ES2560807T3 - Nuevos reactivos y procedimiento de conjugación de moléculas biológicas - Google Patents
Nuevos reactivos y procedimiento de conjugación de moléculas biológicas Download PDFInfo
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- ES2560807T3 ES2560807T3 ES11171786.4T ES11171786T ES2560807T3 ES 2560807 T3 ES2560807 T3 ES 2560807T3 ES 11171786 T ES11171786 T ES 11171786T ES 2560807 T3 ES2560807 T3 ES 2560807T3
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- pegylation
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- 238000002360 preparation method Methods 0.000 description 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 description 1
- 102000004196 processed proteins & peptides Human genes 0.000 description 1
- 230000004952 protein activity Effects 0.000 description 1
- 239000012460 protein solution Substances 0.000 description 1
- 238000010926 purge Methods 0.000 description 1
- 238000011002 quantification Methods 0.000 description 1
- BOLDJAUMGUJJKM-LSDHHAIUSA-N renifolin D Natural products CC(=C)[C@@H]1Cc2c(O)c(O)ccc2[C@H]1CC(=O)c3ccc(O)cc3O BOLDJAUMGUJJKM-LSDHHAIUSA-N 0.000 description 1
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- 229920006395 saturated elastomer Polymers 0.000 description 1
- 229910000029 sodium carbonate Inorganic materials 0.000 description 1
- 235000017550 sodium carbonate Nutrition 0.000 description 1
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Classifications
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- C—CHEMISTRY; METALLURGY
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- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C317/00—Sulfones; Sulfoxides
- C07C317/44—Sulfones; Sulfoxides having sulfone or sulfoxide groups and carboxyl groups bound to the same carbon skeleton
- C07C317/48—Sulfones; Sulfoxides having sulfone or sulfoxide groups and carboxyl groups bound to the same carbon skeleton the carbon skeleton being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups
- C07C317/50—Sulfones; Sulfoxides having sulfone or sulfoxide groups and carboxyl groups bound to the same carbon skeleton the carbon skeleton being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups at least one of the nitrogen atoms being part of any of the groups, X being a hetero atom, Y being any atom
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- C—CHEMISTRY; METALLURGY
- C08—ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
- C08G—MACROMOLECULAR COMPOUNDS OBTAINED OTHERWISE THAN BY REACTIONS ONLY INVOLVING UNSATURATED CARBON-TO-CARBON BONDS
- C08G65/00—Macromolecular compounds obtained by reactions forming an ether link in the main chain of the macromolecule
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- 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
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- 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
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C233/00—Carboxylic acid amides
- C07C233/64—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings
- C07C233/67—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms
- C07C233/68—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom
- C07C233/73—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom of a carbon skeleton containing six-membered aromatic rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C317/00—Sulfones; Sulfoxides
- C07C317/26—Sulfones; Sulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton
- C07C317/32—Sulfones; Sulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton with sulfone or sulfoxide groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C49/00—Ketones; Ketenes; Dimeric ketenes; Ketonic chelates
- C07C49/20—Unsaturated compounds containing keto groups bound to acyclic carbon atoms
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D295/00—Heterocyclic 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
- C07D295/04—Heterocyclic 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
- C07D295/14—Heterocyclic 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 carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D295/155—Heterocyclic 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 carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with the ring nitrogen atoms and the carbon atoms with three bonds to hetero atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
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- C—CHEMISTRY; METALLURGY
- C08—ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
- C08G—MACROMOLECULAR COMPOUNDS OBTAINED OTHERWISE THAN BY REACTIONS ONLY INVOLVING UNSATURATED CARBON-TO-CARBON BONDS
- C08G65/00—Macromolecular compounds obtained by reactions forming an ether link in the main chain of the macromolecule
- C08G65/02—Macromolecular compounds obtained by reactions forming an ether link in the main chain of the macromolecule from cyclic ethers by opening of the heterocyclic ring
- C08G65/32—Polymers modified by chemical after-treatment
Landscapes
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- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Engineering & Computer Science (AREA)
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- Bioinformatics & Cheminformatics (AREA)
- Polymers & Plastics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Preparation (AREA)
- Polyethers (AREA)
- Peptides Or Proteins (AREA)
- Addition Polymer Or Copolymer, Post-Treatments, Or Chemical Modifications (AREA)
- Other Resins Obtained By Reactions Not Involving Carbon-To-Carbon Unsaturated Bonds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
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| GB0905762A GB0905762D0 (en) | 2009-04-02 | 2009-04-02 | Novel reagents and method for conjugating biological molecules |
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| GB0316294D0 (en) * | 2003-07-11 | 2003-08-13 | Polytherics Ltd | Conjugated biological molecules and their preparation |
| BRPI0720282B8 (pt) | 2006-12-15 | 2021-05-25 | Baxalta GmbH | construção proteica, composição farmacêutica, e, kit |
| EP2326349B1 (en) | 2008-07-21 | 2015-02-25 | Polytherics Limited | Novel reagents and method for conjugating biological molecules |
| WO2010100430A1 (en) | 2009-03-04 | 2010-09-10 | Polytherics Limited | Conjugated proteins and peptides |
| CN104530182A (zh) | 2009-07-27 | 2015-04-22 | 利普森技术有限公司 | 非凝血蛋白的糖基多唾液酸化 |
| US9795683B2 (en) | 2009-07-27 | 2017-10-24 | Lipoxen Technologies Limited | Glycopolysialylation of non-blood coagulation proteins |
| US8809501B2 (en) | 2009-07-27 | 2014-08-19 | Baxter International Inc. | Nucleophilic catalysts for oxime linkage |
| US8642737B2 (en) | 2010-07-26 | 2014-02-04 | Baxter International Inc. | Nucleophilic catalysts for oxime linkage |
| HRP20160916T1 (hr) | 2009-07-27 | 2016-11-18 | Baxalta GmbH | Konjugati proteina za koagulaciju krvi |
| GB201007356D0 (en) | 2010-04-30 | 2010-06-16 | Leverton Licence Holdings Ltd | Conjugated factor VIIa |
| GB201007357D0 (en) * | 2010-04-30 | 2010-06-16 | Leverton Licence Holdings Ltd | Conjugated factor VIII |
| CN103209710B (zh) * | 2010-09-21 | 2016-04-06 | 克里斯特欧德里发里有限公司 | 用于药物递送系统中组分的短暂连接的可调的、可生物降解的接头分子以及利用其制备的药物递送系统 |
| SG191298A1 (en) | 2010-12-22 | 2013-07-31 | Baxter Int | Materials and methods for conjugating a water soluble fatty acid derivative to a protein |
| EP3412314A1 (en) * | 2011-05-27 | 2018-12-12 | Baxalta GmbH | Therapeutic proteins conjugated to polysialic acid and methods of preparing same |
| JP5841768B2 (ja) * | 2011-08-05 | 2016-01-13 | 花王株式会社 | 脂肪蓄積抑制剤 |
| WO2013156488A2 (en) | 2012-04-16 | 2013-10-24 | Leverton Licence Holdings Limited | Optimised subcutaneous therapeutic agents |
| GB201210770D0 (en) * | 2012-06-18 | 2012-08-01 | Polytherics Ltd | Novel conjugation reagents |
| US9650331B2 (en) | 2012-06-18 | 2017-05-16 | Polytherics Limited | Conjugation reagents |
| MY174813A (en) | 2013-03-15 | 2020-05-16 | Zymeworks Inc | Cytotoxic and anti-mitotic compounds, and methods of using the same |
| BR112015022585B1 (pt) | 2013-03-15 | 2023-04-04 | Regeneron Pharmaceuticals, Inc | Composto, composição farmacêutica, conjugado droga-anticorpo, e, uso dos mesmos |
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| CA2935077C (en) | 2013-12-27 | 2022-03-15 | Geoffrey C. Winters | Sulfonamide-containing linkage systems for drug conjugates |
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| KR20240142591A (ko) | 2015-03-27 | 2024-09-30 | 리제너론 파아마슈티컬스, 인크. | 메이탄시노이드 유도체, 이의 컨주게이트, 및 사용 방법 |
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| US5414135A (en) | 1991-12-30 | 1995-05-09 | Sterling Winthrop Inc. | Vinyl sulfone coupling of polyoxyalkylenes to proteins |
| US5446090A (en) | 1993-11-12 | 1995-08-29 | Shearwater Polymers, Inc. | Isolatable, water soluble, and hydrolytically stable active sulfones of poly(ethylene glycol) and related polymers for modification of surfaces and molecules |
| US5877224A (en) | 1995-07-28 | 1999-03-02 | Rutgers, The State University Of New Jersey | Polymeric drug formulations |
| GB9713979D0 (en) * | 1997-07-03 | 1997-09-10 | Univ Nottingham | Method for attaching peg to macromolecules |
| US6958212B1 (en) * | 1999-02-01 | 2005-10-25 | Eidgenossische Technische Hochschule Zurich | Conjugate addition reactions for the controlled delivery of pharmaceutically active compounds |
| US6828412B1 (en) | 1999-09-03 | 2004-12-07 | School Of Pharmacy, University Of London | Degradable polymers |
| WO2001018080A1 (en) | 1999-09-08 | 2001-03-15 | School Of Pharmacy, University Of London | Uniform molecular weight polymers |
| WO2004060965A2 (en) * | 2002-12-31 | 2004-07-22 | Nektar Therapeutics Al, Corporation | Hydrolytically stable maleimide-terminated polymers |
| JP4009721B2 (ja) * | 2003-05-23 | 2007-11-21 | 独立行政法人産業技術総合研究所 | イオン結合性ポリマー含有基板、該基板を含有する検出用センサー及び病原菌又は病原菌が生産する毒素の検出方法 |
| GB0316294D0 (en) * | 2003-07-11 | 2003-08-13 | Polytherics Ltd | Conjugated biological molecules and their preparation |
| WO2006067221A2 (en) | 2004-12-22 | 2006-06-29 | Kuros Biosurgery Ag | Michael-type addition reaction functionalised peg hydrogels with factor xiiia incorporated biofactors |
| WO2009047500A1 (en) | 2007-10-09 | 2009-04-16 | Polytherics Limited | Novel conjugated proteins and peptides |
| EP2326349B1 (en) | 2008-07-21 | 2015-02-25 | Polytherics Limited | Novel reagents and method for conjugating biological molecules |
| WO2010100430A1 (en) | 2009-03-04 | 2010-09-10 | Polytherics Limited | Conjugated proteins and peptides |
| GB0912485D0 (en) | 2009-07-17 | 2009-08-26 | Polytherics Ltd | Improved conjugation method |
-
2009
- 2009-07-17 EP EP09784718.0A patent/EP2326349B1/en not_active Not-in-force
- 2009-07-17 JP JP2011519228A patent/JP5622117B2/ja not_active Expired - Fee Related
- 2009-07-17 US US13/055,455 patent/US8969626B2/en not_active Expired - Fee Related
- 2009-07-17 DK DK09784718.0T patent/DK2326349T3/en active
- 2009-07-17 CN CN200980128495.3A patent/CN102099058B/zh not_active Expired - Fee Related
- 2009-07-17 WO PCT/GB2009/001764 patent/WO2010010324A1/en not_active Ceased
- 2009-07-17 ES ES11171786.4T patent/ES2560807T3/es active Active
- 2009-07-17 EP EP11171786.4A patent/EP2374481B1/en not_active Not-in-force
- 2009-07-17 PL PL09784718T patent/PL2326349T3/pl unknown
- 2009-07-17 DK DK11171786.4T patent/DK2374481T3/en active
- 2009-07-17 KR KR1020117003833A patent/KR101763559B1/ko not_active Expired - Fee Related
- 2009-07-17 AU AU2009275358A patent/AU2009275358C1/en not_active Ceased
- 2009-07-17 ES ES09784718.0T patent/ES2536882T3/es active Active
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2011
- 2011-07-01 US US13/175,820 patent/US8618333B2/en not_active Expired - Fee Related
- 2011-08-22 JP JP2011180530A patent/JP5626655B2/ja not_active Expired - Fee Related
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2013
- 2013-11-21 US US14/086,702 patent/US9896412B2/en not_active Expired - Fee Related
-
2015
- 2015-02-04 US US14/614,152 patent/US20150148544A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| AU2009275358C1 (en) | 2015-09-24 |
| US20110262994A1 (en) | 2011-10-27 |
| EP2374481A3 (en) | 2012-06-13 |
| US20110136723A1 (en) | 2011-06-09 |
| JP5626655B2 (ja) | 2014-11-19 |
| EP2326349B1 (en) | 2015-02-25 |
| DK2374481T3 (en) | 2016-02-01 |
| CN102099058B (zh) | 2014-10-22 |
| US8618333B2 (en) | 2013-12-31 |
| PL2326349T3 (pl) | 2015-08-31 |
| US20140081047A1 (en) | 2014-03-20 |
| EP2326349A1 (en) | 2011-06-01 |
| EP2374481A2 (en) | 2011-10-12 |
| ES2536882T3 (es) | 2015-05-29 |
| DK2326349T3 (en) | 2015-05-26 |
| JP2011528706A (ja) | 2011-11-24 |
| EP2374481B1 (en) | 2015-11-04 |
| JP5622117B2 (ja) | 2014-11-12 |
| KR20110053430A (ko) | 2011-05-23 |
| CN102099058A (zh) | 2011-06-15 |
| AU2009275358B2 (en) | 2015-05-28 |
| US8969626B2 (en) | 2015-03-03 |
| US9896412B2 (en) | 2018-02-20 |
| US20150148544A1 (en) | 2015-05-28 |
| JP2011252167A (ja) | 2011-12-15 |
| KR101763559B1 (ko) | 2017-08-14 |
| WO2010010324A1 (en) | 2010-01-28 |
| AU2009275358A1 (en) | 2010-01-28 |
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