103438-85-3Relevant articles and documents
Benzylideneacetone Derivatives Inhibit Osteoclastogenesis and Activate Osteoblastogenesis Independently Based on Specific Structure-Activity Relationship
Pativada, Triveni,Kim, Myung Hwan,Lee, Jung-Hun,Hong, Seong Su,Choi, Chun Whan,Choi, Yun-Hyeok,Kim, Woo Jung,Song, Da-Woon,Park, Serk In,Lee, Eun Jung,Seo, Bo-Yeon,Kim, Hankyeom,Kim, Hong Kyu,Lee, Kee Ho,Ahn, Sung K.,Ku, Jin-Mo,Park, Gil Hong
, p. 6063 - 6082 (2019)
(E)-3,4-Dihydroxybenzylideneacetone (compound 1) inhibited receptor activator of NF-κB ligand-induced osteoclastogenesis of C57BL/6 bone marrow monocyte/macrophages with IC50 of 7.8 μM (IC50 of alendronate, 3.7 μM) while stimulating the differentiation of MC3T3-E1 osteoblastic cells, accompanied by the induction of Runt-related transcription factor 2, alkaline phosphatase, and osteocalcin. (E)-4-(3-Hydroxy-4-methoxyphenyl)-3-buten-2-one (compound 2c) showed a dramatically increased osteoclast-inhibitory potency with IC50 of 0.11 μM while sustaining osteoblast-stimulatory activity. (E)-4-(4-Hydroxy-3-methoxyphenyl)-3-buten-2-one (compound 2g) stimulated alkaline phosphatase production 2-fold at 50 μM without changing osteoclast-inhibitory activity, compared with compound 1. Oral administration of compounds 1, 2c, and 2g prevented ovariectomy-induced osteoporosis in ddY mice to a degree proportional to their osteoclastogenesis-inhibitory potencies. The administration of 1 (mg/kg)/d compound 2c ameliorated histomorphometry of osteoporotic bone to a degree comparable with 10 (mg/kg)/d alendronate. Conclusively, the in vitro capacity of a few benzylideneacetone derivatives to inhibit osteoclastogenesis supported by independent osteoblastogenesis activation was convincingly reflected in in vivo management of osteoporosis, suggesting a potential novel therapeutics for osteopenic diseases.
NOVEL BENZYLIDENEACETONE DERIVATIVE AND USE THEREOF
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Paragraph 0113-0114, (2020/06/23)
The present invention relates to novel benzylideneacetone derivatives or uses thereof, more specifically, the present invention relates to a pharmaceutical composition for preventing or treating, or food composition for ameliorating a cancer or a bone disease comprising a compound defined by Formula 1 or pharmaceutically acceptable salt thereof as an active ingredient. Since compounds according to the present invention exhibit strong inhibitory activity on proliferation and differentiation of osteoclast, and activity on proliferation and differentiation of osteoblast, it can be usefully used to develop safe and effective anti-cancer agents, and therapeutic agents for preventing and treating or foods for ameliorating bone diseases including osteoporosis, and the like.
NOVEL COMPOUNDS, USES AND METHODS FOR THEIR PREPARATION
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Paragraph 00341, (2018/03/06)
The present disclosure relates to novel compounds HIF-2α inhibitors and pharmaceutical compositions thereof which may be useful in the treatment and/or prevention of various conditions. The present disclosure also provides methods of preparing such HIF-2α inhibitors and compositions, and methods of using the same.
Macrocyclic compounds and methods for their production
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Page/Page column 38, (2015/11/10)
There is provided inter alia compounds of formula (I): for use in treatment of viral infection or as an immunosuppressant.
Sanglifehrin Derivatives and Methods for Their Production
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Paragraph 0150; 0151, (2014/04/03)
There are provided inter alia compounds of formula (I) and (II) and their use in therapy, particularly for the treatment of viral infection.
Novel Dosage Form
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Paragraph 0255; 0256, (2014/09/03)
There is provided inter alia a pharmaceutical dosage form for oral administration comprising a sanglifehrin as active ingredient in which the sanglifehrin active ingredient is protected from acid degradation in the stomach environment following oral admin
TRICYCLIC BORON COMPOUNDS FOR ANTIMICROBIAL THERAPY
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Paragraph 0167, (2013/07/05)
Provided herein are antimicrobial tricyclic boron compounds of the following formula I: or pharmaceutically acceptable salts, complexes, or tautomers thereof that are antibacterial agents, pharmaceutical compositions containing them, methods for their use
NOVEL DOSAGE FORM
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Page/Page column 62, (2013/05/21)
There is provided inter alia apharmaceutical dosage form fororal administration comprising a sanglifehrin as active ingredient in which the sanglifehrin active ingredient is protected from acid degradation in the stomach environment following oral adminis
Novel Compounds
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Page/Page column 64, (2011/06/24)
The present invention provides compounds of formula (I): wherein Ra, Rb, Rc, R1, R2, R3, X1, Y1, Z1, A, n and m are as defined in the specification, and pharmaceutically acceptable salts thereof, as well as processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
NOVEL GLUCOCORTICOID RECEPTOR AGONISTS
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Page/Page column 39, (2010/12/26)
This invention relates to novel glucocorticoid receptor agonists of formula (I) and to processes and intermediates for their preparation. The present invention also relates to pharmaceutical compositions containing these compounds, to their combination with one or more other therapeutic agents, as well as to their use for the treatment of a number of inflammatory and allergic diseases, disorders and conditions.