Patents Represented by Attorney, Agent or Law Firm Grover F. Fuller, Jr.
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Patent number: 6316631Abstract: 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: GrantFiled: March 4, 1999Date of Patent: November 13, 2001Assignee: Pfizer Inc.Inventors: Yuhpyng L. Chen, Sally Gut Ruggeri
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Patent number: 6313302Abstract: 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: GrantFiled: January 26, 2001Date of Patent: November 6, 2001Assignee: Pfizer Inc.Inventors: Fumitaka Ito, Hiroshi Kondo
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Patent number: 6310061Abstract: 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: GrantFiled: January 26, 2001Date of Patent: October 30, 2001Assignee: Pfizer Inc.Inventors: Fumitaka Ito, Hiroshi Kondo
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Patent number: 6307061Abstract: 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: GrantFiled: January 26, 2001Date of Patent: October 23, 2001Assignee: Pfizer Inc.Inventors: Fumitaka Ito, Hiroshi Kondo
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Patent number: 6303602Abstract: 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: GrantFiled: January 26, 2001Date of Patent: October 16, 2001Assignee: Pfizer Inc.Inventors: Fumitaka Ito, Hiroshi Kondo
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Patent number: 6294569Abstract: 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: GrantFiled: January 26, 2001Date of Patent: September 25, 2001Assignee: Pfizer Inc.Inventors: Fumitaka Ito, Hiroshi Kondo
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Patent number: 6294557Abstract: 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: GrantFiled: January 26, 2001Date of Patent: September 25, 2001Assignee: Pfizer Inc.Inventors: Fumitaka Ito, Hiroshi Kondo
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Patent number: 6261540Abstract: Oral rinse and dentifrice compositions, comprising a mint flavor, mint flavor ingredient, citrus flavor, citrus flavor ingredient, phenolic ingredient, or mixtures thereof, said phenolic ingredient selected from the group consisting of menthol, eucalyptol, methyl salicylate, thymol, triclosan, and mixtures thereof; a cyclodextrin selected from the group consisting of hydroxypropyl &bgr;-cyclodextrin, hydroxyethyl &bgr;-cyclodextrin, hydroxypropyl &ggr;-cyclodextrin, hydroxyethyl &ggr;-cyclodextrin, &agr;-cyclodextrin, methyl &bgr;-cyclodextrin, and mixtures thereof; and from about 0.1% by weight to about 10% by weight of hydrogen peroxide. These compositions are useful in retarding the development of plaque, treating gingivitis, and in treating the presence of micro-organisms in the oral cavity.Type: GrantFiled: October 20, 1998Date of Patent: July 17, 2001Assignee: Warner-Lambert CompanyInventor: Dennis G. A. Nelson
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Patent number: 6245321Abstract: Oral rinse and dentifrice compositions, comprising a phenolic selected from the group consisting of menthol, eucalyptol, methyl salicylate, thymol, triclosan, and mixtures thereof; and a cyclodextrin selected from the group consisting of hydroxypropyl &bgr;-cyclodextrin, hydroxyethyl &bgr;-cyclodextrin, hydroxypropyl &ggr;-cyclodextrin, hydroxyethyl &ggr;-cyclodextrin, &agr;-cyclodextrin, methyl &bgr;-cyclodextrin, and mixtures thereof. These compositions are useful in retarding the development of plaque, treating gingivitis, and in treating the presence of micro-organisms in the oral cavity.Type: GrantFiled: April 23, 1999Date of Patent: June 12, 2001Assignee: Pfizer Inc.Inventors: Dennis G. A. Nelson, Craig J. Sheehan
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Patent number: 6235267Abstract: An oral rinse, dentifrice, or oral gel composition comprising: a) about 0.01 weight % to about 5 weight % of a citrus flavor, citrus flavor ingredient, or mixtures thereof; b) about 0.01 weight % to about 5 weight % of a phenolic, said phenolic selected from the group consisting of menthol, eucalyptol, methyl salicylate, thymol, triclosan, and mixtures thereof; and c) an orally acceptable carrier. The claimed composition is useful in retarding the development of plaque, treating gingivitis, and reducing the viable population of micro-organisms in the oral cavity of a mammal.Type: GrantFiled: April 23, 1999Date of Patent: May 22, 2001Assignee: Pfizer Inc.Inventors: Patricia A. Delli Santi, Dennis G. A. Nelson
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Patent number: 6225351Abstract: 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: GrantFiled: July 6, 1998Date of Patent: May 1, 2001Assignee: Pfizer Inc.Inventor: Edward F. Kleinman
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Patent number: 6201007Abstract: A compound of the following formula: and the salts thereof wherein A is hydrogen, halo, or hydroxy, 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: GrantFiled: March 12, 1999Date of Patent: March 13, 2001Assignee: Pfizer Inc.Inventors: Fumitaka Ito, Hiroshi Kondo
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Patent number: 6150388Abstract: Compounds of the formula ##STR1## where W is ##STR2## n is 0, 1, or 2; m is 0, 1, 2, or 3; Y and G are each independently oxygen or sulfur; Z is --O--, --S--, --NH, or --CH.sub.2 ; R.sub.1 is hydrogen, C.sub.1 to C.sub.8 alkyl, substituted C.sub.1 to C.sub.8 alkyl substituted with one hydroxy, C.sub.3 to C.sub.8 alkenyl, C.sub.3 to C.sub.8 alkynyl, aryl, C.sub.1 to C.sub.3 alkylaryl, C.sub.1 to C.sub.3 alkylheteroaryl, or --Q--R.sub.4 ; R.sub.2 and R.sub.3 are each independently hydrogen, C.sub.1 to C.sub.6 alkyl, aryl, C.sub.1 to C.sub.3 alkylaryl, or C.sub.1 to C.sub.3 alkylheteroaryl; R.sub.4 is cyano, trifluoromethyl, --COR.sub.9, --CO.sub.2 R.sub.9, --CONR.sub.9 R.sub.10, --OR.sub.9, --SO.sub.2 NR.sub.9 R.sub.10, or --S(O).sub.q R.sub.9 ; R.sub.9 and R.sub.10 are each independently hydrogen, C.sub.1 to C.sub.8 alkyl, C.sub.1 to C.sub.3 alkylaryl, aryl, or R.sub.9 and R.sub.Type: GrantFiled: April 14, 1998Date of Patent: November 21, 2000Assignee: Pfizer, Inc.Inventors: John Eugene Macor, Martin James Wythes
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Patent number: 6113893Abstract: The present invention is directed to a topical composition for the treatment of psoriasis. The composition comprises a film forming agent, a plasticizer, an aqueous alcoholic solution and an amount of alkali effective to prevent the gellation of the film forming agent.Type: GrantFiled: July 1, 1998Date of Patent: September 5, 2000Assignee: Pfizer Inc.Inventors: Debbie L. Burnett, Victor M. Wong, Darius D. Dubash, Athanasios S. Ladas
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Patent number: 6110940Abstract: The present invention relates to hydrobromide salts of 3-(N-methyl-2(R)-pyrrolidinylmethyl)-5-(2-phenylsulphonylethyl)-1H-indole having the formula (I): ##STR1##Type: GrantFiled: February 2, 1997Date of Patent: August 29, 2000Assignee: Pfizer Inc.Inventors: Valerie Denise Harding, Ross James Macrae, Ronald James Ogilvie
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Patent number: 6093822Type: GrantFiled: November 13, 1998Date of Patent: July 25, 2000Assignee: Pfizer Inc.Inventor: John Eugene Macor
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Patent number: 5994387Abstract: The fumarate salt of (R)-5-(methylaminosulphonylmethyl)-3-(N-methylpyrrolidin-2-ylmethyl)-1H-in dole, useful in the treatment of migraine.Type: GrantFiled: November 12, 1997Date of Patent: November 30, 1999Assignee: Pfizer Inc.Inventor: Martin James Wythes
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Patent number: D430703Type: GrantFiled: October 1, 1999Date of Patent: September 5, 2000Assignee: Pfizer Inc.Inventors: Stuart M. Leslie, Charles Curtiss, Chen Jiang
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Patent number: D431093Type: GrantFiled: October 1, 1999Date of Patent: September 19, 2000Assignee: Pfizer Inc.Inventors: Stuart M. Leslie, Charles Curtiss, Chen Jiang
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Patent number: D432714Type: GrantFiled: October 1, 1999Date of Patent: October 24, 2000Assignee: Pfizer Inc.Inventors: Stuart M. Leslie, Charles Curtiss, Chen Jiang