- Metal-ion sensing europium(III) complexes with bidentate phosphine oxide ligands containing a 2,2′-bipyridine framework
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Novel EuIII complexes with bidentate phosphine oxide ligands containing a bipyridine framework, i.e., [3,3′-bis(diphenylphosphoryl)-2, 2′-bipyridine]tris(hexafluoroacetylacetonato)europium(III) ([Eu-(hfa) 3(BIPYPO)]) and [3,3′-bis(diphenylphosphoryl)-6,6′- dimethyl-2,2′-bipyridine]tris(hexafluoroacetylacetonato)europium(III) ([Eu(hfa)3(Me-BIPYPO)]), were synthesized for lanthanide-based sensor materials having high emission quantum yields and effective chemosensing properties. The emission quantum yields of [Eu(hfa)3(BIPYPO)] and [Eu(hfa)3(Me-BIPYPO)] were 71 and 73%, respectively. Metal-ion sensing properties of the EuIII complexes were also studied by measuring the emission spectra of EuIII complexes in the presence of ZnII or CuII ions. The metal-ion sensing and the photophysical properties of luminescent EuIII complexes with a bidentate phosphine oxide containing 2,2′-bipyridine framework are demonstrated for the first time.
- Hasegawa, Yasuchika,Hieda, Ryo,Nakagawa, Tetsuya,Kawai, Tsuyoshi
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- FUSED HETEROCYCLIC DERIVATIVES, THEIR PREPARATION METHODS THEREOF AND MEDICAL USES THEREOF
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The present invention relates to fused heterocyclic derivatives, processes for their preparation and their use in medicine. Specifically, the present invention relates to a novel derivative represented by the formula (I′), or its pharmaceutically acceptable salt thereof, a pharmaceutical composition containing the derivative or its pharmaceutically acceptable salt thereof, and the method for preparing the derivative and its pharmaceutically acceptable salt thereof. The present invention also relates to the use of the derivative and its pharmaceutically acceptable salt thereof, or a pharmaceutical composition containing the derivative and its pharmaceutically acceptable salt thereof in the preparation of medicines, in particularly as IDO inhibitor medicines, for treating and/or preventing cancers. Wherein each substituent of the formula (I′) is the same as defined in the specification.
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Paragraph 0246; 0252; 0395-0398
(2019/07/03)
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- ROR-GAMMA INHIBITORS
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The present invention relates to compounds of formula I and pharmaceutical compositions comprising compounds of formula I. Compounds of Formula I are useful in treatment of inflammatory, metabolic or autoimmune diseases which are mediated by RORy.
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Page/Page column 253-254
(2019/04/26)
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- HETEROCYCLIC COMPOUND AND PHARMACEUTICAL COMPOSITION COMPRISING SAME
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The invention relates to a novel heterocyclic compound inhibiting a cyclin-dependent kinase (CDK) and a pharmaceutical composition comprising the same as an effective ingredient. The heterocyclic compound according to the present invention or pharmaceutically acceptable salt thereof can be effectively used in treating or preventing cancers, degenerative brain diseases, etc.
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Paragraph 0122; 0123
(2018/01/11)
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- COMPOSITIONS AND USES OF AMIDINE DERIVATIVES
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Use of a compound of formula (I): wherein A, X, Y, R1 and R2 as defined herein, in treating hereditary angioedema is disclosed. A composition containing the compounds, a polar organic solvent or a mixture thereof; and optionally a co-solvent, is also disclosed.
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Page/Page column 147-148
(2016/03/14)
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- DI-MACROCYCLES
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The invention relates to chemical compounds and complexes that can be used in therapeutic and diagnostic applications.
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Paragraph 00201
(2014/06/11)
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- COMPOUNDS THAT MODULATE INTRACELLULAR CALCIUM
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Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combinatio
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Page/Page column 93
(2013/02/27)
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- PYRIDINYL- AND PYRAZINYL -METHYLOXY - ARYL DERIVATIVES USEFUL AS INHIBITORS OF SPLEEN TYROSINE KINASE (SYK)
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A compound of formula (I) or a salt thereof; which is an inhibitor of spleen tyrosine kinase (SYK) and therefore potentially of use in treating diseases resulting from inappropriate activation of mast cells, macrophages, and B-cells and related inflammato
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Page/Page column 43-44
(2012/10/07)
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- NOVEL COMPOUNDS
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A compound of formula (I): or a salt thereof; which is an inhibitor of spleen tyrosine kinase (SYK) and therefore potentially of use in treating diseases resulting from inappropriate activation of mast cells, macrophages, and B-cells and related inflammat
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Page/Page column 20-21
(2012/09/22)
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- INHIBITORS OF HIF AND ANGIOGENESIS
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Inhibitors of the Hypoxia Inducible Factor (HIF) and angiogenesis and their methods of use including the treatment of cancer, hypoxia related pathologies, disorders leading to ischemia, for example stroke and ischemic heart disease, and non-cancerous angiogenic diseases are provided.
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Page/Page column 62-63
(2011/11/06)
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- Design and synthesis of novel small-molecule inhibitors of the hypoxia inducible factor pathway
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Hypoxia, a reduction in partial oxygen pressure, is a salient property of solid tumors. Hypoxia drives malignant progression and metastasis in tumors and participates in tumor resistance to radio- and chemotherapies. Hypoxia activates the hypoxia-inducible factor (HIF) family of transcription factors, which induce target genes that regulate adaptive biological processes such as anaerobic metabolism, cell motility, and angiogenesis. Clinical evidence has demonstrated that expression of HIF-1 is strongly associated with poor patient prognosis and activation of HIF-1 contributes to malignant behavior and therapeutic resistance. Consequently, HIF-1 has become an important therapeutic target for inhibition by small molecules. Herein, we describe the design and synthesis of small molecules that inhibit the HIF-1 signaling pathway. Many of these compounds exhibit inhibitory activity in the nanomolar range. Separate mechanistic studies indicate that these inhibitors do not alter HIF-1 levels but interfere with the ability of HIF-1α/HIF-1β to interact with cofactors p300/CBP to form an active transcriptional complex. (Figure presented)
- Mooring, Suazette Reid,Jin, Hui,Devi, Narra S.,Jabbar, Adnan A.,Kaluz, Stefan,Liu, Yuan,Van Meir, Erwin G.,Wang, Binghe
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scheme or table
p. 8471 - 8489
(2012/02/03)
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- Efficient and fast Heck vinylation of 2-bromo-6-methyl pyridines with methylacrylate. Application to the synthesis of 6-methyl cyclopenta[b]pyridinone
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Heck vinylation of 2-bromo-6-methyl-3-substituted pyridines using η3-allylpalladium chloride dimer/P(o-Tol)3 complex/toluene and dimethylacetamide (DMA) as co-solvent with methyl acrylate is reported. Electronic and steric effects were investigated engaging diversely 2-bromo-3,6-disubstituted pyridines. As application, a new synthesis of the 6-methyl cyclopenta[b]pyridinone building-block connecting Heck vinylation, alkene reduction and Dieckmann condensation is described.
- Robert, Nicolas,Hoarau, Christophe,Célanire, Sylvain,Ribéreau, Pierre,Godard, Alain,Quéguiner, Guy,Marsais, Francis
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p. 4569 - 4576
(2007/10/03)
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- Efficient regioselective preparation of monobromo and bromoiodo hydroxy pyridines from dibromoderivatives via bromine-lithium exchange
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Annular dibromination of hydroxypyridines with NBS in acetonitrile followed by bromine-lithium exchange with RLi and subsequent trapping with H2O or I2 afforded monobromo and bromoiodo derivatives in a completely regioselective way. Iodination of bromo hydroxypyridines with NIS is totally regioselective.
- Meana, ángela,Rodríguez, Justo F.,Sanz-Tejedor, M. Ascensión,García-Ruano, José L.
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p. 1678 - 1682
(2007/10/03)
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- Oxime derivatives for the treatment of dyslipidemia and hypercholesteremia
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The present invention relates to compounds of Formula (I) which may be useful in the treatment of diseases, such as, metabolic disorders, dyslipidemia and/or hyperchloesterolemia: 1
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- Heterocyclic derivatives for the treatment of diabetes and other diseases
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The present invention relates to certain substituted heterocycles of Formula (I) which are useful in the treatment of diseases related to lipid and carbohydrate metabolism, such as type 2 diabetes, adipocyte differentiation, uncontrolled proliferation, such as lymphoma, Hodgkin's Disease, leukemia, breast cancer, prostate cancer or cancers in general; and inflammation, such as osteoarthritis, rheumatoid arthritis, Crohn's Disease or Inflammatory Bowel Disease.
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- N-(phenylsulfonyl)picolinamide derivatives, process for producing the same, and herbicide
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A herbicide containing as the active ingredient an N-(henylsulfonyl)picolinamide derivative represented by general formula (I) wherein X reprcsents a halogeno, a C1-4 alkyl, a C1-4 haloalkyl, a C1-4 alkoxy, a C1-4 haloalkoxy, a (C1-4 alkoxy)carbonyl, a [di(C1-4 alkyl)amino]sulfonyl, an [N—(C1-4 alkyl)-N—(C1-4 alkoxy)amino]sulfonyl, a (C1-4 alkylamino)sulfonyl, a C1-4 alkylthio, a C1-4 alkylsulfinyl, a C1-4 alkylsulfonyl, or nitro; n is an integer of 0 to 5; Y represets a halogeno, a C1-4 alkyl, a C1-4 haloalkyl, a C1-4 alkoxy, C1-4 haloalkoxy, a C1-4 alkylthio, a C1-4 haloalkylthio, amino, a C1-4 alkylamino, a di(C1-4 alkyl)amino, a (C1-4 alkoxy) C1-4 alkyl, a (C1-4 alkylthio) C1-4 alkyl, or nitro; and m is an integer of 0 to 4. This active ingredient is synthesized by condensing a substituted picolinic acid with a substituted benzenesulfonamide under dehydration, or by reacting the phenyl ester of a substituted picolinic acid with a substituted benzenesulfonamide in the presence of a basic compound.
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- Aza- and polyaza-naphthalenyl carboxamides useful as HIV integrase inhibitors
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Aza- and polyaza-naphthalenyl carboxamide derivatives including certain quinoline carboxamide and naphthyridine carboxamide derivatives are described. These compounds are inhibitors of HIV integrase and inhibitors of HIV replication, and are useful in the
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- Total synthesis of dimethyl sulfomycinamate
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Dimethyl sulfomycinamate (1), a methanolysis product from the natural antibiotic sulfomycin I, is synthesized in 11 steps. The chemistry of various pyridine, thiazole, and oxazole heterocycles and their coupling reactions under palladium catalysis are examined. The key transformations in the synthesis are the selective palladium-catalyzed coupling reactions on doubly activated pyridine 62 and the condensation reaction between bromo ketone 69 and amide 28 to form the oxazole moiety 76. The first preparation of oxazole triflates is described, as are some of their chemical properties.
- Kelly, T. Ross,Lang, Fengrui
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p. 4623 - 4633
(2007/10/03)
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- Total synthesis of dimethyl sulfomycinamate
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The first total synthesis of dimethyl sulfomycinamate (1) is described. Highlights of the synthesis include a selective palladium-catalyzed coupling reaction on the bromotriflate 21, and a condensation reaction to form the oxazole ring.
- Ross Kelly,Lang, Fengrui
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p. 5319 - 5322
(2007/10/02)
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- Bipyridyls and their use as inks
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Process employing bipyridyls as inks, of the general formula STR1 in which R, R' are, for example, alkyl and R1, R2, R3, R4, R5, R6 are, for example hydrogen or alkyl radicals, or R1 and R2 or R2 and R3, and/or R4 and R5 or R5 and R6 together with the pyridine ring form in isoquinoline or quinoline ring system.
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- Syntheses of the Piperidine Alkaloids (+/-)-Cassine, (+/-)-Spectaline, (+/-)-Spicigerine Methyl Ester and of (+/-)-Azimic Acid and (+/-)-Carpamic acid
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The piperidine alkaloids (+/-)-cassine (1), (+/-)-spectaline (2), (+/-)-spicigerine methyl ester (3), (+/-)-azimic acid (4), and (+/-)-carpamic acid (5) have been synthesized stereoselectively in the following way: In the SEM ether 7 of 2,6-dibromo-3-pyridinol (6) the bromine atom in position 2 can be regiospecifically exchanged with nBuLi to give 8.Reaction of 8 with methyl iodide gave the key compound 9 exclusively.In the presence of Kumada's NidpppCl2 catalyst in ether solution 9 reacts with the Grignard reagents from the bromides 14-18 to give the products 19-23.Methanolysis of the products gave the substituted 3-pyridinol derivatives 24-28.Subsequent acetalisation led to 29, 30 and hydrolysis to 31, 32.Hydrogenation of 28-32 with Rh on alumina catalyst and 90 bar pressure gave exclusively the (+/-) products 33, 34, 3, 4, and 5 with (2r,3c,6c) configuration.Hydrolysis of the ethylene acetal group in 33 and 34 gave (+/-)-1 and (+/-)-2.
- Hasseberg, Hans-Albrecht,Gerlach, Hans
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p. 255 - 262
(2007/10/02)
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