917396-39-5Relevant academic research and scientific papers
Discovery of novel chiral diazepines as bombesin receptor subtype-3 (BRS-3) agonists with low brain penetration
Matsufuji, Tetsuyoshi,Shimada, Kousei,Kobayashi, Shozo,Kawamura, Asuka,Fujimoto, Teppei,Arita, Tsuyoshi,Hara, Takashi,Konishi, Masahiro,Abe-Ohya, Rie,Izumi, Masanori,Sogawa, Yoshitaka,Nagai, Youko,Yoshida, Kazuhiro,Takahashi, Hisashi
, p. 750 - 755 (2014)
The discovery and optimization of a novel series of BRS-3 agonists are described. We explored a potent BRS-3 agonist with low brain penetration to avoid an adverse effect derived from central nervous system exposure. Through the derivatization process, chiral diazepines 9f and 9g were identified as possessing low brain penetration as well as potent in vitro activity against human and mouse BRS-3s.
Synthesis and biological evaluation of novel chiral diazepine derivatives as bombesin receptor subtype-3 (BRS-3) agonists incorporating an antedrug approach
Matsufuji, Tetsuyoshi,Shimada, Kousei,Kobayashi, Shozo,Ichikawa, Masanori,Kawamura, Asuka,Fujimoto, Teppei,Arita, Tsuyoshi,Hara, Takashi,Konishi, Masahiro,Abe-Ohya, Rie,Izumi, Masanori,Sogawa, Yoshitaka,Nagai, Yoko,Yoshida, Kazuhiro,Abe, Yasuyuki,Kimura, Takako,Takahashi, Hisashi
, p. 89 - 104 (2015)
Novel compounds based on the lead BRS-3 agonists from our HTS compounds 2a and 2b have been synthesized with the focus on obtaining peripheral BRS-3 agonists. To identify potent anti-obesity compounds without adverse effects on the central nerve system, a
HETEROARYL COMPOUNDS FOR TREATMENT OF COMPLEMENT FACTOR D MEDIATED DISORDERS
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Paragraph 112; 177-178, (2021/08/27)
Compounds, methods of use, and processes for making inhibitors of complement factor D or a pharmaceutically acceptable salt or composition thereof are provided. The inhibitors described herein target factor D and inhibit or regulate the complement cascade. The inhibitors of factor D described herein reduce the excessive activation of complement.
COMPOUNDS THAT MODULATES AMPA RECEPTOR FUNCTION
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Page/Page column 74; 75, (2019/09/18)
The invention provides compounds of the formula (I): (I) wherein A1, A2, R2, R4, B1, B2, X, X1, n, a and b are as defined are defined in the specification, to pharmaceutical comp
COMPOUNDS WITH NEMATICIDAL ACTIVITY
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, (2013/05/22)
The present invention relates to the use of known pyridyl carboxamide derivatives and novel pyridyl carboxamide derivatives as nematicides, compositions containing such compounds and methods for the control of nematodes.
CYCLOBUTYL SUBSTITUTED PYRROLOPYRIDINE AND PYRROLOPYRIMIDINE DERIVATIVES AS JAK INHIBITORS
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Page/Page column 204-205, (2012/06/01)
The present invention provides cyclobutyl substituted pyrrolopyrimidines and pyrrolopyridines of Formula I: wherein X, Y, Z, L, A, R5, n and m are defined above, as well as their compositions and methods of use, that modulate the activity of Janus kinases (JAKs) and are useful in the treatment of diseases related to the activity of JAKs including, for example, inflammatory disorders, autoimmune disorders, cancer, and other diseases.
Characterization of a novel and selective CB1 antagonist as a radioligand for receptor occupancy studies
Yang, Yifan,Miller, Keith J.,Zhu, Yeheng,Hong, Yang,Tian, Yuan,Murugesan, Natesan,Gu, Zhengxiang,O'Tanyi, Eva,Keim, William J.,Rohrbach, Kenneth W.,Johnghar, Susan,Behnia, Kamelia,Pelleymounter, Mary Ann,Carlson, Kenneth E.,Ewing, William R.
scheme or table, p. 6856 - 6860 (2012/01/03)
Obesity remains a significant public health issue leading to Type II diabetes and cardiovascular disease. CB1 antagonists have been shown to suppress appetite and reduce body weight in animal models as well as in humans. Evaluation of pre-clinical CB1 antagonists to establish relationships between in vitro affinity and in vivo efficacy parameters are enhanced by ex vivo receptor occupancy data. Synthesis and biological evaluation of a novel and highly selective radiolabeled CB1 antagonist is described. The radioligand was used to conduct ex vivo receptor occupancy studies.
FLUOROISOQUINOLINE SUBSTITUTED THIAZOLE COMPOUNDS AND METHODS OF USE
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Page/Page column 105, (2010/08/08)
The invention relates to thiazole compounds of Formula (I) and compositions thereof useful for treating diseases mediated by protein kinase B (PKB) where the variables have the definitions provided herein. The invention also relates to the therapeutic use of such thiazole compounds and compositions thereof in treating disease states associated with abnormal cell growth, cancer, inflammation, and metabolic disorders.
Triazolopyridine cannabinoid receptor 1 antagonists
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Page/Page column 81, (2008/06/13)
The present application describes compounds according to Formula I, pharmaceutical compositions comprising at least one compound according to Formula I and optionally one or more additional therapeutic agents, and methods of treatment using the compounds according to Formula I both alone and in combination with one or more additional therapeutic agents. The compounds have the following general formula: including all prodrugs, solvates, pharmaceutically acceptable salts and stereoisomers, wherein R1, R2, R3, R4 and R5 are described herein.
Triazolopyrimidine cannabinoid receptor 1 antagonists
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Page/Page column 45, (2010/11/25)
The present application describes compounds according to both Formulas I and II, pharmaceutical compositions comprising at least one compound according to either Formula I or II and optionally one or more additional therapeutic agents, and methods of treatment using the compounds according to Formulas I and II both alone and in combination with one or more additional therapeutic agents. The compounds have the following general formulas: including all prodrugs, solvates, pharmaceutically acceptable salts and stereoisomers, wherein R1, R2, R3, R4 and R5 are described herein.
