cas 161814-49-9, Amprenavir | Articles data

Articles about 161814-49-9Total 11 be found

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PROCESS FOR SYNTHESIS OF SYN AZIDO EPOXIDE AND ITS USE AS INTERMEDIATE FOR THE SYNTHESIS OF AMPRENAVIR and SAQUINAVIR
Disclosed herein is a novel route of synthesis of syn azide epoxide of formula 5, which is used as a common intermediate for asymmetric synthesis of HIV protease inhibitors such as Amprenavir, Fosamprenavir, Saquinavir and formal synthesis of Darunavir an
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(2015/02/18)

Enantioselective synthesis of HIV protease inhibitor amprenavir via Co-catalyzed HKR of 2-(1-azido-2-phenylethyl)oxirane
A short and efficient enantioselective synthesis of the HIV protease inhibitor amprenavir 1 (99% ee) as well as a formal synthesis of saquinavir 3 have been achieved in high enantiomeric purity starting from commercially available materials. Our strategy mainly comprises a Co-catalyzed two-stereocentred hydrolytic kinetic resolution (HKR) of racemic 2-(1-azido-2-phenylethyl)oxirane as the chirality inducing step. Also presented is a concise synthesis of (S)-3-hydroxytetrahydrofuran 4, the key structural feature, in high enantiomeric purity (98% ee).
Gadakh, Sunita K.,Santhosh Reddy,Sudalai, Arumugam
p. 898 - 903
(2012/09/22)

Methods for predicting the response to statins
The invention provides methods for optimizing therapeutic efficacy for treating hypercholesterolemia in a subject having a cardiovascular disease (CVD), comprising (a) determining subject characteristics that affect the likelihood of reaching a goal level of low density lipoprotein (LDL); and (b) obtaining success probabilities of a variety of statin treatments for reaching said goal level of LDL using said subject characteristics and a multivariate model; and (c) administrating the optimal statin treatment with the highest success probability of step (b) to said subject thereby optimizing therapeutic efficacy for treating hypercholesterolemia in said subject.
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(2011/10/13)

TREATMENT OF THE CNS EFFECTS OF HIV WITH VX-478, ALONE OR IN COMBINATION WITH AZT OR 3TC
Methods and compositions for treating the central nervous system (CNS) effects of HIV, particularly AIDS related dementia.
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Page/Page column 8

(2008/06/13)

Sulfonamide inhibitors of aspartyl protease
The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.
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Example 168

(2008/06/13)

Efficient method to prepare hydroxyethylamine-based aspartyl protease inhibitors with diverse P1 side chains
An efficient procedure for the solid-phase synthesis of hydroxyethylamine-based aspartyl protease inhibitors is described. The 1,2-bromo alcohol 4 is the key intermediate and is prepared in four-steps in good overall yield from commercial available amino acids.
Chino, Masao,Wakao, Masahiro,Ellman, Jonathan A
p. 6305 - 6310
(2007/10/03)

Synthesis of a chiral aziridine derivative as a versatile intermediate for HIV protease inhibitors.
[reaction: see text] Chiral aziridine derivative 1 was prepared from D-tartaric acid. This compound could be utilized as a common intermediate for the synthesis of hydroxyethylamine class HIV protease inhibitors such as saquinavir, amprenavir, or nelfinavir.
Kim,Bae,So,Yoo,Chang,Lee,Kang
p. 2349 - 2351
(2007/10/03)

Process for the synthesis of HIV protease inhibitors
An improved process for the synthesis of (3S)-tetrahydro-3-furyl N-[(1S,2R)-3 -(4-amino-N-isobutylbenzenesulphonamido)-1-benzyl-2-hydroxypropyl]carbamate comprising four steps form the compound of formula A and a novel intermediate thereto.
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(2008/06/13)

Potent HIV protease inhibitors incorporating high-affinity P2-ligands and (R)-(hydroxyethylamino)sulfonamide isostere
Design and synthesis of a series of very potent nonpeptide HIV protease inhibitors are described. The inhibitors are derived from novel high affinity P2-ligands and (R)-(hydroxyethylamino)sulfonamide isostere.
Ghosh, Arun K.,Kincaid, John F.,Cho, Wonhwa,Walters, D. Eric,Krishnan,Hussain, Khaja Azhar,Koo, Yumee,Cho, Hanna,Rudall, Clare,Holland, Louis,Buthod, Jim
p. 687 - 690
(2007/10/03)

SULFONAMIDE INHIBITORS OF ASPARTYL PROTEASE
The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.
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(2010/12/01)

SULFONAMIDE INHIBITORS OF ASPARTYL PROTEASE
The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.
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(2010/11/30)

Chemical Properties

Appearance/Colour :off-white to pale yellow
Melting Point: 72-74 °C
Density: 1.3 g/cm³
Solubility:DMSO: soluble20mg/mL, clear
Storage Temp.:-20°C Freezer
Refractive Index: 1.61
PKA: 11.54±0.46(Predicted)
PSA: 139.57000
LogP: 4.45570

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161814-49-9

Articles about 161814-49-9Total 11 be found

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Chemical Properties

Appearance/Colour :off-white to pale yellow

Melting Point: 72-74 °C

Density: 1.3 g/cm³

Solubility:DMSO: soluble20mg/mL, clear

Storage Temp.:-20°C Freezer

Refractive Index: 1.61

PKA: 11.54±0.46(Predicted)

PSA: 139.57000

LogP: 4.45570

Global suppliers and manufacturers of 161814-49-9total 88 suppliers on LookChem

Article Database

161814-49-9

Articles about 161814-49-9Total 11 be found

More Articles about upstream products of 161814-49-9

Chemical Properties

Appearance/Colour :off-white to pale yellow

Melting Point: 72-74 °C

Density: 1.3 g/cm3

Solubility:DMSO: soluble20mg/mL, clear

Storage Temp.:-20°C Freezer

Refractive Index: 1.61

PKA: 11.54±0.46(Predicted)

PSA: 139.57000

LogP: 4.45570

Global suppliers and manufacturers of 161814-49-9total 88 suppliers on LookChem

Density: 1.3 g/cm³