- Design and synthesis of novel 3-(benzo[d]oxazol-2-yl)-5-(1-(piperidin-4-yl) -1H-pyrazol-4-yl)pyridin-2-amine derivatives as selective G-protein-coupled receptor kinase-2 and -5 inhibitors
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G-protein-coupled receptor kinase (GRK)-2 and -5 are emerging therapeutic targets for the treatment of cardiovascular disease. In our efforts to discover novel small molecules to inhibit GRK-2 and -5, a class of compound based on 3-(benzo[d]oxazol-2-yl)-5-(1-(piperidin-4-yl)-1H-pyrazol-4-yl)pyridin-2-amine was identified as a novel hit by high throughput screening campaign. Structural modification of parent benzoxazole scaffolds by introducing substituents on phenyl displayed potent inhibitory activities toward GRK-2 and -5.
- Cho, Sung Yun,Lee, Byung Ho,Jung, Heejung,Yun, Chang Soo,Ha, Jae Du,Kim, Hyoung Rae,Chae, Chong Hak,Lee, Jeong Hyun,Seo, Ho Won,Oh, Kwang-Seok
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- An improved process for the preparation of Eltrombopag Olamine and its intermediates
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The present invention relates to an improved process for the purification of Eltrombopag olamine of compound of formula (2). The present invention also relates to an improved process for the preparation of Eltrombopag olamine intermediates and further conversion to Eltrombopag olamine of a compound of formula (2).
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Paragraph 0091-0092
(2021/07/30)
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- JAK INHIBITORS
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Disclosed is a series of JAK inhibitors, which specifically relates to a compound shown in formula (I) or pharmaceutically acceptable salts thereof.
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Paragraph 0163; 0164
(2018/05/03)
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- Preparation method of eltrombopag medicine for treating idiopathic thrombocytopenic purpura
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The invention discloses a preparation method of an eltrombopag medicine for treating idiopathic thrombocytopenic purpura. A chemical name of the eltrombopag is 3-{(2Z)-2-[1-(3,4-xylyl)-3-methyl-5-oxo-1,5-dihydrogen-4H-pyrazole-4-idene]hydrazine}-2- hydroxyl-3-biphenyl carboxylic acid-2-amine ethanol salt. The preparation method has the advantages that the preparation process is concise, the raw materials are easy to obtain, the hypertoxic iodomethane is not used, the economic and environment-friendly effects are realized, the industrialization is favorably realized, the economic and technicaldevelopment of the crude drug of the eltrombopag can be promoted, the production cost is reduced, and the preparation method is suitable for large-batch production.
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Paragraph 0016
(2018/04/28)
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- Unexpected one pot C (aryl)-N bond cleavage and Questiomycin A formation from the reduction reaction of 2-amino-6-nitrophenol derivatives
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2-Amino-6-nitrophenol derivatives 5A and 5B have been prepared from the bromonitro phenol derivative 4 using the Buchwald conditions. While attempting one pot reduction of nitro group and deprotection of phenolic benzyl group of the compounds 5A and 5B separately using Pd/C in methanol under H2 atmosphere, an unexpected C(aryl)-N bond cleavage reaction had occurred which was followed by formation of a known compound Questiomycin A (2-amino-3H-phenoxazin-3-one) 1 from both the compounds. In the present study, the danger of deamination of Buchwald products 5A and 5B under the conditions of catalytic hydrogenation and the simultaneous formation of phenoxazine 1 is disclosed.
- Mustafa, Shaik,Santhosh Reddy,Surendra Babu
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p. 6104 - 6107
(2015/10/28)
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- Process for the preparation of a thrombopoietin agonist
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The present invention relates to a process for the preparation of a thrombopoietin agonist, intermediates useful in its preparation, and a process for the preparation of said intermediates.
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Paragraph 0054; 0055; 0056
(2015/05/06)
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- A practical nickel-catalyzed reductive alkylation of amidophenyl bromides
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A modified Weix's reductive coupling for alkylation of amidoaryl bromides based on Ni(COD)2 precatalyst and 2,2′-dipyridyl ligand was developed. This reaction is reliable for amidophenyl bromides and gives yields up to 87%, and is potentially useful in the synthesis of amidophenyl-containing molecules.
- Liu, Xuge,Yang, Zhilin,Li, Ya-Min,Yang, Fan,Feng, Liang,Wang, Nengzhong,Ma, Debiao,Chang, Kwen-Jen,Shen, Yuehai
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p. 9522 - 9529
(2015/03/04)
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- Substituted phenylimidazopyrazoles and their use
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The present application relates to novel 1-phenyl-1H-imidazo[1,2-b]pyrazole derivatives, to processes for their preparation, to their use for the treatment and/or prevention of diseases and to their use for preparing medicaments for the treatment and/or prevention of diseases, in particular angiogenic disorders and hyperproliferative disorders, where neovascularization plays a role, such as, for example, neoplastic disorders and tumour disorders. Such treatments can be carried out as monotherapy or else in combination with other medicaments or further therapeutic measures.
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Paragraph 1053; 1054; 1055; 1056
(2013/07/31)
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- FARNESOID X RECEPTOR AGONISTS
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The present invention relates to famesoid X receptors (FXR, NR1H4) FXR is a member of the nuclear receptor class of ligand-activate transcription factors More particularly, the present invention relates to compounds useful as agonists for FXR, pharmaceutical formulations comprising such compounds, and therapeutic use of the same Novel isoxazole compounds are disclosed as part of pharmaceutical compositions for the treatment of a condition mediated by decreased FXR activity, such as obesity, diabetes, cholestatic liver disease, liver fibrosis, and metabolic syndrome
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Page/Page column 199
(2009/03/07)
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- FXR agonist activity of conformationally constrained analogs of GW 4064
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Two series of conformationally constrained analogs of the FXR agonist GW 4064 1 were prepared. Replacement of the metabolically labile stilbene with either benzothiophene or naphthalene rings led to the identification of potent full agonists 2a and 2g.
- Akwabi-Ameyaw, Adwoa,Bass, Jonathan Y.,Caldwell, Richard D.,Caravella, Justin A.,Chen, Lihong,Creech, Katrina L.,Deaton, David N.,Madauss, Kevin P.,Marr, Harry B.,McFadyen, Robert B.,Miller, Aaron B.,Navas III, Frank,Parks, Derek J.,Spearing, Paul K.,Todd, Dan,Williams, Shawn P.,Bruce Wisely
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supporting information; experimental part
p. 4733 - 4739
(2010/06/12)
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