176772-96-6Relevant articles and documents
Design, synthesis and dopamine D4 receptor binding activities of new N-heteroaromatic 5/6-ring Mannich bases
Linz, Sabine,Mueller, Joerg,Huebner, Harald,Gmeiner, Peter,Troschuetz, Reinhard
experimental part, p. 4448 - 4458 (2009/12/04)
A series of phenylpiperazine-methyl-substituted 1H-pyrrolo[2,3-c]pyridine, imidazo[1,2-c]-, pyrrolo[2,3-d]- and pyrrolo[3,2-d]pyrimidines were prepared as selective dopamine D4-ligands. The pyrrolo[2,3-d]pyrimidine derivatives 12d (Ki = 1,9 nM)
Process for Preparing 4-Aminopyrimidine Compound
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Page/Page column 3, (2008/06/13)
The present invention is to provide a process for preparing a 4-aminopyrimidine compound represented by the formula (3): wherein R1 and R2 each represent a hydrogen atom or group which does not participate in the reaction and which may have a substituent(s), and R1 and R2 may be bonded to each other to form a ring, and R4 represents a hydrogen atom or a hydrocarbon group, which comprises reacting ammonia, a 3-substituted or unsubstituted acrylonitrile compound represented by the formula (1): [in-line-formulae]CR1(CN)═CR2Y??(1) [/in-line-formulae]wherein R1 and R2 have the same meanings as defined above, and Y represents an amino group or OR, where R represents a hydrogen atom or a hydrocarbon group, and an organic acid compound represented by the formula (2): [in-line-formulae](R3O)3CR4??(2) [/in-line-formulae]wherein R3 represents a hydrocarbon group, and R4 has the same meaning as defined above.
CRF receptor antagonists and methods relating thereto
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, (2008/06/13)
CRF receptor antagonists are disclosed. Such receptor antagonists are thiadiazole-, pyrimidine-, triazine-, and triazole-containing compounds substituted with both a C3-C14 monocyclic or fused, homoaryl or heteroaryl group and a substituted amine group. The CFR receptor antagonists have utility in the treatment of a variety of disorders, including disorders associated with the hypersecretion of CRF.
Cephalosporin antibiotics
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, (2008/06/13)
The present invention relates to a cephalosporin compound represented by the following general formula (I): STR1 its pharmaceutically acceptable non-toxic salt, physiologically hydrolyzable ester, hydrate or solvate, or isomers thereof, in whichR 1 represents hydrogen or an amino-protecting group,R 2 and R 3 can be identical or different and independently of one another represent hydrogen or a hydroxy-protecting group, orR 2 and R 3 together can form a cyclic diol-protecting group,R 4 represents hydrogen or a carboxyl-protecting group,R 5, R 6 and R 7 independently of one another represent hydrogen, amino or substituted amino, hydroxy, alkoxy, C 1-4 alkyl, carboxyl or alkoxycarbonyl, orR 5 and R 6 together with the carbon atoms to which they are attached can form a C 3-7 cycle, andQ represents CH or N,and to a process for preparation thereof and a pharmaceutical composition containing the compound (I) as an active ingredient.
Novel cephalosporin antibiotics and processes for preparation thereof
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, (2008/06/13)
The present invention relates to a cephalosporin compound represented by the following general formula (I) : its pharmaceutically acceptable non-toxic salt, physiologically hydrolyzable ester, hydrate or solvate, or isomers thereof, in which R1represents
Artificial DNA base pair analogues
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, (2008/06/13)
The present invention is directed to new artificial base pairs comprising complementary artificial purines and pyrimidines and methods of using artificial complementary base pairs.
1H NMR Evidence for High Barriers to Amino Group Rotation in 4-Aminopyrimidines, Including Thiamin, at Low pH in Water
Jordan, Frank
, p. 2748 - 2753 (2007/10/02)
The 1H NMR spectrum of thiamin (1), 4-aminopyrimidine (2), 4-amino-5-(methoxymethyl)-2-methylpyrimidine (3), and thiothiamin (4) was recorded at a variety of concentrations, temperatures, and pH's in 80:20 (v/v) H2O-(2)H2O employing correlation spectroscopy and Redfield 2-1-4 sequences at 360 and 500 MHz.At pH's 1.5 to 3.0 units below the pK for N1 protonation, two amino hydrogen resonances were observed to persist at temperatures below about 10 deg C for 1, 26 deg C for 2, 40 deg C for 3, and 15 deg C for 4, indicative of hindered amino group rotation under these conditions.The concentration and temperature dependence of the behavior of the two NH resonances at low pH suggest that the increased barrier is not due to intermolecular interactions but simply to the favorable resonance interaction between the amino group nitrogen lone pair and the pyrimidine ring once the latter is N1 protonated.The barrier to amino group rotation in N1'-protonated thiamin was estimated to be 14.6 kcal/mol at pH 1.56, 12 deg C, in 1 M KCl solution.
On the Amination of Azaheterocycles. A New Procedure for the Introduction of an Amino Group
Hara, Hiroshi,Plas, Henk C. van der
, p. 1285 - 1287 (2007/10/02)
A new method of amination of diazines and triazines, using potassium amide, liquid ammonia and potassium permanganate, has been described.
