63050-11-3Relevant academic research and scientific papers
A cocktail of165Er(iii) and Gd(iii) complexes for quantitative detection of zinc using SPECT and MRI
Malikidogo, Kyangwi P.,Da Silva, Isidro,Morfin, Jean-Fran?ois,Lacerda, Sara,Barantin, Laurent,Sauvage, Thierry,Sobilo, Julien,Lerondel, Stéphanie,Tóth, éva,Bonnet, Célia S.
supporting information, p. 7597 - 7600 (2018/07/15)
We propose quantitative assessment of zinc by combining nuclear and MR imaging. We use a cocktail of a Gd3+-complex providing a Zn2+-dependent MRI response and its165Er3+ analogue allowing for concentration assessment.165Er is readily obtained in a cyclotron and purified, which is indispensable for successful quantification of metal ions.
DUAL NAV1.2/5HT2A INHIBITORS FOR TREATING CNS DISORDERS
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Paragraph 0145; 0279, (2018/03/28)
Compounds of formula I: I are disclosed, as are pharmaceutical compositions containing such compounds. Methods of treating neurological or psychiatric disorders in a patient in need are also disclosed. Such disorders include depression, bipolar disorder, pain, schizophrenia, obsessive compulsive disorder, addiction, social disorder, attention deficit hyperactivity disorder, an anxiety disorder, autism, a cognitive impairment, or a neuropsychiatric symptom such as apathy, depression, anxiety, psychosis, aggression, agitation, impulse control disorders, and sleep disorders in neurological disorders such as Alzheimer's and Parkinson's diseases.
HETEROCYCLIC COMPOUND AND H1 RECEPTOR ANTAGONIST
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Paragraph 0184; 0185; 0186, (2013/04/13)
A heterocyclic compound useful as an antiallergic agent is provided. A compound represented by the following formula (1) or a salt thereof: wherein the ring A is a homocyclic or heterocyclic ring; the ring B is a heterocyclic ring which contains G and nitrogen atom N as constituent atoms thereof, wherein G is CH or N; R1 is a carbonyl group or an alkylene group; R2a and R2b are an alkyl group, a cycloalkyl group, an aryl group, or a heterocyclic group; X is an oxygen atom or a sulfur atom; Z is a hydroxyl group, an alkoxy group, a cycloalkyloxy group, an aryloxy group, an aralkyloxy group, an amino group, or an N-substituted amino group; and n is 0 or 1; with the proviso that when the ring A is a benzene ring or when the ring B is a piperazine ring, R1 is an alkylene group which may have a substituent.
TETRACYCLIC COMPOUND
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Page/Page column 47, (2011/04/25)
Provided are a tetracyclic compound represented by the formula (I): [in the formula(I),the formula (A) represents a benzene ring or the like, X represents CH or a nitrogen atom, Q represents -O- or the like, R1, R2, and R3 may be the same or different and each represent a hydrogen atom or the like, 1, m, and n each represent an integer from one to the maximum substitutable number of substituents, and R4 and R5 may be the same or different and each represent a hydrogen atom or the like], or a pharmaceutically acceptable salt thereof, and the like.
BENZAZEPINE DERIVATIVES FOR THE TREATMENT OF CENTRAL NERVOUS SYSTEM DISORDERS
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Page/Page column 28-29, (2011/08/03)
A compound having the formula (1) wherein: Ra represents C1-6 alkyl, cyclobutyl or cyclopentyl; R1 represents H or C1-6 alkyl; R2 represents H or R1 and R2 together represent =0; X1 represents CR3 or N; X2 represents CR4 or N; X3 represents CR5 or N; X4 represents CR6 or N; wherein one or two of X1, X2, X3 and X4 represents N; R3, R4, R5 and R6 each independently represent H, C1-6 alkoxy or -NR7R8; R7 and R8 independently represent H or C1-6 alkyl; or R7 and R8 and the N atom to which they are attached are joined to form a N-containing heterocyclyl ring optionally substituted with one or more substituents independently selected from halogen, C1-6 alkyl and C1-6 alkoxy; or a pharmaceutically acceptable salt thereof, is provided. Compounds of the invention have been found to modulate the histamine H3 receptor.
Design, synthesis, and biological evaluation of AT1 angiotensin II receptor antagonists based on the pyrazolo[3,4-b]pyridine and related heteroaromatic bicyclic systems
Cappelli, Andrea,Nannicini, Chiara,Gallelli, Andrea,Giuliani, Germano,Valenti, Salvatore,Mohr, Galla Pericot,Anzini, Maurizio,Mennuni, Laura,Ferrari, Flora,Caselli, Gianfranco,Giordani, Antonio,Peris, Walter,Makovec, Francesco,Giorgi, Gianluca,Vomero, Salvatore
, p. 2137 - 2146 (2008/12/20)
Novel AT1 receptor antagonists bearing the pyrazolo[3,4-b] pyridine bicyclic heteroaromatic system (or structurally related moieties) were designed and synthesized as the final step of a large program devoted to the development of new antihypertensive agents and to the understanding of the molecular basis of their pharmacodynamic and pharmacokinetic properties. The preliminary pharmacological characterization revealed nanomolar AT1 receptor affinity for several compounds of the series and a potent antagonistic activity in isolated rabbit aortic strip functional assay for 7c and 8a. These results stimulated the study of the biopharmaceutical properties of some selected compounds, which were found to be characterized by a permeability from medium to high. Remarkably, the least permeable 7c showed both permeability and oral bioavailability (80%) higher than losartan, but its terminal half-life was shorter. These results suggest that the permeability is not a limiting factor in the pharmacokinetics of these AT1 receptor antagonists.
PYRIDINE DERIVATIVES AS DIPEPTEDYL PEPTIDASE INHIBITORS
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Page/Page column 60, (2008/06/13)
The present invention is directed to compounds of formula (I) or a pharmaceutically acceptable salt thereof; wherein A is (1); X is selected from CH, CF and N; R5 is selected from H, C1-C6 alkyl, C1-C6 fluoroalk
Dipeptidyl peptidase-IV inhibitors
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Page/Page column 26, (2010/02/14)
The invention provides compounds of Formula (I) or prodrugs thereof, or pharmaceutically acceptable salts of said compounds or prodrugs, or solvates of said compounds, prodrugs or salts, wherein A, N, X and R1 are as defined herein; pharmaceutical compositions thereof; and methods of using the pharmaceutical compositions for the treatment of diseases, including Type 2 diabetes, Type 1 diabetes, impaired glucose tolerance, hyperglycemia, metabolic syndrome (syndrome X and/or insulin resistance syndrome), glucosuria, metabolic acidosis, arthritis, cataracts, diabetic neuropathy, diabetic nephropathy, diabetic retinopathy, diabetic cardiomyopathy, obesity, conditions exacerbated by obesity, hypertension, hyperlipidemia, atherosclerosis, osteoporosis, osteopenia, frailty, bone loss, bone fracture, acute coronary syndrome, short stature due to growth hormone deficiency, infertility due to polycystic ovary syndrome, anxiety, depression, insomnia, chronic fatigue, epilepsy, eating disorders, chronic pain, alcohol addiction, diseases associated with intestinal motility, ulcers, irritable bowel syndrome, inflammatory bowel syndrome; short bowel syndrome; and the prevention of disease progression in Type 2 diabetes.
Novel heterocyclic compounds, method for preparing same and use thereof as medicines, in particular as antibacterial agents
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Page/Page column 66, (2010/02/14)
The invention relates to new heterocyclic compounds of general formula (I), and their salts with a base or an acid: The invention also relates to a process for the preparation of these compounds, as well as their use as medicaments, in particular as anti-bacterial agents.
Chiral NADH models with restricted or blocked rotation at the amide function: Attempts to interpret the mechanism of the enantioselective hydrogen transfer to methyl benzoylformate
Vitry, Christiane,Bédat, Joelle,Prigent, Yann,Levacher, Vincent,Dupas, Georges,Salliot, Isabelle,Quéguiner, Guy,Bourguignon, Jean
, p. 9101 - 9108 (2007/10/03)
Various NADH models with the following characteristics were studied and compared with previously reported models: (1) use of (S)-phenylalaninol as chiral auxiliary; (2) orientation in or out of the plane of the amide carbonyl. Despite the occurrence of apparently similar characteristics, they gave very different results in the asymmetric reduction of methyl benzoylformate. A detailed NMR study was performed in order to explain the behaviour of these models.
