149505-02-2Relevant academic research and scientific papers
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
, 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 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.
Heterocyclic compounds, their production and use
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, (2008/06/13)
Heterocyclic compounds represented by the general formula (I) wherein R stands for an optionally substituted aromatic heterocyclic group; X stands for oxygen atom, an optionally oxidated sulfur atom, —C(═O)— or —CH(OH)—; Y stands for CH or N; m denotes an integer of 0 to 10: n denotes an integer of 1 to 5: cyclic group ?stands for an optionally substituted aromatic azole group; and ring A is optionally further substituted, or salts thereof. The compound (I) possesses action of inhibiting tyrosine kinase and useful as antitumor agents.
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.
