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- RABOISSON, P. J. B., et al.
(författare)
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PYRIMIDINE SUBSTITUTED MACROCYCLIC HCV INHIBITORS
- 2008
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Patent (populärvet., debatt m.m.)abstract
- Compounds of the Formula (I) including a stereoisomer thereof, or an N-oxide, a pharmaceutically acceptable addition salt, or a pharmaceutically acceptable addition solvate thereof; useful as HCV inhibitors; processes for preparing these compounds as well as pharmaceutical compositions comprising these compounds as active ingredient.
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- Antonov, D, et al.
(författare)
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HCV inhibiting macrocyclic phenylcarbamates
- 2008
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Patent (populärvet., debatt m.m.)abstract
- Compounds of the formula I: including a stereoisomer thereof, or an N-oxide, a pharmaceutically acceptable addition salt, or a pharmaceutically acceptable addition solvate thereof; useful as HCV inhibitors; processes for preparing these compounds as well as pharmaceutical compositions comprising these compounds as active ingredient.
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- Simmen, K. A., et al.
(författare)
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Macrocylic inhibitors of hepatitis C virus
- 2012
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Patent (populärvet., debatt m.m.)abstract
- Inhibitors of HCV replication of formula (I)and the N-oxides, salts, and stereoisomers, whereineach dashed line represents an optional double bond;X is N, CH and where X bears a double bond it is C;R1 is —OR7, —NH—SO2R8;R2 is hydrogen, and where X is C or CH, R2 may also be C1-6alkyl;R3 is hydrogen, C1-6alkyl, C1-6alkoxyC1-6alkyl, C3-7cycloalkyl;R4 is aryl or Het; n is 3, 4, 5, or 6;R5 is halo, C1-6alkyl, hydroxy, C1-6alkoxy, phenyl, or Het;R6 is C1-6alkoxy, or dimethylamino;R7 is hydrogen; aryl; Het; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl, aryl or with Het;R8 is aryl; Het; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl, aryl or with Het;aryl is phenyl optionally substituted with one, two or three substituents;Het is a 5 or 6 membered saturated, partially unsaturated or completely unsaturated heterocyclic ring containing 1 to 4 heteroatoms selected from nitrogen, oxygen and sulfur, and being optionally substituted with one, two or three substituents;pharmaceutical compositions containing compounds (I) and processes for preparing compounds (I). Bioavailable combinations of the inhibitors of HCV of formula (I) with ritonavir are also provided.
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| 16. |
- Ayesa, S., et al.
(författare)
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CYSTEINE PROTEASE INHIBITORS
- 2011
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Patent (populärvet., debatt m.m.)abstract
- Compounds of the formula IwhereinR1a is H; and R1b is C1-C6 alkyl, Carbocyclyl or Het; orR1a and R1b together define a saturated cyclic amine with 3-6 ring atoms;R2a and R2b are H, halo, C1-C4alkyl, C1-C4haloalkyl, C1-C4alkoxy; orR2a and R2b together with the carbon atom to which they are attached form a C3-C6cycloalkyl;R3 is a branched C5-C10alkyl chain, C2-C4haloalkyl or C3-C7cycloalkylmethyl,R4 is Het, Carbocyclyl,optionally substituted as defined in the specification and pharmaceutically acceptable salts,hydrates and N-oxides thereof; are inhibitors of cathepsin S and have utility in the treatment of psoriasis, autoimmune disorders and other disorders such as asthma, arteriosclerosis, COPD and chronic pain.
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- Belfrage, B., et al.
(författare)
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Performance and interpretation of spirometry among Swedish hospitals
- 2016
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Ingår i: Clinical Respiratory Journal. - : Wiley. - 1752-6981 .- 1752-699X. ; 10:5, s. 567-573
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Tidskriftsartikel (refereegranskat)abstract
- Background and Aims: It is unclear to what extent spirometric performance and interpretation is standardized in Sweden. The aim of this study was to find out how spirometry is performed and interpreted in large Swedish hospitals. Methods: In telephone interviews, technicians and physicians working with lung function measurements at 21 large Swedish hospitals were interviewed about routines for spirometry. Results: Answers were obtained from 37 of the 42 departments contacted revealing differences in the spirometric routines. Some departments lack a written method description, and three different prediction equations were used among the departments. Different ways of calculating the forced expiratory volume in 1 s (FEV1)/vital capacity (VC) ratio (FEV%) were found and also differences in performance and interpretation of the reversibility test. When diagnosing chronic obstructive pulmonary disease, none of the departments reported using an individualized diagnostic limit of FEV1/VC based on age, sex and height. Conclusion: There is a need for standardization of performance and interpretation of the spirometry test in Sweden and probably also in other countries. © 2014 John Wiley & Sons Ltd
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| 21. |
- Brem, Jürgen, et al.
(författare)
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Imitation of β-lactam binding enables broad-spectrum metallo-β-lactamase inhibitors
- 2022
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Ingår i: Nature Chemistry. - : Springer Nature. - 1755-4330 .- 1755-4349. ; 14:1, s. 15-24
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Tidskriftsartikel (refereegranskat)abstract
- Carbapenems are vital antibiotics, but their efficacy is increasingly compromised by metallo-β-lactamases (MBLs). Here we report the discovery and optimization of potent broad-spectrum MBL inhibitors. A high-throughput screen for NDM-1 inhibitors identified indole-2-carboxylates (InCs) as potential β-lactamase stable β-lactam mimics. Subsequent structure-activity relationship studies revealed InCs as a new class of potent MBL inhibitor, active against all MBL classes of major clinical relevance. Crystallographic studies revealed a binding mode of the InCs to MBLs that, in some regards, mimics that predicted for intact carbapenems, including with respect to maintenance of the Zn(II)-bound hydroxyl, and in other regards mimics binding observed in MBL-carbapenem product complexes. InCs restore carbapenem activity against multiple drug-resistant Gram-negative bacteria and have a low frequency of resistance. InCs also have a good in vivo safety profile, and when combined with meropenem show a strong in vivo efficacy in peritonitis and thigh mouse infection models.
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| 22. |
- Casper, CHE, et al.
(författare)
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Link between the X4 phenotype in human immunodeficiency virus type 1-infected mothers and their children, despite the early presence of R5 in the child
- 2002
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Ingår i: Journal of Infectious Diseases. - : Oxford University Press (OUP). - 1537-6613 .- 0022-1899. ; 186:7, s. 914-921
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Tidskriftsartikel (refereegranskat)abstract
- Coreceptor use was determined for human immunodeficiency virus type 1 (HIV-1) isolates of various subtypes from 11 women during pregnancy and their infected children. Isolates from peripheral blood mononuclear cells (n = 79) and from plasma (n = 59) were available. The clinical and immunological stages of HIV-1 infection were recorded. Coreceptor use was tested on human cell lines expressing CD4 and different chemokine receptors. The R5 virus predominated, and only 9 isolates from 2 mothers used CXC chemokine receptor 4. All children carried the R5 virus at the time of diagnosis of HIV-1 infection. In 2 children of mothers carrying the X4 virus, the virus switched from R5 to X4 or to R5X4 by age 18 months (child no. 9) and age 48 months (child no. 10), whereas no children followed up to a similar age whose mothers were carrying the R5 virus experienced such a switch (). This points to a link between the P = .048 presence of X4 virus in the mother and the emergence of X4 virus in her child.
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| 24. |
- Fredrikson, G, et al.
(författare)
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Use of protein G for preparation and characterization of rabbit antibodies against rat adipose tissue hormone-sensitive lipase
- 1987
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Ingår i: Journal of Immunological Methods. - : Elsevier BV. - 0022-1759. ; 97:1, s. 65-70
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Tidskriftsartikel (refereegranskat)abstract
- The newly described immunoglobulin G-binding streptococcal surface protein, protein G, was used to prepare and characterize rabbit antibodies. The antibodies were directed against rat hormone-sensitive lipase, the rate-limiting enzyme in the hydrolysis of the triacylglycerols stored in adipose tissue. Antiserum was obtained after two injections with 20 micrograms enzyme protein, and the immunoglobulin fraction was obtained using a protein G-based solid-phase radioimmunoassay. The hydrolysis of acylglycerols by the enzyme was inhibited by the antibodies, and the enzyme could be efficiently removed from a solution using the antibodies and heat-killed streptococci expressing surface protein G. By Western blot and detection with 125I-protein G, the antibodies were found to selectively bind to hormone-sensitive lipase and to a smaller extent to two minor contaminants, possibly proteolytic fragments of the lipase. The amount of 125I-labelled protein G bound to the lipase on the blot was quantitatively related to the amount of enzyme protein down to the detection limit 10 ng.
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