, tiazolil, triazolil, tetrazolil, tiadiazol, piperidin-1-il, pirolidin-1-il, tetrahidropiranil, 1,2-oksazinan-2-il, 1,2,5-oksadiazinan-2-il, 1,3-oksazinan-3-il ili heksahidropirimidinil, svaki od kojih je nesupstituiran ili je jednostruko-, dvostruko- ili trostruko- supstituiran s A i/ili OA, Het2 označava izoindolil, A označava nerazgranati ili razgranati alkil koji ima 1-10 C atoma, u kojem 1-7 H atoma mogu biti zamijenjeni s F, Cl, Br, OH, CHO, COA, COOA, CN, CONA2, CONHA i/ili CONH2, i/ili u kojem jedna ili dvije ne-susjedne CH i/ili CH2 skupine mogu biti zamijenjene s O, ili Cyc, Alk označava alkenil koji ima 2, 3, 4, 5 ili 6 C atoma, Cyc označava ciklički alkil koji ima 3-7 C atoma koji je nesupstituiran ili je jednostruko-, dvostruko- ili trostruko- supstituiran s NHCOA, NHSO2, OH, OA, A, NH2, NHA, NA2, COOA, COOH i/ili CONHA, Hal označava F, Cl, Br ili I, m označava 1, 2, 3 ili 4, n označava 0, 1, 2, 3 ili 4, p označava 1, 2 ili 3, i njihove farmaceutski korisne soli, tautomeri i stereoizomeri, uključujući njihove smjese u svim omjerima.
5. Spojevi prema zahtjevu 1, naznačeni time da su odabrani iz skupine koja sadrži: [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] i njihove farmaceutski korisne soli, tautomeri i stereoizomeri, uključujući njihove smjese u svim omjerima.
6. Postupak za pripremanje spojeva s formulom I prema zahtjevima 1-5 i njihovih farmaceutski korisnih soli, tautomera i stereoizomera, naznačen time da a) za pripremanje spojeva s formulom I u kojoj Y označava CO i R označava NR2R4, spoj s formulom II [image] u kojoj X, R1, R3, R5, R6, R7 i p imaju značenja navedena u zahtjevu 1, i L označava Cl, Br, I ili slobodnu ili reaktivno funkcionalno modificiranu OH skupinu, reagira sa spojem s formulom III [image] u kojoj R2 i R4 imaju značenja navedena u zahtjevu 1, ili b) spoj s formulom IV [image] u kojoj R1, R5, R6, R7, R, X, Y i p imaju značenja navedena u zahtjevu 1, se oksidira, ili c) za pripremanje spojeva s formulom I u kojoj X i Y označavaju CH2, spoj s formulom I u kojoj X i Y označavaju CO se reducira, i/ili baza ili kiselina s formulom I se prevodi u jednu od njihovih soli.
7. Lijekovi naznačeni time da sadrže barem jedan spoj formule I prema zahtjevima 1-5 i/ili njihove farmaceutski korisne soli, tautomere i stereoizomere, uključujući njihove smjese u svim omjerima, te proizvoljno pomoćna sredstva i/ili adjuvante.
8. Spojevi s formulom I prema zahtjevima 1-5, i njihove farmaceutski korisne soli, tautomeri i stereoizomeri, uključujući njihove smjese u svim omjerima, naznačeni time da su za uporabu za liječenje tumora, metastaza tumora, proliferativnih bolesti mezangijalnih stanica, hemangioma, proliferativne retinopatije, reumatoidnog artritisa, aterosklerozne neovaskularizacije, psorijaze, okularne neovaskularizacije, osteoporoze, dijabetesa i pretilosti, limfoidne leukemije, limfoma, malarije i hipertrofije prostate.
9. Spojevi za uporabu za liječenje prema zahtjevu 8, naznačeni time da se tumorska bolest bira iz skupine koja sadrži tumore pločastog epitela, mokraćnog mjehura, želuca, bubrega, glave i vrata, jednjaka, vrata maternice, štitnjače, crijeva, jetre, mozga, prostate, urogenitalnog trakta, limfnog sustava, želuca, grkljana, pluća, kože, monocitnu leukemiju, adenokarcinom pluća, karcinom malih stanica pluća, rak gušterače, glioblastom, karcinom dojke, akutnu mijeloidnu leukemiju, kroničnu mijeloidnu leukemiju, akutnu limfocitnu leukemiju, kroničnu limfocitnu leukemiju, Hodgkinov limfom, ne-Hodgkinov limfom.
10. Spojevi s formulom I prema zahtjevima 1-5 i/ili njihove fiziološki prihvatljive soli za uporabu za liječenje tumora, naznačeni time da se terapijski učinkovita količina spoja s formulom I daje u kombinaciji sa spojem iz skupine koja sadrži 1) modulator estrogenskih receptora, 2) modulator androgenih receptora, 3) modulator retinoidnih receptora, 4) citotoksično sredstvo, 5) antiproliferativno sredstvo, 6) inhibitor prenil-protein transferaze, 7) inhibitor HMG-CoA reduktaze, 8) inhibitor HIV proteaze, 9) inhibitor reverzne transkriptaze i 10) dodatne inhibitore angiogeneze.
11. Spojevi s formulom I prema zahtjevima 1-5 i/ili njihove fiziološki prihvatljive soli za uporabu za liječenje tumora, naznačeni time da se terapijski učinkovita količina spoja s formulom I daje u kombinaciji s radioterapijom i spojem iz skupine koja sadrži 1) modulator estrogenskih receptora, 2) modulator androgenih receptora, 3) modulator retinoidnih receptora, 4) citotoksično sredstvo, 5) antiproliferativno sredstvo, 6) inhibitor prenil-protein transferaze, 7) inhibitor HMG-CoA reduktaze, 8) inhibitor HIV proteaze, 9) inhibitor reverzne transkriptaze i 10) dodatne inhibitore angiogeneze.
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EA026851B1 (ru) 2017-05-31
CA2869337C (en) 2020-06-30

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