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1. Full Text Discovery of Potent and Selective RSK Inhibitors as Biological Probes
by Jain, Rama and Mathur, Michelle and Lan, Jiong and Costales, Abran and Atallah, Gordana and Ramurthy, Savithri and Subramanian, Sharadha and Setti, Lina and Feucht, Paul and Warne, Bob and Doyle, Laura and Basham, Stephen and Jefferson, Anne B and Lindvall, Mika and Appleton, Brent A and Shafer, Cynthia M
Journal of Medicinal Chemistry, ISSN 0022-2623, 09/2015, Volume 58, Issue 17, pp. 6766 - 6783
While the p90 ribosomal S6 kinase (RSK) family has been implicated in multiple tumor cell functions, the full understanding of this kinase family has been... 
CELLS | DESIGN | CHEMISTRY, MEDICINAL | PHOSPHORYLATION | PATHWAY | RIBOSOMAL S6 KINASE | BI-D1870 | FAMILY | Cell Line | Phosphorylation | Signal Transduction | Pyrazoles - chemical synthesis | Pyridines - chemistry | Pyrimidines - chemical synthesis | Humans | Pyridines - chemical synthesis | Models, Molecular | Crystallography, X-Ray | Male | Structure-Activity Relationship | Pyrimidines - pharmacology | Rats, Sprague-Dawley | Pyrimidines - chemistry | Pyrazoles - chemistry | Animals | Y-Box-Binding Protein 1 - metabolism | Ribosomal Protein S6 Kinases, 90-kDa - antagonists & inhibitors | Protein Conformation | Mice | Pyridines - pharmacology | Pyrazoles - pharmacology
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2. Full Text Design and synthesis of potent RSK inhibitors
by Jain, Rama and Mathur, Michelle and Lan, Jiong and Costales, Abran and Atallah, Gordana and Ramurthy, Savithri and Subramanian, Sharadha and Setti, Lina and Feucht, Paul and Warne, Bob and Doyle, Laura and Basham, Stephen and Jefferson, Anne B and Appleton, Brent A and Lindvall, Mika and Shafer, Cynthia M
Bioorganic & Medicinal Chemistry Letters, ISSN 0960-894X, 10/2018, Volume 28, Issue 19, pp. 3197 - 3201
Utilizing the already described 3,4-bi-aryl pyridine series as a starting point, incorporation of a second ring system with a hydrogen bond donor and... 
Oncology | Azaindole | p90 ribosomal S6 kinase | CHEMISTRY, MEDICINAL | ISOFORMS | KINASE | CHEMISTRY, ORGANIC | CANCER | DISCOVERY | Protein Kinase Inhibitors - chemical synthesis | Protein Kinase Inhibitors - chemistry | Animals | Proton Magnetic Resonance Spectroscopy | Humans | Mass Spectrometry | Drug Design | Chromatography, Liquid | Protein Kinase Inhibitors - pharmacology | Structure-Activity Relationship | Phenols - pharmacology | Hydrogen | Analysis | Pyridine
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3. Full Text 2-Amino-7-substituted benzoxazole analogs as potent RSK2 inhibitors
by Costales, Abran and Mathur, Michelle and Ramurthy, Savithri and Lan, Jiong and Subramanian, Sharadha and Jain, Rama and Atallah, Gordana and Setti, Lina and Lindvall, Mika and Appleton, Brent A and Ornelas, Elizabeth and Feucht, Paul and Warne, Bob and Doyle, Laura and Basham, Stephen E and Aronchik, Ida and Jefferson, Anne B and Shafer, Cynthia M
Bioorganic & Medicinal Chemistry Letters, ISSN 0960-894X, 03/2014, Volume 24, Issue 6, pp. 1592 - 1596
2-Amino-7-substituted benzoxazole analogs were identified by HTS as inhibitors of RSK2. Molecular modeling and medicinal chemistry techniques were employed to... 
RSK | Heterocycle | Kinase | HTS | Benzoxazole | Protein Structure, Tertiary | Protein Kinase Inhibitors - chemical synthesis | Humans | Benzoxazoles - metabolism | Crystallography, X-Ray | Structure-Activity Relationship | Molecular Dynamics Simulation | Benzoxazoles - chemical synthesis | Protein Kinase Inhibitors - chemistry | Ribosomal Protein S6 Kinases, 90-kDa - metabolism | Benzoxazoles - chemistry | Ribosomal Protein S6 Kinases, 90-kDa - antagonists & inhibitors | Protein Binding | Binding Sites
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4. Full Text Discovery and Evaluation of Clinical Candidate IDH305, a Brain Penetrant Mutant IDH1 Inhibitor
by Cho, Young Shin and Levell, Julian R and Liu, Gang and Caferro, Thomas and Sutton, James and Shafer, Cynthia M and Costales, Abran and Manning, James R and Zhao, Qian and Sendzik, Martin and Shultz, Michael and Chenail, Gregg and Dooley, Julia and Villalba, Brian and Farsidjani, Ali and Chen, Jinyun and Kulathila, Raviraj and Xie, Xiaoling and Dodd, Stephanie and Gould, Ty and Liang, Guiqing and Heimbach, Tycho and Slocum, Kelly and Firestone, Brant and Pu, Minying and Pagliarini, Raymond and Growney, Joseph D
ACS Medicinal Chemistry Letters, ISSN 1948-5875, 10/2017, Volume 8, Issue 10, pp. 1116 - 1121
Inhibition of mutant IDH1 is being evaluated clinically as a promising treatment option for various cancers with hotspot mutation at Arg132. Having identified... 
Mutant IDH1 | clinical candidate | inhibition of 2-HG production | in vivo anticancer activity | brain penetration | ISOCITRATE DEHYDROGENASE 1 | SELECTIVE-INHIBITION | CHEMISTRY, MEDICINAL | SMALL-MOLECULE | ACUTE MYELOID-LEUKEMIA | OPPORTUNITIES | HYPOXIA | Mutant IDHI | METABOLISM | MUTATIONS
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5. Full Text Design and Synthesis of Orally Bioavailable Benzimidazoles as Raf Kinase Inhibitors
by Ramurthy, Savithri and Subramanian, Sharadha and Aikawa, Mina and Amiri, Payman and Costales, Abran and Dove, Jeff and Fong, Susan and Jansen, Johanna M and Levine, Barry and Ma, Sylvia and McBride, Christopher M and Michaelian, Jonah and Pick, Teresa and Poon, Daniel J and Girish, Sandhya and Shafer, Cynthia M and Stuart, Darrin and Sung, Leonard and Renhowe, Paul A
Journal of Medicinal Chemistry, ISSN 0022-2623, 11/2008, Volume 51, Issue 22, pp. 7049 - 7052
A series of arylaminobenzimidazoles was designed and synthesized as Raf kinase inhibitors. Exploration of the structure−activity relationship resulted in... 
ACTIVATION | CHEMISTRY, MEDICINAL | BAY-43-9006 | MELANOMA | SIGNALING PATHWAY | BRAF MUTATIONS | B-RAF | CANCER | DISCOVERY | UREAS | Stereoisomerism | raf Kinases - antagonists & inhibitors | Humans | Biological Availability | Crystallography, X-Ray | Structure-Activity Relationship | Benzimidazoles - chemistry | raf Kinases - metabolism | Dose-Response Relationship, Drug | Protein Kinase Inhibitors - chemistry | Benzimidazoles - administration & dosage | Drug Design | Female | Molecular Structure | Protein Structure, Tertiary | Protein Kinase Inhibitors - chemical synthesis | Administration, Oral | Benzimidazoles - chemical synthesis | Models, Molecular | Xenograft Model Antitumor Assays | Protein Kinase Inhibitors - administration & dosage | Animals | Cell Line, Tumor | Benzimidazoles - pharmacology | Cell Proliferation - drug effects | Mice | Protein Kinase Inhibitors - pharmacology
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6. Full Text Design and synthesis of 6,6-fused heterocyclic amides as raf kinase inhibitors
by Ramurthy, Savithri and Costales, Abran and Jansen, Johanna M and Levine, Barry and Renhowe, Paul A and Shafer, Cynthia M and Subramanian, Sharadha
Bioorganic & Medicinal Chemistry Letters, ISSN 0960-894X, 02/2012, Volume 22, Issue 4, pp. 1678 - 1681
Compounds belonging to several scaffolds—quinazolines, quinolines and quinoxalines—were designed and synthesized as Raf kinase inhibitors. Scaffolds were... 
Potency | Selectivity | Raf kinase inhibitors | Quinazolines | Potency; Selectivity | ACTIVATION | CHEMISTRY, MEDICINAL | CHEMISTRY, ORGANIC | CANCER | UREAS | MELANOMA | SIGNALING PATHWAY | BRAF MUTATIONS | B-RAF | Amides - pharmacology | Amides - chemical synthesis | raf Kinases - antagonists & inhibitors | Humans | Cells, Cultured | Enzyme Inhibitors - pharmacology | Heterocyclic Compounds - pharmacology | Models, Molecular | Heterocyclic Compounds - chemical synthesis | Enzyme Activation - drug effects | Enzyme Inhibitors - chemical synthesis | Heterocyclic Compounds - chemistry | Enzyme Inhibitors - chemistry | Drug Design | Amides - chemistry | Molecular Structure | Binding Sites | Tyrosine | Amides | Phosphotransferases | Vascular endothelial growth factor
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7. Full Text Design, Structure–Activity Relationship, and in Vivo Characterization of the Development Candidate NVP-HSP990
by McBride, Christopher M and Levine, Barry and Xia, Yi and Bellamacina, Cornelia and Machajewski, Timothy and Gao, Zhenhai and Renhowe, Paul and Antonios-McCrea, William and Barsanti, Paul and Brinner, Kristin and Costales, Abran and Doughan, Brandon and Lin, Xiaodong and Louie, Alicia and McKenna, Maureen and Mendenhall, Kris and Poon, Daniel and Rico, Alice and Wang, Michael and Williams, Teresa E and Abrams, Tinya and Fong, Susan and Hendrickson, Thomas and Lei, Dachuan and Lin, Julie and Menezes, Daniel and Pryer, Nancy and Taverna, Pietro and Xu, Yongjin and Zhou, Yasheen and Shafer, Cynthia M
Journal of Medicinal Chemistry, ISSN 0022-2623, 11/2014, Volume 57, Issue 21, pp. 9124 - 9129
Utilizing structure-based drug design, a novel dihydropyridopyrimidinone series which exhibited potent Hsp90 inhibition, good pharmacokinetics upon oral... 
HSP90 MOLECULAR CHAPERONE | CHEMISTRY, MEDICINAL | INHIBITORS | Pyridones - pharmacokinetics | Pyrimidines - chemical synthesis | Antineoplastic Agents - chemical synthesis | Structure-Activity Relationship | Pyrimidines - pharmacology | Pyridones - chemical synthesis | Animals | HSP90 Heat-Shock Proteins - antagonists & inhibitors | Pyrimidines - pharmacokinetics | Antineoplastic Agents - pharmacokinetics | Antineoplastic Agents - pharmacology | Mice | Pyridones - pharmacology
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8. Full Text Design and synthesis of 5,6-fused heterocyclic amides as Raf kinase inhibitors
by Ramurthy, Savithri and Aikawa, Mina and Amiri, Payman and Costales, Abran and Hashash, Ahmad and Jansen, Johanna M and Lin, Song and Ma, Sylvia and Renhowe, Paul A and Shafer, Cynthia M and Subramanian, Sharadha and Sung, Leonard and Verhagen, Joelle
Bioorganic & Medicinal Chemistry Letters, ISSN 0960-894X, 2011, Volume 21, Issue 11, pp. 3286 - 3289
Two scaffolds based on 5,6-fused heterocyclic backbones were designed and synthesized as Raf kinase inhibitors. The scaffolds were assessed for in vitro... 
Pharmacokinetic profile | Raf kinase inhibitors | 5,6-Fused heterocycles | Benzoxazoles | Benzothiazoles | ACTIVATION | CHEMISTRY, MEDICINAL | BAY-43-9006 | CHEMISTRY, ORGANIC | CANCER | UREAS | MELANOMA | SIGNALING PATHWAY | BRAF MUTATIONS | B-RAF | BENZIMIDAZOLES | Amides - pharmacology | Cell Proliferation | Amides - chemical synthesis | raf Kinases - antagonists & inhibitors | Enzyme Inhibitors - pharmacology | Heterocyclic Compounds - pharmacology | Models, Molecular | Heterocyclic Compounds - chemical synthesis | Structure-Activity Relationship | Enzyme Activation - drug effects | Enzyme Inhibitors - chemical synthesis | Heterocyclic Compounds - chemistry | Enzyme Inhibitors - chemistry | Drug Design | Amides - chemistry | Molecular Structure | Binding Sites
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9. Full Text Discovery of RAF265: A Potent mut-B-RAF Inhibitor for the Treatment of Metastatic Melanoma
by Williams, Teresa E and Subramanian, Sharadha and Verhagen, Joelle and McBride, Christopher M and Costales, Abran and Sung, Leonard and Antonios-McCrea, William and McKenna, Maureen and Louie, Alicia K and Ramurthy, Savithri and Levine, Barry and Shafer, Cynthia M and Machajewski, Timothy and Renhowe, Paul A and Appleton, Brent A and Amiri, Payman and Chou, James and Stuart, Darrin and Aardalen, Kimberly and Poon, Daniel
ACS Medicinal Chemistry Letters, ISSN 1948-5875, 09/2015, Volume 6, Issue 9, pp. 961 - 965
Abrogation of errant signaling along the MAPK pathway through the inhibition of B-RAF kinase is a validated approach for the treatment of pathway-dependent... 
serine/threonine kinases | vegf | tyrosine kinases | map | b-raf | SELECTIVE INHIBITOR | DESIGN | CHEMISTRY, MEDICINAL | VEGF | KINASE INHIBITORS | B-RAF | MAP | CANCER
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10. Full Text Optimization of 3‑Pyrimidin-4-yl-oxazolidin-2-ones as Orally Bioavailable and Brain Penetrant Mutant IDH1 Inhibitors
by Zhao, Qian and Manning, James R and Sutton, James and Costales, Abran and Sendzik, Martin and Shafer, Cynthia M and Levell, Julian R and Liu, Gang and Caferro, Thomas and Cho, Young Shin and Palermo, Mark and Chenail, Gregg and Dooley, Julia and Villalba, Brian and Farsidjani, Ali and Chen, Jinyun and Dodd, Stephanie and Gould, Ty and Liang, Guiqing and Slocum, Kelly and Pu, Minying and Firestone, Brant and Growney, Joseph and Heimbach, Tycho and Pagliarini, Raymond
ACS Medicinal Chemistry Letters, ISSN 1948-5875, 07/2018, Volume 9, Issue 7, pp. 746 - 751
Mutant isocitrate dehydrogenase 1 (IDH1) is an attractive therapeutic target for the treatment of various cancers such as AML, glioma, and glioblastoma. We... 
Mutant IDH1 | clinical candidate | inhibition of 2-HG production | in vivo anticancer activity | brain penetration | ISOCITRATE DEHYDROGENASE 1 | SELECTIVE-INHIBITION | CHEMISTRY, MEDICINAL | SMALL-MOLECULE | GLIOMA | MECHANISMS | IDENTIFICATION | REVEAL | DISCOVERY | IN-VIVO | MUTATIONS
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11. Full Text Erratum: Design and synthesis of orally bioavailable benzimidazole reverse amides as pan RAF Kinase inhibitors
by Subramanian, Sharadha and Costales, Abran and Williams, Teresa E and Levine, Barry and McBride, Christopher M and Poon, Daniel and Amiri, Payman and Renhowe, Paul A and Shafer, Cynthia M and Stuart, Darrin and Verhagen, Joelle and Ramurthy, Savithri
ACS Medicinal Chemistry Letters, 12/2014, Volume 5, Issue 12, p. 1340
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12. Full Text Correction to Design and Synthesis of Orally Bioavailable Benzimidazole Reverse Amides as Pan RAF Kinase Inhibitors
by Subramanian, Sharadha and Costales, Abran and Williams, Teresa E and Levine, Barry and McBride, Christopher M and Poon, Daniel and Amiri, Payman and Renhowe, Paul A and Shafer, Cynthia M and Stuart, Darrin and Verhagen, Joelle and Ramurthy, Savithri
ACS Medicinal Chemistry Letters, ISSN 1948-5875, 12/2014, Volume 5, Issue 12, pp. 1340 - 1340
[This corrects the article DOI: 10.1021/ml5002272.]. 
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13. Full Text Design and Synthesis of Orally Bioavailable Benzimidazole Reverse Amides as Pan RAF Kinase Inhibitors
by Subramanian, Sharadha and Costales, Abran and Williams, Teresa E and Levine, Barry and McBride, Christopher M and Poon, Daniel and Amiri, Payman and Renhowe, Paul A and Shafer, Cynthia M and Stuart, Darrin and Verhagen, Joelle and Ramurthy, Savithri
ACS Medicinal Chemistry Letters, ISSN 1948-5875, 09/2014, Volume 5, Issue 9, pp. 989 - 992
Benzimidazole reverse amides were designed and synthesized as Pan RAF kinase inhibitors. Investigation of the structure–activity relationship of the compounds... 
CSF1R | receptor tyrosine kinases | colony stimulating factor-1 receptor | VEGF | ras-mitogen activated protein kinase | vascular endothelial growth factor receptor | RTKs | tyrosine kinases | MAP | serine threonine kinases | TKs | STKs | CHEMISTRY, MEDICINAL | CSFIR | BRAF | RTKS | Map | HUMAN CANCER
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14. Full Text Origins of Regioselectivity in the Reactions of α-Lactams with Nucleophiles. Two Distinct Acid-Catalyzed Pathways Involving O- and N-Protonation
by Hoffman, Robert V and Zhao, Zhiqiang and Costales, Abran and Clarke, David
The Journal of Organic Chemistry, ISSN 0022-3263, 07/2002, Volume 67, Issue 15, pp. 5284 - 5294
Sterically stabilized α-lactams react by two distinct acid-catalyzed pathways. Protonation on oxygen results in nucleophilic attack at the acyl carbon and... 
SECONDARY | CHEMISTRY, ORGANIC | AZIRIDINONES | BASE-PROMOTED REACTIONS | SULFONYLATED HYDROXAMIC ACIDS | AMIDES | Oxygen | Chemistry, Organic | Analysis | Physiological aspects | Chemical reactions | Research | Catalysis | Nitrogen | Sialic acids
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15. DISPERSANTS, METHOD OF MAKING, AND USING SAME
by Miller, John Robert and Ruhe, JR., William Raymond and Masson, Georgeta and Chang, Young A and Costales, Abran and Nass, Kirk
11/2018
Disclosed is a dispersant composition, suitable for use in lubricating oils. The dispersant composition is a reaction product of (i) a polyalkenyl succinimide... 
INDEXING SCHEME ASSOCIATED WITH SUBCLASS C10M RELATING TO LUBRICATINGCOMPOSITIONS | TECHNICAL GASES CONTAINING CARBON MONOXIDE | ORGANIC MACROMOLECULAR COMPOUNDS | THEIR PREPARATION OR CHEMICAL WORKING-UP | LUBRICANTS | PEAT | MACROMOLECULAR COMPOUNDS OBTAINED BY REACTIONS ONLY INVOLVINGCARBON-TO-CARBON UNSATURATED BONDS | LUBRICATING COMPOSITIONS | METALLURGY | USE OF CHEMICAL SUBSTANCES EITHER ALONE OR AS LUBRICATINGINGREDIENTS IN A LUBRICATING COMPOSITION | CHEMISTRY | PETROLEUM, GAS OR COKE INDUSTRIES | FUELS | COMPOSITIONS BASED THEREON
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16. SUBSTITUTED BENZAZOLES AND USE THEREOF AS INHIBITORS OF RAF KINASE
by ABRAN COSTALES
06/2006, 7
New substituted benzazole compounds of formula (I), compositions and methods of inhibition of Raf kinase activity in a human or animal subject are provided.... 
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS | HYGIENE | ORGANIC CHEMISTRY | HETEROCYCLIC COMPOUNDS | MEDICAL OR VETERINARY SCIENCE | ARTIFICIAL STONE | TREATMENT OF NATURAL STONE | HUMAN NECESSITIES | CEMENTS | CONCRETE | REFRACTORIES | LIME, MAGNESIA | METALLURGY | PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES | CHEMISTRY | SLAG | COMPOSITIONS THEREOF, e.g. MORTARS, CONCRETE OR LIKE BUILDINGMATERIALS | CERAMICS
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17. "compostos e composições como inibidores de proteína cinase"
by Sabina Pecchi and Zuosheng Liu and Abran Q. Costales and Daniel Poon and John Tellew and Qiong Zhang and Jeff (Xianming) Jin and Shenlin Huang
05/2017
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS | METALLURGY | HYGIENE | PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES | ORGANIC CHEMISTRY | CHEMISTRY | HETEROCYCLIC COMPOUNDS | MEDICAL OR VETERINARY SCIENCE | HUMAN NECESSITIES
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18. 3-pyrimidin-4-yl-oxazolidin-2-ones as inhibitors of mutant IDH
by Levell, Julian Roy and Liu, Gang and Cho, Young Shin and Zhao, Qian and Sutton, James Clifford and Chen, Zhuoliang and Manning, James R and Costales, Abran Q and Sendzik, Martin and Shultz, Michael David and Caferro, Thomas Raymond and Shafer, Cynthia and Wang, Yaping
10/2018
The invention is directed to a formula (I): or a pharmaceutically acceptable salt thereof, wherein R1, R2a, R2b and R3-R7 are herein. The invention is also... 
METALLURGY | HYGIENE | PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES | ORGANIC CHEMISTRY | CHEMISTRY | HETEROCYCLIC COMPOUNDS | MEDICAL OR VETERINARY SCIENCE | HUMAN NECESSITIES
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19. 3-pyrimidin-4-yl-oxazolidin-2-ones comme inhibiteurs d'idh mutante
by SENDZIK, Martin and MANNING, James R and WANG, Yaping and CHO, Young Shin and LEVELL, Julian Roy and CHEN, Zhuoliang and CAFERRO, Thomas Raymond and COSTALES, Abran Q and SUTTON, James and SHAFER, Cynthia and ZHAO, Qian and LIU, Gang and SHULTZ, Michael David
09/2018
L'invention concerne également des compositions contenant un composé de formule (i) et l'utilisation de ces composés dans l'inhibition de protéines idh... 
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS | HYGIENE | METALLURGY | PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES | ORGANIC CHEMISTRY | CHEMISTRY | MEDICAL OR VETERINARY SCIENCE | HETEROCYCLIC COMPOUNDS | HUMAN NECESSITIES
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20. COMPOUNDS AND COMPOSITIONS AS PROTEIN KINASE INHIBITORS
by JIN, JEFF (XIANMING) and TELLEW, JOHN and ZHANG, QIONG and PECCHI, SABINA and LIU, ZUOSHENG and COSTALES, ABRAN Q and POON, DANIEL and HUANG, SHENLIN
07/2016
The present invention provides compounds of Formula I or II (see formula I) (see formula II) wherein R1, R1B, R2, R3, R4, R5, R6 and R7 are defined herein. The... 
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS | METALLURGY | HYGIENE | PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES | ORGANIC CHEMISTRY | CHEMISTRY | HETEROCYCLIC COMPOUNDS | MEDICAL OR VETERINARY SCIENCE | HUMAN NECESSITIES
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