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公开(公告)号：US09161988B2
公开(公告)日：2015-10-20
申请号：US13382069
申请日：2010-06-30
申请人： Jean-Paul Castaigne , Michel Demeule , Christian Che , Carine Thiot , Catherine Gagnon , Betty Lawrence
发明人： Jean-Paul Castaigne , Michel Demeule , Christian Che , Carine Thiot , Catherine Gagnon , Betty Lawrence
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.
摘要翻译： 本发明涉及能够穿过血脑屏障（BBB）或有效进入特定细胞类型的多聚体（例如二聚体，三聚体）形式的肽载体。 当与试剂（例如治疗剂）缀合时，这些多聚体肽载体能够将该药物转运穿过BBB或特定的细胞类型。 因此，这些化合物特别可用于治疗神经疾病。
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公开(公告)号：US20120015876A1
公开(公告)日：2012-01-19
申请号：US13124013
申请日：2009-10-15
IPC分类号： A61K38/22 , A61P3/04 , A61P3/10 , C07K19/00 , C07K14/575 , C07K1/04 , A61P3/06 , A61P9/12 , A61P9/00 , A61P3/08 , A61P25/16 , A61P25/22 , A61P25/28 , A61P25/20 , A61P25/14 , A61P25/18 , A61P25/08 , A61P25/00 , A61P1/16 , A61P1/00 , A61P9/10 , A61P13/00 , A61P13/12 , A61P9/04 , A61P11/00 , A61P15/00 , A61P29/00 , C07H21/00
CPC分类号： C07K14/57563 , A61K38/00 , A61K47/64 , A61K47/65 , C07K2319/01
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 GLP-1 agonist (e.g., exendin-4 or an exendin-4 analog). The compounds of the invention can be used to treat any disease where increased GLP-1 activity is desired, for example, metabolic diseases, such as obesity and diabetes.
摘要翻译： 本发明的特征在于具有式AXB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GLP-1激动剂（例如， ，毒蜥外泌肽-4或毒蜥外泌肽-4类似物）。 本发明的化合物可用于治疗需要增加GLP-1活性的任何疾病，例如代谢疾病，例如肥胖症和糖尿病。
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公开(公告)号：US08921314B2
公开(公告)日：2014-12-30
申请号：US13124013
申请日：2009-10-15
IPC分类号： A61K38/00 , A61P3/10 , A61P3/04 , C07K14/605 , C07K14/575 , A61K47/48
CPC分类号： C07K14/57563 , A61K38/00 , A61K47/64 , A61K47/65 , C07K2319/01
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 GLP-1 agonist (e.g., exendin-4 or an exendin-4 analog). The compounds of the invention can be used to treat any disease where increased GLP-1 activity is desired, for example, metabolic diseases, such as obesity and diabetes.
摘要翻译： 本发明的特征在于具有式AXB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GLP-1激动剂（例如， ，毒蜥外泌肽-4或毒蜥外泌肽-4类似物）。 本发明的化合物可用于治疗需要增加GLP-1活性的任何疾病，例如代谢疾病，例如肥胖症和糖尿病。
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公开(公告)号：US20110288011A1
公开(公告)日：2011-11-24
申请号：US13133002
申请日：2009-12-07
IPC分类号： A61K38/22 , C07K19/00 , C07K14/575 , C07H21/00 , A61P3/04 , A61P3/10 , A61P9/00 , A61P9/12 , A61K38/17 , A61P25/28 , A61P3/00 , A61P3/08 , A61P25/22 , A61P25/14 , A61P25/16 , A61P25/08 , A61P25/18 , A61P25/20 , A61P25/00 , A61P1/18 , A61P1/16 , A61P13/12 , A61P1/00 , A61P13/00 , A61P9/04 , A61P11/00 , A61P3/06 , A61P29/00 , A61P35/00 , A61P43/00 , C07K14/435
CPC分类号： A61K47/48246 , A61K38/00 , A61K38/2264 , A61K38/2278 , A61K47/64 , C07K7/08 , C07K14/001 , C07K14/57563 , C07K14/5759 , C07K14/8117 , C07K2319/00
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. The compounds of the invention can be used to treat any disease for which the peptide therapeutic is useful.
摘要翻译： 本发明的特征在于具有式A-X-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是肽治疗剂。 本发明的化合物可用于治疗肽治疗剂可用的任何疾病。
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公开(公告)号：US20110288009A1
公开(公告)日：2011-11-24
申请号：US13132838
申请日：2009-12-07
IPC分类号： A61K38/22 , C07K19/00 , C07H21/00 , A61P3/04 , A61P9/12 , A61P3/06 , A61P3/00 , A61P3/08 , A61P9/00 , C07K14/575 , A61P3/10
CPC分类号： C07K14/5759 , A61K38/00 , A61K47/64 , C07K14/8117 , C07K2319/10
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 leptin, a leptin analog, or OB receptor agonist. The compounds of the invention can be used to treat any disease in which increased amounts of leptin are desired, such as metabolic diseases including obesity and diabetes.
摘要翻译： 本发明的特征在于具有式AXB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是瘦蛋白，瘦蛋白类似物， 或OB受体激动剂。 本发明的化合物可用于治疗任何需要增加瘦素量的疾病，例如包括肥胖症和糖尿病在内的代谢疾病。
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6.发明授权Treatment of ovarian cancer using an anticancer agent conjugated to an angiopep-2 analog 有权使用与angiopep-2类似物缀合的抗癌剂治疗卵巢癌公开(公告)号：US09173891B2
公开(公告)日：2015-11-03
申请号：US13265309
申请日：2010-04-20
IPC分类号： A61K38/04 , A61K31/70 , A61K31/337 , A61K31/475 , A61K31/704 , A61K38/10
CPC分类号： A61K31/70 , A61K31/337 , A61K31/475 , A61K31/704 , A61K38/10 , A61K2300/00
摘要： Ovarian cancer is treated with conjugates of an anticancer agent and an Angiopep-2 polypeptide analog (i.e. a polypeptide comprising an amino acid sequence at least 80% identical to Seq. ID NO:97). Such treatment includes utility in treating metastatic ovarian cancer and in treating patients who have previously exhibited resistance to standard chemotherapeutic agents. Preferred anticancer agents include taxanes while the preferred conjugate is ANG1005, a conjugate comprising three molecules of paclitaxel conjugated to the peptide Angiopep-2.
摘要翻译： 用抗癌剂和Angiopep-2多肽类似物（即包含与Seq.ID NO：97至少80％相同的氨基酸序列的多肽）的缀合物处理卵巢癌。 这种治疗包括治疗转移性卵巢癌和治疗先前对标准化学治疗剂具有抗性的患者的效用。 优选的抗癌剂包括紫杉烷，而优选的缀合物是ANG1005，包含与肽Angiopep-2缀合的三分子紫杉醇的缀合物。
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7.发明申请TREATMENT OF OVARIAN CANCER USING AN ANTICANCER AGENT CONJUGATED TO AN ANGIOPEP-2 ANALOG 有权使用与ANGIOPEP-2模拟相结合的ANTICANCER AGENT治疗OVARIAN癌症公开(公告)号：US20120122798A1
公开(公告)日：2012-05-17
申请号：US13265309
申请日：2010-04-20
CPC分类号： A61K31/70 , A61K31/337 , A61K31/475 , A61K31/704 , A61K38/10 , A61K2300/00
摘要： Ovarian cancer is treated with conjugates of an anticancer agent and an Angiopep-2 polypeptide analog (i.e. a polypeptide comprising an ammo acid sequence at least 80% identical to Seq. ID NO:97). Such treatment includes utility in treating metastatic ovarian cancer and in treating patients who have previously exhibited resistance to standard chemotherapeutic agents. Preferred anticancer agents include taxanes while the preferred conjugate is ANG1005, a conjugate comprising three molecules of paclitaxel conjugated to the peptide Angiopep-2.
摘要翻译： 用抗癌剂和Angiopep-2多肽类似物（即包含与Seq.ID NO：97至少80％相同的氨基酸序列的多肽）的缀合物处理卵巢癌。 这种治疗包括治疗转移性卵巢癌和治疗先前对标准化学治疗剂具有抗性的患者的效用。 优选的抗癌剂包括紫杉烷，而优选的缀合物是ANG1005，包含与肽Angiopep-2缀合的三分子紫杉醇的缀合物。
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公开(公告)号：US20050100507A1
公开(公告)日：2005-05-12
申请号：US11014403
申请日：2004-12-16
CPC分类号： C07K7/06 , A61K51/08 , A61K51/088 , C07K7/02
摘要： Radiopharmaceuticals comprising molecules that target to N-formyl-methionyl-leucyl-phenylalanine (fMLF) receptor on leukocytes in order to target sites of inflammation for diagnostic imaging are described. The targeting molecules are attached to capping groups that make the entire molecule either antagonists or weak agonists of fMLF receptor and therefore do not elicit a chemotactic response resulting in neutropenia. The preferred targeting molecule is ReO-Gly-lys(Dimethylgly-t-Butylgly-cys-gly)-glu-trp-phe-leu-nle-NHCOcyclopropyl. The invention also relates to the use of combinatorial chemistry to obtain preferred molecules that target sites of inflammation for diagnostic imaging.
摘要翻译： 描述了包含靶向白细胞上的N-甲酰基 - 甲硫氨酰 - 亮氨酰 - 苯丙氨酸（fMLF）受体以靶向用于诊断成像的炎症部位的分子的放射性药物。 靶向分子连接到使整个分子成为fMLF受体的拮抗剂或弱激动剂的封端基团，因此不引起导致中性粒细胞减少的趋化性反应。 优选的靶向分子是ReO-Gly-lys（Dimethylgly-t-Butylgly-cys-gly）-glu-trp-phe-leu-nle-NHCO环丙基。 本发明还涉及组合化学的用途以获得靶向诊断成像炎症部位的优选分子。
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