JP5026426B2 - ７−クロロ−Ｎ，Ｎ，５−トリメチル−４−オキソ−３−フェニル−３，５−ジヒドロ−４Ｈ−ピリダジノ［４，５−ｂ］インドール−１−アセトアミドのアモルファス固体分散体 - Google Patents

７−クロロ−Ｎ，Ｎ，５−トリメチル−４−オキソ−３−フェニル−３，５−ジヒドロ−４Ｈ−ピリダジノ［４，５−ｂ］インドール−１−アセトアミドのアモルファス固体分散体 Download PDF

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JP5026426B2
JP5026426B2 JP2008529117A JP2008529117A JP5026426B2 JP 5026426 B2 JP5026426 B2 JP 5026426B2 JP 2008529117 A JP2008529117 A JP 2008529117A JP 2008529117 A JP2008529117 A JP 2008529117A JP 5026426 B2 JP5026426 B2 JP 5026426B2
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solid dispersion
treating
pyridazino
acetamide
indole
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Expired - Fee Related
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Japanese (ja)
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JP2009506114A5 (enExample
JP2009506114A (ja
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ヤコブス，アーウイン・シー
ヒギンス，ジヨン・デイー
ギヨー，マイケル
フランソン，ナンシー・エム
ロツコ，ウイリアム・エル
アブ−イザ，ハワラ・アブダラ
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サノフイ−アベンテイス・ユー・エス・エルエルシー
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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
    • 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
    • A61P25/02—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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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • 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)
JP2008529117A 2005-08-29 2006-08-24 ７−クロロ−Ｎ，Ｎ，５−トリメチル−４−オキソ−３−フェニル−３，５−ジヒドロ−４Ｈ−ピリダジノ［４，５−ｂ］インドール−１−アセトアミドのアモルファス固体分散体 Expired - Fee Related JP5026426B2 (ja)

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

Publications (3)

Publication Number Publication Date
JP2009506114A JP2009506114A (ja) 2009-02-12
JP2009506114A5 JP2009506114A5 (enExample) 2009-06-25
JP5026426B2 true JP5026426B2 (ja) 2012-09-12

Family

ID=37499538

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2008529117A Expired - Fee Related JP5026426B2 (ja) 2005-08-29 2006-08-24 ７−クロロ−Ｎ，Ｎ，５−トリメチル−４−オキソ−３−フェニル−３，５−ジヒドロ−４Ｈ−ピリダジノ［４，５−ｂ］インドール−１−アセトアミドのアモルファス固体分散体

Country Status (30)

Country Link
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)

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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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US5091381A (en) * 1991-04-12 1992-02-25 Biomeasure, Inc. 2H-1,3,4-benzotriazepin-2-ones
TW487582B (en) * 1995-08-11 2002-05-21 Nissan Chemical Ind Ltd Method for converting sparingly water-soluble medical substance to amorphous state
FR2766823B1 (fr) 1997-07-30 1999-10-08 Synthelabo Derives de 4-oxo-3,5-dihydro-4h-pyridazino[4,5-b] indole-1-acetamide, leur preparation et leur application en therapeutique
ATE364374T1 (de) * 1997-08-11 2007-07-15 Pfizer Prod Inc Feste pharmazeutische dispersionen mit erhöhter bioverfügbarkeit
AUPP278498A0 (en) * 1998-04-03 1998-04-30 Australian Nuclear Science & Technology Organisation Peripheral benzodiazepine receptor binding agents
FR2788696B1 (fr) * 1999-01-26 2004-03-05 Synthelabo Utilisation de derives de pyridazino [4,5-b] indole-1-acetamide pour la preparation de medicaments destines aux maladies du systeme nerveux central
ATE400251T1 (de) 1999-02-09 2008-07-15 Pfizer Prod Inc Zusammensetzungen basischer arzneistoffe mit verbesserter bioverfügbarkeit
ES2310164T3 (es) * 1999-02-10 2009-01-01 Pfizer Products Inc. Dispositivo de liberacion controlada por la matriz.
ATE400252T1 (de) 1999-02-10 2008-07-15 Pfizer Prod Inc Pharmazeutische feste dispersionen
EP1120109A3 (en) * 2000-01-24 2002-07-10 Pfizer Products Inc. Rapidly disintegrating and fast dissolving solid dosage form
FR2829939B3 (fr) * 2001-09-21 2003-11-28 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
CL2004001884A1 (es) 2003-08-04 2005-06-03 Pfizer Prod Inc Procedimiento de secado por pulverizacion para la formacion de dispersiones solidas amorfas de un farmaco y polimeros.
US20050220881A1 (en) * 2003-10-10 2005-10-06 Bvm Holding Co. Pharmaceutical composition

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CR9750A (es) 2008-06-18
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
CN101272767B (zh) 2012-08-29
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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