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1. 发明申请

US20060058475A1 Polymers comprising in their skeleton an internal ethylenic unsaturation, and methods for preparing same 失效
标题翻译：在其骨架中包含内部烯属不饱和基团的聚合物及其制备方法
公开(公告)号：US20060058475A1
公开(公告)日：2006-03-16
申请号：US10530802
申请日：2003-10-10
申请人： Thierry Le Gall , Jean-Philippe Goddard , Charles Mioskowski
发明人： Thierry Le Gall , Jean-Philippe Goddard , Charles Mioskowski
IPC分类号： C08F2/00
CPC分类号： C08G61/04 , C08G61/08
摘要： The invention relates to polymers comprising a sequence of units comprising an ethylenic unsaturation, the unsaturation being located every 3 carbon atoms between two successive units. The invention also relates to processes for preparing such polymers.
摘要翻译：本发明涉及包含包含烯属不饱和键的单元序列的聚合物，不饱和键位于两个连续单元之间的每3个碳原子。本发明还涉及制备这种聚合物的方法。

2. 发明授权

US06878745B2 Selective preventives/remedies for progressive lesions after organ damage 失效
标题翻译：器官损伤后进行性病变的选择性预防措施/补救措施
公开(公告)号：US06878745B2
公开(公告)日：2005-04-12
申请号：US10239783
申请日：2001-03-27
申请人： Michio Ishibashi , Alain Wagner , Charles Mioskowski , Catherine Sylvain
发明人： Michio Ishibashi , Alain Wagner , Charles Mioskowski , Catherine Sylvain
IPC分类号： A61K31/341 , A61K31/343 , A61K31/365 , A61P1/18 , A61P13/12 , A61P37/06 , A61P43/00 , C07D307/33 , C07D307/68 , A61K31/34 , A61K31/585
CPC分类号： C07D307/33 , A61K31/341 , A61K31/343 , A61K31/365 , C07D307/68 , G01N2500/10
摘要： Drugs for preventing and/or treating progressive lesions after organ damage without inhibiting the function of the organ or the regeneration function thereof, by selectively regulating the induction of cytotoxic effecter macrophages which are induced into damaged organ tissues in response to chemokines or cytokines expressed depending on the type of the damaged organ tissues.
摘要翻译：用于预防和/或治疗器官损伤后不进行器官功能或其再生功能的进行性病变的药物，其通过选择性调节细胞毒性作用剂巨噬细胞的诱导，所述细胞毒性巨噬细胞响应于依赖于表达的趋化因子或细胞因子而被诱导到损伤的器官组织受损器官组织的类型。

3. 发明授权

US06331434B1 Nitrogen-containing silicone useful for compacting nucleic acid sequences and use for transforming cells 失效
标题翻译：用于压实核酸序列和用于转化细胞的含氮硅氧烷
公开(公告)号：US06331434B1
公开(公告)日：2001-12-18
申请号：US09521822
申请日：2000-03-09
申请人： Rachel Decor , Charles Mioskowski , Marc Schmutz , Alain Wagner
发明人： Rachel Decor , Charles Mioskowski , Marc Schmutz , Alain Wagner
IPC分类号： C12N1588
CPC分类号： C08G83/001 , C08G77/388 , C12N15/8207 , C12N15/87 , C12N15/895
摘要： The present invention relates to a method of transforming cells in which an appropriate quantity of nucleic acid fragments is introduced into the cells. The nucleic acid fragments are introduced in the form of a nucleic acid composition comprising a nitrogen-containing silicone, useful for compacting the nucleic acid fragments; the compositions comprise aggregates of nucleic acid fragments and silicones according to the invention.
摘要翻译：本发明涉及转化细胞的方法，其中将适量的核酸片段引入细胞。以核酸组合物的形式引入核酸片段，所述核酸组合物包含可用于压实核酸片段的含氮硅氧烷; 组合物包含根据本发明的核酸片段和硅氧烷的聚集体。

4. 发明授权

US08304545B2 Quinuclidine derivative useful in the preparation of mequitazine 失效
公开(公告)号：US08304545B2
公开(公告)日：2012-11-06
申请号：US13313809
申请日：2011-12-07
申请人： Charles Mioskowski , Vanessa Gonnot , Rachid Baati , Marc Nicolas
发明人： Charles Mioskowski , Vanessa Gonnot , Rachid Baati , Marc Nicolas
IPC分类号： C07D417/14 , C07D453/02
CPC分类号： C07D207/08 , C07D211/26 , C07D211/70 , C07D279/26 , C07D453/02 , C07D471/04
摘要： The invention relates to a 1-aza-bicyclo[2.2.2]oct-2-en-3-ylmethyl acetate of the formula (I), wherein said compound is useful as a synthesis intermediate for the production of mequitazine.

5. 发明申请

US20070049773A1 Process for functionalising a phenolic compound carrying an electron-donating group 审中-公开
标题翻译：功能化携带电子给予基团的酚类化合物的方法
公开(公告)号：US20070049773A1
公开(公告)日：2007-03-01
申请号：US11592930
申请日：2006-11-03
申请人： Charles Mioskowski , Alain Wagner , Nicolas Bensel , Virginie Pevere , Jean-Roger Desmurs
发明人： Charles Mioskowski , Alain Wagner , Nicolas Bensel , Virginie Pevere , Jean-Roger Desmurs
IPC分类号： C07C39/24 , C07C39/34 , C07C45/90
CPC分类号： C07C45/46 , C07C45/565 , C07C231/12 , C07C231/14 , C07C303/28 , C07C303/30 , C07C233/18 , C07C309/66 , C07C49/84 , C07C47/575
摘要： The invention concerns a method for functionalizing a phenolic compound bearing an electron-donor group, in said group para position, inter alia a method for the amidoalkylation of a phenolic compound bearing an electron-donor group, and more particularly, a phenolic compound bearing an electron-donor group preferably, in the hydroxyl group ortho position. The method for functionalizing in para position with respect to an electron-donor group carried by a phenolic compound is characterised in that the phenolic compound bearing an electron-donor group is subjected to the following steps: a first step which consists of protecting the hydroxyl group in the form of a sulphonic ester function; a second step which consists in reacting the protected phenolic compound with an electrophilic reagent; optionally, a third step deprotecting the hydroxyl group.
摘要翻译：本发明涉及一种用于官能化带有电子给体基团的酚类化合物的方法，尤其是具有电子给体基团的酚类化合物的酰胺基烷基化方法，更具体地说，涉及带有电子给体基团优选在羟基邻位。相对于由酚类化合物携带的电子给体基团在对位官能化的方法的特征在于具有电子给体基团的酚类化合物经受以下步骤：第一步，其保护羟基呈磺酸酯官能团的形式; 第二步是使受保护的酚类化合物与亲电试剂反应; 任选地，第三步骤使羟基脱保护。

6. 发明申请

US20060199853A1 Analogs of 4-hydroxyisoleucine and uses thereof 审中-公开
标题翻译： 4-羟基异亮氨酸的类似物及其用途
公开(公告)号：US20060199853A1
公开(公告)日：2006-09-07
申请号：US11356848
申请日：2006-02-17
申请人： Charles Mioskowski , Sandra Marin , Martine Maruani , Manjinder Gill
发明人： Charles Mioskowski , Sandra Marin , Martine Maruani , Manjinder Gill
IPC分类号： A61K31/41 , C07D233/61 , A61K31/4172 , A61K31/198
CPC分类号： C07C229/22 , C07B2200/07 , C07C229/28 , C07C229/30 , C07C229/36 , C07C229/50 , C07C271/22 , C07C309/18 , C07C311/19 , C07C2601/08 , C07C2601/14 , C07C2601/18 , C07C2603/74 , C07D207/16 , C07D211/60 , C07D211/78 , C07D257/04 , C07D261/18 , C07D265/06 , C07D295/185 , C07D307/33 , C07D405/06 , C07D491/08 , C07F9/3808
摘要： The invention relates to analogs of 4-hydroxyisoleucine, and to lactones, pharmaceutically acceptable salts, and prodrugs thereof, to processes for their preparation, and to pharmaceutical compositions comprising the same. The analogs of the invention stimulate both glucose uptake and insulin secretion, and may thus be useful for the prevention and treatment of disorders of carbohydrate or lipid metabolism, including diabetes mellitus (type 1 and type 2 diabetes), pre-diabetes, and Metabolic Syndrome.
摘要翻译：本发明涉及4-羟基异亮氨酸的类似物及其内酯，其药学上可接受的盐和前药，其制备方法以及包含其的药物组合物。本发明的类似物刺激葡萄糖摄取和胰岛素分泌，因此可用于预防和治疗糖或脂质代谢紊乱，包括糖尿病（1型和2型糖尿病），前期糖尿病和代谢综合征。

7. 发明授权

US5519128A Process for the synthesis of acylated derivatives of fatty acid-transporting thiols and in particular acyl-coenzymes A and the thus obtained acyl-coenzymes A 失效
公开(公告)号：US5519128A
公开(公告)日：1996-05-21
申请号：US392172
申请日：1995-02-22
申请人： Jean-Paul Lellouche , Karine Levannier , Charles Mioskowski
发明人： Jean-Paul Lellouche , Karine Levannier , Charles Mioskowski
IPC分类号： C07C327/06 , C07F9/6561 , C07H19/20 , C07H17/00
CPC分类号： C07H19/20
摘要： The invention relates to a process for the synthesis of an acylated derivative of a fatty acid-transporting thiol such as the coenzyme A.According to this process, a silylated or stannylated thiol is prepared by reacting the thiol with a silylation or stannylation reagent in order to at least partly replace the unstable hydrogens of the thiol by SiR.sub.3 or SnR.sub.3 groups with R being an alkyl or aryl group. The silylated or stannylated thiol is then reacted in an anhydrous organic medium with an activated organic acid and a deprotection reagent able to eliminate the silyl or stannyl groups.In this way it is possible to obtain acylated derivatives of the coenzyme A, in which the acyl group can have up to 30 carbon atoms with high yields.

8. 发明授权

US07420087B2 Method for preparing 4-hydroxyisoleucine diastereoisomers and enantiomers and derivatives thereof 失效
标题翻译：制备4-羟基异亮氨酸非对映异构体及其对映体及其衍生物的方法
公开(公告)号：US07420087B2
公开(公告)日：2008-09-02
申请号：US10537293
申请日：2003-12-01
申请人： Charles Mioskowski , Alain Wagner , Sandra De Lamo Marin , Cedric Catala , Jean-Michel Becht
发明人： Charles Mioskowski , Alain Wagner , Sandra De Lamo Marin , Cedric Catala , Jean-Michel Becht
IPC分类号： C07C229/00 , C07D305/12
CPC分类号： C07D307/66 , C07C227/32 , C07C229/22
摘要： The invention concerns a method for preparing 4-hydroxyisoleucine diastereoisomers and enantiomers and derivatives thereof of general formula (I), characterized in that it consists in reducing an isoxazole derivative of formula (II) in conditions directly resulting in the derivatives of formula (I), or in obtaining at least a lactone of structure (III) in racemic form(s), or a enantiomerically enriched mixture, followed by opening, in basic conditions, in an aprotic or protic solvent, the desired lactone(s) and, optionally, separating the desired form. The invention is useful for preparing in particular (2S, 3R, 4S)-4-hydroxyisoleucine.
摘要翻译：本发明涉及一种制备通式（I）的4-羟基异亮氨酸非对映异构体及其衍生物的方法，其特征在于其在直接得到式（I）衍生物的条件下还原式（II）的异恶唑衍生物，，或至少获得外消旋形式的结构（III）的内酯或对映异构体富集的混合物，然后在碱性条件下，在非质子或质子溶剂中，所需的内酯和任选的，分离所需的形式。本发明可用于特别制备（2S，3R，4S）-4-羟基异亮氨酸。

9. 发明授权

US07326805B2 Method for the synthesis of 4-hydroxyisoleucine and the derivatives thereof 失效
公开(公告)号：US07326805B2
公开(公告)日：2008-02-05
申请号：US10555875
申请日：2004-05-07
申请人： Charles Mioskowski , Cédric Catala , Alain Wagner
发明人： Charles Mioskowski , Cédric Catala , Alain Wagner
IPC分类号： C07C229/00
CPC分类号： C07C227/30 , C07B2200/07 , C07C227/16
摘要： The invention relates to a method for the synthesis of two isomers, at function OH, alone or in mixtures, of amino acids α or the derivatives thereof, having general formula (B), wherein: linkage C—O of the 4-position carbon (represented by symbol) denotes one or other of isomers III or IV, or mixtures thereof. Moreover, R1 and R2 represent: a hydrogen atom; or either R1 or R2 represents a hydrogen atom and the other substituent is a radical Ra, an acyl group —CORa, such as acetyl, or a functional group —COORa, —SO2Ra, —N (Ra, Rb), Ra and Rb, which are identical or different, representing a C1-C12 linear or branched alkyl radical, optionally substituted, an aryl group with one or more aromatic rings and heterocycles, comprising between 5 and 8C, optionally substituted, or aralkyl, the alkyl substituent and the aryl group being as defined above; or R1 and R2 both represent a substituent as defined above. R3 represents a hydrogen atom or Ra and R4 has the significance of Ra. The invention is characterised in that it comprises: the isomerisation of a compound having formula (I), wherein R1, R2, Ra, R3 and R4 are as defined above, such as to produce a compound having formula (II); and the reduction of the carbonyl function thereof which, depending on the catalytic system employed and the formula (I) compound used, produces one of the isomers having general formula (III) or (IV) or a mixture thereof having formula (B). The invention can be used for the synthesis of (2S, 3R, 4S)-4-hydroxyisoleucine.

10. 发明申请

US20050143453A1 Selective preventing and therapeutic agents for progressive lesion after organic damage 审中-公开
标题翻译：有机损伤后进行性病变的选择性预防和治疗剂
公开(公告)号：US20050143453A1
公开(公告)日：2005-06-30
申请号：US11045394
申请日：2005-01-31
申请人： Michio Ishibashi , Alain Wagner , Charles Mioskowski , Catherine Sylvain
发明人： Michio Ishibashi , Alain Wagner , Charles Mioskowski , Catherine Sylvain
IPC分类号： A61K31/341 , A61K31/343 , A61K31/365 , A61P1/18 , A61P13/12 , A61P37/06 , A61P43/00 , C07D307/33 , C07D307/68 , C07D305/12 , C07D307/62
CPC分类号： C07D307/33 , A61K31/341 , A61K31/343 , A61K31/365 , C07D307/68 , G01N2500/10
摘要： An object of the present invention is to provide a pharmaceutical agents for preventing and/or treating the progressive lesion after the organic damage without inhibiting organic function or regeneration function thereof, by selectively suppressing the induction of cytotoxic effector macrophages which are induced into the damaged organs in response to chemokines and cytokines which are expressed depending on the type of damaged organic tissues.
摘要翻译：本发明的目的是提供一种用于预防和/或治疗有机损伤后的进行性损伤而不抑制其有机功能或再生功能的药剂，通过选择性地抑制诱导到受损器官中的细胞毒性效应物巨噬细胞的诱导响应于根据损伤的有机组织的类型表达的趋化因子和细胞因子。

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