Abstract: The present invention provides compounds of formula (I):
and pharmaceutically acceptable salts and solvates thereof, together with processes for the preparation of, compositions containing, uses of and intermediates used in the preparation of such compounds that have A2a receptor agonist activity.
Abstract: N6 heterocyclic 8 modified adenosine derivatives that are selective, partial or full 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:
Grant
Filed:
December 3, 1999
Date of Patent:
September 25, 2001
Assignee:
CV Therapeutics, Inc.
Inventors:
Jeff A. Zablocki, Venkata P. Palle, Prabha N. Ibrahim, Luiz Belardenelli
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:
Grant
Filed:
December 3, 1999
Date of Patent:
July 10, 2001
Assignee:
CV Therapeutics, Inc.
Inventors:
Venkata P. Palle, Jeff A. Zablocki, Prabha N. Ibrahim, Vaibhav Varkhedkar, Luiz Belardenelli
Abstract: A novel process for preparing 2-halo-6-aminopurine derivatives and their analogs is disclosed. The method comprises halogenation of 2,6-diaminopurine derivatives at the C-2 position in a specific combination of aprotic polar and nonpolar organic solvents to give the corresponding halogenated derivatives.
Abstract: The present invention is directed to reduce elevated levels of tumor necrosis factor-alpha (TNF-&agr;) found in a failing heart. The present invention is directed to a composition and method of regulating TNF-&agr; expression in myocardial tissue by treating the myocardial tissue with biological equivalents of endogenous adenosine. A composition and method of using the composition to treat patients with damaged myocardial tissue is provided which increases the cellular availability of adenosine with a resulting decrease of TNF-&agr; levels in the heart. The present invention provides a novel pharmacological intervention program in failing mammalian hearts, and more particularly provides a cardioprotective treatment to patients with congestive heart failure.
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: The present invention relates to novel adenosine derivatives having the formula (I):
wherein R is a lower alkyl group; R′ is hydrogen or a lower alkyl group; X is a cycloalkyl group, an alkyl group having at least one hydroxy group, an alkyl group having at least one phenyl group, a bicycloalkyl group, a naphthylalkyl group, an acenaphthylenylalkyl group or a group of the formula (II) or (III);
Z is hydrogen, a hydroxy group or a lower alkoxy group, Q is hydrogen or a hydroxy group, A is —CH2—, —O—, —S— or shows a direct connection; Y is —(CH2)n— or shows a direct connection; n is an integer of 1 to 3; and the broken line is a double bond or a single bond.
and pharmaceutically acceptable salt thereof, which are useful as antihypertensive agents.