Plural Double Bonds Between The Ring Members Of The Oxazole Ring Patents (Class 548/235)
  • Publication number: 20030069291
    Abstract: Compounds of formula (I): 1
    Type: Application
    Filed: March 29, 2002
    Publication date: April 10, 2003
    Inventors: Simon Bailey, Paul Vincent Fish, Kim James, Gavin Alistar Whitlock
  • Publication number: 20030055265
    Abstract: The present invention relates to novel oxazole compounds which act as PPAR&agr; and PPAR&ggr; agonists and are accordingly useful for the treatment of diseases modulated by PPAR&agr; and PPAR&ggr; such as diabetes.
    Type: Application
    Filed: May 9, 2002
    Publication date: March 20, 2003
    Inventors: Alfred Binggeli, Markus Boehringer, Uwe Grether, Hans Hilpert, Hans-Peter Maerki, Markus Meyer, Peter Mohr, Fabienne Ricklin
  • Patent number: 6531609
    Abstract: The present invention is concerned with a novel process for the preparation of compounds of formula I comprising bromomethylation or chloromethylation of a compound of formula II and subsequent reaction with a compound of formula IV The compounds of formula I and the corresponding salts, e.g. the sodium salts, are pharmaceutically active substances.
    Type: Grant
    Filed: March 22, 2001
    Date of Patent: March 11, 2003
    Assignee: Hoffmann-LA Roche Inc.
    Inventor: Michelangelo Scalone
  • Publication number: 20030045558
    Abstract: The present invention is directed to compounds represented by Structural Formula I and pharmaceutically acceptable salts, solvates and hydrates thereof, and methods of making, methods of using and pharmaceutical compositions having compounds represented by Structural Formula I and pharmaceutically acceptable salts, solvates and hydrates thereof: 1
    Type: Application
    Filed: April 11, 2002
    Publication date: March 6, 2003
    Applicant: Eli Lilly & Company Lily Corporate Center
    Inventors: Dawn A. Brooks, Christopher J. Rito, Anthony J. Shuker, Samuel J. Dominianni, Alan M. Warshawsky, Lynn S. Gossett, Donald P. Matthews, David A. Hay, Robert J. Ardecky, Pierre-Yves Michellys, John S. Tyhonas
  • Publication number: 20030040534
    Abstract: Endothelin antagoninst N-[[2′-[[(4,5-dimethyl-3-isoxazolyl)amino]sulfonyl]-4-(2-oxazolyl)[1,1′-biphenyl]-2-yl]methyl]-N,3,3-trimethylbutanamide surprisingly exists as separable enantiomeric atropisomers. The (+) dextrorotatory atropisomer demonstrates remarkably higher potency than either the (−) levorotatory atropisomer or the racemate.
    Type: Application
    Filed: April 12, 2002
    Publication date: February 27, 2003
    Inventors: David E. Hughes, Beth C. Seidenberg
  • Patent number: 6515136
    Abstract: Methods for the preparation of biphenyl isoxazole sulfonamides and intermediates thereof. The present invention also relates to the novel intermediates prepared by these methods. The biphenyl isoxazole sulfonamides prepared by the present methods are endothelin antagonists useful, inter alia, for the treatment of hypertension.
    Type: Grant
    Filed: August 27, 1998
    Date of Patent: February 4, 2003
    Assignee: Bristol-Myers Squibb Company
    Inventors: Richard P. Polniaszek, Xuebao Wang, Jeffrey S. DePue, Chennagiri R. Pandit, Kumar G. Gadamasetti, Yadagiri Pendri, Eduardo J. Martinez
  • Patent number: 6506747
    Abstract: 1-(4-aminophenyl)pyrazoles optionally substituted on the 3- and 5-positions of the pyrazole ring and on the amino group at the 4-position of the phenyl ring are disclosed and described, which pyrazoles inhibit IL-2 production in T-lymphocytes.
    Type: Grant
    Filed: June 3, 1999
    Date of Patent: January 14, 2003
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Rajashekhar Betageri, Charles L. Cywin, Karl Hargrave, Mary Ann Hoermann, Thomas M. Kirrane, Thomas M. Parks, Usha R. Patel, John R. Proudfoot, Rajiv Sharma, Sanxing Sun, Xiao-Jun Wang
  • Patent number: 6506781
    Abstract: A method is disclosed for rational design of a PPAR, FXR, LXR-alpha, or LXR-beta antagonist comprising chemical modification of a PPAR, FXR, LXR-alpha, or LXR-beta agonist to: a) prevent formation of a hydrogen bond between the agonist and tyrosine or histidine, or tryptophan involved in receptor activation; and/or b) displace the tyrosine or histidine, or tryptophan involved in receptor activation from its agonist bound position. Preferably, little or no additional changes are made in the structure of the agonist so that the resulting antagonist is a close structural analogue of the agonist.
    Type: Grant
    Filed: March 7, 2002
    Date of Patent: January 14, 2003
    Assignee: SmithKline Beecham Corporation
    Inventors: Jeffrey Edmond Cobb, Millard Hurst Lambert, III, Michael Vance Milburn, Barry George Shearer
  • Patent number: 6503912
    Abstract: The present application relates to novel guanidine derivatives of the formula (I) in which R1 represents a five- or six-membered heterocyclic group; R2 represents hydrogen or alkyl, R3 represents the groupings —OR4, —OCOR5, —OCOOR6, —OCONR7R8 and —OSO2R9, where R4, R5 and R6 independently of one another represent alkyl, alkoxyalkyl, halogenoalkyl, alkenyl, alkinyl, alkylaminoalkyl, dialkylaminoalkyl, optionally substituted cycloalkyl and in each case optionally substituted phenyl or benzyl, R7 and R8 independently of one another represent hydrogen, alkyl, alkenyl and in each case optionally substituted phenyl or benzyl and R9 represents alkyl or optionally substituted phenyl, A represents the groupings —CH2CH2—, (CH2)3 and —CH═CH— and z represents cyano or nitro, with the proviso that, if Z represents NO2 and A represents —CH2CH2—, the radical R2 represents hydrogen; and the compound of the formula (I) in which
    Type: Grant
    Filed: June 28, 2000
    Date of Patent: January 7, 2003
    Assignee: Bayer Aktiengesellschaft
    Inventors: Klaus Wagner, Christoph Erdelen, Wolfram Andersch, Ulrike Wachendorff-Neumann, Andreas Turberg, Norbert Mencke
  • Patent number: 6500950
    Abstract: Benzylidenepyrazolones of the formula I, where the substituents and the index n have the following meanings: R1 is unsubstituted or substituted C1-C6-alkyl; R2 is unsubstituted or substituted C1-C6-alkyl, unsubstituted or substituted C1-C6-alkoxy, halogen, nitro, cyano; R3 is hydrogen, halogen, nitro, cyano, a group NR5R6, OCOR5, NR5COR6, CO2R5, —COSR5, —CONR5R6, C1-C4-alkoxyiminoalkyl, C1-C6-alkylcarbonyl, unsubstituted or substituted C1-C6-alkyl, unsubstituted or substituted C1-C6-alkoxy, unsubstituted or substituted C1-C6-alkylthio, unsubstituted or substituted C2-C6-alkenyl, unsubstituted or substituted C2-C6-alkynyl, unsubstituted or substituted phenyl, unsubstituted or substituted phenoxy, an unsubstituted or substituted 5- or 6-membered saturated or unsaturated heterocycle which may contain up to 4 nitrogen atoms and/or up to 2 oxygen or sulfur atoms as ring members; R4 is C1-C6-alkyl, C1-C4-haloalkyl; R3 and R4 form an optionally substituted saturated or unsaturated
    Type: Grant
    Filed: January 22, 2001
    Date of Patent: December 31, 2002
    Assignee: BASF Aktiengesellschaft
    Inventors: Joachim Rheinheimer, Matthias Witschel, Stefan Engel, Ernst Baumann, Wolfgang von Deyn, Regina Luise Hill, Guido Mayer, Ulf Misslitz, Oliver Wagner, Martina Otten, Karl-Otto Westphalen, Helmut Walter
  • Publication number: 20020198244
    Abstract: A heterocyclic aromatic oxazole compound of the formula (I) 1
    Type: Application
    Filed: July 18, 2001
    Publication date: December 26, 2002
    Inventors: Junichi Haruta, Hiromasa Hashimoto, Mutsuyoshi Matsushita
  • Publication number: 20020198245
    Abstract: A heterocyclic aromatic oxazole compound of the formula (I) 1
    Type: Application
    Filed: July 18, 2001
    Publication date: December 26, 2002
    Inventors: Junichi Haruta, Hiromasa Hashimoto, Mutsuyoshi Matsushita
  • Patent number: 6498174
    Abstract: The present invention discloses compounds of formula (I), and tautomeric forms, pharmaceutically acceptable salts, or solvates thereof. Preferably, the compounds of the invention are dual activators of hPPAR&ggr; and hPPAR{acute over (&agr;)}.
    Type: Grant
    Filed: February 22, 2001
    Date of Patent: December 24, 2002
    Assignee: SmithKline Beecham Corporation
    Inventors: Jon Loren Collins, Milana Dezube, Jeffrey Alan Oplinger, Timothy Mark Willson
  • Publication number: 20020188123
    Abstract: Novel polydentate asymmetric nitrogen-oxygen-containing binaphthyl derivatives of the formulae (I) and (II), and metal complexes of these compounds may be used as catalysts for enantioselective transformations.
    Type: Application
    Filed: May 2, 2002
    Publication date: December 12, 2002
    Applicant: DEGUSSA AG
    Inventors: Axel Monsees, Carsten A. Schneider, Thomas Riermeier, Uwe Dingerdissen
  • Patent number: 6492396
    Abstract: The present invention is directed to chemical compositions of substituted thioacetamides, processes for the preparation thereof and uses of the compositions in the treatment of diseases.
    Type: Grant
    Filed: May 15, 2001
    Date of Patent: December 10, 2002
    Assignee: Cephalon, Inc.
    Inventors: Edward R. Bacon, Sankar Chatterjee, Derek Dunn, John P. Mallamo, Jeffry L. Vaught, Matthew S. Miller
  • Publication number: 20020177586
    Abstract: Provided, among other things, is a method of treating or ameliorating or preventing an indication of the invention in an animal, including a human comprising administering an effective amount of a compound of the formula I: 1
    Type: Application
    Filed: December 31, 2001
    Publication date: November 28, 2002
    Inventors: John J. Egan, Dilip Wagle, Sara Vasan, Martin Gall, Stanley Bell, Edmond J. LaVoie
  • Publication number: 20020177595
    Abstract: This invention relates to novel phenyl oxazoles, thiazoles, oxazolines, oxadiazoles and benzoxazoles useful as neuro-protective agents.
    Type: Application
    Filed: March 27, 2002
    Publication date: November 28, 2002
    Inventors: Jill Ann Panetta, John Kevin Shadle, Lawrence Joseph Heinz, Michael LeRoy Phillips, John Robert Rizzo, Benjamin Alan Anderson, John Allan Rieck, David Lee Varie
  • Publication number: 20020173526
    Abstract: A compound represented by the formula: 1
    Type: Application
    Filed: July 24, 2001
    Publication date: November 21, 2002
    Inventors: Akihiro Tasaka, Takenori Hitaka, Etsuya Matsutani
  • Patent number: 6482842
    Abstract: The present invention describes compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds are protein kinase inhibitors and are useful in the treatment of proliferative diseases, for example, cancer, inflammation and arthritis. They may also be useful in the treatment of Alzheimer's disease, and cardiovascular disease.
    Type: Grant
    Filed: February 6, 2001
    Date of Patent: November 19, 2002
    Assignee: Bristol-Myers Squibb Company
    Inventors: Mark E. Salvati, S. David Kimball
  • Publication number: 20020156289
    Abstract: Commercially feasible methods for synthesizing various epothilones precursors needed for the preparation of final epothilones are provided, including techniques for the synthesis of epothilone segment A and C precursors. Segment C precursors are prepared using starting nitriles, which can alternately be oxidized to ketones and converted, or reacted to form the diol with subsequent conversion to the segment. Segment A precursors are prepared by reacting a starting enone with a chiral catalyst to give an intermediate alcohol in high enantomeric excess, followed by conversion of the alcohol to the desired Segment A precursor.
    Type: Application
    Filed: December 11, 2001
    Publication date: October 24, 2002
    Applicant: THE UNIVERSITY OF KANSAS
    Inventors: Gunda I. Georg, Sajiv K. Nair, Emily Reiff, Ashok Rao Tunoori
  • Patent number: 6465646
    Abstract: Compounds of Formula 1 and of Formula 2 where the symbols have the meaning defined in the specification, have retinoid, retinoid antagonist or retinoid negative hormone like biological activity.
    Type: Grant
    Filed: August 4, 2000
    Date of Patent: October 15, 2002
    Assignee: Allergan, Inc.
    Inventors: Richard L. Beard, Diana F. Colon, Roshantha A. Chandraratna
  • Patent number: 6465647
    Abstract: Compounds of the Formula 1, Formula 2, Formula 3 and Formula 4 wherein the symbols have the meaning assigned to them in the disclosure have retinoid-like biological activity.
    Type: Grant
    Filed: August 4, 2000
    Date of Patent: October 15, 2002
    Assignee: Allergan, Inc.
    Inventors: Richard L. Beard, Diana F. Colon, Roshantha A. Chandraratna
  • Publication number: 20020143040
    Abstract: A heterocyclic aromatic oxazole compound of the formula (I) 1
    Type: Application
    Filed: July 18, 2001
    Publication date: October 3, 2002
    Inventors: Junichi Haruta, Hiromasa Hashimoto, Mutsuyoshi Matsushita
  • Patent number: 6458803
    Abstract: The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N-phenyl-N-heteroaralkyl aminoalcohols.
    Type: Grant
    Filed: November 23, 2001
    Date of Patent: October 1, 2002
    Assignee: G.D. Searle & Co.
    Inventors: James A. Sikorski, Richard C. Durley, Deborah A. Mischke, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Margaret L. Grapperhaus, Brian S. Hickory, Mark A. Massa, Monica B. Norton, William F. Vernier, Barry L. Parnas, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
  • Patent number: 6451824
    Abstract: Compounds of formula (I) are suitable for the production of pharmaceuticals for the prophylaxis and therapy of disorders in the course of which an increased activity of matrix-degrading metalloproteinases is involved.
    Type: Grant
    Filed: May 8, 1998
    Date of Patent: September 17, 2002
    Assignee: Aventis Pharma Deutschland GmbH
    Inventors: Werner Thorwart, Wilfried Schwab, Manfred Schudok, Burkhard Haase
  • Patent number: 6451830
    Abstract: The invention relates to use of substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N,N-disubstituted non-fused heterocyclo amines.
    Type: Grant
    Filed: November 14, 2001
    Date of Patent: September 17, 2002
    Assignee: G.D. Searle & Co.
    Inventors: James A. Sikorski, Richard C. Durley, Deborah A. Mischke, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Margaret L. Grapperhaus, Brian S. Hickory, Mark A. Massa, Monica B. Norton, William F. Vernier, Barry L. Parnas, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
  • Patent number: 6448396
    Abstract: The present invention provides a process of preparing a compound of the formula IV wherein: R1 and R2 are each individually -(C1-C6)alkyl, -(C1-C6)alkoxy or phenyl, R3 is H or -(C1-C6)alkyl, R6 is —NR7R8, morpholin-1-yl, imidazol-1-yl, 4,5-dihydro-1H-imidazol-2-yl, thiomorpholin-1-yl, piperazin-1-yl or piperazin-1-yl substituted with -(C1-C4)alkyl or  and R7 and R8 are each individually hydrogen, -(C1-C6)alkyl, —(CH2)pOH,  —(CH2)p-piperidyl, —(CH2)pS(C1-C6)alkyl, —(CH2)pO(C1-C6)alkyl  where R9 is (C1-C6)alkyl; P is an integer from 1-3 both inclusive; q is 0 or 1; and t is 1 to 6 both inclusive; or a pharmaceutically acceptable salt, hydrate or optical isomer thereof, which is useful as a neuroprotective agent.
    Type: Grant
    Filed: September 23, 1998
    Date of Patent: September 10, 2002
    Assignee: Eli Lilly and Company
    Inventors: Benjamin Alan Anderson, Lawrence Joseph Heinz, Jill Ann Panetta, Michael LeRoy Phillips, John Allan Rieck, III, John Robert Rizzo, John Kevin Shadle, David Lee Varie
  • Patent number: 6444827
    Abstract: The present invention relates to a novel method for producing an intermediate compound [6] wherein R is as defined above, at high yield.
    Type: Grant
    Filed: April 23, 2001
    Date of Patent: September 3, 2002
    Assignee: Japan Tobacco Inc.
    Inventors: Koji Ando, Masanobu Suzuki
  • Patent number: 6444662
    Abstract: Described are salts of hyperforin and adhyperforin of formula I [A−]m[B]p+  (I) wherein m is an integer from 1 to 3, p is equal to m and gives the total number of positive charges of the residue [B], [A−] is an anion of formula II with n=0 or 1 and [B]p+ is an ion of an alkali metal or an ammonium ion of a salt-forming nitrogen base of formula III wherein R1 through R4 have a variety of meanings including hydrogen, alkyl, cycloalkyl and similar groups which in turn may be substituted with one or more substituents. The salts serve inter alia for enriching or purifying hyperforin and adhyperforin from St. John's Wort extracts. Pharmaceutical preparations containing the salts are used for treating Alzheimer's Disease.
    Type: Grant
    Filed: August 11, 2000
    Date of Patent: September 3, 2002
    Assignee: Willmar Schwabe GmbH & Co.
    Inventors: Shyam Sunder Chatterjee, Clemens Erdelmeier, Klaus Klessing, Dieter Marme, Christoph Schächtele
  • Patent number: 6441013
    Abstract: The present invention relates to sulphonylexazolamines of general formula (I), wherein R1, R2 represent independently from each other H, A, —(CH2)n—Ar or alkenyl with 2-6 C atoms, R1 and R2 together also represent a mononuclear saturated heterocycle with 1-2 N, O and/or S atoms, Z is H, A, CF3, NO2, Hal, OH, OA, NH2, NHA or NH2. A represents alkyl with 1-6 C atoms, Ar is Z-monosubstituted or Z-disubstituted phenyl, Hal is F, Cl, Br, or L n is 1 or 2 of the physiologically acceptable salts or solvates thereof. Said sulphonyloxazolamines are used as therapeutic active ingredients. The invention also relates to the use of sulphonyloxazolamines as therapeutic active ingredients and/or to the production of pharmaceutical preparations to combat diseases of the central nervous system. The invention further relates to a pharmaceutical preparation and the production thereof.
    Type: Grant
    Filed: June 14, 2001
    Date of Patent: August 27, 2002
    Assignee: Merck Patent GmbH
    Inventors: Hartmut Greiner, Gerd Bartoszyk, Henning Böttcher, Gerhard Barnickel, Bertram Cezanne
  • Publication number: 20020115701
    Abstract: A heterocyclic aromatic oxazole compound of the formula (I) 1
    Type: Application
    Filed: July 18, 2001
    Publication date: August 22, 2002
    Inventors: Junichi Haruta, Hiromasa Hashimoto, Mutsuyoshi Matsushita
  • Patent number: 6437144
    Abstract: The present invention is concerned with a novel process for the preparation of the hydroxybenzothiophene of formula I comprising cyclocarbonylation of a compound of formula II wherein Y is as defined in the specification, followed by saponification. The compound of Formula I is a building block of pharmaceutically active substances, e.g. 5-[4-[2-(5-methyl-2-phenyl-4-oxazolyl)ethoxy]-7-benzothiophenylmethyl]-2,4-thiazolidinedione and the corresponding sodium salt which are from agents useful in the treatment of diabetes.
    Type: Grant
    Filed: May 8, 2001
    Date of Patent: August 20, 2002
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Bernd Junghans, Michelangelo Scalone, Thomas Albert Zeibig
  • Patent number: 6436967
    Abstract: This invention is in the field of antiinflammatory pharmaceutical agents and specifically relates to prodrugs of compounds which selectively inhibit cyclooxygenase-2. The use of non-steroidal antiinflammatory drugs (NSAIDs) in treating pain and the swelling associated with inflammation also produce severe side effects, including life threatening ulcers. The recent discovery of an inducible enzyme associated with inflammation (“prostaglandin G/H synthase II” or “cyclooxygenase-2 (COX-2)”) provides a viable target of inhibition which more effectively reduces inflammation and produces fewer and less drastic side effects.
    Type: Grant
    Filed: September 14, 2000
    Date of Patent: August 20, 2002
    Assignee: Pharmacia Corporation
    Inventors: John J Talley, James W Malecha, Stephen Bertenshaw, Matthew J Graneto, Jeffery Carter, Jinglin Li, Srinivasan Nagarajan, David L Brown, Donald J Rogier, Jr., Thomas D Penning, Ish K Khanna, Xiangdong Xu, Richard M Weier
  • Publication number: 20020107270
    Abstract: A heterocyclic aromatic oxazole compound of the formula (I) 1
    Type: Application
    Filed: July 18, 2001
    Publication date: August 8, 2002
    Inventors: Junichi Haruta, Hiromasa Hashimoto, Mutsuyoshi Matsushita
  • Publication number: 20020107271
    Abstract: A heterocyclic aromatic oxazole compound of the formula (I) 1
    Type: Application
    Filed: July 18, 2001
    Publication date: August 8, 2002
    Inventors: Junichi Haruta, Hiromasa Hashimoto, Mutsuyoshi Matsushita
  • Patent number: 6426355
    Abstract: Compounds having the formula: wherein R1-R5, X and G are described herein and which are useful in the treatment of diseases associated with herpes viruses including human cytomegalovirus, herpes simplex viruses, Epstein-Barr virus, varicella-zoster virus, human herpesviruses-6 and -7, and Kaposi herpesvirus.
    Type: Grant
    Filed: September 27, 2000
    Date of Patent: July 30, 2002
    Assignee: American Home Products
    Inventors: Jonathan Bloom, Kevin Curran, Martin DiGrandi, Russell Dushin, Thomas Jones, Stanley Lang, Adma Ross, Eugene A. Terefenko, Bryan O'Hara
  • Patent number: 6423849
    Abstract: A 5-(2-substituted-4-nitrophenyl)-oxazole is prepared by decarboxylating a 5-(2-substituted-4-nitrophenyl)-4-oxazolecarboxylic acid in an aprotic amide solvent containing a protic compound. A 5-(2-substituted-4-nitrophenyl)-oxazolecarboxylic acid and a 5-(2-substituted-4-nitrophenyl)-carboalkoxyoxazole, which are novel compounds, are provided.
    Type: Grant
    Filed: December 26, 2000
    Date of Patent: July 23, 2002
    Assignee: The Nippon Synthetic Chemical Industry Co., Ltd.
    Inventors: Akio Katsuura, Azusa Yonezawa, Keisuke Tsuzuki, Kazumasa Hirata
  • Publication number: 20020091264
    Abstract: Compounds of the formula (I) are disclosed which are vitronectin receptor antagonists and are useful in the treatment of osteoporosis: 1
    Type: Application
    Filed: December 17, 2001
    Publication date: July 11, 2002
    Applicant: SmithKline Beecham Corporation
    Inventors: William E. Bondinell, William H. Miller, Dirk Heerding, James M. Samanen
  • Patent number: 6417212
    Abstract: The present invention is directed to compounds represented by Structural Formula I and pharmaceutically acceptable salts, solvates and hydrates thereof, and methods of making, methods of using and pharmaceutical compositions having compounds represented by Structural Formula I and pharmaceutically acceptable salts, solvates and hydrates thereof: In Structural Formula I, n is 2, 3, or 4; V is O or S; W is O, S, or SO2; R1 is H, a C1-C4 alkyl, phenyl or trifluoromethyl; R2 are each, independently, H, a C1-C6 alkyl, an aryl-C1-C6 alkyl, a cycloalkyl-C1-C4 alkyl, an aryl, a cycloalkyl, or together with the phenyl to which they are bound form naphthyl or 1,2,3,4-tetrahydronaphthyl; R3 are each, independently, H, a C1-C6 alkyl, an aryl-C1-C6 alkyl, a cycloalkyl-C1-C4 alkyl, an aryl, or a cycloalkyl; R4 are each, independently, H, a C1-C4 alkyl, an aryl, or benzyl; R5 are each, independently, H, a substituted or unsubstituted aryl or a heteroaryl, provided that at least one R5 is a substituted or u
    Type: Grant
    Filed: August 23, 2000
    Date of Patent: July 9, 2002
    Assignees: Eli Lilly & Company, Ligand Pharmaceuticals, Inc.
    Inventors: Dawn A. Brooks, Christopher J. Rito, Anthony J. Shuker, Samuel J. Dominianni, Alan M. Warshawsky, Lynn S. Gossett, Donald P. Matthews, David A. Hay, Robert J. Ardecky, Pierre-Yves Michellys, John S. Tyhonas
  • Patent number: 6414001
    Abstract: Ether and amide derivatives are disclosed, which are represented by the following formula (I) and its pharmaceutical acceptable salt, and which are useful for the treatment of diabetes. R1—A—R2  (I) wherein (with the provisos that (i) when A is —O—, then n is 2 or 3 (ii) when then n is 1 or 2. R3 is OH—, CH3SO2NH—, CF3SO2NH—, CH3SO2NHCH2—, CF3SO2NHCH2—, HOOC—, CH3OOC—, HOOC—CH2SO2NH—, CF3—CH2SO2NH—,  R8—NHSO2—, R8—NHSO2—CH2—, HOOC—CH2—O—, HSO3N═CH—, or R9—SO2NHCO—; R4 is H, OH, O-alkyl or O—CH2OCH3; R5 is H, halogen atom, —CH2COOH or OH; R6 and R7 are hydrogen, t-butyl or pyrolidyl; R8 is hydrogen or lower alkyl; R9 is alkyl or thienyl; R10 is lower alkyl) or a pharmaceutically acceptable salt.
    Type: Grant
    Filed: January 10, 2001
    Date of Patent: July 2, 2002
    Assignee: Kotobuki Pharmaceutical Co. Ltd.
    Inventors: Tsuyoshi Tomiyama, Akira Tomiyama, Hiroshi Tomiyama, Keiko Kuroiwa
  • Patent number: 6410740
    Abstract: The present invention relates to new heterocyclylmethyl-substituted pyrazole derivatives, processes for their preparation and their use as medicaments, in particular as medicaments for treatment of cardiovascular diseases.
    Type: Grant
    Filed: August 25, 2000
    Date of Patent: June 25, 2002
    Assignee: Bayer Aktiengesellschaft
    Inventors: Alexander Straub, Chantal Fürstner, Ulrich Niewöhner, Thomas Jaetsch, Achim Feurer, Raimund Kast, Johannes-Peter Stasch, Elisabeth Perzborn, Joachim Hütter, Klaus Dembowsky, Dieter Arlt
  • Publication number: 20020077483
    Abstract: The invention relates to methods of synthesizing libraries of diverse and complex 2-substituted azole compounds of the general formula (I) or (II) 1
    Type: Application
    Filed: May 22, 2001
    Publication date: June 20, 2002
    Inventors: Yijun Deng, Dennis Hlasta
  • Publication number: 20020072613
    Abstract: The present invention relates to a method for producing a compound of the formula [7] 1
    Type: Application
    Filed: February 6, 2002
    Publication date: June 13, 2002
    Applicant: Japan Tobacco Inc.
    Inventors: Koji Matsuda, Katsuyoshi Hara, Minoru Akamatsu
  • Patent number: 6399782
    Abstract: Novel benzimidazole compounds of the following structure and their use as fructose-1,6-bisphosphatase inhibitors is described
    Type: Grant
    Filed: April 11, 2000
    Date of Patent: June 4, 2002
    Assignee: Metabasis Therapeutics, Inc.
    Inventors: Srinivas Rao Kasibhatla, K. Raja Reddy, Mark D. Erion, Qun Dang, Gerard R. Scarlato, M. Rami Reddy
  • Patent number: 6395724
    Abstract: Disclosed are multibinding compounds which inhibit cyclooxygenase-2 (COX-2), an enzyme which catalyzes the first committed step in the biosynthesis of prostaglandins. The multibinding compounds of this invention containing from 2 to 10 ligands covalently attached to one or more linkers. Each ligand is a moiety capable of binding to COX-2. The multibinding compounds of this invention are useful in the treatment inflammation, pain, fever and the like.
    Type: Grant
    Filed: June 7, 1999
    Date of Patent: May 28, 2002
    Assignee: Advanced Medicine, Inc.
    Inventors: J. Kevin Judice, Deborah L. Higgins, John H. Griffin
  • Patent number: 6392055
    Abstract: The present invention provides an efficient synthetic strategy for the preparation of analogs that incorporate important structural elements of the marine natural product curacin A, the compositions and various uses of the compositions. The most active of these compounds at nanomolar concentrations inhibit tubulin polymerization, show growth inhibition activity, inhibited colchicines binding to tubulin and block mitotic progression. The compounds of the present invention represent some of the most potent synthetic curacin A analogs synthesized, with an activity profile rivaling that of the natural product despite the simplified structure, greater water solubility, and increased chemical stability.
    Type: Grant
    Filed: July 19, 2001
    Date of Patent: May 21, 2002
    Assignee: The University of Pittsburgh
    Inventors: Peter Wipf, Jonathan T. Reeves, Billy W. Day, Raghavan Balachandran
  • Publication number: 20020058690
    Abstract: The invention encompasses the novel compounds of Formula I, which are useful in the treatment of cyclooxygenase-2 mediated diseases.
    Type: Application
    Filed: June 27, 2001
    Publication date: May 16, 2002
    Inventors: Chun-Sing Li, Cheuk Kun Lau, Michel Therien, Petpiboon Prasit
  • Patent number: 6387940
    Abstract: The present invention relates to new heterocyclylmethyl-substituted pyrazole derivatives, processes for their preparation and their use as medicaments, in particular as medicaments for treatment of cardiovascular diseases.
    Type: Grant
    Filed: August 23, 2000
    Date of Patent: May 14, 2002
    Assignee: Bayer Aktiengesellschaft
    Inventors: Alexander Straub, Chantal Fürstner, Ulrich Niewöhner, Thomas Jaetsch, Achim Feurer, Raimund Kast, Johannes-Peter Stasch, Elisabeth Perzborn, Joachim Hütter, Klaus Dembowsky, Dieter Arlt
  • Publication number: 20020052392
    Abstract: The instant invention provides &bgr;3 adrenergic receptor agonists of structural Formula (I), 1
    Type: Application
    Filed: October 17, 2001
    Publication date: May 2, 2002
    Inventors: Robert F. Day, Jennifer A. Lafontaine
  • Patent number: 6380258
    Abstract: A sulfonyl divalent aromatic or heteroaromatic ring hydroxamic acid compound that inter alia inhibits matrix metalloprotease activity is disclosed as are a treatment process that comprises administering a contemplated sulfonyl divalent aromatic or heteroaromatic ring hydroxamic acid compound in a MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity.
    Type: Grant
    Filed: June 24, 1999
    Date of Patent: April 30, 2002
    Assignee: G. D. Searle, L.L.C.
    Inventors: Louis J. Bedell, Joseph J. McDonald, Thomas E. Barta, Daniel P. Becker, Shashidhar N. Rao, John N. Freskos, Brent V. Mischke, Daniel P. Getman, Gary A. DeCrescenzo