DK3153504T3 - Fremgangsmåder til fremstilling af ladede tværbindere - Google Patents
Fremgangsmåder til fremstilling af ladede tværbindere Download PDFInfo
- Publication number
- DK3153504T3 DK3153504T3 DK16186412.9T DK16186412T DK3153504T3 DK 3153504 T3 DK3153504 T3 DK 3153504T3 DK 16186412 T DK16186412 T DK 16186412T DK 3153504 T3 DK3153504 T3 DK 3153504T3
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- DK
- Denmark
- Prior art keywords
- compound
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Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
- C07D213/28—Radicals substituted by singly-bound oxygen or sulphur atoms
- C07D213/32—Sulfur atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
- C07D213/62—Oxygen or sulfur atoms
- C07D213/70—Sulfur atoms
- C07D213/71—Sulfur atoms to which a second hetero atom is attached
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C305/00—Esters of sulfuric acids
- C07C305/02—Esters of sulfuric acids having oxygen atoms of sulfate groups bound to acyclic carbon atoms of a carbon skeleton
- C07C305/04—Esters of sulfuric acids having oxygen atoms of sulfate groups bound to acyclic carbon atoms of a carbon skeleton being acyclic and saturated
- C07C305/06—Hydrogenosulfates
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic 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
- C07D207/44—Heterocyclic 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
- C07D207/444—Heterocyclic 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
- C07D207/448—Heterocyclic 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
- C07D207/452—Heterocyclic 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/46—Heterocyclic 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
-
- C—CHEMISTRY; METALLURGY
- C08—ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
- C08K—Use of inorganic or non-macromolecular organic substances as compounding ingredients
- C08K5/00—Use of organic ingredients
- C08K5/36—Sulfur-, selenium-, or tellurium-containing compounds
- C08K5/37—Thiols
- C08K5/372—Sulfides, e.g. R-(S)x-R'
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Medicinal Chemistry (AREA)
- Polymers & Plastics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Pyridine Compounds (AREA)
- Processes Of Treating Macromolecular Substances (AREA)
- Addition Polymer Or Copolymer, Post-Treatments, Or Chemical Modifications (AREA)
- Manufacture Of Macromolecular Shaped Articles (AREA)
- Polyamides (AREA)
Claims (14)
- FREMGANGSMÅDER TIL FREMSTILLING AF LADEDE TVÆRBINDERE1. Fremgangsmåde til fremstilling af en forbindelse repræsenteret ved formlen (V):der omfatter følgende trin: a) omsætning af en forbindelse med formlen (2a):eller et salt deraf, med et sulfoneringsmiddel for at danne en forbindelse med formlen (IV):eller et salt deraf; b) omsætning af forbindelsen med formlen (IV), eller et salt deraf, med N-hydroxysuccinimid i nærvær af en base for at danne et salt af forbindelsen med formlen (V); og c) oprensning af saltet af forbindelsen med formlen (V) ved krystallisering af saltet af forbindelsen med formlen (V) i et organisk opløsningsmiddel eller en blanding af et organisk opløsningsmiddel og vand i nærvær af en syre for at danne den neutrale form af forbindelsen med formlen (V).
- 2. Fremgangsmåde ifølge krav 1, hvor sulfoneringsmidlet er chlorsulfonsyre eller svovldioxid.
- 3. Fremgangsmåde ifølge krav 1, hvor sulfoneringsmidlet er chlorsulfonsyre.
- 4. Fremgangsmåde ifølge et hvilket som helst af kravene 1-3, hvor sulfoneringsreaktionen udføres i nærvær af PySSPy.
- 5. Fremgangsmåde ifølge krav 4, hvor ca. 0,5 ækvivalent PySSPy er til stede.
- 6. Fremgangsmåde ifølge et hvilket som helst af kravene 1-5, hvor omsætningen mellem forbindelsen med formlen (IV) og N-hydroxysuccinimid sker i nærvær af et koblingsmiddel.
- 7. Fremgangsmåde ifølge krav 6, hvor koblingsmidlet vælges fra MV'-dicyclohexylcarbodiimid (DCC), l-ethyl-3-(3-dimethylaminopropyl)carbodiimid (EDC), ΛξΜ-diisopropylcarbodiimid (DIC) og 1-ethoxycarbonyl-2-ethoxy-l,2-dihydroquinolin (EEDQ).
- 8. Fremgangsmåde ifølge krav 7, hvor koblingsmidlet er EDC.
- 9. Fremgangsmåde ifølge et hvilket som helst af kravene 1-8, hvor basen er diisopropylethylamin (DIPEA).
- 10. Fremgangsmåde ifølge krav 1, hvor fremgangsmåden omfatter følgende trin:a) omsætning af forbindelsen med formlen (2a) eller et salt deraf med chlorsulfonsyre for at danne forbindelsen med formlen (IV); og b) omsætning af forbindelsen med formlen (IV) med N-hydroxysuccinimid i nærvær af EDC for at danne forbindelsen med formlen (V).
- 11. Fremgangsmåde ifølge et hvilket som helst af kravene 1-10, hvor syren er HC1 eller H2SO4.
- 12. Fremgangsmåde ifølge krav 11, hvor syren er HC1.
- 13. Fremgangsmåde ifølge et hvilket som helst af kravene 1-12, hvor krystallisering udføres i en blanding af et organisk opløsningsmiddel og vand.
- 14. Fremgangsmåde ifølge krav 13, hvor blandingen af et organisk opløsningsmiddel og vand er acetone/vand, DMF/vand, DMSO/vand eller acetonitril/vand.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US42135710P | 2010-12-09 | 2010-12-09 | |
| EP11846704.2A EP2648510B1 (en) | 2010-12-09 | 2011-12-08 | Methods for the preparation of charged crosslinkers |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| DK3153504T3 true DK3153504T3 (da) | 2019-01-07 |
Family
ID=46207513
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| DK16186412.9T DK3153504T3 (da) | 2010-12-09 | 2011-12-08 | Fremgangsmåder til fremstilling af ladede tværbindere |
Country Status (18)
| Country | Link |
|---|---|
| US (5) | US8598362B2 (da) |
| EP (2) | EP3153504B1 (da) |
| KR (1) | KR101959578B1 (da) |
| CN (2) | CN103260406B (da) |
| CY (1) | CY1121055T1 (da) |
| DK (1) | DK3153504T3 (da) |
| ES (2) | ES2702926T3 (da) |
| HR (1) | HRP20182026T1 (da) |
| HU (1) | HUE041699T2 (da) |
| IL (3) | IL226795A (da) |
| LT (1) | LT3153504T (da) |
| PL (1) | PL3153504T3 (da) |
| PT (1) | PT3153504T (da) |
| RS (1) | RS58033B1 (da) |
| SG (3) | SG190214A1 (da) |
| SI (1) | SI3153504T1 (da) |
| TR (1) | TR201819440T4 (da) |
| WO (1) | WO2012078868A1 (da) |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SG190214A1 (en) * | 2010-12-09 | 2013-06-28 | Immunogen Inc | Methods for the preparation of charged crosslinkers |
| JP6026305B2 (ja) | 2013-02-04 | 2016-11-16 | 古河電気工業株式会社 | 標識抗体の製造方法 |
| US9518017B2 (en) | 2013-06-28 | 2016-12-13 | Immunogen, Inc. | Purification of intermediates used in the preparation of heterobifunctional linkers |
| US10208125B2 (en) | 2013-07-15 | 2019-02-19 | University of Pittsburgh—of the Commonwealth System of Higher Education | Anti-mucin 1 binding agents and uses thereof |
| US10464955B2 (en) | 2014-02-28 | 2019-11-05 | Hangzhou Dac Biotech Co., Ltd. | Charged linkers and their uses for conjugation |
| CN104892748B (zh) * | 2014-03-04 | 2018-12-21 | 深圳翰宇药业股份有限公司 | 人类松弛素-2衍生物以及由其制备人类松弛素-2的方法 |
Family Cites Families (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US1926422A (en) | 1930-12-29 | 1933-09-12 | Fred C Armbruster | Pipe joint |
| DE800410C (de) * | 1948-10-02 | 1950-11-06 | Basf Ag | Verfahren zur Herstellung von Lactonsulfonsaeuren |
| US2822387A (en) * | 1955-12-07 | 1958-02-04 | Universal Oil Prod Co | Method of producing sulfonated alkanes |
| US3418290A (en) * | 1965-10-18 | 1968-12-24 | Du Pont | Sulfonated caprolactones and polymerization with 2,2-dialkyl-3-propiolactones |
| US4244885A (en) * | 1977-12-08 | 1981-01-13 | Yeda Research And Development Co. Ltd. | α-Substituted-3-(halomethyl)-4-hydroxybenzeneacetic acids |
| US4563304A (en) | 1981-02-27 | 1986-01-07 | Pharmacia Fine Chemicals Ab | Pyridine compounds modifying proteins, polypeptides or polysaccharides |
| US5208020A (en) | 1989-10-25 | 1993-05-04 | Immunogen Inc. | Cytotoxic agents comprising maytansinoids and their therapeutic use |
| EP0563475B1 (en) | 1992-03-25 | 2000-05-31 | Immunogen Inc | Cell binding agent conjugates of derivatives of CC-1065 |
| CA2130723C (en) * | 1993-09-03 | 2006-01-31 | Wilhelm Quittmann | Process for preparing y-mercaptocarboxylic acid derivatives |
| DE19609338A1 (de) | 1996-03-11 | 1997-09-18 | Hoechst Ag | Benzothioxanthen-Farbstoffe, ihre Herstellung und ihre Verwendung |
| AU765588C (en) | 1999-11-24 | 2004-12-16 | Immunogen, Inc. | Cytotoxic agents comprising taxanes and their therapeutic use |
| US6716821B2 (en) | 2001-12-21 | 2004-04-06 | Immunogen Inc. | Cytotoxic agents bearing a reactive polyethylene glycol moiety, cytotoxic conjugates comprising polyethylene glycol linking groups, and methods of making and using the same |
| US6756397B2 (en) | 2002-04-05 | 2004-06-29 | Immunogen, Inc. | Prodrugs of CC-1065 analogs |
| US6747048B2 (en) | 2002-05-08 | 2004-06-08 | Bristol-Myers Squibb Company | Pyridine-based thyroid receptor ligands |
| DE60336149D1 (de) | 2002-08-16 | 2011-04-07 | Immunogen Inc | Vernetzer mit hoher reaktivität und löslichkeit und ihre verwendung bei der herstellung von konjugaten für die gezielte abgabe von kleinmolekularen arzneimitteln |
| US7276497B2 (en) | 2003-05-20 | 2007-10-02 | Immunogen Inc. | Cytotoxic agents comprising new maytansinoids |
| EP1688415A1 (en) | 2004-12-07 | 2006-08-09 | Aventis Pharma S.A. | Cytotoxic agents comprising new C-2 modified taxanes |
| KR20100137585A (ko) | 2008-04-30 | 2010-12-30 | 이뮤노젠 아이엔씨 | 강력한 복합체 및 친수성 링커 |
| CN104524592B (zh) * | 2008-04-30 | 2018-06-05 | 伊缪诺金公司 | 交联剂和它们的用途 |
| MX2011008328A (es) | 2009-02-05 | 2011-11-04 | Immunogen Inc | Derivados novedosos de benzodiacepina. |
| SG190214A1 (en) * | 2010-12-09 | 2013-06-28 | Immunogen Inc | Methods for the preparation of charged crosslinkers |
-
2011
- 2011-12-08 SG SG2013035555A patent/SG190214A1/en unknown
- 2011-12-08 CN CN201180059248.XA patent/CN103260406B/zh active Active
- 2011-12-08 ES ES16186412T patent/ES2702926T3/es active Active
- 2011-12-08 SG SG10202005580RA patent/SG10202005580RA/en unknown
- 2011-12-08 RS RS20181471A patent/RS58033B1/sr unknown
- 2011-12-08 TR TR2018/19440T patent/TR201819440T4/tr unknown
- 2011-12-08 WO PCT/US2011/063944 patent/WO2012078868A1/en active Application Filing
- 2011-12-08 DK DK16186412.9T patent/DK3153504T3/da active
- 2011-12-08 HU HUE16186412A patent/HUE041699T2/hu unknown
- 2011-12-08 EP EP16186412.9A patent/EP3153504B1/en active Active
- 2011-12-08 EP EP11846704.2A patent/EP2648510B1/en active Active
- 2011-12-08 PT PT16186412T patent/PT3153504T/pt unknown
- 2011-12-08 US US13/315,005 patent/US8598362B2/en active Active
- 2011-12-08 ES ES11846704.2T patent/ES2602118T3/es active Active
- 2011-12-08 PL PL16186412T patent/PL3153504T3/pl unknown
- 2011-12-08 LT LTEP16186412.9T patent/LT3153504T/lt unknown
- 2011-12-08 SI SI201131636T patent/SI3153504T1/sl unknown
- 2011-12-08 SG SG10201509886YA patent/SG10201509886YA/en unknown
- 2011-12-08 CN CN201610836137.XA patent/CN107011253B/zh active Active
- 2011-12-08 KR KR1020137015769A patent/KR101959578B1/ko active IP Right Grant
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2013
- 2013-06-06 IL IL226795A patent/IL226795A/en active IP Right Grant
- 2013-10-03 US US14/045,151 patent/US8921566B2/en active Active
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2014
- 2014-11-12 US US14/539,361 patent/US9242936B2/en active Active
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2015
- 2015-07-28 IL IL240201A patent/IL240201A0/en unknown
- 2015-07-28 IL IL240200A patent/IL240200A/en active IP Right Grant
- 2015-12-15 US US14/969,720 patent/US9663492B2/en active Active
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2017
- 2017-04-25 US US15/496,775 patent/US10112925B2/en active Active
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2018
- 2018-12-03 HR HRP20182026TT patent/HRP20182026T1/hr unknown
- 2018-12-10 CY CY181101315T patent/CY1121055T1/el unknown
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