HRP20211225T1 - Sulfoniluree i srodni spojevi i njihova uporaba - Google Patents

Sulfoniluree i srodni spojevi i njihova uporaba Download PDF

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HRP20211225T1
HRP20211225T1 HRP20211225TT HRP20211225T HRP20211225T1 HR P20211225 T1 HRP20211225 T1 HR P20211225T1 HR P20211225T T HRP20211225T T HR P20211225TT HR P20211225 T HRP20211225 T HR P20211225T HR P20211225 T1 HRP20211225 T1 HR P20211225T1
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Croatia
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disease
alkyl
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group
compound according
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HRP20211225TT
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Inventor
Luke O'neill
Matthew Cooper
Avril Robertson
Kate SCHRODER
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The University Of Queensland
The Provost, Fellows, Foundation Scholars, and the other members of Board, of the College of the Holy& Undiv. Trinity of Queen Elizabeth near Dublin
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=56691944&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=HRP20211225(T1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Priority claimed from AU2015900507A external-priority patent/AU2015900507A0/en
Application filed by The University Of Queensland, The Provost, Fellows, Foundation Scholars, and the other members of Board, of the College of the Holy& Undiv. Trinity of Queen Elizabeth near Dublin filed Critical The University Of Queensland
Publication of HRP20211225T1 publication Critical patent/HRP20211225T1/hr

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Claims (20)

1. Spoj formule (I), ili njegova farmaceutski prihvatljiva sol ili solvat: [image] pri čemu je W odabran od O, S i Se; J je odabran od S i Se; R1 je odabran iz skupine koja se sastoji od 5-eročlanog i 6-eročlanog heterociklila, koji svi mogu biti po izboru supstituirani, pri čemu je bilo koji izborni supstituent neovisno odabran iz skupine koju čine C1-10 alkil; C3-6 cikloalkil; hidroksialkil; C1-10 alkoksi; C2-10 alkenil; C2-10 alkinil; C6-C12 aril; ariloksi; heteroaril; heterociklil; halo; hidroksil; halogenirani alkil; amino; alkilamino; arilamino; acil; amido; CN; NO2; N3; CH20H; CONH2; CONR24R25; CO2R24; CH2OR24; NHCOR24; NHCO2R24; C1-3 alkiltio; sulfat; sulfonska kiselina; sulfonatni esteri; fosfonska kiselina; fosfat; fosfonat; mono-, di- ili trifosfatni esteri; tritil; monometoksitrtil; R24SO; R24S02; CF3S; CF3SO2; i trialkilsilil; pri čemu su R24 i R25 svaki neovisno odabrani između H i C1-10 alkila; R2 je odabran između 2,6-dialkilfenil, 2,6-dialkil-4-halofenil, 2,6-dicikloalkilfenil, 2,6-dicikloalkil-4-halofenil i: [image] pri čemu se svaka incidencija Y neovisno bira između C, N, S i O, koji se prema potrebi mogu supstituirati, pri čemu se bilo koji izborni supstituent neovisno bira iz skupine koja se sastoji od C1-10 alkil; C3-6 cikloalkil; hidroksialkil; C1-10 alkoksi; C2-10 alkenil; C2-10 alkinil; C6-C12 aril; ariloksi; heteroaril; heterociklil; halo; hidroksil; halogenirani alkil; amino; alkilamino; arilamino; acil; amido; CN; NO2; N3; CH20H; CONH2; CONR24R25; CO2R24; CH2OR24; NHCOR24; NHCO2R24; C1-3 alkiltio; sulfat; sulfonska kiselina; sulfonatni esteri; fosfonska kiselina; fosfat; fosfonat; mono-, di- ili trifosfatni esteri; tritil; monometoksitrtil; R24SO; R24S02; CF3S; CF3SO2; i trialkilsilil; pri čemu su R24 i R25 svaki neovisno odabrani između H i C1-10 alkila; R5 je odabran iz skupine koju čine vodik, halo, cijano, amid, sulfonamid, acil, hidroksil, C1-C6 alkil, C1-C6 haloalkil, C3-C5 ciloalkil i C1-C6 alkoksi, koje sve skupine mogu biti po želji supstituirane, prema potrebi, s halo, cijano ili C1-C6 alkoksi; i oba R1 su izravno vezana za J, a R2 je izravno vezan za susjedni dušik, preko atoma ugljika.
2. Spoj u skladu s patentnim zahtjevom 1, naznačen time što R1 je 6-člani heterociklil, koji može biti prema potrebi supstituiran, pri čemu je bilo koji izborni supstituent neovisno odabran iz skupine koja se sastoji od C1-10 alkil; C3-6 cikloalkil; hidroksialkil; C1-10 alkoksi; C2-10 alkenil; C2-10 alkinil; C6-C12 aril; ariloksi; heteroaril; heterociklil; halo; hidroksil; halogenirani alkil; amino; alkilamino; arilamino; acil; amido; CN; NO2; N3; CH2OH; CONH2; CONR24R25; CO2R24; CH2OR24; NHCOR24; NHCO2R24; C1-3 alkiltio; sulfat; sulfonska kiselina; sulfonatni esteri; fosfonska kiselina; fosfat; fosfonat; mono-, di- ili trifosfatni esteri; tritil; monometoksitrtil; R24SO; R24SO2; CF3S; CF3SO2; i trialkilsilil; pri čemu su R24 i R25 svaki neovisno odabrani između H i C1-10 alkila.
3. Spoj prema bilo kojem od prethodnih zahtjeva, naznačen time, da je R1 potpuno zasićeni heterociklil, koji može biti prema potrebi supstituiran, pri čemu je bilo koji izborni supstituent neovisno odabran iz skupine koja se sastoji od C1-10 alkil; C3-6 cikloalkil; hidroksialkil; C1-10 alkoksi; C2-10 alkenil; C2-10 alkinil; C6-C12 aril; ariloksi; heteroaril; heterociklil; halo; hidroksil; halogenirani alkil; amino; alkilamino; arilamino; acil; amido; CN; NO2; N3; CH2OH; CONH2; CONR24R25; CO2R24; CH2OR24; NHCOR24; NHCO2R24; C1-3 alkiltio; sulfat; sulfonska kiselina; sulfonatni esteri; fosfonska kiselina; fosfat; fosfonat; mono-, di- ili trifosfatni esteri; tritil; monometoksitrtil; R24SO; R24SO2; CF3S; CF3SO2; i trialkilsilil; pri čemu su R24 i R25 svaki neovisno odabrani između H i C1-10 alkila.
4. Spoj prema bilo kojem od prethodnih zahtjeva, naznačen time, da R1 je dušikov heterociklil, koji može biti prema potrebi supstituiran, pri čemu je bilo koji izborni supstituent neovisno odabran iz skupine koja se sastoji od C1-10 alkil; C3-6 cikloalkil; hidroksialkil; C1-10 alkoksi; C2-10 alkenil; C2-10 alkinil; C6-C12 aril; ariloksi; heteroaril; heterociklil; halo; hidroksil; halogenirani alkil; amino; alkilamino; arilamino; acil; amido; CN; NO2; N3; CH2OH; CONH2; CONR24R25; CO2R24; CH2OR24; NHCOR24; NHCO2R24; C1-3 alkiltio; sulfat; sulfonska kiselina; sulfonatni esteri; fosfonska kiselina; fosfat; fosfonat; mono-, di- ili trifosfatni esteri; tritil; monometoksitrtil; R24SO; R24SO2; CF3S; CF3SO2; i trialkilsilil; pri čemu su R24 i R25 svaki neovisno odabrani između H i C1-10 alkila.
5. Spoj prema bilo kojem od prethodnih zahtjeva, naznačen time, da je R1 odabran iz skupine koju čine tetrahidrofuran, tetrahidropiran, piran, pirolidin, morfolin, piperazin i piperidin, koji svi mogu biti prema potrebi supstituirani, pri čemu je bilo koji izborni supstituent neovisno odabran iz skupine koju čine C1-10 alkil; C3-6 cikloalkil; hidroksialkil; C1-10 alkoksi; C2-10 alkenil; C2-10 alkinil; C6-C12 aril; ariloksi; heteroaril; heterociklil; halo; hidroksil; halogenirani alkil; amino; alkilamino; arilamino; acil; amido; CN; NO2; N3; CH2OH; CONH2; CONR24R25; CO2R24; CH2OR24; NHCOR24; NHCO2R24;; C1-3 alkiltio; sulfat; sulfonska kiselina; sulfonatni esteri; fosfonska kiselina; fosfat; fosfonat; mono-, di- ili trifosfatni esteri; tritil; monometoksitrtil; R24SO; R24SO2; CF3S; CF3SO2; i trialkilsilil; pri čemu su R24 i R25 svaki neovisno odabrani između H i C1-10 alkila.
6. Spoj prema bilo kojem od prethodnih zahtjeva, naznačen time, da je R1 odabran iz skupine koju čine tetrahidrofuran, tetrahidropiran, pirolidin, morfolin, piperazin i piperidin, koji svi mogu biti prema potrebi supstituirani, pri čemu je bilo koji izborni supstituent neovisno odabran iz skupine koju čine C1-10 alkil; C3-6 cikloalkil; hidroksialkil; C1-10 alkoksi; C2-10 alkenil; C2-10 alkinil; C6-C12 aril; ariloksi; heteroaril; heterociklil; halo; hidroksil; halogenirani alkil; amino; alkilamino; arilamino; acil; amido; CN; NO2; N3; CH2OH; CONH2; CONR24R25; CO2R24; CH2OR24; NHCOR24; NHCO2R24; C1-3 alkiltio; sulfat; sulfonska kiselina; sulfonatni esteri; fosfonska kiselina; fosfat; fosfonat; mono-, di- ili trifosfatni esteri; tritil; monometoksitrtil; R24SO; R24SO2; CF3S; CF3SO2; i trialkilsilil; pri čemu su R24 i R25 svaki neovisno odabrani između H i C1-10 alkila.
7. Spoj prema bilo kojem od prethodnih zahtjeva, naznačen time, da je R1 odabran iz skupine koju čine pirolidin, piperazin i piperidin, a svi oni mogu biti prema potrebi supstituirani, pri čemu je bilo koji izborni supstituent neovisno odabran iz skupine koju čine C1-10 alkil; C3-6 cikloalkil; hidroksialkil; C1-10 alkoksi; C2-10 alkenil; C2-10 alkinil; C6-C12 aril; ariloksi; heteroaril; heterociklil; halo; hidroksil; halogenirani alkil; amino; alkilamino; arilamino; acil; amido; CN; NO2; N3; CH2OH; CONH2; CONR24R25; CO2R24; CH2OR24; NHCOR24; NHCO2R24; C1-3 alkiltio; sulfat; sulfonska kiselina; sulfonatni esteri; fosfonska kiselina; fosfat; fosfonat; mono-, di- ili trifosfatni esteri; tritil; monometoksitrtil; R24SO; R24SO2; CF3S; CF3SO2; i trialkilsilil; pri čemu su R24 i R25 svaki neovisno odabrani između H i C1-10 alkila.
8. Spoj prema bilo kojem od zahtjeva 1, 2, 3, 5 ili 6, naznačen time, da je R1 odabran iz skupine koja se sastoji od: [image] i u kombinaciji sa svakom takvom R1 skupinom, R2 se neovisno bira iz skupine koju čine: [image] [image] [image] [image]
9. Spoj prema bilo kojem od prethodnih zahtjeva, naznačen time, da se R2 bira između: [image] pri čemu su Y i R5 definirani u bilo kojem od prethodnih zahtjeva.
10. Spoj prema bilo kojem od prethodnih zahtjeva, naznačen time, da se R2 bira između: [image] pri čemu je svaka incidencija Y ugljik, a R5 je vodik ili halo.
11. Spoj prema bilo kojem od prethodnih zahtjeva, naznačen time, da je R2 odabran između supstituiranog ili hidrogeniranog indacena, 2,6-dialkilfenila, 2,6-dialkil-4-halofenila, 2,6-dicikloalkilfenila i 2,6-dicikloalkil-4-halofenila.
12. Spoj prema bilo kojem od prethodnih zahtjeva, naznačen time, da je R2 odabran između heksahidroindacena, 2,6-diizopropilfenil, 2,6-diizopropil-4-klorofenil, 2,6-diciklopropilfenil i 2,6-diciklopropil-4-klorofenila.
13. Spoj prema bilo kojem od prethodnih zahtjeva, naznačen time, da je J atom sumpora.
14. Spoj prema bilo kojem od prethodnih zahtjeva, naznačen time, da je W atom kisika.
15. Spoj prema bilo kojem od prethodnih zahtjeva, naznačen time, da je spoj spoj formule (Ia), (Ib) ili (Ic), ili njegova farmaceutski prihvatljiva sol ili solvat: [image] pri čemu je R1 definiran u bilo kojem od prethodnih zahtjeva.
16. Spoj prema bilo kojem od zahtjeva 1-3, 5-6 ili 8-15, naznačen time, da je spoj odabran iz skupine koju čine: [image] i njihove farmaceutski prihvatljive soli i solvati.
17. Farmaceutski pripravak, naznačen time što sadrži spoj prema bilo kojem od zahtjeva 1 do 16, ili njegova farmaceutski prihvatljiva sol ili solvat, i farmaceutski prihvatljiv nosač, razrjeđivač i/ili pomoćnu tvar.
18. Spoj ili farmaceutski prihvatljiva sol ili solvat prema bilo kojem od zahtjeva 1 do 16, naznačen time, da se koristi u medicini.
19. Spoj ili farmaceutski prihvatljiva sol ili solvat prema bilo kojem od zahtjeva 1 do 16, naznačen time, da se koristi u liječenju ili prevenciji navedenih: (a) bolest, poremećaj ili stanje imunološkog sustava; i/ili (b) upalna bolest, poremećaj ili stanje ili autoimuna bolest, poremećaj ili stanje; i/ili (c) bolest, poremećaj ili stanje kože; i/ili (d) bolest, poremećaj ili stanje kardiovaskularnog sustava; i/ili (e) rak, tumor ili drugi zloćudni tumor; i/ili (f) bolest, poremećaj ili stanje bubrežnog sustava; i/ili (g) bolest, poremećaj ili stanje gastrointestinalnog trakta; i/ili (h) bolest, poremećaj ili stanje dišnog sustava; i/ili (i) bolest, poremećaj ili stanje endokrinog sustava; i/ili (j) bolest, poremećaj ili stanje središnjeg živčanog sustava (CNS); i/ili (k) bolest, poremećaj ili stanje odabrano iz skupine koja se sastoji od konstitutivne upale, uključujući periodične sindrome povezane s kriopirinom (CAPS): Muckle-Wellsov sindrom (MWS), obiteljski hladni autoinflamatorni sindrom (FCAS) i multisustavna upalna bolest s novorođenčetom (NOMID); uključujući autoinflamatorne bolesti: obiteljska mediteranska groznica (FMF), periodični sindrom povezan s TNF receptorima (TRAPS), nedostatak mevalonate kinaze (MKD), hiperimunoglobulinemija D i sindrom periodične groznice (HIDS), nedostatak antagonista receptora za interleukin 1 (DIRA), Majeedov sindrom, piogeni artritis, gangrenozna piodermija i akne (PAPA), haploinsuficijencija A20 (HA20), dječji granulomatozni artritis (PGA), nedostatak protutijela povezan s PLCG2 i imunološka disregulacija (PLAID), autoinflamacija povezana s PLCG2, nedostatak protutijela i imunološka disregulacija , sideroblastična anemija s imunodeficijencijom B-stanica, periodična groznica i zastoj u razvoju (SIFD); Sweetov sindrom, kronični nebakterijski osteomijelitis (CNO), kronični recidivni multifokalni osteomijelitis (CRMO) i sinovitis, akne, pustuloza, hiperostoza, sindrom osteitisa (SAPHO); autoimune bolesti, uključujući multiple sklerozu (MS), dijabetes tipa 1, psorijazu, reumatoidni artritis, Behcetovu bolest, Sjogrenov sindrom i Schnitzlerov sindrom; respiratorne bolesti, uključujući kronični opstruktivni plućni poremećaj (KOPB), steroidno rezistentna astma, azbestoza, silikoza i cistična fibroza; bolesti središnjeg živčanog sustava, uključujući Parkinsonovu bolest, Alzheimerovu bolest, bolest motornih neurona, Huntingtonovu bolest, cerebralnu malariju i ozljedu mozga od pneumokoknog meningitisa; metaboličke bolesti, uključujući dijabetes tipa 2, aterosklerozu, pretilost, giht, pseudo-giht; očne bolesti, uključujući one očnog epitela, starosnu degeneraciju makule (AMD), infekciju rožnice, uveitis i suho oko; bolesti bubrega, uključujući kroničnu bolest bubrega, oksalatnu nefropatiju i dijabetičku nefropatiju; bolesti jetre, uključujući bezalkoholni steatohepatitis i alkoholnu bolest jetre; upalne reakcije na koži, uključujući kontaktnu preosjetljivost i opekline; upalne reakcije u zglobovima, uključujući osteoartritis, sistemski juvenilni idiopatski artritis, Stillova bolest kod odraslih, recidivirajući polihondritis; virusne infekcije, uključujući alfa virus, uključujući Chikungunya i rijeku Ross, i flavivirus, uključujući denga i zika viruse, gripu, HIV; hidradenitis suppurativa (HS) i druge kožne bolesti koje uzrokuju ciste; karcinomi, uključujući metastaze raka pluća, karcinom gušterače, rak želuca, mijelodisplastični sindrom, leukemija; polimiozitis; moždani udar; infarkt miokarda; Kalemljenje naspram bolesti domaćina; hipertenzija; kolitis; infekcija helminthima; bakterijska infekcija; aneurizam trbušne aorte; zarastanje rana; depresija, psihološki stres; perikarditis, uključujući Dresslerov sindrom, reperfuzijsku ozljedu ishemije i bilo koju bolest kod koje je utvrđeno da pojedinac nosi zametnu liniju ili somatsku netihu mutaciju u NLRP3.
20. Spoj ili farmaceutski prihvatljiva sol ili solvat prema bilo kojem od zahtjeva 1 do 16, naznačen time, da se koristi za dijagnosticiranje bolesti, poremećaja ili stanja kod sisavaca, uključujući korak davanja obilježenog spoja prema bilo kojem od zahtjeva 1 do 16., ili njihova farmaceutski prihvatljiva sol ili solvat, ili njegov kompleks helata metalnih iona, sisavcu ili biološkom uzorku dobivenom od sisavca radi olakšavanja dijagnoze bolesti, poremećaja ili stanja sisavca.
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