JP2005504006A - シンナメートとのアシル化によるプロドラッグ結合 - Google Patents

シンナメートとのアシル化によるプロドラッグ結合 Download PDF

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JP2005504006A
JP2005504006A JP2002580872A JP2002580872A JP2005504006A JP 2005504006 A JP2005504006 A JP 2005504006A JP 2002580872 A JP2002580872 A JP 2002580872A JP 2002580872 A JP2002580872 A JP 2002580872A JP 2005504006 A JP2005504006 A JP 2005504006A
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group
compound
alkyl
cinn
biologically active
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JP2005504006A5 (enExample
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ギルバート,カール・ダブリュー
マクゴーワン,エレノア・ビー
ブラック,カービー・エス
ハーパー,グレゴリー・ティー・ピー
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クリオライフ インコーポレーテッド
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/30Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
    • C07D207/34Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members 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
    • C07D207/36Oxygen or sulfur atoms
    • C07D207/402,5-Pyrrolidine-diones
    • C07D207/4162,5-Pyrrolidine-diones 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 other ring carbon atoms
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/44Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having three double bonds between ring members or between ring members and non-ring members
    • C07D207/444Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having three double bonds between ring members or between ring members and non-ring members having two doubly-bound oxygen atoms directly attached in positions 2 and 5
    • C07D207/448Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having three double bonds between ring members or between ring members and non-ring members having two doubly-bound oxygen atoms directly attached in positions 2 and 5 with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to other ring carbon atoms, e.g. maleimide
    • C07D207/452Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having three double bonds between ring members or between ring members and non-ring members having two doubly-bound oxygen atoms directly attached in positions 2 and 5 with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to other ring carbon atoms, e.g. maleimide with hydrocarbon radicals, substituted by hetero atoms, directly attached to the ring nitrogen atom
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/46Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with hetero atoms directly attached to the ring nitrogen atom
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D231/00Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/12Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D233/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/56Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D249/00Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/081,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D295/00Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/08Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms
    • C07D295/096Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms with the ring nitrogen atoms and the oxygen or sulfur atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D305/00Heterocyclic compounds containing four-membered rings having one oxygen atom as the only ring hetero atoms
    • C07D305/14Heterocyclic compounds containing four-membered rings having one oxygen atom as the only ring hetero atoms condensed with carbocyclic rings or ring systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/22Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains four or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H15/00Compounds containing hydrocarbon or substituted hydrocarbon radicals directly attached to hetero atoms of saccharide radicals
    • C07H15/20Carbocyclic rings
    • C07H15/24Condensed ring systems having three or more rings
    • C07H15/252Naphthacene radicals, e.g. daunomycins, adriamycins

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Molecular Biology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biochemistry (AREA)
  • Biotechnology (AREA)
  • Genetics & Genomics (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Saccharide Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Epoxy Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyrrole Compounds (AREA)
JP2002580872A 2001-04-17 2002-04-12 シンナメートとのアシル化によるプロドラッグ結合 Pending JP2005504006A (ja)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US28430401P 2001-04-17 2001-04-17
US31578201P 2001-08-28 2001-08-28
US10/066,306 US6774116B2 (en) 2001-04-17 2002-01-31 Prodrugs via acylation with cinnamate
PCT/US2002/011330 WO2002083067A2 (en) 2001-04-17 2002-04-12 Prodrugs via acylation with cinnamate

Publications (2)

Publication Number Publication Date
JP2005504006A true JP2005504006A (ja) 2005-02-10
JP2005504006A5 JP2005504006A5 (enExample) 2005-12-22

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JP2002580872A Pending JP2005504006A (ja) 2001-04-17 2002-04-12 シンナメートとのアシル化によるプロドラッグ結合

Country Status (5)

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US (1) US6774116B2 (enExample)
EP (1) EP1395256A4 (enExample)
JP (1) JP2005504006A (enExample)
CA (1) CA2444264A1 (enExample)
WO (1) WO2002083067A2 (enExample)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2010533233A (ja) * 2007-07-11 2010-10-21 エンゾン ファーマシューティカルズ,インコーポレーテッド 芳香族アリル酸を含むポリマー性薬剤送達システム
JP2015508055A (ja) * 2012-01-27 2015-03-16 エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft Lfa−1を発現する細胞への標的化送達のためのインテグリンアンタゴニスト結合体

Families Citing this family (24)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7157458B2 (en) * 2001-04-17 2007-01-02 Cryolife, Inc. Bifunctional energy-reversible acyl-compositions
AU2002953533A0 (en) * 2002-12-24 2003-01-16 Arthron Limited Fc receptor modulating compounds and compositions
KR101025143B1 (ko) 2002-12-31 2011-04-01 넥타르 테라퓨틱스 가수분해상으로 안정한 말레이미드-종결 중합체
US7432331B2 (en) 2002-12-31 2008-10-07 Nektar Therapeutics Al, Corporation Hydrolytically stable maleimide-terminated polymers
CA2543722C (en) * 2003-10-29 2011-01-04 Sonus Pharmaceuticals, Inc. Tocopherol-modified therapeutic drug compounds
US20080119421A1 (en) * 2003-10-31 2008-05-22 Jack Tuszynski Process for treating a biological organism
US6887952B1 (en) * 2004-02-12 2005-05-03 Biosite, Inc. N-aryl-carbamic acid ester-derived and valeric acid ester-derived cross-linkers and conjugates, and methods for their synthesis and use
US20080177220A1 (en) * 2006-01-06 2008-07-24 The Curators Of The University Of Missouri Ultrasound-Mediated Transcleral Drug Delivery
FR2902792A1 (fr) * 2006-06-21 2007-12-28 Servier Lab Nouveaux derives cinnamates de tetrahydro-7h-pyrano(2,3-c)acridin-7-one, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
CA2698812A1 (en) * 2007-09-14 2009-03-19 Nitto Denko Corporation Drug carriers
US20100068233A1 (en) * 2008-09-16 2010-03-18 Searete Llc, A Limited Liability Corporation Of The State Of Delaware Modifiable dosage form
US20100068256A1 (en) * 2008-09-16 2010-03-18 Searete Llc, A Limited Liability Corporation Of The State Of Delaware Ex vivo modifiable medicament release-substance
US20100068153A1 (en) * 2008-09-16 2010-03-18 Searete Llc, A Limited Liability Corporation Of The State Of Delaware Ex vivo activatable final dosage form
US20100069821A1 (en) * 2008-09-16 2010-03-18 Searete Llc, A Limited Liability Corporation Of The State Of Delaware Ex vivo modifiable medicament release-sites final dosage form
US20100068254A1 (en) * 2008-09-16 2010-03-18 Mahalaxmi Gita Bangera Modifying a medicament availability state of a final dosage form
US20100068235A1 (en) * 2008-09-16 2010-03-18 Searete LLC, a limited liability corporation of Deleware Individualizable dosage form
US20100068275A1 (en) * 2008-09-16 2010-03-18 Searete Llc, A Limited Liability Corporation Of The State Of Delaware Personalizable dosage form
US20100068152A1 (en) * 2008-09-16 2010-03-18 Searete Llc, A Limited Liability Corporation Of The State Of Delaware Ex vivo modifiable particle or polymeric based final dosage form
GB2528643A (en) * 2014-07-08 2016-02-03 Adc Biotechnology Ltd Method of synthesising ADCs
KR20240074000A (ko) 2017-02-28 2024-05-27 다이이찌 산쿄 가부시키가이샤 항 her3 항체-약물 콘주게이트 투여에 의한 egfr-tki 저항성의 비소세포 폐암의 치료 방법
CN107365283B (zh) * 2017-08-07 2020-12-08 无锡紫杉药业有限公司 一种紫杉醇光降解获得杂质的方法
WO2020059772A1 (ja) 2018-09-20 2020-03-26 第一三共株式会社 抗her3抗体-薬物コンジュゲート投与によるher3変異がんの治療
CN113101372B (zh) * 2019-12-24 2025-02-14 北京大学 具有辐射响应基团的缀合物及其用途
WO2025002105A1 (zh) * 2023-06-26 2025-01-02 北京大学 可通过辐射激活的化合物及其用途

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5218136A (en) * 1987-12-28 1993-06-08 Sumitomo Chemical Company, Limited Styryl compounds, process for preparing the same and photoresist compositions comprising the same
US5114851A (en) * 1989-08-29 1992-05-19 Duke University Light activated acyl-enzymes
US5218137A (en) * 1989-08-29 1993-06-08 Duke University Light activated acyl-enzymes
EP0936211B1 (en) * 1998-02-13 2010-07-07 Givaudan SA Aryl-acrylic acid esters useful as precursors for organoleptic compounds
JP2000264868A (ja) * 1999-01-12 2000-09-26 Bunshi Biophotonics Kenkyusho:Kk 新規ケージドアミノ酸
JP2000319202A (ja) * 1999-01-12 2000-11-21 Bunshi Biophotonics Kenkyusho:Kk 新規ケージド化合物調製用試薬、及びケージド化方法

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2010533233A (ja) * 2007-07-11 2010-10-21 エンゾン ファーマシューティカルズ,インコーポレーテッド 芳香族アリル酸を含むポリマー性薬剤送達システム
JP2015508055A (ja) * 2012-01-27 2015-03-16 エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft Lfa−1を発現する細胞への標的化送達のためのインテグリンアンタゴニスト結合体

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Publication number Publication date
US20020187992A1 (en) 2002-12-12
CA2444264A1 (en) 2002-10-24
WO2002083067A2 (en) 2002-10-24
US6774116B2 (en) 2004-08-10
WO2002083067A3 (en) 2003-12-11
EP1395256A2 (en) 2004-03-10
WO2002083067A9 (en) 2004-02-26
EP1395256A4 (en) 2005-10-05

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