2528-30-5

Upstream product

• 10541-83-0 N-methyl-p-aminobenzoic acid 
• 501-53-1 benzyl chloroformate 

Downstream Products

• 93960-26-0 4-[4-(Benzyloxycarbonyl-methyl-amino)-benzoylamino]-4-(diethoxy-phosphoryl)-butyric acid methyl ester 
• 93960-25-9 2-[4-(Benzyloxycarbonyl-methyl-amino)-benzoylamino]-4-(diethoxy-phosphoryl)-butyric acid ethyl ester 
• 93960-27-1 [3-[4-(Benzyloxycarbonyl-methyl-amino)-benzoylamino]-3-(diethoxy-phosphoryl)-propyl]-phosphonic acid diethyl ester 
• 66891-86-9 benzyl (4-(chlorocarbonyl)phenyl)(methyl)carbamate 
• 173282-19-4 DL-N-<4-benzoyl>-4,4-difluoroglutamic acid di-tert-butyl ester 
• 178207-64-2 2-[4-(Benzyloxycarbonyl-methyl-amino)-benzoylamino]-5-tert-butoxycarbonylamino-4,4-difluoro-pentanoic acid tert-butyl ester 
• 875668-13-6 2-({(S)-3-[4-(Benzyloxycarbonyl-methyl-amino)-benzoylamino]-3-methoxycarbonyl-propyl}-methoxy-phosphinoylmethyl)-pentanedioic acid dimethyl ester 
• 875668-14-7 2-({3-[4-(benzyloxycarbonyl-methyl-amino)-benzoylamino]-3-tert-butoxycarbonyl-propyl}-methoxy-phosphinoylmethyl)-pentanedioic acid di-tert-butyl ester 
• 875668-08-9 methyl (2S)-4-bromo-2-N-[4-(N-benzyloxycarbonyl-N-methyl)aminobenzoyl]aminobutyrate 
• 875667-97-3 (4-azidocarbonyl-phenyl)-methyl-carbamic acid benzyl ester 
• 178207-65-3 5-tert-Butoxycarbonylamino-4,4-difluoro-2-(4-methylamino-benzoylamino)-pentanoic acid tert-butyl ester 
• 93960-29-3 4-(Diethoxy-phosphoryl)-4-(4-methylamino-benzoylamino)-butyric acid methyl ester 
• 93960-28-2 4-(Diethoxy-phosphoryl)-2-(4-methylamino-benzoylamino)-butyric acid ethyl ester 
• 93960-30-6 [3-(Diethoxy-phosphoryl)-3-(4-methylamino-benzoylamino)-propyl]-phosphonic acid diethyl ester 

Relevant academic research and scientific papers

ANTIFOLATE-CARRYING NANOPARTICLES AND THEIR USE IN MEDICINE

The present invention provides a nanoparticle comprising: a core comprising a metal and/or a semiconductor; and a plurality of ligands covalently linked to the core, wherein said ligands comprise: (i) at least one dilution ligand comprising a carbohydrate, glutathione or an ethylene glycol-containing moiety; and (ii) a ligand of the formula D-L1-Z-L2, wherein D comprises an antifolate drug or folic acid, L1 comprises a first linker portion comprising a C2-C12 glycol and/or C2-C12 alkyl chain, L2 comprises a second linker portion comprising a C2-C12 glycol and/or C2-C12 alkyl chain, wherein L1 and L2 may be the same or different, and wherein Z represents a carbonyl-containing group linking L1 and L2, and wherein L2 is coupled to said core, Also provided are pharmaceutical compositions comprising such nanoparticles, medical uses thereof and methods for producing the nanoparticles.

PRODRUGS ACTIVATED BY REACTIVE OXYGEN SPECIES FOR USE IN THE TREATMENT OF INFLAMMATORY DISEASES AND CANCER

Prodrugs activated predominantly or exclusively in inflammatory tissue, more particularly prodrugs of methotrexate and derivatives thereof, which are selectively activated by Reactive Oxygen Species (ROS) in inflammatory tissues associated with cancer and inflammatory diseases, as well as method for preparing said prodrugs.

PYRAZOLE COMPOUNDS AND THIAZOLE COMPOUNDS AS PROTEIN KINASES INHIBITORS

A compound of formula (I): wherein A, B, D, X, Y, R1, R2, R3, m, p, and q are defined herein. Also disclosed is a method for inhibiting FMS-like tyrosine kinase 3, aurora kinase, or vascular endothelial growth factor receptor.

Novel hyaluronic acid-methotrexate conjugates for osteoarthritis treatment

Hyaluronic acid (HA) provides synovial fluid viscoelasticity and has a lubricating effect. Injections of HA preparations into the knee joint are widely used as osteoarthritis therapy. The current HA products reduce pain but do not fully control inflammation. Oral methotrexate (MTX) has anti-inflammatory efficacy but is associated with severe adverse events. Based on the rationale that a conjugation of HA and MTX would combine the efficacy of the two clinically evaluated agents and avoid the risks of MTX alone, we designed HA-MTX conjugates in which the MTX connects with the HA through peptides susceptible to cleavage by lysosomal enzymes. Intra-articular injection of our HA-MTX conjugate (conjugate 4) produced a significant reduction of the knee swelling in antigen-induced arthritis rat, whereas free MTX, HA or a mixture of HA and MTX showed no or marginal effects on the model. The efficacy of conjugate 4 was almost the same as that of MTX oral treatment. Conjugate 4 has potential as a compound for the treatment of osteoarthritis.

Helical structures of N-alkylated poly(p-benzarnide)s

Poly(p-benzamide)s 1 bearing a chiral side chain on the nitrogen atom were synthesized by chain-growth polycondensation methodology. The polyamides exhibited well-defined molecular weights with narrow polydispersities. Solutions of the polyamides in sever

Amethopterine (methotrexate) phosphonoglutamic analogues. Part I. Synthesis

Even if debatable, the concept of bioequivalence (carboxylic acid-phosphonic acid functions) has already led to therapeutic uses. Selecting a Methotrexate model, a useful antineoplasic agent, we wished to define less toxic structures of compounds leading