- Corresponding amine nitrile and method of manufacturing thereof
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The invention relates to a manufacturing method of nitrile. Compared with the prior art, the manufacturing method has the characteristics of significantly reduced using amount of an ammonia source, low environmental pressure, low energy consumption, low production cost, high purity and yield of a nitrile product and the like, and nitrile with a more complex structure can be obtained. The invention also relates to a method for manufacturing corresponding amine from nitrile.
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Paragraph 0133-0136; 0165-0169; 0199-0202
(2017/10/22)
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- SUBSTITUTED NICOTINIMIDE INHIBITORS OF BTK AND THEIR PREPARATION AND USE IN THE TREATMENT OF CANCER, INFLAMMATION AND AUTOIMMUNE DISEASE
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Compounds of Formula I, as shown below and defined herein: and pharmaceutically acceptable salts, syntheses, intermediates, formulations, and methods of treating diseases including cancer, inflammation, and autoimmune disease mediated at least in part by Bruton's Tyrosine Kinase (BTK).
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Page/Page column 142
(2015/04/15)
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- HETEROCYCLE-SUBSTITUED TETRACYCLIC COMPOUNDS AND METHODS OF USE THEREOF FOR TREATMENT OF VIRAL DISEASES
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The present invention relates to novel Heterocycle-Substituted Tetracyclic Compounds of Formula (I): (I) and pharmaceutically acceptable salts thereof, wherein A, A', R 2 R 3, R 4 and R are as defined herein. The present i
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Page/Page column 84
(2014/08/06)
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- THIAZOLYL-SUBSTITUED TETRACYCLIC COMPOUNDS AND METHODS OF USE THEREOF FOR TREATMENT OF VIRAL DISEASES
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The present invention relates to novel Thiazolyl-Substituted Tetracyclic Compounds of Formula (I) and pharmaceutically acceptable salts thereof, wherein A, A', R2R3, R4 and R5 are as defined herein. The present
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Page/Page column 65
(2014/08/06)
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- N-Acyl-N'-(pyridin-2-yl) Ureas and Analogs Exhibiting Anti-Cancer and Anti-Proliferative Activities
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Described are compounds of Formula I which find utility in the treatment of cancer, autoimmune diseases and metabolic bone disorders through inhibition of c-FMS (CSF-1R), c-KIT, and/or PDGFR kinases. These compounds also find utility in the treatment of other mammalian diseases mediated by c-FMS, c-KIT, or PDGFR kinases.
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Paragraph 0439
(2014/09/30)
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- Hypervalent iodine catalyzed hofmann rearrangement of carboxamides using oxone as terminal oxidant
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Hofmann rearrangement of carboxamides to carbamates using Oxone as an oxidant can be efficiently catalyzed by iodobenzene. This reaction involves hypervalent iodine species generated in situ from catalytic amount of PhI and Oxone in the presence of 1,1,1,3,3,3-hexafluoroisopropanol (HFIP) in aqueous methanol solutions. Under these conditions, Hofmann rearrangement of various carboxamides affords corresponding carbamates in high yields.
- Yoshimura, Akira,Middleton, Kyle R.,Luedtke, Matthew W.,Zhu, Chenjie,Zhdankin, Viktor V.
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p. 11399 - 11404
(2013/02/23)
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- Heteroalicyclic carboxamidines as inhibitors of inducible nitric oxide synthase; The identification of (2R)-2-pyrrolidinecarboxamidine as a potent and selective haem-co-ordinating inhibitor
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Heteroalicyclic carboxamidines were synthesised and evaluated as inhibitors of nitric oxide synthases. (2R)-2-Pyrrolidinecarboxamidine, in particular, was shown to be a highly potent in vitro (IC50 = 0.12 μM) and selective iNOS inhibitor (>100-fold vs both eNOS and nNOS), with probable binding to the key anchoring glutamate residue and co-ordination to the haem iron.
- Young, Robert J.,Alderton, Wendy,Angell, Anthony D.R.,Beswick, Paul J.,Brown, David,Chambers, C. Lynn,Crowe, Miriam C.,Dawson, John,Hamlett, Christopher C.F.,Hodgson, Simon T.,Kleanthous, Savvas,Knowles, Richard G.,Russell, Linda J.,Stocker, Richard,Woolven, James M.
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scheme or table
p. 3037 - 3040
(2011/06/26)
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- Gold Activation of Nitriles: Catalytic Hydration to Amides
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A gold-based catalytic system that efficiently mediates the hydration of a broad spectrum of nitriles, including aromatic, heteroaromatic and aliphatic examples and efficiently catalyze the hydration of a range of organonitriles has been reported. Nitriles are considered inert in the context gold catalysis and have only been used as reaction solvent or as throw-away ligands in well-defined cationic gold catalysis. The obtained product was purified by flash chromatography using a gradient of pentane/ethyl acetate and compound 1 was isolated as a colorless solid. Aromatic substrates bearing two nitrile groups as in rn-benzenedinitrile and p-benzenedinitrile underwent double nitrile hydration and afforded excellent yields in the corresponding diamides. There is high relevance for the use of cationic gold complexes bearing such ligands and should have important implications in catalysis.
- Ramon, Ruben S.,Marion, Nicolas,Nolan, Steven P.
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supporting information; experimental part
p. 8695 - 8697
(2010/03/24)
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- THIAZOLES, IMIDAZOLES, AND PYRAZOLES USEFUL AS INHIBITORS OF PROTEIN KINASES
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The present invention relates to compounds useful as inhibitors of protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising said compounds and methods of using the compounds and the compositions in the treatment of
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Page/Page column 51-52
(2008/06/13)
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- Mild oxidative one-carbon homologation of aldehyde to amide
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One-carbon homologation of aldehyde into amide is realized in one-pot by its reaction with potassium α-p-methoxyphenyl-α-isocyano acetic acid (1c) and hydrochloride salt of dimethylamine (3a) in toluene at room temperature followed by acidic workup. In this multicomponent reaction, 1c served as donor of the CONH2 function to aldehyde, while the dimethylamine acted as a shuttle molecule to initiate/terminate the sequence and to mediate the internal redox process of one of the three-component adducts. Ready accessibility, nominal cost of the reagents, and mild conditions are attractive features of the present method. Copyright
- Bonne, Damien,Dekhane, Mouloud,Zhu, Jieping
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p. 6926 - 6927
(2007/10/03)
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- Cycloalkylamides and their therapeutic applications
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The present invention relates to the use of compounds of formula (I) for the treatment of a variety of disorders including, but not limited to, epilepsy, bipolar disorder, psychiatric disorders, migraine, pain, neuroprotection, and movement disorders.
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- Cycloalkylamides and their therapeutic applications
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The present invention relates to the use of compounds of formula (I) for the treatment of a variety of disorders including, but not limited to, epilepsy, bipolar disorder, psychiatric disorders, migraine, pain, neuroprotection, and movement disorders.
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- Organic compounds substituted heptadeca-5,9- and 5,10-dienoic acid
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The present invention provides novel substituted heptadeca-5,9- and 5,10-dienoic acid and similar fatty acid compounds which are derivatives of certain prostaglandins and are potent thromboxane A2 inhibitors. By virtue of this pharmacological property, they represent useful pharmacological agents for a wide variety of purposes.
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