25074-25-3Relevant articles and documents
Synthesis and pharmacological evaluation of thienocinnolin-3-(2H)-ones, bioisosters of antihypertensive and antithrombotic benzo(h)cinnolinones
Pinna, G.A.,Curzu, M.M.,Cignarella, G.,Barlocco, D.,D'Amico, M.,et al.
, p. 447 - 454 (1994)
A number of thienocinnolin-3(2H)-ones (2b, c; 3a, b) have been synthesized and tested for their pharmacological profile.These were compared with the bioisoster 8-acetylamino-4,4a,5,6-tetrahydrobenzo(h)cinnolin-3-(2H)-one 1, which we reported to be a potent antihypertensive and antithrombotic agent.Binding studies on phosphodiesterase (PDE) isoenzymes indicate that the test compounds exhibited a modest affinity towards PDE III (2c, 3a, b) and PDE V (2b, c).In vivo tests indicated that only 3b displayed antihypertensive properties comparable to the model while all the new derivatives exhibited lower hypotensive activity.All compounds, with the exception of 2b, were more potent than 1 in inhibiting collagen-induced platelet aggregation.Molecular mechanics calculations were performed on compounds 2 and 3 which were compared with the model 1. tetrahydrobenzo(h)cinnolin-3-(2H)-ones / tetrahydrothienocinnolin-3-(2H)-ones / PDE isoenzymes / antihypertensive activity / hypotensive activity / antiplatelet aggregation activity
FUSED DIHYDROINDAZOLE DERIVATIVES HAVING MULTIMODAL ACTIVITY AGAINST PAIN
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Page/Page column 119, (2020/02/14)
The present invention relates to fused dihydroindazole derivatives having pharmacological activity towards the α2δ subunit, in particular the α2δ subunit, of the voltage-gated calcium channel. It also relates to compounds having dual pharmacological activ
4,5-DIHYDRO-1H-THIENO[2,3-G]INDAZOLYL DERIVATIVES HAVING MULTIMODAL ACTIVITY AGAINST PAIN
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Page/Page column 103, (2019/07/13)
wherein the meanings for the various substituents are as disclosed in the description, having dual pharmacological activity towards both the α2δ subunit, in particular the α2δ-1 subunit, of the voltage-gated calcium channel and the μ-opioid receptor, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use in therapy, in particular for the treatment of pain.
p-diaminobenzene derivative as potassium channel regulator, preparation method and medical applications thereof
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Paragraph 0284-0288, (2019/12/09)
The invention relates to a p-diaminobenzene derivative as a potassium channel regulator, a preparation method and medical applications thereof, and specifically discloses a compound represented by a general formula A or a pharmaceutically acceptable salt
Tricycloisoxazole compound and preparation and application methods thereof
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Paragraph 0177; 0178, (2019/03/31)
The invention discloses a tricycloisoxazole compound and a medically acceptable salt thereof. The structure of the tricycloisoxazole compound is shown as the formula I, wherein A is thienyl, furyl, phenyl and pyridyl; R1 is hydrogen, halogen, amido, substituted amido, nitro, acylamino, substituted acylamino, cyan, low alkyl and alkoxy; R2 is alkyl, alkoxy, alkoxy alkyl, substituted or unsubstituted aryl, and substituted or unsubstituted heterocyclyl; R3 is carbon or hydroxyl; X is carbon atom or oxygen atom, and when being carbon atom, is connected with the substituted group R3, which is carbonyl or carboxyl. The invention also provides preparation and application methods of the tricycloisoxazole compound, namely, the tricycloisoxazole compound can serve as an antifungal small-molecule inhibitor. In vitro antifungal activity experiment results show that most of the tricycloisoxazole compound shown as the formula I achieves good antifungal activity, especially significantly higher antifungal activity on Cryptococcus neoformans compared with a positive fungicide of fluconazole, thereby being applicable to preparing antifungal drugs.
BENZOXAZINONE DERIVATIVES AND ANALOGUES THEREOF AS MODULATORS OF TNF ACTIVITY
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Page/Page column 102, (2016/12/26)
A series of substituted 3,4-dihydro-2H-.1,4-benzoxazin-3-one derivatives, and analogues thereof, being potent modulators of human TNFa activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune
Spiro tetrahydro-benzothiophen derivatives useful for the treatment of neurodegenerative diseases
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Paragraph 0149-0151, (2014/01/07)
The present invention provide compounds of Formula (I) used as BACE inhibitors for the treatment of neurodegenerative diseases.
SPIRO TETRAHYDRO - BENZOTHIOPHEN DERIVATIVES USEFUL FOR THE TREATMENT NEURODEGENERATIVE DISEASES
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Page/Page column 64; 65, (2014/01/07)
The present invention provide compounds of Formula (I) used as BACE inhibitors for the treatment of neurodegenerative diseases
PHARMACEUTICAL COMPOUNDS
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Page/Page column 23, (2010/09/05)
Condensed tricyclic pyrazole compounds having affinity for the CB1 and/or CB2 cannabinoidergic receptors, with activity both on the peripheral and central nervous system, of formula (I): wherein: A represents a group selected from —(CH2)t
Pharmaceutical compounds
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Page/Page column 28, (2010/10/03)
Condensed tricyclic pyrazole compounds having affinity for the CB1 and/or CB2 cannabinoidergic receptors, with activity both on the peripheral and central nervous system, of formula (I) : wherein: A represents a group selected from -(CH2)t