- HETEROCYCLIC COMPOUNDS FOR THE TREATMENT OF EPILEPSY
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The present invention provides a novel heterocyclic compound represented by Formula [I] and a salt thereof: wherein the symbols are as defined in the specification, which is useful for treating, preventing and/or diagnosing seizure and the like in disease involving epileptic seizure or convulsive seizure (including multiple drug resistant seizure, refractory seizure, acute symptomatic seizure, febrile seizure and status epilepticus), as well as a medical use therefor.
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Paragraph 0134; 0143; 0144
(2020/06/19)
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- AGRICULTURAL CHEMICALS
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The present invention relates to picolinic acid derivatives that are useful in treating fungal diseases ofplants.
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Page/Page column 55; 90
(2019/08/08)
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- Novel cobalt-valine catalyzed O-arylation of phenols with electron deficient aryl iodides
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Abstract: A Novel cobalt-catalyzed O-arylation of phenols with electron deficient aryl iodides is described. The reaction employs cheap and easy-to-handle cobalt acetate tetrahydrate as the catalyst precursor and naturally occurring l-valine as the ligand without the use of any transmetallating or reducing agents. The new protocol offers a wide scope for a variety of phenols towards O-arylation with moderate to excellent yields with electron deficient aryl iodides.
- Ujwaldev, Sankuviruthiyil M.,Saranya, Salim,Harry, Nissy Ann,Anilkumar, Gopinathan
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p. 339 - 346
(2019/01/18)
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- Synthesis and characterization of the first inhibitor of: N -acylphosphatidylethanolamine phospholipase D (NAPE-PLD)
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N-Acylphosphatidylethanolamine phospholipase D (NAPE-PLD) is a membrane-associated zinc enzyme that catalyzes the hydrolysis of N-acylphosphatidylethanolamines (NAPEs) into fatty acid ethanolamides (FAEs). Here, we describe the identification of the first small-molecule NAPE-PLD inhibitor, the quinazoline sulfonamide derivative 2,4-dioxo-N-[4-(4-pyridyl)phenyl]-1H-quinazoline-6-sulfonamide, ARN19874.
- Castellani, Beatrice,Diamanti, Eleonora,Pizzirani, Daniela,Tardia, Piero,Maccesi, Martina,Realini, Natalia,Magotti, Paola,Garau, Gianpiero,Bakkum, Thomas,Rivara, Silvia,Mor, Marco,Piomelli, Daniele
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supporting information
p. 12814 - 12817
(2017/12/06)
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- Thieme Chemistry Journals Awardees - Where Are They Now? Rhodium-Catalyzed Synthesis of Unsymmetric Di(heteroaryl) Ethers Using Heteroaryl Exchange Reaction
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Unsymmetric di(heteroaryl) ethers were synthesized by the rhodium-catalyzed heteroaryl exchange reaction of heteroaryl aryl ethers and heteroaryl esters at equilibrium. Diverse unsymmetric di(heteroaryl) ethers containing five- and six-membered heteroaren
- Tanii, Saori,Arisawa, Mieko,Tougo, Takaya,Horiuchi, Kiyofumi,Yamaguchi, Masahiko
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supporting information
p. 1601 - 1607
(2017/08/11)
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- N-Picolinamides as ligands in Ullman type C–O coupling reactions
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Copper-catalyzed modified Ullmann coupling reactions creating C–O bonds, including diaryl ethers or phenols, are vital to organic synthesis. Synthesized N-phenyl-2-pyridinecarboxamide and its derivatives were used as ligands in conjunction with catalytic copper sources in the formation of various diaryl ethers and phenols. Various aryl and heteroaryl halides with electron donating and withdrawing groups were reacted with various phenols under mild reaction conditions providing moderate to excellent yields.
- Damkaci, Fehmi,Sigindere, Cihad,Sobiech, Thomas,Vik, Erik,Malone, Joshua
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supporting information
p. 3559 - 3564
(2017/10/05)
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- Pyrrole inhibitors of S-nitrosoglutathione reductase as therapeutic agents
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The present invention is directed to inhibitors of S-nitrosoglutathione reductase (GSNOR), pharmaceutical compositions comprising such GSNOR inhibitors, and methods of making and using the same.
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Page/Page column 309
(2015/11/16)
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- INHIBITORS OF BRUTON'S TYROSINE KINASE
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This application discloses compounds according to generic Formula (I): wherein all variables are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are useful for the treatment of oncological, auto-immune, and inflammatory diseases caused by aberrant B-cell activation. Also disclosed are compositions containing compounds of Formula I and at least one carrier, diluent or excipient.
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Page/Page column 48; 50; 53; 57
(2015/06/25)
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- Base-mediated N- And O-arylations of NH-containing heterocycles, heterocyclic amines and phenols
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Nucleophilic substitution reactions of N-heterocycles such as imidazole, benzimidazole, indole and pyrazole as well as NH2 or OH containing heterocycles, with electron-deficient aryl halides in the presence of t-BuOK or K2CO3as base and DMSO as solvent are reported. A series of N-aryl azoles, unsymmetric diaryl ethers and diaryl amines were obtained in good yields.
- Ghasemi, Zarrin,Shahrak, Nasim Shahi,Roomi, Behzad Jalali,Zakeri, Ziba
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-
- Synthesis of benzofuro[3,2-b]pyridines via palladium-catalyzed dual C-H activation of 3-phenoxypyridine 1-oxides
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An efficient oxidative cyclization to straightforward synthesis of benzofuro[3,2-b]pyridine 1-oxides with high regioselectivity via Pd-catalyzed intramolecular dual C-H activation was developed. The resulting products could be deoxygenated easily to the corresponding benzofuro[3,2-b]pyridines in excellent yields.
- Sun, Wei,Wang, Min,Zhang, Yicheng,Wang, Lei
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supporting information
p. 426 - 429
(2015/03/03)
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- COMPOUNDS USEFUL AS ANTIBIOTIC TOLERANCE INHIBITORS
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The disclosure provides compounds and pharmaceutical compositions of the compounds useful for treating chronic and acute bacterial infections. Certain of the compounds are compounds and salts of general Formula VIII Certain compounds of this disclosure are MvfR inhibitors. MvfR inhibitors reduce the formation of antibiotic tolerant bacterial strains and are useful for treating Gram-negative bacterial infections and reducing the virulence of Pseudomonas aeruginosa. Methods of treating bacterial infections in a patient, including Pseudomonas aeruginosa infections, are also provided by the disclosure.
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Page/Page column 29; 30
(2014/11/13)
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- Discovery of 1,4-disubstituted 3-cyano-2-pyridones: A new class of positive allosteric modulators of the metabotropic glutamate 2 receptor
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The discovery and characterization of compound 48, a selective and in vivo active mGlu2 receptor positive allosteric modulator (PAM), are described. A key to the discovery was the rational exploration of the initial HTS hit 13 guided by an overlay model built with reported mGlu2 receptor PAM chemotypes. The initial weak in vitro activity of the hit 13 was quickly improved, although compounds still had suboptimal druglike properties. Subsequent modulation of the physicochemical properties resulted in compounds having a more balanced profile, combining good potency and in vivo pharmacokinetic properties. Final refinement by addressing cardiovascular safety liabilities led to the discovery of compound 48. Besides good potency, selectivity, and ADME properties, compound 48 displayed robust in vivo activity in a sleep-wake electroencephalogram (sw-EEG) assay consistent with mGlu2 receptor activation, in accordance with previous work from our laboratories.
- Cid, Jose María,Duvey, Guillaume,Tresadern, Gary,Nhem, Vanthea,Furnari, Rocco,Cluzeau, Philippe,Vega, Juan Antonio,De Lucas, Ana Isabel,Matesanz, Encarnación,Alonso, José Manuel,Linares, María Lourdes,Andrés, José Ignacio,Poli, Sonia M.,Lutjens, Robert,Himogai, Hassan,Rocher, Jean-Philippe,MacDonald, Gregor J.,Oehlrich, Daniel,Lavreysen, Hilde,Ahnaou, Abdelah,Drinkenburg, Wilhelmus,MacKie, Claire,Trabanco, Andrés A.
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experimental part
p. 2388 - 2405
(2012/05/05)
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- INDOLE COMPOUNDS AS AN INHIBITOR OF CELLULAR NECROSIS
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The present invention relates to new indole compounds, pharmaceutically acceptable salts or isomers thereof which are useful for the prevention or treatment of cellular necrosis and necrosis-associated diseases. The present invention also relates to a method and a composition for the prevention or treatment of cellular necrosis and necrosis-associated diseases, comprising said indole compounds as an active ingredient.
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Page/Page column 17
(2010/08/22)
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- GLUCOKINASE ACTIVATORS AND PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME AS AN ACTIVE INGREDIENT
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The present invention relates to new compounds of formula (1) exhibiting excellent activity for glucokinase, and pharmaceutical compositions comprising the same as an active ingredient.
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Page/Page column 22
(2010/11/03)
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- INDOLE COMPOUNDS AS AN INHIBITOR OF CELLULAR NECROSIS
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The present invention relates to new indole compounds, pharmaceutically acceptable salts or isomers thereof which are useful for the prevention or treatment of cellular necrosis and necrosis-associated diseases. The present invention also relates to a method and a composition for the prevention or treatment of cellular necrosis and necrosis-associated diseases, comprising said indole compounds as an active ingredient.
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Page/Page column 57
(2009/04/25)
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- GLUCOKINASE ACTIVATORS AND PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME AS AN ACTIVE INGREDIENT
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The present invention relates to new compounds of formula (1) exhibiting excellent activity for glucokinase, and pharmaceutical compositions comprising the same as an active ingredient.
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Page/Page column 73-74
(2009/07/25)
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- HETEROCYCLIC MODULATORS OF GPR119 FOR TREATMENT OF DISEASE
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The present invention relates to compounds and methods which may be useful as inhibitors of GPR119 for the treatment or prevention of metabolic, cardiovascular, and metabolic diseases.
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Page/Page column 207
(2009/10/22)
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- QUINAZOLINE DERIVATIVES AS ERBB RECEPTOR TYROSINE KINASES
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The invention concerns quinazoline derivatives of the formula (I), wherein each of R1, R2, R3, R4, R5, R6, R7, X1, Q1, m and n have any of the meanings defined in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use as an antiproliferative agent in the prevention or treatment of tumours which are sensitive to inhibition of erbB receptor tyrosine kinases.
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Page/Page column 204-205
(2010/02/15)
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- BENZIMIDAZOLE CARBOXAMIDES AS RAF KINASE INHIBITORS
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The present invention relates to benzimidazole carboxamides of formula (I), the use of the compounds of formula (I) as inhibitors of as inhibitors of one or more kinases, the use of the compounds of formula (I) for the manufacture of a pharmaceutical composition and a method of treatment, comprising administering said pharmaceutical composition to a patient. Accordingly, the compound of Formula (I) or a pharmaceutically acceptable salt thereof is administered for the treatment of diseases mediated by one or more kinase phathways, preferably by the raf kinase pathway, especially cancers.
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Page/Page column 128
(2008/06/13)
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- MALONAMIDE DERIVATIVES
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The present invention relates to malonamide derivatives of formula (I): A-D-B, the use of the compounds of formula (I) as inhibitors of raf-kinase, the use of the compounds of formula (I) for the manufacture of a pharmaceutical composition and a method of treatment, comprising administering said pharmaceutical composition to a patient.
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- 2-{2-[3-(Pyridin-3-yloxy)phenyl]-2H-tetrazol-5-yl}pyridine: A highly potent, orally active, metabotropic glutamate subtype 5 (mGlu5) receptor antagonist
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Structure-activity relationship studies on 3-(5-pyridin-2-yl-2H-tetrazol-2- yl)benzonitrile 2 led to the discovery of 2-{2-[3-(pyridin-3-yloxy)phenyl]-2H- tetrazol-5-yl}pyridine (10)-a highly potent and selective mGlu5 receptor antagonist with good brain penetration and in vivo receptor occupancy in rat and cross-species oral bioavailability. Structure-activity relationship studies on 3-(5-pyridin-2-yl-2H-tetrazol-2-yl)benzonitrile 2 led to the discovery of 2-{2-[3-(pyridin-3-yloxy)phenyl]-2H-tetrazol-5-yl}pyridine (10)-a highly potent and selective mGlu5 receptor antagonist with good brain penetration and in vivo receptor occupancy in rat and cross-species oral bioavailability.
- Huang, Dehua,Poon, Steve F.,Chapman, Deborah F.,Chung, Janice,Cramer, Merryl,Reger, Thomas S.,Roppe, Jeffrey R.,Tehrani, Lida,Cosford, Nicholas D.P.,Smith, Nicholas D.
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p. 5473 - 5476
(2007/10/03)
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- OXAMIDE DERIVATIVES USEFUL AS RAF-KINASE INHIBITORS
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The present invention relates to oxamide derivatives of Formula (I), the use of the compounds of Formula (I) as inhibitors of raf-kinase, the use of the compounds of Formula (I) for the manufacture of a pharmaceutical composition and a method of treatment, comprising administering said pharmaceutical composition to a patient.
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Page 167; 168
(2008/06/13)
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- GLYCINAMIDE DERIVATIVES AS RAF-KINASE INHIBITORS
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The present invention relates to glycinamide derivatives of formula (I), the use of the compounds of formula (I) as inhibitors of raf-kinase, the use of the compounds of formula (I) for the manufacture of a pharmaceutical composition and a method of treatment, comprising administering said pharmaceutical composition to a patient.
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Page/Page column 154
(2008/06/13)
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- Synthesis and activity studies of conformationally restricted α-ketoamide factor Xa inhibitors
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Confomationally restricted borolysine compounds containing a 2-(2-cyanophenylthio) benzoyl in the P3 position unexpectedly led to enhanced factor Xa inhibition. In an effort to improve both the potency and selectivity of this series by extending into the S' domain, we have replaced the boronic acid with α-ketoamides, utilizing a novel process that was developed in our labs. (C) 2000 DuPont Pharmaceuticals Company. Published by Elsevier Science Ltd. All rights reserved.
- Cacciola, Joseph,Fevig, John M.,Stouten, Pieter F. W.,Alexander, Richard S.,Knabb, Robert M.,Wexler, Ruth R.
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p. 1253 - 1256
(2007/10/03)
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