公开(公告)号：EP0552138A2

公开(公告)日：1993-07-21

申请号：EP93830010.0

申请日：1993-01-15

申请人： Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.

发明人： Santaniello, Mosè ,  Tinti, Maria Ornella ,  Misiti, Domenico ,  Foresta, Piero

IPC分类号： C07C229/22 ,  A61K31/195 ,  A61K31/22

CPC分类号： C07C229/22

摘要： Esters of acyl L-carnitines of general formula (I)
wherein

R is a straight or branched acyl group having 2 to 16 carbon atoms, in particular isobutyryl and isovaleryl ;
n is an integer comprised between 7 and 15, particularly 10 ; and,
X- is the anion of a pharmacologically acceptable acid are endowed with potent antimycotic activity particularly against yeast like fungi, such as Candida albicans, the aetiologic agent of candidiasis and against filamentous fungi, such as Aspergillus fumigatus, the aetiologic agent of aspergillosis.
Orally or parenterally administrable or topically applicable pharmaceutical compositions comprise an ester of formula (I) as active ingredient.

摘要翻译： 通式（I） worin R是具有2至16个碳原子，特别是异丁和异戊酰基的直链或支链酰基的N-酰基L-肉碱的酯; n为7和15，特别是10之间包含的整数; 并且，X是被赋予了特别是对样真菌,:如白色念珠菌，念珠菌aetiologic剂和抗丝状真菌，：例如烟曲霉病，曲霉病的aetiologic剂酵母有效的抗真菌活性的药理学上可接受酸的阴离子。 口服或肠胃外给药或局部应用药物组合物包含式（I）作为活性的酯的成分。

公开(公告)号：EP0429403A2

公开(公告)日：1991-05-29

申请号：EP90830465.2

申请日：1990-10-18

申请人： Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.

发明人： Tinti, Maria Ornella ,  Misiti, Domenico ,  Cavazza, Claudio

IPC分类号： C07C229/22 ,  A61K31/22

CPC分类号： C07C229/22

摘要： The L-carnitine ester with gamma-hydroxybutyric acid and its pharmacologically accceptable salts of formula (I)
wherein X⁻ 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 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： 左旋肉碱酯与γ-羟丁酸和式或其药理学accceptable盐（I） worin X < - >是药理学可接受的盐的阴离子，E.G. 氯化物，溴化物，乳清酸盐，酸式天冬氨酸盐，酸式柠檬酸盐，酸式磷酸盐，酸式富马酸盐，乳酸盐，马来酸，草酸盐，酸式硫酸盐和磷酸葡萄糖都在积极抑制神经元变性（如它的阿耳茨海默氏老年性痴呆症和帕金森氏病发生时），并在 治疗昏迷。

公开(公告)号：EP0169821B1

公开(公告)日：1991-02-06

申请号：EP85830182.3

申请日：1985-07-16

申请人： Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.

发明人： Colombo, Paolo ,  Conte, Ubaldo ,  Reiner, Alberto

IPC分类号： A61K9/22

CPC分类号： A61K9/209 ,  Y10S514/965

公开(公告)号：EP0402322A3

公开(公告)日：1991-01-02

申请号：EP90830159.1

申请日：1990-04-11

申请人： Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.

发明人： Tinti, Maria Ornella ,  Misiti, Domenico

IPC分类号： C07C227/34 ,  C07C229/26

CPC分类号： C07C227/34

摘要： A process for the production of R(+)-aminocarnitine and S(-)-aminocarnitine is disclosed by resolution of the mixture of the diastereoisomers of N-(alpha-methylbenzyl) aminocarnitine benzyl ester chloride, wherein the separated diastereoisomers are subsequently debenzylated to give R(+)-aminocarnitine chloride and S(-)-aminocarnitine chloride.

公开(公告)号：EP0309421A3

公开(公告)日：1990-05-02

申请号：EP88830373.2

申请日：1988-09-19

申请人： SIGMA TAU Industrie Farmaceutiche Riunite S.p.A.

发明人： Bagolini, Carlo Alberto ,  Pacifici, Licia ,  Quaresima, Emma Teresa

IPC分类号： C07C309/18 ,  A61K31/205

CPC分类号： A61K31/205 ,  C07C309/14

摘要： O-alkanoyl derivatives of 3-amino-2-hydroxypropanesulfonic acid having anticonvulsivant activity and pharmaceutical compositions containing same fot the therapeutical treatment of epilepsy

公开(公告)号：EP0273017A2

公开(公告)日：1988-06-29

申请号：EP87830449.2

申请日：1987-12-21

申请人： SIGMA TAU Industrie Farmaceutiche Riunite S.p.A.

发明人： Marzi, Mauro ,  Tinti, Maria Ornella ,  Di Fabio, Romano ,  Misiti, Domenico

IPC分类号： C07C217/60 ,  A61K31/13

CPC分类号： A61K31/13

摘要： N-alkyl derivatives of 2-amino-6,7-dimethoxy tetraline having general formula (I)
    wherein R is selected from hydrogen, ethyl, n-propyl and methyl cycloproyl;
    R₁ is selected from hydrogen, hydroxy and -OR₃ wherein R₃ is selected from methyl, ethyl and n-propyl; and
    R₂ is selected from hydrogen, methyl, hydroxy, tri­fluoromethyl, fluoro and methoxy,
are endowed with potent antihypertensive activity.

摘要翻译： 具有通式（I）的2-氨基-6,7-二甲氧基四线 worin的R N-烷基衍生物选自氢，乙基，正丙基和甲基cycloproyl选择; R 1是选自氢，羟基和-OR 3 worin R 3选自甲基，乙基和正丙基; 且R 2选自氢，甲基，羟基，三氟甲基，氟和甲氧基，被赋予了有效的抗高血压活性。

公开(公告)号：EP0150688B1

公开(公告)日：1987-04-22

申请号：EP84830329.3

申请日：1984-12-05

申请人： Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.

发明人： Cavazza, Claudio

IPC分类号： C07C101/30 ,  A61K31/195

CPC分类号： A61K31/195

公开(公告)号：EP0169821A2

公开(公告)日：1986-01-29

申请号：EP85830182.3

申请日：1985-07-16

申请人： Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.

发明人： Colombo, Paolo ,  Conte, Ubaldo ,  Reiner, Alberto

IPC分类号： A61K9/22

CPC分类号： A61K9/209 ,  Y10S514/965

摘要： A delivery device for zero-order release of an active principle into a dissolution fluid includes a reservoir consisting of a solid matrix of a homogeneous mixture of a polymer material, at least a portion of the active principle and an additive soluble in the dissolution fluid with negative heat of solution, a coating on the solid matrix-type reservoir of a first, release rate-controlling insoluble membrane which modulates the active principle release according to the desired kinetics; and a second, protective membrane on the release rate-controlling membrane of a soluble polymer material.

公开(公告)号：EP0150688A1

公开(公告)日：1985-08-07

申请号：EP84830329.3

申请日：1984-12-05

申请人： Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.

发明人： Cavazza, Claudio

IPC分类号： C07C101/30 ,  A61K31/195

CPC分类号： A61K31/195

摘要： Novel L-carnitine and alkanoyl L-carnitine salts and a process for their preparation are disclosed. The salts have general formula
wherein

X- ist an anion selected among acid aspartate, acid citrate, acid phosphate, acid fumarate, lactate, acid maleate, acid oxalate, acid sulphate and orotate;
R is hydrogen provided that X- is other than orotate, or lower alkanoyl selected among acetyl, propionyl and butyryl; and
n is ½ if X - is orotate, and 1 if X- is one of the other anions.

Since they are not hygroscopic, these salts can be easily compounded and are favourably suitable for manufacturing solid administration forms. Their aqueous solutions are less acid than those of the corresponding chlorides: consequently, these salts are also suitable for manufacturing injectable administration forms.

公开(公告)号：EP0742214B1

公开(公告)日：1999-06-16

申请号：EP96830206.7

申请日：1996-04-11

申请人： Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.

发明人： Gobbini, Mauro ,  Ferrari, Patrizia ,  Melloni, Piero ,  Torri, Marco

IPC分类号： C07D307/42 ,  C07D307/46 ,  C07D307/54 ,  C07D307/52 ,  A61K31/58

CPC分类号： C07D307/42 ,  C07D307/46 ,  C07D307/52 ,  C07D307/54