262450-67-9Relevant academic research and scientific papers
HETEROCYCLIC CARBOXYLIC ACIDS AS ACTIVATORS OF SOLUBLE GUANYLATE CYCLASE
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Paragraph 0346; 0350, (2016/02/18)
The present invention relates to compounds of formula I: and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R5, R6, R7, R8, R9, B, V, W, X, Y, Z and m are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
ALKOXY PYRAZOLES AS SOLUBLE GUANYLATE CYCLASE ACTIVATORS
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Paragraph 0302; 0316, (2014/03/25)
The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6 and R7 are as defined herein. The inventi
8-Substituted isoquinoline derivative and the use thereof
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Page/Page column 119, (2010/11/03)
The present invention relates to a compound represented by the following formula (1): wherein D1, A1, D2, R1, D3, and R2 each have the same meaning as defined in the present specification or a salt thereof. The compound represented by the formula (1) or a salt thereof has an IKKβ inhibiting activity and the like and is useful for the prevention and/or treatment of IKKβ-associated diseases or symptoms and the like.
Binding and preliminary evaluation of 5-hydroxy- and 10-hydroxy- 2,3,12,12a-tetrahydro-1H-[1]benzoxepino[2,3,4-ij]isoquinolines as dopamine receptor ligands
Claudi, Francesco,Di Stefano, Antonio,Napolitani, Fabrizio,Cingolani, Gian Mario,Giorgioni, Gianfabio,Fontenla, Josè A.,Montenegro, Gisela Y.,Rivas, Maria E.,Rosa, Elizabeth,Michelotto, Barbara,Orlando, Giustino,Brunetti, Luigi
, p. 599 - 608 (2007/10/03)
The N-methyl, N-ethyl, and N-n-propyl derivatives of 5-hydoxy- and 10- hydroxy-2,3,12,12a-tetrahydro-1H-[1]benzoxepino[2,3,4-ij]isoquinolines were prepared as monophenolic ligands for the dopamine receptor and evaluated for their affinity at D1-like and D2-like subtypes. All compounds showed very low D1 affinities. This could be ascribed to the absence of a catechol nucleus or of the β-phenyldopamine pharmacophore. Only the N-methyl-5- hydroxy- (5a), N-methyl-10-hydroxy-(6a), and N-methyl-4-bromo-10-methoxy- 2,3,12,12a-tetrahydro-1H-[1]-benzoxepino[2,3,4-ij]isoquinolines (26a) bound the D2 receptors with low affinity, in the same range as dopamine. In compounds 5a and 6a, the 2-(3-hydroxyphenyl)-ethylamine moiety does not meet the requirements of the D2 agonist pharmacophore: namely, the 2-(3- hydroxyphenyl)ethylamine does not reach the trans, fully extended conformation. The three compounds did not interact with recombinant human D4 receptors, and only 5a showed low affinity for rat recombinant D3 receptors. Analysis of the influence of Na+ on [3H]spiperone binding showed that 5a displays a potential dopamine D2 agonist profile, whereas 6a probably has a dopamine D2 antagonist activity. The D2 agonist activity of 5a was proved by the effects on prolactin release from primary cultures of rat anterior pituitary cells.
