Bicyclo Ring System Having The Additional Hetero Ring As One Of The Cyclos Patents (Class 544/376)
Plural ring chalcogens in the bicyclo ring system (Class 544/377)
  • Aminoalkoxybenzoyl-benzofuran or benzothiophene derivatives, method of preparing same and compositions containing same
    Publication number: 20030225100
    Abstract: Benzothiophenes and related compounds of formula (1), wherein A, B, Z are independently —CH═, —CR4═ or ═N—; X is —S—, —O—, —NH—, —NR2, —CH2—CH2—, CH2—CH2—CH2—, —CH2—O—; —OCH2—, —CH2—S—, —CO—, —SCH2—.
    Type: Application
    Filed: February 20, 2003
    Publication date: December 4, 2003
    Inventors: Jean-Louis Assens, Claude Bernhart, Frederique Cabanel-Haudricourt, Patrick Gautier, Dino Nisato
  • PNA monomer and precursor
    Publication number: 20030225252
    Abstract: This application relates to monomers of the general formula (I) for the preparation of PNA (peptide nucleic acid) oligomers and provides method for the synthesis of both predefined sequence PNA oligomers and random sequence PNA oligomers: 1
    Type: Application
    Filed: April 25, 2003
    Publication date: December 4, 2003
    Inventors: Sung Kee Kim, Hyunil Lee, Jong Chan Lim, Hoon Choi, Jae Hoon Jeon, Sang Youl Ahn, Sung Hee Lee, Won Jun Yoon
  • Preparing amidines derived from 6-hydroxy-2,5,7,8-tetramethylchromane-2-carboxylic acid
    Patent number: 6653472
    Abstract: New intermediates of the formula (II)B described below for the synthesis of amidine derivatives of (−)-6-hydroxy-2,5,7,8-tetramethylchromane-2-carboxylic acid, such as for example (S)-N-{4-[4-[(3,4-dihydro-6-hydroxy-2,5,7,8-tetramethyl-2H-1-benzopyran-2-yl)-carbonyl]-1-piperazinyl]phenyl}-2-thiophenecarboximidamide wherein A′ is X is —Z1—CO; &rgr; is a bond or a heterocycle selected from the group consisting of piperidine, piperazine, homopiperazine, 2-methylpiperazine, 2,5-dimethyl-piperazine and 4-aminopiperidine; Y is —Z2— or —NR3—Z2, R3 is hydrogen, alkyl of 1 to 6 carbon atoms or —COR4, R4 is alkyl of 1 to 6 carbon atoms; Z1 and Z2 independently are a single bond or alkylene of 1 to 6 carbon atoms; and R6 is hydrogen or OH.
    Type: Grant
    Filed: April 26, 2002
    Date of Patent: November 25, 2003
    Assignee: Societe de Conseils de Recherches et d'Applications Scientifiques (S.C.R.A.S.)
    Inventors: Christine Le Breton, Eric Manginot, Jean-Bernard Cazaux
  • Dihydrobenzofuran and dihydrobenzothiophene 2,4-pentadienoic acid derivatives having selective activity for retinoid X (RXR) receptors
    Publication number: 20030216570
    Abstract: Compounds of the formula 1
    Type: Application
    Filed: April 30, 2002
    Publication date: November 20, 2003
    Inventors: Jayasree Vasudevan, Dehua Huang, Vidyasagar Vuligonda, Roshantha S. Chandraratna
  • Benzopyran or thiobenzopyran derivatives
    Patent number: 6645951
    Abstract: The present invention provides novel benzopyran compounds, pharmaceutically acceptable salts thereof and stereoisomers thereof where the benzopyran compounds of the invention are compounds according to Formula I: The present invention further provides pharmaceutical compositions which possess anti-estrogenic activity and comprise at least one benzopyran compound of the invention and a method of treating breast cancer by administration of an effective amount of a benzopyran compound provided by the present invention.
    Type: Grant
    Filed: July 16, 2001
    Date of Patent: November 11, 2003
    Assignee: Chugai Seiyaku Kabushiki Kaisha
    Inventors: Jae Chon Jo, Hyun Suk Lim, Jong Min Kim, Ju Su Kim, Kazumi Morikawa, Yoshitake Kanbe, Myung Hwa Kim, Masahiro Nishimoto
  • Gamma-hydroxy-2-(fluoroalkylaminocarbonyl)-1-piperazinepentanamides and uses thereof
    Patent number: 6642237
    Abstract: &ggr;-Hydroxy-2-(fluoroalkylaminocarbonyl)-1-piperazinepentanamide compounds are inhibitors of HIV protease and inhibitors of HIV replication. These compounds are useful in the prevention or treatment of infection by HV and the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described. These compounds are effective against HIV viral mutants which are resistant to HIV protease inhibitors currently used for treating AIDS and HIV infection.
    Type: Grant
    Filed: November 21, 2000
    Date of Patent: November 4, 2003
    Assignee: Merck & Co., Inc.
    Inventors: James R. Tata, Kevin T. Chapman, Joseph Leslie Duffy, Nancy J. Kevin, Yuan Cheng, Thomas A. Rano, Fengqi Zhang, Tracy Huening, Brian Anthony Kirk, Zhijian Lu, Subharekha Raghavan, Fred J. Fleitz, Daniel E. Petrillo, Joseph D. Armstrong, III, Richard J. Varsolona, David Askin, R. Scott Hoerrner, Robert Purick
  • Benzofurylpiperazine serotonin agonists
    Patent number: 6638936
    Abstract: The present invention provides serotonergic benzofurans of Formula I: where R is methyl or ethyl, or pharmaceutically acceptable acid addition salts thereof.
    Type: Grant
    Filed: May 6, 2002
    Date of Patent: October 28, 2003
    Assignee: Eli Lilly and Company
    Inventors: Karin Briner, Timothy Paul Burkholder, Mark Louis Heiman, David Lloyd Garver Nelson
  • Benzofuran and dihydrobenzofuran derivatives useful as beta-3 adrenoreceptor agonists
    Publication number: 20030195352
    Abstract: This invention relates to novel benzofuran and dihydrobenzofuran compounds, pharmaceutical compositions containing such compounds, and methods of treating beta-3 adrenoreceptor-mediated conditions with such compositions.
    Type: Application
    Filed: September 10, 2002
    Publication date: October 16, 2003
    Inventors: Gaetan H. Ladouceur, William R. Schoen, Michael J. Burke
  • Indole derivatives useful for the treatment of CNS disorders
    Publication number: 20030191133
    Abstract: The present invention relates to dopamine D4 ligands having the general formula I 1
    Type: Application
    Filed: December 9, 2002
    Publication date: October 9, 2003
    Applicant: H. Lundbeck A/S
    Inventors: Benny Bang-Andersen, Jakob Felding, Jan Kehler, Kim Andersen
  • Derivatives of sulphonamides, their preparation and use as medicaments
    Publication number: 20030191124
    Abstract: The present invention relates to new derivatives of sulphonamides, with the general formula (I), as well as to their physiologically acceptable salts, the processes for their preparation, their application as medicaments in human and/or veterinary therapy and the pharmaceutical compositions that contain them 1
    Type: Application
    Filed: November 13, 2002
    Publication date: October 9, 2003
    Inventors: Ramon Merce-Vidal, Blas Andaluz-Mataro, Jordi Frigola-Constansa
  • New linear cyclic ureas
    Publication number: 20030191132
    Abstract: Compound of formula (I): 1
    Type: Application
    Filed: November 12, 2002
    Publication date: October 9, 2003
    Inventors: Jean-Louis Peglion, Christophe Poitevin, Jean-Paul Vilaine, Nicole Villeneuve, Marie-Pierre Bourguignon, Catherine Thollon
  • Coumarin derivatives with comt inhibiting activity
    Publication number: 20030186975
    Abstract: Compounds of formula (I′) wherein the two OH— substituents in the phenyl moiety are in a position ortho to one another and R1 in a position ortho to one of the hydroxy groups; and X, R1 to R6 are as defined in claims, exhibit COMT enzyme inhibiting activity so that they are useful as COMT inhibitors.
    Type: Application
    Filed: March 31, 2003
    Publication date: October 2, 2003
    Inventors: Jarmo Pystynen, Martti Ovaska, Jukka Vidgren, Timo Lotta, Marjo Yliperttula-Ikonen
  • Substituted piperazine derivatives, the preparation thereofand their use as medicaments
    Publication number: 20030166637
    Abstract: The present invention relates to substituted piperazine derivatives of general formula 1
    Type: Application
    Filed: October 9, 2002
    Publication date: September 4, 2003
    Inventors: Thorsten Lehmann-Lintz, Armin Heckel, Leo Thomas, Michael Mark
  • Novel substituted aryl alkenoic acid heterocyclic amides
    Publication number: 20030161860
    Abstract: The present invention relates to novel compounds possessing specific hot, pungent and spicy taste when subjected to direct pungency evaluation, which may be useful as food additives and anti-oxidants, however the said compounds do not add to any nutritional value but the synthesised compounds can possess useful pharmacological properties which is expected to find application in new test models for the development of anti-inflammatory drugs, bioavailability enhancers and for the study of hepatic drug metabolising mechanism; also relates to a process for preparing the said compounds.
    Type: Application
    Filed: February 7, 2002
    Publication date: August 28, 2003
    Inventors: Subhash Chandra Taneja, Surrinder Koul, Jawahir Lal Koul, Beenu Moza, Sukhdev Swami Handa
  • Novel compounds for treatment of cardiac arrhythmia, synthesis, and methods of use
    Publication number: 20030158194
    Abstract: 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: Application
    Filed: December 10, 2002
    Publication date: August 21, 2003
    Inventor: Pascal Druzgala
  • Derivatives of flavones, xanthones and coumarins
    Patent number: 6608089
    Abstract: Compounds having the formula (I) Z—OCH2—C≡CCH2—NRR1  (I) or a pharmaceutically acceptable salt or solvate thereof wherein Z can represent the formula (1A) or (1B). The compounds possess antiproliferative activity and are useful as modulators of multiple drug resistance in cancer chemotherapy. The compounds may also be useful for the manufacture of a medicament for the treatment or prevention of neoplasms, menopausal disorders and osteoporosis.
    Type: Grant
    Filed: February 15, 2002
    Date of Patent: August 19, 2003
    Assignee: Indena S.p.A.
    Inventors: Ezio Bombardelli, Piero Valenti
  • 7-phenyl-benzo [b] thiophen amide derivatives
    Publication number: 20030149030
    Abstract: A compound of the formula 1
    Type: Application
    Filed: December 10, 2002
    Publication date: August 7, 2003
    Inventors: Alexander Alanine, Alexander Flohr
  • Piperidine, tetrahydropyridine and piperazine derivatives, their preparation and use
    Patent number: 6596722
    Abstract: A piperidine, tetrahydropyridine or piperazine derivative having formula (I), any of its enantiomers or any mixture thereof, or an acid addition salt thereof, wherein B is C1-10-alkylene, C1-10-alkenylene or C1-10-alkynylene; X is —O—, —S—, or CR4R5—; and Y is —CR6R7, —CR6R7—CR8R9, or CR6═CR7—; or X and Y together form a group —CR4═CR5, or —CR4—CR5—CR6R7-; Z is —O—, or —S—; W is N, C, or CH, and the dotted line is an optional bond; A is a bicyclic ring selected from (Ia) or (Ib) wherein E1, E2 and E3 are selected from O, S, N, NR11, C, CR12 and CHR13, and the dotted line indicates an optional bond, provided that E2 and E1 and/or E3 may not simultaneously be O, or S.
    Type: Grant
    Filed: July 9, 2001
    Date of Patent: July 22, 2003
    Assignee: H. Lundbeck A/S
    Inventors: Ejner Knud Moltzen, Christian Krog-Jensen, Berith Bjørnholm
  • Substituted phenyl-piperazine derivatives, their preparation and use
    Publication number: 20030125320
    Abstract: The present invention provides compounds of the formula: 1
    Type: Application
    Filed: June 20, 2002
    Publication date: July 3, 2003
    Applicant: H. Lundbeck A/S
    Inventors: Thomas Ruhland, Christian Krog-Jensen, Mario Rottlander, Gitte Mikkelsen, Ejner Knud Moltzen, Kim Andersen
  • Method for producing 5-(1-piperazinyl) -benzofuran-2-carboxamide by transition metal-catalyzed amination
    Publication number: 20030125558
    Abstract: 1. Process for the preparation of 5-(1-piperazinyl)benzofuran-2-carboxamide in which, as intermediate step, 5-bromosalicylaldehyde or one of its derivatives is reacted in a transition metal-catalysed amination with R2-piperazine, in which R2 is as defined in claim 1.
    Type: Application
    Filed: October 10, 2002
    Publication date: July 3, 2003
    Inventors: Andreas Bathe, Steffen Emmert, Bernd Helfert, Henning Boettcher
  • Flavone derivatives, preparation method and use as medicines
    Publication number: 20030119816
    Abstract: The invention concerns novel products of formula (I) wherein: R1 represents a carbocyclic or heterocyclic radical optionally substituted; R2 and R3 are such that one represents hydrogen and the other represents piperidinyl optionally substituted; R4 represents hydrogen, alkyl or phenyl optionally substituted, said products being in all isomeric and salt forms and used as medicines.
    Type: Application
    Filed: September 4, 2002
    Publication date: June 26, 2003
    Inventors: Jean-Luc Haesslein, Dominique Lefrancois, Eric Uridat, Jidong Zhang
  • N-(3-benzofuranyl)urea-derivatives
    Publication number: 20030109578
    Abstract: 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: Application
    Filed: May 24, 2002
    Publication date: June 12, 2003
    Inventors: 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
  • Novel compounds
    Publication number: 20030105110
    Abstract: Compounds of general formula (I), wherein R1 selected from phenyl, pyridinyl, thiophenyl, furanyl, imidazolyl, and triazolyl; where each R1 phenyl ring and R1 heteroaromatic ring may optionally and independently be further substituted by 1, 2 or 3 substituents selected from straight and branched C1-C6 alkyl, NO2, CF3, C1-C6 alkoxy, chloro, fluoro, bromo, and iodo.
    Type: Application
    Filed: October 21, 2002
    Publication date: June 5, 2003
    Inventors: William Brown, Christopher Walpole, Niklas Plobeck
  • Substituted chroman derivatives
    Publication number: 20030100556
    Abstract: The present invention relates to new new piperidyl- or piperazinyl-substituted dihydro-2H-1-benzopyran derivatives compound having the formula (I) 1
    Type: Application
    Filed: November 1, 2002
    Publication date: May 29, 2003
    Inventors: Stefan Berg, Martin Nylof, Svante Ross, Seth-Olov Thorberg
  • Process for synthesis of 2-yl chroman derivatives
    Publication number: 20030100774
    Abstract: This invention provides a process for the stereospecific preparation of 2-yl-chroman and -chromene derivatives of the formula: 1
    Type: Application
    Filed: October 4, 2002
    Publication date: May 29, 2003
    Applicant: Wyeth
    Inventor: Jonathan L. Gross
  • 2,6-Substituted chroman derivatives useful as beta-3 adrenoreceptor agonists
    Publication number: 20030078260
    Abstract: This invention relates to novel 2,6-substituted chroman derivatives which are useful in the treatment of beta-3 adrenoreceptor-mediated conditions.
    Type: Application
    Filed: April 22, 2002
    Publication date: April 24, 2003
    Inventors: Stephen J. O'Connor, Gaetan H. Ladouceur, William H. Bullock, Ann-Marie Campbell, Miao Dai, Robert Dally, Jacques Dumas, Holia N. Hatoum-Mokdad, Uday Khire, Wendy Lee, Qingjie Liu, Derek B. Lowe, Steven R. Magnuson, Ning Qi, Tatiana E. Shelekhin, Quanrong Shen, Roger A. Smith, Ming Wang
  • Compounds useful for preparation of Beta-3 adrenoreceptor agonist
    Publication number: 20030073839
    Abstract: This invention related to novel sulfonamide substituted chroman derivatives which are useful in the treatment of beta-3 receptor mediated conditions.
    Type: Application
    Filed: March 7, 2000
    Publication date: April 17, 2003
    Inventors: Gaetan H. Ladouceur, Richard D. Connell, Jeremy Baryza, Anne-Marie Campbell, Timothy G. Lease, James H. Cook
  • Inhibition by 3-deoxyflavonoids of T-lymphocyte activation and therapies related thereto
    Publication number: 20030069192
    Abstract: 3-Deoxyflavonoid compounds and methods for inhibiting T-cell activity and treating diseases and disorders (e.g., autoimmune disorders, inflammatory disorders, diabetes, ALS, MS, rheumatoid arthritis, etc.). In some cases the efficacy and/or duration of action of luteolin and/or other 3-dioxyflavinoid compounds may be increased by administering such compounds along with Rutin, a Rutin congener and/or a Rutin derivative. Also, in some cases, first pass metabolism of luteolin or other 3-deoxyflavinoids may be avoided by administering such compounds by parenteral routes (e.g., sublingual, buccal, intranasal, injection, etc.).
    Type: Application
    Filed: September 6, 2002
    Publication date: April 10, 2003
    Applicant: SynorX, Inc.
    Inventors: Thomas P. Lahey, V.J. Rajadhyaksha
  • Piperazine derivatives and their use as anti-inflammatory agents
    Patent number: 6541476
    Abstract: This invention is directed to acyl piperazine derivatives, for example, of the following formula (Ia): wherein R1a, R2, R3, R4, R5, and R6 are described herein. These derivatives are useful anti-inflammatory agents. This invention is also directed to pharmaceutical compositions containing the derivatives, and methods of using the derivatives to treat inflammatory disorders in humans.
    Type: Grant
    Filed: November 14, 2000
    Date of Patent: April 1, 2003
    Assignee: Schering Aktiengesellschaft
    Inventors: John G. Bauman, Brad O. Buckman, Ameen F. Ghannam, Joseph E. Hesselgesser, Richard Horuk, Imadul Islam, Meina Liang, Karen B. May, Sean D. Monahan, Michael M. Morrissey, Howard P. Ng, Kenneth J. Shaw, Guo Ping Wei, Wei Xu, Zuchun Zhao, Wei Zheng
  • Novel chalcones
    Publication number: 20030055056
    Abstract: The present invention discloses new and useful compounds including methyl p-hydroxyphenyllactate, its analogues, chemical derivatives and chemically related compounds and their use as antitumor and immune suppressive agents, as inhibitors of proliferative cell growth and as prophylactic agents to inhibit and prevent cancer and non-malignant cell growth.
    Type: Application
    Filed: February 15, 2002
    Publication date: March 20, 2003
    Inventors: Ezio Bombardelli, Piero Valenti
  • Derivatives of benzofuran or benzodioxole
    Patent number: 6514996
    Abstract: 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 C
    Type: Grant
    Filed: November 19, 1997
    Date of Patent: February 4, 2003
    Assignee: 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
  • Urotensin-II receptor antagonists
    Patent number: 6514970
    Abstract: The present invention relates to pyrrolidiones, pharmaceutical compostions containing them and their use as antagonist of urotensin II.
    Type: Grant
    Filed: June 13, 2002
    Date of Patent: February 4, 2003
    Assignee: SmithKline Beecham Corporation
    Inventors: Dashyant Dhanak, Steven David Knight, Gregory Lee Warren, Jian Jin, Katherine L. Widdowson, Richard McCulloch Keenan
  • Compound for preparing medicines for treating pathologies involving extracellular glutamate, and methods for obtaining same
    Patent number: 6514967
    Abstract: The invention relates to compounds of the following general formula (I): in which: R1 and R2 represent a hydrogen atom, or form a ring, especially a benzene ring, R3 represents a hydrogen atom or an alkyl group, especially a methyl group, X and Y, independently of one another, represent a carbon atom, or a heteroatom such as a sulphur atom S, or a group with the formula (a) in which R4 and R5 represent a hydrogen atom or a methyl group, or R4 and R5 form a heterocycle, and their use for the preparation of a drug intended for the treatment of pathologies associated with abnormally high concentrations of extracellular glutamate.
    Type: Grant
    Filed: December 16, 1999
    Date of Patent: February 4, 2003
    Assignee: Centre National de la Recherche Scientifique
    Inventors: Jean-Marc Kamenka, Isoline Caubere, Gerard Barbanel
  • Novel carboxyl substituted chroman derivatives useful as beta 3 adrenoreceptor agonists
    Publication number: 20030013705
    Abstract: This invention is related to novel carboxyl substituted chroman derivatives which are useful in the treatment of beta-3 receptor mediated conditions.
    Type: Application
    Filed: August 21, 2002
    Publication date: January 16, 2003
    Inventors: Richard D. Connell, Timothy G. Lease, Jeremy L. Baryza
  • (Benzodioxan, benzofuran or benzopyran) derivatives having fundic relaxation properties
    Patent number: 6495547
    Abstract: The present invention of compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, wherein Alk1 is C1-6alkanediyl optionally substituted with hydroxy, C1-4alkyloxy or C1-4alkylcarbonyloxy; —Z1—Z2— is a bivalent radical; R1, R2 and R3 are each independently selected from hydrogen, C1-6alkyl, hydroxy, halo and the like; or when R1 and R2 are on adjacent carbon atoms, R1 and R2 taken together may form a bivalent radical; R4 is hydrogen or C1-6alkyl; A is a bivalent radical of formula —NR6—Alk2— (b-1), or —Npiperidinyl-(CH2)m (b-2) wherein m is 0 or 1; R5 is a radical of formula wherein n is 1 or 2; p1 is 0, and p2 is 1 or 2; or p1 is 1 or 2, and p2 is 0; X is oxygen.
    Type: Grant
    Filed: August 18, 2000
    Date of Patent: December 17, 2002
    Assignee: Janssen Pharmaceutica, N.V.
    Inventors: Piet Tom Bert Paul Wigerinck, Wim Gaston Verschueren, Marc Francis Josephine Schroven, Marcel Frans Leopold De Bruyn
  • 2-(4-bromo or 4-iodo phenylamino) benzoic acid derivatives
    Patent number: 6492363
    Abstract: Phenylamino benzoic acid, benzamides, and benzyl alcohol derivatives of the formula where R1, R2, R3, R4, R5, and R6 are hydrogen or substituent groups such as alkyl, and where R7 is hydrogen or an organic radical, and Z is COOR7, tetrazolyl, CONR6R7, or CH2OR7, are potent inhibitors of MEK and, as such, are effective in treating cancer and other proliferative diseases such as inflammation, psoriasis and restenosis, as well as stroke, heart failure, and immunodeficiency disorders.
    Type: Grant
    Filed: August 16, 2001
    Date of Patent: December 10, 2002
    Assignee: Warner-Lambert Company
    Inventors: Stephen Douglas Barrett, Alexander James Bridges, Donna Reynolds Cody, Annette Marian Doherty, David Thomas Dudley, Alan Robert Saltiel, Mel Conrad Schroeder, Haile Tecle
  • Benzofuran derivatives, their preparation and use
    Patent number: 6492374
    Abstract: The present invention relates to benzofuran derivatives having general Formula (I) wherein A is selected from (1), (2), (3), (4) wherein Z is O or S; s is 0 or 1; q is 0 or 1; R4 is hydrogen, C1-6-alkyl, C2-6-alkenyl, C26-alkynyl, C1-6-alkyl-aryl, or C1-6-alkyl-O-aryl; D is a spacer group selected from branched or straight chain C1-6-alkylene, C2-6-alkenylene and C2-6-alkynylene; its enantiomers, and pharmaceutically acceptable acid addition salt thereof. The compounds are potently binding to the 5-HT1A receptor.
    Type: Grant
    Filed: June 4, 2001
    Date of Patent: December 10, 2002
    Assignee: H. Lundbeck A/S
    Inventors: Kim Andersen, Mario Rottländer, Klaus Peter Bøgesø, Henrik Pedersen, Thomas Ruhland, Robert Dancer
  • Benzamidine derivatives as factor XA inhibitors
    Patent number: 6492368
    Abstract: Novel compounds of the formula I in which X, Y, R1, R2 and R3 are as defined in Patent Claim 1 are inhibitors of coagulation factor Xa and can be employed for the prophylaxis and/or therapy of thromboembolic disorders.
    Type: Grant
    Filed: March 31, 2000
    Date of Patent: December 10, 2002
    Assignee: Merck Patent GmbH
    Inventors: Dieter Dorsch, Hanns Wurziger, Guido Melzer, Horst Juraszyk, Sabine Bernotat-Danielowski
  • Novel derivatives of flavones, xanthones and coumarins
    Publication number: 20020183318
    Abstract: A marked up versions of the abstract showing insertions and deletions are included in Appendix A.
    Type: Application
    Filed: February 15, 2002
    Publication date: December 5, 2002
    Inventors: Ezio Bombardelli, Piero Valenti
  • 6-(4-arylalkylpiperazin-1-yl) benzodioxane and 6-(4-arylalkylpiperazin-1-yl) chromane derivatives: dopamine receptor subtype specific ligands
    Patent number: 6486164
    Abstract: Disclosed are compounds of the formula: or the pharmaceutically acceptable acid addition salts thereof wherein: R1, R2, R3, R4 and R5 are the same or different and represent hydrogen, halogen, C1-C6 alkyl, C1-C6 alkoxy, C1-C4 alkylthio, hydroxy, amino, mono- or di(C1-C6)alkylamino, cyano, nitro, trifluoromethyl or trifluoromethoxy; and X is oxygen, a bond, C1-C2 alkylene, or methyleneoxy, which compounds are useful for the treatment and/or prevention of neuropsychological disorders including, but not limited to, schizophrenia, mania, dementia, depression, anxiety, compulsive behavior, substance abuse, Parkinson-like motor disorders and motion disorders related to the use of neuroleptic agents.
    Type: Grant
    Filed: December 20, 2001
    Date of Patent: November 26, 2002
    Assignee: Neurogen Corporation
    Inventors: Jennifer N. Tran, Andrew Thurkauf
  • Piperidine, tetrahydropyridine and piperazine derivatives, their preparation and use
    Publication number: 20020173512
    Abstract: A piperidine, tetrahydropyridine or piperazine derivative having formula (I), 1
    Type: Application
    Filed: May 16, 2002
    Publication date: November 21, 2002
    Applicant: H. Lundbeck A/S
    Inventors: Ejner Knud Moltzen, Christian Krog-Jensen, Berith Bjornholm
  • Matrix metalloproteinase inhibitors
    Patent number: 6482827
    Abstract: A compound, which is an amine derivative of formula (I) wherein W is —CNHOH or —COOH: R1 and R2 are each hydrogen or an organic residue, R3 is an organic group, Q is a secondary or tertiary acyclic or cyclic amido group, and the pharmaceutically acceptable salts, solvates and hydrates thereof, are inhibitors of matrix metalloproteinases (MMPs) and of the release of tumor necrosis factor-alpha (TNF) from cells. They are therefore useful in the prevention, control and treatment of diseases in which MMPs or TNF are involved, especially tumoral and inflammatory diseases. Processes for their preparation and pharmaceutical compositions containing them are also described.
    Type: Grant
    Filed: March 10, 1999
    Date of Patent: November 19, 2002
    Assignee: Pharmacia & Upjohn S.p.A.
    Inventors: Marco Alpegiani, Pierluigi Bissolino, Francesca Abrate, Ettore Perrone, Riccardo Corigli, Daniela Jabes
  • Substituted chroman derivatives
    Patent number: 6479497
    Abstract: The present invention relates to new new piperidyl or piperazinyl-substituted dihydro-2H-1-benzopyran derivatives compound having the formula (I) wherein X is N or CH; Y is NR2CH2, CH2NR2, NR2CO, CONR2, NR2SO2 or NR2CONR2 wherein R2 is H or C1-C6 alkyl; R1 is H, C1-C6 alkyl or C3-C6 cycloalkyl; R3 is C1-C6 alkyl, C3-C6 cycloalkyl or (CH2)n-aryl, wherein aryl is phenyl or a heteroaromatic ring containing one or two heteroatoms selected from N, O and S and which may be mono- or di-substituted with R4 and/or R5; and n is 0-4; as (R)-enantiomers, (S)-enantiomers or a racemate in the form of a free base or a pharmaceutically acceptable salt or solvate thereof, a process for their preparation, pharmaceutical compositions containing said therapeutically active compounds and to the use of said active compounds.
    Type: Grant
    Filed: October 21, 1998
    Date of Patent: November 12, 2002
    Assignee: Astrazeneca AB
    Inventors: Stefan Berg, Martin Nylöf, Svante Ross, Seth-Olov Thorberg
  • Compositions for the treatment of the catabolic state of prolonged critical illness
    Publication number: 20020160961
    Abstract: Compositions comprising TRH and a compound of the general formula A—B—C—D(—E)p are used for treating the catabolic state of prolonged critical illness.
    Type: Application
    Filed: December 4, 2001
    Publication date: October 31, 2002
    Inventor: Michael Ankersen
  • Synthesis of 3-[4-(2-aminoethoxy)-benzoyl]-2-aryl-6-hydroxybenzo[b]thiophenes
    Patent number: 6472531
    Abstract: The present invention is directed to chemical processes for preparing 2-aryl-6-hydroxy-3-[4-(2-aminoethoxy)benzoyl]benzo[b]-thiophenes. The present invention is also directed to crystalline solvates and a non-solvated crystalline form of 6-hydroxy-2-(4-hydroxyphenyl)-3-[4-(2-piperidinoethoxy)benzoyl]-benzo[b]thiophene hydrochloride, as well as processes for their preparation.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: October 29, 2002
    Assignee: Eli Lilly and Company
    Inventors: Elizabeth Smith LaBell, John McNeill McGill, Randal Scot Miller
  • Nitrogen-containing heterocyclic compounds and therapeutic agents for hyperlipidemia comprising the same
    Publication number: 20020156276
    Abstract: Disclosed are compounds represented by formula (I) and pharmaceutically acceptable salts and solvates thereof. The compounds can inhibit the biosynthesis of triglycerides in the liver and can inhibit the secretion of lipoprotein containing apolipoprotein B from the liver. Therefore, they are useful for the prevention or treatment of hyperlipidemia (particularly hyper-very-low-density-lipoproteinemia) and arteriosclerotic diseases, such as cardiac infarction, or pancreatitis induced by hyperlipidemia.
    Type: Application
    Filed: April 23, 2002
    Publication date: October 24, 2002
    Inventors: Naoto Ohkura, Takashi Tsuruoka, Takayuki Usui, Yukiko Hiraiwa, Tetsuya Matsushima, Masaharu Shiotani, Tetsutaro Niizato, Yuuko Nakatani, Shigeki Suzuki, Chidsuko Kuroda, Kiyoaki Katano
  • Medicament for the alleviation or treatment of symptom derived from the ischemic disease and compound useful thereof
    Patent number: 6469010
    Abstract: A medicine having the following basic structure, for the alleviation or treatment of symptoms derived from ischemic diseases and seizures, epilepsy, and migraine, having a powerful action in suppressing cytotoxic Ca2+ overload and free from side-effects: wherein Z═C, CH, or N, X═O or CH2, E and Y═H, OH, a halogen, alkoxy, alkyl, or a halogen-substituted alkyl.
    Type: Grant
    Filed: March 22, 2000
    Date of Patent: October 22, 2002
    Assignee: Suntory Limited
    Inventors: Hirokazu Annoura, Mayumi Uesugi, Shinsuke Matsuki, Atsuko Fukunaga, Toshio Tatsuoka, Shigeki Tamura, Norio Inomata
  • Benzamide derivatives and their use as cytokine inhibitors
    Patent number: 6455520
    Abstract: The invention concerns amide derivatives of formula (I) wherein R3 is (1-6C)alkyl or halogeno; m is 0-3, p is 0-2 and q is 0-4; each of R1 and R2 is a group such as hydroxy, halogeno, trifluoromethyl and cyano; R4 is a basic group such as amino, (1-6C)alkylamino, di-[(1-6C)alkyl]amino, di-[(1-6C)alkyl]amino-(1-6C)alkyl, di-[(1-6C)alkyl]amino-(2-6C)alkoxy, heteroaryl, heteroaryloxy, heteroaryl-(1-6C)alkoxy, heterocyclyl, heterocyclyloxy and heterocyclyl-(1-6C)alkoxy; and Q2 is a group such as heteroaryl, heteroaryloxy or heteroaryl-(1-6C)alkoxy which is optionally substituted; or pharmaceutically-acceptable salts or in-vivo-cleavable esters thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases or medical conditions mediated by cytokines.
    Type: Grant
    Filed: March 23, 2001
    Date of Patent: September 24, 2002
    Assignee: Astra Zeneca AB
    Inventors: Dearg S Brown, George R Brown
  • Somatostatin antagonists and agonists that act at the sst subtype 2 receptor
    Publication number: 20020128206
    Abstract: Compounds according to the formula: 1
    Type: Application
    Filed: March 7, 2002
    Publication date: September 12, 2002
    Inventors: Bruce A. Hay, Anthony P. Ricketts, Bridget M. Cole
  • &agr;- and &bgr;-amino acid hydroxyethylamino sulfamic acid derivatives useful as retroviral protease inhibitors
    Patent number: 6444678
    Abstract: Certain Alpha- and Beta-amino acid hydroxyethylamino sulfamic acid derivatives represented by the following formula are useful as retroviral protease inhibitors:
    Type: Grant
    Filed: August 4, 2000
    Date of Patent: September 3, 2002
    Assignee: G. D. Searle & Co.
    Inventors: Michael L Vazquez, Richard A Mueller, John J Talley, Daniel P Getman, Gary A DeCrescenzo, Eric T Sun