JP4663233B2 - ベンジル脱離系を利用する高分子チオール結合プロドラッグ - Google Patents

ベンジル脱離系を利用する高分子チオール結合プロドラッグ Download PDF

Info

Publication number
JP4663233B2
JP4663233B2 JP2003543529A JP2003543529A JP4663233B2 JP 4663233 B2 JP4663233 B2 JP 4663233B2 JP 2003543529 A JP2003543529 A JP 2003543529A JP 2003543529 A JP2003543529 A JP 2003543529A JP 4663233 B2 JP4663233 B2 JP 4663233B2
Authority
JP
Japan
Prior art keywords
compound
group
independently
alkyl
substituted
Prior art date
Legal status (The legal status 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 status listed.)
Expired - Fee Related
Application number
JP2003543529A
Other languages
English (en)
Japanese (ja)
Other versions
JP2005513006A6 (ja
JP2005513006A5 (enExample
JP2005513006A (ja
Inventor
チョー，ユン，ファン
グリーンウォルド，リチャード，ビー．
Original Assignee
エンゾン，インコーポレーテッド
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 エンゾン，インコーポレーテッド filed Critical エンゾン，インコーポレーテッド
Publication of JP2005513006A publication Critical patent/JP2005513006A/ja
Publication of JP2005513006A6 publication Critical patent/JP2005513006A6/ja
Publication of JP2005513006A5 publication Critical patent/JP2005513006A5/ja
Application granted granted Critical
Publication of JP4663233B2 publication Critical patent/JP4663233B2/ja
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

Links

Images

Classifications

    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Biomedical Technology (AREA)
  • Transplantation (AREA)
  • Neurology (AREA)
  • Neurosurgery (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)
JP2003543529A 2001-11-09 2002-11-08 ベンジル脱離系を利用する高分子チオール結合プロドラッグ Expired - Fee Related JP4663233B2 (ja)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US34491201P 2001-11-09 2001-11-09
US60/344,912 2001-11-09
US36732002P 2002-03-25 2002-03-25
US60/367,320 2002-03-25
PCT/US2002/035871 WO2003041642A2 (en) 2001-11-09 2002-11-08 Polymeric thiol-linked prodrugs employing benzyl elimination systems

Related Child Applications (1)

Application Number Title Priority Date Filing Date
JP2010093856A Division JP2010195810A (ja) 2001-11-09 2010-04-15 ベンジル脱離系を利用する高分子チオール結合プロドラッグ

Publications (4)

Publication Number Publication Date
JP2005513006A JP2005513006A (ja) 2005-05-12
JP2005513006A6 JP2005513006A6 (ja) 2005-08-04
JP2005513006A5 JP2005513006A5 (enExample) 2006-01-05
JP4663233B2 true JP4663233B2 (ja) 2011-04-06

Family

ID=26994160

Family Applications (2)

Application Number Title Priority Date Filing Date
JP2003543529A Expired - Fee Related JP4663233B2 (ja) 2001-11-09 2002-11-08 ベンジル脱離系を利用する高分子チオール結合プロドラッグ
JP2010093856A Pending JP2010195810A (ja) 2001-11-09 2010-04-15 ベンジル脱離系を利用する高分子チオール結合プロドラッグ

Family Applications After (1)

Application Number Title Priority Date Filing Date
JP2010093856A Pending JP2010195810A (ja) 2001-11-09 2010-04-15 ベンジル脱離系を利用する高分子チオール結合プロドラッグ

Country Status (6)

Country Link
US (1) US7262164B2 (enExample)
EP (1) EP1450844A4 (enExample)
JP (2) JP4663233B2 (enExample)
AU (1) AU2002359364A1 (enExample)
CA (1) CA2465090C (enExample)
WO (1) WO2003041642A2 (enExample)

Families Citing this family (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DK1450822T3 (da) * 2001-11-09 2010-04-19 Enzon Inc Polyalkylenoxidkonjugater af thiolholdige medicinske præparater
US7595318B2 (en) * 2004-01-23 2009-09-29 Elan Pharmaceuticals, Inc. Polyethylene glycol conjugates of heterocycloalkyl carboxamido propanoic acids
WO2006015318A2 (en) * 2004-07-30 2006-02-09 Biogen Idec Inc. Antibody conjugated to a drug moiety via a poptidic linker
AU2006322254B2 (en) * 2005-12-05 2012-08-02 Nitto Denko Corporation Polyglutamate-amino acid conjugates and methods
JP5341879B2 (ja) 2007-05-09 2013-11-13 日東電工株式会社 疎水性化合物及びポリアミノ酸複合体を含む組成物
US20090092664A1 (en) * 2007-10-08 2009-04-09 University Of Kentucky Research Foundation Polymer-metal chelator conjugates and uses thereof
CN102482278B (zh) 2009-06-29 2015-04-22 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
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
TW201249844A (en) 2010-12-20 2012-12-16 Incyte Corp 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
US9126948B2 (en) 2011-03-25 2015-09-08 Incyte Holdings Corporation Pyrimidine-4,6-diamine derivatives as PI3K inhibitors
TWI648277B (zh) 2011-09-02 2019-01-21 美商英塞特控股公司 作為ｐｉ３ｋ抑制劑之雜環基胺
AR090548A1 (es) 2012-04-02 2014-11-19 Incyte Corp Azaheterociclobencilaminas biciclicas como inhibidores de pi3k
TWI636046B (zh) 2013-05-17 2018-09-21 美國禮來大藥廠 苯氧基乙基二氫－１ｈ－異喹啉化合物
WO2015191677A1 (en) 2014-06-11 2015-12-17 Incyte Corporation Bicyclic heteroarylaminoalkyl phenyl derivatives as pi3k inhibitors
CA3285092A1 (en) 2015-02-27 2025-11-29 Incyte Holdings Corporation Salts of pi3k inhibitor and processes for their preparation
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
US11007273B2 (en) 2017-07-05 2021-05-18 Duke University Prochelators as targeted prodrugs for prostate cancer and methods of making and using same
CN120053645A (zh) 2018-06-01 2025-05-30 因赛特公司 治疗pi3k相关病症的给药方案

Family Cites Families (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2944902A (en) * 1956-07-30 1960-07-12 Eastman Kodak Co Sensitization of photographic emulsions with ionic polyalkylene oxide salts
DE2343147C2 (de) * 1973-08-27 1982-06-09 Henkel KGaA, 4000 Düsseldorf Pyrrolidon-5,5-diphosphonsäuren, deren wasserlösliche Salze, und Verfahren zu ihrer Herstellung
US4479002A (en) * 1975-12-01 1984-10-23 Union Carbide Corporation Carbamate-carbamoyl fluoride compounds
US4623715A (en) * 1984-10-22 1986-11-18 Hoechst Aktiengeselleschaft Novel peptides which are active on the central nervous system and have an action on the cholinergic system
US4772586A (en) * 1985-01-23 1988-09-20 Medical College Of Ohio Novel derivatives of arginine vasopressin antagonists
US5112739A (en) * 1988-08-02 1992-05-12 Polaroid Corporation Enzyme controlled release system
JPH05132431A (ja) * 1990-03-28 1993-05-28 Nippon Oil & Fats Co Ltd 高分子化薬剤およびその製造法
US5130126A (en) * 1990-07-09 1992-07-14 Nippon Oil & Fats Co., Ltd. Polymer-drug conjugate and a method of producing it
US5245032A (en) * 1990-09-20 1993-09-14 Union Carbide Chemicals & Plastics Technology Corporation Catalytic processes for the preparation of n,n,n-trisubstituted nitrogen-containing compounds
US5681811A (en) * 1993-05-10 1997-10-28 Protein Delivery, Inc. Conjugation-stabilized therapeutic agent compositions, delivery and diagnostic formulations comprising same, and method of making and using the same
WO1995010860A1 (en) * 1993-10-13 1995-04-20 Valence Technology, Inc. Solid electrolytes containing oxyalkylene solvents and/or oxyalkylene polymers and electrolytic cells produced therefrom
US5880131A (en) * 1993-10-20 1999-03-09 Enzon, Inc. High molecular weight polymer-based prodrugs
US5932462A (en) * 1995-01-10 1999-08-03 Shearwater Polymers, Inc. Multiarmed, monofunctional, polymer for coupling to molecules and surfaces
US6255361B1 (en) * 1995-11-21 2001-07-03 Acushnet Company Golf ball compositions and method of making same
WO1998025934A1 (en) * 1996-12-13 1998-06-18 Kyowa Hakko Kogyo Co., Ltd. Dc 107 derivatives (2)
EP1037649B1 (en) * 1997-12-17 2009-09-30 Enzon, Inc. Polymeric prodrugs of amino- and hydroxyl-containing bioactive agents
US6765019B1 (en) 1999-05-06 2004-07-20 University Of Kentucky Research Foundation Permeable, water soluble, non-irritating prodrugs of chemotherapeutic agents with oxaalkanoic acids
DK1450822T3 (da) * 2001-11-09 2010-04-19 Enzon Inc Polyalkylenoxidkonjugater af thiolholdige medicinske præparater

Also Published As

Publication number Publication date
CA2465090C (en) 2010-02-02
EP1450844A2 (en) 2004-09-01
AU2002359364A1 (en) 2003-05-26
CA2465090A1 (en) 2003-05-22
EP1450844A4 (en) 2009-07-29
WO2003041642A2 (en) 2003-05-22
US20030157052A1 (en) 2003-08-21
WO2003041642A3 (en) 2004-04-01
US7262164B2 (en) 2007-08-28
JP2010195810A (ja) 2010-09-09
JP2005513006A (ja) 2005-05-12

Similar Documents

Publication Publication Date Title
JP4663233B2 (ja) ベンジル脱離系を利用する高分子チオール結合プロドラッグ
JP2005513006A6 (ja) ベンジル脱離系を利用する高分子チオール結合プロドラッグ
JP4675028B2 (ja) トリメチルロック型テトラパルテートプロドラッグ
EP1362053B1 (en) Terminally-branched polymeric linkers and polymeric conjugates containing the same
JP4824404B2 (ja) 脂肪族生物分解性リンカーに基づく放出可能なポリマー複合体
US6720306B2 (en) Tetrapartate prodrugs
US20090311182A1 (en) Macromolecular Delivery Systems for Non-Invasive Imaging, Evaluation and Treatment of Arthritis and Other Inflammatory Diseases
JP2009197023A (ja) ヒドロキシアパタイト標的化ポリ（エチレングリコール）および関連重合体
EP1361895B1 (en) Terminally-branched polymeric linkers and polymeric conjugates containing the same
ES2331562T3 (es) Profarmacos de agentes anticancerigenos que emplean acidos aromaticos sustituidos.
JP2004518776A (ja) テトラパルテートプロドラッグ
EP1450822B1 (en) Polyalkylene oxide conjugates of thiol-containing drugs
JP2005512991A6 (ja) 高分子チオール結合プロドラッグ
CN117122695A (zh) 一种靶向活化cd44分子的透明质酸功能化偶联物及制备方法和应用
JP2009531478A (ja) 新規な活性化ポリ（エチレングリコール）及び関連ポリマー並びにそれらの適用
US10945997B2 (en) Polymer derivative of macrolide immunosuppressant

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20051020

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20051020

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20090609

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20090903

A602 Written permission of extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A602

Effective date: 20090910

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20091104

A02 Decision of refusal

Free format text: JAPANESE INTERMEDIATE CODE: A02

Effective date: 20091215

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20100415

A911 Transfer to examiner for re-examination before appeal (zenchi)

Free format text: JAPANESE INTERMEDIATE CODE: A911

Effective date: 20100602

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20100803

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20101020

TRDD Decision of grant or rejection written
A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

Effective date: 20101214

A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20110105

R150 Certificate of patent or registration of utility model

Free format text: JAPANESE INTERMEDIATE CODE: R150

FPAY Renewal fee payment (event date is renewal date of database)

Free format text: PAYMENT UNTIL: 20140114

Year of fee payment: 3

LAPS Cancellation because of no payment of annual fees