HRP20150586T1 - Derivat adenina kao inhibitor pi3k - Google Patents
Derivat adenina kao inhibitor pi3k Download PDFInfo
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- HRP20150586T1 HRP20150586T1 HRP20150586TT HRP20150586T HRP20150586T1 HR P20150586 T1 HRP20150586 T1 HR P20150586T1 HR P20150586T T HRP20150586T T HR P20150586TT HR P20150586 T HRP20150586 T HR P20150586T HR P20150586 T1 HRP20150586 T1 HR P20150586T1
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Claims (29)
1. Spoj, naznačen time što ima formulu:
[image]
,
ili njegova farmaceutski prihvatljiva sol.
2. Spoj u skladu s patentnim zahtjevom 1, naznačen time što je spoj:
[image]
,
ili njegova farmaceutski prihvatljiva sol.
3. Spoj u skladu s patentnim zahtjevom 1, naznačen time što je spoj S-enantiomer čija je enantiomerna čistoća veća od 55%, veća od 80%, veća od 90% ili veća od 95%.
4. Farmaceutski pripravak, naznačen time što sadrži spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 3, ili njegovu farmaceutski prihvatljivu sol, kao i farmaceutski prihvatljivu pomoćnu tvar.
5. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 3, ili njegova farmaceutski prihvatljiva sol, ili farmaceutski pripravak u skladu s patentnim zahtjevom 4, naznačeni time što su namijenjeni upotrebi u liječenju poremećaja kojeg se bira između raka, poremećaja kostiju, upalne bolesti, autoimune bolesti, bolesti živčanog sustava, metaboličke bolesti, bolesti dišnog sustava, tromboza i bolesti srca.
6. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 3, ili njegova farmaceutski prihvatljiva sol, ili farmaceutski pripravak u skladu s patentnim zahtjevom 4, naznačeni time što su namijenjeni upotrebi u liječenju poremećaja kojeg se bira između astme, emfizem, alergije, dermatitisa, reumatoidnog artritisa, upalnog osteoartritisa, upalnih bolesti crijeva, kroničnog opstruktivnog plućnog poremećaja, psorijaze, multiple skleroze, poremećaja povezanih s komplikacijama dijabetesa, eritematoznog lupusa, skleroderme, bolesti reakcije presatka prema domaćinu, restenoze, ateroskleroze i mastocitoze.
7. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 3, ili njegova farmaceutski prihvatljiva sol, ili farmaceutski pripravak u skladu s patentnim zahtjevom 4, naznačeni time što su namijenjeni upotrebi u liječenju raka.
8. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 3, ili njegova farmaceutski prihvatljiva sol, ili farmaceutski pripravak u skladu s patentnim zahtjevom 4, namijenjeni upotrebi u skladu s patentnim zahtjevom 7, naznačeni time što se rak bira između raka timusa, mozga, pluća, pločastih stanica, kože, oka, retinoblastoma, intraokularnog melanoma, raka usne šupljine i orofarinksa, mokraćnog mjehura, želučanog raka, raka želuca, gušterače, mokraćnog mjehura, dojke, vrata maternice, glave, vrata, bubrežnog raka, raka bubreg, jetre, jajnika, prostate, kolorektalnog raka, raka jednjaka, testisa, ginekološkog raka, raka štitnjače, CNS-a, PNSa, raka povezanog s AIDS-om, Kaposijevog sarkoma i raka uzrokovanog virusima.
9. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 3, ili njegova farmaceutski prihvatljiva sol, ili farmaceutski pripravak u skladu s patentnim zahtjevom 4, namijenjeni upotrebi u skladu s patentnim zahtjevom 7, naznačeni time što je rak leukemija ili limfom.
10. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 3, ili njegova farmaceutski prihvatljiva sol, ili farmaceutski pripravak u skladu s patentnim zahtjevom 4, namijenjeni upotrebi u skladu s patentnim zahtjevom 9, naznačeni time što se leukemiju bira između akutna mijelogena leukemija (AML), akutne limfocitne leukemije, leukemije T-stanica kod odraslih, kronične limfocitne leukemija (CLL), leukemije vlasastih stanica, mijelodisplazije, mijeloproliferativnih poremećaja, kronične mijelogene leukemije (CML), multiplog mijeloma (MM), mijelodisplastičnog sindroma (MDS), leukemija uzrokovana ljudskim limfotropnim virusom tip 1 (HTLV-1), mastocitoze i akutne limfoblastične leukemije B-stanica.
11. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 3, ili njegova farmaceutski prihvatljiva sol, ili farmaceutski pripravak u skladu s patentnim zahtjevom 4, namijenjeni upotrebi u skladu s patentnim zahtjevom 9, naznačeni time što se limfom bira između difuznog limfoma velikih B-stanica, imunoblastičnog limfoma B-stanica, limfoma malih nesegmentiranih stanica, leukemije odnosno limfoma uzrokovanog ljudskim limfotropnim virusom tip 1 (HTLV-1), limfoma T-stanica kod odraslih, limfoma stanica plašta (MCL), Hodgkinove bolesti, nehodgkinskih limfoma, limfoma povezanog s AIDS-om, limfoma perifernih T-stanica, limfoma kutanih T-stanica, multiplog mijeloma i folikularnog limfoma.
12. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 3, ili njegova farmaceutski prihvatljiva sol, ili farmaceutski pripravak u skladu s patentnim zahtjevom 4, namijenjeni upotrebi u skladu s patentnim zahtjevom 9, naznačeni time što je leukemija kronična limfocitna leukemija.
13. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 3, ili njegova farmaceutski prihvatljiva sol, ili farmaceutski pripravak u skladu s patentnim zahtjevom 4, namijenjeni upotrebi u skladu s patentnim zahtjevom 9, naznačeni time što je limfom nehodgkinski limfom.
14. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 3, ili njegova farmaceutski prihvatljiva sol, ili farmaceutski pripravak u skladu s patentnim zahtjevom 4, namijenjeni upotrebi u skladu s patentnim zahtjevom 9, naznačeni time što je limfom difuzni limfom velikih B-stanica.
15. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 3, ili njegova farmaceutski prihvatljiva sol, ili farmaceutski pripravak u skladu s patentnim zahtjevom 4, namijenjeni upotrebi u skladu s patentnim zahtjevom 9, naznačeni time što je limfom limfom stanica plašta.
16. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 3, ili njegova farmaceutski prihvatljiva sol, ili farmaceutski pripravak u skladu s patentnim zahtjevom 4, namijenjeni upotrebi u skladu s patentnim zahtjevom 9, naznačeni time što je limfom limfom T-stanica kod odraslih.
17. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 3, ili njegova farmaceutski prihvatljiva sol, ili farmaceutski pripravak u skladu s patentnim zahtjevom 4, namijenjeni upotrebi u skladu s patentnim zahtjevom 5, naznačeni time što je poremećaj upalna bolest ili autoimuna bolest koju se bira između:
(i) bursitisa, lupusa, akutnog diseminiranog encefalomijelitisa (ADEM), Addisonove bolesti, sindroma protutijela protiv fosfolipida (APS), aplastične anemije, autoimunog hepatitisa, celijačne bolesti, Crohnove bolesti, dijabetesa melitusa (tip 1), Goodpastureovog sindroma, Gravesove bolesti, Guillain-Barréovog sindroma (GBS), Hashimotove bolesti, upalne bolesti crijeva, eritematoznog lupusa, miastenije gravis, opsoklonusno-mioklonusnog sindroma (OMS), neuritisa vidnog živca, Ordovog tireoiditisa, osteoartritisa, uveoretinitisa, pemfigusa, poliartritisa, primarne bilijarne ciroze, Reiterovog sindroma, Takayasuovog arteritisa, temporalnog arteritisa, tople autoimune hemolitičke anemije, Wegenerove granulomatoze, alopecije universalis, Chagasove bolesti, sindroma kroničnog zamora, disautonomije, endometrioze, gnojnog hidradenitisa, intersticijskog cistitisa, neuromiotonije, sarkoidoze, skleroderme, ulceroznog kolitisa, vitiliga, vulvodinije, apendicitisa, arteritisa, artritisa, blefaritisa, bronhiolitisa, bronhitisa, cervicitisa, kolangitisa, kolecistitisa, korioamnionitisa, kolitisa, konjunktivitisa, cistitis, dakrioadenitisa, dermatomiozitisa, endokarditisa, endometritisa, enteritisa, enterokolitisa, epikondilitis, epididimitisa, fasciitisa, fibrozitisa, gastritisa, gastroenteritisa, gingivitisa, hepatitisa, hidradenitisa, ileitisa, iritisa, laringitisa, mastitisa, meningitisa, mijelitisa, miokarditisa, miozitisa, nefritisa, omfalitisa, ooforitisa, orhitisa, osteitisa, otitisa, pankreatitisa, parotitisa, perikarditisa, peritonitisa, faringitisa, pleuritisa, flebitisa, pneumonitisa, proktitisa, prostatitisa, pijelonefritisa, rinitisa, salpingitisa, sinusitisa, stomatitisa, sinovitisa, tendonitisa, tonzilitisa, uveitisa, vaginitisa, vaskulitisa i vulvitisa;
(ii) cjelogodišnjeg alergijskog rinitisa, mezenteritisa, akrodermatitisa, angiodermatitisa, atopičnog dermatitisa, kontaknog dermatitisa, egzema, multiformnog eritema, intertriga, Stevens-Johnsonovog sindroma, toksične nekroliza epidermisa, kožne alergije, teške alergijske reakcije odnosno anafilaksije, alergijske granulomatoze, alergijskog konjunktivitisa, korioretinitisa, zaraznog keratokonjunktivitisa, keratokonjunktivitisa, oftalmije novorođenčadi, trahoma, upale oka, blefarokonjunktivitisa, perikoronitisa, rinofaringitisa, sijaladenitisa, upale mišićnokoštanog sustava, Stillove bolesti s početkom u odrasloj dobi, Behçetove bolesti, kondrokalcinoze, daktilitisa, Feltyjevog sindroma, gihta, zaraznog artritisa, lajmske bolesti, upalnog osteoartritisa, periartritisa, infekcije virusom Ross River, sindroma akutnog respiratornog distresa, akutnog bronhitisa, akutnog sinusitisa, alergijskog rinitisa, astme, teške refrakterne astme, pleuritisa, sezonskog alergijskog rinitisa, astmatičnog statusa, traheobronhitisa, serozitisa, neuromijelitisa vidnog živca, infekcije poliovirusom, Alportovog sindroma, balanitisa, epididimo orhitis, fokalne segmentalne glomeruloskleroze, glomerulonefritisa, IgA nefropatije (Bergerove bolesti), orhitisa, parametritisa, upalne bolesti zdjelice, pijelitisa, pijelocistitisa, hiperurikemije, aortitisa, hiloperikarditisa, Dresslerovog sindroma, endarteritisa, ekstrakranijalnog temporalnog arteritisa, arteritisa povezanog s HIV-om, intrakranijalnog temporalnog arteritisa, Kawasaki bolest, limfangioflebitis, Mondorove bolesti i periarteritisa; i
(iii) jejunitisa, mukozitisa, nealkoholnog steatohepatitisa, nevirusnog hepatitisa, autoimunog pankreatitisa, perihepatitisa, upale ilealnog sprenika, pseudomembranoznog kolitisa, rektosigmoiditisa, salpingoperitonitisa, sigmoiditisa, steatohepatitisa, Churg-Straussovog sindroma, ulceroznog proktitisa, sindroma iritabilnog crijeva, želučanocrijevne upale, akutnog enterokolitisa, anusitisa, Balserove nekroze, divertikulitisa, enterohepatitisa, eozinofilnog ezofagitisa, ezofagitisa, hemoragijskog enteritisa, infekcije virusom hepatitisa, hepatokolangitisa, hipertrofičnog gastritisa, ileocecitisa, ankilozantnog spondilitisa, reumatoidnog artritisa, mladalačkog reumatoidnog artritisa, psorijaze, psorijatičnog artritisa, lupusa (kutanog/sistemnog/nefritisa), AIDS-a, agamaglobulinemije, kompleksa povezanog s AIDS-om, Brutonove bolesti, Chédiak-Higashijevog sindroma, obične varijabilne imunodeficijencije, DiGeorgeovog sindroma, disgamaglobulinemije, imunoglobulindeficijencije, Jobovog sindroma, Nezelovljevog sindroma, fagocittnog baktericidnog poremećaja, Wiskott-Aldrichevog sindroma, asplenije, elefantijaze, hipersplenizma, limfadenopatije, limfedema, limfokele, Nonne-Milroy-Meigeovog sindroma, bolesti slezene, splenomegalije, timoma, bolesti timusa, perivaskulitisa, pleuroperikarditisa, nodoznog poliarteritisa, tromboangiitisa, obliterirajućeg tromboangiitisa, tromboendokarditisa, tromboflebitisa i COPD.
18. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 3, ili njegova farmaceutski prihvatljiva sol, ili farmaceutski pripravak u skladu s patentnim zahtjevom 4, namijenjeni upotrebi u skladu s patentnim zahtjevom 5 ili 6, naznačeni time što je upalna ili autoimuna bolest astma.
19. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 3, ili njegova farmaceutski prihvatljiva sol, ili farmaceutski pripravak u skladu s patentnim zahtjevom 4, namijenjeni upotrebi u skladu s patentnim zahtjevom 5 ili 6, naznačeni time što je upalna ili autoimuna bolest reumatoidni artritis.
20. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 3, ili njegova farmaceutski prihvatljiva sol, ili farmaceutski pripravak u skladu s patentnim zahtjevom 4, naznačeni time što su namijenjeni upotrebi u ublažavanju simptoma povezanih s reumatoidnim artritisom koje se bira između jednog ili više od smanjivanja otekline zglobova, smanjivanja razina protutijela protiv kolagena u serumu, smanjivanja resorpcije kostiju, smanjivanja oštećenja hrskavice, smanjivanja panusa i smanjivanja upale.
21. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 3, ili njegova farmaceutski prihvatljiva sol, ili farmaceutski pripravak u skladu s patentnim zahtjevom 4, naznačeni time što su namijenjeni upotrebi u liječenju bolesti dišnog sustava.
22. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 3, ili njegova farmaceutski prihvatljiva sol, ili farmaceutski pripravak u skladu s patentnim zahtjevom 4, namijenjeni upotrebi u skladu s patentnim zahtjevom 21, naznačen time što se bolest dišnog sustava bira između astme, kronične opstruktivne plućne bolesti (COPD), kroničnog bronhitisa, emfizema i bronhiektazije.
23. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 3, ili njegova farmaceutski prihvatljiva sol, ili farmaceutski pripravak u skladu s patentnim zahtjevom 4, namijenjeni upotrebi u skladu s patentnim zahtjevima 5 do 22, naznačeni time što prilikom liječenja treba primijeniti i drugo terapijsko sredstvo.
24. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 3, ili njegova farmaceutski prihvatljiva sol, ili farmaceutski pripravak u skladu s patentnim zahtjevom 4, namijenjeni upotrebi u skladu s patentnim zahtjevom 23, naznačeni time što je drugo terapijsko sredstvo koje treba primijeniti prilikom liječenja kemoterapijsko sredstvo.
25. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 3, ili njegova farmaceutski prihvatljiva sol, ili farmaceutski pripravak u skladu s patentnim zahtjevom 4, namijenjeni upotrebi u skladu s patentnim zahtjevom 24, naznačeni time što se kemoterapijsko sredstvo bira između inhibitora mitoze, alkilirajućih sredstava, antimetabolita, interkalirajućih antibiotika, inhibitora čimbenika rasta, inhibitora staničnog ciklusa, enzima, inhibitora topoizomeraze, modifikatora biološkog odgovora, antihormona, inhibitora angiogeneze, antiandrogena, alkilirajućih sredstava, alkilsulfonata, aziridina, etilenimina, metilamelamina, dušičnih iperita, nitrozourea, antimetabolita, analoga folne kiseline, analoga purina, sredstava za obnavljanje folne kiseline, taksana, antihormonskih sredstava koja djeluju reguliranjem ili inhibiranjem djelovanja hormona na tumore, antiestrogena, antiandrogena, agonista LHRH, fotodinamičkih terapija, nitrozourea, alkilsulfonata, triazena, spojeva koji sadrže platinu, vinka alkaloida, taksoida, epipodofilina, inhibitora DHFR, inhibitora IMP-dehidrogenaze, inhibitora ribonukleotid-reduktaze, analoga uracila, analoga citozina, analoga purina, analoga vitamina D, inhibitora izopreniliranja, dopaminergičkih neurotoksina, inhibitora staničnog ciklusa, inhibitora MDR, inhibitora Ca2+-ovisne ATPaze, inhibitora tirozinskih kinaza, proteasomnij inhibitora i inhibitora mTOR.
26. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 3, ili njegova farmaceutski prihvatljiva sol, ili farmaceutski pripravak u skladu s patentnim zahtjevom 4, namijenjeni upotrebi u skladu s patentnim zahtjevom 24, naznačeni time što se kemoterapijsko sredstvo bira iz skupine koju čine imatinib, bortezomib, bikalutamid, adriamicin, tiotepa, ciklofosfamid, busulfan, improsulfan, piposulfan, benzodopa, karbokvon, meturedopa, uredopa, altretamin, trietilenemelamin, trietilenfosforamid, trietilentiofosforamid, trimetilolomelamin, klorambucil, klornafazin, ifosfamid, mekloretamin, mekloretamin-oksid-hidroklorid, melfalan, novembikin, fenesterin, prednimustin, trofosfamid, uracilni iperit, klorozotocin, fotemustin, nimustin, ranimustin, antibiotici, poput aklacinomisina, aktinomicina, autramicina, azaserina, bleomicina, kaktinomicina, kaliheamicina, karabicina, karminomicina, karcinofilin, kromomicina, daunorubicina, detorubicina, 6-diazo-5-okso-1-norleucina, esorubicina, idarubicina, marcelomicina, mitomicina, mikofenolne kiseline, nogalamicina, olivomicina, peplomicina, puromicina, kvelamicina, rodorubicina, streptonigrina, streptozocina, tubercidina, ubenimeksa, zinostatina, zorubicina, 5-fluoruracil (5-FU), pteropterina, trimetreksat, denopterin, metotreksat, pteropterin, trimetreksat, ancitabin, azacitidin, 6-azauridin, karmofur, citarabin, dideoksiuridin, doksifluridin, enocitabin, floksuridin, kalusteron, dromostanolon-propionat, epitiostanol, mepitiostan, testolakton, aminoglutetimid, mitotan, trilostan, frolinska kiselina, aceglaton, aldofosfamid-glikozid, aminolevulinska kiselina, amsakrin, bestrabucil, bisantren, edatraksat, defofamin, demekolcin, diazikvon, elfomitin, eliptinijev acetat, etoglucid, galijev nitrat, lentinan, lonidamin, mitogvazon, mitoksantron, mopidamol, nitrakrin, pentostatin, fenamet, pirarubicin, podofilinska kiselina, 2-etilhidrazid, prokarbazin, polisaharid K, razoksan, sizofiran, spirogermanij, tenuazonska kiselina, triazikvon, 2,2′,2′′-triklortrietilamin, uretan, manomustin, mitobronitol, mitolaktol, pipobroman, gacitozin, arabinozid ("Ara-C"), paklitaksel, docetaksel, retinska kiselina, esperamicin, raloksifen, 4-hidroksitamoksifen, trioksifen, keoksifen, LY 117018, onapriston, toremifen, flutamid, nilutamid, leuprolid, goserelin, 6-tiogvanin, merkaptopurin, cisplatin, karboplatin, vinblastin, platina, mitomicin C, vineristin, vinorelbin, navelbin, novantron, tenipozid, daunomicin, aminopterin, Xeloda, ibandronat, kamptotecin-11 (CPT-11), inhibitor topoizomeraze RFS 2000, difluormetilornitin (DMFO), tamoksifen, megestrol, leuprolid, flutamid, vertoporfin(BPD-MA), ftalocijanin, fotosenzibilizator Pc4, demetoksihipokrelin A (2BA-2-DMHA), estramustin, karmustin (BCNU), lomustin (CCNU), treosulfan, dakarbazin, temozolomid, oksaliplatin, vindezin, DHA-paklitaksel, Taxoprexin, PG-paklitaksel, paklitaksel-poliglumeks, CT-2103, Xyotaks, ANG1005, paklitaksel-EC-1, paklitaksel konjugiran s glukozom, etopozid, etopozid-fosfat, topotekan, 9-aminokamptotecin, kamptoirinotekan, irinotekan, krisnatol, mitomicin C, diklormetotreksat, edatreksat, tiazofurin, ribavirin, EICAR, hidroksiurea, deferoksamin, 5-fluoruracil (5-FU), ratitreksed, tegafur-uracil, kapecitabin, citozin-arabinozid, fludarabin, merkaptopurin-tiogvanin, EB 1089, CB 1093, KH 1060, lovastatin, 1-metil-4-fenilpiridinijev ion, staurosporin, aktinomicin D, daktinomicin, bleomicin A2, bleomicin B2, peplomicin, doksorubicin, pegilirani liposomski doksorubicin, epirubicin, pirarubicin, verapamil, tapsigargin, talidomid, lenalidomid, aksitinib (AG013736), bosutinib (SKI-606), cediranib (AZD2171), dasatinib (BMS-354825), erlotinib, gefitinib, lapatinib, lestaurtinib (CEP-701), neratinib (HKI-272), nilotinib, semaksanib, sunitinib SU11248, toceranib, vandetanib (ZD6474), vatalanib (PTK787, PTK/ZK), trastuzumab, bevacizumab, rituksimab, cetuksimab, panitumumab, ranibizumab, sorafenib, everolimus, alemtuzumab, gemtuzumab, ozogamicin, temsirolimus, ENMD-2076, PC1-32765, AC220, dovitinib-laktat (TKI258, CHIR-258), BIBW 2992, SGX523, PF-04217903, PF-02341066, PF-299804, BMS-777607, ABT-869, MP470, BIBF 1120, AP24534, JNJ-26483327, MGCD265, DCC-2036, BMS-690154, CEP-11981, tivozanib (A-951), OSI-930, MM-121, XL-184, XL-647, XL228, rapamicin, ridaforolimus, AP23573, AZD8055, BEZ235, BGT226, XL765, PF-4691502, GDC0980, SF1126, OSI-027, oblimersen, gemcitabin, leukovorin, pemetreksed, prednizolon, deksametazon, kampatecin, plikamicin, asparaginaza, metopterin, porfiromicin, leurosidin, leurozin, trabektedin, prokarbazin, diskodermolid i heksametilmelamin, ili njihove farmaceutski prihvatljive soli.
27. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 3, ili njegova farmaceutski prihvatljiva sol, ili farmaceutski pripravak u skladu s patentnim zahtjevom 4, namijenjeni upotrebi u skladu s patentnim zahtjevom 23, naznačeni time što se drugo terapijsko sredstvo bira između
(i) sredstva koje inhibira proizvodnju ili aktivnost IgE, ili
(ii) protuupalnog lijeka, ili
(iii) antikoagulansa, ili
(iv) bioterapijskog sredstva, ili
(v) bronhodilatatora, ili
(vi) sredstava protiv angiogeneze, ili
(vii) diuretičkog sredstva, ili
(viii) hormona ili terapijskog peptida ili proteina, ili
(ix) terapije ozračivanjem, ili
(x) terapijskog protutijela.
28. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 3, ili njegova farmaceutski prihvatljiva sol, ili farmaceutski pripravak u skladu s patentnim zahtjevom 4, namijenjeni upotrebi u skladu s patentnim zahtjevom 27, naznačeni time što
(i) sredstvo koje inhibira proizvodnju ili aktivnost IgE se bira između TEI-9874, 2-(4-(6-cikloheksiloksi-2-naftiloksi)fenilacetamid)benzojeve kiseline, rapamicina, analoga rapamicina, inhibitora TORC1, inhibitora TORC2, protutijela protiv IgE, omalizumaba i TNX-901; ili
(ii) nesteroidni protuupalni lijek se bira između acetilsalicilne kiseline, ibuprofena, naproksena, indometacina, nabumetona, tolmetina, kortikosteroida, prednizona, klorokina i hidroksiklorokina; ili
(iii) antikoagulans se bira između aspirina, heparina i Coumadin-a; ili
(iv) bioterapijsko sredstvo se bira između čimbenika tumorske nekroze, interferona α, interferona γ, IL-1, IL-2, IL-4, IL-6, IL-12, GM-CSF, Herceptin-a (trastuzumaba), T-DM1, bevacizumaba, cetuksimaba, panitumumaba, rituksimaba i tositumomaba; ili
(v) bronhodilatator se bira između efedrina, adrenalina, fenoterola, formoterola, izoprenalina, metaproterenola, fenilefrina, fenilpropanolamina, pirbuterola, reproterola, rimiterola, salbutamola, salmeterola, terbutalina, izoetarina, tulobuterola, orciprenalina ili (–)-4-amino-3,5-diklor-α-[[[6-[2-(2-piridinil)etoksi]heksil]amino]metil]benzenmetanola; ili
(vi) sredstvo protiv angiogeneze se bira između inhibitora MMP-2 (matrične metaloproteinaze 2), inhibitora MMP-9 (matrične metaloproteinaze 9) i inhibitora COX-II (ciklooksigenaze II); ili
(vii) diuretičko sredstvo se bira između amilorida, antikolinergika, ipratropija, atropin i oksitropija; ili
(viii) hormon ili terapijski peptid ili protein se bira između kortizona, hidrokortizona, prednizolona, ksantina, aminofilina, kolin-teofilinata, lizin-teofilinata, teofilina, inzulina i glukagona; ili
(ix) terapija ozračivanjem se bira između terapije vanjskim snopom, terapije unutarnjim ozračivanjem, ozračivanjem iz usatka, stereotaktičkog radiokirurškog zahvata, terapije sistemnim ozračivanjem, radioterapije i trajne ili privremene intersticijske brahiterapije.
29. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 3, ili njegova farmaceutski prihvatljiva sol, ili farmaceutski pripravak u skladu s patentnim zahtjevom 4, namijenjeni upotrebi u skladu s patentnim zahtjevom 27, naznačeni time što je drugo terapijsko sredstvo terapijsko protutijelo, koje se bira između cetuksimaba, panitumumaba, trastuzumaba, rituksimaba, tositumomaba, alemtuzumaba, bevacizumaba, gemtuzumaba, protutijela protiv CD20 i protutijela protiv receptorskih tirozinskih kinaza.
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PCT/US2010/002020 WO2011008302A1 (en) | 2009-07-15 | 2010-07-15 | Certain chemical entities, compositions and methods |
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