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11. 发明申请

WO2011115871A1 PHARMACEUTICAL COMPOSITIONS OF GROWTH HORMONE SECRETAGOGUE RECEPTOR LIGANDS 审中-公开
标题翻译：生长激素分泌受体配体的药物组合物
公开(公告)号：WO2011115871A1
公开(公告)日：2011-09-22
申请号：PCT/US2011/028283
申请日：2011-03-14
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： A61K38/08 , A61K38/04
CPC分类号： A61K38/1796 , A61K9/0024 , A61K9/08 , A61K38/08 , A61K47/02 , A61K47/10 , C07K5/06 , C07K5/08 , C07K5/10 , C07K7/06
摘要： The present invention relates to improvements in compositions containing peptides that are ligands of the GHS receptor, or pharmaceutically acceptable salts thereof, methods for preparing such compositions, and methods of using such compositions to treat mammals. In particular, the present invention relates to a pharmaceutical composition comprising a pamoate salt of H-Inp-D-Bal-D-Trp-Phe-Apc-NH2, which is a ligand of the GHS receptor and in which, after subcutaneous or intramuscular administration to a subject, the peptide forms an in situ depot at physiological pH 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 lower than 1000.
摘要翻译：本发明涉及包含作为GHS受体的配体的肽或其药学上可接受的盐的组合物的组合物的改进，以及制备该组合物的方法，以及使用这些组合物治疗哺乳动物的方法。特别地，本发明涉及包含作为GHS受体的配体的H-Inp-D-Bal-D-Trp-Phe-Apc-NH2的双羟萘酸盐的药物组合物，其中皮下或肌内给予受试者，肽在生理pH下形成原位贮藏，其缓慢溶解并释放到体液和血流中。本发明还可以包含平均分子量低于1000的有机组分如二甲基乙酰胺（DMA）或聚乙二醇。

12. 发明申请

WO2011011073A1 SITE-SPECIFIC PEGYLATED OR SITE-SPECIFIC LIPIDATED IGF-1 AND ANALOGUES OF IGF-1 审中-公开
标题翻译： IGF-1的特异性聚乙二醇酸或特异性脂质体IGF-1和模拟物
公开(公告)号：WO2011011073A1
公开(公告)日：2011-01-27
申请号：PCT/US2010/002063
申请日：2010-07-22
申请人： IPSEN PHARMA S.A.S. , DONG, Zheng, Xin , PRAIRIE, Nicholas, C. , EYNON, John, S.
发明人： DONG, Zheng, Xin , PRAIRIE, Nicholas, C. , EYNON, John, S.
IPC分类号： C07K14/475 , C07K14/62
CPC分类号： C07K14/65 , A61K38/00 , A61K47/60
摘要： The present invention relates to novel site-specific pegylated or site-specific lipidated IGF-1 and analogues of IGF-1, e.g., [2-(ethoxyimino(2-carbamate-20K branched PEG))acetyl-Gly 1 , Asn 59 ]hIGF-1(1 -7O)-OH (SEQ ID NO: 106) and [2-(n- octadecoxyimino)acetyl-Gly 1 , Asn 59 ]hIGF- 1 ( 1 -7O)-OH (SEQ ID NO: 109), and the use of said compounds for treatment of IGF-1 -receptor mediated conditions, such as short stature, diabetes therapy, neurodegenerative disease treatment, and cartilage repair. The site- specifically modified IGF-1 and analogues of IGF-1 according to the present invention have improved pharmacokinetic profile, improved biological activity, and/or decreased immunogenicity.
摘要翻译：本发明涉及新的位点特异性聚乙二醇化或位点特异性脂质化IGF-1和IGF-1的类似物，例如[2-（乙氧基亚氨基（2-氨基甲酸酯-20K支化PEG））乙酰基-Gly1，Asn59] hIGF- 1（1-70）-OH（SEQ ID NO：106）和[2-（正十八烷氧基亚氨基）乙酰基-Gly1，Asn59] hIGF-1（1-70）-OH（SEQ ID NO：109）所述化合物用于治疗IGF-1受体介导的病症，例如身材矮小，糖尿病治疗，神经变性疾病治疗和软骨修复。根据本发明的位点特异性修饰的IGF-1和IGF-1的类似物具有改善的药代动力学特征，改善的生物学活性和/或降低的免疫原性。

13. 发明申请

WO2011011072A2 ANALOGUES OF INSULIN-LIKE GROWTH FACTOR-1 (IGF-1) HAVING AMINO ACID SUBSTITUTION AT POSITION 59 审中-公开
标题翻译：胰岛素样生长因子-1（IGF-1）类似物氨基酸置换59
公开(公告)号：WO2011011072A2
公开(公告)日：2011-01-27
申请号：PCT/US2010/002062
申请日：2010-07-22
申请人： IPSEN PHARMA S.A.S. , DONG, Zheng, Xin , PRAIRIE, Nicholas, C. , UFRET, Maria, L. , ZHANG, Jundong , ROTHMAN, Deborah , COMSTOCK, Jeanne, Mary
发明人： DONG, Zheng, Xin , PRAIRIE, Nicholas, C. , UFRET, Maria, L. , ZHANG, Jundong , ROTHMAN, Deborah , COMSTOCK, Jeanne, Mary
IPC分类号： C07K14/65
CPC分类号： C07K14/65
摘要： The present invention relates to novel analogues of insulin-like growth factor- 1 (IGF- 1), pharmaceutical compositions containing said analogues, and the use of said analogues for treatment of IGF-1 -receptor mediated conditions, such as short stature, diabetes therapy, neurodegenerative disease treatment, and cartilage repair. More particularly, the present invention relates to novel analogues of IGF-I having an amino acid substitution at position 59, e.g., (Asn 59 )hIGF- 1(1 -7O)-OH (SEQ ID NO: 1), and other substitution(s) as defined herein.
摘要翻译：本发明涉及胰岛素样生长因子-1（IGF-1）的新型类似物，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。更具体地说，本发明涉及在位置59具有氨基酸取代的新型IGF-I类似物，例如（Asn 59）hIGF-1（1-7）-OH（SEQ ID NO ：1）和本文定义的其他替代物。

14. 发明申请

WO2010016938A3 GLUCOSE-DEPENDENT INSULINOTROPIC POLYPEPTIDE ANALOGUES 审中-公开
公开(公告)号：WO2010016938A3
公开(公告)日：2010-02-11
申请号：PCT/US2009/004550
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： A61K38/00
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.

15. 发明申请

WO2014070965A3 SOMATOSTATIN ANALOGS AND DIMERS THEREOF 审中-公开
公开(公告)号：WO2014070965A3
公开(公告)日：2014-05-08
申请号：PCT/US2013/067651
申请日：2013-10-31
申请人： IPSEN PHARMA S.A.S , DONG, Zheng, Xin , FERRANDIS, Eric
发明人： DONG, Zheng, Xin , FERRANDIS, Eric
IPC分类号： A61K38/00
摘要： The present invention relates to novel somatostatin analogs, dimers thereof, and methods of using the same to treat various diseases. Naturally occurring somatostatins (SSTs), which are also known as somatotropin release-inhibiting factors (SRIFs), have diverse biological effects in many cells and organs 10 throughout the body. They are produced by normal endocrine, gastrointestinal, immune and neuronal cells, as well as by certain tumors (Patel, Y. C, Frontiers in Neuroendocrinology, 20(3): 157-198 (1999); Froidevaux, et al., Biopolymers, 66(3): 161-83 (2002)).

16. 发明申请

WO2010096188A3 ANALOGUES OF NEUROPEPTIDE Y HAVING PROLINE SUBSTITUTION AT POSITION 34 审中-公开
公开(公告)号：WO2010096188A3
公开(公告)日：2010-08-26
申请号：PCT/US2010/000493
申请日：2010-02-19
申请人： IPSEN PHARMA S.A.S , DONG, Zheng, Xin
发明人： DONG, Zheng, Xin
IPC分类号： A61K38/16
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 proline substitution at position 34 and other substitution(s) as defined herein that selectively bind to the neuropeptide Yl receptor subtype compared to the neuropeptide Y2 receptor subtype.

17. 发明申请

WO2010016936A1 PHARMACEUTICAL COMPOSITIONS OF 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模拟物的药物组合物
公开(公告)号：WO2010016936A1
公开(公告)日：2010-02-11
申请号：PCT/US2009/004545
申请日：2009-08-07
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： A61K38/00
CPC分类号： A61K38/28
摘要： The present invention relates to improvements in compositions containing an analogue of glucose-dependent insulinotropic polypeptide or pharmaceutical salts thereof, and the use of such compositions for treatment of GIP-receptor mediated conditions, such as non-insulin dependent diabetes mellitus and obesity. In particular, the present invention relates to a pharmaceutical composition of a clear aqueous solution, or a gel or a semi-solid, comprising the native GIP, a fragment thereof, an analogue of GIP, or a pharmaceutically acceptable salt thereof (which are collectively referred to as "GIP peptide" or "GIP compound"), and a divalent metal or divalent metal salt component such as ZnCl 2 or ZnAc 2 , in which the clear aqueous solution of the GIP peptide precipitates in vivo at physiological pH to form an in situ deposit that is slowly dissolved and released into the body fluid and bloodstream.
摘要翻译：本发明涉及包含葡萄糖依赖性促胰岛素多肽类似物或其药用盐的组合物的改进，以及这些组合物用于治疗GIP受体介导的病症如非胰岛素依赖性糖尿病和肥胖症的用途。特别地，本发明涉及包含天然GIP，其片段，GIP的类似物或其药学上可接受的盐（它们共同地组合）的透明水溶液或凝胶或半固体的药物组合物称为“GIP肽”或“GIP化合物”）和二价金属或二价金属盐组分如ZnCl 2或ZnAc 2，其中GIP肽的透明水溶液在体内在生理pH下沉淀形成原位沉积物缓慢溶解并释放到体液和血液中。

18. 发明申请

WO2004093807A2 SOMATOSTATIN VECTORS 审中-公开
公开(公告)号：WO2004093807A2
公开(公告)日：2004-11-04
申请号：PCT/US2004/012200
申请日：2004-04-21
申请人： SOCIETE DE CONSEILS DE RECHERCHES ET D'APPLICATIONS SCIENTIFIQUES S.A.S. , DONG, Zheng, Xin , SHEN, Yeelana , COMSTOCK, Jeanne, Mary , KIM, Sun, H.
发明人： DONG, Zheng, Xin , SHEN, Yeelana , COMSTOCK, Jeanne, Mary , KIM, Sun, H.
IPC分类号： A61K
CPC分类号： C07K14/655 , A61K38/00 , A61K47/64 , C07K7/086 , C07K7/23 , C07K14/6555
摘要： The invention features targeted cytotoxic compounds and methods relating to their therapeutic use for the treatment of neoplasia and other conditions.
摘要翻译：本发明的特征在于靶向的细胞毒性化合物和与其用于治疗瘤形成和其他病症的治疗用途有关的方法。

19. 发明申请

WO2007038678A2 ANALOGS OF GHRELIN 审中-公开
标题翻译： GHRELIN的模拟
公开(公告)号：WO2007038678A2
公开(公告)日：2007-04-05
申请号：PCT/US2006/037889
申请日：2006-09-27
申请人： SOCIETE DE CONSEILS DE RECHERCHES ET D'APPLICATIONS SCIENTIFIQUES S.A.S. , DONG, Zheng, Xin , CULLER, Michael, DeWitt , SHEN, Yeelana , COMSTOCK, Jeanne, Mary
发明人： DONG, Zheng, Xin , CULLER, Michael, DeWitt , SHEN, Yeelana , COMSTOCK, Jeanne, Mary
IPC分类号： A61K38/22
CPC分类号： C07K14/60 , A61K38/00 , G01N2500/00 , Y02A50/463 , Y02A50/475
摘要： The invention comprises peptidyl analogs according to formulae (I) or (II) as depicted below: (R 2 R 3 )-A 1 -A 2 -A 3 -A 4 -A 5 -A 6 -A 7 -A 8 -A 9 -A 10 -A 11 -A 12 -A 13 -A 14 -A 15 -A 16 -A 17 -A 18 -A 19 -A 20 -A 21 -A 22 -A 23 -A 24 -A 25 -A 26 -A 27 -A 28 -R 1 wherein the definitions of A 1 to A 28 and R 1 to R 3 are provided for in the specification for each of formulae (I) and (II), pharmaceutically acceptable salts thereof and pharmaceutical compositions comprising an effective amount of a compound of formula (I), that possess agonist or antagonist ghrelin activity, along with therapeutic and non-therapeutic uses thereof.
摘要翻译：本发明包括如下所述的式（I）或（II）的肽基类似物：（R 2）3 - A ^{2 -A ^{3 -A ^{4 -A ^{5 -A ^{6 - A ^{7 -A ^{8 -A ^{9 -A ^{10 -A ^{11 - A ^{12 -A ^{13 -A ^{14 -A ^{15 -A ^{16 - A ^{17 -A ^{18 -A ^{19 -A ^{20 -A ^{21 - A ^{22 -A ^{23 -A ^{24 -A ^{25 -A ^{26 - 其中A 1至A 28的定义为：A 在式（I）和（II）中的每一个的说明书中提供了R 0和R 1至R 3，其药学上可接受的盐和包含有效的具有激动剂或拮抗性生长素释放肽活性的式（I）化合物的量以及其治疗和非治疗用途。}}}}}}}}}}}}}}}}}}}}}}}}}

20. 发明申请

WO2008051421A2 PEPTIDE-CYTOTOXIC CONJUGATES 审中-公开
标题翻译：肽类 - 细胞毒素结合蛋白
公开(公告)号：WO2008051421A2
公开(公告)日：2008-05-02
申请号：PCT/US2007/022179
申请日：2007-10-17
申请人： SOCIETE DE CONSEILS DE RECHERCHES ET D'APPLICATIONS SCIENTIFIQUES S.A.S. , DONG, Zheng, Xin , SHEN, Yeelana , CULLER, Michael, Dewitt , THURIEAU, Christophe, Alain
发明人： DONG, Zheng, Xin , SHEN, Yeelana , CULLER, Michael, Dewitt , THURIEAU, Christophe, Alain
IPC分类号： A61K38/12
CPC分类号： C07K14/655 , A61K38/00 , C07D491/22
摘要： The invention features targeted cytotoxic compounds and methods relating to their therapeutic use for the treatment of neoplasia and other conditions.
摘要翻译：本发明的特征在于靶向的细胞毒性化合物和与其用于治疗瘤形成和其他病症的治疗用途有关的方法。

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