- BENZAMIDES OF PYRAZOLYL-AMINO-PYRIMIDINYL DERIVATIVES, AND COMPOSITIONS AND METHODS THEREOF
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Provided is a novel class of orally and/or topically available, selective and potent JAK inhibitors as safe and effective therapeutics against various diseases and disorders. More particularly, provided are pharmaceutical composition of these compounds and methods of their preparation and use thereof.
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Paragraph 00394
(2020/07/07)
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- Method for synthesizing 8,8-difluoro-1,4- dioxaspiro[4.5]decane
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The invention discloses a method for synthesizing 8,8-difluoro-1,4-dioxaspiro[4.5]decane. The method comprises the following steps: first, 1,4-cyclohexanedione monoethylene ketal is reacted with a fluorinating agent to form a mixture of 8,8-difluoro-1,4-dioxaspiro[4.5]decane and impurity 8-fluoro-1,4-dioxaspiro[4.5]deca-7-ene; and using a substitute of the mixture and anhydrous hydrofluoric acid to obtain 8,8-difluoro-1,4-dioxaspiro[4.5]decane under the action of the catalyst boron trifluoride complex. In the synthetic method, raw material sources are wide, the price is low, impurities are reutilized by reasonable adding of the catalyst, the production cost is reduced, the production efficiency is improved, raw material and product waste is avoided, the problems of low product yield and low purity are effectively solved, the economic benefit is very obvious, the environmental pollution is small, and the method is especially suitable for large-scale industrial application and promotion.
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Paragraph 0077-0082
(2018/11/26)
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- Method for synthesizing 4-fluorocyclohexanone
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The invention discloses a method for synthesizing 4-fluorocyclohexanone. The method comprises steps as follows: under the alkaline condition, 1,4-cyclohexanedione monoethylene ketal and a fluorinatingagent are subjected to highly selective reaction, and 8-fluoro-1,4-dioxaspiro[4.5]deca-7-ene is produced; 8-fluoro-1,4-dioxaspiro[4.5]decane is prepared from 8-fluoro-1,4-dioxaspiro[4.5]deca-7-ene and hydrogen under the action of a palladium-carbon catalyst; 8-fluoro-1,4-dioxaspiro[4.5]decane is subjected to deprotection with added acid, and 4-fluorocyclohexanone is obtained. According to the method, 1,4-cyclohexanedione monoethylene ketal which is widely sourced and low in cost is taken as a reaction raw material, a high-purity intermediate can be obtained maximumly in each reaction, so thatthe total yield of the whole reaction is high, purity of a final product is up to 98%, the economic benefit is quite remarkable, less environmental pollution is produced, and the method is particularly suitable for large-scale industrial application and popularization.
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Paragraph 0100-0105
(2018/05/16)
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- Fused tricyclic hepatitis virus inhibitor and application thereof
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The invention belongs to the field of medical chemistry, relates to a fused tricyclic hepatitis virus inhibitor and application thereof, and particularly, provides a compound of the general formula I or pharmaceutically acceptable salt, isomer, solvate, crystal or prodrug thereof, and a medicine composition containing the compounds and application of the compounds or the composition in medicine preparation. The compound has the good inhibiting activity on hepatitis C virus, meanwhile has the low toxicity on host cells, and is high in effectiveness, good in safety and likely to become the medicine for treating and/or preventing diseases relevant to HCV infection.
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Paragraph 0670; 0671; 0672; 0673
(2016/12/26)
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- NOVEL BENZAMIDE DERIVATIVE AND USE THEREOF
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Disclosed are a novel benzamide derivative and pharmaceutical use thereof, and more particularly, a novel benzamide derivative having a structure of Formula 1 or pharmaceutically acceptable salts thereof, and a composition for prevention or treatment of pain or itching including the above material. The novel benzamide derivative and pharmaceutically acceptable salt thereof according to the present invention exhibit excellent pain-suppressive effect and, in particular, pain-suppressive effect in not only a neuropathic animal model but also other models such as a formalin model, and therefore, may be used in suppression of different pains such as nociceptive pain, chronic pain, etc. Further, since it was demonstrated that the present invention displays anti-pruritic efficacy even in an itching model, to which a mechanism and treatment concept established with respect to pain is applied, the present invention may also be effectively used in radical treatment of atopic dermatitis by applying the inventive product to an anti-pruritic composition in order to suppress an initial itching stage and treat symptoms thereof, thus preventing skin damage or inflammation after the scratching stage.
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Paragraph 0190; 0191; 0192; 0193
(2014/11/27)
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- NOVEL BENZAMIDE DERIVATIVE AND USE THEREOF
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Disclosed are a novel benzamide derivative and pharmaceutical use thereof, and more particularly, a novel benzamide derivative having a structure of Formula 1 or pharmaceutically acceptable salts thereof, and a composition for prevention or treatment of pain or itching including the above material. The novel benzamide derivative and pharmaceutically acceptable salt thereof according to the present invention exhibit excellent pain-suppressive effect and, in particular, pain-suppressive effect in not only a neuropathic animal model but also other models such as a formalin model, and therefore, may be used in suppression of different pains such as nociceptive pain, chronic pain, etc. Further, since it was demonstrated that the present invention displays anti-pruritic efficacy even in an itching model, to which a mechanism and treatment concept established with respect to pain is applied, the present invention may also be effectively used in radical treatment of atopic dermatitis by applying the inventive product to an anti-pruritic composition in order to suppress an initial itching stage and treat symptoms thereof, thus preventing skin damage or inflammation after the scratching stage.
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Paragraph 0122-0124
(2014/10/16)
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- Palladium catalyzed decarboxylative rearrangement of N-alloc indoles
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A highly efficient palladium catalyzed decarboxylative allylic rearrangement of alloc indoles has been developed. This can also be combined with a Suzuki-Miyaura cross-coupling reaction in a single pot transformation. Substituted alloc groups and benzylic variants have also been demonstrated alongside promising initial results on the enantioselective variant.
- Chen, Jun,Cook, Matthew J.
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supporting information
p. 1088 - 1091
(2013/04/10)
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- 1-Amino-4,4-difluorocyclohexanecarboxylic acid as a promising building block for drug discovery: Design, synthesis and characterization
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1-Amino-4,4-difluorocyclohexanecarboxylic acid has been designed as a fluorinated analogue of the pharmacologically relevant 1- aminocyclohexanecarboxylic acid. The synthesis has been performed in three steps from a commercially available material in 22% overall yield. An impact of fluorine atoms on conformation, lipophilicity, acidity and fluorescent properties of the amino acid has been studied. Various practical applications of the obtained compound are suggested.
- Mykhailiuk, Pavel K.,Starova, Viktoriia,Iurchenko, Vladimir,Shishkina, Svitlana V.,Shishkin, Oleg V.,Khilchevskyi, Oleksandr,Zaporozhets, Olga
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p. 4066 - 4075
(2013/06/26)
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- Deoxofluorination reactions using N,N-disubstituted aminodifluorosulfinium tetrafluoroborate salts
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The synthesis of N,N-disubstituted aminodifluorosulfinium tetrafluoroborate salts is reported, and their behavior as deoxofluorinating agent was evaluated. The deoxofluorination reactions were performed using a primary alcohol, a secondary alcohol and a ketone. Results show that subtle modification of the structure of the reagents can noticeably affect the reactivity and the selectivity in deoxofluorination reactions.
- Mahé, Olivier,L'Heureux, Alexandre,Couturier, Michel,Bennett, Christopher,Clayton, Simon,Tovell, David,Beaulieu, Francis,Paquin, Jean-Fran?ois
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- Aminodifluorosulfinium salts: Selective fluorination reagents with enhanced thermal stability and ease of handling
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Diethylaminodifluorosulfinium tetrafluoroborate (XtalFluor-E) and morpholinodifluorosulfinium tetrafluoroborate (XtalFluor-M) are crystalline fluorinating agents that are more easily handled and significantly more stable than Deoxo-Fluor, DAST, and their analogues. These reagents can be prepared in a safer and more cost-efficient manner by avoiding the laborious and hazardous distillation of dialkylaminosulfur trifluorides. Unlike DAST, Deoxo-Fluor, and Fluolead, XtalFluor reagents do not generate highly corrosive free-HF and therefore can be used in standard borosilicate vessels. When used in conjunction with promoters such as Et3N3HF, Et3N2HF, or DBU, XtalFluor reagents effectively convert alcohols to alkyl fluorides and carbonyls to gem-difluorides. These reagents are typically more selective than DAST and Deoxo-Fluor and exhibit superior performance by providing significantly less elimination side products.
- Lheureux, Alexandre,Beaulieu, Francis,Bennett, Christopher,Bill, David R.,Clayton, Simon,Laflamme, Franois,Mirmehrabi, Mahmoud,Tadayon, Sam,Tovell, David,Couturier, Michel
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supporting information; experimental part
p. 3401 - 3411
(2010/07/07)
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- MELANOCORTIN RECEPTOR AGONISTS
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The present invention relates to a compound having a good agonistic activity to melanocortin receptor, or pharmaceutically acceptable salt or isomer thereof, and an agonistic composition for melanocortin receptor comprising the same as an active ingredient.
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Page/Page column 10
(2010/06/11)
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- MELANOCORTIN RECEPTOR AGONISTS
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The present invention relates to a compound having a good agonistic activity to melanocortin receptor, or pharmaceutically acceptable salt or isomer thereof, and an agonistic composition for melanocortin receptor comprising the same as an active ingredient.
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Page/Page column 23
(2010/06/15)
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- DIPHENYL SUBSTITUTED CYCLOALKANES
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The present invention provides compounds of Formula I which are FLAP inhibitors useful as anti-atherosclerotic, anti-asthmatic, anti-allergic, anti-inflammatory and cytoprotective agents.
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Page/Page column 40
(2009/05/28)
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- Aminodifluorosulfinium Tetrafluoroborate salts as stable and crystalline deoxofluorinating reagents
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Aminodifluorosulfinium tetrafluoroborate salts were found to act as efficient deoxofluorinating reagents when promoted by an exogenous fluoride source and, In most cases, exhibited greater selectivity by providing less elimination byproduct as compared to DAST and DeoxoFluor. Aminodifluorosulfinium tetrafluoroborates are easy handled crystalline salts that show enhanced thermal stability over dialkylaminosulfur trifluorides, are storage-stable, and unlike DAST and Deoxo-Fluor do not react violently with water.
- Beaulieu, Francis,Beauregard, Louis-Philippe,Courchesne, Gabriel,Couturier, Michel,Laflamme, Francois,L'Heureux, Alexandre
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supporting information; experimental part
p. 5050 - 5053
(2009/12/28)
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- MELANOCORTIN RECEPTOR AGONISTS
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The present invention relates to a compound of the following formula 1, pharmaceutically acceptable salt and isomer thereof effective as agonist of melanocortin receptor, and an agonistic composition of melanocortin receptor comprising the same as active ingredient.
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Page/Page column 28
(2008/06/13)
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- Benzamide derivatives and uses related thereto
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Benzamide derivatives of formulae I and II, and pharmaceutically acceptable salts, solvates, stereoisomers, and prodrugs thereof, and pharmaceutical compositions comprising the same, are described and have therapeutic utility, particularly in the treatment of diabetes, obesity, and related conditions and disorders: wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, and R12 are defined as provided herein.
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Page/Page column 51
(2008/06/13)
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- Substituted benzothiazole amide derivatives
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A compound of formula I and a method of treatment of diseases, related to modulation of the adenosine A2 receptor system comprising administering a compound of formula 1to a person in need of such treatment.
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