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1. 发明授权

US6127552A Process for producing (R)-3-hydroxy-4-butyrolactone useful for preparing (R)-carnitine 失效
标题翻译：用于制备（R） - 肉碱的（R）-3-羟基-4-丁内酯的制备方法
公开(公告)号：US6127552A
公开(公告)日：2000-10-03
申请号：US200852
申请日：1998-11-30
申请人： Fabio Giannessi , Maria Ornella Tinti , Francesco De Angelis
发明人： Fabio Giannessi , Maria Ornella Tinti , Francesco De Angelis
IPC分类号： C07C227/32 , C07C229/22 , C07D305/12 , C07D307/33 , C07D307/02 , C07D307/56
CPC分类号： C07D307/33 , C07C227/32 , C07D305/12 , C07B2200/07
摘要： A process is disclosed for producing (R)-3-hydroxy-4-butyrolactone from its enantiomer, (S)-3-hydroxy-4-butyrolactone. The (R)-enantiomer can be advantageously utilized in several organic synthesis and industrial processes, such as e.g. GABOB and (R)-carnitine preparation.
摘要翻译：公开了从其对映异构体（S）-3-羟基-4-丁内酯制备（R）-3-羟基-4-丁内酯的方法。（R） - 对映异构体可有利地用于几种有机合成和工业过程，例如 GABOB和（R） - 肉碱制剂。

2. 发明授权

US06528684B1 Synthesis of (R) and (S) -aminocarnitine and their derivatives starting from D- and L-aspartic acid 失效
标题翻译：从D-和L-天冬氨酸开始合成（R）和（S） - 氨基卡尼汀及其衍生物
公开(公告)号：US06528684B1
公开(公告)日：2003-03-04
申请号：US10018794
申请日：2001-12-21
申请人： Fabio Giannessi , Natalina Dell'uomo , Maria Ornella Tinti , Francesco De Angelis
发明人： Fabio Giannessi , Natalina Dell'uomo , Maria Ornella Tinti , Francesco De Angelis
IPC分类号： C07C22900
CPC分类号： C07C227/14 , C07C229/26
摘要： R or S aminocarnitine and their derivatives with formula (I) where Y is as described in the description, starting with aspartic acid with the same configuration as the aminocarnitine desired. This process has advantage in the type of reactants used, reduced volumes of solvents and the possibility of avoiding purification of intermediate products.
摘要翻译： R或S氨卡尼汀及其衍生物，其中Y如描述中所述，以与所需胺氨基酸相同构型的天冬氨酸开始。该方法在所用反应物的类型，溶剂体积减少和避免中间产物净化的可能性方面具有优势。

3. 发明授权

US06822115B2 Synthesis of (R) and (S)-aminocarnitine, (R) and (S)-4-phosphonium-3-amino-butanoate, (R) and (S) 3,4-diaminobutanoic acid, and their derivatives starting from D- and L-aspartic acid 失效
标题翻译：（R）和（S） - 氨基卡那提定，（R）和（S）-4-鏻-3-氨基丁酸酯，（R）和（S）3,4-二氨基丁酸及其衍生物 - 和L-天冬氨酸
公开(公告)号：US06822115B2
公开(公告)日：2004-11-23
申请号：US10372627
申请日：2003-02-25
申请人： Fabio Giannessi , Natalina Dell'uomo , Maria Ornella Tinti , Francesco De Angelis
发明人： Fabio Giannessi , Natalina Dell'uomo , Maria Ornella Tinti , Francesco De Angelis
IPC分类号： C07C22900
CPC分类号： C07C227/16 , C07C227/14 , C07C229/26 , C07F9/5407
摘要： R or S aminocarnitine, R or S phosphonium aminocarnitine and R and S 3,4 diaminobutanoic acid, and their derivatives are prepared using starting from aspartic acid with the same configuration as the desired compounds. This process is advantageous from the industrial point of view in terms of the type of reactants used, the reduced volumes of solvents and the possibility of avoiding purification of the intermediate products.
摘要翻译： R或S氨卡尼汀，R或S鏻氨卡尼丁和R和S 3,4二氨基丁酸及其衍生物使用与所需化合物相同构型的天冬氨酸开始制备。从工业观点来看，该方法在所用反应物的类型，减少的溶剂体积和避免中间产物净化的可能性方面是有利的。

4. 发明授权

US06369073B1 Compounds having reversible inhibiting activity of carnitine palmitoyl-transferase 有权
公开(公告)号：US06369073B1
公开(公告)日：2002-04-09
申请号：US09677328
申请日：2000-10-02
申请人： Fabio Giannessi , Mauro Marzi , Patrizia Minetti , Francesco De Angelis , Maria Ornella Tinti , Piero Chiodi , Arduino Arduini
发明人： Fabio Giannessi , Mauro Marzi , Patrizia Minetti , Francesco De Angelis , Maria Ornella Tinti , Piero Chiodi , Arduino Arduini
IPC分类号： A61K3146
CPC分类号： C07D257/04 , C07C229/22 , C07C229/26 , C07C271/12 , C07C271/22 , C07C275/16 , C07C311/06 , C07C335/08 , C07D295/15 , C07D453/02 , C07F9/5407
摘要： Compounds of formula (I) wherein the groups are as defined in the description are disclosed. The compounds of formula (I) are endowed with reversible inhibiting activity of carnitine palmitoyl-transferase and are useful in the preparation of medicaments useful in the pathologies related to a hyperactivity of carnitine palmitoyl-transferase, such as hyperglycemia, diabetes and pathologies related thereto, heart failure, ischemia.

5. 再颁专利

USRE41226E1 Compounds having reversible inhibiting activity of carnitine palmitoyl-transferase 失效
标题翻译：肉碱棕榈酰转移酶具有可逆抑制活性的化合物
公开(公告)号：USRE41226E1
公开(公告)日：2010-04-13
申请号：US11607078
申请日：2006-12-01
申请人： Fabio Giannessi , Mauro Marzi , Patrizia Minetti , Francesco De Angelis , Maria Ornella Tinti , Piero Chiodi , Arduino Arduini
发明人： Fabio Giannessi , Mauro Marzi , Patrizia Minetti , Francesco De Angelis , Maria Ornella Tinti , Piero Chiodi , Arduino Arduini
IPC分类号： A61K31/27 , C07C271/06
CPC分类号： C07D257/04 , C07C229/22 , C07C229/26 , C07C271/12 , C07C271/22 , C07C275/16 , C07C311/06 , C07C335/08 , C07D295/15 , C07D453/02 , C07F9/5407
摘要： Compounds of formula (I) wherein the groups are as defined in the description are disclosed. The compounds of formula (I) are endowed with reversible inhibiting activity of carnitine palmitoyl-transferase and are useful in the preparation of medicaments useful in the pathologies related to a hyperactivity of carnitine polymitoyl-transferase, such as hyperglycemia, diabetes and pathologies related thereto, heart failure, ischemia.
摘要翻译：公开了其中基团如说明书中定义的式（I）化合物。式（I）化合物具有肉毒碱棕榈酰转移酶的可逆抑制活性，可用于制备与肉碱多聚酰胺转移酶多动症有关的病症，如高血糖症，糖尿病及其相关疾病，心力衰竭，局部缺血。

6. 发明授权

US06444701B1 Compounds having reversible inhibiting activity of carnitine palmitoyl-transferase 有权
标题翻译：肉碱棕榈酰转移酶具有可逆抑制活性的化合物
公开(公告)号：US06444701B1
公开(公告)日：2002-09-03
申请号：US09986327
申请日：2001-11-08
申请人： Fabio Giannessi , Mauro Marzi , Patrizia Minetti , Francesco De Angelis , Maria Ornella Tinti , Piero Chiodi , Arduino Arduini
发明人： Fabio Giannessi , Mauro Marzi , Patrizia Minetti , Francesco De Angelis , Maria Ornella Tinti , Piero Chiodi , Arduino Arduini
IPC分类号： A61K31195
CPC分类号： C07D257/04 , C07C229/22 , C07C229/26 , C07C271/12 , C07C271/22 , C07C275/16 , C07C311/06 , C07C335/08 , C07D295/15 , C07D453/02 , C07F9/5407
摘要： Compounds of formula (I) wherein the groups are as defined in the description are disclosed. The compounds of formula (I) are endowed with reversible inhibiting activity of carnitine palmitoyl-transferase and are useful in the preparation of medicaments useful in the pathologies related to a hyperactivity of carnitine palmitoyl-transferase, such as hyperglycemia, diabetes and pathologies related thereto, heart failure, ischemia.
摘要翻译：公开了式（I）化合物，其中基团如说明书中所定义。式（I）化合物具有肉碱棕榈酰转移酶的可逆抑制活性，并且可用于制备可用于与肉碱棕榈酰转移酶的多动症，例如高血糖症，糖尿病和与之相关的病理，心力衰竭，局部缺血。

7. 发明授权

US06316667B2 Process for the preparation of R-(-)-carnitine 失效
标题翻译：制备R - （ - ） - 肉碱的方法
公开(公告)号：US06316667B2
公开(公告)日：2001-11-13
申请号：US09740806
申请日：2000-12-21
申请人： Fabio Giannessi , Maria Ornella Tinti , Francesco De Angelis
发明人： Fabio Giannessi , Maria Ornella Tinti , Francesco De Angelis
IPC分类号： C07C22900
CPC分类号： C07C227/32 , C07B2200/07 , C07C229/22
摘要： R-(−)-carnitine is prepared by (a) conversion of (S)-3-hydroxy-4-butyrolactone [1] to alkyl (S)-4-halogen-3-hydroxy-butyrate [2] by reaction with a linear or branched C1-C7 alcohol (b), substitution of a CN group for the halogen of compound [2] to yield the alkyl ester of (R)-4-cyano-3-hydroxybutyric acid [3], (c) conversion of alkyl ester [3] to yield (R)-4-cyano-3-hydroxybutyramide [4], (d) cyclization of compound [4] to yield (R)-5-(cyanomethyl)-2-oxazolidone [5] via conversion of the amide function to isocyanate, (e) hydrolysis of compound [5] to yield (R)-4-amino-3-hydroxybutyric acid [6], and finally (f) methylation of the amino group of compound [6] to yield the end product (R)-carnitine.
摘要翻译：通过（a）通过与（S）-3-羟基-4-丁内酯[1]转化为（S）-4-卤素-3-羟基 - 丁酸烷基酯[2]的方法制备R - （ - ） - 肉碱直链或支链C 1 -C 7醇（b），CN基团取代化合物[2]的卤素，得到（R）-4-氰基-3-羟基丁酸的烷基酯[3]，（c）烷基酯[3]转化成（R）-4-氰基-3-羟基丁酰胺[4]，（d）化合物[4]环化得到（R）-5-（氰基甲基）-2-恶唑烷酮[5 ]通过将酰胺官能团转化为异氰酸酯，（e）化合物[5]的水解产生（R）-4-氨基-3-羟基丁酸[6]，最后（f）化合物[ 6]，得到最终产物（R） - 肉碱。

8. 发明申请

US20080161395A1 Derivatives of Aminobutanoic Acid Inhibiting Cpt 审中-公开
标题翻译：氨基丁酸抑制剂的衍生物
公开(公告)号：US20080161395A1
公开(公告)日：2008-07-03
申请号：US11815068
申请日：2006-02-13
申请人： Fabio Giannessi , Emanuela Tassoni , Maria Ornella Tinti , Roberto Conti , Natalina Dell'Uomo , Tiziana Brunetti
发明人： Fabio Giannessi , Emanuela Tassoni , Maria Ornella Tinti , Roberto Conti , Natalina Dell'Uomo , Tiziana Brunetti
IPC分类号： A61K31/21 , C07C229/02 , A61P3/10
CPC分类号： C07C275/16 , C07D211/90 , C07D213/82
摘要： The invention relates to a new class of compounds with action inhibiting carnitine palmitoyl transferase (CPT), pharmaceutical compounds which contain at least one new compound according to the invention, and their therapeutic use in the treatment of hyperglycaemic conditions such as diabetes and the pathologies associated with it, congestive heart failure and obesity.
摘要翻译：本发明涉及具有抑制作用的肉碱棕榈酰转移酶（CPT）的新一类化合物，其含有至少一种本发明新化合物的药物化合物及其治疗用于治疗高血糖病症如糖尿病和相关病理伴有它，充血性心力衰竭和肥胖。

9. 发明授权

US06420599B2 Chemical process for the stereoselective synthesis of R-(-)-carnitine 失效
标题翻译：用于立体选择性合成R - （ - ） - 肉碱的化学方法
公开(公告)号：US06420599B2
公开(公告)日：2002-07-16
申请号：US09725141
申请日：2000-11-29
申请人： Mauro Marzi , Maria Ornella Tinti , Francesco De Angelis
发明人： Mauro Marzi , Maria Ornella Tinti , Francesco De Angelis
IPC分类号： C07C22900
CPC分类号： C07C227/32 , C07B2200/07 , C07C303/38 , C07C2603/66 , C07C229/22
摘要： A process is described for the stereoselective synthesis of R-(−)-carnitine in which the characterizing step is condensation of glycerol with an amine of (−)camphorsulfonic acid.
摘要翻译：描述了用于立体选择性合成R - （ - ） - 肉碱的方法，其中表征步骤是甘油与（ - ）樟脑磺酸的胺缩合。

10. 发明授权

US5925369A Bis alkanoyl esters of carnitine having bactericidal, fungicidal and antiprotozoal activity 失效
标题翻译：具有杀菌，杀真菌和抗原虫活性的肉碱的双链烷酰基酯
公开(公告)号：US5925369A
公开(公告)日：1999-07-20
申请号：US818737
申请日：1997-03-14
申请人： Nazareno Scafetta , Maria Ornella Tinti , Francesco De Angelis , Gian Carlo Gramiccioli
发明人： Nazareno Scafetta , Maria Ornella Tinti , Francesco De Angelis , Gian Carlo Gramiccioli
IPC分类号： A61K31/22 , A01N37/44 , A61P17/00 , A61P31/04 , A61P31/10 , A61P33/02 , C07C227/18 , C07C227/40 , C07C229/22 , A01N25/00
CPC分类号： C07C229/22
摘要： DL-, D- or L-carnitine esters of formula ##STR1## wherein R, Y and X.sup.- have the meaning shown in the specification which possess potent bactericidal, fungicidal and antiprozoal activity, processes for their preparation and compositions topically applicable for treating infections of the skin, outer ear and mucosa, are disclosed.
摘要翻译：具有下式的DL-，D-或L-肉碱酯其中R，Y和X-具有说明书所示的含有有效杀菌，杀真菌和抗原虫活性的含义，其制备方法和局部适用于治疗皮肤感染的组合物，外耳和粘膜。

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