- S-triazine compounds as well as preparation method and application thereof
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The invention discloses s-triazine compounds and pharmaceutically acceptable salts thereof; experiments prove that the compounds can be used for treating or preventing diseases related to protein kinase activity, such as leukemia and lymphoma, by inhibiti
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Paragraph 0104-0106
(2020/05/05)
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- Synthesis method of 3-(4-nitrophenyl)pyridine
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The invention relates to a synthesis method of 3-(4-nitrophenyl)pyridine. The synthesis method of the 3-(4-nitrophenyl)pyridine comprises the following steps: S1, under the protection of inert gas, mixing 4-nitrophenylboronic acid, 3-chloropyridine, n-het
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Paragraph 0027; 0028; 0029; 0030; 0031; 0032; 0033-0113
(2019/02/04)
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- Synthesis method of S-3-(4-aminophenyl) piperidine
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The invention relates to a synthesis method of S-3-(4-aminophenyl) piperidine. The synthetic method of the S-3-(4-aminophenyl) piperidine includes the following steps: taking 3-pyridineboronic acid (I) as a raw material, and preforming Suzuki coupling wit
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Paragraph 0058; 0084; 0098; 0111; 0112; 0126; 0140
(2019/01/23)
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- Synthesis of Bi(hetero)aryls via Sequential Oxidation and Decarboxylation of Benzylamines in a Batch/Fully Automated Continuous Flow Process
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Catalytic dehydrogenative cross-coupling of two C–H bonds represents a green strategy in view of the atom- and step-economy. However, the challenge is to discover a new innovative bond strategy, especially for the direct coupling between Csp2–H
- Mahajan, Bhushan,Aand, Dnyaneshwar,Singh, Ajay K.
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supporting information
p. 2831 - 2835
(2018/06/21)
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- Design, synthesis, and evaluation of potent Wnt signaling inhibitors featuring a fused 3-ring system
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The Wnt signaling pathway is a critical developmental pathway which operates through control of cellular functions such as proliferation and differentiation. Aberrant Wnt signaling has been linked to the formation and metastasis of tumors. Porcupine, a member of the membrane-bound O-acyltransferase family of proteins, is an important component of the Wnt pathway. Porcupine catalyzes the palmitoylation of Wnt proteins, a process needed for their secretion and activity. Here we report a novel series of compounds obtained by a scaffold hybridization strategy from a known porcupine inhibitor class. The leading compound 59 demonstrated subnanomolar inhibition of Wnt signaling in a paracrine cellular assay. Compound 59 also showed excellent chemical, plasma and liver microsomal stabilities. Furthermore, compound 59 exhibited good pharmacokinetic profiles with 30% oral bioavailability in rat. Collectively, these results strongly support further optimization of this novel scaffold to develop better Wnt pathway inhibitors.
- Xu, Zhixiang,Li, Jiajun,Wu, Yiyuan,Sun, Zhijian,Luo, Lusong,Hu, Zhilin,He, Sudan,Zheng, Jiyue,Zhang, Hongjian,Zhang, Xiaohu
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p. 154 - 165
(2015/12/04)
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- NOVEL NAPHTHOTRIAZOLE DERIVATIVE AND ORGANIC ELECTROLUMINESCENCE ELEMENT
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Naphthotriazole derivatives represented by the following general formula (1), wherein, Ar 1 is an aromatic hydrocarbon group or an aromatic heterocyclic group, and A is a group that contains an aromatic heterocyclic group. The compound features excellent electron injection/transporting capability, a high hole-blocking power and a high stability in the form of a thin film, and can be used as a material for producing highly efficient and highly durable organic electroluminescent devices.
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Paragraph 0398-0410
(2016/11/17)
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- FAK AND FLT3 INHIBITORS
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The use of a compound of the formula (I): (Formula (I)) in the preparation of a medicament for treating Acute Myeloid Leukemia or a disease ameliorated by the inhibition of Flt3, or Flt3 and FAK.
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Page/Page column 67
(2014/03/22)
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- NEW BENZOTRIAZOLE DERIVATIVE AND ORGANIC ELECTROLUMINESCENT ELEMENT IN WHICH SAID DERIVATIVE IS USED
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Benzotriazole derivatives represented by the following general formula (1), wherein Ar1 and Ar2 are, for example, aromatic hydrocarbon groups or aromatic heterocyclic ring groups, and A is a group including a pyridine ring. The compounds excel in electron injection/transport capability, feature a high hole-blocking power and a high stability in their thin-film form, and are useful as materials for producing highly efficient and highly durable organic electroluminescent devices.
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Paragraph 0092
(2014/09/02)
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- PYRAZINE KINASE INHIBITORS
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Provided are pyrazine compounds for inhibiting of Syk kinase, intermediates used in making such compounds, methods for their preparation, pharmaceutical compositions thereof, methods for inhibition Syk kinase activity, and methods for treating conditions mediated at least in part by Syk kinase activity.
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Paragraph 0370
(2013/06/04)
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- Facile synthesis of 3-arylpyridine derivatives by palladacycle-catalyzed Stille cross-coupling reaction
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The Stille cross-coupling reaction of a variety of aryl halides (X=Cl, Br, I) with 3-alkylstannylpyridines highly catalyzed by cyclopalladated ferrocenylimine has been developed. This reaction allows formation of arylpyridine derivatives in moderate to excellent yields. Functional groups on aryl halides, such as amino, hydroxyl, keto, and aldehyde are tolerated and the reactions with arylbenzoxale substrates also proceed well.
- Ma, Gaizhi,Leng, Yuting,Wu, Yusheng,Wu, Yangjie
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p. 902 - 909
(2013/07/25)
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- NAPHTHALENE DERIVATIVE
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The present invention provides compounds which can regulate VCP activity. The present invention provides the compound of formula (I) (R is as defined in the description) or oxides, esters, prodrugs, pharmaceutically acceptable salts or solvates thereof. The compounds can regulate VCP activity, and thus are useful for treating VCP-mediated diseases such as neurodegenerative diseases.
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Paragraph 0572
(2013/06/27)
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- FAK INHIBITORS
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A compound of the formula (I): where R1 or R2 is a cycle amine group and R5 is an aromatic group with a carbonyl containing substituent for use as a FAK inhibitor.
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Page/Page column 65
(2012/09/10)
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- Synthesis, crystal structures, and catalytic activities of palladium imidazole complexes formed by 2-hydroxyethyl group cleavage
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N-4,6-dimethyl-2-pyrimidinylimidazole 1 and its hydroxyethyl derivative 1-(2-hydroxyethyl)-3-(4,6-dimethyl-2-pyrimidinyl)imidazolium chloride 2 have been synthesized and characterized. The attempted synthesis of bis(N-heterocyclic carbene)palladium complexes via the direct reaction of 2 with Pd(OAc)2 results in the unexpected formation of a bis(N-arylimidazole) palladium complex 3. Additionally, the analogous bis(N-methylimidazole) palladium complex 4 has also been synthesized by the above method. Compounds 1-4 were characterized by elemental analysis, IR, and 1H NMR. Additionally, their crystal structures have been determined by X-ray diffraction. Complexes 3 and 4 were found to be efficient catalysts for the Suzuki reaction.
- Xu, Chen,Li, Zhen,Duan, Lu-Meng,Wang, Zhi-Qiang,Fu, Wei-Jun,Hao, Xin-Qi,Song, Mao-Ping
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supporting information; experimental part
p. 373 - 378
(2012/07/31)
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- Development of a fit-for-purpose large-scale synthesis of an oral PARP inhibitor
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Compound (1) a poly(ADP-ribose)polymerase (PARP) inhibitor has been made by a fit-for-purpose large-scale synthesis using either a classical resolution or chiral chromatographic separation. The development and relative merits of each route are discussed,
- Wallace, Debra J.,Baxter, Carl A.,Brands, Karel J. M.,Bremeyer, Nadine,Brewer, Sarah E.,Desmond, Richard,Emerson, Khateeta M.,Foley, Jennifer,Fernandez, Paul,Hu, Weifeng,Keen, Stephen P.,Mullens, Peter,Muzzio, Daniel,Sajonz, Peter,Tan, Lushi,Wilson, Robert D.,Zhou, George,Zhou, Guoyue
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experimental part
p. 831 - 840
(2012/07/03)
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- Theramutein modulators
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This invention relates to agents that are inhibitors or activators of variant forms of endogenous proteins and novel methods of identifying such variants. Of particular interest are inhibitors and activators of endogenous protein variants, encoded by genes which have mutated, which variants often arise or are at least first identified as having arisen following exposure to a chemical agent which is known to be an inhibitor or activator of the corresponding unmutated endogenous protein.
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Page/Page column 174-175
(2010/02/17)
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- Discovery of 2-{4-[(3S)-piperidin-3-yl]phenyl}-2H-indazole-7-carboxamide (MK-4827): A novel oral poly(ADP-ribose)polymerase (PARP) inhibitor efficacious in BRCA-1 and -2 mutant tumors
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We disclose the development of a novel series of 2-phenyl-2H-indazole-7- carboxamides as poly(ADP-ribose) polymerase (PARP) 1 and 2 inhibitors. This series was optimized to improve enzyme and cellular activity, and the resulting PARP inhibitors display antiproliferation activities against BRCA-1 and BRCA-2 deficient cancer cells, with high selectivity over BRCA proficient cells. Extrahepatic oxidation by CYP450 1A1 and 1A2 was identified as a metabolic concern, and strategies to improve pharmacokinetic properties are reported. These efforts culminated in the identification of 2-{4-[(3S)-piperidin-3-yl] phenyl}-2H-indazole-7-carboxamide 56 (MK-4827), which displays good pharmacokinetic properties and is currently in phase I clinical trials. This compound displays excellent PARP 1 and 2 inhibition with IC50 = 3.8 and 2.1 nM, respectively, and in a whole cell assay, it inhibited PARP activity with EC50 = 4 nM and inhibited proliferation of cancer cells with mutant BRCA-1 and BRCA-2 with CC50 in the 10-100 nM range. Compound 56 was well tolerated in vivo and demonstrated efficacy as a single agent in a xenograft model of BRCA-1 deficient cancer.
- Jones, Philip,Altamura, Sergio,Boueres, Julia,Ferrigno, Federica,Fonsi, Massimiliano,Giomini, Claudia,Lamartina, Stefania,Monteagudo, Edith,Ontoria, Jesus M.,Orsale, Maria Vittoria,Palumbi, Maria Cecilia,Pesci, Silvia,Roscilli, Giuseppe,Scarpelli, Rita,Schultz-Fademrecht, Carsten,Toniatti, Carlo,Rowley, Michael
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experimental part
p. 7170 - 7185
(2010/07/04)
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- Efficient diphosphane-based catalyst for the palladium-catalyzed suzuki cross-coupling reaction of 3-pyridylboronic acids
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A highly active catalyst system derived from PdCl2 and 2,2',6,6'- tetramethoxy-4,4'-bis(diphenylphosphanyl)-3,3'-bi- pyridine (P-Phos) has been developed for the Suzuki cross- coupling reaction of pyridylboronic acid with a variety of aryl halides in good to excellent yields, even in the presence of hindered and functional groups. In addition, P-Phos also exhibited high activity in the palladium-catalyzed Suzuki reaction of 2,6-dimethoxypyridylboronic acid in excellent yields with a fast rate. The steric and electronic effects of the P- Phos-palladium complex to this cross-coupling reaction were also discussed.
- Fu, Xing-Li,Wu, Lei-Lei,Fu, Hai-Yan,Chen, Hua,Li, Rui-Xiang
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experimental part
p. 2051 - 2054
(2009/09/06)
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- THERAMUTEIN MODULATORS
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This invention relates to agents that are inhibitors or activators of variant forms of endogenous proteins and novel methods of identifying such variants. Of particular interest are inhibitors and activators of endogenous protein variants, encoded by genes which have mutated, which variants often arise or are at least first identified as having arisen following exposure to a chemical agent which is known to be an inhibitor or activator of the corresponding unmutated endogenous protein.
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Page/Page column 207
(2008/12/07)
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- Highly efficient cyclopalladated ferrocenylimine catalyst for Suzuki cross-coupling reaction of 3-pyridylboronic pinacol ester with aryl halides
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The Suzuki cross-coupling reaction of 3-pyridylboronic pinacol ester with aryl iodides, bromides and chlorides was carried out in DMF/H2O (3/1, v/v) at 110 °C in the presence of cyclopalladated ferrocenylimine I and K2CO3 or CsCO3 (1.0 equiv.) without the protection of inert gas. By using this method the synthesis of 3-pyridyl biaryl compounds could be readily achieved.
- Zhang, Jinli,Zhao, Liang,Song, Maoping,Mak, Thomas C.W.,Wu, Yangjie
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p. 1301 - 1306
(2007/10/03)
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- NOVEL COMPOUNDS
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The present invention relates to novel pyridone derivatives capable of inhibiting a4 integrin medicated cell adhesion, processes for their preparation, compositions comprising them and their use in the treatment of diseases capable of being modulated by t
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- C-H Activation and Palladium Migration within Biaryls under Heck Reaction Conditions
-
(Equation Presented) Biaryl bromides such as 1 (R=NO2, H, OMe) undergo the Heck reaction to give both the expected products 3 ("retention") as well as "crossover" products 4 derived from a migration of Pd and net transfer of reactivity from one
- Karig, Gunter,Moon, Maria-Teresa,Thasana, Nopporn,Gallagher, Timothy
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p. 3115 - 3118
(2007/10/03)
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- STEROID RECEPTOR MODULATOR COMPOUNDS AND METHODS
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Non-steroidal compounds which are high affinity, high selectivity modulators for steroid receptors are disclosed. Also disclosed are pharmaceutical compositions incorporating such compounds, methods for employing the disclosed compounds and compositions for treating patients requiring steroid receptor agonist or antagonist therapy, intermediates useful in the preparation of the compounds and processes for the preparation of the steroid receptor modulator compounds.
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- STEROID RECEPTOR MODULATOR COMPOUNDS AND METHODS
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Non-steroidal compounds which are high affinity, high selectivity modulators for steroid receptors are disclosed. Also disclosed are pharmaceutical compositions incorporating such compounds, methods for employing the disclosed compounds and compositions for treating patients requiring steroid receptor agonist or antagonist therapy, intermediates useful in the preparation of the compounds and processes for the preparation of the steroid receptor modulator compounds.
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- N-Arylation of Pyridine with Diazonium Salts
-
N-Arylation of pyridine with arenediazonium salts have been accomplished. 2,7-Dioxo-2,3-dihydro-7H-dibenzisoquinoline-1- and 2-methyl-6-oxo-2,6-dihydronaphthindole-1-diazonium salts have been converted into respectively N-substituted pyridines in quantitative yields.With 2,4-dinitrobenzenediazonium salts as an example, the reaction was shown to be of general character.Strong electron-acceptor properties of the arene residue in the diazo cation are necessary for the reaction to occur, since 4-nitrobenzenediazonium salts react to only a minor extent and benzenediazonium salts give no N-arylation products at all.
- Kazankov, M. V.,Makshanova, N. P.,Sadovykh, E. G.
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p. 414 - 417
(2007/10/03)
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- 6-(1H-imidazol-1-yl)-7-nitro-2,3 (1H,4H)-quinoxalinedione hydrochloride (YM90K) and related compounds: Structure-activity relationships for the AMPA- type non-NMDA receptor
-
A novel series of quinoxalinediones possessing imidazolyl and related heteroaromatic substituents was synthesized and evaluated for their activity to inhibit [3H]AMPA binding from rat whole brain. From the structure- activity relationships, it was found that the 1H-imidazol-1-yl moiety could function as a bioisostere for the cyano and nitro groups, and that 6-(1H- imidazol-yl)-7-nitro-2,3(1H,4H)-quinoxalinedione (11) showed the most potent activity for the AMPA receptor. Compound 11 was evaluated for selectivity versus other excitatory amino acid receptors, and its action against AMPA at its receptor in the rat striatum was characterized. These data showed that compound 11 was a selective antagonist for the AMPA receptor with a K(i) value of 0.084 μM, being approximately equipotent with 2,3-dihydro-6-nitro- 7-sulfamoylbenzo(f)quinoxaline (3) (NBQX; K(i) = 0.060 μM). Compound 11 was also found to give protection against sound-induced seizure on DBA/2 mice at the minimum effective dose of 3 mg/kg ip (3; 10 mg/kg ip).
- Ohmori,Sakamoto,Kubota,Shimizu-Sasamata,Okada,Kawasaki,Hidaka,Togami,Furuya,Murase
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p. 467 - 475
(2007/10/02)
-
- Cross-Coupling Reaction of Alkyl- or Arylboronic Acid Esters with Organic Halides Induced by Thallium(I) Salts and Palladium-Catalyst
-
The cross-coupling reaction of alkylboronic acid esters with 1-alkenyl- or aryl halides is succesfully catalyzed by PdCl2 (dppf) or Pd(PPh3)4 in the presence of thallium(I) hydroxide or carbonate to give the corresponding alkenes or arenes in good yields.The coupling reaction of arylboronic acid esters with aryl halides under similar conditions to provide biaryls is also described.
- Sato, Makoto,Miyaura, Norio,Suzuki, Akira
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p. 1405 - 1408
(2007/10/02)
-
- Pyridyl-substituted-benzofurans
-
The present invention provides novel pyridinyl-benzofurans and derivatives thereof which are useful as thromboxane A2 (TXA2) synthetase inhibitors and as such represent potent pharmacological agents.
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-
-
- The Reactions of Superoxide Ion with Arylhydrazines
-
Arylhydrazines react with potassium superoxide to give a variety of products, most of which are derived from interaction of aryl radicals with the solvent.Phenylhydrazine in toluene gives three isomeric metylbiphenyls, diphenylmethane and bibenzyl.In pyridine, the products identified were 2-, 3-, and 4-phenylpyridine.A more complex range of products was obtained from substituted phenylhydrazines.Products are consistent with a process in which superoxide ion abstracts hydrogen atoms from the hydrazines giving radical intermediates, including aryl radicals, which react with the solvents.
- Crank, George,Gately, Garry E.,Makin, Mohammad I. H.
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p. 2499 - 2507
(2007/10/02)
-
- A CONVENIENT SYNTHESIS OF 3-ARYLPYRIDINES BY THE PALLADIUM CATALYZED COUPLING REACTION OF DIETHYL(3-PYRIDYL)BORANE WITH ARYL HALIDES
-
The utilization of heteroarylborane to the preparation of a variety of 3-arylpyridines by the palladium catalyzed cross coupling reaction between diethyl(3-pyridyl)borane and aryl halides in the presence of bases is described.
- Ishikura, Minoru,Kamada, Machiko,Terashima, Masanao
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p. 265 - 268
(2007/10/02)
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- PROPERTIES OF THE LIQUID CRYSTALS FORMED BY CERTAIN 4-(2 prime -PYRIDYL)PHENYL AND 4-(4 prime -PYRIDYL)PHENYL 4 double prime -N-ALKOXYBENZOATES.
-
Nine members of each of two homologous series of esters, the 4-(2 prime -pyridyl)phenyl and the 4-(4 prime -pyridyl)phenyl 4 double prime -n-alkoxybenzoates, were prepared and their liquid crystal transition temperatures measured. Both homologous series w
- Byron,Lacey,Wilson
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p. 103 - 114
(2007/10/02)
-