TWI398250B - 非晶形固態分散體 - Google Patents

非晶形固態分散體 Download PDF

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Publication number
TWI398250B
TWI398250B TW095131682A TW95131682A TWI398250B TW I398250 B TWI398250 B TW I398250B TW 095131682 A TW095131682 A TW 095131682A TW 95131682 A TW95131682 A TW 95131682A TW I398250 B TWI398250 B TW I398250B
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TW
Taiwan
Prior art keywords
solid dispersion
acetamide
dihydro
trimethyl
chloro
Prior art date
Application number
TW095131682A
Other languages
English (en)
Chinese (zh)
Other versions
TW200727902A (en
Inventor
Irwin C Jacobs
John D Higgins
Micael Guillot
Nancy M Franson
William L Rocco
Khawla Abdullah Abu-Izza
Original Assignee
Sanofi Aventis Us Llc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
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Publication date
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=37499538&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=TWI398250(B) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Sanofi Aventis Us Llc filed Critical Sanofi Aventis Us Llc
Publication of TW200727902A publication Critical patent/TW200727902A/zh
Application granted granted Critical
Publication of TWI398250B publication Critical patent/TWI398250B/zh

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Classifications

    • 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
    • A61K9/141Intimate 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
    • A61K9/146Intimate 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
    • 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
    • A61K31/495Heterocyclic 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
    • A61K31/50Pyridazines; Hydrogenated pyridazines
    • A61K31/5025Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring systems
    • 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
    • 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
    • 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
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2022Organic macromolecular compounds
    • A61K9/205Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • 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
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2022Organic macromolecular compounds
    • A61K9/205Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2059Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
    • 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
    • A61K9/4866Organic macromolecular compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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
    • A61P25/02Drugs for disorders of the nervous system for peripheral neuropathies
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system

Landscapes

  • 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)
TW095131682A 2005-08-29 2006-08-29 非晶形固態分散體 TWI398250B (zh)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US71215005P 2005-08-29 2005-08-29

Publications (2)

Publication Number Publication Date
TW200727902A TW200727902A (en) 2007-08-01
TWI398250B true TWI398250B (zh) 2013-06-11

Family

ID=37499538

Family Applications (1)

Application Number Title Priority Date Filing Date
TW095131682A TWI398250B (zh) 2005-08-29 2006-08-29 非晶形固態分散體

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

Citations (1)

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US6395729B1 (en) * 1999-01-26 2002-05-28 Sanofi-Synthelabo Use of pyridazino[4,5-b]indole-1-acetamide derivatives for preparing medicines for treating diseases related to the dysfunction of peripheral benzodiazepin receptors

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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
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

Patent Citations (1)

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Publication number Priority date Publication date Assignee Title
US6395729B1 (en) * 1999-01-26 2002-05-28 Sanofi-Synthelabo Use of pyridazino[4,5-b]indole-1-acetamide derivatives for preparing medicines for treating diseases related to the dysfunction of peripheral benzodiazepin receptors

Also Published As

Publication number Publication date
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
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
AR055615A1 (es) 2007-08-29
NZ566313A (en) 2011-04-29
US20080160080A1 (en) 2008-07-03

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