Donald Alan Mcafee

US Patent:

6339072, Jan 15, 2002

Filed:

Feb 15, 2001

Appl. No.:

09/783032

Inventors:

Pauline L. Martin - Boston MA
Donald A. McAfee - Richmond VA

Assignee:

Discovery Therapeutics Inc. - Richmond VA

International Classification:

A61K 3170

US Classification:

514 46, 514 45, 514 47

Abstract:

In the present invention, a method is provided which reduces or prevents restenosis following revascularization procedures. It has now been found that selective stimulation of adenosine A receptors can reduce or prevent such restenosis. This method may be achieved either by: (a) the administration of selective adenosine A receptor agonists, (b) the administration of a selective adenosine A antagonist in combination with either a selective adenosine A receptor agonist or a non-selective adenosine agonist, or (c) the administration of a selective adenosine A antagonist in order to block adenosine A receptor activation by endogenously-released adenosine. The present invention is also directed to an improved surgical procedure that relies upon selective stimulation of adenosine A receptors.

US Patent:

6372723, Apr 16, 2002

Filed:

Dec 8, 1999

Appl. No.:

09/456432

Inventors:

Pauline L. Martin - Boston MA
Donald A. McAfee - Richmond VA

Assignee:

Discovery Therapeutics, Inc. - Richmond VA

International Classification:

A61K 3170

US Classification:

514 45, 514 46

Abstract:

In the present invention, a method is provided which reduces or prevents restenosis following revascularization procedures. It has now been found that selective stimulation of adenosine A receptors can reduce or prevent such restenosis. This method may be achieved either by: (a) the administration of selective adenosine A receptor agonists, (b) the administration of a selective adenosine A antagonist in combination with either a selective adenosine A receptor agonist or a non-selective adenosine agonist, or (c) the administration of a selective adenosine A antagonist in order to block adenosine A receptor activation by endogenously-released adenosine. The present invention is also directed to an improved surgical procedure that relies upon selective stimulation of adenosine A receptors.

US Patent:

54778573, Dec 26, 1995

Filed:

Sep 10, 1993

Appl. No.:

8/119774

Inventors:

Donald A. McAfee - Richmond VA
Geoffrey Allan - Richmond VA
Richard J. Barrett - Midlothian VA

Assignee:

Discovery Therapeutics, Inc. - Richmond VA

International Classification:

A61B 600

US Classification:

128654

Abstract:

The present invention discloses a method for measuring myocardial function in a mammal in need of such measurement by: a) administering 0. 01-15. mu. g/kg/min of a compound of the formula: ##STR1## where R. sub. 1 is hydrogen or the group ##STR2## where R. sub. 3 and R. sub. 4 are the same or different and are hydrogen, C. sub. 1 to C. sub. 12 linear or branched alkyl, C. sub. 3 to C. sub. 7 cycloalkyl, C. sub. 6 to C. sub. 10 aryl unsubstituted or substituted with C. sub. 1 to C. sub. 6 linear or branched alkyl, C. sub. 1 to C. sub. 6 linear or branched alkoxy, nitro, amino, amino substituted with at least one C. sub. 1 to C. sub. 6 linear or branched alkyl or phenyl, C. sub. 2 to C. sub. 10 aralkyl, C. sub. 4 to C. sub. 8 heteroaryl wherein said heteroatom is nitrogen, phosphorous, sulfur or oxygen, and R. sub.

US Patent:

51178303, Jun 2, 1992

Filed:

Nov 8, 1990

Appl. No.:

7/610544

Inventors:

Donald A. McAfee - Richmond VA
Luiz Belardinelli - Gainesville FL

Assignee:

Whitby Research, Inc. - Richmond VA

International Classification:

A61B 600

US Classification:

128654

Abstract:

A method and composition for determining the viability of tissue in a region of an organism having a vascular circulatory system that supplies blood to said region including the steps of dilating said vascular circulation system by introducing adenosine or an adenosine agonist into said vascular circulation system in order to increase the flow of blood into said region; introducing a blood flow marking medium into said region; alleviating the non-dilating effects of adenosine or said adenosine agonist by introducing an A. sub. 1 adenosine receptor antagonist into said vascular circulatory system; and determining the amount of marking medium in said region. A composition is disclosed which includes the combination of adenosine or an adenosine agonist in combination with an A. sub. 1 adenosine receptor which may be: ##STR1## wherein R. sub. 1 is hydrogen or R. sub. 2 ; R. sub.

US Patent:

53149084, May 24, 1994

Filed:

Nov 17, 1992

Appl. No.:

7/977455

Inventors:

Donald A. McAfee - Richmond VA

Assignee:

Whitby Research, Inc. - Richmond VA

International Classification:

C07D20910

US Classification:

514415

Abstract:

Melatonin compounds are disclosed of the formula ##STR1## where R is hydrogen or C. sub. 1 to C. sub. 6 linear or branched alkylene substituted with phenyl; R. sub. 1 is hydrogen, substituted benzyl, naphthylmethyl or taken together with R. sub. 2 and the two carbon atoms of the five-membered hetero ring form the group ##STR2## where R. sub. 1 ' is C. sub. 1 to C. sub. 6 linear or branched alkanoyl and R. sub. 1 " is hydrogen, C. sub. 1 to C. sub. 6 linear or branched alkyl or phenyl optionally substituted with one or more halogen, amino, nitro, hydroxy, alkyl, alkoxy or haloalkyl; R. sub. 2 is hydrogen, 1-pyrrolyl, 1-pyrrolyl substituted with one or more alkyl or alkoxy, the group --(CH. sub. 2). sub. m --NHR. sub. 2 '1, where m is 1 to 3 and R. sub. 2 ' is phenyl sulfonyl, the phenyl group optionally substituted with alkyl, or --C(O)--R. sub.

US Patent:

52563987, Oct 26, 1993

Filed:

Jan 30, 1992

Appl. No.:

7/828115

Inventors:

Donald A. McAfee - Richmond VA
Luiz Belardinelli - Gainesville FL

Assignee:

Whitby Research, Inc. - Richmond VA

International Classification:

A61K 3152

US Classification:

424 9

Abstract:

A method and composition of determining the viability of tissue in a region of an organism having a vascular circulatory system that supplies blood to said region is disclosed. The composition includes the combination of adenosine or an adenosine antagonist in combination with an A. sub. 1 adenosine receptor which may be: ##STR1## wherein R. sub. 1 is hydrogen or R. sub. 2 ; R. sub. 2 is selected from the group consisting of endo-2-norbornyl or cyclopentyl; R. sub. 3 is selected from the group consisting of hydrogen, halogen, amine, carboxy, alkyl radicals having 1 to 10 carbon atoms, cycloalkyl radicals having from 3 to 8 ring carbon atoms, thio sulfonate, sulfonamide, sulfone, sulfoxamide, phenyl, alkyl-substituted amine, and cycloalkyl substituted amine; R. sub. 4 is selected from the group consisting of benzyl, phenyl, alkyl groups comprising from 1 to 4 carbon atoms, wherein said alkyl group can be substituted with oxygen, for instance ethers and alcohols; and R. sub. 5 is selected from the group consisting of hydrogen, hydroxy, sulfonate, halogen, alkoxy and cycloalkoxy groups comprising 1 to 6 carbon atoms.

US Patent:

52063771, Apr 27, 1993

Filed:

Dec 5, 1991

Appl. No.:

7/802723

Inventors:

Donald A. McAfee - Richmond VA

Assignee:

Whitby Research, Inc. - Richmond VA

International Classification:

C07D20910

US Classification:

548253

Abstract:

Melatonin compounds are disclosed of the formula ##STR1## where R is hydrogen or C. sub. 1 to C. sub. 6 linear or branched alkylene substituted with phenyl; R. sub. 1 is hydrogen, substituted benzyl, naphthylmethyl or taken together with R. sub. 2 and the two carbon atoms of the five-membered hetero ring form the group ##STR2## where R. sub. 1 ' is C. sub. 1 to C. sub. 6 linear or branched alkanoyl and R. sub. 1 " is hydrogen, C. sub. 1 to C. sub. 6 linear or branched alkyl or phenyl optionally substituted with one or more halogen, amino, nitro, hydroxy, alkyl, alkoxy or haloalkyl; R. sub. 2 is hydrogen, 1-pyrrolyl, 1-pyrrolyl substituted with one or more alkyl or alkoxy, the group --(CH. sub. 2). sub. m --NHR. sub. 2 '1, where m is 1 to 3 and R. sub. 2 ' is phenyl sulfonyl, the phenyl group optionally substituted with alkyl, or --C(O)--R. sub.