1.
Eriksson, Leif A., 1964-, et al.
(författare)
Tetrazole derivatives as cytochrome p450 inhibitors
2019
Patent (populärvet., debatt m.m.) abstract
According to the invention there is provided a compound of formula I, wherein R1 and R2 have meanings given in the description, which compounds are useful in the treatment of skin disorders and other diseases.
2.
Ragno, Rino, et al.
(författare)
Structure-based modeling and target-selectivity prediction
2014
Patent (populärvet., debatt m.m.) abstract
The present invention provides, inter alia, methods, models, and systems for selecting an effector having specificity for a target molecule. The methods and systems of the present invention involve several steps, including compiling a database containing structural data for a library of molecules and a population of ligands and activity data, establishing structure-based equivalence of sequence elements in the library of molecules, determining likely spatial orientations of population ligands in library molecules, calculating interaction energies for each ligand-molecule pair, generating statistical models that are predictive of sequence elements likely to contribute to a differential effect of ligands on molecules, selecting an effector that is likely to have a desired specificity for the target molecule, experimentally determining activity data for effector-library molecule pairs, and at least once repeating the steps listed above wherein the effector is a member of the population of ligands.
3.
Svenson, Johan
(författare)
På jakt efter nya läkemedel i Ishavet
2016
Ingår i: Naturvetare. - : Naturvetarna. - 2000-2424. ; 6, s. 24-28
Tidskriftsartikel (populärvet., debatt m.m.) abstract
Ungefär en tredjedel av alla läkemedel har sin källa i naturen. Forskaren Johan Svenson skriver själv om sin expedition i Arktis, där forskarna samlar in alger och andra organismer i sökandet efter nya molekyler, som till exempel kan bli ny antibiotika.
4.
Vinge, Ellen
(författare)
Glukosamin för lindring av besvär vid artros
2005
Ingår i: Tidsskrift for den Norske Laegeforening. - 0807-7096. ; 125:12, s. 8-1667
Tidskriftsartikel (populärvet., debatt m.m.) abstract
Glukosamin ingår i glykosaminoglykaner i ledbrosk och synovialvätska. Tidigare gavs glukosamin som kosttillskott, men det klassificeras numera som ett icke-steroidliknande, antiinflammatoriskt läkemedel. Det beror på att flera kliniska studier har visat att glukosamin kan ge symtomlindring hos en del patienter med lätt till måttlig knäartros. Det brukar ta 2 - 4 veckor innan symtomlindringen kan mätas. Det är oklart om långtidsbehandling med glukosamin kan ge skydd mot fortsatt degeneration av brosket.
5.
Aahlin, Kristofer, et al.
(författare)
Preparation of 1-(4-(5-amino-6-(oxazolo[4,5-c]pyridin-2-yl)pyrazin-2-yl)benzoyl)piperazine derivatives as glycogen synthase kinase 3 inhibitors.
2011
Patent (populärvet., debatt m.m.) abstract
Title compds. I [R1 = H or Me], and their pharmaceutically acceptable salts, are prepd. and disclosed as glycogen synthase kinase 3 (GSK3) inhibitors. Thus, e.g., II was prepd. by cyclization of 3-amino-N-(4-hydroxypyridin-3-yl)pyrazine-2-carboxamide (prepn. given) to get intermediate 3-(oxazolo[4,5-c]pyridin-2-yl)pyrazin-2-amine, which underwent bromination followed by Suzuki reaction with (4-methylpiperazin-1-yl)(4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl)methanone. Compds. of the invention were tested for their selective inhibitory activity of GSK3β, e.g., II exhibited Ki value of 2.3 nM. The invention compds. are useful for the treatment of cognitive disorders, diabetes, cancer, etc. [on SciFinder(R)]
6.
Antonov, D, et al.
(författare)
HCV inhibiting macrocyclic phenylcarbamates
2008
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.
7.
Arvidsson, Per I., et al.
(författare)
Preparation of imidazolylpyrimidine derivatives for treatment of glycogen synthase kinase 3 related disorders such as Alzheimer's disease.
2010
Patent (populärvet., debatt m.m.) abstract
Title compds. I [R1 = H or F; R2 and R3 independently = H or Me], and their pharmaceutically acceptable salts, are prepd. and disclosed as agents for treatment of glycogen synthase kinase 3 (GSK3) related disorders such as Alzheimer's disease. Thus, e.g., II.HCl was prepd. by reductive amination of 4-bromo-3-fluorobenzaldehyde with (S)-3-methylmorpholine followed by amination with 2-amino-5-fluoro-4-(2-methyl-1-(tetrahydro-2H-pyran-4-yl)-1H-imidazol-5-yl)pyrimidine. Select I were evaluated for GSK3β inhibitory activity, and e.g., II·HCl demonstrated a Ki value of 30 nM. [on SciFinder(R)]
8.
Arvidsson, Per, et al.
(författare)
Preparation of arylimidazopyridine derivatives for use as GSK3 modulators.
2008
Patent (populärvet., debatt m.m.) abstract
Title compds. I [A = (un)substituted aryl or heteroaryl; Q = halo; R1 = C(O)NR6R7; R2 and R4 independently = H, halo, CN, NO2, alkyl, or haloalkyl; R3 and R5 independently = H, halo, alkyl, or haloalkyl; R6 and R7 = together with the atoms to which they are attached form an (un)substituted heterocyclic ring contg. one or more heteroatoms selected from N, O, or S;], and their pharmaceutically acceptable salts, are prepd. and disclosed as glycogen synthase kinase-3 (GSK3) modulators. Thus, e.g., II•HCl was prepd. by cyclocondensation of 5-bromopyridine-2,3-diamine with terephthalic monomethyl ester followed by chlorination, iodination, sapon., amidation with N-methylpiperazine, and coupling with 4-methoxyphenyl boronic acid. I were evaluated in GSK3β scintillation proximity assays, e.g., II•HCl demonstrated an Ki value of 97 nM. [on SciFinder(R)]
9.
Arvidsson, Per, et al.
(författare)
Preparation of imidazopyridinecarboxamide derivatives for use as GSK3 modulators.
2008
Patent (populärvet., debatt m.m.) abstract
Title compds. I [Q = halo; R1 = CH2NR3R4; each R2 independently = H or alkyl; R3 and R4 = together with the atoms to which they are attached form an (un)substituted heterocyclic ring contg. one or more heteroatoms selected from N, O, or S; R6 = H or alkyl; R7 = H, (un)substituted alkyl, alkylaryl, aryl, or heteroaryl], and their pharmaceutically acceptable salts, are prepd. and disclosed as glycogen synthase kinase-3 (GSK3) modulators. Thus, e.g., II•HCl was prepd. by cyclocondensation of 5-bromopyridine-2,3-diamine with terephthalic monomethyl ester followed by chlorination, iodination, sapon., amidation with morpholine, redn., and coupling with carbon monoxide and 3-methoxy-1-propanamine. I were evaluated in GSK3β scintillation proximity assays, e.g., II•HCl demonstrated an Ki value of 390 nM. [on SciFinder(R)]
10.
Ayesa, S., et al.
(författare)
CYSTEINE PROTEASE INHIBITORS
2011
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.
