Takeda Pharmaceutical Company Limited

Cmg Pharmaceutical Co., Ltd.

The Asan Foundation

Sungkwang Medical Foundation

Suk Young Cho

Albert Charles Gyorkos

Christopher Peter Corrette

Kazuyoshi Aso

Eun Kyung Choi

Jeongbeob Seo

Gilnam Lee

Choung Soo Kim

Jung Jin Hwang

Jin Sung Kim

Masakuni Kori

Michiyo Mochizuki

Christopher Stephen Siedem

Scott Alan Pratt

Timothy Mark Turner

Chul Soo Lim

Han Won Cho

Steven Armen Boyd

Kevin Ronald Condroski

Hee Jung An

Hye Sun Jeon

Yong Wha Moon

Jung Shin Lee

Chul Yun Rhim

Michiyo Gyoten

Ki Joon Jeon

The invention provides novel substituted heterocyclic compounds represented by Formula I and Formula II, or a pharmaceutically acceptable salt, solvate, polymorph, ester, tautomer or prodrug thereof, and a composition comprising these compounds. The compounds provided can be used as inhibitors of MEK and are useful in the treatment of inflammatory diseases, cancer and other hyperproliferative diseases. The invention further provides a method of treatment for inflammatory diseases, cancer and other hyperproliferative diseases in mammals, especially humans.

Substituted pyridinone compounds as MEK inhibitors

The invention provides novel substituted pyridopyrimidines represented by Formula I or a pharmaceutically acceptable salt, solvate, polymorph, ester, tautomer or prodrug thereof, and a composition comprising these compounds. The compounds provided can be used as inhibitors of the phosphoinositide 3' OH kinase family (PI3K) for the treatment of inflammatory diseases, cancer, cardiovascular diseases, allergy, asthma and autoimmune disorders. 

Pyridopyrimidine derivatives and use thereof

There is provided a CRF receptor antagonist comprising a compound of the formula (I): wherein Ris an optionally substituted hydrocarbyl, an optionally substituted C-linked heterocyclic group, an optionally substituted N-linked heteroaryl group, a cyano or an acyl; Ris an optionally substituted cyclic hydrocarbyl or an optionally substituted heterocyclic group; X is oxygen, sulfur or &#x2014;NR&#x2014; (wherein Ris a hydrogen, an optionally substituted hydrocarbyl or an acyl); Y, Yand Yare each an optionally substituted carbon or a nitrogen, provided that one or less of Y, Yand Yis nitrogen; and Z is a bond, &#x2014;CO&#x2014;, oxygen, sulfur, &#x2014;SO&#x2014;, &#x2014;SO&#x2014;, &#x2014;NR&#x2014;, &#x2014;NR-alk-, &#x2014;CONR&#x2014; or &#x2014;NRCO&#x2014; (wherein alk is an optionally substituted Calkylene and Ris a hydrogen, an optionally substituted hydrocarbyl or an acyl); or a salt thereof or a prodrug thereof.

Fused heterocyclic compounds

There is provided a CRF receptor antagonist comprising a compound of the formula (I):A-W&#x2014;Ar&#x2003;&#x2003;(I) 

Cyclic compounds

There is provided a CRF receptor antagonist comprising a compound of the formula (I): wherein, ring A is a 5-membered ring represented by the formula (A'): wherein X is a carbon and Xis an oxygen, a sulfur or &#x2014;NR&#x2014;, or formula (A&#x2033;): wherein X is a nitrogen and Ris an optionally substituted hydrocarbyl, Ris an amino substituted by two optionally substituted hydrocarbyl groups, Ris an phenyl, Yis CRor a nitrogen, Yis CRor a nitrogen and Yis CRor a nitrogen, provided that one or less of Y, Y, and Yis nitrogen, W is a bond, &#x2014;(CH)n-, and Z is a bond, &#x2014;NR&#x2014;, etc.; or a salt thereof or a prodrug thereof.

Nitrogen-containing fused heterocyclic compounds

Growing community of inventors

Chungcheongnam-do, South Korea

Suk Young Cho