公开(公告)号：EP3220961A4

公开(公告)日：2018-06-20

申请号：EP15852241

申请日：2015-10-21

申请人： EXTEND BIOSCIENCES INC

发明人： SOLIMAN TARIK ,  HALES LAURA M ,  HALL DANIEL B ,  SO CHRISTOPHER ,  SARD HOWARD P ,  HEGDE VISHNUMURTHY

IPC分类号： A61K47/60 ,  A61K38/10 ,  A61K38/22

CPC分类号： A61K38/10 ,  A61K9/0019 ,  A61K38/22 ,  A61K47/48107 ,  A61K47/48215 ,  A61K47/551 ,  A61K47/60

摘要： The invention provides non-hormonal vitamin D conjugated to apelin proteins that result in increased absorption, bioavailability or circulating half-life when compared to non-conjugated forms. In some embodiments, the vitamin D targeting groups are coupled to the apelin proteins via the third carbon on the vitamin D backbone.

公开(公告)号：EP3129357A4

公开(公告)日：2018-06-13

申请号：EP15776253

申请日：2015-04-09

申请人： AF CHEMICALS LLC

发明人： KELNER MICHAEL

IPC分类号： C07D235/02 ,  A01N47/10 ,  C07C209/62 ,  C07D493/00

CPC分类号： A61K31/122 ,  A61K31/19 ,  A61K47/481 ,  A61K47/48107 ,  A61K47/48123 ,  A61K47/48238 ,  A61K47/48246 ,  A61K47/48261 ,  A61K47/48269 ,  A61K47/48338 ,  A61K47/48369 ,  A61K47/48384 ,  A61K47/48715 ,  A61K47/551 ,  A61K47/554 ,  A61K47/62 ,  A61K47/642 ,  A61K47/6803 ,  A61K47/6889

摘要： In an embodiment of the invention, a composition for treating a cell population comprises an Affinity Medicant Conjugate (AMC). The medicant moiety can be a toxin including an acylfulvene or a drug moiety. The affinity moiety can be an antibody, a binding protein, a steroid, a lipid, a growth factor, a protein, a peptide or non peptidic. The affinity moiety can be covalently bound to the medicant via a linker. Novel linkers that can be directed to cysteine, arginine or lysine residues based on solution pH allow greater flexibility in preserving and/or generating specific epitopes in the AMC.

公开(公告)号：EP2766364A1

公开(公告)日：2014-08-20

申请号：EP12746091.3

申请日：2012-08-10

申请人： Merck & Cie

发明人： SCHIBLI, Roger ,  MOSER, Rudolf ,  MÜLLER, Cristina Magdalena ,  STRUTHERS, Harriet ,  GROEHN, Viola ,  AMETAMEY, Simon Mensah ,  FISCHER, Cindy Ramona

IPC分类号： C07D475/04 ,  A61K31/519 ,  A61P35/00 ,  C07K5/02

CPC分类号： A61K51/0497 ,  A61K47/48107 ,  A61K47/551 ,  A61K51/0472 ,  A61K51/0491 ,  C07B59/002 ,  C07D475/04 ,  G01N33/56966

摘要： The present invention is directed towards new trifunctional folate-conjugates comprising a folate, an albumin binder and a radionuclide-based therapeutic or diagnostic moiety as well as pharmaceutical compositions thereof, their method of production and their use in diagnostic and therapeutic medical applications, such as diagnostic nuclear imaging and radionuclide therapy.

摘要翻译： 本发明涉及包含叶酸，白蛋白粘合剂和基于放射性核素的治疗或诊断部分的新的三官能叶酸盐缀合物，以及其药物组合物，其生产方法及其在诊断和治疗医学应用中的用途，例如 诊断性核成像和放射性核素治疗。

公开(公告)号：EP3204004A1

公开(公告)日：2017-08-16

申请号：EP15848354.5

申请日：2015-10-08

申请人： Epigenetics Pharma LLC

发明人： DAIFUKU, Richard

IPC分类号： A61K31/355 ,  A61K31/70 ,  A61K31/7068

CPC分类号： A61K31/7068 ,  A61K31/355 ,  A61K47/48061 ,  A61K47/48092 ,  A61K47/48107 ,  A61K47/549 ,  A61K47/55 ,  C07H19/10 ,  C07H19/20

摘要： The present disclosure describes nucleoside and nucleoside analogues that are conjugated to a vitamin E derivative via a phosphate ester or a phosphoramidate linkage. The nucleoside or nucleoside analogues can provide enhanced therapeutic activity (e.g., antiproliferative activity against tumor cells) and/or greater chemical stability in aqueous solutions.

摘要翻译： 本公开描述了通过磷酸酯或氨基磷酸酯键与维生素E衍生物缀合的核苷和核苷类似物。 核苷或核苷类似物可在水溶液中提供增强的治疗活性（例如抗肿瘤细胞的抗增殖活性）和/或更高的化学稳定性。

公开(公告)号：EP2349274A4

公开(公告)日：2014-12-17

申请号：EP09815218

申请日：2009-09-17

申请人： ENDOCYTE INC ,  PURDUE RESEARCH FOUNDATION

发明人： LEAMON CHRISTOPHER PAUL ,  VLAHOV IONTCHO RADOSLAVOV ,  LOW PHILIP STEWART

IPC分类号： A61K31/517 ,  A61K47/48 ,  A61P11/06

CPC分类号： A61K47/48338 ,  A61K31/475 ,  A61K31/517 ,  A61K47/48061 ,  A61K47/481 ,  A61K47/48107 ,  A61K47/55 ,  A61K47/551 ,  C07D487/04

摘要： Conjugates of antifolates, releasable linkers, and drugs, and pharmaceutical compositions containing them are described. The conjugates are useful for treating diseases arising from pathogenic cell populations. Methods for treating such diseases are also described.

公开(公告)号：EP3057619A1

公开(公告)日：2016-08-24

申请号：EP14795563.7

申请日：2014-10-16

申请人： Université Libre de Bruxelles

发明人： AMIGHI, Karim ,  ROSIÈRE, Rémi ,  WAUTHOZ, Nathalie ,  GELBCKE, Michel

IPC分类号： A61K47/48 ,  A61P35/00

CPC分类号： A61K47/48107 ,  A61K9/0075 ,  A61K9/50 ,  A61K9/5089 ,  A61K9/51 ,  A61K9/5123 ,  A61K9/5161 ,  A61K9/5192 ,  A61K31/337 ,  A61K31/495 ,  A61K33/24 ,  A61K47/551 ,  A61K47/61 ,  A61K47/6927 ,  A61K47/6939

摘要： The present application provides a pharmaceutical formulation comprising a folate receptor (FR)-targeting antineoplastic substance or composition, wherein the pharmaceutical formulation is configured for administration by inhalation, wherein the FR-targeting antineoplastic substance or composition is comprised in a nanoparticle and wherein the nanoparticles are comprised in microparticles, and its use in the treatment of a proliferative disease affecting at least part of the respiratory tract. The present application further provides a pharmaceutical formulation comprising an antineoplastic agent and a FR-targeting excipient, for use in the treatment of a proliferative disease affecting at least part of the respiratory tract.

公开(公告)号：EP2822386A4

公开(公告)日：2016-01-20

申请号：EP13754418

申请日：2013-02-28

申请人： PURDUE RESEARCH FOUNDATION

发明人： LOW PHILIP STEWART ,  VAITILINGAM BALASUBRAMANIAN ,  CHELVAM VENKATESH

IPC分类号： A01N43/54 ,  A61K31/06 ,  A61K31/475 ,  A61K38/06 ,  A61K47/48 ,  A61K49/00 ,  A61K51/04 ,  A61P35/00

CPC分类号： A61K47/48061 ,  A61K31/475 ,  A61K38/06 ,  A61K47/48107 ,  A61K47/545 ,  A61K47/551 ,  A61K49/0052 ,  A61K51/0459

摘要： The invention described herein pertains to targeted drug delivery conjugates comprising folate receptor α (FR-α) selective binding ligands and methods for diagnosing, monitoring, and eliminating pathological cells that express FR-α.

摘要翻译： 本文描述的本发明涉及包含叶酸受体α（FR-α）选择性结合配体的靶向药物递送缀合物以及用于诊断，监测和消除表达FR-α的病理细胞的方法。

公开(公告)号：EP3204004A4

公开(公告)日：2018-05-30

申请号：EP15848354

申请日：2015-10-08

申请人： EPIGENETICS PHARMA LLC

发明人： DAIFUKU RICHARD

IPC分类号： A61K47/54 ,  A61K31/355 ,  A61K31/70 ,  A61K31/7068 ,  A61K47/55 ,  A61P35/00 ,  A61P35/02 ,  C07H19/10 ,  C07H19/20

CPC分类号： A61K31/7068 ,  A61K31/355 ,  A61K47/48061 ,  A61K47/48092 ,  A61K47/48107 ,  A61K47/549 ,  A61K47/55 ,  C07H19/10 ,  C07H19/20

摘要： The present disclosure describes nucleoside and nucleoside analogues that are conjugated to a vitamin E derivative via a phosphate ester or a phosphoramidate linkage. The nucleoside or nucleoside analogues can provide enhanced therapeutic activity (e.g., antiproliferative activity against tumor cells) and/or greater chemical stability in aqueous solutions.

公开(公告)号：EP3131587A4

公开(公告)日：2017-11-01

申请号：EP15779751

申请日：2015-04-14

申请人： ENDOCYTE INC

发明人： VLAHOV IONTCHO RADOSLAVOV ,  LEAMON CHRISTOPHER PAUL ,  REDDY JOSEPH ANAND

IPC分类号： A61K47/55

CPC分类号： A61K47/48107 ,  A61K31/282 ,  A61K31/337 ,  A61K31/357 ,  A61K31/4745 ,  A61K31/704 ,  A61K33/24 ,  A61K39/3955 ,  A61K47/551 ,  A61K47/64 ,  A61K2039/505 ,  C07K16/22 ,  C07K2317/24

公开(公告)号：EP3131587A1

公开(公告)日：2017-02-22

申请号：EP15779751.5

申请日：2015-04-14

申请人： Endocyte, Inc.

发明人： VLAHOV, Iontcho Radoslavov ,  LEAMON, Christopher Paul ,  REDDY, Joseph Anand

IPC分类号： A61K47/50

CPC分类号： A61K47/48107 ,  A61K31/282 ,  A61K31/337 ,  A61K31/357 ,  A61K31/4745 ,  A61K31/704 ,  A61K33/24 ,  A61K39/3955 ,  A61K47/551 ,  A61K47/64 ,  A61K2039/505 ,  C07K16/22 ,  C07K2317/24

摘要： Described herein are drug delivery conjugates for targeted therapy. In particular, described herein are drug delivery conjugates that include polyvalent linkers comprising one or more unnatural amino acids that are useful for treating cancers and inflammatory diseases. In some embodiments, the cancer is selected from the group consisting of a carcinoma, a sarcoma, a lymphoma, Hodgekin's disease, a melanoma, a mesothelioma, Burkitfs lymphoma, a nasopharyngeal carcinoma, a leukemia, and a myeloma.

摘要翻译： 描述是靶向治疗药物递送轭合物。 特别地，在描述的是药物递送缀合物也包括多价连接体包括一个或多个非天然氨基酸确实是用于治疗癌症和炎性疾病是有用的。 在一些实施方案中，所述癌症选自癌，肉瘤，淋巴瘤的选择，Hodgekin氏病，黑色素瘤，间皮瘤，伯基特淋巴瘤，鼻咽癌，白血病，和骨髓瘤。