Patents by Inventor Gevork Minaskanian
Gevork Minaskanian has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).
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Patent number: 5118676Abstract: This invention relates to a method for administering systemically active agents including therapeutic agents through the skin or mucosal membranes of humans and animals and into the blood stream in a transdermal device or formulation comprising topically administering with said systemic agent an effective amount of a membrane penetration enhancer being a carboxylic acid derivative or a salt thereof represented in one embodiment by the general formula ##STR1## wherein W represents oxygen, sulfur, or two hydrogen radicals; wherein Z represents oxygen, sulfur, or --CH.sub.2 --;wherein R represents alkyl optionally substituted with one to three double or triple bonds, --SR'", --OR'", --NHR'", --CH.sub.3, or COOR.sub.1, and wherein R.sub.1 represents hydrogen or lower alkyl;wherein R'" represents alkyl, alkylthioalkyl, alkoxyalkyl, substituted aminoalkyl, optionally substituted with a phenyl, benzoyl or heterocyclic group;wherein R' represents hydrogen, alkyl, alkoxy, acyloxy, alkylthio, hydroxy, --(CH.sub.2).sub.Type: GrantFiled: November 13, 1990Date of Patent: June 2, 1992Assignee: Whitby Research, Inc.Inventors: Gevork Minaskanian, James V. Peck
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Patent number: 5073544Abstract: This invention provides compositions for enhancing penetration of physiologically active agents through the skin or mucosal membranes and for retaining these agents in body tissues, said composition comprising effective amounts of a physiologically-active agent and a compound represented by the general formula ##STR1## wherein X may represent sulfur, oxygen or nitrogen; a and b may be 0 or 1, c may be 0, 1 or 2, except that when X is oxygen, a, b and c are 0, when X is nitrogen c is 0 and only one of a or b is 1, and when X is sulfur a and b are 0; A is a branched or a straight chain, divalent aliphatic radical having from 0 to 2 double bonds; R' is selected from the group consisting of H, a lower alkyl group having from 1 to 4 carbon atoms, phenyl, lower alkyl or halogen substituted phenyl, acetamido, halogen, piperidinyl, lower alkyl or halogen substituted piperidinyl, carbalkoxy, carboxamide, and alkanoyl; and R is hydrogen or a lower alkyl group having from 1 to 4 carbon atoms, ##STR2## wherein R" is H orType: GrantFiled: March 23, 1989Date of Patent: December 17, 1991Assignee: Whitby, Inc.Inventors: James V. Peck, Gevork Minaskanian
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Patent number: 5043441Abstract: This invention provides compositions comprising a physiologically-active agent and a compound having the structural formula ##STR1## wherein each X, Y and Z may represent oxygen, sulfur or two hydrogen atoms, provided however that, when Z represents two hydrogen atoms, both X and Y represent oxygen or sulfur and when Z represents oxygen or sulfur at least one of X and Y must represent oxygen or sulfur; m is 2-6; R' is H or a lower alkyl group having 1-4 carbon atoms; n is 0-17 and R is --CH.sub.3, ##STR2## wherein R" is H or halogen in an amount effective to enhance the penetration of the physiologically-active agent through the skin or other membrane of the body of an animal.Type: GrantFiled: January 22, 1990Date of Patent: August 27, 1991Assignee: Whitby Research, Inc.Inventors: James V. Peck, Gevork Minaskanian
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Patent number: 5034386Abstract: This invention provides compositions comprising a physiologically-active agent and a compound having the structural formula ##STR1## wherein each X, Y and Z may represent oxygen, sulfur or two hydrogen atoms, provided however that, when Z represents two hydrogen atoms, both X and Y represent oxygen or sulfur and when Z represents oxygen or sulfur at least one of X and Y must represent oxygen or sulfur; m is 2-6; R' is H or a lower alkyl group having 1-4 carbon atoms; n is 0-17 and R is --CH.sub.3, ##STR2## wherein R" is H or halogen in an amount effective to enhance the penetration of the physiologically-active agent through the skin or other membrane of the body of an animal.Type: GrantFiled: August 17, 1988Date of Patent: July 23, 1991Assignee: Whitby Research, Inc.Inventors: James V. Peck, Gevork Minaskanian
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Patent number: 4996199Abstract: This invention relates to a method for administering systemically active agents including therapeutic agents through the skin or mucosal membranes of humans and animals and into the blood stream in a transdermal device or formulation comprising topically administering with said systemic agent an effective amount of a membrane penetration enhancer being a carboxylic acid derivative or a salt thereof represented in one embodiment by the general formula ##STR1## wherein W represents oxygen, sulfur, or two hydrogen radicals;wherein Z represents oxygen, sulfur, or --CH.sub.2 --;wherein R represents alkyl optionally substituted with one to three double or triple bonds, --SR'", --OR'", --NHR'", --CH.sub.3, or COOR.sub.1, and wherein R.sub.1 represents hydrogen or lower alkyl;wherein R'" represents alkyl, alkylthioalkyl, alkoxyalkyl, substituted aminoalkyl, optionally substituted with a phenyl, benzoyl or heterocyclic group;wherein R' represents hydrogen, alkyl, alkoxy, acyloxy, alkylthio, hydroxy, --(CH.sub.2).sub.Type: GrantFiled: June 20, 1988Date of Patent: February 26, 1991Assignee: Whitby Research, Inc.Inventors: Gevork Minaskanian, James V. Peck
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Patent number: 4992422Abstract: This invention provides compositions comprising a physiologically-active agent and a compound having the structural formula ##STR1## Wherein X may represent sulfur or two hydrogen atoms; R' is H or a lower alkyl group having 1-4 carbon atoms; m is 2-6; n is 0-18 and R is --Ch.sub.3, ##STR2## wherein R" is H or halogen, in an amount effective to enhance the penetration of the physiologically-active agent through the skin or other membrane of the body of an animal.Type: GrantFiled: April 19, 1989Date of Patent: February 12, 1991Assignee: Whitby Research, Inc.Inventors: Gevork Minaskanian, James Peck, Eric L. Nelson
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Patent number: 4965371Abstract: This invention provides a process for preparing lactams, by selectively reacting a novel 1-hydrocarbylamino (or heteroatom-substituted hydrocarbylamino); 1,1-dicarboxylic acid, alkylesters; 1-hydrocarbyl (or heteroatom-substituted hydrocarbyl) carboxylic acid, alkyl ester methane, as the salt of an acid having a pKa of 0 or more, in the absence or presence of a base, whereby novel lactams wherein one or both hydrocarbyl moieties are incorporated into the lactam ring are obtained. That is, the acid moiety of said novel salt promotes the reaction whereby both hydrocarbyl moieties are incorporated into the ring, while the presence of a base, in an amount substantially equivalent to said acid promotes the reaction whereby only one hydrocarbyl is incorporated into the ring.Type: GrantFiled: May 25, 1989Date of Patent: October 23, 1990Assignee: Whitby Research, Inc.Inventors: Gevork Minaskanian, James V. Peck
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Patent number: 4920101Abstract: This invention provides compositions comprising a physiologically-active agent and a compound represented by the general formula ##STR1## wherein X may represent sulfur, oxygen or 2 hydrogen radicals; Y may represent --CH.sub.2 --, --NH-- or oxygen; n and m are integers of from 1 to 3; p is an integer of from 3 to 17; q is 2, 4, 6 or 8; wherein p.gtoreq.9; and R' is selected from the group consisting of H, a lower alkyl group having from 1 to 4 carbon atoms, phenyl, lower alkyl or halogen substituted phenyl, acetamido, halogen, piperidinyl, lower alkyl or halogen substituted piperidinyl, carbalkoxy, carboxamide, and alkanoyl. These compositions are useful in topical or transdermal applications of the physiologically-active agent.Type: GrantFiled: September 30, 1987Date of Patent: April 24, 1990Assignee: Nelson Research & Development Co.Inventors: Gevork Minaskanian, James V. Peck
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Patent number: 4917896Abstract: This invention relates to a method for administering systemically active agents including therapeutic agents through the skin or mucosal membranes of humans and animals in a transdermal device or formulation comprising topically administering with said systemic agent an effective amount of a membrane penetration enhancer having the structural formula ##STR1## wherein X may represent sulfur, oxygen or nitrogen; a and b may be 0 or 1, c may be 0, 1 or 2, except that when X is oxygen, a, b and c are 0, when X is nitrogen c is 0 and only one of a or b is 1, and when X is sulfur a and b are 0; A is a branched or a straight chain, divalent aliphatic radical having from 0 to 2 double bonds; R' is selected from the group consisting of H, a lower alkyl group having from 1 to 4 carbon atoms, phenyl, lower alkyl or halogen substituted phenyl, acetamido, halogen, piperidinyl, lower alkyl or halogen substituted piperidinyl, carboalkoxy, carboxamide, and alkanoyl; and R is hydrogen or a lower alkyl group having from 1 to 4Type: GrantFiled: November 19, 1986Date of Patent: April 17, 1990Assignee: Nelson Research & Development Co.Inventors: James V. Peck, Gevork Minaskanian
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Patent number: 4912223Abstract: This invention provides novel compounds represented by the general formula: ##STR1## R.sub.1 and R.sub.2 are each independently selected from the group consisting of hydrocarbyl radicals and heteroatom-substituted hydrocarbyl radicals, wherein said heteroatoms are selected from the group consisting of nitrogen, oxygen, sulfur, phosphorus and halogen atoms; A is a straight or branched chain hydrocarbon moiety containing from 1 to 12 carbon atoms and from 0 to 2 double bonds; R.sub.3 is selected from the group consisting of oxa- or dioxacycloalkanyl radicals which may be substituted with one or more hydroxy, keto, lower alkyl, phenyl or alkylenedioxy radicals; R.sub.4 is an aryl or heteroaryl radical; and R.sub.5 is a lower alkyl radical or A-R.sub.3 ; and pharmaceutically-acceptable salts thereof. These compounds are useful for treating coronary insufficiency, hypertension, angina pectoris, cardiac arrythmia, heart attack, or coronary vasospasm.Type: GrantFiled: January 28, 1988Date of Patent: March 27, 1990Assignee: Nelson Research & Development Co.Inventor: Gevork Minaskanian
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Patent number: 4902676Abstract: This invention provides compositions comprising a physiologically-active agent and a compound represented by the general formula ##STR1## wherein R.sup.1 and R.sup.2 are independently selected from the group consisting of alkyl radicals and cycloalkyl radicals comprising from 1 to 10 carbon atoms and R is selected from the group consisting of alkyl radicals and cycloalkyl radicals comprising from 1 to 30 carbon atoms; provided, however, that the total number of carbon atoms in said compound is 15 or more and the total number of carbon atoms in R.sup.1 and R.sup.2 is 5 or more.Type: GrantFiled: September 29, 1986Date of Patent: February 20, 1990Assignee: Nelson Research & Development Co.Inventors: James V. Peck, Gevork Minaskanian
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Patent number: 4886545Abstract: This invention provides compositions comprising a compound having the structural formula ##STR1## wherein each X, Y and Z may represent oxygen, sulfur or two hydrogen atoms, provided however that, when Z represents two hydrogen atoms, both X and Y represent oxygen or sulfur and when Z represents oxygen or sulfur at least one of X and Y must represent oxygen or sulfur; m is 2-6; R' is H or a lower alkyl group having 1-4 carbon atoms; n is 0-17 and R is --CH.sub.3, ##STR2## wherein R" is H or halogen. The invention also provides compositions comprising a physiologically-active agent and the hereinabove recited 1-substituted azacycloalkane compound in an amount effective to enhance the penetration of the physiologically-active agent through the skin or other membrane of the body of an animal.Type: GrantFiled: July 23, 1987Date of Patent: December 12, 1989Assignee: Nelson Research & Development CompanyInventors: James V. Peck, Gevork Minaskanian
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Patent number: 4886783Abstract: This invention relates to a method for administering systemically active agents including therapeutic agents through the skin or mucosal membranes of humans and animals in a transdermal device or formulation comprising topically administering with said systemic agent an effective amount of a membrane penetration enhancer having the structural formula ##STR1## wherein each X, Y and Z may represent oxygen, sulfur or two hydrogen atoms, provided however that, when Z represents two hydrogen atoms, both X and Y represent oxygen or sulfur and when Z represents oxygen or sulfur at least one of X and Y must represent oxygen or sulfur; m is 2-6; R' is H or a lower alkyl group having 1-4 carbon atoms; n is 0-16 and R is --CH.sub.3, ##STR2## wherein R" is H or halogen.Type: GrantFiled: August 17, 1988Date of Patent: December 12, 1989Assignee: Nelson Research & Development Co.Inventors: Gevork Minaskanian, James V. Peck
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Patent number: 4880924Abstract: This invention relates to a selective process for preparing bicyclic lactam-lactone compounds wherein the rings are fused, i.e. the rings share at least two carbon atoms, or are isolated. In particular, the present invention provides a process for selectively reacting novel 1-hydrocarbylamino (or heteroatom-substituted hydrocarbylamino); 1,1-dicarboxylic acid, alkylesters; 1-alkanolactonyl or hydrocarbyl (or heteroatom-substituted hydrocarbyl) alkanonylactonyl methane, as the salt of an acid having a pKa of 0 or more, to provide bicyclic lactam-lactone compounds. The selectively of the reaction to either fused or isolated bicyclic compounds is controlled by cyclizing the novel salts, in the absence of a base, a cyclizing said novel salts, in the presence of an amount of base substantially equivalent to said acid, respectively.Type: GrantFiled: April 3, 1986Date of Patent: November 14, 1989Assignee: Nelson Research & Development Co.Inventors: James V. Peck, Gevork Minaskanian
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Patent number: 4879275Abstract: This invention relates to a method for administering systemically active agents including therapeutic agents through the skin or mucosal membranes of humans and animals in a transdermal device or formulation comnprising topically administering with said systemic agent an effective amount of a membrane penetration enhancer having the structural formula ##STR1## wherein X represents sulfur, oxygen or 2 hydrogen radicals; Y represents --CH.sub.2 --, --NH-- or oxygen; n and m are integers of from 1 to 3; p is an integer of from 3 to 17; wherein p.gtoreq.9; q is 2, 4, 6 or 8; and R' is selected from the group consisting of H, a lower alkyl group having from 1 to 4 carbon atoms, phenyl, lower alkyl or halogen substituted phenyl, acetamido, halogen, piperidinyl, lower alkyl or halogen substituted piperidinyl, carbalkoxy, carboxamide, and alkanoyl.Type: GrantFiled: May 27, 1988Date of Patent: November 7, 1989Assignee: Nelson Research & Development Co.Inventors: Gevork Minaskanian, James V. Peck
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Patent number: 4870173Abstract: This invention provides a process for preparing lactams, by selectively reacting a novel 1-hydrocarbyl-amino (or heteroatom-substituted hydrocarbylamino); 1,1-dicarboxylic acid, alkylesters; 1-hydrocarbyl (or heteroatom-substituted hydrocarbyl) carboxylic acid, alkyl ester methane, as the salt of an acid having a pKa of 0 or more, in the absence or presence of a base, whereby novel lactams wherein one or both hydrocarbyl moieties are incorporated into the lactam ring are obtained. That is, the acid moiety of said novel salt promotes the reaction whereby both hydrocarbyl moieties are incorporated into the ring, while the presence of a base, in an amount substantially equivalent to said acid promotes the reaction whereby only one hydrocarbyl is incorporated into the ring.Type: GrantFiled: April 3, 1986Date of Patent: September 26, 1989Assignee: Nelson Research & Development Co.Inventors: Gevork Minaskanian, James V. Peck
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Patent number: 4849436Abstract: This invention provides compounds useful for treating coronary insufficiency, hypertension, angina pectoris, cardiac arrythmia, heart attack or coronary vasospasm and represented by the general formula: ##STR1## R.sub.1 and R.sub.2 are each independently selected from the group consisting of lower alkyl, N-alkylphthalimido and derivatives of N-alkylphthalimido, wherein said N-alkyl group comprises at least 2 carbon atoms;A is a straight or branched chain hydrocarbon moiety containing from 1 to 12 carbon atoms and from 0 to 2 double bonds;R.sub.3 is selected from the group of radicals consisting of hydrogen, --NH.sub.2 and --NCS;R.sub.4 is an aryl or heteroaryl radical; andR.sub.5 is a lower alkyl radical or A--R.sub.3 ; provided that when R.sub.3 is a hydrogen radical at least one of R.sub.1 and R.sub.2 is not lower alkyl, including both pure enantiomers as well as mixtures thereof; andpharmaceutically-acceptable salts thereof.Type: GrantFiled: March 11, 1986Date of Patent: July 18, 1989Assignee: Nelson Research & Development Co.Inventor: Gevork Minaskanian
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Patent number: 4833150Abstract: Compounds having calcium channel antagonist activity of the formula: ##STR1## wherein R.sub.1 and R.sub.2 are each independently amino, trifluoromethyl, pentafluoroethyl, alkoxy, lower alkenyl, or lower alkynyl or branched or unbranched lower alkyl, which is unsubstituted or is substituted with cyano, hydroxy, acyloxy, hydrazino, lower alkyl amino, or di(lower alkyl)-amino or 5 or 6 membered saturated nitrogen-containing heterocyclic-1-yl, which is unsubstituted or is substituted with oxo, hydroxy, alkyl, and hydroxy (lower alkyl) R.sub.3 is straight- or branched-chain C.sub.1 to C.sub.12 alkyl, alkenyl, alkynyl, or cycloalkyl, and is either unsubstituted or substituted with hydroxy, acyloxy, cyano, di(lower alkyl) amino 5- or 6-membered saturated nitrogen-containing heterocyclic -1-yl or R.sub.3 is --A--R.sub.4, A is a straight- or branched-chain hydrocarbon moiety containing from 2 to 12 carbon atoms and from 0 to 2 double bonds, R.sub.4 is selected from the group consisting of: ##STR2## R.sub.Type: GrantFiled: January 12, 1987Date of Patent: May 23, 1989Assignee: Nelson Research & Development Co.Inventors: Gevork Minaskanian, Vithal J. Rajadhyaksha
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Patent number: 4808414Abstract: This invention relates to a method for administering systemically active agents including therapeutic agents through the skin or mucosal membranes of humans and animals in a transdermal device or formulation comprising topically administering with said systemic agent an effective amount of a membrane penetration enhancer having the structural formula ##STR1## wherein R.sup.1 and R.sup.2 are independently selected from the group consisting of alkyl radicals and cycloalkyl radicals comprising from 1 to 20 carbon atoms and R is selected from the group consisting of alkyl radicals and cycloalkyl radicals comprising from 1 to 30 carbon atoms; provided, however, that the total number of carbon atoms in said compound is 15 or more and the total number of carbon atoms in R.sup.1 and R.sup.2 is 5 or more.Type: GrantFiled: November 19, 1986Date of Patent: February 28, 1989Assignee: Nelson Research & Development Co.Inventors: James V. Peck, Gevork Minaskanian
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Patent number: 4801586Abstract: This invention relates to a method for administering systemically active agents including therapeutic agents through the skin or mucosal membranes of humans and animals in a transdermal device or formulation comprising topically administering with said systemic agent an effective amount of a membrane penetration enhancer having the structural formula ##STR1## wherein X and Y, each, may represent sulfur, oxygen or two hydrogen atoms, A is a branched or a straight chain, divalent aliphatic radical having from 0 to 2 double bonds; R' is selected from the group consisting of H, a lower alkyl group having 1-4 carbon atoms, phenyl, lower alkyl or halogen substituted phenyl, acetamido, halogen, piperidinyl, lower alkyl or halogen substituted piperidinyl, carbalkoxy, carboxamide, and alkylformyl; m is 3-7; q is 2m-2x, wherein x equals the number of double bonds in the lactam ring and may be 1, 2 or 3, and R is CH.sub.3, ##STR2## wherein R" is H or halogen.Type: GrantFiled: October 7, 1986Date of Patent: January 31, 1989Assignee: Nelson Research & Development Co.Inventors: Gevork Minaskanian, James V. Peck