Patents Represented by Attorney, Agent or Law Firm Grover F. Fuller, Jr.
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Patent number: 5767139Abstract: The present invention provides compounds of the formula: ##STR1## and the pharmaceutically acceptable salts thereof, together with pharmaceutically compositions containing, uses of, processes for the preparation of and intermediates used in the preparation of, such compounds.Type: GrantFiled: August 2, 1994Date of Patent: June 16, 1998Assignee: Pfizer, Inc.Inventors: Graham Nigel Maw, Julian Blagg, Colin William Greengrass, Paul William Finn
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Patent number: 5747501Abstract: 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: September 16, 1994Date of Patent: May 5, 1998Assignee: Pfizer, Inc.Inventors: John Eugene Macor, Martin James Wythes
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Patent number: 5747064Abstract: The present invention is directed to a topical composition for the treatment of psoriasis. The composition comprises a film forming agent, especially vinyl acetate crotonic acid copolymer a plasticizer, an aqueous alcoholic solution and an amount of alkali effective to prevent the gellation of the film forming agent.Type: GrantFiled: July 17, 1997Date of Patent: May 5, 1998Assignee: Pfizer Inc.Inventors: Debbie L. Burnett, Darius D. Dubash, Athanasios S. Ladas, Victor M. Wong
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Patent number: 5717102Abstract: Compounds of the formula ##STR1## where A represents a direct bond, C.sub.1 -C.sub.4 alkyl, or C.sub.1 -C.sub.4 alkenyl; n is 0, 1, or 2; R.sub.1 is hydrogen, C.sub.1 -C.sub.6 alkyl, aryl, C.sub.1 -C.sub.3 alkylaryl, C.sub.1 -C.sub.3 alkylheteroaryl, or --(CH.sub.2).sub.m R.sub.6 ; W, X, Y, and Z are each independently oxygen, sulfur, nitrogen or carbon, provided that at least one of W, X, Y or Z is nitrogen; R.sub.2, R.sub.3, R.sub.4, and R.sub.5 are each independently hydrogen, C.sub.1 -C.sub.6 alkyl, aryl, C.sub.1 -C.sub.3 alkylaryl, C.sub.1 -C.sub.3 alkylheteroaryl, halogen, cyano, trifluommethyl, nitro, --OR.sub.7, --NR.sub.7 R.sub.8, --(CH.sub.2).sub.s OR.sub.7, --SR.sub.7, --SO.sub.2 NR.sub.7 R.sub.8, --NR.sub.7 SO.sub.2 R.sub.8, --NR.sub.7 CO.sub.2 R.sub.8, --CONR.sub.7 R.sub.8, or --CO.sub.2 R.sub.7 ; one of R.sub.2 and R.sub.3, R.sub.3 and R.sub.4, or R.sub.4 and R.sub.Type: GrantFiled: December 31, 1996Date of Patent: February 10, 1998Assignee: Pfizer Inc.Inventors: John Eugene Macor, Jolanta T. Nowakowski
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Patent number: 5714628Abstract: The invention provides a process for preparing a compound of the formula: ##STR1## or a base salt thereof, wherein R.sup.2 is hydrogen or C.sub.1 -C.sub.6 alkyl optionally substituted by up to 3 substituents each independently selected from the group consisting of C.sub.1 -C.sub.6 alkoxy and C.sub.1 -C.sub.6 alkoxy(C.sub.1 -C.sub.6 alkoxy)-; and R.sup.3 is C.sub.1 -C.sub.6 alkyl or benzyl, said benzyl group being optionally ring-substituted by up to 2 nitro or C.sub.1 -C.sub.4 alkoxy substituents. comprising reacting a compound of the formula: ##STR2## wherein R.sup.1 is C.sub.1 -C.sub.4 alkyl, phenyl or benzyl or C.sub.1 -C.sub.4 alkoxy; and R.sup.2 and R.sup.3 are as previously defined for a compound of the formula (I), with hydrogen peroxide or a source of peroxide ions: said process being optionally followed by conversion of the compound of the formula (I) to a base salt thereof. The present invention also relates to novel compounds of the formula (II).Type: GrantFiled: June 28, 1996Date of Patent: February 3, 1998Assignee: Pfizer, Inc.Inventor: Stephen Challenger
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Patent number: 5698568Abstract: Quinuclidine derivatives of the formula ##STR1## and the pharmaceutically acceptable salts thereof, wherein m, P, Z, Y, R.sup.1, R.sup.2 and R.sup.3 are as defined below. The compounds are substance P antagonists and, therefore, are useful in treating gastrointestinal disorders, central nervous system disorders, inflammatory diseases, pain and migraine.Type: GrantFiled: March 14, 1995Date of Patent: December 16, 1997Assignee: Pfizer Inc.Inventor: John Adams Lowe, III
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Patent number: 5677458Abstract: Compounds of the formula ##STR1## which are intermediates in the preparation of hydantoin aldose reductase inhibitors and methods of preparing these intermediates.Type: GrantFiled: October 3, 1996Date of Patent: October 14, 1997Assignee: Pfizer Inc.Inventor: George J. Quallich
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Patent number: 5641786Abstract: Quinuclidine derivatives of the formula ##STR1## and the pharmaceutically acceptable salts thereof, wherein m, P, Z, Y, R.sup.1, R.sup.2 and R.sup.3 are as defined below. The compounds are substance P antagonist and, therefore, are useful in treating gastrointestinal disorders, central nervous system disorders, inflammatory diseases, pain and migraine.Type: GrantFiled: March 14, 1995Date of Patent: June 24, 1997Inventor: John Adams Lowe, III
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Patent number: 5639752Abstract: Compounds of the formula ##STR1## wherein Z is ##STR2## R.sub.1 is ##STR3## X is O, NH, or S; A, B, D, E, and F are each independently C, N, O, or S; wherein the remaining variables are defined in the specification, and the pharmaceutically acceptable salts thereof. These compounds are useful psychotherapeutics and are potent serotonin (5-HT.sub.1) agonists and may be used in the treatment of depression, anxiety, eating disorders, obesity, drug abuse, cluster headache, migraine, pain, chronic paroxysmal hemicrania and headache associated with vascular disorders, and other disorders arising from deficient serotonergic neurotransmission. The compounds can also be used as centrally acting antihypertensives and vasodilators.Type: GrantFiled: May 20, 1994Date of Patent: June 17, 1997Assignee: Pfizer IncInventor: John Eugene Macor
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Patent number: 5639779Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein R.sup.1 is a substituted alkylene; C.sub.3 -C.sub.7 cycloalkyl optionally substituted with HO; C.sub.3 -C.sub.6 alkenyl optionally substituted with aryl; C.sub.5 -C.sub.7 cycloalkenyl; or C.sub.3 -C.sub.6 alkynyl; R.sup.2 is H; halo; F.sub.3 C; NC; R.sup.8 R.sup.9 NOC; a substituted alkylene; R.sup.8 R.sup.9 NO.sub.2 S; R.sup.10 S(O).sub.m ; R.sup.12 CON(R.sup.11); R.sup.10 SO.sub.2 N(R.sup.11); R.sup.8 R.sup.9 NOCN(R.sup.11); R.sup.10 O.sub.2 CN(R.sup.11); R.sup.13 (CH.sub.2).sub.n CH.dbd.CH; or R.sup.7 O are selective 5-HT.sub.1 -like receptor agonists useful in the treatment of migraine, cluster headache, chronic paroxysmal hemicrania and headache associated with vascular disorders.Type: GrantFiled: October 6, 1994Date of Patent: June 17, 1997Assignee: Pfizer Inc.Inventors: Martin James Wythes, John Eugene Macor
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Patent number: 5618808Abstract: The present invention relates to novel substituted benzothiazepines and benzoxazepines of the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.7, R.sup.8, R.sup.9 and X are as defined below, and to novel intermediates used in the synthesis of such compounds.Such compounds are useful in the treatment and prevention of gastrointestinal disorders, pain and anxiety disorders.Type: GrantFiled: December 21, 1994Date of Patent: April 8, 1997Assignee: Pfizer, Inc.Inventor: Arthur A. Nagel
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Patent number: 5618834Abstract: Compounds of formula I, ##STR1## wherein R.sup.1 represents hydrogen; R.sup.2 represents hydrogen, halogen, cyano, OR.sup.4, --(CH.sub.2).sub.m CONR.sup.5 R.sup.6, --(CH.sub.2).sub.m SO.sub.2 NR.sup.5 R.sup.6, --(CH.sub.2).sub.m NR.sup.7 COR.sup.8, --(CH.sub.2).sub.m S(O).sub.x R.sup.8, --(CH.sub.2).sub.m NR.sup.7 CONR.sup.5 R.sup.6, --(CH.sub.2).sub.m NR.sup.7 COOR.sup.9 or --CH.dbd.CH(CH.sub.2).sub.y R.sup.10 ; R.sup.3 represents hydrogen or C.sub.1-6 alkyl; R.sup.4 represents hydrogen, C.sub.1-6 alkyl or aryl; R.sup.5 and R.sup.6 are independently represent hydrogen, C.sub.1-6 alkyl, aryl or (C.sub.1-3 alkyl)aryl; or R.sup.5 and R.sup.6 taken together may form a 4-, 5- or 6-membered ring; R.sup.7 and R.sup.8 independently represent hydrogen, C.sub.1-6 alkyl, aryl or (C.sub.1-3 alkyl)aryl; R.sup.9 represents hydrogen, C.sub.1-6 alkyl, aryl or (C.sub.1-3 alkyl)aryl; R.sup.10 represents --CONR.sup.5 R.sup.6, --SO.sub.2 NR.sup.5 R.sup.6, --NR.sup.7 COR.sup.8, --NR.sup.7 SO.sub.2 R.sup.8, --NR.sup.7 CONR.sup.Type: GrantFiled: November 30, 1995Date of Patent: April 8, 1997Assignee: Pfizer Inc.Inventor: Paul Butler
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Patent number: 5607960Abstract: The present invention relates to 3,5-disubstituted indole compounds which are selective agonists which act on 5-hdroxytryptamine receptors useful in the treatment of migraine.Type: GrantFiled: October 20, 1995Date of Patent: March 4, 1997Assignee: Pfizer Inc.Inventor: Martin J. Wythes
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Patent number: 5607951Abstract: Compounds of the formula ##STR1## wherein the substituents are as defined in the description and the pharmaceutically acceptable salts thereof are new. These compounds are useful psychotherapeutics and are potent serotonin (5-HT.sub.1) agonists and may be used in the treatment of depression, anxiety, eating disorders, obesity, drug abuse, cluster headache, migraine, pain, chronic paroxysmal hemicrania and headache associated with vascular disorders, and other disorders arising from deficient serotonergic neurotransmission. The compounds can also be used as centrally acting antihypertensives and vasodilators. A process for forming indoles by transition metal catalyzed cyclization of a dihalogenated intermediate.Type: GrantFiled: June 6, 1995Date of Patent: March 4, 1997Assignee: Pfizer IncInventors: John E. Macor, Martin J. Wythes
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Patent number: 5608071Abstract: Compounds of the formula ##STR1## which are intermediates in the preparation of hydantoin aldose reductase inhibitors and methods of preparing these intermediates.Type: GrantFiled: April 26, 1995Date of Patent: March 4, 1997Assignee: Pfizer Inc.Inventor: George J. Quallich
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Patent number: 5594014Abstract: Compounds of the formula (I) where A represents a direct bond, C.sub.1 -C.sub.4 alkyl, or C.sub.1 -C.sub.4 alkenyl; n is 0, 1, or 2; W, X, Y, and Z are each independently oxygen, sulfur, nitrogen or carbon, provided that at least one of W, X, Y, or Z is nitrogen. These compounds are useful psychotherapeutics and are potent serotonin (5-HT.sub.1) agonists and may be used in the treatment of depression, anxiety, eating disorders, obesity, drug abuse, cluster headache, migraine, pain and chronic paroxysmal hemicrania and headache associated with vascular disorders, and other disorders arising from deficient serotonergic neurotransmission. The compounds can also be used as centrally acting antihypertensives and vasodilators.Type: GrantFiled: August 19, 1994Date of Patent: January 14, 1997Assignee: Pfizer IncInventors: John E. Macor, Jolanta T. Nowakowski
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Patent number: 5578612Abstract: Compounds of the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, X and n are as defined in the claims and the pharmaceutically acceptable salts thereof are new. These compounds are useful psychotherapeutics and are potent serotonin (5-HT.sub.1) agonists and may be used in the treatment of depression, anxiety, eating disorders, obesity, drug abuse, cluster headache, migraine, pain, chronic paroxysmal hemicrania and headache associated with vascular disorders, and other disorders arising from deficient serotonergic neurotransmission. The compounds can also be used as centrally acting hypertensives and vasodilators. A process for forming indoles by transition metal catalyzed cyclization of dihalogenated intermediate is also disclosed.Type: GrantFiled: June 6, 1995Date of Patent: November 26, 1996Assignee: Pfizer Inc.Inventors: John E. Macor, Martin J. Wythes
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Patent number: 5560859Abstract: A post-foaming gel shaving composition is disclosed which contains from about 40 to about 90 percent by weight water; from about 4 to about 25 percent by weight water-soluble soap; from about 0.5 to about 12 percent by weight aliphatic liquid post-foaming agent selected from the group consisting of saturated aliphatic hydrocarbons; from about 0.01 to about 5 percent by weight of at least one water-soluble gelling agent forming in said composition a gel having a yield value sufficiently high to restrain said composition from foaming for at least about 60 seconds; and from about 0.1 to about 2 percent by weight of a poly(ethylene oxide) having an average molecular weight of at least 2.times.10.sup.5.Type: GrantFiled: June 1, 1995Date of Patent: October 1, 1996Assignee: Pfizer Inc.Inventors: Barbara A. Hartmann, Athanasios S. Ladas, Dino G. Muccia
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Patent number: 5559129Abstract: Compounds of the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, X and n are as defined in the claims and the pharmaceutically acceptable salts thereof are new. These compounds are useful psychotherapeutics and are potent serotonin (5-HT.sub.1) agonists and may be used in the treatment of depression, anxiety, eating disorders, obesity, drug abuse, cluster headache, migraine, pain, chronic paroxysmal hemicrania and headache associated with vascular disorders, and other disorders arising from deficient serotonergic neurotransmission. The compounds can also be used as centrally acting hypertensives and vasodilators. A process for forming indoles by transition metal catalyzed cyclization of dihalogenated intermediate is also disclosed.Type: GrantFiled: June 6, 1995Date of Patent: September 24, 1996Assignee: Pfizer IncInventors: John E. Macor, Martin J. Wythes
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Patent number: 5559246Abstract: Compounds of the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, X and n are as defined in the claims and the pharmaceutically acceptable salts thereof are new. These compounds are useful psychotherapeutics and are potent serotonin (5-HT.sub.1) agonists and may be used in the treatment of depression, anxiety, eating disorders, obesity, drug abuse, cluster headache, migraine, pain, chronic paroxysmal hemicrania and headache associated with vascular disorders, and other disorders arising from deficient serotonergic neurotransmission. The compounds can also be used as centrally acting hypertensives and vasodilators. A process for forming indoles by transition metal catalyzed cyclization of dihalogenated intermediate is also disclosed.Type: GrantFiled: June 6, 1995Date of Patent: September 24, 1996Assignee: Pfizer Inc.Inventor: John E. Macor