JP2010511717A - プロドラッグおよびその作成ならびに使用方法 - Google Patents

プロドラッグおよびその作成ならびに使用方法 Download PDF

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JP2010511717A
JP2010511717A JP2009540292A JP2009540292A JP2010511717A JP 2010511717 A JP2010511717 A JP 2010511717A JP 2009540292 A JP2009540292 A JP 2009540292A JP 2009540292 A JP2009540292 A JP 2009540292A JP 2010511717 A JP2010511717 A JP 2010511717A
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hydrogen
prodrug
compound
prodrug moiety
moiety
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Japanese (ja)
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JP2010511717A5 (enExample
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ナウィード ムハマド，
キース アール． ブレイ，
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ニューロジェシックス， インコーポレイテッド
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Publication of JP2010511717A5 publication Critical patent/JP2010511717A5/ja
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D489/00—Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula:
    • C07D489/09—Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula: containing 4aH-8, 9 c-Iminoethano- phenanthro [4, 5-b, c, d] furan ring systems condensed with carbocyclic rings or ring systems
    • C07D489/10—Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula: containing 4aH-8, 9 c-Iminoethano- phenanthro [4, 5-b, c, d] furan ring systems condensed with carbocyclic rings or ring systems with a bridge between positions 6 and 14
    • C07D489/12—Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula: containing 4aH-8, 9 c-Iminoethano- phenanthro [4, 5-b, c, d] furan ring systems condensed with carbocyclic rings or ring systems with a bridge between positions 6 and 14 the bridge containing only two carbon atoms
    • 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
    • A61K47/54—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 compound
    • A61K47/548—Phosphates or phosphonates, e.g. bone-seeking
    • 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
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/34—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
    • A61K31/343—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide condensed with a carbocyclic ring, e.g. coumaran, bufuralol, befunolol, clobenfurol, amiodarone
    • 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
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • 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
    • 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
    • A61P25/20—Hypnotics; Sedatives
    • 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
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/08—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
    • C07D211/18—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D211/26—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by nitrogen atoms
    • C07D211/28—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by nitrogen atoms to which a second hetero atom is attached
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D225/00—Heterocyclic compounds containing rings of more than seven members having one nitrogen atom as the only ring hetero atom
    • C07D225/04—Heterocyclic compounds containing rings of more than seven members having one nitrogen atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
    • C07D225/06—Heterocyclic compounds containing rings of more than seven members having one nitrogen atom as the only ring hetero atom condensed with carbocyclic rings or ring systems condensed with one six-membered ring

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Pain & Pain Management (AREA)
  • Epidemiology (AREA)
  • Biophysics (AREA)
  • Rheumatology (AREA)
  • Molecular Biology (AREA)
  • Psychology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Immunology (AREA)
  • Anesthesiology (AREA)
  • Psychiatry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicinal Preparation (AREA)
JP2009540292A 2006-12-05 2007-12-05 プロドラッグおよびその作成ならびに使用方法 Pending JP2010511717A (ja)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US87351906P 2006-12-05 2006-12-05
PCT/US2007/024984 WO2008070149A2 (en) 2006-12-05 2007-12-05 Prodrugs and methods of making and using the same

Publications (2)

Publication Number Publication Date
JP2010511717A true JP2010511717A (ja) 2010-04-15
JP2010511717A5 JP2010511717A5 (enExample) 2011-01-27

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JP2009540292A Pending JP2010511717A (ja) 2006-12-05 2007-12-05 プロドラッグおよびその作成ならびに使用方法

Country Status (12)

Country Link
US (1) US20080318905A1 (enExample)
EP (1) EP2121029A2 (enExample)
JP (1) JP2010511717A (enExample)
KR (1) KR20090086627A (enExample)
CN (1) CN101678120A (enExample)
AU (1) AU2007328007A1 (enExample)
BR (1) BRPI0719937A2 (enExample)
CA (1) CA2671737A1 (enExample)
MX (1) MX2009006007A (enExample)
NO (1) NO20092527L (enExample)
RU (1) RU2009125597A (enExample)
WO (1) WO2008070149A2 (enExample)

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2021065898A1 (ja) * 2019-09-30 2021-04-08 日本ケミファ株式会社 アゼパン誘導体
JP2022512687A (ja) * 2018-10-13 2022-02-07 バイオヘイブン・ファーマシューティカル・ホールディング・カンパニー・リミテッド Ｃｇｒｐアンタゴニストのプロドラッグ
JP2022532568A (ja) * 2019-05-07 2022-07-15 ブリストル－マイヤーズ スクイブ カンパニー プロドラッグ化合物

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TWI385169B (zh) 2005-10-31 2013-02-11 Eisai R&D Man Co Ltd 經雜環取代之吡啶衍生物及含有彼之抗真菌劑
CN101622263B (zh) * 2007-03-06 2013-05-29 卫材R&D管理有限公司 稳定性被改善的含有磷酸氯甲酯衍生物的组合物及其制备方法
TW200841879A (en) 2007-04-27 2008-11-01 Eisai R&D Man Co Ltd Pyridine derivatives substituted by heterocyclic ring and phosphonoamino group, and anti-fungal agent containing same
US8513287B2 (en) 2007-12-27 2013-08-20 Eisai R&D Management Co., Ltd. Heterocyclic ring and phosphonoxymethyl group substituted pyridine derivatives and antifungal agent containing same
KR101677126B1 (ko) 2008-05-20 2016-11-22 노이로제스엑스, 인코포레이티드 탄산염 프로드러그 및 그것의 사용 방법
BRPI0912820A2 (pt) 2008-05-20 2015-10-13 Neurogesx Inc pró-fármacos de relação hepatoprotetora de acetaminofeno
JP5757864B2 (ja) 2008-05-20 2015-08-05 ニューロジェシックス， インコーポレイテッド 水溶性アセトアミノフェン類似体
ES2527137T3 (es) 2008-07-28 2015-01-21 Pfizer Inc. Compuestos de fenantrenona, composiciones y procedimientos
WO2010033540A1 (en) * 2008-09-19 2010-03-25 Mallinckrodt Inc. Crystalline forms of fentanyl alkaloid
ES3031438T3 (en) 2009-06-25 2025-07-08 Alkermes Pharma Ireland Ltd Heterocyclic compounds for the treatment of neurological and psychological disorders
CA2937222C (en) 2009-06-25 2019-06-04 Alkermes Pharma Ireland Limited Prodrugs of nh-acidic compounds
WO2011163594A2 (en) 2010-06-24 2011-12-29 Alkermes, Inc. Prodrugs of nh-acidic compounds: ester, carbonate, carbamate and phosphonate derivatives
US9034867B2 (en) 2011-03-18 2015-05-19 Alkermes Pharma Ireland Limited Pharmaceutical compositions comprising sorbitan esters
CA3123900A1 (en) * 2011-07-28 2013-01-31 Kempharm Inc. Methylphenidate-prodrugs, processes of making and using the same
AU2012312136B2 (en) 2011-09-22 2017-06-29 Acorda Therapeutics, Inc. Acetaminophen conjugates, compositions and methods of use thereof
WO2013088255A1 (en) 2011-12-15 2013-06-20 Alkermes Pharma Ireland Limited Prodrugs of secondary amine compounds
WO2013142205A1 (en) 2012-03-19 2013-09-26 Alkermes Pharma Ireland Limited Pharmaceutical compositions comprising benzyl alcohol
JP6219918B2 (ja) 2012-03-19 2017-10-25 アルカームス ファーマ アイルランド リミテッド グリセロールエステルを含む医薬組成物
WO2013142198A1 (en) 2012-03-19 2013-09-26 Alkermes Pharma Ireland Limited Pharmaaceutical compositions comprising fatty acid esters
EP3718536A1 (en) 2012-09-19 2020-10-07 Alkermes Pharma Ireland Limited Pharmaceutical compositions having improved storage stability
EP2986294A4 (en) 2013-04-17 2016-11-16 Biopharma Works PROCESS FOR PAIN TREATMENT
EP2986295A4 (en) 2013-04-17 2016-11-09 Biopharma Works PROCESS FOR PAIN TREATMENT
CA2913558C (en) 2013-05-24 2021-06-29 Rhodes Technologies Opioid ketal compounds and uses thereof
ES2784690T3 (es) 2013-12-05 2020-09-29 Univ Bath Nuevos compuestos opioides y sus usos
EP3119399A4 (en) 2014-03-20 2017-09-27 Alkermes Pharma Ireland Limited Aripiprazole formulations having increased injection speeds
CA2985546A1 (en) * 2015-05-13 2016-11-17 4P-Pharma Stimulant abuse-deterrent compositions
WO2017164084A1 (ja) * 2016-03-24 2017-09-28 株式会社メドレックス 誤用防止特性を有する貼付製剤
EP3703694A4 (en) * 2017-11-03 2021-08-18 Nirsum Laboratories, Inc. MEDICINES ANTAGONISTS OF OPIOID RECEPTORS
AU2019224127B2 (en) 2018-02-23 2021-12-09 Rhodes Technologies Novel opioid compounds and uses thereof
CA3092335A1 (en) 2018-03-05 2019-09-12 Alkermes Pharma Ireland Limited Aripiprazole dosing strategy
WO2020012245A1 (en) 2018-07-13 2020-01-16 Alkermes Pharma Ireland Limited Thienothiophene-naltrexone prodrugs for long-acting injectable compositions
US10799496B2 (en) 2018-07-13 2020-10-13 Alkermes Pharma Ireland Limited Naphthylenyl compounds for long-acting injectable compositions and related methods
US10975099B2 (en) 2018-11-05 2021-04-13 Alkermes Pharma Ireland Limited Thiophene compounds for long-acting injectable compositions and related methods
FI130262B (en) * 2019-08-30 2023-05-17 Medicortex Finland Oy Formulations and compositions for use in the prevention or treatment of brain injury and neurodegenerative diseases
CN114380859B (zh) * 2020-10-22 2024-11-01 威智医药股份有限公司 磷酸二苄酯及焦磷酸四苄酯的制备方法
CN117805249A (zh) * 2022-09-23 2024-04-02 合肥瀚微生物科技有限公司 一种抑郁症诊断的生物标记物及其应用

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Cited By (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2022512687A (ja) * 2018-10-13 2022-02-07 バイオヘイブン・ファーマシューティカル・ホールディング・カンパニー・リミテッド Ｃｇｒｐアンタゴニストのプロドラッグ
JP7295944B2 (ja) 2018-10-13 2023-06-21 ファイザー アイルランド ファーマシューティカルズ Ｃｇｒｐアンタゴニストのプロドラッグ
JP2022532568A (ja) * 2019-05-07 2022-07-15 ブリストル－マイヤーズ スクイブ カンパニー プロドラッグ化合物
JP7767151B2 (ja) 2019-05-07 2025-11-11 ブリストル－マイヤーズ スクイブ カンパニー プロドラッグ化合物
WO2021065898A1 (ja) * 2019-09-30 2021-04-08 日本ケミファ株式会社 アゼパン誘導体
JPWO2021065898A1 (enExample) * 2019-09-30 2021-04-08
JP7678756B2 (ja) 2019-09-30 2025-05-16 日本ケミファ株式会社 アゼパン誘導体

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AU2007328007A1 (en) 2008-06-12
WO2008070149A2 (en) 2008-06-12
MX2009006007A (es) 2009-07-17
WO2008070149A3 (en) 2009-12-10
CN101678120A (zh) 2010-03-24
KR20090086627A (ko) 2009-08-13
EP2121029A2 (en) 2009-11-25
US20080318905A1 (en) 2008-12-25
CA2671737A1 (en) 2008-06-12
BRPI0719937A2 (pt) 2014-03-11
NO20092527L (no) 2009-09-04
RU2009125597A (ru) 2011-01-20

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