The Substituent Nitrogen Is An Amino Nitrogen Attached Indirectly To A Ring By Acyclic Nonionic Bonding Patents (Class 564/164)
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Publication number: 20030216427Abstract: The present invention is related to substituted amine derivatives notably for use as pharmaceutically active compounds, as well as to pharmaceutical formulations containing such amine derivatives of formula (I). Said substituted amine derivatives are efficient modulators, in particular inhibitors, of the Bax function and/or activation. The present invention is furthermore related to novel substituted amine derivatives as well as methods of their preparation.Type: ApplicationFiled: December 26, 2002Publication date: November 20, 2003Inventors: Serge Halazy, Matthias Schwarz, Bruno Antonsson, Agnes Bombrun, Jean-Claude Martinou, Dennis Church
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Patent number: 6646151Abstract: The invention relates to a process for the preparation of compounds of the formula or, if appropriate, a tautomer thereof, in each case in the free form or in salt form, in which A, X, Y, Z, R2, R3, R4, R5, R7, R9 and n are as defined in claim 1 and the C═N double bond marked with E has the E configuration, which comprises a1) reacting either a compound of the formula (II) mentioned above with a compound of the formula (III) mentioned above, in which X1 is a leaving group, or a2) a compound of the formula (IV) mentioned above, if appropriate in the presence of a base, with a compound of the formula (V) mentioned above, or b1) reacting a compound of the formula (VI) mentioned above with a compound of the formula R7—A—X2 (VII), in which X2 is a leaving group, and either further reacting the compound thus obtainable, of the formula (IV), for example according to method a2), or b2) reacting it with hydroxylamine or a salt thereof, if appropriate in the presence of a basic orType: GrantFiled: September 26, 2000Date of Patent: November 11, 2003Assignee: Bayer AktiengesellschaftInventors: Saleem Farooq, Stephan Trah, Hugo Ziegler, René Zurflüh
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Patent number: 6638927Abstract: Compounds of formula IA and IB are new where the variables R1 through R10 have the values set forth herein. Such compounds have use in treating diseases such as obesity and type II diabetes, and may be provided as pharmaceutical formulations in conjunction with a pharmaceutically acceptable carrier.Type: GrantFiled: August 31, 2001Date of Patent: October 28, 2003Assignee: Chiron CorporationInventors: Paul A. Renhowe, Daniel Chu, Rustum S. Boyce, Zhi-Jie Ni, David Duhl, Effie Tozzo, Kirk Johnson, David C. Myles
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Patent number: 6638980Abstract: Novel compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds are useful in vitro or in vivo for preventing or treating coagulation disorders.Type: GrantFiled: May 24, 2000Date of Patent: October 28, 2003Assignee: Millennium Pharmaceuticals, Inc.Inventors: Ting Su, Bing-Yan Zhu, Kim Kane-Maguire, Robert M. Scarborough, Penglie Zhang
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Publication number: 20030181490Abstract: The present invention relates to the inhibition of HIV integrase, and to the treatment of AIDS or ARC by administering compounds of the formula 1Type: ApplicationFiled: September 25, 2002Publication date: September 25, 2003Inventors: Michael A. Walker, Timothy D. Johnson, Nicholas A. Meanwell, Jacque Banville
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Publication number: 20030176485Abstract: A novel calcium receptor active compound having the formula is provided:Type: ApplicationFiled: November 21, 2002Publication date: September 18, 2003Applicant: NPS Pharmaceuticals, Inc.Inventors: Teruyuki Sakai, Atsuya Takami, Rika Nagao
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Patent number: 6620933Abstract: A azomethine yellow dye compound of general formula (I): General formula (I) wherein R1 and R2 each independently represent a hydrogen atom or a substituent; R3 represents a substituent; m indicates an integer from 0 to 3; when m is 2 or greater, R3's may be the same or different and may be mutually bonded to form a condensed ring; R3 may be bonded to R1 or R2 to form a condensed ring; R4 represents an aryl group or a heterocyclic group; R5 and R6 each independently represent a hydrogen atom or a substituent; R7 represents a substituent; n indicates an integer from 0 to 4; when n is 2 or greater, R7's may be the same or different and the may be mutually bonded to form a condensed ring; R7 may be bonded to R5 or R6 to form a condensed ring; and R5 and R6 may be bonded to each other to form a ring.Type: GrantFiled: September 26, 2002Date of Patent: September 16, 2003Assignee: Fuji Photo Film Co., Ltd.Inventors: Kiyoshi Takeuchi, Shigeki Uehira
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Patent number: 6620960Abstract: Disclosed is a process for the preparation of a compound of the formula (1) wherein R1 is unsubstituted or substituted sing reacting a compound of the formula (2) with a compound of the formula (3) in the presence of an aqueous base ransfer catalyst.Type: GrantFiled: October 1, 2002Date of Patent: September 16, 2003Assignee: Ciba Specialty Chemicals CorporationInventors: Vadiraj S. Ekkundi, Vilas N. Mumbaikar, Niranjan Paingankar, Paul Adriaan Van Der Schaaf
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Patent number: 6610886Abstract: The invention provides a process for the preparation of 2-amino-N-[2-(2,5-dimethoxyphenyl)-2-hydroxyethyl]acetamide of the formula 1 by hydrogenolysis of substituted 2-dibenzylamino-N-[2-(2′,5′-dimethoxyphenyl)-2-hydroxy-ethyl]acetamide having the formula (5), wherein Ar and Ar′ are aryl groups.Type: GrantFiled: July 30, 2002Date of Patent: August 26, 2003Assignee: Chemagis Ltd.Inventors: Michael Brand, Ronit Chen, Deby Yigal, Joseph Kaspi
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Publication number: 20030153787Abstract: Compounds of the formula R2.[(AO)n.R3]m, where R2 is a residue of a group having at least m active hydrogen atoms derived from hydroxyl and/or amino and/or amido groups, AO is alkyleneoxy, n is 2 to 200; R3 includes residue(s) of alkenyl succinic acids and optionally other acids, and m is 2 to 10, but when m is 2 there are other restrictions in the definitions, are disclosed as useful thickeners and/or dispersants in aqueous systems. The use of such materials as thickeners is also disclosed.Type: ApplicationFiled: December 10, 2002Publication date: August 14, 2003Applicant: Imperial Chemical Industries PLCInventors: Neil Michael Carpenter, Steven John Anderson, Richard Robert Tenore, Peter Glynn Hibbert
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Publication number: 20030149303Abstract: Compounds of formula (II) are simultaneously halogenated in the 5 position and hydroxylated in the 4 position under lactonization, the halolactone is converted into a hydroxylactone and then the hydroxy group into a leaving group, the leaving group is replaced with azide, the lactone amidated and then the azide converted to the amine group, in order to obtain compounds of formula (I).Type: ApplicationFiled: January 3, 2003Publication date: August 7, 2003Inventors: Stefan Stutz, Peter Herold, Felix Spindler
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Patent number: 6603043Abstract: Process for the preparation of a Schiff base of an &agr;-alkyl-&agr;-amino acid amide and an aldehyde, wherein the corresponding &agr;-aminonitrile is contacted with a base and the aldehyde and wherein it is ensured that the reagents are in good contact. The Schiff base obtained may be further hydrolysed to form the &agr;-alkyl-&agr;-amino acid amide and the aldehyde. Preferably a substituted or unsubstituted benzaldehyde is used as the aldehyde. The reaction is preferably carried out in a practically homogeneously mixed phase obtained by using a solvent, for example methanol or ethanol. Preferably NaOH or KOH is used as the base.Type: GrantFiled: July 13, 2001Date of Patent: August 5, 2003Assignee: DSM N.V.Inventors: Dominique Monique Charles Callant, Daniel Mink, Anna Maria Cornelia Francisca Castelijns
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Patent number: 6600072Abstract: Substituted 1-naphthoylguanidines, process for their preparation, their use as a medicament or diagnostic, and medicament containing them. Substituted 1-naphthoylguanidines of the formula I in which R2 to R8 have the meanings indicated in the claims, are suitable as antiarrhythmic pharmaceuticals having a cardioprotective component for infarct prophylaxis and infarct treatment and for the treatment of angina pectoris. They also preventively inhibit the pathophysiological processes in the formation of ischemically induced damage, in particular in the production of ischemically induced cardiac arrhythmias.Type: GrantFiled: August 14, 2002Date of Patent: July 29, 2003Assignee: Aventis Pharma Deutschland GmbHInventors: Joachim Brendel, Heinz-Werner Kleeman, Heinrich Christian Englert, Hans Jochen Lang, Udo Albus, Bansi Lal, Anil Vasantrao Ghate
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Patent number: 6593312Abstract: A compound of formula (I): wherein: represents an optionally substituted saturated carbon ring having from 4 to 8 ring members, R1 and R4, which may be identical or different, each represents hydrogen or acyl, R2 and R3, which may be identical or different, each represents hydrogen or alkyl, R5 and R6, which may be identical or different, each represents hydrogen or alkyl, or R5 and R6 together, with the nitrogen atom carrying them, form an optionally substituted nitrogen-containing heterocycle, stereoisomers thereof, and also addition salts thereof with a pharmaceutically acceptable acid. Medicinal products containing the same which are useful for treatment of glucose intolerance or of disorders associated with hyperglycaemia.Type: GrantFiled: June 18, 2002Date of Patent: July 15, 2003Assignee: Les Laboratoires ServierInventors: Michel Wierzbicki, Jean-Marie Fourquez, Nigel Levens, Bernadette Husson-Robert, Olivier Nosjean, Michelle Boulanger
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Patent number: 6576769Abstract: The present invention is a process, including intermediates, to produce (2S)-2-dipropylamino)-6-ethoxy-2,3-dihydro-1H-indene-5-carboxamide which is a useful pharmaceutical agent.Type: GrantFiled: June 6, 2002Date of Patent: June 10, 2003Assignee: Pharmacia & Upjohn CompanyInventors: Jiong Jack Chen, Arthur Glenn Romero, Styrbjorn Bystrom
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Patent number: 6573387Abstract: &agr;,&bgr;-Unsaturated amides and esters are converted to &agr;,&bgr;-substituted amino amides, esters, and acids. An &agr;,&bgr;unsaturated amide or ester is first converted to an &agr;,&bgr;-hydroxysulfonamide or hydroxycarbamate amide or ester using an osmium-catalyzed aminohydroxylation. The &agr;,&bgr;-hydroxysulfonamide or hydroxycarbamate amides or esters is then cyclodehydrated to produce a &agr;,&bgr;-N-sulfonyl- or the &agr;,&bgr;-N-carbamoylaziridine amide or ester. The ring of aziridine intermediate is then nucleophilically opened in a regioselective manner with a variety of nucleophiles to give the $g(&agr;,&bgr;-substituted amino- amides or esters. Preferred nucleophiles include sulfur, oxygen, carbon, and nitrogen nucleophiles.Type: GrantFiled: January 31, 2000Date of Patent: June 3, 2003Assignee: The Scripps Research InstituteInventors: K. Barry Sharpless, A. Erik Rubin
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Publication number: 20030092747Abstract: The present invention relates to compounds of formula (I): 1Type: ApplicationFiled: June 13, 2002Publication date: May 15, 2003Inventors: Heinrich Josef Schostarez, Robert Alan Chrusciel
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Publication number: 20030083524Abstract: Hydrated N-[3-[[2-(3,4-dimethoxyphenyl)ethyl]amino]propyl]-4-nitro benzamide hydrochloride characterized in that it:Type: ApplicationFiled: August 20, 2002Publication date: May 1, 2003Applicant: SmithKline Beecham p.l.c.Inventors: Graham Ralph Slater, Paul Jeffrey Westlake
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Publication number: 20030083356Abstract: The present invention relates to compounds of formula (I): 1Type: ApplicationFiled: July 10, 2002Publication date: May 1, 2003Inventors: Heinrich Josef Schostarez, Robert Alan Chrusciel
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Publication number: 20030078284Abstract: The subject invention provides compounds which are easily metabolized by the metobolic drug detoxification systems. Particularly, fluvoxamine analogs which have been designed to include esters within the structure of the compounds are taught. Also provided are methods of treating depression and affective disorders, such as obsessive compulsive disorder. Pharmaceutical compositions of the fluvoxamine analogs are also taught.Type: ApplicationFiled: October 18, 2002Publication date: April 24, 2003Inventor: Pascal Druzgala
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Publication number: 20030069288Abstract: A substituted aminomethyl-phenyl-cyclohexane derivative of formula I or Ia, 1Type: ApplicationFiled: July 5, 2002Publication date: April 10, 2003Inventors: Claudia Puetz, Wolfgang Strassburger, Babette-Yvonne Koegel
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Patent number: 6545054Abstract: Alkenyl and alkynyl compounds as potent and highly selective inhibitors of factor Xa isolated or assembled in the prothrombinase complex and compositions containing such alkenyl and alkynyl compounds are described. Such compounds show selectivity for factor Xa over other proteases of the coagulation (e.g., thrombin, fvIIa, flXa) or the fibrinolytic cascades (e.g., plasminogen activators, plasmin). Methods for using such alkenyl and alkynyl compounds as diagnostic or therapeutic agents for prevention or treatment of a condition in a mammal characterized by undesired coagulation disorders, such as thrombosis, are also described.Type: GrantFiled: February 11, 2000Date of Patent: April 8, 2003Assignee: Millennium Pharmaceuticals, Inc.Inventors: Yonghong Song, Robert M. Scarborough, Bing-Yan Zhu
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Publication number: 20030060632Abstract: The present invention provides compounds that block calcium channels having the Formula I shown below.Type: ApplicationFiled: September 23, 2002Publication date: March 27, 2003Inventors: Lain-Yen Hu, Michael Francis Rafferty, Todd Robert Ryder
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Patent number: 6521663Abstract: Phenyl acetamide compounds are described, including compounds of Formula I: or a solvate, hydrate or pharmaceutically acceptable salt thereof; wherein R3-R6, R11, B, Y and W are set forth in the specification. The compounds of the invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as thrombin and factor Xa. Compositions for inhibiting loss of blood platelets, inhibiting formation of blood platelet aggregates, inhibiting formation of fibrin, inhibiting thrombus formation, and inhibiting embolus formation are described. Other uses of compounds of the invention are as anticoagulants either embedded in or physically linked to materials used in the manufacture of devices used in blood collection, blood circulation, and blood storage, such as catheters, blood dialysis machines, blood collection syringes and tubes, blood lines and stents. Additionally, the compounds can be detectably labeled and employed for in vivo imaging of thrombi.Type: GrantFiled: October 5, 2001Date of Patent: February 18, 2003Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Wenxi Pan, Tianbao Lu, Thomas P. Markotan, Bruce E. Tomczuk
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Patent number: 6518310Abstract: Aminoguanidine and alkoxyguanidine compounds, including compounds of the formula: wherein X is O or NR9 and R1-R4, R6-R9, R11, R12, Ra, Rb, Rc, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin are described. Also described are methods for preparing the compounds of Formula I. The novel compounds of the present invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin, or are intermediates useful for forming compounds having antithrombotic activity.Type: GrantFiled: March 16, 2001Date of Patent: February 11, 2003Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Bruce E. Tomczuk, Richard M. Soll, Tianbao Lu, Cynthia L Fedde, Carl R Illig, Thomas P. Markotan, Thomas P Stagnaro
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Publication number: 20030027862Abstract: The invention relates to novel amino- and amido-diphenyl ethers, processes for their preparation and their use in pharmaceuticals, in particular for the indications of arteriosclerosis and hypercholesterolaemia.Type: ApplicationFiled: July 31, 2001Publication date: February 6, 2003Inventors: Helmut Haning, Josef Pernerstorfer, Gunter Schmidt, Michael Woltering, Hilmar Bischoff, Verena Vohringer, Axel Kretschmer, Christiane Faeste
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Publication number: 20030027847Abstract: The present invention relates to the inhibition of HIV integrase, and to the treatment of AIDS or ARC by administering compounds of the formula 1Type: ApplicationFiled: June 18, 2001Publication date: February 6, 2003Inventors: Michael A. Walker, Timothy D. Johnson, Nicholas A. Meanwell, Jacque Banville
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Publication number: 20030023096Abstract: The naphthyloxyacetic acid derivatives of the formula (I) 1Type: ApplicationFiled: December 19, 2001Publication date: January 30, 2003Inventors: Yuuki Nagao, Kazuhiko Torisu, Nobuyuki Hamanaka
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Patent number: 6511988Abstract: A series of activated iodo-benzamide derivatives are described as antineoplastic and antiviral drug compounds. The compounds generally possess a chelating group, a thiol trapping group and an activating group. The presumptive mechanism of action in preventing cancer cell and virus replication is through inhibition of the binding of transcription factors to zinc finger binding domains. The compounds are effective in inhibiting growth of a variety of human and animal tumor and leukemia cell lines at low concentrations.Type: GrantFiled: August 10, 2001Date of Patent: January 28, 2003Assignee: Isotechnika Inc.Inventors: Randall W. Yatscoff, Robert T. Foster, Selvaraj Naicker
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Publication number: 20030018059Abstract: Compounds of formula (I) 1Type: ApplicationFiled: June 3, 2002Publication date: January 23, 2003Inventors: Sarah Elizabeth Lively, Bohdan Waszkowycz, Martin JAMES Harrison, Christopher Neil Farthing, Keith Michael Johnson
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Patent number: 6509379Abstract: Phenylacetic acid derivatives of the formula I where the variables are as disclosed herein, their salts, processes and intermediates for their preparation, and their use for controlling harmful fungi and animal pests.Type: GrantFiled: April 23, 1998Date of Patent: January 21, 2003Assignee: BASF AktiengesellschaftInventors: Herbert Bayer, Hubert Sauter, Klaus Oberdorf, Wassilios Grammenos, Thomas Grote, Reinhard Kirstgen, Bernd Müller, Ruth Müller, Franz Röhl, Eberhard Ammermann, Volker Harries, Gisela Lorenz, Siegfried Strathmann, Norbert Götz, Albrecht Harreus
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Patent number: 6506910Abstract: A more practical synthesis for preparing discodermolide and structurally related analogues, novel compounds useful in the process and novel compounds prepared by the process.Type: GrantFiled: August 3, 2001Date of Patent: January 14, 2003Assignee: Novartis AGInventor: Frederick Ray Kinder, Jr.
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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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Patent number: 6489365Abstract: Compounds of the formula which is explained more fully in the specification, may be prepared by conventional methods and used therapeutically in conventional galenic preparations.Type: GrantFiled: January 18, 2000Date of Patent: December 3, 2002Assignee: Boehringer Ingelheim KGInventors: Ralf Anderskewitz, Kurt Schromm, Ernst-Otto Renth, Frank Himmelsbach, Franz Birke, Armin Fugner
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Patent number: 6482984Abstract: Iminooxy-substituted benzyl phenyl ethers of the formula I in which the substituents and the index are as defined below: Y is H, CH3, F or Cl; Q is C(═CHOCH3)—COOCH3, C(═CHCH3)—COOCH3, C(═NOCH3)—COOCH3, C(═NOCH3)—CONHCH3 or N(—OCH3)—COOCH3; X is hydrogen, halogen, alkyl, alkoxy or CF3; m is 1 or 2, where the radicals X may be different if m=2; R1 is alkyl and R2 is hydrogen or alkyl; or R1 and R2 together are cyclopropyl, cyclopentyl or cyclohexyl; R3 is alkyl or CF3; and R4 is alkyl, alkenyl, alkynyl, haloalkyl, haloalkenyl or haloalkynyl; processes and intermediates for their preparation, compositions comprising them, and their use, are described.Type: GrantFiled: January 17, 2001Date of Patent: November 19, 2002Assignee: BASF AktiengesellschaftInventors: Wassilios Grammenos, Hubert Sauter, Andreas Gypser, Markus Gewehr, Jordi Tormo i Blasco, Arne Ptock, Bernd Müller, Oliver Cullmann, Thomas Grote, Eberhard Ammermann, Siegfried Strathmann, Gisela Lorenz
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Patent number: 6479518Abstract: The present invention is directed to certain novel compounds represented by structural formula I: or a pharmaceutically acceptable salt thereof, wherein R3, R5, R6, R7, R8, R11, R12, R13, Q, W, X, Y and Z are defined herein. The invention is also concerned with pharmaceutical formulations comprising these novel compounds as active ingredients and the use of the novel compounds and their formulations in the treatment of certain disorders. The compounds of this invention are tachykinin receptor antagonists and are useful in the treatment of psychiatric disorders including depression and anxiety.Type: GrantFiled: September 21, 2001Date of Patent: November 12, 2002Assignee: Merck & Co., Inc.Inventors: Paul E. Finke, Laura C. Meurer, Sander G. Mills, Malcolm MacCoss, Hongbo Qi
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Publication number: 20020156281Abstract: The present invention provides compounds having the Formula I 1Type: ApplicationFiled: December 12, 2001Publication date: October 24, 2002Inventors: Richard John Booth, Helen Tsenwhei Lee, Jason Keith Pontrello, Randy Ranjee Ramharack, Bruce David Roth
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Publication number: 20020156311Abstract: Compounds of formula (I) 1Type: ApplicationFiled: February 8, 2002Publication date: October 24, 2002Inventors: James T. Link, Bryan K. Sorensen, Jyoti R. Patel, David L. Arendsen, Gaoquan Li
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Patent number: 6469209Abstract: The present invention relates to novel acrylate-type N-methyl E-2-(2-methylphenyl)oxymethyl)-6-methylphenyl-glyoxylamide O-methyl oxime represented by formula (1), its preparation method and its use as fungicides. The compound of the present invention has not only stronger fungicidal effect on plant pathogens at low concentrations but also broader fungicidal spectrum than the conventional fungicides. Especially, because the compound has excellent systemic and curative effect as well as no toxicity, it can be used as an efficacious agricultural fungicide. In addition, the compound of the present invention can be useful as environmental-friendly fungicide capable of causing less environmental pollution fungicide due to its strong fungicidal effect at low concentrations.Type: GrantFiled: December 14, 2001Date of Patent: October 22, 2002Assignee: Dongbu Hannong Chemical Co., Ltd.Inventors: Hong Lim, Bong Jin Chung, Jong Sang Chung, In Young Choi, Dae Jong Park, Chang Il Hwang
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Patent number: 6458781Abstract: The present invention provides compounds that block calcium channels and have the Formula I: The present invention also provides pharmaceutical compositions containing the compounds of Formula I and methods of using them to treat stroke, cerebral ischemia, head trauma, and epilepsy.Type: GrantFiled: October 25, 1999Date of Patent: October 1, 2002Inventors: David Thomas Connor, Lain-Yen Hu, Thomas Charles Malone, Michael Francis Rafferty, Bruce David Roth, Todd Robert Ryder, Anthony Denver Sercel, Yuntao Song
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Patent number: 6444850Abstract: A fungicidal compound of formula (I) having a fluorovinyloxyphenyl moiety and stereoisomers thereof are useful for protecting crops from fungal diseases: wherein: X is CH or N; Y is O or S; Z is O or NH; R1 is hydrogen or CF3; and R2 is hydrogen, a C1-10 alkyl, naphthyl, thiophenyl or a phenyl group optionally carrying one or more substituents selected from the group consisting of C1-6 alkyl, halogen-substituted C1-6 alkyl, C1-6 alkoxy, phenoxy, halogen, and methylenedioxy radicals.Type: GrantFiled: February 8, 2000Date of Patent: September 3, 2002Assignee: Korea Research Institute of Chemical TechnologyInventors: Chwang-Siek Pak, Bum-Tae Kim, No-Kyun Park, Gyung-Ja Choi, Heung-Tae Kim
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Publication number: 20020111340Abstract: Compounds of formula (I) 1Type: ApplicationFiled: November 16, 2001Publication date: August 15, 2002Inventors: Youssef Bennani, Ramin Faghih
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Publication number: 20020107406Abstract: A novel calcium receptor active compound having the formula is provided:Type: ApplicationFiled: January 17, 2002Publication date: August 8, 2002Applicant: NPS Pharmaceuticals, Inc.Inventors: Teruyuki Sakai, Atsuya Takami, Rika Nagao
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Publication number: 20020099220Abstract: The present invention features calcilytic compounds. “Calcilytic compounds” refer to compounds able to inhibit calcium receptor activity. Also described are the use of calcilytic compounds to inhibit calcium receptor activity and/or achieve a beneficial effect in a patient; and techniques which can be used to obtain additional calcilytic compounds.Type: ApplicationFiled: October 19, 2001Publication date: July 25, 2002Applicant: NPS Pharmaceuticals, Inc.Inventors: Eric G. Del Mar, Robert M. Barmore, Derek Sheehan, Bradford C. Van Wagenen, James F. Callahan, Richard M. Keenan, Nikesh R. Kotecha, Maria Amparo Lago, Linda Sue Southall, Mervyn Thompson
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Patent number: 6417200Abstract: This application relates to a compound of formula (I), a pharmaceutically acceptable salt of the compound, or a 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: May 9, 2000Date of Patent: July 9, 2002Assignee: 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, 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: 6410787Abstract: The present invention relates to (2S)-enantiomers of 2-aminoindan derivatives of formula I: and a novel process for the preparation of them.Type: GrantFiled: February 14, 2001Date of Patent: June 25, 2002Assignee: Pharmacia & Upjohn CompanyInventors: Arthur Glenn Romero, Thomas Andrew Runge, Bradley D. Hewitt, Kjell Anders Ivan Svensson, Chiu-Hong Lin, Kerry Anne Cleek, Susanne R. Haadsma-Svensson
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Publication number: 20020072634Abstract: Process for the preparation of a Schiff base of an &agr;-alkyl-&agr;-amino acid amide and an aldehyde, wherein the corresponding &agr;-aminonitrile is contacted with a base and the aldehyde and wherein it is ensured that the reagents are in good contact. The Schiff base obtained may be further hydrolysed to form the &agr;-alkyl-&agr;-amino acid amide and the aldehyde.Type: ApplicationFiled: July 13, 2001Publication date: June 13, 2002Inventors: Dominique Monique Charles Callant, Daniel Mink, Anna Maria Cornelia Francisca Castelijns
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Patent number: 6391175Abstract: The invention pertains to a novel ionophore having the general structure: wherein R1, R2, R3 and R4 are independently straight or branched chain alkyl having 4 to 12 carbon atoms or the alkyl groups may optionally contain a cycloalkyl group having 3 to 8 carbon atoms or R1 and R2 or R3 and R4 together with N to which they are attached, can form a ring having 5 to 8 carbon atoms. This ionophore has increased selectivity for carbonate ions over other ions, especially salicylate. The invention includes membranes containing effective amounts of the novel ionophores and -sensors containing these membranes.Type: GrantFiled: November 21, 2000Date of Patent: May 21, 2002Assignee: Dade Behring Inc.Inventors: Chengrong Wang, Daniel Brown
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Patent number: RE37839Abstract: O-Benzyloxime ethers of the formula I wherein 5 x is substituted or unsubstituted CH2, NOalkyl Y is O, S, NR5 R1, R2, R5 are H, alkyl Z1, Z2 are H, halogen, methyl, methoxy, cyano R3, R4 are hydrogen, cyano, substituted or unsubstituted alkyl, alkenyl, cycloalkyl, cycloalkenyl, alkynyl, alkoxy, haloalkoxy, alkylthio, benzylthio, alkylcarbonyl, substituted or unsubstituted benzylcarbonyl, alkoxycarbonyl, substituted or unsubstituted phenoxycarbonyl substituted or unsubstituted benzyloxycarbonyl, N(R6)2, where R6 is H, alkyl, substituted or unsubstituted phenyl, —CO—N(R7)2, where R7 is H, substituted or unsubstituted alkyl, substituted or unsubstituted aryl, substituted or unsubstituted aryloxy, substituted or unsubstituted arylthio, substituted or unsubstituted hetaryl, substituted or unsubstituted hetaryloxy, substituted or unsubstituted hetarylthio, substituted or unsubstituted heterocyclyl, substituted or unsubstituted heterocyclyloxy, R3 and R4 together may form a caType: GrantFiled: April 5, 1996Date of Patent: September 10, 2002Assignee: BASF AktiengesellschaftInventors: Siegbert Brand, Uwe Kardorff, Reinhard Kirstgen, Bernd Mueller, Klaus Oberdorf, Hubert Sauter, Gisela Lorenz, Eberhard Ammermann, Christoph Kuenast, Albrecht Harreus
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Patent number: RE37873Abstract: Phenylacetic acid derivatives of the formula IType: GrantFiled: April 16, 2001Date of Patent: October 8, 2002Assignee: BASF AktiengesellschaftInventors: Herbert Bayer, Hubert Sauter, Ruth Müller, Wassilios Grammenos, Albrecht Harreus, Reinhard Kirstgen, Franz Röhl, Eberhard Ammermann, Gisela Lorenz