Patents Represented by Attorney, Agent or Law Firm Steven R. Eck
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Patent number: 6391897Abstract: This invention provides substituted compounds of the general formulae: wherein B and E are C or N; D, G and W are O, S, or N; or salt forms thereof, and methods and pharmaceutical compositions for their use in treating disorders related to insulin resistance or hyperglycemia.Type: GrantFiled: March 2, 2001Date of Patent: May 21, 2002Assignee: American Home Products CorporationInventors: Michael S. Malamas, Robert E. McDevitt, Folake O. Adebayo
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Patent number: 6372745Abstract: This invention provides compounds of formula I, wherein R is hydrogen or alkyl of 1-6 carbon atoms; R′ is hydrogen, alkyl of 1-6 carbon atoms, acyl of 2-7 carbon atoms, or aroyl; R1, R2, R3, and R4 are each, independently, hydrogen, alkyl of 1-6 carbon atoms, alkoxy of 1-6 carbon atoms, halogen, trifluoroalkyl, —CN, alkyl sulfonamide of 1-6 carbon atoms, alkyl amide of 1-6 carbon atoms, amino, alkylamino of 1-6 carbon atoms, dialkylamino of 1-6 carbon atoms per alkyl moiety, trifluoroalkoxy of 1-6 carbon atoms, acyl of 2-7 carbon atoms, or aroyl; X is CR5R6 or a carbonyl group; R5 and R6 are each, independently, hydrogen or alkyl of 1-6 carbon atoms; or a pharmaceutically acceptable salt thereof, with the proviso that at least one of R1, R2, R3, or R4 are not hydrogen; which are 5HT2C receptor agonists useful for the treatment of disorders involving the central nervous system such as obsessive-compulsive disorder, depression, anxiety, schizophrenia, migraine, sleep disordeType: GrantFiled: December 6, 1999Date of Patent: April 16, 2002Assignee: American Home Products CorporationInventors: Annmarie L. Sabb, Gregory S. Welmaker, James A. Nelson
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Patent number: 6369072Abstract: This invention provides substituted compounds of the general formulae: wherein B and E are C or N; D, G and W are O, S, or N; or salt forms thereof, and methods and pharmaceutical compositions for their use in treating disorders related to insulin resistance or hyperglycemia.Type: GrantFiled: March 2, 2001Date of Patent: April 9, 2002Assignee: American Home Products CorporationInventors: Michael S. Malamas, Robert E. McDevitt, Folake O. Adebayo
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Patent number: 6352718Abstract: This invention provides novel formulations for N-[4-(5H-pyrrolo[2,1-c][1,4]benzodiazepin-10(11H)ylcarbonyl)-3-chlorophenyl]-5-fluoro-2-methyl-benzamide, or a pharmaceutically acceptable salt thereof, and processes for making them, the formulations comprising from about 1% to about 20% of active ingredient, from about 1% to about 18% of a surfactant component, from about 50% to about 80% of a component of one or more polyethylene glycols, from about 1% to about 20% of a component of one or more sucrose fatty acid esters and/or polyvinylpyrrolidone and, optionally, one or more pharmaceutically acceptable preservatives or antioxidantsType: GrantFiled: September 25, 2000Date of Patent: March 5, 2002Assignee: American Cyanamid CompanyInventors: Joseph K. Yoon, Richard W. Saunders, Mahdi Fawzi
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Patent number: 6350773Abstract: Therapeutic combinations useful in the treatment or prevention of psychotic disorders, to pharmaceutical compositions containing said combinations, and to their use in the treatment or prophylaxis of prevention disorders are provided.Type: GrantFiled: December 4, 2000Date of Patent: February 26, 2002Assignee: American Home Products CorporationInventor: Karen L. Marquis
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Patent number: 6348486Abstract: This invention provides methods and pharmaceutical compositions for maintaining bladder control or treating urinary incontinence in a mammal utilizing agonists of KCNQ potassium channels, including KCNQ2, KCNQ3, KCNQ4 and KCNQ5 potassium channels, alone or in combination. Compounds useful in these methods include the 1,2,4-triamino-benzene derivatives described in U.S. Pat. No. 5,384,330 (Dieter et al.) and the substituted 3-phenyl oxindole compounds described in U.S. Pat. No. 5,565,483 (Hewawasam et al.). Among the preferred compounds of this invention is N-[2-amino-4-(4-fluorobenzylamino)-phenyl]carbamic acid ethyl ester, also referred to as retigabine.Type: GrantFiled: October 15, 2001Date of Patent: February 19, 2002Assignee: American Home Products CorporationInventors: Thomas Michael Argentieri, Jeffrey Howard Sheldon, Mark R. Bowlby
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Patent number: 6344451Abstract: The present invention provides compounds of the formula: wherein: X, Y and Z are independently selected from O, S, CH, CH2, N, or NR4; W is moiety selected from (CH2)n; n=1-2; R1, R2 are independently, hydrogen, straight chain alkyl (C1-C6), branched chain alkyl (C3-C7), cycloalkyl (C3-C7), alkoxyalkyl (C2-C7), halogen, straight or branched chain alkoxy (C1-C6), hydroxy, CF3, or perfluoroalkyl (C2-C6); R3 is hydrogen or a straight chain alkyl group (C1-C6), branched chain alkyl (C3-C7), cycloalkyl (C3-C7), alkoxyalkyl (C2-C7), or hydroxyalkyl (C1-C6); R4 is selected from hydrogen, or (lower alkyl (C1-C6); and R5 is selected from halogen or hydrogen; or a pharmaceutically acceptable salt thereof: as well as methods and pharmaceutical compositions utilizing these compounds for the treatment of disorder which may be remedied or alleviated by vasopressin agonist activity, including diabetes insipidus, nocturnal enuresis, nocturia, urinary incontinence, bleeding and coagulation disType: GrantFiled: February 1, 2000Date of Patent: February 5, 2002Assignee: American Home ProductsInventors: Robert J. Steffan, Amedeo A. Failli
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Patent number: 6340676Abstract: This invention provides compounds of Formula I having the structure wherein B and D are each, independently, hydrogen, halogen, —CN, alkyl of 1-6 carbon atoms, aryl, or aralkyl of 6-12 carbon atoms; R1 is hydrogen, alkyl of 1-6 carbon atoms, —CH(R2)W, —C(CH3)2CO2R3, 5-thiazolidine-2,4-dione, —CH(R4)CH2CO2R3, —COR3, or —PO3(R3)2; R2 is hydrogen, alkyl of 1-6 carbon atoms, aralkyl of 6-12 carbon atoms, aryl, —CH2(1H-imidazol-4-yl), —CH2(3-1H-indolyl), —CH2CH2(1,3-dioxo-1,3-dihydro-isoindol-2-yl), —CH2CH2(1-oxo-1,3-dihydro-isoindol-2-yl), or —CH2(3-pyridyl); W is —CO R3, —CONH2, —CONHOH, —CN, CONH(CH2)2CN, 5-tetrazole, or —PO3(R3)2; R3 is hydrogen, alkyl of 1-6 carbon atoms, or aryl; R4 is hydrogen or alkyl of 1-6 carbon atoms; or a pharmaceutically acceptable salt thereof, which are useful in treating metabolic disorders related to insulin resistance or hyperglycemia.Type: GrantFiled: April 20, 2001Date of Patent: January 22, 2002Assignee: American Home Products CorporationInventors: Jay E. Wrobel, Zenan Li
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Patent number: 6326367Abstract: The present invention relates to new 2-Phenyl-1-[4-(2-Aminoethoxy)-Benzyl]-Indole compounds which are useful as estrogenic agents, as well as pharmaceutical compositions and methods of treatment utilizing these compounds, which have the general structures below:Type: GrantFiled: September 2, 1999Date of Patent: December 4, 2001Assignee: American Home Products CorporationInventors: Chris P. Miller, Michael D. Collini, Bach D. Tran, Arthur A. Santilli
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Patent number: 6310081Abstract: This invention provides compounds of Formula I having the structure wherein A, Q, R3, and R4 are as defined hereinbefore in the specification, or a pharmaceutically acceptable salt thereof, which are useful in treating metabolic disorders related to insulin resistance or hyperglycemia.Type: GrantFiled: March 1, 2001Date of Patent: October 30, 2001Assignee: American Home Products CorporationInventors: Michael S. Malamas, Folake O. Adebayo, Paul J. Dollings
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Patent number: 6297234Abstract: The present invention provides compounds of the general formula: wherein Y is a moiety selected independently, from NH or —(CH2)n— wherein n is 1; m is an integer from 1 to 2; and the moiety represents: (1) a 5-membered aromatic (unsaturated) heterocyclic ring having one nitrogen (wherein A is nitrogen, and B and C are CH), (2) a 6-membered aromatic (unsaturated) heterocyclic ring having one nitrogen (wherein A is carbon, B is nitrogen, and C is —CH—CH—), (3) a 6-membered aromatic (unsaturated) ring (wherein A is carbon, B is CH, and C is —CH—CH—); as well as methods and pharmaceutical compositions utilizing these compounds for the treatment of disorder which may be remedied or alleviated by vasopressin agonist activity, including diabetes insipidus, nocturnal enuresis, nocturia, urinary incontinence, bleeding and coagulation disorders, or temporary delay of urination.Type: GrantFiled: February 1, 2000Date of Patent: October 2, 2001Assignee: American Home Products CorporationInventors: Amedeo A. Failli, David K. Williams, Thomas J. Caggiano, Jay S. Shumsky, Mark A. Ashwell
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Patent number: 6288100Abstract: Disclosed herein are compounds of formula I or II: wherein R is alkyl phenyl or substituted phenyl; R2 is hydrogen, halogen, alkoxy or alkyl; R1 is hydrogen, alkyl, aryl, arylalkyl, or substituted benzyl; or a pharmaceutically acceptable salt thereof, which are useful as inhibitors of smooth muscle cell proliferation.Type: GrantFiled: June 6, 1995Date of Patent: September 11, 2001Assignee: American Home Products CorporationInventors: Hassan M. Elokdah, Sie-Yearl Chai, Theodore S. Sulkowski
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Patent number: 6281238Abstract: This invention provides compounds of Formula I having the structure wherein B and D are each, independently, hydrogen, halogen, —CN, alkyl of 1-6 carbon atoms, aryl, or aralkyl of 6-12 carbon atoms; R1 is hydrogen, alkyl of 1-6 carbon atoms, —CH(R2)W, —C(CH3)2CO2R3, 5-thiazolidine-2,4-dione, —CH(R4)CH2CO2R3, —COR3, or —PO3(R3)2; R2 is hydrogen, alkyl of 1-6 carbon atoms, aralkyl of 6-12 carbon atoms, aryl, —CH2(1H-imidazol-4-yl), —CH2(3-1H-indolyl), —CH2CH2(1,3-dioxo-1,3-dihydro-isoindol-2-yl), —CH2CH2(1-oxo-1,3-dihydro-isoindol-2-yl), or —CH2(3-pyridyl); W is —CO2R3, —CONH2, —CONHOH, —CN, CONH(CH2)2CN, 5-tetrazole, or —PO3(R3)2; R3 is hydrogen, alkyl of 1-6 carbon atoms, or aryl; R4 is hydrogen or alkyl of 1-6 carbon atoms; or a pharmaceutically acceptable salt thereof, which are useful in treating metabolic disorders related to insulin resistance or hyperglycemia.Type: GrantFiled: March 16, 2000Date of Patent: August 28, 2001Assignee: American Home Products CorporationInventors: Jay E. Wrobel, Zenan Li
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Patent number: 6268504Abstract: The present invention provides compounds useful in the synthesis of biologically active compounds, and processes for their production, the compounds having the formula: wherein: R1 and R2 are, independently, selected from H; C1-C12 alkyl or C1-C6 perfluorinated alkyl; X represents a leaving group; A is O or S; m is an integer from 1 to 3, preferably 2; R3, R4, R5, and R6 are independently selected from H, halogen, —NO2, alkyl, alkoxy, C1-C6 perfluorinated alkyl, OH or the C1-C4 esters or alkyl ethers thereof, —CN, —O—R1, —O—Ar, —S—R1, —S—Ar, —SO—R1, —SO—Ar, —SO2—R1, —SO2—Ar, —CO—R1, —CO—Ar, —CO2—R1, or —CO2—Ar; and Y is selected from a) the moiety: wherein R7 and R8 are independently selected from the group of H, C1-C6 alkyl, or phenyl; or b) an optionally substituted five-, six- or seven-membered saturated, unsaturatedType: GrantFiled: December 10, 1999Date of Patent: July 31, 2001Assignee: American Home Products CorporationInventors: Panolil Raveendranath, Joseph Zeldis, Galina Vid, John R. Potoski, Jianxin Ren, Silvio Iera
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Patent number: 6268360Abstract: The present invention provides compounds of the general formula: wherein Y is a moiety selected independently, from NH or —(CH2)n— wherein n is 1; m is an integer from 1 to 2; and the moiety represents: (1) a 5-membered aromatic (unsaturated) heterocyclic ring having one nitrogen (wherein A is nitrogen, and B and C are CH), (2) a 6-membered aromatic (unsaturated) heterocyclic ring having one nitrogen (wherein A is carbon, B is nitrogen, and C is —CH—CH—), (3) a 6-membered aromatic (unsaturated) ring (wherein A is carbon, B is CH, and C is —CH—CH—); as well as methods and pharmaceutical compositions utilizing these compounds for the treatment of disorder which may be remedied or alleviated by vasopressin agonist activity, including diabetes insipidus, nocturnal enuresis, nocturia, urinary incontinence, bleeding and coagulation disorders, or temporary delay of urination.Type: GrantFiled: October 27, 2000Date of Patent: July 31, 2001Assignee: American Home Products CorporationInventors: Amedeo A. Failli, David K. Williams, Thomas J. Caggiano, Jay S. Shumsky, Mark A. Ashwell
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Patent number: 6242605Abstract: The present invention provides compounds useful in the synthesis of biologically active compounds, and processes for their production, the compounds having the formula: wherein: R1 and R2 are, independently, selected from H; C1-C12 alkyl or C1-C6 perfluorinated alkyl; X represents a leaving group; A is 0 or S; m is an integer from 1 to 3, preferably 2; R3, R4, R5, and R6 are independently selected from H, halogen, —NO2, alkyl, alkoxy, C1-C6 perfluorinated alkyl, OH or the C1-C4 esters or alkyl ethers thereof, —CN, —O—R1, —O—Ar, —S—R1, —S—Ar, —SO—R1, —SO—Ar, —SO2—R1, —SO2—Ar, —CO—R1, —CO—Ar, —CO2—R1, or —CO2—Ar; and Y is selected from a) the moiety: wherein R7 and R8 are independently selected from the group of H, C1-C6 alkyl, or phenyl; or b) an optionally substituted five-, six- or seven-membered saturated, unsaturatedType: GrantFiled: December 10, 1999Date of Patent: June 5, 2001Assignee: American Home Products CorporationInventors: Panolil Raveendranath, Joseph Zeldis, Galina Vid, John R. Potoski, Jianxin Ren, Silvio Iera
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Patent number: 6235900Abstract: The present invention provides compounds of the general formula: as well as methods and pharmaceutical compositions utilizing these compounds for the inducement of temporary delay of urination or the treatment of disorders which may be remedied or alleviated by vasopressin agonist activity, including diabetes insipidus, nocturnal enuresis, nocturia, urinary incontinence, bleeding and coagulation disorders.Type: GrantFiled: February 1, 2000Date of Patent: May 22, 2001Assignee: American Home Products CorporationInventors: Amedeo A. Failli, Jay S. Shumsky, Eugene J. Trybulski
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Patent number: 6232307Abstract: The present invention relates to new 2-Phenyl-1-[4-(2-Aminoethoxy)-Benzyl]-Indole compounds which are useful as estrogenic agents, as well as pharmaceutical compositions and methods of treatment utilizing these compounds, which have the general structures below:Type: GrantFiled: October 12, 1999Date of Patent: May 15, 2001Assignee: American Home Products CorporationInventors: Chris P. Miller, Michael D. Collini, Bach D. Tran, Arthur A. Santilli
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Patent number: 6225308Abstract: The present invention relates to new 2-Phenyl-1-[4-(2-Aminoethoxy)-Benzyl]-Indole compounds which are useful as estrogenic agents, as well as pharmaceutical compositions and methods of treatment utilizing these compounds, which have the general structures below:Type: GrantFiled: October 12, 1999Date of Patent: May 1, 2001Assignee: American Home Products CorporationInventors: Chris P. Miller, Michael D. Collini, Bach D. Tran, Arthur A. Santilli
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Patent number: 6204274Abstract: The present invention provides compounds of the formula (1): wherein R1 and R2 each independently represent hydrogen, hydroxy, F, Cl, Br, I, CN, 1 to 6 carbon alkyl, 1 to 6 carbon alkoxy, nitro, CF3 and phenyloxy or benzyloxy, in which the aromatic ring can be optionally substituted by from 1 to 3 groups selected from C1-C6 alkoxy (preferably OMe), F, Cl, Br, I, and CF3; R3 and R4 are each independently a hydrogen, a 1 to 6 carbon alkyl or a CH2Ph in which the phenyl ring can be optionally substituted by from 1 to 3 groups selected from C1-C6 alkoxy (preferably OMe), F, Cl, Br, I, and CF3; Y is selected from CH2 or CH and, X is selected from a group represented by N, CR3, CHR3, CHCH; or a pharmaceutically acceptable salt thereof, as well as pharmaceutical compositions and methods of using the compounds to treat central nervous system disorders, such as depression, anxiety, drug withdrawal, eating and sexual disorders and other conditions for which serotonin reuptake inhibitors are used.Type: GrantFiled: April 23, 1999Date of Patent: March 20, 2001Assignee: American Home Products CorporationInventors: Michael G. Kelly, Young H. Kang