ChemGenesis Incorporated

Chūō-ku, Japan

ChemGenesis Incorporated

Chūō-ku, Japan
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Fuse S.,Tokyo Institute of Technology | Okada K.,Tokyo Institute of Technology | Iijima Y.,Tokyo Institute of Technology | Munakata A.,Japan Biological Informatics Consortium JBIC | And 5 more authors.
Organic and Biomolecular Chemistry | Year: 2011

The total synthesis of a natural product HDAC inhibitor, spiruchostatin B, was successfully achieved. A 5-step synthesis that included an asymmetric aldol reaction was carried out in an automated synthesizer to provide an (E)-(S)-3-hydroxy-7-thio-4-heptenoic acid segment that is the crucial structure of cysteine-containing, depsipeptidic natural products such as spiruchostatins, FK228, FR901375, and largazole for their inhibitory activity against HDACs. © 2011 The Royal Society of Chemistry.


Fuse S.,Tokyo Institute of Technology | Nakamura K.,Tokyo Institute of Technology | Mifune Y.,Tokyo Institute of Technology | Marubayashi H.,Tokyo Institute of Technology | And 4 more authors.
Synlett | Year: 2014

Linear and branched amphiphiles with different lengths of lipids and different numbers of hydroxyl groups were rapidly synthesized based on a dioxinone scaffold. The liquid crystalline (LC) properties of the synthesized amphiphiles in excess water were investigated by polarizing optical microscopy and small-angle X-ray scattering (SAXS) analysis. Novel β-keto ester based amphiphiles that formed non-lamellar, inverted LC phases were identified. © Georg Thieme Verlag Stuttgart · New York.


PubMed | Yokohama College of Pharmacy, Pharma Eight Co., Doshisha University and ChemGenesis Inc.
Type: Journal Article | Journal: Bioorganic & medicinal chemistry letters | Year: 2016

Alzheimers disease (AD) is the most common form of dementia. In an AD patients brain, senile plaques and neurofibrillary tangles, the abnormal aggregates of amyloid (A) peptide and tau protein, are observed as the two major hallmarks of this disease. To develop a new drug for treatment of AD, we have designed and synthesized a series of curcumin derivatives and evaluated their inhibitory activities against both tau and A aggregation. In this study, we describe the development of the more potent aggregation inhibitor 3-[(1E)-2-(1H-indol-6-yl)ethenyl]-5-[(1E)-2-[2-methoxy-4-(2-pyridylmethoxy) phenyl] ethenyl]-1H-pyrazole (compound 4, PE859). This compound has a better pharmacokinetic profile and pharmacological efficacy in vivo than curcumin, making it suitable as a drug for AD.


PubMed | ChemGenesis Inc., Yokohama College of Pharmacy, Pharma Eight Co., Eisai Co. and 4 more.
Type: Journal Article | Journal: PloS one | Year: 2015

In tauopathies, a neural microtubule-associated protein tau (MAPT) is abnormally aggregated and forms neurofibrillary tangle. Therefore, inhibition of the tau aggregation is one of the key approaches for the treatment of these diseases. Here, we have identified a novel tau aggregation inhibitor, PE859. An oral administration of PE859 resulted in the significant reduction of sarkosyl-insoluble aggregated tau along with the prevention of onset and progression of the motor dysfunction in JNPL3 P301L-mutated human tau transgenic mice. These results suggest that PE859 is useful for the treatment of tauopathies.


Takahashi J.,Kyoto University | Hijikuro I.,ChemGenesis Incorporated | Kihara T.,Kyoto University | Murugesh M.G.,ChemGenesis Incorporated | And 8 more authors.
Bioorganic and Medicinal Chemistry Letters | Year: 2010

We synthesized a series of N1-substituted norcymserine derivatives 7a-p and evaluated their anti-cholinesterase activities. In vitro evaluation showed that the pyridinylethyl derivatives 7m-o and the piperidinylethyl derivative 7p improved the anti-butyrylcholinesterase activity by approximately threefold compared to N1-phenethylnorcymserine (PEC, 2). A quantitative structure-activity relationship (QSAR) study indicated that logS might be a key feature of the improved compounds. © 2010 Elsevier Ltd. All rights reserved.


Takahashi J.,Kyoto University | Hijikuro I.,ChemGenesis Incorporated | Kihara T.,Kyoto University | Murugesh M.G.,ChemGenesis Incorporated | And 6 more authors.
Bioorganic and Medicinal Chemistry Letters | Year: 2010

We synthesized carbamate-modified (-)-N1-phenethylnorphysostigmine derivatives 3a-u and evaluated their anti-cholinesterase activities. In vitro evaluation showed that cyclohexylmethylcarbamate derivative 3u potently and selectively inhibits butyrylcholinesterase. © 2010 Elsevier Ltd. All rights reserved.


Machida K.,ChemGenesis Incorporated | Hirose Y.,ChemGenesis Incorporated | Fuse S.,Tokyo Institute of Technology | Sugawara T.,ChemGenesis Incorporated | Takahashi T.,Tokyo Institute of Technology
Chemical and Pharmaceutical Bulletin | Year: 2010

In this paper we describe the development of a fully-automated solution-phase synthesizer, 'ChemKonzert' that can be used to prepare a wide variety of organic compounds. The automated synthesizer is ingeniously designed to perform most of the chemical reactions currently used by synthetic organic chemists and utilizes a centrifugal separator to efficiently achieve liquid-liquid extraction. The design of the hardware and software will be described in this paper, and several examples of organic reactions will also be presented as applications of the apparatus. © 2010 Pharmaceutical Society of Japan.


Patent
ChemGenesis Incorporated | Date: 2012-10-31

The present invention relates to a liquid crystal compound that can be used as a base for injection formulations. The present invention provides an amphipathic compound having the following general formula (I):


Patent
Chemgenesis Incorporated | Date: 2014-02-28

The present invention relates to a liquid crystal compound that can be used as a base for injection formulations. The present invention provides an amphipathic compound having the following general formula (I): wherein X and Y each denotes a hydrogen atom or together denote an oxygen atom, n denotes an integer from 0 to 2, m denotes the integer 1 or 2, and R denotes a hydrophilic group generated by removal of one hydroxyl group from any one selected from the group consisting of glycerol, erythritol, pentaerythritol, diglycerol, triglycerol, xylose, sorbitol, ascorbic acid, glucose, galactose, mannose, dipentaerythritol, maltose, mannitol, and xylitol; as well as a base for injection formulations and depot formulation comprising the same.


Patent
Chemgenesis Incorporated | Date: 2010-12-27

The present invention relates to a liquid crystal compound that can be used as a base for injection formulations. The present invention provides an amphipathic compound having the following general formula (I): wherein X and Y each denotes a hydrogen atom or together denote an oxygen atom, n denotes an integer from 0 to 2, m denotes the integer 1 or 2, and R denotes a hydrophilic group generated by removal of one hydroxyl group from any one selected from the group consisting of glycerol, erythritol, pentaerythritol, diglycerol, triglycerol, xylose, sorbitol, ascorbic acid, glucose, galactose, mannose, dipentaerythritol, maltose, mannitol, and xylitol; as well as a base for injection formulations and depot formulation comprising the same.

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