公开(公告)号：WO2019129880A1

公开(公告)日：2019-07-04

申请号：PCT/EP2018/097128

申请日：2018-12-28

申请人： INVIVOGEN

发明人： LIOUX, Thierry ,  VERNEJOUL, Fabienne ,  BOULARAN, Cédric ,  TIRABY, Michèle

IPC分类号： A61K47/65 ,  A61K47/68

CPC分类号： A61K47/6807 ,  A61K47/65 ,  A61K47/6889

摘要： The present invention provides a Pro-cyclic dinucleotide (Pro-CDN) comprising a STING agonist cyclic dinucleotide which is coupled to a linker system. The Pro-CDNs of the present invention can be metabolized at a targeted site into CDNs and exert their full immunomodulatory effects at said targeted site. The present invention also provides conjugates wherein a Pro-CDN is conjugated to a Biologically Active Molecule (BAM) such as e.g. a cytotoxic molecule, a lipid, a protein, a peptide, a nucleic acid, a sugar or a PRR ligand. The invention provides also methods related to the use of such compounds to perform their activities at their targeted sites, to exert cytotoxic, cytostatic or immunomodulatory effects, to treat or to prevent diseases such as cancers, immunological disorders or infections.

公开(公告)号：WO2019119141A1

公开(公告)日：2019-06-27

申请号：PCT/CA2018/051638

申请日：2018-12-20

申请人： ONTARIO INSTITUTE FOR CANCER RESEARCH (OICR)

发明人： AL-AWAR, Rima ,  MAMAI, Ahmed

IPC分类号： C07D498/18 ,  A61K47/68 ,  C07D215/42 ,  C07D223/16 ,  C07D311/68 ,  C07D335/06 ,  C07D401/12 ,  C07D403/12 ,  C07D409/12 ,  C07K16/00 ,  C07K16/28 ,  C07K16/46 ,  C07K5/027

CPC分类号： A61P35/00 ,  A61K47/6803 ,  A61K47/6889 ,  C07D215/42 ,  C07D223/16 ,  C07D311/68 ,  C07D335/06 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D498/18 ,  C07K16/32

摘要： The present application is directed to compounds of Formula (I): compounds of Formula (II): compounds of Formula (III): and compounds of Formula (IV): compositions comprising these compounds and their uses, for example as medicaments and /or diagnostics. Specifically claimed are: (1) compounds containing reactive functional groups (compound of formula I), compounds containing compounds to be linked together (compound of formula II) and compounds having a reactive functional group/a compound to be linked (compound of formula IV), (2) an antibody-drug conjugate (compound of formula III), wherein the antibody is covalently attached by a linker to one or more drugs, (3) pharmaceutical compositions comprising compounds of Formula (II) or Formula (III), (4) treatment/diagnosis of disease comprising compounds of Formula (II) or Formula (III), and (5) methods of preparing an ADC of Formula III.

公开(公告)号：WO2018169953A1

公开(公告)日：2018-09-20

申请号：PCT/US2018/022178

申请日：2018-03-13

申请人： R.P. SCHERER TECHNOLOGIES, LLC

发明人： KIM, Yun Cheol ,  HUANG, Chao Bai ,  DRAKE, Penelope M. ,  RABUKA, David

IPC分类号： A61K39/44 ,  A61K47/68 ,  C07K1/13 ,  C12N15/09

CPC分类号： A61K47/6849 ,  A61K47/65 ,  A61K47/6803 ,  A61K47/6889 ,  C07K1/13 ,  C07K16/00 ,  C07K2317/52

摘要： Antibodies that include a sulfatase motif-containing tag in a constant region of an immunoglobulin (Ig) heavy chain polypeptide are disclosed. The sulfatase motif can be converted by a formylglycine-generating enzyme (FGE) to produce a formylglycine (fGly)- modified Ig heavy chain polypeptide. An fGly-modified Ig heavy chain polypeptide of the antibody can be covalently and site-specifically bound to a moiety of interest to provide an antibody conjugate. The disclosure also encompasses methods of production of such tagged Ig heavy chain polypeptides, fGly-modified Ig heavy chain polypeptides, and antibody conjugates, as well as methods of use of same.

公开(公告)号：WO2018004338A1

公开(公告)日：2018-01-04

申请号：PCT/NL2017/050427

申请日：2017-06-27

申请人： TAGWORKS PHARMACEUTICALS B.V.

发明人： ROBILLARD, Marc Stefan ,  TEN HOEVE, Wolter ,  HOEBEN, Freek Johannes Maria ,  VERSTEEGEN, Ronny Mathieu ,  JANSSEN, Hendricus Marie ,  VAN ONZEN, Arthur Henry Antoon Marie ,  ROSSIN, Raffaella

IPC分类号： A61K47/54 ,  A61K47/69 ,  B82Y5/00 ,  C07D257/08

CPC分类号： A61K47/6889 ,  A61K47/555 ,  A61K47/60 ,  A61K47/6415 ,  A61K47/66 ,  A61K47/6817 ,  A61K47/6897 ,  A61K2039/505 ,  C07D257/08 ,  C07K16/30 ,  C07K16/3046 ,  C07K2317/626 ,  C07K2317/94

摘要： Disclosed is an advancement in provoked chemical cleavage. Thereby the invention provides the use of a diene as a chemically cleavable group attached to a Construct, and the use of a dienophile to provoke the release of the Construct by allowing the diene to react with a dienophile capable of undergoing an inverse electron demand Diels Alder reaction with the diene. The invention includes a kit for releasing a Construct C A bound to a Trigger T R , the kit comprising a tetrazine and a dienophile, wherein the Trigger is the tetrazine. The invention also includes the use of the formation of a pyridazine by reacting a tetrazine comprising a Construct C A bound thereto and a dienophile, as a chemical tool for the release, in a chemical, biological or physiological environment, of said Construct.

摘要翻译： 公开的是引起化学切割的进步。 因此，本发明提供了二烯作为连接到构建体的化学可切割基团的用途，以及使用亲二烯体通过使二烯与能够经历逆电子需求的亲二烯体反应而引发构建体的释放Diels Alder 与二烯反应。 本发明包括用于释放结合触发剂T的构建体C 的试剂盒，所述试剂盒包含四嗪和亲二烯体，其中触发剂是四嗪。 本发明还包括在化学，生物或生理学环境中通过使包含结合于其上的构建体C ^和亲二烯体的四嗪作为释放的化学工具反应形成哒嗪的用途 ，所述构造的

公开(公告)号：WO2017143026A1

公开(公告)日：2017-08-24

申请号：PCT/US2017/018116

申请日：2017-02-16

申请人： RESEARCH DEVELOPMENT FOUNDATION

发明人： LIN, Xinjian ,  SHANG, Xiying ,  HOWELL, Stephen, B.

IPC分类号： C12N9/52 ,  C12N9/64

CPC分类号： C12N9/6467 ,  A61K47/65 ,  A61K47/6889 ,  A61K48/00 ,  C07K14/43504 ,  C07K14/59 ,  C07K2319/00 ,  C07K2319/21 ,  C07K2319/33 ,  C07K2319/40 ,  C07K2319/55 ,  C07K2319/70 ,  C07K2319/74 ,  C07K2319/90 ,  C12N9/52 ,  C12N9/6424 ,  C12N9/96 ,  C12Y304/21079 ,  C12Y304/22007 ,  C12Y304/2207

摘要： Cell-targeted cytotoxic agents, including sortase serine protease constructs, are provided. Such compounds can be used in methods for targeted cell killing such as for treatment cell of proliferative diseases (e.g., cancer). In some aspects, recombinant sortase serine proteases, such as Granzyme B polypeptides, are provided that exhibit improved stability and cell toxicity.

摘要翻译： 提供了细胞靶向细胞毒性剂，包括分选酶丝氨酸蛋白酶构建体。 这样的化合物可以用于靶向细胞杀伤的方法，例如用于增殖性疾病（例如癌症）的治疗细胞。 在一些方面，提供了表现出改善的稳定性和细胞毒性的重组分选酶丝氨酸蛋白酶，例如粒酶B多肽。

公开(公告)号：WO2017139623A1

公开(公告)日：2017-08-17

申请号：PCT/US2017/017435

申请日：2017-02-10

申请人： IMMUNOMEDICS, INC.

发明人： CHANG, Chien-Hsing ,  GOLDENBERG, David M.

IPC分类号： A61K45/06 ,  A61K47/48 ,  C07K16/30

CPC分类号： C07K16/3061 ,  A61K31/4535 ,  A61K31/473 ,  A61K31/4745 ,  A61K31/4985 ,  A61K39/3955 ,  A61K41/0038 ,  A61K45/06 ,  A61K47/48384 ,  A61K47/48569 ,  A61K47/48584 ,  A61K47/48592 ,  A61K47/486 ,  A61K47/48607 ,  A61K47/48615 ,  A61K47/48623 ,  A61K47/4863 ,  A61K47/48638 ,  A61K47/48684 ,  A61K47/6803 ,  A61K47/6851 ,  A61K47/6889 ,  A61K51/1057 ,  C07K16/2887 ,  C07K16/30 ,  C07K16/3007 ,  C07K16/3015 ,  C07K16/3023 ,  C07K16/303 ,  C07K16/3038 ,  C07K16/3046 ,  C07K16/3053 ,  C07K16/3069 ,  C07K16/3092 ,  C07K2317/24 ,  C07K2317/565 ,  C07K2317/732 ,  C07K2317/77 ,  C07K2317/90 ,  C07K2317/92 ,  A61K2300/00

摘要： The present invention relates to therapeutic ADCs comprising a drug attached to an anti-cancer antibody or antigen-binding antibody fragment. Preferably the drug is SN-38. More preferably the antibody or fragment thereof binds to Trop-2 and the therapy is used to treat a Trop-2 positive cancer. Most preferably the antibody is hRS7. The ADC is administered to a subject with a cancer in combination with an ABCG2 inhibitor. The combination therapy is effective to treat cancers that are resistant to drug alone and/or to ADC alone.

摘要翻译： 本发明涉及包含附着于抗癌抗体或抗原结合抗体片段的药物的治疗性ADC。 优选药物是SN-38。 更优选地，抗体或其片段结合Trop-2并且该疗法用于治疗Trop-2阳性癌症。 最优选地，抗体是hRS7。 将ADC施用给患有癌症的受试者并结合ABCG2抑制剂。 联合治疗有效治疗单独对抗药物和/或单独对ADC有抗性的癌症。

公开(公告)号：WO2017137556A1

公开(公告)日：2017-08-17

申请号：PCT/EP2017/052991

申请日：2017-02-10

申请人： ADC THERAPEUTICS SA ,  MEDIMMUNE LIMITED

发明人： VAN BERKEL, Patricius Hendrikus Cornelis ,  HOWARD, Philip Wilson ,  DUNNY, Elizabeth ,  HUTCHINSON, Ian ,  MASTERSON, Luke

IPC分类号： A61K47/68 ,  A61P35/00 ,  A61K31/5517

CPC分类号： A61K47/6855 ,  A61K47/6803 ,  A61K47/6851 ,  A61K47/6889

摘要： A conjugate of formula (I) L - (D L ) p (I) wherein L is an antibody (Ab) which binds HER2, D is a Drug Linker unit of formula (A) wherein p is an integer of from 1 to 20.

摘要翻译： 式（I）L - （D L）p（I）的缀合物，其中L是结合HER2的抗体（Ab） ，D是式（A）的药物接头单元，其中p是1至20的整数。

公开(公告)号：WO2017122018A1

公开(公告)日：2017-07-20

申请号：PCT/GB2017/050075

申请日：2017-01-12

申请人： CRESCENDO BIOLOGICS LIMITED

发明人： BALLOI, Eleanora ,  GOODWIN, Normann ,  MCGUINNESS, Brian ,  ROSSANT, Chris ,  SANDAL, Thomas ,  THOMPSON, Lorraine

IPC分类号： C07K16/30 ,  G01N33/53

CPC分类号： C07K16/3069 ,  A61K47/6811 ,  A61K47/6869 ,  A61K47/6889 ,  C07K2317/21 ,  C07K2317/35 ,  C07K2317/569 ,  C07K2317/77 ,  C07K2317/92 ,  C07K2317/94 ,  G01N33/57434

摘要： The disclosure relates to binding molecules that bind specifically to prostate specific membrane antigen (PSMA), in particular, single human variable heavy chain domain antibodies and related methods for treatment of cancer.

摘要翻译： 本公开涉及特异性结合前列腺特异性膜抗原（PSMA）的结合分子，特别是单个人可变重链结构域抗体和用于治疗癌症的相关方法。

公开(公告)号：WO2017112624A1

公开(公告)日：2017-06-29

申请号：PCT/US2016/067663

申请日：2016-12-20

申请人： BRISTOL-MYERS SQUIBB COMPANY

发明人： SHEPPARD, Paul O. ,  ANDERSEN, Henrik ,  SHAO, Xiang ,  RAO-NAIK, Chetana ,  RAJPAL, Arvind

IPC分类号： C07K16/00 ,  A61K47/68

CPC分类号： C07K16/00 ,  A61K47/6803 ,  A61K47/6849 ,  A61K47/6851 ,  A61K47/6889 ,  C07K16/2875 ,  C07K16/30 ,  C07K2317/52 ,  C07K2317/524 ,  C07K2317/526

摘要： Variant antibodies having cysteine substitutions at selected positions in the Fc region can be conjugated via the thiol group of the substituted-in cysteine.

摘要翻译： 在Fc区中的选定位置具有半胱氨酸取代的变体抗体可通过取代的半胱氨酸的巯基缀合。

公开(公告)号：WO2017095808A1

公开(公告)日：2017-06-08

申请号：PCT/US2016/063998

申请日：2016-11-29

申请人： ABBVIE INC. ,  ABBVIE BIOTHERAPEUTICS INC.

发明人： GISH, Kurt C. ,  HICKSON, Jonathan A. ,  PURCELL, James W. ,  MORGAN-LAPPE, Susan Elizabeth

IPC分类号： C07K16/28 ,  C07K16/30 ,  A61K47/68

CPC分类号： A61K31/5517 ,  A61K38/07 ,  A61K47/6803 ,  A61K47/6849 ,  A61K47/6851 ,  A61K47/6889 ,  C07K16/28 ,  C07K16/30 ,  C07K2317/24 ,  C07K2317/77 ,  C07K2317/92

摘要： The present disclosure provides antibodies, antibody binding fragments, and antibody drug conjugates that bind human LRRC15, their methods of making, and their uses to treat patients having cancer.

摘要翻译： 本公开提供了结合人LRRC15的抗体，抗体结合片段和抗体药物缀合物，它们的制备方法以及它们用于治疗患有癌症的患者的用途。