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Inventor:
Jacobson; Kenneth A.
Address:
Silver Spring, MD
No. of patents:
34
Patents:












Patent Number Title Of Patent Date Issued
8153781 Dendrimer conjugates of agonists and antagonists of the GPCR superfamily April 10, 2012
Disclosed are conjugates comprising a dendrimer and a ligand, which is a functionalized congener of an agonist or antagonist of a receptor of the G-protein coupled receptor (GPCR) superfamily, for example, wherein the functionalized congener is an A.sub.1 adenosine receptor agonist havin
7825126 Purine derivatives as A3 and A1 adenosine receptor agonists November 2, 2010
Disclosed are (N)-methanocarba adenine nucleosides of the formula: ##STR00001## as highly potent A.sub.3 adenosine receptor agonists, pharmaceutical compositions comprising such nucleosides, and a method of use of these nucleosides, wherein R.sub.1-R.sub.6 are as defined in the spec
7790735 Methanocarba cycloalkyl nucleoside analogues September 7, 2010
The present invention provides novel nucleoside and nucleotide derivatives that are useful agonist or antagonists of P1 and P2 receptors. For example, the present invention provides a compound of formula A-M, wherein A is modified adenine or uracil and M is a constrained cycloalkyl g
7348315 Methods of treating heart failure with modified ATP, ADP and AMP compounds March 25, 2008
Disclosed herein are methods of using an adenosine analog or derivative for treating heart failure, increasing cardiac muscle contractility, increasing cardiac diastolic relaxation, and increasing vasodilation. Exemplary adenosine analogs/derivatives include compounds of the followin
7199127 Purine nucleosides April 3, 2007
Disclosed are purine nucleoside compounds that are selective to A.sub.3 adenosine receptors and are useful for the treatment of cancer and inflammatory diseases. The compounds are shown by the following general formula (I), including isomers thereof: ##STR00001## wherein X is sulfur
7087589 Methanocarba cycloakyl nucleoside analogues August 8, 2006
The present invention provides novel nucleoside and nucleotide derivatives that are useful agonists or antagonists of P1 or P2 receptors. For example, the present invention provides a compound of formula A-M, wherein A is modified adenine or uracil and M is a constrained cycloalkyl g
6586413 Methods and compositions for reducing ischemic injury of the heart by administering adenosine re July 1, 2003
Compositions and methods for reducing or preventing ischemic damage of the heart are disclosed. A preferred embodiment of the invention comprises the simultaneous administration of specific A3/A1 receptor agonists, to patients suffering from ischemic damage or at risk for the same. In ye
6545002 Substituted 8-phenylxanthines useful as antagonists of A2B adenosine receptors April 8, 2003
The present invention provides compounds having the formula I: ##STR1## X is (C.sub.1 -C.sub.8)alkylene, (C.sub.2 -C.sub.8)alkenylene, (C.sub.2 -C.sub.8)alkynylene, wherein one of the carbon atoms in the alkylene, alkenylene or alkynylene groups is optionally replaced with a group hav
6376521 A3 adenosine receptor antagonists April 23, 2002
Disclosed are pyridine and dihydropyridine derivatives, pharmaceutical compositions comprising one or more of these derivatives, and a method of selectively blocking an A.sub.3 adenosine receptor of a mammal by the use of one or more of these derivatives. An example of the pyridine deriv
6316423 Method of treating ischemic, hypoxic and anoxic brain damage November 13, 2001
The present invention provides a method of treating ischemic, hypoxic or anoxic brain damage in an animal comprising administering to an animal afflicted with ischemic, hypoxic, or anoxic brain damage, or an animal in imminent danger of suffering ischemic, hypoxic, or anoxic brain damage
6083954 Method of treating cystic fibrosis July 4, 2000
The present invention provides a method of identifying CFTR-binding compounds for treating cells having a reduced apical Cl.sup.- conductance, such as cystic fibrosis cells. This identification method involves the use of polypeptide I.alpha., which constitutes a portion of the CFTR p
6066642 Dihydropyridine-, pyridine-, benzopyran-4-one- and triazoloquinazoline derivative, their prepara May 23, 2000
The present invention provides certain novel compounds, compositions, and a method of treating a mammal by blocking its adenosine receptors comprising administering at least one compound of the present invention. Examples of the present inventive compounds include certain flavonoids of f
5877179 Xanthines for identifying CFTR--binding compounds useful for activating chloride conductance in March 2, 1999
The present invention provides novel compounds and pharmaceutical compositions comprising such compounds useful for treating cystic fibrosis cells, wherein such compounds have the formula ##STR1## wherein (a) R.sub.1 and R.sub.3 are methyl, R.sub.7 is ethyl or cyclopropylmethyl,
5861405 S-substituted 1,3,7-trialkyl-xanthine derivatives January 19, 1999
The present invention provides 8-substituted 1,3,7-trialkylxanthines useful as A.sub.2 -selective adenosine receptor antagonists and compositions comprising such compounds. Examples of the 8-substituted 1,3,7-trialkyl xanthines include: ##STR1## In compound (a), R.sub.1, R.sub.3,
5859019 Methods for protecting against cardiac ischemia by administering adenosine A.sub.2a receptor ant January 12, 1999
Methods for reducing or preventing ischemic damage of the heart are disclosed. A preferred embodiment of the invention comprises the administration of a specific A.sub.2a receptor antagonist, 8-(3-chlorostyryl) caffeine, to patients suffering from ischemic damage or at risk for the s
5773423 A3 adenosine receptor agonists June 30, 1998
The present invention provides N.sup.6 -benzyladenosine-5'-N-uronamide and related substituted compounds, particularly those containing substituents on the benzyl and/or uronamide groups, and modified xanthine ribosides, as well as pharmaceutical compositions containing such compounds. T
5688774 A.sub.3 adenosine receptor agonists November 18, 1997
The present invention provides A.sub.3 selective agonists, particularly, adenine compounds having selected substituents at the 2, 6, and 9 positions, and related substituted compounds, particularly those containing substituents on the benzyl and/or uronamide groups, as well as pharma
5620676 Biologically active ATP analogs April 15, 1997
The present invention provides certain novel adenosine triphosphate (ATP) analogs, pharmaceutical compositions, and methods of using such analogs in the treatment of septic shock and other disease conditions. Examples of the ATP analogs include the mono-, di- and triphosphates of adenosi
5545627 Irreversible inhibitors of adenosine receptors August 13, 1996
Irreversible ligands for adenosine receptors are derived from agonist and antagonist functionalized congeners which contain electrophilic acylating and alkylating groups for reaction at nucleophilic residues of adenosine receptors. The ligands are based on 8-aryl-substituted xanthines as
5498605 Sulfo-derivatives of adenosine March 12, 1996
The adenosine derivatives which contain a sulfohydrocarbon substituent, as depicted in the formula: ##STR1## wherein at least one of R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, and R.sub.6 is a sulfohydrocarbon radical and W is --OCH.sub.2 --, --NHCH.sub.2 --, --SCH.sub.2 --, or
5453426 Sulfur-containing xanthine derivatives as adenosine antagonists September 26, 1995
The present invention provides sulfur-containing xanthine derivatives which are 1,3-disubstituted with a C.sub.1 -C.sub.12 alkyl, which may be further substituted with a hydroxy, amino, or halo group, and are 8-substituted with either a cycloalkyl, furyl, thienyl, or substituted phenyl g
5366977 Method of treating cystic fibrosis using 8-cyclopentyl-1,3-dipropylxanthine or xanthine amino co November 22, 1994
A method of treating cells having a reduced apical Cl.sup.- conductance, such as that characteristic of cystic fibrosis cells, by contacting cells having a reduced apical Cl.sup.- conductance with a therapeutically effective quantity of a compound that antagonizes the A.sub.1 -adenosine
5324832 Muscarinic antagonists June 28, 1994
Muscarinic antagonists formed by substitution of the distal N-methyl group of pirenzepine or telenzepine. The group used for substitution can be, for example, a propargyl group, a benzyl group, a substituted benzyl group, a hydroxyethyl group, a chloroethyl group, an aminoethyl group, an
5310916 Trifunctional agents useful as irreversible inhibitors of A1-adenosine receptors May 10, 1994
Trifunctional agents useful as inhibitors of A.sub.1 -Adenosine receptors may be formulated into pharmaceutical compositions. These agents are represented by formula (I): ##STR1## wherein X is CH or N, R is an isothiocyanate group, an amino group or --NHCO.sub.2 C(CH.sub.3).sub.3
5298508 Irreversible inhibitors of adenosine receptors March 29, 1994
Irreversible ligands for adenosine receptors are derived from agonist and antagonist functionalized congeners which contain electrophilic acylating and alkylating groups for reaction at nucleophilic residues of adenosine receptors. The ligands are based on 8-aryl-substituted xanthines as
5284834 Adenosine functionalized congeners as cardiovascular treating agents for animals and methods for February 8, 1994
This invention comprises a series of N.sup.6 -substituted adenosine analogues bearing functionalized chains for the covalent attachment to probes or solid supports. In these compounds coronary vasodilation in the open thorax dog model, typical of A.sub.2 -adenosine receptor agonists, is
5280015 2-substituted adenosines and 2-substituted adenosine 5'-carboxamides January 18, 1994
The present invention is directed to compounds useful as probes for characterizing and studying the adenosine A.sub.2 receptor. The present invention is also directed to methods of treating central nervous system disorders and cardiovascular disorders which include treating hypertension
5274121 N-methyl-N-[4-(1-pyrrolidinyl)-2-butynyl]amide congeners as muscarinic agents December 28, 1993
Compounds, which are muscarinic agents, having the formula ##STR1## wherein Am is --N(R).sub.a).sub.2, --N(R.sub.a).sub.3.sup.+ I.sup.-, --N (CH.sub.2).sub.n', or ##STR2## n' is an integer from 2 to 7 and R.sub.a is an alkyl having 1 to 4 carbon atoms, and each R.sub.a may be
5248770 Molecular probes for adenosine receptors September 28, 1993
This application discloses probes for adenosine receptors which are functionalized congeners of the following compound: ##STR1## wherein R is --CH.sub.2 --C(O)--R' or ##STR2## These probes bind to A.sub.2 and A.sub.3 adenosine receptors and aid in quantifying and characterizi
5098996 Process for introducing fluorine into biologically active materials March 24, 1992
Radioactive fluorine can be easily introduced into biologically active molecules containing amino groups. A p-bromomethyl benzoyl group is coupled to the amino group of the biologically active molecule, and bromine is displaced by fluorine. Alternatively, the bromine on the bromometh
4968672 Adenosine receptor prodrugs November 6, 1990
A functionalized congener approach to drugs acting at A.sub.1 and A.sub.2 adenosine receptor types is applicable to prodrug design. The prodrugs affect a more efficient delivery of the drug at the particular site of the body affected and take advantage of selective biochemical cleavages
4908322 Derivatization of amines for electrochemical detection March 13, 1990
Primary and secondary amines in biological fluids are selectively derivitized by reaction with esters of N-hydroxysuccinimide or N-hydroxysulfosuccinimide to form an N-acylated derivative. Those N-acylated derivatives may then be extracted into a polar organic phase and extracted. No
4696932 Biologically-active xanthine derivatives September 29, 1987
Certain functionalized cogeners of 1,3-dialkylxanthine exhibit high potency and selectivity as antagonists for A.sub.1 - and A.sub.2 -adenosine receptors and are suitable for attachment to probes, drug carriers, or solid supports. These derivatives are characterized by the presence of a
4612315 Biologically-active 1,3-dipropyl-8-phenylxanthine derivatives September 16, 1986
Certain functionalized congeners of 1,3-dialkylxanthine exhibit high potency and selectivity as antagonists for A.sub.1 - and A.sub.2 -adenosine receptors and are suitable for attachment to probes, drug carriers, or solid supports. These derivatives are characterized by the presence










 
 
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