MA43354A - Conjugués médicamenteux à pont disulfure encombré - Google Patents

Conjugués médicamenteux à pont disulfure encombré

Info

Publication number
MA43354A
MA43354A MA43354A MA43354A MA43354A MA 43354 A MA43354 A MA 43354A MA 43354 A MA43354 A MA 43354A MA 43354 A MA43354 A MA 43354A MA 43354 A MA43354 A MA 43354A
Authority
MA
Morocco
Prior art keywords
drug conjugates
disulphide
cloudy
linker
disulfide
Prior art date
Application number
MA43354A
Other languages
English (en)
Inventor
Jinhua Chen
Peter DRAGOVICH
Zhonghua Pei
Thomas Pillow
Jack Sadowsky
John Wai
Original Assignee
Genentech Inc
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.)
Publication date
Publication of MA43354A publication Critical patent/MA43354A/fr

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    • A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/05—Dipeptides
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    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5365—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines ortho- or peri-condensed with heterocyclic ring systems
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    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
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    • C07D233/66—Heterocyclic 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 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
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    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/24—Benzimidazoles; Hydrogenated benzimidazoles 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 in position 2
    • C07D235/28—Sulfur atoms
    • C—CHEMISTRY; METALLURGY
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    • C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
    • C07D249/10—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles 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
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    • C07D263/54—Benzoxazoles; Hydrogenated benzoxazoles
    • C07D263/58—Benzoxazoles; Hydrogenated benzoxazoles 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 in position 2
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    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
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Abstract

L'invention concerne généralement des conjugués de médicament disulfure dans lesquels un lieur comprenant un atome de carbone soufré substitué par au moins un hydrocarbyle ou hydrocarbyle substitué est conjugué par une liaison disulfure à un atome de soufre de cystéine d'un support de ciblage et dans lequel le lieur est en outre conjugué à un fragment de médicament. L 'invention concerne en outre des conjugués activés de médicament lieur pouvant être conjugués à un porteur de ciblage par une liaison disulfure. L'invention concerne en outre des procédés de préparation de conjugués de médicament à base de disulfure encombré.
MA43354A 2015-10-16 Conjugués médicamenteux à pont disulfure encombré MA43354A (fr)

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WO (1) WO2017064675A1 (fr)

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WO2017064675A1 (fr) 2017-04-20
EP3362100A1 (fr) 2018-08-22
JP2018537416A (ja) 2018-12-20
US20170112891A1 (en) 2017-04-27
CN108472384A (zh) 2018-08-31
CN108472384B (zh) 2021-09-24
US10729738B2 (en) 2020-08-04
EP3362100B1 (fr) 2022-06-22

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