- Heterocyclic compound as well as pharmaceutical composition, preparation method, intermediate and application thereof
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The invention discloses a heterocyclic compound as well as a pharmaceutical composition, a preparation method, an intermediate and application thereof. The structure of the heterocyclic compound is shown as a formula I, and the heterocyclic compound has CDK7 inhibitory activity and can be used for treating diseases such as tumors.
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- Preparation method, product and application of 2-amino-5-methylpyrazine
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The invention belongs to the field of chemical synthesis, and relates to a preparation method, product and application of 2-amino-5-methylpyrazine. The preparation method comprises the following steps: reacting 2-aminomalonamide with pyruvic aldehyde to generate 2-methyl-5-hydroxy-4-pyrazinamide; enabling 2-methyl-5-hydroxy-4-pyrazinamide to react with phosphorus oxychloride so as to generate 2-methyl-5-chloro-4-cyanopyrazine; carrying out a hydrogenation reaction on the 2-methyl-5-chloro-4-cyanopyrazine to generate 2-methyl-4-cyanopyrazine, and hydrolyzing the 2-methyl-4-cyanopyrazine to obtain 2-methyl-4-amide pyrazine; and carrying out Hofmann degradation on the 2-methyl-4-amide pyrazine so as to obtain the 2-methyl-5-aminopyrazine. The method belongs to a brand-new 2-amino-5-methylpyrazine preparation method, is simple and convenient to operate, high in yield and low in cost, and is suitable for industrial large-scale production.
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Paragraph 0037; 0046-0048; 0057-0059; 0068-0069
(2020/11/25)
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- Synthesis and Characterization of 2-(2-Pyridinyl)pyrazine and 2,2′-Bipyrazine Derivatives
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A convenient and high yield preparation of derivatives of 2-(2-pyridinyl)pyrazine and derivatives of 2,2′-bipyrazine compounds from their derivatives of bromopyrazine using Stille coupling is reported. X-ray structures, elemental analyses, 1H, 13C-NMR, and mass spectral data of the compounds are given.
- KomReddy, Venugopal,Rillema, D. Paul,Nguyen, Huy,Kadel, Lava
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p. 972 - 979
(2019/02/05)
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- Use of a Curtius Rearrangement as Part of the Multikilogram Manufacture of a Pyrazine Building Block
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Commercial route definition for a glucokinase activator called for a reevaluation of the synthesis and processes used to access multikilogram quantities of 2-amino-5-methylpyrazine. After consideration of different options, a variation of the Curtius rearrangement used by the medicinal chemistry route was selected for further development. The formation of an acyl azide for the Curtius rearrangement required a process safety control strategy to be put in place. The process developed was used to successfully deliver multikilogram quantities of 2-amino-5-methylpyrazine in an overall yield of 68%, starting from 5-methylpyrazine-2-carboxylic acid.
- Steven, Alan,Hopes, Phillip
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- Multimodal Vacuum-Assisted Plasma Ion (VaPI) Source with Transmission Mode and Laser Ablation Sampling Capabilities
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We have developed a multimodal ion source design that can be configured on the fly for various analysis modes, designed for more efficient and reproducible sampling at the mass spectrometer atmospheric pressure (AP) interface in a number of different applications. This vacuum-assisted plasma ionization (VaPI) source features interchangeable transmission mode and laser ablation sampling geometries. Operating in both AC and DC power regimes with similar results, the ion source was optimized for parameters including helium flow rate and gas temperature using transmission mode to analyze volatile standards and drug tablets. Using laser ablation, matrix effects were studied, and the source was used to monitor the products of model prebiotic synthetic reactions. [Figure not available: see fulltext.]
- Keelor, Joel D.,Farnsworth, Paul B.,L. Weber, Arthur,Abbott-Lyon, Heather,Fernández, Facundo M.
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p. 897 - 907
(2016/05/02)
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- NITROGEN-CONTAINING FUSED RING COMPOUNDS FOR USE AS CRTH2 ANTAGONISTS
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The present application relates to nitrogen-containing fused ring compounds shown by general formula (I), a pharmaceutically acceptable salt thereof and a stereoisomer thereof as CRTH2 antagonist, wherein X1, X2, X3, X4, X5, W, X, Y, L1, L2, L3, A, B are as defined in the description; the present application further relates to a method for preparing the compounds, a pharmaceutical formulation and a pharmaceutical composition comprising the compounds, a use of the compounds for the manufacture of a medicament for the treatment and/or prevention of diseases related to activity of CRTH2.
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Paragraph 0154
(2014/11/13)
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- NITROGEN-CONTAINING FUSED RING COMPOUNDS AS CRTH2 ANTAGONISTS
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The present application relates to nitrogen-containing fused ring compounds shown by general formula (I), a pharmaceutically acceptable salt thereof and a stereoisomer thereof as CRTH2 antagonist, wherein X1, X2, X3, X4, X5, W, X, Y, L1, L2, L3, A, B are as defined in the description; the present application further relates to a method for preparing the compounds, a pharmaceutical formulation and a pharmaceutical composition comprising the compounds, a use of the compounds for the manufacture of a medicament for the treatment and/or prevention of diseases related to activity of CRTH2.
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Paragraph 0299
(2014/10/16)
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- Peptide deformylase inhibitors
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The present invention relates to a compound of Formula (I): or a pharmaceutically acceptable salt thereof, corresponding pharmaceutical compositions, compound preparation and treatment methods directed to bacterial infections and inhibition of bacterial peptide deformylase (PDF) activity.
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Page/Page column
(2014/12/09)
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- PEPTIDE DEFORMYLASE INHIBITORS
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The present invention relates to a compound of Formula (I): or a pharmaceutically acceptable salt thereof, corresponding pharmaceutical compositions, compound preparation and treatment methods directed to bacterial infections and inhi-bition of bacterial peptide deformylase (PDF) activity
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Page/Page column
(2014/02/15)
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- TYPE II RAF KINASE INHIBITORS
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The present invention relates to novel compounds which are able to modulate b-raf kinases, and the use of such compounds in the treatment of various diseases, disorders or conditions.
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Page/Page column 50
(2011/08/08)
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- CHEMICAL PROCESS 632
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A process for preparing pharmaceutically active compounds of formula (I) or a salt thereof wherein R1, n, m, R3, R6, X1, X2, X3 and X4 are as defined in the specification, is described. Novel intermediates are also described and claimed.
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Page/Page column 19
(2010/08/22)
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- QUINUCLIDINOL DERIVATIVES AS MUSCARINIC RECEPTOR ANTAGONISTS
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The invention provides compounds of formula (I) wherein R5 is a group of formula (II) or (III) and R1, R2, R3, R4, R6, a, b, Z, Y and X are as defined in the specification, a process for their preparation, pharmaceutical compositions containing them, a process for preparing pharmaceutical compositions, their use in therapy and intermediates of use in their preparation.
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Page/Page column 46
(2010/05/13)
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- CRYSTALLINE POLYMORPHIC FORM 631
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A new polymorphic form of 3-{[5-(azetidin-1-ylcarbonyl)pyrazin-2-yl]oxy}-5-{[(1S)-1-methyl-2-(methyloxy)ethyl]oxy}-N-(5-methylpyrazin-2-yl)benzamide, processes for making it and its use as an activator of glucokinase are described.
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- HETEROARYL UREA DERIVATIVES USEFUL FOR INHIBITING CHKl
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Substituted urea compounds useful in the treatment of diseases and conditions related to DNA damage or lesions in DNA replication are disclosed. Methods of making the compounds, and their use as therapeutic agents, for example, in treating cancer and other diseases characterized by defects in DNA replication, chromosome segregation, or cell division, also are disclosed.
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Page/Page column 65
(2008/06/13)
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- HETROARYL BENZAMIDE DERIVATIVES FOR USE AS GLK ACTIVATORS IN THE TREATMENT OF DIABETES
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Compounds of Formula (I) wherein: R1 is hydroxymethyl; R2 is selected from -C(O)NR4R5, SO2NR4R5, S(O)pR4 and HET-2; HET-1 is a 5- or 6-membered, optionally substituted C-linked heteroaryl ring; HET-2 is a 4-, 5- or 6-membered, C- or N-linked optionally substituted heterocyclyl ring; R3 is selected from halo, fluoromethyl, difluoromethyl, trifluoromethyl, methyl, methoxy and cyano; R4 is selected from for example hydrogen, optionally substituted (1-4C)alkyl and HET-2; R5 is hydrogen or (1-4C)alkyl; or R4 and R5 together with the nitrogen atom to which they are attached may form a heterocyclyl ring system as defined by HET-3; HET-3 is for example an optionally substituted N-linked, 4, 5 or 6 membered, saturated or partially unsaturated heterocyclyl ring; p is (independently at each occurrence) 0, 1 or 2; m is 0 or 1; n is 0, 1 or 2; provided that when m is 0, then n is 1 or 2; or a salt, pro drug or solvate thereof, are described. Their use as GLK activators, pharmaceutical compositions containing them, and processes for their preparation are also described.
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Page/Page column 111
(2008/06/13)
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- Substituted-cycloalkyl and oxygenated-cycloalkyl glucokinase activators
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2,3-Di-substituted N-heteroaromatic propionamides with said substitution at the 2-position being a substituted phenyl group and at the 3-position being a polar ring, said propionamides being glucokinase activators which increase insulin secretion in the treatment of type II diabetes.
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- Efficient synthesis of substituted 2-aminopyrazines: FeCl3-promoted condensation of hydroxyiminoketones with aminoacetonitriles
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FeCl3-promoted condensation of hydroxyiminoketones with aminoacetonitriles followed by catalytic hydrogenation afforded the desired pyrazines in moderate-good yields. This protocol provides an efficient and practical synthesis of substituted 2-
- Itoh, Takahiro,Maeda, Kenji,Wada, Toshihiro,Tomimoto, Koji,Mase, Toshiaki
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p. 9287 - 9290
(2007/10/03)
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- Studies on Pyrazines. 6. A Facile Separation Method for a Mixture of the Isomeric 2-Amino-3,5, and 6-methylpyrazines
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This paper describes a facile separation method for a mixture of the isomeric aminomethylpyrazines by two-stage processes.Thus the mixture of aminomethylpyrazines was converted into that of the aminobromomethylpyrazines, which could be separated by chromatography on silica gel.Each of the bromopyrazines was hydrogenated to regenerate the original aminopyrazine as a pure form.
- Sato, Nobuhiro
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p. 143 - 147
(2007/10/02)
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