- NEW COMPOUND HAVING FGFR INHIBITORY ACTIVITY AND PREPARATION AND APPLICATION THEREOF
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The present invention relates to a new compound having an FGFR inhibitory activity and preparation and application thereof. In particular, the compound according to the present invention has a structure as shown in formula I, wherein each group and substituent are as defined in the description. Also disclosed in the present invention are a preparation method for the compound and a use thereof in preparation of a drug for treating and/or preventing a tumor-related disease and/or an FGFR-related disease.
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- NITROGEN-CONTAINING AROMATIC COMPOUNDS AND ORGANIC ELECTROLUMINESCENT ELEMENTS
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Provided are a nitrogen-containing aromatic compound useful for an organic electroluminescent device, and an organic electroluminescent device (organic EL device) that improves luminous efficiency of the device and sufficiently ensures driving stability of the device. The nitrogen-containing aromatic heterocyclic compound is represented by the following formula (1). The organic EL device includes an organic layer that contains the nitrogen-containing aromatic heterocyclic compound between an anode and a cathode laminated on a substrate. In the formula (1), a ring A represents an aromatic ring represented by the formula (1a) and fused with two adjacent rings, a ring B represents a heterocycle represented by the formula (1b) and fused with two adjacent rings, Y's each represent C-R or N, X's each represent N-Z, O, S, or Se, R represents hydrogen, an alkyl group, an aromatic group, or the like, and Z represents an alkyl group, an aromatic group, or the like.
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- Potassium [1-(tert-butoxycarbonyl)-1H-indol-2-yl]trifluoroborate as an efficient building block in palladium-catalyzed Suzuki-Miyaura cross couplings
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Potassium [1-(tert-butoxycarbonyl)-1H-indol-2-yl]trifluoroborate (1) was used in Suzuki-type coupling reactions. First, the best coupling conditions were assessed using bromobenzene as the electrophile. Then, 1 was successfully coupled with various aryl a
- Kassis, Pamela,Beneteau, Valerie,Merour, Jean-Yves,Routier, Sylvain
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experimental part
p. 2447 - 2453
(2010/02/27)
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- Trisoxazoline/Cu(II)-catalyzed asymmetric intramolecular Friedel-Crafts alkylation reaction of indoles
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Intramolecular Friedel-Crafts alkylation reaction of indoles catalyzed by trisoxazoline/copper(II) is described. This annulation provides an easy access to polycyclic indole derivatives with up to 90% ee in up to 99% yield.
- Zhou, Jiao-Long,Ye, Meng-Chun,Sun, Xiu-Li,Tang, Yong
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supporting information; experimental part
p. 6877 - 6881
(2009/12/06)
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- Combined directed ortho and remote metalation-suzuki cross-coupling strategies. Efficient synthesis of heteroaryl-fused benzopyranones from biaryl O-carbamates
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(Chemical Equation Presented) A concise synthesis of heteroaryl dibenzopyranones 9a,b, 10a,b, 11a-c, and 12a-c has been achieved by the LDA-induced migration of heterobiaryl O-carbamates 18, 21, 25, and 30 which, in turn, were prepared in good yield using
- James, Clint A.,Coelho, Antonio Luiz,Gevaert, Matt,Forgione, Pat,Snieckus, Victor
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experimental part
p. 4094 - 4103
(2009/09/25)
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- QUINOLONES USEFUL AS INDUCIBLE NITRIC OXIDE SYNTHASE INHIBITORS
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The present invention relates to novel quinolones of Formula I that inhibit inducible NOS synthase together with methods of synthesizing and using the compounds including methods for inhibiting or modulating nitric oxide synthesis and/or lowering nitric oxide levels in a patient by administering the compounds for the treatment of disease.
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- Role and substrate specificity of the Streptomyces coelicolor RedH enzyme in undecylprodiginine biosynthesis
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The function of RedH from Streptomyces coelicolor as an enzyme that catalyses the condensation of 4-methoxy-2,2′-bipyrrole-5-carboxaldehyde (MBC) and 2-undecylpyrrole to form the natural product undecylprodiginine has been experimentally proven, and the s
- Haynes, Stuart W.,Sydor, Paulina K.,Stanley, Anna E.,Song, Lijiang,Challis, Gregory L.
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p. 1865 - 1867
(2008/12/22)
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- Fluorescent pyrimidopyrimidoindole nucleosides: Control of photophysical characterizations by substituent effects
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(Chemical Equation Presented) 10-(2-Deoxy-β-D-ribofuranosyl) pyrimido[4′,5′:4,5]pyrimido[1,6-a]indole-6,9(7H)-dione (dC PPI) and its derivatives were synthesized via the Suzuki-Miyaura coupling reaction of 5-iododeoxycytidine with 5-substituted N-Boc-indole-2- borates and characterized by UV-vis and fluorescence spectroscopy. The new fluorescent nucleosides showed rather large Stokes shifts (116-139 nm) in an aqueous buffer. The fluorescent intensities were dependent on the nature of the substituents on the indole rings. The electron-withdrawing groups increased the fluorescent intensity while the electron-donating groups having lone pairs decreased it. Among the substituted dCPPI derivatives tested, the trimethylammonium derivative of dCPPI was found to emit the brightest fluorescent light. The solvatochromism of dCPPI and its derivatives was also studied. Some of the dCPPI derivatives showed interesting solvent-dependent fluorescence enhancement and could be useful as new fluorescent structural probes for nucleic acids. The Lippert-Mataga analyses of the Stokes shift were also carried out to obtain estimated values of the dipole moment of the excited states of some of the derivatives.
- Mizuta, Masahiro,Seio, Kohji,Miyata, Kenichi,Sekine, Mitsuo
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p. 5046 - 5055
(2008/02/08)
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- Ruthenium half-sandwich complexes as protein kinase inhibitors: Derivatization of the pyridocarbazole pharmacophore ligand
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A general route to ruthenium pyridocarbazole half-sandwich complexes is presented and applied to the synthesis of sixteen new compounds, many of which have modulated protein kinase inhibition properties. For example, the incorporation of a fluorine into t
- Pagano, Nicholas,Maksimoska, Jasna,Bregman, Howard,Williams, Douglas S.,Webster, Richard D.,Xue, Feng,Meggers, Eric
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p. 1218 - 1227
(2008/02/04)
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- Synthesis of the dibenzopyrrocoline alkaloid skeleton: indolo[2,1-a]isoquinolines and related analogues
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The indolo[2,1-a]isoquinoline and pyrrolo[2,1-a]isoquinoline nuclei have been synthesized from N-benzylindole or ethyl 1H-indol-1-ylacetate and N-benzylpyrrole precursors, respectively. Firstly, at C-2 of either the indole or pyrrole nucleus, aromatic rin
- L?tter, Angelique N.C.,Pathak, Rakhi,Sello, Thato S.,Fernandes, Manuel A.,van?Otterlo, Willem A.L.,de Koning, Charles B.
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p. 2263 - 2274
(2007/10/03)
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- PYRIMIDINE COMPOUNDS FOR THE TREATMENT OF INFLAMMATION
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Compounds of Formula (I): wherein A, X, R2 and R4 are as defined herein, are disclosed.
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Page/Page column 155-156
(2010/02/11)
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- A non-cryogenic method for the preparation of 2-(indolyl) borates, silanes, and silanols
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2-Indolyl borates are prepared via addition of LDA to a mixture of N-Bo-indole and triisopropyl borate at 0-5 °C. Following acidic hydrolysis, the boronic acids are isolated by crystallization in good to excellent yield (73-99%). The method is quite general, tolerating a wide range of functional groups, and also provides access to 2-silyl derivatives (80-91%).
- Vazquez, Enrique,Davies, Ian W.,Payack, Joseph F.
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p. 7551 - 7552
(2007/10/03)
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- A versatile and convenient method for the synthesis of substituted benzo[a]carbazoles and pyrido[2,3-a]carbazoles
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Treatment of 2-(o-tolyl)- or 2-(3-methyl-2-pyridyl)-substituted indole-3-carbaldehydes with potassium tert-butoxide in DMF at 70-80°C with simultaneous irradiation from a 400 W high-pressure mercury lamp afforded benzo[a]carbazoles and pyrido[2,3-a]carbaz
- De Koning, Charles B.,Michael, Joseph P.,Rousseau, Amanda L.
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p. 1705 - 1713
(2007/10/03)
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- Indolyl-pyrrolydenemethylpyrrole derivatives and process for their preparation
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PCT No. PCT/EP98/01285 Sec. 371 Date Nov. 12, 1998 Sec. 102(e) Date Nov. 12, 1998 PCT Filed Feb. 27, 1998 PCT Pub. No. WO98/40380 PCT Pub. Date Sep. 17, 1998The present invention relates to substituted (1H-indol-2-yl)-5[(2H-pyrrol-2-ylidene) methyl]-1H-pyrrole compounds and their use as immunomodulating agents, to the preparation of the compounds and to pharmaceutical compositions comprising them.
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- Application of the Pd-catalyzed heteroarylation to the synthesis of 5- (indol-2'-yl)pyridin-2-one and 5-(indol-2'-yl)pyran-2-one
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The synthesis of 5-(indol-2'-yl)pyridin-2-ones and 5-(indol-2'-yl)pyran- 2-one by Pd-catalyzed reactions is described. The best results are obtained using 2-indolylstannanes or 2-indolylzinc halides to be coupled with 5- bromopyridin-2-ones or 5-bromopyran-2-one in the presence of Pd(PPh3)4 as catalyst. Other Pd-catalyzed reactions are discussed.
- Danieli, Bruno,Lesma, Giordano,Martinelli, Marisa,Passarella, Daniele,Peretto, Ilaria,Silvani, Alessandra
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p. 14081 - 14088
(2007/10/03)
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