18699-02-0Relevant articles and documents
HYALURONIC ACID DERIVATIVE AND DRUG CONTAINING THE SAME
-
Paragraph 0148, (2018/09/08)
The present invention relates to a hyaluronic acid derivative in which an anti-inflammatory drug is bound via a covalent bond, wherein the structure of the hyaluronic acid derivative is represented by following formula (4) or (5): ???????? HA-SP-NSAID?????(4) ???????? HA-SP-DMARD?????(5) wherein HA represents a hyaluronic acid chain; SP represents a spacer residue; NSAID represents a non-steroidal anti-inflammatory drug residue, DMARD represents a disease-modifying anti-rheumatic drug residue, and - represents the covalent bond, wherein the spacer binds to a carboxyl group of the hyaluronic acid via an amide bond and the anti-inflammatory drug selected from non-steroidal anti-inflammatory drugs and disease-modifying anti-rheumatic drugs binds to the spacer via an ester bond, an amide bond or a thioester bond.
Pharmacomodulation of the antimalarial plasmodione: Synthesis of biaryl-and N-arylalkylamine analogues, antimalarial activities and physicochemical properties
Urgin, Karène,Jida, Mouhamad,Ehrhardt, Katharina,Müller, Tobias,Lanzer, Michael,Maes, Louis,Elhabiri, Mourad,Davioud-Charvet, Elisabeth
, (2017/02/15)
With the aim of increasing the structural diversity on the early antimalarial drug plasmodione, an efficient and versatile procedure to prepare a series of biaryl- and N-arylalkylamines as plasmodione analogues is described. Using the naturally occurring and commercially available menadione as starting material, a 2-step sequence using a Kochi-Anderson reaction and subsequent Pd-catalyzed Suzuki-Miyaura coupling was developed to prepare three representative biphenyl derivatives in good yields for antimalarial evaluation. In addition, synthetic methodologies to afford 3-benzylmenadione derivatives bearing a terminal -N(Me)2 or -N(Et)2 in different positions (ortho, meta and para) on the aryl ring of the benzylic chain of plasmodione were investigated through reductive amination was used as the optimal route to prepare these protonable N-arylalkylamine privileged scaffolds. The antimalarial activities were evaluated and discussed in light of their physicochemical properties. Among the newly synthesized compounds, the para-position of the substituent remains the most favourable position on the benzyl chain and the carbamate -NHBoc was found active both in vitro (42 nM versus 29 nM for plasmodione) and in vivo in Plasmodium berghei-infected mice. The measured acido-basic features of these new molecules support the cytosol-food vacuole shuttling properties of non-protonable plasmodione derivatives essential for redox-cycling. These findings may be useful in antimalarial drug optimization.
ROR-GAMMA MODULATORS AND USES THEREOF
-
Page/Page column 40, (2016/01/21)
The present invention relates to a compound of formula I, or an isotopic form, stereoisomer, a tautomer, a pharmaceutically acceptable salt, a solvate, a polymorph, a prodrug, N-oxide or S-oxide thereof; and processes for their preparation. The invention further relates to pharmaceutical compositions containing the compounds and their use in the treatment of diseases or disorders mediated by RORγ.