HRP20190972T1 - Indazoli supstituirani amidom kao inhibitori poli(adp-riboza)polimeraze(parp) - Google Patents
Indazoli supstituirani amidom kao inhibitori poli(adp-riboza)polimeraze(parp) Download PDFInfo
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- HRP20190972T1 HRP20190972T1 HRP20190972TT HRP20190972T HRP20190972T1 HR P20190972 T1 HRP20190972 T1 HR P20190972T1 HR P20190972T T HRP20190972T T HR P20190972TT HR P20190972 T HRP20190972 T HR P20190972T HR P20190972 T1 HRP20190972 T1 HR P20190972T1
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- Prior art keywords
- inhibitors
- agents
- combination according
- methyl
- carboxamide
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- 239000003112 inhibitor Substances 0.000 title claims 26
- 102000012338 Poly(ADP-ribose) Polymerases Human genes 0.000 title claims 5
- 108010061844 Poly(ADP-ribose) Polymerases Proteins 0.000 title claims 5
- 229920000776 Poly(Adenosine diphosphate-ribose) polymerase Polymers 0.000 title claims 5
- 125000003368 amide group Chemical group 0.000 title 1
- 150000002473 indoazoles Chemical class 0.000 title 1
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- VSJKWCGYPAHWDS-FQEVSTJZSA-N camptothecin Chemical compound C1=CC=C2C=C(CN3C4=CC5=C(C3=O)COC(=O)[C@]5(O)CC)C4=NC2=C1 VSJKWCGYPAHWDS-FQEVSTJZSA-N 0.000 claims 3
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- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 3
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- MSRILKIQRXUYCT-UHFFFAOYSA-M valproate semisodium Chemical compound [Na+].CCCC(C(O)=O)CCC.CCCC(C([O-])=O)CCC MSRILKIQRXUYCT-UHFFFAOYSA-M 0.000 claims 1
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Classifications
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- C07D401/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing aromatic rings
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- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
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Claims (20)
1. Kombinacija koja sadrži spoj formule I:
pri čemu:
R1 je vodik ili fluor; i
R2 je vodik ili fluor;
ili njegova farmaceutski prihvatljiva sol, stereoizomer ili tautomer i jedno ili više sredstava protiv karcinoma.
2. Kombinacija prema patentnom zahtjevu 1, naznačena time što sredstva protiv karcinoma su izabrana od inhibitora HDAC, modulatora receptora za estrogen, modulatora receptora za androgen, modulatora receptora za retinoid, citotoksičnog/citostatičkog sredstva, antiproliferativnog sredstva, inhibitora prenil-protein transferaze, inhibitora HMG-CoA reduktaze, inhibitora HIV proteaze, inhibitora reverzne transkriptaze i drugih inhibitora angiogeneze, inhibitora stanične proliferacije i prijenosa signala preživljavanja, sredstava za indukciju apoptoze i sredstava koja ometaju kontrolne točke staničnog ciklusa.
3. Kombinacija prema patentnom zahtjevu 1, naznačena time što sredstva protiv karcinoma su izabrana od:
inhibitora HDAC izabranih od suberoilanilid hidroksamske kiseline (SAHA), LAQ824, LBH589, PXD101, MS275, FK228, valproinske kiseline, maslačne kiseline i CI-994;
modulatora receptora za estrogen izabranih od tamoksifena, raloksifena, idoksifena, LY353381, LY117081, toremifena, fulvestranta, 4-[7-(2,2-dimetil-1-oksopropoksi-4-metil-2-[4-[2-(1-piperidinil)etoksi]fenil]-2H-1-benzopiran-3-il]-fenil-2,2-dimetilpropanoata, 4,4’-dihidroksibenzofenon-2,4-dinitrofenil-hidrazona i SH646;
modulatora receptora za androgen izabranih od finasterida i ostalih inhibitora 5α-reduktaze, nilutamida, flutamida, bikalutamida, liarozola i abirateron acetata;
modulatora receptora za retinoid izabranih od beksarotena, tretinoina, 13-cis-retinoične kiseline, 9-cis-retinoične kiseline, α-difluorometilornitina, ILX23-7553, trans-N-(4’-hidroksifenil) retinamida i N-4-karboksifenil retinamida;
citotoksičnih/citostatičkih sredstava izabranih od alkilacijskih sredstava, faktora nekroze tumora, interkalatora, spojeva koji se mogu aktivirati hipoksijom, inhibitora mikrotubula/sredstava koja stabiliziraju mikrotubule, inhibitora mitotičkih kinezina, inhibitora kinaza uključenih u napredovanje mitoze, antimetabolita, modifikatora biološkog odgovora, hormonalnih/anti-hormonalnih terapeutskih sredstava, hematopoetskih faktora rasta, terapeutskih sredstava koja ciljno djeluju na monoklonska antitijela, inhibitora topoizomeraze, inhibitora proteazoma i inhibitora ubikvitin ligaze;
antiproliferativnih sredstava izabranih od antisens RNK i DNK oligonukleotida kao što su G3139, ODN698, RVASKRAS, GEM231 i INX3001, i antimetabolita kao što su enocitabin, karmofur, tegafur, pentostatin, doksifluridin, trimetreksat, fludarabin, kapecitabin, galocitabin, citarabin okfosfat, fosteabin natrij hidrat, raltitreksed, paltitreksid, emitefur, tiazofurin, decitabin, nolatreksed, pemetreksed, nelzarabin, 2’-deoksi-2’-metilidencitidin, 2’-fluorometilen-2’-deoksicitidin, N-[5-(2,3-dihidro-benzofuril)sulfonil]-N’-(3,4-dikklorofenil)urea, N6-[4-deoksi-4-[N2-[2(E),4(E)-tetradekadienoil]glicilamino]-L-glicero-B-L-mano-heptopiranozil]adenin, aplidin, ekteinascidin, troksacitabin, 4-[2-amino-4-okso-4,6,7,8-tetrahidro-3H-pirimidino[5,4-b][1,4]tiazin-6-il-(S)-etil]-2,5-tienoil-L-glutaminska kiselina, aminopterin, 5-flurouracil, alanozin, ester 11-acetil-8-(karbamoiloksimetil)-4-formil-6-metoksi-14-oksa-1,11-diazatetraciklo(7.4.1.0.0)-tetradeka-2,4,6-trien-9-il octene kiseline, svainsonin, lometreksol, deksrazoksan, metioninaza, 2’-cijano-2’-deoksi-N4-palmitoil-1-B-D-arabino furanozil citozin i 3-aminopiridin-2-karboksaldehid tiosemikarbazon;
inhibitora HMG-CoA reduktaze izabranih od lovastatina, simvastatina, pravastatina, fluvastatina i atorvastatina;
inhibitora prenil-protein transferaze izabranih od farnezil-protein transferaze (FPTaze), geranilgeranil-protein transferaze tipa I (GGPTaze-I) i geranilgeranil-protein transferaze tipa-II (GGPTaze-II, također označena kao Rab GGPTaza);
inhibitora angiogeneze izabranih od inhibitora tirozin kinaze, kao što su inhibitori receptora tirozin kinaze Flt-1 (VEGFR1) i Flk-1/KDR (VEGFR2), inhibitora faktora rasta porijeklom od epiderma, porijeklom od fibroblasta ili porijeklom od trombocita, inhibitora MMP (matriksne metaloproteaze), blokatora integrina, interferona-a, interleukina-12, pentosan polisulfata, inhibitora ciklooksigenaze, uključujući nesteroidna anti-inflamatorna sredstva (NSAIDs) kao što je aspirin i ibuprofen kao i selektivni inhibitori ciklooksigenaze-2 kao što je celekoksib i rofekoksib, steroidnih anti-inflamatornih sredstava (kao što su kortikosteroidi, mineralokortikoidi, deksametazon, prednizon, prednizolon, metilpred, betametazon), karboksiamidotriazola, kombretastatina A-4, skvalamina, 6-O-kloroacetil-karbonil)-fumagilola, talidomida, angiostatina, troponina-1, antagonista angiotenzina II i antitijela za VEGF, sredstava koju moduliraju ili inhibiraju koagulaciju i sisteme fibrinolize kao što su heparin, heparini niske molekulske mase i inhibitori karboksipeptidaze U (također poznati kao inhibitori aktivnog trombina koji se mogu aktivirati inhibitorom fibrinolize [TAFIa]);
sredstava koja ometaju kontrolne točke staničnog ciklusa izabranih od ATR, ATM, Chk1 i Chk2 kinaza i inhibitora cdk i cdc kinaze izabranih od 7-hidroksistaurosporina, staurosporina, flavopiridola, CYC202 (Cyclacel) i BMS-387032;
inhibitora stanične proliferacije i puta prijenosa signala preživljavanja izabranih od inhibitora EGFR (uključujući gefitinib i erlotinib), inhibitora ERB-2 (uključujući trastuzumab), inhibitora IGFR, inhibitora receptora za citokin, inhibitora MET, inhibitora PI3K (uključujući LY294002), serin/treonin kinaza (uključujući, ali bez ograničenja na inhibitore Akt, inhibitore Raf kinaze (uključujući BAY-43-9006), inhibitora MEK (uključujući CI-1040 i PD-098059) i inhibitora mTOR (uključujući Wyeth CCI-779 i Ariad AP23573);
sredstava koja induciraju apoptozu koja su aktivatori članova porodice TNF receptora (uključujući TRAIL receptore); i
inhibitora angiogeneze izabranih od endostatina, ukraina, ranpirnaze, IM862, 5-metoksi-4-[2-metil-3-(3-metil-2-butenil)oksiranil]-1-oksaspiro[2,5]okt-6-il(kloroacetil)karbamata, acetildinanalina, 5-amino-1-[[3,5-dikloro-4-(4-klorobenzoil)fenil]metil]-1H-1,2,3-triazol-4-karboksamida, CM101, skvalamina, kombretastatina, RPI4610, NX31838, sulfatiranog manopentaoze fosfata, 7,7-(karbonil-bis[imino-N-metil-4,2-pirolokarbonilimino[N-metil-4,2-pirol]-karbonilimino]-bis-(1,3-naftalen disulfonata) i 3-[(2,4-dimetilpirol-5-il)metilen]-2-indolinona (SU5416).
4. Kombinacija prema patentnom zahtjevu 1, naznačena time što sredstva protiv karcinoma su izabrana od:
citotoksičnih sredstava izabranih od ciklofosfamida, hlorambucil karmustina (BCNU), lomustina (CCNU), busulfana, treosulfana, sertenefa, kahektina, ifosfamida, tasonermina, lonidamina, karboplatina, altretamina, prednimustina, dibromodulcitola, ranimustina, fotemustina, nedaplatina, aroplatina, oksaliplatina, metil metansulfonata, prokarbazina, dakarbazina, heptaplatina, estramustina, improsulfan tozilata, trofosfamida, nimustina, dibrospidijum hlorida, pumitepa, lobaplatina, satraplatina, profiromicina, cisplatina, irofulvena, deksifosfamida, cis-amindikloro(2-metil-piridin)platine, benzilguanina, glufosfamida, GPX100, (trans, trans, trans)-bis-mu-(heksan-1,6-diamin)-mu-[diamin-platina(II)]bis[diamin(kloro)platina (II)]tetraklorida, diarizidinilspermina, arsen trioksida, 1-(11-dodecilamino-10-hidroksiundecil)-3,7-dimetilksantina, zorubicina, idarubicina, daunorubicina, bisantrena, mitoksantrona, pirarubicina, pinafida, valrubicina, amrubicina, doksorubicina, epirubicina, pirarubicina, antineoplastona, 3’-deamino-3’-morfolino-13-deokso-10-hidroksikarminomicina, anamicina, galarubicina, elinafida, MEN10755 i 4-demetoksi-3-deamino-3-aziridinil-4-metilsulfonil-daunorubicina;
sličnih sredstava izabranih od azotnih iperita: ciklofosfamid, ifosfamid, trofosfamid i klorambucil;
nitrozourea: karmustina (BCNU) i lomustina(CCNU); alkilsulfonata: busulfana i treosulfana; triazena: dakarbazina i prokarbazina; kompleksa koji sadrže platinu: cisplatina, karboplatina, aroplatina i oksaliplatina;
anti-mitotičkih sredstava izabranih od alokolhicina, halihondrina B, kolhicina, derivata kolhicina, dolstatina 10, majtanzina, rizoksina, tiokolhicina i tritil cisteina;
inhibitora proteazoma izabranih od laktacistina, bortezomiba, epoksomicina i peptidnih aldehida kao što je MG 132, MG 115 i PSI;
inhibitora mikrotubula/sredstava za stabilizaciju mikrotubula izabranih od paklitaksela, vindezin sulfata, vinkristina, vinblastina, vinorelbina, 3’,4’-didehidro-4’-deoksi-8’-norvinkaleukoblastina, docetaksola, rizoksina, dolastatina, mivobulin izetionata, auristatina, cemadotina, RPR109881, BMS184476, vinflunina, kriptoficina, 2,3,4,5,6-pentafluoro-N-(3-fluoro-4-metoksifenil) benzen sulfonamida, anhidrovinblastina, N,N-dimetil-L-valil-L-valil-N-metil-L-valil-L-prolil-L-prolin-t-butilamida, TDX258, epotilona i BMS188797;
inhibitora topoizomeraze izabranih od topotekana, hikaptamina, irinotekana, rubitekana, eksatekana, gimetekana, diflomotekana, silil-kamptotecina, 9-aminokamptotecina, kamptotecina, krisnatola, mitomicina C, 6-etoksipropionil-3’,4’-O-ekso-benziliden-hartreuzina, 9-metoksi-N,N-dimetil-5-nitropirazolo[3,4,5-kl]akridin-2-(6H)propanamina, 1-amino-9-etil-5-fluoro-2,3-dihidro-9-hidroksi-4-metil-1H,12H-benzo[de]pirano[3’,4’:b,7]-indolizino[1,2b]hinolin-10,13(9H,15H)diona, lurtotekana, 7-[2-(N-izopropilamino)etil]-(20S)kamptotecina, BNP1350, BNPI1100, BN80915, BN80942, etoposid fosfata, teniposida, sobuzoksana, 2’-dimetilamino-2’-deoksi-etoposida, GL331, N-[2-(dimetilamino)etil]-9-hidroksi-5,6-dimetil-6H-pirido[4,3-b]karbazol-1-karboksamida, asulakrina, (5a, 5aB, 8aa,9b)-9-[2-[N-[2-(dimetilamino)etil]-N-metilamino]etil]-5-[4-hidroksi-3,5-dimetoksifenil]-5,5a,6,8,8a,9-heksohidrofuro(3’,4’:6,7)nafto (2,3-d)-1,3-dioksol-6-ona, 2,3-(metilendioksi)-5-metil-7-hidroksi-8-metoksibenzo[c]-fenantridinija, 6,9-bis[(2-aminoetil)amino]benzo[g]izoguinolin-5,10-diona, 5-(3-aminopropilamino)-7,10-dihidroksi-2-(2-hidroksietilaminometil)-6H-pirazolo[4,5,1-de]akridin-6-ona, N-[1-[2(dietilamino)etilamino]-7-metoksi-9-okso-9H-tioksanten-4-ilmetil]formamida, N-(2-(dimetilamino)etil)akridin-4-karboksamida, 6-[[2-(dimetilamino)etil]amino]-3-hidroksi-7H-indeno[2,1-c]hinolin-7-ona, i dimesna; inhibitora ne-kamptotecin topoizomeraze-1 kao što su indolokarbazoli; i dualnih inhibitora topoizomeraze-1 i II kao što su benzofenazini, XR 20 115761MLN 576 i benzopiridoindoli;
mitotičkih kinazina izabranih od kinezina KSP, inhibitora KSP, inhibitora MKLP1, inhibitora CENP-E, inhibitora MCAK, inhibitora Kifl4, inhibitora Mphosph1 i inhibitora Rab6-KIFL;
inhibitora kinaza uključenih u napredovanje mitoze izabranih od inhibitora aurora kinaze, inhibitora kinaza sličnih Polo (PLK) (naročito inhibitora PLK-1), inhibitora bub-1 i inhibitora bub-R1;
terapeutskog sredstva tositumomaba koje ciljno djeluje na monoklonsko antitijelo (Bexxar); i
inhibitora tirozin kinaze izabranih od N-(trifluorometilfenil)-5-metilizoksazol-4-karboksamida, 3-[(2,4-dimetilpirol-5-il)metilidenil)indolin-2-ona, 17-(alilamino)-17-demetoksigeldanamicina, 4-(3-kloro-4-fluorofenilamino)-7-metoksi-6-[3-(4-morfolinil)propoksil]hinazolin, N-(3-etinilfenil)-6,7-bis(2-metoksietoksi)-4-hinazolinamina, BIBX1382, 2,3,9,10,11,12-heksahidro-10-(hidroksimetil)-10-hidroksi-9-metil-9,12-epoksi-1H-diindolo[1,2,3-fg:3’,2’,1’-kl]pirolo[3,4-i][1,6]benzodiazocin-1-ona, SH268, genisteina, STI571, CEP2563, 4-(3-klorofenilamino)-5,6-dimetil-7H-pirolo[2,3-d]pirimidinmetan sulfonata, 4-(3-bromo-4-hidroksifenil)amino-6,7-dimetoksihinazolina, 4-(4’-hidroksifenil)amino-6,7-dimetoksihinazolina, SU6668, STI571A, N-4-klorofenil-4-(4-piridilmetil)-1-ftalazinamina i EMD121974.
5. Kombinacija prema patentnom zahtjevu 1, naznačena time što, sredstvo protiv karcinoma je abirateron acetat.
6. Kombinacija prema patentnom zahtjevu 1, naznačena time što, sredstvo protiv karcinoma je karboplatin.
7. Kombinacija prema bilo kojem od patentnih zahtjeva 1-4, naznačena time što, navedeni spoj je:
2-(4-piperidin-3-ilfenil)-2H-indazol-7-karboksamid;
2- {4-[(3R)-piperidin-3-il]fenil}-2H-indazol-7-karboksamid;
2-{4-[(3S)-piperidin-3-il]fenil}-2H-indazol-7-karboksamid;
ili njegova farmaceutski prihvatljiva sol, stereoizomer ili tautomer.
8. Kombinacija prema bilo kojem od patentnih zahtjeva 1-4, naznačena time što, navedeni spoj je:
2-(4-piperidin-3-ilfenil)-2H-indazol-7-karboksamid;
ili njegova farmaceutski prihvatljiva sol ili tautomer.
9. Kombinacija prema bilo kojem od patentnih zahtjeva 1-4, naznačena time što, navedeni spoj je:
2- {4-[(3R)-piperidin-3-il]fenil} -2H-indazol-7-karboksamid;
ili njegova farmaceutski prihvatljiva sol ili tautomer.
10. Kombinacija prema bilo kojem od patentnih zahtjeva 1-4, naznačena time što, navedeni spoj je:
2-{4-[(3S)-piperidin-3-il]fenil}-2H-indazol-7-karboksamid;
ili njegova farmaceutski prihvatljiva sol ili tautomer.
11. Farmaceutska kompozicija koja sadrži kombinaciju prema bilo kojem prethodnom patentnom zahtjevu zajedno sa farmaceutski prihvatljivim nosačem.
12. Kombinacija prema bilo kojem od patentnih zahtjeva 1-10 za uporabu u terapiji.
13. Upotreba kombinacije prema bilo kojem od patentnih zahtjeva 1-10 za proizvodnju lijeka za liječenje ili prevenciju stanja koja mogu biti poboljšana inhibicijom poli(ADP-riboza) polimeraze (PARP).
14. Upotreba kombinacije prema bilo kojem od patentnih zahtjeva 1-10 za proizvodnju lijeka za liječenje ili prevenciju karcinoma, upalnih bolesti, reperfuzijskih povreda, ishemijskih stanja, moždanog udara, bubrežne insuficijencije, kardiovaskularnih bolesti, vaskularnih bolesti različitih od kardiovaskularnih bolesti, dijabetesa, neurodegenerativnih bolesti, retrovirusnih infekcija, oštećenja retine ili starenja kože i oštećenja kože izazvanih UV-zračenjem.
15. Upotreba kombinacije prema bilo kojem od patentnih zahtjeva 1-10 za proizvodnju lijeka za liječenje ili prevenciju karcinoma.
16. Upotreba prema patentnom zahtjevu 15 naznačena time što, karcinom je karcinom koji je deficijentan u DNK DSB reparacijskoj aktivnosti zavisnoj od homologne rekombinacije (HR).
17. Kombinacija prema bilo kojem od patentnih zahtjeva 1-10 za uporabu u liječenju ili prevenciji stanja koja mogu biti poboljšana inhibicijom poli(ADP-riboza)polimeraze (PARP).
18. Kombinacija prema bilo kojem od patentnih zahtjeva 1-10 za uporabu u liječenju ili prevenciji karcinoma, upalnih bolesti, reperfuzijskih povreda, ishemijskih stanja, moždanog udara, bubrežne insuficijencije, kardiovaskularnih bolesti, vaskularnih bolesti različitih od kardiovaskularnih bolesti, dijabetesa, neurodegenerativnih bolesti, retrovirusnih infekcija, oštećenja retine ili starenja kože i oštećenja kože izazvanih UV-zračenjem.
19. Kombinacija prema bilo kojem od patentnih zahtjeva 1-10 za uporabu u liječenju ili prevenciji karcinoma.
20. Kombinacija prema bilo kojem od patentnih zahtjeva 1-10 za uporabu u liječenju ili prevenciji karcinoma koji je deficijentan u DNK DSB reparacijskoj aktivnosti zavisnoj od homologne rekombinacije (HR).
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