CN108530458A - 治疗化合物的结晶形式及其用途 - Google Patents

治疗化合物的结晶形式及其用途 Download PDF

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Publication number
CN108530458A
CN108530458A CN201810252366.6A CN201810252366A CN108530458A CN 108530458 A CN108530458 A CN 108530458A CN 201810252366 A CN201810252366 A CN 201810252366A CN 108530458 A CN108530458 A CN 108530458A
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China
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less
equal
crystal form
particle
pharmaceutical composition
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CN201810252366.6A
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English (en)
Chinese (zh)
Inventor
伊丽莎白·恩洛
阮明玉
温斯顿·Z·昂
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Ok A Karaoke Club Drugmaker
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Ok A Karaoke Club Drugmaker
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Publication of CN108530458A publication Critical patent/CN108530458A/zh
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    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Organic Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Ophthalmology & Optometry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Dispersion Chemistry (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Urology & Nephrology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Reproductive Health (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Vascular Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Steroid Compounds (AREA)
  • Medicinal Preparation (AREA)
CN201810252366.6A 2013-11-01 2014-10-31 治疗化合物的结晶形式及其用途 Pending CN108530458A (zh)

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
CN201480065624.XA CN106061261B (zh) 2013-11-01 2014-10-31 治疗化合物的结晶形式及其用途

Related Parent Applications (1)

Application Number Title Priority Date Filing Date
CN201480065624.XA Division CN106061261B (zh) 2013-11-01 2014-10-31 治疗化合物的结晶形式及其用途

Publications (1)

Publication Number Publication Date
CN108530458A true CN108530458A (zh) 2018-09-14

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CN201810252366.6A Pending CN108530458A (zh) 2013-11-01 2014-10-31 治疗化合物的结晶形式及其用途
CN201480065624.XA Expired - Fee Related CN106061261B (zh) 2013-11-01 2014-10-31 治疗化合物的结晶形式及其用途

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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)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN119097710A (zh) * 2024-09-11 2024-12-10 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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US11596599B2 (en) * 2012-05-03 2023-03-07 The Johns Hopkins University Compositions and methods for ophthalmic and/or other applications
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
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
EP3509421A4 (en) 2016-09-08 2020-05-20 Kala Pharmaceuticals, Inc. CRYSTALLINE FORMS OF THERAPEUTIC COMPOUNDS AND USES THEREOF
AU2017324713B2 (en) * 2016-09-08 2020-08-13 KALA BIO, Inc. Crystalline forms of therapeutic compounds and uses thereof
EP3509423A4 (en) * 2016-09-08 2020-05-13 Kala Pharmaceuticals, Inc. CRYSTALLINE FORMS OF THERAPEUTIC COMPOUNDS AND USES THEREOF
EP3697775A1 (en) * 2017-10-20 2020-08-26 Kala Pharmaceuticals, Inc. Ret9 and vegfr2 inhibitors
EP3723733A4 (en) * 2017-12-15 2021-11-24 Board of Regents, The University of Texas System METHODS AND COMPOSITIONS FOR THE TREATMENT OF CANCER USING EXOSOMES ASSOCIATED WITH GENE EDITING
CN112513297B (zh) 2018-03-28 2024-10-22 得克萨斯州大学系统董事会 鉴定从外排体分离的dna中的表观遗传改变
CN115279769A (zh) * 2019-10-10 2022-11-01 梦欧文科学有限责任公司 N-(4-(1-(2,6-二氟苄基)-5-((二甲基氨基)甲基)-3-(6-甲氧基-3-哒嗪基)-2,4-二氧代-1,2,3,4-四氢噻吩并[2,3-d]嘧啶-6-基)苯基)-n’-甲氧基脲的结晶形式
CN114761025B (zh) * 2019-12-02 2024-03-12 施明哲 PDIA4抑制剂及其用于抑制β细胞病变及治疗糖尿病的用途
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
EP4489884B1 (en) 2023-01-18 2025-09-24 Nanoform Finland Oyj A method for crystallization of active pharmaceutical ingredients

Citations (4)

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CN1346271A (zh) * 1999-02-10 2002-04-24 阿斯特拉曾尼卡有限公司 用作血管生成抑制剂的喹唑啉衍生物
CN1625555A (zh) * 2002-02-01 2005-06-08 阿斯特拉曾尼卡有限公司 喹唑啉化合物
CN102153543A (zh) * 2003-12-24 2011-08-17 阿斯利康(瑞典)有限公司 用作抗血管发生剂的喹唑啉衍生物的马来酸盐
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