1107643-81-1

Upstream product

• 70918-53-5 (+)-(2R)-2,3-dihydro-1,4-benzodioxine-2-carboxylic acid 

Downstream Products

• 1106939-93-8 (R)-2,3-dihydrobenzo[1,4]dioxin-2-yl-((R)-3-(3-fluorophenyl)piperidin-1-yl)methanone 
• 1106939-95-0 (R)-2,3-dihydrobenzo[1,4]dioxin-2-yl-((S)-3-(3-fluorophenyl)piperidin-1-yl)methanone 
• 1106939-91-6 (R)-2,3-dihydrobenzo[1,4]dioxin-2-yl-((S)-3-(2-fluorophenyl)piperidin-1-yl)methanone 
• 1106939-89-2 (R)-2,3-dihydrobenzo[1,4]dioxin-2-yl-((R)-3-(2-fluorophenyl)piperidin-1-yl)methanone 
• 1106939-97-2 (R)-2,3-dihydrobenzo[1,4]dioxin-2-yl-((R)-3-(4-fluorophenyl)piperidin-1-yl)methanone 
• 1106939-99-4 (R)-2,3-dihydrobenzo[1,4]dioxin-2-yl-((S)-3-(4-fluorophenyl)piperidin-1-yl)methanone 
• 1106940-09-3 (R)-2,3-dihydrobenzo[1,4]dioxin-2-yl-((R)-3-(4-trifluoromethylphenyl)piperidin-1-yl)methanone 
• 1106940-12-8 (R)-2,3-dihydrobenzo[1,4]dioxin-2-yl-((S)-3-(4-trifluoromethylphenyl)piperidin-1-yl)methanone 
• 1106940-05-9 (R)-2,3-dihydrobenzo[1,4]dioxin-2-yl-((R)-3-(3-trifluoromethylphenyl)piperidin-1-yl)methanone 
• 1106940-07-1 (R)-2,3-dihydrobenzo[1,4]dioxin-2-yl-((S)-3-(3-trifluoromethylphenyl)piperidin-1-yl)methanone 
• 1106941-02-9 (R*)-3-(1-((R)-2,3-dihydrobenzo[1,4]dioxin-2-carbonyl)piperidin-3-yl)benzoic acid methyl ester 

Relevant academic research and scientific papers

Quinazoline based α1-adrenoreceptor antagonists with potent antiproliferative activity in human prostate cancer cell lines

New α1-adrenoreceptor (α1-AR) antagonists related to prazosin and doxazosin were synthesized by replacing piperazine ring with (S)- or (R)-3-aminopiperidine. Binding studies indicated that the S configuration at the 3-C position of the piperidine ring is crucial for an optimal interaction of the compounds at all three α1-AR subtypes. Quinazolines 9 and 10, bearing a quinone ring on the lateral chain, exhibited also potent antiproliferative activity in LNCaP androgen-sensitive prostate cancer cell lines, higher than that of doxazosin. Compound 10 increased apoptosis, in terms of DNA fragmentation, without triggering cell necrosis. The prooxidant activity found in compound 10 may underlie its ability to inhibit cell proliferation in synergy with the effect mediated by α1-AR antagonism. Due to its better biological profile compared to doxazosin for LNCaP cell line, compound 10 might be a valuable lead compound for the design of new prostate antitumor agents.

NOVEL TRICYCLIC COMPOUNDS AS INHIBITORS OF MUTANT IDH ENZYMES

The present invention is directed to tricyclic compounds of formula (I) which are inhibitors of one or more mutant IDH enzymes (I); wherein A is -C(R1)= or -N=; and X is selected from the group consisting of: (II-i), and (II-ii). The present invention is also directed to uses of the tricyclic compounds described herein in the potential treatment or prevention of cancers in which one or more mutant IDH enzymes are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such cancers.

ARYL PIPERAZINE AND THEIR USE AS ALPHA2C ANTAGONISTS

Compounds of formula (I), wherein X, Z, A, B, D, E, R1-R4 and m are as defined in the claims, exhibit alpha2C antagonistic activity and are thus useful as alpha2C antagonists.

2,3-DIHYDROBENZO[l,4] DIOXIN-2-YLMETHYL DERIVATIVES AS ALPHA2C ANTAGONISTS FOR USE IN THE TREATMENT OF PERIPHERIC AND CENTRAL NERVOUS SYSTEME DISEASES

Compounds of formula (I), wherein X, Z, R1-R4, and m are as defined in the claims, exhibit alpha2C antagonistic activity and are thus useful for the treatment of diseases and conditions of the peripheric system and the central nervous system (CNS).