- PYRIDO OXAZINE AMINO DERIVATIVES AS ALK5 INHIBITORS
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The present invention relates to a compound of general formula (I) inhibiting the growth factor receptor transforming β (TGF-β) type I (ALK5), methods for preparing these compounds, pharmaceutical compositions containing them and their therapeutic use. The compounds according to the invention may be useful in the treatment of diseases or conditions associated with the disruption of the ALK5 signaling pathway in a mammal.
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Paragraph 0420
(2022/01/24)
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- BORON-CONTAINING RHO KINASE INHIBITORS
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The present invention provides boron-containing isoquinoline compounds as protein kinase-modulating compounds. These compounds are useful as neuroprotective and neuro-regenerative agents for the amelioration of glaucoma and other ocular neuropathies.
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Paragraph 00307
(2021/02/12)
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- Iron-catalyzed reaction of urea with alcohols and amines: A safe alternative for the synthesis of primary carbamates
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A general study of the iron-catalyzed reaction of urea with nucleophiles is here presented. The carbamoylation of alcohols allows for the synthesis of N-unsubstituted (primary) carbamates, including present drugs (Felbamate and Meprobamat, without the necessity to apply phosgene and related derivatives. Using amines as nucleophiles gave rise to the respective mono-and disubstituted ureas via selective transamidation reaction. These atom-economical transformations provide a direct and selective access to valuable compounds from cheap and readily available urea using a simple Lewis-acidic iron(Icatalyst.
- Pe?a-López, Miguel,Neumann, Helfried,Beller, Matthias
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p. 2233 - 2238
(2017/07/25)
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- Synthesis of 8-Aminoquinolines by Using Carbamate Reagents: Facile Installation and Deprotection of Practical Amidating Groups
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Described herein is the development of practical routes to 8-aminoquinolines by using readily installable and easily deprotectable amidating reagents. Two scalable procedures were optimized under RhIII-catalyzed conditions: i) the use of pre-generated chlorocarbamates and ii) a two-step one-pot process that directly employs carbamates. Both approaches are highly convenient for the gram-scale synthesis of 8-aminoquinolines under mild conditions. Facile deprotection of the synthetically versatile amidating groups was achieved under the Pd-catalyzed transfer hydrogenation conditions with simultaneous deoxygenation of quinoline N-oxides, thus yielding 8-aminoquinolines in excellent overall efficiency.
- Gwon, Donghyeon,Hwang, Heejun,Kim, Hye Kyung,Marder, Seth R.,Chang, Sukbok
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supporting information
p. 17200 - 17204
(2016/01/25)
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- Piperidine derivatives having renin inhibiting activity
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Novel piperidine derivatives, their manufacture and use as medicaments, are disclosed. The invention is concerned with the novel piperidine derivatives of general formula I wherein R1, R2, R3, R4, Q, X, Z, m and n are as described herein.
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- N-chloro-N-sodio-2-trimethylsilyl ethyl carbamate: A new nitrogen source for the catalytic asymmetric aminohydroxylation
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The use of N-chloro-N-sodio-2-trimethylsilyl ethyl carbamate in the osmium-catalyzed asymmetric aminohydroxylation of alkenes leads to enantiomerically enriched N-trimethylsilylethoxycarbonyl (TeoC) protected aminoalcohols in yields up tO 80% and ee's up to 99%.
- Reddy, K. Laxma,Dress, K. Ruprecht,Sharpless, K. Barry
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p. 3667 - 3670
(2007/10/03)
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- Processes for preparing bis-naphthalimides containing amino-acid derived linkers
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This invention relates to bis-naphthalimides, including 2,2'-[1,2-ethanediylbis[imino(1-methyl-2,1-ethanediyl)]]-bis[5-nitro-1H-benz[de]isoquinoline-1,3(2H)-dione] and 2,2'-[1,2-ethanediylbis[imino(2-methyl-2,1-ethanediyl)]]-bis[5-nitro-1H-benz[de]isoquinoline-1,3(2H)-dione], processes for their preparation, pharmaceutical compositions containing them, and methods of using them to treat cancer in mammals.
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