- ISOINDOLINES AS HDAC INHIBITORS
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The present disclosure relates to inhibitors of zinc-dependent histone deacetylases (HDACs), having the formula: (I) wherein Z, X1, X2, Y1, Y2, Y3, L, Z, and R are described herein.
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Paragraph 00123
(2019/11/12)
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- NOVEL INHIBITOR COMPOUNDS OF PHOSPHODIESTERASE TYPE 10A
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The present invention relates to novel carboxamide compounds, pharmaceutical compositions containing them, and their use in therapy. The compounds possess valuable therapeutic properties and are particularly suitable for treating or controlling medical disorders selected from neurological disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders and for reducing the risk of such disorders
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- Supramolecular control of selectivity in hydroformylation of vinyl arenes: Easy access to valuable β-aldehyde intermediates
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Go against the flow! A rationally designed regioselective hydroformylation catalyst, [Rh/L], in which noncovalent ligand-substrate interactions allow the unprecedented reversal of selectivity from the typical α-aldehyde to the otherwise unfavored product β-aldehyde, is reported. This catalytic system opens up novel and sustainable synthetic pathways to important intermediates for the fine-chemicals industry.
- Dydio, Pawel,Reek, Joost N. H.
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supporting information
p. 3878 - 3882
(2013/05/09)
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- PHARMACEUTICAL PRODUCT CONTAINING LACTAM OR BENZENE SULFONAMIDE COMPOUND
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The present invention provides, for example, the following compounds as a pharmaceutical composition for treating diseases induced by production, secretion or deposition of amyloid β proteins. The present invention provides a pharmaceutical composition for suppressing amyloid β production comprising a compound of the formula: wherein A is a benzene ring, a pyridine ring or a pyrimidine ring, X is sultam, lactam, sulfonamide or the like, C is substituted or unsubstituted imidazolyl, substituted or unsubstituted oxazolyl or the like, R2, R3 and R4 are each independently hydrogen, halogen, hydroxy, carboxy, substituted or unsubstituted alkyl, substituted or unsubstituted alkoxy or the like, its pharmaceutically acceptable salt or a solvate thereof.
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Page/Page column 101
(2012/06/01)
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- Discovery and SAR of substituted 3-oxoisoindoline-4-carboxamides as potent inhibitors of poly(ADP-ribose) polymerase (PARP) for the treatment of cancer
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Through conformational restriction of a benzamide by formation of a seven-membered hydrogen-bond with an oxindole carbonyl group, a series of PARP inhibitors was designed for appropriate orientation for binding to the PARP surface. This series of compound
- Gandhi, Viraj B.,Luo, Yan,Liu, Xuesong,Shi, Yan,Klinghofer, Vered,Johnson, Eric F.,Park, Chang,Giranda, Vincent L.,Penning, Thomas D.,Zhu, Gui-Dong
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scheme or table
p. 1023 - 1026
(2010/06/14)
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- Total synthesis of the aspercyclides
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Two different approaches to the eleven-membered biaryl ether lactones of the aspercyclide family are disclosed. The core regions of these highly strained targets, which are able to interfere with the binding of immunoglobulinE to its high affinity receptor, can either be forged by ring-closing olefin metathesis (RCM) or by a highly diastereoselective chromium-mediated Nozaki-Hiyama-Kishi (NHK) reaction. Whereas the RCM approach turned out to be responsive to minor changes in the substitution pattern of the substrate, the NHK route is more generally applicable. The preparation of the required cyclization precursor 43 hinged on a palladium-catalyzed orthoiodination reaction of 2-methylbenzoic acid, an efficient copper-catalyzed Ullmann coupling, and a Takai-Utimoto olefination as the key steps. Moreover, the esterification of the 2,6-disubstituted benzoic acid 34 with the sterically hindered secondary alcohol 37 was far from trivial. However, this and related transformations were accomplished by recourse to the corresponding acid fluorides, which provided excellent yields in cases in which the more commonly used acid chlorides or mixed anhydrides failed to afford any of the desiredproducts.
- Pospisil, Jiri,Mueller, Christoph,Fuerstner, Alois
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supporting information; experimental part
p. 5956 - 5968
(2010/03/03)
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- POLY(ADP-RIBOSE)POLYMERASE INHIBITORS
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Compounds which inhibit the activity of poly(ADP-ribose)polymerase, compositions containing the compounds and methods of treating diseases using the compounds is disclosed.
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Page/Page column 11
(2008/12/04)
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- SUBSTITUTED DIHYDRO-ISOINDOLONES USEFUL IN TREATING KINASE DISORDERS
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The present invention is directed to novel substituted dihydro-isoindolone compounds of formula (I): and forms thereof, wherein Ring A, X3, R1, R2, R3, R4 and R6 are as herein defined, and their synthesis and use as protein kinase inhibitors and interactions thereof.
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Page/Page column 52
(2008/06/13)
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- Total synthesis of aspercyclide C
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The first total synthesis of (+)-aspercyclide C (1) is reported using a kinetically controlled RCM reaction to form the 11-membered, unsaturated lactone ring of this bioactive diaryl ether macrolide. The Royal Society of Chemistry 2005.
- Fuerstner, Alois,Mueller, Christoph
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p. 5583 - 5585
(2007/10/03)
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- Substituted 2,3-dihydro-1h-isoindol-1-one derivatives and methods of use
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Selected compounds are effective for prophylaxis and treatment of diseases, such as angiogenesis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
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Page/Page column 27
(2010/02/11)
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- COMPOUNDS HAVING ACTIVITY AT 5HT2C RECEPTOR AND USES THEREOF
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Compounds of formula (I) and pharmaceutically acceptable salts thereof are disclosed: wherein R1 is halogen, cyano, C1-6alkyl, C3-7cycloalkyl, C3-7cycloalkyloxy, C1-6alkoxy, C1 6alkylthio, hydroxy, amino, mono or di C1 6alkylamino, an N-linked 4 to 7 memb
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- Suzuki couplings with phthalimidines - An efficient route to staurosporinone analogs
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Staurosporinone analogs have been prepared by an efficient process. The key step is a palladium mediated Suzuki coupling between a bromophthalimidine and an aromatic boronic acid.
- Rupert, Kenneth C.,Dodd, John H.,Henry, James R.
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p. 2217 - 2221
(2007/10/03)
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