- 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 00395
(2020/07/07)
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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 0639; 0640; 0641; 0674; 0675; 0676; 0677
(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 0125-0127
(2014/10/16)
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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 0194; 0195; 0196; 0197
(2014/11/27)
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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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- 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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- 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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