CN101272767B - 7-氯-N,N,5-三甲基-4-氧-3-苯基-3,5-二氢-4H-哒嗪并[4,5-b]吲哚-1-乙酰胺的无定形固体分散体 - Google Patents

7-氯-N,N,5-三甲基-4-氧-3-苯基-3,5-二氢-4H-哒嗪并[4,5-b]吲哚-1-乙酰胺的无定形固体分散体 Download PDF

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CN101272767B
CN101272767B CN2006800317142A CN200680031714A CN101272767B CN 101272767 B CN101272767 B CN 101272767B CN 2006800317142 A CN2006800317142 A CN 2006800317142A CN 200680031714 A CN200680031714 A CN 200680031714A CN 101272767 B CN101272767 B CN 101272767B
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solid dispersion
polymer
dispersion according
medicine
treating
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CN101272767A (zh
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I·C·雅各布斯
J·D·希金斯
M·奎洛特
N·M·弗兰森
W·L·罗科
K·A·阿布-伊扎
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    • 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
    • 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
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/5025—Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring systems
    • 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
    • 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
    • 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
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • 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
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2059—Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
    • 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
    • A61K9/4866—Organic macromolecular compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
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    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • 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
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • 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
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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

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  • Veterinary Medicine (AREA)
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  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
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  • Chemical Kinetics & Catalysis (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Psychiatry (AREA)
  • Immunology (AREA)
  • Pain & Pain Management (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Dermatology (AREA)
  • Hospice & Palliative Care (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Cardiology (AREA)
  • Inorganic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Agricultural Chemicals And Associated Chemicals (AREA)
CN2006800317142A 2005-08-29 2006-08-24 7-氯-N,N,5-三甲基-4-氧-3-苯基-3,5-二氢-4H-哒嗪并[4,5-b]吲哚-1-乙酰胺的无定形固体分散体 Expired - Fee Related CN101272767B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US71215005P 2005-08-29 2005-08-29
US60/712,150 2005-08-29
PCT/US2006/033022 WO2007027494A2 (en) 2005-08-29 2006-08-24 Morphous solid dispersions of 7-chloro-n,n, 5-trimethyl-4-oxo-3-phenyl-3, 5,-dihydro-4h-pyridazino [4, 5-b] indole-1-acetamide

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Publication Number Publication Date
CN101272767A CN101272767A (zh) 2008-09-24
CN101272767B true CN101272767B (zh) 2012-08-29

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CN2006800317142A Expired - Fee Related CN101272767B (zh) 2005-08-29 2006-08-24 7-氯-N,N,5-三甲基-4-氧-3-苯基-3,5-二氢-4H-哒嗪并[4,5-b]吲哚-1-乙酰胺的无定形固体分散体

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US (1) US7713548B2 (enExample)
EP (1) EP1926476B1 (enExample)
JP (1) JP5026426B2 (enExample)
KR (1) KR20080061354A (enExample)
CN (1) CN101272767B (enExample)
AR (1) AR055615A1 (enExample)
AU (1) AU2006285111B8 (enExample)
BR (1) BRPI0615609A2 (enExample)
CA (1) CA2619438A1 (enExample)
CR (1) CR9750A (enExample)
DK (1) DK1926476T3 (enExample)
EA (1) EA015715B1 (enExample)
EC (1) ECSP088203A (enExample)
ES (1) ES2414434T3 (enExample)
HN (1) HN2008000360A (enExample)
HR (1) HRP20130533T1 (enExample)
IL (1) IL189587A (enExample)
MA (1) MA29783B1 (enExample)
ME (1) ME01560B (enExample)
NO (1) NO20081364L (enExample)
NZ (1) NZ566313A (enExample)
PL (1) PL1926476T3 (enExample)
PT (1) PT1926476E (enExample)
RS (1) RS52914B (enExample)
SI (1) SI1926476T1 (enExample)
TN (1) TNSN08069A1 (enExample)
TW (1) TWI398250B (enExample)
UA (1) UA93517C2 (enExample)
WO (1) WO2007027494A2 (enExample)
ZA (1) ZA200801893B (enExample)

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PT2674428T (pt) 2006-04-07 2016-07-14 Vertex Pharma Modeladores de transportadores de cassetes de ligação de atp
USRE50453E1 (en) 2006-04-07 2025-06-10 Vertex Pharmaceuticals Incorporated Indole derivatives as CFTR modulators
CA2686756A1 (en) * 2007-05-11 2008-11-20 F. Hoffmann-La Roche Ag Pharmaceutical compositions for poorly soluble drugs
WO2009114601A2 (en) * 2008-03-11 2009-09-17 Dr. Reddy's Laboratories Ltd. Preparation of lenalidomide
KR20110052640A (ko) * 2008-08-18 2011-05-18 사노피-아벤티스 유.에스. 엘엘씨 7-클로로-Ｎ,Ｎ,5-트리메틸-4-옥소-3-페닐-3,5-디하이드로-4Ｈ-피리다지노[4,5-ｂ]인돌-1-아세트아미드의 다형체의 제조방법
RU2711481C2 (ru) * 2010-03-25 2020-01-17 Вертекс Фармасьютикалз Инкорпорейтед ТВЕРДЫЕ ФОРМЫ (R)-1-(2, 2-ДИФТОРБЕНЗО[d][1, 3]ДИОКСОЛ-5-ИЛ)-N-(1-(2, 3-ДИГИДРОКСИПРОПИЛ)-6-ФТОР-2-(1-ГИДРОКСИ-2-МЕТИЛПРОПАН-2-ИЛ)-1H-ИНДОЛ-5-ИЛ)ЦИКЛОПРОПАНКАРБОКСАМИДА
US8802868B2 (en) 2010-03-25 2014-08-12 Vertex Pharmaceuticals Incorporated Solid forms of (R)-1(2,2-difluorobenzo[D][1,3]dioxo1-5-yl)-N-(1-(2,3-dihydroxypropyl-6-fluoro-2-(1-hydroxy-2-methylpropan2-yl)-1H-Indol-5-yl)-Cyclopropanecarboxamide
IN2012DE00674A (enExample) 2012-03-07 2015-08-21 Nat Inst Of Pharmaceutical Education And Res Niper
KR101986683B1 (ko) * 2012-12-13 2019-06-10 한미약품 주식회사 테트라졸 유도체를 활성 성분으로 포함하는 용해도가 개선된 고체 분산체
CN105493092A (zh) * 2013-08-30 2016-04-13 慧与发展有限责任合伙企业 实时移动与模式分布的比较
US10231929B2 (en) 2014-03-18 2019-03-19 Takeda Pharmaceutical Company Limited Solid dispersion
CA2944140C (en) 2014-04-15 2022-10-04 Vertex Pharmaceuticals Incorporated Pharmaceutical compositions for the treatment of cystic fibrosis transmembrane conductance regulator mediated diseases
ES2913494T3 (es) 2016-02-29 2022-06-02 Hoffmann La Roche Composiciones de forma farmacéutica que comprenden un inhibidor de tirosina cinasa de Bruton
WO2019007317A1 (zh) * 2017-07-04 2019-01-10 江苏恒瑞医药股份有限公司 一种药物组合物及其制备方法

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CN1207896A (zh) * 1997-08-11 1999-02-17 辉瑞产品公司 提高生物利用度的固体药物分散体
CN1344161A (zh) * 1999-01-26 2002-04-10 圣诺菲-合成实验室公司 哒嗪并[4,5－b]吲哚－1－乙酰胺衍生物在制备用于治疗与周围神经受体苯并二氮杂䓬的失调有关的疾病的药物中的用途
FR2829939A1 (fr) * 2001-09-21 2003-03-28 Sanofi Synthelabo Utilisation du 7-chloro-n,n,5-trimethyl-4-oxo-3-phenyl-3,5- dihydro-4h-pyridazino(4,5-b)indole-1-acetamide pour la preparation de medicaments destines au traitement de la polyarthrite rhumatoide
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CN1207896A (zh) * 1997-08-11 1999-02-17 辉瑞产品公司 提高生物利用度的固体药物分散体
CN1344161A (zh) * 1999-01-26 2002-04-10 圣诺菲-合成实验室公司 哒嗪并[4,5－b]吲哚－1－乙酰胺衍生物在制备用于治疗与周围神经受体苯并二氮杂䓬的失调有关的疾病的药物中的用途
FR2829939A1 (fr) * 2001-09-21 2003-03-28 Sanofi Synthelabo Utilisation du 7-chloro-n,n,5-trimethyl-4-oxo-3-phenyl-3,5- dihydro-4h-pyridazino(4,5-b)indole-1-acetamide pour la preparation de medicaments destines au traitement de la polyarthrite rhumatoide
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BADIA FERZAZ et. al.."SSR180575 (7-Chloro-N,N,5-trimethyl-4-oxo-3-phenyl-3,5-dihydro-4H-pyridazino[4,5-b]indole-1-acetamide), a PeripheralBenzodiazepine Receptor Ligand, Promotes NeuronalSurvival and Repair".J. Pharmacol. Exp. Ther.vol 311 no 3.2002,vol 311(no 3),1067,1074.
BADIA FERZAZ et. al.."SSR180575 (7-Chloro-N,N,5-trimethyl-4-oxo-3-phenyl-3,5-dihydro-4H-pyridazino[4,5-b]indole-1-acetamide), a PeripheralBenzodiazepine Receptor Ligand, Promotes NeuronalSurvival and Repair".J. Pharmacol. Exp. Ther.vol 311 no 3.2002,vol 311(no 3),1067,1074. *

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CR9750A (es) 2008-06-18
JP5026426B2 (ja) 2012-09-12
UA93517C2 (en) 2011-02-25
AU2006285111A1 (en) 2007-03-08
HRP20130533T1 (en) 2013-07-31
WO2007027494A2 (en) 2007-03-08
IL189587A0 (en) 2008-08-07
ZA200801893B (en) 2009-08-26
US7713548B2 (en) 2010-05-11
EP1926476B1 (en) 2013-04-10
CN101272767A (zh) 2008-09-24
ES2414434T3 (es) 2013-07-19
TNSN08069A1 (en) 2009-07-14
TW200727902A (en) 2007-08-01
AU2006285111B8 (en) 2012-05-17
WO2007027494A3 (en) 2007-08-02
HN2008000360A (es) 2011-05-31
EA200800713A1 (ru) 2008-10-30
SI1926476T1 (sl) 2013-07-31
ECSP088203A (es) 2008-06-30
EP1926476A2 (en) 2008-06-04
BRPI0615609A2 (pt) 2011-05-24
CA2619438A1 (en) 2007-03-08
PT1926476E (pt) 2013-07-10
ME01560B (me) 2014-04-20
RS52914B (sr) 2014-02-28
AU2006285111B2 (en) 2012-04-26
HK1124785A1 (en) 2009-07-24
NO20081364L (no) 2008-04-03
JP2009506114A (ja) 2009-02-12
PL1926476T3 (pl) 2013-08-30
KR20080061354A (ko) 2008-07-02
DK1926476T3 (da) 2013-07-01
MA29783B1 (fr) 2008-09-01
IL189587A (en) 2012-12-31
EA015715B1 (ru) 2011-10-31
TWI398250B (zh) 2013-06-11
AR055615A1 (es) 2007-08-29
NZ566313A (en) 2011-04-29
US20080160080A1 (en) 2008-07-03

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