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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JP2008529117A
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JP2009506114A (ja
JP2009506114A5 (https=
Inventor
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)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Psychiatry (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Immunology (AREA)
  • Hospice & Palliative Care (AREA)
  • Dermatology (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 (https=) 2009-06-25
JP5026426B2 true JP5026426B2 (ja) 2012-09-12

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ID=37499538

Family Applications (1)

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

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2025008679A (ja) * 2023-07-05 2025-01-20 学校法人 名城大学 非晶質性化有機化合物を含む複合粒子の製造方法

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USRE50453E1 (en) 2006-04-07 2025-06-10 Vertex Pharmaceuticals Incorporated Indole derivatives as CFTR modulators
EP2674428B1 (en) 2006-04-07 2016-04-06 Vertex Pharmaceuticals Incorporated Modulators of ATP-binding cassette transporters
CN101702878B (zh) * 2007-05-11 2012-11-28 弗·哈夫曼-拉罗切有限公司 可溶性差的药物的药物组合物
CA2717326C (en) * 2008-03-11 2018-10-23 Dr. Reddy's Laboratories Ltd. Preparation of lenalidomide
RU2011110241A (ru) * 2008-08-18 2012-09-27 САНОФИ-АВЕНТИС Ю.Эс. ЭлЭлСи (US) СПОСОБ ПОЛУЧЕНИЯ ПОЛИМОРФА 7-ХЛОР-N,N,5-ТРИМЕТИЛ-4-ОКСО-3-ФЕНИЛ-3,5-ДИГИДРО-4Н-ПИРИДАЗИНО[4,5-b]ИНДОЛ-1-АЦЕТАМИДА
SI2826776T1 (sl) * 2010-03-25 2021-02-26 Vertex Pharmaceuticals Incorporated Trdna disperzija amorfne oblike (R)-1(2,2-difluorobenzo(D)(1,3)dioksol-5-il)-N-(1-(2,3-dihidroksipropil) -6-fluoro-2-(1-hidroksi-2-metilpropan-2-il)-1H-indol-5-il)- ciklopropankarboksamida
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
US9801855B2 (en) 2012-03-07 2017-10-31 National Institute Of Pharmaceutical Education And Research (Niper) Nanocrystalline solid dispersion compositions and process of preparation thereof
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
CN106232144B (zh) * 2014-03-18 2019-12-06 武田药品工业株式会社 固体分散体
RU2744460C2 (ru) 2014-04-15 2021-03-09 Вертекс Фармасьютикалз Инкорпорейтед Фармацевтические композиции для лечения заболеваний, опосредованных муковисцидозным трансмембранным регулятором проводимости
EP4049660B1 (en) 2016-02-29 2025-02-19 F. Hoffmann-La Roche AG Dosage form compositions comprising an inhibitor of bruton's tyrosine kinase
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JP2025008679A (ja) * 2023-07-05 2025-01-20 学校法人 名城大学 非晶質性化有機化合物を含む複合粒子の製造方法

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JP2009506114A (ja) 2009-02-12
EP1926476A2 (en) 2008-06-04
ECSP088203A (es) 2008-06-30
WO2007027494A3 (en) 2007-08-02
EA200800713A1 (ru) 2008-10-30
US7713548B2 (en) 2010-05-11
PL1926476T3 (pl) 2013-08-30
TW200727902A (en) 2007-08-01
KR20080061354A (ko) 2008-07-02
SI1926476T1 (sl) 2013-07-31
NO20081364L (no) 2008-04-03
RS52914B (sr) 2014-02-28
UA93517C2 (en) 2011-02-25
BRPI0615609A2 (pt) 2011-05-24
ME01560B (me) 2014-04-20
DK1926476T3 (da) 2013-07-01
EA015715B1 (ru) 2011-10-31
IL189587A (en) 2012-12-31
CR9750A (es) 2008-06-18
AU2006285111B8 (en) 2012-05-17
ES2414434T3 (es) 2013-07-19
WO2007027494A2 (en) 2007-03-08
IL189587A0 (en) 2008-08-07
PT1926476E (pt) 2013-07-10
NZ566313A (en) 2011-04-29
HK1124785A1 (en) 2009-07-24
CN101272767A (zh) 2008-09-24
AU2006285111A1 (en) 2007-03-08
EP1926476B1 (en) 2013-04-10
CA2619438A1 (en) 2007-03-08
HRP20130533T1 (en) 2013-07-31
AR055615A1 (es) 2007-08-29
HN2008000360A (es) 2011-05-31
AU2006285111B2 (en) 2012-04-26
ZA200801893B (en) 2009-08-26
MA29783B1 (fr) 2008-09-01
CN101272767B (zh) 2012-08-29
TWI398250B (zh) 2013-06-11
US20080160080A1 (en) 2008-07-03
TNSN08069A1 (en) 2009-07-14

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