- NEW BICYCLIC DERIVATIVES HAVING BETA2 ADRENERGIC AGONIST AND M3 MUSCARINIC ANTAGONIST ACTIVITIES
-
The present invention relates to novel compounds having β2 adrenergic agonist and M3 muscarinic antagonist dual activity, to pharmaceutical compositions containing them, to the process for their preparation and to their use in respiratory therapies.
- -
-
Page/Page column 68
(2016/04/20)
-
- TYK2 INHIBITORS AND USES THEREOF
-
The present invention provides compounds, compositions thereof, and methods of using the same for the inhibition of TYK2, and the treatment of TYK2-mediated disorders.
- -
-
Paragraph 001078; 001079
(2015/09/28)
-
- The effect of dye structure on the dyeing and optical properties of dichroic dyes for PVA polarizing film
-
The dyeing behaviour and optical properties of four novel dyes in PVA polarizing films were determined in terms of the linearity, hydrogen bonding ability, intermolecular interaction and transition moment. The linearity and H-bonding ability of the dyes w
- Chang, Jae Bok,Hwang, Jong Hak,Park, Jong S.,Kim, Jae Pil
-
experimental part
p. 366 - 371
(2011/06/21)
-
- IMIDAZOLOPYRAZINE COMPOUNDS USEFUL FOR THE TREATMENT OF DEGENERATIVE AND INFLAMMATORY DISEASES
-
Novel imidazo[1,2-a]pyrazine compounds are disclosed that have a formula ( I ) represented by the following:The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, arthritis, inflammation, and others.
- -
-
Page/Page column 56-57
(2008/06/13)
-
- AZAINDOLE DERIVATIVES AS INHIBITORS OF P38 KINASE
-
The invention is directed to methods to inhibit p38 kinase, preferably p38-α using compounds which are azaindoles wherein the azaindoles are coupled through an azacyclic linker to another cyclic moiety.
- -
-
Page/Page column 81
(2010/11/24)
-
- Comparison of two synthetic methods to obtain [18F] N-(2-aminoethyl)-5-fluoropyridine-2-carboxamide, a potential MAO-B imaging tracer for PET
-
The compound Ro 19-6327, N-(2-aminoethyl)-5-chloropyridine-2-carboxamide, is known to inhibit reversibly and site specifically the enzyme monoamine oxidase B (MAO-B). The 123I-labelled iodo-analogue N-(2-aminoethyl)-5-iodopyridine-2-carboxamide (Ro 43-0463) was investigated successfully in human volunteers by means of SPET (Single Photon Emission Tomography). We developed therefore the synthesis and radiolabelling of the corresponding fluoro-analogue N-(2-aminoethyl)-5-fluoropyridine-2-carboxamide with 18F in order to carry out PET (Position Emission Tomography) investigations of MAO-B related neuropsychiatric diseases. For this purpose two synthetic approaches leading to the electrophilic and the nucleophilic methods of 18F radiolabelling were undertaken. The nucleophilic approach appeared to be superior when factors such as precursor synthesis, beam time, specific activity and radiochemical purity of the product are considered.
- Beer,Haerberli,Ametamey,Schubiger
-
p. 933 - 945
(2007/10/02)
-
- Aminopyridine compounds
-
An aminopyridine compound represented by the formula: STR1 wherein n represents 0 or 1; Z represents =S, =O, =NCN or =CHNO2 ; R1 represents --CN, --NR3 R4, --CONR3 R4, --NHNR3 R4, --NHCONHR3, --NHSO2 R3 or --SR3 ; R2 represents H, or substituted or unsubstituted alkyl; R3 and R4, which may be the same or different, represent H, substituted or unsubstituted alkyl, aryl, substituted or unsubstituted acyl or alkoxycarbonyl group; and R3 and R4 may form a heterocyclic ring together with a nitrogen atom to which R3 and R4 are bound, through another heteroatom or without it; or an acid salt thereof, which is excellent in pharmacological effect and repressed in side effects as a drug for circulatory diseases.
- -
-
-
- The preparation of Some 4- and 5-Substituted Pyridine-2-carboxylic Acids as Fusaric Acid Analogues.
-
In view of future studies on the structure-activity relationships involved in the inhibition of dopamine β-hydroxylase, the authors synthetized 5-substituted picolinic acids and 4-substituted fusaric acids selected by means of a random sampling procedure suited for small series.On this occasion, they succeeded in improving markedly the well-known synthesis of 5-nitropicolinic acid via a Rosenmund-v.Braun reaction with 2-bromo-5-nitropyridine. 5-Hydroxypicolinic acid which is easily accessible in the same way could be converted into 5-alkyloxypicolinic acids by reaction with alkyl halides in DMSO in the presence of silver oxide. 4-Substituted fusaric acids became accessible via 5-n-butyl-2-methyl-4-nitropyridine-N-oxide.
- Oehlke, J.,Schroetter, E.,Dove, S.,Schick, H.,Niedrich, H.
-
p. 591 - 596
(2007/10/02)
-
