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在“Elsevier电子期刊”中，命中：407条，耗时：0.0709646 秒

在所有数据库中总计命中：1,130条

1.Structure-activity relationships of 4-hydroxy-4-biaryl-proline acylsulfonamide tripeptides: A series of potent NS3 protease inhibitors for the treatment of hepatitis C virus

作者：Alan Xiangdong Wang^a ; ^{alan.wang@bms.com} ; Jie Chen^a ; Qian Zhao^a ; Li-Qiang Sun^a ; Jacques Friborg^b ; Fei Yu^b ; Dennis Hernandez^b ; Andrew C. Good^c ; Herbert E. Klei^c ; Ramkumar Rajamani^c ; Kathy Mosure^d ; Jay O. Knipe^d ; Danshi Li^d ; Jialong Zhu^d ; Paul C. Levesque^d ; Fiona McPhee^b ; Nicholas A. Meanwell^a ; Paul M. Scola^a ;

关键词：HCV NS3/4A serine protease inhibitors ; Tripeptide acylsulfonamides ; C4 aryl ; C4 hydroxy-proline ; Potent and orally bioavailable ; Cardiovascular profiles

刊名：Bioorganic & Medicinal Chemistry Letters

出版年：2017

2.The drug candidate, ADX71441, is a novel, potent and selective positive allosteric modulator of the GABA_B receptor with a potential for treatment of anxiety, pain and spasticity

作者：Mikhail Kalinichev ; ^{mikhail.kalinichev@ipsen.com} ; Franç ; oise Girard ; Hasnaà ; Haddouk ; Mé ; lanie Rouillier ; Eric Riguet ; Isabelle Royer-Urios ; Vincent Mutel ; Robert Lü ; tjens ; Sonia Poli

关键词：Allosteric modulator ; GABA ; Anxiety ; Pain ; Body temperature ; Baclofen ; Spasticity ; Clinical candidate

刊名：Neuropharmacology

出版年：2017

3.Discovery of 7-(3-(piperazin-1-yl)phenyl)pyrrolo[2,1-f][1,2,4]triazin-4-amine derivatives as highly potent and selective PI3Kδ inhibitors

作者：Lan-Ying Qin ; ^{lan-ying.qin@bms.com} ; Zheming Ruan ; Robert J. Cherney ; T.G. Murali Dhar ; James Neels ; Carolyn A. Weigelt ; John S. Sack ; Anurag S. Srivastava ; Lyndon A.M. Cornelius ; Joseph A. Tino ; Kevin Stefanski ; Xiaomei Gu ; Jenny Xie ; Vojkan Susulic ; Xiaoxia Yang ; Melissa Yarde-Chinn ; Stacey Skala ; Ruth Bosnius ; Christine Goldstein ; Paul Davies ; Stefan Ruepp ; Luisa Salter-Cid ; Rajeev S. Bhide ; Michael A. Poss

关键词：PI3Kδ ; 7-Phenylpyrrolo[2 ; 1-f][12 ; 4]triazin-4-amine ; Autoimmune diseases ; Rheumatoid arthritis ; Phosphoinositide 3-kinases

刊名：Bioorganic & Medicinal Chemistry Letters

出版年：2017

4.Optimisation of a novel series of potent and orally bioavailable azanaphthyridine SYK inhibitors

作者：Neil S. Garton^a ; ^{Neil.S.Garton@gsk.com" class="auth_mail" title="E-mail the corresponding author} ; Michael D. Barker^a ; Rob P. Davis^a ; Clement Douault^a ; Edward Hooper-Greenhill^a ; Emma Jones^a ; Huw D. Lewis^a ; John Liddle^a ; Dave Lugo^a ; Scott McCleary^a ; Alex G.S. Preston^a ; Cesar Ramirez-Molina^a ; Margarete Neu^a ; Tracy J. Shipley^a ; Don O. Somers^a ; Robert J. Watson^a ; David M. Wilson^b

关键词：SYK ; Spleen Tyrosine Kinase ; Selective ; Potent ; Orally bioavailable ; Azanaphthyridine ; Lead optimisation ; Medicinal chemistry

刊名：Bioorganic & Medicinal Chemistry Letters

出版年：2016

5.Potent, selective and orally bioavailable leucine-rich repeat kinase 2 (LRRK2) inhibitors

作者：Thomas J. Greshock^a ; ^{thomas_greshock@merck.com" class="auth_mail" title="E-mail the corresponding author} ; John M. Sanders^b ; ^{john_sanders@merck.com" class="auth_mail" title="E-mail the corresponding author} ; Robert E. Drolet^c ; Hemaka A. Rajapakse^a ; Ronald K. Chang^a ; Boyoung Kim^a ; Vanessa L. Rada^a ; Heather E. Tiscia^a ; Hua Su^d ; Ming-Tain Lai^e ; Sylvie M. Sur^e ; Rosa I. Sanchez^f ; Mark T. Bilodeau^a ; John J. Renger^c ; Jonathan T. Kern^c ; John A. McCauley^a

关键词：LRRK2 ; Parkinson&rsquo ; s disease ; Leucine rich repeat kinase ; CNS ; Kinase

刊名：Bioorganic & Medicinal Chemistry Letters

出版年：2016

6.Discovery of novel pyrrole-based scaffold as potent and orally bioavailable free fatty acid receptor 1 agonists for the treatment of type 2 diabetes

作者：Zheng Li^a ; Miaobo Pan^a ; Xin Su^a ; Yuxuan Dai^a ; Mian Fu^a ; Xingguang Cai^a ; Wei Shi^a ; Wenlong Huang^a ; ^b ; ^{ydhuangwenlong@126.com" class="auth_mail" title="E-mail the corresponding author} ; Hai Qian^a ; ^b ; ^{qianhai24@163.com" class="auth_mail" title="E-mail the corresponding author}

关键词：FFA1 agonist ; GPR40 ; Ligand efficiency ; Type 2 diabetes ; Pyrrole

刊名：Bioorganic & Medicinal Chemistry

出版年：2016

7.Lead optimization of a pyrazolo[1,5-a]pyrimidin-7(4H)-one scaffold to identify potent, selective and orally bioavailable KDM5 inhibitors suitable for in vivo biological studies

作者：Jun Liang^a ; ^{liang.jun@gene.com" class="auth_mail" title="E-mail the corresponding author} ; Birong Zhang^a ; Sharada Labadie^a ; Daniel F. Ortwine^a ; Maia Vinogradova^a ; James R. Kiefer^a ; Victor S. Gehling^b ; Jean-Christophe Harmange^b ; Richard Cummings^b ; Tommy Lai^c ; Jiangpeng Liao^c ; Xiaoping Zheng^c ; Yichin Liu^a ; Amy Gustafson^a ; Erica Van der Porten^a ; Weifeng Mao^c ; Bianca M. Liederer^a ; Gauri Deshmukh^a ; Marie Classon^a ; Patrick Trojer^b ; Peter S. Dragovich^a ; Lesley Murray^a

关键词：Histone demethylase ; KDM5 ; Selective KDM5 inhibitors ; Epigenetics ; Drug resistance ; Lead optimization

刊名：Bioorganic & Medicinal Chemistry Letters

出版年：2016

8.Discovery of potent and orally bioavailable inhibitors of Human Uric Acid Transporter 1 (hURAT1) and binding mode prediction using homology model

作者：Jianbiao Peng ; ^{pengjb@shhrp.com" class="auth_mail" title="E-mail the corresponding author} ; Qiyue Hu ; Chunyan Gu ; Bonian Liu ; Fangfang Jin ; Jijun Yuan ; Jun Feng ; Lei Zhang ; Jiong Lan ; Qing Dong ; Guoqing Cao

关键词：Gout ; Hyperuricemia ; URAT1 inhibitors ; URAT1 homology model ; 3D pharmacophore

刊名：Bioorganic & Medicinal Chemistry Letters

出版年：2016

9.Discovery of novel 2′,4′-dimethyl-[4,5′-bithiazol]-2-yl amino derivatives as orally bioavailable TRPV4 antagonists for the treatment of pain: Part 1

作者：Naoki Tsuno^a ; ^{naoki.tsuno@shionogi.co.jp" class="auth_mail" title="E-mail the corresponding author} ; Akira Yukimasa^a ; Osamu Yoshida^a ; Yusuke Ichihashi^a ; Takatsugu Inoue^a ; Tatsuhiko Ueno^a ; Hiroki Yamaguchi^a ; Hidetoshi Matsuda^b ; Satoko Funaki^c ; Natsue Yamanada^a ; Miki Tanimura^a ; Daiki Nagamatsu^c ; Yoko Nishimura^c ; Tetsuji Ito^c ; Masahiko Soga^a ; Narumi Horita^b ; Miyuki Yamamoto^a ; Mikie Hinata^a ; Masayuki Imai^d ; Yasuhide Morioka^a ; Toshiyuki Kanemasa^a ; Gaku Sakaguchi^d ; Yasuyoshi Iso^a

关键词：Transient Receptor Potential Vanilloid 4 ; TRPV4 antagonist ; Ion channel ; Vanilloid receptor ; Thiazole ; Bi-cyclic ; Pain

刊名：Bioorganic & Medicinal Chemistry Letters

出版年：2016

10.Metabolism-based structure optimization: Discovery of a potent and orally available tyrosine kinase ALK inhibitor bearing the tetracyclic benzo[b]carbazolone core

作者：Mei Han^a ; ^&dagger ; ; Chengyan Wang^d ; ^&dagger ; ; Yinchun Ji^b ; Zilan Song^c ; Li Xing^c ; Yi Su^b ; Xisheng Wang^d ; Ao Zhang^c ; ^e ; ^{aozhang@simm.ac.cn" class="auth_mail" title="E-mail the corresponding author} ; Jing Ai^b ; ^e ; ^{jai@simm.ac.cn" class="auth_mail" title="E-mail the corresponding author} ; Meiyu Geng^b ; ^e ; ^{mygeng@simm.ac.cn" class="auth_mail" title="E-mail the corresponding author}

关键词：EML4-ALK kinase ; Oxidative metabolism ; Benzo[b]carbazolone ; hERG ; Antitumor activity

刊名：Bioorganic & Medicinal Chemistry Letters

出版年：2016

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