- (PYRIDIN-2-YL)AMINE DERIVATIVES AS TGF-BETA R1 (ALK5) INHIBITORS FOR THE TREATMENT OF CANCER
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The present invention relates to pharmaceutical compounds, compositions and methods, especially as they are related to compositions and methods for the treatment and/or prevention of a proliferation disorder associated with ΤGFβR1 activity, such as a cancer or fibrosis. The invention provides compounds of Formula (I) and Formula (II) as further described herein having an acidic moiety that enhances tissue specificity for targeted tissues and organs. The invention includes pharmaceutical compositions, pharmaceutical combinations, and methods of use of these compounds for treating conditions including cancer or fibrosis.
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- Palladium on calcium carbonate combined to 2-hydroxypropyl-α/β- cyclodextrins: A selective catalytic system for aqueous heck coupling and hydroarylation
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An efficient, selective and recoverable catalytic system for ligand-free aqueous Heck reactions using hydroxypropylated cyclodextrins (HPCDs) and palladium on calcium carbonate (Pd/CaCO3) is highlighted. Remarkably, stereo- and chemoselectivities could be tuned by the cavity size of cyclodextrins, exploiting the relevance of host-guest interactions. UVVis experiments have led to strong evidence concerning an interplay between Pd(II) and α-HPCD, possibly ascribed to a reduction/stabilization effect of CDs. Unexpectedly, hydroarylation was the favored pathway with acrylonitrile which provided access to 3-phenylpropionitrile derivatives without usual hydride donors. Finally, determination of soluble Pd(0/II) via AAS enabled the definition of a predominant homogeneous mechanism in which TONs over 5000 were observed.
- Senra, Jaqueline D.,Malta, Luiz Fernando B.,Souza, Andrea Luzia F.,Aguiar, Lucia C. S.,Antunesa
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experimental part
p. 2551 - 2558
(2009/08/14)
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- 1H-IMIDAZO[4,5-C]QUINOLINE DERIVATIVES IN THE TREATMENT OF PROTEIN KINASE DEPENDENT DISEASES
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The invention relates to the use of imidazoquinolines and salts thereof in the treatment of protein kinase diseases and for the manufacture of pharmaceutical preparations for the treatment of said diseases, imidazoquinolines for use in the treatment of protein kinase dependent diseases, a method of treatment against said diseases, comprising administering the imidazoquinolines to a warm-blooded animal, especially a human, pharmaceutical preparations comprising an imidazoquinoline, especially for the treatment of a protein kinase dependent disease, novel imidazoquinolines, and a process for the preparation of the novel imidazoquinolines.
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Page/Page column 101
(2010/02/12)
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- 1H-IMIDAZOQUINOLINE DERIVATIVES AS PROTEIN KINASE INHIBITORS
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The invention relates to imidazoquinolines of formula (I) for use in the treatment of protein kinase dependent diseases; pharmaceutical preparations comprinsing an imidazoquinoline, especially for the treatment of a pretein kinase dependent disease; novel imidazoquinolines; and a process for the preparation of the novel imidazoquinilines.
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Page/Page column 65-66; 71
(2010/02/12)
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- One-step conversion of alcohols into nitriles with simultaneous two-carbon chain elongation. (Cyanomethyl)trimethylphosphonium iodide as a reagent with a dual mode of action
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Treatment of alcohols with an excess of (cyanomethyl)trimethylphosphonium iodide leads, after aqueous hydrolysis, to the clean formation of nitriles with two more carbon atoms than present in the original alcohol. Benzylic, allylic, and aliphatic alcohols without β-branching (RCH2- CH2OH) have been converted to nitriles with success. The required phosphonium iodide is simple to prepare and can be stored for a long time at room temperature.
- Zaragoza, Florencio
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p. 4963 - 4964
(2007/10/03)
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- Experiments on the Chaperon effect in the nitration of aromatics
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A nitro group may be effectively delivered to the ortho position of alkylbenzenes, provided that a suitable chaperon function is located in α- position and a dilute of HNO3 in CH2Cl2 is used. The carbonyl function of an aldehyde or ketone is the best choice, but a carboxyl, alkoxycarbonyl, and amide groups all work well. The ether function showed a less pronounced ortho orientation effect, whereas the hydroxyl group was too prone to oxidation. Side reactions were minimal under the conditions employed. A para chaperon effect was seemingly at work in the CH2Cl2 nitration of benzenepropanenitrile. All the results were compared with the corresponding classical nitration in H2SO4.
- Strazzolini, Paolo,Giumanini, Angelo G.,Runcio, Antonio,Scuccato, Massimo
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p. 952 - 958
(2007/10/03)
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- ARYL RADICALS BY COPPER(II) OXIDATION OF HYDRAZINES: A NEW METHOD FOR THE OXIDATIVE AND REDUCTIVE ARYLATION OF ALKENES
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A new source of aryl radicals interesting from the preparative point of view has been found in the reaction of arylhydrazines and copper(II) sulfate.The process allows selectively both the reductive and oxidative arylation of alkenes.
- Varea, Teresa,Gonzalez-Nunez, Maria E.,Rodrigo-Chiner, Javier,Asensio, Gregorio
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p. 4709 - 4712
(2007/10/02)
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