Patents by Inventor Vithal J. Rajadhyaksha

Vithal J. Rajadhyaksha 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).

  • Publication number: 20040102386
    Abstract: 3-Deoxyflavonoid compounds and methods for inhibiting T-cell activity and treating diseases and disorders (e.g., autoimmune disorders, inflammatory disorders, diabetes, ALS, MS, rheumatoid arthritis, etc.). In some cases the efficacy and/or duration of action of luteolin and/or other 3-deoxyflavonoid compounds may be increased by administering such compounds along with Rutin, a Rutin congener and/or a Rutin derivative. Also, in some cases, first pass metabolism of luteolin or other 3-deoxyflavonoids may be avoided by administering such compounds by parenteral routes (e.g., routes wherein absorption occurs at sites other than the stomach or intestinal mucosa, such as sublingual, buccal, intranasal, injection, etc.).
    Type: Application
    Filed: August 29, 2003
    Publication date: May 27, 2004
    Inventors: Thomas Lahey, Vithal J. Rajadhyaksha
  • Patent number: 5482965
    Abstract: A method and compositions for enhancing absorption of topically administered physiologically active agents through the skin and mucous membranes of humans and animals in a transdermal device or formulation for local or systemic use, comprising a therapeutically effective amount of a pharmaceutically active agent and a non-toxic, effective amount of penetration enhancing agent of the formula I or a physiologically acceptable salt thereof: ##STR1## wherein: R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are as defined herein.
    Type: Grant
    Filed: September 3, 1993
    Date of Patent: January 9, 1996
    Inventor: Vithal J. Rajadhyaksha
  • Patent number: 5283343
    Abstract: This invention relates to novel melatonin derivatives, such as 2-aryl substituted N-acetyltryptamines, having pharmacological activity, e.g., melatonin antagonist activity, and methods for the synthesis thereof.
    Type: Grant
    Filed: June 18, 1991
    Date of Patent: February 1, 1994
    Assignee: Whitby Research, Inc.
    Inventors: Margarita L. Dubocovich, Vithal J. Rajadhyaksha, James V. Peck, Atef A. Helmy
  • Patent number: 5204339
    Abstract: 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 is selected from the group consisting of oxygen and sulfur; R' is H or a lower alkyl group having 1-4 carbon atoms; m is 2-6; n is 0-17 and R is --CH.sub.3 ; wherein R is H or a lower alkyl group, m is 5-7 and n is 0-17.
    Type: Grant
    Filed: August 6, 1990
    Date of Patent: April 20, 1993
    Assignee: Whitby Research, Inc.
    Inventors: Gevork Minaskanian, James V. Peck, Vithal J. Rajadhyaksha
  • Patent number: 5162315
    Abstract: Pharmaceutical compositions for enhancing absorption of a topically administered formulation through dermal or mucosal membrane, for local or systemic application, comprising one or more agents of formula I: ##STR1## where: R is a saturated or unsaturated, straight or branched, cyclic or acyclic hydrocarbon group with from 1 to 19 carbon atoms or an alkoxyalkyl group; n is 2-20; X is selected from H, OR.sub.2 or NR.sub.2 R.sub.3 ; wherein R.sub.1, R.sub.2 and R.sub.3 are independently selected from H, alkyl, haloalkyl, acyl, carbalkoxy, carbalkoxyalkyl, hydroyalkyl, acyloxyalkyl, alkoxyalkyl, aminoalkyl- and acylaminoalkyl; i) with the proviso that when n is 2, X is OR.sub.2 and R.sub.2 is H, then R.sub.1 is not hydroxyalkyl, specifically, 2-hydroxyethyl; and ii) with the proviso that when n is 2 and X is NR.sub.2 R.sub.3, then R.sub.1 and R.sub.2 may combine to form a heterocyclic ring and R.sub.3 is not acyl; and iii) with the proviso that when X is NR.sub.2 R.sub.3, then R.sub.2 and R.sub.
    Type: Grant
    Filed: May 8, 1989
    Date of Patent: November 10, 1992
    Inventors: Vithal J. Rajadhyaksha, Richard S. Graham
  • Patent number: 5108991
    Abstract: Compositions useful for carrying physiologically active agents such as therapeutic agents through skin and other body membranes comprising the agent and an effective, non-toxic amount of a compound having the structural formula ##STR1## wherein R' is H or a lower alkyl group, m is 3, N is 6-11 and R is --CH.sub.3.
    Type: Grant
    Filed: December 31, 1985
    Date of Patent: April 28, 1992
    Assignee: Whitby Research, Inc.
    Inventor: Vithal J. Rajadhyaksha
  • Patent number: 5030629
    Abstract: A method and compositions for enhancing absorption of topically administered physiologically active agents through the skin and mucous membranes of humans and animals in a transdermal device or formulation for local or systemic use, comprising a therapeutically effective amount of a pharmaceutically active agent and a non-toxic, effective amount of penetration enhancing agent of the formula I: ##STR1## wherein R is a saturated or unsaturated, straight or branched, cyclic or acyclic hydrocarbon group with from 1 to 19 carbon atoms, alkoxyalkyl, haloalkyl, specifically trifluoromethyl, alkoxy, amino, alkylamino and acylamino; R' and R" are hydrogen, alkyl, trifluoromethyl, alkoxyalkyl, aminoalkyl, alkyl- and acylaminoalkyl, carboxy, carbalkoxy, hydroxyalkyl or lower alkyl ester thereof; X is O or NR.sub.1 wherein R.sub.
    Type: Grant
    Filed: August 11, 1989
    Date of Patent: July 9, 1991
    Inventor: Vithal J. Rajadhyaksha
  • Patent number: 4960771
    Abstract: Compositions for carrying physiologically active agents through body membranes having the structural formula I: ##STR1## where: R=H, Alkyl group containing from 1-18 carbon atoms, cycloalkyl, aryl, aralkyl, alkoxy, hydroxyalkyl, alkoyloxyalkyl, acyloxyalkyl and alkoxyalkyl;X=O and NR.sub.1, where R.sub.1 is selected from H, alkyl, aralkyl acyl group containing from 1-18 carbon atoms, cycloalkyl, hydroxyalkyl, alkoyloxyalkyl acyloxyalkyl and alkoxyalkyl;Y=O and NR.sub.2, where R.sub.2 is selected from H, alkyl, aralkyl, cycloalkyl, acyl group containing from 1-18 carbon atoms, hydroxyalkyl, alkoyloxyalkyl, acyloxyalkyl and alkoxyalkyl;m=2-4; andn=0-4,are disclosed.
    Type: Grant
    Filed: July 12, 1988
    Date of Patent: October 2, 1990
    Inventor: Vithal J. Rajadhyaksha
  • Patent number: 4876249
    Abstract: A method and compositions for topically administering physiologically active agents through the skin and mucous membranes of humans and animals in a transdermal device or formulation for systemic use or to the skin of humans and animals for localized use comprising applying to such skin or membrane a mixture of said physiologically active agent and a non-toxic, effective penetrating amount of penetration enhancing compound having the structural formula I: ##STR1## wherein: R is a saturated or unsaturated hydrocarbon group with from 5 to 19 carbon atoms; R' and R" are hydrogen, lower alkyl, trifluoromethyl, lower hydroxyalkyl or lower alkyl ester of lower hydroxyalkyl, with the proviso that both R' and R" are not lower hydroxyalkyl; X is O or NR.sub.1 ; R.sub.1 being hydrogen, lower alkyl, lower alkenyl, lower hydroxyalkyl or lower alkyl ester of lower hydroxyalkyl are disclosed.
    Type: Grant
    Filed: January 12, 1987
    Date of Patent: October 24, 1989
    Inventor: Vithal J. Rajadhyaksha
  • Patent number: 4833150
    Abstract: 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: Grant
    Filed: January 12, 1987
    Date of Patent: May 23, 1989
    Assignee: Nelson Research & Development Co.
    Inventors: Gevork Minaskanian, Vithal J. Rajadhyaksha
  • Patent number: 4762549
    Abstract: The disclosure describes compositions and methods for improved delivery of plant growth regulators comprising contacting a plant with a composition comprising an effective amount of a plant growth regulator and an effective delivery enhancing amount of compound having the structural formula ##STR1## wherein R' is H or a lower alkyl group having 1-4 carbon atoms, m is 3-7, n is 0-17 and R is --CH.sub.3, ##STR2## where R" is H or halogen, with the proviso that if m is 3 and R is CH.sub.3, then n is 5-17.
    Type: Grant
    Filed: April 11, 1983
    Date of Patent: August 9, 1988
    Assignee: Nelson Research & Development Co.
    Inventor: Vithal J. Rajadhyaksha
  • Patent number: 4716060
    Abstract: The coating of surfaces to impart gloss and protect from weathering, and the use of solvents in paint formulations, are disclosed; the following being exemplary: Compounds having the formula: ##STR1## wherein R.sub.1, R.sub.2, and R.sub.3 are saturated alkyls having from 2 to 20 carbon atoms therein. R.sub.1 and R.sub.2, or R.sub.2 and R.sub.3, alternatively, may be the same and form a nitrogen heterocyclic compound such as that derived from, for example, a pyrrolidine, a piperidine or a hexahydroazepine.
    Type: Grant
    Filed: May 2, 1986
    Date of Patent: December 29, 1987
    Inventors: Vithal J. Rajadhyaksha, Nelly M. Rajadhyaksha
  • Patent number: 4652573
    Abstract: 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: Grant
    Filed: March 14, 1985
    Date of Patent: March 24, 1987
    Assignee: Nelson Research & Development Co.
    Inventors: Gevork Minaskanian, Vithal J. Rajadhyaksha
  • Patent number: 4562075
    Abstract: In a method for administering systemically active agents including therapeutic agents through the skin or other body membranes of humans and animals typically in the form of a transdermal device or formulation, the improvement comprising the use therewith of an effective amount of a membrane penetration enhancer having the structural formula. ##STR1## wherein R is H or a lower alkyl group, m is 5-7 and n is 0-17.
    Type: Grant
    Filed: July 25, 1983
    Date of Patent: December 31, 1985
    Assignee: Nelson Research & Development Co.
    Inventor: Vithal J. Rajadhyaksha
  • Patent number: 4461638
    Abstract: The disclosure describes compositions and methods for improved delivery of plant nutrients comprising contacting a plant with a composition comprising an effective amount of a plant nutrient and an effective delivery enhancing amount of compound having the structural formula ##STR1## wherein R' is H or a lower alkyl group having 1-4 carbon atoms, m is 3-7, n is 0-17 and R is --CH.sub.3, ##STR2## where R" is H or halogen, with the proviso that if m is 3 and R is CH.sub.3, then n is 5-17.
    Type: Grant
    Filed: April 11, 1983
    Date of Patent: July 24, 1984
    Assignee: Nelson Research & Development Company
    Inventor: Vithal J. Rajadhyaksha
  • Patent number: 4444762
    Abstract: Compositions useful for carrying physiologically active agents such as therapeutic agents through skin and other body membranes comprising the agent and an effective, non-toxic amount of a compound having the structural formula ##STR1## wherein R' is H or a lower alkyl group, m is 3-7, N is 0-17 and R is --CH.sub.3, phenyl or substituted phenyl or ##STR2## with the proviso that if m is 3 and R is --CH.sub.3, then n is not 0-6.
    Type: Grant
    Filed: December 7, 1981
    Date of Patent: April 24, 1984
    Assignee: Nelson Research & Development Company
    Inventor: Vithal J. Rajadhyaksha
  • Patent number: 4424210
    Abstract: Compositions useful for carrying physiologically active agents such as therapeutic agents through skin and other body membranes comprising the agent and an effective, non-toxic amount of a compound having the structural formula ##STR1## wherein R' is H or a lower alkyl group, m is 3-7, N is 0-17 and R is --CH.sub.3, phenyl or substituted phenyl or ##STR2## with the proviso that if m is 3 and R is --CH.sub.3, then n is not 0-6.
    Type: Grant
    Filed: December 7, 1981
    Date of Patent: January 3, 1984
    Assignee: Nelson Research & Development Company
    Inventor: Vithal J. Rajadhyaksha
  • Patent number: 4423040
    Abstract: Compositions useful for carrying physiologically active agents such as therapeutic agents through skin and other body membranes comprising the agent and an effective, non-toxic amount of a compound having the structural formula ##STR1## wherein R' is H or a lower alkyl group, m is 3-7, N is 0-17 and R is --CH.sub.3, phenyl or substituted phenyl or ##STR2## with the proviso that if m is 3 and R is --CH.sub.3, then n is not 0-6.
    Type: Grant
    Filed: December 7, 1981
    Date of Patent: December 27, 1983
    Assignee: Nelson Research & Development Company
    Inventor: Vithal J. Rajadhyaksha
  • Patent number: 4422970
    Abstract: In a method of synthesis of 1-substituted azacycloalkan-2-ones with primary alkyl halides and aralkyl halides as alkylating agents, the improvement comprising carrying out the N-alkylation in the presence of a phase transfer catalyst having the structural formula ##STR1## where X is suitable anion; and R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are each alkyl or aralkyl groups having 1-18 carbon atoms, or R.sub.2, R.sub.3 and R.sub.4 can form a part of a heterocyclic ring, with the proviso that the combined total of carbon atoms is between 16 and 40.
    Type: Grant
    Filed: May 20, 1982
    Date of Patent: December 27, 1983
    Assignee: Nelson Research & Development Company
    Inventors: Vithal J. Rajadhyaksha, James V. Peck, Gevork Minaskanian
  • Patent number: 4415563
    Abstract: Compositions useful for carrying physiologically active agents such as therapeutic agents through skin and other body membranes comprising the agent and an effective, non-toxic amount of a compound having the structural formula ##STR1## wherein R' is H or a lower alkyl group, m is 3-7, N is 0-17 and R is --CH.sub.3, phenyl or substituted phenyl or ##STR2## with the proviso that if m is 3 and R is --CH.sub.3, then n is not 0-6.
    Type: Grant
    Filed: December 7, 1981
    Date of Patent: November 15, 1983
    Assignee: Nelson Research & Development Company
    Inventor: Vithal J. Rajadhyaksha