公开(公告)号：EP2917244A1

公开(公告)日：2015-09-16

申请号：EP13853308.8

申请日：2013-11-12

申请人： Angiochem Inc.

发明人： TRIPATHY, Sasmita ,  DEMEULE, Michel ,  CURRIE, Jean-Christophe

IPC分类号： C07K19/00 ,  A61K47/48 ,  A61P35/00 ,  A61P35/04 ,  C07K14/81 ,  C07K16/28

CPC分类号： A61K38/57 ,  A61K47/6811 ,  A61K47/6843 ,  A61K47/6849 ,  A61K47/6855 ,  A61K47/6889 ,  C07K14/8117 ,  C07K2319/00

摘要： The present invention relates to protein conjugates comprising an aprotinin-derived polypeptide, which facilitates transport of the conjugate across the blood-brain barrier, and an antibody moiety that selectively binds a target within the CNS. The protein conjugates are further defined by the inclusion of a linker; by the number of polypeptides conjugated to each antibody moiety; by the positions at which the antibody moiety and the polypeptides are conjugated; and by the larger configuration of the conjugate (in which every polypeptide is linked only to the antibody moiety). Modified aprotinin-derived polypeptides, linker-bound antibody moieties, pharmaceutical compositions, kits, and methods of making and using the protein conjugates are also features of the invention.

公开(公告)号：EP1859041B1

公开(公告)日：2012-03-28

申请号：EP05770546.9

申请日：2005-07-21

申请人： Angiochem Inc.

发明人： BÉLIVEAU, Richard ,  DEMEULE, Michel ,  CHÉ, Christian ,  REGINA, Anthony

IPC分类号： C12N15/15 ,  C07K14/81 ,  A61K47/48 ,  A61K47/42 ,  A61K51/08 ,  A61K49/14 ,  A61P25/00

CPC分类号： A61K47/48246 ,  A61K31/337 ,  A61K38/00 ,  A61K39/44 ,  A61K47/64 ,  A61K2039/505 ,  C07K14/8117 ,  Y10S977/915

摘要： The invention relates to improvements in the field of drug delivery. More particularly, the invention relates to polypeptides derived from aprotinin and from aprotinin analogs as well as conjugates and pharmaceutical compositions comprising these polypeptides or conjugates. The present invention also relates to the use of these polypeptide for transporting a compound or drug across the blood-brain barrier of a mammal and in the treatment and diagnosis of neurological diseases.

公开(公告)号：EP2885318A1

公开(公告)日：2015-06-24

申请号：EP13829574.6

申请日：2013-08-14

申请人： Angiochem Inc.

发明人： DEMEULE, Michel ,  LAROCQUE, Alain ,  YANG, Gaoqiang ,  TRIPATHY, Sasmita

IPC分类号： C07K14/81 ,  A61K47/48 ,  A61K49/00 ,  C07K14/00

CPC分类号： A61K47/48253 ,  A61K38/10 ,  A61K47/593 ,  A61K47/595 ,  A61K47/64 ,  A61K47/641 ,  C07K14/8117

摘要： The invention relates to dendrimers conjugated to multiple targeting peptides and one or more therapeutic, diagnostic, or imaging agents for delivery of such agents across the blood-brain barrier and into certain cell types including, cells expressing the LRP-1 receptor. Also described are methods of making compounds that comprise dendrimers conjugated to targeting peptides and therapeutic, diagnostic, or imaging agents.

公开(公告)号：EP2861729A1

公开(公告)日：2015-04-22

申请号：EP13803602.5

申请日：2013-06-14

申请人： Angiochem Inc.

发明人： BOIVIN, Dominique ,  CASTAIGNE, Jean-Paul ,  DEMEULE, Michel

IPC分类号： C12N9/24 ,  A61K47/48 ,  A61P3/00 ,  C07K14/81 ,  C07K19/00 ,  C12N9/96

CPC分类号： C12N9/2402 ,  A61K38/47 ,  A61K47/48246 ,  A61K47/64 ,  C07K7/08 ,  C07K2319/06 ,  C07K2319/21 ,  C07K2319/33 ,  C07K2319/50 ,  C12Y302/01076

摘要： The present invention is related to a compound that includes (a) α-L-iduronidase (IDUA), fragment, or analog thereof and (b) a targeting moiety, for example, where compound is a fusion protein including IDUA and Angiopep-2. In certain embodiments, these compounds, owning to the presence of the targeting moiety can crossing the blood-brain barrier or accumulate in the lysosome more effectively than the enzyme alone. The invention also features methods for treating mucopolysaccharidosis type I (MPS-I) using such compounds.

公开(公告)号：EP2588490A1

公开(公告)日：2013-05-08

申请号：EP11800042.1

申请日：2011-07-04

申请人： Angiochem Inc.

发明人： CASTAIGNE, Jean-Paul ,  DEMEULE, Michel ,  CHE, Christian ,  THIOT, Carine ,  PESLHERBE, Laurence

IPC分类号： C07K7/06 ,  A61K38/16 ,  A61K47/48 ,  A61P35/00 ,  C07K14/00 ,  C07K19/00 ,  C07K7/08 ,  C07K14/575 ,  C07K14/605

CPC分类号： A61K47/6811 ,  A61K38/10 ,  A61K38/185 ,  A61K38/2264 ,  A61K38/2278 ,  A61K47/64 ,  C07K14/8117 ,  C07K2319/00 ,  Y02A50/463

摘要： The present invention relates to short polypeptides (e.g., fewer than 19 amino acids in length) and longer polypeptides (e.g., 19 or more amino acids in length) having one or more D-amino acids as targeting moieties. These polypeptides, when conjugated to agents (e.g., therapeutic agents or transport vectors) are capable of transporting the agents across the BBB or into particular cell types. In particular, the short polypeptides can include one or more D-amino acids. These compounds are therefore particularly useful in the treatment of neurological diseases or diseases associated with particular cell types, organs, or tissues.

公开(公告)号：EP2486061A1

公开(公告)日：2012-08-15

申请号：EP10821522.9

申请日：2010-10-05

申请人： Angiochem Inc.

发明人： CASTAIGNE, Jean-Paul ,  DEMEULE, Michel ,  CHE, Christian ,  REGINA, Anthony

IPC分类号： C07K17/00 ,  A61K47/48 ,  A61P25/28 ,  A61P3/00 ,  A61P35/00 ,  C07K17/08 ,  C12N11/00 ,  C07K14/81 ,  C12N15/113

CPC分类号： A61K47/48246 ,  A61K47/62 ,  A61K47/64 ,  A61K47/6907 ,  A61K47/6911 ,  A61K47/6921 ,  A61K47/6929 ,  C07K7/083 ,  C07K14/475 ,  C07K14/5759 ,  C07K14/8117

摘要： The present invention is directed to conjugates that include a polypeptide capable of crossing the blood-brain barrier or entering one or more cell types attached to a transport vector, i.e., a compostion capable of transporting an agent (e.g., a therapeutic agent). In certain cases, the polypeptides are directly conjugated to a lipid or polymeric vector to allow targeted application of a therapeutic agent to treat, for example, a cancer, a neurodegenerative disease, or a lysosomal storage disorder.

公开(公告)号：EP2448965A1

公开(公告)日：2012-05-09

申请号：EP10793472.1

申请日：2010-06-30

申请人： Angiochem Inc.

发明人： DEMEULE, Michel ,  CHE, Christian ,  THIOT, Carine

IPC分类号： C07K14/81 ,  A61K39/44 ,  A61K47/48 ,  C07K7/08

CPC分类号： A61K47/48246 ,  A61K47/64

摘要： The present invention relates to multimeric (e.g., dimeric, trimeric) forms of peptide vectors that are capable of crossing the blood-brain barrier (BBB) or efficiently entering particular cell types. These multimeric peptide vectors, when conjugated to agents (e.g., therapeutic agents) are capable of transporting the agents across the BBB or into particular cell types. These compounds are therefore particularly useful in the treatment of neurological diseases.

公开(公告)号：EP2370471A1

公开(公告)日：2011-10-05

申请号：EP09829934.0

申请日：2009-12-07

申请人： Angiochem Inc.

发明人： CASTAIGNE, Jean-Paul ,  DEMEULE, Michel ,  CHE, Christian ,  THIOT, Carine ,  GAGNON, Catherine

IPC分类号： C07K19/00 ,  A61K38/16 ,  A61K47/48 ,  C07K7/08 ,  C12N15/62 ,  C07K14/81 ,  C07K17/00

CPC分类号： C07K7/083 ,  A61K38/00 ,  A61K47/64 ,  C07K14/8117 ,  C07K2319/03

摘要： The present invention features a compound having the formula A-X-B, where A is peptide vector capable of enhancing transport of the compound across the blood-brain barrier or into particular cell types, X is a linker, and B is a peptide therapeutic selected from the group consisting of neurotensin, a neurotensin analog, or a neurotensin receptor agonist. The compounds of the invention can be used to treat any disease in which increased neurotensin activity is useful and can be used to induce hypothermia or analgesia.

摘要翻译： 本发明的特征在于具有式AX-B的化合物，其中A是能够增强化合物穿过血脑屏障或特定细胞类型的转运的肽载体，X是接头，B是选自 由神经丝氨酸，神经降压素类似物或神经降压素受体激动剂组成的组。 本发明的化合物可用于治疗其中增加的神经降压素活性有用并可用于诱导低体温或镇痛的任何疾病。

公开(公告)号：EP2346896A1

公开(公告)日：2011-07-27

申请号：EP09820163.5

申请日：2009-10-15

申请人： Angiochem Inc.

发明人： DEMEULE, Michel ,  CHE, Christian ,  GABATHULER, Reinhard ,  YANG, Gaoqiang

IPC分类号： C07K14/81 ,  A61K31/704 ,  A61K31/7048 ,  A61K47/42 ,  A61K47/48 ,  A61P35/00 ,  C07H15/252 ,  C07H17/04 ,  C07K14/00 ,  C07K7/08 ,  C07K14/705

CPC分类号： A61K47/48246 ,  A61K31/04 ,  A61K31/337 ,  A61K31/704 ,  A61K31/7048 ,  A61K38/10 ,  A61K39/39558 ,  A61K45/06 ,  A61K47/62 ,  A61K47/64 ,  C07H17/04 ,  C07K14/515 ,  A61K2300/00

摘要： The invention relates to improvements in the field of drug delivery. More particularly, the invention relates to polypeptides having a hydrolyzable covalent bond to a therapeutic agent that includes, etoposide, etoposide 4'- dimethylglycine or doxorubicin. These polypeptide conjugates can be used as vectors to transport the podophyllotoxin derivative across the blood brain barrier (BBB) or into particular cell types such as ovary, liver, lung, or kidney. The invention also relates to pharmaceutical compositions that include the compounds of the invention and to uses thereof in methods of treatment.

摘要翻译： 本发明涉及药物递送领域的改进。 更具体地说，本发明涉及具有包含依托泊苷，依托泊苷4'-二甲基甘氨酸或多柔比星的治疗剂的可水解共价键的多肽。 这些多肽缀合物可用作载体，以将鬼臼毒素衍生物跨越血脑屏障（BBB）或特定的细胞类型如卵巢，肝，肺或肾运送。 本发明还涉及包含本发明化合物及其在治疗方法中的用途的药物组合物。

公开(公告)号：EP2885321A1

公开(公告)日：2015-06-24

申请号：EP13829923.5

申请日：2013-08-14

申请人： Angiochem Inc.

发明人： CASTAIGNE, Jean-Paul ,  YANG, Gaoqiang ,  CHE, Christian ,  DEMEULE, Michel

IPC分类号： C07K19/00 ,  A61K47/48 ,  A61P35/00 ,  C07K14/81 ,  C07K16/18 ,  C07K16/28

CPC分类号： A61K47/48246 ,  A61K31/337 ,  A61K47/482 ,  A61K47/48384 ,  A61K47/48407 ,  A61K47/48561 ,  A61K47/48569 ,  A61K47/48584 ,  A61K47/48684 ,  A61K47/487 ,  A61K47/593 ,  A61K47/64 ,  A61K47/6803 ,  A61K47/6809 ,  A61K47/6849 ,  A61K47/6851 ,  A61K47/6855 ,  A61K47/6881 ,  A61K47/6885 ,  C07K14/8117 ,  C07K16/2863 ,  C07K16/3015 ,  C07K16/32 ,  C07K2317/24 ,  C07K2319/33

摘要： The present invention relates to antibody-polypeptide-cytotoxin conjugates and methods of making, packaging, and using the conjugates. The polypeptide can be a Kunitz-type protease inhibitor or a derivative thereof that facilitates transport of the conjugate across the blood-brain barrier and/or into cancer cells outside the CNS, and the antibody moiety selectively binds a target within the CNS or in peripheral tumors to direct the cytotoxic agent to that target (e.g., a tumor or cancer cell). The conjugates can be further defined by the inclusion of a linker between the antibody moiety and the polypeptide; by the number of polypeptides and cytotoxic agents conjugated thereto; by the positions at which the entities within the conjugates are bound to one another; and by the larger configuration of the conjugate. Modified polypeptides (e.g., polypeptides conjugated to cytotoxic agents but not to an antibody moiety), pharmaceutical compositions, kits (e.g., including a modified polypeptide and an as-yet unconjugated antibody), and methods of making and using the conjugates are also features of the invention.