Bristol-myers Squibb Compnay

Cerep Sa

Other

Edwin J Iwanowicz

T G Murali Dhar

Henry H Gu

Eric Nicolai

Michele Launay

Dominique Potin

Magali Jeannine Blandine Maillet

Scott Hunter Watterson

Katerina Leftheris

Ping Chen

Chunjian Liu

William John Pitts

Joel C Barrish

Jagabandhu Das

Derek J Norris

Yufen Zhao

Toomas Mitt

Kyoung S Kim

Gregory S Bisacchi

Spencer David Kimball

Jacques Y Roberge

Wen-Ching Han

Timothy F Herpin

Gary L Schieven

Ramesh Padmanabha

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

The present invention is directed to compounds having the formula (I): useful in treating inflammatory and immune diseases, in which K and L are independently, O or S; Q is &#x2014;C(&#x2550;O)&#x2014; or optionally substituted Calkylene; Ar is optionally-substituted aryl or heteroaryl; J, J, Jand Y are selected so that ring A is a five-to-six membered optionally-substituted cycloalkenyl or heterocyclo ring having 0 to 2 nitrogen heteroatoms; Ris N or C(R); and R, and R, are as defined in the specification.

Spiro-cyclic compounds useful as anti-inflammatory agents

Compounds having the formula (I), and pharmaceutically-acceptable salts, hydrates, enantiomers, and diastereomers, and prodrugs thereof, are useful as inhibitors of LFA-1/ICAM and as anti-inflammatory agents, wherein L and K are O or S; Z is N or CR; Ar is an optionally-substituted aryl or heteroaryl; G is a linker attached to T or M or is absent; J, M and T are selected to define a three to six membered saturated or partially unsaturated non-aromatic ring; and R, R, R, and Rare as defined in the specification.

Spiro-hydantoin compounds useful as anti-inflammatory agents

Compounds having the formula (I), and pharmaceutically-acceptable salts, hydrates, enantiomers, and diastereomers, and prodrugs thereof,are useful as inhibitors of LFA-1/ICAM and as anti-inflammatory agents, wherein L and K are O or S; Z is N or CR; Ar is an optionally-substituted aryl or heteroaryl; G is a linker attached to T or M or is absent; J, M and T are selected to define a three to six membered saturated or partially unsaturated non-aromatic ring; and R,R, R, and Rare as defined in the specification.

The present invention is directed to compounds having the formula (I):useful in treating inflammatory and immune diseases, in which K is O or S; Q is &#x2014;C(&#x2550;O)&#x2014; or optionally substituted Calkylene; Ar is optionally-substituted aryl or heteroaryl; J, J, J, and Y are selected so that ring A is a five-to-six membered optionally-substituted cycloalkenyl or heterocyclo ring having 0 to 2 nitrogen heteroatoms; Z is N or C(R); and R, R, Rand Rare as defined in the specification.

Hexahydro-benzimidazolone compounds useful as anti-inflammatory agents

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

Hydantoin compounds useful as anti-inflammatory agents

Urazole compounds useful as anti-inflammatory agents

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

Amino-substituted compounds useful as inhibitors of IMPDH enzyme

Compounds derived from an amine nucleus and pharmaceutical compositions comprising same

Growing community of inventors

Cranbury, NJ, United States of America

Edwin J Iwanowicz