Bristol-myers Squibb Compnay

Henry H Gu

Edwin J Iwanowicz

T G Murali Dhar

William John Pitts

Scott Hunter Watterson

Katerina Leftheris

Ping Chen

Chunjian Liu

Yufen Zhao

Gregory S Bisacchi

Timothy F Herpin

Tg Murali Dhar

Compounds having the formula (I), wherein Ris selected from H, OH and NH; Ris selected from &#x2550;O and &#x2550;S; W is &#x2014;C(&#x2550;O)&#x2014;, &#x2014;S(&#x2550;O)&#x2014;, or &#x2014;S(O)&#x2014;; or W may be &#x2014;CH&#x2014; if X is &#x2014;C(&#x2550;O)&#x2014;; X is selected from &#x2014;CH&#x2014;, &#x2014;N(R)&#x2014;, and &#x2014;O&#x2014;, except that when W is &#x2014;CH&#x2014;, X is &#x2014;C(&#x2550;O)&#x2014;; Y is a bond or &#x2014;C(R)(R)&#x2014;; Q is a linker; Z is optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heteroaryl, or heterocyclyl; and R, R, R, and Rare as defined in the specification.

Acridone inhibitors of IMPDH enzyme

The present invention discloses the identification of the novel inhibitors of IMPDH (inosine-5'-monophosphate dehydrogenase). The compounds and pharmaceutical compositions disclosed herein are useful in treating or preventing IMPDH associated disorders, such as transplant rejection and autoimmune diseases.

Inhibitors of IMPDH enzyme

Compounds of the formulawherein Xis C(O), &#x2014;S(O)&#x2014;, or &#x2014;S(O)&#x2014;;Xis CRor N; Xis &#x2014;NH&#x2014;, &#x2014;O&#x2014;, or &#x2014;S&#x2014;;Xis CRor N; Xis CRor N; and Xis CRor N are useful as inhibitors of IMPDH enzyme. Thus, these compounds can be used as therapeutic agents for IMPDH-associated disorders.

Heterocycles that are inhibitors of IMPDH enzyme

Compounds having the formula (I),wherein Ris selected from H, OH and NH; Ris selected from &#x2550;O and &#x2550;S; W is &#x2014;C(&#x2550;O)&#x2014;, &#x2014;S(&#x2550;O)&#x2014;, or &#x2014;S(O)&#x2014;; or W may be &#x2014;CH&#x2014; if X is &#x2014;C(&#x2550;O)&#x2014;; X is selected from &#x2014;CH&#x2014;, &#x2014;N(R)&#x2014;, and &#x2014;O&#x2014;, except that when W is &#x2014;CH&#x2014;, X is &#x2014;C(&#x2550;O)&#x2014;; Y is a bond or &#x2014;C(R)(R)&#x2014;; Q is a linker; Z is optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heteroaryl, or heterocyclyl; and X, X, X, X, X, X, X, X, X, Xand Xare selected such a tricyclic heteroaryl ring system is formed as further defined in the specification.

Heterocyclic acridone inhibitors of IMPDH enzyme

The present invention discloses the identification of the inhibitors of IMPDH (inosine-5&prime;-monophosphate dehydrogenase). The compounds and pharmaceutical compositions disclosed herein are useful in treating or preventing IMPDH associated disorders, such as transplant rejection and autoimmune diseases.

Amide and diamide inhibitors of IMPDH enzyme for use in treating IMPDH-associated disorders

Compounds derived from an amine nucleus and pharmaceutical compositions comprising same

The present invention discloses the identification of the novel inhibitors of IMPDH (inosine-5&prime;-monophosphate dehydrogenase). The compounds and pharmaceutical compositions disclosed herein are useful in treating or preventing IMPDH mediated diseases, such as transplant rejection and autoimmune diseases.

Growing community of inventors

Bordentown, NJ, United States of America

Henry H Gu