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| Number | Title | Issue Date |
| 8097729 | Polymorphic 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 |
| 7858801 | Process 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 |
| 7772401 | Process 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 |
| 7772400 | Optical 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 |
| 7683179 | Lercanidipine 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 |
| 7678921 | Method 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 |
| 7585978 | Processes 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 |
| 7482464 | Processes 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 |
| 7442714 | Amlodipine 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 |
| 7320993 | Aryl-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 |
| 7303768 | Preparation 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 |
| 7279492 | S-(−)-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 |
| 7247645 | Dihydropyridine 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 |
| 7235570 | 1,4-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 |
| 7202365 | Processes 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 |
| 7199247 | Amide 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 |
| 7157583 | Process 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 |
| 7153970 | High 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 |
| 7148358 | Process 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 |
| 7115638 | Amide 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 |
| 7115632 | Sulfonyl 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 |
| 7101909 | Calcium 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 |
| 7060838 | Industrial 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 |
| 7015238 | Crystalline 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 |
| 7009058 | Method 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 |
| 6936625 | Amlodipine 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 |
| 6919087 | Pharmaceutical 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 |
| 6903124 | Organic 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 |
| 6890944 | Organic 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 |
| 6858747 | Process 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 |
| 6852742 | 1,4-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 |
| 6846932 | Process 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 |
| 6846931 | Organic 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 |
| 6828339 | Amlodipine 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 |
| 6822099 | Method 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 |
| 6818200 | Method 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 |
| 6794399 | 1,4-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 |
| 6784297 | Process 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 |
| 6726894 | Transport 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 |
| 6680334 | Crystalline 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 |