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)

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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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US8168793B2 (en) 2005-07-26 2012-05-01 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
PL2481410T3 (pl) 2007-01-31 2017-03-31 Bial - Portela & Ca., S.A. Pochodne nitrokatecholu jako inhibitory COMT podawane w określonym schemacie dawkowania
CL2009000628A1 (es) 2008-03-17 2010-04-09 Bial Portela & Companhia S A Forma cristalina de 5-[3-(2,5-dicloro-4,6-dimetil-1-oxi-piridin-3-il)-[1,2,4]oxadiazol-5-il]-3-nitrobenceno-1,2-diol, composicion farmaceutica que la comprende, proceso para obtenerla y su uso para tratar trastornos del animo, enfermedad de parkinson y trastornos parkinsonianos, alteraciones gastrointestinales, entre otros.
US9132094B2 (en) 2009-04-01 2015-09-15 Bial—Portela & Ca, S.A. Pharmaceutical formulations comprising nitrocatechol derivatives and methods of making thereof
US20140045900A1 (en) * 2011-02-11 2014-02-13 Bial-Portela & Ca, S.A. Administration regime for nitrocatechols
PT2791134T (pt) 2011-12-13 2019-12-18 BIAL PORTELA & Cª S A Composto químico útil como intermediário para a preparação de um inibidor de catecol-o-metiltransferase
NO2699580T3 (enExample) 2014-01-24 2018-02-24
RU2017120184A (ru) 2014-11-28 2018-12-28 БИАЛ - ПОРТЕЛА ЭНД Ка, С.А. Лекарства для замедления течения болезни паркинсона
JP2021506762A (ja) * 2017-12-18 2021-02-22 ユニケム ラボラトリーズ リミテッド オピカポンとその中間体の製造方法
HRP20250115T1 (hr) 2018-03-01 2025-05-23 Astrazeneca Ab Farmaceutski pripravci koji sadrže (2s)-{(1s)-1-cijano-2-[4-(3-metil-2-okso-2,3-dihidro-1,3-benzoksazol-5-il)fenil]etil} -1,4-oksazepan-2-karboksamid
CA3106269A1 (en) 2018-07-17 2020-01-23 Insmed Incorporated Certain (2s)-n-[(1s)-1-cyano-2-phenylethyl]-1,4-oxazepane-2-carboxamides for treating lupus nephritis
EP3860602A1 (en) 2018-10-05 2021-08-11 Neurocrine Biosciences, Inc. Methods for the administration of comt inhibitors
US12097193B2 (en) 2018-10-05 2024-09-24 Bial—Portela & Ca, S.A. Methods for the administration of COMT inhibitors
EP4117637A1 (en) 2020-03-13 2023-01-18 Bial-Portela & CA, S.A. Micronised opicapone
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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
AU2023449890A1 (en) 2023-05-25 2025-11-27 Bial-Portela & Ca., S.A. Treatment regimens for early idiopathic parkinson's disease

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WO2008094053A1 (en) * 2007-01-31 2008-08-07 Bial-Portela & Ca, S.A. Dosage regimen for comt inhibitors

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

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