1822-32-8Relevant academic research and scientific papers
A fragment merging approach towards the development of small molecule inhibitors of Mycobacterium tuberculosis EthR for use as ethionamide boosters
Nikiforov, Petar O.,Surade, Sachin,Blaszczyk, Michal,Delorme, Vincent,Brodin, Priscille,Baulard, Alain R.,Blundell, Tom L.,Abell, Chris
supporting information, p. 2318 - 2326 (2016/03/01)
With the ever-increasing instances of resistance to frontline TB drugs there is the need to develop novel strategies to fight the worldwide TB epidemic. Boosting the effect of the existing second-line antibiotic ethionamide by inhibiting the mycobacterial
NOVEL MULTIMERIC MOLECULES, A PROCESS FOR PREPARING THE SAME AND THE USE THEREOF FOR MANUFACTURING MEDICINAL DRUGS
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, (2010/06/16)
The invention relates to a compound of the formula (I): in which k and j are independently 0 or 1, Y is a macrocycle in which the cycle includes 9 to 36 carbon atoms and is functionalised by three amino functions and by a chain for attaching the spacer arm Z via an X bond, Rc is a binding pattern with a receptor of the TNF superfamily, X is a chemical function for binding the Y group to the space arm, and Z is a bi-, tri- or tetra-functional spacer arm.
NOVEL MULTIMERIC CD40 LIGANDS, METHOD FOR PREPARING SAME AND USE THEREOF FOR PREPARING DRUGS
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, (2010/08/07)
The invention concerns a compound of formula (I), wherein Y represents a macrocycle whereof the cycle comprises 9 to 36 atoms, and is functionalized by three amine or COOH functions; Rc represents a group of formula H—Xa—Xb—Xc—Xd—Xe—(Xf)i—, wherein i represents 0 or 1, Xn is in particular selected among lysine, arginine, ornithine residues, Xb is in particular selected among glycine, asparagine, L-proline or D-proline residues, Xc et Xd are in particular selected among tyrosine, phenylalanine or 3-nitrotyrosine residues, Xe et Xf are in particular selected among the following amino acid residues: NH2—(CH2)n—COOH, n ranging from 1 to 10 or NH2—(CH2—CH2—O)m—CH2CH2COOH, m ranging from 3 to 6, provided that one at least of the amino acid residues Xa, Xb, Xc and Xd is different from the corresponding amino acid in the sequence of the natural CD40 143Lys-Gly-Tyr-Tyr146 fragment
NOVEL TRICYCLIC PIPERIDINYL COMPOUNDS USEFUL AS INHIBITORS OF FARNESYL-PROTEIN TRANSFERASE
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Page/Page column 72, (2008/06/13)
Novel tricyclic compounds of formula (1.0) or a pharmaceutically acceptable salt or solvate thereof, wherein: one of a, b, c, and d represents N or NR, wherein R is O-, -CH3 or -(CH2)nCO2H wherein n is 1 to 3, and the remaining a, b, c and d groups represent CR or CR; or each of a, b, c and d is independently selected from CR or CR; each R and each R is independently selected from H, halo, -CR3, -OR, -COR, -SR, -S(O)tR (wherein t is 0, 1 or 2), -SCN, -N(R)2, -NRR, -NO2, -OC(O)R, -CO2R, -OCO2R, -CN, -NHC(O)R, -NHSO2R, -CONHR, -CONHCH2CH2OH, -NRCOOR, -SRC(O)OR, -SRN(R); n is 0 (zero), 1, 2, 3, 4, 5 or 6; T is -CO-; -SO-; -SO2-; or -CRR-; Z represents alkyl, aryl, aralkyl, heteroalkyl, heteroaryl, heteroarylalkyl, heterocycloalkyl, heterocycloalkylalkyl, -OR, -SR, -CRR, -NRR, formulae (i), (ii), (iii), (iv), (v) and (vi). Pharmaceutical compositions are disclosed which are inhibitors of the enzyme, farnesyl protein transferase. Also disclosed is a method of inhibiting Ras function and therefore inhibiting the abnormal growth of cells. The method comprises administering the novel tricyclic compound to a biological system. In particular, the method inhibits the abnormal growth of cells in a mammal such as a human.
Design and synthesis of potent, orally active, inhibitors of carboxypeptidase U (TAFIa)
Polla, Magnus O.,Tottie, Louise,Norden, Carita,Linschoten, Marcel,Muesil, Djordje,Trumpp-Kallmeyer, Susanne,Aukrust, Inger R.,Ringom, Rune,Holm, Kjetil H.,Neset, Siren M.,Sandberg, Marcel,Thurmond, John,Yu, Peng,Hategan, Georgeta,Anderson, Herb
, p. 1151 - 1175 (2007/10/03)
A series of 3-mercapto-propionic acid derivatives that function as reversible inhibitors of carboxypeptidase U have been prepared. We present a successful design strategy using cyclic, low basicity guanidine mimetics resulting in potent, selective and bioavailable inhibitors of carboxypeptidase U (TAFIa).
A Practical Synthesis of the Platelet Fibrinogen Antagonist, Elarofiban
Cohen, Judith H.,Roessler, Armin,Scott, Lorraine,Sorgi, Kirk L.,Villani Jr., Frank J.,Webster, Robin R. H.,Weh, Christian,Bos, Mary Ellen,Cesco-Cancian, Sergio,Harris, Bruce D.,Hortenstine, John T.,Justus, Michael,Maryanoff, Cynthia A.,Mills, John,Muller, Stefan
, p. 866 - 872 (2013/09/05)
Elarofiban is a novel, nonpeptide, orally active fibrinogen receptor antagonist useful for the treatment of platelet mediated thrombotic disorders (Costanzo, M. J.; Hoekstra, W. J.; Maryanoff, B. E. WO, 97/41102,1997). Herein we describe the process research that was carried out for the synthesis of elarofiban that eventually led to the development of a safe and cost-effective commercial scale process.
Process for preparing [S- (R*, S*) ] -beta- [ [ [1- [1-oxo-3- (4-piperidinyl) propyl] -3-piperidinyl] carbonyl]amino] -3-pyridinepropanoic acid and derivatives
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, (2008/06/13)
A process for preparing a compound of formula I wherein R1 and R2 are independently selected from the group consisting of hydrogen, lower alkyl and halogen
Synthesis of substituted oxazolo[4,5-b]-pyridine derivatives
Grumel, Vale?rie,Me?rour, Jean-Yves,Guillaumet, Ge?rald
, p. 1329 - 1345 (2007/10/03)
Synthesis of new functionnalized oxazolo[4,5-b]pyridines was described. 5-Bromo-3-hydroxy-2-aminopyridine was heated, in the presence of PPSE or PPA, with 4-cyanobenzoic acid, (4-piperidinyl)acetic or propanoic acid to afford 1,3-oxazolo derivatives. Intr
Dibasic inhibitors of human mast cell tryptase. Part 3: Identification of a series of potent and selective inhibitors containing the benzamidine functionality
Dener, Jeffrey M.,Rice, Kenneth D.,Newcomb, William S.,Wang, Vivian R.,Young, Wendy B.,Gangloff, Anthony R.,Kuo, Elaine Y.-L.,Cregar, Lynne,Putnam, Daun,Wong, Martin
, p. 1629 - 1633 (2007/10/03)
A survey of charged groups and linkers for a series of symmetrical and unsymmetrical dibasic inhibitors is described, leading to several classes of potent and selective inhibitors. In particular, the benzamidine functionality was identified as the most potent charged group investigated.
Serine protease inhibitors
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, (2008/06/13)
The invention relates to a cornound having formula (I), wherein A, B, X, Y and r are as defined in the description, or a prodrug thereof or a pharnnaceutically acceptable salt thereof. The compounds of the invention have anticoagulant activity and can be used in treating or preventing thrombin-related diseases.
