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 NO ET HYPERTENSION

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5 participants
AuteurMessage
bob




Nombre de messages : 506
Age : 71
Localisation : YONNE
Date d'inscription : 17/11/2007

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MessageSujet: NO ET HYPERTENSION   NO ET HYPERTENSION Icon_minitimeVen 2 Mar - 14:50

Une synthèse 2012 interessante sur les recherches concernant les antihypertenseurs

On y parle de merck :nicox
et du role croissant des moles+NO

entre autre page 54 tableau des brevets merck correspondants

cdt

http://www.future-science.com/doi/pdf/10.4155/ppa.12.5
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Raymond




Nombre de messages : 170
Date d'inscription : 30/04/2011

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MessageSujet: Re: NO ET HYPERTENSION   NO ET HYPERTENSION Icon_minitimeVen 2 Mar - 16:56

Merci beaucoup! Très intéressant.
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Gregdu12




Nombre de messages : 69
Date d'inscription : 27/08/2010

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MessageSujet: Re: NO ET HYPERTENSION   NO ET HYPERTENSION Icon_minitimeVen 2 Mar - 23:01

oui tres bien mais pas d'impact sur l'action
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Seb

Seb


Nombre de messages : 751
Age : 51
Localisation : 64122 URRUGNE
Date d'inscription : 27/08/2010

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MessageSujet: Re: NO ET HYPERTENSION   NO ET HYPERTENSION Icon_minitimeSam 3 Mar - 2:07

Merci bob,





NicOx has described analogs of isosorbide mononitrate , nous les retrouvons dans les nouvelles molécules de Merck/hypertention
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vinsse

vinsse


Nombre de messages : 515
Date d'inscription : 15/05/2008

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MessageSujet: p52 53 merck et nicox patents 2007 2011 review   NO ET HYPERTENSION Icon_minitimeMar 6 Mar - 11:02

http://www.future-science.com/doi/pdf/10.4155/ppa.12.5
(je ne vous colle pas les mol et le reste voir le doc)

A combination of Ang II receptor blockade with
NO-donating activity may be effective in treating resistant
hypertension in patients with elevated SBP, primarily
the elderly [23,24]. These patients have impaired
endothelial
function, resulting in diminished formation
of NO. ARBs have been shown to improve endothelium
function and increase endogenous NO formation.
ARB/NO donors have been disclosed by three companies,
two of which (Merck and NicOx) were joint
assignees on many applications as part of a research collaboration.
ARB/NO donors from Merck and NicOx
were derived by linking ARBs with NO-releasing
moieties via ester groups or other ‘soft’ functionalities
(Figure 6; compounds 7 and Cool [108,109]. These ARB/NO
donors are prodrugs that must undergo metabolism
(mostly ester hydrolysis) to liberate the pharmacologically
active ARB species. Compound 8 with two nitrooxy
groups was shown to decrease SBP in the conscious
spontaneously hypertensive rat (SHR) over a 24-h period,
in contrast to compounds such as 9 with only a single
nitrooxy group, which did not show significant blood
pressure-lowering activity in the SHR at the 24-h time
point. NicOx has patented a series of ARB/NO donors
such as 10, which are claimed to be long-acting agents,
with potent in vitro activity in isolated rabbit thoracic
preparations and extended pharmacological activity in
the SHR [110]. NitroMed
has identified a series of valsartan
analogs with nitrooxy groups such as 11, which
exhibit potent affinity in an Ang II receptor-binding assay
(Figure 7) [111]. Merck has also investigated a series of
diazeniumdiolates such as 12, which can be metabolized
in vivo to give an ARB and an intermediate
capable of releasing two
molecules of NO under physiological
conditions [112]. The formation
of NO from diazeniumdiolates has
been recently reviewed [25].
The ARB/NO donors are part
of a broader class of NO pathway
modulators that saw considerable
patent activity between 2007 and
2011, including endothelial NO
synthase upregulators, PDE5 inhibitors,
sGC activators and a variety
of other NO-donating agents
(Figure 8 & Supplementary Table 2).
Summaries of the pharmacology
underlying the different drug
classes in the NO pathway and a
description of the role of NO as a
vasodilating agent are provided in
the section ‘NO pathway modulators’.
Non-NO donor modulators
of this pathway may address one
of the shortcomings associated
with nitrate (NO-donating) monotherapy
(i.e., the development of
tolerance) that has prevented more
widespread use of the therapy.
In the NO pathway, four drug
classes attracted the most interest,
including sGC activators, PDE5
inhibitors, ARB/NO donors and
endothelial NO synthase upregulators,
with patent counts of 22,
18, 13 and eight applications, respectively.
Novel diuretic agents
and PDE3 inhibitors with NOdonating
capacity were also disclosed,
although the patent counts
were low.
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Seb

Seb


Nombre de messages : 751
Age : 51
Localisation : 64122 URRUGNE
Date d'inscription : 27/08/2010

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MessageSujet: Re: NO ET HYPERTENSION   NO ET HYPERTENSION Icon_minitimeMar 6 Mar - 11:47

Merci vinsse!!! sûrement un frère du brevet ci-dessous.



Application Number: 09747197 Application Date: 06.05.2009
Publication Number: 2291076 Publication Date: 09.03.2011
Publication Kind : A1

IPC: A61K 31/445
A01N 43/40
A01N 43/50
Applicants: MERCK SHARP & DOHME
NICOX SA
Inventors: ALI AMJAD
LO MICHAEL MAN-CHU
SEBHAT IYASSU K
FRANKLIN CHRIS
ALMIRANTE NICOLETTA
STEFANINI SILVIA
BIONDI STEFANO
ONGINI ENNIO
Priority Data: 12780708 15.05.2008 US
2009042951 06.05.2009 US
Title: (FR) ANTAGONISTES DU RÉCEPTEUR DE L'ANGIOTENSINE LL
(EN) ANGIOTENSIN II RECEPTOR ANTAGONISTS
(DE) ANGIOTENSIN-II-REZEPTORANTAGONISTEN
Abstract:
(FR) L'invention porte sur un composé présentant une structure dans laquelle: R est par exemple (i), Y est sélectionné parmi: 1) R5, 2) -C(R1R2)(C(R3R4))0-1Y1R5, et 3) -C(R1R2)-O-Y1R5; R1, R2, R3 et R4 sont sélectionnés indépendamment parmi hydrogène et C1-4 alkyle; R5 est (ii); Y1 est sélectionné parmi C(O)-O- et P(O)(OR6)-O-; et R6 est hydrogène ou CH3, ou l'un de ses composés pharmacocompatibles. L'invention porte également sur l'utilisation desdits composés pour traiter l'hypertension.
(EN) A compound having the structure wherein R is, for example, Y is selected from the group consisting of 1) R5, 2) -C(R1R2)(C(R3R4))0-1Y1R5, and 3) -C(R1R2)-O-Y1R5; R1, R2, R3 and R4 are independently selected from the group consisting of hydrogen and C1-4 alkyl; R5 is; Y1 is selected from the group consisting of C(O)-O- and P(O)(OR6)-O-; and R6 is hydrogen or CH3, or a pharmaceutically acceptable salt thereof, and methods of using the compounds for treating hypertension.
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