13958-93-5Relevant academic research and scientific papers
NOVEL COMPOUNDS AS DUAL INHIBITORS OF PHOSPHODIESTERASES AND HISTONE DEACETYLASES
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Page/Page column 53, (2014/09/16)
It relates to certain compounds having a polycyclic structure and a hydroxamic acid moiety, wherein the polycyclic structure comprises at least three ring systems, wherein one ring system is a polycyclic ring system comprising from 2 to 4 rings; at least one ring is an aromatic ring; and wherein the structure comprises at least 3 nitrogen atoms and 1 oxygen atom. It also relates to a process for their preparation, as well as to pharmaceutical compositions containing them, and to their use in medicine, in particular in the treatment and/or prevention of neurological disorders coursing with a cognition deficit or impairment, or neurodegenerative diseases. wherein B1 is a radical selected from the group consisting of formula (A"), formula (B"), formula (C"), and formula (D"):
Identification of aminopyrazolopyridine ureas as potent VEGFR/PDGFR multitargeted kinase inhibitors
Dai, Yujia,Hartandi, Kresna,Soni, Niru B.,Pease, Lori J.,Reuter, David R.,Olson, Amanda M.,Osterling, Donald J.,Doktor, Stella Z.,Albert, Daniel H.,Bouska, Jennifer J.,Glaser, Keith B.,Marcotte, Patrick A.,Stewart, Kent D.,Davidsen, Steven K.,Michaelides, Michael R.
, p. 386 - 390 (2008/04/03)
Tumor angiogenesis is mediated by KDR and other VEGFR and PDGFR kinases. Their inhibition presents an attractive approach for developing anticancer therapeutics. Here, we report a series of aminopyrazolopyridine ureas as potent VEGFR/PDGFR multitargeted k
PHENYLALANINE ENAMIDE DERIVATIVES CONTAINING A SPIRO`3.5!NON-1-ENE RING FOR USE AS INTEGRIN INHIBITORS
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Page/Page column 15, (2010/02/06)
Phenylalanine enamide derivatives of formula (1) are described: wherein R1 is a -CH3, -(CH2)3CH3, -CH2CH20H, -CH2CH20CH3, -CH2CH2
PROCESS FOR THE PREPARATION OF PHENYLALANINE ENAMIDE DERIVATIVES
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Page 42, (2010/02/06)
A process for the preparation of a class of phenylalanine enamide derivatives is described formula (1) wherein: Ar1 is an optionally substituted aromatic or heteroaromatic group; L2 is a linker group selected from -N(R4)- [where R4 is a hydrogen atom or an optionally substituted straight or branched C1-6alkyl group], -CON(R4)-, or -S(O)2N(R4)-; R1 is a carboxylic acid (-CO2H) or a derivative or biostere thereof; R2 is a hydrogen atom or a C1-6alkyl group; Rx, Ry and Rz which may be the same or different is each an atom or group -L1(Alk1)n(R3)v; and the salts, solvates, hydrates and N-oxides thereof; which comprises reacting a compound of formula (2): wherein: Qa is a group -N(R4)H; and the salts, solvates, hydrates and N-oxides thereof; with a compound Ar1W wherein W is a group selected from X1 (wherein X1 is a leaving atom or group), -COX2 (wherein X2 is a halogen atom or a -OH group) or -SO2 X3 (in which X3 is a halogen atom).
Piperazine-based CCR5 antagonists as HIV-1 inhibitors. III: Synthesis, antiviral and pharmacokinetic profiles of symmetrical heteroaryl carboxamides
McCombie, Stuart W.,Tagat, Jayaram R.,Vice, Susan F.,Lin, Sue-Ing,Steensma, Ruo,Palani, Anandan,Neustadt, Bernard R.,Baroudy, Bahige M.,Strizki, Julie M.,Endres, Michael,Cox, Kathleen,Dan, Niya,Chou, Chuan-Chu
, p. 567 - 571 (2007/10/03)
The unsymmetrical nicotinamide-N-oxide moiety in compound 1 was replaced with symmetrical isonicotinamides as well as 4,6-dimethyl pyrimidine-5-carboxamides. Compound 16 from the latter set reduced the number of rotamers, improved potency of inhibiting UIV entry, slightly diminished the affinity for the muscarine receptors and showed very good oral absorption.
Oximino-piperidino-piperidine-based CCR5 antagonists. Part 2: Synthesis, SAR and biological evaluation of symmetrical heteroaryl carboxamides
Palani, Anandan,Shapiro, Sherry,Clader, John W.,Greenlee, William J.,Vice, Susan,McCombie, Stuart,Cox, Kathleen,Strizki, Julie,Baroudy, Bahige M.
, p. 709 - 712 (2007/10/03)
The synthesis, SAR and biological evaluation of symmetrical amide analogues of our clinical candidate SCH 351125 are described. A series of potent and orally bioavailable CCR5 antagonists containing symmetrical 2,6-dimethyl isonicotinamides and 2, 6-dimethyl pyrimidines amides were generated with enhanced affinity for the CCR5 receptor.
N-arylsulfonyl aza-bicyclic derivatives as potent cell adhesion inhibitors
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, (2008/06/13)
Compounds of Formula I are antagonists of VLA-4 and/or alpha4/beta7, and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These compounds may be formulated into pharmaceutical compositions and are suitable for use in the treatment of AIDS-related dementia, allergic conjunctivitis, allergic rhinitis, Alzheimer's disease, asthma, atherosclerosis, autologous bone marrow transplantation, certain types of toxic and immune-based nephritis, contact dermal hypersensitivity, inflammatory bowel disease including ulcerative colitis and Crohn's disease, inflammatory lung diseases, inflammatory sequelae of viral infections, meningitis, multiple sclerosis, multiple myeloma, myocarditis, organ transplantation, psoriasis, pulmonary fibrosis, restenosis, retinitis, rheumatoid arthritis, septic arthritis, stroke, tumor metastasis, uveititis, and type I diabetes.
2,3-DIPHENYLPROPIONIC ACID DERIVATIVES OR THEIR SALTS, MEDICINES OR CELL ADHESION INHIBITORS CONTAINING THE SAME, AND THEIR USAGE
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, (2008/06/13)
A 2,3-diphenylpropionic acid derivatives or the salts represented by general formula (1) below; and pharmaceutical compositions and cell adhesion inhibitors comprising the derivatives or the salts as the active ingredient. In the formula, A, B and C indep
Phenylalanine derivatives
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Page column 18, (2010/01/30)
Phenylalanine derivatives of formula (1) are described: in which:Ar1 is an aromatic or heteroaromatic group;L1 is a linker atom or group;R is a carboxylic acid or a derivative thereof;Ar2 is an optionally substituted aromatic or heteroaromatic group;and the salts, solvates, hydrates and N-oxides thereof.The compounds are able to inhibit the binding of à4 integrins to their ligands and are of use in the prophylaxis and treatment of immune or inflammatory disorders.
Discovery and evaluation of N-(triazin-1,3,5-yl) phenylalanine derivatives as VLA-4 integrin antagonists.
Porter, John R,Archibald, Sarah C,Brown, Julien A,Childs, Kirstie,Critchley, David,Head, John C,Hutchinson, Brian,Parton, Ted A H,Robinson, Martyn K,Shock, Anthony,Warrellow, Graham J,Zomaya, Alex
, p. 1591 - 1594 (2007/10/03)
SAR studies aimed at improving the rate of clearance of a series of VLA-4 integrin antagonists by the introduction of a 1,3,5-triazine as an amide isostere are described.
