- HETEROCYCLIC SULFONAMIDE DERIVATIVE AND MEDICINE COMPRISING SAME
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The present invention provides a compound represented by the formula (I): wherein each symbol is as defined in the DESCRIPTION, or a pharmaceutically acceptable salt thereof. The compound has a superior TRPA1 antagonist activity, and can provide a medicament useful for the prophylaxis or treatment of diseases involving TRPA1 antagonist and TRPA1.
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Paragraph 0350; 0351
(2016/12/01)
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- Discovery of a 4-aryloxy-1H-pyrrolo[3,2-c]pyridine and a 1-aryloxyisoquinoline series of TRPA1 antagonists
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A series of TRPA1 antagonists is described having a 4-aryloxy-1H-pyrrolo[3,2-c]pyridine or a 1-aryloxyisoquinoline scaffold. These compounds have high ligand efficiency and favorable physical properties and may thus serve as scaffolds for further optimization.
- Hu, Yun-Jin,St.-Onge, Miguel,Laliberté, Sébastien,Vallée, Frédéric,Jin, Shujuan,Bedard, Leanne,Labrecque, Jean,Albert, Jeffrey S.
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supporting information
p. 3199 - 3203
(2015/02/19)
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- Discovery and optimization of 7-aminofuro[2,3-c]pyridine inhibitors of TAK1
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The discovery and potency optimization of a series of 7-aminofuro[2,3-c] pyridine inhibitors of TAK1 is described. Micromolar hits taken from high-throughput screening were optimized for biochemical and cellular mechanistic potency to ~10 nM, as exemplified by compound 12az. Application of structure-based drug design aided by co-crystal structures of TAK1 with inhibitors significantly shortened the number of iterations required for the optimization.
- Hornberger, Keith R.,Berger, Dan M.,Crew, Andrew P.,Dong, Hanqing,Kleinberg, Andrew,Li, An-Hu,Medeiros, Matthew R.,Mulvihill, Mark J.,Siu, Kam,Tarrant, James,Wang, Jing,Weng, Felix,Wilde, Victoria L.,Albertella, Mark,Bittner, Mark,Cooke, Andrew,Gray, Michael J.,Maresca, Paul,May, Earl,Meyn, Peter,Peick Jr., William,Romashko, Darlene,Tanowitz, Michael,Tokar, Brianna
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p. 4517 - 4522
(2013/08/23)
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- IMIDAZOTHIADIAZOLE DERIVATIVES AS PROTEASE ACTIVATED RECEPTOR 4 (PAR4) INHIBITORS FOR TREATING PLATELET AGGREGATION
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The present invention provides imidazothiadiazole compounds of Formula (I) wherein A, B, D, Rx, R1, R2, R3, X1, X2 and s are as defined herein, or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein all of the variables are as defined herein. These compounds are inhibitors of platelet aggregation and thus can be used as medicaments.
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- 7-AMINOFUROPYRIDINE DERIVATIVES
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Compounds of Formula 1, as shown below and defined herein: pharmaceutically acceptable salts thereof, synthesis, intermediates, formulations, and methods of disease treatment therewith, including treatment of cancers, such as tumors driven at least in part by TAK1 or for which an appropriate TAK1 inhibitor is effective. This Abstract is not limiting of the invention.
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Page/Page column 23
(2011/09/15)
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- Toolbox for regioselective lithiations of furo[2,3-c]pyridine
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Chemical Reaction Reprentation A detailed procedure for successive regioselective lithiations of furo[2,3-c]pyridine is described by using n-BuLi and the [n-BuLi/LiDMAE] Superbase. Several polysubstituted furo[2,3-c]pyridines have been efficiently synthesized and some of them were engaged in Pd- or Ni-catalyzed coupling reactions leading to 2,2'- or 7,7'-bifuro[2,3-c]pyridine ligands.
- Chartoire, Anthony,Comoy, Corinne,Fort, Yves
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scheme or table
p. 2227 - 2235
(2010/06/15)
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- Design and synthesis of piperazinylpyridine derivatives as novel 5-HT 1A agonists/5-HT3 antagonists for the treatment of irritable bowel syndrome (IBS)
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We have prepared a series of piperazinylpyridine derivatives for the treatment of irritable bowel syndrome (IBS). These compounds, which were designed by pharmacophore analysis, bind to both serotonin subtype 1A (5-HT 1A) and subtype 3 (5-HT3) receptors. The nitrogen atom of the isoquinoline, a methoxy group and piper-azine were essential to the pharmacophore for binding to these receptors. We also synthesized furo- and thienopyridine derivatives according to structure-activity relationship analyses. Compound 17c (TZB-20810) had high affinities to these receptors and exhibited 5-HT1A agonistic activity and 5-HT3 antagonistic activity concurrently, and is a promising drug for further development in the treatment of IBS.
- Asagarasu, Akira,Matsui, Teruaki,Hayashi, Hiroyuki,Tamaoki, Satoru,Yamauchi, Yukinao,Sato, Michitaka
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experimental part
p. 34 - 42
(2009/07/18)
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- PYRIMIDINE DERIVATIVE
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This invention provides pyrimidine derivatives represented by a formula, in the formula, ring A stands for carbocyclic group or heterocyclic group, X 1 stands for hydrogen, lower alkyl, amino, etc., X 2 stands for hydrogen or lower alkyl, Y stands for a direct bond or sulfur or nitrogen, n stands for an integer of 0 - 4, and Ar stands for a group of the following formula, or a salt thereof, which concurrently exhibit 5-HT 1A agonistic activity and 5-HT 3 antagonistic activity and are useful for therapy and treatments of diseases such as IBS. The invention furthermore provides a therapeutic method of IBS, characterized by having 5-HT 1A agonistic activity and 5-HT 3 antagonistic activity work simultaneously and cooperatively in vivo, which comprises either administering 5-HT 3 antagonistic agent which concurrently exhibits 5-HT 1A agonistic activity, or administering 5-HT 1A agonistic agent and 5-HT 3 antagonistic agent simultaneously, in sequence or at an interval.
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Page/Page column 129
(2010/11/24)
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- FUNGAL CELL WALL SYNTHESIS GENE
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A reporter system reflecting the transport process that transports GPI-anchored proteins to the cell wall was constructed and compounds inhibiting this process were discovered. Further, genes conferring resistance to the above compounds were identified and methods of screening for compounds that inhibit the activity of the proteins encoded by these genes were developed.Therefore, through the novel compounds, the present invention showed that antifungal agents having a novel mechanism, i.e. inhibiting the process that transports GPI-anchored proteins to the cell wall, could be achieved.
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- 7-Methoxyfuro[2,3-c]pyridine-4-carboxamides as PDE4 inhibitors: A potential treatment for asthma
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The synthesis and pharmacological profile of a novel series of 7-methoxy-furo[2,3-c]pyridine-4-carboxamides is described. Some of these compounds were found to be potent inhibitors of phosphodiesterase type 4 (PDE4). Initial
- Buckley, George M.,Cooper, Nicola,Davenport, Richard J.,Dyke, Hazel J.,Galleway, Fiona P.,Gowers, Lewis,Haughan, Alan F.,Kendall, Hannah J.,Lowe, Christopher,Montana, John G.,Oxford, Janet,Peake, Joanna C.,Picken,Richard, Marianna D.,Sabin, Verity,Sharpe, Andrew,Warneck, Julie B.H.
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p. 509 - 512
(2007/10/03)
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- Furopyridines. XXIII [1]. Synthesis and Reactions of Chloropyridine Derivatives of Furo[2,3-b]-, -[2,3-c]- and -[3,2-c]pyridine
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Chlorination of the N-oxides of furo[2,3-b]- 1a, -[2,3-c]- 1b and -[3,2-c]pyridine 1c with phosphorus oxychloride afforded compounds substituted normally at the α- or γ-position to the ring nitrogen, 2a, 2′a, 2b, 2c, 2′c and 2″c, and in addition, in the case of 1b, compounds substituted on the furan ring, 2′b and 2″b. The structures of these compounds were confirmed from their ir, nmr and mass spectra. The major chlorinated products 2a, 2b and 2c were converted to methoxy- 5a, 5b and 5c, N-pyrrolidyl- 7a, 7b and 7c, and phenylthiofuropyridines 8a, 8b, and 8c.
- Shiotani, Shunsaku,Taniguchi, Katsunori
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p. 925 - 929
(2007/10/03)
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- Furopyridines. I. Synthesis of Furopyridine
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The parent framework of furopyridine has been synthesized. 3-Furoic acid chloride (2) was reduced with bis(triphenylphosphine) copper(I) tetrahydroborate to afford 3-furaldehyde (3) which was condensed with malonic acid to give β-(3-furyl)acrylic acid (4).The acrylic acid 4 was converted to the acid azide (5), which in turn was cyclized to give furopyridin-7(6H)-one (6) by heating at 180 deg in diphenylmethane.The pyridone 6 was chlorinated with phosphorus oxychloride, followed by reduction with zinc and acetic acid to give furopyridine (8).
- Shiotani, Shunsaku,Morita, Hiroyuki
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p. 1207 - 1209
(2007/10/02)
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