Abstract: The invention relates to nucleoside derivatives with photolabile protecting groups of general formula (I), where R1=H, F, Cl, Br, I, NO2; R2=H, CN, where R1 and R2 are not simultaneously H; R3=H, 1-4 C alkyl, phenyl; R4=H or a conventional functional group for the synthesis of oligonucleotides; R5=H, OH, halogen or XR6, where X=O or S and R6=a conventional nucleotide protecting group; B=adenine, cytosine, guanine, thymine, uracil, 2,6-diaminopurin-9-yl, hypoxanthin-9-yl, 5-methylcytosin-1-yl, 5-amino-4-imidazolcarboxamid-1-yl or 5-amino-4-imidazolcarboxamid-3-yl, where, if B=adenine, cytosine or guanine the primary amine functionality, optionally, carries a permanent protecting group. Furthermore, these derivatives may be used for the light-controlled synthesis of oligonucleotides on a DNA chip.
Type:
Application
Filed:
March 29, 2002
Publication date:
October 10, 2002
Inventors:
Wolfgang Pfleiderer, Sigrid Buhler, Heiner Giegrich
Abstract: N6 heterocyclic 5′ modified adenosine derivatives that are adenosine A1 receptor partial or full agonists, and as such, are useful for modifying cardiac activity, modifying adipocyte function, treating central nervous system disorders, and treating diabetic disorders and obesity in mammals, and especially in humans.
Type:
Application
Filed:
June 8, 2001
Publication date:
March 28, 2002
Applicant:
CV Therapeutics, Inc.
Inventors:
Venkata P. Palle, Jeff A. Zablocki, Prabha N. Ibrahim, Vaibhav Varkhedkar, Luiz Belardinelli
Abstract: 2-adenosine propargyl phenyl ether compositions having the following formula:
and methods for using the compositions as A2A receptor agonists to stimulate mammalian coronary vasodilatation for therapeutic purposes and for purposes of imaging the heart.
Type:
Grant
Filed:
June 22, 1999
Date of Patent:
January 30, 2001
Assignee:
CV Therapeutics, Inc.
Inventors:
Jeff A. Zablocki, Venkata P. Palle, Elfatih O. Elzein, Grigory Nudelman
Abstract: Compounds of the formula
are disclosed, wherein R1, represents secondary alkyl; aralkyl; cycloalkyl; heteroaryl substituted alkyl; norbornyl; and substituted secondary alkyl, aralkyl, cycloalkyl, heteroaryl substituted alkyl, norbornyl; and para-substituted phenyl groups; and R2 and R3 are hydrogen or pharmacologically acceptable acyl groups. The compounds of the invention are useful as cardiovascular vasodilator or anti-hypertensive agents. The therapeutically useful compounds of the invention as well as similar 5-N and N-6 substituted adenosine 5-uronamides are prepared, in accordance with a novel process, from isopropylidene (or otherwise suitably blocked) inosine-5′-uronic acid. Isopropylideneinosine-5′-uronic acid is reacted with a suitable inorganic acid halide, such as thionyl chloride, to yield 6-halogeno-9-[2′,3′-O-isopropylidene-&bgr;-D-ribofuranosyl-5-uronic acid halide]-9H-purine.