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Class 546/321 - Additional -COO- group bonded directly to the six-membered hetero ring


Subclass of Class 546 - Organic compounds -- part of the class 532-570 series
Definition: Compounds which contain an additional -COO- group bonded
No. of patents: 356
Last issue date: 01/17/2012


1                  
NumberTitleIssue Date
8097729Polymorphic form of lercanidipine hydrochloride and process for the preparation thereof
Processes for the purification of lercanidipine hydrochloride are provided which uses a binary system of an alcohol-containing solvent such as methanol and an aliphatic ester-containing solvent such as isopropyl acetate. Processes for the preparation of substantiall...
01/17/2012
7858801Process for producing enantiomer of amlodipine in high optical purity
The present invention relates to a process for preparation of optically pure (S)-amlodipine-L-hemitartrate DMF solvate comprising the steps of treating (R,S) amlodipine base with L-tartaric acid in the presence of dimethyl formamide and a co-solvent. The invention a...
12/28/2010
7772401Process for the preparation of lercanidipine
The invention provides a novel process for the preparation of lercanidipine or a pharmaceutical acceptable salt using novel intermediates. Thus, 2,N-dimethyl-N-(3,3-diphenylpropy1)-1-amino-2-propanol is reacted with trimethylsilyl chloride in presence of triethyl am...
08/10/2010
7772400Optical resolution method of amlodipine
The present invention relates to a method for optical resolution of amlodipines by using isopropanol solvent and optically active O,O′-dibenzoyl tartaric acid as chiral reagent. More particularly, the present invention relates to a method comprising (a) obtaining ...
08/10/2010
7683179Lercanidipine salts
The present invention relates to new addition salts of lercanidipine comprising lercanidipine and an acid counterion wherein the acid counterion is selected from the group consisting of: (i) inorganic acids, (ii) sulfonic acids, (iii) monocarboxylic acids, (iv) dica...
03/23/2010
7678921Method for the enantiomoeric separation of optical active amlodipine
The present invention relates to the preparation of the (S)-(−)-amlodipine and (R)-(+)-amlodipine by means of enantiomeric separation of racemic amlodipine mixture, in which, L- or D-tartaric acid is used as resolution agent, and organic solvent containing 2-butan...
03/16/2010
7585978Processes of manufacturing substituted-1,4-dihydropyridines, improved aqueous solutions thereof, and processes of manufacturing the solutions
A process of preparing a stable parenteral solution of a 1,4-dihydropyridine salt, such as nicardipine hydrochloride, in an acidic aqueous medium. The presence of L-arginine in the solution enhances the solubility of the salt, which is poorly soluble in water.
09/08/2009
7482464Processes for the preparation of S-(-)-amlodipine
Provided is a process for the preparation of S-(−)-amlodipine from (R,S)-amlodipine in industrial-scale using L-(+)-tartaric acid, which is much cheaper than D-(−)-tartaric acid. ...
01/27/2009
7442714Amlodipine gentisate and a method of its preparation
The present invention relates to an acid salt of amlodipine gentisate and a method of its preparation. More particularly, the present invention relates to a crystalline acid salt of amlodipine gentisate of the following formula 1 prepared by reacting amlodipine and ...
10/28/2008
7320993Aryl-substituted pyridylalkane, alkene, and alkine carboxamides useful as cytostatic useful as cytostatic and immuosuppressive agents
The invention relates to new pyridylalkane, alkene, and alkine acid amides substituted with an aryl and/or heteroaryl residue according to the general formula (I), with a saturated or one or several-fold unsaturated hydrocarbon residue in the carboxylic acid group, ...
01/22/2008
7303768Preparation of aqueous clear solution dosage forms with bile acids
Compositions for pharmaceutical and other uses comprising clear aqueous solutions of bile acids which do not form any detectable precipitates over selected ranges of pH values of the aqueous solution and methods of making such solutions. The compositions of the inve...
12/04/2007
7279492S-(−)-amlodipine nicotinate and process for the preparation thereof
The present invention provides a novel salt of S-(−)-amlodipine, i.e., a nicotinic acid salt of S-(−)-amlodipine, a process for preparing the same, and a pharmaceutical composition comprising the same as an active ingredient. ...
10/09/2007
7247645Dihydropyridine derivatives
Compounds having a selective N-type calcium channel antagonistic activity are provided. Dihydropyridine derivatives represented by the following formula: analogs thereof and pharmaceutically acceptable salts ther...
07/24/2007
72355701,4-dihydropyridine and pyridine compounds as calcium channel blockers
The present invention is directed in part towards methods of modulating the function of calcium channels with pyridine- or 1,4-dihydropyridine-based compounds. In addition, the invention describes methods of preventing and treating protein kinase-related abnormal co...
06/26/2007
7202365Processes for the preparation of S-(-)-amlodipine
Provided is a process for the preparation of S-(−)-amlodipine from (R,S)-amlodipine in industrial-scale using L-(+)-tartaric acid, which is much cheaper than D-(−)-tartaric acid. ...
04/10/2007
7199247Amide derivative of amlodipine
A derivative of amlodipine having the following formula is useful as a pharmaceutical, either alone or in combination with amlodipine, in treating angina and hypertension. ...
04/03/2007
7157583Process for producing high-purity 2,3-pyridinedicarboxylic acid
A process for producing 2,3-pyridinedicarboxylic acid having a significantly decreased heavy metal content and capable of satisfying the purity level required for medicinal and agricultural chemicals comprising the steps of: adding at least one sulfur-containing sub...
01/02/2007
7153970High purity amlodipine benzenesulfonate and a process for its preparation
3-ethyl 5-methyl (+/−) 2-[(2-aminoethoxy)methyl]-4-(2-chlorophenyl)-1,4-dihydro-6-methyl-3,5-pyridinedicarboxylate benzenesulfonate, containing overall impurities of significantly less than 0.3% is disclosed, as well as process for its preparation, according to wh...
12/26/2006
7148358Process for the preparation of S(−) amlodipine-L(+)-hemi taratarte
The present invention relates to a process for the preparation of [S(−) amlodipine-L(+)-hemi taratarte] from RS amlodipine base using L(+) tartaric acid in the presence of dimethyl sulfoxide. ...
12/12/2006
7115638Amide derivative of amlodipine
A derivative of amlodipine having the following formula is useful as a pharmaceutical, either alone or in combination with amlodipine, in treating angina and hypertension ...
10/03/2006
7115632Sulfonyl aryl or heteroaryl hydroxamic acid compounds
A sulfonyl aromatic or heteroaromatic ring hydroxamic acid compound that inter alia inhibits matrix metalloprotease activity is disclosed as are a treatment process that comprises administering a contemplated sulfonyl aromatic or heteroaromatic ring hydroxamic acid ...
10/03/2006
7101909Calcium channel drugs and uses
Novel multibinding compounds are disclosed. The compounds of this invention comprise 2–10 ligands covalently connected, each of the ligands being capable of binding to a ligand binding site in a Ca++ channel, thereby modulating the biological activities...
09/05/2006
7060838Industrial process for the synthesis of isobutyl methyl 1,4-dihydro-2,6-dimethyl-4-(2-nitrophenyl)-3,5-pyridine dicarboxylate (nisoldipine)
Synthetic process of isobutyl methyl 1,4,-dihydro-2,6-dimethyl-4-(2-nitrophenyl)3,5-pyridine dicarboxylate (Nisoldipine) comprising on the reaction of isobutyl 2-(2-nitrobenzylidene)acetoacetate with methyl 3-aminocrotonate in an apolar solvent. ...
06/13/2006
7015238Crystalline organic acid salt of amlodipine
A novel crystalline organic acid salt of amlodipine having improved physiochemical properties, a preparation method thereof and a pharmaceutical composition comprising the same are provided. ...
03/21/2006
7009058Method for preparing pyridine-2,3-dicarboxylic acid esters
A method for preparing pyridine-2,3-dicarboxylic acid esters of the general formula: wherein R is C1-6-alkyl, C3-6-cycloalkyl, aryl or arylalkyl, and R1 to R3, independently o...
03/07/2006
6936625Amlodipine camsylate and method for preparing thereof
Amlodipine camsylate of the present invention is a crystalline salt of amlodipine suitable for pharmaceutical formulation, which is prepared by using low toxic camphor sulfonic acid to meet required pharmaceutical properties for treating cardiovascular diseases....
08/30/2005
6919087Pharmaceutical compositions comprising amlodipine maleate
An amlodipine maleate pharmaceutical composition is provided with good stability when formulated with a pH within the range of 5.5 to 7, when measured as a 20 wt % aqueous slurry. The stability can also be aided by making the pharmaceutical composition from amlodipi...
07/19/2005
6903124Organic acid salt of amlodipine
Disclosed are a novel organic acid salt of amlodipine, its preparation method, and a pharmaceutical composition containing as a therapeutically active ingredient the same. ...
06/07/2005
6890944Organic acid salt of amlodipine
Disclosed are a novel organic acid salt of amlodipine, its preparation method, and a pharmaceutical composition containing the same as a therapeutically active ingredient. ...
05/10/2005
6858747Process to prepare, 1,4-dihydropyridine intermediates and derivatives thereof
An improved catalyst is disclosed for a process involving the preparation of benzylidene intermediates useful in the preparation of 1,4-dihydropyridine compounds and derivatives thereof useful as medicines such as for example felodipine. This is accomplished by the ...
02/22/2005
68527421,4-dihydropyridine and pyridine compounds as calcium channel blockers
The present invention is directed in part towards methods of modulating the function of calcium channels with pyridine- or 1,4-dihydropyridine-based compounds. In addition, the invention describes methods of preventing and treating protein kinase-related abnormal co...
02/08/2005
6846932Process for preparation of chiral amlodipine salts
A process for the preparation of pharmaceutically acceptable salts of chiral Amlodipine namely S(−) Amlodipine and R(+) Amlodipine from without isolation of a free base from with optical purity rank between 96-99% is described in the present invention. The process...
01/25/2005
6846931Organic acid salt of amlodipine
Disclosed are a novel organic acid salt of amlodipine, its preparation method, and a pharmaceutical composition containing the same as a therapeutically active ingredient. ...
01/25/2005
6828339Amlodipine salt forms and processes for preparing them
Amlodipine besylate forms are described, including amlodipine besylate hydrates and novel amlodipine besylate anhydrates. A method of making various amlodipine besylate forms from an aqueous medium as well as the use of the same as a calcium channel blocker are desc...
12/07/2004
6822099Method of resolving amlodipine racemate
The invention relates to methods of resolving racemic amlodipine into enantiomerically enriched compositions by precipitation with tartaric acid in the presence of a non-aqueous solvent, such as N,N′-dimethylacetamide. The molar ratio of tartaric acid:amlodipine i...
11/23/2004
6818200Method of using deuterated calcium channel blockers
A method of enhancing the efficiency and increasing the duration of action of drugs (e.g. dihydropyridines and anti-bacterials) and particularly of nifedipine and penicillins wherein one or more hydrogen atoms are deuterated and wherein the deuterated drug has unexp...
11/16/2004
67943991,4-dihydropyridine derivative with a guaiacoxypropanolamine and/or phenoxypropanolamine moiety
The invention disclosed some 1,4-dihydropiridine derivative chemically with guaiacoxypropanolamine based phenoxypropanolamine moiety and pharmacologically with β-adrenoceptor blocking and partial β2-agonist activities, is now emerging. The compou...
09/21/2004
6784297Process for the preparation of anti-ischemic and anti-hypertensive drug amlodipine besylate
Process for the preparation of anti-ischemic and anti-hypertensive drug amlodipine besylate [2-{(2-aminoethoxy)-methyl-4-(2-chlorophenyl) 3-ethoxy carbonyl-5-methoxycarbonyl-6-methyl-1,4-dihydropyridine} benzene sulphonate]. Phthalic anhydride is condensed with mono...
08/31/2004
6726894Transport vehicles for macromolecules
The invention relates to new compounds with the general formula I for use as a tool to introduce macromolecules into cells. The invention further relates to compositions for introducing macromolecules into cells, comprising vesicles formed by at least one compound i...
04/27/2004
6680334Crystalline material
The present invention relates to amlodipine free base in a crystalline form, to pharmaceutical formulations comprising such material, processes of manufacture and its use in therapy....
01/20/2004
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