- Mild, General, and Regioselective Synthesis of 2-Aminopyridines from Pyridine N -Oxides via N -(2-Pyridyl)pyridinium Salts
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A synthesis of 2-aminopyridines from pyridine N-oxides via their corresponding N-(2-pyridyl)pyridinium salts has been demonstrated and investigated. The reaction sequence features a highly regioselective conversion of the N-oxide into its pyridinium salt
- Xiong, Hui,Hoye, Adam T.
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p. 371 - 375
(2022/01/27)
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- 2-pyridine substituted urea structural small molecule compounds as well as synthesis and application thereof
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The invention relates to 2-pyridine substituted urea structural small molecule compounds as well as synthesis and application thereof. Specifically, the invention discloses the compounds represented by a formula (I) shown in the specification, enantiomers, diastereomers, racemates or a mixture of the compounds, or a pharmaceutically acceptable salt, hydrate and solvate of the compounds, a preparation method of the above materials, and applications of the above materials in preparation of an ASK1 small molecule inhibitor, or medicines for preventing and/or treating diseases related to ASK1, especially liver diseases, lung diseases, cardiovascular diseases, kidney diseases and metabolic diseases.
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Paragraph 0197; 0702; 0706-0707
(2020/03/03)
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- WNT PATHWAY MODULATORS
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The present invention relates to dihydropyrazolo[l,5-a]pyrimidine compounds of formula I, defined herein, as WNT pathways modulators, processes for making them, and pharmaceutical compositions comprising them. Methods of treatment of conditions mediated by WNT pathway signalling including cancer, fibrosis, stem cell and diabetic retinopathy, rheumatoid arthritis, psoriasis and myocardial infarction, comprising the compounds of formula I are also provided.
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Paragraph 0301; 0302; 0311; 0312
(2015/07/07)
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- Trimethoxybenzanilide-based P-glycoprotein modulators: An interesting case of lipophilicity tuning by intramolecular hydrogen bonding
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One of the principal reasons for the chemotherapy failure is the overexpression of drug efflux pumps, ABCB1 (also known as MDR1 or P-gp) and ABCC1 (also known as MRP1), whose inhibition remains a priority to circumvent drug resistance. We have recently sh
- Tardia, Piero,Stefanachi, Angela,Niso, Mauro,Stolfa, Diana Antonella,Mangiatordi, Giuseppe Felice,Alberga, Domenico,Nicolotti, Orazio,Lattanzi, Gianluca,Carotti, Angelo,Leonetti, Francesco,Perrone, Roberto,Berardi, Francesco,Azzariti, Amalia,Colabufo, Nicola Antonio,Cellamare, Saverio
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p. 6403 - 6418
(2014/10/16)
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- Tetraphosphine/palladium-catalyzed Suzuki-Miyaura coupling of heteroaryl halides with 3-pyridine- and 3-thiopheneboronic acid: An efficient catalyst for the formation of biheteroaryls
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An easily prepared tetraphosphine N,N,N′,N′- tetra(diphenylphosphinomethyl)-1,2-ethylenediamine (L1) associated with [Pd(η3-C3H5)Cl]2 affords an efficient catalyst for Suzuki-Miyaura coupling of 3-pyridineboronic acid with heteroaryl bromides. Reaction could be performed with as little as 0.02 mol% catalyst and a high turnover number of 2500 is obtained. A wide range of substrates is investigated with satisfactory yields, and good compatibility with aminogroup-substituted pyridines and unprotected indole is exhibited. This protocol can also be applied successfully to the reaction of heteroaryl bromides with 3-thiopheneboronic acid. This Pd-tetraphosphine catalyst efficiently restrains the poisoning effect from heteroaryls, and shows good stability and longevity. Copyright 2013 John Wiley & Sons, Ltd. An easily prepared tetraphosphine L1 was successfully used in Pd catalyzed Suzuki reaction of heteroaryl bromides with 3-pyridineboronic acid. A high turnover number of 2 500 was achieved and a wide range of heteroaryl halides including aminopyridines and indole was tolerated. With this protocol the coupling of 3-thiopheneboronic acid with heteroaryl bromides could also proceed in good yields. This catalyst system efficiently restrained poisoning effect from heteroaryls, and exhibited good stability and longevity. Copyright
- Wang, Kun,Fu, Qi,Zhou, Rong,Zheng, Xueli,Fu, Haiyan,Chen, Hua,Li, Ruixiang
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p. 232 - 238
(2013/05/08)
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- Spiro Compounds As NPY Y5 Receptor Antagonists
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The present invention relates to novel compounds of formula (I), or a pharmaceutically acceptable salt thereof, wherein R is an aryl or heteroaryl, which may be substituted by one or more: halogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, cyano;Z1 is H, C1-C4 alkyl or F;Z is CH2, CH(C1-C4 alkyl), C(C1-C4 alkyl)2 or a bond;A is a 6-10 membered aryl or heteroaryl, which may be substituted by one or more: halogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, cyano; or —C(═O)—X; or —O(CH2)0-1R1;B is hydrogen or is a 5-6 membered heteroaryl, or a 4-6 membered heterocycle, or phenyl, which may be substituted by one or more: halogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, hydroxyl, cyano; A and B being linked via any atom;R1 is —(C1-C4)alkyl(C1-C4)alkoxy; or C3-C8 cycloalkyl; or R1 is an aryl or heteroaryl, which may be substituted by one or more: halogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, cyano; or R1 is a 4-6 membered heterocycle, which may be substituted by one or more: halogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, cyano;X is OR2 or NR3R4;R2 is C1-C4 alkyl;R3 is hydrogen or together with R4 and the nitrogen form a 5-6 saturated membered ring;R4 is C3-C8 cycloalkyl; processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as NPY Y5 receptor antagonists and as agents for the treatment and/or prophylaxis of eating disorders such as a binge eating disorder.
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Page/Page column 51
(2009/08/18)
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- DNA gyrase (GyrB)/topoisomerase IV (ParE) inhibitors: Synthesis and antibacterial activity
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The synthesis and antibacterial activities of three chemotypes of DNA supercoiling inhibitors based on imidazolo[1,2-a]pyridine and [1,2,4]triazolo[1,5-a]pyridine scaffolds that target the ATPase subunits of DNA gyrase and topoisomerase IV (GyrB/ParE) is reported. The most potent scaffold was selected for optimization leading to a series with potent Gram-positive antibacterial activity and a low resistance frequency.
- East, Stephen P.,White, Clara Bantry,Barker, Oliver,Barker, Stephanie,Bennett, James,Brown, David,Boyd, E. Andrew,Brennan, Christopher,Chowdhury, Chandana,Collins, Ian,Convers-Reignier, Emmanuelle,Dymock, Brian W.,Fletcher, Rowena,Haydon, David J.,Gardiner, Mihaly,Hatcher, Stuart,Ingram, Peter,Lancett, Paul,Mortenson, Paul,Papadopoulos, Konstantinos,Smee, Carol,Thomaides-Brears, Helena B.,Tye, Heather,Workman, James,Czaplewski, Lloyd G.
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scheme or table
p. 894 - 899
(2009/08/15)
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- Highly efficient monophosphine-based catalyst for the palladium-catalyzed Suzuki-Miyaura reaction of heteroaryl halides and heteroaryl boronic acids and esters
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A highly active and efficient catalyst system derived from a palladium precatalyst and monophosphine ligands 1 or 2 for the Suzuki-Miyaura cross-coupling reaction of heteroaryl boronic acids and esters has been developed. This method allows for the preparation of a wide variety of heterobiaryls in good to excellent yields and displays a high level of activity for the coupling of heteroaryl chlorides as well as hindered aryl and heteroaryl halides. Specific factors that govern the efficacy of the transformation for certain heterocyclic motifs were also investigated.
- Billingsley, Kelvin,Buchwald, Stephen L.
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p. 3358 - 3366
(2007/10/03)
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- A highly active catalyst for Suzuki-Miyaura cross-coupling reactions of heteroaryl compounds
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(Chemical Equation Presented) Unprecedented activity: Catalysts derived from Pd and bulky dialkylphosphinobiaryl ligands are shown to be highly stable and active in Suzuki-Miyaura reactions of heteroaryl halides and heteroaryl boronic acids/esters (e.g., 3-or 4-pyridine, indole, and N-protected pyrrole derivatives). Furthermore, this catalyst system is not inhibited by the presence of highly basic aminopyridines or aminopyrimidines.
- Billingsley, Kelvin L.,Anderson, Kevin W.,Buchwald, Stephen L.
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p. 3484 - 3488
(2007/10/03)
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- Polycyclic thiazoles as potassium ion channel modulators
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The present invention provides a genus of polycyclic thiazoles that are useful as modulators of potassium ion channels. The modulators of the invention are of use in both therapeutic and diagnostic methods.
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Page/Page column 13
(2008/06/13)
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- POLYCYCLIC PYRIMIDINES AS POTASSIUM ION CHANNEL MODULATORS
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The present invention provides a genus of polycyclic pyrimidines that are useful as modulators of potassium ion channels. The modulators of the invention are of use in both therapeutic and diagnostic methods.
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Page/Page column 13
(2008/06/13)
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- POLYCYCLIC PYRIDINES AS POTASSIUM ION CHANNEL MODULATORS
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The present invention provides a genus of polycyclic pyridines that are useful as modulators of potassium ion channels. The modulators of the invention are of use in both therapeutic and diagnostic methods.
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Page/Page column 44
(2010/02/14)
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- Polycyclic pyrazines as potassium ion channel modulators
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The present invention provides a genus of polycyclic pyrazines that are useful as modulators of potassium ion channels. The modulators of the invention are of use in both therapeutic and diagnostic methods.
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Page/Page column 17
(2010/02/14)
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