HRP20161036T1 - IMIDAZOPIRAZIN Syk INHIBITORI - Google Patents

IMIDAZOPIRAZIN Syk INHIBITORI Download PDF

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Publication number
HRP20161036T1
HRP20161036T1 HRP20161036TT HRP20161036T HRP20161036T1 HR P20161036 T1 HRP20161036 T1 HR P20161036T1 HR P20161036T T HRP20161036T T HR P20161036TT HR P20161036 T HRP20161036 T HR P20161036T HR P20161036 T1 HRP20161036 T1 HR P20161036T1
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Croatia
Prior art keywords
pharmaceutically acceptable
compound
acceptable salt
leukemia
lymphoma
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HRP20161036TT
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English (en)
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Scott A. Mitchell
Kevin S. Currie
Peter A. Blomgren
Jeffrey E. Kropf
Seung H. Lee
Jianjun Xu
Douglas G. Stafford
James P. Harding
Antonio J. Barbosa
Zhongdong Zhao
David M Armistead
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Gilead Connecticut, Inc. c/o Gilead Sciences, Inc.
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Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=42242994&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=HRP20161036(T1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Gilead Connecticut, Inc. c/o Gilead Sciences, Inc. filed Critical Gilead Connecticut, Inc. c/o Gilead Sciences, Inc.
Publication of HRP20161036T1 publication Critical patent/HRP20161036T1/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
    • A61K31/495Heterocyclic 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
    • 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
    • A61K31/498Pyrazines or piperazines ortho- and peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
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    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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    • A61P35/00Antineoplastic agents
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
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    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
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    • C07D491/02Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
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    • C12Q1/00Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions
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    • C12Q1/485Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving transferase involving kinase
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    • G01MEASURING; TESTING
    • G01NINVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
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    • G01N33/48Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
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    • G01N2333/00Assays involving biological materials from specific organisms or of a specific nature
    • G01N2333/90Enzymes; Proenzymes
    • G01N2333/91Transferases (2.)
    • G01N2333/912Transferases (2.) transferring phosphorus containing groups, e.g. kinases (2.7)
    • G01N2333/91205Phosphotransferases in general

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Claims (17)

1. Spoj koji ima strukturu: [image] ili njegova farmaceutski prihvatljiva sol.
2. Farmaceutski pripravak naznačen time da sadrži: spoj iz patentnog zahtjeva 1, ili njegovu farmaceutski prihvatljivu sol; i najmanje jedan farmaceutski prihvatljiv nosač, odabrano iz skupine koja se sastoji od nosača, adjuvanata, i ekscipijenata.
3. Spoj iz patentnog zahtjeva 1, ili njegova farmaceutski prihvatljiva sol, naznačen time da je za upotrebu u postupku liječenja osobe kojoj je to potrebno.
4. Spoj iz patentnog zahtjeva 1, ili njegova farmaceutski prihvatljiva sol, naznačen time da je za upotrebu u postupku liječenja osobe koja ima bolest koja reagira na inhibiciju Syk aktivnosti odabrano iz, liječenja karcinoma, uključujući B-stanični limfom i leukemiju, alergijske poremećaje, autoimune bolesti i inflamatorne bolesti kao što su: SLE, reumatični artritis, multiple vaskulitidi, idiopatska trombocitopenijska purpura (ITP), mijastenija gravis, alergijski rinitis, kronična opstruktivna bolest pluća ("COPD"), sindrom akutnog respiratornog poremećaja odraslih ("ARDs") i astma.
5. Spoj iz patentnog zahtjeva 1, ili njegova farmaceutski prihvatljiva sol, naznačen time da je za upotrebu u postupku liječenja osobe koja ima bolest izabranu iz grupe koja se sastoji od karcinoma, autoimune bolesti, inflamatorne bolesti, i alergijskog poremećaja.
6. Spoj iz patentnog zahtjeva 1, ili njegova farmaceutski prihvatljiva sol, naznačen time da je za upotrebu u postupku liječenja osobe koja ima karcinom.
7. Spoj iz patentnog zahtjeva 1, ili njegova farmaceutski prihvatljiva sol, naznačen time da je za upotrebu u postupku liječenja osobe koja ima limfom ili leukemiju.
8. Spoj iz patentnog zahtjeva 1, ili njegova farmaceutski prihvatljiva sol, naznačen time da je za upotrebu u postupku liječenja osobe koja ima bolest izabranu iz grupe koja se sastoji od B-ćelijskog limfoma, Hodgkin’sovog limfoma, ne-Hodgkin’sovog limfoma, leukemija "hairy" stanica (kronična limfoidna leukemija), multipli mijeloma, kronične mijeloidne leukemije, akutne mijeloidne leukemije, kronične limfocitne leukemije, i akutne limfocitne leukemije.
9. Spoj za upotrebu prema bilo kojem od patentnih zahtjeva od 3 do 8, ili njegova farmaceutski prihvatljiva sol, naznačen time da je dan osobi, u kombinaciji sa jednim ili više dodatnih aktivnih agenasa.
10. Spoj iz patentnog zahtjeva 1, ili njegova farmaceutski prihvatljiva sol, naznačen time da je za upotrebu u postupku liječenja karcinoma kod osobe kojoj je to potrebno, obuhvaća primjenu na ljude terapeutski efikasne količine spoja ili farmaceutski prihvatljive soli zajedno sa drugim aktivnim agensom korisnim u liječenju karcinoma.
11. Spoj za upotrebu prema patentnom zahtjevu 10, ili njegova farmaceutski prihvatljiva sol, naznačen time da se drugi aktivni agens primjenjuje prije, istovremeno, ili nakon tretmana sa spojem ili farmaceutski prihvatljivom soli.
12. Spoj za upotrebu prema patentnom zahtjevu 10 ili 11, ili njegova farmaceutski prihvatljiva sol, naznačen time da je karcinom limfom ili leukemija.
13. Spoj za upotrebu prema patentnom zahtjevu 12, ili njegova farmaceutski prihvatljiva sol, naznačen time da su limfom ili leukemija odabrani iz grupe koja se sastoji od B-ćelijskog limfoma, Hodgkin’sovog limfoma, ne-Hodgkin’sovog limfoma, leukemije "hairy" stanica (kronična limfoidna leukemija), multiple mijeloma, kronične mijeloidne leukemije, akutne mijeloidne leukemije, kronične limfocitne leukemije, i akutne limfocitne leukemije.
14. Spoj iz patentnog zahtjeva 1, ili njegova farmaceutski prihvatljiva sol, naznačen time da je za upotrebu u postupku povećanja osjetljivosti stanica karcinoma na kemoterapiju kod osobe koja je podvrgnuta kemoterapiji sa hemoterapeutskim agensom.
15. Postupak za utvrđivanje prisustva Syk-a u uzorku, naznačen time da sadrži kontakt uzorka sa spojem iz patentnog zahtjeva 1, ili njegovom farmaceutski prihvatljivom soli, pod uvjetima koji dozvoljavaju detekciju Syk aktivnosti, detektiranje nivoa Syk aktivnosti u uzorku, i iz toga utvrđivanje prisustva ili odsustva Syk-a u uzorku.
16. In vitro postupak za inhibiciju B-stanične aktivnosti naznačen time da obuhvaća kontakt stanica sa ekspresijom Syk sa Spojm iz patentnog zahtjeva 1, ili njegovim farmaceutski prihvatljivim solima, u količini dovoljnoj da detektirano umanji razinu B-stanične aktivnosti in vitro.
17. In vitro postupak za inhibiranje ATP hidrolize, naznačen time da postupak obuhvaća kontaktiranje stanica koje eksprimiraju Syk sa spojem iz patentnog zahtjeva 1, ili njegovim farmaceutski prihvatljivim solima, u količini dovoljnoj da detektirano umanji nivo ATP hidrolize in vitro.
HRP20161036TT 2008-12-08 2016-08-17 IMIDAZOPIRAZIN Syk INHIBITORI HRP20161036T1 (hr)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US12058708P 2008-12-08 2008-12-08
US14051408P 2008-12-23 2008-12-23
US24097909P 2009-09-09 2009-09-09
EP13005979.3A EP2716157B1 (en) 2008-12-08 2009-12-07 Imidazopyrazine Syk inhibitors

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HRP20161036T1 true HRP20161036T1 (hr) 2017-06-16

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HRP20161036TT HRP20161036T1 (hr) 2008-12-08 2016-08-17 IMIDAZOPIRAZIN Syk INHIBITORI

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US (7) US8455493B2 (hr)
EP (3) EP2716157B1 (hr)
JP (4) JP5567587B2 (hr)
KR (4) KR20170066685A (hr)
CN (2) CN104744476B (hr)
AU (1) AU2009325132B2 (hr)
BR (1) BRPI0922225B1 (hr)
CA (1) CA2746023C (hr)
CL (1) CL2011001360A1 (hr)
CO (1) CO6390078A2 (hr)
CY (1) CY1118377T1 (hr)
DK (1) DK2716157T3 (hr)
EA (3) EA201690111A1 (hr)
ES (2) ES2545610T3 (hr)
HR (1) HRP20161036T1 (hr)
HU (1) HUE030427T2 (hr)
IL (3) IL213365A (hr)
LT (1) LT2716157T (hr)
MX (1) MX2011006091A (hr)
NZ (1) NZ593459A (hr)
PE (2) PE20140975A1 (hr)
PL (2) PL2373169T3 (hr)
PT (2) PT2373169E (hr)
RS (1) RS55055B1 (hr)
SG (1) SG171991A1 (hr)
SI (2) SI2373169T1 (hr)
SM (1) SMT201600267B (hr)
TW (2) TWI478922B (hr)
VN (1) VN28228A1 (hr)
WO (1) WO2010068257A1 (hr)

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