Patents Represented by Attorney Richard K. Jackson
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Patent number: 5684039Abstract: Compounds of the formula: ##STR1## in which R is a straight or branched chain alkyl group of 1 to 6 carbon atoms, hydroxyalkyl of 1 to 6 carbon atoms or a cycloalkyl group of 3 to 8 carbon atoms; or a pharmaceutically acceptable salt thereof are inhibitors of dopamine synthesis and release, useful in the treatment of schizophrenia, Parkinson's Disease, Tourette's Syndrome, alcohol addiction, cocaine addiction, and addiction to analagous drugs.Type: GrantFiled: July 19, 1996Date of Patent: November 4, 1997Assignee: American Home Products CorporationInventor: Richard E. Mewshaw
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Patent number: 5684030Abstract: Disclosed herein are compounds of the formula: ##STR1## where R.sub.1 is substituted phenyl in which the substituents are one or two halogens, alkyl groups, carboxyl groups or alkoxycarbonyl groups;R.sub.2 is H or alkyl;R.sub.3 and R.sub.4 are, independently, H, alkyl, halogen or nitro;and n is 1, 2 or 3;or a pharmaceutically acceptable salt thereof, which are useful as inhibitors of smooth muscle cell proliferation.Type: GrantFiled: June 7, 1995Date of Patent: November 4, 1997Assignee: American Home Products CorporationInventors: Hassan M. Elokdah, Sie-Yearl Chai, Theodore S. Sulkowski
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Patent number: 5670667Abstract: Compounds of the formula: ##STR1## in which Z is hydrogen or a halogen; n is one of the integers 1, 2, 3, or 4; m is one of the integers 0 or 1; R is a substituted or unsubstituted aryl group in which the substituents are, independently, one or two members selected from the group consisting of alkyl, hydroxy, halo or amino groups; R.sup.2 is hydrogen or alkyl; or a pharmaceutically acceptable salt thereof, are inhibitors of dopamine synthesis and release, useful in the treatment of schizophrenia, Parkinson's Disease, Tourette's Syndrome, alcohol addiction, cocaine addiction, and addiction to analagous drugs.Type: GrantFiled: April 10, 1996Date of Patent: September 23, 1997Assignee: American Home Products CorporationInventor: Richard E. Mewshaw
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Patent number: 5668144Abstract: The compounds of the formula: ##STR1## where R is H, alkyl, haloalkyl, cycloalkyl, alkenyl or alkynyl; Y is oxygen, sulfur or NR.sub.2 where R.sub.2 is H or alkyl; or a pharmaceutically acceptable salt thereof, are useful centrally active muscarinic agents.Type: GrantFiled: October 30, 1996Date of Patent: September 16, 1997Assignee: American Home Products CorporationInventors: Annmarie L. Sabb, Reinhardt P. Stein
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Patent number: 5663194Abstract: Described herein are compounds of the formula: ##STR1## in which n is 1, 2 or 3; m is 0 or 1; and R is a substituted or unsubstituted phenyl group in which the substitutents are, independently, one or two members selected from the group consisting of alkyl, hydroxy, halo or amino groups or R is alkyl of 1 to 6 carbon atoms or hydroxyalkyl of 1 to 6 carbon atoms; or a pharmaceutically acceptable salt thereof, which are inhibitors of dopamine synthesis and release, and are useful in the treatment of schizophrenia, Parkinson's Disease, Tourette's Syndrome, alcohol addiction, cocaine addiction, and addiction to analagous drugs.Type: GrantFiled: July 19, 1996Date of Patent: September 2, 1997Inventor: Richard E. Mewshaw
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Patent number: 5663363Abstract: The compound of formula I ##STR1## in which R is alkynyl; and X and Y are, independently, alkyl, halo, perfluoralkyl, perfluoralkoxy, or, taken together, X and Y are ortho substituted trimethylene or tetramethylene are useful for increasing blood serum HDL levels.Type: GrantFiled: November 21, 1996Date of Patent: September 2, 1997Assignee: American Home Products CorporationInventors: Hassan M. Elokdah, Sie-Yearl Chai, Theodore S. Sulkowski, Donald P. Strike
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Patent number: 5637731Abstract: This disclosure describes novel substituted oxotremorine derivatives of formula I having nitrogen, oxygen or sulfur groups and the prodrug forms of these derivatives. The compounds have cholinergic activity. Also disclosed are methods for treating diseases of the central nervous system in mammals employing the compounds, pharmaceutical preparations containing the compounds and the processes for the production of the compounds.Type: GrantFiled: April 30, 1996Date of Patent: June 10, 1997Assignee: American Home Products CorporationInventors: Eugene J. Trybulski, Richard H. Kramss, Herbert J. Brabander
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Patent number: 5605909Abstract: The compounds of formula I are smooth muscle relaxants: ##STR1## wherein R.sub.1 is hydrogen, alkyl, cycloalkyl, alkanoyl, alkylsulfonyl, aroyl, arylalkenoyl, arylsulfonyl, arylalkanoyl or arylalkylsulfonyl; R.sub.Type: GrantFiled: February 14, 1996Date of Patent: February 25, 1997Assignee: American Home Products CorporationInventors: John A. Butera, Schuyler A. Antane, Bradford H. Hirth
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Patent number: 5602151Abstract: The compounds of the formula: ##STR1## in which X is ##STR2## where R.sup.7 is hydrogen, alkyl, hydroxy, alkanoyloxy, hydroxyalkyl, hydroxycarbonyl, alkoxycarbonyl, phenyl or substituted phenyl, in which the substituent is alkyl, alkoxy, halo, nitro, cyano, haloalkyl, perhaloalkyl or dialkylaminoalkyl; R.sup.8 is hydrogen or alkyl or R.sup.7 and R.sup.8 taken together are polymethylene; R.sup.9 is hydrogen, alkyl, phenyl or substituted phenyl, in which the substituent is alkyl, alkoxy, halo, nitro, cyano or perhaloalkyl; R.sup.10 is hydrogen, alkyl or gemdialkyl; n is one of the integers 0, 1 or 2; and R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are, independently, hydrogen, alkyl, alkoxy, halo, nitro, cyano or perhaloalkyl, alkoxycarbonyl or hydroxycarbonyl; and when X is --NR.sup.9 -- or R.sup.7 is an amino alkyl group, a pharmaceutically acceptable salt thereof; are useful as inhibitors of cholesterol ester hydrolase.Type: GrantFiled: December 15, 1995Date of Patent: February 11, 1997Assignee: American Home Products CorporationInventors: Richard E. Mewshaw, Thomas J. Commons, Donald P. Strike
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Patent number: 5602128Abstract: The compounds ##STR1## where R and R.sup.6 are members independently selected from the group consisting of H, CN, OR.sup.2, NO.sub.2, NR.sup.2 R.sup.3, NR.sup.2 COR.sup.3, NR.sup.2 COOR.sup.3, COR.sup.2, COOR.sup.2, CONR.sup.2 R.sup.3, SR.sup.2, SOR.sup.2, SO.sub.2 R.sup.2, SO.sub.2 NR.sup.2 R.sup.3, alkyl, alkenyl, alkynyl, perhaloalkyl, and a halogen; in which R.sup.2 and R.sup.3 are alkyl, alkenyl, alkynyl, phenyl, or benzyl; R.sup.4 is a member selected from the group consisting of H, alkyl, heteroalkyl, in which the hetero atom is oxygen, sulfur or nitrogen, alkenyl and alkynyl; R.sup.5 is ##STR2## where X is O, S or NR.sup.7 and R.sup.7 is H or alkyl and n is 1, 2, 3, 4, 5, or 6; or a pharmaceutically acceptable salt thereof, are useful anxiolytic/antidepressant agents.Type: GrantFiled: December 2, 1994Date of Patent: February 11, 1997Assignee: American Home Products CorporationInventors: Reinhardt B. Baudy, Scott C. Berta
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Patent number: 5599829Abstract: A method for increasing blood serum HDL cholesterol levels in a mammal in need of increased HDL cholesterol blood serum levels, which comprises administering to said mammal, an effective amount of a compound of formula I: ##STR1## wherein R is phenyl or phenyl optionally substituted with one or more groups selected from halogen, alkyl, perfluoroalkyl, alkoxy, perfluoroalkoxy, hydroxy, alkanoyloxy, aroyloxy or arylalkanoyloxy; R.sup.3 is alkyl, aryl or arylalkyl; or a pharmaceutically acceptable salt thereof.Type: GrantFiled: November 28, 1995Date of Patent: February 4, 1997Assignee: American Home Products CorporationInventors: Hassan M. Elokdah, Theodore S. Sulkowski, Donald P. Strike
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Patent number: 5591823Abstract: Chimeric DNA fragments are provided which include a nucleotide sequence substantially the same as that which codes for the HA surface protein of an influenza A virus having five immunodominant antigenic sites, wherein a nucleotide sequence substantially the same as that which codes for a foreign epitope is inserted into the nucleotide sequence of an antigenic site. Corresponding chimeric peptides, expression vectors, and transformed hosts are provided as well. These peptides are useful in providing vaccines against the respective antigens and in test kits to detect the exposure to such antigens. Additionally, these peptides or their corresponding antibodies are useful in methods of treatment and prevention of the manifestations of exposure to these antigens, including immunotherapy.Type: GrantFiled: December 17, 1993Date of Patent: January 7, 1997Assignee: American Home Products CorporationInventors: Paul P. Hung, Shaw-Guang L. Lee, Narender K. Kalyan
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Patent number: 5554607Abstract: A method for increasing the HDL cholesterol concentration in the blood of a mammal in need of increased HDL cholesterol blood concentration, which comprises administering to said mammal, orally or parenterally, a compound of formula I: ##STR1## wherein R is alkyl; a substituted or unsubstituted aromatic N, O or S heterocycle; substituted or unsubstituted aryl, arylalkyl, benzhydryl or indanyl, in which the substituents are one to three members independently selected from the group consisting of alkyl, alkoxy, alkylthio, alkenyl, alkynyl, halo, perfluoroalkyl, perfluoroalkyl or hydroxy; and R.sup.1 is aryl, alkyl, alkenyl, alkynyl or substituted aryl where the substituents are one to three members independently selected from the group consisting of alkyl, alkoxy, alkylthio, alkenyl, alkynyl, halo, perfluoroalkyl, perfluoroalkoxy or hydroxy.Type: GrantFiled: November 28, 1995Date of Patent: September 10, 1996Assignee: American Home Products CorporationInventors: Hassan M. Elokdah, Sie-Yearl Chai, Theodore S. Sulkowski, Donald P. Strike
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Patent number: 5550257Abstract: This disclosure describes novel substituted oxotremorine derivatives of formula I having nitrogen, oxygen or sulfur groups and the prodrug forms of these derivatives. The compounds have cholinergic activity. Also disclosed are methods for treating diseases of the central nervous system in mammals employing the compounds, pharmaceutical preparations containing the compounds and the processes for the production of the compounds.Type: GrantFiled: February 22, 1995Date of Patent: August 27, 1996Assignee: American Cyanamid CompanyInventors: Eugene J. Trybulski, Richard H. Kramss, Herbert J. Brabander
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Patent number: 5547948Abstract: A sugar coating composition for application to a compressed medicinal tablet comprising a sugar, a dose of a hormonal steroid and a steroid release rate controlling amount of microcrystalline cellulose.Type: GrantFiled: January 17, 1995Date of Patent: August 20, 1996Assignee: American Home Products CorporationInventor: Reginald J. Barcomb
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Patent number: 5541199Abstract: Compounds of the formula: ##STR1## in which n is one of the integers 1, 2, 3,or 4; m is one of the integers 0 or 1; R is ##STR2## or a pharmaceutically acceptable salt thereof, are inhibitors of dopamine synthesis and release, useful in the treatment of schizophrenia, Parkinson's Disease, Tourette's Syndrome, alcohol addiction, cocaine addiction, and addiction to analagous drugs.Type: GrantFiled: June 2, 1995Date of Patent: July 30, 1996Assignee: American Home Products CorporationInventor: Richard E. Mewshaw
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Patent number: 5538977Abstract: Disclosed are 3-substituted-7-[3-(imidazol-1-yl)phenyl]-pyrazolo[1,5-a]pyrimidines of the formula: ##STR1## wherein R.sup.1, R.sup.3 and R.sup.4 are defined in the specification which compounds have anxiolytic, anti-convulsant, sedative-hypnotic and skeletal muscle relaxant activity.Type: GrantFiled: March 17, 1995Date of Patent: July 23, 1996Assignee: American Cyanamid CompanyInventors: John P. Dusza, Jay D. Albright, Andrew S. Tomcufcik
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Patent number: 5536741Abstract: The compound of the formula: ##STR1## wherein R.sub.1 and R.sub.2 are, independent from each other, hydrogen, alkyl or cyclic or bicyclic alkyl; R.sub.3 is an acyl substituent selected from the group consisting of formyl, alkanoyl, alkenoyl, alkylsulfonyl, aroyl, arylalkenoyl, arylsulfonyl, arylalkanoyl or arylalkylsulfonyl; A is selected from the group consisting of: ##STR2## wherein R.sub.4 is hydrogen, alkyl, perfluoroalkyl, alkoxy, perfluoroalkoxy, amino, alkylamino, dialkylamino, alkylsulfonamido, alkylcarboxamido, nitro, cyano or carboxyl; or a pharmaceutically acceptable salt thereof, are smooth muscle relaxants.Type: GrantFiled: May 31, 1995Date of Patent: July 16, 1996Assignee: American Home Products CorporationInventors: Madelene M. Antane, John A. Butera, Bradford H. Hirth, Schuyler A. Antane
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Patent number: 5536731Abstract: The compounds of the formula: ##STR1## wherein R.sub.1 and R.sub.2 are, independent from each other, hydrogen, alkyl, or cyclic or bicyclic alkyl; R.sub.3 is an acyl substituent selected from the group consisting of formyl, alkanoyl, alkenoyl, alkylsulfonyl, aroyl, arylalkenoyl, arylsulfonyl, arylalkanoyl or arylalkylsulfonyl; A is selected from the group consisting of: ##STR2## wherein R.sub.4 is hydrogen, alkyl, perfluoroalkyl, alkoxy, perfluoroalkoxy, amino, alkylamino, dialkylamino, alkylsulfonamido, alkylcarboxamido, nitro, cyano or carboxyl; or a pharmaceutically acceptable salt thereof, are smooth muscle relaxants.Type: GrantFiled: May 31, 1995Date of Patent: July 16, 1996Assignee: American Home Products CorporationInventors: Madelene M. Antane, John A. Butera, Bradford H. Hirth, Schuyler A. Antane
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Patent number: 5532245Abstract: The compounds of the formula: ##STR1## wherein R.sub.1 is hydrogen, straight or branched chain alkyl, cyclic or bicyclic alkyl, alkanoyl, alkylsulfonyl, aroyl, arylalkenoyl, arylsulfonyl, arylalkanoyl or arylalkylsulfonyl; R.sub.2 is hydrogen, straight or branched chain alkyl or cyclic or bicyclic alkyl; A is selected from the following: ##STR2## wherein R.sub.9 is hydrogen, alkyl, perfluoroalkyl, alkoxy, perfluoroalkoxy, amino, mono- or dialkylamino, alkylsulfonamido, alkylcarboxamido, nitro, cyano, carboxyl, chloro, bromo, fluoro or iodo; n is an integer from 0 to 6; R.sub.3 and R.sub.4, independent from each other, are hydrogen, straight or branched chain alkyl, cyclic or bicyclic alkyl, perfluoroalkyl, hydroxyalkyl, alkoxyalkyl, fluoro, or, when taken together, form a spirocyclic ring; R.sub.5 and R.sub.Type: GrantFiled: June 7, 1995Date of Patent: July 2, 1996Assignee: American Home Products CorporationInventors: John A. Butera, Schuyler A. Antane, Bradford H. Hirth