- CARBOXAMIDE AND SULFONAMIDE DERIVATIVES USEFUL AS TEAD MODULATORS
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The invention is concerned with the compounds of formula (I) and formula (II): and pharmaceutically acceptable salts thereof. In addition, the present invention relates to methods of using the compounds of formula (I) and formula (II) as well as pharmaceutical compositions containing such compounds. The compounds are useful in treating diseases and conditions mediated by TEAD, such as cancer.
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Paragraph 0506-0508; 0511-0512
(2020/03/29)
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- Compositions for Treatment of Cystic Fibrosis and Other Chronic Diseases
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The present invention relates to pharmaceutical compositions comprising an inhibitor of epithelial sodium channel activity in combination with at least one ABC Transporter modulator compound of Formula A, Formula B, Formula C, or Formula D. The invention also relates to pharmaceutical formulations thereof, and to methods of using such compositions in the treatment of CFTR mediated diseases, particularly cystic fibrosis using the pharmaceutical combination compositions.
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Paragraph 0415; 1634
(2015/09/22)
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- Iridium-catalyzed methylation of indoles and pyrroles using methanol as feedstock
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Iridium-catalyzed methylation of indoles and pyrroles using methanol as the methylating agent was achieved. This transformation takes place via a borrowing hydrogen methodology under an air atmosphere, which constitutes a direct route to 3-methyl-indoles and methyl-pyrroles.
- Chen, Shu-Jie,Lu, Guo-Ping,Cai, Chun
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p. 70329 - 70332
(2015/09/07)
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- Regioselective hydroarylation reactions of C3 electrophilic N-acetylindoles activated by FeCl3: An entry to 3-(Hetero)arylindolines
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A method for the direct and rare umpolung of the 3 position of indoles is reported. The activation of N-acetylindole with iron(III) chloride allows the C-H addition of aromatic and heteroaromatic substrates to the C2-C3 double bond of the indole nucleus to generate a quaternary center at C3 and leads regioselectively to 3-arylindolines. Optimization, scope (50 examples), practicability (gram scale, air atmosphere, room temperature), and mechanistic insights of this process are presented. Synthetic transformations of the indoline products into drug-like compounds are also described.
- Beaud, Rodolphe,Guillot, Regis,Kouklovsky, Cyrille,Vincent, Guillaume
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supporting information
p. 7492 - 7500
(2014/06/23)
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- MODULATORS OF ATP-BINDING CASSETTE TRANSPORTERS
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The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.
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- COMPOSITIONS FOR TREATMENT OF CYSTIC FIBROSIS AND OTHER CHRONIC DISEASES
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The present invention relates to pharmaceutical compositions comprising an inhibitor of epithelial sodium channel activity in combination with at least one ABC Transporter modulator compound of Formula A, Formula B, Formula C, or Formula D. The invention also relates to pharmaceutical formulations thereof, and to methods of using such compositions in the treatment of CFTR mediated diseases, particularly cystic fibrosis using the pharmaceutical combination compositions.
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- One-pot N-alkylation/Heck approach to substituted indoles
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Here, we report the palladium-catalyzed one-pot N-alkylation/Heck cyclization of anilines to substituted indoles employing Pd(OAc)2/XPhos. The scope and limitations of this methodology will be described.
- Weinrich, Melissa L.,Beck, Hilary P.
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experimental part
p. 6968 - 6972
(2010/02/27)
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- Modulators of ATP-binding cassette transporters
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Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.
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Page/Page column 111
(2008/06/13)
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- Reaction of indole and alkylindoles with ceric ammonium nitrate on silica gel
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Treatment of N-methylindole with CAN-on-SiO2 furnished 2,2-bis(N-methyl-3′-indolyl)-N-methylindoxyl, whereas that of skatole, N-methyl and N-ethyl skatoles produced the respective 2-nitroskatoles along with 6-nitroskatole and N-methyl-5-nitroskatole.
- Chakrabarty, Manas,Sarkar, Sandipan,Basak, Ramkrishna
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p. 664 - 665
(2007/10/03)
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- Synthesis of Indoles via Ring Closure of 2-Alkylnitroaniline Derivatives.
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A variety of nitroindoles have been prepared from imidate, amidine, and sec-anilide derivatives of 2-alkyl-3- or 5-nitroanilines by a base-induced cyclization promoted by dialkyl oxalates.It is shown that essentially the same procedure also can be used to synthesize the corresponding nitroindole-3-glyoxylates in one simple operation.The synthetic potential is discussed and a mechanism is proposed.
- Bergman, Jan,Sand, Peter
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p. 6085 - 6112
(2007/10/02)
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