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1. 发明申请

US20200024366A1 ANTIBODIES WITH pH DEPENDENT ANTIGEN BINDING 审中-公开
公开(公告)号：US20200024366A1
公开(公告)日：2020-01-23
申请号：US16296852
申请日：2019-03-08
申请人： Pfizer Inc. , RINAT NEUROSCIENCE CORP.
发明人： Jaume PONS , Jeffrey Raymond CHABOT , Javier Fernando CHAPARRO RIGGERS , Bruce Charles GOMES , Hong LIANG , KapiI MAYAWALA , Jerome Thomas METTETAL, II , Arvind RAJPAL , David Louis SHELTON
IPC分类号： C07K16/42 , C07K16/40 , C07K16/28
摘要： The present invention relates to antibodies with pH dependent binding to its antigen such that the affinity for antigen binding at physiological pH (i.e., pH 7.4) is greater than at endosomal pH (i.e., pH 6.0 or 5.5). In other words, the KD or koff ratio at pH 5.5/pH 7.4 or at pH 6.0/pH 7.4 is more than, or ranges between, 2, 3, 4, 8, 10, 16, 20, 30, 40, or 100 or more. Such pH dependent antibodies preferentially dissociate from the antigen in the endosome. This can increase antibody half life, as compared to antibodies with equivalent KDs at pH 7.4 but with no pH dependent binding, when the antigen is one that undergoes antigen-mediated clearance (e.g., PCSK9). Antibodies with pH dependent binding can decrease total antigen half life when the antigen undergoes reduced clearance when bound to antibody (e.g., IL6). Antibodies with pH dependent binding can also prolong the decrease in antigen which is not antibody-bound. This can be important when antagonizing a target antigen typically present at high levels (e.g., IgE, DKK1, C5 and SOST). In addition, such antibodies can increase antigen half life when the antigen is a receptor and the receptor has increased clearance when bound to antibody (e.g., GMCSF receptor).

2. 发明申请

US20160096898A1 PC33718E 审中-公开
公开(公告)号：US20160096898A1
公开(公告)日：2016-04-07
申请号：US14864750
申请日：2015-09-24
申请人： RINAT NEUROSCIENCE CORP. , Pfizer Inc.
发明人： Hong LIANG , Yasmina Noubia ABDICHE , Javier Fernando CHAPARRO RIGGERS , Bruce Charles GOMES , Julie Jia Li HAWKINS , Jaume PONS , Xiayang QIU , Pavel STROP , Yuli WANG
IPC分类号： C07K16/40
CPC分类号： C07K16/40 , A61K39/3955 , A61K45/06 , A61K2039/505 , C07K2299/00 , C07K2317/24 , C07K2317/33 , C07K2317/76 , C07K2317/92
摘要： The present invention provides antagonizing antibodies, antigen-binding portions thereof, and aptamers that bind to proprotein convertase subtilisin kexin type 9 (PCSK9). Also provided are antibodies directed to peptides, in which the antibodies bind to PCSK9. The invention further provides a method of obtaining such antibodies and antibody-encoding nucleic acid. The invention further relates to therapeutic methods for use of these antibodies and antigen-binding portions thereof to reduce LDL-cholesterol levels and/or for the treatment and/or prevention of cardiovascular disease, including treatment of hypercholesterolemia.
摘要翻译：本发明提供了与抗蛋白转化酶枯草杆菌蛋白酶Kexin 9型（PCSK9）结合的拮抗抗体，其抗原结合部分和适体。还提供了针对肽的抗体，其中抗体结合PCSK9。本发明还提供了获得这样的抗体和抗体编码核酸的方法。本发明还涉及使用这些抗体及其抗原结合部分来降低LDL-胆固醇水平和/或用于治疗和/或预防心血管疾病（包括治疗高胆固醇血症）的治疗方法。

3. 发明申请

US20130273069A1 PCSK9 ANTAGONISTS 审中-公开
公开(公告)号：US20130273069A1
公开(公告)日：2013-10-17
申请号：US13857063
申请日：2013-04-04
申请人： Pfizer Inc. , Rinat Neuroscience Corp.
发明人： Hong LIANG , Yasmina Noubia ABDICHE , Javier Fernando CHAPARRO RIGGERS , Bruce Charles GOMES , Julie Jia Li HAWKINS , Jaume PONS , Xiayang QIU , Pavel STROP , Yuli WANG
IPC分类号： C07K16/40 , A61K45/06 , A61K39/395
CPC分类号： C07K16/40 , A61K39/3955 , A61K45/06 , A61K2039/505 , C07K2299/00 , C07K2317/24 , C07K2317/33 , C07K2317/76 , C07K2317/92
摘要： The present invention provides antagonizing antibodies, antigen-binding portions thereof, and aptamers that bind to proprotein convertase subtilisin kexin type 9 (PCSK9). Also provided are antibodies directed to peptides, in which the antibodies bind to PCSK9. The invention further provides a method of obtaining such antibodies and antibody-encoding nucleic acid. The invention further relates to therapeutic methods for use of these antibodies and antigen-binding portions thereof to reduce LDL-cholesterol levels and/or for the treatment and/or prevention of cardiovascular disease, including treatment of hypercholesterolemia.
摘要翻译：本发明提供了与抗蛋白转化酶枯草杆菌蛋白酶Kexin 9型（PCSK9）结合的拮抗抗体，其抗原结合部分和适体。还提供了针对肽的抗体，其中抗体结合PCSK9。本发明还提供了获得这样的抗体和抗体编码核酸的方法。本发明还涉及使用这些抗体及其抗原结合部分来降低LDL-胆固醇水平和/或用于治疗和/或预防心血管疾病（包括治疗高胆固醇血症）的治疗方法。

4. 发明申请

US20150266974A1 ANTIBODIES WITH pH DEPENDENT ANTIGEN BINDING 审中-公开
标题翻译：具有pH依赖性抗原结合的抗体
公开(公告)号：US20150266974A1
公开(公告)日：2015-09-24
申请号：US14677983
申请日：2015-04-03
申请人： RINAT NEUROSCIENCE CORP. , PFIZER INC.
发明人： Jaume PONS , Jeffrey Raymond CHABOT , Javier Fernando CHAPARRO RIGGERS , Bruce Charles GOMES , Hong LIANG , Kapil MAYAWALA , Jerome Thomas METTETAL, II , Arvind RAJPAL , David Louis SHELTON
IPC分类号： C07K16/42 , C07K16/40 , C07K16/28
CPC分类号： C07K16/4291 , C07K16/28 , C07K16/40 , C07K2317/56 , C07K2317/565 , C07K2317/70 , C07K2317/732 , C07K2317/734 , C07K2317/76 , C07K2317/92 , C07K2317/94 , C07K2319/21
摘要： The present invention relates to antibodies with pH dependent binding to its antigen such that the affinity for antigen binding at physiological pH (i.e., pH 7.4) is greater than at endosomal pH (i.e., pH 6.0 or 5.5). In other words, the KD or koff ratio at pH 5.5/pH 7.4 or at pH 6.0/pH 7.4 is more than, or ranges between, 2, 3, 4, 8, 10, 16, 20, 30, 40, or 100 or more. Such pH dependent antibodies preferentially dissociate from the antigen in the endosome. This can increase antibody half life, as compared to antibodies with equivalent KDs at pH 7.4 but with no pH dependent binding, when the antigen is one that undergoes antigen-mediated clearance (e.g., PCSK9). Antibodies with pH dependent binding can decrease total antigen half life when the antigen undergoes reduced clearance when bound to antibody (e.g., IL6). Antibodies with pH dependent binding can also prolong the decrease in antigen which is not antibody-bound. This can be important when antagonizing a target antigen typically present at high levels (e.g., IgE, DKK1, C5 and SOST). In addition, such antibodies can increase antigen half life when the antigen is a receptor and the receptor has increased clearance when bound to antibody (e.g, GMCSF receptor).
摘要翻译：本发明涉及与其抗原具有pH依赖性结合的抗体，使得在生理pH（即pH 7.4）下抗原结合的亲和力大于内体pH（即pH6.0或5.5）时的亲和力。换句话说，pH5.5 / pH7.4或pH6.0 / pH7.4下的KD或koff比大于或等于2,3,4,8,10,16,20,30,40或100 或者更多。这种pH依赖性抗体优先从内体中的抗原解离。与抗原为经过抗原介导的清除（例如，PCSK9）的抗原相比，与具有pH 7.4但具有pH依赖性结合的等效KD的抗体相比，可以增加抗体半衰期。当与抗体（例如IL6）结合时，当抗原经历减少的清除时，具有pH依赖性结合的抗体可降低总抗原半衰期。具有pH依赖性结合的抗体也可以延长不抗体结合的抗原的降低。当拮抗通常以高水平存在的靶抗原（例如IgE，DKK1，C5和SOST）时，这可能是重要的。此外，当抗原是受体时，这种抗体可以增加抗原半衰期，并且当与抗体（例如，GMCSF受体）结合时，该受体具有增加的清除能力。

5. 发明申请

US20130164308A1 STAPHYLOCOCCUS AUREUS SPECIFIC ANTIBODIES AND USES THEREOF 失效
标题翻译：。US US US。。。。。。。。。。。。。。。。。。
公开(公告)号：US20130164308A1
公开(公告)日：2013-06-27
申请号：US13719214
申请日：2012-12-18
申请人： RINAT NEUROSCIENCE CORP.
发明人： Davide Luciano FOLETTI , Javier Fernando CHAPARRO RIGGERS , Jacob Eli Gunn GLANVILLE , Lee Mary Beth SHAUGHNESSY , David Louis SHELTON , Pavel STROP , Wenwu ZHAI
IPC分类号： C07K16/12 , A61K45/06 , A61K39/40
CPC分类号： C07K16/1271 , A61K39/40 , A61K2039/505 , C07K2317/34 , C07K2317/565 , C07K2317/76 , C07K2317/92 , C07K2317/94 , A61K2300/00
摘要： The present invention provides antagonizing antibodies that bind to S. aureus alpha-toxin. The invention further provides a method of obtaining such antibodies and antibody encoding nucleic acids. The invention further relates to therapeutic methods for use of these antibodies for the treatment and/or prevention of staphylococcal disease, including, for example, pneumonia, bacteremia, sepsis, eye infection, and abscess.
摘要翻译：本发明提供了结合金黄色葡萄球菌α-毒素的拮抗性抗体。本发明还提供了获得这样的抗体和编码抗体的核酸的方法。本发明进一步涉及使用这些抗体治疗和/或预防葡萄球菌疾病，包括例如肺炎，菌血症，败血症，眼睛感染和脓肿的治疗方法。

6. 发明申请

US20200031947A1 ANTI-GITR ANTIBODIES AND METHODS OF USE THEREOF 审中-公开
公开(公告)号：US20200031947A1
公开(公告)日：2020-01-30
申请号：US16488040
申请日：2018-02-21
申请人： Rinat Neuroscience Corp.
发明人： Samantha Lisa BUCKTROUT , Bevin Marie Brady SMITH , Edward Derrick PASCUA , Javier Fernando CHAPARRO RIGGERS
IPC分类号： C07K16/28 , A61P35/00
摘要： The present invention provides antibodies that bind Glucocorticoid Induced Tumor necrosis factor Receptor family related protein (GITR) and methods of using same. The anti-GITR antibodies can be used therapeutically alone or in combination with other therapeutics to treat cancer and other diseases.

7. 发明申请

US20140335091A1 ANTI-GLUCAGON RECEPTOR ANTIBODIES AND METHODS OF USE THEREOF 审中-公开
标题翻译：抗GLUCAGON受体抗体及其使用方法
公开(公告)号：US20140335091A1
公开(公告)日：2014-11-13
申请号：US14268933
申请日：2014-05-02
申请人： RINAT NEUROSCIENCE CORP.
发明人： Alison Jane FORGIE , Javier Fernando CHAPARRO RIGGERS , Edward Roland LAVALLIE , Chia-Yang LIN , Lidia MOSYAK , Andrea ROSSI , Thomas John VAN BLARCOM
IPC分类号： A61K39/395 , A61K31/155 , A61K45/06 , C07K16/28
CPC分类号： C07K16/2869 , A61K31/155 , A61K31/4353 , A61K39/39541 , A61K39/3955 , A61K45/06 , A61K2039/505 , C07K2317/33 , C07K2317/55 , C07K2317/76 , C07K2317/92 , C07K2317/94 , A61K2300/00
摘要： The present invention provides antagonizing antibodies that bind to glucagon receptor and methods of using same. The anti-glucagon receptor antibodies can be used therapeutically to lower glucose levels in blood, and can be in the prevention and/or treatment of glucose-related disorders, including diabetes, hyperglycemia, hyperinsulinemia, impaired fasting glucose, impaired glucose tolerance, dyslipidemia, or metabolic syndrome.
摘要翻译：本发明提供了结合胰高血糖素受体的拮抗性抗体及其使用方法。抗胰高血糖素受体抗体可用于治疗降低血液中的葡萄糖水平，并可用于预防和/或治疗葡萄糖相关疾病，包括糖尿病，高血糖症，高胰岛素血症，空腹血糖受损，葡萄糖耐量异常，血脂异常，或代谢综合征。

8. 发明申请

US20180171018A1 THERAPEUTIC ANTIBODIES AND THEIR USES 审中-公开
公开(公告)号：US20180171018A1
公开(公告)日：2018-06-21
申请号：US15878344
申请日：2018-01-23
申请人： PFIZER INC.
发明人： Tracy Chia-Chien KUO , Javier Fernando CHAPARRO RIGGERS , Wei CHEN , Amy Shaw-Ru CHEN , Edward Derrick PASCUA , Thomas John VAN BLARCOM , Leila Marie BOUSTANY , Weihsien HO , Yik Andy YEUNG , Pavel STROP , Arvind RAJPAL
IPC分类号： C07K16/28 , A61K39/395 , A61K47/68 , A61K31/454 , A61K31/69 , A61K31/704 , A61K39/00
CPC分类号： C07K16/2878 , A61K31/454 , A61K31/69 , A61K31/704 , A61K39/3955 , A61K39/39558 , A61K47/6801 , A61K47/6849 , A61K2039/505 , C07K16/2803 , C07K16/2809 , C07K2317/21 , C07K2317/31 , C07K2317/56 , C07K2317/565 , C07K2317/73 , C07K2317/732 , C07K2317/92 , A61K2300/00
摘要： The present invention relates to antibodies, e.g., full length antibodies or antigen binding fragments thereof, that specifically bind to BCMA (B-Cell Maturation Antigen) and/or CD3 (Cluster of Differentiation 3). The invention also relates to antibody conjugates (e.g., antibody-drug-conjugates) comprising the BCMA antibodies, compositions comprising the BCMA antibodies, and methods of using the BCMA antibodies and their conjugates for treating conditions associated with cells expressing BCMA (e.g., cancer or autoimmune disease). The invention further relates to heteromultimeric antibodies that specifically bind to CD3 and a tumor cell antigen, (e.g., bispecific antibodies that specifically bind to CD3 and BCMA). Compositions comprising such heteromultimeric antibodies, methods for producing and purifying such heterodimeric antibodies, and their use in diagnostics and therapeutics are also provided.

9. 发明申请

US20210054087A1 THERAPEUTIC ANTIBODIES AND THEIR USES 有权
公开(公告)号：US20210054087A1
公开(公告)日：2021-02-25
申请号：US17005073
申请日：2020-08-27
申请人： PFIZER INC.
发明人： Tracy Chia-Chien KUO , Javier Fernando CHAPARRO RIGGERS , Wei CHEN , Amy Shaw-Ru CHEN , Edward Derrick PASCUA , Thomas John VAN BLARCOM , Leila Marie BOUSTANY , Weihsien HO , Yik Andy YEUNG , Pavel STROP , Arvind RAJPAL
IPC分类号： C07K16/28 , A61K39/395 , A61K31/454 , A61K31/704 , A61K31/69 , A61K47/68
摘要： The present invention relates to antibodies, e.g., full length antibodies or antigen binding fragments thereof, that specifically bind to BCMA (B-Cell Maturation Antigen) and/or CD3 (Cluster of Differentiation 3). The invention also relates to antibody conjugates (e.g., antibody-drug-conjugates) comprising the BCMA antibodies, compositions comprising the BCMA antibodies, and methods of using the BCMA antibodies and their conjugates for treating conditions associated with cells expressing BCMA (e.g., cancer or autoimmune disease). The invention further relates to heteromultimeric antibodies that specifically bind to CD3 and a tumor cell antigen, (e.g., bispecific antibodies that specifically bind to CD3 and BCMA). Compositions comprising such heteromultimeric antibodies, methods for producing and purifying such heterodimeric antibodies, and their use in diagnostics and therapeutics are also provided.

10. 发明申请

US20160297885A1 THERAPEUTIC ANTIBODIES AND THEIR USES 审中-公开
标题翻译：治疗性抗体及其用途
公开(公告)号：US20160297885A1
公开(公告)日：2016-10-13
申请号：US15085644
申请日：2016-03-30
申请人： PFIZER INC.
发明人： Tracy Chia-Chien KUO , Javier Fernando CHAPARRO RIGGERS , Wei CHEN , Amy Shaw-Ru CHEN , Edward Derrick PASCUA , Thomas John VAN BLARCOM , Leila Marie BOUSTANY , Weihsien HO , Yik Andy YEUNG , Pavel STROP , Arvind RAJPAL
IPC分类号： C07K16/28 , A61K31/704 , A61K38/07 , A61K38/05 , A61K39/395 , A61K31/454
CPC分类号： C07K16/2878 , A61K31/454 , A61K31/69 , A61K31/704 , A61K39/3955 , A61K39/39558 , A61K47/6801 , A61K47/6849 , A61K2039/505 , C07K16/2803 , C07K16/2809 , C07K2317/21 , C07K2317/31 , C07K2317/56 , C07K2317/565 , C07K2317/73 , C07K2317/732 , C07K2317/92 , A61K2300/00
摘要： The present invention relates to antibodies, e.g., full length antibodies or antigen binding fragments thereof, that specifically bind to BCMA (B-Cell Maturation Antigen) and/or CD3 (Cluster of Differentiation 3). The invention also relates to antibody conjugates (e.g., antibody-drug-conjugates) comprising the BCMA antibodies, compositions comprising the BCMA antibodies, and methods of using the BCMA antibodies and their conjugates for treating conditions associated with cells expressing BCMA (e.g., cancer or autoimmune disease). The invention further relates to heteromultimeric antibodies that specifically bind to CD3 and a tumor cell antigen, (e.g., bispecific antibodies that specifically bind to CD3 and BCMA). Compositions comprising such heteromultimeric antibodies, methods for producing and purifying such heterodimeric antibodies, and their use in diagnostics and therapeutics are also provided.
摘要翻译：本发明涉及特异性结合BCMA（B细胞成熟抗原）和/或CD3（分化群3）的抗体，例如全长抗体或其抗原结合片段。本发明还涉及包含BCMA抗体的抗体缀合物（例如，抗体 - 药物偶联物），包含BCMA抗体的组合物，以及使用BCMA抗体及其缀合物治疗与表达BCMA的细胞相关的病症的方法（例如癌症或自身免疫性疾病）。本发明还涉及特异性结合CD3和肿瘤细胞抗原的异源多聚体抗体（例如，特异性结合CD3和BCMA的双特异性抗体）。还提供了包含这种异源多聚体抗体的组合物，用于产生和纯化此类异二聚体抗体的方法及其在诊断和治疗中的应用。

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