99985-27-0

Upstream product

• 90564-14-0 1-(2-methoxy-4-nitrophenyl)ethanone 
• 75-05-8 acetonitrile 
• 3240-34-4 [bis(acetoxy)iodo]benzene 
• 39787-83-2 2-methoxy-4-nitrobenzoyl chloride 
• 108-59-8 malonic acid dimethyl ester 
• 121974-56-9 2-amino-1-(2-methoxy-4-nitro-phenyl)-ethanone; hydrochloride 
• 678970-09-7 1-(1-ethoxy-vinyl)-2-methoxy-4-nitro-benzene 
• 568556-26-3 2-bromo-1-(2-methoxy-4-nitro-phenyl)-ethanone 
• 77337-82-7 1-bromo-2-methoxy-4-nitrobenzene 
• 568556-27-4 Acetic acid (Z)-2-azido-1-(2-methoxy-4-nitro-phenyl)-vinyl ester 
• 100061-19-6 N-(2-methoxy-4-nitro-phenacyl)-acetamide 
• 75-36-5 acetyl chloride 

Downstream Products

• 568556-28-5 3-methoxy-4-(2-methyloxazol-5-yl)aniline 

Relevant academic research and scientific papers

NOVEL SUBSTITUTED TRIAZOLE DERIVATIVES AS GAMMA SECRETASE MODULATORS

The present invention is concerned with novel substituted triazole derivatives of Formula (I) wherein Het1, R1, R2, A1, A2, A3, A4, L1, and L2 have the mean

Aminothiazoles as γ-secretase modulators

We herein report the discovery of a new γ-secretase modulator class with an aminothiazole core starting from a HTS hit (3). Synthesis and SAR of this series are discussed. These novel compounds demonstrate moderate to good in vitro potency in inhibiting amyloid beta (Aβ) peptide production. Overall c-secretase is not inhibited but the formation of the aggregating, toxic Aβ42 peptide is shifted to smaller non-aggregating Ab peptides. Compound 15 reduced brain Abβ42 in vivo in APPSwe transgenic mice at 30 mg/kg p.o.

NOVEL SUBSTITUTED TRIAZOLE DERIVATIVES AS GAMMA SECRETASE MODULATORS

The present invention is concerned with novel substituted triazole derivatives of Formula (I) wherein Het1, R1, R2, A1, A2, A3, A4, L1, and L2 have the meaning defined in the claims. The compounds according to the present invention are useful as gamma sec

NOVEL SUBSTITUTED BICYCLIC HETEROCYCLIC COMPOUNDS AS GAMMA SECRETASE MODULATORS

The present invention is concerned with substituted bicyclic heterocyclic compounds of Formula (I) wherein Het1, Het2, A1, A2, A3 and A4 have the meaning defined in the claims. The compounds according to the present invention are useful as gamma secretase modulators. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.

NOVEL SUBSTITUTED INDAZOLE AND AZA-INDAZOLE DERIVATIVES AS GAMMA SECRETASE MODULATORS

The present invention is concerned with novel substituted indazole and aza-indazole derivatives of Formula (I), wherein R1, R2, R3, R4, Y, A1, A2, A3, A4, X1, X2, X3 and Het1 have the meaning defined in the claims. The compounds according to the present invention are useful as gamma secretase modulators. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.

Inhibitors of inosine monophosphate dehydrogenase: SARs about the N-[3-methoxy-4-(5-oxazolyl)phenyl moiety

The first reported structure-activity relationships (SARs) about the N-[3-methoxy-4-(5-oxazolyl)phenyl moiety for a series of recently disclosed inosine monophosphate dehydrogenase (IMPDH) inhibitors are described. The syntheses and in vitro inhibitory values for IMPDH II, and T-cell proliferation (for select analogues) are given.