Additional Hetero Ring, Which Is Attached Directly Or Indirectly To The Five-membered Hetero Ring By Nonionic Bonding Patents (Class 548/517)
The additional hetero ring also contains nitrogen (Class 548/518)
Polycyclo ring system which includes ring chalcogen (Class 548/525)
Sulfur containing hetero ring (Class 548/527)
  • Process for the preparation of pyrrolidinyl ethylamine compounds via a copper-mediated aryl amination
    Publication number: 20040152896
    Abstract: The invention provides a new process for the preparation of compounds of formula (XI): 1
    Type: Application
    Filed: October 31, 2003
    Publication date: August 5, 2004
    Inventors: Stephane Caron, Arun Ghosh, Janice Ethel Sieser
  • Optically active fluorine-containing compounds and processes for their production
    Publication number: 20040147756
    Abstract: An optically active fluorine-containing compound represented by the following formula (1): 1
    Type: Application
    Filed: November 25, 2003
    Publication date: July 29, 2004
    Inventors: Takuya Miyata, Toshio Naka, Takumi Kagawa
  • Substituted pyrroles as kinase inhibitors
    Publication number: 20040138269
    Abstract: The present invention relates to certain substituted pyrroles which modulate the activity of protein kinases (“PKs”). The compounds of this invention are therefore useful in treating disorders related to abnormal PK activity. Pharmaceutical compositions comprising these compounds, methods of treating diseases utilizing pharmaceutical compositions comprising these compounds and methods of preparing them are also disclosed.
    Type: Application
    Filed: October 7, 2003
    Publication date: July 15, 2004
    Applicant: Sugen, Inc.
    Inventors: Connie Li Sun, Peng Cho Tang, Denise Ockey
  • Modulation of anxiety through blockade of anandamide hydrolysis
    Publication number: 20040127518
    Abstract: Fatty acid amide hydrolase inhibitors of the Formula: 1
    Type: Application
    Filed: October 7, 2003
    Publication date: July 1, 2004
    Applicant: The Regents of the University of California
    Inventors: Daniele Piomelli, Andrea Duranti, Andrea Tontini, Marco Mor, Giorgio Tarzia
  • Pharmaceutical compositions as inhibitors of dipeptidyl peptidase-IV (DPP-IV)
    Publication number: 20040121964
    Abstract: The present invention relates to compounds which inhibit dipeptidyl peptidase IV (DPP-IV) and are useful for the prevention or treatment of diabetes, especially type II diabetes, as well as hyperglycemia, Syndrome X, hyperinsulinemia, obesity, atherosclerosis, and various immunomodulatory diseases.
    Type: Application
    Filed: September 11, 2003
    Publication date: June 24, 2004
    Inventors: David J. Madar, Stevan W. Djuric, Melissa J. Feenstra, Hana A. Kopecka, Xiaofeng Li, Kenton L. Longenecker, ZhongHua Pei, Daisy Pireh, Hing L. Sham, Kent D. Stewart, Bruce G. Szczepankiewicz, Paul E. Wiedeman, Hong Yong
  • Alkynyl containing hydroxamic acid compounds as matrix metalloproteinase/tace inhibitors
    Patent number: 6753337
    Abstract: Compounds of the formula: useful in the treatment of arthritis, tumor metastasis, tissue ulceration, abnormal wound healing, periodontal disease, bone disease, diabetes (insulin resistance) and HIV infection.
    Type: Grant
    Filed: December 21, 2001
    Date of Patent: June 22, 2004
    Assignee: Wyeth Holdings Corporation
    Inventors: Jeremy I. Levin, Aranapakam M. Venkatesan, James M. Chen, Arie Zask, Vincent P. Sandanayaka, Mila T. Du, Jannie L. Baker
  • Compounds, compositions, and methods
    Publication number: 20040116400
    Abstract: Compounds useful for treating cellular proliferative diseases and disorders by modulating the activity of KSP are disclosed.
    Type: Application
    Filed: July 17, 2003
    Publication date: June 17, 2004
    Applicants: CYTOKINETICS, INC., SMITHKLINE BEECHAM CORPORATION
    Inventors: Andrew McDonald, Gustave Bergnes, David J. Morgans, Dashyant Dhanak, Steven David Knight
  • 2-Heteroaryl-3,4-dihydro-2h-pyrrole derivatives and the use thereof as pesticides
    Publication number: 20040116477
    Abstract: Novel &Dgr;1-pyrrolines of the formula (I) 1
    Type: Application
    Filed: January 12, 2004
    Publication date: June 17, 2004
    Inventors: Andrew Plant, R?uuml;diger Fischer, Thomas Seitz, Christoph Erdelen, Andreas Turberg, Olaf Hansen
  • Couplers for use in oxidative hair dyeing
    Patent number: 6750337
    Abstract: Couplers for hair coloring compositions for oxidative dyeing of hair are compounds of the formula (1): wherein X is selected from halogen and R5SO4 where the halogen is preferably Cl, Br or I; R, R1 and R2 are each individually selected from C1 to C22 alkyl and C1 to C22 mono or dihydroxyalkyl, or two of R, R1 and R2 together with the nitrogen atom to which they are attached form a C3 to C6 saturated or unsaturated ring optionally containing in the ring one or more additional hetero atoms selected from O, S and N atoms; R3 and R 4 are each individually selected from C1 to C6 alkyl, C1 to C6 hydroxyalkyl, C1 to C6 alkoxy, C1 to C6 aminoalkyl or R3 and R4 together form a C1 to C5 alkylene group; and R5 is selected from C1 to C22 alkyl and C1 to C22 mono or dihydroxyalkyl.
    Type: Grant
    Filed: January 18, 2002
    Date of Patent: June 15, 2004
    Assignee: The Procter & Gamble Company
    Inventors: Mu-Ill Lim, Yuh-Guo Pan, Gottfried Wenke
  • Pyrrolecarboxamides and pyrrolethioamides as fungicides
    Publication number: 20040106521
    Abstract: Novel pyrrole derivatives of formula I 1
    Type: Application
    Filed: October 7, 2003
    Publication date: June 3, 2004
    Applicant: Syngenta Crop Protection, Inc.
    Inventors: Harald Walter, Hermann Schneider
  • Novel compounds and therapeutic uses thereof
    Publication number: 20040106802
    Abstract: The invention discloses a novel series of compound represented by general formula (I), 1
    Type: Application
    Filed: November 26, 2003
    Publication date: June 3, 2004
    Applicant: TORRENT PHARMACEUTICALS LTD.
    Inventor: Alangudi Sankaranarayanan
  • Substituted pyrrole derivatives
    Publication number: 20040102511
    Abstract: The present invention relates to substituted pyrrole derivatives, which can be used as 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase inhibitors. Compounds disclosed herein can function as cholesterol lowering agents and can be used for the treatment of cholesterol-related diseases and related symptoms. Processes for the preparation of disclosed compounds are provided, as well as, pharmaceutical compositions containing the disclosed compounds, and methods of treating cholesterol-related diseases and related symptoms.
    Type: Application
    Filed: May 5, 2003
    Publication date: May 27, 2004
    Inventors: Jitendra Sattigeri, Mohammad Salman, Sachin Sethi, Shobhanna Rawat, Yatendra Kumar
  • Thrombin inhibitors
    Patent number: 6740647
    Abstract: Novel five-membered heterocyclic amidines, their preparation and use as competitive inhibitors of trypsin-like serine proteases, especially thrombin and kininogenases such as kallikrein. Pharmaceutical compositions which contain the compounds as active ingredients, and use of the compounds as thrombin inhibitors, anticoagulants and antiinflammatory agents.
    Type: Grant
    Filed: June 21, 2000
    Date of Patent: May 25, 2004
    Assignee: Abbott GmbH & Co., KG
    Inventors: Dorit Baucke, Udo Lange, Helmut Mack, Werner Seitz, Hans Wolfgang Höffken, Wilfried Hornberger
  • Aromatic sulfonyl alpha-cycloamino hydroxamic acid compounds
    Publication number: 20040097487
    Abstract: An aromatic sulfonyl alpha-cycloamino hydroxamic acid compound that inter alia inhibits matrix metalloprotease activity is disclosed as are a treatment process that comprises administering a contemplated aromatic sulfonyl alpha-cycloamino hydroxamic acid compound in a MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity.
    Type: Application
    Filed: October 27, 2003
    Publication date: May 20, 2004
    Applicant: G.D. Searle & Co.
    Inventors: Hui Li, Daniel P. Becker, Clara I. Villamil, Terri L. Boehm, Daniel P. Getman, Joseph J. McDonald, Gary A. DeCrescenzo
  • Heteroaryl-hexanoic acid amide derivatives as immonomodulatory agents
    Publication number: 20040097554
    Abstract: The present invention relates to compounds of the formula (I) 1
    Type: Application
    Filed: October 16, 2003
    Publication date: May 20, 2004
    Applicant: Pfizer Inc
    Inventors: Matthew F. Brown, Anderson S. Gaweco, Ronald P. Gladue, John C. Kath, Christopher S. Poss
  • Hetaryl substituted homotetramic and homtetronic acids and the use thereof as pesticides
    Publication number: 20040097558
    Abstract: The present invention relates to new hetaryl-substituted homotetramic and homotetronic acids of the formula (I) 1
    Type: Application
    Filed: November 24, 2003
    Publication date: May 20, 2004
    Inventors: Reiner Fischer, Astrid Ullmann, Axel Trautwein, Mark Wilhelm Drewes, Christoph Erdelen, Peter Dahmen, Dieter Feucht, Rolf Pontzen, Peter Losel
  • 3-oxa-8-azaprostaglandin analogs as agents for lowering intraocular pressure
    Patent number: 6734206
    Abstract: The present invention provides a method of treating ocular hypertension or glaucoma which comprises administering to an animal having ocular hypertension or glaucoma therapeutically effective amount of a compound represented by the general formula I; wherein X, Y, Z, D and R3 are as defined in the specification.
    Type: Grant
    Filed: June 2, 2003
    Date of Patent: May 11, 2004
    Assignee: Allergan, Inc.
    Inventors: David W. Old, Thang D. Dinh, Robert M. Burk
  • Pharmaceutically active sulfonamide derivatives bearing both lipophilic and ionisable moietties as inhibitors of protein junkinases
    Publication number: 20040077854
    Abstract: The present invention is related to sulfonamide derivatives having a lipophilic moiety and which are substantially soluble. Said compounds are notably for use as pharmaceutically active compounds. The present invention also related to pharmaceutical formulations containing such sulfonamide derivatives. Said sulfonamide derivatives are efficient modulators of the JNK pathway, they are in particular efficient and selective inhibitors of JNK 2 and 3. The present invention is furthermore related to novel sulfonamide derivatives as well as to methods of their preparation.
    Type: Application
    Filed: October 10, 2003
    Publication date: April 22, 2004
    Inventors: Serge Halazy, Dennis Church, Stephen J. Arkinstall, Marco Biamonte, Montserrat Camps, Jean-Pierre Gotteland, Thomas Rueckle
  • Pyrrole based inhibitors of glycogen synthase kinase 3
    Publication number: 20040077707
    Abstract: New pyrrole based compounds, compositions and methods of inhibiting the activity of glycogen synthase kinase (GSK3) in vitro and of treatment of GSK3 mediated disorders in vivo are provided. The methods, compounds and compositions of the invention may be employed alone, or in combination with other pharmacologically active agents in the treatment of disorders mediated by GSK3 activity, such as diabetes, Alzheimer's disease and other neurodegenerative disorders, obesity, atherosclerotic cardiovascular disease, essential hypertension, polycystic ovary syndrome, syndrome X, ischemia, traumatic brain injury, bipolar disorder, immunodeficiency or cancer.
    Type: Application
    Filed: August 21, 2003
    Publication date: April 22, 2004
    Inventors: Manoj C. Desai, Simon Ng, Zhi-Jie Ni, Keith B. Pfister, Savithri Ramurthy, Sharadah Subramanian, Allan S. Wagman
  • Peptide deformylase inhibitors
    Publication number: 20040077856
    Abstract: PDF inhibitors and novel methods for their use are provided.
    Type: Application
    Filed: August 29, 2003
    Publication date: April 22, 2004
    Inventors: Jia-Ning Xiang, Siegfried B. Christensen IV, Xiangmin Liao, Maxwell D. Cummings
  • Methods of labelling polynucleotides with dibenzorhodamine dyes
    Publication number: 20040072209
    Abstract: Dibenzorhodamine compounds having the structure 1
    Type: Application
    Filed: May 20, 2003
    Publication date: April 15, 2004
    Applicant: Applera Corporation
    Inventors: Scott C. Benson, Joe Y.L. Lam, Steven Micheal Menchen
  • Substituted propane-1,3-diamine derivatives and the pharmaceutical use thereof
    Publication number: 20040067928
    Abstract: Substituted propane-1,3-diamine derivatives, methods for producing such derivatives, and medicaments and pharmaceutical compositions containing such derivatives useful for the treatment or prophylaxis of pain, urinary incontinence, itching, tinitus aurium, or diarrhea are provided.
    Type: Application
    Filed: August 21, 2003
    Publication date: April 8, 2004
    Applicant: Gruenenthal GmbH
    Inventors: Bernd Sundermann, Helmut Buschmann, Babette-Yvonne Koegel, Beatrix Merla, Nikolaus Risch
  • Process for preparing 5-(4-fluorophenyl)-1-[2-((2R,4R)-4-hydroxy-6-oxo-tetrahydro-pyran-2-yl)ethyl]-2-isopropyl-4-phenyl-1H-pyrrole-3-carboxylic acid phenylamide
    Publication number: 20040068121
    Abstract: A method for preparing 5-(4-fluorophenyl)-1-[2-((2R,4R)4-hydroxy-6-oxo-tetrahydro-pyran-2-yl)-ethyl]-2-isopropyl-4-phenyl-1H-pyrrole-3 -carboxylic acid phenylamide (I), a key intermediate in the synthesis of atorvastatin calcium, is described.
    Type: Application
    Filed: August 6, 2003
    Publication date: April 8, 2004
    Inventors: Jade D. Nelson, Michael G. Pamment
  • Arylated furan- and thiophenecarboxamides, processes for their preparation, their use as medicaments, and pharmaceutical preparations comprising them
    Publication number: 20040068120
    Abstract: Compounds of the formulae Ia and Ib 1
    Type: Application
    Filed: December 12, 2001
    Publication date: April 8, 2004
    Inventors: Stefan Peukert, Joachim Brendel, Horst Hemmerle, Heinz-Werner Kleemann
  • Derivatives of benzofuran or benzodioxazole compounds
    Patent number: 6716987
    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
    Type: Grant
    Filed: December 20, 2001
    Date of Patent: April 6, 2004
    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
  • Five-membered heterocyclic alkanoic acid derivative
    Publication number: 20040063775
    Abstract: The present invention relates to a compound represented by the formula 1
    Type: Application
    Filed: September 22, 2003
    Publication date: April 1, 2004
    Inventors: Yu Momose, Tsuyoshi Maekawa, Hiroshi Imoto, Hiroyuki Odaka, Hiroyuki Kimura
  • Acid derivatives useful as serine protease inhibitors
    Patent number: 6713467
    Abstract: Compounds of formula I and II, or pharmaceutically-acceptable salts thereof, are useful as inhibitors of Factor VIIa, Factor IXa, Factor Xa, Factor FXIa, tryptase, and urokinase, wherein ring B is phenyl or pyridyl, L is a linker, and R1-R27, W, Z1, and Z2 are as defined in the specification.
    Type: Grant
    Filed: November 7, 2001
    Date of Patent: March 30, 2004
    Assignee: Bristol-Myers Squibb Company
    Inventors: Gregory S. Bisacchi, James C. Sutton, Shung C. Wu
  • Substituted dipeptides as growth hormone secretagogues
    Publication number: 20040058971
    Abstract: This invention relates to novel compounds which are useful in the modulation of endogenous growth hormone levels in a mammal. The invention further relates to novel intermediates for usein the synthesis of said compounds, as well as novel processes employed in these syntheses. Also included are methods of treating a mammal which include the administration of said compounds.
    Type: Application
    Filed: March 14, 2003
    Publication date: March 25, 2004
    Inventors: Jeffrey Alan Dodge, Britta Evers, Louis Nickolaus Jungheim, Brian Stephen Muehl, Gerd Ruehter, Kenneth Jeff Thrasher
  • Useful aroyl pyrrole heteroaryl methanones and methanols
    Publication number: 20040058980
    Abstract: This invention is directed to aroyl pyrrole heteroaryl methanone and methanol compounds pharmaceutically useful as agents for treating or modulating a central nervous system disorder and methods for treating or modulating a central nervous system disorder.
    Type: Application
    Filed: December 23, 2002
    Publication date: March 25, 2004
    Inventors: John R. Carson, Ellen E. Codd, Phillip M. Pitis
  • Cyclic protein tyrosine kinase inhibitors
    Publication number: 20040054186
    Abstract: Novel cyclic compounds and salts thereof, pharmaceutical compositions containing such compounds, and methods of using such compounds in the treatment of protein tyrosine kinase-associated disorders such as immunologic and oncologic disorders.
    Type: Application
    Filed: March 24, 2003
    Publication date: March 18, 2004
    Inventors: Jagabandhu Das, Ramesh Padmanabha, Ping Chen, Derek J. Norris, Arthur M.P. Doweyko, Joel C. Barrish, John Wityak, Louis J. Lombardo, Francis Y.F. Lee
  • Cyanine dyes
    Publication number: 20040054192
    Abstract: A compound represented by the following formula (I) or a salt thereof: 1
    Type: Application
    Filed: September 10, 2003
    Publication date: March 18, 2004
    Inventors: Masayuki Kawakami, Hiroshi Kitaguchi
  • 2-substituted-4-nitrogen heterocycles as modulators of chemokine receptor activity
    Patent number: 6706735
    Abstract: The present application describes modulators of CCR3 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases.
    Type: Grant
    Filed: June 26, 2002
    Date of Patent: March 16, 2004
    Assignee: Bristol-Myers Squibb Pharma Company
    Inventors: Paul S. Watson, Soo S. Ko, George V. DeLucca, John V. Duncia, Joseph B. Santella, III, Dean A. Wacker
  • Integrin receptor inhibitors
    Patent number: 6706753
    Abstract: Provided are compounds of formula (I) wherein A, Q, W, X, Y, Z, R1 to R4, m and n are as defined herein. Compounds of the invention bind to &agr;4 integrin receptors and thereby inhibit binding of ligands for &agr;4 integrins which is useful for prophylactic and/or therapeutic treatment of diseases and conditions associated with &agr;4 integrins or their ligands.
    Type: Grant
    Filed: December 6, 2002
    Date of Patent: March 16, 2004
    Assignee: Genentech, Inc.
    Inventors: Dean R. Artis, David Y. Jackson, Thomas E. Rawson, Mark E. Reynolds, Daniel P. Sutherlin, Mark S. Stanley
  • Caspase-1 inhibitors and methods for their use
    Publication number: 20040048895
    Abstract: The invention provides compounds of Formula I and derivatives thereof, pharmaceutical compositions comprising a compound of Formula I, and methods of treatment utilizing such compounds and compositions: 1
    Type: Application
    Filed: June 5, 2003
    Publication date: March 11, 2004
    Inventors: Darin Allen, Bruce Fahr, Johan Oslob, Brian C. Raimundo, Michael J. Romanowski
  • Small molecule inhibitors of rotamase enzyme activity
    Publication number: 20040049046
    Abstract: This invention relates to neurotrophic N-glyoxylprolyl ester compounds having an affinity for FKBP-type immunophilins, their preparation and use as inhibitors of the enzyme activity associated with immunophilin proteins, and particularly inhibitors of peptidyl-prolyl isomerase or rotamase enzyme activity.
    Type: Application
    Filed: August 16, 2002
    Publication date: March 11, 2004
    Applicant: GPI NIL Holdings, Inc.
    Inventors: Gregory S. Hamilton, Joseph P. Steiner
  • Monocyclic derivatives as matrix metalloproteinase inhibitors
    Publication number: 20040043979
    Abstract: This invention provides compounds defined by Formula I
    Type: Application
    Filed: August 5, 2003
    Publication date: March 4, 2004
    Inventor: Joseph Armand Picard
  • Novel substituted sulfamate anticonvulsant derivatives
    Publication number: 20040038911
    Abstract: The present invention is directed to novel compounds of the formula (I) 1
    Type: Application
    Filed: May 8, 2003
    Publication date: February 26, 2004
    Inventors: Ahmed Abdel-Magid, Cynthia Maryanoff, Steven Mehrman, Kirk Sorgi, Frank Villani, Cheryl Kordik, Allen B. Reitz, Bruce Maryanoff
  • Mono-and bis-hydrazone pigments
    Publication number: 20040039182
    Abstract: Mono- and Bis-Azo/Hydrazone Pyrrole Pigments and Methods for preparing same.
    Type: Application
    Filed: January 6, 2003
    Publication date: February 26, 2004
    Inventors: Terence Chamberlain, Norman W. Smith, Donald T. DeRussy
  • Muscarinic receptor antagonists
    Patent number: 6693202
    Abstract: Disclosed are multibinding compounds which are muscarinic receptor antagonists. The multibinding compounds of this invention containing from 2 to 10 ligands covalently attached to one or more linkers. Each ligand is, independently of each other, a muscarinic receptor antagonist or an allosteric modulator provided that at least one of said ligand is a muscarinic receptor antagonist. The multibinding compounds of this invention are useful in the treatment and prevention of diseases such as chronic obstructive pulmonary disease, chronic bronchitis, irritable bowel syndrome, urinary incontinence, and the like.
    Type: Grant
    Filed: August 25, 2000
    Date of Patent: February 17, 2004
    Assignee: Theravance, Inc.
    Inventors: James Aggen, John H. Griffin, Mathai Mammen, Daniel Marquess, Edmund J. Moran, David Oare
  • Histone deacetylase inhibitors based on alpha-ketoepoxide compounds
    Publication number: 20040029922
    Abstract: Histone deacetylase is a metallo-enzyme with zinc at the active site. Compounds having a zinc-binding moiety, for example, an alpha-ketoepoxide group, such as an alpha-ketothio group, can inhibit histone deacetylase. Histone deacetylase inhibition can repress gene expression, including expression of genes related to tumor suppression. Accordingly, inhibition of histone deacetylase can provide an alternate route for treating cancer, hematological disorders, e.g., hemoglobinopathies, autosomal dominant disorders, e.g. spinal muscular atrophy and Huntington's disease, genetic related metabolic disorders, e.g., cystic fibrosis and adrenoleukodystrophy, or to stimulate hematopoietic cells ex vivo.
    Type: Application
    Filed: May 21, 2003
    Publication date: February 12, 2004
    Applicant: Beacon Laboratories, Inc.
    Inventors: Hsuan-Yin Lan-Hargest, Robert J. Kaufman
  • Aromatic sulfone hydroxamates and their use as protease inhibitors
    Patent number: 6689794
    Abstract: This invention is directed to aromatic sulfone hydroxamates (also known as “aromatic sulfone hydroxamic acids”) and salts thereof that, inter alia, inhibit matrix metalloproteinase (also known as “matrix metalloprotease” or “MMP”) activity and/or aggrecanase activity. This invention also is directed to a prevention or treatment method that comprises administering such a compound or salt in an MMP-inhibiting and/or aggrecanase-inhibiting effective amount to an animal, particularly a mammal having (or disposed to having) a pathological condition associated with MMP and/or aggrecanase activity.
    Type: Grant
    Filed: May 10, 2002
    Date of Patent: February 10, 2004
    Assignee: Pharmacia Corporation
    Inventors: John N. Freskos, Yvette M. Fobian, Thomas E. Barta, Daniel P. Becker, Louis J. Bedell, Terri L. Boehm, Jeffery N. Carroll, Gary A. DeCrescenzo, Susan L. Hockerman, Darren J. Kassab, Steve A. Kolodziej, Joseph McDonald, Deborah A. Mischke, Monica B. Norton, Joseph G. Rico, John J. Talley, Clara I. Villamil, Lijuan Jane Wang
  • Novel compounds
    Publication number: 20040024218
    Abstract: Compounds of formula I, or a salt thereof or a hydrate thereof, as follows: 1
    Type: Application
    Filed: December 19, 2002
    Publication date: February 5, 2004
    Applicant: SmithKline Beecham SpA
    Inventors: Daniela Barlocco, Giorgio Cignarella, Giuseppe Arnaldo Maria Giardina, Mario Grugni, Silvano Ronzoni
  • Copper-catalyzed formation of carbon-heteroatom and carbon-carbon bonds
    Publication number: 20040019216
    Abstract: The present invention relates to copper-catalyzed carbon-heteroatom and carbon-carbon bond-forming methods. In certain embodiments, the present invention relates to copper-catalyzed methods of forming a carbon-nitrogen bond between the nitrogen atom of an amide or amine moiety and the activated carbon of an aryl, heteroaryl, or vinyl halide or sulfonate. In additional embodiments, the present invention relates to copper-catalyzed methods of forming a carbon-nitrogen bond between a nitrogen atom of an acyl hydrazine and the activated carbon of an aryl, heteroaryl, or vinyl halide or sulfonate. In other embodiments, the present invention relates to copper-catalyzed methods of forming a carbon-nitrogen bond between the nitrogen atom of a nitrogen-containing heteroaromatic, e.g., indole, pyrazole, and indazole, and the activated carbon of an aryl, heteroaryl, or vinyl halide or sulfonate.
    Type: Application
    Filed: May 8, 2003
    Publication date: January 29, 2004
    Inventors: Stephen L. Buchwald, Artis Klapars, Jon C. Antilla, Gabriel E. Job, Martina Wolter, Fuk Y. Kwong, Gero Nordmann, Edward J. Hennessy
  • Dihydoxyhexanoic acid derivatives, their intermediates, and methods of making
    Publication number: 20040019217
    Abstract: This invention relates to dihydroxyhexanoic acid derivatives and their intermediates, as well as to methods of preparing such compounds. Additionally, present invention relates to removing a protecting group from a protected amine wherein the method comprises reacting the protected amine with phosphoric acid.
    Type: Application
    Filed: May 7, 2003
    Publication date: January 29, 2004
    Applicant: Pfizer Inc.
    Inventors: John C. Kath, Zhengong B. Li, V. John Jasys, Frank J. Urban
  • N-(4-carbamimidoyl-phenyl)-glycine derivatives
    Patent number: 6683215
    Abstract: The invention is concerned with novel N-(4-carbamimidoyl-phenyl)-glycine derivatives of the formula: wherein R1, E, X1 to X4 and G1 and G2 are as defined in the description and the claims, as well as hydrates or solvates and physiologically usable salts thereof.
    Type: Grant
    Filed: October 4, 2002
    Date of Patent: January 27, 2004
    Assignee: Hoffman-La Roche Inc.
    Inventors: Jean Ackermann, Leo Alig, Alexander Chucholowski, Katrin Groebke, Kurt Hilpert, Holger Kuehne, Ulrike Obst, Lutz Weber, Hans Peter Wessel
  • Red light emitting materials
    Publication number: 20040013902
    Abstract: This invention features a compound having the formula: 1
    Type: Application
    Filed: July 9, 2002
    Publication date: January 22, 2004
    Inventors: Chin-Ti Chen, Hsiu-Chih Yeh, Wei-Ching Wu, Li-Hsin Chan
  • Non-peptide GnRH agents, pharmaceutical compositions and methods for their use
    Publication number: 20040014787
    Abstract: Non-peptide GnRH agents capable of inhibiting the effect of gonadotropin-releasing hormone are described. Such compounds and their pharmaceutically acceptable salts, prodrugs, and active metabolites are suitable for treating mammalian reproductive disorders and steroid hormone-dependent tumors as well as for regulating fertility, where suppression of gonadotropin release is indicated. Methods for synthesizing the compounds and intermediates useful in their preparation are also described.
    Type: Application
    Filed: June 11, 2003
    Publication date: January 22, 2004
    Applicant: Agouron Pharmaceuticals, Inc.
    Inventors: Mark B. Anderson, Lance Christopher Christie, Quyen-Quyen Thuy Do, Jun Feng, Yufeng Hong, Haitao Li, Ved P. Pathak, Ranjan Jagath Rajapakse, Eric T. Sun, Eileen Valenzuela Tompkins
  • Polycyclic aryl and heteroaryl substituted 4-pyrones useful for selective inhibition of the coagulation cascade
    Publication number: 20040006227
    Abstract: The invention relates to polycyclic aryl and heteroaryl substituted 4-pyrone 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: January 8, 2004
    Inventors: Michael S. South, Chun C Ma, Kevin J Koeller, Hayat K Rahman, William L Neumann
  • Substituted alkanoic acids
    Publication number: 20040006056
    Abstract: The invention is directed to physiologically active compounds of general formula (I): 1
    Type: Application
    Filed: May 1, 2003
    Publication date: January 8, 2004
    Inventors: Neil Victor Harris, Garry Fenton
  • Synthetic derivatives
    Publication number: 20030236302
    Abstract: This invention features a 5,6-dihydro-2-pyrone compound of formula (I), wherein R1 is H, OH, or C2˜C5 alkoxyl; and R2 is 2-phenyl ethyl, 2-phenyl ethenyl, 2-heteroaryl ethyl, or 2-heteroaryl ethenyl; in which the phenyl or the heteroaryl is optionally mono-, di-, or tri-substituted with R3, R4, or R5; each of R3, R4, and R5, independently, is Cl, F, Br, I, CN, C1˜C5 alkyl, C1˜C5 alkoxyl, C3˜C5 alkenyloxy, C4˜C6 cycloalkoxyl, C4˜C8 cycloalkyl alkoxyl, C3˜C5 alkoxy alkoxyl, or C1˜C4 alkoxy carbonyl.
    Type: Application
    Filed: February 27, 2003
    Publication date: December 25, 2003
    Inventors: Shoujun Chen, Lijun Sun, Joel McCleary