288383-69-7Relevant articles and documents
THIAZOLIDINONE COMPOUNDS AND USE THEREOF
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Paragraph 1004-1005, (2017/09/21)
A pharmaceutical composition containing a compound of Formula (I) for treating an opioid receptor-associated condition. Also disclosed is a method for treating an opioid receptor-associated condition using such a compound. Further disclosed are two sets of thiazolidinone compounds of formula (I): (i) compounds each having an enantiomeric excess greater than 90% and (ii) compounds each being substituted with deuterium.
DIHYDROPYRIDAZINE-3,5-DIONE DERIVATIVE AND PHARMACEUTICALS CONTAINING THE SAME
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Paragraph 2295, (2016/01/30)
The present invention provides a dihydropyridazine-3,5-dione derivative or a salt thereof, or a solvate of the compound or the salt, a pharmaceutical drug, a pharmaceutical composition, a sodium-dependent phosphate transporter inhibitor, and a preventive and/or therapeutic agent for hyperphosphatemia, secondary hyperparathyroidism, chronic renal failure, chronic kidney disease, and arteriosclerosis associated with vascular calcification comprising the compound as an active ingredient, and a method for prevention and/or treatment.
QUINAZOLINE DERIVATIVES AS TAM FAMILY KINASE INHIBITORS
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Paragraph 0149, (2015/06/08)
Disclosed are compounds, compositions and methods for treating diseases, syndromes, conditions and disorders that are affected by the modulation of the activity of, e.g., the inhibition of, one or more members of the TAM family kinases.
Comprehensive evaluation of the physicochemical properties of Ln III complexes of aminoethyl-DO3A as pH-responsive T1-MRI contrast agents
Baranyai, Zsolt,Rolla, Gabriele A.,Negri, Roberto,Forgacs, Attila,Giovenzana, Giovanni B.,Tei, Lorenzo
supporting information, p. 2933 - 2944 (2014/03/21)
N-Substituted aminoethyl groups were attached to 1,4,7,10- tetraazacyclododecane-1,4,7-triacetic acid (DO3A) with the aim to design pH-responsive LnIII complexes based on the pH-dependent on/off ligation of the amine nitrogen to the metal ion. The following ligands were synthesized: AE-DO3A (aminoethyl-DO3A), MAE-DO3A (N-methylaminoethyl-DO3A), DMAE-DO3A (N,N-dimethylaminoethyl-DO3A) and MEM-AE-DO3A (N-methoxyethyl-N- methylaminoethyl-DO3A). The physicochemical properties of the LnIII complexes were investigated for the evaluation of their potential applicability as magnetic resonance imaging (MRI) contrast agents. In particular, a 1H and 17ONMR relaxometric study was carried out for these GdIII complexes at two different pH values: at basic pH (pendant amino group coordinated to the metal centre) and at acidic pH (protonated amine, not interacting with the metal ion). EuIII complexes allow one to estimate the number of inner-sphere water molecules through luminescence lifetime measurements and obtain some structural information through variable-temperature (VT) high-resolution 1HNMR studies. Equilibria between differently hydrated species were found for most of the complexes at both acidic and basic pH. The thermodynamic stability of CaII, ZnII, CuII and LnIII complexes and kinetics of formation and dissociation reactions of LnIII complexes of AE-DO3A and DMAE-DO3A were investigated showing stabilities comparable to currently approved GdIII-based CAs. In detail, higher total basicity (Σlog KiH) and higher stability constants of Ln III complexes were found for AE-DO3A with respect to DMAE-DO3A (i.e., log KGd-AE-DO3A=22.40 and log KGd-DMAE-DO3A=20.56). The transmetallation reactions of GdIII complexes are very slow (Gd-AE-DO3A: t1/2=2.7×104h; Gd-DMAE-DO3A: 1.1×105h at pH7.4 and 298K) and occur through proton-assisted dissociation. pH Switches: N-Substituted aminoethyl-1,4,7,10- tetraazacyclododecane-1,4,7-triacetic acid (DO3A)-based complexes were prepared to obtain pH-sensitive T1-MRI contrast agents. A detailed evaluation of the physicochemical properties of LnIII complexes was undertaken by different techniques, highlighting the structural variations triggered by the protonation of the pendant amine and the effect of the substituents on the corresponding nitrogen atom (see figure).
COMPOUNDS FOR INHIBITING CELL PROLIFERATION IN EGFR-DRIVEN CANCERS
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Page/Page column 76-77, (2013/12/03)
The invention features compounds, pharmaceutical compositions and methods for treating patients who have an EGFR-driven cancer of Formula (I), wherein the variables are as defined herein.
COMPOUNDS FOR INHIBITING CELL PROLIFERATION IN EGFR-DRIVEN CANCERS
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Page/Page column 70, (2012/11/14)
The invention features compounds, pharmaceutical compositions and methods for treating patients who have an EGFR-driven cancer of formula (I), wherein the variables are as defined herein.
NOVEL THIENOPYRIMIDINE DERIVATIVES OR PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF, PROCESS FOR THE PREPARATION THEREOF AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME
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Page/Page column 111, (2010/11/28)
The present invention relates to a novel thienopyrimidine derivative having an excellent anti? inflammatory and anti-cancer activity, or a pharmaceutically acceptable salt thereof, a process for the preparation thereof and a pharmaceutical composition comprising the same. The compound according to the present invention strongly inhibits IKB kinase-β (IKK-β) involved in the activation of a transcriptional factor, NF-κB, which is associated with inducing various immune and inflammatory diseases, whereby a composition comprising the compound is a useful therapeutic agent against inflammatory diseases, in particular, arthritis and cancer.
QUINAZOLINE DERIVATIVES AS ANGIOGENESIS INHIBITORS
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Page/Page column 72, (2008/06/13)
The invention relates to the use of compounds of the formula I: wherein ring C is an 8, 9, 10, 12 or 13-membered bicyclic or tricyclic moiety which optionally may contain 1-3 heteroatoms selected independently from O, N and S; Z is -O-, -NH-, -S-, -CH2- or a direct bond; n is 0-5; m is 0-3; R represents hydrogen, hydroxy, halogeno, cyano, nitro, trifluoromethyl, C1-3alkyl, C1-3alkoxy, C1-3alkylsulphanyl, -NRR (wherein R and R, which may be the same or different, each represents hydrogen or C1-3alkyl), or RX- (wherein X and R are as defined herein; R represents hydrogen, oxo, halogeno, hydroxy, C1-4alkoxy, C1-4alkyl, C1-4alkoxymethyl, C1-4alkanoyl, C1-4haloalkyl, cyano, amino, C2-5alkenyl, C2-5alkynyl, C1-3alkanoyloxy, nitro, C1-4alkanoylamino, C1-4alkoxycarbonyl, C1-4alkylsulphanyl, C1-4alkylsulphinyl, C1-4alkylsulphonyl, carbamoyl, N-C1-4alkylcarbamoyl, N,N-di(C1-4alkyl)carbamoyl, aminosulphonyl, N-C1-4alkylaminosulphonyl, N,N-di(C1-4alkyl)aminosulphonyl, N-(C1-4alkylsulphonyl)amino, N-(C1-4alkylsulphonyl)-N-(C1-4alkyl)amino, N,N-di(C1-4alkylsulphonyl)amino, a C3-7alkylene chain joined to two ring C carbon atoms, C1-4alkanoylaminoC1-4alkyl, carboxy or a group RX (wherein X and R are as defined herein); and salts thereof, in the manufacture of a medicament for use in the production of an antiangiogenic and/or vascular permeability reducing effect in warm-blooded animals, processes for the preparation of such compounds, pharmaceutical compositions containing a compound of formula I or a pharmaceutically acceptable salt thereof as active ingredient and compounds of formula I. The compounds of formula I and the pharmaceutically acceptable salts thereof inhibit the effects of VEGF, a property of value in the treatment of a number of disease states including cancer and rheumatoid arthritis.
Quinazoline derivatives
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Page column 59, (2010/02/08)
The invention concerns quinazoline derivatives of Formula (I) wherein Q1includes a quinazoline ring optionally substituted with a group such as halogeno, trifluoromethyl and cyano, or a group of the formula: Q3—X1— wherein X1includes a direct bond and O and Q3includes aryl, aryl-(1-6C)alkyl, heterocyclyl and heterocyclyl-(1-6C)alkyl; each of R2and R3is hydrogen or (1-6C)alkyl; Z includes O, S and NH; and Q2includes aryl and aryl-(1-3C)alkyl or a pharmaceutically-acceptable salt thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the prevention or treatment of T cell mediated diseases or medical conditions in a warm-blooded animal.