- Synthesis, characterization and dynamic behavior of (π-allyl)palladium complexes with polydentate nitrogen ligands, evidence of a dissociative mechanism
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New examples of the fluxional behavior of (η3-allyl)palladium complexes are described. Variable-temperature experiments and line-shape analysis of two (η3-allyl)palladium complexes containing 2-(1H-pyrazol-1-yl)azine ligands were performed in order to determine the activation free energies, enthalpies and entropies of the process. A dissociative mechanism pointing to a selective Pd-N cleavage is proposed on the basis of these results and NOE experiments above and below the coalescence temperature. VCH Verlagsgesellschaft mbH, 1996.
- Elguero, Jose,Fruchier, Alain,De La Hoz, Antonio,Jalon, Felix A.,Manzao, Blanca R.,Oteroo, Antonio,Torre, Felipe Gomez-De La
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Read Online
- A four-coordinate Cu(I)–N-heterocyclic carbene complex: Synthesis, structure, properties, and application in amination for the synthesis of 1-(2-N-heteroaryl)-1H-pyrazoles
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A new luminescent, cationic, heteroleptic, four-coordinate Cu(I)–N-heterocyclic carbene complex [Cu(Br-Pyim)(POP)](PF6) is successfully prepared and characterized, where Br-Pyim and POP are 1-(6-bromopyridin-2-yl)imidazole-3-benzyl-2-ylidene an
- Xu, Chen,Li, Hong-Mei,Wang, Zhi-Qiang,Fu, Wei-Jun
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p. 689 - 694
(2020/06/01)
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- CALPAIN MODULATORS AND THERAPEUTIC USES THEREOF
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Disclosed herein are small molecule calpain modulator compositions, pharmaceutical compositions, the use and preparation thereof.
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Paragraph 1477
(2018/04/17)
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- THERAPEUTICALLY ACTIVE COMPOUNDS AND THEIR METHODS OF USE
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Provided are methods of treating a cancer characterized by the presence of a mutant allele of IDH1/2 comprising administering to a subject in need thereof a compound described here.
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(2015/03/31)
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- Imidazopyridazines as potent inhibitors of Plasmodium falciparum calcium-dependent protein kinase 1 (PfCDPK1): Preparation and evaluation of pyrazole linked analogues
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The structural diversity and SAR in a series of imidazopyridazine inhibitors of Plasmodium falciparum calcium dependent protein kinase 1 (PfCDPK1) has been explored and extended. The opportunity to further improve key ADME parameters by means of lowering log D was identified, and this was achieved by replacement of a six-membered (hetero)aromatic linker with a pyrazole. A short SAR study has delivered key examples with useful in vitro activity and ADME profiles, good selectivity against a human kinase panel and improved levels of lipophilic ligand efficiency. These new analogues thus provide a credible additional route to further development of the series.
- Large, Jonathan M.,Osborne, Simon A.,Smiljanic-Hurley, Ela,Ansell, Keith H.,Jones, Hayley M.,Taylor, Debra L.,Clough, Barbara,Green, Judith L.,Holder, Anthony A.
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p. 6019 - 6024
(2013/10/22)
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- THERAPEUTICALLY ACTIVE COMPOUNDS AND THEIR METHODS OF USE
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Provided are methods of treating a cancer characterized by the presence of a mutant allele of IDH1/2 comprising administering to a subject in need thereof a compound described here.
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Page/Page column 111
(2013/07/31)
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- Synthesis, X-ray characterization and computational Studies of N-imidazolyl and N-pyrazolyl pyrimidine derivatives
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In this manuscript we report the synthesis and X-ray characterization of neutral 2-(1H-imidazol-1-yl)-pyrimidine (1), 2-(1H-pyrazol-1-yl)-pyrimidine (2) and 1-(2-pyrimidinyl)-1H-benzimidazole (3). We have also obtained crystals of the corresponding hydrochlorides of compounds 1 and 3. Finally, the outer sphere complex of protonated 2-(1H-imidazol-1-yl)-pyrimidine with [CoCl 4]2- as counterion is described. In several charged structures interesting anion-π interactions determine the crystal packing. Moreover, in neutral systems some stacking interactions are governed by double lone pair-π interactions. High level ab initio calculations (RI-MP2/def2-TZVP) have been used to evaluate the noncovalent interactions observed in the solid state and the interplay between them.
- Torres, Marta,Ca?ellas, Pablo,Estarellas, Carolina,García-Raso, Angel,Fiol, Juan J.,Albertí, Francisca M.,Frontera, Antonio,Molins, Elies,Mata, Ignasi,Deyà, Pere M.
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experimental part
p. 2374 - 2382
(2012/04/17)
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- N-aryl pyrazoles: DFT calculations of CH acidity and deprotonative metallation using a combination of lithium and zinc amides
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A series of N-aryl and N-heteroaryl pyrazoles have been deproto-metallated using a 2,2,6,6-tetramethylpiperidino-based mixed lithium-zinc combination. Mono-, di-, and tri-iodides have been obtained after subsequent trapping with iodine, depending on the s
- Chevallier, Floris,Halauko, Yury S.,Pecceu, Christelle,Nassar, Ibrahim F.,Dam, To Uyen,Roisnel, Thierry,Matulis, Vadim E.,Ivashkevich, Oleg A.,Mongin, Florence
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scheme or table
p. 4671 - 4684
(2011/07/07)
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- Direct, metal-free amination of heterocyclic amides/ureas with NH-heterocycles and N-substituted anilines in POCl3
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A POCl3-mediated, direct amination reaction of heterocyclic amides/ureas with NH-heterocycles or N-substituted anilines is described. Compared to the existing methods, this operationally simple protocol provides unique reactivity and functional
- Deng, Xiaohu,Roessler, Armin,Brdar, Ivana,Faessler, Roger,Wu, Jiejun,Sales, Zachary S.,Mani, Neelakandha S.
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experimental part
p. 8262 - 8269
(2011/12/04)
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- HETEROCYCLIC COMPOUNDS AND USE THEREOF AS ERK INHIBITORS
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Disclosed are the ERK inhibitors of formula 1.0: [Formula (1.0)] and the pharmaceutically acceptable salts, esters and solvates thereof. Q is a piperidine or piperazine ring that can have a bridge or a fused ring. The piperidine ring can have a double bond in the ring. All other substitutents are as defined herein. Also disclosed are methods of treating cancer using the compounds of formula 1.0.
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Page/Page column 252
(2009/01/23)
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- POLYCYCLIC INDAZOLE DERIVATIVES AND THEIR USE AS ERK INHIBITORS FOR THE TREATMENT OF CANCER
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Disclosed are the ERK inhibitors of formula 1.0: (Chemical formula should be inserted here as it appears on abstract in paper form) and the pharmaceutically acceptable salts, esters and solvates thereof. Q is a piperidine or piperazine ring that can have a bridge or a fused ring. The piperidine ring can have a double bond in the ring. All other substitutents are as defined herein. Also disclosed are methods of treating cancer using the compounds of formula 1.0.
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Page/Page column 262
(2009/01/24)
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- Efficient nucleophilic substitution reactions of pyrimidyl and pyrazyl halides with nucleophiles under focused microwave irradiation
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Rapid nucleophilic displacement reactions of 2-chloropyrimidine, 2-bromopyrimidine, 5-bromopyrimidine and chloropyrazine with nucleophiles under microwave irradiation was complete within several minutes with yields up to 99%. The method using microwave irradiation is superior to the classical heating processes.
- Cherng, Yie-Jia
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p. 887 - 890
(2007/10/03)
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- Synthesis and cytoprotective antiulcer activity of 2- or 4-(1H-pyrazol- 1-yl)pyrimidine derivatives related to mepirizole and dulcerozine
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(1H-Pyrazol-1-yl)-, (1H-imidazol-1-yl)-, and (1H-1,2,4-triazol-1- yl)pyrimidines were prepared and evaluated for cytoprotective antiulcer activity. Among them, 4-methoxy-6-methyl-2-(1H-pyrazol-1-yl)pyrimidine (18) showed potent inhibition of the HCl-ethanol-induced and water-immersion stress-induced ulcers in rats, as well as low acute toxicity.
- Ikeda, Masazumi,Maruyama, Kazumi,Nobuhara, Youichi,Yamada, Toshihiro,Okabe, Susumu
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p. 1700 - 1706
(2007/10/03)
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- SYNTHESES OF NEW PYRAZOLE-DERIVED CHELATING LIGANDS
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The preparations and spectral data for nine new N,N'-chelating ligands (5)-(13), each consisting of a pyrazole group N-linked to an azine or azole, are described.
- Steel, Peter J.,Constable, Edwin C.
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p. 1601 - 1611
(2007/10/02)
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