887587-20-4Relevant academic research and scientific papers
Discovery of a novel bicyclic compound, DS54360155, as an orally potent analgesic without mu-opioid receptor agonist activity
Arita, Tsuyoshi,Asano, Masayoshi,Kubota, Kazufumi,Domon, Yuki,Machinaga, Nobuo,Shimada, Kousei
supporting information, (2019/11/11)
We synthesized derivatives of a natural alkaloid, conolidine, and evaluated these derivatives in the acetic acid-induced writhing test and formalin test in ddY mice after oral administration. As a result, we identified (5S)-6-methyl-1,3,4,5,6,8-hexahydro-7H-2,5-methano[1,5]diazonino[7,8-b]indol-7-one sulfate salt, 15a (DS54360155), with a unique and original bicyclic skeleton, as an analgesic more potent than conolidine. Moreover, 15a did not exhibit mu-opioid receptor agonist activity.
Discovery of quinazoline-2,4(1: H,3 H)-dione derivatives as novel PARP-1/2 inhibitors: Design, synthesis and their antitumor activity
Zhou, Jie,Ji, Ming,Yao, Haiping,Cao, Ran,Zhao, Hailong,Wang, Xiaoyu,Chen, Xiaoguang,Xu, Bailing
, p. 3189 - 3202 (2018/05/15)
Novel quinazoline-2,4(1H,3H)-dione derivatives bearing a 3-amino pyrrolidine moiety were designed and synthesized as PARP-1/2 inhibitors. Structure-activity relationships were examined which revealed a number of potent PARP-1/2 inhibitors with moderate se
3-amino nafoxidine-containing quinazoline ketone PARP (Poly Adenosine Diphosphate Ribose Polymerase)-1/2 inhibitor as well as preparation method, medicinal composition and application thereof
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, (2018/11/22)
The invention discloses a novel 3-amino nafoxidine-containing quinazoline-2,4(1H, 3H)-diketone PARP-1/2 (Poly Adenosine Diphosphate Ribose Polymerase) inhibitor as well as a preparation method, a medicinal composition and application thereof. Specifically, the invention relates to a 3-amino nafoxidine-containing quinazoline-2,4(1H, 3H)-diketone derivative and a medicinal salt thereof of formula (I) as shown in the specification, a preparation method thereof, a composition with one or more such compounds, preparation of the compounds, and application thereof in preparing medicines for preventing and/or treating PARP-1/2 related diseases.
NOVEL COMPOUNDS
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Page/Page column 35, (2008/06/13)
A compound of Formula (I) and pharmaceutically and/or veterinarily acceptable derivatives thereof, wherein: R1 is H, C1-6alkyl, - C(A)D, C3-8cycloalkyl, aryl, het, aryl-C1-4alkyl or het-C1-4/sub
