JP2015509973A - 結晶性pi3キナーゼ阻害剤 - Google Patents

結晶性pi3キナーゼ阻害剤 Download PDF

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Publication number
JP2015509973A
JP2015509973A JP2014561515A JP2014561515A JP2015509973A JP 2015509973 A JP2015509973 A JP 2015509973A JP 2014561515 A JP2014561515 A JP 2014561515A JP 2014561515 A JP2014561515 A JP 2014561515A JP 2015509973 A JP2015509973 A JP 2015509973A
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compound
formula
lactose
solid crystalline
anhydrous form
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Japanese (ja)
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JP2015509973A5 (enExample
Inventor
ブロークス,ルデイ・ローラン・マリア
フイリエール,ワルター・フエルデイナンド・マリア
ニーステ,パトリク・ユベール・ジエイ
コプマン,アレツクス・ヘルマン
バンウツト,フイリツプ・マルセル・シー
レイズ,カリナ
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レスピバート・リミテツド
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Publication of JP2015509973A publication Critical patent/JP2015509973A/ja
Publication of JP2015509973A5 publication Critical patent/JP2015509973A5/ja
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    • 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
    • A61K31/495Heterocyclic 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
    • A61K31/52Purines, e.g. adenine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/12Carboxylic acids; Salts or anhydrides thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/26Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/007Pulmonary tract; Aromatherapy
    • A61K9/0073Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/007Pulmonary tract; Aromatherapy
    • A61K9/0073Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy
    • A61K9/0075Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy for inhalation via a dry powder inhaler [DPI], e.g. comprising micronized drug mixed with lactose carrier particles
    • 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
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/14Antitussive agents
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/04Antineoplastic agents specific for metastasis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Organic Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pulmonology (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Otolaryngology (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Oncology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
JP2014561515A 2012-03-13 2013-03-13 結晶性pi3キナーゼ阻害剤 Pending JP2015509973A (ja)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201261610023P 2012-03-13 2012-03-13
US201261610012P 2012-03-13 2012-03-13
US61/610,023 2012-03-13
US61/610,012 2012-03-13
PCT/GB2013/050624 WO2013136076A1 (en) 2012-03-13 2013-03-13 Crystalline pi3 kinase inhibitors

Related Child Applications (1)

Application Number Title Priority Date Filing Date
JP2017151378A Division JP2018008992A (ja) 2012-03-13 2017-08-04 結晶性pi3キナーゼ阻害剤

Publications (2)

Publication Number Publication Date
JP2015509973A true JP2015509973A (ja) 2015-04-02
JP2015509973A5 JP2015509973A5 (enExample) 2016-04-14

Family

ID=49160309

Family Applications (3)

Application Number Title Priority Date Filing Date
JP2014561515A Pending JP2015509973A (ja) 2012-03-13 2013-03-13 結晶性pi3キナーゼ阻害剤
JP2014561514A Expired - Fee Related JP6189874B2 (ja) 2012-03-13 2013-03-13 新規製薬学的製剤
JP2017151378A Withdrawn JP2018008992A (ja) 2012-03-13 2017-08-04 結晶性pi3キナーゼ阻害剤

Family Applications After (2)

Application Number Title Priority Date Filing Date
JP2014561514A Expired - Fee Related JP6189874B2 (ja) 2012-03-13 2013-03-13 新規製薬学的製剤
JP2017151378A Withdrawn JP2018008992A (ja) 2012-03-13 2017-08-04 結晶性pi3キナーゼ阻害剤

Country Status (35)

Country Link
US (3) US9642799B2 (enExample)
EP (2) EP2825202B1 (enExample)
JP (3) JP2015509973A (enExample)
KR (2) KR20140131971A (enExample)
CN (2) CN104302650B (enExample)
AU (2) AU2013234080B2 (enExample)
CA (2) CA2864652A1 (enExample)
CL (2) CL2014002385A1 (enExample)
CO (2) CO7061079A2 (enExample)
CR (2) CR20140417A (enExample)
CY (1) CY1118565T1 (enExample)
DK (1) DK2834244T3 (enExample)
EA (2) EA025465B1 (enExample)
EC (2) ECSP14018142A (enExample)
ES (2) ES2650791T3 (enExample)
GT (2) GT201400182A (enExample)
HR (1) HRP20161383T1 (enExample)
HU (1) HUE029420T2 (enExample)
IL (2) IL233883A0 (enExample)
IN (2) IN2014MN02000A (enExample)
LT (1) LT2834244T (enExample)
MX (2) MX357170B (enExample)
MY (1) MY171125A (enExample)
NI (2) NI201400101A (enExample)
NZ (2) NZ627963A (enExample)
PE (2) PE20142342A1 (enExample)
PH (2) PH12014501713A1 (enExample)
PL (1) PL2834244T3 (enExample)
PT (1) PT2834244T (enExample)
SG (2) SG11201404522VA (enExample)
SI (1) SI2834244T1 (enExample)
TW (2) TWI586378B (enExample)
UA (1) UA115544C2 (enExample)
WO (2) WO2013136076A1 (enExample)
ZA (2) ZA201407373B (enExample)

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