93428-56-9Relevant academic research and scientific papers
TETRAHYDROQUINAZOLINONE DERIVATIVES AS PARP INHIBITORS
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Page/Page column 70, (2014/02/15)
Disclosed are compounds of formula (I), their tautomeric forms, stereoisomers, and pharmaceutically acceptable salts thereof, wherein R1-R6, R7a-d, R8a-d, A, M, n, and p are as defined in the specification, pharmaceutical compositions including a compound, tautomer, stereoisomer, or salt thereof, and methods of treating or preventing diseases or disorders, for example, cancer, that are amenable to treatment or prevention by inhibiting the PARP enzyme of a subject.
UROTENSIN II RECEPTOR ANTAGONISTS
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Page/Page column 191, (2010/11/28)
The invention is directed to Urotensin II antagonists. More specifically, the present invention relates to certain novel compounds, methods for preparing compounds, compositions, intermediates and derivatives thereof and methods for treating Urotensin-II mediated disorders. Pharmaceutical and veterinary compositions and methods of treating cardiovascular disorders and various other disease states or conditions using compounds of the invention are also described.
Novel amides useful for treating pain
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Page/Page column 19, (2010/02/11)
The present invention relates to compounds of formula (I-VII) or a pharmaceutically acceptable salt or prodrug thereof, in which A, L, R6, R7 and R8 are defined herein. The present invention also relates to methods of trating pain using these compounds and pharmaceutical compositions including these compounds.
Novel amides useful for treating pain
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Page/Page column 14, (2010/02/10)
The present invention relates to compounds of formula (I) that useful in treating pain.
Substituted diazabicycloakane derivatives
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Page/Page column 17-18, (2010/02/11)
Compounds of formula (I) Z-Ar1—Ar2??(I) wherein Z is a diazabicyclic amine, Ar1 is a 5- or 6-membered aromatic ring, and Ar2 is selected from an unsubstituted or substituted 5-membered heteroaryl ring; an unsubstituted or substituted 6-membered heteroaryl ring; 3,4-(methylenedioxy)phenyl; and phenyl substituted with 0, 1, 2, or 3 substituents in the meta- or para-positions. The compounds are useful in treating conditions or disorders prevented by or ameliorated by α7 nAChR ligands. Also disclosed are pharmaceutical compositions comprising compounds of formula (I) and methods for using such compounds and compositions.
Substituted diazabicycloalkane derivatives
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Page/Page column 25, (2010/02/11)
Compounds of formula (I) [in-line-formulae]Z-Ar1—Ar2??(I) [/in-line-formulae] wherein Z is a diazabicyclic amine, Ar1 is a 5- or 6-membered aromatic ring, and Ar2 is selected from the group consisting of an unsubstituted or substituted 5- or 6-membered heteroaryl ring; unsubstituted or substituted bicyclic heteroaryl ring; 3,4-(methylenedioxy)phenyl; carbazolyl; tetrahydrocarbazolyl; naphthyl; and phenyl; wherein the phenyl is substituted with 0, 1, 2, or 3 substituents in the meta- or para-positions. The compounds are useful in treating conditions or disorders prevented by or ameliorated by α7 nAChR ligands. Also disclosed are pharmaceutical compositions comprising compounds of formula (I) and methods for using such compounds and compositions.
3,8-Diazabicyclo[3.2.1]octanes and their use in the treatment of cardiac arrhythmias
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, (2008/06/13)
There is provided compounds of formula (I), wherein R1, R2 and Ra to Rb have meanings given in the description, which are useful in the prophylaxis and in the treatment of arrhythmias, in particular atrial and v
Synthesis and Structure-Activity Relationship of Di-(3,8-diazabicyclo[3.2.1]octane) Diquaternary Ammonium Salts as Unique Analgesics
Liu, Hong,Cheng, Tie-Ming,Zhang, Hong-Mei,Li, Run-Tao
, p. 510 - 513 (2007/10/03)
Based on the structure characteristics of the lead compounds, 1,1′2-octanedioyl-4,4′-dimethyl-4,4′-dibenzyl dipiperazinium dibromide (2) and 3,8-disubstituted-3,8-diazabicyclo[3.2.1]octanes (DBO), di-(3,8-diazabicyclo[3.2.1]octane) diquaternary ammonium salts 3 a-c were designed and synthesized through a highly practical procedure. Target compounds 3 a-c and the hydrochloride salts of their precursors 10 a-c were evaluated for their in vivo analgesic and sedative activities. Interestingly, the introduction of an endoethylenic bridge in the piperazine of lead compound 2 causes loss of the analgesic activity and increases the toxicity dramatically. This result shows that the flexible conformation of piperazine in compound 2 is favorable for interaction with the receptor, and the quaternization of compounds 10 a-c is the main reason for the toxicity increase.
Mono- and disubstituted-3,8-diazabicyclo[3.2.1]octane derivatives as analgesics structurally related to epibatidine: Synthesis, activity, and modeling
Barlocco, Daniela,Cignarella, Giorgio,Tondi, Donatella,Vianello, Paola,Villa, Stefania,Bartolini, Alessandro,Ghelardini, Carla,Galeotti, Nicoletta,Anderson, David J.,Kuntzweiler, Theresa A.,Colombo, Diego,Toma, Lucio
, p. 674 - 681 (2007/10/03)
A series of 3,8-diazabicyclo[3.2.1]octanes substituted either at the 3 position compounds 1) or at the 8 position (compounds 2) by a chlorinated heteroaryl ring were synthesized, as potential analogues of the potent natural analgesic epibatidine. When tested in the hot plate assay, the majority of the compounds showed significant effects, the most interesting being the 3-(6-chloro-3-pyridazinyl)-3,8-diazabicyclo[3.2.1]octane (la). At a subcutaneous dose of 1 mg/kg, 1a induced a significant increase in the pain threshold, its action lasting for about 45 min. 1a also demonstrated good protection at a dose of 5 mg/kg in the mouse abdominal constriction test, while at 20 mg/kg it completely prevented the constrictions in the animals. Administration of naloxone (1 mg/kg ip) did not antagonize its antinociception while mecamylamine (2 mg/kg ip) did, thus suggesting the involvement of the nicotinic system in its action. Binding studies confirmed high affinity for the αβ2 nAChR subtype (K(i) = 4.1±0.21 nM). nAChR functional activity studies on three different cell lines showed that 1a was devoid of any activity at the neuromuscular junction. Finally, due to the analogy in their pharmacological profile with that of epibatidine, compounds were compared from a structural and conformational point of view through theoretical calculations and high-field 1H NMR spectroscopy. Results indicate that all of them present one conformation similar to that of epibatidine.
