DK2895174T3 - Prolægemidler af aminoquinazolin-kinase inhibitor - Google Patents

Prolægemidler af aminoquinazolin-kinase inhibitor Download PDF

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DK2895174T3
DK2895174T3 DK13837571.2T DK13837571T DK2895174T3 DK 2895174 T3 DK2895174 T3 DK 2895174T3 DK 13837571 T DK13837571 T DK 13837571T DK 2895174 T3 DK2895174 T3 DK 2895174T3
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compound
pharmaceutically acceptable
acceptable salt
benzo
oxy
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DK13837571.2T
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Linda N Casillas
Pamela A Haile
Robert W Marquis Jr
Gren Wang
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Glaxosmithkline Ip Dev Ltd
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic 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
    • C07D417/02—Heterocyclic 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
    • C07D417/12—Heterocyclic 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/075—Ethers or acetals
    • A61K31/085—Ethers or acetals having an ether linkage to aromatic ring nuclear carbon
    • A61K31/09—Ethers or acetals having an ether linkage to aromatic ring nuclear carbon having two or more such linkages
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
    • A61K31/197—Carboxylic 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 or pantothenic acid
    • A61K31/198—Alpha-amino acids, e.g. alanine or edetic acid [EDTA]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/38—Heterocyclic compounds having sulfur as a ring hetero atom
    • A61K31/381—Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic 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
    • A61K31/425—Thiazoles
    • A61K31/428—Thiazoles condensed with carbocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic 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
    • A61K31/433—Thidiazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6561—Heterocyclic 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Pulmonology (AREA)
  • Rheumatology (AREA)
  • Endocrinology (AREA)
  • Transplantation (AREA)
  • Dermatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Emergency Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)

Claims (11)

1, Forbindelse, som er 2 - (( 4 -{ b e n zo [d] th i a zoi - 5 - y i a m i n o) - 6 - (tert-b uty I s u i f o n y S} -quinazoiin“7-yl)oxy)ethyidihydrogenphosphat med formlen:
eller et farmaceutisk acceptabelt salt deraf eller et. hydrat deraf,
2, Forbindelse eller farmaceutisk acceptabelt salt deraf eller hydrat deraf Ifølge krav if som er 2-((4-{benzo[d]thiazQi-5-yiamino3-6-{t'e.ri'-butyisuifony!3quinaz:o!in-?-y i }oxy)-ethyl-dihydrogenphosphat,
3, Forbindelse eller farmaceutisk acceptabelt salt deraf eller hydrat deraf Ifølge krav 1, som er 2-((4-(&βηζο[03^·3£θΙ-5-γΐ3ηιϊηο}-6“(ί'β/ΐ··5υίνΐ5υΙίοηγΙ^υϊη3ΖθΙιη·-7-γ!)οχν)“ ethyldinatriumphcsphat,
4, Forbindelse eller farmaceutisk acceptabelt salt deraf eller hydrat deraf ifølge krav 1, hvilket er €8ίαυηι(Ι}-2~({4~φβηζο[^3^ί8ΖθΙ~5-γΐ8ηιίηο3-6~(ίβΓί^ηΐγΐ5ϋΙί0ηγΙ)-quinazø!in-7-yi)øxy}ethy!hydrogenpho$phattrihydrat,
5, Forbindelse eller farmaceutisk acceptabelt salt deraf eller hydrat deraf ifølge krav i, søm er 2~((4-{benzQ[d]thiazoi-5~y!aminQ)~6-{te/t~buty!suiforsy!)quinazo!in~7-yi)oxy)-ethySdlhydrogenphosphathydrochloridmcnohydrat.
6, Farmaceutisk præparat omfattende forbindelsen eller farmaceutisk acceptabelt salt deraf eller hydrat deraf Ifølge et hvilket som helst af kravene 1 til 5 og en farmaceutisk acceptabel excipiens,
7, Forbindelse eller farmaceutisk acceptabelt salt deraf eller et hydrat deraf ifølge et hvilket som helst af kravene i til 5 til anvendelse i terapi,
8, Forbindelse eller farmaceutisk acceptabelt salt deraf eller hydrat deraf ifølge et hvilket som helst af kravene i til 5 til anvendelse tii behandling af en sygdom eller lidelse valgt blandt uveitis, Interleukin-i-omdannende enzym-associeret feber-syndrom, dermatitis, akutte lungeskader, type 2 diabetes meilltus, arthritis, reumatold arthritis, uicerøs colitis, Crohns sygdom, tidligt indtrædende inflammatorisk tarmsygdomme, ekstrakfcestlnai inflammatorisk tarmsygdom, forebyggelse af iskæmie-reperfusionsskade ved fast organ-transplantation, non-alkoholisk steatohepatitls, aSkohoistatohepatstis, au to irn mu o hepatitis, astma, transplantat versus vært sygdom, systemisk lupus erythematosus, multipel sklerose, sarcoidose, Blau syndrom/tidilgt indtrædende sarcoidose, Wegner's granuiomatose og infcerstitfel lungesygdom,
9, Forbindelse eller farmaceutisk acceptabelt salt deraf eller hydrat deraf til anvendelse ifølge krav 8, hvor sygdommen eller lidelsen er valgt blandt Crohns sygdom, uicera- tiv colitis og 8!au syndrom.
10. Forbindelse eller farmaceutisk acceptabelt salt deraf eller hydrat deraf Ifølge krav 4, som er krystallinsk calc}um(I)-2-((4-(benzo[d]t.hia7.o!"5-yiamino)"6-{tert"butylsulfonyl)-qulnazo!in-7-yl)oxy}ethy!hydrogenphosphattrihydrat med PXRD i figur 1,
11. Forbindelse eller farmaceutisk acceptabelt salt deraf eller hydrat deraf ifølge krav 5, hvilket er krystallinsk 2-((4~(benzo[d3:thiazoi~5-yiamino)-6-(ferf-butyisuifonyl)-quinazo!in-7-yl)oxy}efchy!dihydrogenphosphathydrochioridmonohydrat med PXRD I figur 2.
DK13837571.2T 2012-09-13 2013-09-13 Prolægemidler af aminoquinazolin-kinase inhibitor DK2895174T3 (da)

Applications Claiming Priority (3)

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

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DK2895174T3 true DK2895174T3 (da) 2018-02-26

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EP (2) EP3323819B1 (da)
JP (1) JP6246813B2 (da)
KR (1) KR102101527B1 (da)
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AR (1) AR092529A1 (da)
AU (1) AU2013315396B2 (da)
BR (1) BR112015005694A2 (da)
CA (1) CA2886467C (da)
CL (1) CL2015000614A1 (da)
CR (1) CR20150132A (da)
CY (1) CY1120236T1 (da)
DK (1) DK2895174T3 (da)
DO (1) DOP2015000060A (da)
EA (1) EA028146B1 (da)
ES (1) ES2663237T3 (da)
HK (2) HK1212223A1 (da)
HR (1) HRP20180411T1 (da)
HU (1) HUE036347T2 (da)
IL (1) IL237263B (da)
LT (1) LT2895174T (da)
ME (1) ME02985B (da)
MX (1) MX371356B (da)
NZ (1) NZ628452A (da)
PE (1) PE20150635A1 (da)
PH (1) PH12015500363A1 (da)
PL (1) PL2895174T3 (da)
PT (1) PT2895174T (da)
RS (1) RS57144B1 (da)
SG (1) SG11201501139RA (da)
SI (1) SI2895174T1 (da)
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