19068-80-5Relevant academic research and scientific papers
An application of borane as a protecting group for pyridine
Zajac, Matthew A.
, p. 6899 - 6901 (2008)
(Chemical Equation Presented) Efforts to couple 4 with 12 employing base mediation are problematic due to the formation of 6. To circumvent this issue, 12 was converted to the pyridine borane complex (13). Alkylation of 4 with 13 provided 3 after removal of the borane under acidic conditions and saponification of the ester.
Computer-Aided Identification and Lead Optimization of Dual Murine Double Minute 2 and 4 Binders: Structure-Activity Relationship Studies and Pharmacological Activity
Giustiniano, Mariateresa,Daniele, Simona,Pelliccia, Sveva,La Pietra, Valeria,Pietrobono, Deborah,Brancaccio, Diego,Cosconati, Sandro,Messere, Anna,Giuntini, Stefano,Cerofolini, Linda,Fragai, Marco,Luchinat, Claudio,Taliani, Sabrina,La Regina, Giuseppe,Da Settimo, Federico,Silvestri, Romano,Martini, Claudia,Novellino, Ettore,Marinelli, Luciana
, p. 8115 - 8130 (2017)
The function of p53 protein, also known as "genome guardian", might be impaired by the overexpression of its primary cellular inhibitor, the murine double minute 2 protein (MDM2). However, the recent finding that MDM2-selective inhibitors induce high leve
Probing integrin selectivity: rational design of highly active and selective ligands for the α5β1 and αvβ3 integrin receptor
Heckmann, Dominik,Meyer, Axel,Marinelli, Luciana,Zahn, Grit,Stragies, Roland,Kessler, Horst
, p. 3571 - 3574 (2007)
(Chemical Equation Presented) Try and fit in: A strategy for the rational design of α5β1 ligands for the purpose of lead generation and biochemical studies on integrin selectivity is based α5β1 homology modeling. Ligand 1 can bind α5β1 with activities in
Design, synthesis, and biological evaluation of novel potent and selective αvβ3/αvβ5 integrin dual inhibitors with improved bioavailability. Selection of the molecular core
Marugán, Juan José,Manthey, Carl,Anaclerio, Beth,Lafrance, Lou,Lu, Tianbao,Markotan, Tom,Leonard, Kristi A.,Crysler, Carl,Eisennagel, Stephen,Dasgupta, Malini,Tomczuk, Bruce
, p. 926 - 934 (2007/10/03)
A novel series of potent and selective αvβ 3/αvβ5 dual inhibitors was designed, synthesized, and evaluated against several integrins. These compounds were synthesized through a Mitsunobu reaction between the gua
Substituted indoles and their use as integrin antagonists
-
, (2008/06/13)
The present invention relates to novel substituted indole compounds that are antagonists of alpha V (αv) integrins, for example αvβ3 and αvβ5 integrins, their pharmaceutically acceptable salts, and pharmaceutical compositions thereof. The compounds may be used in the treatment of pathological conditions mediated by αvβ3 and αvβ5 integrins, including such conditions as tumor growth, metastasis, restenosis, osteoporosis, inflammation, macular degeneration, diabetic retinopathy, and rheumatoid arthritis. The compounds have the general formula: where R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, D, X, W, a, m, n, i, j, k and v are defined herein.
Vitronectin receptor antagonists
-
, (2008/06/13)
PCT No. PCT/US96/20327 Sec. 371 Date Jul. 27, 1999 Sec. 102(e) Date Jul. 27, 1999 PCT Filed Dec. 20, 1996 PCT Pub. No. WO97/24124 PCT Pub. Date Jul. 10, 1999Compounds of formula (I) are disclosed, wherein: A is a fibrinogen antagonist template; W is a linking moiety of the form -(CHRg)a-U-(CHRg)b-V-; Q1, Q2, Q3 and Q4 are independently N or C-Ry, provided that no more than one Q1, Q2, Q3 and Q4 is N; R' is H or C1-6alkyl, C3-7cycloalkyl-C0-6-alkyl or Ar-C0-6alkyl; Rg is H or C1-6alkyl, Het-C0-6alkyl, C3-7cycloalkyl-C0-6alkyl or Ar-C0-6alkyl; Rk is Rg, -C(O)Rg or -C(O)ORg Ri is H, C1-6alkyl, Het-C0-6alkyl, C3-7cycloalkyl-C0-6alkyl, Ar-C0-6alkyl, Het-C0-6alkyl-U'-C1-6alkyl, C3-7cycloalkyl-C0-6alkyl-U'-C1-6alkyl or Ar-C0-6alkyl-U'-C1-6alkyl; Ry is H, halo, -ORg, -SRg, -CN, -NRgRk, -NO2, -CF3, CF3S(O)r, -CO2Rg, -CORg or -CONRg2, or C1-6alkyl optionally substituted by halo, -ORg, -SRg, -CN, -NR8R'', -NO2, -CF3, R'S(O)3-, -CO2Rg, -CORg or -CONRg2; U and V are absent or CO, CRg2, C(=CRg2), S(O)c, O, NRg, CRgORg, CRg(ORk)CRg2, CRg7CRg(ORk), C(O)CRg2, CRg2C(O), CONRi, NRiCO, OC(O), C(O)O, OC(S), C(S)NRg, NR8C(S), S(O2NRg, NRgS(O)2N=N, NRgNRg, NRgCRg2, NRgCRg2, CRg2O, OCRg2, CRg=CRg, C=C, Ar or Het; a is 0, 1 or 2; c is 0, 1 or 2; r is 0, 1 or 2; and u is 0 or 1; or pharmaceutically acceptable salts thereof, which are vitronectin receptor antagonists useful in the treatment of osteoporosis.
