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公开(公告)号：US20180134656A1
公开(公告)日：2018-05-17
申请号：US15870014
申请日：2018-01-12
申请人： PFIZER INC.
发明人： Robert Wayne Dugger , Leo Joseph Letendre , Vimalkumar Babubhai Patel , Amarnauth Shastrie Prashad , Chunchun Zhang
IPC分类号： C07C323/48 , C07C323/60 , C07C319/20 , C07D207/46 , C07C319/28 , C07C319/06 , C07H1/06 , C07H15/26
摘要： The present invention relates to intermediates of Formula I and to methods of synthesizing and purifying calicheamicin derivatives.
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公开(公告)号：US20190030183A1
公开(公告)日：2019-01-31
申请号：US15748268
申请日：2016-08-09
申请人： PFIZER INC.
发明人： Xiaotian Zhong , Amarnauth Shastrie Prashad , Ronald William Kriz , Tao He , Will Somers , Wenge Wang , Leo Joseph Letendre
摘要： An antibody production process in mammalian cells in which engineered unpaired cysteine residues are post-translationally modified and capped with particular chemical entities, which capped antibodies are well suited to further site-specific conjugation steps to form antibody-drug conjugates (ADCs) or protein drug conjugates; ADCs produced using these capped antibodies including in particular ADCs formed by the selective reduction of the capped antibodies' cysteine residues, and ADCs formed using chemical handles such as aldehyde/azide/alkyne biorthogonal groups, which permit additional drug conjugation chemistry; and uncapped antibodies produced by cells in low cysteine, cysteine and glutathione media, and ADCs produced via direct conjugation to these uncapped antibodies.
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3.发明申请公开(公告)号：US20160251389A1
公开(公告)日：2016-09-01
申请号：US15030563
申请日：2014-10-28
申请人： Pfizer Inc.
发明人： Robert Wayne Dugger , Leo Joseph Letendre , Vimalkumar Babubhai Patel , Amarnauth Shastrie Prashad , Chunchun Zhang
IPC分类号： C07H15/26 , C07C319/06 , C07C319/20 , A61K47/48 , C07H1/06 , C07C323/60 , C07D207/46
CPC分类号： C07C323/48 , A61K47/6809 , C07C319/06 , C07C319/20 , C07C319/28 , C07C323/60 , C07D207/46 , C07H1/06 , C07H15/26
摘要： The present invention relates to intermediates of Formula I and to methods of synthesizing and purifying calicheamicin derivatives.
摘要翻译： 本发明涉及式I的中间体以及合成和提纯加利车霉素衍生物的方法。
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公开(公告)号：US11980669B2
公开(公告)日：2024-05-14
申请号：US16807375
申请日：2020-03-03
申请人： PFIZER INC.
发明人： Xiaotian Zhong , Amarnauth Shastrie Prashad , Ronald William Kriz , Tao He , Will Somers , Wenge Wang , Leo Joseph Letendre
CPC分类号： A61K47/6889 , A61K38/05 , A61K47/68 , A61K47/6817 , A61K47/6851 , A61K47/6855 , C07K16/00 , C07K16/30 , C07K2317/14 , C07K2317/40 , C07K2317/526 , C07K2317/55 , C07K2317/94
摘要： An antibody production process in mammalian cells in which engineered unpaired cysteine residues are post-translationally modified and capped with particular chemical entities, which capped antibodies are well suited to further site-specific conjugation steps to form antibody-drug conjugates (ADCs) or protein drug conjugates; ADCs produced using these capped antibodies including in particular ADCs formed by the selective reduction of the capped antibodies' cysteine residues, and ADCs formed using chemical handles such as aldehyde/azide/alkyne biorthogonal groups, which permit additional drug conjugation chemistry; and uncapped antibodies produced by cells in low cysteine, cysteine and glutathione media, and ADCs produced via direct conjugation to these uncapped antibodies.
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公开(公告)号：US10508081B2
公开(公告)日：2019-12-17
申请号：US15870014
申请日：2018-01-12
申请人： PFIZER INC.
发明人： Robert Wayne Dugger , Leo Joseph Letendre , Vimalkumar Babubhai Patel , Amarnauth Shastrie Prashad , Chunchun Zhang
IPC分类号： C07C323/48 , C07C319/20 , C07C323/60 , C07C319/28 , A61K47/68 , C07C319/06 , C07D207/46 , C07H1/06 , C07H15/26
摘要： The present invention relates to intermediates of Formula I and to methods of synthesizing and purifying calicheamicin derivatives.
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公开(公告)号：US12121588B2
公开(公告)日：2024-10-22
申请号：US16480792
申请日：2018-02-01
申请人： PFIZER INC.
发明人： Kaushik Dutta , Jose Manuel Gomes , Frank W. Kotch , Vimalkumar B. Patel , Amarnauth Shastrie Prashad , Renee L. Procopio-Melino , Xiaotian Zhong
IPC分类号： A61K47/42 , A61K47/50 , A61K47/64 , A61K47/68 , C07B31/00 , C07B33/00 , C07K1/00 , C07K16/30 , C07K1/107 , C07K1/20
CPC分类号： A61K47/6843 , A61K47/6855 , A61K47/6889 , C07K1/00 , C07K16/3015 , C07K1/1077 , C07K1/20 , C07K2317/14
摘要： Optimizing production of selectively capped, and uncapped, cysteines on antibodies by manipulation of cell growth conditions including the deliberate depletion of cysteine and/or cystine in the cell culture process by way of media components, batch duration, or cell density to achieve efficient production of proteins including antibody-drug-conjugates (ADCs).; conjugating a TNB-capped cysteine-containing protein by reacting it with a reducing agent capable of detaching the TNB-capping moieties from the protein without significantly reducing antibody inter-chain sulfur bonds, and conjugating reduced sulfur bonds on the protein to a payload through a reactive linking moiety.
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公开(公告)号：US20200230256A1
公开(公告)日：2020-07-23
申请号：US16807375
申请日：2020-03-03
申请人： PFIZER INC.
发明人： Xiaotian Zhong , Amarnauth Shastrie Prashad , Ronald William Kriz , Tao He , Will Somers , Wenge Wang , Leo Joseph Letendre
摘要： An antibody production process in mammalian cells in which engineered unpaired cysteine residues are post-translationally modified and capped with particular chemical entities, which capped antibodies are well suited to further site-specific conjugation steps to form antibody-drug conjugates (ADCs) or protein drug conjugates; ADCs produced using these capped antibodies including in particular ADCs formed by the selective reduction of the capped antibodies' cysteine residues, and ADCs formed using chemical handles such as aldehyde/azide/alkyne biorthogonal groups, which permit additional drug conjugation chemistry; and uncapped antibodies produced by cells in low cysteine, cysteine and glutathione media, and ADCs produced via direct conjugation to these uncapped antibodies.
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公开(公告)号：US10653794B2
公开(公告)日：2020-05-19
申请号：US15748268
申请日：2016-08-09
申请人： PFIZER INC.
发明人： Xiaotian Zhong , Amarnauth Shastrie Prashad , Ronald William Kriz , Tao He , Will Somers , Wenge Wang , Leo Joseph Letendre
摘要： An antibody production process in mammalian cells in which engineered unpaired cysteine residues are post-translationally modified and capped with particular chemical entities, which capped antibodies are well suited to further site-specific conjugation steps to form antibody-drug conjugates (ADCs) or protein drug conjugates; ADCs produced using these capped antibodies including in particular ADCs formed by the selective reduction of the capped antibodies' cysteine residues, and ADCs formed using chemical handles such as aldehyde/azide/alkyne biorthogonal groups, which permit additional drug conjugation chemistry; and uncapped antibodies produced by cells in low cysteine, cysteine and glutathione media, and ADCs produced via direct conjugation to these uncapped antibodies.
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公开(公告)号：US09902691B2
公开(公告)日：2018-02-27
申请号：US15030563
申请日：2014-10-28
申请人： Pfizer Inc.
发明人： Robert Wayne Dugger , Leo Joseph Letendre , Vimalkumar Babubhai Patel , Amarnauth Shastrie Prashad , Chunchun Zhang
IPC分类号： C07C323/48 , C07C319/20 , C07C319/28 , C07C319/06 , C07C323/60 , C07D207/46 , C07H1/06 , C07H15/26 , A61K47/68
CPC分类号： C07C323/48 , A61K47/6809 , C07C319/06 , C07C319/20 , C07C319/28 , C07C323/60 , C07D207/46 , C07H1/06 , C07H15/26
摘要： The present invention relates to intermediates of Formula I and to methods of synthesizing and purifying calicheamicin derivatives.
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