HRP20180157T1 - Spojevi pirazolopirimidina kao jak-inhibitori i odgovarajući postupci - Google Patents

Spojevi pirazolopirimidina kao jak-inhibitori i odgovarajući postupci Download PDF

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Publication number
HRP20180157T1
HRP20180157T1 HRP20180157TT HRP20180157T HRP20180157T1 HR P20180157 T1 HRP20180157 T1 HR P20180157T1 HR P20180157T T HRP20180157T T HR P20180157TT HR P20180157 T HRP20180157 T HR P20180157T HR P20180157 T1 HRP20180157 T1 HR P20180157T1
Authority
HR
Croatia
Prior art keywords
disease
colitis
pyrazolo
carboxamide
methoxyphenyl
Prior art date
Application number
HRP20180157TT
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English (en)
Inventor
Paul Gibbons
Emily Hanan
Wendy Liu
Joseph P. Lyssikatos
Steven R. Magnuson
Rohan Mendonca
Richard Pastor
Thomas E. Rawson
Michael Siu
Mark E. Zak
Aihe Zhou
Bing-Yan Zhu
Christopher Hurley
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Genentech, Inc.
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Publication date
Application filed by Genentech, Inc. filed Critical Genentech, Inc.
Publication of HRP20180157T1 publication Critical patent/HRP20180157T1/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
    • A61K31/4353Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • 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
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/06Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms

Claims (6)

1. Spoj, naznačen time, da je odabran od sljedećih: N-(4-(5-kloro-2-metoksifenil)-2-(2-hidroksi-2-metilpropil)tiazol-5-il)pirazolo [1,5-a]pirimidin-3-karboksamid; N-(4-(5-kloro-2-metoksifenil)-2-(2-metilprop-1-enil)tiazol-5-il)pirazolo [1,5-a]pirimidin-3-karboksamid; N-(2-bromo-4-(5-kloro-2-metoksifenil)tiazol-5-il)pirazolo[1,5-a]pirimidin-3-karboksamid; N-(4-(5-kloro-2-metoksifenil)tiazol-5-il)pirazolo[1,5-a]pirimidin-3-karboksamid; N-(4-(5-kloro-2-metoksifenil)-2-metiltiazol-5-il)pirazolo[1,5-a]pirimidin-3-karboksamid; N-(4-(5-kloro-2-metoksifenil)-2-(tetrahidro-2H-piran-4-il)tiazol-5-il)pirazolo [1,5-a]pirimidin-3-karboksamid; i njihove farmaceutski prihvatljive soli.
2. Farmaceutski sastav, naznačen time, da obuhvaća spoj prema zahtjevu 1 i farmaceutski prihvatljiv nosač, pomoćno sredstvo ili prijenosno sredstvo.
3. Spoj prema zahtjevu 1, naznačen time, da se upotrebljava u medicini.
4. Terapeutski učinkovita količina spoja prema zahtjevu 1, naznačena time, da se upotrebljava u prevenciji, liječenju ili smanjivanju težine bolesti ili stanja koja/koje je odabrana/odabrano od sljedećih: moždani udar, dijabetes, hepatomegalija, kardiovaskularna bolest, cistična fibroza, virusna bolest, autoimune bolesti, alergijski poremećaji, upala, neurološki poremećaji, bolest koja se odnosi na hormone, stanja povezana s transplantacijom organa, poremećaji imunodeficijencije, poremećaji destrukcije kostiju, proliferativni poremećaji, zarazne bolesti, stanja povezana sa smrću stanice, agregacija pločastih stanica inducirana trombinom, bolesti jetre, patološka imuna stanja koja uključuju aktiviranje T-stanice, CNS poremećaji, ili mijeloproliferativni poremećaj.
5. Spoj za uporabu prema zahtjevu 4, naznačen time, da je bolest ili stanje odabrana/odabrano od sljedećih: rak; kardiovaskularna bolest odabrana od restenoze, kardiomegalije, ateroskleroze, infarkta miokarda ili kongestivnog srčanog zastoja; neurološki poremećaj koji je neurodegenerativna bolest odabrana od Alzheimerove bolesti, Parkinsonove bolesti, amiotrofne lateralne skleroze, Huntingtonove bolesti i cerebralne ishemije; upala koja je upalna bolest odabrana od upalne bolesti crijeva, reumatoidnog artritisa, psorijaze, kontaktnog dermatitisa, ili odgođenih hipersenzitivnih reakcija; autoimuna bolest odabrana od lupusa ili multiple skleroze, Crohnove bolesti, ulcerativnog kolitisa, kolagenoznog kolitisa, limfocitnog kolitisa, ishemijskog kolitisa, diverzijskog kolitisa, Behçetovog sindroma, infektivnog kolitisa i neodređenog kolitisa; i psorijaza.
6. Spoj za uporabu prema zahtjevu 3, naznačen time, da se upotrebljava u prevenciji, liječenju ili smanjivanju težine bolesti ili stanja koja/koje je odabrana/odabrano od sljedećih: rak, policitemija vera, esencijalna trombocitoza, mijelofibroza, kronična mijelogena leukemija (CML), reumatoidni artritis, kronična upalna crijevna bolest, Crohnova bolest, psorijaza, kontaktni dermatitis ili odgođene hipersenzitivne reakcije.
HRP20180157TT 2009-07-02 2018-01-26 Spojevi pirazolopirimidina kao jak-inhibitori i odgovarajući postupci HRP20180157T1 (hr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US22291809P 2009-07-02 2009-07-02
PCT/US2010/040906 WO2011003065A2 (en) 2009-07-02 2010-07-02 Pyrazolopyrimidine jak inhibitor compounds and methods
EP10794815.0A EP2448941B1 (en) 2009-07-02 2010-07-02 Pyrazolopyrimidine jak inhibitor compounds and methods

Publications (1)

Publication Number Publication Date
HRP20180157T1 true HRP20180157T1 (hr) 2018-03-09

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US (5) US8999998B2 (hr)
EP (3) EP2448941B1 (hr)
JP (4) JP5769261B2 (hr)
KR (3) KR101903305B1 (hr)
CN (2) CN102482284B (hr)
AU (1) AU2010266188B2 (hr)
BR (1) BRPI1010197A2 (hr)
CA (1) CA2767097A1 (hr)
CL (1) CL2012000001A1 (hr)
CO (1) CO6491081A2 (hr)
CR (2) CR20170115A (hr)
DK (1) DK2448941T3 (hr)
EC (1) ECSP12011645A (hr)
ES (1) ES2657839T3 (hr)
HR (1) HRP20180157T1 (hr)
HU (1) HUE035537T2 (hr)
IL (3) IL217224B (hr)
IN (1) IN2012DN00755A (hr)
LT (1) LT2448941T (hr)
MA (1) MA33502B1 (hr)
MX (1) MX2012000169A (hr)
MY (1) MY160156A (hr)
NO (1) NO2448941T3 (hr)
NZ (4) NZ738778A (hr)
PE (2) PE20120575A1 (hr)
PH (1) PH12015500666A1 (hr)
PL (1) PL2448941T3 (hr)
PT (1) PT2448941T (hr)
RS (1) RS56671B1 (hr)
RU (2) RU2675857C2 (hr)
SG (2) SG177454A1 (hr)
SI (1) SI2448941T1 (hr)
UA (1) UA110324C2 (hr)
WO (1) WO2011003065A2 (hr)
ZA (2) ZA201200490B (hr)

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