Patents Assigned to Pfizer
  • Patent number: 6313142
    Abstract: Methods of preparing CETP inhibitors are disclosed.
    Type: Grant
    Filed: October 10, 2000
    Date of Patent: November 6, 2001
    Assignee: Pfizer Inc.
    Inventors: David B. Damon, Robert W. Dugger
  • Patent number: 6313100
    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: January 7, 2000
    Date of Patent: November 6, 2001
    Assignee: Pfizer Inc
    Inventors: Katherine Elizabeth Brighty, Subramanian Sam Guhan, Martin Raymond Jefson, Robert Gerald Linde, III, Ellen Lester McCormick
  • Patent number: 6313312
    Abstract: Compounds of formula (I), their salts and prodrugs thereof, where the substituents are as defined herein are disclosed as opiate binding agents useful in the treatment of opiate-mediated conditions. Also described are processes for making such substances.
    Type: Grant
    Filed: December 20, 1999
    Date of Patent: November 6, 2001
    Assignee: Pfizer INC
    Inventors: Bernard Joseph Banks, Robert James Crook, Stephen Paul Gibson, Graham Lunn, Alan John Pettman
  • Patent number: 6313302
    Abstract: A compound of the following formula: and the salts thereof, wherein A is hydrogen, halo, or hydroxy; the broken line represents an optional double bond with proviso that if the broken line is a double bond, then A is absent; Ar1 is optionally substituted phenyl; Ar2 is aryl or heteroaryl selected from phenyl, napththyl, or pyridyl, the aryl or heteroaryl being optionally substituted; R1 is hydrogen, hydroxy, or C1-C4 alkyl; and R2 and R3 are independently selected from optionally substituted C1-C7 alkyl, C3-C6 cycloalkyl, C2-C6 alkenyl, C2-C6 alkynyl, or R2 and R3, together with the nitrogen atom to which they are attached, form an optionally substituted pyrrolidine. These compounds are useful as kappa agonists.
    Type: Grant
    Filed: January 26, 2001
    Date of Patent: November 6, 2001
    Assignee: Pfizer Inc.
    Inventors: Fumitaka Ito, Hiroshi Kondo
  • Patent number: 6313140
    Abstract: 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 useful for the treatment and prevention of osteoporosis, 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: Grant
    Filed: June 13, 2000
    Date of Patent: November 6, 2001
    Assignee: Pfizer Inc.
    Inventors: Philip A Carpino, Paul A DaSilva-Jardine, Bruce A Lefker, John A Ragan
  • Patent number: 6310079
    Abstract: This invention provides a compound of the following formula: or the pharmaceutically acceptable salts thereof, wherein Ar is heteroaryl; X1 and X2 are independently selected from halo, C1-C4 alkyl, hydroxy, C1-C4 alkoxy, amino, C1-C4 alkanoyl, carboxy, carbamoyl, cyano, nitro, mercapto, (C1-C4 alkyl)thio, (C1-C4 alkyl)sulfinyl, (C1-C4 alkyl)sulfonyl, aminosulfonyl, or the like; R1 is selected from hydrogen, straight or branched C1-C4 alkyl, C3-C8 cycloalkyl, C4-C8 cycloalkenyl, phenyl , heteroaryl and the like; R2 and R3 are independently selected from hydrogen, halo, C1-C4 alkyl, phenyl and the like; or R1 and R2 can form, together with the carbon atom to which they are attached, a C5-C7 cycloalkyl ring; and m and n are independently 0, 1, 2 or 3. These compounds and pharmaceutical compositions containing such compounds are useful as analgesics and anti-inflammatory agents.
    Type: Grant
    Filed: February 5, 1999
    Date of Patent: October 30, 2001
    Assignee: Pfizer Inc.
    Inventors: Yoshiyuki Okumura, Yoshinori Murata, Takashi Mano
  • Patent number: 6310075
    Abstract: Cholesteryl ester transfer protein inhibitors, pharmaceutical compositions containing such inhibitors and the use of such inhibitors to elevate certain plasma lipid levels, including high density lipoprotein-cholesterol and to lower certain other plasma lipid levels, such as LDL-cholesterol and triglycerides and accordingly to treat diseases which are exacerbated by low levels of HDL cholesterol and/or high levels of LDL-cholesterol and triglycerides, such as atherosclerosis and cardiovascular diseases in some mammals, including humans.
    Type: Grant
    Filed: September 27, 2000
    Date of Patent: October 30, 2001
    Assignee: Pfizer Inc.
    Inventors: Michael P. DeNinno, Roger B. Ruggeri, Ronald T. Wester
  • Patent number: 6310061
    Abstract: A compound of the following formula: and the salts thereof, wherein A is hydrogen, halo, or hydroxy; the broken line represents an optional double bond with proviso that if the broken line is a double bond, then A is absent; Ar1 is optionally substituted phenyl; Ar2 is aryl or heteroaryl selected from phenyl, napththyl, or pyridyl, the aryl or heteroaryl being optionally substituted; R1 is hydrogen, hydroxy, or C1-C4 alkyl; and R2 and R3 are independently selected from optionally substituted C1-C7 alkyl, C3-C6 cycloalkyl, C2-C6 alkenyl, C2-C6 alkynyl, or R2 and R3, together with the nitrogen atom to which they are attached, form an optionally substituted pyrrolidine, piperidine or morpholine ring. These compounds are useful as kappa agonists.
    Type: Grant
    Filed: January 26, 2001
    Date of Patent: October 30, 2001
    Assignee: Pfizer Inc.
    Inventors: Fumitaka Ito, Hiroshi Kondo
  • Patent number: 6307061
    Abstract: A compound of the following formula: and the salts thereof, wherein A is hydrogen, halo, hydroxy, or the like; the broken line represents an optional double bond with proviso that if the broken line is a double bond, then A is absent; Ar1 is optionally substituted phenyl or the like; Ar2 is aryl or heteroaryl selected from phenyl, napththyl, pyridyl, and the like, the aryl or heteroaryl being optionally substituted; R1 is hydrogen, hydroxy, C1-C4 alkyl, or the like; and R2 and R3 are independently selected from optionally substituted C1-C7 alkyl, C3-C6 cycloalkyl, C2-C6 alkenyl, C2-C6 alkynyl, and the like or R2 and R3, together with the nitrogen atom to which they are attached, form an optionally substituted pyrrolidine, piperidine or morpholine ring. These compounds are useful as kappa agonists.
    Type: Grant
    Filed: January 26, 2001
    Date of Patent: October 23, 2001
    Assignee: Pfizer Inc.
    Inventors: Fumitaka Ito, Hiroshi Kondo
  • Patent number: 6306875
    Abstract: 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 useful for the treatment and prevention of osteoporosis, 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, maintanence of skin thickness, metabolic homeostasis or renal homeostasis.
    Type: Grant
    Filed: June 13, 2000
    Date of Patent: October 23, 2001
    Assignee: Pfizer Inc.
    Inventors: Philip A Carpino, Paul A DaSilva-Jardine, Bruce A Lefker, John A Ragan
  • Patent number: 6306887
    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: June 23, 1999
    Date of Patent: October 23, 2001
    Assignee: Pfizer Inc
    Inventors: Louis S. Chupak, Allen J. Duplantier, Anthony J. Milici
  • Patent number: 6306864
    Abstract: The present invention relates to novel atropisomers of 2-(aryl or heteroaryl)-3-aryl-4(3H)-quinazolinones of the formula I, and their pharmaceutically acceptable salts, and pharmaceutical compositions and methods of treating neurodegenerative and CNS-trauma related conditions.
    Type: Grant
    Filed: January 13, 2000
    Date of Patent: October 23, 2001
    Assignee: Pfizer Inc.
    Inventors: Willard McKowan Welch, Jr., Keith Michael DeVries
  • Patent number: 6306852
    Abstract: Compounds of formula (I), and their pharmaceutically acceptable derivatives, wherein R1 and R2 are optional substituents and independently represent C1-6 alkyl, C2-6 alkenyl, optionally substituted by CO2H or CO2(C1-6 alkyl), C2-6 alkynyl, halogen, C1-3 perfluoroalkyl, (CH2)mAr1, (CH2)mHet1, (CH2)mCONR7R8, (CH2)mCO2R8, O(CH2)qCO2R8, (CH2)mCOR8, (CH2)mOR8, O(CH2)pOR8, (CH2)mNR7R8, CO2(CH2)qNR7R8, (CH2)mCN, S(O)nR8, SO2NR7R8, CONH(CH2)mAr1 or CONH(CH2)mHet1; R3 represents H, C1-6 alkyl, (CH2)pNR9R10, SO2R10, SO2NR9R10, (CH2)mCO2R10, C2-6 alkenyl, C2-6 alkynyl, (CH2)mCONR9R10, (CH2)mCO2R10, (CH2)pCN, (CH2)pR10 or (CH2)pOR10; R4 represents H or C1-6 alkyl; R5 represents H or OH; R6 represents phenyl optionally fused to a herterocyclic ring, the group as a whole being optionally substituted; R7-10 are fully defined herein and may independently represent Ar2 or Het2; Z represents CO2H, CONH(tetrazol-5-yl), CONHSO2O(C1-4 alkyl), CO2Ar3, CO2(C1-6 alkyl), tetrazol-5-yl, CONHSO2Ar3, CONHSO2(CH2)qAr3 o
    Type: Grant
    Filed: April 24, 2000
    Date of Patent: October 23, 2001
    Assignee: Pfizer Inc.
    Inventors: David James Rawson, Kevin Neil Dack, Roger Peter Dickinson, Kim James
  • Patent number: 6303636
    Abstract: A compound of the formula wherein R1, R2 and Q are as defined above, useful in the treatment of a condition selected from the group consisting of arthritis, cancer, tissue ulceration, macular degeneration, restenosis, periodontal disease, epidermolysis bullosa, scleritis, and other diseases characterized by matrix metalloproteinase activity, AIDS, sepsis, septic shock and other diseases involving the production of TNF.
    Type: Grant
    Filed: July 22, 1999
    Date of Patent: October 16, 2001
    Assignee: Pfizer Inc
    Inventors: Ralph Pelton Robinson, Jr., Kim Francis McClure
  • Patent number: 6303633
    Abstract: Compounds of the formula wherein ring A, ring B, ring D, R2, R3, R4, R5, R6, R11, R12, R13, E, G, X and P are as defined 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: November 11, 1999
    Date of Patent: October 16, 2001
    Assignee: Pfizer Inc
    Inventors: Yuhpyng L. Chen, Arthur A. Nagel
  • Patent number: 6303628
    Abstract: This invention provides a compound of the following formula: or the pharmaceutically acceptable salts thereof wherein A is C 1-6 alkylene or —NR1—; Z is C(═L)R2, or SO2R3; U is CH or N; W and Y are independently selected from —CH2—, O, S and —N—R1; m is 1, 2 or 3; q and r are independently 0, 1 or 2; X is independently selected from halogen, C1-4 alkyl, halo-substituted C1-4 alkyl, hydroxy, C1-4 alkoxy, halo-substituted C1-4 alkoxy or the like; n is 1 or 2; L is oxygen or sulfur; R1 is hydrogen or C1-4 alkyl; R2 is hydroxy, C1-6alkyl, halo-substituted C1-6 alkyl, C1-6 alkoxy, halo-substituted C1-6 alkoxy, C3-7 cycloalkoxy, C1-4 alkyl(C3-7 cycloalkoxy), —NR4R5 or the like; R3 is C1-6 alkyl or halo-substituted C1-6 alkyl; and R4 and R5 are independently selected from hydrogen, C1-6 alkyl and halo-substituted C1-6alkyl.
    Type: Grant
    Filed: June 28, 2000
    Date of Patent: October 16, 2001
    Assignee: Pfizer Inc
    Inventors: Kazunari Nakao, Shigeo Hayashi, Rodney W. Stevens
  • Patent number: 6303615
    Abstract: The present invention relates to novel 2,3 disubstituted-4(3H)-quinazolinone compounds of the formula I: wherein, R1, R2 and R3 are as defined in the specification; and to the pharmaceutically acceptable salts of compounds of formula I, and to pharmaceutical compositions and methods of treating neurodegenerative and CNS-trauma related conditions.
    Type: Grant
    Filed: November 23, 1999
    Date of Patent: October 16, 2001
    Assignee: Pfizer Inc
    Inventors: Mark L. Elliott, Willard M. Welch, Bertrand L. Chenard
  • 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: Stéphane Caron
  • Patent number: 6303602
    Abstract: A compound of the following formula: or a salt thereof, wherein A is hydrogen, halo, hydroxy; the broken line represents an optional double bond with proviso that if the broken line is a double bond, then A is absent; Ar1 is optionally substituted phenyl; Ar2 is aryl or heteroaryl selected from phenyl, napththyl, furanyl or thienyl, the aryl or heteroaryl being optionally substituted; R1 is hydrogen, hydroxy, or C1-C4 alkyl; and R2 and R3 are independently selected from optionally substituted C1-C7 alkyl, C3-C6 cycloalkyl, C2-C6 alkenyl, C2-C6 alkynyl, or R2 and R3, together with the nitrogen atom to which they are attached, form an optionally substituted pyrrolidine, piperidine or morpholine ring. These compounds are useful as kappa agonists.
    Type: Grant
    Filed: January 26, 2001
    Date of Patent: October 16, 2001
    Assignee: Pfizer Inc.
    Inventors: Fumitaka Ito, Hiroshi Kondo
  • Patent number: D450153
    Type: Grant
    Filed: February 28, 2001
    Date of Patent: November 6, 2001
    Assignee: Pfizer Inc.
    Inventor: Paul Knieriemen