- Amine compound for inhibiting SSAO/VAP-1 and application thereof in medicines
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The present invention relates to an amine compound for inhibiting SSAO/VAP-1 and application thereof in medicines. In particular, the present invention relates to an amine compound for inhibiting a semicarbazide-sensitive oxidase (SSAO) and/or vascular adhesion protein-1 (VAP-1) inhibitor, or a pharmaceutically acceptable salt thereof, a stereoisomer or an/a E/Z isomer, further relates to a pharmaceutical composition containing the amine compound. The invention further relates to the application of the amine compound and the pharmaceutical composition in manufacture of the medicines for treatment of inflammation, inflammation-related diseases and immune diseases.
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Paragraph 0482; 0483; 0484; 0485
(2018/09/08)
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- NOVEL CRYPTOPHYCIN COMPOUNDS AND CONJUGATES, THEIR PREPARATION AND THEIR THERAPEUTIC USE
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The present invention relates to cryptophycin compounds of formula (I). The invention also relates to cryptophycin payloads, to cryptophycin conjugates, to compositions containing them and to their therapeutic use, especially as anticancer agents. The inv
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Page/Page column 163
(2017/06/30)
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- Direct C-H alkylation of naphthoquinones with amino acids through a revisited Kochi-Anderson radical decarboxylation: Trends in reactivity and applications
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In our ongoing research program into the discovery of new anticancer drugs, we were interested in the preparation of naphthoquinone scaffolds bearing aminoalkyl side-chains. Following this aim, we revisited the Kochi-Anderson radical decarboxylation of amino acids in order to set up a versatile route to the direct functionalization of naphthoquinones. The best reaction conditions were applied to a selected series of compounds in a systematic methodological study which allowed us to establish important trends in reactivity. We found that α-substituted β-amino acids were the most suitable substrates for the radical addition. In contrast, α-amino acids gave modest results. The influence of the amine protecting groups on the reaction outcome has also been studied. This practical procedure allows the introduction of various unsymmetrical moieties, including orthogonally protected linear aminoalkyl chains or chiral dipeptidic chains, and opens the door to a wide scope of easily accessible chemical diversity.
- Naturale, Guillaume,Lamblin, Marc,Commandeur, Claude,Dessolin, Jean,Felpin, Francois-Xavier
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supporting information
p. 5774 - 5788,15
(2020/09/15)
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- New 7,8-dihydro-1,6-naphthyridin-5(6h)-one-derivatives as PDE4 inhibitors
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New 7,8-dihydro-1,6-naphthyridin-5(6H)-one derivatives derivatives having the chemical structure of formula (I) are disclosed; as well as process for their preparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of the phosphodiesterase IV (PDE4).
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Page/Page column 19
(2011/11/07)
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- PROKINETICIN RECEPTOR ANTAGONISTS AND USES THEREOF
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Contemplated compounds, compositions, and methods of prokineticin antagonists are presented where a prokineticin antagonist is used in the treatment and prevention of various conditions and disorders, and especially type II diabetes.
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Page/Page column 28
(2010/08/04)
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- Exploring the original proposed biosynthesis of (+)-symbioimine: Remote exocyclic stereocontrol in a type i IMDA reaction
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(Figure Presented) The originally proposed biosynthesis of (+)-symbioimine was explored, resulting in the successful intramolecular Diels-Alder (IMDA) cyclization of an appropriate (E,E,E)-1,7,9-decatrien-3-one. In contrast to the originally proposed bios
- Burke, Jason P.,Sabat, Michal,Iovan, Diana A.,Myers, William H.,Chruma, Jason J.
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supporting information; experimental part
p. 3192 - 3195
(2010/10/04)
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- One-pot synthesis of β-amino acid derivatives via addition of bis(O-silyl) ketene acetals on iminium salts
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We report here our findings on a new and highly efficient strategy for the synthesis of β-amino acids involving the addition of bis(O-silyl) ketene acetals on Mannich type iminium electrophiles.
- Moumné, Roba,Denise, Bernard,Parlier, Andrée,Lavielle, Solange,Rudler, Henri,Karoyan, Philippe
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p. 8277 - 8280
(2008/03/30)
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- Efficient synthesis of β2-amino acid by homologation of α-amino acids involving the reformatsky reaction and Mannich-type imminium electrophile
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Development of new methods for the synthesis of β-amino acids is important as polymers of these compounds are promising peptidomimetic candidates in medicinal chemistry. We report here our findings on a new and highly efficient general strategy for the synthesis of β2-amino acids by homologation of α-amino acids, involving the Reformatsky reaction and Mannich-type imminium electrophile.
- Moumne, Roba,Lavielle, Solange,Karoyan, Philippe
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p. 3332 - 3334
(2007/10/03)
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- PYRIDYLPYRROLE DERIVATIVES ACTIVE AS KINASE INHIBITORS
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Pyridylpyrrole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful, in therapy, in the treat
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Page/Page column 25
(2010/02/10)
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- PHARMACEUTICAL COMPOUNDS
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The invention provides novel cryptophycin compounds which can be useful for disrupting the microtubulin system, as antineoplastic agents, and for the treatment of cancer. The invention further provides a formulation for administering the novel cryptophycin compounds.
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- Optical resolution of aminoisobobutyric acid
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A process for resolving amino protected racemic 3-amino-2-methylpropionic acid which comprises the steps of: (1) reacting said amino protected acid with a protected amino group with an enantiomer of a chiral amine to form diastereomeric salts; (2) recrystallizing the diastereomeric salts from ethyl acetate to separate the diastereomeric salts into crystal fractions; and (3) releasing the resolved acid from the diastereomeric salt by treating the diastereomeric salt with a basic solution is disclosed. A process for the preparation of the cryptophycin molecules is also disclosed.
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Page column 4
(2008/06/13)
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- Urethane N-carboxyanhydrides from β-amino acids
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A general method has been developed for the synthesis of N-tert-butyloxycarbonyl N-carboxyanhydrides from β-amino acids using Vilsmeier complex. These β-UNCA are stable, and the reactivity with different nucleophiles (alcohol, amine, lithium enolate) was studied.
- McKiernan,Huck,Fehrentz,Roumestant,Viallefont,Martinez
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p. 6541 - 6544
(2007/10/03)
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