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    Carnitinamides of optically active aminoacids
    4.
    发明授权
    Carnitinamides of optically active aminoacids 失效
    光学活性氨基酸的肉碱酰胺

    公开(公告)号：US4343947A

    公开(公告)日：1982-08-10

    申请号：US220492

    申请日：1980-12-29

    申请人： Paolo De Witt ,  Maria O. Tinti

    发明人： Paolo De Witt ,  Maria O. Tinti

    IPC分类号： A61K20060101 ,  A61K31/16 ,  A61K31/205 ,  C07C20060101 ,  C07C237/12 ,  C07C323/25 ,  C07D233/58 ,  C07D233/64 ,  C07C101/26 ,  C07C101/30 ,  C07C101/32

    CPC分类号： C07C237/12 ,  C07C323/58

    摘要： Amides of carnitine or acyl-carnitines having general formula: ##STR1## wherein X.sup.- is a halogen anion, e.g. the chloride anionR is either hydrogen or an acyl radical, such as acetyl, propionyl or butyryl; andY is the residue of an optically active esterified amino-acid (e.g. the residue of L-phenylglycine methyl ester, ##STR2## are prepared by either (a) directly condensing D,L-carnitine (or acyl-D,L-carnitine) with an ester of an optically active aminoacid, or (b) preparing the acid halogenide of D,L-carnitine or acyl-D,L-carnitine and subsequently condensing it with an ester of an optically active aminoacid.The mixture of the diastereoisomer amides thus obtained is resolved by fractional crystallization from organic solvents into the respective separated diastereoisomers.These optically active amides are useful therapeutic agents for treating cardiac disorders, hyperlipidaemias and hyperlipoproteinaemias and, furthermore, can be hydrolyzed with procedures known per se into L-carnitine and D-carnitine, respectively.

    摘要翻译： 具有以下通式的肉碱或酰基肉碱的酰胺：其中X是卤素阴离子，例如， 氯离子R是氢或酰基，如乙酰基，丙酰基或丁酰基; 并且Y是光学活性酯化氨基酸的残基（例如，L-苯基甘氨酸甲酯的残基，通过以下方法制备：（a）直接冷凝D，L-肉毒碱（或酰基-D，L-肉毒碱 ），或（b）制备D，L-肉碱或酰基-D，L-肉毒碱的酰卤，然后将其与光学活性氨基酸的酯缩合，非对映异构体的混合物 这些光学活性酰胺是治疗心脏疾病，高脂血症和高脂蛋白血症的有用治疗剂，此外，可以用本身已知的方法将其水解成L-肉碱和 D-肉碱分别。

    Esters of acyl l-carnitines with gamma-hydroxybutyric acid and pharmaceutical compositions containing them for inhibiting neuronal degeneration and for the treatment of coma
    9.
    发明授权
    Esters of acyl l-carnitines with gamma-hydroxybutyric acid and pharmaceutical compositions containing them for inhibiting neuronal degeneration and for the treatment of coma 失效
    具有γ-羟基丁酸的酰基l-肉碱的酯和含有它们的药物组合物用于抑制神经元变性和治疗昏迷

    公开(公告)号：US5543556A

    公开(公告)日：1996-08-06

    申请号：US317750

    申请日：1994-10-04

    申请人： Maria O. Tinti ,  Domenico Misiti ,  Claudio Cavazza ,  Nazareno Scafetta

    发明人： Maria O. Tinti ,  Domenico Misiti ,  Claudio Cavazza ,  Nazareno Scafetta

    IPC分类号： A61K31/22 ,  A61P25/00 ,  A61P25/28 ,  C07C219/22 ,  C07C229/22 ,  C07C229/00

    CPC分类号： C07C219/22

    摘要： The esters of acyl L-carnitines with gamma-hydroxybutyric acid in the form of pharmacologically acceptable salts of formula (I) ##STR1## wherein X.sup.- is the anion of a pharmacologically acceptable salt, e.g. chloride, bromide, orotate, acid aspartate, acid citrate, acid phosphate, acid fumarate, lactate, acid maleate, acid oxalate, acid sulfate and glucosephosphate or in the form of inner salts of formula (I') ##STR2## wherein R is a straight or branched acyl group having from 2 to 5 carbon atoms, such as e.g. acetyl, propionyl, n-butyryl, isobutyryl and isovaleryl, are active in inhibiting neuronal degeneration (as it occurs in Alzheimer's senile dementia and Parkinson's disease) and in the treatment of coma.

    摘要翻译： 酰基L-肉碱与式（I）的药理学上可接受的盐形式的γ-羟基丁酸的酯，其中X是药理学上可接受的盐的阴离子，例如， 氯化物，溴酸盐，乳清酸，天冬氨酸，酸式柠檬酸盐，酸式磷酸盐，富马酸酸盐，乳酸盐，酸性马来酸盐，酸性草酸盐，酸式硫酸盐和磷酸二氢盐或以式（I'）的内盐形式。 其中R是具有2至5个碳原子的直链或支链酰基，例如 乙酰基，丙酰基，正丁酰基，异丁酰基和异戊酰基在抑制神经元变性（如在阿尔茨海默病老年痴呆和帕金森病中发生）和在昏迷的治疗中是有活性的。

    Thioalkanoyl-carnitines, process for their preparation and mucolytic pharmaceutical compositions containing same
    10.
    发明授权
    Thioalkanoyl-carnitines, process for their preparation and mucolytic pharmaceutical compositions containing same 失效
    硫酰基肉碱，其制备方法和含有它们的粘液溶解药物组合物

    公开(公告)号：US4518613A

    公开(公告)日：1985-05-21

    申请号：US436190

    申请日：1982-10-22

    申请人： Claudio Cavazza ,  Maria O. Tinti

    发明人： Claudio Cavazza ,  Maria O. Tinti

    IPC分类号： C07C327/28 ,  A61K20060101 ,  A61K31/14 ,  A61K31/205 ,  A61K31/255 ,  A61K31/265 ,  A61P11/00 ,  A61P11/14 ,  C07C20060101 ,  C07C67/00 ,  C07C325/00 ,  C07C327/22 ,  C07D405/06 ,  C07C153/017

    CPC分类号： C07C327/32 ,  A61K9/0019 ,  A61K9/0031 ,  A61K9/0078 ,  A61K9/009 ,  A61K9/0095 ,  A61K9/02

    摘要： Thioalkanoyl-carnitines of general formula (I) ##STR1## wherein R is a straight alkylene radical having from 2 to 6 carbon atoms, or is a branched alkylene radical having from 3-6 carbon atoms, or is a branched alkylene radical having from 3-6 carbon atoms,R.sub.1 is a straight or branched lower alkyl radical having from 1 to 4 carbon atoms, andX.sup.- is a halogen anionare prepared by reacting a thio-acid (II) of general formula R.sub.1 COSH(a) if in (I) the thioalkanoyl radical R.sub.1 COS-- is in terminal position, with a compound of general formula (III) ##STR2## wherein n is an integer comprised between 0 and 4 or(b) if in (I) the thioalkanoyl radical R.sub.1 COS-- is not in terminal position, with a compound of general formula (IV) ##STR3## wherein m and m.sup.1 are integers comprised between 0 and 3, andR.sub.2 is a lower alkyl radical having from 1 to 4 carbon atoms.The pharmaceutical compositions containing the thioalkanoyl-carnitines (I) possess mucolytic and antitussive activity.

    摘要翻译： 通式（I）的硫代酰基 - 肉碱其中R是具有2至6个碳原子的直链亚烷基，或是具有3-6个碳原子的支链亚烷基，或是具有3个 -6个碳原子，R 1是具有1至4个碳原子的直链或支链低级烷基，X-是卤素阴离子是通过使通式R 1 COSH（a）的硫代酸（II）如果在（ I）硫代烷酰基R1COS-位于末端，与通式（III）的化合物其中n是0至4之间的整数，或（b）如果在（I）中硫代烷酰基R1COS-不是 在末端位置与通式（IV）的化合物其中m和m1是0和3之间的整数，R2是具有1至4个碳原子的低级烷基。 含有硫代链烷酰基肉碱（I）的药物组合物具有粘液分解和镇咳活性。