- C-H Amination of Arenes with Hydroxylamine
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This Letter describes the development of a TiIII-mediated reaction for the C-H amination of arenes with hydroxylamine. This reaction is applied to a variety of electron-rich (hetero)arene substrates, including a series of natural products and pharmaceuticals. It offers the advantages of mild conditions (room temperature), fast reaction rates (30 min), compatibility with ambient moisture and air, scalability, and the use of inexpensive commercial reagents.
- See, Yi Yang,Sanford, Melanie S.
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supporting information
p. 2931 - 2934
(2020/04/09)
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- PYRIMIDINE FGFR4 INHIBITORS
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Provided herein are compounds of Formula I useful as FGFR4 inhibitors, as well as methods of use of the same.
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- COMPOSITIONS FOR THE TREATMENT OF HYPERTENSION AND/OR FIBROSIS
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The present invention relates to novel compounds and their use in the prophylactic and/or therapeutic treatment of hypertension and/or fibrosis.
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Page/Page column 57
(2015/04/15)
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- HETEROARYL COMPOUNDS AND USES THEREOF
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The present invention relates to compounds useful as inhibitors of protein kinases, containing a cysteine residue in the ATP binding site. The invention further provides for pharmaceutically acceptable compositions comprising therapeutically effective amounts of one or more of the protein kinase inhibitor compounds and methods of using said compositions in the treatment of cancers and carcinomas.
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- Discovery of 3-(2,6-Dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl- piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea (NVP-BGJ398), A potent and selective inhibitor of the fibroblast growth factor receptor family of receptor tyrosine kinase
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A novel series of N-aryl-N′-pyrimidin-4-yl ureas has been optimized to afford potent and selective inhibitors of the fibroblast growth factor receptor tyrosine kinases 1, 2, and 3 by rationally designing the substitution pattern of the aryl ring. On the b
- Guagnano, Vito,Furet, Pascal,Spanka, Carsten,Bordas, Vincent,Le Douget, Micka?l,Stamm, Christelle,Brueggen, Josef,Jensen, Michael R.,Schnell, Christian,Schmid, Herbert,Wartmann, Markus,Berghausen, Joerg,Drueckes, Peter,Zimmerlin, Alfred,Bussiere, Dirksen,Murray, Jeremy,Graus Porta, Diana
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p. 7066 - 7083
(2011/12/04)
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- PYRAZOLYL QUINAZOLINE KINASE INHIBITORS
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The invention relates to new quinoxaline derivative compounds, to pharmaceutical compositions comprising said compounds, to processes for the preparation of said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.
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- 2-Phenylquinazolin-4(3H)-one, a class of potent PDE5 inhibitors with high selectivity versus PDE6
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In our efforts to minimize the side effects associated with low selectivity against the other PDE isozymes, a novel class of 2-phenylquinazolin-4(3H)-one derivatives were designed and prepared as potent PDE5 inhibitors with high selectivity against PDE6.
- Duan, Hongliang,Zheng, Jin,Lai, Qinglin,Liu, Zheng,Tian, Guanghui,Wang, Zhen,Li, Jianfeng,Shen, Jingshan
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supporting information; experimental part
p. 2777 - 2779
(2009/12/31)
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- Bicyclic pyrimidines and bicyclic 3,4-dihydropyrimidines as inhibitors of cellular proliferation
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This invention provides bicyclic heterocycles that are useful for treating cell proliferative disorders, such as cancer and restenosis, as well as angiogenesis and atherosclerosis. We have now discovered a group of bicyclic compounds that are potent inhibitors of cyclin-dependent kinases (cdks), growth factor-mediated kinases, and non-receptor kinases. The compounds are readily synthesized and can be administered by a variety of routes, including orally, and have sufficient bioavailability for clinical use. This invention provides compounds of Formula I: where Z is N or CH; G is N or CH; W is NH, S, SO, or SO2, R1 includes phenyl and substituted phenyl, R2 includes alkyl and cycloalkyl, R3 includes alkyl and hydrogen, R8 and R9 include hydrogen and alkyl, and the pharmaceutically acceptable salts thereof. This invention also provides pharmaceutical formulations comprising a compound of Formula I together with a pharmaceutically acceptable carrier, diluent, or excipient therefor.
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- 2'-Halo-3',5'-dialkoxyphen-1'-yl-imino-2-imidazolidine and the use thereof as a drug
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The present invention relates to 2′-halo-3′,5′-dialkoxyphen-1′-yl-imino-2-imidazolidine, the tautomeric 2′-halo-3′,5′-dialkoxyanilino-2-imidazoline and/or the pharmacologically acceptable salts thereof and their use as pharmaceutical compositions.
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- 2'-Halo-3',5'-dialkoxyphen-1'-yl-imino-2-imidazolidine derivatives and the use thereof for the treatment of urinary incontinence
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The present invention relates to 2'-halo-3',5'-dialkoxyphen-1'-yl-imino-2-imidazolidine, the tautomeric 2'-halo-3',5'-dialkoxyanilino-2-imidazoline and/or the pharmacologically acceptable salts thereof and their use as pharmaceutical compositions, in the
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