公开(公告)号：US5047433A

公开(公告)日：1991-09-10

申请号：US135335

申请日：1987-12-21

申请人： Mauro Marzi ,  Maria O. Tinti ,  Romano Di Fabio ,  Domenico Misiti

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

IPC分类号： C07C217/74 ,  A61K31/13 ,  A61K31/135 ,  A61P9/12 ,  C07C67/00 ,  C07C213/00 ,  C07C213/02

CPC分类号： A61K31/13

摘要： N-alkyl derivatives of 2-amino-6,7-dimethoxy tetraline having general formula (I) ##STR1## wherein R is selected from hydrogen, ethyl, n-propyl and methyl cyclopropyl;R.sub.1 is selected from hydrogen, hydroxy and --OR.sub.3 wherein R.sub.3 is selected from methyl, ethyl and n-propyl; andR.sub.2 is selected from hydrogen, methyl, hydroxy, trifluoromethyl, fluoro and methoxy,are endowed with potent antihypertensive activity.

公开(公告)号：USRE40861E1

公开(公告)日：2009-07-21

申请号：US11606322

申请日：2006-11-30

申请人： Fabio Giannessi ,  Mauro Marzi ,  Patrizia Minetti ,  Francesco De Angelis ,  Maria O. Tinti ,  Piero Chiodi ,  Arduino Arduini

发明人： Fabio Giannessi ,  Mauro Marzi ,  Patrizia Minetti ,  Francesco De Angelis ,  Maria O. Tinti ,  Piero Chiodi ,  Arduino Arduini

IPC分类号： A61K31/46 ,  C07D453/02

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.

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：US4593043A

公开(公告)日：1986-06-03

申请号：US359732

申请日：1982-03-19

申请人： Maria O. Tinti ,  Emma Quaresima ,  Carlo Bagolini ,  Paolo DeWitt

发明人： Maria O. Tinti ,  Emma Quaresima ,  Carlo Bagolini ,  Paolo DeWitt

IPC分类号： C07C323/52 ,  A61K20060101 ,  A61K31/095 ,  A61K31/195 ,  A61K31/205 ,  A61K31/21 ,  A61K31/22 ,  A61K31/23 ,  A61K31/24 ,  A61K31/255 ,  A61K31/265 ,  A61P3/02 ,  A61P11/00 ,  A61P43/00 ,  C07C20060101 ,  C07C67/00 ,  C07C233/45 ,  C07C313/00 ,  C07C319/14 ,  C07C149/243

CPC分类号： C07C323/00 ,  Y10S424/13

摘要： A novel class of mercapto acyl-carnitines is disclosed, wherein the mercapto acyl radical is the radical of saturated mercapto acids having from 2 to 10 carbon atoms. These mercapto acyl-carnitines are prepared, e.g., by first preparing the corresponding halogen acyl-carnitine and then substituting therein, by nucleophylic substitution, the --SH group for the halogen atom.These mercapto acyl-carnitines are useful therapeutic agents, e.g., for the treatment of intoxications and burns and as mucolytic agents. Dithio diacyl carnitines and hydrochloride salts thereof, which are intermediates, are also disclosed.

摘要翻译： 公开了一类新的巯基酰基肉碱，其中巯基酰基是具有2-10个碳原子的饱和巯基的基团。 这些巯基酰基肉碱例如通过首先制备相应的卤素酰基肉毒碱，然后通过碱基取代代替卤素原子的-SH基来制备。 这些巯基酰基肉碱是有用的治疗剂，例如用于治疗中毒和烧伤以及作为粘液溶解剂。 也公开了作为中间体的二硫代二酰基肉碱及其盐酸盐。

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。