CN102438595B - 包括硝基儿茶酚衍生物的药物制剂及其制备方法 - Google Patents

包括硝基儿茶酚衍生物的药物制剂及其制备方法 Download PDF

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CN102438595B
CN102438595B CN201080022455.3A CN201080022455A CN102438595B CN 102438595 B CN102438595 B CN 102438595B CN 201080022455 A CN201080022455 A CN 201080022455A CN 102438595 B CN102438595 B CN 102438595B
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CN102438595A (zh
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T·C·d·瓦斯康塞洛斯
R·J·D·S·利马
P·M·D·C·巴罗卡斯
L·S·D·C·佩雷拉
R·C·D·C·科斯塔
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Bial Portela and Cia SA
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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
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • A61K31/41Heterocyclic 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
    • A61K31/4245Oxadiazoles
    • 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
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4415Pyridoxine, i.e. Vitamin B6
    • 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
    • A61K47/30Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/36Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
    • 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
    • A61K47/30Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/36Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
    • A61K47/38Cellulose; Derivatives thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/14Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605Excipients; Inactive ingredients
    • A61K9/1617Organic compounds, e.g. phospholipids, fats
    • A61K9/1623Sugars or sugar alcohols, e.g. lactose; Derivatives thereof; Homeopathic globules
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/48Preparations in capsules, e.g. of gelatin, of chocolate
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/48Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841Filling excipients; Inactive ingredients
    • A61K9/4858Organic compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • 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
    • A61P7/10Antioedematous agents; Diuretics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Molecular Biology (AREA)
  • Biophysics (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Psychology (AREA)
  • Inorganic Chemistry (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
CN201080022455.3A 2009-04-01 2010-03-31 包括硝基儿茶酚衍生物的药物制剂及其制备方法 Active CN102438595B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US16579409P 2009-04-01 2009-04-01
US61/165,794 2009-04-01
PCT/PT2010/000015 WO2010114405A2 (en) 2009-04-01 2010-03-31 Pharmaceutical formulations comprising nitrocatechol derivatives and methods of making the same

Related Child Applications (1)

Application Number Title Priority Date Filing Date
CN201610184873.1A Division CN105816456A (zh) 2009-04-01 2010-03-31 包括硝基儿茶酚衍生物的药物制剂及其制备方法

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CN102438595A CN102438595A (zh) 2012-05-02
CN102438595B true CN102438595B (zh) 2016-04-27

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CN201080022455.3A Active CN102438595B (zh) 2009-04-01 2010-03-31 包括硝基儿茶酚衍生物的药物制剂及其制备方法
CN201610184873.1A Pending CN105816456A (zh) 2009-04-01 2010-03-31 包括硝基儿茶酚衍生物的药物制剂及其制备方法

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Country Status (15)

Country Link
US (3) US20100256194A1 (enExample)
EP (1) EP2413913B1 (enExample)
JP (2) JP5864410B2 (enExample)
KR (1) KR101824257B1 (enExample)
CN (2) CN102438595B (enExample)
AU (1) AU2010231962B2 (enExample)
BR (1) BRPI1016132B8 (enExample)
CA (1) CA2757418C (enExample)
DK (1) DK2413913T3 (enExample)
ES (1) ES2915698T3 (enExample)
MX (1) MX361618B (enExample)
PL (1) PL2413913T3 (enExample)
PT (1) PT2413913T (enExample)
RU (1) RU2550133C2 (enExample)
WO (1) WO2010114405A2 (enExample)

Families Citing this family (22)

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AU2006272978B2 (en) 2005-07-26 2012-06-07 Bial - Portela & Ca, S.A. Nitrocatechol derivatives as COMT inhibitors
EP1845097A1 (en) 2006-04-10 2007-10-17 Portela & Ca., S.A. Oxadiazole derivatives as COMT inhibitors
CN101631548B (zh) 2007-01-31 2014-08-27 比艾尔-坡特拉有限公司 Comt抑制剂的单次药物剂量单元和药物组合物
AU2009226221A1 (en) 2008-03-17 2009-09-24 Bial - Portela & Ca., S.A. Crystal forms of 5- [3- (2, 5-dichloro-4, 6-dimethyl-1-oxy-pyridine-3-yl) [1,2,3] oxadiazol-5-yl] -3-nit robenzene-1, 2-diol
KR102023255B1 (ko) * 2009-04-01 2019-09-19 바이알 - 포르텔라 앤드 씨에이 에스에이 니트로카테콜 유도체를 포함하는 제약 제제 및 그의 제조 방법
US20140045900A1 (en) * 2011-02-11 2014-02-13 Bial-Portela & Ca, S.A. Administration regime for nitrocatechols
BR112014014341A2 (pt) 2011-12-13 2017-08-22 Bial Portela & Ca Sa Intermediário metilado, seu método de preparação e seus usos, e composição farmacêutica
NO2699580T3 (enExample) 2014-01-24 2018-02-24
WO2016083863A1 (en) 2014-11-28 2016-06-02 Bial - Portela & Ca, S.A. Medicaments for slowing parkinson's disease
KR20200100075A (ko) * 2017-12-18 2020-08-25 유니켐 레버러토리스 리미티드 오피카폰 및 그의 중간체의 제조방법
FI3758708T3 (fi) * 2018-03-01 2025-02-18 Astrazeneca Ab (2s)-{(1s)-1-syano-2-[4-(3-metyyli-2-okso-2,3-dihydro-1,3-bentsoksatsol-5-yyli)fenyyli]etyyli}-1,4-oksatsepaani-2-karboksamidia käsittäviä farmaseuttisia koostumuksia
KR20210032431A (ko) 2018-07-17 2021-03-24 인스메드 인코포레이티드 루푸스 신염을 치료하기 위한 특정 (2s)-n-[(1s)-1-시아노-2-페닐에틸]-1,4-옥사제판-2-카복스아미드
EP3860602A1 (en) 2018-10-05 2021-08-11 Neurocrine Biosciences, Inc. Methods for the administration of comt inhibitors
WO2020072886A1 (en) 2018-10-05 2020-04-09 Neurocrine Biosciences, Inc. Methods for the administration of comt inhibitors
CN120478288A (zh) 2020-03-13 2025-08-15 巴尔-波特拉及康邦亚股份有限公司 微粉化的奥匹卡朋
GB202011709D0 (en) 2020-07-28 2020-09-09 Bial Portela & Ca Sa Solid dispersion of opicapone
GB202016425D0 (en) 2020-10-16 2020-12-02 Bial Portela & Ca Sa Treatment regimens for parkinson's disease
WO2022131944A1 (en) 2020-12-17 2022-06-23 Bial-Portela & Ca., S.A. Treatment regimens for early idiopathic parkinson's disease
US20240300930A1 (en) * 2021-02-26 2024-09-12 Msn Laboratories Private Limited, R&D Center Novel process for the preparation of 2,5-dichloro-3-(5-(3,4-dihydroxy-5-nitrophenyl)-1,2,4-oxadiazol-3-yl)-4,6-dimethylpyridine-1-oxide
GB202212082D0 (en) 2022-08-18 2022-10-05 Bial Portela & Ca Sa Treatment regimens for parkinson's disease
EP4646265A1 (en) 2023-01-06 2025-11-12 Insmed Incorporated Novel, reversible dpp1 inhibitors and uses thereof
WO2024242579A1 (en) 2023-05-25 2024-11-28 Bial-Portela & Ca., S.A. Treatment regimens for early idiopathic parkinson's disease

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Also Published As

Publication number Publication date
CN105816456A (zh) 2016-08-03
BRPI1016132A2 (pt) 2016-04-19
US20210315824A1 (en) 2021-10-14
JP6336420B2 (ja) 2018-06-06
KR101824257B1 (ko) 2018-01-31
RU2550133C2 (ru) 2015-05-10
JP5864410B2 (ja) 2016-02-17
WO2010114405A3 (en) 2011-01-06
KR20120008040A (ko) 2012-01-25
US20190008774A1 (en) 2019-01-10
MX361618B (es) 2018-12-13
ES2915698T3 (es) 2022-06-24
JP2012522764A (ja) 2012-09-27
CN102438595A (zh) 2012-05-02
BRPI1016132B1 (pt) 2020-11-24
US20100256194A1 (en) 2010-10-07
WO2010114405A2 (en) 2010-10-07
CA2757418C (en) 2021-06-15
AU2010231962A1 (en) 2011-11-17
EP2413913A2 (en) 2012-02-08
EP2413913B1 (en) 2022-05-18
PL2413913T3 (pl) 2022-09-26
BRPI1016132B8 (pt) 2021-05-25
MX2011010311A (es) 2012-03-07
JP2016020369A (ja) 2016-02-04
PT2413913T (pt) 2022-06-09
RU2011143619A (ru) 2013-05-10
CA2757418A1 (en) 2010-10-07
AU2010231962B2 (en) 2015-05-21
DK2413913T3 (da) 2022-06-13

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