40570-64-7Relevant academic research and scientific papers
Novel 5-hydroxytryptamine and norepinephrine dual reuptake inhibitor and medical application thereof
-
Paragraph 0058; 0060-0061, (2020/07/06)
The invention belongs to the field of medicinal chemistry, particularly relates to a novel serotonin and norepinephrine dual reuptake inhibitor and medical application thereof, and discloses a compound as represented by a formula I and a pharmaceutically acceptable salt thereof, and application of the compound and the pharmaceutically acceptable salt in preparation of antidepressant drugs.
COMPOUNDS HAVING MULTIMODAL ACTIVITY AGAINST PAIN
-
Page/Page column 59, (2019/01/17)
The present invention relates to a compound of formula (I): wherein the meanings for the various substituents are as disclosed in the description, having dual pharmacological activity towards both the α2δ subunit, in particular the α2δ- 1 subunit, of the voltage-gated calcium channel and the NET receptor, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use in therapy, in particular for the treatment of pain.
Chemoenzymatic synthesis of (S)-duloxetine using carbonyl reductase from Rhodosporidium toruloides
Chen, Xiang,Liu, Zhi-Qiang,Lin, Chao-Ping,Zheng, Yu-Guo
supporting information, p. 82 - 89 (2016/02/23)
A chemoenzymatic strategy was developed for (S)-duloxetine production employing carbonyl reductases from newly isolated Rhodosporidium toruloides into the enantiodetermining step. Amongst the ten most permissive enzymes identified, cloned, and overexpressed in Escherichia coli, RtSCR9 exhibited excellent activity and enantioselectivity. Using co-expressed E. coli harboring both RtSCR9 and glucose dehydrogenase, (S)-3-(dimethylamino)-1-(2-thienyl)-1-propanol 3a was fabricated with so far the highest substrate loading (1000 mM) in a space-time yield per gram of biomass (DCW) of 22.9 mmol L-1 h-1 g DCW-1 at a 200-g scale. The subsequent synthetic steps from RtSCR9-catalyzed (S)-3a were further performed, affording (S)-duloxetine with 60.2% overall yield from 2-acethylthiophene in >98.5% ee.
OLIGOMER-ARYLOXY-SUBSTITUTED PROPANAMINE CONJUGATES
-
Paragraph 0255; 0257, (2016/11/17)
The invention relates to (among other things) oligomer- aryloxy-substituted propanamine conjugates and related compounds. A conjugate of the invention, when administered by any of a number of administration routes, exhibits advantages over un-conjugated aryloxy-substituted propanamine compounds.
A method for preparing optically active 3-amino-1-propanol derivatives as an intermediate and a method for preparing (S)-duloxetine using the same
-
Paragraph 0118-0121, (2016/12/01)
The present invention relates to a method for preparing optically active 3-AMNO1-propanol derivatives as an intermediate and a method for preparing (s)-duloxetine using the same. This method can obtain optically active 3-AMNO1-propanol with higher yield and optical purity (ee) than any other conventional methods. Using this as an intermediate compound, it is possible to manufacture duloxetine which is enantiomerically pure and has high optical purity (ee).(DD) Nisoxetine(EE) Duloxetine(CC) 3-amino-1-propanol(BB) Fluoxetine(AA) TomoxetineCOPYRIGHT KIPO 2015
Pharmaceutical compounds wiht angiogenesis inbhibitory activity
-
Paragraph 0095, (2014/10/28)
Compounds of formula (I): wherein: A, R, T, Q, L, Z, G, X and A' are as defined in the description. B and D, equal to or different from each other, are selected between heteroaryl and aryl, wherein at least one of the hydrogen atoms of said heteroaryl and aryl are substituted with groups selected from SO3-, SO3H, COO-, COOH, and one or more of the other hydrogen atoms of said heteroaryl and aryl are optionally substituted as reported in the description.
PHARMACEUTICAL COMPOUNDS
-
Paragraph 0249; 0250, (2014/12/09)
Compounds of formula (I): wherein: A, R, T, Q, L, Z, G, X and A′ are as defined in the description.B and D, equal to or different from each other, are selected between heteroaryl and aryl, wherein at least one of the hydrogen atoms of said heteroaryl and aryl are substituted with groups selected from SO3?, SO3H, COO?, COOH, and one or more of the other hydrogen atoms of said heteroaryl and aryl are optionally substituted as reported in the description.
PERMANENTLY POSITIVELY CHARGED ANTIDEPRESSANTS
-
Page/Page column 67; 68, (2013/03/26)
The present invention provides compounds comprising a substructure of below formula 3: or a salt or prodrug thereof and the use of such compounds in treatment of e.g. CNS disorders.
Inhibition of serotonin and norepinephrine reuptake and inhibition of phosphodiesterase by multi-target inhibitors as potential agents for depression
Cashman, John R.,Ghirmai, Senait
experimental part, p. 6890 - 6897 (2010/01/06)
Compounds possessing more than one functional activity incorporated into the same molecule may have advantages in treating complex disease states. Balanced serotonin/norepinephrine reuptake inhibitors (SNRIs) (i.e., (R)- and (S)-norduloxetine) were chemically linked to a PDE4 inhibitor via a five carbon bridge. The new dual SNRI/PDE4 inhibitors (i.e., (R)-15 and (S)-15) showed moderately potent serotonin reuptake inhibition (IC50 values of 442 and 404 nM, respectively) but low reuptake inhibition of norepinephrine (IC50 values of 2097 and 2190 nM, respectively) in vitro. The dual SNRI/PDE4 inhibitors (i.e., (R)-15 and (S)-15) also inhibited PDE4D2 (i.e., Ki values of 23 and 45 nM, respectively). Due to their synergistic functional activity, SNRI/PDE4 inhibitors may be effective in treating diseases such as depression.
