- QUINOLINO-PYRROLIDIN-2-ONE DERIVATIVE AND APPLICATION THEREOF
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Disclosed are a series of quinolino-pyrrolidin-2-one compounds, and application thereof in preparation of drugs for ATM inhibitor-related diseases. The present disclosure specifically relates to a derivative compound represented by formula (I), tautomers thereof or pharmaceutically acceptable compositions thereof.
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Paragraph 0076-0077; 0083-0084
(2021/07/08)
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- 5-bromo-6-chloro-3-indolyl caprylate synthesis method
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The invention discloses a 5-bromo-6-chloro-3-indolyl caprylate synthesis method, which is characterized in that 4-chloro-2-aminobenzoic acid and N-bromosuccinimide are subjected to a bromination reaction to obtain 5-bromo-4-chloro-2-aminobenzoic acid, 5-b
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Paragraph 0024; 0025; 0026; 0027; 0028; 0029; 0030
(2017/09/01)
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- A 5 - bromo - 4 - chloro - 2 - amino preparation method of acetophenone (by machine translation)
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The invention discloses a 5 - bromo - 4 - chloro - 2 - amino acetophenone preparation method, the method comprises the following steps: to 4 - chloro - 2 - aminobenzoic acid as the starting material, the reaction of halide 5 - bromo - 4 - chloro - 2 - ami
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Paragraph 0019; 0020; 0028; 0029; 0036; 0037
(2017/08/29)
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- INHIBITORS OF THE FIBROBLAST GROWTH FACTOR RECEPTOR
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Described herein are inhibitors of FGFR-4, pharmaceutical compositions including such compounds, and methods of using such compounds and compositions.
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Paragraph 0407; 0408; 0409
(2015/05/05)
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- Indoxylic acid esters as convenient intermediates towards indoxyl glycosides
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Indoxylic acid methyl and allyl esters with varied halide-substitution patterns were obtained in excellent yields using a scalable route. Phase-transfer glycosylation of these key intermediates was carried out with various glycosyl halides. Subsequent mild silver-mediated decarboxylation followed by Zemplen deacetylation led to indoxyl glycosides in good overall yields. Indoxyl glycosides are well-established and widely used tools for enzyme screening and enzyme-activity monitoring. In the past, their synthesis has been difficult, so this new approach has led to a variety of useful structures. Indoxyl glycosides with varied halide-substitution patterns were synthesized using indoxylic acid esters as key intermediates. Glycosylation under phase-transfer conditions, ester cleavage, and mild decarboxylation led to the indoxyl glycosides in good yields. This approach enables access to a number of different indoxyl compounds. Copyright
- Boettcher, Stephan,Thiem, Joachim
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p. 564 - 574
(2014/02/14)
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- Synthesis of DIBAC analogues with excellent SPAAC rate constants
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In search for increased reactivity in strain-promoted azide alkyne cycloadditions (SPAAC), the synthesis of new and more reactive cyclooctynes is of pivotal importance. To identify cyclooctynes with enhanced reactivity, without loss of stability, the synthesis and kinetic analysis of new dibenzoazacyclooctyne (DIBAC) analogues were conducted. Starting from iodobenzyl alcohol analogues and ortho-ethynylaniline various substituted dihydrodibenzo[b,f]azocines were produced. Subsequent bromination and elimination proved to be difficult depending on the aromatic substitution pattern, yielding chloro-, bromo-, and methoxy-substituted DIBACs in moderate yield. In the elimination reaction towards nitro- and Br,Cl-DIBAC, the corresponding cyclooctene was obtained instead of the cyclooctyne. Additionally, a dimethoxy-substituted DIBAC analogue was prepared following an alternative route involving light-induced deprotection of a cyclopropenone derivative. In total, four DIBAC analogues were successfully prepared showing excellent rate constants in the SPAAC reaction ranging from 0.45 to 0.9 M-1 s -1, which makes them comparable to the fastest cyclooctynes currently known. This journal is the Partner Organisations 2014.
- Debets, Marjoke F.,Prins, Jasper S.,Merkx, Donny,Van Berkel, Sander S.,Van Delft, Floris L.,Van Hest, Jan C. M.,Rutjes, Floris P. J. T.
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supporting information
p. 5031 - 5037
(2014/07/07)
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- SUBSTITUTED AZADIBENZOCYCLOOCTYNE COMPOUNDS AND THEIR USE IN METAL-FREE CLICK REACTIONS
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The invention relates to a substituted azadibenzocyclooctyne compound according to Formula (5): The invention also relates to a conjugate wherein a substituted azadibenzocyclooctyne according to the invention is conjugated to a label, and to the use of these conjugates for bioorthogonal labeling, imaging or modification of a target molecule, e.g. surface modification. The invention further relates to a method for the modification of a target molecule, wherein a conjugate according to the invention is reacted with a compound comprising a 1,3-dipole or a 1,3-(hetero)diene.
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Page/Page column 27
(2014/12/12)
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- 1H-IMIDAZO[4,5-C]QUINOLINE DERIVATIVES IN THE TREATMENT OF PROTEIN KINASE DEPENDENT DISEASES
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The invention relates to the use of imidazoquinolines and salts thereof in the treatment of protein kinase diseases and for the manufacture of pharmaceutical preparations for the treatment of said diseases, imidazoquinolines for use in the treatment of protein kinase dependent diseases, a method of treatment against said diseases, comprising administering the imidazoquinolines to a warm-blooded animal, especially a human, pharmaceutical preparations comprising an imidazoquinoline, especially for the treatment of a protein kinase dependent disease, novel imidazoquinolines, and a process for the preparation of the novel imidazoquinolines.
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Page/Page column 70
(2010/02/12)
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- 1H-IMIDAZOQUINOLINE DERIVATIVES AS PROTEIN KINASE INHIBITORS
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The invention relates to imidazoquinolines of formula (I) for use in the treatment of protein kinase dependent diseases; pharmaceutical preparations comprinsing an imidazoquinoline, especially for the treatment of a pretein kinase dependent disease; novel imidazoquinolines; and a process for the preparation of the novel imidazoquinilines.
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Page/Page column 81-82
(2010/02/12)
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