Abstract: 4-[(Haloalkyl)(dimethyl)ammonio]butanoates of formula wherein Hal is Cl or F, n=1 or 2, method for preparing thereof and use thereof for treating cardiovascular disease.
Type:
Grant
Filed:
April 27, 2012
Date of Patent:
January 27, 2015
Assignee:
JSC Grindeks
Inventors:
Ivars Kalvins, Edgars Liepins, Einars Loza, Maija Dambrova, Ilmars Stonans, Daina Lola, Janis Kuka, Osvalds Pugovics, Viktors Andrianovs, Marina Makrecka, Daina Gustina, Solveiga Grinberga
Abstract: The invention relates to the 5S,4R-enantiomer of 2-(5-methyl-2-oxo-4-phenyl-pyrrolidin-1-yl)-acetamide with cognition enhancing activity of high pharmacological value and to its preparation method which includes the synthesis of 5S-methyl-4R-phenylpyrrolidin-2-one, its N-alkylation with ethyl haloacetate and the treatment of intermediate ethyl 2-(5S-methyl-2-oxo-4R-phenyl-pyrrolidin-1-yl)-acetate with ammonia.
Type:
Grant
Filed:
November 4, 2010
Date of Patent:
July 29, 2014
Assignee:
JSC Grindeks
Inventors:
Ivars Kalvins, Antons Lebedevs, Aleksandrs Cernobrovijs, Maija Dambrova, Liga Zvejniece, Maksims Vorona, Grigorijs Veinbergs
Abstract: 4-[(Haloalkyl)(dimethyl)ammonio]butanoates of formula wherein Hal is Cl or F, n=1 or 2, method for preparing thereof and use thereof for treating cardiovascular disease.
Type:
Application
Filed:
April 27, 2012
Publication date:
April 17, 2014
Applicant:
JSC GRINDEKS
Inventors:
Ivars Kalvins, Edgars Liepins, Einars Loza, Maija Dambrova, Ilmars Stonans, Daina Lola, Janis Kuka, Osvalds Pugovics, Viktos Andrianovs, Marina Makrecka, Daina Gustina, Solveiga Grinberga
Abstract: New compounds of 2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylic acid ester type having general formula I wherein R is a lower alkyl group, which is methyl or ethyl R1 and R2 is sodium carboxylate-methyl ester, having synergistic cytotoxic effect combined with 5-fluorouracil.
Abstract: 2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylic acid ester type compounds having general formula I wherein R is hydrogen or carboxylate-methyl ester, R1 is sodium carboxylate-methyl ester R2 is methyl, ethyl or sodium carboxyate-methyl ester possessing antiviral efficacy.
Abstract: The invention provides an improved, highly efficient method for preparing 5-(2-ethyl-2,3-dihydro-1H-inden-2-yl)-1H-imidazole, and its salts, in particular its pharmaceutically acceptable salts.
Abstract: The invention relates to the 5S,4R-enantiomer of 2-(5-methyl-2-oxo-4-phenyl-pyrrolidin-1-yl)-acetamide with cognition enhancing activity of high pharmacological value and to its preparation method which includes the synthesis of 5S-methyl-4R-phenylpyrrolidin-2-one, its N-alkylation with ethyl haloacetate and the treatment of intermediate ethyl 2-(5S-methyl-2-oxo-4R-phenyl-pyrrolidin-1-yl)-acetate with ammonia.
Type:
Application
Filed:
November 4, 2010
Publication date:
August 23, 2012
Applicant:
JSC Grindeks
Inventors:
Ivars Kalvins, Antons Lebedevs, Aleksandrs Cernobrovijs, Maija Dambrova, Liga Zvejniece, Maksims Vorona, Grigorijs Veinbergs
Abstract: A method for preparation of 6-[3-(1-adamantyl)-4-methoxyphenyl]-2-naphthoic acid is disclosed based on “one pot” synthesis approach including a direct synthesis of boronic acid derivative from 2-(1-adamantyl)-4-bromoanisole and cycloboranes with a subsequent Suzuki-Miyaura coupling with 6-halonaphtenoates and basic hydrolysis of the reaction product in ethylene glycol or 1,2-propanediol.
Type:
Grant
Filed:
December 28, 2007
Date of Patent:
February 21, 2012
Assignee:
JSC Grindeks
Inventors:
Ivars Kalvinsh, Aleksandrs Chernobrovijs, Vyacheslav Tribulovich, Vladimir Labeish
Abstract: New compounds of 2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylic acid ester type having general formula I wherein R is a lower alkyl group, which is methyl or ethyl R1 and R2 is sodium carboxylate-methyl ester, having synergistic cytotoxic effect combined with 5-fluorouracil.
Abstract: The invention provides an improved, highly efficient method for preparing Medetomidine, and its salts, in particular its pharmaceutically acceptable salts. The method utilizes the high reactivity of halogenated imidazoles towards transmetalation with Grignard reagents and the subsequent reaction with 2,3-dimethylbenzaldehyde.
Abstract: Novel medical use of 3-(2,2,2-trimethylhydrazinium) propionate salts for the manufacture of a medicament for prevention and therapy of atherosclerosis.
Type:
Application
Filed:
December 3, 2008
Publication date:
September 16, 2010
Applicant:
JSC GRINDEKS
Inventors:
Ilmars Stonans, Eduard Tararak, Elena Andreyeva