169808-01-9

Upstream product

• 96-34-4 methyl chloroacetate 
• 169808-00-8 4-(R,S)-(4-cyanophenyl)-4-methyl-2,5-dioxoimidazolidine 
• 1443-80-7 4-cyanophenyl methyl ketone 

Downstream Products

• 169808-04-2 methyl ((R,S)-4-(4-cyanophenyl)-3,4-dimethyl-2,5-dioxoimidazolidin-1-yl)acetate 
• 207604-18-0 methyl ((R,S)-4-(4-cyanophenyl)-3-benzyl-4-methyl-2,5-dioxoimidazolidin-1-yl)acetate 
• 169808-22-4 {2-[4-(R,S)-(4-tert-butoxycarbonylaminomethyl-phenyl)-4-methyl-2,5-dioxoimidazolidin-1-yl]acetyl}-Asp(O-t-Bu)-(S)-phenylglycine-O-t-Bu 
• 762217-10-7 N-(tert-butoxycarbonyl-phenyl-methyl)-3-{2-[4-(4-carbamimidoyl-phenyl)-4-methyl-2,5-dioxo-imidazolidin-1-yl]-acetylamino}-succinamic acid tert-butyl ester 
• 736115-77-8 2-benzyloxycarbonylamino-3-{2-[4-(4-carbamimidoyl-phenyl)-4-methyl-2,5-dioxo-imidazolidin-1-yl]-acetylamino}-propionic acid tert-butyl ester 

Relevant academic research and scientific papers

Novel heterocycles as inhibitors of leucocyte adhesion and as VLA-4 antagonists

The present invention relates to compounds of the formula I which are inhibitors of the adhesion and migration of leucocytes and/or antagonists of the adhesion receptor VLA-4 which belongs to the group of integrins. The invention also relates to processes

Discovery of an orally active non-peptide fibrinogen receptor antagonist based on the hydantoin scaffold

Antagonists of the platelet fibrinogen receptor (GP IIb/IIIa receptor) are expected to be a promising new class of antithrombotic agents. The binding of fibrinogen to the fibrinogen receptor depends on an Arg-Gly-Asp-Ser (RGDS) tetrapeptide recognition motif. Structural modifications of the RGDS lead have led to the discovery of a non-peptide RGD mimetic GP IIb/IIIa antagonist 44 (S 1197). Compound 44 inhibited, in a dose dependent and reversible manner, human and dog platelet aggregation as well as 125I-fibrinogen binding to ADP-activated human gel filtered platelets and isolated GP IIb/IIIa with Ki values of 9 nM and 0.17 nM, respectively. A pharmacophore mapping procedure with QXP and a 3D-QSAR analysis applying the GRID/GOLPE methodology yielded a stable, rather predictive model and revealed structural features which are important for binding. Hydrophobic substitutions both at the hydantoin nucleus and at the C-terminus increase the affinity toward the fibrinogen receptor. The crystalline ethyl ester prodrug 48 (HMR 1794) is an orally active antithrombotic agent which is a promising drug candidate for the treatment of thrombotic diseases in humans.

Heterocyclic compounds, their preparation and their use as leucocyte adhesion inhibitors and VLA-4-antagonists

Compounds of the formula I, in which B, E, W, Y, Z, R, R2, R2a, R2b, R3, g and h have the meanings indicated in the specifications. The compounds of the formula I are valuable pharmaceutical active compounds, which are suitable, for example, for the thera

Substituted 5-membered ring heterocycles, their preparation and their use

The present invention pertains to 5-ring heterocycles of general formula (I), wherein W, Y, Z, B, D, E and R as well as b, c, d, e, f, g, and h are as indicated in the description; to methods for preparing them, and to their use as inhibitors of platelet aggregation, metastasizing of carcinomatous cells and the attachment of osteoclasts to the bone surface. STR1