Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK
Galkin, Anna V, Melnick, Jonathan S, Kim, Sungjoon, Hood, Tami L, Li, Nanxin, Li, Lintong, Xia, Gang, Steensma, Ruo, Chopiuk, Greg, Jiang, Jiqing, Wan, Yongqin, Ding, Peter, Liu, Yi, Sun, Fangxian, Schultz, Peter G, Gray, Nathanael S, Warmuth, Markus
Published in Proceedings of the National Academy of Sciences - PNAS (02.01.2007)
Published in Proceedings of the National Academy of Sciences - PNAS (02.01.2007)
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Piperazine-Based CCR5 Antagonists as HIV-1 Inhibitors. IV. Discovery of 1-[(4,6-Dimethyl-5-pyrimidinyl)carbonyl]- 4-[4-{2-methoxy-1(R)-4-(trifluoromethyl)phenyl}ethyl-3(S)-methyl-1-piperazinyl]- 4-methylpiperidine (Sch-417690/Sch-D), a Potent, Highly Selective, and Orally Bioavailable CCR5 Antagonist
Tagat, Jayaram R, McCombie, Stuart W, Nazareno, Dennis, Labroli, Marc A, Xiao, Yushi, Steensma, Ruo W, Strizki, Julie M, Baroudy, Bahige M, Cox, Kathleen, Lachowicz, Jean, Varty, Geoffrey, Watkins, Robert
Published in Journal of medicinal chemistry (06.05.2004)
Published in Journal of medicinal chemistry (06.05.2004)
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Piperazine-Based CCR5 Antagonists as HIV-1 Inhibitors. II. Discovery of 1-[(2,4-Dimethyl-3-pyridinyl)carbonyl]-4- methyl-4-[3(S)-methyl-4-[1(S)-[4-(trifluoro- methyl)phenyl]ethyl]-1-piperazinyl]- piperidine N1-Oxide (Sch-350634), an Orally Bioavailable, Potent CCR5 Antagonist
Tagat, Jayaram R, Steensma, Ruo W, McCombie, Stuart W, Nazareno, Dennis V, Lin, Sue-Ing, Neustadt, Bernard R, Cox, Kathleen, Xu, Serena, Wojcik, Lisa, Murray, Michael G, Vantuno, Nicole, Baroudy, Bahige M, Strizki, Julie M
Published in Journal of medicinal chemistry (11.10.2001)
Published in Journal of medicinal chemistry (11.10.2001)
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Piperazine-Based CCR5 antagonists as HIV-1 inhibitors. I: 2( S)-methyl piperazine as a key pharmacophore element
Tagat, Jayaram R., McCombie, Stuart W., Steensma, Ruo W., Lin, Sue-Ing, Nazareno, Dennis V., Baroudy, Bahige, Vantuno, Nicole, Xu, Serena, Liu, Jia
Published in Bioorganic & medicinal chemistry letters (20.08.2001)
Published in Bioorganic & medicinal chemistry letters (20.08.2001)
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Synthesis, Structure–Activity Relationships, and in Vivo Efficacy of the Novel Potent and Selective Anaplastic Lymphoma Kinase (ALK) Inhibitor 5-Chloro- N 2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)- N 4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine (LDK378) Currently in Phase 1 and Phase 2 Clinical Trials
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Published in Journal of medicinal chemistry (25.07.2013)
Published in Journal of medicinal chemistry (25.07.2013)
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Discovery and SAR of JTE-151: A Novel RORγ Inhibitor for Clinical Development
Maeba, Takaki, Hirata, Kazuyuki, Kotoku, Masayuki, Seki, Noriyoshi, Maeda, Katsuya, Hirashima, Shintaro, Yamanaka, Hiroshi, Sakai, Takayuki, Obika, Shingo, Hori, Akimi, Hara, Yoshinori, Noji, Satoru, Suwa, Yoshihiro, Yokota, Masahiro, Fujioka, Shingo, Yamaguchi, Takayuki, Katsuda, Yoshiaki, Hata, Takahiro, Miyagawa, Naoki, Arita, Kojo, Nomura, Yukihiro, Taniguchi, Toshio, Asahina, Kota, Aratsu, Yusuke, Naka, Yuichi, Adachi, Tsuyoshi, Nomura, Akihiro, Akai, Shota, Oshida, Shin-ichi, Pai, Sudhakar, Crowe, Paul, Bradley, Erin, Steensma, Ruo, Tao, Haiyan, Fenn, Morgan, Babine, Robert, Li, Xiaolin, Thacher, Scott, Soeta, Takahiro, Ukaji, Yutaka, Shiozaki, Makoto
Published in Journal of medicinal chemistry (25.01.2024)
Published in Journal of medicinal chemistry (25.01.2024)
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Fragment-based discovery of JAK-2 inhibitors
Antonysamy, Stephen, Hirst, Gavin, Park, Frances, Sprengeler, Paul, Stappenbeck, Frank, Steensma, Ruo, Wilson, Mark, Wong, Melissa
Published in Bioorganic & medicinal chemistry letters (01.01.2009)
Published in Bioorganic & medicinal chemistry letters (01.01.2009)
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SAR Exploration Guided by LE and Fsp(3): Discovery of a Selective and Orally Efficacious ROR gamma Inhibitor
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Published in ACS medicinal chemistry letters (14.01.2016)
Published in ACS medicinal chemistry letters (14.01.2016)
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Ternary complex of human ROR[gamma] ligand-binding domain, inverse agonist and SMRT peptide shows a unique mechanism of corepressor recruitment
Noguchi, Masato, Nomura, Akihiro, Murase, Ken, Doi, Satoki, Yamaguchi, Keishi, Hirata, Kazuyuki, Shiozaki, Makoto, Hirashima, Shintaro, Kotoku, Masayuki, Yamaguchi, Takayuki, Katsuda, Yoshiaki, Steensma, Ruo, Li, Xioalin, Tao, Haiyan, Tse, Bruno, Fenn, Morgan, Babine, Robert, Bradley, Erin, Crowe, Paul, Thacher, Scott, Adachi, Tsuyoshi, Kamada, Masafumi
Published in Genes to cells : devoted to molecular & cellular mechanisms (01.06.2017)
Published in Genes to cells : devoted to molecular & cellular mechanisms (01.06.2017)
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Ternary complex of human RORγ ligand‐binding domain, inverse agonist and SMRT peptide shows a unique mechanism of corepressor recruitment
Noguchi, Masato, Nomura, Akihiro, Murase, Ken, Doi, Satoki, Yamaguchi, Keishi, Hirata, Kazuyuki, Shiozaki, Makoto, Hirashima, Shintaro, Kotoku, Masayuki, Yamaguchi, Takayuki, Katsuda, Yoshiaki, Steensma, Ruo, Li, Xioalin, Tao, Haiyan, Tse, Bruno, Fenn, Morgan, Babine, Robert, Bradley, Erin, Crowe, Paul, Thacher, Scott, Adachi, Tsuyoshi, Kamada, Masafumi
Published in Genes to cells : devoted to molecular & cellular mechanisms (01.06.2017)
Published in Genes to cells : devoted to molecular & cellular mechanisms (01.06.2017)
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Inhibition of the development of collagen‐induced arthritis in rhesus monkeys by a small molecular weight antagonist of CCR5
Vierboom, Michel P. M., Zavodny, Paul J., Chou, Chuan‐Chu, Tagat, Jayaram R., Pugliese‐Sivo, Catherine, Strizki, Julie, Steensma, Ruo W., McCombie, Stuart W., Çelebi‐Paul, Liesbeth, Remarque, Ed, Jonker, Margreet, Narula, Satwant K., Hart, Bert't
Published in Arthritis and rheumatism (01.02.2005)
Published in Arthritis and rheumatism (01.02.2005)
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SAR Exploration Guided by LE and Fsp3: Discovery of a Selective and Orally Efficacious RORγ Inhibitor
Hirata, Kazuyuki, Kotoku, Masayuki, Seki, Noriyoshi, Maeba, Takaki, Maeda, Katsuya, Hirashima, Shintaro, Sakai, Takayuki, Obika, Shingo, Hori, Akimi, Hase, Yasunori, Yamaguchi, Takayuki, Katsuda, Yoshiaki, Hata, Takahiro, Miyagawa, Naoki, Arita, Kojo, Nomura, Yukihiro, Asahina, Kota, Aratsu, Yusuke, Kamada, Masafumi, Adachi, Tsuyoshi, Noguchi, Masato, Doi, Satoki, Crowe, Paul, Bradley, Erin, Steensma, Ruo, Tao, Haiyan, Fenn, Morgan, Babine, Robert, Li, Xiaolin, Thacher, Scott, Hashimoto, Hiromasa, Shiozaki, Makoto
Published in ACS medicinal chemistry letters (14.01.2016)
Published in ACS medicinal chemistry letters (14.01.2016)
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Journal Article
SAR Exploration Guided by LE and Fsp 3 : Discovery of a Selective and Orally Efficacious RORγ Inhibitor
Hirata, Kazuyuki, Kotoku, Masayuki, Seki, Noriyoshi, Maeba, Takaki, Maeda, Katsuya, Hirashima, Shintaro, Sakai, Takayuki, Obika, Shingo, Hori, Akimi, Hase, Yasunori, Yamaguchi, Takayuki, Katsuda, Yoshiaki, Hata, Takahiro, Miyagawa, Naoki, Arita, Kojo, Nomura, Yukihiro, Asahina, Kota, Aratsu, Yusuke, Kamada, Masafumi, Adachi, Tsuyoshi, Noguchi, Masato, Doi, Satoki, Crowe, Paul, Bradley, Erin, Steensma, Ruo, Tao, Haiyan, Fenn, Morgan, Babine, Robert, Li, Xiaolin, Thacher, Scott, Hashimoto, Hiromasa, Shiozaki, Makoto
Published in ACS medicinal chemistry letters (14.01.2016)
Published in ACS medicinal chemistry letters (14.01.2016)
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Piperazine-based CCR5 antagonists as HIV-1 inhibitors. III: synthesis, antiviral and pharmacokinetic profiles of symmetrical heteroaryl carboxamides
McCombie, Stuart W., Tagat, Jayaram R., Vice, Susan F., Lin, Sue-Ing, Steensma, Ruo, Palani, Anandan, Neustadt, Bernard R., Baroudy, Bahige M., Strizki, Julie M., Endres, Michael, Cox, Kathleen, Dan, Niya, Chou, Chuan-Chu
Published in Bioorganic & medicinal chemistry letters (10.02.2003)
Published in Bioorganic & medicinal chemistry letters (10.02.2003)
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SUBSTITUTED PYRROLOPYRIDINES AND PYRAZOLOPYRIDINES AS KINASE MODULATORS
HOPKINS STEPHANIE A, STEENSMA RUO W, HIRST GAVIN, GOSBERG ANDREAS, GRADL STEFAN N, SPRENGELER PAUL A, BLANEY JEFFREY M, UY JOHNNY N
Year of Publication 22.04.2010
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Year of Publication 22.04.2010
Patent
Piperazine-based CCR5 antagonists as HIV-1 inhibitors. IV. Discovery of 1-[(4,6-dimethyl-5-pyrimidinyl)carbonyl]- 4-[4-[2-methoxy-1(R)-4-(trifluoromethyl)phenyl]ethyl-3(S)-methyl-1-piperazinyl]- 4-methylpiperidine (Sch-417690/Sch-D), a potent, highly selective, and orally bioavailable CCR5 antagonist
Tagat, Jayaram R, McCombie, Stuart W, Nazareno, Dennis, Labroli, Marc A, Xiao, Yushi, Steensma, Ruo W, Strizki, Julie M, Baroudy, Bahige M, Cox, Kathleen, Lachowicz, Jean, Varty, Geoffrey, Watkins, Robert
Published in Journal of medicinal chemistry (06.05.2004)
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Published in Journal of medicinal chemistry (06.05.2004)
Journal Article
Piperazine-Based CCR5 Antagonists as HIV-1 Inhibitors. II. Discovery of 1-[(2,4-Dimethyl-3-pyridinyl)carbonyl]-4- methyl-4-[3( S )-methyl-4-[1( S )-[4-(trifluoro- methyl)phenyl]ethyl]-1-piperazinyl]- piperidine N 1-Oxide (Sch-350634), an Orally Bioavailable, Potent CCR5 Antagonist
Tagat, Jayaram R., Steensma, Ruo W., McCombie, Stuart W., Nazareno, Dennis V., Lin, Sue-Ing, Neustadt, Bernard R., Cox, Kathleen, Xu, Serena, Wojcik, Lisa, Murray, Michael G., Vantuno, Nicole, Baroudy, Bahige M., Strizki, Julie M.
Published in Journal of medicinal chemistry (01.10.2001)
Published in Journal of medicinal chemistry (01.10.2001)
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LRRK2 INHIBITORS
STEENSMA RUO W, LOWE, III JOHN A, BOUNAUD PIERRE-YVES, NIENABER VICKI
Year of Publication 24.07.2014
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Year of Publication 24.07.2014
Patent