- 3-HYDROXY-IMIDAZOLIDIN-4-ONE COMPOUNDS AS INHIBITORS OF INDOLEAMINE 2,3-DIOXYGENASE
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The invention relates to a compound of Formula (I) : Formula (I), or pharmaceutically acceptable enantiomers, or salts thereof. The present invention also relates to the use of compounds of Formula (I) as selective inhibitors of indoleamine 2,3-dioxygenas
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Page/Page column 38
(2019/03/17)
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- INHIBITORS OF INDOLEAMINE 2,3-DIOXYGENASE
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The invention relates to a compound of Formula (I), or pharmaceutically acceptable enantiomers, or salts thereof. The present invention also relates to the use of compounds of Formula (I) as selective inhibitors of indoleamine 2,3-dioxygenase. The inventi
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Page/Page column 38
(2017/09/28)
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- TETRAHYDROISOQUINOLINE DERIVATIVES
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The present invention relates to tetrahydroisoquinoline derivatives according to formula (I), which are Positive Allosteric Modulators of D1 and accordingly of benefit as pharmaceutical agents for the treatment of diseases in which D1 receptors play a role.
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Page/Page column 92-93
(2016/05/02)
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- 2 - (2, 4, 5 - SUBSTITUTED -ANILINO) PYRIMIDINE DERIVATIVES AS EGFR MODULATORS USEFUL FOR TREATING CANCER
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The present invention relates to certain 2-(2,4,5-substituted-anilino) pyrimidine compounds and pharmaceutically acceptable salts thereof which may be useful in the treatment or prevention of a disease or medical condition mediated through certain mutated forms of epidermal growth factor receptor (for example the L858R activating mutant, the Exonl9 deletion activating mutant and the T790M resistance mutant). Such compounds and salts thereof may be useful in the treatment or prevention of a number of different cancers. The invention also relates to pharmaceutical compositions comprising said compounds and salts thereof, especially useful polymorphic forms of these compounds and salts, intermediates useful in the manufacture of said compounds and to methods of treatment of diseases mediated by various different forms of EGFR using said compounds and salts thereof.
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Page/Page column 100
(2013/03/26)
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- A short way to switchable carbenes
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A new, one-step route to N-heterocyclic oxo-carbene complexes (NHOCs), representatives of chemo-switchable NHC complexes, is reported. This simple procedure provides an easy access to gold, palladium and platinum complexes of these ligands. Copyright
- Hashmi, A. Stephen K.,Lothschuetz, Christian,Graf, Katharina,Haeffner, Tobias,Schuster, Andreas,Rominger, Frank
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supporting information; experimental part
p. 1407 - 1412
(2011/08/07)
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- 1,3-dipolar cycloaddition of nitrones with 5-methylenehydantoins: Synthesis and transformation of new spirohydantoin derivatives
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1,3-Dipolar cycloaddition of various acyclic nitrones with 5-methylenehydantoin derivatives afforded new chiral spiroadducts in good yields. All the spirohydantoins were obtained through a regio-and stereospecific pathway, and the spirocarbon atom was linked to the isoxazolidine oxygen atom. A representative example of the reduction of the spirohydantoin 8 with Zn/AcOH led to the substituted 1,3-aminoalcohol hydantoin 20.
- Bahy, Amira,Kacem, Yakdhane,Hassine, Bechir Ben
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experimental part
p. 1377 - 1390
(2010/06/21)
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- New strategies for the design of folded peptoids revealed by a survey of noncovalent interactions in model systems
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Controlling the equilibria between backbone cis- and trans-amides in peptoids, or N-substituted glycine oligomers, constitutes a significant challenge in the construction of discretely folded peptoid structures. Through the analysis of a set of monomeric peptoid model systems, we have developed new and general strategies for controlling peptoid conformation that utilize local noncovalent interactions to regulate backbone amide rotameric equilibria, including n→π*, steric, and hydrogen bonding interactions. The chemical functionalities required to implement these strategies are typically confined to the peptoid side chains, preserve chirality at the side chain N-α-carbon known to engender peptoid structure, and are fully compatible with standard peptoid synthesis techniques. Our examinations of peptoid model systems have also elucidated how solvents affect various side chain-backbone interactions, revealing fundamental aspects of these noncovalent interactions in peptoids that were largely uncharacterized previously. As validation of our monomeric model systems, we extended the scope of this study to include peptoid oligomers and have now demonstrated the importance of local steric and n→π* interactions in dictating the structures of larger, folded peptoids. This new, modular design strategy has guided the construction of peptoids containing 1-naphthylethyl side chains, which we show can be utilized to effectively eliminate trans-amide rotamers from the peptoid backbone, yielding the most conformationally homogeneous class of peptoid structures yet reported in terms of amide rotamerism. Overall, this research has afforded a valuable and expansive set of design tools for the construction of both discretely folded peptoids and structurally biased peptoid libraries and should shape our understanding of peptoid folding.
- Gorske, Benjamin C.,Stringer, Joseph R.,Bastian, Brent L.,Fowler, Sarah A.,Blackwell, Helen E.
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scheme or table
p. 16555 - 16567
(2010/02/15)
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- OCTAHYDRO-PYRROLO[3,4-B]PYRROLE N-OXIDES
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The invention relates to octahydro-pyrrolo[3,4-b]pyrrole N-oxides as prodrugs of CNS-active compounds, compositions comprising such compounds, methods for making the compounds, salts, and polymorphs, and methods of treating conditions and disorders using
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Page/Page column 17
(2009/04/25)
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- Local and tunable n→π* interactions regulate amide isomerism in the peptoid backbone
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We report that n→π* interactions are operative in peptoids and play a major role in controlling amide isomerism. These interactions can be tuned using α-chiral amide side chains known to promote peptoid folding. To our knowledge, this is the first report of n→π* interactions between amides in non-prolyl systems. Furthermore, we have characterized an n→π* interaction between backbone carbonyls and side chain aromatic rings that can dramatically stabilize the cis-amides required for peptoid helix formation. The tunability of both types of n→π* interactions in peptoids has significant implications for peptoid folding and could be exploited for the design of new peptoid architectures. Copyright
- Gorske, Benjamin C.,Bastian, Brent L.,Geske, Grant D.,Blackwell, Helen E.
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p. 8928 - 8929
(2008/02/09)
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- OCTAHYDRO-PYRROLO[3,4-B]PYRROLE DERIVATIVES
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Octahydro-pyrrolo[3,4-b]pyrrole derivatives are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Octahydro-pyrrolo[3,4-b]pyrrole compounds, methods for using such compounds, compositions for making th
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Page/Page column 73
(2008/06/13)
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- Functionalized alkyl and alenyl side chain derivatives of glycinamides as farnesyl transferase inhibitors
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The present invention provides compounds of Formula (I). The present invention also provides a method of treating cancer and treating or preventing restenosis or atherosclerosis. Also provided by the present invention is a pharmaceutically acceptable comp
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- Diazabicyclooctane derivatives
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PCT No. PCT/GB96/02312 Sec. 371 Date Mar. 12, 1998 Sec. 102(e) Date Mar. 12, 1998 PCT Filed Sep. 19, 1996 PCT Pub. No. WO97/11949 PCT Pub. Date Apr. 3, 1997A class of 2,7-diazabicyclo[3.3.0]octane derivatives represented by formula I are selective agonist
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