- Decarboxylative Bromination of Heteroarenes: Initial Mechanistic Insights
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After an initial report from our laboratory describing metal-free decarboxylative halogenation of various azaheteroarenes, we set out to investigate the possible mechanism by which this chemistry occurs. Evidence from this mechanistic investigation sugges
- Patel, Pritesh R.,Henderson, Scott H.,Roe, Mark S.,Honey, Mark A.
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supporting information
p. 1603 - 1607
(2020/09/09)
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- INHIBITORS OF CYCLIN DEPENDNT KINASE 7 (CDK7)
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The present invention provides novel compounds of Formula (I) and pharmaceutically acceptable salts, solvates, hydrates, tautomers, stereoisomers, isotopically labeled derivatives, and compositions thereof. Also provided are methods and kits involving the compounds or compositions for treating or preventing proliferative diseases (e.g., cancers (e.g., leukemia, melanoma, multiple myeloma), benign neoplasms, angiogenesis, inflammatory diseases, autoinflammatory diseases, and autoimmune diseases) in a subject. Treatment of a subject with a proliferative disease using a compound or composition of the invention may inhibit the aberrant activity of cyclin-dependent kinase 7 (CDK7), and therefore, induce cellular apoptosis and/or inhibit transcription in the subject.
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Paragraph 506
(2018/02/28)
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- Evaluation and synthesis of polar aryl- and heteroaryl spiroazetidine-piperidine acetamides as ghrelin inverse agonists
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Several polar heteroaromatic acetic acids and their piperidine amides were synthesized and evaluated as ghrelin or type 1a growth hormone secretagogue receptor (GHS-R1a) inverse agonists. Efforts to improve pharmacokinetic and safety profile was achieved
- Orr, Suvi T. M.,Beveridge, Ramsay,Bhattacharya, Samit K.,Cameron, Kimberly O.,Coffey, Steven,Fernando, Dilinie,Hepworth, David,Jackson, Margaret V.,Khot, Vishal,Kosa, Rachel,Lapham, Kimberly,Loria, Paula M.,McClure, Kim F.,Patel, Jigna,Rose, Colin,Saenz, James,Stock, Ingrid A.,Storer, Gregory,Von Volkenburg, Maria,Vrieze, Derek,Wang, Guoqiang,Xiao, Jun,Zhang, Yingxin
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supporting information
p. 156 - 161
(2015/03/04)
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- INHIBITORS OF INFLUENZA VIRUSES REPLICATION
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Methods of inhibiting the replication of influenza viruses in a biological sample or patient, of reducing the amount of influenza viruses in a biological sample or patient, and of treating influenza in a patient, comprises administering to said biological sample or patient an effective amount of a compound represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof, wherein the values of Structural Formula (I) are as described herein. A compound is represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof, wherein the values of Structural Formula (I) are as described herein. A pharmaceutical composition comprises an effective amount of such a compound or pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, adjuvant or vehicle.
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Page/Page column 126-127
(2012/06/30)
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- PYRAZOLE [3, 4-B] PYRIDINE RAF INHIBITORS
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Compounds of Formula I are useful for inhibition of Raf kinases. Methods of using compounds of Formula I and stereoisomers, tautomers, prodrugs and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.
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Page/Page column 81
(2009/10/22)
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- The Semmler-Wolff Aromatization and Schmidt Reaction Applied to Some Pyridopyrazolobenzotriazines
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Pyridopyrazolobenzotriazin-4(1H)ones were transformed via their oximes in a Semmler-Wolff aromatization process in the tetracyclic heteroaromatic amines 4 or by Schmidt reaction into a mixture of the same amine 4 and a ring enlarg
- Kocevar, Marijan,Stanovnik, Branko,Tisler, Miha
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p. 597 - 604
(2007/10/02)
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