HRP20180411T1 - Predlijekovi inhibitora aminokinazolinske kinaze - Google Patents

Predlijekovi inhibitora aminokinazolinske kinaze Download PDF

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Publication number
HRP20180411T1
HRP20180411T1 HRP20180411TT HRP20180411T HRP20180411T1 HR P20180411 T1 HRP20180411 T1 HR P20180411T1 HR P20180411T T HRP20180411T T HR P20180411TT HR P20180411 T HRP20180411 T HR P20180411T HR P20180411 T1 HRP20180411 T1 HR P20180411T1
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Croatia
Prior art keywords
pharmaceutically acceptable
hydrate
compound
acceptable salt
butylsulfonyl
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HRP20180411TT
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English (en)
Inventor
Linda N. Casillas
Pamela A. Haile
Robert W. Marquis
Gren WANG
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Glaxosmithkline Intellectual Property Development Limited
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Application filed by Glaxosmithkline Intellectual Property Development Limited filed Critical Glaxosmithkline Intellectual Property Development Limited
Publication of HRP20180411T1 publication Critical patent/HRP20180411T1/hr

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/075Ethers or acetals
    • A61K31/085Ethers or acetals having an ether linkage to aromatic ring nuclear carbon
    • A61K31/09Ethers or acetals having an ether linkage to aromatic ring nuclear carbon having two or more such linkages
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/185Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19Carboxylic acids, e.g. valproic acid
    • A61K31/195Carboxylic acids, e.g. valproic acid having an amino group
    • A61K31/197Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid, pantothenic acid
    • A61K31/198Alpha-aminoacids, e.g. alanine, edetic acids [EDTA]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/38Heterocyclic compounds having sulfur as a ring hetero atom
    • A61K31/381Heterocyclic compounds having sulfur as a ring hetero atom having five-membered 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
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425Thiazoles
    • A61K31/428Thiazoles condensed with carbocyclic 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
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/433Thidiazoles
    • 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
    • A61K31/517Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic System
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6561Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings

Claims (11)

1. Spoj, naznačen time što je 2-((4-(benzo[d]tiazol-5-ilamino)-6-(terc-butilsulfonil)kinazolin-7-il)oksi)etil-dihidrogenfosfat, formule: [image] ili njegova farmaceutski prihvatljiva sol, ili njezin hidrat.
2. Spoj, ili njegova farmaceutski prihvatljiva sol, ili njezin hidrat, u skladu s patentnim zahtjevom 1, naznačen time što je 2-((4-(benzo[d]tiazol-5-ilamino)-6-(terc-butilsulfonil)kinazolin-7-il)oksi)etil-dihidrogenfosfat.
3. Spoj, ili njegova farmaceutski prihvatljiva sol, ili njezin hidrat, u skladu s patentnim zahtjevom 1, naznačen time što je dinatrijev 2-((4-(benzo[d]tiazol-5-ilamino)-6-(terc-butilsulfonil)kinazolin-7-il)oksi)etil-fosfat.
4. Spoj, ili njegova farmaceutski prihvatljiva sol, ili njezin hidrat, u skladu s patentnim zahtjevom 1, naznačen time što je kalcijev (I) 2-((4-(benzo[d]tiazol-5-ilamino)-6-(terc-butilsulfonil)kinazolin-7-il)oksi)etil-hidrogenfosfat trihidrat.
5. Spoj, ili njegova farmaceutski prihvatljiva sol, ili njezin hidrat, u skladu s patentnim zahtjevom 1, naznačen time što je 2-((4-(benzo[d]tiazol-5-ilamino)-6-(terc-butilsulfonil)kinazolin-7-il)oksi)etil-dihidrogenfosfat-hidroklorid monohidrat.
6. Farmaceutski pripravak, naznačen time što sadrži spoj, ili njegovu farmaceutski prihvatljivu sol, ili njezin hidrat, u skladu s bilo kojim od patentnih zahtjeva 1 do 5, kao i farmaceutski prihvatljivu pomoćnu tvar.
7. Spoj, ili njegova farmaceutski prihvatljiva sol, ili njezin hidrat u skladu s bilo kojim od patentnih zahtjeva 1 do 5, naznačen time što je namijenjen upotrebi u terapiji.
8. Spoj ili njegova farmaceutski prihvatljiva sol, ili njezin hidrat, u skladu s bilo kojim od patentnih zahtjeva 1 do 5, naznačen time što je namijenjen upotrebi u liječenju bolesti ili poremećaja koji se bira između uveitisa, sindroma groznice povezanim s interleukin-1-konvertirajućim enzimom, dermatitisa, akutne ozljede pluća, dijabetesa melitusa tip 2, artritisa, reumatoidnog artritisa, ulceroznog kolitisa, Crohnove bolesti, upalne crijevne bolesti s ranim početkom, ekstraintestinalne upalne crijevne bolesti, sprječavanja ishemijsko-reperfuzijske ozljede u presatku čvrstog organa, nealkoholnog steatohepatitisa, alkoholnog steatohepatitisa, autoimunog hepatitisa, astme, reakcije presatka prema domaćinu, sistemnog eritematoznog lupusa, multiple skleroze, sarkoidoze, Blauovog sindroma/sarkoidoze s ranim početkom, Wegnerove granulomatoze, te intersticijske plućne bolesti.
9. Spoj, ili njegova farmaceutski prihvatljiva sol, ili njezin hidrat, namijenjen upotrebi u skladu s patentnim zahtjevom 8, naznačen time što se bolest ili poremećaj bira između Crohnove bolesti, ulceroznog kolitisa i Blauovog sindroma.
10. Spoj, ili njegova farmaceutski prihvatljiva sol, ili njezin hidrat, u skladu s patentnim zahtjevom 4, naznačen time što je kristalni kalcijev (I) 2-((4-(benzo[d]tiazol-5-ilamino)-6-(terc-butilsulfonil)kinazolin-7-il)oksi)etil-hidrogenfosfat trihidrat, koji ima PXRD kao na Slici 1.
11. Spoj, ili njegova farmaceutski prihvatljiva sol, ili njezin hidrat, u skladu s patentnim zahtjevom 5, naznačen time što je kristalni 2-((4-(benzo[d]tiazol-5-ilamino)-6-(terc-butilsulfonil)kinazolin-7-il)oksi)etil-dihidrogenfosfat-hidroklorid monohidrat, koji ima PXRD kao na Slici 2.
HRP20180411TT 2012-09-13 2018-03-08 Predlijekovi inhibitora aminokinazolinske kinaze HRP20180411T1 (hr)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US201261700422P 2012-09-13 2012-09-13
US201361767387P 2013-02-21 2013-02-21
PCT/US2013/059619 WO2014043446A1 (en) 2012-09-13 2013-09-13 Prodrugs of amino quinazoline kinase inhibitor
EP13837571.2A EP2895174B1 (en) 2012-09-13 2013-09-13 Prodrugs of amino quinazoline kinase inhibitor

Publications (1)

Publication Number Publication Date
HRP20180411T1 true HRP20180411T1 (hr) 2018-04-20

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ID=50278703

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Application Number Title Priority Date Filing Date
HRP20180411TT HRP20180411T1 (hr) 2012-09-13 2018-03-08 Predlijekovi inhibitora aminokinazolinske kinaze

Country Status (33)

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US (3) US9586953B2 (hr)
EP (2) EP3323819B1 (hr)
JP (1) JP6246813B2 (hr)
KR (1) KR102101527B1 (hr)
CN (1) CN104619327B (hr)
AR (1) AR092529A1 (hr)
AU (1) AU2013315396B2 (hr)
BR (1) BR112015005694A2 (hr)
CA (1) CA2886467C (hr)
CL (1) CL2015000614A1 (hr)
CR (1) CR20150132A (hr)
CY (1) CY1120236T1 (hr)
DK (1) DK2895174T3 (hr)
DO (1) DOP2015000060A (hr)
EA (1) EA028146B1 (hr)
ES (1) ES2663237T3 (hr)
HK (2) HK1212223A1 (hr)
HR (1) HRP20180411T1 (hr)
HU (1) HUE036347T2 (hr)
IL (1) IL237263B (hr)
LT (1) LT2895174T (hr)
ME (1) ME02985B (hr)
MX (1) MX371356B (hr)
NZ (1) NZ628452A (hr)
PE (1) PE20150635A1 (hr)
PH (1) PH12015500363B1 (hr)
PL (1) PL2895174T3 (hr)
PT (1) PT2895174T (hr)
RS (1) RS57144B1 (hr)
SG (1) SG11201501139RA (hr)
SI (1) SI2895174T1 (hr)
TW (1) TWI592417B (hr)
WO (1) WO2014043446A1 (hr)

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