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 PDFInfo
- 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
Links
- 0 CC(C(CC(*)=O)N)=O Chemical compound CC(C(CC(*)=O)N)=O 0.000 description 2
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)
- Saccharide Compounds (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
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 (https=) | 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 (https=) |
| EP (1) | EP1450844A4 (https=) |
| JP (2) | JP4663233B2 (https=) |
| AU (1) | AU2002359364A1 (https=) |
| CA (1) | CA2465090C (https=) |
| WO (1) | WO2003041642A2 (https=) |
Families Citing this family (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE60234858D1 (de) * | 2001-11-09 | 2010-02-04 | Enzon Inc | Polyalkylenoxid-Konjugate von thiolhaltigen Arzneistoffen |
| WO2005070921A1 (en) * | 2004-01-23 | 2005-08-04 | 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 |
| ATE465205T1 (de) * | 2005-12-05 | 2010-05-15 | Nitto Denko Corp | Polyglutamat-aminosäure-konjugate und verfahren |
| PT2155255E (pt) | 2007-05-09 | 2013-10-15 | Nitto Denko Corp | Composições que incluem um composto hidrofóbico e um conjugado de poliaminoácido |
| US20090092664A1 (en) * | 2007-10-08 | 2009-04-09 | University Of Kentucky Research Foundation | Polymer-metal chelator conjugates and uses thereof |
| CN104945420A (zh) | 2009-06-29 | 2015-09-30 | 因塞特公司 | 作为pi3k抑制剂的嘧啶酮类 |
| US8680108B2 (en) * | 2009-12-18 | 2014-03-25 | 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 |
| AR081823A1 (es) | 2010-04-14 | 2012-10-24 | Incyte Corp | DERIVADOS FUSIONADOS COMO INHIBIDORES DE PI3Kd |
| US9062055B2 (en) | 2010-06-21 | 2015-06-23 | Incyte Corporation | Fused pyrrole derivatives as PI3K inhibitors |
| EP2655374B1 (en) | 2010-12-20 | 2019-10-23 | Incyte Holdings Corporation | 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 |
| WO2012135009A1 (en) | 2011-03-25 | 2012-10-04 | Incyte Corporation | Pyrimidine-4,6-diamine derivatives as pi3k inhibitors |
| KR102507287B1 (ko) | 2011-09-02 | 2023-03-07 | 인사이트 홀딩스 코포레이션 | Pi3k 억제제로서 헤테로시클릴아민 |
| 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 |
| SI3831833T1 (sl) | 2015-02-27 | 2023-03-31 | Incyte Holdings Corporation | Postopki za pripravo inhibitorja PI3K |
| 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 |
| WO2019010231A1 (en) * | 2017-07-05 | 2019-01-10 | Duke University | APPARATUS AS TARGETED PRODRUGS FOR PROSTATE CANCER AND METHODS OF MAKING AND USING THE SAME |
| CA3101323A1 (en) | 2018-06-01 | 2019-12-05 | Incyte Corporation | Dosing regimen for the treatment of pi3k related disorders |
Family Cites Families (18)
| 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 |
| AU7932494A (en) * | 1993-10-13 | 1995-05-04 | 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 |
| CA2245922A1 (en) * | 1996-12-13 | 1998-06-18 | Shun-Ichi Ikeda | Dc 107 derivatives (2) |
| WO1999030727A1 (en) * | 1997-12-17 | 1999-06-24 | 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 |
| DE60234858D1 (de) * | 2001-11-09 | 2010-02-04 | Enzon Inc | Polyalkylenoxid-Konjugate von thiolhaltigen Arzneistoffen |
-
2002
- 2002-11-08 WO PCT/US2002/035871 patent/WO2003041642A2/en not_active Ceased
- 2002-11-08 AU AU2002359364A patent/AU2002359364A1/en not_active Abandoned
- 2002-11-08 JP JP2003543529A patent/JP4663233B2/ja not_active Expired - Fee Related
- 2002-11-08 CA CA002465090A patent/CA2465090C/en not_active Expired - Fee Related
- 2002-11-08 EP EP02793896A patent/EP1450844A4/en not_active Withdrawn
- 2002-11-08 US US10/290,694 patent/US7262164B2/en not_active Expired - Fee Related
-
2010
- 2010-04-15 JP JP2010093856A patent/JP2010195810A/ja active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| EP1450844A2 (en) | 2004-09-01 |
| CA2465090C (en) | 2010-02-02 |
| US7262164B2 (en) | 2007-08-28 |
| EP1450844A4 (en) | 2009-07-29 |
| JP2005513006A (ja) | 2005-05-12 |
| JP2010195810A (ja) | 2010-09-09 |
| WO2003041642A3 (en) | 2004-04-01 |
| US20030157052A1 (en) | 2003-08-21 |
| CA2465090A1 (en) | 2003-05-22 |
| AU2002359364A1 (en) | 2003-05-26 |
| WO2003041642A2 (en) | 2003-05-22 |
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 | |
| US20030092608A1 (en) | Pharmaceutical composition for inhibiting the metastasis or preventing the recurrence of malignant tumor | |
| 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 |