Hetero Ring Is Six-membered Consisting Of Three Nitrogens And Three Carbon Atoms Patents (Class 514/241)
Asymmetrical (e.g., 1,2,4-triazine, etc.) (Class 514/242)
Hexamethylenetetramines (Class 514/244)
Nitrogen bonded directly to ring carbon of the hetero ring (Class 514/245)
Polycyclo ring system having a 1,3,5-triazine as one of the cyclos (Class 514/246)
  • (R)-Chiral halogenated substituted heteroaryl benzyl aminoalcohol compounds useful for inhibiting cholesteryl ester transfer protein activity
    Patent number: 6677341
    Abstract: The invention relates to substituted aryl and heteroaryl (R)-Chiral Halogenated 1-Substitutedamino-(n+1)-Alkanol 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. Novel high yield, stereoselective processes for the preparation of the chiral substituted alkanol compounds from chiral and achiral intermediates are described. Preferred (R)-Chiral 1-Substitutedamino-(n+1)-Alkanol compounds are substituted (R)-Chiral heteroaryl aminoalcohols.
    Type: Grant
    Filed: December 12, 2001
    Date of Patent: January 13, 2004
    Assignee: Pharmacia Corporation
    Inventors: James A. Sikorski, Richard C. Durley, Margaret L. Grapperhaus, Mark A. Massa, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Brian S. Hickory, Monica B. Norton, William F. Vernier, Deborah A. Mischke, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
  • Substituted N-phenyl-N-heteroaralkyl aminoalcohol compounds useful for inhibiting cholesteryl ester transfer protein activity
    Patent number: 6677353
    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: May 23, 2002
    Date of Patent: January 13, 2004
    Assignee: Pharmacia Corporation
    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
  • Phenylalanine derivatives
    Patent number: 6677339
    Abstract: Phenylalanine derivatives of formula (1) are described: in which: Ar1 is an aromatic or heteroaromatic group; L1 is a linker atom or group; R is a carboxylic acid or a derivative thereof; Ar2 is an optionally substituted aromatic or heteroaromatic group; and the salts, solvates, hydrates and N-oxides thereof. The compounds are able to inhibit the binding of &agr;4 integrins to their ligands and are of use in the prophylaxis and treatment of immune or inflammatory disorders.
    Type: Grant
    Filed: August 10, 2001
    Date of Patent: January 13, 2004
    Assignee: Celltech R & D Limited
    Inventors: John Clifford Head, John Robert Porter, Graham John Warrellow, Sarah Catherine Archibald, Brian Woodside Hutchinson
  • 1,2,4-triazolol[4,3-a][1,3,5]triazine-3,5,7-substituted precursor, and process, and compounds therefrom
    Patent number: 6673924
    Abstract: The present invention includes a precursor compound pertaining to a 1,2,4-Triazolo[4,3-a][1,3,5] Triazine compound, particularly a 1,2,4-Triazolo[4,3-a][1,3,5] Triazine-3,5,7-Triamine, and novel fused ring structures such as triazolyl-tetrazinyl-aminotriazine compounds, and complexes and salts thereof, and other such chemical structures.
    Type: Grant
    Filed: July 10, 2002
    Date of Patent: January 6, 2004
    Assignee: The United States of America as represented by the Secretary of the Navy
    Inventors: William M. Koppes, Michael E. Sitzmann
  • Actinium-225 complexes and conjugates for targeted radiotherapy
    Patent number: 6670456
    Abstract: Actinium-225 complexes comprising functionalized polyazamacrocyclic chelant compounds are disclosed. Such complexes show improved stability and can be conjugated to a biological carrier.
    Type: Grant
    Filed: February 27, 2002
    Date of Patent: December 30, 2003
    Assignee: Dow Global Technologies Inc.
    Inventors: R. Keith Frank, Garry E. Kiefer, Jaime Simon
  • Melanocortin receptor ligands
    Publication number: 20030236230
    Abstract: The present invention relates to compounds which comprise a 4-substituted piperidine ring linked to a substituted or unsubstituted hydrocarbyl ring.
    Type: Application
    Filed: April 9, 2003
    Publication date: December 25, 2003
    Applicant: The Procter & Gamble Company
    Inventors: Frank Hallock Ebetino, Xuewei Liu, Mark Gregory Solinsky, John August Wos
  • Immunosuppressive effects of pteridine derivatives
    Publication number: 20030236255
    Abstract: Novel poly-substituted pteridinediones (lumazines), and mono- or polysubstituted 2-thiolumazines, 4-thiolumazines or 2,4-dithiolumazines, having disclosed substituents in positions 1, 3, 6 and 7 of the pteridine ring, and pharmaceutically acceptable salts thereof, are useful as biologically active ingredients in preparing pharmaceutical compositions especially for the treatment or prevention of a CNS disorder, a cell proliferative disorder, a viral infection, an immune or auto-immune disorder or a transplant rejection. Combinations of the pteridine derivatives of the invention with an immunosuppressant or immunomodulator drug, an antineoplastic drug or an antiviral agent, providing potential synergistic effects, are also disclosed.
    Type: Application
    Filed: May 23, 2003
    Publication date: December 25, 2003
    Inventors: Mark Jozef Albert Waer, Piet Andre Maurits Maria Herdewijn, Wolfgang Eugen Pfleiderer
  • Polycyclic aryl and heteroaryl substituted 4-pyridones useful for selective inhibition of the cogulation cascade
    Publication number: 20030236257
    Abstract: The invention relates to polycyclic aryl and heteroaryl substituted 4-pyridone compounds useful as inhibitors of serine proteases of the coagulation cascade and compounds, compositions and methods for anticoagulant therapy for the treatment and prevention of a variety of thrombotic conditions including coronary artery and cerebrovascular diseases.
    Type: Application
    Filed: January 31, 2003
    Publication date: December 25, 2003
    Inventors: Michael S. South, Chun C. Ma, Kevin J. Koeller, Hayat K. Rahman, William L. Neumann
  • Small molecules useful for the treatment of inflammatory disease
    Publication number: 20030232817
    Abstract: Compounds of the formula I 1
    Type: Application
    Filed: February 24, 2003
    Publication date: December 18, 2003
    Applicant: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventor: Roman Wolfgang Fleck
  • Non-covalent inhibitors of AmpC beta-lactamase
    Publication number: 20030232830
    Abstract: &bgr;-lactamases are the most widespread resistance mechanism to &bgr;-lactam antibiotics, such as penicillins and cephalosporins. In response to these enzymes, inhibitors have been introduced. Unfortunately, these inhibitors are also &bgr;-lactams, and resistance to them has developed rapidly. Consequently, the present invention provides a novel structure-based approach to inhibitors of these enzymes.
    Type: Application
    Filed: February 19, 2003
    Publication date: December 18, 2003
    Inventors: Brian K. Shoichet, Rachel A. Powers
  • Composition including a triamine and a biocide and a method for inhibiting the growth of microorganisms with the same
    Publication number: 20030228373
    Abstract: The present invention is directed to a composition for inhibiting microbial growth, which includes a biocide (other than a triamine) and a triamine. The biocide is an oxidizing biocide, a non-oxidizing biocide, or a combination thereof. This composition is particularly effective at preventing the growth of various microorganisms in aqueous solutions, such as industrial waters. The present invention also relates to a method of controlling the growth of microorganisms in an aqueous composition by adding the composition of the present invention to the solution.
    Type: Application
    Filed: January 22, 2003
    Publication date: December 11, 2003
    Applicants: Lonza Inc., Lonza AG
    Inventors: Michael Ludensky, Christopher Hill, Florian Christof Albrecht Lichtenberg
  • Heteroaromatic substituted cyclopropane as corticotropin releasing hormone ligands
    Publication number: 20030229091
    Abstract: Provided herein are novel heteroaromatic substituted cyclopropanes of the Formula (I): 1
    Type: Application
    Filed: September 5, 2002
    Publication date: December 11, 2003
    Inventors: Andreas Termin, Peter D.J. Grootenhuis, Dean M. Wilson, Valentina Molteni, Long Mao, Angelo Castellino, Zhicai Yang, Anthony Pechulis, Mark Suto
  • N-alkyl-N-phenylhydroxylamine compounds containing metal chelating groups, their preparation and their therapeutic uses
    Publication number: 20030225087
    Abstract: The present invention provides novel N-alkyl-N-phenylhydroxylamine derivatives containing metal chelating groups, a process for preparing the same, the use of the novel compounds as therapeutics for treating and/or preventing various medical dysfunctions and diseases arising from reactive oxygen species (ROS) and/or excess Zn ions, in particular stroke, Parkinson's disease and Alzheimer's disease. The compounds of the invention possess similar or superior LPO inhibition activity to the reference compounds of Trolox and Ebselen. While showing lower toxicity, they also effectively inhibit the cerebral neuronal cell death caused by ROS and/or zinc ion, and show neuroprotective effects against ischemic neuronal degeneration.
    Type: Application
    Filed: June 5, 2003
    Publication date: December 4, 2003
    Inventors: Eu-Gene Oh, Sung-Bo Ko, Won-Yeob Kim, Kyung-Hwa Kim, Dennis W. Choi, Laura L. Dugan, Tae-Cheon Kang, Jae-Young Koh, Kyung-Mi Kim, In-Jae Shin
  • Polycyclic aryl and heteroaryl substituted 1,4-quinones useful for selective inhibition of the coagulation cascade
    Publication number: 20030225086
    Abstract: The invention relates to polycyclic aryl and heteroaryl substituted 1,4-quinone compounds useful as inhibitors of serine proteases of the coagulation cascade and compounds, compositions and methods for anticoagulant therapy for the treatment and prevention of a variety of thrombotic conditions including coronary artery and cerebrovascular diseases.
    Type: Application
    Filed: February 19, 2003
    Publication date: December 4, 2003
    Inventors: Michael S. South, John J. Parlow
  • Pyridazinones and triazinones and medicinal use thereof
    Publication number: 20030225081
    Abstract: The present invention provides a novel compound exhibiting an excellent inhibitory action on AMPA receptor and/or kainate receptor. That is, it provides a compound represented by the following formula, a salt thereof or a hydrate of them.
    Type: Application
    Filed: March 18, 2003
    Publication date: December 4, 2003
    Inventors: Satoshi Nagato, Koki Kawano, Koichi Ito, Yoshihiko Norimine, Koshi Ueno, Takahisa Hanada, Hiroyuki Amino, Makoto Ogo, Shinji Hatakeyama, Masataka Ueno, Anthony John Groom, Leanne Rivers, Terence Smith
  • Use of interleukin-19 to treat ovarian cancer
    Publication number: 20030223958
    Abstract: The present invention relates to the anti-cancer activity of IL-19 polypeptide molecules. IL-19 is a cytokine involved in inflammatory processes and human disease. The present invention includes Use of IL-19 for decreasing proliferation of ovarian cancer cells, treating ovarian cancer, amongst other uses disclosed. IL-19 polypeptides can be administered alone, or can be fused to cytotoxic moieties, and can be administered in conjunction with radiation or chemotherapeutic agents.
    Type: Application
    Filed: April 8, 2003
    Publication date: December 4, 2003
    Inventors: Yasmin A. Chandrasekher, Patricia A. McKernan
  • Compositions useful as inhibitors of protein kinases
    Publication number: 20030225073
    Abstract: The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.
    Type: Application
    Filed: March 14, 2003
    Publication date: December 4, 2003
    Inventors: David Bebbington, Hayley Binch, Jean-Damien Charrier, Simon Everitt, Julian M.C. Golec, David Kay, Ronald Knegtel, Andrew Miller, Francoise Pierard, Albert C. Pierce
  • 8-aza-bicyclo[3.2.1]octan-3-ol derivatives of 2,3-dihydro-1,4-benzodioxan as 5-HT1A antagonists
    Patent number: 6656951
    Abstract: Compounds of the formula: are useful for treating the cognitive deficits due to aging, stroke, head trauma, Alzheimer's disease or other neurodegenerative diseases, or schizophrenia and also treatment of disorders related to excessive serotonergic stimulation, such as anxiety, aggression and stress, and for the control of various physiological phenomena, such as appetite, thermoregulation, sleep and sexual behavior, which are known to be, at least in part, under serotonergic influence.
    Type: Grant
    Filed: April 23, 2002
    Date of Patent: December 2, 2003
    Assignee: Wyeth
    Inventors: Adam M. Gilbert, Gary P. Stack
  • Pyrrolo [3,4-d] pyrimidines as corticotropin releasing factor (CRF) antagonists
    Publication number: 20030220333
    Abstract: Corticotropin releasing factor (CRF) antagonists of Formula (II) 1
    Type: Application
    Filed: June 9, 2003
    Publication date: November 27, 2003
    Inventor: Rajagopal Bakthavatchalam
  • Seleno compounds containing nitrone moiety, their preparation and their therapeutic uses
    Publication number: 20030220337
    Abstract: The present invention provides novel seleno compounds containing nitrone moiety, a process for preparing the same, the use of the novel compounds as therapeutics for treating and/or preventing various medical dysfunctions and diseases arising from reactive oxygen species, in particular stroke, Parkinson's disease, Alzheimer's disease. The compounds of the invention have similar or superior lipid peroxidation (LPO) inhibition activity to the reference compounds. While showing lower toxicity and better water solubility, they also effectively inhibit the cerebral neuronal cell death caused by ROS and show neuroprotective effects against ischemic neuronal degeneration.
    Type: Application
    Filed: June 6, 2003
    Publication date: November 27, 2003
    Inventors: Sung-Bo Ko, Eu-Gene Oh, Eon-Kyeom Kim, Won-Yeob Kim, Dennis W. Choi, Laura L. Dugan, Jae-Young Koh, Moo-Ho Won, Myung-Bok Wie
  • Use of interleukin-24 to treat ovarian cancer
    Publication number: 20030215388
    Abstract: The present invention relates to the anti-cancer activity of IL-24 polypeptide molecules. IL-24 is a cytokine involved in inflammatory processes and human disease. The present invention includes Use of IL-24 for decreasing proliferation of ovarian cancer cells, treating ovarian cancer, amongst other uses disclosed. IL-24 polypeptides can be administered alone, or can be fused to cytotoxic moieties, and can be administered in conjunction with radiation or chemotherapeutic agents.
    Type: Application
    Filed: April 8, 2003
    Publication date: November 20, 2003
    Inventors: Yasmin A. Chandrasekher, Patricia A. McKernan
  • Method for preventing tissue injury from hypoxia
    Publication number: 20030216414
    Abstract: There is disclosed a method for preventing tissue injury caused by tissue hypoxia and reoxygenation, comprising administering a compound that inhibits signal transduction by inhibiting cellular accumulation of linoleoyl phosphatidic acid (PA) through an inhibition of the enzyme LPAAT (lysophosphatidic acyltransferase).
    Type: Application
    Filed: May 9, 2003
    Publication date: November 20, 2003
    Applicant: Cell Therapeutics,Inc.
    Inventors: Stuart L. Bursten, Jack W. Singer, Glenn C. Rice
  • Etylene derivatives and pesticides containing said derivatives
    Publication number: 20030216394
    Abstract: Ethylene derivatives of formula (I): 1
    Type: Application
    Filed: August 8, 2002
    Publication date: November 20, 2003
    Applicant: Nissan Chemical Industries, Ltd.
    Inventors: Tomoyuki Ogura, Hiroshi Murakami, Akira Numata, Rika Miyachi, Toshiro Miyake, Norihiko Mimori, Shinji Takii
  • Method of treating colonic adenomas
    Patent number: 6649649
    Abstract: This invention is directed to a method of retarding or preventing the transformation of a colonic adenoma to a colonic adenocarcinoma comprising the administration to a patient with FAP or a patient with one or more of said adenomas a non-toxic therapeutically effective amount of NSAID, said amount effective to inhibit the PGHS-2 in said adenoma. The preferred method comprises the administration of a specific PGHS-2 inhibiting agent as defined herein.
    Type: Grant
    Filed: March 2, 1999
    Date of Patent: November 18, 2003
    Assignees: Merck & Co., Inc., Merck Frosst Canada, & Co.
    Inventors: Stacia Kargman, Thomas J. Simon, Jilly Evans
  • Pharmaceutically active pyrrolidine derivatives
    Publication number: 20030212012
    Abstract: The present invention is related to pyrrolidine derivatives of formula (I).
    Type: Application
    Filed: February 10, 2003
    Publication date: November 13, 2003
    Inventors: Serge Halazy, Anna Quattropani, Alexander Scheer, Mattias Schwarz, Russell Thomas, Antony Baxter
  • Aminoalkyl-substituted aromatic bicyclic compounds, methods for their preparation and their use as pharmaceuticals
    Publication number: 20030212070
    Abstract: The present invention relates to aminoalkyl-substituted aromatic bicyclic compounds of formula I, 1
    Type: Application
    Filed: August 14, 2002
    Publication date: November 13, 2003
    Inventors: Lothar Schwink, Siegfried Stengelin, Matthias Gossel
  • Thiazolyl urea compounds and methods of uses
    Patent number: 6645990
    Abstract: Selected novel urea compounds are effective for prophylaxis and treatment of diseases, such as cell proliferation or apoptosis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving stoke, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
    Type: Grant
    Filed: February 15, 2002
    Date of Patent: November 11, 2003
    Assignee: Amgen Inc.
    Inventors: Benny C. Askew, Frenel F. De Morin, Andrew Hague, Ellen Laber, Aiwen Li, Gang Liu, Patricia Lopez, Rana Nomak, Vincent Santora, Christopher Tegley, Kevin Yang
  • Inhibitors of Src and other protein kinases
    Publication number: 20030207873
    Abstract: The present invention provides compounds of formula I: 1
    Type: Application
    Filed: April 10, 2002
    Publication date: November 6, 2003
    Inventor: Edmund Harrington
  • Aromatic heterocyclic non-covalent inhibitors of urokinase and blood vessel formation
    Publication number: 20030207842
    Abstract: Novel compounds having activity as non-covalent inhibitors of urokinase and having activity in reducing or inhibiting blood vessel formation are provided. These compounds have at a group having a guanidino moiety or derivative thereof. These compounds are useful in vitro for monitoring plasminogen activator levels and in vivo in treatment of conditions which are ameliorated by inhibition of or decreased activity of urokinase and in treating pathologic conditions wherein blood vessel formation is related to a pathologic condition.
    Type: Application
    Filed: December 4, 2002
    Publication date: November 6, 2003
    Inventors: Amir P. Tamiz, L. Josue Alfaro-Lopez, Odile Esther Levy, Joseph Edward Semple
  • Imidazopyrimidines and imidazopyridines for the treatment of neurological disorders
    Patent number: 6642230
    Abstract: Corticotropin releasing factor (CRF) antagonists of formula (I): and their use in treating psychiatric disorders and neurological diseases, anxiety-related disorders, post-traumatic stress disorder, supranuclear palsy and feeding disorders as well as treatment of immunological, cardiovascular or heart-related diseases and colonic hypersensitivity associated with psychopathological disturbance and stress in mammals.
    Type: Grant
    Filed: November 7, 2001
    Date of Patent: November 4, 2003
    Assignee: Bristol-Myers Squibb Pharma Company
    Inventors: Richard Gerald Wilde, Rajagopal Bakthavatchalam, James Peter Beck, Argyrios Georgious Arvanitis
  • Novel pyrazinone derivatives
    Publication number: 20030203907
    Abstract: The present invention relates to a compound of the general formula (I): 1
    Type: Application
    Filed: January 31, 2003
    Publication date: October 30, 2003
    Inventors: Takashi Hayama, Nobuhiko Kawanishi, Tooru Takaki
  • Preparation of thioarabinofuranosyl compounds and use thereof
    Publication number: 20030203872
    Abstract: Patients suffering from cancer are treated by being administered a compound represented by the following formula: 1
    Type: Application
    Filed: April 7, 2003
    Publication date: October 30, 2003
    Inventors: John A. Secrist, Kamal N. Tiwari, John A. Montgomery
  • 2,4-disubstituted triazine derivatives
    Patent number: 6638932
    Abstract: This invention concerns the use of the compounds of formula the N-oxides, the pharmaceutically acceptable addition salts, quaternary amines and the stereochemically isomeric forms thereof, wherein —a1═a2—a3═a4— forms a phenyl, pyridinyl, pyrimidinyl, pyridazinyl or pyrazinyl with the attached vinyl group; n is 0 to 4; and where possible 5; R1 is hydrogen, aryl, formyl, C1-6alkylcarbonyl, C1-6alkyl, C1-6alkyloxycarbonyl or substituted C1-6alkyl; each R2 independently is hydroxy, halo, optionally substituted C1-6alkyl, C2-6alkenyl or C2-6alkynyl, C3-7cycloalkyl, C1-6alkyloxy, C1-6alkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono- or di(C1-6alkyl)amino, polyhalomethyl, polyhalomethyloxy, polyhalomethylthio, —S(═O)pR4, —NH—S(═O)pR4, —C(═O)R4, —NHC(═O)H, —C(═O)NHNH2, —NHC(═O)R4, —C(═NH)R4 or a 5-membered heterocyclic ring; p is 1 or 2; L is optionally substituted C1-10alkyl, C2-10alk
    Type: Grant
    Filed: August 2, 2001
    Date of Patent: October 28, 2003
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Bart De Corte, Marc René de Jonge, Jan Heeres, Paul Adriaan Jan Janssen, Robert W. Kavash, Lucien Maria Henricus Koymans, Michael Joseph Kukla, Donald William Ludovici, Koen Jeanne Alfons Van Aken
  • Small molecule inhibitors targeted at BCL-2
    Publication number: 20030199489
    Abstract: The present invention relates to small molecule antagonists of Bcl-2 family proteins such as Bcl-2 and/or Bcl-XL. In particular, the present invention provides non-peptide cell permeable small molecules (e.g., tricyclo-dibenzo-diazocine-dioxides) that bind to a pocket in Bcl-2/Bcl-XL that block the anti-apoptotic function of these proteins in cancer cells and tumor tissues exhibiting Bcl-2 protein overexpression. In preferred embodiments, the small molecules of the present invention are active at the BH3 binding pocket of Bcl-2 family proteins (e.g., Bcl-2, Bcl-XL, and Mcl-1). The compositions and methods of the present invention are useful therapeutics for cancerous diseases either alone or in combination with chemotherapeutic or other drugs.
    Type: Application
    Filed: November 1, 2002
    Publication date: October 23, 2003
    Applicant: The Regents of the University of Michigan
    Inventor: Shaomeng Wang
  • Heterocyclic derivatives
    Publication number: 20030195203
    Abstract: The invention relates to heterocyclic derivatives of formula (I)
    Type: Application
    Filed: September 27, 2001
    Publication date: October 16, 2003
    Inventors: Andrew Stocker, John Preston, John Wall Rayner, Michael James Smithers, Paul Turner
  • Compounds, compositions and methods for treating or preventing viral infections and associated diseases
    Publication number: 20030195213
    Abstract: Compounds, compositions and methods are provided for the treatment and prophylaxis of infections and associated diseases caused by viruses of the Flaviviridae family by administering certain rhodanine derivatives, and analogs thereof, tri- and tetracyclic rhodanine alkanoic acids and rhodanine benzoic acids being particularly effective.
    Type: Application
    Filed: February 14, 2003
    Publication date: October 16, 2003
    Inventors: Thomas R. Bailey, Dorothy C. Young
  • Vanilloid receptor ligands and their use in treatments
    Publication number: 20030195201
    Abstract: Compounds having the general structure 1
    Type: Application
    Filed: December 10, 2002
    Publication date: October 16, 2003
    Inventors: Yunxin Y. Bo, Partha P. Chakrabarti, Ning Chen, Elizabeth M. Doherty, Christopher H. Fotsch, Nianhe Han, Michael G. Kelly, Qingyian Liu, Mark Henry Norman, Vassil I. Ognyanov, Xianghong Wang, Jiawang Zhu
  • 1,2,4-triazolo[4,3-a][1,3,5]triazine-3,5,7-substituted precursor, and process, and compounds therefrom
    Patent number: 6632305
    Abstract: The present invention includes a precursor compound pertaining to a 1,2,4-Triazolo[4,3-a][1,3,5]Triazine compound, particularly a 1,2,4-Triazolo[4,3-a][1,3,5]Triazine-3,5,7-Triamine, and novel fused ring structures such as triazolyl-tetrazinyl-aminotriazine compounds, and complexes and salts thereof, and other such chemical structures.
    Type: Grant
    Filed: June 14, 2002
    Date of Patent: October 14, 2003
    Assignee: The United States of America as represented by the Secretary of the Navy
    Inventors: William M. Koppes, Michael E. Sitzmann
  • Fluoromethoximino compounds
    Patent number: 6632817
    Abstract: The invention relates to novel fluoromethoximino compounds, to a process for their preparation and to their use as pesticides, and also to novel intermediates and to a plurality of processes for their preparation.
    Type: Grant
    Filed: August 20, 2001
    Date of Patent: October 14, 2003
    Inventors: Ulrich Heinemann, Herbert Gayer, Peter Gerdes, Albrecht Marhold, Uwe Stelzer, Reinhard Lantzsch, Ralf Tiemann, Klaus Stenzel, Astrid Mauler-Machnik, Stefan Dutzmann, Martin Kugler, Hans-Ulrich Buschhaus
  • Serotonin reuptake inhibitor
    Publication number: 20030191126
    Abstract: A serotonin reuptake inhibitor containing a cyclic amine represented by the following formula, a prodrug thereof, or a pharmaceutically acceptable salt of said cyclic amine or prodrug as an active ingredient: 1
    Type: Application
    Filed: January 17, 2003
    Publication date: October 9, 2003
    Applicant: SUMITOMO PHARMACEUTICALS COMPANY LIMITED
    Inventors: Toru Kodo, Shuji Masumoto, Koji Koyama, Naoya Kinomura
  • Modulators of the cholesterol biosynthetic pathway
    Publication number: 20030191110
    Abstract: The present invention relates to methods for modulating the cholesterol biosynthetic pathway. The level of cholesterol in the body is linked to numerous pathological states. The methods of the present invention alter the transcription levels of genes involved in the cholesterol biosynthesis. The methods of the present invention can used for treating diseases mediated by the cholesterol biosynthetic pathway.
    Type: Application
    Filed: November 1, 2002
    Publication date: October 9, 2003
    Inventors: Martyn Botfield, Fiona McDonald, Joern Kraetzschmar, Bernhard Lindenthal, Bertold Kreft
  • C12-cyano epothilone derivatives
    Publication number: 20030186965
    Abstract: The present invention relates to compounds useful in the treatment of cancer or other proliferative diseases represented by the formula 1
    Type: Application
    Filed: March 11, 2003
    Publication date: October 2, 2003
    Inventors: Gregory D. Vite, Alicia Regueiro-Ren
  • 3-(Diarylmethylene)-8-azabicyclo[3.2.1]octane derivatives
    Publication number: 20030181447
    Abstract: This invention is directed to 3-(diarylmethylene)-8-azabicyclo[3.2.1]octane derivatives useful as &dgr;-opioid or &mgr;-opioid receptor modulators. Depending on their agonist or antagonist effect, the compounds are useful analgesics, immunosuppressants, antiinflammatory agents, agents for the treatment of neurological and psychiatric conditions, medicaments for drug and alcohol abuse, agents for treating gastritis and diarrhea, cardiovascular agents and agents for the treatment of respiratory diseases.
    Type: Application
    Filed: February 7, 2003
    Publication date: September 25, 2003
    Inventors: Robert E. Boyd, John R. Carson, Steven J. Coats, Lou Anne Neilson, Philip M. Pitis, Wu-Nan Wu
  • Use of triazinetrione sulfoxides for controlling coccidioses
    Publication number: 20030181451
    Abstract: The present invention relates to the use of specific derivatives of triazinetriones for controlling coccidioses in livestock, especially pigs.
    Type: Application
    Filed: February 18, 2003
    Publication date: September 25, 2003
    Inventors: Gisela Greif, Hans-Christian Mundt, Iris Heep
  • Pyridazines as interleukin-1&bgr; converting enzyme inhibitors
    Patent number: 6624166
    Abstract: Disclosed are compounds of the formula (I) and pharmaceutically acceptable salts thereof: wherein R1 is a halogen, or an oxygen linked leaving group including an aromatic ether, an alkyl sulfonate, an aryl sulfonate, an alkyl phosphonate, an aryl phosphonate, an alkyl phosphate or aryl phosphate; R2 is COOR5, C(═O)NH(CHR5)m—COOR5, NH(CHR5)mCON(R5)R6, C(═O)N(R5)R6 or NH(CHR5)mOH; R3 is H or alkyl; R4 is H, sybstituted or unsubstituted aryl, heteroaryl or alkyl; R5 and R6 are independently H, lower alkyl, aryl, hydroxy alkyl, amino alkyl, heteroaryl, lower alkylene-aryl, lower alkylene-heteroaryl or lower cycloalkyl; and m=0-6; pharmaceutical compositions containing the compounds; and a method for inhibiting interleukin-1&bgr; protease activity in a mammal utilizing the compounds and compositions.
    Type: Grant
    Filed: April 3, 1996
    Date of Patent: September 23, 2003
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Roland E. Dolle, Denton W. Hoyer, Tina Morgan Ross, James M. Rinker, Stanley J. Schmidt, Mark A. Ator
  • Pharmaceutically active pyrrolidine derivatives as bax inhibitors
    Publication number: 20030171309
    Abstract: The present invention is related to new substituted pyrrolidine derivatives of formula (I). Said compounds are preferably for use as pharmaceutically active compounds. Specifically, pyrrolidine derivatives of formula (I) are useful in the treatment and/or prevention of neurodegenerative disorders, diseases associated with polygultamine tracts, epilepsy, ischemia, infertility, cardiovascular disorders renal hypoxia, hepatitis and AIDS. Said pyrrolidine derivatives display a modulatory and most notably a down-regulating-up to an inhibitory-activity with respect to the cellular death agonist Bax and/or the activation pathways leading to Bax and allows therefore to block the release of cytochrome (c).
    Type: Application
    Filed: April 28, 2003
    Publication date: September 11, 2003
    Inventors: Serge Halazy, Anna Quattropani, Agnes Bombrun, Mattias Schwarz, Russel Thomas, Anthony Baxter
  • HIV replication inhibitors
    Publication number: 20030171374
    Abstract: This invention concerns HIV replication inhibitors of formula 1
    Type: Application
    Filed: November 8, 2002
    Publication date: September 11, 2003
    Inventors: Michael Joseph Kukla, Donald William Ludovici, Robert William Kavash, Bart Lieven Daniel De Corte, Jan Heeres, Paul Adriaan Jan Janssen, Lucien Maria Henricus Koymans, Marc Rene de Jonge, Koen Jeanne Alfons Van Aken, Alain Krief, Ruben Gerardus George Leenders
  • Biphenyl derivatives, production thereof and uses as medicines
    Patent number: 6617325
    Abstract: The present invention relates to biphenyl derivatives of general formula wherein Ra to Rg and n are defined as in claim 1, the isomers and salts thereof, particularly the physiologically acceptable salts thereof, which are valuable inhibitors of the microsomal triglyceride-transfer protein (MTP), medicaments containing these compounds and their use, as well as the preparation thereof.
    Type: Grant
    Filed: May 15, 2002
    Date of Patent: September 9, 2003
    Assignee: Boehringer Ingelheim Pharma KG
    Inventors: Thorsten Lehmann-Lintz, Armin Heckel, Leo Thomas, Michael Mark
  • Compounds and uses thereof for decreasing activity of hormone-sensitive lipase
    Publication number: 20030166644
    Abstract: Use of compounds to inhibit hormone-sensitive lipase, pharmaceutical compositions comprising the compounds, methods of treatment employing these compounds and compositions, and novel compounds. The present compounds are inhibitors of hormone-sensitive lipase and may be useful in the treatment and/or prevention of medical disorders where a decreased activity of hormone-sensitive lipase is desirable.
    Type: Application
    Filed: December 13, 2002
    Publication date: September 4, 2003
    Inventors: Soren Ebdrup, Johannes Cornelis de Jong, Poul Jacobsen, Holger Claus Hansen, Per Vedso
  • Fungicides
    Patent number: 6613773
    Abstract: The invention provides fungicidal compounds of formula (I) or stereoisomers thereof: wherein X is CH2O; A is hydrogen; E is hydrogen; q is 1; any two of K, L and M are nitrogen and the other is CH; T is oxygen or sulfur; and Z is an optionally substituted phenyl group or an optionally substituted heterocyclyl group.
    Type: Grant
    Filed: March 5, 2002
    Date of Patent: September 2, 2003
    Assignee: Syngenta Limited
    Inventors: John Martin Clough, Christopher Richard Ayles Godfrey, Ian Thomas Streeting, Rex Cheetham, Paul John de Fraine, David Bartholomew, James John Eshelby