7309-42-4Relevant academic research and scientific papers
PHARMACEUTICAL COMPOUNDS
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Page/Page column 48, (2011/07/06)
Diazapolycyclic compounds having affinity for the opioidergic receptors, preferably for the delta opioidergic receptors, with central and/or peripheral activity, having formula: [in-line-formulae]A1-D1-T1??(I)[/in-line-formulae] wherein: A1 is a group of formula (II): wherein: R1 is phenyl wherein one of the ring hydrogen atoms is substituted with a group selected from C(O)R′, C(O)OR′, C(O)NHR′ or C(O)NR3R4, R′, R3 and R4, being as defined in the application; R2 is phenyl, optionally substituted D1 is a diazapolycyclic group T1 is a group selected from H, alkyl, alkenyl, alkynyl and from the following optionally substituted groups: cycloalkyl, heterocycloalkyl, aryl, heteroaryl, cycloalkylalkyl, heterocycloalkylalkyl, arylalkyl or heteroarylalkyl, and their hydrates and solvates and pharmaceutically acceptable salts.
MICROEMULSIONS
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Page/Page column 16, (2010/03/02)
Pharmaceutical compositions in the form of microemulsions comprising the following components, in amounts expressed as % by weight, the sum of the components being 100%: S) from 0.01 to 95% of one or more pharmaceutically acceptable compounds, selected fr
Diazabicyclic compounds as opioid receptor agonists
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Page/Page column 26, (2010/03/02)
Nonane and decane diazabicyclic derivatives having homopiperazine as main ring, having affinity for the opioidergic μ and/or δ and/or k receptors and/or for all their receptorial subclasses, with central and/or peripheral activity, having formula (I), the
Compounds for the Treatment of Hepatitis C
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Page/Page column 124, (2008/12/07)
The invention encompasses compounds of formula I, including pharmaceutically acceptable salts, as well as compositions and methods of using these compounds. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV.
Identification of a butyrophenone analog as a potential atypical antipsychotic agent: 4-[4-(4-Chlorophenyl)-1,4-diazepan-1-yl]-1-(4-fluorophenyl)butan-1-one
Ablordeppey, Seth Y.,Altundas, Ramazan,Bricker, Barbara,Zhu, Xue Y.,Suresh Kumar, Eyunni V.K.,Jackson, Tanise,Khan, Abdul,Roth, Bryan L.
, p. 7291 - 7301 (2008/12/23)
The synthesis and exploration of novel butyrophenones have led to the identification of a diazepane analogue of haloperidol, 4-[4-(4-chlorophenyl)-1,4-diazepan-1-yl]-1-(4-fluorophenyl)butan-1-one (compound 13) with an interesting multireceptor binding profile. Compound 13 was evaluated for its binding affinities at DA subtype receptors, 5HT subtype receptors, H-1, M-1 receptors and at NET, DAT, and SERT transporters. At each of these receptors, compound 13 was equipotent or better than several of the standards currently in use. In in vivo mouse and rat models to evaluate its efficacy and propensity to elicit catalepsy and hence EPS in humans, compound 13 showed similar efficacy as clozapine and did not produce catalepsy at five times its ED50 value.
New ligands with affinity for the α4β2 subtype of nicotinic acetylcholine receptors. Synthesis, receptor binding, and 3D-QSAR modeling
Audouze, Karine,Nielsen, Elsebet ?stergaard,Olsen, Gunnar M.,Ahring, Philip,J?rgensen, Tino Dyhring,Peters, Dan,Liljefors, Tommy,Balle, Thomas
, p. 3159 - 3171 (2007/10/03)
A new series of piperazines, diazepanes, diazocanes, diazabicyclononanes, and diazabicyclodecanes with affinity for the α4β 2 subtype of nicotinic acetylcholine receptors were synthesized on the basis of results from a previous computational study. A predictive 3D-QSAR model was developed using the GRID/GOLPE approach (R2 = 0.94, Q 2 = 0.83, SDEP = 0.34). The SAR was interpreted in terms of contour maps of the PLS coefficients and in terms of a homology model of the α4β2 subtype of the nicotinic acetylcholine receptors. The results reveal that hydrogen bonding from both hydrogens on the protonated amine and from the pyridine nitrogen to a water molecule as well as van der Waals interactions between the substituent bearing the protonated amine and the receptor is of importance for ligand affinity. The combination of 3D-QSAR and homology modeling proved successful for the interpretation of structure-affinity relationships as well as the validation of the individual modeling approaches.
Synthesis and transporter binding properties of bridged piperazine analogues of 1-{2-[bis(4-fluorophenyl)methoxy]ethyl}-4-(3-phenylpropyl)piperazine (GBR 12909)
Zhang,Rothman,Dersch,De Costa,Jacobson,Rice
, p. 4840 - 4849 (2007/10/03)
A series of analogues related to 1-[2-(diphenylmethoxy)ethyl]-4-(3-phenylpropyl)piperazine (2) and 1-{2-[bis(4-fiuorophenyl)methoxy]ethyl}-4-(3-phenylpropyl)piperazine(3) (GBR 12935 and GBR 12909, respectively), in which the piperazine moiety was replaced
Substituted bridged diazabicycloalkyl quinolone carboxylic acids
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, (2008/06/13)
Antibacterial compounds have the formula STR1 wherein R1 is hydrogen, a pharmaceutically acceptable cation, or alkyl; A is CH, CF, CCl or N; Y is alkyl, haloalkyl, cyclopropyl, vinyl, methoxy, N-methylamino, p-fluorophenyl, p-hydroxyphenyl or p
Anti-bacterial substituted bridged-diazabicycloalkyl quinolone carboxylic acids
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, (2008/06/13)
Antibacterial compounds have the formula STR1 wherein R1 is hydrogen, a pharmaceutically acceptable cation, or alkyl; A is CH, CF, CCl or N; Y is alkyl, haloalkyl, cyclopropyl, vinyl, methoxy, N-methylamino, p-fluorophenyl, p-hydroxyphenyl or p
Substituted bridged-diazabicycloalkyl quinolone carboxylic acids and anti-bacterial use thereof
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, (2008/06/13)
Antibacterial compounds have the formula STR1 wherein R1 is hydrogen, a pharmaceutically aceptable cation, or alkyl; A is CH, CF, CCl or N; Y is alkyl, haloalkyl, cyclopropyl, vinyl, methoxy, N-methylamino, p-fluorophenyl, p-hydroxyphenyl or p-
