摘要:
Compounds represented by the following general formula (I), pharmacologically acceptable salts thereof or hydrates of the same: (I) wherein W represents and R3, R7, R16, R17, R20, R21 and R21′ are the same or different and each represents hydrogen, etc. Because of inhibiting angiogenesis and inhibiting the production of VEGF particularly in hypoxia, the compounds (I) are useful as remedies for solid cancer.
摘要:
The present invention provides a novel carboxylic acid derivative, a salt thereof or a hydrate of them which is useful as an insulin sensitizer, and a medicament comprising the derivative as the effective ingredient. More specifically, it provides a carboxylic acid compound represented by the formula (I), a salt thereof or a hydrate of them. In the formula, Ar represents a 6- to 14-membered aromatic ring group which may have at least one substituent; R1, R2, R3, R4, R5, R6, R7 and R8 are the same as or different from each other and each represents a hydrogen atom, a halogen atom, a hydroxyl group, a C1-6 alkyl group or a C1-6 alkoxy group; X represents an oxygen atom or a methylene group; Y represents a group represented by the formula (II) or (III): (wherein Z represents a group represented by the formula (IV): (wherein R9, R10, R11 and R12 are the same as or different from each other and each represents a hydrogen atom, a halogen atom, a hydroxyl group, a C1-6 alkyl group or a C1-6 alkoxy group)); m is 0 or 1; and n is 0 or 1.
摘要:
The present invention relates to compounds and methods useful in the prevention or treatment of diseases or conditions associated with Toll-like receptor 2 activation.
摘要:
The present invention relates to calcium bis[(2S)-3-[3-[(2S)-3-(4-chloro-2-cyanophenoxy)-2-fluoropropoxy]phenyl]-2-isopropoxypropionate] represented by formula (I), a hydrate thereof, a crystal of the compound of formula (I), and a crystal of the hydrate of the compound of formula (I) which are useful as pharmaceuticals, and to processes for producing the same, and intermediates therefore, and processes for production thereof. [Problem]There is need for (2S)-3-[3-[(2S)-3-(4-chloro-2-cyanophenoxy)-2-fluoropropoxy]phenyl]-2-isopropoxypropionic acid, in the form of a drug substance, purified so as to minimize a residual solvent content and having a uniformized specification and a highly favorable workability, and a process for producing the same. [Solution]Crystalline calcium bis[(2S)-3-[3-[(2S)-3-(4-chloro-2-cyanophenoxy)-2-fluoropropoxy]phenyl]-2-isopropoxypropionate], a calcium salt of (2S)-3-[3-[(2S)-3-(4-chloro-2-cyanophenoxy)-2-fluoropropoxy]phenyl]-2-isopropoxypropionic acid, solves the above problem. [Selected Drawing] None
摘要:
The present invention provides methods for preparing TLR-4 receptor agonist E6020: and stereoisomers thereof, which compounds are useful as an immunological adjuvants when co-administered with antigens such as vaccines for bacterial and viral diseases. Also provided are synthetic intermediates.
摘要:
The present invention provides the mPrickle gene which encodes a protein present in mammalian PSD fractions. The mPrickle protein is localized in synapses, and binds to the scaffold protein PSD-95. Precipitation of endogenous mPrickle using an anti-mPrickle antibody results in the coprecipitation of NMDA receptors, and thus, mPrickle can be used in drug delivery systems that target NMDA receptors. NMDA receptors are closely related to learning and memory, and are also suggested to be involved in mental disorders. Thus, in the future, mPrickle is expected to be applicable to the diagnosis and/or treatment of neurodegenerative diseases associated with learning/memory, such as mental deterioration and dementia.
摘要:
In the present invention, because no examples are known of binding of magnetic particle to mesenchymal cell or chondrocyte which might be used in regenerative medicine, whether or not a cell having the magnetic particle bound thereto is retained in local by external magnetism after administration and whether or not the cell can exhibit intrinsic activity is studied. According to the present invention, a magnetic cell comprising mesenchymal cell or cultured chondrocyte having magnetic particle bound to the surface thereof is provided, and when the cell is administered in vivo and an external magnetic field is applied, the cell can be retained for a long time at a disease site. Moreover, a drug delivery system can be constructed by causing the magnetic cells to contain a drug.
摘要:
In neuron transplantation therapy, in terms of safety, it is preferable to use a cell population consisting only of a desired type of cells, and to use postmitotic neurons in consideration to avoid the risk of tumorigenesis. Moreover, greater therapeutic effects would be expected through the use of earlier progenitor cells in consideration of post-transplantation viability, proper network formation ability, and such. According to the present invention, Lrp4, a gene that is specifically expressed in dopaminergic neuron proliferative progenitor cells prior to cell cycle exit, was identified. The use of Lrp4 expression in cells as an index allows for the isolation. of cells suitable for transplantation therapy of neurodegenerative diseases such as Parkinson's disease in terms of safety, survival rate, and network formation ability.
摘要:
A reporter system reflecting the transport process that transports GPI-anchored proteins to the cell wall was constructed and compounds inhibiting this process were discovered. Further, genes conferring resistance to the above compounds were identified and methods of screening for compounds that inhibit the activity of the proteins encoded by these genes were developed. Therefore, through the novel compounds, the present invention showed that antifungal agents having a novel mechanism, i.e. inhibiting the process that transports GPI-anchored proteins to the cell wall, could be achieved.
摘要:
The present invention provides a system for testing the influence of a drug on integrin expression, which comprises measuring an integrin expression level in platelets of an individual to which the drug is administered and, based on the measured expression amount, determining what effect the drug has on integrin expression in cells other than platelets.