CN102159541B - 抗癌口服制剂 - Google Patents

抗癌口服制剂 Download PDF

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Publication number
CN102159541B
CN102159541B CN200980126979.4A CN200980126979A CN102159541B CN 102159541 B CN102159541 B CN 102159541B CN 200980126979 A CN200980126979 A CN 200980126979A CN 102159541 B CN102159541 B CN 102159541B
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China
Prior art keywords
polyethylene glycol
formulation
weight
weight percent
groups
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Expired - Fee Related
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CN200980126979.4A
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English (en)
Chinese (zh)
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CN102159541A (zh
Inventor
叶燈光
陈炯东
赵宇生
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National Health Research Institutes
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National Health Research Institutes
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Publication of CN102159541A publication Critical patent/CN102159541A/zh
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Expired - Fee Related legal-status Critical Current
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    • 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
    • A61K31/41—Heterocyclic 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
    • A61K31/425—Thiazoles
    • A61K31/427—Thiazoles not condensed and containing further heterocyclic rings
    • 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
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
    • 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
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/22—Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
    • 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
    • A61K47/50—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/56—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule
    • A61K47/59—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes
    • A61K47/60—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
    • 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
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • 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
    • A61K9/0087—Galenical forms not covered by A61K9/02 - A61K9/7023
    • A61K9/0095—Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches
    • 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
    • A61K9/08—Solutions
    • 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
    • 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
    • A61K9/4858—Organic compounds

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Dermatology (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
CN200980126979.4A 2008-07-11 2009-07-10 抗癌口服制剂 Expired - Fee Related CN102159541B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US12/171,515 2008-07-11
US12/171,515 US8026271B2 (en) 2008-07-11 2008-07-11 Formulations of indol-3-yl-2-oxoacetamide compounds
PCT/US2009/050210 WO2010006234A2 (en) 2008-07-11 2009-07-10 Anticancer oral formulation

Publications (2)

Publication Number Publication Date
CN102159541A CN102159541A (zh) 2011-08-17
CN102159541B true CN102159541B (zh) 2014-06-04

Family

ID=41505721

Family Applications (1)

Application Number Title Priority Date Filing Date
CN200980126979.4A Expired - Fee Related CN102159541B (zh) 2008-07-11 2009-07-10 抗癌口服制剂

Country Status (8)

Country Link
US (1) US8026271B2 (https=)
EP (1) EP2310363B1 (https=)
JP (1) JP5596680B2 (https=)
KR (1) KR101627382B1 (https=)
CN (1) CN102159541B (https=)
ES (1) ES2426599T3 (https=)
TW (1) TWI384984B (https=)
WO (1) WO2010006234A2 (https=)

Families Citing this family (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8026271B2 (en) * 2008-07-11 2011-09-27 National Health Research Institutes Formulations of indol-3-yl-2-oxoacetamide compounds
CN104945420A (zh) 2009-06-29 2015-09-30 因塞特公司 作为pi3k抑制剂的嘧啶酮类
WO2011075643A1 (en) 2009-12-18 2011-06-23 Incyte Corporation Substituted heteroaryl fused derivatives as pi3k inhibitors
US8680108B2 (en) * 2009-12-18 2014-03-25 Incyte Corporation Substituted fused aryl and heteroaryl derivatives as PI3K inhibitors
AR081823A1 (es) 2010-04-14 2012-10-24 Incyte Corp DERIVADOS FUSIONADOS COMO INHIBIDORES DE PI3Kd
US9062055B2 (en) 2010-06-21 2015-06-23 Incyte Corporation Fused pyrrole derivatives as PI3K inhibitors
EP2655374B1 (en) 2010-12-20 2019-10-23 Incyte Holdings Corporation N-(1-(substituted-phenyl)ethyl)-9h-purin-6-amines as pi3k inhibitors
US9108984B2 (en) 2011-03-14 2015-08-18 Incyte Corporation Substituted diamino-pyrimidine and diamino-pyridine derivatives as PI3K inhibitors
WO2012135009A1 (en) 2011-03-25 2012-10-04 Incyte Corporation Pyrimidine-4,6-diamine derivatives as pi3k inhibitors
DK2707101T3 (da) * 2011-05-12 2019-05-13 Proteostasis Therapeutics Inc Proteostaseregulatorer
KR102507287B1 (ko) 2011-09-02 2023-03-07 인사이트 홀딩스 코포레이션 Ｐｉ３ｋ 억제제로서 헤테로시클릴아민
AR090548A1 (es) 2012-04-02 2014-11-19 Incyte Corp Azaheterociclobencilaminas biciclicas como inhibidores de pi3k
WO2015073528A1 (en) 2013-11-12 2015-05-21 Proteostasis Therapeutics, Inc. Proteasome activity enhancing compounds
WO2015191677A1 (en) 2014-06-11 2015-12-17 Incyte Corporation Bicyclic heteroarylaminoalkyl phenyl derivatives as pi3k inhibitors
SI3831833T1 (sl) 2015-02-27 2023-03-31 Incyte Holdings Corporation Postopki za pripravo inhibitorja PI3K
US9732097B2 (en) 2015-05-11 2017-08-15 Incyte Corporation Process for the synthesis of a phosphoinositide 3-kinase inhibitor
US9988401B2 (en) 2015-05-11 2018-06-05 Incyte Corporation Crystalline forms of a PI3K inhibitor
CA3101323A1 (en) 2018-06-01 2019-12-05 Incyte Corporation Dosing regimen for the treatment of pi3k related disorders

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2003045357A1 (en) * 2001-11-27 2003-06-05 Transform Pharmaceuticals, Inc. Oral pharmaceutical formulations comprising paclitaxel, derivatives and methods of administration thereof
US6903104B2 (en) * 2001-12-06 2005-06-07 National Health Research Institutes Indol-3-YL-2-oxoacetamide compounds and methods of use thereof

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6979456B1 (en) * 1998-04-01 2005-12-27 Jagotec Ag Anticancer compositions
US6372251B2 (en) * 1999-06-11 2002-04-16 Abbott Laboratories Formulations comprising lipid-regulating agents
MX2007006183A (es) * 2004-11-24 2007-09-11 Merck & Co Inc Formulaciones farmaceuticas liquidas y semisolidas para administracion oral de una amida sustituida.
US20060134204A1 (en) * 2004-12-21 2006-06-22 Wong Patrick S Complexes made using low solubility drugs
TWI376239B (en) * 2006-02-01 2012-11-11 Andrew Xian Chen Vitamin e succinate stabilized pharmaceutical compositions, methods for the preparation and the use thereof
AU2007325628A1 (en) * 2006-11-28 2008-06-05 Marinus Pharmaceuticals Nanoparticulate formulations and methods for the making and use thereof
AU2008206294A1 (en) * 2007-01-16 2008-07-24 Bipar Sciences, Inc. Formulations for cancer treatment
US8026271B2 (en) * 2008-07-11 2011-09-27 National Health Research Institutes Formulations of indol-3-yl-2-oxoacetamide compounds

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2003045357A1 (en) * 2001-11-27 2003-06-05 Transform Pharmaceuticals, Inc. Oral pharmaceutical formulations comprising paclitaxel, derivatives and methods of administration thereof
US6903104B2 (en) * 2001-12-06 2005-06-07 National Health Research Institutes Indol-3-YL-2-oxoacetamide compounds and methods of use thereof

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
Developing early formulations: Practice and perspective;Ping Li et al.;《INTERNATIONAL JOURNAL OF PHARMACEUTICS》;20070526;第341卷;1-19 *
Synthesis and biological Evaluation of N-Heterocyclic Indolyl Glyoxylamides as Orally Active Anticancer Agents;Wen-Tai Li et al.;《J.Med.Chem.》;20030325;第46卷;1706-1715 *

Also Published As

Publication number Publication date
JP2011527704A (ja) 2011-11-04
WO2010006234A3 (en) 2010-04-08
KR101627382B1 (ko) 2016-06-03
EP2310363A2 (en) 2011-04-20
ES2426599T3 (es) 2013-10-24
EP2310363A4 (en) 2012-03-28
JP5596680B2 (ja) 2014-09-24
TWI384984B (zh) 2013-02-11
US20100010059A1 (en) 2010-01-14
US8026271B2 (en) 2011-09-27
CN102159541A (zh) 2011-08-17
TW201002319A (en) 2010-01-16
KR20110038135A (ko) 2011-04-13
EP2310363B1 (en) 2013-06-05
WO2010006234A2 (en) 2010-01-14

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