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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    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non 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
    • 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
    • A61K31/41—Heterocyclic 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
    • A61K31/4245—Oxadiazoles
    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4415—Pyridoxine, i.e. Vitamin B6
    • 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
    • A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
    • 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
    • A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
    • A61K47/38—Cellulose; Derivatives thereof
    • 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
    • A61K9/1605—Excipients; Inactive ingredients
    • A61K9/1617—Organic compounds, e.g. phospholipids, fats
    • A61K9/1623—Sugars or sugar alcohols, e.g. lactose; Derivatives thereof; Homeopathic globules
    • 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
    • A61K9/20—Pills, tablets, discs, rods
    • 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
    • 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
    • A61K9/4841—Filling excipients; Inactive ingredients
    • A61K9/4858—Organic compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • 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
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/10—Antioedematous agents; Diuretics
    • 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
    • A61P9/12—Antihypertensives

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Molecular Biology (AREA)
  • Biophysics (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Psychology (AREA)
  • Inorganic Chemistry (AREA)
  • Hematology (AREA)
  • Cardiology (AREA)
  • Diabetes (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 (https=)
EP (1) EP2413913B1 (https=)
JP (2) JP5864410B2 (https=)
KR (1) KR101824257B1 (https=)
CN (2) CN102438595B (https=)
AU (1) AU2010231962B2 (https=)
BR (1) BRPI1016132B8 (https=)
CA (1) CA2757418C (https=)
DK (1) DK2413913T3 (https=)
ES (1) ES2915698T3 (https=)
MX (1) MX361618B (https=)
PL (1) PL2413913T3 (https=)
PT (1) PT2413913T (https=)
RU (1) RU2550133C2 (https=)
WO (1) WO2010114405A2 (https=)

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PL1907382T3 (pl) 2005-07-26 2016-01-29 Bial Portela & Ca Sa Pochodne nitrokatecholowe jako inhibitory COMT
EP1845097A1 (en) 2006-04-10 2007-10-17 Portela & Ca., S.A. Oxadiazole derivatives as COMT inhibitors
BRPI0721213B1 (pt) 2007-01-31 2021-11-09 Bial - Portela & Ca, S.A. Uso de nitrocatecóis substituídos, e embalagem
WO2009116882A1 (en) 2008-03-17 2009-09-24 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
PT2413912T (pt) 2009-04-01 2019-06-11 Bial Portela & Ca Sa Formulações farmacêuticas compreendendo derivados de nitrocatecol e métodos para as produzir
US20140045900A1 (en) * 2011-02-11 2014-02-13 Bial-Portela & Ca, S.A. Administration regime for nitrocatechols
JP6456143B2 (ja) 2011-12-13 2019-01-23 ノヴィファーマ，エス．アー． カテコール−ｏ−メチル転移酵素阻害剤を調製するための中間体として有用な化学的化合物
NO2699580T3 (https=) 2014-01-24 2018-02-24
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EP4262798A1 (en) 2020-12-17 2023-10-25 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
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JP2026503035A (ja) 2023-01-06 2026-01-27 インスメッド インコーポレイテッド 新規な可逆性ｄｐｐ１阻害剤及びその用途
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MX361618B (es) 2018-12-13
PL2413913T3 (pl) 2022-09-26
CA2757418C (en) 2021-06-15
US20100256194A1 (en) 2010-10-07
BRPI1016132B8 (pt) 2021-05-25
CN105816456A (zh) 2016-08-03
EP2413913A2 (en) 2012-02-08
RU2011143619A (ru) 2013-05-10
KR101824257B1 (ko) 2018-01-31
AU2010231962A1 (en) 2011-11-17
JP5864410B2 (ja) 2016-02-17
US20190008774A1 (en) 2019-01-10
WO2010114405A2 (en) 2010-10-07
CA2757418A1 (en) 2010-10-07
BRPI1016132A2 (pt) 2016-04-19
MX2011010311A (es) 2012-03-07
EP2413913B1 (en) 2022-05-18
KR20120008040A (ko) 2012-01-25
CN102438595A (zh) 2012-05-02
JP6336420B2 (ja) 2018-06-06
DK2413913T3 (da) 2022-06-13
JP2012522764A (ja) 2012-09-27
WO2010114405A3 (en) 2011-01-06
PT2413913T (pt) 2022-06-09
JP2016020369A (ja) 2016-02-04
RU2550133C2 (ru) 2015-05-10
ES2915698T3 (es) 2022-06-24
BRPI1016132B1 (pt) 2020-11-24
AU2010231962B2 (en) 2015-05-21
US20210315824A1 (en) 2021-10-14

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