- BICYCLIC HETEROCYCLIC DERIVATIVES AS BROMODOMAIN INHIBITORS
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The present disclosure provides bicyclic heterocyclic derivatives of formula (I), which may be therapeutically useful, more particularly as bromodomain inhibitors; (I), in which R1, R2, R3, R4, L1, L2, Cy1, Cy2, X, n, and dotted line have the same meaning given in the specification, and pharmaceutically acceptable salts or pharmaceutically acceptable stereoisomers thereof that are useful in the treatment and prevention of diseases or disorders, in particular their use in diseases or disorders associated as bromodomain inhibitors. The present disclosure also provides preparation of compounds and pharmaceutical formulations comprising at least one of bicyclic heterocyclic derivatives of formula (I), together with a pharmaceutically acceptable carrier, diluent, or excipient.
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Paragraph 0229
(2017/04/04)
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- BICYCLIC HETEROCYCLIC DERIVATIVES AS BROMODOMAIN INHIBITORS
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The present invention provides bicyclic heterocyclic derivatives of formula (I), which may be therapeutically useful, more particularly as bromodomain inhibitors; (I), in which R1, R2, R3, R4, L1, L2, Cy1, Cy2, X, n and dotted line are have the same meaning given in the specification, and pharmaceutically acceptable salts or pharmaceutically acceptable stereoisomers thereof that are useful in the treatment and prevention of diseases or disorder, in particular their use in diseases or disorder associated as bromodomain inhibitors. The present invention also provides preparation of the compounds and pharmaceutical formulations comprising at least one of bicyclic heterocyclic derivatives of formula (I), together with a pharmaceutically acceptable carrier, diluent or excipient therefor.
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Page/Page column 57
(2015/07/23)
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- NOVEL 4,6-DISUBSTITUTED AMINOPYRIMIDINE DERIVATIVES HAVING BOTH AROMATIC AND HALOGENIC SUBSTITUENTS
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Certain 4,6-disubstituted aminopyrimidine derivatives having both aromatic and halogenic substituents.
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Paragraph 0635
(2014/03/24)
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- A novel method for the nitration of simple aromatic compounds
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Simple aromatic compounds such as benzene, alkylbenzenes, halogenobenzenes, and some disubstituted benzenes are nitrated in excellent yields with high regioselectivity under mild conditions using zeolite β as a catalyst and a stoichiometric quantity of nitric acid and acetic anhydride. The zeolite can be recycled, and the only byproduct is acetic acid, which can be separated easily from the nitration product by distillation; the process is inexpensive and represents an attractive method for the clean synthesis of a range of nitroaromatic compounds. For example, nitration of toluene gives a quantitative yield of mononitrotoluenes, of which 79% is 4-nitrotoluene; fluorobenzene gives a quantitative yield of mononitro compounds, of which 94% is 4-nitrofluorobenzene; and 2-fluorotoluene gives a 96% yield of mononitro products, of which 90% is the 5-nitro isomer and 10% is the 4-nitro isomer.
- Smith, Keith,Musson, Adam,DeBoos, Gareth A.
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p. 8448 - 8454
(2007/10/03)
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- Facile preparation of aromatic fluorides by deaminative fluorination of aminoarenes using hydrogen fluoride combined with bases
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One-pot deaminative fluorination of aminoarenes including heteroaromatics, namely, diazotization of aminoarenes followed by in situ fluoro-dediazoniation of the corresponding diazonium ions, was successfully accomplished to produce fluoroarenes in high yields by using hydrogen fluoride combined with base solutions. The diazotization stage has been found to play the most important part in yielding fluoroarenes effectively. It was greatly influenced by the composition of the HF solution and enhanced by employing appropriate amounts of bases such as pyridine under carefully controlled conditions. The fluoro-dediazoniation stage was effectively accelerated photochemically to afford fluoroarenes having polar substituents such as hydroxyl, nitro and so on in high yields.
- Yoneda,Fukuhara
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- PREPARATION OF AROMATIC FLUORIDES VIA DIAZOTIZATION AND PHOTOCHEMICALLY INDUCED FLUORO-DEDIAZONIATION OF AROMATIC AMINES IN ANHYDROUS HYDROGEN FLUORIDE - ORGANIC BASE SOLUTIONS
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Fluoro-dediazoniation of aromatic diazonium ions, produced by the diazotization of the corresponding aromatic amines with NaNO2 in anhydrous hydrogen fluorides (AHF) - organic base solutions, was accelerated photochemically to afford Ar-F efficiently in AHF - organic base solutions in situ.
- Yoneda, Norihiko,Fukuhara, Tsuyoshi,Kikuchi, Tetsuo,Suzuki, Akira
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p. 865 - 872
(2007/10/02)
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- Phenyl benzoic acid compounds
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The invention relates to substituted 5-(phenyl)benzoic acid esters and non-toxic pharmaceutically accepted salts thereof and processes for their preparation. The substituted 5-(phenyl)benozic acids are useful as anti-inflammatory compounds. Also included are method of treating inflammation claims by administering these particular compounds to patients.
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