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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CN
China
Prior art keywords
polyethylene glycol
formulation
weight
weight percent
groups
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Expired - Fee Related
Application number
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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Classifications

    • 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)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Dermatology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (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 (enExample)
EP (1) EP2310363B1 (enExample)
JP (1) JP5596680B2 (enExample)
KR (1) KR101627382B1 (enExample)
CN (1) CN102159541B (enExample)
ES (1) ES2426599T3 (enExample)
TW (1) TWI384984B (enExample)
WO (1) WO2010006234A2 (enExample)

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
EP2448938B9 (en) 2009-06-29 2015-06-10 Incyte Corporation Pyrimidinones as pi3k inhibitors
WO2011075630A1 (en) * 2009-12-18 2011-06-23 Incyte Corporation Substituted fused aryl and heteroaryl derivatives as pi3k inhibitors
WO2011075643A1 (en) * 2009-12-18 2011-06-23 Incyte Corporation Substituted heteroaryl fused derivatives as pi3k inhibitors
EP2558463A1 (en) 2010-04-14 2013-02-20 Incyte Corporation Fused derivatives as i3 inhibitors
US9062055B2 (en) 2010-06-21 2015-06-23 Incyte Corporation Fused pyrrole derivatives as PI3K inhibitors
JP5961187B2 (ja) 2010-12-20 2016-08-02 インサイト・ホールディングス・コーポレイションＩｎｃｙｔｅ Ｈｏｌｄｉｎｇｓ Ｃｏｒｐｏｒａｔｉｏｎ Ｐｉ３ｋ阻害剤としてのｎ−（１−（置換フェニル）エチル）−９ｈ−プリン−６−アミン
US9108984B2 (en) 2011-03-14 2015-08-18 Incyte Corporation Substituted diamino-pyrimidine and diamino-pyridine derivatives as PI3K inhibitors
US9126948B2 (en) 2011-03-25 2015-09-08 Incyte Holdings Corporation Pyrimidine-4,6-diamine derivatives as PI3K inhibitors
TR201906779T4 (tr) * 2011-05-12 2019-05-21 Proteostasis Therapeutics Inc Proteostaz regülatörleri.
MX389479B (es) 2011-09-02 2025-03-20 Incyte Holdings Corp Heterociclilaminas como inhibidores de fosfoinositida 3-cinasas (pi3k)
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
US10077277B2 (en) 2014-06-11 2018-09-18 Incyte Corporation Bicyclic heteroarylaminoalkyl phenyl derivatives as PI3K inhibitors
SG10201912302VA (en) 2015-02-27 2020-02-27 Incyte Corp Salts of pi3k inhibitor and processes for their preparation
WO2016183060A1 (en) 2015-05-11 2016-11-17 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
IL278889B2 (en) 2018-06-01 2025-11-01 Incyte Corp 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
AU2005309808A1 (en) * 2004-11-24 2006-06-01 Merck & Co., Inc. Liquid and semi-solid pharmaceutical formulations for oral administration of a substituted amide
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
WO2008066899A2 (en) * 2006-11-28 2008-06-05 Marinus Pharmaceuticals Nanoparticulate formulations and methods for the making and use thereof
CA2674600A1 (en) * 2007-01-16 2008-07-24 Valeria Ossovskaya 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
US8026271B2 (en) 2011-09-27
US20100010059A1 (en) 2010-01-14
TW201002319A (en) 2010-01-16
ES2426599T3 (es) 2013-10-24
TWI384984B (zh) 2013-02-11
KR20110038135A (ko) 2011-04-13
EP2310363A4 (en) 2012-03-28
WO2010006234A2 (en) 2010-01-14
KR101627382B1 (ko) 2016-06-03
EP2310363B1 (en) 2013-06-05
EP2310363A2 (en) 2011-04-20
JP5596680B2 (ja) 2014-09-24
WO2010006234A3 (en) 2010-04-08
JP2011527704A (ja) 2011-11-04
CN102159541A (zh) 2011-08-17

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