公开(公告)号：US5272151A

公开(公告)日：1993-12-21

申请号：US854916

申请日：1992-03-20

申请人： Mauro Marzi ,  Patrizia Minetti ,  Piero Foresta ,  Maria O. Tinti

发明人： Mauro Marzi ,  Patrizia Minetti ,  Piero Foresta ,  Maria O. Tinti

IPC分类号： A61K31/505 ,  A61K31/519 ,  A61K38/00 ,  A61P31/04 ,  A61P35/00 ,  A61P37/00 ,  A61P37/04 ,  C07D487/04 ,  C07K5/04 ,  C07K5/06 ,  C07K5/08 ,  C07K5/10 ,  C07K7/06 ,  A61K31/495

CPC分类号： C07K5/06026 ,  C07K5/04 ,  A61K38/00

摘要： The present invention concerns aminoacyl and oligopeptidyl derivatives of allopurinol (1,5-dihydro-4H-pyrazolo-[3,4-d]-pyrimidin-4-one) of general formula (I), and related salts with ##STR1## pharmacologically-acceptable cations, in which n is an integer between 2 and 6, preferably 5, Y is H or CO--A, in which A is a racemic or chiral amino acid, dipeptide, tripeptide, tetrapeptide, or pentapeptide chosen, respectively, from the groups consisting of:a) arginine, aspartic acid, lysine, leucine;b) glycylaspartate, glycylglycine, aspartylarginine, leucylarginine, alanylglycine;c) arginyllysylaspartate, aspartyllysylarginine, lysylprolylarginine, prolylprolylarginine, lysylhistidylglycinamide, prolylphenylalanylarginine, phenylalanylprolylarginine;d) arginyllysylaspartylvaline, valylaspartyllysylarginine, threonylvalylleucylhistidine;e) arginyllysylaspartylvalyltyrosine.

公开(公告)号：US5192759A

公开(公告)日：1993-03-09

申请号：US809874

申请日：1991-12-18

申请人： Fabio Giannessi ,  Orlando Ghirardi ,  Domenico Misiti ,  Maria O. Tinti ,  Roberto Cozzolino

发明人： Fabio Giannessi ,  Orlando Ghirardi ,  Domenico Misiti ,  Maria O. Tinti ,  Roberto Cozzolino

IPC分类号： A61K31/135 ,  A61K31/195 ,  A61P25/28 ,  C07C229/22 ,  C07C233/23 ,  C07C237/04 ,  C07C237/10 ,  C07D207/16 ,  C07D207/26 ,  C07D207/27 ,  C07D207/273 ,  C07D207/28 ,  C07D211/76 ,  C07D223/10

CPC分类号： C07D207/27 ,  C07C229/22 ,  C07D207/16 ,  C07D207/273 ,  C07D207/28 ,  C07D211/76 ,  C07D223/10

摘要： 1,2,3,4-tetrahydronaphthlamines of formula (1) ##STR1## wherein R is H or OCH.sub.3 ; ##STR2## is either at 1 or 2 position R.sub.1 is H;R.sub.2 is selected from:L-prolyl, optionally N-substituted with acetyl or carbobenzoxy,L-pyroglutamyl,(pyrrolidin-2-one-1-yl)acetyl,3-carboxy-2-hydroxypropyl:or R.sub.1 and R.sub.2 taken together with the nitrogen atom form the ring ##STR3## wherein n=1,2,3 and R.sub.3 -H, OH are nootropic substances potent enhancers of learning processes and memory.Orally or parenterally administrable pharmaceutical compositions in unit dosage form comprise between about 100 and about 500 mg of a compound of formula (1).

公开(公告)号：US5061725A

公开(公告)日：1991-10-29

申请号：US551951

申请日：1990-07-12

申请人： Fabio Giannessi ,  Orlando Ghirardi ,  Domenico Misiti ,  Maria O. Tinti ,  Carlo Sclolastico

发明人： Fabio Giannessi ,  Orlando Ghirardi ,  Domenico Misiti ,  Maria O. Tinti ,  Carlo Sclolastico

IPC分类号： A61K31/40 ,  A61K31/4015 ,  A61P25/28 ,  C07D207/26 ,  C07D207/27 ,  C07D207/273 ,  C07D401/12 ,  C07F9/572

CPC分类号： C07D207/27 ,  C07D207/273 ,  C07D401/12 ,  C07F9/5721

摘要： (Pyrrolidin-2-one-1-yl)acetamides of general formula (I) ##STR1## wherein R is hydrogen or hydroxyl, R.sub.1 is hydrogen, R.sub.2 is selected from the group consisting of:2-aminoethyl,2-(N,N-diisopropyl) aminoethyl,3-(pyrrolidin-2-one-1-yl) propyl,2-[N-(pyrrolidin-2-one-1-yl) acetyl] aminoethyl,2-hydroxyethyl,(glycerophosphorylethanolamino) carbonylmethyl,1-trimethylammonium-3-carboxy-2-propyloxy-carbonylmethyl chloride,(prolinol-1-yl) carbonylmethyl,1-trimethylammonium-3-carboxyisopropyl), and3-pyridylcarbamide;or R.sub.1 and R.sub.2 taken together, are such as to form a cycle of formula ##STR2## wherein R.sub.3 is selected from the group consisting of phenyl substituted with halogens or halogen-substituted lower (C.sub.1 -C.sub.4) alkyls and 4-morpholinocarbonylmethyl are potent enhancers of learning and memory.Orally or parenterally administrable pharmaceutical compositions in unit dosage form comprise from about 100 to 500 mg of one of the compound of formula (I).

公开(公告)号：US4812478A

公开(公告)日：1989-03-14

申请号：US67694

申请日：1987-06-29

申请人： Maria O. Tinti ,  Carlo A. Bagolini ,  Domenico Misiti ,  Carlo Scolastico

发明人： Maria O. Tinti ,  Carlo A. Bagolini ,  Domenico Misiti ,  Carlo Scolastico

IPC分类号： C07C279/14 ,  C07C149/243 ,  A61K31/22

CPC分类号： C07C279/14 ,  Y02P20/55

摘要： L-aminoacyl derivatives of L-carnitine of general formula (I) ##STR1## wherein R is an alkyl radical selected from 1-methyl-propyl, isobutyl, isopropyl, mercaptomethyl and 3-guanidino propyl, and their pharmacologically acceptable salts, are prepared e.g. by reacting a solution in an organic solvent of L-carnitine whose carboxyl group is protected with an N-protected aminoacid in the presence of a condensing agent and then removing the aminoacid and carnitine protecting groups, thus obtaining the desired compound.

摘要翻译： 通式（I）的L-肉碱的L-氨基酰基衍生物其中R是选自1-甲基 - 丙基，异丁基，异丙基，巯基甲基和3-胍基丙基的烷基，以及它们的药理学上可接受的盐 ，准备例如 通过在缩合剂的存在下使羧基受保护的L-肉碱的有机溶剂中的溶液与N-保护的氨基酸反应，然后除去氨基酸和肉碱保护基团，由此得到所需化合物。

公开(公告)号：US4600794A

公开(公告)日：1986-07-15

申请号：US750690

申请日：1985-06-28

申请人： Maria O. Tinti

发明人： Maria O. Tinti

IPC分类号： C07C227/06 ,  A61K20060101 ,  C07C20060101 ,  C07C67/00 ,  C07C227/00 ,  C07C227/08 ,  C07C227/18 ,  C07C229/22 ,  C07C101/30

CPC分类号： C07C229/22 ,  C07C227/08 ,  C07C227/18

摘要： Gamma dimethylamino L-beta hydroxy butyric acid (L-norcarnitine) is prepared by reacting gamma-iodo beta hydroxy butyric acid octyl ester with dimethylamine in a lower alkanol, e.g. ethanol, thereby obtaining a mixture of the hydroiodides of the gamma-dimethylamino L-beta hydroxy butyric acid ethyl ester and dimethylamide (in a molar ratio of about 60:40). The mixture is eluted on a weakly basic ion exchange resin activated in the OH.sup.- form in order to remove the iodide ions. Upon subsequent alkaline hydrolysis the desired compound is obtained.

摘要翻译： γ-氨基丁酸丁酯（L-norcarnitine）是通过使γ-碘代丁羟酸辛酯与低级链烷醇中的二甲胺反应来制备的。 乙醇，从而得到γ-二甲基氨基L-β羟基丁酸乙酯和二甲基酰胺（摩尔比约为60:40）的氢碘酸盐的混合物。 将该混合物在以OH-形式活化的弱碱性离子交换树脂上洗脱，以除去碘离子。 随后碱性水解，得到所需化合物。

公开(公告)号：US4599447A

公开(公告)日：1986-07-08

申请号：US750689

申请日：1985-06-28

申请人： Maria O. Tinti

发明人： Maria O. Tinti

IPC分类号： C07C227/18 ,  A61K20060101 ,  A61K31/195 ,  C07C20060101 ,  C07C67/00 ,  C07C215/08 ,  C07C227/00 ,  C07C229/02 ,  C07C229/22 ,  C07C101/30

CPC分类号： C07C227/18

摘要： L-norcarnitine hydrochloride gamma-dimethylamino L-beta-hydroxy butyric acid hydrochloride is prepared by demethylation of L-carnitine chloride with 1,4-diazabicyclo[2,2,2]-octane as demethylating agent.

摘要翻译： L-左旋肉碱盐酸盐通过L-肉碱氯化物与1,4-二氮杂双环[2,2,2] - 辛烷的去甲基化作为去甲基化剂制备γ-二甲基氨基L-β-羟基丁酸盐酸盐。

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。

公开(公告)号：US5637614A

公开(公告)日：1997-06-10

申请号：US639431

申请日：1996-04-29

申请人： Piero Foresta ,  Mauro Marzi ,  Maria O. Tinti

发明人： Piero Foresta ,  Mauro Marzi ,  Maria O. Tinti

IPC分类号： A61K31/135 ,  A61K31/216 ,  A61K31/675 ,  A61P37/00 ,  C07C211/38 ,  C07C217/74 ,  C07C219/26 ,  A61K31/225 ,  C07C69/00

CPC分类号： C07C219/26 ,  A61K31/135 ,  A61K31/216 ,  A61K31/675 ,  C07C2102/10

摘要： 6,7-disubstituted-2-aminotetralines of general formula (1) ##STR1## and their pharmacologically acceptable salts, wherein X and Y, identical or different are selected from the group consisting of methoxy, acetoxy and fluoro; and R and R.sub.1, identical or different, are selected from the group consisting of hydrogen, ethyl, propyl, cyclopropylmethyl, 2-hydroxy-2-phenylethyl, 2-hydroxy-2-(4-methylphenyl)ethyl and 2-hydroxy-3-(4-methoxyphenoxy)propyl are endowed with immunomodulator activity.

摘要翻译： 通式（1）的6,7-二取代-2-氨基四氢萘酮（1）及其药理学上可接受的盐，其中X和Y相同或不同选自甲氧基，乙酰氧基和氟; 和R和R 1相同或不同，选自氢，乙基，丙基，环丙基甲基，2-羟基-2-苯基乙基，2-羟基-2-（4-甲基苯基）乙基和2-羟基-3 - （4-甲氧基苯氧基）丙基具有免疫调节剂活性。

公开(公告)号：US5625085A

公开(公告)日：1997-04-29

申请号：US274686

申请日：1994-07-14

申请人： Piero Foresta ,  Vito Ruggiero ,  Maria O. Tinti ,  Nazareno Scafetta

发明人： Piero Foresta ,  Vito Ruggiero ,  Maria O. Tinti ,  Nazareno Scafetta

IPC分类号： A61K31/195 ,  A61K31/22 ,  A61P39/02 ,  C07C229/22 ,  C07C229/00

CPC分类号： C07C229/22 ,  A61K31/22

摘要： Esters of alkanoyl L-carnitines wherein the alkanoyl is a saturated or unsaturated, straight or branched alkanoyl having 2-26 carbon atoms, optionally .omega.-substituted with trialkylammonium, dialkylsulfonium, hydroxyl, carboxyl, halogen, methanesulfonyl and hydroxysulfonyl, are useful for preparing pharmaceutical compositions for the treatment of endotoxic shock.

摘要翻译： 烷酰基L-肉碱的酯，其中烷酰基是具有2-26个碳原子的饱和或不饱和的直链或支链烷酰基，任选被三烷基铵，二烷基锍，羟基，羧基，卤素，甲磺酰基和羟基磺酰基取代的ω-取代，可用于制备药物 用于治疗内毒素性休克的组合物。

公开(公告)号：US5547986A

公开(公告)日：1996-08-20

申请号：US412858

申请日：1995-03-29

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

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

IPC分类号： A61K31/19 ,  A61K31/205 ,  A61P25/26 ,  A61P25/28 ,  C07C229/22 ,  A61K31/225

CPC分类号： C07C229/22

摘要： The L-carnitine ester with gamma-hydroxybutyric acid and its 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 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： 具有γ-羟基丁酸的L-肉碱酯及其药学上可接受的式（I）的盐其中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，酸式硫酸盐和磷酸葡萄糖酸盐对抑制神经元变性（如在阿尔茨海默病老年痴呆和帕金森病中发生） 治疗昏迷。