Nitrogen Attached Directly Or Indirectly To The Hetero Ring By Acyclic Nonionic Bonding Patents (Class 549/467)
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Publication number: 20030158194Abstract: The subject invention pertains to novel compounds (and salts thereof), and compositions comprising the compounds, for the treatment of cardiac arrhythmias. The subject invention further concerns methods of making the novel compounds. The novel compounds are rapidly metabolized analogs of amiodarone, having the distinct and advantageous characteristic of being metabolized to a less lipophilic compound. This results in an improved safety profile. The new compounds have particular utility for treating life-threatening ventricular tachyarrhythmias, especially in patients with congestive heart failure (CHF). The compounds also provide effective management for ventricular arrhythmias and supraventricular arrhythmias, including atrial fibrillation and re-entrant tachyarrhythmias involving accessory pathways.Type: ApplicationFiled: December 10, 2002Publication date: August 21, 2003Inventor: Pascal Druzgala
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Publication number: 20030153604Abstract: This invention is directed to an (aminoiminomethyl or aminomethyl)benzoheteroaryl compound of formula I which is useful for inhibiting the activity of Factor Xa by combining said compound with a composition containing Factor Xa. The present invention is also directed to compositions containing compounds of the formula I, methods for their preparation, their use, such as in inhibiting the formation of thrombin or for treating a patient suffering from, or subject to, a disease state associated with a physiologically detrimental excess amount of thrombin.Type: ApplicationFiled: February 24, 2003Publication date: August 14, 2003Applicant: Aventis Pharmaceuticals Inc.Inventors: William P. Dankulich, Daniel G. McGarry, Christopher Burns, Timothy F. Gallagher, Francis A. Volz
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Publication number: 20030153774Abstract: The present invention provides, inter alia, a novel process for the preparation of Citalopram, a known antidepressant.Type: ApplicationFiled: September 11, 2002Publication date: August 14, 2003Applicant: Pharmachem Technologies Limited,Inventors: Aslam A. Malik, Hasan Palandoken, Joy A. Stringer, DerShing Huang, Antonio Romero, Olivier Dapremont
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Patent number: 6605626Abstract: This application relates to a compound of formula I (or a prodrug thereof or a pharmaceutically acceptable salt of the compound or prodrug thereof) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well as a process for its preparation and intermediates therefor.Type: GrantFiled: September 21, 2001Date of Patent: August 12, 2003Assignee: Eli Lilly and CompanyInventors: Douglas Wade Beight, Trelia Joyce Craft, Jeffry Bernard Franciskovich, Theodore Goodson Jr., Steven Edward Hall, David Kent Herron, Valentine Joseph Klimkowski, Jeffrey Alan Kyle, John Joseph Masters, David Mendel, Guy Milot, Jason Scott Sawyer, Robert Theodore Shuman, Gerald Floyd Smith, Anne Louise Tebbe, Jennifer Marie Tinsley, Leonard Crayton Weir, James Howard Wikel, Michael Robert Wiley, Ying Kwong Yee
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Patent number: 6603025Abstract: The present invention relates to a novel process for preparing known benzofuranone oximes, and to a novel process for preparing known benzofuranyl alkanoates which are used as intermediates in the synthesis sequence.Type: GrantFiled: May 13, 2002Date of Patent: August 5, 2003Assignee: Bayer AktiengesellschaftInventors: Reinhard Lantzsch, Herbert Gayer, Peter Gerdes, Walter Hübsch, Lubbertus Mulder, Bernd Gallenkamp, Matthias Decker
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Publication number: 20030144534Abstract: Process for preparing purified citalopram or one of its salts that comprises the purification of citalopram by selective extractions of citalopram or of its impurities with organic solvents and water under specific conditions of pH and temperature. The crude citalopram can be prepared by a process that comprises reacting 1-[3-(dimethylamine)propyl]-1-(4-fluorophenyl)-1,3-dihydro-5-bromoisobenzofuran with copper cyanide.Type: ApplicationFiled: January 24, 2003Publication date: July 31, 2003Inventors: Laura Coppi, Yolanda Gasanz Guillen, Julio Campon Pardo
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Patent number: 6599918Abstract: This invention is directed to substituted (aminoiminomethyl or aminomethyl) dihydrobenzofurans and benzopyrans that inhibit Factor Xa, pharmaceutical compositions comprising these compounds and their use for inhibiting Factor Xa or treating pathological conditions in a patient that may be ameliorated by administration of such compounds. This invention is also is also directed to substituted (aminoiminomethyl or aminomethyl) dihydrobenzofurans and benzopyrans which directly inhibit both Factor Xa and Factor IIa (thrombin), to pharmaceutical compositions comprising these compounds, to intermediates useful for preparing these compounds and to a method of simultaneously directly inhibiting both Factor Xa and Factor IIa (thrombin).Type: GrantFiled: February 22, 2002Date of Patent: July 29, 2003Assignee: Aventis Pharmaceuticals Inc.Inventors: Christopher J. Burns, William P. Dankulich, Daniel G. McGarry, Francis A. Volz
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Publication number: 20030134895Abstract: A method for the preparation of citalopram comprising reaction of a compound of formula 5-aminomethyl-1-(3-dimethylamino-propyl)-1-(4-fluoro-phenyl)-1,3-dihydro-isobenzofuran with an oxidising agent to prepare citalopram.Type: ApplicationFiled: November 8, 2002Publication date: July 17, 2003Applicant: H. Lundbeck A/SInventors: Hans Petersen, Robert Dancer
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Publication number: 20030130527Abstract: Method for the preparation of 1-(3-dimethylaminopropyl)-1-(4-fluorophenyl)-1,3-dihydroisobenzofuran-5-carbonitrile (citalopram) comprising the reaction of a compound of formula 1Type: ApplicationFiled: February 24, 2003Publication date: July 10, 2003Applicant: ORION CORPORATION FERMIONInventors: Leif Hilden, Tuomas Huuhtanen, Petteri Rummakko, Arne Grumann, Pekka Pietikaeinen
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Patent number: 6589970Abstract: This invention provides novel compounds, pharmaceutical compositions and methods of treating thrombotic disorders in mammals, the compounds having the formula: Wherein: Ar is phenyl, naphthyl, furanyl, benzofuranyl, indolyl, pyrazolyl, oxazolyl, fluorenyl, phenylcycloalkane where the cycloalkane can be cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl and Ar can be optionally substituted by 1 to 3 groups selected from C1-C6 alkyl, C1-C6 alkoxy, hydroxy, phenyl-(CH2)0-6—, phenyl-(CH2)0-6O—, C3-C6 cycloalkyl, —(CH2)—C3-C6 cycloalkyl, halogen, C1-C3 perflouroalkyl and C1-C3 perfluoroalkoxy where phenyl can be substituted with from 1 to 3 groups selected from C1-C6 alkyl, C1-C6 alkoxy, phenyl, halogen, trifluoromethyl or trifluoromethoxy; R1 is hydrogen, C1-C6 alkyl or phenyl-(CH2)1-6— where phenyl can be substituted with C1-C6 alkyl, C1-C6 alkoxy, halo, trifluoromethyl or trifluoromethoxy; R2 and R3 are H, C1-C6 alkyl, phenyl-(CH2)0-3—, halo and C1-C3 perfluType: GrantFiled: June 13, 2002Date of Patent: July 8, 2003Assignee: WyethInventors: Thomas Joseph Commons, Susan Christman Croce, Richard Page Woodworth, Eugene John Trybulski, Hassan Mahmoud Elokdah, David LeRoy Crandall
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Patent number: 6586606Abstract: The instant invention discloses a process for the preparation of compounds of formula I wherein the general symbols are as defined in claim 1, which process comprises hydrolyzing a compound of formula V wherein the general symbols are as defined in claim 1, in an aqueous solvent in the presence of an acid. The compounds of the formula V are new and useful as stabilizers for protecting organic materials, in particular polymers and lubricants, against oxidative, thermal or light-induced degradation.Type: GrantFiled: July 5, 2001Date of Patent: July 1, 2003Assignee: Ciba Specialty Chemicals CorporationInventors: Michèle Gerster, Paul Dubs
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Publication number: 20030114692Abstract: A method for the preparation of citalopram wherein the aldehyde of formula 1Type: ApplicationFiled: November 1, 2002Publication date: June 19, 2003Applicant: H. Lundbeck A/SInventors: Hans Petersen, Michael Harold Rock
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Publication number: 20030109547Abstract: An amidinophenylpyruvic acid derivative of the following formula, analogs thereof and pharmaceutically acceptable salts thereof have an excellent antagonistic effect against activated blood coagulation factor VII.Type: ApplicationFiled: June 5, 2002Publication date: June 12, 2003Applicant: AJINOMOTO CO. INCInventors: Masayuki Sugiki, Kazuyuki Sagi, Kohichi Fujita, Takashi Kayahara, Shunji Takehana, Kuniya Sakurai, Kazumi Tashiro
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Publication number: 20030109576Abstract: A new salt (R)-3-N,N-dicyclobutylamino-8-fluoro-3,4-dihydro-2H-1-benzopyran-5-carboxamide hydrogen tartrate, particularly the (2R,3R)-tartrate thereof, most particularly the (R)-3-N,N-dicyclobutylamino-8-fluoro-3,4-dihydro-2H-1-benzopyran-5-carboxamide hydrogen (2R,3R)-tartrate monohydrate, processes for the manufacture of said tartrate salt, the use of the salt in medicine, the use of the tartrate salt in the manufacture of pharmaceutical formulations, and a method for the treatment of CNS disorders by administration of the tartrate salt to a host in need of such treatment.Type: ApplicationFiled: June 8, 1998Publication date: June 12, 2003Inventors: HAKAN NYQVIST, DANIEL D SOHN
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Publication number: 20030109577Abstract: A solid unit dosage form comprising citalopram, which is prepared by direct compression of a mixture of citalopram base or a pharmaceutically acceptable salt thereof and pharmaceutically acceptable excipients, or by filling of said mixture in a hard gelatine capsule. Large crystals of a pharmaceutical acceptable salt of citalopram and method for the manufacture of said large crystals.Type: ApplicationFiled: December 5, 2000Publication date: June 12, 2003Inventors: Ken Liljegren, Per Holm, Ole Nielsen, Sven Wagner
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Publication number: 20030109578Abstract: N-(3-benzofuranyl)urea-derivatives are prepared by reacting of 3-amino-substituted benzofuranes with appropriate substituted isocyanates or isothiocyanates. The N(3-benzofuranyl)urea-derivatives can be used as active ingredients in medicaments particularly for the treatment of acute and chronic inflammatory processes.Type: ApplicationFiled: May 24, 2002Publication date: June 12, 2003Inventors: Gabriele Braunlich, Rudiger Fischer, Mazen Es-Sayed, Rolf Henning, Michael Sperzel, Karl-Heinz Schlemmer, Ulrich Nielsch, Stephen Tudhope, Graham Sturton, Trevor S. Abram, Mary F. Fitzgerald
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Patent number: 6573295Abstract: This invention concerns compounds for inhibiting intracellular signal transduction, especially intracellular signal transduction mediated by one or more molecular interactions involving a phosphotyrosine-containing protein. This invention also relates to pharmaceutical compositions containing the compounds and prophylactic and therapeutic methods involving pharmaceutical and veterinary administration of the compounds. The compounds are of the formula as defined herein.Type: GrantFiled: November 21, 2001Date of Patent: June 3, 2003Assignee: Ariad Pharmaceuticals, Inc.Inventors: William C. Shakespeare, Michael G. Yang, Rajeswari Sundaramoorthi, Regine Bohacek, Charles Joseph Eyermann, Tomi K. Sawyer
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Patent number: 6569882Abstract: Bis-sulfonamido hydroxyethylamino compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to retroviral protease inhibiting compounds of the formula: or a pharmaceutically acceptable salt, prodrug or ester thereof, wherein the variables are as defined herein.Type: GrantFiled: February 19, 2002Date of Patent: May 27, 2003Assignee: G. D. Searle & Co.Inventors: John N. Freskos, Daniel P. Getman, John J. Talley, James A. Sikorski
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Patent number: 6569894Abstract: Novel benzofuran and dihydrobenzofuran derivatives which have a binding affinity for the human melatonin receptor and, therefore, are useful as melatonergic agents.Type: GrantFiled: October 3, 2002Date of Patent: May 27, 2003Assignee: Bristol-Myers Squibb CompanyInventors: Katherine S. Takaki, Li-Quang Sun, Graham Johnson, James R. Epperson, Stephen R. Bertenshaw
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Patent number: 6566540Abstract: A method for the preparation of S-citalopram comprising reaction of a compound of Formula (IV), wherein R is C1-6 alkyl, acyl, C1-6 alkylsulfonyl or arylsulfonyl, with 3-(N,N-dimethylamino)-propyl magnesium halide, to prepare citalopram.Type: GrantFiled: May 3, 2002Date of Patent: May 20, 2003Assignee: H. Lundbeck A/SInventors: Michael Harold Rock, Hans Petersen, Peter Ellegaard
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Publication number: 20030092761Abstract: The invention relates to a method for the preparation of citalopram comprising reaction of a compound of formula II 1Type: ApplicationFiled: August 29, 2002Publication date: May 15, 2003Applicant: H. Lundbeck A/SInventors: Michael Harold Rock, Haleh Ahmadian
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Publication number: 20030092919Abstract: The present invention relates to a method for the preparation of citalopram by alkylation of a 1-(4-fluorophenyl)-1,3-dihydroisobenzofurane derivative.Type: ApplicationFiled: September 5, 2002Publication date: May 15, 2003Applicant: H. Lundbeck A/SInventor: Hans Petersen
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Patent number: 6562848Abstract: This invention relates generally to bis-amino acid sulfonamides containing substituted benzyl amines of formula I: or stereoisomeric forms, stereoisomeric mixtures, or pharmaceutically acceptable salt forms thereof, which are useful as HIV protease inhibitors, pharmaceutical compositions and diagnostic kits comprising the same, methods of using the same for treating viral infection or as assay standards or reagents, and intermediates and processes for making the same.Type: GrantFiled: September 18, 2002Date of Patent: May 13, 2003Assignee: Bristol-Myers Squibb CompanyInventor: Robert F. Kaltenbach
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Publication number: 20030083508Abstract: A method for the preparation of citalopram wherein the aldehyde of formula 1Type: ApplicationFiled: August 23, 2002Publication date: May 1, 2003Applicant: H. Lundbeck A/SInventors: Hans Petersen, Michael Harold Rock
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Publication number: 20030083509Abstract: Methods for manufacture of citalopram through stepwise alkylation of 5-substituted 1-(4-fluorophenyl)-1,3-dihydroisobenzofurans are disclosed.Type: ApplicationFiled: September 10, 2002Publication date: May 1, 2003Applicant: H. Lundbeck A/SInventors: Hans Petersen, Haleh Ahmadian
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Publication number: 20030078422Abstract: Process for the preparation of benzo-fused heterocycles of general formula I: 1Type: ApplicationFiled: October 9, 2002Publication date: April 24, 2003Inventors: Frank-Hardi Wartenberg, Thomas Koppe, Walter Wetzel, Markus Wydra, Achim Benz
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Publication number: 20030078442Abstract: The present invention relates to the crystalline base of the well known antidepressant drug citalopram,1-[3-(dimethylamino)propyl]-1-(4-fluorophenyl)-1,3-dihydro-5-isobenzofurancarbonitrile, formulations of said base, a process for the preparation of purified salts of citalopram, such as the hydrobromide, using the base, the salts obtained by said process and formulations containing such salts.Type: ApplicationFiled: September 12, 2002Publication date: April 24, 2003Applicant: H. Lundbeck A/SInventors: Hans Petersen, Klaus Peter Bogeso, Per Holm
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Publication number: 20030069304Abstract: The present invention relates to a method for the preparation of citalopram comprising reduction of a compound of formula 1Type: ApplicationFiled: September 9, 2002Publication date: April 10, 2003Applicant: H. Lundbeck A/SInventor: Hans Petersen
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Publication number: 20030065007Abstract: Non-peptide acetamide derivatives of Formula I are specific NK1 antagonists, 1Type: ApplicationFiled: October 9, 2002Publication date: April 3, 2003Inventors: Mark Wallace Creswell, Michael Higginbottom, David Christopher Horwell, Russel Andrew Lewthwaite, Martyn Clive Pritchard, Jennifer Raphy
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Patent number: 6541473Abstract: The present invention relates to certain resorcinol derivatives and their use as skin lightening agents.Type: GrantFiled: September 17, 2001Date of Patent: April 1, 2003Assignee: Warner Lambert CompanyInventors: Stuart E. Bradley, Eric W. Collington, Matthew C. Fyfe, William T. Gattrell, Joanna V. Geden, Peter J. Murray, Martin J. Procter, Robert J. Rowley, Jonathan G. Williams
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Publication number: 20030060641Abstract: The present invention relates to a method for the preparation of citalopram or any of its enantiomers and acid addition salts thereof comprising reaction of a compound of formula II 1Type: ApplicationFiled: June 25, 2002Publication date: March 27, 2003Applicant: H. Lundbeck A/SInventors: Hans Petersen, Jakob Felding
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Publication number: 20030050484Abstract: The invention relates to a method for the preparation of citalopram comprising, in either order, subjecting a compound of formula 1Type: ApplicationFiled: September 6, 2002Publication date: March 13, 2003Applicant: H. Lundbeck A/SInventor: Hans Petersen
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Patent number: 6518291Abstract: The present invention relates to a novel class of compounds which are IMPDH inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting IMPDH enzyme activity and consequently, may be advantageously used as therapeutic agents for IMPDH mediated processes. This invention also relates to methods for inhibiting the activity of IMPDH using the compounds of this invention and related compounds.Type: GrantFiled: September 14, 1999Date of Patent: February 11, 2003Assignee: Vertex Pharmaceuticals, IncorporatedInventors: Jeffrey O. Saunders, David M. Armistead, Michael C. Badia, Randy S. Bethiel, Catherine A. Frank, Doug Naegele, Perry M. Novak, David A. Pearlman, Steven M. Ronkin
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Patent number: 6514996Abstract: An oxygen-containing heterocyclic compound represented by following Formula (I): wherein R1 and R2 independently represent hydrogen, lower alkyl, cyano, —(CH2)n—E1—CO—G1 (wherein E1 represents a bond, O, or NH; and G1 represents hydrogen, substituted or unsubstituted lower alkyl, OR6, or NR7R8; and n represents an integer of 0 to 4), or the like; R1 and R2 are combined to represent a saturated carbon ring together with a carbon atom adjacent thereto; or R2, and R11 or R13 described below are combined to form a single bond; R3 represents hydrogen, phenyl, or halogen; R4 represents hydroxy, lower alkoxy, or the like; A represents —C(R9)(R10)— or O; B represents O, NR11, —C(R12)(R13)—, or —C(R14)(R15)—C(R16)(R17)—; D represents (i) —C(R18)(R19)—X— (wherein X represents —C(R21)(R22)—, S, or NR23), (ii) —C(R19a)═Y— [Y represents —C(R24)—Z— (wherein Z represents CType: GrantFiled: November 19, 1997Date of Patent: February 4, 2003Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Etsuo Ohshima, Takashi Kawakita, Koji Yanagawa, Kyoichiro Iida, Rie Koike, Yoshisuke Nakasato, Tohru Matsuzaki, Kenji Ohmori, Soichiro Sato, Hidee Ishii, Haruhiko Manabe, Michio Ichimura, Fumio Suzuki
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Publication number: 20030018062Abstract: The present invention provides hydroxamate compounds which are deacetylase inhibitors. The compounds are suitable for pharmaceutical compositions having anti-proliferative properties.Type: ApplicationFiled: August 31, 2001Publication date: January 23, 2003Inventors: Stacy W. Remiszewski, Kenneth W. Bair, Richard W. Versace, Lawrence B. Perez, Michael A. Green, Lidia C. Sambucetti, Sushil Sharma
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Publication number: 20030018064Abstract: The present invention relates to novel substituted benzofurans and benzothiophenes compounds that are antagonists of alpha V (&agr;v) integrins, for example &agr;v&bgr;3 and &agr;v&bgr;5 integrins, their pharmaceutically acceptable salts, and pharmaceutical compositions thereof. The compounds may be used in the treatment of pathological conditions mediated by &agr;v&bgr;3 and &agr;v&bgr;5 integrins, including such conditions as tumor growth, metastasis, restenosis, osteoporosis, inflammation, macular degeneration, diabetic retinopathy, and rheumatoid arthritis.Type: ApplicationFiled: April 26, 2002Publication date: January 23, 2003Applicant: 3-Dimensional Pharmaceuticals, Inc.Inventors: Beth M. Anaclerio, Juan Jose Marugan Sanchez, Victor J. Marder, David C. U'Prichard
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Patent number: 6509483Abstract: A method for the preparation of citalopram comprising reacting 5-carboxyphthalide successively with a Grignard reagent of 4-halo-fluorophenyl and a Grignard reagent of 3-halo-N,N-dimethyl-propylamine and then effecting ring closure of the resulting compound of Formula XI to a compound of Formula IV followed by conversion of the compound of Formula IV into citalopram is disclosed. Methods for the manufacture and conversion of the compound of Formula IV are also disclosed.Type: GrantFiled: August 14, 2001Date of Patent: January 21, 2003Assignee: H. Lundbeck A/SInventors: Hans Petersen, Haleh Ahmadian, Robert Dancer
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Publication number: 20020193410Abstract: This invention is directed to substituted (aminoiminomethyl or aminomethyl) dihydrobenzofurans and benzopyrans that inhibit Factor Xa, pharmaceutical compositions comprising these compounds and their use for inhibiting Factor Xa or treating pathological conditions in a patient that may be ameliorated by administration of such compounds. This invention is also is also directed to substituted (aminoiminomethyl or aminomethyl) dihydrobenzofurans and benzopyrans which directly inhibit both Factor Xa and Factor IIa (thrombin), to pharmaceutical compositions comprising these compounds, to intermediates useful for preparing these compounds and to a method of simultaneously directly inhibiting both Factor Xa and Factor IIa (thrombin).Type: ApplicationFiled: February 22, 2002Publication date: December 19, 2002Inventors: Christopher J. Burns, William P. Dankulich, Daniel G. McGarry, Francis A. Volz
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Patent number: 6495546Abstract: Propanolamine derivatives represented by the following formula (I): These derivatives may be &bgr;3 agonists and exert sympathomimetic, anti-ulcerous, anti-pancreatitis, lipolytic and anti-urinary incontinence and anti-pollakiuria activities. Pharmaceutical compositions containing such propanolamine derivatives, methods for the prevention and/or treatment diseases using these propanolamine derivatives, and processes for their preparation are also described.Type: GrantFiled: November 22, 2000Date of Patent: December 17, 2002Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Kiyoshi Taniguchi, Minoru Sakurai, Naoaki Fujii, Kumi Hosoi, Yasuyo Tomishima, Hisashi Takasugi, Hajime Sogabe, Hirofumi Ishikawa, Naomi Hanioka
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Publication number: 20020187976Abstract: A compound of the formula 1Type: ApplicationFiled: June 26, 2002Publication date: December 12, 2002Applicant: Aventis Pharma S.A.Inventors: Denis Carniato, Jean-Francois Gourvest, Jochen Knolle, Anurschirwan Peyman, Sarah Bodary, Thomas R. Gadek
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Publication number: 20020177722Abstract: A method for the preparation of escitalopram comprising reaction of a compound of 1Type: ApplicationFiled: May 3, 2002Publication date: November 28, 2002Applicant: H. Lundbeck A/SInventors: Michael Harold Rock, Hans Petersen, Peter Ellegaard
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Patent number: 6479675Abstract: The present invention relates to a plurality of novel processes and novel intermediates for preparing 3-(1-hydroxyphenyl-1-alkoximinomethyl)dioxazines, which are known as intermediates for preparing compounds having fungicidal properties (WO 95-04728).Type: GrantFiled: July 19, 2000Date of Patent: November 12, 2002Assignee: Bayer AktiengesellschaftInventors: Herbert Gayer, Bernd Gallenkamp, Peter Gerdes, Ulrich Heinemann, Bernd-Wieland Krüger, Reinhard Lantzsch, Thomas Seitz, Uwe Stelzer
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Publication number: 20020165403Abstract: 5-carboxyphthalide is obtained with very high purity and in high yields by a convenient process comprising reaction of terephthalic acid 1Type: ApplicationFiled: May 6, 2002Publication date: November 7, 2002Applicant: H. Lundbeck A/SInventors: Hans Petersen, Poul Dahlberg Nielsen
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Publication number: 20020151728Abstract: The present invention provides a production method of a 5-phthalancarbonitrile compound, which comprises the use of a novel compound of the formula [I] 1Type: ApplicationFiled: June 21, 2002Publication date: October 17, 2002Applicant: Sumika Fine Chemicals Co., Ltd.Inventors: Tetsuya Ikemoto, Masami Igi
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Patent number: 6465468Abstract: The subject invention concerns methods and compounds that have utility in the treatment of a condition associated with matrix metalloproteinase, ADAM or ADAM-TS enzymes, a condition that is mediated by TNF &agr; or a condition involving a membrane-shedding event that is mediated by a metalloproteinase. Compounds of the invention are of formula I (B)2N—X—(CH2)m—W—(CR1R2)n—COY (I) wherein n=0 or 1; m=0 or 1; X is S(O)1-2; Y is OH or NHOH; W is aryl or heteroaryl; and the other groups are as defined herein.Type: GrantFiled: March 22, 2000Date of Patent: October 15, 2002Assignee: Darwin Discovery LimitedInventors: Andrew Douglas Baxter, David Alan Owen, Duncan Batty, Robert John Watson
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Patent number: 6465508Abstract: Ortho-sulfonamido aryl hydroxamic acids are provided which are useful, inter alia, for the inhibition of matrix metalloproteinases and the treatment of conditions associated with overexpression of MMPs.Type: GrantFiled: February 23, 2001Date of Patent: October 15, 2002Assignee: WyethInventors: Frances Christy Nelson, Arie Zask, James Ming Chen, Dominick Mobilio, Ramaswamy Nilakantan
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Patent number: 6462055Abstract: Compounds having the formula: wherein R1-R5 are independently selected from hydrogen, alkyl of 1 to 6 carbon atoms, alkenyl of 2 to 6 carbon atoms, alkynyl of 2 to 6 carbon atoms, perhaloalkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 10 carbon atoms, heterocycloalkyl of 3 to 10 carbon members, aryl, heteroaryl, halogen, —CN, —NO2, —CO2R6, —COR6, —OR6, —SR6, —SOR6, —SO2R6, —CONR7R8, —NR6N(R7R8), —N(R7R8) or W-Y-(CH2)n-Z provided that at least one of R1-R5 is not hydrogen; or R1 and R2 or R3 and R4, taken together form a 3 to 7 membered heterocycloalkyl or 3 to 7 membered heteroaryl; R6 and R7 are independently hydrogen, alkyl of 1 to 6 carbon atoms, perhaloalkyl of 1 to 6 carbon atoms, or aryl; R8 is hydrogen, alkyl of 1 to 6 carbon atoms, perhaloalkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 10 carbon atoms, heterocycloalkyl of 3 to 10 members, aryl or heteroaryl, or R7 and R8, taken together may form a 3 to 7 memberedType: GrantFiled: April 30, 2001Date of Patent: October 8, 2002Assignee: WyethInventors: Jonathan Bloom, Kevin Curran, Martin DiGrandi, Russell Dushin, Stanley Lang, Emily Norton, Adma Ross, Bryan O'Hara
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Patent number: 6458975Abstract: Citalopram can be industrially and economically produced and at a high yield by reacting a compound of the following formula [VI] with 3-(dimethylamino)propyl chloride in the presence of at least one of N,N,N′,N′-tetramethylethylenediamine and 1,3-dimethyl-2-imidazolidinone and a condensing agent.Type: GrantFiled: November 28, 2001Date of Patent: October 1, 2002Assignee: Sumika Fine Chemicals Co., Ltd.Inventors: Tetsuya Ikemoto, Wei-Guo Gao, Nobuhiro Arai, Masami Igi
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Publication number: 20020128497Abstract: A method for the manufacture of citalopram characterized in (i) reaction of 1-(4-fluorophenyl)-1-(3-dimethylaminopropyl)-5-halophthalane with an activated magnesium to form the Grignard reagent [3-[1-(4-fluorophenyl)-1,3 dihydro-isobenzofuran-1-yl]propyl]dimethylamine 5-magnesium halide followed by (ii) reaction of [3-[1-(4-fluorophenyl)-1,3 dihydro-isobenzofuran-1-yl]propyl)dimethylamine 5-magnesium halide with a compound containing a —CN group bound to a leaving group to form citalopram.Type: ApplicationFiled: March 6, 2002Publication date: September 12, 2002Applicant: H. Lundbeck A/SInventors: Eva Bolzonella, Andrea Castellin, Andrea Nicole
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Publication number: 20020120005Abstract: The present invention relates to the process for the preparation and purification of citalopram (I) 1Type: ApplicationFiled: January 8, 2002Publication date: August 29, 2002Applicant: H. Lundbeck A/SInventors: Marco Villa, Federico Sbrogio, Robert Dancer