Osi Pharmaceuticals, Inc.

Cadus Pharmaceutical Corp.

Bryan McKibben

Arlindo Lucas Castelhano

David James Witter

Arno G Steinig

Eric W Collington

Douglas S Werner

The subject invention provides compounds having the structure: 

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This invention pertains to compounds which specifically inhibit the adenosine Areceptor and the use of these compounds to treat a disease associated with Aadenosine receptors in a subject.

Compounds specific to adenosine A, receptors and uses thereof

This invention pertains to compounds having the structure: wherein which specifically inhibit the adenosine A1 and A3 receptors and the use of these compounds to treat a disease associated with A3 adenosine receptor in a subject, comprising administering to the subject a therapeutically effective amount of the compound.

The subject invention provides compounds having the structure: wherein Ris substituted or unsubstituted phenyl or a 5-6 membered heterocyclic or heteroaromatic ring containing from 1 to 5 heteroatoms; Ris hydrogen, or a substituted or unsubstituted alkyl, &#x2014;C(O)-alkyl, &#x2014;C(O)&#x2014;O-alkyl, alkoxy, cycloalkyl, alkenyl, monocyclic or bicyclic aryl, heteroaryl or heterocyclic moiety; Ris hydrogen, or a substituted or unsubstituted alkyl, &#x2014;C(O)-alkyl, &#x2014;C(O)&#x2014;O-alkyl, alkoxy, cycloalkyl, alkenyl, monocyclic or bicyclic aryl, heteroaryl or heterocyclic moiety, or Rand Rare joined to form a heterocyclic ring; wherein the dashed line represents a second bond which may be present or absent, and when present Ris oxygen; Rand Rare each independently substituted or unsubstituted alkyl, &#x2014;C(O)-alkyl, &#x2014;C(O)&#x2014;O-alkyl, alkoxy, cycloalkyl, alkenyl, monocyclic or bicyclic aryl, heteroaryl or heterocyclic moiety, or RNRtogether form a substituted or unsubstituted monocyclic or bicyclic, heterocyclic or heteroaryl moiety containing from 1 to 6 heteroatoms;

Novel deazapurines are disclosed which are useful for the treatment of adenosine receptor stimulated diseases.

4-heterocyclo-pyrrolo[2,3d] pyrimidine compositions and their use

This invention pertains to compounds which specifically inhibit the adenosine Areceptor and the use of these compounds to treat a disease associated with Aadenosine receptor in a subject, comprising administering to the subject a therapeutically effective amount of the compounds.

The subject invention provides compounds having the structure:wherein Ris substituted or unsubstituted phenyl or a 5-6 membered heterocyclic or heteroaromatic ring containing from 1 to 5 heteroatoms; Ris hydrogen, or a substituted or unsubstituted alkyl, &#x2014;C(O)-alkyl, &#x2014;C(O)&#x2014;O-alkyl, alkoxy, cycloalkyl, alkenyl, monocyclic or bicyclic aryl, heteroaryl or heterocyclic moiety; Ris hydrogen, or a substituted or unsubstituted alkyl, &#x2014;C(O)-alkyl, &#x2014;C(O)&#x2014;O-alkyl, alkoxy, cycloalkyl, alkenyl, monocyclic or bicyclic aryl, heteroaryl or heterocyclic moiety, or Rand Rare joined to form a heterocyclic ring; wherein the dashed line represents a second bond which may be present or absent, and when present Ris oxygen; Rand Rare each independently substituted or unsubstituted alkyl, &#x2014;C(O)-alkyl, &#x2014;C(O)&#x2014;O-alkyl, alkoxy, cycloalkyl, alkenyl, monocyclic or bicyclic aryl, heteroaryl or heterocyclic moiety, or RNRtogether form a substituted or unsubstituted monocyclic or bicyclic, heterocyclic or heteroaryl moiety containing from 1 to 6 heteroatoms; Ris hydrogen, alkyl, halogen or cyano; and n is 0, 1, 2, 3 or 4, or an enantiomer, or a specific tautomer, or a pharmaceutically acceptable salt thereof and a method for treating a disease associated with the Aadenosine receptor by administering a therapeutically effective amount of the compounds of the invention.

Pyrimidine A2b selective antagonist compounds, their synthesis and use

Compounds specific to adenosine A1 receptor and uses thereof

Pyrrolo&lsqb;2,3d&rsqb;pyrimidine compositions and their use

This invention pertains to compounds which specifically inhibit the adenosine A receptor and the use of these compounds to treat a disease associated with A adenosine receptor in a subject, comprising administering to the subject a therapeutically effective amount of the compounds.

Compounds specific to adenosine A3 receptor and uses thereof

This invention pertains to compounds which specifically inhibit the adenosine A receptor and the use of these compounds to treat a disease associated with A adenosine receptors in a subject.

Compounds specific to adenosine A1 receptors and uses thereof

4-aminopyrrolo&lsqb;2,3-d&rsqb;pyrimidine compounds specific to adenosine A2a receptor and uses thereof

Methods for preparing thiophene and pyrrole-based heterocyclic compounds are disclosed. Also disclosed are libraries of thiophene and pyrrole-based heterocyclic compounds, methods for preparing the libraries of thiophene and pyrrole-based heterocyclic compounds, and methods for using the thiophene and pyrrole-based heterocyclic compounds and compound libraries of the invention. The compounds of the invention have biological activity including anti-cancer activity.

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White Plains, NY, United States of America

Bryan McKibben