Patents Represented by Attorney Richard K. Jackson
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Patent number: 5530025Abstract: The compounds of formula I: ##STR1## wherein R.sub.1 and R.sub.2 are hydrogen, alkyl or cyclic or bicyclic alkyl; R.sub.3 is formyl, alkanoyl, alkenoyl, alkylsulfonyl, aroyl, arylalkenoyl, arylsulfonyl arylalkanoyl or arylalkylsulfonyl; A is a substituted phenyl group of the following formula: ##STR2## wherein R.sub.5 is cyano and R.sub.6 is alkyl, chloro, bromo, fluoro or iodo and pharmaceutically acceptable salts thereof, are smooth muscle relaxants.Type: GrantFiled: June 2, 1995Date of Patent: June 25, 1996Assignee: American Home Products CorporationInventors: Madelene M. Antane, John A. Butera, Bradford H. Hirth, Schuyler A. Antane
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Patent number: 5527794Abstract: The compound of the formula: ##STR1## where R.sub.1 and R.sub.5 are independently hydrogen, fluorine, chlorine, bromine, iodine, trifluoromethyl, cyano, nitro, CO.sub.2 H, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.10 alkenyl, C.sub.1 -C.sub.6 alkoxy, C.sub.3 -C.sub.8 cycloalkyl, cycloalkylalkyl, C.sub.3 -C.sub.8 cycloalkyloxy, C.sub.2 -C.sub.7 alkylcarbonyl, C.sub.2 -C.sub.7 alkylcarbonyloxy, C.sub.2 -C.sub.7 alkoxycarbonyl, mono- or di-alkylaminocarbonyl, tetrazolyl, --OH, --(CH.sub.2).sub.1-6 OH, --SH, --NH.sub.2 or --(CH.sub.2).sub.1-6 NR.sub.8 R.sub.9 where R.sub.8 is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.7 alkylcarbonyl, C.sub.2 -C.sub.7 alkoxycarbonyl and R.sub.9 is hydrogen or C.sub.1 -C.sub.6 alkyl; R.sub.2 is hydrogen or C.sub.1 -C.sub.6 alkyl; R.sub.3 and R.sub.4 are hydrogen or taken together with the carbon atoms to which they are attached form a double bond; R.sub.6 and R.sub.7 are independently H, C.sub.1 -C.sub.10 alkyl, C.sub.2 -C.sub.10 alkenyl, C.sub.3 -C.sub.Type: GrantFiled: May 23, 1995Date of Patent: June 18, 1996Assignee: American Home Products CorporationInventors: Thomas J. Commons, Christa M. LaClair, Susan Christman
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Patent number: 5523427Abstract: The solvate 3.beta.,5.alpha.,6.beta.-trihydroxy-6.alpha.,17.alpha.-dimethylpregnan-20- one monomethanolate, a crystalline intermediate in the manufacture of medrogestone, and a method for its production by displacing the solvent in a solution of 3.beta.,5.alpha.,6.beta.-trihydroxy-6.alpha.,17.alpha.-dimethylpregnan-20- one with methanol are disclosed.Type: GrantFiled: March 14, 1995Date of Patent: June 4, 1996Assignee: American Home Products CorporationInventor: Michael W. Winkley
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Patent number: 5519025Abstract: This invention provides anxiolytic/antidepressant agents of the formula: ##STR1## in which R.sup.1 is alkyl;R.sup.2 and R.sup.3 are alkyl or taken together they are polymethylene;R.sup.4 is hydrogen or alkyl;R.sup.5 is phenyl, benzyl, substituted phenyl, or substituted benzyl in which the substituents are hydroxy, halo, alkoxy, trifluoromethyl, nitro, cyano, alkoxycarbonyl, amino or dialkylamino;or a pharmaceutically acceptable salt thereof.Type: GrantFiled: April 10, 1995Date of Patent: May 21, 1996Assignee: American Home Products CorporationInventors: John P. Yardley, Horace Fletcher, III
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Patent number: 5519153Abstract: A process for the production of 6,17.alpha.-dimethylpregna-4,6-diene-3,20-dione which comprises isolating 3.beta.,5.alpha., 6.beta.-trihydroxy- 6.alpha.,17.alpha.- dimethylpregnan-20-one monomethanolate from the solution of a Grignard reaction product of 3.beta.,5.alpha.-dihydroxy -17.alpha.-methyl-17.beta.-carbomethoxyandrostane-6-one and a methylmagnesium halide by solvent displacement with methanol; oxidizing the monomethanolate to the 3,20-dione; dehydrating the said 3,20-dione to the 4-ene-3,20-dione; dehydrating the 4-ene-3,20 dione; removing a 6-methylene-4-ene-3,20-dione byproduct and isolating the desired product.Type: GrantFiled: March 14, 1995Date of Patent: May 21, 1996Assignee: American Home Products CorporationInventor: Michael W. Winkley
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Patent number: 5512574Abstract: The compound of the formula: ##STR1## in which Y is oxygen or sulfur; A is oxygen, sulfur or --NR.sub.2, where R.sub.2 is hydrogen or alkyl; R is --CH.sub.2 CH.sub.3, --CH.sub.2 CH.sub.2 CH.sub.3, --CH(CH.sub.3).sub.2, --CH.sub.2 CH(CH.sub.3).sub.2, --CH.sub.2 CF.sub.3, --CH.sub.2 CH.sub.2 CF.sub.3, --CH(CF.sub.3).sub.2, --CH.sub.2 CH(CF.sub.3).sub.2, --C.sub.3 H.sub.5, --CH.sub.2 C.sub.3 H.sub.5, --CH.sub.2 CH.sub.2 C.sub.3 H.sub.5, --C.sub.4 H.sub.7, --CH.sub.2 C.sub.4 H.sub.7, --C.sub.5 H.sub.9, --CH.sub.2 C.sub.9, --C.sub.6 H.sub.10, --CH.sub.2 C.sub.6 H.sub.10, --C.sub.4 H.sub.3 S, --CH.sub.2 C.sub.4 H.sub.3 S, --C.sub.6 H.sub.5 or --CH.sub.2 C.sub.6 H.sub.5 ; and n is one of the integers 1 or 2; or a pharmaceutically acceptable salt thereof are centrally active muscarinic agents.Type: GrantFiled: March 31, 1995Date of Patent: April 30, 1996Assignee: American Home Products CorporationInventors: George E. M. Husbands, Joseph Tokolics
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Patent number: 5512585Abstract: The compound of the formula: ##STR1## wherein: R.sub.1 and R.sub.2 are, independent from each other, hydrogen, C.sub.1-10 straight chain alkyl, C.sub.1-10 branched alkyl, or C.sub.3-10 cyclic or bicyclic alkyl;R.sub.3 is an acyl substituent selected from the group consisting of formyl, alkanoyl of 2 to 7 carbon atoms, alkenoyl of 3 to 7 carbon atoms, alkylsulfonyl of 1 to 7 carbon atoms, aroyl of 7 to 12 carbon atoms, arylalkenoyl of 9 to 20 carbon atoms, arylsulfonyl of 6 to 12 carbon atoms, arylalkanoyl of 8 to 12 carbon atoms or arylalkylsulfonyl of 7 to 12 carbon atoms;A is selected from the group consisting of: ##STR2## wherein: R.sub.4 is hydrogen, C.sub.1-6 alkyl, C.sub.1-6 perfluoroalkyl, C.sub.1-6 alkoxy, C.sub.1-6 perfluoroalkoxy, amino, C.sub.1-6 alkylamino, C.sub.2-12 dialkylamino, C.sub.1-6 alkylsulfonamido, alkylcarboxamido containing 2 to 7 carbon atoms, nitro, cyano or carboxyl;or a pharmaceutically acceptable salt thereof, are smooth muscle relaxants.Type: GrantFiled: June 2, 1995Date of Patent: April 30, 1996Assignee: American Home Products CorporationInventors: Madelene M. Antane, John A. Butera, Bradford H. Hirth, Schuyler A. Antane
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Patent number: 5512565Abstract: The compounds of the formula: ##STR1## in which ##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: March 30, 1995Date of Patent: April 30, 1996Assignee: American Home Products CorporationInventors: Richard E. Mewshaw, Thomas J. Commons, Donald P. Strike
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Patent number: 5510478Abstract: The compound of the formula: ##STR1## where R.sub.1, R.sub.2 and R.sub.3 are, independently, H, alkyl, halo, perhaloalkyl, hydroxy, alkoxy, aryl or arylalkyl; n is an integer from 0-5; R is azabicyclo 2.2.2!octyl or azabicyclo 2.2.1!heptyl when n.sub.1 is zero, or R is NR.sub.4 R.sub.5 when n.sub.1 is 1, 2, 3, 4, or 5, in which R.sub.4 and R.sub.5 are alkyl or R.sub.4 and R.sub.5, taken with the nitrogen atom to which they are attached, are N-(substituted aryl)piperazinyl in which said substituent is alkoxy, halo, or perhaloalkyl; N-(pyridyl)piperazinyl; N-(pyrimidinyl)piperazinyl; or 3-azabicyclo- 3.2.2!non-3-yl; X is oxygen or NH; n and n.sub.1 are, independently, one of the integers 0, 1, 2, 3, 4 or 5; or a pharmaceutically acceptable salt thereof are centrally active muscarinic agents.Type: GrantFiled: November 30, 1994Date of Patent: April 23, 1996Assignee: American Home Products CorporationInventor: Annmarie L. Sabb
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Patent number: 5508401Abstract: This invention involves novel neuroprotectant agents of the formula: ##STR1## in which R.sup.1 and R.sup.3 are, independently, hydrogen, cyano, nitro, halo or perhaloalkyl, with the proviso that one of R.sup.1 and R.sup.3 is other than hydrogen; R.sub.2 is alkyl; or a pharmaceutically acceptable salt thereof.Type: GrantFiled: February 20, 1991Date of Patent: April 16, 1996Assignee: American Home Products CorporationInventors: Wayne E. Childers, Jr., Magid A. Abou-Gharbia, Edward J. Podlesny
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Patent number: 5506252Abstract: The compounds of the formula: ##STR1## wherein: R.sub.1 and R.sub.2 are, independently, hydrogen, straight or branched chain alkyl or mono- or bi-cyclic alkyl; A is a substituted phenyl group containing one cyano substituent and one substituent selected from cyano, nitro, alkyl, perfluoroalkyl, alkoxy, perfluoroalkoxy, amino, alkylamino, dialkylamino, sulfamyl, alkylsulfonamido, arylsulfonamido, alkylcarboxamido, arylcarboxamido, alkylsulfonyl, perfluoroalkylsulfonyl, arylsulfonyl, chloro, bromo, fluoro, iodo, 1-imidazolyl or carboxyl; or a pharmaceutically acceptable salt thereof, are smooth muscle relaxants.Type: GrantFiled: October 2, 1994Date of Patent: April 9, 1996Assignee: American Home Products CorporationInventors: John A. Butera, Schuyler A. Antane
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Patent number: 5486518Abstract: This invention provides anxiolytic/antidepressant agents of the formula:A compound of the formula: ##STR1## in which R.sup.1 is alkyl, cycloalkyl, aryl or arylalkyl;R.sup.2 is hydrogen or alkyl;R.sup.3 is phenyl, benzyl, substituted phenyl, or substituted benzyl in which the substituents are hydroxy, halo, alkoxy, trifluoromethyl, nitro, cyano, alkoxycarbonyl, amino or dialkylamino;or a pharmaceutically acceptable salt thereof.Type: GrantFiled: April 10, 1995Date of Patent: January 23, 1996Assignee: American Home Products CorporationInventors: John P. Yardley, Horace Fletcher, III, Michael G. Kelly, Alan C. White
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Patent number: 5482935Abstract: A method for the treatment of atherosclerosis by administering to a patient in need of anti-atherosclerotic treatment, an effective amount of 17 alpha-dihydroequilin, a C.sub.2 -C.sub.6 alkanoyloxy ester thereof or a pharmaceutically acceptable salt of it's sulfate or phosphate ester, in the absence of naturally occurring estrogenic sreroids. A pharmaceutical composition containing 17 alpha-dihydroequilin, a C.sub.2 -C.sub.6 alkanoyloxy ester thereof or a pharmaceutically acceptable salt of it's sulfate or phosphate ester, in the absence of naturally occurring estrogenic sreroids, and a pharmaceutically acceptable carrier therefor.Type: GrantFiled: December 1, 1993Date of Patent: January 9, 1996Assignee: American Home Product CorporationInventors: Steven J. Adelman, Kurt E. Steiner
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Patent number: 5478939Abstract: Compounds of the Formulae I or II ##STR1## wherein Z and R.sub.1, are as described herein which compounds are muscarinic agonists useful in treating central cholinergic disfunction and pharmaceutical compositions containing the compounds.Type: GrantFiled: July 20, 1994Date of Patent: December 26, 1995Assignee: American Cyanamid CompanyInventors: Eugene Trybulski, Jing Zhang
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Patent number: 5468875Abstract: The compound 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 centrally active muscarinic agents.Type: GrantFiled: December 22, 1994Date of Patent: November 21, 1995Assignee: American Home Products CorporationInventors: Annmarie L. Sabb, Reinhardt P. Stein
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Patent number: 5466688Abstract: The compound of the formula: ##STR1## where R.sub.1 and R.sub.5 are independently hydrogen, fluorine, chlorine, bromine, iodine, trifluoromethyl, cyano, nitro, CO.sub.2 H, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.10 alkenyl, C.sub.1 -C.sub.6 alkoxy, C.sub.3 -C.sub.8 cycloalkyl, cycloalkylalkyl, C.sub.3 -C.sub.8 cycloalkyloxy, C.sub.2 -C.sub.7 alkylcarbonyl, C.sub.2 -C.sub.7 alkylcarbonyloxy, C.sub.2 -C.sub.7 alkoxycarbonyl, mono- or di-alkylaminocarbonyl, tetrazolyl, --OH, --(CH.sub.2).sub.1-6 OH, --SH, --NH.sub.2 or --(CH.sub.2).sub.1-6 NR.sub.8 R.sub.9 where R.sub.8 is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.7 alkylcarbonyl, C.sub.2 -C.sub.7 alkoxycarbonyl and R.sub.9 is hydrogen or C.sub.1 -C.sub.6 alkyl; R.sub.2 is hydrogen or C.sub.1 -C.sub.6 alkyl; R.sub.3 and R.sub.4 are hydrogen or taken together with the carbon atoms to which they are attached form a double bond; R.sub.6 and R.sub.7 are independently H, C.sub.1 -C.sub.10 alkyl, C.sub.2 -C.sub.10 alkenyl, C.sub.3 -C.sub.Type: GrantFiled: October 20, 1994Date of Patent: November 14, 1995Assignee: American Home Products CorporationInventors: Thomas J. Commons, Christa M. LaClair, Susan Christman
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Patent number: 5466712Abstract: The compound of the formula (I) or a pharmaceutically acceptable salt thereof, are smooth muscle relaxants ##STR1##Type: GrantFiled: November 4, 1994Date of Patent: November 14, 1995Assignee: American Home Products CorporationInventors: John A. Butera, Schuyler A. Antane, Bradford H. Hirth
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Patent number: 5464867Abstract: The compound of the formula (I) or a pharmaceutically acceptable salt thereof, are smooth muscle relaxants.Type: GrantFiled: November 16, 1994Date of Patent: November 7, 1995Assignee: American Home Products CorporationInventors: Madelene M. Antane, John A. Butera, Bradford H. Hirth, Schuyler A. Antane
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Patent number: 5459131Abstract: Renin inhibiting compounds of the formula: ##STR1## wherein A is a moiety selected from those of the formula: ##STR2## where Z is O, S, SO, or SO.sub.2, P is 1 or 2 and X is --O-- or --S--; and analogs thereof which inhibit the substrate-cleaving acting of renin, pharmaceutical compositions containing these compounds, processes for producing the compounds and methods of treating hypertension which employ the novel renin inhibitors.Type: GrantFiled: March 15, 1991Date of Patent: October 17, 1995Assignee: American Cyanamid CompanyInventors: Jay D. Albright, Charles F. Howell
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Patent number: 5451685Abstract: 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: July 13, 1994Date of Patent: September 19, 1995Assignee: American Cyanamid CompanyInventors: Eugene J. Trybulski, Richard H. Kramss, Herbert Brabander