Patents Represented by Attorney, Agent or Law Firm Paul H. Ginsburg
  • Processes and intermediates for preparing substituted chromanol derivatives
    Patent number: 6355825
    Abstract: The invention relates to processes for preparing a compound of the formula and the enantiomer of said compound, wherein the benzoic acid moiety is attached at position 6 or 7 of the chroman ring, and R1, R2, and R3 are as defined herein. The invention further relates to intermediates that are useful in the preparation of the compound of formula X above.
    Type: Grant
    Filed: March 21, 2001
    Date of Patent: March 12, 2002
    Assignee: Pfizer Inc.
    Inventors: Anthony Piscopio, Joel M. Hawkins, Stephanie Caron, Sarah E. Kelly, Jeffrey W. Raggon, Michael J. Castaldi, Robert W. Dugger, Sally G. Ruggeri
  • Matrix metalloprotease inhibitors
    Patent number: 6350907
    Abstract: Compounds of formula (I): or pharmaceutically acceptable salts thereof, or solvates of either entity, wherein the substituents have the values described herein, are useful as matrix metalloprotease (MMP) inhibitors
    Type: Grant
    Filed: April 11, 2000
    Date of Patent: February 26, 2002
    Assignee: Pfizer Inc
    Inventors: Michael Jonathan Fray, Roger Peter Dickinson, Kevin Neil Dack
  • Purine derivatives
    Patent number: 6350735
    Abstract: The present invention relates to compounds of the formula and pharmaceutically acceptable salts and solvates thereof, to processes for the preparation of, intermediates used in the preparation of, and compositions containing such compounds and the uses of such compounds as adenosine A2a receptor agonists.
    Type: Grant
    Filed: October 16, 2000
    Date of Patent: February 26, 2002
    Assignee: Pfizer Inc
    Inventor: Sandra Marina Monaghan
  • Process for making 5-lipoxygenase inhibitors having varied heterocyclic ring systems
    Patent number: 6346624
    Abstract: A novel process intermediate, tetrahydro-4-[3-(4-fluorophenyl)thio]phenyl-2H-pyran-4-carboxamide, of the formula: is described, as well as its use in a process of preparing 5-lipoxygenase inhibitors of the formula: which comprises establishing a reaction mixture consisting of: and an electron deficient monocyclic or benzo-fused bicyclic N-heterocycle containing two nitrogen atoms of the formula:  in an aprotic solvent; in the presence of a carbonate of the formula: (M)2-CO3, where M is an alkali metal, Group 1/Ia element, selected from the group consisting of lithium, Li; sodium,Na; potassium, K; rubidium, Rb; and cesium, Cs; followed by heating of said reaction mixture under a nitrogen atmosphere; whereby there is produced the desired compound of the above-recited formula.
    Type: Grant
    Filed: June 29, 2000
    Date of Patent: February 12, 2002
    Assignee: Pfizer Inc
    Inventors: Timothy Norris, Megan E. Hnatow, John F. Lambert
  • 3-(arylsulfonylamino)-tetrahydrofuran-3-carboxylic acid hydroxamides
    Patent number: 6342521
    Abstract: A compound of the formula wherein R1, R2 and Q is as defined above, are useful in the treatment of a arthritis (including osteoarthritis and rheumatoid arthritis), cancer (such as solid tumor cancer including colon cancer, breast cancer, lung cancer and prostrate cancer and hematopoietic malignancies including leukemias and lymphomas), and other disorders. In addition, the compounds of the present invention may be used in combination therapy with standard non-steroidal anti-inflammatory drugs (NSAID'S) and analgesics, and in combination with cytotoxic drugs such as adriamycin, daunomycin, cis-platinum, etoposide, taxol, taxotere and other alkaloids, such as vincristine, in the treatment of cancer.
    Type: Grant
    Filed: May 25, 2000
    Date of Patent: January 29, 2002
    Assignee: Pfizer Inc.
    Inventor: Lawrence A. Reiter
  • 2?-deoxy hygromycin derivatives
    Patent number: 6342497
    Abstract: This invention relates to compounds of the formula and to pharmaceutically acceptable salts, prodrugs and solvates thereof, wherein R1 and R2 are as defined herein. The compounds of formula 1 are antibacterial and antiprotozoal agents that may be used to treat various bacterial and protozoal infections and disorders related to such infections. The invention also relates to pharmaceutical compositions containing the compounds of formula 1 and to methods of treating bacterial and protozoal infections by administering the compounds of formula 1.
    Type: Grant
    Filed: September 7, 1999
    Date of Patent: January 29, 2002
    Assignee: Pfizer Inc
    Inventor: Robert Gerald Linde, II
  • 2-benzimidazolylamine compounds as ORL-1-receptor agonists
    Patent number: 6340681
    Abstract: A compound of the formula: or a pharmaceutically acceptable salt thereof, wherein R1 and R2 are independently selected from hydrogen, halo, hydroxy, (C1-C4)alkyl, halo (C1-C4)alkyl and the like; R3 and R4 are independently selected from hydrogen, halo(C1-C10)alkyl, optionally substituted (C1-C6)alkyl and the like, or R3 and R4, together with the nitrogen atom to which they are attached, form an optionally substituted fully saturated, partially saturated or fully unsaturated heterocyclic ring; and R5 is (C4-C11)cycloalkyl and the like, has ORL1-receptor agonist activity, and are useful as analgesics or the like in mammalian subjects.
    Type: Grant
    Filed: June 29, 2000
    Date of Patent: January 22, 2002
    Assignee: Pfizer Inc
    Inventor: Fumitaka Ito
  • Phenylamino-substituted tricyclic derivatives for treatment of hyperproliferative diseases
    Patent number: 6335344
    Abstract: The present invention relates to compounds of the formula (I) and to pharmaceutically acceptable salts thereof, wherein R1-R4 and Z are as defined herein. The compounds of formula (I) are useful as antiproliferative agents. The invention further relates to pharmaceutical compositions and methods of treating hyperproliferative disorders such as cancer, using such compounds.
    Type: Grant
    Filed: September 29, 1999
    Date of Patent: January 1, 2002
    Assignee: Pfizer Inc.
    Inventor: Rodney C. Schnur
  • Hydroxy pipecolate hydroxamic acid derivatives
    Patent number: 6329397
    Abstract: A compound of the formula wherein R1, R2 R3, R4 R5, R6, R7, R8, R9 and Ar are as defined above, useful in the treatment of a condition selected from the group consisting of arthritis, cancer, and other diseases characterized by matrix metalloproteinase or mammalian reprolysin activity. In addition, the compounds of the present invention may be used in combination therapy with standard non-steroidal anti-inflammatory drugs (NSAID'S), COX-2 inhibitors and analgesics, and in combination with cytotoxic drugs such as adriamycin, daunomycin, cis-platinum, etoposide, taxol, taxotere and other alkaloids, such as vincristine, in the treatment of cancer.
    Type: Grant
    Filed: August 12, 1999
    Date of Patent: December 11, 2001
    Assignee: Pfizer
    Inventors: Kim F. McClure, Mark C. Noe, Michael A. Letavic, Louis S. Chupak
  • Substituted benzylaminopiperidine compounds
    Patent number: 6329396
    Abstract: The invention provides a substituted benzylaminopiperidine compounds that are useful in the treatment of gastrointestinal disorders; central nervous system (CNS) disorders; inflammatory disease; emesis; urinary incontinence; pain; migraine; sunburn; diseases, disorders and adverse conditions caused by Heliobacter pylori; or angiogenesis, especially CNS disorders in a mammalian subject, especially in humans.
    Type: Grant
    Filed: May 1, 2000
    Date of Patent: December 11, 2001
    Assignee: Pfizer Inc.
    Inventors: Kunio Satake, Yuji Shishido, Hiroaki Wakabayashi
  • 13-membered azalides and their use as antibiotic agents
    Patent number: 6329345
    Abstract: The invention relates to a method of preparing compounds of the formula 1 and to pharmaceutically acceptable salts thereof. The compounds of formula 1 are antibacterial agents that may be used to treat various bacterial and protozoa infections. The invention also relates to pharmaceutical compositions containing the compounds of formula 1 and to methods of treating bacterial protozoa infections by administering the compounds of formula 1. The invention also relates to methods of preparing the compounds of formula 1 and to intermediates useful in such preparation.
    Type: Grant
    Filed: November 18, 1999
    Date of Patent: December 11, 2001
    Assignee: Pfizer Inc
    Inventors: Robert J. Rafka, Barry J. Morton, Colman B. Ragan, Peter Bertinato, John P. Dirlam, Alan E. Blize, Carl B. Ziegler
  • Immunogenic compositions that potentiate growth hormone activity
    Patent number: 6328974
    Abstract: This invention relates to immunogenic compositions capable of potentiality growth hormone activity, comprising an immunologically effective amount of a composite peptide comprising at least two non-contiguous somatotropin epitope amino acid sequences, wherein said composite peptide is substantially free of receptor binding domain sequences; and an immunologically acceptable excipient. The invention further relates to methods of using an immunogenic composition of the invention to potentiate the action of growth hormone in pigs.
    Type: Grant
    Filed: March 26, 1999
    Date of Patent: December 11, 2001
    Assignee: Pfizer Inc
    Inventors: Hector Wasunna Alila, Michael Thomas Clark, Elaine Verne Jones, Timothy Joe Miller, Shawn Patrick O'Brien, Ganesh Madhusudan Sathe
  • Bisamidine compounds as antiproliferative agents
    Patent number: 6329412
    Abstract: Known bisamidine compounds are newly discovered to possess DNA methyltransferase inhibiting properties, making them useful for preparing pharmaceutical compositions useful as antiproliferative agents for treating a neoplastic or a non-neoplastic disease characterized by abnormally rapid proliferation of tissue involved in said disease; wherein said bisamidines comprise a compound of Formula (5.0.0): and a pharmaceutically acceptable salt thereof, wherein: —X is —C(R34)—; or —N—; —R23, R24, R28 and R29 are each independently —H; or —CH2— where R23 and R24 and R28 and R29 are taken together with the nitrogen atoms to which they are attached, to form an imidazolinyl group; and —R34 is —H; or —CH3. A preferred species of Formula (5.0.0) is the following: 2-(4-Carbamimidoyl-phenyl)-1H-indole-6-carboxamidine.
    Type: Grant
    Filed: March 24, 2000
    Date of Patent: December 11, 2001
    Assignee: Pfizer Inc
    Inventors: Steven W. Goldstein, Banauara L. Mylari, Jose R. Perez, Edward A. Glazer
  • Heterocyclic-cyclic amine derivatives
    Patent number: 6326382
    Abstract: Compounds of the formula wherein R1 R2, R7, R8, X, Y, M and L are defined as below. The compounds of formula I are cholinesterase inhibitors and are useful in enhancing memory in patients suffering from dementia and Alzheimer's disease.
    Type: Grant
    Filed: July 14, 2000
    Date of Patent: December 4, 2001
    Assignee: Eisai Co., LTD
    Inventors: Anabella Villalobos, Arthur A. Nagel, Yuhpyng L. Chen
  • Adenosine A2A receptor agonists as antiinflammatory agents
    Patent number: 6326359
    Abstract: The present invention provides compounds of formula (I): and pharmaceutically acceptable salts and solvates thereof, together with processes for the preparation of, compositions containing, uses of and intermediates used in the preparation of such compounds that have A2a receptor agonist activity.
    Type: Grant
    Filed: October 15, 1999
    Date of Patent: December 4, 2001
    Assignee: Pfizer Inc
    Inventors: Sandra M. Monaghan, Simon J. Mantell
  • Screening novel human phosphodiesterase IV isozymes for compounds which modify their enzymatic activity
    Patent number: 6323041
    Abstract: This invention relates to novel nucleic acid sequences encoding three novel human phosphodiesterase (hPDE IV) isozymes. It also relates to polypeptides encoded by such sequences. This invention also relates to an assay method for detecting the presence of such novel isozymes in human cells, and to a method of identifying compounds or other substances that inhibit or modify the activity of such isozymes.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: November 27, 2001
    Assignee: Pfizer Inc.
    Inventors: Douglas A. Fisher, Michael D. Robbins
  • Atropisomers of 2,3-disubstituted-(5.6)-heteroaryl fused-pyrimidin-4-ones
    Patent number: 6323208
    Abstract: The present invention relates to novel atropisomers of 2,3-disubstituted-(5,6)-heteroarylfused-pyrimidin-4-ones, pharmaceutical compositions containing such compounds the use of such compounds to treat neurodegenerative, psychotropic, and drug and alcohol induced central and peripheral nervous system disorders.
    Type: Grant
    Filed: July 23, 1998
    Date of Patent: November 27, 2001
    Assignee: Pfizer Inc
    Inventors: Bertrand L. Chenard, Willard M. Welch, Jr.
  • N-acyl and N-aroyl aralkylamides
    Patent number: 6323229
    Abstract: A compound of the formula wherein m, R1, R2, R3, R4, R5 and X are as defined, useful in treating or preventing migraine, depression and other disorders for which a 5-HT1 agonist or antagonist is indicated.
    Type: Grant
    Filed: April 14, 1999
    Date of Patent: November 27, 2001
    Assignee: Pfizer INC
    Inventor: Harry R. Howard
  • Benzazepine derivatives as inhibitors of hyperproliferation diseases
    Patent number: 6319915
    Abstract: A method of treating hyperproliferation diseases in mammals in need of such treatment which method includes administering to said mammal a therapeutically effective amount of a compound of the formula: or a pharmaceutically acceptable salt, hydrate or prodrug thereof, wherein R1, R2, R3, R4, W, X, Y, Z and t are as defined herein.
    Type: Grant
    Filed: April 13, 2000
    Date of Patent: November 20, 2001
    Assignee: Pfizer Inc.
    Inventors: Steven W. Goldstein, Kelly P. Longo, Arthur A. Nagel, John A. Lowe, III
  • Process for converting 2,4-dichloropyridines into 2-aryloxy-4-chloropyridines
    Patent number: 6316631
    Abstract: This invention relates to a process for converting 2,4-dichloropyridines into 2-aryloxy-4-chloropyridines, comprising reacting a compound of formula (I), wherein R1 is (C1-C4)alkyl; R2 is methyl or ethyl; and R3, R4 and R5 are selected, independently, from (C1-C4)alkyl and (C1-C4)alkoxy; or a pharmaceutically acceptable salt thereof; comprising reacting a compound of formula (II), wherein R1 and R2 are defined as above, with a compound of formula (III), wherein R3, R4 and R5 are defined as above, in the presence of a base that is capable of deprotonating the compound of formula (III), optionally in the presence of an organometallic halide or oxide and a suitable solvent, and then optionally converting the resulting compound of formula (I) into a pharmaceutically acceptable salt of such compound.
    Type: Grant
    Filed: March 4, 1999
    Date of Patent: November 13, 2001
    Assignee: Pfizer Inc.
    Inventors: Yuhpyng L. Chen, Sally Gut Ruggeri