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1. 发明申请

WO2010016935A2 TRUNCATED ANALOGUES OF GLUCOSE-DEPENDENT INSULINOTROPIC POLYPEPTIDE 审中-公开
标题翻译：葡萄糖依赖性胰岛素多肽的截短类似物
公开(公告)号：WO2010016935A2
公开(公告)日：2010-02-11
申请号：PCT/US2009/004543
申请日：2009-08-07
申请人： IPSEN PHARMA S.A.S. , DONG, Zheng, Xin , SHEN, Yeelana , DEOLIVEIRA, Daniel, B.
发明人： DONG, Zheng, Xin , SHEN, Yeelana , DEOLIVEIRA, Daniel, B.
IPC分类号： A61K38/16
CPC分类号： C07K14/605 , A61K38/00
摘要： There is provided a novel series of analogues of glucose-dependent insulinotropic polypeptide, pharmaceutical compositions containing said compounds, and the use of said compounds as GIP- receptor agonists or antagonists for treatment of GIP-receptor mediated conditions, such as non- insulin dependent diabetes mellitus and obesity.
摘要翻译：提供了一系列新的葡萄糖依赖性促胰岛素多肽类似物，含有所述化合物的药物组合物，以及所述化合物作为GIP-受体激动剂或拮抗剂在治疗GIP-受体介导的病症中的用途如非胰岛素依赖性糖尿病和肥胖。

2. 发明申请

WO2010096175A1 CYTOTOXIC CONJUGATES HAVING NEUROPEPTIDE Y RECEPTOR BINDING COMPOUND 审中-公开
标题翻译：具有神经元Y受体结合化合物的CYTOTOXIC结合物
公开(公告)号：WO2010096175A1
公开(公告)日：2010-08-26
申请号：PCT/US2010/000473
申请日：2010-02-19
申请人： IPSEN PHARMA S.A.S. , DEOLIVEIRA, Daniel, B. , DONG, Zheng, Xin , ZHOU, Kevin, L.
发明人： DEOLIVEIRA, Daniel, B. , DONG, Zheng, Xin , ZHOU, Kevin, L.
IPC分类号： A61K38/16
CPC分类号： C07K14/70571 , A61K38/00
摘要： There is provided a series of novel neuropeptide Y-cytotoxic conjugates, compositions comprising the same, and methods relating to their therapeutic use for the treatment of disease or condition states associated with aberrant or undesirable proliferation of cells that express NPY-Yl receptors.
摘要翻译：提供了一系列新型神经肽Y细胞毒性缀合物，包含其的组合物，以及涉及其治疗用于治疗与表达NPY-Y1受体的细胞异常或不期望的增殖相关的疾病或状况状态的方法。

3. 发明申请

WO2010096186A1 ANALOGUES OF NEUROPEPTIDE Y HAVING AT LEAST ONE SYNTHETIC AMINO ACID SUBSTITUTION 审中-公开
标题翻译：具有至少一种合成氨基酸替代物的神经元肽的模拟物
公开(公告)号：WO2010096186A1
公开(公告)日：2010-08-26
申请号：PCT/US2010/000491
申请日：2010-02-19
申请人： IPSEN PHARMA S.A.S , DONG, Zheng, Xin , ZHOU, Kevin, L. , DEOLIVEIRA, Daniel, B.
发明人： DONG, Zheng, Xin , ZHOU, Kevin, L. , DEOLIVEIRA, Daniel, B.
IPC分类号： A61K38/00
CPC分类号： C07K14/57545 , A61K38/00
摘要： The present invention relates to novel analogues of neuropeptide Y, pharmaceutical compositions containing the same, pharmaceutical formulations containing the same, and method of treating diseases or conditions mediated by neuropeptide Y-receptor binding. More particularly, the present invention relates to novel analogues of neuropeptide Y having at least one unnatural amino acid substitution, such as 4Hyp at position 34, that selectively bind to the neuropeptide Yl receptor subtype compared to the neuropeptide Y2 receptor subtype.
摘要翻译：本发明涉及神经肽Y的新型类似物，含有它们的药物组合物，含有它们的药物制剂，以及治疗由神经肽Y受体结合介导的疾病或病症的方法。更具体地，本发明涉及具有至少一种非天然氨基酸取代的神经肽Y的新型类似物，例如与34位神经肽Y 1受体亚型相比，其选择性地结合神经肽Y2受体亚型。

4. 发明申请

WO2009108364A2 ANTAGONISTIC ANALOGUES OF GHRH 审中-公开
标题翻译： GHRH的拮抗剂类似物
公开(公告)号：WO2009108364A2
公开(公告)日：2009-09-03
申请号：PCT/US2009/001279
申请日：2009-02-27
申请人： IPSEN PHARMA S.A.S. , DONG, Zheng, Xin , DEOLIVEIRA, Daniel, B.
发明人： DONG, Zheng, Xin , DEOLIVEIRA, Daniel, B.
IPC分类号： A61K38/16
CPC分类号： C07K14/60 , A61K38/00
摘要： There is provided a novel series of synthetic antagonistic analogues of hGHRH(l- 29)NH 2 (SEQ E) NO: 1). These analogues inhibit the activity of endogenous hGHRH on the pituitary GHRH receptors, and therefore prevent the release of growth hormone. The analogues also inhibit the proliferation of human cancers through a direct effect on the cancer cells. The inhibitory potencies of the new analogues result from replacement of various amino acids.
摘要翻译：提供了一系列hGHRH（1-29）NH2（SEQ ID NO：1）的合成拮抗类似物。这些类似物抑制内源性hGHRH对垂体GHRH受体的活性，因此防止生长激素的释放。类似物也通过对癌细胞的直接作用来抑制人类癌症的增殖。新类似物的抑制效力是由于各种氨基酸的替换而产生的。

5. 发明申请

WO2014070971A2 SOMATOSTATIN-DOPAMINE CHIMERIC ANALOGS 审中-公开
公开(公告)号：WO2014070971A2
公开(公告)日：2014-05-08
申请号：PCT/US2013/067661
申请日：2013-10-31
申请人： IPSEN PHARMA S.A.S. , DONG, Zheng, Xin , SHEN, Yeelana , KIM, Sun, Hyuk
发明人： DONG, Zheng, Xin , SHEN, Yeelana , KIM, Sun, Hyuk
IPC分类号： C07K14/655
CPC分类号： A61K47/64 , A61K38/00 , A61K38/31 , A61K47/55 , C07C215/52 , C07K14/655 , C07K19/00
摘要： The present invention relates to novel somatostatin-dopamine chimeric analogs and their therapeutic uses for the inhibition, prevention, and/or treatment of neoplasia, neuroendocrine tumors, Cushing's disease/syndrome, and other conditions.
摘要翻译：本发明涉及新的生长抑素 - 多巴胺嵌合类似物及其治疗用途，用于抑制，预防和/或治疗瘤形成，神经内分泌肿瘤，库兴氏病/综合征和其他病症。

6. 发明申请

WO2010016944A3 ANALOGUES OF GLUCOSE-DEPENDENT INSULINOTROPIC POLYPEPTIDE (GIP) MODIFIED AT N-TERMINAL 审中-公开
公开(公告)号：WO2010016944A3
公开(公告)日：2010-02-11
申请号：PCT/US2009/004559
申请日：2009-08-07
申请人： IPSEN PHARMA S.A.S. , DONG, Zheng, Xin
发明人： DONG, Zheng, Xin
IPC分类号： C07K14/62 , C07K14/46
摘要： There is provided a novel series of analogues of glucose-dependent insulinotropic polypeptide, pharmaceutical compositions containing said compounds, and the use of said compounds as GIP- receptor agonists or antagonists for treatment of GIP -receptor mediated conditions, such as non- insulin dependent diabetes mellitus and obesity.

7. 发明申请

WO2010016940A2 ANALOGUES OF GLUCOSE-DEPENDENT INSULINOTROPIC POLYPEPTIDE 审中-公开
标题翻译：类似于葡萄糖的胰岛素样多肽
公开(公告)号：WO2010016940A2
公开(公告)日：2010-02-11
申请号：PCT/US2009/004552
申请日：2009-08-07
申请人： IPSEN PHARMA S.A.S. , DONG, Zheng, Xin
发明人： DONG, Zheng, Xin
IPC分类号： A61K38/16
CPC分类号： C07K14/645 , A61K38/00 , C07K14/605 , C07K19/00
摘要： There is provided a novel series of analogues of glucose-dependent insulinotropic polypeptide, pharmaceutical compositions containing said compounds, and the use of said compounds as GIP- receptor agonists or antagonists for treatment of GIP -receptor mediated conditions, such as non- insulin dependent diabetes mellitus and obesity.
摘要翻译：提供了一系列新的葡萄糖依赖性促胰岛素多肽类似物，含有所述化合物的药物组合物，以及所述化合物作为GIP-受体激动剂或拮抗剂在治疗GIP-受体介导的病症中的用途如非胰岛素依赖性糖尿病和肥胖。

8. 发明申请

WO2009139855A2 PHARMACEUTICAL COMPOSITIONS OF SOMATOSTATIN-DOPAMINE CONJUGATES 审中-公开
标题翻译：生长抑素 - 多巴胺偶联物的药物组合物
公开(公告)号：WO2009139855A2
公开(公告)日：2009-11-19
申请号：PCT/US2009/002943
申请日：2009-05-12
申请人： IPSEN PHARMA S.A.S. , DONG, Zheng, Xin , ZHANG, Jundong
发明人： DONG, Zheng, Xin , ZHANG, Jundong
IPC分类号： A61K38/12
CPC分类号： A61K38/31
摘要： The present invention is directed to improvements in compositions containing a somatostatin- dopamine conjugate which retains both somatostatin and dopamine activity in vivo, methods for preparing such compositions, and method of using such compositions to treat mammals. In particular, the present invention relates to a pharmaceutical composition comprising Dop2-DLys(Dop2)- cyclo[Cys-Tyr-DTrp-Lys-Abu-Cys]-Thr-NH 2 (SEQ ID NO: 1), in which the somatostatin-dopamine conjugate precipitates in vivo at physiological pH to form an in situ deposit that is slowly dissolved and released into the body fluid and bloodstream. The present invention may further comprise an organic component such as dimethylacetamide (DMA) or polyethylene glycol with an average molecular weight of 400 (PEG400).
摘要翻译：本发明涉及含有生长激素抑制素 - 多巴胺缀合物的组合物的改进，所述组合物在体内既保留生长激素抑制素又保持多巴胺活性，制备所述组合物的方法以及使用所述组合物治疗哺乳动物的方法。具体而言，本发明涉及包含Dop2-DLys（Dop2） - 环[Cys-Tyr-DTrp-Lys-Abu-Cys] -Thr-NH2（SEQ ID NO： 1），其中生长激素抑制素 - 多巴胺缀合物在生理pH下在体内沉淀以形成缓慢溶解并释放到体液和血流中的原位沉积物。本发明可进一步包含有机组分，如二甲基乙酰胺（DMA）或平均分子量为400的聚乙二醇（PEG400）。

9. 发明申请

WO2011011071A2 ANALOGUES OF INSULIN-LIKE GROWTH FACTOR-1 (IGF-1) 审中-公开
标题翻译：类胰岛素生长因子-1（IGF-1）类似物
公开(公告)号：WO2011011071A2
公开(公告)日：2011-01-27
申请号：PCT/US2010/002061
申请日：2010-07-22
申请人： IPSEN PHARMA S.A.S. , DONG, Zheng, Xin , PRAIRIE, Nicholas, C. , ZHANG, Jundong , COMSTOCK, Jeanne, Mary
发明人： DONG, Zheng, Xin , PRAIRIE, Nicholas, C. , ZHANG, Jundong , COMSTOCK, Jeanne, Mary
IPC分类号： C07K14/65
CPC分类号： C07K14/65
摘要： There is provided a novel series of analogues of insulin-like growth factor- 1 as defined herein, pharmaceutical compositions containing said analogues, and the use of said analogues for treatment of IGF-I -receptor mediated conditions, such as short stature, diabetes therapy, neurodegenerative disease treatment, and cartilage repair.
摘要翻译：本文提供了一系列如本文所定义的胰岛素样生长因子-1类似物，含有所述类似物的药物组合物，以及所述类似物用于治疗IGF-1受体介导的病症的用途，如身材矮小，糖尿病治疗，神经退行性疾病治疗和软骨修复。

10. 发明申请

WO2008147556A2 MELANOCORTIN RECEPTOR LIGANDS MODIFIED WITH HYDANTOIN 审中-公开
标题翻译：梅兰康汀受体配体用HYDANTOIN修饰
公开(公告)号：WO2008147556A2
公开(公告)日：2008-12-04
申请号：PCT/US2008/006675
申请日：2008-05-23
申请人： SOCIETE DE CONSEILS DE RECHERCHES ET D'APPLICATIONS SCIENTIFIQUES S.A.S. , DONG, Zheng, Xin , DEOLIVEIRA, Daniel, B. , COMSTOCK, Jeanne, Mary
发明人： DONG, Zheng, Xin , DEOLIVEIRA, Daniel, B. , COMSTOCK, Jeanne, Mary
IPC分类号： A61K38/12
CPC分类号： C07K7/06 , A61K38/00 , C07K7/56 , C07K14/68
摘要： The present invention relates to peptide ligands of the melanocortin receptors, in particular the melancortin-4 receptor, and as such, are useful in the treatment of disorders responsive to the activation of this receptor, such as obesity, diabetes mellitus and sexual dysfunction.
摘要翻译：本发明涉及黑皮质素受体，特别是melancortin-4受体的肽配体，因此可用于治疗对该受体的活化（如肥胖症，糖尿病和性功能障碍）有反应的病症。

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