Additional -coo- Group Bonded Directly To The Six-membered Hetero Ring Patents (Class 546/321)
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Patent number: 6822099Abstract: 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 is preferably less than 0.25:1.0 or greater than 0.75:1.0.Type: GrantFiled: December 20, 2002Date of Patent: November 23, 2004Assignee: Sepracor, Inc.Inventors: Chris H. Senanayake, Gerald J. Tanoury, Harold S. Wilkinson, Roger P. Bakale, Andrei A. Zlota
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Patent number: 6818200Abstract: 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 unexpectedly improved properties when used in much lower concentrations than unmodified drug. A method for determining the identity and bioequivalency of a new drug is also disclosed wherein the molecular and isotope structure of a new drug is determined by isotope ratio mass spectrometry and compared with the molecular and isotope structure of a known human drug.Type: GrantFiled: November 14, 2001Date of Patent: November 16, 2004Assignee: Isotechnika Inc.Inventors: Robert T. Foster, Richard Lewanczuk, Gilles Caille
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Patent number: 6794399Abstract: The invention disclosed some 1,4-dihydropiridine derivative chemically with guaiacoxypropanolamine based phenoxypropanolamine moiety and pharmacologically with &bgr;-adrenoceptor blocking and partial &bgr;2-agonist activities, is now emerging. The compound of 1,4-dihydropiridine derivative wherein has the formula I, wherein R selected from four group as follow R1 selected from X, H, NO2 saturated C1-C6 alkyl chain, unsaturated C6-C6 alkyl chain, R2 selected from H, CH3 R3 and R4 are individually selected from saturated C1-C6 alkyl chain, unsaturated C1-C6 alkyl chain; R5 selected from OH, saturated C1-C6 alkyl chain, unsaturated C1-C6 alkyl chain.Type: GrantFiled: April 11, 2002Date of Patent: September 21, 2004Inventor: Ing-Jun Chen
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Patent number: 6784297Abstract: 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 monoethanol amine at 150-190° C. The resulting N-(2-hydroxyethyl) phthalimide is coupled with 4-chloroethyl acetoacetate in the presence of sodium hydride in an organic solvent in an inert atmosphere at −11 to −15° C. Ethyl-4-[-2(phthalimido) ethoxy] acetoacetate formed is coupled with orthochloro benzaldehyde in the presence of pyridine salt at 70-90° C. Ethyl-2-(2-chloro benzylidine)4-[-2(phthalimido) ethoxy] acetoacetate fanned is condensed with methyl amino crotonate at 20-40° C.Type: GrantFiled: September 4, 2003Date of Patent: August 31, 2004Assignee: Kopran LimitedInventors: Arun Kumar Purohit, Brahmader Chilu Desai, Balasaheb Dashrath Shete, Salim Abbas Bagwan
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Patent number: 6726894Abstract: 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 in a solvent. The macromolecule can be incorporated in the vesicles and/or bound to the vesicles or another aggregate of the new compounds.Type: GrantFiled: December 28, 1998Date of Patent: April 27, 2004Assignee: Synvolux IP B.V.Inventors: Jan Bernard Frederik Nicolaas Engberts, Anno Wagenaar, Dirk Hoekstra, Irene Van Der Woude, Marcel Herman Jozef Ruiters
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Patent number: 6680334Abstract: 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.Type: GrantFiled: August 20, 2002Date of Patent: January 20, 2004Assignee: Pfizer IncInventors: Alan Craig Bentham, Alan John Pettman, Keith Stephen Ruddock
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Patent number: 6649767Abstract: A process for preparing a 1,4-dihydropyridine compound comprising contacting an enamine compound and a compound having a structure of in the presence of a base; and treating the reaction mixture thus obtained in the presence of an acid or a combination of acids under mild reaction conditions. A resulting 1,4-dihydropyridine compound is useful as an anti-inflammatory agent or the like.Type: GrantFiled: August 20, 2002Date of Patent: November 18, 2003Assignee: Pfizer, Inc.Inventors: Kunio Satake, Noriaki Murase
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Patent number: 6646131Abstract: The invention provides a feasible method for the separation of both (S)-(−)-enantiomer and (R)-(+)-enantiomer of racemic amlodipine with higher optically purity. The chiral reagent for separation is tartaric acid and the chiral auxiliary reagent is hexadeuterium dimethyl sulphoxide (DMSO-d6).Type: GrantFiled: August 16, 2002Date of Patent: November 11, 2003Inventor: Xitian Zhang
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Publication number: 20030204093Abstract: 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.Type: ApplicationFiled: May 12, 2003Publication date: October 30, 2003Inventors: Jacobus M. Lemmens, Theodorus H. A. Peters, Franciscus B. G. Benneker
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Patent number: 6608206Abstract: A process for the preparation of S(−) Amlodipine salts which comprises reaction of S(−)Amlodipine base with a solution of pharmaceutically acceptable acid such as benzene sulfonic acid, oxalic acid, maleic acid, succinic acid and p-toluene sulfonic acid. The reaction is carried out in the presence of an organic solvent at room temperature. The organic solvents include alcohols like ethanol methanol 2 propanol hydrocarbons like toluene and polar solvent like dimethyl sulfoxide. The salt is obtained by addition of water and isolation of the salt formed by filtration. The unique feature of the invention is production of S(−) Amlodipine besylate in good chemical yield, high enantiomeric purity and with the quality required for preparation of pharmaceutical composition i.e. tablet formulation.Type: GrantFiled: October 30, 2002Date of Patent: August 19, 2003Assignee: Council of Scientific & Industrial ResearchInventors: Rohini Ramesh Joshi, Ramesh Anna Joshi, Mukund Keshav Gurjar
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Patent number: 6602893Abstract: 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.Type: GrantFiled: August 27, 2001Date of Patent: August 5, 2003Assignee: Synthon BVInventors: Jacobus M. Lemmens, Theodorus H. A. Peters, Franciscus B. G. Benneker
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Patent number: 6600047Abstract: A process for making amlodipine maleate comprises reacting amlodipine or an acid addition salt thereof with maleic acid under an acidic environment to form an amlodipine maleate product. The process allows for the formation of amlodipine maleate substantially free from amlodipine aspartate.Type: GrantFiled: August 27, 2001Date of Patent: July 29, 2003Assignee: Synthon BVInventors: Franciscus B. G. Benneker, Pavel Slanina, Frantisek Picha
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Patent number: 6596874Abstract: The invention relates to a novel process of amalodipine benzenesulphonate of formula (I) by reacting a new 2-[/2-carboxy-benzoyl)-aminoethoxy/methyl/]-4-(2-chlorophenyl)-3-ethoxycarbonyl-5-methoxycarbonyl-6-methyl-1,4-di-hydropyridine derivative of general formula (II) wherein X represents hydrogen or alkali metal or alkali earth metal or quaternary ammonium—with benzenesulphonic acid.Type: GrantFiled: December 20, 2001Date of Patent: July 22, 2003Assignee: Richter Gedeon Vegyeszeti Gyar RT.Inventors: Janos Fischer, Katalin Szöke, Laszlo Dobay, Sandor Leval
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Patent number: 6566359Abstract: A new series of derivatives of 2,4,6-trimethyl-1,4-dihydropyridine-3,5-dicarboxylic acid and their synthesis have been discovered. Surprisingly, by modifying the substituent of the 3-carboxylic acid group, new compounds were produced with high activity as PAF receptor antagonists. These compounds were shown to protect neurons from brain damage that normally occurs in response to stroke and other cerebrovascular diseases. These compounds are also protective against edema generation resulting from traumatic breakdown of the blood-brain barrier. Moreover, these compounds were found to be non-toxic and cytoprotective of cells undergoing oxidative stress that would normally trigger apoptotic cell death; and to have activity as (a) antagonists of an intracellular platelet activating factor (“PAF”)-binding site, (b) inhibitors of PAF- and cytokine-mediated c-aminoterminal jun kinase (JNK) and extracellular regulated kinase (ERK), and (c) transcriptional inhibitors of COX-2 expression.Type: GrantFiled: May 20, 2002Date of Patent: May 20, 2003Assignee: Board of Supervisors of Louisiana State University and Agricultural and Mechanical CollegeInventors: Nicholas G. Bazan, Carlos Sunkel, Victor L. Marcheselli, Julio Builla-G.
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Patent number: 6562824Abstract: This invention relates to novel dihydropyridine soft drugs of the formula &PHgr;OOR1, where &PHgr; is a dihydropyridine moiety. These compounds are useful as calcium channel antagonists with cardiovascular, antiasthmatic and antibroncho-constriction activity. Use of such soft drug analogs permits the administration of greater doses of the claimed dihydropyridine compounds without intolerable systemic effects. Thus, this invention also provides pharmaceutical compositions, as well as methods, for preventing and treating disorders such as hypersensitivity, allergy, asthma, bronchospasim, dysmenorrhea, esophageal spasm, glaucoma, premature labor, urinary tract disorders, gastrointestinal motility disorders and cardiovascular disorders, while avoiding unwanted systemic effects.Type: GrantFiled: May 2, 2001Date of Patent: May 13, 2003Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: John H. Dodd, James L. Bullington, Daniel A. Hall, James R. Henry, Kenneth C. Rupert
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Patent number: 6538012Abstract: Amlodipine hemimaleate is useful as a calcium channel blocker and can be used to treat or prevent angina or hypertension.Type: GrantFiled: August 27, 2001Date of Patent: March 25, 2003Assignee: Synthon BVInventor: Gerrit J. B. Ettema
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Patent number: 6518288Abstract: Amlodipine fumarate salt compounds are useful as calcium channel blockers and in treating or preventing angina or hypertension. The fumarate salts avoid the formation of certain potential impurities that have been found to be associated with amlodipine maleate.Type: GrantFiled: August 27, 2001Date of Patent: February 11, 2003Assignee: Synthon BVInventors: Jacobus M. Lemmens, Theodorus H. A. Peters, Franciscus B. G. Benneker, Frantisek Picha
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Patent number: 6492523Abstract: Amlodipine is prepared in a high yield by subjecting a pyrrole derivative, methyl aminocrotonate and 2-chlorobenzaldehyde to a Hantzsch reaction, and converting the pyrrole residue of the resulting 1,4-dihydropyridine derivative to an amine group by the action of hydroxylamine hydrochloride.Type: GrantFiled: March 11, 2002Date of Patent: December 10, 2002Assignee: Hanmi Pharm. Co., Ltd.Inventors: Young-Ho Moon, Nam-Du Kim, Kyung-Ik Lee, Kwan-Sun Lee
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Patent number: 6479525Abstract: An amlodipine derivative having the following formula is useful, either alone or in combination with amlodipine, as a pharmaceutical in treating angina and hypertension.Type: GrantFiled: August 27, 2001Date of Patent: November 12, 2002Assignee: Synthon BVInventors: Jacobus M. Lemmens, Theodorus H. A. Peters, Franciscus B. G. Benneker
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Patent number: 6476058Abstract: Methods and compositions are disclosed utilizing the optically pure S(−) isomer of amlodipine. This compound is a potent drug for the treatment of hypertension while avoiding the concomitant liability of adverse effects associated with the administration of the racemic mixture of amlodipine. The S(−) isomer of amlodipine is also useful for the treatment of angina and such other conditions as may be related to the activity of S(−) amlodipine as a calcium channel antagonist without the concomitant liability of adverse effects associated with the racemic mixture of amlodipine.Type: GrantFiled: November 15, 2001Date of Patent: November 5, 2002Assignee: Isotechnika, Inc.Inventor: Robert T. Foster
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Patent number: 6407125Abstract: A biological response modifying metal ion chelating agent such as picolinic acid, analogs or derivatives thereof, and methods of using the same. The agents chelate metals in metal containing protein complexes and enzymes required for growth, replication or inflammatory response. The preparations can be administered systemically or topically. The products can be used to reduce systemic levels of metals in disease states such as Wilson's disease, iron or lead toxicity. The preparations have antineoplastic, antiviral, antiinflammatory, analgesic antiangiogenic, antiproliferative as well as hematopoetic and immune stimulant, effects and are used in the treatment of warts, psoriasis, acne, cancers, sunburn, inflammatory responses, untoward angiogenesis, immune depression and other diseases and in the prevention of sexually transmitted diseases such as genital warts, herpes and AIDS.Type: GrantFiled: October 2, 2000Date of Patent: June 18, 2002Assignee: Novactyl, Inc.Inventor: Jose A. Fernandez-Pol
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Patent number: 6403618Abstract: A metal ion chelating agent such as picolinic acid or derivatives thereof, and methods of using the same. The agents chelate metals in metal containing protein complexes and enzymes required for growth and replication of blood vessel cells. The preparations can be administered systemically or for topical use. The preparations have antineoplastic activity augmented by the antiangiogenic properties.Type: GrantFiled: October 2, 2000Date of Patent: June 11, 2002Assignee: Novactyl, Inc.Inventor: Jose A. Fernandez-Pol
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Patent number: 6395903Abstract: Process for the preparation of pure 2,3-pyridinedicarboxylic acids of the formula I which are substituted in position 4 and/or 5 and/or 6 by R1, where R1 is hydrogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 alkoxy-C1-C4 alkyl, halogen, hydroxyl or nitro, from quinolines of the formula II in which R1 is as defined above, and which are substituted in position 6 and/or 7 by R2, where R2 is hydrogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 alkoxy-C1-C4 alkyl, halogen, hydroxyl, nitro or amino, which are reacted in the first step in aqueous sulfuric acid or nitric acid solution with ozone in the ratio of from 1:2 to 1:3 at temperatures from 0 to +50° C., and the resulting peroxide solution is then reacted at temperatures of from +0 to +100° C. in the presence of 0.5-4.0 mol of oxidizing agent per mole of ozonolysis product formed, after which the pH of the reaction solution is adjusted to 0.2 to 3, the mixture is cooled to 0 to 30° C.Type: GrantFiled: May 10, 2000Date of Patent: May 28, 2002Assignee: DSM Fine Chemicals Austria Nfg GmbH & CoKGInventors: Karlheinz Giselbrecht, Eduard Perndorfer, Klaus Reiter
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Publication number: 20020062025Abstract: Process for the preparation of pure 2,3-pyridinedicarboxylic acids of the formula I 1Type: ApplicationFiled: May 10, 2000Publication date: May 23, 2002Inventors: Karlheinz Giselbrecht, Eduard Perndorfer, Klaus Reiter
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Patent number: 6392050Abstract: The invention relates to a process for preparing substituted pyridines in a simple and cost-effective manner in good yields by reacting substituted 1,4-dihydropyridines with methyl nitrite in the presence of an acid that contains less than 20% by weight of oxidizing components.Type: GrantFiled: June 4, 2001Date of Patent: May 21, 2002Assignee: Bayer AktiengesellschaftInventors: Norbert Lui, Hans Panskus, Albert Schnatterer
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Patent number: 6376521Abstract: Disclosed are pyridine and dihydropyridine derivatives, pharmaceutical compositions comprising one or more of these derivatives, and a method of selectively blocking an A3 adenosine receptor of a mammal by the use of one or more of these derivatives. An example of the pyridine derivative is of the formula (I): wherein R2 is ethyl, R3 is ethylsulfanyl; R4 is ethyl, propyl, or hydroxypropyl; R5 is ethyl, propyl, fluoroethyl, or fluoropropyl; and R6 is phenyl or fluorophenyl. The derivatives of the present invention can be used for inhibiting binding of ligands to an adenosine receptor. The derivatives also can be used for characterizing an adenosine receptor.Type: GrantFiled: April 2, 2001Date of Patent: April 23, 2002Assignee: The United States of America as represented by the Secretary of the Department of Health and Human ServicesInventors: Kenneth A. Jacobson, An-Hu Li
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Patent number: 6350766Abstract: Dihydropyridine derivatives of the following formula, analogs thereof and pharmaceutically acceptable salts thereof have an activity of selectively inhibiting the action of N-type calcium channel. They are used as remedies for various diseases relating to the N-type calcium channel such as encephalopathies caused by the ischemia in the acute phase after the onset of cerebral infarction, cerebral hemorrhage or the like, Alzheimer's disease, etc.Type: GrantFiled: October 25, 1999Date of Patent: February 26, 2002Assignee: Ajinomoto Co., Inc.Inventors: Hisayuki Uneyama, Seiji Niwa, Tomoyuki Onishi
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Patent number: 6350877Abstract: A method for the manufacture of clevidipine by reaction of an inorganic salt of 4-(2′,3′-dichlorophenyl)-1,4-dihydro-5-methoxycarbonyl-2,6-dimethyl-3-pyridine-carboxylate and chloro methyl butyrate.Type: GrantFiled: March 8, 2000Date of Patent: February 26, 2002Assignee: AstraZeneca ABInventors: Anders Mattson, Carina Svensson, Karin Thörnblom, Christina Ă–dman
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Patent number: 6333342Abstract: Methods and compositions are disclosed utilizing the optically pure S(−) isomer of amlodipine. This compound is a potent drug for the treatment of hypertension while avoiding the concomitant liability of adverse effects associated with the administration of the racemic mixture of amlodipine. The S(−) isomer of amlodipine is also useful for the treatment of angina and such other conditions as may be related to the activity of S(−) amlodipine as a calcium channel antagonist without the concomitant liability of adverse effects associated with the racemic mixture of amlodipine.Type: GrantFiled: November 4, 1999Date of Patent: December 25, 2001Assignee: Isotechnika, INCInventor: Robert T. Foster
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Patent number: 6294673Abstract: The invention relates to a process for the preparation of nifedipine by the reaction of methyl 2-(2-nitrobenzylidene)acetoacetate and methyl 3-aminocrotonate and the use of the nifedipine thus prepared for the production of a medicament.Type: GrantFiled: April 26, 2000Date of Patent: September 25, 2001Assignee: Bayer AktiengesellschaftInventors: Mathias Berwe, Herbert Diehl, Karl Rittner, Karl-Heinz Wahl, Hans-Peter Wirges
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Patent number: 6262092Abstract: This invention relates to a mutual salt of amlodipine and atorvastatin, pharmaceutical compositions thereof and methods of treating angina pectoris, atherosclerosis and combined hypertension and hyperlipidemia in mammals with such a mutual salt and compositions. This invention also relates to methods of managing cardiac risk in a mammal presenting with symptoms of cardiac risk, including humans by administering such a mutual salt and compositions.Type: GrantFiled: May 24, 2000Date of Patent: July 17, 2001Assignee: Pfizer Inc.Inventors: George Chang, Ernest S. Hamanaka
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Patent number: 6251925Abstract: The present invention relates to therapeutic biaryl derivatives of formula (I), and pharmaceutically acceptable derivatives thereof wherein R1 is a phenyl, naphthyl, pyridyl, thiazolyl, phenoxymethyl, or pyrimidyl group, optionally substituted by one or more substituents selected from the group consisting of halogen, hydroxy, C1-6alkoxy, C1-6alkyl, nitro, cyano, hydroxymethyl, trifluoromethyl, —NR6R6, and —NHSO2R6, where each R6 is independently hydrogen or C1-4alkyl; R2 is hydrogen or C1-6alkyl; X is oxygen, sulfur, —NH, or —NC1-4alkyl; R3 is cyano, tetrazol-5-yl, or —CO2R7 where R7 is hydrogen or C1-6alkyl; R4 and R5 are independently hydrogen, C1-6alkyl, —CO2H, —CO2C1-6alkyl, cyano, tetrazol-5-yl, halogen, trifluoromethyl, or C1-6alkoxy, or, when R4 and R5 are bonded to adjacent carbon atoms, R4 and R5 may, together with the carbon atoms to which they are bonded, form a fused 5 or 6 membered ring optionally containing one or two nitrogen, oxygen,Type: GrantFiled: December 13, 2000Date of Patent: June 26, 2001Assignee: Glaxo Wellcome Inc.Inventors: Kelly Horne Donaldson, Barry George Shearer, David Edward Uehling
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Patent number: 6239155Abstract: Novel phenyl-substituted 1,4-dihydropyridines, prepared by reacting halogenophenyl-aldehydes with &bgr;-ketoesters, if appropriate with isolation of the ylidene compounds and enamines. The substances can be employed as active compounds in medicaments, in particular in cerebrally active compositions.Type: GrantFiled: December 2, 1994Date of Patent: May 29, 2001Assignee: Bayer AktiengesellschaftInventors: Heinrich Meier, Wolfgang Hartwig, Bodo Junge, Rudolf Schohe-Loop, Zhan Gao, Bernard Schmidt, Maarten de Jonge, Teunis Schuurman
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Patent number: 6133450Abstract: Process for recovering a pyridine-2,3-dicarboxylic acid from a process stream in the preparation process of the pyridine-2,3-dicarboxylic acid in which the process stream is subjected to nanofiltration at a pH higher than 4.5 and the pyridine-2,3-dicarboxylic acid-containing concentrate is utilised. Preferably, the pH is chosen to be between 7 and 9 and the concentration factor in nanofiltration greater than 3.In a suitable embodiment the process stream is formed by the mother liquor obtained in the preparation of pyridine-2,3-dicarboxylic acid by oxidising a suitable quinoline or the corresponding 2,3-lutidine and separating the solid material.Type: GrantFiled: April 2, 1999Date of Patent: October 17, 2000Assignee: DSM N.V.Inventors: Veerle Cauwenberg, Peter J. D. Maas, Franciscus H. P. Vergossen
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Patent number: 6127393Abstract: An antiproliferative, antiinflammatory, antiinfective, immunization agent of a metal ion chelating agent such as picolinic acid or derivatives thereof, and methods of using the same. The agents chelate metals in metal containing protein complexes required for growth, replication or inflammatory response. The preparations can be administered systemically or for topical use. The preparations have antineoplastic, antiviral, antiinflammatory and antiproliferative effects and are used in the treatment of warts, psoriasis, acne, skin cancers, sunburn and other proliferative diseases and in the prevention of sexually transmitted diseases such as genital warts, herpes and AIDS. The agents also can be used to induce autologous immunological response.Type: GrantFiled: August 1, 1998Date of Patent: October 3, 2000Assignee: Novactyl, Inc.Inventor: Jose A. Fernandez-Pol
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Patent number: 6080867Abstract: The present invention provides a process to prepare a pyridine-2,3-dicarboxylate derivative via the reaction of a dialkyl alkoxy(or alkylthio)oxalacetate with an appropriately substituted acrolein compound in the presence of an ammonia source and a solvent.The present invention also provides useful intermediate compounds of formula IV.Type: GrantFiled: June 15, 1999Date of Patent: June 27, 2000Assignee: American Cyanamid CompanyInventor: Wen-Xue Wu
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Patent number: 6066655Abstract: 4-Phenyl-3-substituted 1,4-dihydropyridine esters are prepared by reaction of benzaldehydes with ketoesters and enamines, if appropriate with isolation of the ylidene intermediate products, or by esterification of corresponding dihydropyridinecarboxylic acids with alcohols.The new 4-phenyl-3-substituted 1,4-dihydropyridine esters can be employed as active compounds in medicaments for the treatment of the central nervous system, in particular as cerebral therapeutics.Type: GrantFiled: December 10, 1997Date of Patent: May 23, 2000Assignee: Bayer AktiengesellschaftInventors: Heinrich Meier, Wolfgang Hartwig, Bodo Junge, Rudolf Schohe-Loop, Zhan Gao, Bernard Schmidt, Maarten de Jonge, Teunis Schuurman
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Patent number: 6046338Abstract: A method for the separation of R-(+)- and S-(-)-isomers of amlodipine (I) from mixtures thereof, which comprises the reaction of the mixture of isomers with either L- or D-tartaric acid in an organic solvent containing sufficient dimethyl sulphoxide (DMSO) for the precipitation of, respectively, a DMSO, solvate of an L-tartate salt of R-(+)-amlodipine, or a DMSO solvate of a D-tartrate salt of S-(-)-amlodipine.Type: GrantFiled: May 5, 1998Date of Patent: April 4, 2000Assignee: Pfizer Inc.Inventor: Peter Lionel Spargo
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Patent number: 6046337Abstract: The invention relates to a new process for the preparation of amlodipine besylate of the Formula ##STR1## Amlodipine besylate of the Formula I is a valuable known blood pressure decreasing antianginal agent.The advantage of the process of the present invention is that it can be carried out in a simple way with high yields and there is no need to isolate the amlodipine base.Type: GrantFiled: August 12, 1998Date of Patent: April 4, 2000Assignee: EGIS Gyogyszergyar Rt.Inventors: Daniel Bozsing, Gyorgyi Lax Kovanyi, Gyula Simig, Gyorgy Krasznai, Gabor Blasko, Peter Tompe, Kalman Nagy, Gyorgyi Donath Vereczkey, Gabor Nemei, Norbert Nemeth
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Patent number: 6015906Abstract: A method for the preparation of 4-(nitrophenyl)-dihydro-pyridines by reacting a benzaldehyde with an acetoacetate and reacting the resulting benzylidene derivative with an enamine derivative. Both reactions are catalyzed by dimethylamine benzoate or p-anisate.Type: GrantFiled: August 18, 1997Date of Patent: January 18, 2000Assignee: Lusochimica S.p.A.Inventors: Bruno Perego, Elso Manghisi
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Patent number: 6001836Abstract: A series of non-peptidergic antagonists of NPY have been synthesized and are comprised of cyanoguanidine derivatives of 4-phenyl-1,4-dihydropyridines of Formula (I). ##STR1## As antagonists of NPY-induced feeding behavior, these compounds are expected to act as effective anorexiant agents in promoting weight loss and treating eating disorders.Type: GrantFiled: May 26, 1998Date of Patent: December 14, 1999Assignee: Bristol-Myers Squibb CompanyInventors: Graham S. Poindexter, R. Thomas Swann, Marc A. Bruce, Mendi A. Morton, Yazhong Huang, Sing-Yuen Sit, James Guy Breitenbucher
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Patent number: 6002012Abstract: There is provided a process for the preparation of [(5,6-dicarboxy-3-pyridyl)methyl]ammonium halides having the structural formula I ##STR1## The [(5,6-dicarboxy-3-pyridyl)methyl]ammonium halides are useful as intermediates in the preparation of herbicidal 5-(alkoxymethyl)-2-(2-imidazolin-2-yl)-nicotinic acids, esters and salts.Type: GrantFiled: March 20, 1998Date of Patent: December 14, 1999Assignee: American Cyanamid CompanyInventor: Wen-Xue Wu
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Patent number: 5998448Abstract: The invention relates to new combinations of dihydropyridines of the general formula (I) ##STR1## in which R.sup.1 to R.sup.5 have the meaning indicated in the description, for the prevention and treatment of vascular disorders, in particular of cardiovascular and cerebrovascular disorders, containing dihydropyridines having calcium antagonist activity, acetylsalicylic acid nitroesters and vitamins, and, if appropriate, also further auxiliaries or active compounds.Type: GrantFiled: October 24, 1997Date of Patent: December 7, 1999Assignee: Bayer AktiengeselechaftInventors: Eva Lesur, Dieter Neuser, Oswald Lockhoff, Elisabeth Perzborn, Johannes Peter Stasch, Peter Kurka
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Patent number: 5977369Abstract: A novel process is disclosed for the preparation of dihydropyridine compounds and derivatives thereof, and more particularly felodipine. The process to prepare felodipine involves a two step procedure condensing 2,3-dichlorobenzaldehyde with methyl acetoacetate in the presence of a catalyst system. The resultant benzylidine intermediate is sequentially reacted with ethyl aminocrotonate to provide felodipine. The novelty of the present invention resides in part on (1) a new catalyst system not previously disclosed for the preparation of felodipine, (2) the absence of acid(s), (3) the control of reaction conditions to yield lower amounts of unreacted aldehyde compared to known reactions, (4) a simplified purification process, and (5) formation of negligible quantities of symmetrical diester byproducts.Type: GrantFiled: December 28, 1995Date of Patent: November 2, 1999Assignee: Napp Technologies, Inc.Inventors: Ranjit Desai, Daniel Alfonso Aguilar, Mohammad Aslam, Nicholas Gallegos
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Patent number: 5959116Abstract: A pyridine-2,3-dicarboxylic acid diester of the formula Va ##STR1## where the radicals R.sup.2 and R.sup.4 have the meanings set out in the specification and where R.sup.8 is a C.sub.1 -C.sub.4 -alkyl, C.sub.3 -C.sub.5 -alkenyl or C.sub.3 -C.sub.5 -alkynyl radical, which may be substituted by halogen, phenyl or C.sub.1 -C.sub.4 -alkoxy.Type: GrantFiled: July 12, 1996Date of Patent: September 28, 1999Assignee: BASF AktiengesellschaftInventors: Gerhard Hamprecht, Peter Munster, Matthias Gerber, Helmut Walter, Karl-Otto Westphalen
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Patent number: 5955482Abstract: The present invention relates to the use of 1,4-dihydropyridine-3,5-dicarboxylic acid esters, some of which are known, of the general formula (I) ##STR1## in which A and R.sup.1 -R.sup.3 have the meaning given in the description, as medicaments, in particular for treatment of the central nervous system, and new selected active compounds.Type: GrantFiled: March 28, 1997Date of Patent: September 21, 1999Assignee: Bayer AktiengesellschaftInventors: Klaus Urbahns, Otto Behner, Siegfried Goldmann, Hans-Georg Heine, Bodo Junge, Rudolf Schohe-Loop, Egbert Wehinger, Hartmund Wollweber, Henning Sommermeyer, Thomas Glaser, Reilinde Wittka, Jean-Marie-Viktor de Vry
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Patent number: 5942526Abstract: The present invention relates to the new use of 1-alkyl-3,5-diacyl-1,4-dihydropyridines which are known in some cases, of the general formula (I) ##STR1## in which R.sup.1 to R.sup.4 have the meaning indicated in the description, processes for their preparation and their use as medicaments, as selective potassium channel modulators, in particular for the treatment of the central nervous system.Type: GrantFiled: February 11, 1997Date of Patent: August 24, 1999Assignee: Bayer AktiengesellschaftInventors: Klaus Urbahns, Hans-Georg Heine, Thomas Glaser, Reilinde Wittka, Jean-Marie-Viktor De Vry, Henning Sommermeyer
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Patent number: 5942624Abstract: A method for the manufacture of felodipine by reaction of dichlorobenzylidene and ethyl 3-aminocrotonate using an alcohol as solvent.Type: GrantFiled: February 13, 1997Date of Patent: August 24, 1999Assignee: Astra AktiebolagInventors: Anders Gustavsson, .ANG.ke Kallstrom, Sven Palmer
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Patent number: 5925764Abstract: The present invention provides a process to prepare a pyridine-2,3-dicarboxylate derivative via the reaction of a dailkyl alkoxy(or alkylthio)oxalacetate with an appropriately substituted acrolein compound in the presence of an ammonia source and a solvent.The present invention also provides useful intermediate compounds of formula IV.Type: GrantFiled: June 15, 1998Date of Patent: July 20, 1999Inventor: Wen-Xue Wu
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Patent number: 5919792Abstract: This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as vitronectin receptor antagonists. The vitronectin receptor antagonist compounds of the present invention are .alpha.v.beta.3 antagonists, .alpha.v.beta.5 antagonists or dual .alpha.v.beta.3/.alpha.v.beta.5 antagonists useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammation and tumor growth.Type: GrantFiled: October 28, 1997Date of Patent: July 6, 1999Assignee: Merck & Co., Inc.Inventors: Mark E. Duggan, George D. Hartman, William F. Hoffman, Nathan C. Ihle