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1.发明申请CYTOTOXIC CONJUGATES HAVING NEUROPEPTIDE Y RECEPTOR BINDING COMPOUND 审中-公开具有神经元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
Applicant: IPSEN PHARMA S.A.S. , DEOLIVEIRA, Daniel, B. , DONG, Zheng, Xin , ZHOU, Kevin, L.
Inventor： DEOLIVEIRA, Daniel, B. , DONG, Zheng, Xin , ZHOU, Kevin, L.
IPC: A61K38/16
CPC classification number: C07K14/70571 , A61K38/00
Abstract: 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.
Abstract translation: 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。
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公开(公告)号：WO2010016940A3
公开(公告)日：2010-04-15
申请号：PCT/US2009004552
申请日：2009-08-07
Applicant: IPSEN PHARMA SAS , DONG ZHENG XIN
Inventor： DONG ZHENG XIN
CPC classification number: C07K14/645 , A61K38/00 , C07K14/605 , C07K19/00
Abstract: 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.
Abstract translation: 提供了一系列葡萄糖依赖性促胰岛素多肽的类似物，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用于治疗GIP受体介导的病症例如非胰岛素依赖型糖尿病 恶心和肥胖。
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3.发明申请
公开(公告)号：WO2010016935A3
公开(公告)日：2010-04-08
申请号：PCT/US2009004543
申请日：2009-08-07
Applicant: IPSEN PHARMA SAS , DONG ZHENG XIN , SHEN YEELANA , DEOLIVEIRA DANIEL B
Inventor： DONG ZHENG XIN , SHEN YEELANA , DEOLIVEIRA DANIEL B
IPC: A61K38/00
CPC classification number: C07K14/605 , A61K38/00
Abstract: 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.
Abstract translation: 提供了葡萄糖依赖性促胰岛素多肽的类似物的新系列，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用于治疗GIP-受体介导的病症例如非胰岛素依赖性糖尿病 恶心和肥胖。
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4.发明申请ANALOGUES OF GLUCOSE-DEPENDENT INSULINOTROPIC POLYPEPTIDE (GIP) MODIFIED AT N-TERMINAL 审中-公开葡萄糖依赖性胰岛素多肽（GIP）在N-末端修饰的模拟物
公开(公告)号：WO2010016944A2
公开(公告)日：2010-02-11
申请号：PCT/US2009004559
申请日：2009-08-07
Applicant: IPSEN PHARMA SAS , DONG ZHENG XIN
Inventor： DONG ZHENG XIN
IPC: A61K38/16
CPC classification number: C07K14/001 , A61K38/00 , A61K38/16 , A61K47/60 , C07K14/605
Abstract: 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.
Abstract translation: 提供了葡萄糖依赖性促胰岛素多肽的类似物的新系列，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用于治疗GIP受体介导的病症例如非胰岛素依赖型糖尿病 恶心和肥胖。
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5.发明申请METHOD FOR INHIBITING INFLAMMATION AND PRE-INFLAMMATORY CYTOKINE/CHEMOKINE EXPRESSION USING A GHRELIN ANALOGUE 审中-公开使用GHRELIN模拟物抑制炎症和预炎性细胞因子/趋化因子表达的方法
公开(公告)号：WO2009020643A3
公开(公告)日：2009-12-30
申请号：PCT/US2008009494
申请日：2008-08-07
Applicant: IPSEN PHARMA SAS , DONG ZHENG XIN , TAYLOR JOHN E , CULLER MICHAEL DEWITT , DATTA RAKESH
Inventor： DONG ZHENG XIN , TAYLOR JOHN E , CULLER MICHAEL DEWITT , DATTA RAKESH
IPC: A61K39/395
Abstract: The present invention provides a method of ameliorating inflammation, inhibiting proinflammatory cytokine and/or chemokine expression and treating various diseases and/or conditions incidental to the onset of inflammation, in a subject in need of treatment for such conditions, by administering select analogues of native hGhrelin.
Abstract translation: 本发明提供了在需要治疗此类病症的受试者中改善炎症，抑制促炎细胞因子和/或趋化因子表达以及治疗与炎症发作相关的各种疾病和/或病症的方法，其通过施用选择性的天然 hGhrelin。
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Patent Agency Ranking6.发明申请METHODS AND INTERMEDIATES FOR CHEMICAL SYNTHESIS OF POLYPEPTIDES AND PROTEINS 审中-公开化学合成多肽和蛋白质的方法与中间体
公开(公告)号：WO2009032181A3
公开(公告)日：2009-04-23
申请号：PCT/US2008010226
申请日：2008-08-28
Applicant: SOD CONSEILS RECH APPLIC , DONG ZHENG XIN , KIM SUN H
Inventor： DONG ZHENG XIN , KIM SUN H
Abstract: The present invention relates to methods and intermediates for chemical synthesis of polypeptides and proteins, and more particularly to methods and intermediates for chemically ligating a peptide fragment containing N-terminal ß-methyl-cysteine (SEQ ID NO: 1) with another peptide fragment having C-terminal thioester to generate a ß-amino-thioester intermediate that spontaneously rearranges to form an amide bond. The invention also relates to methods of synthesizing ß-methyl-cysteine (SEQ ID NO: 1) and its protected forms. Furthermore, the invention relates to converting a ß-methyl-thiazolidine residue to a ß-methyl-cysteine (SEQ ID NO: 1) residue of polypeptides and proteins.
Abstract translation: 本发明涉及用于化学合成多肽和蛋白质的方法和中间体，更具体地涉及用于化学连接含有N-末端β-甲基半胱氨酸（SEQ ID NO：1）的肽片段与另一个具有 C末端硫代酯以产生自发重排形成酰胺键的β-氨基 - 硫酯中间体。 本发明还涉及合成β-甲基半胱氨酸（SEQ ID NO：1）及其受保护形式的方法。 此外，本发明涉及将β-甲基 - 噻唑烷残基转化成多肽和蛋白质的β-甲基 - 半胱氨酸（SEQ ID NO：1）残基。
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公开(公告)号：WO2008039415A3
公开(公告)日：2008-11-13
申请号：PCT/US2007020595
申请日：2007-09-24
Applicant: SOD CONSEILS RECH APPLIC , DONG ZHENG XIN
Inventor： DONG ZHENG XIN
Abstract: The invention comprises peptidyl analogs of ghrelin having greater stability which are active at the GHS receptor according to formulae depicted below: (R2)-A1-A2-A3-A4-A5-A6-A7-A8-A9-A10-A11-A12-A13-A14-A15-A16-A17-A18-A19-A20-A21-A22- A23-A24-A25-A26-A27-A28-R1 wherein the definitions of A1 to A28, R1 and R2 are provided for in the specification, with the exception that the N-terminal amino acid must be selected from the group consisting of Inp, 1-Apc and 4-Apc, the pharmaceutically acceptable salts thereof and pharmaceutical compositions comprising an effective amount of said compound together with therapeutic and non-therapeutic uses thereof.
Abstract translation: （R 2）-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 1 -A 7 -A 8 -A 9 -A 10 -A 11 -A 12 -A13-A14-A15-A16-A17-A18-A19-A20-A21-A22-A23-A24-A25-A26-A27-A28-R1其中A1至A28，R1和R2的定义在 除N末端氨基酸必须选自由Inp，1-Apc和4-Apc组成的组外，其药学上可接受的盐和药物组合物包含有效量的所述化合物以及治疗性和非治疗性 - 其治疗用途。
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公开(公告)号：WO2007139997A2
公开(公告)日：2007-12-06
申请号：PCT/US2007012621
申请日：2007-05-25
Applicant: SOD CONSEILS RECH APPLIC , DONG ZHENG XIN , EYNON JOHN S
Inventor： DONG ZHENG XIN , EYNON JOHN S
IPC: C07K14/47
CPC classification number: C07K1/1077 , A61K47/60 , C08G65/329 , C08G65/334 , C08G65/3348
Abstract: The present invention relates to methods for the chemo-selective pegylation of the cysteine residue having unoxidized sulfhydryl side-chain and free a-amino group in proteins, peptides and other molecules. Similar methods are provided for the chemo- selective pegylation of the homocysteine, selenocysteine, penicillamine, and N-methyl- cysteine residues.
Abstract translation: 本发明涉及在蛋白质，肽和其他分子中具有未氧化巯基侧链和游离α-氨基的半胱氨酸残基的化学选择性聚乙二醇化的方法。 提供了类似的方法，用于同型半胱氨酸，硒代半胱氨酸，青霉胺和N-甲基 - 半胱氨酸残基的化学选择性聚乙二醇化。
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公开(公告)号：WO2007041278B1
公开(公告)日：2007-12-06
申请号：PCT/US2006038027
申请日：2006-09-28
Applicant: SOD CONSEILS RECH APPLIC , DATTA RAKESH , DONG ZHENG XIN
Inventor： DATTA RAKESH , DONG ZHENG XIN
CPC classification number: C07K14/575 , A61K38/00 , A61K38/25 , C07K14/60
Abstract: The present invention relates to a method of treating a transient impairment of the motility of the gastrointestinal system resulting from postoperative ileus in a patient wherein said method includes the step of administering a therapeutically effective amount of a peptidyl analog of ghrelin to said patient.
Abstract translation: 本发明涉及一种治疗由患者术后肠梗阻引起的胃肠系统的运动性的瞬时损伤的方法，其中所述方法包括向所述患者施用治疗有效量的生长素释放肽的肽基类似物的步骤。
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公开(公告)号：WO2007014258A3
公开(公告)日：2007-12-06
申请号：PCT/US2006029002
申请日：2006-07-24
Applicant: SOD CONSEILS RECH APPLIC , DONG ZHENG XIN , EYNON JOHN S , SHEN YEELANA
Inventor： DONG ZHENG XIN , EYNON JOHN S , SHEN YEELANA
CPC classification number: C07K14/72 , C07K5/06026 , C07K5/06086
Abstract: A family of peptides and peptidomimetic compounds useful as GHS analogs according to either formula (I) or (II) as depicted below: or a pharmaceutically acceptable salts thereof, wherein the variables are as defined in the specification.
Abstract translation: 可用作如下所述的式（I）或（II）的GHS类似物的肽和拟肽化合物家族：或其药学上可接受的盐，其中变量如说明书中所定义。
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