公开(公告)号：EP4257134A2

公开(公告)日：2023-10-11

申请号：EP23175990.3

申请日：2016-06-23

申请人： Immunomedics, Inc.

发明人： GOLDENBERG, David M. ,  CARDILLO, Thomas, M.

IPC分类号： A61K31/52

摘要： The present invention is related to an immunoconjugate that binds to CEACAM5 for use in a method of treating CEACAM5 expressing cancer, wherein the method comprises:
a) administering to a human subject with the cancer the immunoconjugate; and
b) administering to the subject at least one therapeutic agent selected from the group consisting of a PARP inhibitor and a microtubule inhibitor
wherein the immunoconjugate comprises an anti- CEACAM5 antibody conjugated to SN-38.

公开(公告)号：EP4121564A1

公开(公告)日：2023-01-25

申请号：EP21719335.8

申请日：2021-03-19

申请人： Immunomedics, Inc.

发明人： FALTAS, Bishoy M. ,  TAGAWA, Scott T. ,  ELEMENTO, Olivier ,  VLACHOSTERGIOS, Panagiotis J. ,  SPERBER, Thorsten RJ ,  CARDILLO, Thomas M. ,  GOSWAMI, Trishna

IPC分类号： C12Q1/6886 ,  A61K31/137 ,  A61K31/198 ,  A61K31/255

公开(公告)号：EP4035689A1

公开(公告)日：2022-08-03

申请号：EP22156351.3

申请日：2013-07-23

申请人： Immunomedics Inc.

发明人： GOVINDAN, Serengulam V. ,  GOLDENBERG, David M.

IPC分类号： A61K51/00 ,  A61M36/14 ,  A61K39/00 ,  A61P35/00

摘要： The present invention relates to therapeutic immunoconjugates comprising SN-38 attached to an antibody or antigen-binding antibody fragment. The antibody may bind to EGP-1 (TROP-2), CEACAM5, CEACAM6, CD74, CD19, CD20, CD22, CSAp, HLA-DR, AFP or MUC5ac and the immunoconjugate may be administered at a dosage of between 4 mg/kg and 24 mg/kg, preferably 4, 6, 8, 9, 10, 12, 16 or 18 mg/kg. When administered at specified dosages and schedules, the immunoconjugate can reduce solid tumors in size, reduce or eliminate metastases and is effective to treat cancers resistant to standard therapies, such as radiation therapy, chemotherapy or immunotherapy.

公开(公告)号：EP3939617A1

公开(公告)日：2022-01-19

申请号：EP21189065.2

申请日：2009-12-02

申请人： Immunomedics, Inc.

发明人： GOVINDAN, Serengulam V. ,  MOON, Sung-Ju ,  GOLDENBERG, David M.

IPC分类号： A61K47/68 ,  A61P35/00 ,  A61P31/18 ,  A61P37/02

摘要： The present invention relates to a process for preparing a CL2A-SN-38 compound, comprising: (a) derivatizing an SN-38 drug with a first linker, wherein the first linker contains a reactive moiety that is capable of combining with a second linker, a PEG moiety comprising 8 monomeric subunits, a lysine amino acid spacer between the drug and the first linker, and a carbonate intracellularly-cleavable moiety, which is cleavable by intracellular peptidases or cleavable by the low pH environment of endosomal and lysosomal vesicles; (b) providing a second linker, which contains a targeting-moiety-coupling group, which is a maleimide group, and further contains a reactive group capable of reacting with the drug-first linker conjugate; and (c) reacting the second linker with the drug-first linker conjugate by a copper (+1) ion-catalyzed acetylene-azide cycloaddition reaction, to produce a compound having a structure represented by:

公开(公告)号：EP3160504B1

公开(公告)日：2020-09-16

申请号：EP15812106.1

申请日：2015-06-23

申请人： Immunomedics, Inc.

发明人： KUMAR, Santhosh V. R. ,  ANDERS, Hans-Joachim

IPC分类号： A61K38/19 ,  A61P13/12 ,  A61K38/20 ,  A61K31/727 ,  A61K38/21 ,  A61K45/06 ,  C07K16/18 ,  A61K38/36 ,  A61K39/00 ,  A61K38/48

公开(公告)号：EP3110445A4

公开(公告)日：2017-09-27

申请号：EP15755115

申请日：2015-01-22

申请人： IMMUNOMEDICS INC

发明人： CHANG CHIEN-HSING ,  GOLDENBERG DAVID M

IPC分类号： A61K39/395 ,  A61K39/00 ,  A61K45/06 ,  A61K47/68 ,  A61K51/10 ,  A61P35/00 ,  C07K16/28

CPC分类号： C07K16/2803 ,  A61K39/3955 ,  A61K39/39558 ,  A61K45/06 ,  A61K47/48384 ,  A61K47/48407 ,  A61K47/48561 ,  A61K47/4863 ,  A61K47/6803 ,  A61K47/6809 ,  A61K47/6867 ,  A61K51/1027 ,  A61K51/1069 ,  A61K2039/505 ,  A61K2039/507 ,  C07K16/2851 ,  C07K2317/24 ,  C07K2317/31 ,  C07K2317/54 ,  C07K2317/56 ,  C07K2317/565 ,  C07K2317/567 ,  C07K2317/569 ,  C07K2317/622 ,  C07K2317/73 ,  C07K2317/92

摘要： Disclosed are humanized RFB4 antibodies or antigen-binding fragments thereof. therapy of B-cell associated diseases, such as B-cell malignancies, autoimmune disease and immune dysfunction disease. Preferably, hRFB4 comprises the light and heavy chain RFB4 CDR sequences with human antibody FR and constant region sequences, along with heavy chain framework region (FR) amino acid residues Q1, F27, V48, A49, F68, R98, T117 and light chain residues L4, S22, K39, G100, V104, and K107. More preferably, the heavy and light chain variable region sequences of hRFB4 comprise SEQ ID NO:7 and SEQ ID NO:8, respectively. In certain embodiments, trogocytosis (antigen shaving) induced by hRFB4 plays a significant role in determining antibody efficacy and disease responsiveness for treatment of B-cell diseases, such as hematopoietic cancers, immune system dysfunction and/or autoimmune disease.

摘要翻译： 公开了人源化RFB4抗体或其抗原结合片段。 B细胞相关疾病的治疗，例如B细胞恶性肿瘤，自身免疫疾病和免疫功能障碍疾病。 优选地，hRFB4包含具有人抗体FR和恒定区序列的轻链和重链RFB4CDR序列以及重链构架区（FR）氨基酸残基Q1，F27，V48，A49，F68，R98，T117和轻链残基 L4，S22，K39，G100，V104和K107。 更优选地，hRFB4的重链和轻链可变区序列分别包含SEQ ID NO：7和SEQ ID NO：8。 在某些实施方案中，由hRFB4诱导的trogocytosis（抗原剃须）在确定用于治疗B细胞疾病（例如造血系统癌症，免疫系统功能障碍和/或自身免疫性疾病）的抗体功效和疾病反应性中起重要作用。

公开(公告)号：EP1543839B1

公开(公告)日：2017-09-20

申请号：EP05075555.2

申请日：2000-06-09

申请人： Immunomedics, Inc.

发明人： Goldenberg, David M. ,  Hansen, Hans J.

IPC分类号： A61K39/395 ,  C07K16/28 ,  C07K19/00 ,  A61P37/06

CPC分类号： C07K16/28 ,  A61K47/6813 ,  A61K47/6849 ,  A61K2039/505 ,  C07K16/2803 ,  C07K16/2896 ,  C07K2317/24

公开(公告)号：EP2301570B8

公开(公告)日：2017-01-25

申请号：EP10012296.9

申请日：2003-12-31

申请人： Immunomedics, Inc.

发明人： Goldenberg, David M. ,  Hansen, Hans

IPC分类号： A61K51/10 ,  C07K16/28

CPC分类号： C07K16/2896 ,  A61K51/1018 ,  A61K51/1045 ,  A61K51/109 ,  A61K51/1093 ,  C07K16/2812 ,  C07K16/2815 ,  C07K16/2821 ,  C07K16/2827 ,  C07K16/2845 ,  C07K16/2851 ,  C07K16/2878 ,  C07K16/2887 ,  C07K16/2893

公开(公告)号：EP2651411A4

公开(公告)日：2016-07-27

申请号：EP11847956

申请日：2011-12-12

申请人： IMMUNOMEDICS INC

发明人： D SOUZA CHRISTOPHER A ,  MCBRIDE WILLIAM J ,  GOLDENBERG DAVID M

IPC分类号： A61K49/10 ,  A61K51/04

CPC分类号： A61K51/088 ,  A61K47/6897 ,  A61K49/106 ,  A61K49/14 ,  A61K51/0459 ,  A61K51/0482 ,  A61K51/082 ,  A61K51/083 ,  B82Y5/00

摘要： The present application discloses compositions and methods of synthesis and use of 18F or 19F-labeled molecules of use in PET, SPECT and/or MR imaging. Preferably, the 18F or 19F is conjugated to a targeting molecule by formation of a complex with a group IIIA metal and binding of the complex to a bifunctional chelating agent, which may be directly or indirectly attached to the targeting molecule. In other embodiments, the 18F or 19F labeled moiety may comprise a targetable construct used in combination with a bispecific antibody to target a disease-associated antigen. The disclosed methods and compositions allow the simple and reproducible labeling of molecules at very high efficiency and specific activity in 30 minutes or less. In preferred embodiments, the labeled molecule may be used for imaging in a subject without purification after labeling.

公开(公告)号：EP2962699A3

公开(公告)日：2016-04-06

申请号：EP15002212.7

申请日：2004-12-01

申请人： Immunomedics Inc.

发明人： Griffiths, Gary L. ,  Govindan, Serengulam

IPC分类号： A61K51/08

CPC分类号： A61K51/1027 ,  A61K51/0482 ,  A61K51/1045

摘要： The present invention is related to a method of preparing a conjugate comprising:
(a) reacting a chelating agent and a protein to form the conjugate; and
(b) reacting the conjugate with a quenching agent.

摘要翻译： 本发明涉及一种制备轭合物的方法，包括：（a）使螯合剂和蛋白质反应以形成缀合物; 和（b）使该缀合物与淬灭剂反应。