公开(公告)号：US06482797B1

公开(公告)日：2002-11-19

申请号：US09719573

申请日：2001-01-30

申请人： Vincent Dive ,  Joël Cotton ,  Philippe Cuniasse ,  Athanasios Yiotakis ,  Pierre Corvol ,  Annie Michaud ,  Marie-Thérèse Chauvet ,  Joël Menard ,  Eric Ezan

发明人： Vincent Dive ,  Joël Cotton ,  Philippe Cuniasse ,  Athanasios Yiotakis ,  Pierre Corvol ,  Annie Michaud ,  Marie-Thérèse Chauvet ,  Joël Menard ,  Eric Ezan

IPC分类号： A61K3800

CPC分类号： C07F9/301 ,  C07F9/572

摘要： The invention relates to peptide derivatives that can be used as selective inhibitors of the N-terminal site of human angiotensin-converting enzyme. The derivatives comprise the amino acid sequence with the following formula: -Asp-Phe-&PSgr;(PO2CH2)-Ala-Xaa′-  (I) wherein: &PSgr;(PO2CH2) indicates that the peptide bond (CONH) between Phe and Ala has been replaced by the phosphonic bond PO2CH2, and Xaa′ represents an amino acid residue. They can be used in pharmaceutical formulations, particularly to protect haematopoietic strain cells of patients undergoing aggressive chemotherapy or radiotherapy treatment.

摘要翻译： 本发明涉及可用作人血管紧张素转换酶的N-末端位点的选择性抑制剂的肽衍生物。该衍生物包含具有下式的氨基酸序列：其中：＆amp; PSgr;（PO2CH2）表示肽键 Phe和Ala之间的（CONH）已被膦酸键PO2CH2代替，Xaa'代表氨基酸残基。它们可用于药物制剂，特别是用于保护接受侵袭性化疗或放疗治疗的患者的造血细胞株。

公开(公告)号：US07541157B2

公开(公告)日：2009-06-02

申请号：US10514562

申请日：2003-05-28

申请人： Vincent Dive ,  André Menez ,  Reto Stocklin ,  Bertrand Tavitian ,  Fabrice Beau ,  Bertrand Czarny ,  Joël Cotton

发明人： Vincent Dive ,  André Menez ,  Reto Stocklin ,  Bertrand Tavitian ,  Fabrice Beau ,  Bertrand Czarny ,  Joël Cotton

IPC分类号： G01N33/53 ,  C40B50/06

CPC分类号： C07K5/1027 ,  G01N33/5082

摘要： The invention relates to an amplification-free method of screening groups of radioactive molecules, comprising at least the following steps: (1) the group of molecules is administered to at least one animal; (2) at least one of the animals is slaughtered and the tissue distribution of the radioactivity of the molecules administered is analyzed in vivo; (3) sections of tissue or organs in which a radioactivity signal is detected are selected; (4) radioactive fractions from the sections of tissue or organs are isolated using suitable techniques such as chromatography and/or extraction techniques; and (5) the molecule(s) from the radioactive fractions obtained in step 4 are characterized using suitable analysis techniques such as chromatography and/or mass spectrometry.

摘要翻译： 本发明涉及筛选放射性分子组的无扩增方法，该方法至少包括以下步骤：（1）向至少一种动物施用分子组; （2）屠宰至少一只动物，并在体内分析给予的分子的放射性的组织分布; （3）选择检测放射性信号的组织或器官的部分; （4）使用合适的技术如色谱和/或提取技术分离来自组织或器官切片的放射性级分; 和（5）来自步骤4中获得的放射性级分的分子使用合适的分析技术如色谱和/或质谱鉴定。