56813-54-8Relevant academic research and scientific papers
TRIAZOLOPHTHALAZINE COMPOUNDS, USE AS ANTI-HUMAN IMMUNODEFICIENCY VIRUS INHIBITORS OF HIV VIF-DEPENDENT DEGRADATION OF APOBEC3
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Paragraph 00330; 00342, (2019/07/17)
The present disclosure is concerned with triazolophthalazine compounds that are capable of inhibiting infection by the Human Immunodeficiency Virus (HIV) by inhibiting HIV Vif-dependent degradation of the APOBEC3 innate immune system. The present disclosu
Synthesis and antimicrobial activities of novel 1,2,4-triazolo [3,4-a] phthalazine derivatives
Zhang, Qiu-Rong,Xue, Deng-Qi,He, Peng,Shao, Kun-Peng,Chen, Peng-Ju,Gu, Yi-Fei,Ren, Jing-Li,Shan, Li-Hong,Liu, Hong-Min
, p. 1236 - 1238 (2014/03/21)
A series of novel 1,2,4-triazolo [3,4-a] phthalazine derivatives were synthesized in five steps from a common precursor, phthalic anhydride. Most of synthesized phthalazine derivatives showed inhibitory activity against Staphylococcus aureus. One of phthalazine derivatives 5l showed inhibitory activity against all tested bacterial and fungal strains.
Synthesis and anticancer activities of novel 1,2,4-triazolo[3,4-a] phthalazine derivatives
Xue, Deng-Qi,Zhang, Xu-Yao,Wang, Chao-Jie,Ma, Li-Ying,Zhu, Nan,He, Peng,Shao, Kun-Peng,Chen, Peng-Ju,Gu, Yi-Fei,Zhang, Xiao-Song,Wang, Cai-Feng,Ji, Cong-Hui,Zhang, Qiu-Rong,Liu, Hong-Min
, p. 235 - 244 (2014/08/18)
Trying to develop potent and selective anticancer agents, two series of novel 1,2,4-triazolo[3,4-a]phthalazine derivatives were designed and synthesized. Their antitumor activities were evaluated by MTT method against four selected human cancer cell lines (MGC-803, EC-9706, HeLa and MCF-7). Our results showed that compound 11h exhibited good anticancer activities compared to 5-fluorouracil against the four tested cell lines, with IC50 values ranging from 2.0 to 4.5 μM. Flow cytometry analysis indicated that compound 11h induced the cellular early apoptosis and cell cycle arrest at G2/M phase in EC-9706.
NITROGENOUS FUSED HETEROAROMATIC RING DERIVATIVE
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Page/Page column 48, (2010/11/24)
The invention provides a compound or its pharmaceutically-acceptable salt of formula (I): wherein A1 is a hydrogen, etc.; j and k are 0 or 1; is a double bond, etc.; is a double bond, etc.; one of W1 and W2 is E-O-W, etc., and the other is a hydrogen atom, etc.; E is a divalent group derived from a benzene ring, etc., by removing two hydrogen atoms therefrom; W is a group of formula (II-1): which has a histamine-H3 receptor antagonistic effect or a histamine-H3 receptor inverse-agonistic effect and is useful for prevention or remedy of metabolic system diseases, circulatory system diseases or nervous system diseases.
TRIAZOLO-PYRIDAZINE COMPOUNDS AND DERIVATIVES THEREOF USEFUL IN THE TREATMENT OF NEUROPATHIC PAIN
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Page/Page column 64-65, (2010/02/11)
The present invention is directed to a method of use of triazolo-pyridazine compounds in the treatment of neuropathic pain. The present invention is also directed to the use of triazolo-pyridazine compounds in the treatment of psychiatric and mood disorders such as, for example, schizophrenia, anxiety, depression, bipolar disorders, and panic, as well as in the treatment of pain, Parkinson’s disease, cognitive dysfunction, epilepsy, circadian rhythm and sleep disorders - such as shift-work induced sleep disorder and jet-lag, drug addiction, drug abuse, drug withdrawal and other diseases. The present invention is also directed to novel triazolo-pyridazine compounds that selectively bind to α2δ-1 subunit of Ca channels.
Identification and synthesis of [1,2,4]triazolo[3,4-a]phthalazine derivatives as high-affinity ligands to the α2δ -1 subunit of voltage gated calcium channel
Lebsack, Alec D.,Gunzner, Janet,Wang, Bowei,Pracitto, Richard,Schaffhauser, Herve,Santini, Angelina,Aiyar, Jayashree,Bezverkov, Robert,Munoz, Benito,Liu, Wensheng,Venkatraman, Shankar
, p. 2463 - 2467 (2007/10/03)
We have identified and synthesized a series of [1,2,4]triazolo[3,4-a] phthalazine derivatives as high-affinity ligands to α2δ-1 subunit of voltage gated calcium channels. Structure-activity relationship studies directed toward improving the potency and physical properties of 2 lead to the discovery of 20 (IC50=15nM) and (S)-22 (IC50=30nM). A potent and selective radioligand, [3H]-(S)-22 was also synthesized to demonstrate that this ligand binds to the same site as gabapentin.
Combination therapy
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, (2008/06/13)
The present invention relates to methods of treating cancer using a combination of at least two Akt inhibitors or a compound which is an inhibitor of Akt and an inhibitor of a protein kinase, which methods comprise administering to a mammal, either sequentially in any order or simultaneously, amounts of at least two therapeutic agents selected from a group consisting of a compound(s) which are inhibitors of Akt and compound(s) which are inhibitors of protein kinases. The invention also relates to methods of preparing such compositions.
Substituted triazolo-pyridazine derivatives as ligands for GABA receptors
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, (2008/06/13)
Substituted triazolo-pyridazine derivative compounds represented by wherein the variables are disclosed herein are selective ligands for GABA-A receptors, particularly for the α2 and/or α3 subunits.
6-substituted-s-triazolo[3,4-a]phthalazine derivatives
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, (2008/06/13)
The present invention refers to new s-triazolo[3,4-a]phthalazine derivatives, to the process for their preparation and to the pharmaceutical compositions containing them.
6-(Alkylamino)-3-aryl-1,2,4-triazolophthalazines. A New Class of Benzodiazepine Receptor Ligands
Tarzia, Giorgio,Occelli, Emilio,Toja, Emilio,Barone, Domenico,Corsico, Nerina,et al.
, p. 1115 - 1123 (2007/10/02)
Some 6-(alkylamino)-3-aryl-1,2,4-triazolophthalazines have been shown to displace diazepam from rat brain specific binding sites, in vitro, with Ki (nM) values comparable to those of reference benzodiazepines and to have anticonvulsant (
