Cortech, Inc.

Takeda Pharmaceutical Company Limited

The Asan Foundation

Sungkwang Medical Foundation

Crestone, Inc.

Cmg Pharmaceutical Co., Ltd.

Albert Charles Gyorkos

Lyle W Spruce

Christopher Peter Corrette

Suk Young Cho

Scott Alan Pratt

John C Cheronis

Kazuyoshi Aso

Tsuneo Yasuma

Kazuyuki Ohmoto

Masato Yoshida

Hiroyuki Kimura

Masakuni Kori

Michiyo Mochizuki

Eun Kyung Choi

Jeongbeob Seo

Gilnam Lee

Akira Mori

Christopher Stephen Siedem

Masahiro Kawase

Kazuhito Kawabata

Jung Jin Hwang

Choung Soo Kim

Axel H Leimer

Timothy Mark Turner

Chul Soo Lim

Han Won Cho

Nebojsa Janjic

Jin Sung Kim

Steven Armen Boyd

Xicheng David Sun

Kevin Ronald Condroski

Sarah A Strong

John M Young

Eric T Whalley

Joseph Guiles

Val S Goodfellow

Hee Jung An

Yong Wha Moon

James Ivan Gerrity

Michiyo Gyoten

There is provided a calcium receptor modulator comprising a compound of the formula (I): wherein ring A is an optionally substituted 5- to 7-membered ring; ring B is an optionally substituted 5- to 7-membered heterocyclic ring; Xis CR, CRR, N or NR; Xis N or NR; Y is C, CRor N, Z is CR, CRR, N or NR; Ar is an optionally substituted cyclic group; R is H, an optionally substituted hydrocarbon group, etc.; andis a single bond or a double bond; R, R, R, R, R, R, Rand Rare independently H, an optionally substituted hydrocarbon group; or a salt thereof or a prodrug thereof. Compounds of the formula (II) and (III): wherein ring A is an optionally substituted 5- to 7-membered ring; Q is C, CRor N; R, R, R, Rand Rare independently, H, an optionally substituted hydrocarbon group, etc., or a salt thereof are also provided. Also specify X, R, R, Y and Xin formula (II) and (III) as before.

Substituted pyrazolo[1,5-A] pyrimidines as calcium receptor modulating agents

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

Novel compounds in enantiomeric excess that are inhibitors of bacterial methionyl synthetase (MetRS) are disclosed. Also disclosed are methods for their preparation and their use in therapy as antibacterial agents, and in particular their use in therapy forinfection.

Enantiomeric compounds with antibacterial activity

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

There is provided a calcium receptor modulator comprising a compound of the formula (I): wherein ring A is an optionally substituted 5- to 7-membered ring; ring B is an optionally substituted 5- to 7-membered heterocyclic ring; Xis CR, CRR, N or NR; Xis N or NR; Y is C, CRor N, Z is CR, CRR, N or NR; Ar is an optionally substituted cyclic group; R is H, an optionally substituted hydrocarbon group, etc.; and&#x2009;is a single bond or a double bond; R, R, R, R, R, R, Rand Rare independently H, an optionally substituted hydrocarbon group; or a salt thereof or a prodrug thereof. Compounds of the formula (II) and (III): wherein ring A is an optionally substituted 5- to 7-membered ring; Q is C, CRor N; R, R, R, Rand Rare independently, H, an optionally substituted hydrocarbon group, etc., or a salt thereof are also provided. Also specify X, R, R, Y and Xin formula (II) and (III) as before.

Substituted pyrazolo [1,5-A]pyrimidines as calcium receptor modulating agents

The present invention relates to certain substituted oxadiazole, thiadiazoles and triazole peptoids which are useful as inhibitors of serine proteases. Compounds of the invention are useful for treating, for example, adult respiratory distress syndrome, septic shock, and myocardial ischemia-reperfusion injury.

Serine protease inhibitors

Certain substituted oxadiazole, thiadiazole and triazole peptoids which are useful as inhibitors of serine proteases, are prepared in various embodiments using Grignard reagents and alkyllithium reagents and various aldehydes to make oxadiazole, thiadiazole and triazole peptoid alcohols, which are then oxidized to the desired keto products.

The present invention relates to certain substituted oxadiazole peptoids and nonpeptoids useful as inhibitors of serine proteases, especially human neutophil elastase (HNE). Compounds of the present invention are useful for the treatment or amelioration of symptoms of adult respiratory distress syndrome, septic shock, and multiple organ failure. Processes mediated by HNE are also implicated in conditions such as arthritis, periodontal disease, glomerulonephritis, and cystic fibrosis.

Peptoid and nonpeptoid containing &agr;-keto oxadiazoles as serine protease inhibitors

Peptoid and nonpeptoid containing alpha-keto oxadiazoles as serine protease inhibitors

Provided are methods of inhibiting the activity of a serine protease using protease inhibitors that include an alpha-keto heterocycle in their structure. The methods are useful in the treatment of ischemic heart or treatment of symptoms associated with blood coagulation disorders. Also provided are methods for detecting or quantifying the activity of a serine protease in a pure sample.

Serine protease inhibitors comprising .alpha.-keto heterocycles

The present invention relates to certain compounds comprising substituted oxadiazole, thiadiazole and triazole structures which are useful as inhibitors of serine proteases, including human neutrophil elastase (HNE). Compounds described herein are characterized by their relatively low molecular weight, high potency and selectivity with respect to HNE, and can be used to effectively prevent, alleviate or otherwise treat disease states characterized by the degradation of connective tissue by proteases in humans.

Serine protease inhibitors-tripeptoid analogs

Growing community of inventors

Westminster, CO, United States of America

Albert Charles Gyorkos