439660-85-2

Upstream product

• 89980-69-8 3,4-dimethoxyphenylmagnesium bromide 
• 85-43-8 1,2,3,6-Tetrahydrophthalic anhydride 
• 935-79-5 cis-1,2,3,6-tetrahydrophthalic anhydride 

Downstream Products

• 415927-43-4 (cis)-4-(3,4-Dimethoxyphenyl)-4a,5,8,8a-tetrahydro-2H-phthalazin-1-one 
• 357980-82-6 4-(3,4-dimethoxy-phenyl)-4a,5,8,8a-tetrahydro-2H-phthalazin-1-one 
• 1116690-31-3 2-(2-bromopentyl)-4-(3,4-dimethoxyphenyl)-4a,5,6,7,8,8a-hexahydrophthalazin-1(2H)-one 
• 878663-15-1 C₃₇H₄₂F₃N₃O₄ 
• 878663-14-0 C₃₇H₄₂F₃N₃O₄ 

Relevant academic research and scientific papers

Stereoselective inhibition of serotonin re-uptake and phosphodiesterase by dual inhibitors as potential agents for depression

Multi-target compounds where more than one functional activity is incorporated into the same molecule may have advantages in treating disease states. Selective serotonin re-uptake inhibitors (SSRIs)a (i.e., (R)- and (S)-norfluoxetine) were chemically linked to a PDE4 inhibitor via a five carbon bridge. The new dual PDE4 inhibitor/SSRIs (i.e., (R)-8 and (S)-8) showed moderately potent but highly selective serotonin re-uptake inhibition (IC50 values of 173 and 42 nM, respectively) in vitro. The dual PDE4 inhibitor/SSRIs (R)-8 and (S)-8 also inhibited PDE4D2 (i.e., Ki values of 106 and 253 nM, respectively). Due to the synergistic functional activity, PDE4 inhibitor/SSRIs may be effective in treating diseases such as depression.

MODULATORS OF CENTRAL NERVOUS SYSTEM NEUROTRANSMITTERS

Disclosed are agents having pharmacological activity against cellular receptors and intracellular singaling, particularly receptors and sigaling pathways of central nervous system (CNS) neurotransmitters. Also disclosed are related methods and compositions for the treatment or prevention of diseases or disorders using the agents.

Phthalazinone PDE III/IV inhibitors

The compounds of formula (I) in which R1, R2, R3, R4, R5, X and Y have the meanings as given in the description are novel effective bronchial therapeutica.