AU2014342042B2 - Crystalline forms of therapeutic compounds and uses thereof - Google Patents

Crystalline forms of therapeutic compounds and uses thereof Download PDF

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Publication number
AU2014342042B2
AU2014342042B2 AU2014342042A AU2014342042A AU2014342042B2 AU 2014342042 B2 AU2014342042 B2 AU 2014342042B2 AU 2014342042 A AU2014342042 A AU 2014342042A AU 2014342042 A AU2014342042 A AU 2014342042A AU 2014342042 B2 AU2014342042 B2 AU 2014342042B2
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AU
Australia
Prior art keywords
less
equal
crystalline form
compound
particles
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Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Ceased
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AU2014342042A
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English (en)
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AU2014342042A1 (en
Inventor
Elizabeth ENLOW
Minh Ngoc Nguyen
Winston Z. ONG
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Kala Bio Inc
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Kala Bio Inc
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Assigned to KALA BIO, Inc. reassignment KALA BIO, Inc. Request to Amend Deed and Register Assignors: KALA PHARMACEUTICALS, INC.
Ceased legal-status Critical Current
Anticipated expiration legal-status Critical

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic 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
    • C07D491/02—Heterocyclic 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
    • C07D491/10—Spiro-condensed systems
    • C07D491/107—Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • 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
    • 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
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0048—Eye, e.g. artificial tears
    • 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
    • A61K9/10—Dispersions; Emulsions
    • 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
    • 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
    • A61K9/141—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers
    • A61K9/146—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers with organic macromolecular compounds
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • 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
    • A61K9/0034—Urogenital system, e.g. vagina, uterus, cervix, penis, scrotum, urethra, bladder; Personal lubricants
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Ophthalmology & Optometry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Dispersion Chemistry (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Urology & Nephrology (AREA)
  • Reproductive Health (AREA)
  • Gynecology & Obstetrics (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Vascular Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicinal Preparation (AREA)
  • Steroid Compounds (AREA)
AU2014342042A 2013-11-01 2014-10-31 Crystalline forms of therapeutic compounds and uses thereof Ceased AU2014342042B2 (en)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US201361898741P 2013-11-01 2013-11-01
US61/898,741 2013-11-01
US201462039192P 2014-08-19 2014-08-19
US201462039177P 2014-08-19 2014-08-19
US62/039,192 2014-08-19
US62/039,177 2014-08-19
PCT/US2014/063444 WO2015066482A1 (en) 2013-11-01 2014-10-31 Crystalline forms of therapeutic compounds and uses thereof

Publications (2)

Publication Number Publication Date
AU2014342042A1 AU2014342042A1 (en) 2016-05-12
AU2014342042B2 true AU2014342042B2 (en) 2017-08-17

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
AU2014342042A Ceased AU2014342042B2 (en) 2013-11-01 2014-10-31 Crystalline forms of therapeutic compounds and uses thereof

Country Status (10)

Country Link
US (6) US9458169B2 (enExample)
EP (1) EP3062618B1 (enExample)
JP (2) JP6426194B2 (enExample)
KR (1) KR20160099084A (enExample)
CN (2) CN108530458A (enExample)
AU (1) AU2014342042B2 (enExample)
CA (1) CA2928658A1 (enExample)
MX (1) MX355330B (enExample)
NZ (1) NZ719185A (enExample)
WO (1) WO2015066482A1 (enExample)

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US10864219B2 (en) * 2012-05-03 2020-12-15 The Johns Hopkins University Compositions and methods for ophthalmic and/or other applications
US9827191B2 (en) * 2012-05-03 2017-11-28 The Johns Hopkins University Compositions and methods for ophthalmic and/or other applications
US11596599B2 (en) * 2012-05-03 2023-03-07 The Johns Hopkins University Compositions and methods for ophthalmic and/or other applications
CN108530458A (zh) 2013-11-01 2018-09-14 卡拉制药公司 治疗化合物的结晶形式及其用途
EP3509423A4 (en) 2016-09-08 2020-05-13 Kala Pharmaceuticals, Inc. CRYSTALLINE FORMS OF THERAPEUTIC COMPOUNDS AND USES THEREOF
US10253036B2 (en) 2016-09-08 2019-04-09 Kala Pharmaceuticals, Inc. Crystalline forms of therapeutic compounds and uses thereof
EP3509421A4 (en) 2016-09-08 2020-05-20 Kala Pharmaceuticals, Inc. CRYSTALLINE FORMS OF THERAPEUTIC COMPOUNDS AND USES THEREOF
AU2018351520A1 (en) * 2017-10-20 2020-05-07 Kala Pharmaceuticals, Inc. RET9 and VEGFR2 inhibitors
KR20200098639A (ko) * 2017-12-15 2020-08-20 보드 오브 리전츠, 더 유니버시티 오브 텍사스 시스템 엑소좀 관련 유전자 편집을 이용한 암 치료 방법 및 조성물
AU2019242912B2 (en) 2018-03-28 2025-07-17 Board Of Regents, The University Of Texas System Identification of epigenetic alterations in DNA isolated from exosomes
WO2021069711A1 (en) * 2019-10-10 2021-04-15 Myovant Sciences Gmbh Crystalline forms of n-(4-(1-(2,6-difluorobenzyl)-5- ((dimethylamino)methyl)-3-(6-methoxy-3-pyridazinyl)-2,4-dioxo- 1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl)phenyl)-n'- methoxyurea
MX2022006397A (es) * 2019-12-02 2022-06-24 Academia Sinica Inhibidores de pdia4 y su uso para inhibir la patogenesis de celulas ? y para tratar diabetes.
WO2021191652A1 (en) * 2020-03-21 2021-09-30 Jafari Javid Mihan Composition and methods for prevention and treatment of vascular disorders
KR102491010B1 (ko) * 2021-09-07 2023-01-20 경희대학교 산학협력단 현탁액에서의 물리적 분쇄를 이용한 안정상 결정 제조방법
AU2024210295A1 (en) 2023-01-18 2025-07-03 Nanoform Finland Oyj A method for crystallization of active pharmaceutical ingredients
CN119097710B (zh) * 2024-09-11 2025-09-02 山东大学齐鲁医院 Ape1抑制剂在制备治疗过敏性鼻炎药物中的应用

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