WO2009038112A1 - Ｎｐｙｙ５受容体拮抗剤を含有する固形製剤 - Google Patents

Ｎｐｙｙ５受容体拮抗剤を含有する固形製剤 Download PDF

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Publication number
WO2009038112A1
WO2009038112A1 PCT/JP2008/066818 JP2008066818W WO2009038112A1 WO 2009038112 A1 WO2009038112 A1 WO 2009038112A1 JP 2008066818 W JP2008066818 W JP 2008066818W WO 2009038112 A1 WO2009038112 A1 WO 2009038112A1
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WO
WIPO (PCT)
Prior art keywords
receptor antagonist
solid preparation
npyy5 receptor
npyy5
amorphia
Prior art date
Application number
PCT/JP2008/066818
Other languages
English (en)
French (fr)
Inventor
Masatoshi Takada
Yuki Murakami
Shunji Ichio
Minako Fujii
Asako Takakura
Takeshi Funaki
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Shionogi & Co., Ltd.
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.)
Filing date
Publication date
Application filed by Shionogi & Co., Ltd. filed Critical Shionogi & Co., Ltd.
Priority to JP2009533170A priority Critical patent/JPWO2009038112A1/ja
Priority to EP08831578A priority patent/EP2191830A4/en
Priority to US12/678,714 priority patent/US20100240711A1/en
Publication of WO2009038112A1 publication Critical patent/WO2009038112A1/ja

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/72—Nitrogen atoms
    • C07D213/76—Nitrogen atoms to which a second hetero atom is attached
    • 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
    • A61K9/1605—Excipients; Inactive ingredients
    • A61K9/1617—Organic compounds, e.g. phospholipids, fats
    • 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
    • A61K9/1605—Excipients; Inactive ingredients
    • A61K9/1617—Organic compounds, e.g. phospholipids, fats
    • A61K9/1623—Sugars or sugar alcohols, e.g. lactose; Derivatives thereof; Homeopathic globules
    • 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
    • A61K9/1605—Excipients; Inactive ingredients
    • A61K9/1629—Organic macromolecular compounds
    • A61K9/1652—Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • 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
    • A61P25/22—Anxiolytics
    • 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
    • A61P25/24—Antidepressants
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity 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
    • 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
    • A61K9/1682—Processes
    • A61K9/1694—Processes resulting in granules or microspheres of the matrix type containing more than 5% of excipient

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  • Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Organic Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Neurology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Neurosurgery (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biomedical Technology (AREA)
  • Epidemiology (AREA)
  • Molecular Biology (AREA)
  • Biophysics (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Child & Adolescent Psychology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychology (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyridine Compounds (AREA)

Abstract

ＮＰＹＹ５受容体拮抗剤が製剤中に高含量含有されていても、ＮＰＹＹ５受容体拮抗剤の水溶解度を改善することができる製剤を提供する。ＮＰＹＹ５受容体拮抗剤、非晶質安定化剤、所望により非晶質化誘導剤を含有する固形製剤、特に非晶質安定化剤としてヒドロキシプロピルメチルセルロースフタレートおよび／またはヒドロキシプロピルメチルセルロースアセテートサクシネート、非晶質化誘導剤として尿素および／またはサッカリンナトリウムの添加量を８重量％未満とすれば、難水溶性のＮＰＹＹ５受容体拮抗剤の溶出性よく改善することができた。
PCT/JP2008/066818 2007-09-21 2008-09-18 Ｎｐｙｙ５受容体拮抗剤を含有する固形製剤 WO2009038112A1 (ja)

Priority Applications (3)

Application Number Priority Date Filing Date Title
JP2009533170A JPWO2009038112A1 (ja) 2007-09-21 2008-09-18 Ｎｐｙｙ５受容体拮抗剤を含有する固形製剤
EP08831578A EP2191830A4 (en) 2007-09-21 2008-09-18 SOLID PREPARATION COMPRISING A NPYY5 RECEPTOR ANTAGONIST
US12/678,714 US20100240711A1 (en) 2007-09-21 2008-09-18 Solid preparation comprising npyy5 receptor antagonist

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
JP2007244949 2007-09-21
JP2007-244949 2007-09-21

Publications (1)

Publication Number Publication Date
WO2009038112A1 true WO2009038112A1 (ja) 2009-03-26

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ID=40467922

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Application Number Title Priority Date Filing Date
PCT/JP2008/066818 WO2009038112A1 (ja) 2007-09-21 2008-09-18 Ｎｐｙｙ５受容体拮抗剤を含有する固形製剤

Country Status (5)

Country Link
US (1) US20100240711A1 (ja)
EP (1) EP2191830A4 (ja)
JP (1) JPWO2009038112A1 (ja)
TW (1) TW200920402A (ja)
WO (1) WO2009038112A1 (ja)

Cited By (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2010107040A1 (ja) * 2009-03-19 2010-09-23 塩野義製薬株式会社 Ｎｐｙｙ５受容体拮抗剤を含有する固形製剤
JP2013533298A (ja) * 2010-08-09 2013-08-22 ラボラトリオス・デル・ドクトル・エステベ・ソシエダッド・アノニマ ４−［−２−［［５−メチル−１−（２−ナフタレニル）−１ｈ−ピラゾール−３−イル］オキシ］エチル］モルホリン塩酸塩の固体形態
US9757358B2 (en) 2010-02-04 2017-09-12 Laboratorios Del Dr. Esteve, S.A. Sigma ligands for potentiating the analgesic effect of opioids and opiates in post-operative pain and attenuating the dependency thereof
US9782483B2 (en) 2010-05-21 2017-10-10 Laboratories Del Dr. Esteve, S.A. Sigma ligands for the prevention and/or treatment of emesis induced by chemotherapy or radiotherapy
US9789117B2 (en) 2011-05-18 2017-10-17 Laboratorios Del Dr. Esteve, S.A. Use of sigma ligands in diabetes type-2 associated pain
US9789115B2 (en) 2010-08-03 2017-10-17 Laboratorios Del Dr. Esteve, S.A. Use of sigma ligands in opioid-induced hyperalgesia
US9844516B2 (en) 2010-02-04 2017-12-19 Laboratorios De Dr. Esteve Sigma ligands for use in the prevention and/or treatment of post-operative pain
US9914705B2 (en) 2008-04-25 2018-03-13 Laboratorios Del Dr. Esteve, S.A. 1-aryl-3-aminoalkoxy pyrazoles as sigma ligands enhancing analgesic effect of opioids and attenuating the dependency thereof
US9931346B2 (en) 2013-12-17 2018-04-03 Laboratorios Del Dr. Esteve S.A. Serotonin-norepinephrine reuptake inhibitors (SNRIs) and Sigma receptor ligands combinations

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8889716B2 (en) 2011-05-10 2014-11-18 Chdi Foundation, Inc. Transglutaminase TG2 inhibitors, pharmaceutical compositions, and methods of use thereof
EP2822539B1 (en) * 2012-03-07 2018-11-21 National Institute Of Pharmaceutical Education And Research (NIPER) Nanocrystalline solid dispersion compositions
CN109864342B (zh) * 2019-04-11 2021-09-28 滁州卷烟材料厂 一种降低卷烟烟气中重金属的复合滤嘴添加材料

Citations (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH0249728A (ja) 1988-05-30 1990-02-20 Zeria Pharmaceut Co Ltd ジヒドロピリジン化合物の製剤組成物
WO1992018106A1 (en) * 1991-04-16 1992-10-29 Nippon Shinyaku Co., Ltd. Method of manufacturing solid dispersion
WO1997006781A1 (fr) 1995-08-11 1997-02-27 Nissan Chemical Industries, Ltd. Procedes permettant de rendre amorphes des medicaments peu solubles
JPH09309834A (ja) 1996-03-18 1997-12-02 Nissan Chem Ind Ltd 塩酸エホニジピン製剤の製造法
EP0901786A2 (en) * 1997-08-11 1999-03-17 Pfizer Products Inc. Solid pharmaceutical dispersions with enhanced bioavailability
JPH11246417A (ja) * 1998-03-04 1999-09-14 Nissan Chem Ind Ltd 糖尿病性腎症治療用医薬組成物
WO2001037826A1 (fr) 1999-11-26 2001-05-31 Shionogi & Co., Ltd. Antagonistes npyy5
JP2002529519A (ja) 1998-11-16 2002-09-10 メドイミューン オンコロジー，インコーポレーテッド 安定な非晶質アミフォスチン組成物およびその製造法および使用法
WO2003076374A1 (fr) 2002-03-12 2003-09-18 Shionogi & Co., Ltd. Procede de production de derive d'acide trans-4-amino-1-cyclohexanecarboxylique
JP2004143185A (ja) 2001-02-27 2004-05-20 Astrazeneca Ab 医薬製剤
JP2004528358A (ja) 2001-05-09 2004-09-16 ノバルティス アクチエンゲゼルシャフト シクロスポリン含有医薬組成物
WO2006064906A1 (ja) * 2004-12-17 2006-06-22 Ono Pharmaceutical Co., Ltd. 非晶質性組成物
WO2007108463A1 (ja) 2006-03-23 2007-09-27 Shionogi & Co., Ltd. 溶解性が改善された固形製剤

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Patent Citations (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH0249728A (ja) 1988-05-30 1990-02-20 Zeria Pharmaceut Co Ltd ジヒドロピリジン化合物の製剤組成物
WO1992018106A1 (en) * 1991-04-16 1992-10-29 Nippon Shinyaku Co., Ltd. Method of manufacturing solid dispersion
WO1997006781A1 (fr) 1995-08-11 1997-02-27 Nissan Chemical Industries, Ltd. Procedes permettant de rendre amorphes des medicaments peu solubles
JPH09309834A (ja) 1996-03-18 1997-12-02 Nissan Chem Ind Ltd 塩酸エホニジピン製剤の製造法
EP0901786A2 (en) * 1997-08-11 1999-03-17 Pfizer Products Inc. Solid pharmaceutical dispersions with enhanced bioavailability
JPH11246417A (ja) * 1998-03-04 1999-09-14 Nissan Chem Ind Ltd 糖尿病性腎症治療用医薬組成物
JP2002529519A (ja) 1998-11-16 2002-09-10 メドイミューン オンコロジー，インコーポレーテッド 安定な非晶質アミフォスチン組成物およびその製造法および使用法
WO2001037826A1 (fr) 1999-11-26 2001-05-31 Shionogi & Co., Ltd. Antagonistes npyy5
JP2004143185A (ja) 2001-02-27 2004-05-20 Astrazeneca Ab 医薬製剤
JP2004528358A (ja) 2001-05-09 2004-09-16 ノバルティス アクチエンゲゼルシャフト シクロスポリン含有医薬組成物
WO2003076374A1 (fr) 2002-03-12 2003-09-18 Shionogi & Co., Ltd. Procede de production de derive d'acide trans-4-amino-1-cyclohexanecarboxylique
WO2006064906A1 (ja) * 2004-12-17 2006-06-22 Ono Pharmaceutical Co., Ltd. 非晶質性組成物
WO2007108463A1 (ja) 2006-03-23 2007-09-27 Shionogi & Co., Ltd. 溶解性が改善された固形製剤

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* Cited by examiner, † Cited by third party
Title
"Design of Prodrugs", 1997, ELSEVIER
"Human Science Study", 2006, article "2005 Report of Important Study of Drug Design etc"
PEPTIDES, vol. 18, 1998, pages 445
See also references of EP2191830A4
TRENDS IN PHARMACOLOGICAL SCIENCES, vol. 15, 1994, pages 153
TRENDS IN PHARMACOLOGICAL SCIENCES, vol. 18, 1997, pages 372

Cited By (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9914705B2 (en) 2008-04-25 2018-03-13 Laboratorios Del Dr. Esteve, S.A. 1-aryl-3-aminoalkoxy pyrazoles as sigma ligands enhancing analgesic effect of opioids and attenuating the dependency thereof
WO2010107040A1 (ja) * 2009-03-19 2010-09-23 塩野義製薬株式会社 Ｎｐｙｙ５受容体拮抗剤を含有する固形製剤
US9757358B2 (en) 2010-02-04 2017-09-12 Laboratorios Del Dr. Esteve, S.A. Sigma ligands for potentiating the analgesic effect of opioids and opiates in post-operative pain and attenuating the dependency thereof
US9844516B2 (en) 2010-02-04 2017-12-19 Laboratorios De Dr. Esteve Sigma ligands for use in the prevention and/or treatment of post-operative pain
US9782483B2 (en) 2010-05-21 2017-10-10 Laboratories Del Dr. Esteve, S.A. Sigma ligands for the prevention and/or treatment of emesis induced by chemotherapy or radiotherapy
US9789115B2 (en) 2010-08-03 2017-10-17 Laboratorios Del Dr. Esteve, S.A. Use of sigma ligands in opioid-induced hyperalgesia
JP2013533298A (ja) * 2010-08-09 2013-08-22 ラボラトリオス・デル・ドクトル・エステベ・ソシエダッド・アノニマ ４−［−２−［［５−メチル−１−（２−ナフタレニル）−１ｈ−ピラゾール−３−イル］オキシ］エチル］モルホリン塩酸塩の固体形態
US9428462B2 (en) 2010-08-09 2016-08-30 Laboratorios Del Dr. Esteve, S.A. 4-[-2-[[5-methyl-1-(2-naphthalenyl)-1H-pyrazol-3-yl]oxy]ethyl]morpholine hydrochloride amorphous solid forms
US9789117B2 (en) 2011-05-18 2017-10-17 Laboratorios Del Dr. Esteve, S.A. Use of sigma ligands in diabetes type-2 associated pain
US9931346B2 (en) 2013-12-17 2018-04-03 Laboratorios Del Dr. Esteve S.A. Serotonin-norepinephrine reuptake inhibitors (SNRIs) and Sigma receptor ligands combinations

Also Published As

Publication number Publication date
TW200920402A (en) 2009-05-16
EP2191830A1 (en) 2010-06-02
US20100240711A1 (en) 2010-09-23
JPWO2009038112A1 (ja) 2011-01-06
EP2191830A4 (en) 2011-11-23

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