Patents Represented by Attorney Raymond M. Speer
  • Patent number: 6448236
    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: September 10, 2002
    Assignee: Pfizer Inc
    Inventor: Sandra Marina Monaghan
  • Patent number: 6391872
    Abstract: Therapeutically active compositions of matter and member species thereof are described which comprise indazole-containing compounds, said compounds and their therapeutic activity resulting directly from an indazole-for-catechol bioisostere replacement of a catechol-containing compound having the same therapeutic activity, where non-catechol substituents are the same or homologous before and after said replacement, and wherein said compositions of matter comprise a compound of Formula (I1) or (I2): or a pharmaceutically acceptable salt thereof, wherein in a preferred embodiment RC is hydrogen; RA is cyclohexyl; and RB is ethyl.
    Type: Grant
    Filed: September 20, 1999
    Date of Patent: May 21, 2002
    Assignee: Pfizer Inc
    Inventor: Anthony Marfat
  • Patent number: 6384236
    Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein R1, R2, AA and Y are as defined herein, inhibit phosphodiesterase type IV or inhibit the production of tumor necrosis factor, and therefore are useful in the treatment of certain conditions and diseases including asthma, arthritis, and sepsis.
    Type: Grant
    Filed: January 25, 2001
    Date of Patent: May 7, 2002
    Assignee: Pfizer Inc
    Inventor: Edward F. Kleinman
  • Patent number: 6380218
    Abstract: A compound of formula (I) wherein m, n, o, p, q, r, A, B, D, E, R1, R2,R3, R4, R5, R6, R7 and R8 are as defined in the description, useful in the treatment of respiratory, allergic, rheumatoid, body weight regulation, inflammatory and central nervous system disorders such as asthma, chronic obstructive pulmonary disease, adult respiratory diseases syndrome, shock, fibrosis, pulmonary hypersensitivity, allergic rhinitis, atopic dermatitis, psoriasis, weight control, rheumatoid arthritis, cachexia, crohn's disease, ulcerative colitis, arthritic conditions and other inflammatory diseases, depression, multi-infarct dementia and AIDS.
    Type: Grant
    Filed: May 27, 1999
    Date of Patent: April 30, 2002
    Assignee: Pfizer Inc
    Inventors: Anthony Marfat, Robert J. Chambers, John W. Watson, John B. Cheng, Allen J. Duplantier, Edward F. Kleinman
  • Patent number: 6355662
    Abstract: Compounds of Formula (1.0.0): are described wherein A is for example aryl, heteroaryl or heterocyclyl, Y is preferably —C(═O)—; B is independently selected from a group of moieties, the most preferred of which are those of partial Formulas (1.1.2) and (1.1.6): and E is a single bond; oxygen; 1,1-cyclopropyl; C(CH3)2; CF2; or a bridging moiety of partial Formula (1.9.0): where R1a is hydrogen when R1 has the meaning of a mono-valent substituent; and R1a is a single bond when R1 has the meaning of a di-valent substituent. Said compounds are useful in methods of treating or preventing an inflammatory, autoimmune or respiratory diseases by inhibiting cell adhesion and consequent or associated pathogenic processes subsequently mediated by VLA-4.
    Type: Grant
    Filed: October 26, 1999
    Date of Patent: March 12, 2002
    Assignee: Pfizer Inc
    Inventors: Allen Jacob Duplantier, Anthony John Milici, Louis Stanley Chupak
  • 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
  • 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
  • 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
  • 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
  • Patent number: 6303782
    Abstract: A process is described for preparing an aromatic compound substituted by a tertiary nitrile of Formula (1.0.0): comprising treating a substituted aromatic compound of Formula (2.0.0): with a secondary nitrile of Formula (3.0.0): in the presence of a base having a pKa numerical value in the range of from about 17 to about 30, provided that the difference in pKa numerical values between said base and the corresponding tertiary nitrile of Formula (3.0.0) is no more than about 6; in an aprotic solvent having a dielectric constant (∈) of less than about 20; and at a reaction temperature in the range of from about 0° C. to about 120° C.; whereby there is formed said tertiary-nitrile-substituted aromatic compound final product of Formula (1.0.0); wherein the constituent parts W1, W2, W3, W4, and W5; and the substituent moieties R1, R2, R3, R4, R5, R6, and R7 in the compounds of Formulas (1.0.0), (2.0.0) and (3.0.
    Type: Grant
    Filed: March 1, 2000
    Date of Patent: October 16, 2001
    Assignee: Pfizer Inc
    Inventor: St├ęphane Caron
  • Patent number: 6262040
    Abstract: The invention relates to compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein R, R1, and R2, are as defined herein. The invention further relates to pharmaceutical compositions containing, and methods of using, the compounds of formula (I), or acceptable salts thereof, for the inhibition of phosphodiesterase (PDE) type IV or the production of tumor necrosis factor (TNF) in a mammal. The invention also relates to intermediates that are useful in the preparation of the compounds of formula (I).
    Type: Grant
    Filed: March 4, 1999
    Date of Patent: July 17, 2001
    Assignee: Pfizer Inc
    Inventor: Anthony Marfat
  • Patent number: 6239285
    Abstract: A process is described for preparing a compound of Formula (1.3.0): comprising: establishing a reaction mixture consisting of in an aprotic solvent; in the presence of NaOH or KOH; optionally in the presence of a phase transfer catalyst, especially a quaternary ammonium salt or a phosphonium salt; followed by heating said reaction mixture under a nitrogen atmosphere.
    Type: Grant
    Filed: June 29, 2000
    Date of Patent: May 29, 2001
    Assignee: Pfizer Inc
    Inventors: Timothy Norris, Megan E. Hnatow
  • Patent number: 6211222
    Abstract: The invention relates to compounds of the formula I and pharmaceutically acceptable salts thereof, wherein R2a and R2b are independently selected from the group consisting essentially of hydrogen and hereinafter recited substituents, provided that one, but not both of R2a and R2b must be independently selected as hydrogen, wherein said substituents comprise: wherein the dashed lines in formulas (Ia) and (Ib) independently and optionally represent a single or double bond, provided that in formula (Ia) both dashed lines cannot both represent double bonds at the same time; and R, R1, R3, R4, R5, R6, R7, R18 and m are as defined. The invention further relates to intermediates for the preparation of the compounds of formula I, and to pharmaceutical compositions containing, and methods of using, the compounds of formula I, or acceptable salts thereof, for the inhibition of phosphodiesterase (PDE) type IV or the production of tumor necrosis factor (TNF) in a mammal.
    Type: Grant
    Filed: November 4, 1997
    Date of Patent: April 3, 2001
    Assignee: Pfizer Inc
    Inventor: Anthony Marfat
  • Patent number: 6127398
    Abstract: The invention relates to compounds of the formula I ##STR1## and pharmaceutically acceptable salts thereof, wherein R.sub.2.sup.a and R.sub.2.sup.b are independently selected from the group consisting essentially of hydrogen and hereinafter recited substituents, provided that one, but not both of R.sub.2.sup.a and R.sub.2.sup.b must be independently selected as hydrogen, wherein said substituents comprise: ##STR2## wherein the dashed lines in formulas (Ia) and (Ib) independently and optionally represent a single or double bond, provided that in formula (Ia) both dashed lines cannot both represent double bonds at the same time; andR, R.sub.1, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.18 and m are as defined.
    Type: Grant
    Filed: September 27, 1999
    Date of Patent: October 3, 2000
    Assignee: Pfizer Inc
    Inventor: Anthony Marfat
  • Patent number: 6093733
    Abstract: This invention relates to a novel class of partial or full muscarinic receptor agonists intermediates for their preparation, and pharmaceutical compositions and methods of use for the treatment or prevention of diseases the treatment or prevention of which is mediated by muscarinic receptor agonism.
    Type: Grant
    Filed: April 30, 1997
    Date of Patent: July 25, 2000
    Inventors: Anabella Villalobos, Daniel Yohannes, Jolanta Nowakowski, Dane R. Liston
  • Patent number: 6063928
    Abstract: Novel compounds having the ability to inhibit 5-lipoxygenase enzyme and having the following formula I: ##STR1## and the pharmaceutically acceptable salts thereof, wherein Ar.sup.1 is a heterocyclic moiety which is selected from imidazolyl, pyrrolyl, pyrazolyl, 1,2,3-triazolyl, 1,2,4-triazolyl, indolyl, indazolyl and benzimidazolyl, which is bonded to X.sup.1 through a ring nitrogen atom, and which may be optionally substituted with one or two substituents selected from halo, hydroxy, cyano, amino, C.sub.1-4 alkyl and the like; X.sup.1 is a direct bond or C.sub.1-4 alkylene; Ar.sup.2 is phenylene optionally substituted with halo, hydroxy, cyano, amino and the like; X.sup.2 is --A--X-- or --X--A-- wherein A is a direct bond or C.sub.1-4 alkylene and X is oxy, thio, sulfinyl or sulfonyl; Ar.sup.3 is phenylene, pyridylene, thienylene, furylene, oxazolylene or thiazolylene optionally substituted with one or two substituents selected from halo, hydroxy, cyano, amino, C.sub.1-4 alkyl and the like; R.sup.1 and R.
    Type: Grant
    Filed: December 8, 1998
    Date of Patent: May 16, 2000
    Assignee: Pfizer Inc
    Inventors: Rodney W. Stevens, Takashi Mano, Kazunari Nakao, Yoshiyuki Okumura
  • Patent number: 6040329
    Abstract: The invention relates to compounds of the formula I ##STR1## and pharmaceutically acceptable salts thereof, wherein R, R.sub.1, and R.sub.2, are as defined herein. The invention further relates to pharmaceutical compositions containing, and methods of using, the compounds of formula I, or acceptable salts thereof, for the inhibition of phosphodiesterase (PDE) type IV or the production of tumor necrosis factor (TNF) in a mammal.
    Type: Grant
    Filed: June 5, 1997
    Date of Patent: March 21, 2000
    Assignee: Pfizer Inc
    Inventor: Anthony Marfat
  • Patent number: 6013808
    Abstract: A process of purifying a (6-chloro-2-carbazolyl)methyl-malonic acid di(C.sub.1 -C.sub.6 alkyl) ester of Formula (I): ##STR1## wherein R.sub.a and R.sub.b must be the same and are selected from the group consisting of C.sub.1 -C.sub.6 alkyl; comprises phase separating one or more impurities from said carbazole ester at least once wherein the solvent used to carry out said phase separation is acetic acid. In a preferred embodiment said acetic acid is glacial acetic acid which is maintained at a temperature of from about 30.degree. to about 110.degree.0 C. and said carbazole ester is obtained in a purity of at least 99.90% by weight, so that the amount of impurities present therein is 0.10% or less by weight. In a more preferred embodiment of said process, said temperature is from about 50.degree. to about 70.degree. C., and said phase separation is carried out only once.
    Type: Grant
    Filed: April 15, 1999
    Date of Patent: January 11, 2000
    Assignee: Pfizer Inc.
    Inventors: Philip D. Hammen, Peter R. Rose, John L. Tucker, Keith M. Devries, Diane M. Rescek
  • Patent number: 6011159
    Abstract: The invention relates to processes and intermediates for preparing compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein R, R.sup.1, R.sup.2, and R.sup.3 are as defined herein. The above compounds of formula (I) are selective inhibitors of phosphodiesterase type IV and the production of tumor necrosis factor, and therefore may be used in the treatment of various inflammatory disorders such as asthma, joint inflammation, and other conditions or diseases.
    Type: Grant
    Filed: May 27, 1999
    Date of Patent: January 4, 2000
    Assignee: Pfizer Inc
    Inventors: Stephane Caron, Shane A. Eisenbeis
  • Patent number: 6005118
    Abstract: An improved process for preparing a compound of Formula (I): ##STR1## comprising: (a) treating a compound of Formula (Ia): ##STR2## with an alcohol comprising a compound of Formula (Ib-A) and an acid comprising a compound of Formula (Ib-B): ##STR3## wherein R.sub.a is selected from the group consisting essentially of hydrogen; (C.sub.1 -C.sub.6) alkyl; phenyl and (C.sub.1 -C.sub.3) alkyl-phenyl wherein said phenyl groups are optionally substituted by one or two substituents selected from the group consisting essentially of --(C.sub.1 -C.sub.4) alkyl; --O(C.sub.1 -C.sub.
    Type: Grant
    Filed: September 15, 1998
    Date of Patent: December 21, 1999
    Inventor: Stephane Caron