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公开(公告)号：US20110256157A1
公开(公告)日：2011-10-20
申请号：US13087575
申请日：2011-04-15
申请人： Philip Wilson Howard , Luke Masterson , Arnaud Tiberghien , John A. Flygare , Janet L. Gunzner , Paul Polakis , Andrew Polson , Helga E. Raab , Susan D. Spencer
发明人： Philip Wilson Howard , Luke Masterson , Arnaud Tiberghien , John A. Flygare , Janet L. Gunzner , Paul Polakis , Andrew Polson , Helga E. Raab , Susan D. Spencer
IPC分类号： A61K39/395 , B65D85/84 , C07K5/062 , C07K17/02 , C07D487/04
CPC分类号： C07D487/04 , A61K47/6849 , A61K47/6855 , A61K47/6869 , C07D519/00
摘要： Conjugates and compounds for making conjugates which are PBD molecules linked via the N10 position are disclosed, along with the use of the conjugates for treating proliferative diseases, including cancer.
摘要翻译： 公开了用于制备作为通过N10位置连接的PBD分子的缀合物的缀合物和化合物，以及缀合物用于治疗包括癌症在内的增殖性疾病的用途。
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公开(公告)号：US20110137017A1
公开(公告)日：2011-06-09
申请号：US12971197
申请日：2010-12-17
CPC分类号： A61K47/6803 , A01K2267/0331 , A61K45/06 , A61K47/6817 , A61K47/6851 , A61K47/6889 , C07K16/00 , C07K16/32 , C07K2317/21 , C07K2317/51 , C07K2317/52 , C07K2317/55 , C07K2317/624
摘要： Antibodies are engineered by replacing one or more amino acids of a parent antibody with non cross-linked, highly reactive cysteine amino acids. Antibody fragments may also be engineered with one or more cysteine amino acids to form cysteine engineered antibody fragments (ThioFab). Methods of design, preparation, screening, and selection of the cysteine engineered antibodies are provided. Cysteine engineered antibodies (Ab), optionally with an albumin-binding peptide (ABP) sequence, are conjugated with one or more drug moieties (D) through a linker (L) to form cysteine engineered antibody-drug conjugates having Formula I: Ab-(L-D)p I where p is 1 to 4. Diagnostic and therapeutic uses for cysteine engineered antibody drug compounds and compositions are disclosed.
摘要翻译： 通过用非交联的高反应性半胱氨酸氨基酸替代亲本抗体的一个或多个氨基酸来设计抗体。 抗体片段也可以用一个或多个半胱氨酸氨基酸进行工程化以形成半胱氨酸改造的抗体片段（ThioFab）。 提供了设计，制备，筛选和选择半胱氨酸改造的抗体的方法。 任选与白蛋白结合肽（ABP）序列的半胱氨酸改造的抗体（Ab）通过接头（L）与一个或多个药物部分（D）缀合，形成具有式I：Ab- （LD）p I，其中p为1至4.披露了半胱氨酸改造的抗体药物化合物和组合物的诊断和治疗用途。
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公开(公告)号：US20090175865A1
公开(公告)日：2009-07-09
申请号：US12399241
申请日：2009-03-06
IPC分类号： A61K39/395 , C07K16/46 , A61P35/00
CPC分类号： A61K47/6803 , A01K2267/0331 , A61K45/06 , A61K47/6817 , A61K47/6851 , A61K47/6889 , C07K16/00 , C07K16/32 , C07K2317/21 , C07K2317/51 , C07K2317/52 , C07K2317/55 , C07K2317/624
摘要： Antibodies are engineered by replacing one or more amino acids of a parent antibody with non cross-linked, highly reactive cysteine amino acids. Antibody fragments may also be engineered with one or more cysteine amino acids to form cysteine engineered antibody fragments (ThioFab). Methods of design, preparation, screening, and selection of the cysteine engineered antibodies are provided. Cysteine engineered antibodies (Ab), optionally with an albumin-binding peptide (ABP) sequence, are conjugated with one or more drug moieties (D) through a linker (L) to form cysteine engineered antibody-drug conjugates having Formula I: Ab-(L-D)p I where p is 1 to 4. Diagnostic and therapeutic uses for cysteine engineered antibody drug compounds and compositions are disclosed.
摘要翻译： 通过用非交联的高反应性半胱氨酸氨基酸替代亲本抗体的一个或多个氨基酸来设计抗体。 抗体片段也可以用一个或多个半胱氨酸氨基酸进行工程化以形成半胱氨酸改造的抗体片段（ThioFab）。 提供了设计，制备，筛选和选择半胱氨酸改造的抗体的方法。 任选与白蛋白结合肽（ABP）序列的半胱氨酸改造的抗体（Ab）通过接头（L）与一个或多个药物部分（D）缀合以形成具有式I的半胱氨酸改造的抗体 - 药物共轭物： in-line-formula description =“In-line Formulas”end =“lead”？> Ab-（LD）p I <？in-line-formula description =“In-line Formulas”end =“tail”？> where p是1至4.公开了半胱氨酸改造的抗体药物化合物和组合物的诊断和治疗用途。
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公开(公告)号：US07521541B2
公开(公告)日：2009-04-21
申请号：US11233258
申请日：2005-09-22
IPC分类号： C07K16/00
CPC分类号： A61K47/6803 , A01K2267/0331 , A61K45/06 , A61K47/6817 , A61K47/6851 , A61K47/6889 , C07K16/00 , C07K16/32 , C07K2317/21 , C07K2317/51 , C07K2317/52 , C07K2317/55 , C07K2317/624
摘要： Antibodies are engineered by replacing one or more amino acids of a parent antibody with non cross-linked, highly reactive cysteine amino acids. Antibody fragments may also be engineered with one or more cysteine amino acids to form cysteine engineered antibody fragments (ThioFab). Methods of design, preparation, screening, and selection of the cysteine engineered antibodies are provided. Cysteine engineered antibodies (Ab), optionally with an albumin-binding peptide (ABP) sequence, are conjugated with one or more drug moieties (D) through a linker (L) to form cysteine engineered antibody-drug conjugates having Formula I: Ab-(L-D)p I where p is 1 to 4. Diagnostic and therapeutic uses for cysteine engineered antibody drug compounds and compositions are disclosed.
摘要翻译： 通过用非交联的高反应性半胱氨酸氨基酸替代亲本抗体的一个或多个氨基酸来设计抗体。 抗体片段也可以用一个或多个半胱氨酸氨基酸进行工程化以形成半胱氨酸改造的抗体片段（ThioFab）。 提供了设计，制备，筛选和选择半胱氨酸改造的抗体的方法。 任选与白蛋白结合肽（ABP）序列的半胱氨酸改造的抗体（Ab）通过接头（L）与一个或多个药物部分（D）缀合以形成具有式I的半胱氨酸改造的抗体 - 药物共轭物： in-line-formula description =“In-line Formulas”end =“lead”？> Ab-（LD）p I <？in-line-formula description =“In-line Formulas”end =“tail”？> where p是1至4.公开了半胱氨酸改造的抗体药物化合物和组合物的诊断和治疗用途。
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公开(公告)号：US07855275B2
公开(公告)日：2010-12-21
申请号：US12399241
申请日：2009-03-06
IPC分类号： C07K16/00
CPC分类号： A61K47/6803 , A01K2267/0331 , A61K45/06 , A61K47/6817 , A61K47/6851 , A61K47/6889 , C07K16/00 , C07K16/32 , C07K2317/21 , C07K2317/51 , C07K2317/52 , C07K2317/55 , C07K2317/624
摘要： Antibodies are engineered by replacing one or more amino acids of a parent antibody with non cross-linked, highly reactive cysteine amino acids. Antibody fragments may also be engineered with one or more cysteine amino acids to form cysteine engineered antibody fragments (ThioFab). Methods of design, preparation, screening, and selection of the cysteine engineered antibodies are provided. Cysteine engineered antibodies (Ab), optionally with an albumin-binding peptide (ABP) sequence, are conjugated with one or more drug moieties (D) through a linker (L) to form cysteine engineered antibody-drug conjugates having Formula I: Ab-(L-D)p I where p is 1 to 4. Diagnostic and therapeutic uses for cysteine engineered antibody drug compounds and compositions are disclosed.
摘要翻译： 通过用非交联的高反应性半胱氨酸氨基酸替代亲本抗体的一个或多个氨基酸来设计抗体。 抗体片段也可以用一个或多个半胱氨酸氨基酸进行工程化以形成半胱氨酸改造的抗体片段（ThioFab）。 提供了设计，制备，筛选和选择半胱氨酸改造的抗体的方法。 任选与白蛋白结合肽（ABP）序列的半胱氨酸改造的抗体（Ab）通过接头（L）与一个或多个药物部分（D）缀合，形成具有式I：Ab- （LD）p I，其中p为1至4.披露了半胱氨酸改造的抗体药物化合物和组合物的诊断和治疗用途。
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公开(公告)号：US20130028917A1
公开(公告)日：2013-01-31
申请号：US13641198
申请日：2011-04-15
申请人： Philip Wilson Howard , Luke Masterson , Arnaud Tiberghien , John A. Flygare , Janet L. Gunzner , Paul Polakis , Andrew Polson , Helga E. Raab , Susan D. Spencer
发明人： Philip Wilson Howard , Luke Masterson , Arnaud Tiberghien , John A. Flygare , Janet L. Gunzner , Paul Polakis , Andrew Polson , Helga E. Raab , Susan D. Spencer
IPC分类号： A61K39/395 , A61P35/00 , C07D519/00 , C07K16/00 , C07K16/30
CPC分类号： C07D487/04 , A61K47/6849 , A61K47/6855 , A61K47/6869 , C07D519/00
摘要： Conjugates and compounds for making conjugates which are PBD molecules linked via the N10 position are disclosed, along with the use of the conjugates for treating proliferative diseases, including cancer.
摘要翻译： 公开了用于制备作为通过N10位置连接的PBD分子的缀合物的缀合物和化合物，以及缀合物用于治疗包括癌症在内的增殖性疾病的用途。
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公开(公告)号：US20100003766A1
公开(公告)日：2010-01-07
申请号：US12427649
申请日：2009-04-21
IPC分类号： G01N33/566
CPC分类号： A61K47/6803 , A01K2267/0331 , A61K45/06 , A61K47/6817 , A61K47/6851 , A61K47/6889 , C07K16/00 , C07K16/32 , C07K2317/21 , C07K2317/51 , C07K2317/52 , C07K2317/55 , C07K2317/624
摘要： Antibodies are engineered by replacing one or more amino acids of a parent antibody with non cross-linked, highly reactive cysteine amino acids. Antibody fragments may also be engineered with one or more cysteine amino acids to form cysteine engineered antibody fragments (ThioFab). Methods of design, preparation, screening, and selection of the cysteine engineered antibodies are provided. Cysteine engineered antibodies (Ab), optionally with an albumin-binding peptide (ABP) sequence, are conjugated with one or more drug moieties (D) through a linker (L) to form cysteine engineered antibody-drug conjugates having Formula I: Ab-(L-D)p I where p is 1 to 4. Diagnostic and therapeutic uses for cysteine engineered antibody drug compounds and compositions are disclosed.
摘要翻译： 通过用非交联的高反应性半胱氨酸氨基酸替代亲本抗体的一个或多个氨基酸来设计抗体。 抗体片段也可以用一个或多个半胱氨酸氨基酸进行工程化以形成半胱氨酸改造的抗体片段（ThioFab）。 提供了设计，制备，筛选和选择半胱氨酸改造的抗体的方法。 任选与白蛋白结合肽（ABP）序列的半胱氨酸改造的抗体（Ab）通过接头（L）与一个或多个药物部分（D）缀合，形成具有式I：Ab- （LD）p I，其中p为1至4.披露了半胱氨酸改造的抗体药物化合物和组合物的诊断和治疗用途。
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