Patents Represented by Attorney, Agent or Law Firm Jolene W. Appleman
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Patent number: 6750231Abstract: There is provided a compound of formula I, wherein Het1, R1, R2, R3, X and n have meanings given in the description, which are useful in the prophylaxis and in the treatment of diseases mediated by opiate receptors, such as pruritus.Type: GrantFiled: March 19, 2002Date of Patent: June 15, 2004Assignee: Pfizer IncInventors: Stephen Paul Gibson, Ivan Tommasini, Kimberley Verrier, Christopher James Dutton, David Morris Gethin, Douglas James Critcher, Richard Edward Armer
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Patent number: 6710071Abstract: This invention relates to a series of difluoromethylene aromatic ethers of the formula wherein ring A and X and Y are defined as in the specification, that exhibit activity as glycine transport inhibitors, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, and their use for the enhancement of cognition and the treatment of the positive and negative symptoms of schizophrenia and other psychoses in mammals, including humans.Type: GrantFiled: August 15, 2002Date of Patent: March 23, 2004Assignee: Pfizer IncInventor: John Adams Lowe, III
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Patent number: 6686507Abstract: A process for the purification of 2-methoxy-5-trifluoro-methoxy benzaldehyde oil in which the oil is converted to amine by reaction of a nitroaniline with the oil; the imine is isolated as a solid; and the solid imine is converted back to the 2-methoxy-5-trifluoromethoxy benzaldehyde oil. The nitroaniline is selected from the group consisting of 3-nitroaniline, 3-methyl-2-nitroaniline, 4-methyl-2-nitroaniline, 2 methyl-3-nitroaniline and 4-methyl-3-nitroaniline.Type: GrantFiled: December 9, 2002Date of Patent: February 3, 2004Assignee: Pfizer IncInventors: Timothy J. N. Watson, Patrice Arpin, Michael G. Vetelino
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Patent number: 6667317Abstract: This invention relates to methods of treating traumatic brain injury (TBI) or hypoxic or ischemic stroke, comprising administering to a patient in need of such treatment an NR2B subtype selective N-methyl-D-aspartate (NMDA) receptor antagonist in combination with either: (a) a neutrophil inhibitory factor (NIF); (b) a sodium channel antagonist; (c) a nitric oxide synthase (NOS) inhibitor; (d) a glycine site antagonist; (e) a potassium channel opener; (f) an AMPA/kainate receptor antagonist; (g) a calcium channel antagonist; (h) a GABA-A receptor modulator (e.g., a GABA-A receptor agonist); or (i) an antiinflammatory agent.Type: GrantFiled: September 6, 2001Date of Patent: December 23, 2003Assignee: Pfizer IncInventors: Bertrand L. Chenard, Frank S. Menniti, Mario D. Saltarelli
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Patent number: 6610711Abstract: Novel compounds having general formula (I), and pharmaceutically and veterinarily acceptable salts thereof wherein R1, R2, R3, W, Y1, Y2, X, n and y are as defined above and processes for their preparation and intermediate compounds prepared therein. The novel compounds are useful for having utility in the treatment of pruritic dermatoses including allergic dermatitis and atopy in animals and humans.Type: GrantFiled: May 11, 2000Date of Patent: August 26, 2003Assignee: Pfizer Inc.Inventors: Richard Edward Armer, Christopher James Dutton, David Morris Gethin, Stephen Paul Gibson, Julian Duncan Smith, Ivan Tommasini
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Patent number: 6498255Abstract: 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: GrantFiled: September 19, 2001Date of Patent: December 24, 2002Assignee: Pfizer Inc.Inventors: Anabella Villalobos, Arthur A. Nagel, Yuhpyng L. Chen
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Patent number: 6465491Abstract: The present invention relates to certain 6-phenyl-pyridin-2-ylamine derivatives that exhibit activity as nitric oxide synthase (NOS) inhibitors, to pharmaceutical compositions containing them and to their use in the treatment and prevention of central nervous system disorders.Type: GrantFiled: April 4, 2001Date of Patent: October 15, 2002Assignee: Pfizer Inc.Inventors: John A. Lowe, III, Peter J. Whittle
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Patent number: 6448293Abstract: A compound of general formula (I), or pharmaceutically acceptable salts, solvates or polymorphs thereof; wherein; R1 and R2, which may be the same or different, are hydrogen, C1-C6alkyl, (CH2)m (C3-C6cycloalkyl) wherein m =0, 1, 2 or 3, or R1 and R2 together with the nitrogen to which they are attached form an azetidine ring; each R3 is independently CF3, OCF3, C1-4alkylthio or C1-C4alkoxy; n is 1, 2 or 3; and R4 and R5, which may be the same or different, are: A—X, wherein A =—CH=CH— or —(CH2)p— where p is 0, 1 or 2; X is hydrogen, F, Cl, Br, I, CONR6R7, SO2NR6R7, SO2NHC(=O)R6, OH, C1-4alkoxy, NR8SO2R9, NO2, NR6R11, CN, CO2R10, CHO, SR10, S(O)R9 or SO2R10; R6, R7, R8 and R10 which may be the same or different, are hydrogen or C1-6alkyl optionally substituted independently by one or more R12; R9 is C1-6 alkyl optionally substituted independently by one or more R12; R11 is hydrogen, C1-6 alkyl optionally substituted independently by one or more R12, C(OType: GrantFiled: March 16, 2001Date of Patent: September 10, 2002Assignee: Pfizer Inc.Inventors: Mark David Andrews, David Hepworth, Donald Stuart Middleton, Alan Stobie
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Patent number: 6444826Abstract: 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: GrantFiled: October 31, 2001Date of Patent: September 3, 2002Assignee: Pfizer Inc.Inventors: Anthony Piscopio, Joel M. Hawkins, Stephane Caron, Sarah E. Kelly, Jeffrey W. Raggon, Michael J. Castaldi, Robert W. Dugger, Sally G. Ruggeri
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Patent number: 6440709Abstract: This invention relates to the isochroman compound of formula (I) and its pharmaceutically acceptable salts, which are useful as an amyloid aggregation inhibitor and for treating Alzheimer's disease. This invention also relates to processes for producing the isochroman compound, which comprises cultivating Penicillium simplicissimum FERM BP-6357 and then isolating the isochroman compound from the fermentation broth. The present invention also relates to a pharmaceutical composition comprising the isochroman compound.Type: GrantFiled: August 30, 2000Date of Patent: August 27, 2002Assignee: Pfizer Inc.Inventors: Hideo Hirai, Toshio Ichiba, Hiroko Tonai
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Patent number: 6436938Abstract: The present invention relates to a method of treating depression, especially refractory depression, in a mammal, including a human, by administering to the mammal a sigma receptor ligand in combination with an antidepressant agent. It also relates to pharmaceutical compositions containing a pharmaceutically acceptable carrier, a sigma receptor ligand and a serotonin reuptake inhibitor.Type: GrantFiled: October 9, 2001Date of Patent: August 20, 2002Assignee: Pfizer Inc.Inventor: Harry Ralph Howard, Jr.
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Patent number: 6387925Abstract: Two crystalline polymorphic forms of (2-Benzhydryl-1-azo-bicyclo[2.2.2]oct-3-yl)-(5-isopropyl-2-methoxybenzyl)-amine citrate monohydrate (the monohydrates) are Form A and Form B. The pharmaceutical composition containing at least one of these polymorphs has advantageous stability for formulation to treat acute emesis in patient receiving chemotherapy. The administration of this pharmaceutical composition is conventional oral by preferably tablet or capsule and intravenous. A method of making A and B Forms is also disclosed.Type: GrantFiled: May 12, 2000Date of Patent: May 14, 2002Assignee: Pfizer Inc.Inventors: George Joseph Quallich, Lewin Theophilus Wint, Peter Robert Rose, Stephen S. Massett
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Patent number: 6355825Abstract: 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: GrantFiled: March 21, 2001Date of Patent: March 12, 2002Assignee: 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
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Patent number: 6288242Abstract: 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: GrantFiled: February 23, 2000Date of Patent: September 11, 2001Assignee: 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
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Patent number: 6262067Abstract: Two crystalline polymorphic forms of (2-Benzhydryl-1-azo-bicyclo(2.2.2]Octyl-3-yl)-(5-iso-propyl-2-methoxybenzyl)amine dihydrochloride dihydrate are Form I and Form II. The pharmaceutical composition containing at least are of these polymorphs has advantageous stability for formulation to treat emesis in patients receiving chemotherapy. The administration of this pharmaceutical composition is conventional oral by preferably tablet or capsule or intravenous. A method of making Forms I and II is also disclosed.Type: GrantFiled: May 4, 2000Date of Patent: July 17, 2001Assignee: Pfizer Inc.Inventors: Douglas J. M. Allen, Troy Anthony Appleton, Michael Jon Gumkowski, David Joseph Muehlbauer, Timothy Norris
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Patent number: 6255320Abstract: A single crystalline polymorphic form (2S,3S)-N-(methoxy-5-t-butylphenylmethyl-2-diphenylmethyl-1-azobicyclo[2,2,2] octan-3-amine citrate(citrate monohydrate) and its pharmaceutical composition. The pharmaceutical composition of the polymorphic form if the citrate monohydrate has advantageous stability for formulation to treat emesis. The administration of this pharmaceutical composition is immediate release, oral dosage form preferably by tablet or capsule or intravenous.Type: GrantFiled: May 8, 2000Date of Patent: July 3, 2001Assignee: Pfizer Inc.Inventors: George Joseph Quallich, Lewin Theophilus Wint, Michael James Castaldi
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Patent number: 6242438Abstract: The present invention provides compounds of formula (I) and the pharmaceutically acceptable salts thereof. Such compounds and salts are tachykinin antagonists.Type: GrantFiled: June 1, 1998Date of Patent: June 5, 2001Assignee: Pfizer Inc.Inventors: Alexander Roderick MacKenzie, Allan Patrick Marchington, Donald Stuart Middleton, Sandra Dora Meadows
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Patent number: 6242461Abstract: This invention relates to novel aryl substituted azabenzimidazoles of Formula (I) and pharmaceutically acceptable salts thereof. or a pharmaceutically acceptable salt thereof wherein n is an integer from 1 to 4 X is CH or N; R1 is H, (C1-C6)alkyl or (C1-C6) alkoxy; R2 is H, (C1-C6)alkyl or (C1-C6) alkoxy; each R3 is independently selected from H, (C1-C6)alkyl (C1-C6) alkyloxy, (C1-C6) alkylthio, halo, nitro, cyano, ethynyl, hydroxy and trifluoromethyl; R4 is H, (C1-C6)alkyl or (C1-C6) alkoxy; R5 is H, (C1-C6)alkyl or (C1-C6) alkyloxy, trifluoromethyl; and W is N or C; Y is N (R4), N, S or O Z is R4, NR4H, O, or OH; Provided that when Y═NR4, W═C, Z═O, there is a single bond between YW and a double bond between WZ; and when Y=O or S, W═C, Z═O, there is a single bond between YW and a double bond between WZ; and when Y═N, W═N, there is a double bond between YW and Z does not exist.Type: GrantFiled: May 25, 2000Date of Patent: June 5, 2001Assignee: Pfizer Inc.Inventors: Steven W. Goldstein, William G. Stirtan, Brian A. Sherer
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Patent number: 6198000Abstract: A process for preparing a compound of the formula wherein R1, m, o and p are described below, which comprises adding a base of the formula wherein R2, R3 and R4 are as described below, to a solution comprising a compound of the formula wherein R1, m, o and p are as described below, and a halonitromethane of the formula O2NCH2X, wherein X is a halogen atom dissolved in a non-aqueous inert solvent. The compounds of formula III are useful as intermediates in the syntheses of azabicyclo quinoline carboxylic acids, and their pharmaceutically acceptable salts and prodrugs, having antibacterial activity. This invention also relates to the base of formula IV wherein each R2 is butyl, R3 is hydrogen and each R4 is t-butyl.Type: GrantFiled: September 21, 1999Date of Patent: March 6, 2001Assignee: Pfizer Inc.Inventor: Joel M. Hawkins
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Patent number: 6194578Abstract: This invention is directed to compounds of the Formula and the pharmaceutically-acceptable salts thereof, where the substituents are as defined in the Specification, which are growth hormone secretogogues and which increase the level of endogenous growth hormone. The compounds of this invention are therapeutically effective in treating osteoporosis and/or frailty, congestive heart failure, frailty associated with aging, obesity; accelerating bone fracture repair, attenuating protein catabolic response after a major operation, reducing cachexia and protein loss due to chronic illness, accelerating wound healing, or accelerating the recovery of burn patients or patients having undergone major surgery; improving muscle strength, mobility, maintenance of skin thickness, metabolic homeostasis or renal homeostasis.Type: GrantFiled: July 7, 1999Date of Patent: February 27, 2001Assignee: Pfizer Inc.Inventors: David A. Griffith, Brian S. Bronk