76074-88-9Relevant academic research and scientific papers
Intermediate for preparing medetomidine and its preparation method and use
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Paragraph 0090-0092, (2018/08/03)
The invention provides an intermediate for preparing medetomidine. The intermediate is a compound shown in the formula (I). The invention also provides a preparation method of the intermediate, and ause of the intermediate in the preparation of medetomidine. The compound shown in the formula (I) is used for preparation of medetomidine so that the raw material is cheap and easy to obtain, synthesis processes are simple, the reaction cycle is short, the environmental pollution is avoided, operation is simple, the harsh reaction conditions are avoided, the operation and post-treatment are simple, the yield and the product purity are high, the intermediate in each step is a solid and is easy to purify, a production cost is low, and the intermediate is suitable for industrial large-scale production and conforms to the principle of green chemistry.
Synthesis and antiproliferatory activity of ruthenium complexes containing N-heterocyclic carboxylates
Kennedy, David C.,James, Brian R.
, p. 32 - 36 (2017/03/11)
Solvates of the complexes Ru2Cl(pic)4(EtOH) (2), Ru(Im-CO2)3 (3), and Ru(Im-CO2)(Im-CO2H)Cl2 (4), were synthesized from reaction of RuCl3·3H2O or K3[RuCl6] with the N-heterocyclic carboxylic acids pyridine-2-carboxylic acid (picolinic acid, Hpic), and imidazole-4-carboxylic acid (Im-CO2H). Crystals of 2–4 could not be grown and hence characterization was done by elemental analysis, NMR, IR, and conductivity data; 2 and 4 were tested for antiproliferatory activity in vitro against a human breast cancer cell line, but were less active than, for example, Ru complexes containing bis-imidazole or 4,4′-biimidazole that we studied previously [see Can. J. Chem. 89 (2011) 948]. Preliminary work with a third potential ligand, 3-nitro-1,2,4-triazole-5-carboxylic acid (abbreviated HCANT), and other nitro heterocyclic compounds is also presented.
ALDOSTERONE SYNTHASE INHIBITOR
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Paragraph 0016; 0088; 0090, (2018/10/10)
PROBLEM TO BE SOLVED: To provide a compound having aldosterone synthase inhibition effect useful for treatment of primary aldosteronism causing hypertension or hypokalemia by overproduction of aldosterone, and a pharmaceuticals containing the compound. SOLUTION: There are provided an imidazole compound including 4-[5-(2-fluoroethyl)-1H-imidazole-1-ylmethyl]-3-iodobenzonitrile, 1-(3-bromo-4-cyanobenzyl)-1H-imidazole-5-carboxylic acid methyl, 1-(2-iodo-4-nitrobenzyl)-1H-imidazole-5-carboxylic acid methyl, 1-(3,5-di-tert-butylphenyl)-1H-imidazole-5-carboxylic acid methyl, 1-(2H-chromene-2-on-6-ylmethyl)-1H-imidazole-5-carboxylic acid methyl and 1-(2H-chromene-2-on-6-ylmethyl)-5-iodo-1H-imidazole as examples, and pharmaceuticals containing the compound. COPYRIGHT: (C)2015,JPOandINPIT
Synthesis, Biological Evaluation, and Molecular Modeling of 1 -Benzyl-1H-imidazoles as Selective Inhibitors of Aldosterone Synthase (CYP11B2)
Roumen, Luc,Peeters, Joris W.,Emmen, Judith M. A.,Beugels, Ilona P. E.,Custers, Erica M. G.,De Gooyer, Marcel,Plate, Ralf,Pieterse, Koen,Hilbers, Peter A. J.,Smits, Jos F. M.,Vekemans, Jef A. J.,Leysen, Dirk,Ottenheijm, Harry C. J.,Janssen, Henk M.,Rob Hermans
experimental part, p. 1712 - 1725 (2010/07/17)
Reducing aldosterone action is beneficial in various major diseases such as heart failure. Currently, this is achieved, with mineralocorticoid, receptor antagonists, however, aldosterone synthase (CYP 11B2) inhibitors may offer a promising alternative. In this study, we used three-dimensional modeling of CYP11B2 to model, the binding modes of the natural substrate 18-hydroxycorticosterone and the recently published CYP11B2 inhibitor R-fadrozole as a rational guide to design 44 structurally simple and achiral 1-benzyl-1H-imidazoles. Their syntheses, in vitro inhibitor potencies, and in silico docking are described. Some promising CYP11B2 inhibitors were identified, with our novel lead, MOERAS 115 (4-((5-phenyl-1H-imidazol-1-yl)methyl) benzonitrile) displaying an IC50 for CYP11B2 of 1.7 nM, and a CYP11B2 (versus CYP11B1) selectivity of 16.5, comparable to R-fadrozole (IC 50 for CYP11B26.0 nM, selectivity 19.8). Molecular docking of the inhibitors in the models enabled us to generate posthoc hypotheses on their binding modes, providing a valuable basis for future studies and further design of CYP11B2 inhibitors.
IMIDAZOLE CARBOXAMIDES
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Page/Page column 17, (2010/02/17)
The present invention provides certain imidazole carboxamide derivatives, pharmaceutical compositions thereof, methods of using the same and processes for preparing the same.
THIA-TRIAZA-CYCLOPENTAZULENES AS PI3-KINASES INHIBITORS FOR THE TREATMENT OF CANCER
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Page/Page column 29-30, (2010/11/05)
The present invention encompasses compounds of general formula (1) wherein 5 R1 to R3 and X are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and th
N-benzyl imidazole derivatives and their use as aldosterone synthase inhibitors
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Page/Page column 12, (2009/09/26)
The invention relates to the use of a N-benzyl 5-substituted imidazole derivative having the general formula I wherein R is (C1-3)alkyl, (C1-3)alkyloxy, halogen, nitro or cyano; R1 is (C1-6)alkyl, optionally substituted with OH, (C1-3)alkyloxy, (C1-3)alkylcarbonyloxy, (C1-3)alkyloxycarbonyl or halogen, or (C1-3)alkyloxycarbonyl; or R1 is phenyl, optionally substituted with 1-3 substituents independently selected from (C1-3)alkyl, (C1-3)alkyloxy, hydroxylmethyl and halogen; or a pharmaceutically acceptable salt thereof, for the preparation of a medicament for the treatment of a disorder or disease in a subject mediated by aldosterone synthase or responsive to inhibition of aldosterone synthase.
Amide substituted xanthine derivatives
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, (2008/06/13)
The present invention is a 1,3,8 substituted xanthine derivative of formula I or a pharmaceutically acceptable salt thereof, wherein R1, R2 and R3 are as defined in the specification. Compounds of formula I and pharmaceutically acceptable salts or prodrugs thereof show activity as modulators of gluconeogenesis.
AMIDE SUBSTITUTED XANTHINE DERIVATIVES WITH GLUCONEOGENESIS MODULATING ACTIVITY
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Page 111, (2012/04/23)
The present invention is a 1,3,8 substituted xanthine derivative of formula (I) or a pharmaceutically acceptable salt thereof, wherein R1, R2 and R3 are as defined in the specification. Compounds of formula (I) and pharmaceutically acceptable salts or prodrugs thereof show activity as modulators of gluconeogenesis.
1-(Aromatic- or heteroaromatic-substituted)-3-(heteroaromatic substituted)-1,3-propanediones and uses thereof
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Page 36-37, (2010/02/06)
Certain 1-(aromatic- or heteroaromatic-substituted-3-(heteroaromatic substituted)-1,3-propanediones are described as inhibitors of HIV integrase and inhibitors of HIV replication. These compounds are useful in the prevention or treatment of infection by HIV and the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.
