57668-35-6Relevant academic research and scientific papers
BICYCLIC COMPOUND
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Paragraph 0965, (2017/12/28)
Provided is a bicyclic compound having an acetyl-CoA carboxylase inhibitory action. A compound represented by the formula: wherein each symbol is as described in the DESCRIPTION, or a salt thereof has an acetyl-CoA carboxylase inhibitory action, is useful for the prophylaxis or treatment of cancer, inflammatory diseases and the like, and has superior efficacy.
Discovery of novel and potent CRTH2 antagonists
Ito, Shinji,Terasaka, Tadashi,Zenkoh, Tatsuya,Matsuda, Hiroshi,Hayashida, Hisashi,Nagata, Hiroshi,Imamura, Yoshimasa,Kobayashi, Miki,Takeuchi, Makoto,Ohta, Mitsuaki
supporting information; experimental part, p. 1194 - 1197 (2012/03/11)
High throughput screening of our chemical library for CRTH2 antagonists provided a lead compound 1a. Initial optimization of the lead led to the discovery of a novel, potent and orally bioavailable CRTH2 antagonist 17.
Preventive/therapeutic method for cancer
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, (2008/06/13)
This invention provides a prophylactic or therapeutic method for cancer. A prophylactic or therapeutic method for cancer, which is characterized by selectively inhibiting ErbB-2 (HER2) to block information signals of multimers of the epithelial growth factor receptor family.
MEDICINAL COMPOSITIONS IMPROVED IN SOLUBLITY IN WATER
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Page/Page column 34, (2010/11/29)
Solid dispersions are provided comprising an HER2 inhibitor which is hardly or not soluble in water and a hydrophilic polymer. These solid dispersions have been improved in the solubility of the HER2 inhibitor, oral absorption and bioavailability in blood
MEDICINAL COMPOSITIONS HAVING IMPROVED ABSORBABILITY
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Page/Page column 38-39, (2010/11/29)
An HER2 inhibitor having an average particle size of about 3 μm or less or a composition containing the same which has improved HER2 inhibitor-absorbability.
Heterocyclic compounds their production and use
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, (2008/06/13)
A compound represented by the formula: wherein m is 1 or 2, R1 is a halogen or an optionally halogenated C1-2 alkyl; one of R2 and R3 is a hydrogen atom and the other is a group represented by the formula: wherein n is 3 or 4; R4 is a C1-4 alkyl group substituted by 1 or 2 hydroxy groups, or a salt thereof shows tyrosine kinase-inhibiting activity.
Cyclic imino derivatives and pharmaceutical compositions containing them
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, (2008/06/13)
The invention relates to cyclic imino compounds which have, inter alia, valuable pharmacological properties, especially inhibitory effects on cell aggregation, pharmaceutical compositions which contain these compounds and processes for preparing them.
Synthesis and biological activity of new 3-hydroxy-3-methylglutaryl-CoA synthase inhibitors: 2-Oxetanones with a meta-substituent on the benzene ring in the side chain
Hashizume,Ito,Kanaya,Nagashima,Usui,Oshima,Kanao,Tomoda,Sunazuka,Kumagai,Omura
, p. 1272 - 1278 (2007/10/02)
Isosteric side chain analogs of 3a were synthesized and tested for inhibitory activities towards 3-hydroxy-3-methylglutaryl coenzyme A (HMG- CoA) synthase and upon cholesterol production in Hep G2 cells and in mouse liver. It became clear that the lipophi
Synthesis and biological activity of new 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) synthase inhibitors: 2-oxetanones with a side chain mimicking the folded structure of 1233A.
Hashizume,Ito,Yamada,Nagashima,Kanao,Tomoda,Sunazuka,Kumagai,Omura
, p. 512 - 520 (2007/10/02)
To mimic the folded side chain conformation of 1233A (1), which is a 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) synthase inhibitor, 1233A analogs with aromatic rings in the side chain were synthesized. The 2-oxetanone moiety was kept intact. Among 1233A and its synthetic analogs, trans-3-hydroxymethyl-4-[2-(7-methoxycarbonyl-1-naphthyl)ethyl]-2-oxe tanone (23) showed the highest HMG-CoA synthase inhibitory activity in vitro. The structure-activity relationship at the side chain is discussed.
Intramolecular arylation of a soft carbon centre using Mn(III) acetate: Studies towards the spirostructure of fredericamycin-A
Aidhen, Indrapal Singh,Narasimhan, N. S.
, p. 222 - 228 (2007/10/02)
The potential of Mn(III) acetate has been explored for oxidative cyclisation in the indanediones 3, for the synthesis of the core subunit 2 of fredericamycin-A(1).
