- Discovery of a Potent, S1P(3)-Sparing Benzothiazole Agonist of Sphingosine-1-Phosphate Receptor 1 (S1P(1))
[作者：LANMAN BRIAN A; CEE VICTOR J; CHERUKU SRINIVASA R; FROHN MIKE; GOLDEN JENNIFER; LIN JIAN; LOBERA MERCEDES; MARANTZ YAEL; MULLER KRISTINE M; NEIRA SUSANA C; PICKRELL ALEXANDER J; RIVENZONSEGAL DALIA; SCHUTZ NILI; SHARADENDU ANURAG; YU XIANG; ZHANG ZHAODA; BUYS JANET; FIORINO MIKE; GORE ANU; HORNER MICHELLE; ITANO ANDREA; MCELVAIN MICHELE; MIDDLETON SCOT; SCHRAG MICHAEL; VARGAS HUGO M; XU HAN; XU YANG; ZHANG XUXIA; SIU JERRY; BUERLI ROLAND W,期刊：ACS Medicinal Chemistry Letters, 页码：102-106 , 文章类型： Article，,卷期：2011年2-2]
- Optimization of a benzofuranyl SIP, agonist lead compound (3) led to the discovery of 1-(3-fluoro-4-(5-(2-fluorobenzyl)benzo[d]thiazol-2-yl)benzyl)-azetidine- 3-carboxylic acid (14), a potent SIP, agonist with minimal ac...
- Discovery of AMG 369, a Thiazolo[5,4-b]pyridine Agonist of S1P(1) and S1P(5)
[作者：CEE VICTOR J; FROHN MIKE; LANMAN BRIAN A; GOLDEN JENNIFER; MULLER KRISTINE; NEIRA SUSANA; PICKRELL ALEX; ARNETT HEATHER; BUYS JANET; GORE ANU; FIORINO MIKE; HORNER MICHELLE; ITANO ANDREA; LEE MATT R; MCELVAIN MICHELE; MIDDLETON SCOT; SCHRAG MICHAEL; RIVENZONSEGAL DALIA; VARGAS HUGO M; XU HAN; XU YANG; ZHANG XUXIA; SIU JERRY; WONG MIN; BUERLI ROLAND W,期刊：ACS Medicinal Chemistry Letters, 页码：107-112 , 文章类型： Article，,卷期：2011年2-2]
- The optimization of a series of thiazolopyridine S1P(1) agonists with limited activity, at the S1P(3) receptor is reported. These efforts resulted in the discovery of 1-(3-fluoro-4-(5-(1-phenylcycloprol)thiazolo[5,4-b]py...
- Inhibition of the Hematopoietic Protein Tyrosine Phosphatase by Phenoxyacetic Acids
[作者：BOBKOVA EKATERINA V; LIU WALLACE H; COLAYCO SHARON; RASCON JUSTIN; VASILE STEFAN; GASIOR CARLTON; CRITTON DAVID A; CHAN XOCHELLA; DAHL RUSSELL; SU YING; SERGIENKO EDUARD; CHUNG THOMAS D Y; MUSTELIN TOMAS; PAGE REBECCA; TAUTZ LUTZ,期刊：ACS Medicinal Chemistry Letters, 页码：113-118 , 文章类型： Article，,卷期：2011年2-2]
- Protein tyrosine phosphatases have only recently become the focus of attention in the search for novel drug targets despite the fact that they play vital roles in numerous cellular processes and are implicated in many hu...
- Identification of Potent and Selective Glucosylceramide Synthase Inhibitors from a Library of N-Alkylated Iminosugars
[作者：GHISAIDOOBE AMAR; BIKKER PIETER; DE BRUIJN ARJAN C J; GODSCHALK FRITHJOF D; ROGAAR EVA; GUIJT MARIEKE C; HAGENS PETER; HALMA JERRE M; VANT HART STEVEN M; LUITJENS STIJN B; VAN RIXEL VINCENT H S; WIJZENBROEK MARK; ZWEEGERS THOR; DONKERKOOPMAN WILMA E; STRIJLAND ANNEKE; BOOT ROLF; VAN DER MAREL GIJS; OVERKLEEFT HERMAN S; AERTS JOHANNES M F G; VAN DEN BERG RICHARD J B H N,期刊：ACS Medicinal Chemistry Letters, 页码：119-123 , 文章类型： Article，,卷期：2011年2-2]
- Glucosylceramide synthase (GCS) is an important target for clinical drug development for the treatment of lysosomal storage disorders and a promising target for combating type 2 diabetes. Iminosugars are useful leads for...
- Discovery of PSI-353661, a Novel Purine Nucleotide Prodrug for the Treatment of HCV Infection
[作者：CHANG WONSUK; BAO DONGHUI; CHUN BYOUNGKWON; NADUTHAMBI DEVAN; NAGARATHNAM DHANAPALAN; RACHAKONDA SUGUNA; REDDY P GANAPATI; ROSS BRUCE S; ZHANG HAIREN; BANSAL SHALINI; ESPIRITU CHRISTINE L; KEILMAN MEG; LAM ANGELA M; NIU CONGRONG; STEUER HOLLY MICOLOCHICK; FURMAN PHILLIP A; OTTO MICHAEL J; SOFIA MICHAEL J,期刊：ACS Medicinal Chemistry Letters, 页码：130-135 , 文章类型： Article，,卷期：2011年2-2]
- Hepatitis C virus afflicts approximately 180 million people worldwide, and the development of direct acting antivirals may offer substantial benefit compared to the current standard of care. Accordingly, prodrugs of 2'-d...
- Discovery of Novel Cyanamide-Based Inhibitors of Cathepsin C
[作者：LAINE DRAMANE; PALOVICH MICHAEL; MCCLELAND BRENT; PETITJEAN EMILIE; DELHOM ISABELLE; XIE HAIBO; DENG JIANGHE; LIN GUOLIANG; DAVIS RODERICK; JOLIT ANAIS; NEVINS NEYSA; ZHAO BAOGUANG; VILLA JIM; SCHNECK JESSICA; MCDEVITT PATRICK; MIDGETT ROBERT; KMETT CASEY; UMBRECHT SANDRA; PECK BRIAN; DAVIS ALICIA BACON; BETTOUN DAVID,期刊：ACS Medicinal Chemistry Letters, 页码：142-147 , 文章类型： Article，,卷期：2011年2-2]
- The discovery of potent and selective cyanamide-based inhibitors of the cysteine protease cathepsin C is detailed. Optimization of the template with regard to plasma stability led to the identification of compound 17, a ...
- Novel 3-Aryl Indoles as Progesterone Receptor Antagonists for Uterine Fibroids
[作者：RICHARDSON TIMOTHY I; CLARKE CHRISTIAN A; YU KUOLONG; YEE YING K; BLEISCH THOMAS J; LOPEZ JOSE E; JONES SCOTT A; HUGHES NORMAN E; MUEHL BRIAN S; LUGAR CHARLES W; MOORE TERRY L; SHETLER PAMELA K; ZINK RICHARD W; OSBORNE JOHN J; MONTROSERAFIZADEH CHAHRZAD; PATEL NITA; GEISER ANDREW G; GALVIN RACHELLE J SELLS; DODGE JEFFREY A,期刊：ACS Medicinal Chemistry Letters, 页码：148-153 , 文章类型： Article，,卷期：2011年2-2]
- We report the synthesis and characterization of novel 3-aryl indoles as potent and efficacious progesterone receptor (PR) antagonists with potential for the treatment of uterine fibroids. These compounds demonstrated exc...
- Discovery of a Potent Nicotinic Acid Receptor Agonist for the Treatment of Dyslipidemia
[作者：QIN JUN; RAO ASHWIN; CHEN XIAO; ZHU XIAOHONG; LIU ZHIDAN; HUANG XIANHAI; DEGRADO SYLVIA; HUANG YING; XIAO DONG; ASLANIAN ROBERT; CHEEWATRAKOOLPONG BOONLERT; ZHANG HONGTAO; GREENFEDER SCOTT; FARLEY CONSTANCE; COOK JOHN; KUROWSKI STAN; LI QIU; VAN HEEK MARGARET; CHINTALA MADHU; WANG GANFENG; HSIEH YUNSHENG; LI FANGBIAO; PALANI ANANDAN,期刊：ACS Medicinal Chemistry Letters, 页码：171-176 , 文章类型： Article，,卷期：2011年2-2]
- Nicotinic acid has been used clinically for decades to control serum lipoproteins. Nicotinic acid lowers very low-density lipoprotein (VLDL)-cholesterol low-density liproprote in (LDL)-cholesterol, and lipoprotein-a (LPa...
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