HRP20200263T1 - Upotreba derivata pirazolopirimidina za liječenje poremećaja povezanih sa pi3k - Google Patents

Upotreba derivata pirazolopirimidina za liječenje poremećaja povezanih sa pi3k Download PDF

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HRP20200263T1
HRP20200263T1 HRP20200263TT HRP20200263T HRP20200263T1 HR P20200263 T1 HRP20200263 T1 HR P20200263T1 HR P20200263T T HRP20200263T T HR P20200263TT HR P20200263 T HRP20200263 T HR P20200263T HR P20200263 T1 HRP20200263 T1 HR P20200263T1
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Croatia
Prior art keywords
compound
use according
methyl
ethyl
pharmaceutically acceptable
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HRP20200263TT
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English (en)
Inventor
Yun-Long Li
Wenqing Yao
Andrew P. Combs
Eddy W. Yue
Song MEI
Wenyu Zhu
Joseph Glenn
Maduskuie, Jr.
Richard B. Sparks
Brent Douty
Chunhong He
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Incyte Holdings Corporation
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Publication of HRP20200263T1 publication Critical patent/HRP20200263T1/hr

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • YGENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02ATECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

Claims (19)

1. Spoj za upotrebu u postupku liječenja idiopatske trombocitopenične purpure (ITP), autoimune hemolitične anemije, Behçetove bolesti, Coganovog sindroma, arteritisa divovskih stanica, reumatske polimialgije (PMR), Takayasuvog arteritisa, Buergerove bolesti (lat. thromboangiitis obliterans), vaskulitisa središnjeg živčanog sustava Kawasaki bolesti, poliarteritis nodoze, Churg-Straussovog sindroma, miješanog krioglobulinemičnog vaskulitisa (esencijalnog ili induciranog virusom hepatitisa C (HCV)), Henoch-Schönleinove purpure (HSP), hipersenzitivnog vaskulitisa, mikroskopskog poliangiitisa, Wegenerove granulomatoze, antineutrofilnih citoplazmatskih anititijela povezanih sa (ANCA) sistemskim vaskulitisom (AASV), pemfigusa, membranske nefropatije, kronične limfocitne leukemije (CLL), leukemije dlakavih stanica, limfoma stanice plašta, malog limfocitnog limfoma, folikularnog limfoma, limfoplazmacitnog limfoma, ekstranodalnog limfoma marginalne zone, difuznog B-velikostaničnog limfoma sličnog aktiviranoj B-stanici (ABC), ili difuznog B-velikostaničnog limfoma B-stanice germinalnog centra (GCB) kod pacijenta, gdje je Spoj Formule IV: [image] ili njegova farmaceutski prihvatljiva sol, gdje: G je NH, n je 1, i V je O; ili G je NH, n je 0, i V je CH2; ili G je O, n je 0 i V je NH; R2 je C1-6 alkil ili C1-6 haloalkil; R4 je halo, OH, CN, C1-4 alkil, C1-4 haloalkil, C1-4 alkoksi, ili C1-4 haloalkoksi; R5 je halo, OH, CN, C1-4 alkil, C1-4 haloalkil, C1-4 alkoksi, ili C1-4 haloalkoksi.
2. Spoj za upotrebu prema zahtjevu 1, gdje: a) R2 je C1-3 alkil ili C1-3 fluoroalkil; ili b) R2 je metil, etil, ili 2,2-difluorometil; ili c) R2 je metil; ili d) R2 je etil.
3. Spoj za upotrebu prema zahtjevu 1 ili 2, gdje: a) R4 je halo, CN, ili C1-3 alkil; ili b) R4 je F, Cl, CN, ili metil; ili c) R4 je F; ili d) R4 je Cl; ili e) R4 je CN; ili f) R4 je metil.
4. Spoj za upotrebu prema bilo kojem od zahtjeva 1 do 3, gdje: a) R5 je halo, CN, ili C1-3 alkil; ili b) R5 je Cl, CN, ili metil; ili c) R5 je Cl; ili d) R5 je CN; ili e) R5 je metil.
5. Spoj za upotrebu prema zahtjevu 1, gdje: R2 je C1-3 alkil ili C1-3 fluoroalkil; R4 je halo, CN, ili C1-3 alkil; i R5 je halo, CN, ili C1-3 alkil.
6. Spoj za upotrebu prema zahtjevu 1, gdje: R2 je metil, etil, ili 2,2-difluorometil; R4 je F, Cl, CN, ili metil; i R5 je Cl, CN, ili metil;
7. Spoj za upotrebu prema bilo kojem od zahtjeva 1 do 6, gdje: a) Spoj je Spoj Formule IVa: [image] ili njegova farmaceutski prihvatljiva sol; ili b) Spoj je Spoj Formule IVb: [image] ili njegova farmaceutski prihvatljiva sol; ili c) Spoj je Spoj Formule IVc: [image] ili njegova farmaceutski prihvatljiva sol.
8. Spoj za upotrebu prema zahtjevu 1, gdje je Spoj izabran od: 4-{3-[1-(4-amino-3-metil-1H-pirazolo[3,4-d]pirimidin-1-il)etil]-5-kloro-2-etoksi-6-fluorofenil} pirolidin-2-ona; 4-[1-(4-amino-3-metil-1H-pirazolo[3,4-d]pirimidin-1-il)etil]-6-kloro-3-etoksi-2-(5-oksopirolidin-3-il)benzonitrila; i 4-{3-[1-(4-amino-3-metil-1H-pirazolo[3,4-d]pirimidin-1-il)etil]-5-kloro-2-etoksi-6-fluorofenil}-1,3-oksazolidin-2-ona; ili farmaceutski prihvatljive soli bilo kojeg od gore spomenutog.
9. Spoj za upotrebu prema zahtjevu 1, gdje je postupak postupak za liječenje idiopatske trombocitopenične purpure (ITP) izabrane od relapsirane ITP i refraktorne ITP.
10. Spoj za upotrebu prema zahtjevu 1, gdje je postupak postupak za liječenje pemfigusa.
11. Spoj za upotrebu prema zahtjevu 1, gdje je postupak postupak za liječenje autoimune hemolitičke anemije.
12. Spoj za upotrebu prema zahtjevu 1, gdje je postupak postupak za liječenje limfoma stanica plašta.
13. Spoj za upotrebu prema zahtjevu 1, gdje je postupak postupak za liječenje folikularnog limfoma.
14. Spoj za upotrebu prema zahtjevu 1, gdje je postupak postupak za liječenje ekstranodalnog limfoma marginalne zone.
15. Spoj za upotrebu prema bilo kojem od zahtjeva 1 do 14, gdje je Spoj 4-{3-[1-(4-amino-3-metil-1H-pirazolo[3,4-d]pirimidin-1-il)etil]-5-kloro-2-etoksi-6-fluorofenil}pirolidin-2-on, ili njegova farmaceutski prihvatljiva sol.
16. Spoj za upotrebu prema zahtjevu 15, gdje je Spoj (R)-4-{3-[(R)-1-(4-amino-3-metil-1H-pirazolo[3,4-d]pirimidin-1-il)etil]-5-kloro-2-etoksi-6-fluorofenil}pirolidin-2-on, ili njegova farmaceutski prihvatljiva sol.
17. Spoj za upotrebu prema zahtjevu 15, gdje je Spoj (R)-4-{3-[(S)-1-(4-amino-3-metil-1H-pirazolo[3,4-d]pirimidin-1-il)etil]-5-kloro-2-etoksi-6-fluorofenil}pirolidin-2-on, ili njegova farmaceutski prihvatljiva sol.
18. Spoj za upotrebu prema zahtjevu 15, gdje je Spoj (S)-4-{3-[(R)-1-(4-amino-3-metil-1H-pirazolo[3,4-d]pirimidin-1-il)etil]-5-kloro-2-etoksi-6-fluorofenil}pirolidin-2-on, ili njegova farmaceutski prihvatljiva sol.
19. Spoj za upotrebu prema zahtjevu 15, gdje je Spoj (S)-4-{3-[(S)-1-(4-amino-3-metil-1H-pirazolo[3,4-d]pirimidin-1-il)etil]-5-kloro-2-etoksi-6-fluorofenil}pirolidin-2-on, ili njegova farmaceutski prihvatljiva sol.
HRP20200263TT 2013-03-01 2020-02-17 Upotreba derivata pirazolopirimidina za liječenje poremećaja povezanih sa pi3k HRP20200263T1 (hr)

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Application Number Priority Date Filing Date Title
US201361771480P 2013-03-01 2013-03-01
EP14710739.5A EP2961410B1 (en) 2013-03-01 2014-02-28 Use of pyrazolopyrimidine derivatives for the treatment of pi3k related disorders
PCT/US2014/019372 WO2014134426A1 (en) 2013-03-01 2014-02-28 USE OF PYRAZOLOPYRIMIDINE DERIVATIVES FOR THE TREATMENT OF PI3Kδ RELATED DISORDERS

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PH12015501920B1 (en) 2016-01-18
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