AU2015364557C1 - Pharmaceutical formulations of tropomyosin related kinase (Trk) inhibitors - Google Patents

Pharmaceutical formulations of tropomyosin related kinase (Trk) inhibitors Download PDF

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Publication number
AU2015364557C1
AU2015364557C1 AU2015364557A AU2015364557A AU2015364557C1 AU 2015364557 C1 AU2015364557 C1 AU 2015364557C1 AU 2015364557 A AU2015364557 A AU 2015364557A AU 2015364557 A AU2015364557 A AU 2015364557A AU 2015364557 C1 AU2015364557 C1 AU 2015364557C1
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AU
Australia
Prior art keywords
benzyl
methoxy
imidazo
pyridin
pyrazol
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AU2015364557A
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English (en)
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AU2015364557B2 (en
AU2015364557A1 (en
Inventor
Chris Ho
Harvey Lieberman
C. Michael Philbrook
Michael Santos
Donglai Yang
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Genzyme Corp
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Genzyme Corp
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    • 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
    • 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
    • A61K31/435—Heterocyclic 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
    • A61K31/4353—Heterocyclic 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
    • A61K31/437—Heterocyclic 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/26—Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/32—Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers, poly(meth)acrylates, or polyvinyl pyrrolidone
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/34—Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1682—Processes
    • A61K9/1694—Processes resulting in granules or microspheres of the matrix type containing more than 5% of excipient
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
    • A61K9/5005—Wall or coating material
    • A61K9/5021—Organic macromolecular compounds
    • A61K9/5026—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • 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
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A61P29/02—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] without antiinflammatory effect
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic 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
    • C07D471/02—Heterocyclic 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
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Organic Chemistry (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Dermatology (AREA)
  • Immunology (AREA)
  • Inorganic Chemistry (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
AU2015364557A 2014-12-18 2015-12-17 Pharmaceutical formulations of tropomyosin related kinase (Trk) inhibitors Active AU2015364557C1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201462093801P 2014-12-18 2014-12-18
US62/093,801 2014-12-18
PCT/US2015/066396 WO2016100677A2 (en) 2014-12-18 2015-12-17 Pharmaceutical formulations of tropomyosin related kinase (trk) inhibitors

Publications (3)

Publication Number Publication Date
AU2015364557A1 AU2015364557A1 (en) 2017-08-03
AU2015364557B2 AU2015364557B2 (en) 2021-04-29
AU2015364557C1 true AU2015364557C1 (en) 2021-11-18

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AU2015364557A Active AU2015364557C1 (en) 2014-12-18 2015-12-17 Pharmaceutical formulations of tropomyosin related kinase (Trk) inhibitors

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US (4) US10219998B2 (cg-RX-API-DMAC10.html)
EP (1) EP3233057A2 (cg-RX-API-DMAC10.html)
JP (1) JP6606183B2 (cg-RX-API-DMAC10.html)
KR (1) KR102561692B1 (cg-RX-API-DMAC10.html)
CN (2) CN107231803B (cg-RX-API-DMAC10.html)
AR (1) AR103176A1 (cg-RX-API-DMAC10.html)
AU (1) AU2015364557C1 (cg-RX-API-DMAC10.html)
BR (1) BR112017012566B1 (cg-RX-API-DMAC10.html)
CA (1) CA2970938C (cg-RX-API-DMAC10.html)
CL (1) CL2017001543A1 (cg-RX-API-DMAC10.html)
CO (1) CO2017007118A2 (cg-RX-API-DMAC10.html)
EA (1) EA201791336A1 (cg-RX-API-DMAC10.html)
IL (1) IL252901B (cg-RX-API-DMAC10.html)
MA (1) MA40698A3 (cg-RX-API-DMAC10.html)
MX (2) MX387694B (cg-RX-API-DMAC10.html)
MY (1) MY195799A (cg-RX-API-DMAC10.html)
NZ (1) NZ733825A (cg-RX-API-DMAC10.html)
PH (1) PH12017501121A1 (cg-RX-API-DMAC10.html)
SG (1) SG11201704872RA (cg-RX-API-DMAC10.html)
TN (1) TN2017000234A1 (cg-RX-API-DMAC10.html)
TW (2) TWI696621B (cg-RX-API-DMAC10.html)
WO (1) WO2016100677A2 (cg-RX-API-DMAC10.html)

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MA40698A3 (fr) 2014-12-18 2020-01-31 Genzyme Corp Formulations pharmaceutiques d'inhibiteurs de kinase associée à la tropomyosine (trk)
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AR114110A1 (es) 2018-02-28 2020-07-22 Lilly Co Eli Anticuerpo anti-trka
EP4180428A1 (en) * 2021-11-12 2023-05-17 Genzyme Corporation Crystalline imidazo[4,5-b]pyridine compound, pharmaceutical compositions, and their use in treating medical conditions
JP2025503380A (ja) * 2022-01-14 2025-02-04 ダイメリックス バイオサイエンス ピーティーワイ リミテッド ケモカインレセプター経路インヒビターを含む組成物
CN114712365B (zh) * 2022-06-07 2022-08-23 山东绿叶制药有限公司 Trk抑制剂在制备治疗迟发性运动障碍药物中的应用
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WO2013176970A1 (en) * 2012-05-22 2013-11-28 Merck Sharp & Dohme Corp. TrkA KINASE INHIBITORS, COMPOSITIONS AND METHODS THEREOF

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CA2970938C (en) 2023-04-18
WO2016100677A3 (en) 2016-08-11
WO2016100677A2 (en) 2016-06-23
US10219998B2 (en) 2019-03-05
BR112017012566B1 (pt) 2024-01-30
CN110950862A (zh) 2020-04-03
MA40698A2 (fr) 2018-10-31
KR20170096160A (ko) 2017-08-23
PH12017501121B1 (en) 2017-11-27
TWI780438B (zh) 2022-10-11
MX2017008058A (es) 2017-09-28
SG11201704872RA (en) 2017-07-28
IL252901A0 (en) 2017-08-31
KR102561692B1 (ko) 2023-07-28
AU2015364557B2 (en) 2021-04-29
MX2020013015A (es) 2021-02-22
US20180000728A1 (en) 2018-01-04
EP3233057A2 (en) 2017-10-25
JP2018503611A (ja) 2018-02-08
US20240189223A1 (en) 2024-06-13
CA2970938A1 (en) 2016-06-23
JP6606183B2 (ja) 2019-11-13
CL2017001543A1 (es) 2018-03-16
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AU2015364557A1 (en) 2017-08-03
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US11110055B2 (en) 2021-09-07
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AR103176A1 (es) 2017-04-19
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