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1. 发明申请

US20120309674A1 PSEUDODIPEPTIDES AS MMP INHIBITORS 有权
标题翻译：作为MMP抑制剂的PSEUDODIPEPTIDES
公开(公告)号：US20120309674A1
公开(公告)日：2012-12-06
申请号：US13392358
申请日：2010-08-26
申请人： Laurent Devel , Fabrice Beau , Bertrand Czarny , Vincent Dive
发明人： Laurent Devel , Fabrice Beau , Bertrand Czarny , Vincent Dive
IPC分类号： C07K5/097 , C07D261/08 , A61K38/05 , C07D211/34 , C07C229/42 , A61P9/10 , C07D333/24 , A61P35/00 , A61P29/00 , A61P11/00 , A61P19/02 , A61K38/06 , C07D409/12
CPC分类号： C07D261/08 , C07D207/327 , C07D231/12 , C07D237/10 , C07D237/12 , C07D239/26 , C07D277/30 , C07D277/66 , C07D285/06 , C07D333/24
摘要： The invention relates to compounds, in particular MMP inhibitors. The compounds of the invention have formula (1). The invention can be used in particular in the pharmaceutical field. The present invention also relates to labeled compounds of formula (2), and to the use thereof as contrast agents for detecting extracellular matrix metalloproteinases.
摘要翻译：本发明涉及化合物，特别是MMP抑制剂。本发明的化合物具有式（1）。本发明特别可用于制药领域。本发明还涉及标记的式（2）化合物及其作为检测细胞外基质金属蛋白酶的造影剂的用途。

2. 发明授权

US08691753B2 Pseudodipeptides as MMP inhibitors 有权
标题翻译：伪二肽作为MMP抑制剂
公开(公告)号：US08691753B2
公开(公告)日：2014-04-08
申请号：US13392358
申请日：2010-08-26
申请人： Laurent Devel , Fabrice Beau , Bertrand Czarny , Vincent Dive
发明人： Laurent Devel , Fabrice Beau , Bertrand Czarny , Vincent Dive
IPC分类号： A61K38/00 , A61P9/10 , C07K14/47 , C07D409/00
CPC分类号： C07D261/08 , C07D207/327 , C07D231/12 , C07D237/10 , C07D237/12 , C07D239/26 , C07D277/30 , C07D277/66 , C07D285/06 , C07D333/24
摘要： The invention relates to compounds, in particular MMP inhibitors. The compounds of the invention have formula (1). The invention can be used in particular in the pharmaceutical field. The present invention also relates to labeled compounds of formula (2), and to the use thereof as contrast agents for detecting extracellular matrix metalloproteinases.
摘要翻译：本发明涉及化合物，特别是MMP抑制剂。本发明的化合物具有式（1）。本发明特别可用于制药领域。本发明还涉及标记的式（2）化合物及其作为检测细胞外基质金属蛋白酶的造影剂的用途。

3. 发明申请

US20060228296A1 Method of screening groups of radioactive molecules and applications thereof 失效
标题翻译：筛选放射性分子组的方法及其应用
公开(公告)号：US20060228296A1
公开(公告)日：2006-10-12
申请号：US10514562
申请日：2003-05-28
申请人： Vincent Dive , Andre Menez , Reto Stocklin , Bertrand Tavitian , Fabrice Beau , Bertrand Czarny , Joel Cotton
发明人： Vincent Dive , Andre Menez , Reto Stocklin , Bertrand Tavitian , Fabrice Beau , Bertrand Czarny , Joel Cotton
IPC分类号： A61K51/00 , C40B30/06
CPC分类号： C07K5/1027 , G01N33/5082
摘要： The invention relates to an amplification-free method of screening groups of radioactive molecules, the products from the molecule groups obtained and the application thereof in order to identify molecules that are capable of binding selectively to a tissue or a particular organ. The inventive method can be used for the development of novel therapeutic compounds and contrast agents for medical imaging and for the screening of medicaments. Said method of screening a group of molecules is characterised in that it comprises at least the following steps: (1) the group of molecules is administered to at least one animal, each molecule being marked first by a suitable radioactive isotope; (2) at least one of the animals is slaughtered and the tissue distribution of the radioactivity of the molecules administered is analysed from sections of tissue or organs taken using suitable imaging devices; (3) sections of tissue or organs in which a radioactivity signal is detected are selected; (4) radioactive fractions from the aforementioned sections of tissue or organs selected during step 3 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 characterised using suitable analysis techniques such as chromatography and/or mass spectrometry. According to one variation of the method, in step 2, where possible, the tissue distribution of the radioactivity of the molecules administered is analysed in vivo using suitable imaging devices from a biological sample which is pre-extracted and selected from the group containing cells and sections of tissue or organs. As a result, said variation does not require the animal to be slaughtered.
摘要翻译：本发明涉及一种无扩增方法，用于筛选放射性分子组，所获得的分子组的产物及其应用，以鉴定能够选择性结合组织或特定器官的分子。本发明的方法可用于开发用于医学成像和药物筛选的新型治疗化合物和造影剂。筛选一组分子的所述方法的特征在于其至少包括以下步骤：（1）向至少一种动物施用分子组，每个分子首先由合适的放射性同位素标记; （2）屠宰至少一只动物，并从使用合适的成像装置取出的组织或器官的部分分析施用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步骤3中选择的组织或器官的前述部分的放射性级分; 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。根据该方法的一个变体，在步骤2中，在可能的情况下，使用来自生物样品的合适的成像装置在体内分析施用的分子的放射性的组织分布，所述生物样品被预先提取并选自含有细胞的组和组织或器官的部分。因此，所述变体不需要屠宰动物。

4. 发明授权

US07541157B2 Method of screening groups of radioactive molecules and applications thereof 失效
标题翻译：筛选放射性分子组的方法及其应用
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。

5. 发明授权

US06630501B1 Phosphinic pseudo-peptides that may be used as matrix zinc metalloprotease inhibitors 失效
标题翻译：可用作基质锌金属蛋白酶抑制剂的磷化假性肽
公开(公告)号：US06630501B1
公开(公告)日：2003-10-07
申请号：US09869303
申请日：2002-03-25
申请人： Vincent Dive , Philippe Cuniasse , Marie-Christine Rio , Paul Basset , Athanasios Yotakis , Fabrice Beau , Stamania Vassiliou
发明人： Vincent Dive , Philippe Cuniasse , Marie-Christine Rio , Paul Basset , Athanasios Yotakis , Fabrice Beau , Stamania Vassiliou
IPC分类号： A61K31404
CPC分类号： C07F9/65586 , C07F9/301 , C07F9/5728 , C07F9/65583
摘要： The invention relates to pseudo-peptides according to the formula: wherein R1 is a group inhibiting an amine function, or an amino acid residue or peptide with an inhibited terminal amino function, R2 represents the lateral chain of a natural or non-natural amino acid, R3 represents: 1) the lateral chain of a natural amino acid except for Gly and Ala, not substituted or substituted by an aryl group, 2) an aralkyl group, or 3) an alkyl group comprising at least 3 carbon atoms, and R4 represents a lateral chain of natural or non-natural amino acid. They are useful as matrix zinc metalloprotease inhibitors, particularly in the treatment of cancer.
摘要翻译：本发明涉及根据下式的假肽：其中R 1是抑制胺官能团的基团，或具有抑制的末端氨基官能团的氨基酸残基或肽，R 2表示天然或侧链的侧链非天然氨基酸，R 3表示：1）除未被芳基取代或取代的Gly和Ala之外的天然氨基酸的侧链，2）芳烷基，或3）包含至少3个碳原子，而R 4表示天然或非天然氨基酸的侧链。它们可用作基质锌金属蛋白酶抑制剂，特别是用于治疗癌症。

6. 发明授权

US07105483B2 Phosphinic pseudopeptide derivatives for the selective inhibition of the C-terminal active site of angiotensin I converting enzyme (ACE) 失效
标题翻译：用于选择性抑制血管紧张素I转换酶（ACE）的C-末端活性位点的磷酸假肽衍生物
公开(公告)号：US07105483B2
公开(公告)日：2006-09-12
申请号：US10500891
申请日：2003-01-16
申请人： Joel Cotton , Dimitri Georgiadis , Vincent Dive
发明人： Joel Cotton , Dimitri Georgiadis , Vincent Dive
IPC分类号： A61K38/00 , A61K38/02 , A61K38/05
CPC分类号： C07F9/3276 , C07F9/303 , C07F9/572 , C07F9/5728 , Y02P20/55
摘要： The invention relates to the use of phosphinic pseudopeptide derivatives for production of a medicament for selectively inhibiting the active C-terminal site of angiotensin I converting enzyme. These derivatives are of formula (II): where, R1 may be a protecting group for amino functions usually used in peptide chemistry or an amino acid or a peptide protected by the above type of protecting groups, R2 and R3 correspond to a natural or unnatural amino acid side chain and R4 and R5 represent a hydrogen atom or a counterion.
摘要翻译：本发明涉及次膦酸假肽衍生物用于制备用于选择性抑制血管紧张素I转化酶的活性C末端位点的药物的用途。这些衍生物具有式（II）：其中R 1可以是肽化学中通常使用的氨基官能团的保护基，或者是由上述类型的保护基保护的氨基酸或肽 R 2和R 3对应于天然或非天然氨基酸侧链，R 4和R 5代表一个氢原子或抗衡离子。

7. 发明申请

US20080153890A1 Phosphinic Amino Acid Compounds 失效
标题翻译：磷酸氨基酸化合物
公开(公告)号：US20080153890A1
公开(公告)日：2008-06-26
申请号：US11885301
申请日：2006-02-28
申请人： Vincent Dive , Nicolas Jullien , Elizabeth Scalbert , Athanasios Yiotakis , Anastasios Makaritis
发明人： Vincent Dive , Nicolas Jullien , Elizabeth Scalbert , Athanasios Yiotakis , Anastasios Makaritis
IPC分类号： A61K31/42 , C07D261/08 , A61P25/00 , A61P9/00 , C07D413/02
CPC分类号： C07F9/653
摘要： Compounds of formula (I): wherein: R1 represents hydrogen, alkylcarbonyloxyalkyl or alkylcarbonylthioalkyl, R2 represents hydrogen, alkylcarbonyloxyalkyl, arylcarbonylthioalkyl or optionally substituted arylalkyl, R3 represents phenyl, which is optionally substituted, or indolyl, their isomers, and addition salts thereof with a pharmaceutically acceptable acid or base. Medicinal products containing the same which are useful in the treatment of arterial hypertension and complications thereof.
摘要翻译：式（I）化合物：其中：R 1表示氢，烷基羰基氧基烷基或烷基羰基硫代烷基，R 2表示氢，烷基羰基氧基烷基，芳基羰基硫代烷基或任选取代的芳基烷基，R 3 代表任意取代的苯基，或吲哚基，它们的异构体及其与药学上可接受的酸或碱的加成盐。含有该药物的药物可用于治疗动脉高血压及其并发症。

8. 发明授权

US5677281A Use of peptide derivatives for the preparation of medicaments inhibiting endopeptidases 24.15 and 24.16 失效
标题翻译：肽衍生物用于制备抑制内肽酶24.15和24.16的药物的用途
公开(公告)号：US5677281A
公开(公告)日：1997-10-14
申请号：US44616
申请日：1993-04-09
申请人： Vincent Dive , Flavio Toma , Athanasios Yiotakis
发明人： Vincent Dive , Flavio Toma , Athanasios Yiotakis
IPC分类号： A61K38/55 , A61P9/12 , A61P25/04 , A61P29/00 , C07K5/08 , A61K38/05
CPC分类号： C07K5/0827 , A61K38/55
摘要： The invention relates to the use of peptide derivatives for the preparation of medicaments inhibiting endopeptidases 24.15 and 24.16. These peptide derivatives are in accordance with the formula: ##STR1## in which R.sup.1 is an optionally substituted aralkyl group, R.sup.2 is Pro, Hyp, thiazolidine or dehydroproline, R.sup.3 is H or an alkyl radical, R.sup.4 is an alkyl group or the side chain of an amino acid, R.sup.5 and R.sup.6 can be H, NH.sub.4 + or metals and R.sup.7 is H or CH.sub.3. N-(phenylethylphosphonyl)-Gly-Pro-aminohexanoic acid and N-(phenylethyl phosphonyl)-Ala-Pro-aminohexanoic acid are examples of effective derivatives.
摘要翻译：本发明涉及肽衍生物用于制备抑制内肽酶24.15和24.16的药物的用途。这些肽衍生物具有下式：其中R 1是任选取代的芳烷基，R 2是Pro，Hyp，噻唑烷或脱氢脯氨酸，R 3是H或烷基，R 4是烷基或氨基酸的侧链R5和R6可以是H，NH4 +或金属，R7是H或CH3。 N-（苯基乙基膦酰基）-Gly-原氨基己酸和N-（苯基乙基膦酰基）-Ala-Pro-氨基己酸是有效衍生物的实例。

9. 发明授权

US06482797B1 N-terminal site selective inhibitors of human angiotensin conversion enzyme (ACE) 失效
标题翻译：人血管紧张素转换酶（ACE）的N-末端位点选择性抑制剂
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。

10. 发明授权

US5389612A Phosphonic peptide inhibitors of bacterial collagenases 失效
标题翻译：细菌胶原酶的膦肽抑制剂
公开(公告)号：US5389612A
公开(公告)日：1995-02-14
申请号：US949760
申请日：1992-09-23
申请人： Vincent Dive , Flavio Toma , Athanasios Yiotakis
发明人： Vincent Dive , Flavio Toma , Athanasios Yiotakis
IPC分类号： C12N9/99 , A61K38/00 , A61K38/55 , A61P1/02 , A61P31/04 , A61P43/00 , C07K5/08 , C07K14/81 , C14C11/00 , A61K37/64 , C07K5/10 , A61K37/02
CPC分类号： C07K5/0827 , A61K38/00 , Y02P20/55
摘要： The invention relates to novel derivatives of peptides usable as inhibitors of bacterial collagenases.These derivatives comply with the formula: ##STR1## in which R.sup.1 is an optionally substituted aryl or aralkyl group or the group ##STR2## with R.sup.6 being the side chain of an .alpha.-amino acid and R.sup.7 R.sup.8 a protective group or a radical derived from an amino acid or a protected peptide, R.sup.2 is derived from proline, hydroxyproline, thiazolidine or dehydroproline, R.sup.3 is H or an alkyl, and R.sup.4 is the side chain of an amino acid and R.sup.5 and R'.sup.5 are H, a metal, an alkyl or benzyl.The derivatives in which R'.sup.5 is a metal or hydrogen can be used as inhibitors of bacterial collagenases.
摘要翻译：本发明涉及可用作细菌胶原酶抑制剂的肽的新衍生物。这些衍生物符合下列公式：其中R 1是任选取代的芳基或芳烷基或R 1是R 6是α-氨基酸的侧链，R 7 R 8是保护基团或基团衍生自氨基酸或受保护的肽，R2衍生自脯氨酸，羟脯氨酸，噻唑烷或脱氢脯氨酸，R3是H或烷基，R4是氨基酸的侧链，R5和R'5是H，金属，烷基或苄基。其中R'5为金属或氢的衍生物可用作细菌胶原酶的抑制剂。

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